Pharmaceutics Basic Principles and Application to Pharmacy Practice 1 st edition Alekha Dash, Somnat

TEST BANK

Practice Questions Part 1 Chapter 1 Numerical Questions: 1. How many micrograms (µg) are equivalent to 2.5 milligrams (mg)? a. b. c. d.

2.

25000 2.5 x 106 2.5 x 10-6 2.5 x 103

Calculate the density of a substance which has a mass and volume of 25 g and 20 mL, respectively. a. b. c. d.

3.

Convert 298.16 degrees Kelvin (K) to degree Celsius (oC): a. b. c. d.

4.

35oC 25oC 30oC 15oC

Convert 104o Fahrenheit to degree Celsius (oC): a. b. c. d.

5.

0.8 g/mL 1.25 g/mL 3.2 kg/m3 320 g/mL

40o Centigrade 50o Centigrade 10o Centigrade 20o Centigrade

Solve and identify the correct answer for the numerical example below 77 x 75 x 72 a. b. c. d.

Undefined 714 770 74

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

6.

Solve and identify the correct answer for the numerical example below (94)2 a. b. c. d.

7.

98 98 96 92

Solve and identify the correct answer for the numerical example below 1000 x 0 a. b. c. d.

8.

1000 0 ∞ undefined

Solve and identify the correct answer for the numerical example below 1000 x ∞ a. b. c. d.

9.

undefined 0 ∞ 1,000

Solve and identify the correct answer for the numerical example below 1000 /∞ a. b. c. d.

∞ 0 1,000 undefined

10. Determine the slope of the line represented by the equation y = 3x + 6 a.

3

b. c. d.

Either 3 or 6 6 Neither 3 nor 6

11. What is the specific gravity of a substance with a density of 10 Kg/m3 at room temperature?

Given that the density of water at room temperature is 1 g/cc (cc = cubic centimeter). (a) 1000 Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

(b) 0.01 (c) 0.001 g/cc (d) 0.001 12. What is the mass of a material having a density 1.25 g/cc and a volume of 16 cc? (a) 0.2 g (b) 20 g (c) 320 g/cc (d) 20 g/cc 13. What would be the weight and mass of a 70 Kg person in an elevator going down vertically at the acceleration of 9.81 m/s2? (a) Weight = 686.7 kg x m/s2; mass = 70 kg (b) Weight = 70 kg x m/s2; mass = 0 kg (c) Weight = 686.7 kg x m/s2; mass = 0 kg (d) Weight = 0 kg x m/s2; mass = 70 kg 14. Express 5 joules in terms of ergs. a. b. c. d.

5000 ergs 5 x 106 ergs 0.5 x 107ergs 5 x 107ergs

15. Express 5 joules in terms of calories. a. b. c. d.

1.5 calories 2.0 calories 1.2 calories 1.2 calories

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

16. Solving 567 i.

1

ii.

1 a. b. c. d.

x 14 is best stated as which of the following:

7

14 log 567

14

7 log 567

Neither i nor ii is correct Both i and ii are correct Only i is correct Only ii is correct

17. The correct answer of this numerical example a. b. c. d. e.

is

317 3 1 35 31.12

18. log xy = a. b. c. d. e.

log (x+y) log x log y log x + log y ( log x )y log y/log x

19. One millimeter is equal to a. b. c. d. e.

10-6 meter 1000 meters 10 centimeters 10-3 meter 10 cm

20. Determine the volume of a substance having a density 1.5 gm/cc and mass of 0.03 kg. a. b. c. d. e.

600 mL 20 Kg 20 cm3 0.6 mL 50 mL

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

21. Ten calories are equivalent to a. b. c. d.

4.2 x 107 ergs 4.2 joules 42 x 107 ergs 420 joules

22. One Angstrom is equal to a. b. c. d. e.

10-8 m 10-5 cm 10-10 m 10-1 cm 10-1 mm

23. The values of abscissa are positive in a. b. c. d. e.

II and III quadrant Only in I quadrant Only in IV quadrant I and IV quadrant None of the above

24. Five individual weights of compounded amoxicillin capsules are 250 mg, 260 mg, 254 mg, 248 mg, and 264 mg. The average weight of capsules is: a. b. c. d. e.

265.2 mg 255.2 mg 275.4 mg 245.2 mg 250mg

25. Find the values of x in 53 x 52 = 5x a. b. c. d. e.

5 6 1 -1 25

26. Find the values of x in 25 x 2-3 = 2x a. -2 b. 8 Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

c. 2 d. -15 e. 15 27. Find the values of x in 2-5 x 22 = 2x a. b. c. d. e.

3 -10 7 -3 -5

28. Find the values of x in 3-5 ÷ 33 =3x a. b. c. d. e.

8 -8 2 -2 15

29. Find the values of x in (2-4)2 = 2x a. b. c. d. e.

6 8 -2 -8 2

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

30. Find the correct value for

2500:

a.

50 = 2 50 b.

250 10 c. 3.398 d.

25 100 e.

.

f. All of the above 31. Find the correct value for

:

a. 2 b. log 4 + log 25 c. log 4 – log 25 d. e. 2

Theoretical questions: 1.

A statement such as “not more than 110.0 percent” in the official compendia of the U.S. Pharmacopeia and National Formulary may mean 110.1 or 110.2 percent. a. True b. False

2. The closeness of a measured value to the correct value is called: a. b. c. d. e.

Sensitivity Precision Accuracy Selectivity Specificity

3. In a set of data samples, the data that occurs the most is called: a. Average b. Mode c. Median Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

d. Mean e. Standard deviation 4. Force per unit area is called: a. b. c. d. e.

Work Energy Displacement Pressure Power

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 2 - Questions Numerical Questions: 1. The total pressure of an aerosol container at 25oC is 2 atm. What will be the pressure of this container at a temperature of 200°C? a. b. c. d.

16 atm 2 atm 3.2 atm 32 atm

2. A gas expands by 0.25 liter against a constant pressure of 1.5 atm at 25oC. What is the work in joules done by the system? a. b. c. d.

6.80 joules 0.38 x 108 joules 3.80 joules 38.0 joules

3. What is the entropy change accompanying the vaporization of 2 moles of water in equilibrium with its vapor at 25oC? (Heat of vaporization required to convert water to its vapor = 10,500 cals/mole). a. b. c. d.

4.

3.52 cal/mole deg 420.0 cal/mole deg 840 cal/mole deg 42.0 cal/mole deg

Compute the vapor pressure of water at 125oC. The vapor pressure of water at 100oC is 1 atmosphere, and the ΔHv is 9,720 calories/mole a. b. c. d.

2.279 atm 2.654 atm 1.95 atm 2.467 atm

5. Calculate H° and

S° for the following reaction are 28.05 kJ and 108.7 J/K, respectively: NH4NO3(s) + H2O(l)

NH4+ (aq) + NO3- (aq)

Calculate the value of Go for this reaction at 25o C, and explain why NH4NO3 spontaneously dissolves in water at room temperature.

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Theoretical questions:

1. The dipole moments of phenacetin, sulfanilamide, and testosterone are 5.67, 5.37, and 4.17. Which one do you expect to be most soluble in water? a. Phenacetin b. Sulfanilamide c. Testosterone 2. Hydrogen bonds have characteristics of: a. Ionic force only b. Both - ionic and dipolar force c. Dipolar force only 3. The critical temperature and pressure for CO2 gas are 31oC and 74.9 atm, respectively. Can you liquefy CO2 stored at 100oC by applying pressure only? a. No b. Yes 4. Which type of solids will dissolve at a greater rate? a. Crystalline b. Amorphous 5. A thermodynamic process, where the heat transfer is not zero, is called: a. Enthalpy driven process b. Isothermal process c. Adiabatic process d. Entropy driven process 6. Sodium chloride and methane are a. b. c. d.

electrovalent and electrovalent compound, respectively (b) covalent and electrovalent compound, respectively covalent and covalent compound, respectively electrovalent and covalent compound, respectively

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

7. The forces that bind molecules include: (i) repulsive and attractive forces (ii) van der Waals forces (iii) ion-dipole and ion-induced dipole forces (iv) hydrogen bonds a. b. c. d.

All of the above None of the above Only (ii), (iii), and (iv) of the above.

Only (i), (iii), and (iv) of the above.

8. Energy of a radiation can be calculated by a. dividing product of velocity of light and Planks constant by frequency of the radiation b. multiplying product of velocity of light and planks constant by wavelength of the radiation c. adding product of velocity of light and planks constant to wavelength of the radiation d. dividing product of velocity of light and planks constant by wavelength of the radiation 9. Aqueous solubility of iodine in presence of KI is due to a. b. c. d.

covalent interaction interaction between ion-dipole and ion-induced dipole electrovalent interaction ion-induced dipole forces only

10. Clausius-Clapeyron equation for liquids establishes relationship between a. b. c. d.

freezing point and absolute temperature vapor pressure and absolute temperature vapor pressure and degree Celsius temperature volume and absolute temperature

11. Polymorphs have different melting point, X-ray diffraction pattern and solubility but same chemical properties. a. b.

True False

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

12.

Polymorphs are same substance but in different crystalline forms which are characterized by a. b. c. d.

different melting points only different melting points, x-ray diffraction patterns, and solubility different x-ray diffraction patterns only different solubility only

13. The crystalline and amorphous solids are characterized by a. b. c. d.

melting point and heat of fusion, respectively freezing point and heat of fusion, respectively melting point and glass transition temperature, respectively glass transition temperature and melting points, respectively

14. In case of crystalline solids, changes in the freezing or melting point with pressure may be obtained by using: a. b. c. d.

Clapeyron Equation Van der Waals equation Gay-Lussac Law Ideal Gas law

15. Glass is an example of: a. b. c. d.

Amorphous Solids Crystalline Solids Uncharacterized solid Liquids

16. The glass transition temperature for an amorphous solid is the mid-point of the transition in which the solid converts from a glassy to rubber state. a. b. c. d.

True Depends on atmospheric condition False There is nothing like glass transition temperature

17. A substance which is bound together by weak forces is said to have: a. b. c. d.

Low heat of fusion and low melting point High heat of fusion and high melting point.

High heat of fusion and low melting point Low heat of fusion and high melting point

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

18. The intermolecular distance in solid is a. b. c. d.

Higher than that in gas but less than that in liquid.

Higher than that in both liquid and gas.

Higher than that in liquid but less than that in gas.

Less than that in both liquid and gas.

19. In a pressure cooker, water boils at a. b. c. d.

20.

temperature significantly higher than 100oC temperature significantly higher or lower than 100oC temperature significantly lower than 100oC 100oC

Select the correct statement(s) involving the 2nd law of thermodynamics. a. the entropy change of reversible thermodynamic processes is always zero b. the entropy change of reversible thermodynamic processes is always positive c. the entropy change of reversible thermodynamic processes is sometimes zero d. the entropy change of reversible thermodynamic processes is always negative

21. Select the correct statement(s) involving the 2nd law of thermodynamics. a. the entropy change of irreversible thermodynamic processes is always zero b. the entropy change of irreversible thermodynamic processes is always positive c. the entropy change of irreversible thermodynamic processes is sometimes zero d. the entropy change of irreversible thermodynamic processes is always negative

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Questions -Chapter 3 Numerical Questions: 1. When a capillary tube is immersed in benzyl benzoate, the liquid rose to a height of 1.63 cm at 25oC. The inside diameter of the capillary is 0.1 cm and the density of benzyl benzoate is 1.1120 g/cm3. What is the surface tension of benzyl benzoate? a. b. c. d.

44.45 dynes/cm 44.45 dynes/cm2 88.9 dynes/cm 04.45 dynes/cm

2. One gram of sucrose, molecular weight 342 g/mole, is dissolved in 100 mL of solution at 25C. What is the osmotic pressure of the solution? Given that R = 0.082 liter atm/mol deg. a. b. c. d.

0.082 atm 0.82 atm 0.71 atm 0.07 atm

3. How much NaCl is required to render 20 mL of a solution containing 0.25 g of apomorphine hydrochloride isotonic with blood serum? (Freezing point depression of 1% apomorphine is 0.08 degree). a. b. c. d.

0.18 g 0.009 g 0.9 g 0.145 g

4. Isotonic sodium chloride solution contains 0.9% w/v sodium chloride. If the E value of anhydrous dextrose is 0.18, calculate the percentage strength (w/v) of an isotonic solution of anhydrous dextrose. a. b. c. d.

5.0% 0.9% 0.5% 0.95%

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

5. Procaine HCl ……………. 0.25 g Sodium Chloride ………… q.s.

Sterile Water for injection .. ad 30 mL Make isotonic sol.

Sig. For injection.

How many grams of sodium chloride should be used in compounding the above prescription? (The E value of Procaine HCl is 0.21). a. b. c. d.

0.9 g 0.218 g 0.271 g 0.95g

6. The “v” value of calcium lactate is equal to 7.7. What is the percentage concentration of its isotonic solution? a. 3.9% b. 0.9% c. 0.5% d. 5.0% 7.

Viscosity of acetone is 0.280 cp at 25°C and the density is 0.788g/cm3. What is the kinematic viscosity of acetone? a. 0.355 poise b. 0.355 centistokes c. 0.355centipoise d. 0.355 stokes

8.

The kinematic viscosity of acetone is 0.397 centistokes and the density of acetone at 25°C is 0.788g/cm3. Calculate the fluidity of acetone. a. 3.196 cps-1 b. 3.025cps c. 3.025 poise d. 3.196 poise

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

9. A plastic material has a yield value of 2500 dynes cm-2. At shearing stress above the yield value, P, was found to increase linearly with rate of shear, Vg. If the rate of shear, Vg, was 160 sec-1 when F was 7500 dynes cm-2. Calculate the plastic viscosity. a. b. c. d.

31.2 centistokes 31.2 stokes 31.2 cps 31.2 poise

Theoretical questions: 1. Using starch in oral rehydration mixture to replenish fluid during diarrhea is a better choice than increasing glucose concentration. a. True b. False 2. Charcoal helps in the treatment of drug poisoning via the mechanism of: a. b. c. d.

adsorption absorption ionization in acidic media ionization in basic media

3. Micelles are used for delivering a drug because: i. micelles can solubilize insoluble drugs ii. micelles may reduce antigenicity a. b. c. d.

Only i is correct Only ii is correct Both i and ii are correct Neither i nor ii is correct

4. Quaternary salts e.g. bephenium hydroxynaphthoate and pyrvinium embonate are used in worm infection of lower bowel because a. being quaternary they are well soluble in both water and lipid b. being quaternary they are poorly soluble in both water and lipid c. being quaternary they are soluble in water but not in lipid d. being quaternary they are soluble in lipid but not in water

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

5. Digoxin is a poorly soluble drug. Therefore, its physical forms such as particle size would have a significant effect on its therapeutic outcomes. (a) True (b) False 6. Administering bentonite or magnesium trisilicate based antacid before a poorly soluble drug such as digoxin would result in excellent bioavailability. (a) True (b) False 7. Two capillary tubes differing in internal diameter are placed in water. Which one of the statements is correct about height of the water level in capillary tubes? i. ii.

a. b. c. d.

8.

Only i is correct Only ii is correct Both i and ii are correct Neither i nor ii are correct

Charcoal adsorbs all drugs with equal efficiency. a. b.

9.

Water level would be higher inside the capillary tube wider in internal diameter.

Water level would be higher inside the capillary tube narrower in internal diameter.

True False

Which of the following flow patterns exhibited by a drug-dosage form is extremely unacceptable? a. b. c. d.

Pseudoplastic Plastic Thixotropic Dilatant

10. Thixotropy is a special characteristic that is exhibited by shear thinning systems, such as: i. ii. iii.

Dilatant Plastic Pseudoplastic

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

a. b. c. d.

All i, ii and iii are correct Only i and ii are correct Only ii and iii are correct Only i and iii are correct

11. Which of the following facts is/are correct with respect to thixotropy: i. ii.

iii.

a. b. c. d.

Thixotropy is exhibited by shear thinning systems, such as pseudoplastic and plastic liquids.

Thixotropy can be defined as, "an isothermal and comparatively slow recovery, on standing of a material, of a consistency lost through shearing".

Thixotropic behavior is useful for many pharmaceutical preparations e.g., suspensions.

Only i correct Both i and ii are correct Only iii is correct All i, ii and iii are correct

12. 1 centipoise is equal to: a. b. c. d.

0.0001 poise 0.01 poise 0.001 poise 0.1 poise

13. The Arrhenius equation of rheology expresses the relationship between: a. b. c. d.

viscosity and temperature viscosity and concentration viscosity and interfacial tension pressure and temperature

14. Blood plasma normally shows viscosity only, while whole blood is both viscous and elastic. a. b.

True False

15. The key factors in the viscoelasticity of blood are: i. ii.

Aggregation Deformability

a.

Both i and ii are correct

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

b. c. d.

Only ii is correct Only i is correct Neither i nor ii is correct

16. Ostwald viscometer: a. b. c. d.

Used for liquids that flow relatively easily Operate at multiple rate of shear Useful for Non-Newtonian liquids.

None of the above

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 4 - Questions Numerical Questions: 1. What molar ratio of sodium acetate and acetic acid should you use to prepare an acetate buffer of pH 5? The pKa of acetic acid is 4.76. a. b. c. d.

1.54:1 1.74:1 1.47:1 1:1

2. A weak basic drug has a pKa 4.8. In urine, with a pH of 5.8, how much % of this medication would exist in its original unionized form? a. b. c. d.

1% 0.99% 99.01% 90.91%

3. When atropine was added to a mixture of water (solvent1) and octanol (solvent2) at 25oC, its concentration in octanol (C1) and in water (C2) was 3.96 mg/ml and 2.2 mg/ml, respectively. What is the partition coefficient (K) of atropine in this system? a. 6.16 octanol/water b. 8.71 octanol/water c. 0.55 octanol/water d. 1.8 octanol/water 4. Five grams of Compound A is added to 100 mL of water. The partition coefficient for Compound A between hexanes and water is 3. How much of Compound A could be in hexane if you extract it from the water by adding 200 mL of hexanes? [Assume that quantity of hexane is more than enough for solubilizing the Compound A and temperature is 20oC] a. (a) 05.0 g b. (b) 3.75 g c. (c) 4.8 g d. (d) 0.6

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

5. If the rate of injection of a drug and its solubility are 5 mg/min and 0.6 mg/mL, respectively, what blood or saline flow rate is required to prevent precipitation of the drug?

a. b. c. d.

Greater than 8.33 mL/min Greater than 1.2 mL/min less than 8.33 mL/min less than 1.2 mL/min

Theoretical questions: 1. In a solution of NaCl, a little amount of a solid was added. Which of the following statements is/are true: i.

Molarity of NaCl will change ii.

Molality of NaCl will not change iii.

Molality of NaCl may or may not change depending on the interaction of solvent and the added solid. a. b. c. d.

Only i is correct Only ii is correct Only iii is correct Both i and iii are correct

2. Which one statement is correct? i.

Ionized drugs are useful for optimum therapeutic effect ii.

Un-ionized drugs are useful for optimum therapeutic effect iii.

Either ionized or unionized drugs could be useful for optimum therapeutic effect depending on site of pharmacological action a. b. c. d.

Only i is correct Only ii is correct Only iii is correct None of the above is correct

3. The greater the pKa value, the stronger the acid would be. a. b.

True False

4. The greater the acidity constant, Ka, the stronger the acid would be. a. b.

True False

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

5. In a medium of pH 5, atropine sulfate (a weak basic drug) will dissolve more than in a medium of pH 10. a. b.

True False

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 5 - Questions Numerical Questions: 1

The time taken for 5% of a drug to decompose by first-order kinetics is (where k1 is the first order rate constant) is: a. b. c. d.

2

What is the remaining concentration in mg/mL of a drug (initial concentration a = 7 mg/mL) after a time equivalent to 3 half-lives assuming that the decomposition follows first-order kinetics? a. b. c. d.

3

0.105/k1 0.051/k1 k1/0.05 0.022/ k1

3.5 1.75 0.875 1.167

The following data were obtained for the hydrolysis of 0.2 M of a drug which follows first order kinetics: Table: The percentage of original amount of the drug remaining at a specific time

% drug remaining 100 97.8 90.3 77.1 63.1 48.9 38.9 Time (hr)

0

1

2

5

9

Calculate the rate constant (a) 0.052 hr (b) 0.52 hr (c) 5.25 hr (d) 5.3 hr

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

14

18

4

The following data were obtained for the hydrolysis of 0.2 M of a drug which follows first order kinetics: Table: The percentage of original amount of the drug remaining at a specific time

% drug remaining 100 97.8 90.3 77.1 63.1 48.9 38.9 Time (hr)

0

1

2

5

9

14

18

Calculate the half time a. b. c. d.

5

33.2 hr 23.2 hr 13.3 hr 3.2 hr

The initial concentration of a drug in an aqueous preparation was 12.0 x 10-3 M. After 24 months the concentration was found to be 9.2 x 10-3 M. The drug is known to be ineffective after it has decomposed to 70% of its original concentration. Assuming that decomposition follows first order kinetics, calculate the expiry date of the drug preparation. a. b. c. d.

40.9 months 35.4 months 30.0 months 32.4 months

Theoretical questions: 1. Which of the following factors can affect diffusion of drug? i. Concentration gradient ii. Particle size iii. Thickness of the diffusion barrier a. b. c. d. e.

Only i is correct Only ii is correct Only iii is correct All I, ii and iii are correct None of the options is correct

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

2. Which of the following statements about zero order reaction is/are correct? i. The rate of reaction is dependent on the concentration of reactant(s). ii. The half-life = 0.693/k where k is zero order reaction rate constant. a. Only i is correct b. Only ii is correct c. Both are correct d. Neither i nor ii is correct.

3. The degradation of local anesthetic procaine can be prevented by making its complex with a. caffeine b. calcium c. sodium d. potassium 4

A drug may be degraded chemically by i. either hydrolysis or oxidation but not by both ii. either hydrolysis or oxidation and even by both a. b. c. d.

5

The empty spaces in parenteral vials or ampoules are filled with nitrogen to prevent the degradation of drugs by: a. b. c. d.

6

only (i) is correct neither (i) nor (ii) is correct only (ii) is correct both (i) and (ii) are correct

oxidation photolysis isomerization hydrolysis

Which is not effective against photolysis? a. using an amber colored container b. coating a tablet with cellulose acetate phthalate c. coating a tablet with UV absorbing material such as vinyl acetate containing oxybenzone. d. storing in the dark

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

7

The overall degradation in case of a suspension is usually: a. zero order

b. second order c. third order d. None of the above 8

In a zero order reaction, the rate of decomposition is dependent on the concentration of one of the reactants. a. True b. False

9

In a zero order reaction: i. the rate of decomposition is dependent on the concentration of one of the reactants ii. the rate of decomposition is independent of the concentration of reactants iii. A plot of the amount remaining (as ordinate) against time (abscissa) is linear with a slope of 1/k a. b. c. d.

only ii is correct none is correct only iii is correct only i is correct

10 In a zero order reaction: i. the half-life is equal to 0.693/k ii. the unit of k is concentration / time iii. a plot of the amount remaining (as ordinate) against time (abscissa) is linear with a slope of 1/k a. b. c. d.

none is correct only ii is correct only i is correct only iii is correct

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

11 In a second order reaction: i. The rate of reaction depends on the concentration of two reacting species. ii. A plot of time (as abscissa) against (as ordinate) is linear with a slope equal to 1/k2 iii. The half-life is independent of concentration a. b. c. d.

none is correct only i is correct only iii is correct only i and ii are correct

12 In a study of the hydrolysis of a drug in aqueous solution a plot of logarithm of the amount of the drug remaining (as ordinate) against time (abscissa) is linear: i. the reaction is zero order ii. the slope is -2.303/k. iii. the half-life does not depends on the initial concentration of reactant a. b. c. d.

only iii is correct only i is correct only ii is correct both i and (ii) are correct

13 Which of the following equations predict the stability of a drug at room temperature from experiments at accelerated condition at higher temperatures? a. b. c. d. e.

The Stokes Equation The Arrhenius Equation The Ideal Gas Equation The Michaelis-Menten Equation Gibbs Equation

14 Fick’s law of diffusion establishes relationship between/among i. flux, diffusion coefficient of a penetrant, concentration, and distance of movement perpendicular to the surface of the barrier. ii. flux, diffusion coefficient of a penetrant, concentration, and distance of movement horizontal to the surface of the barrier. a. Only ii is correct Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

b. Neither i nor ii is correct c. Both i and ii are correct d. Only i is correct 15 Fick’s second law states that the change in concentration with time in a particular region is proportional to the change in the concentration gradient at that point in the system. a. True b. False 16 The apparatus used for measuring the diffusion coefficient of substance is called: a. b. c. d.

osmosis cells rheometer diffusion cells voltmeter

17 In diffusion experiments using diffusion cells, which of the following statement is correct? a. the drug is sometimes added to the donor chamber and sometimes to the receiver chamber. b. the drug is always added to the donor chamber and the penetrant samples are always taken from receiver chamber at different time points. c. the penetrant samples are taken sometimes from receiver chamber and sometimes from donor chamber. d. the drug is always added to the donor chamber and the penetrant samples are sometimes taken from receiver chamber and sometimes from donor chamber at different time points.

18 Diffusion coefficient is not called as a diffusion constant. a. True b. False 19 Diffusion of a drug is inversely proportional to the viscosity of the medium in which diffusion is taking place. a. True b. False 20 Permeability is dependent on the Diffusion coefficient of the penetrant. a. true b. false Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

21 Diffusion of a drug is through a biological membrane is independent of its molecular weight a. true b. false 22 In an diffusion experiment, Lag time can be used to determine the Diffusion coefficient of a drug a. true b. false 23 Temperature at which diffusion is carried out does not affect the diffusion of a drug a. true b. false 24. The passage of drug molecules from a region of high drug concentration to a region of low drug concentration is termed as: a. pinocytosis b. passive diffusion c. active transport d. phagocytosis e. none of the above 25. Amorphous form of drugs have faster dissolution rates than the crystalline forms a. True b. False

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 6 - Questions Numerical 1. A batch of a polymer is made up of two monodisperse or homogenous fractions – labeled fraction A1 and fraction A2. The molecular weights of fractions A1 and A2 are 100,000 and 10,000 g/mole, respectively. The number of moles of fraction A1 and A2 present are 6 and 4, respectively. Calculate the number average molecular weight of the polymer.

2. The following table shows the molecular weights and intrinsic viscosities of various fractions of a polymer:

Fraction 1 2 3 4 5

Intrinsic viscosity (dL/g) 0.297 0.351 0.912 1.234 1.345

Molecular weight (g/mol) 70,000 100,000 300,000 450,000 500,000

Determine the values of “K” and “a” in the Mark-Houwink equation, ሾሿ ൌ ‫ܯܭ‬௔ , for the polymer.

3. The viscosity of pol (caprolactom) of molecular weight 3.24 x 103 at 250C in m-cresol was found to be 0.34 dl/g. if the K value is 1.27 x 10-3 g/dl determine the Mark-Houwink coefficient for this system.

Theoretical questions 1.

Which of the following is not a polymer? a. b. c. d.

Starch Cellulose Protein Amino acid

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

2.

Proteins are formed by the joining of repeated units of: a. b. c. d.

3.

An important property of pharmaceutical polymers to consider is: a. b. c. d.

4.

Molecular weight distribution but not molecular weight Neither molecular weight nor molecular weight distribution Molecular weight but not molecular weight distribution.

Molecular weight and molecular weight distribution

Which of these polymers can be used in enteric coating? a. b. c. d.

7.

DNA Methyl cellulose Carboxy methyl cellulose Nucleotide

Which of the following determines many of the physical properties of polymers? a. b. c. d.

6.

Both molecular weight and molecular weight distribution Neither molecular weight nor molecular weight distribution Molecular weight but not molecular weight distribution Molecular weight distribution but not molecular weight

Which of the following polymers is synthesized by biosynthetic pathway in human? a. b. c. d.

5.

Nucleotide Amino acids Cellulose Sugars

Heparin Cellulose acetate phthalate PLGA Methyl cellulose

Polymers with regular alternation of the side chains on the polymer backbone are referred to as: a. b. c. d.

syndiotactic atactic isotactic isometric

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

8.

Polymers with random alternation of the side chains on the polymer backbone are referred to as: a. b. c. d.

9.

isometric atactic syndiotactic isotactic

Polymers with similar side chains on the polymer backbone are referred to as: a. b. c. d.

isometric isotactic atactic syndiotactic

10. Human Papilloma Virus (HPV) vaccine is used for: i. ii.

prevention of HPV infection treatment of HPV infection

a. b. c. d.

Only i is correct Only ii is correct Both i and ii are correct Neither i nor ii is correct

11. Antisense oligonucleotide is used to inhibit the expression of a specific gene sequence.

True False

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

12. Here are some characteristics of a protein: i. Protein is consisted of regularly repeating backbone with amino acid side chains that interact with each other ii. Protein is consisted of regularly repeating backbone with amino acid side chains that do not interact with each other iii. Three dimensional structure of a protein is essential for its therapeutic activity iv. Three dimensional structure of a protein is not essential for its therapeutic activity Which statements are correct? a. b. c. d.

Only i is correct Only ii is correct Both i and iii are correct Both ii and iv are correct

13. Protein stability refers to the maintenance of: a. the primary structure only b. the secondary structure only c. the tertiary structure only d. the primary, secondary, tertiary, and quaternary structures

14.

Physical instability of protein can occur via: a. b. c. d.

15.

Aggregation only Precipitation only Aggregation, adsorption, precipitation, or denaturation Adsorption only

Chemical instability of protein can occur via: a. b. c. d.

Deamidation only Racemization only Deamidation, racemization, oxidation, disulfide exchange or hydrolysis Oxidation only

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

16.

Select the correct pair of protein/peptide and corresponding comment: Protein/peptide 1. Insulin lispro 2. Insulin glargine 3. Erythropoietin 4. Lactase 5. Bevacizumab 6. Human papillomavirus (HPV) vaccine 7. L-Asparaginase

a. b. c. d.

17.

Comment i. stimulates erythropoiesis ii. relieves bloating iii. prevention of HPV infection. iv. a long-acting insulin v. used in acute lymphocytic leukemia vi. binds to vascular endothelial growth factors (VEGFs) vii. a rapid-acting insulin

1-vii, 2-iv, 3-i, 4-ii, 5-vi, 6-iii, and 7-v 1-iv, 2-vii, 3-i, 4-ii, 5-vi, 6-iii, and 7-v 1-vi, 2-iv, 3-i, 4-ii, 5-vii, 6-iii, and 7-v 1-vii, 2-iv, 3-ii, 4-i, 5-vi, 6-iii, and 7-v

Select the correct pair of protein/peptide and corresponding comment: Oligonucleotides 1. Pegaptanib Sodium 2. Fomivirsen 3. Mipomersen

a. b. c. d.

1-i, 2-iii, 3-ii 1-iii, 2-i, 3-ii 1-iii, 2-ii, 3-i 1-ii, 2-iii, 3-i

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Comment i. inhibits human cytomegalovirus (CMV) replication ii. used in the treatment of familial hypercholesterolemia iii. inhibit vascular endothelial growth factor (VEGF)

Chapter 7 - Questions Mathematical Questions 1. The octanol water partition coefficient of an investigational drug known to be unionized in water or associate in octanol was determined at 23ºC. At this temperature, only 0.24 g of the drug was found in 100 ml of water, but 2.70 g of the same drug was dissolved 100 ml octanol. (a) Calculate the octanol-water partition coefficient of this new drug (b) Do you think this drug is hydrophilic or lipophilic?

2. A drug powder was subjected to angle of repose studies. The heap of the powder formed from a glass funnel was carefully monitored. The height of the heap was 12 mm and the diameter of the heap formed was 30 mm. Determine the angle of repose of this powder.

3. The tap as well as bulk density of a powder sample was determined by appropriate methods on a carefully weighed 120gram sample. After passing through an 18 mesh screen, the volume of the 100 g powder was determined according to specifications. The unsettled apparent volume of powder was found to be 100 cc. During the tap density measurement the final tapped volume was found to be 93 cc. calculate both the bulk and tap density for this powder sample.

Bulk density = Tap density =

= =

= 1.2 g/cc

= 1.29 g/cc

4. A coarse dispersion of a powder drug with a mean particle diameter of 100µm was prepared in a 2% (w/v) methocel solution. Calculate the velocity of sedimentation of the powder in cm/sec, when the density of powder was 2.44 g/cc, the density of the dispersion medium was 1.01 g/cc, and the viscosity of the dispersion medium was 2700 centipoise.

18 V=

.

.

=

.

= 0.00029 cm/sec

Theoretical questions 1. The principal use of titanium dioxide in Pharmaceutics is as a/n a) Antioxidant b) Lubricant c) Disintegrator d) Opacifying agent Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

e) Binder 2. Cellulose acetate phthalate is used in formulation of dosage form as a/n a) Suspending agent b) Enteric coating material c) Emulsifier d) Solubilizing agent e) Flavoring agent 3. In tablet dosage form starch can be used as I. Binder II. Disintegrant III. Flavoring agent a) I only b) II only c) III only d) I and II only e) II and III only 4. Identify the a flavoring agent from the following inactive materials a) Tween 20 b) Starch c) Magnesium stearate d) Gum acacia e) Peppermint oil 5. The needs for various dosage forms may include: I. to mask the unpleasant taste or odor of drug substance II. to protect from the destructive influences of gastric acid during oral administration III. to administer a high dose of insoluble drug in a liquid dosage form a) I only b) II only c) III only d) I and II only e) I, II and III only

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

6. Identify the drug whose physical form is a liquid at room temperature a) Aspirin b) Acetaminophen c) Ibuprofen d) Salicylic acid e) Undecyclenic Acid 7. Gums are used in tableting primarily as a) Disintegrant b) Glindants c) Lubricants d) Flavoring agent e) Binding agents 8. Identify the false statement a) A solid drug is more stable than when it is in solution b) A highly volatile liquid can be flammable c) Liquid drugs can be easily formulated as sold dosage form d) Liquid dosage forms in large volumes are difficult to carry and transport e) Solid dosage forms are dispensed more frequently as compared to other dosage forms in the USA 9. Which of the following is a measure of the flow property of a powder drug? a) Angle of repose b) Bulk density c) True density d) Partition coefficient e) Melting point 10. Particle size of the drug can affect all the following except: a) Solubility b) Molecular weight c) Dissolution d) Absorption e) Stability 11. Equilibrium solubility of an acidic drug is determined in a/n I. Acidic medium II. Basic medium III. Neutral pH Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

a) I only b) II only c) III only d) I and II only e) II and III only 12. Identify the true statement a) Metastable form has a greater dissolution rate compared to the stable form b) Different polymorphs of the same solid are identical in their crystal structures c) The amorphous form of a compound is always less soluble than the corresponding crystal forms d) Different polymorphs of the same solid will have identical solubility e) Polymorphism of a solid dosage form is not an issue during preformulation work 13. Which mesh sieve will yield powders with the smallest particle size? a. b. c. d. e.

10 40 80 270 400

14. The process by which aqueous solubility of a drug is increased by incorporation of a surfactant is called a) equilibrium solubility b) solubilization c) common ion effect d) complexation e) sedimentation 15. The octanol-water partition coefficient of five non-ionizable drugs is listed below. Identify the most lipophilic drug from the list. a) 15.0 b) 16.2 c) 2.3 d) 1.2 e) 0.75 16. Identify the more appropriate drug delivery system from the list of dosage forms a) Procardia xl Tablet b) Aspirin tablet c) Nyquil soft gelatin capsule Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

d) Atropine eye drop e) Calamine Lotion 17. Which of the following pharmaceutic ingredients can be used to enhance flow properties of powders a) Ethyl cellulose b) Tween 20 c) Magnesium stearate d) Lactose e) Mannitol 18. Angle of repose is used in preformulation work to determine a) Particle size b) Sedimentation velocity c) Flow property d) Partition coefficient e) Contact angle 19. Match both columns as appropriate a) X-Ray diffraction b) Stokes Equation c) Noyes Whitney Equation d) Surfactant e) Lactose powder

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

i) particle size ii) polymorphism iii) diluent iv) dissolution v) HLB

Chapter 8 Mathematical questions

1.

During a dissolution study, it was found that when 1.55 grams of granules with a total surface area of 0.28 x 104 cm2 were exposed to 500 mL of water at 25C, 0.76 grams of the granules dissolved in the first minute. Calculate the dissolution rate constant (k) of the granules. The solubility of the drug is 15 mg/mL at 25C.

2. The dissolution of an investigational new drug was studied and the following parameters were available to the preformulation scientist: Total surface area of the drug = 2.5 x 103 cm2.

The saturated solubility of the drug is = 0.35 mg/mL (at room temperature) The diffusion coefficient of the drug in the release medium = 1.75 x 10-7cm2/sec The thickness of the diffusion boundary layer = 1.25 μm = 1.25 x 10-4 cm Conc of drug in the release medium = 2.1 x 10-4mg/mL (a) Determine the dissolution rate of this drug at room temperature. (b) If the surface area is increased by ten times what will be the new dissolution rate for this drug? (c) Is this dissolution carried out under sink condition?

Theoretical Questions

1. The tablet that is intended for placing below the tongue is called: a. chewable tablet b. buccal tablet c. sublingual tablet d. effervescent tablet e. enteric coated tablet 2. Which of the following ingredients can be used as a lubricant in tablet compression: a. lactose b. sugar c. magnesium stearate d. methylcellulose e. none of the above 3. The basic function of cams in a tablet press is to: a. control the size and shape of tablet b. distribute the material into the dies c. guide the punches d. store the materials to be compressed Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

e. guide the dies 4. Eutectic mixtures are powders that: a. liquefy due to absorption of atmospheric moisture b. liquefy upon mixing at a certain composition c. liquefy due to release of water of crystallization d. release carbon dioxide when mixed with water e. none of the above 5. In contrast to hard-gelatin capsules, the shell of soft-gelatin capsules contains: a. b. c. d. e.

plasticizers such as glycerin or sorbitol higher moisture content of 40 to 55% unlike 13-16% for hard-gelatin capsules preservatives such as methyl or propyl paraben all of the above none of the above

6. Which of the following instruments is used to determine the tendency of a tablet to powder, chip or fragment during handling? a.

Roche friabilator b. micrometer calipers c.

USP dissolution apparatus 2 d.

Pfizer tester e.

USP disintegration apparatus 7. Which of the following liquids cannot be incorporated into soft-gelatin capsules? a. ethyl alcohol b. polyethylene glycol (PEG) 200 c. polyethylene glycol (PEG) 600 d. polysorbate 80 e. vegetable oil 8. For best storage and processing conditions of hard gelatin capsules, which of the following humidity conditions is more ideal: a.

0-15% RH b.

15-35% RH c.

35-45% RH d.

45-65% RH e.

65-75% RH

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

9. Identify the plastricizer used in a soft gelatin capsule: a. gelatin b. fumaric acid c. titanium dioxide d. glycerol e. lactose 10. A powder giving up moisture to the air and liquefy during the process is called: a. deliquescent b. efflorescent c. hygroscopic d. effervescent e. eutectic 11. According to the USP disintegration test, which of the following tablets should not dissolve in simulated gastric fluid within 1 hour? a. chewable tablet b. buccal tablet c. sublingual tablet d. effervescent tablet e. enteric coated tablet 12. The most common disintegrator in compressed tablet is a. starch b. magnesium stearate c. mannitol d. lactose e. cellulose acetate phthalate 13. Which of the following may be used for enteric coating? a. starch b. magnesium stearate c. mannitol d. sodium alginate e. cellulose acetate phthalate 14. How can we prevent “Mottling”, or uneven color distribution in the manufacture of a tablet by the wet granulation method? a. dry the granules at a lower temperature b. change the manufacturing procedure to dry granulation c. use direct compression d. all the methods, a, b, or c, may be used e. none of the above Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

15. The dissolution equation is also known as a. Young’s equation b. Noyes Whitney equation c. Henderson-Hasselbalch equation d. Stoke’s equation e. Vanthof’s equation 16. A substance that is often used to subcoat tablets is a. Sugar b. Shellac c. Carnuba wax d. Sodium chloride e. Sodium stearate 17. A satisfactory suppository base must meet all of the following criteria except: a) b) c) d) e) 18.

Which category of suppository bases dose Cocoa butter belongs to? a) b) c) d) e)

19.

It should be compatible with variety of drugs It should be nontoxic and nonirritating It should dissolve or disintegrate rapidly in the body cavity It should melt below 30o C It should be inert

Oleaginous Water soluble Water dispersible Hydrophilic None of the above

Which of the followings statements is not true for suppository bases? a) b) c) d) e)

Low acid values are important for good suppository bases Solidification value of suppository base is defined as the time required for base solidification when it is cooled The water number of suppository base cannot be increased by the addition of surface active agents The possibility of decomposition by moisture, acids, and oxygen increases with high iodine values of suppository bases Suppository bases should melt at body temperature

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 9 - Questions Mathematical questions 1.

A mineral oil emulsion (o/w) contains an internal phase with a density 0.90 g/cc. Density of the external phase is 1.05 g/cc. If the oil particles have an average diameter of 5 µm (5 x 10-4 cm), what is the velocity of creaming in cm per day? The viscosity of the external phase is 0.5 poise and the gravity constant is 981 cm/sec2.

2.

20 mL of a blend of surfactants with HLB of 9.0 are required for preparing an emulsion.

The two surfactants used have the HLB values 8.0 and 12.0 respectively. Compute the ratio of the blend.

3.

A total volume of 100 mL of an emulsion is to be prepared in a pharmacy. The volume of the blend of surfactants that can be used should not exceed 5% v/v. The optimum HLB value required is 12. The two surfactants available in the pharmacy are Span 80 (HLB = 4.3) and Tween 20 (HLB = 16.7). Compute the volume ratio of the blend to be used in the preparation of the emulsion.

4.

The final or ultimate volume of the sediments for three suspensions was 50 mL, 100 mL and 150 mL respectively. If the original volume of the suspensions were 100 mL in each case, determine the sedimentation volume of each suspension.

Theoretical Questions 1. Which of the following is a hydrophilic colloid used as an emulsifying agent? (a) alcohol (b) acacia (c) water (d) glycerol (e) Tween-20 2. All of the following are properties of an oil in water (O/W) emulsion except: (a) Can be diluted with water without separation (b) Oil soluble dyes will dissolve in it (c) Will conduct electricity (d) Can be made into a multiple emulsion of the O/W/O type (e) Oil is present in the internal phase 3. Sedimentation in a suspension can be affected by Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

(a) Particle size of the dispersed particles (b) Differences in the density of the particles and the dispersion medium (c) Viscosity of the dispersion medium (d) Gravity (e) All of the above

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

4. Repulsive forces of interaction between particles in suspension can arise due to? (a) London Forces (b) Zeta potential (c) Dipole-induced dipole attractions (d) (a) and (c) only (e) (a), (b), and (c) 5. Creaming is generally observed in: (a) O/W emulsion (b) W/O emulsion (c) Suspension (d) True solution (e) None of the above 6. Identify the formulation which is an example of a colloidal dispersion used in pharmacy: (a) Sodium valproate syrup (b) Potassium chloride solution (c) Argyrol nasal drop (d) USP syrup (e) Ephedrine elixir 7. Flow of colloidal particles on the application of electrical charges is termed as: (a) Electroosmosis (b) Ultrafiltration (c) Electrophoresis (d) Dialysis (e) Sedimentation 8. Which of the following can be used as a suspending agent? (a) Carbopol 934 (b) alcohol (c ) water (d) acetone (e) Tween-20

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

9. All of the following are properties of water in oil (W/O) emulsion except: (a) Can be diluted with water without separation (b) Oil soluble dyes will dissolve in it (c) Will not conduct electricity (d) Can be made into a multiple emulsion of the W/O/W type (e) Can be diluted with oil 10. All of the following parameters can affect velocity of sedimentation in a suspension except (a) Particle size of the dispersed particles (b) Differences in the density of the particles and the dispersion medium (c) Viscosity of the dispersion medium (d) Gravity (e) Total volume of the suspension

11. Particle charges in a suspension can arise due to: (a) Adsorption (b) Ionization (c) Differences in dielectric constant between dispersed particles and dispersion medium (d) All of the above (e) Only (b) and (c) 12. Which of the following methods of preparation of emulsion uses temperature? (a) Dry gum (b) Wet gum (c) Bottle (d) Beaker (e) None of the above 13. Negative sedimentation is generally observed in case of : (a) W/O emulsion (b) O/W emulsion (c) Suspension (d) True solution (e) None of the above

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

14. Flow of solvent (not the colloidal particles) on the application of electrical charges is termed as: (a) Electroosmosis (b) Ultrafiltration (c) Electrophoresis (d) Dialysis (e) Sedimentation 15. The sedimentation height (SH) for five suspensions are given below. Identify the SH where one should expect the highest supernatant height? (a) 0.25 (b) 0.125 (c) 0.5 (d) 0.625 (e) 0.725 16. Which of the following suspensions is preferred by a pharmacist? (a) Deflocculated (b) Controlled deflocculated (c) Flocculated (d) Controlled flocculated (e) None of the above 17. Which of the following methods is not used to determine the molecular weight of colloidal particles? (a) Osmotic pressure measurement (b) Diffusion (c) Sedimentation (d) Only (a) and (b) (e) None of the above 18. In which of the following liquid dosage forms a high dose of insoluble solid can be administered orally? (a) (b) (c) (d) (e)

Spirits Elixirs Colloids Suspension Emulsion

19. Which of the following liquid oral dosage form contains high percentage of sucrose?

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

(a) (b) (c) (d) (e)

Elixir Tincture Syrup Fluid Extract none of the above

20. Which of the following is used to describe the protective action of a colloid? (a) Avogadro’s number (b) Vanthoff’s number (c) Ideal gas constant (d) HLB number (e) None of the above 21. Which of the following is/are reasons for using an emulsion?

I. Can improve or mask the taste of some medications II. Can improve the bioavailability of some medications III. Can be used to make some products into aerosols (a) (b) (c) (d) (e)

I only II only III only I and II but not III I, II, and III

22. You need to make an oil soluble multivitamin emulsion in water. What properties do you want for your emulsion?

I. W/O emulsion II. O/W emulsion III. HLB of 3-6 IV. HLB of 8-16 (a) (b) (c) (d) (e)

I only II only I and III II and IV I, II, III, and IV

23. The difference in potential between the actual surface of the particle and the electroneutral region (bulk of the dispersion) is termed as: (a) Zeta potential (b) Electrokinetic potential (c) Nernst potential Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

(d) All of the above (e) Non of the above 24. In the case of a coarse dispersion of a solid in an insoluble liquid, identify the FALSE statement: (a) Dispersion exhibits sedimentation (b) Dispersed particles will have no charges (c) Dispersed particles will have some charges (d) Stoke’s law can be used to determine the velocity of sedimentation (e) The velocity of sedimentation will have a positive value

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 10 - Questions A The vapor pressure of pure propellant-A (MW 137.4) at 210C is pA0 = 13.4 psi and that of propellant-B (MW 120.9) is pB0 = 84.9 psi. A 60:40 mixture (A: B) by gram weight of the two propellants were mixed in an aerosol formulation. Answer the following questions (1-5): 1.

The number of moles of propellant-A present in the mixture is: a) 0.364 moles b) 0.437 moles c) 0.291 moles d) 4.48 moles e) 0.496 moles

2.

The number of moles of propellant B present in the mixture is: a) 0.563 moles b) 0.636 moles c) 0.331 moles d) 4.48 moles e) 2.99 moles

3.

The mole fraction of propellant A in the mixture is: a) 0.569 b) 0.431 c) 0.468 d) 0.228 e) 0.208

4.

The partial pressure of propellant A in the mixture is: a) 36.592 psi b) 8.04 psi c) 33.96 psi d) 7.625 psi e) 6.27 psi

5.

The total vapor pressure of the mixture is: a) b) c) d) e)

36.592 psi 8.04 psi 33.96 psi 7.625 psi 44.217 psi

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Sample Discussion Case (6-8) Albuterol is a short-acting moderately selective beta-2-receptor agonist used for acute bronchodilation. It is often used in acute exacerbations of asthma. There are numerous aerosol dosage forms that contain albuterol as an active pharmaceutical ingredient. Three examples of these formulations include: AccuNeb® (albuterol sulfate) Inhalation Solution Foil-wrapped unit dose vials containing 3 mL of drug solution.

Each package contains 5 foil pouches with 5 unit dose vials per pouch.

Recommended to use Pari LC Plus™ nebulizer (with face mask or mouthpiece) connected to a Pari PRONEB™ compressor at a 3.6 L/min airflow rate.

Other nebulizers can be used.

0.63 mg*/3 mL and 1.25 mg*/3 mL as the albuterol base.

Ventolin HFA® 90mcg/actuation Inhalation Aerosol Foil-wrapped pressurized aluminum canister fitted with a counter and a blue plastic actuator.

Easyhaler Salbutamol®

The canister should only be used with the actuator provided.

The device must be primed prior to use.

Shake well before use.

Approved instructions are provided with the product.

Patients are instructed to perform a rapid and forced inhalation through the Easyhaler® device.

Approved instructions are provided with the product.

90 mcg* per actuation.

HFA-134a

Formulation Properties

Sodium chloride, sulfuric acid, water Solution is clear, colorless, isotonic, sterile, preservativefree, 3.5 pH

100 mcg* per actuation and 200 mcg* per actuation as albuterol base.

Lactose monohydrate

Storage Recommendations

Store between 2°C and 25°C (36°F -

How Supplied

Device Used

Dose Information

List of Excipients

The canister contains a crystalline drug suspension in the propellant. Each actuation of the inhaler delivers 120 mcg of albuterol sulfate in 75 mg of suspension from the valve and 108 mcg of albuterol sulfate from the mouthpiece Store between 15° and 25°C (59° and 77°F).

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Dry powder inhaler with 200 actuations.

The inhaler is wrapped in laminate foil and packed in a cardboard box.

White or almost white odorless powder.

Store in a dry place at a temperature not

Company

77°F). Protect from light and excessive heat. Store unit-dose vials in protective foil pouch at all times.

Once removed from the foil pouch, use vial(s) within one week.

DEY Pharma

Store the inhaler with the mouthpiece down.

For best results, the inhaler should be at room temperature before use.

exceeding 25°C. Use within 6 months of opening the foil pouch.

GlaxoSmithKline

Orion Pharma (UK) Ltd.

*Formulated as albuterol sulfate.

6. Compare and contrast the three albuterol drug products with respect to: a. The device and equipment needed for drug administration b. The breathing requirements necessary for optimal drug deposition in the lungs c. The mental cognition and physical dexterity needed to properly self-administer the drug d. The excipients and their function in the formulation 7. Which product could prevent the most challenges for proper aerosol delivery to the lungs in an acute asthma attack? Why? 8. Discussion: Why are there so few excipients used in these formulations?

True-False Questions Answer true or false for the following statements: 9. The Total Lung Capacity (TLC) is an air volume that a typical patient breathes in and out in normal tidal breathing.

10. The Residual Volume (RV) is an air volume that cannot be voluntarily expelled from the lungs.

11. Airflow is considered to be turbulent throughout the entire respiratory tract and causes substantial particle deposition at airway bifurcations.

12. The Minimum Alveolar Concentration (MAC) of anesthetic gasses is the concentration of dissolved gas in the blood and is used as an inverse measure of relative anesthetic potency.

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Matching Questions Match the parameter or description with the change in particle deposition mechanism(s) that is/are most affected compared to normal tidal breathing.

13

Breath holding

A

Increase in inertial impaction

14

Large inhaled particle size

B

Decrease in inertial impaction

15

Lying flat

C

16

Rapid breathing

D

17

Slow breathing

E

Increase in gravimetric sedimentation Decrease in gravimetric sedimentation Increase in diffusion

18

Small inhaled particle size

F

Decrease in diffusion

Multiple-choice Questions 19. A nebulizer would be a preferred device for delivery of aerosol dosage forms based on which of the following patient parameters: a. A female who is very physically active and travels frequently b. A geriatric patient who retains good manual dexterity but limited cognitive ability c. A hospitalized patient on a mechanical ventilator d. A male with impaired lung function and altered breathing parameters 20. A pressurized metered dose inhaler would be a preferred device for delivery of aerosol dosage forms based on which of the following patient parameters: a. A female who is very physically active and travels frequently b. A geriatric patient who retains good manual dexterity but limited cognitive ability c. A hospitalized patient on a mechanical ventilator d. A male with impaired lung function and altered breathing parameters 21. What is the purpose of the valve assembly in a pressurized metered dose inhaler (pMDI)? a. To contain the formulation under high pressure due to the propellant b. To hold the canister in the proper orientation c. To meter the formulation volume into a holding space preparatory for device actuation d. To serve as a space for the propellant to vaporize

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

22. What is the main difference between active dry powder inhaler devices and passive dry powder inhaler devices? a. Active devices utilize an external energy source to aerosolize the powder formulation b. Active devices synchronize actuation with patient inspiration c. Passive devices utilize a vibrating piezoelectric crystal for powder aerosolization d. Passive devices time dose metering with proper orientation 23. Which type of device is used to deliver therapeutic gasses to anesthetized patients? a. Dry Powder Inhaler b. Nebulizer c. Pressurized Metered Dose Inhaler d. Vaporizer 24. Which of the following is called the heart of an aerosol package (pressurized metered dose inhaler) and is responsible for developing the proper pressure in aerosols?

a) b) c) d) e)

25.

Which of the followings in an aerosol package is used for easy opening and closing of the valve? a) b) c) d) e)

26.

Actuator Valve Product concentrate Propellant None of the above

Dip Tube Actuator Propellant Product concentrate None of the above

In the testing of pharmaceutical aerosols, which of the following can be used to study the flammability of an aerosol? a) b) c) d) e)

Pressure gauge Cascade impactor Pycnometer Flash point None of the above

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 11 - Questions Mathematical questions 1.

The permeability of a drug through a polymer membrane is 1.01 x 10-5 cm/sec. Its diffusion coefficient is 4.23 x 10-7 cm2/sec. If the thickness of the membrane used in this study is 0.085 cm, calculate its partition coefficient of the drug.

2.

In a diffusion study through human skin, the lag time of a drug was found to be 50 minutes. If the thickness of the skin is 0.085cm, what is the diffusivity of the drug?

3.

A newly synthesized steroid is allowed to pass through a siloxane membrane, having a cross-sectional area of 10.36 cm2 and a thickness of 0.085 cm, in a diffusion cell at 25 degrees Celsius. From the horizontal intercept of the plot of Q=M/S vs. T, the lag time tL is found to be 47.5 minutes. The original concentration Co is 0.003 millimols/cm3. The amount of steroid passing through the membrane in 4.0 hours is 3.65 x 10-3 m. moles. a) Calculate the parameter, DK and the permeability. b) Using the lag time tL = h2/6D, calculate the diffusion coefficient. c) Calculate the partition coefficient (K).

4. During an in vitro diffusion studies it was found that 3 micrograms of nicotine passed through a 3 cm2 snake skin in one hour. Determine the flux of nicotine through the snake skin.

5. If 60 micrograms of nicotine passed through 3.0 mm2 rabbit skin in 60 minutes at 32°C. How can the flux of nicotine can be expressed?

6. From a diffusion experiment of a new investigational drug through human skin of 3 mm thick, the lag time was found to be 36 min. Determine the diffusion coefficient of the drug is:

Theoretical Questions 1. Creation of transient aqueous pores in the lipid bilayer membranes by application of a short but high voltage pulse is often called: a. b. c. d. e.

Iontophoresis Electroporation Electropermeabilization Both b and c None of the above

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

2. Penetration enhancer can modify: a. Solubility of the drug b. Partition c. Skin structure d. All of the above e. None of the above 3.

The permeability of a drug through skin depends on: I. Diffusion coefficient of the drug a. Skin thickness b. Partition coefficient of the drug a. b. c. d. e.

I only II only III only I and III I, II, and III

4. Which of the following acts as the strongest barrier for skin diffusion? a. b. c. d. e.

5.

Permeability coefficient can have a unit of: a. b. c. d. e.

6.

The dermis Viable epidermis The stratum corneum Sweat glands Hair follicles

cm/sec mm2/h sec/mm2 µg/cm2.hr None of the above The contributing factors affecting the delivery of morphine via transdermal route can include:

a. Molecular weight of insulin b. Isoelectric pH of insulin c. pH of the skin Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

d. skin thickness e. All of the above 7.

Ingredients that soften the skin and make it more flexible when applied on the skin surface is known as: a. coumnterirritant b. keratolytic agent c. astringent d. emmolient e. none of the above

8.

Hydrophilic ointment, USP is an o/w type of ointment base. Which of the following property describes this base well? a. keroatolytic b. greasy c. water washable d. water soluble e. anhydrous

9. Ideal properties of a suppository base exclude: a. melts at body temperature b. should not irritant to the rectal mucosa c. should show polymorphism d. should have no pharmacological effect e. should have no incompatibility with the drug to be administered 10.

Identify the dosage form/delivery system which is not a topical formulation a. medicated shampoo b. Calamine lotion c. salicylic acid ointment d. nicotine patches e. Insulin injection

11. DMSO belongs to which category of the following penetration enhancer a. azone b. sulfoxide c. alkanol d. terpene e. Pyrrolidone

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 12 - Questions Mathematical questions 1. One gram of a hydrocolloid, molecular weight 3000, is dissolved in 100 mL of solution at 25 C. What is the osmotic pressure of the solution?

2. How much shear rate is needed to create a 100 nm droplet oil and water nanoemulsion where the interfacial tension is 10 dyn/cm and viscosity of the continuous phase is 10-2 poise.

3. An in vitro drug release from an investigational new drug was carried out in an osmotic drug delivery system. The area of the semipermeable membrane was 2.5 cm2 with a thickness of 0.03 cm. The permeability coefficient was 2.5 x10-6 cm2/atm.hr. The osmotic pressure differences between the drug core and external environment was 250 atm. Assuming the concentration of the saturated solution Cs at 37oC is 350 mg/cc, determine the zero-order delivery rate of the drug from this device. Assume this is a perfectly semipermeable membrane and no drug diffuse through this membrane.

Theoretical questions 1. Which of the following listed polymers is NOT a bio-degradable one? a. b. c. d. e.

Poly (glycolic acid) Poly (D-lactic acid) Poly (-caprolactone) Silicone rubber PLGA

2. Identify the delivery system which is an osmotic pump/drug delivery system: a. b. c. d. e.

Nitro-Disc Oros delivery Transderm-nitro Esomeprazole (Nexium) Amphotericin B (AmBisome)

3. Which is a true statement for an osmotic drug delivery system?

I. II. III.

Zero-order release can be achieved For oral osmotic release, the drug release is independent of gastric pH Drug release is independent of the diameter of the drilled hole in the device (a) Only I is true

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

(b) Only II is true (c) Only III is true (d) Both I and II are true (e) I, II, and III all are true 4. Which of the following factors can affect the release rate of drugs from an osmotic drug delivery?

I. Osmotic pressure II. Solubility of drug III. Delivery orifice diameter IV. Membrane used (a) I Only (b) II Only (c) III Only (d) IV Only (e) I, II, III and IV all are true 5. A drug needed to have a rapid effect must be injected (a) Intramuscularly (b) Subcutaneously (c) Intrathecally (d) Intravenously (e) Intradermally 6. Water for injection (WFI), USP is prepared by using: (a) Filtration (b) Ion exchange (c) Distillation or reverse osmosis (d) Use of a disinfectant (e) All of the above 7. A small volume parenteral (SVP) has a volume of: (a) 1000mL or more (b) 500 mL or more (c) 250mL or more (d) 100mL or less (e) 125 mL or more

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

8. Electrolytes are added to parenteral formulations to: (a) Improve clarity (b) Prevent water loss (c) Increase conductance (d) Adjust pH and tonicity (e) Sterilize the product 9. Tonicity of a parenteral solution can be tested by: (a) Osmotic pressure (b) Depression of freezing point (c) Elevation of boiling point (d) Exposing them to red blood cells (e) All of the above 10. Which statement is not true for a large volume parenterals (LVP)? (a) packaged in containers labeled as containing more than 100 mL (b) packaged in glass bottles or in large volume flexible containers (c) have to be sterile, pyrogen-free and essentially free of particulate matter (d) Should be isotonic (e) Should have at least one or more antimicrobial agents 11. The term gauge of the needle is a measure of (a) The outside diameter of a needle (b) The inside diameter of a needle (c) The length of the canula (d) Canula wall thickness (e) The Length of the hub 12. Which of the followings can be passively targeted at the leaky vasculature of tumor? (a) Microparticles (5-10 microns in sizes) (b) Nanoparticles (100 nm sizes) (c) Macromolecules (proteins with high molecular weight) (d) Drugs with molecular weight of 5000 g/mole or more (e) Polymeric particles of 50 microns and above sizes 13. Which of the following liposomal structures are used in drug delivery? (a) Unilamellar vesicles (b) Large Unilamellar vesicles (c) Giant Unilamellar vesicles (d) Oligolamellar vesicles (e) Multilamellar vesicles

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

14. Which of the following statements are true for liposomal delivery?

I. Production cost is very low II. Suffer from leakge and fusion of encapsulated drug molecules III. Liposomes are biocompatible, biodegradable and nontoxic since composed of natural lipids (a) I only (b) I and II only (c) II and III only (d) I and III only (e) I, II and III only 15. Which of the following statement is not true for drug delivery systems? a) b) c) d) e)

Colon targeting systems are usually pH controlled Monoclonal antibodies acts by binding to a cancer specific antigen Degradable systems releases drug due to polymer degradation Monolithic systems are not matrix drug delivery systems Reservoir systems drug release is controlled by rate controlling membrane

16. Which of the followings drug delivery system forms spherical vesicles of phospholipids bilayers? a) b) c) d) e)

Liposomes Solid dispersions Self emulsifying drug delivery systems Hydrogels Nanoparticles

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 13 - Questions Mathematical questions

1. If the partition coefficient of a drug through a membrane is 3.0, the membrane thickness is 0.09 cm and the diffusion coefficient of the drug in the same membrane is 4.5 x 10-5 cm2/sec. Determine the permeability of the drug in this membrane.

2. If 20 mg drug passes through a polymeric membrane of 10 mm2 surface area in 20 minutes, determine the flux of the drug through this membrane. The thickness of the above membrane is 5 mm.

3. In a diffusion experiment tlag (tL) for a drug was found to be 10 minutes for a membrane of 5 mm thick. Determine the diffusion coefficient of the drug in this membrane.

Theoretical questions 1.

Which of the following physicochemical properties are the most important factors for a drug to be transported through biological membranes by facilitated diffusion? a.

Poor aqueous solubility

b.

Sharp melting point for the crystalline drug compound

c. d. e.

Small and compact molecular size Strong and localized molecular ionization Structural mimic of an endogenous biological compound

2. Which mechanism of drug transport across biological membranes has a rate of drug movement that is energy dependent?

a. Active Transport b. Passive Diffusion c. Facilitated Diffusion d. Paracellular Transport Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

e. Phagocytosis 3. Which of the following listed drugs is an example of a drug affecting a primary active transport? a. Ibuprofen b. Aspirin c. Omeprazole d. Acetaminophen e. None of the above 4. Which of the following transport process helps the live attenuated oral polio vaccine (OPV) a. Active transport b. Passive diffusion c. M-cell vesicular transport d. Carrier mediated transport e. None of the above 5. Which is the following is true for P-glycoprotein (Pgp) i.

Pgp is a well characterized protein widely distributed and expressed throughout the body ii.

It does not inhibit actively net drug permeation across biological membranes iii.

Pgp can act an efflux pump A. i. only B. ii only C. III only D. I and II E. I and III only 6. True or False: The process of active drug transport across biological membranes will always be saturable if drug concentrations are raised high enough.

7. True or False: If a drug passes through biological membranes through passive diffusion, the only factor governing the rate of drug movement is the concentration gradient across that membrane.

8. True or False: Passive drug diffusion through membranes only occurs in a unidirectional manner from the side of high drug concentration to the side of low drug concentration.

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

9. True or False: All substances are able to diffuse across biological membranes.

10. True or False: Concentration gradient is the driving force for diffusion via biological membranes.

11. True or False: Thickness of the membrane is the resistive force for diffusion via biological membranes.

12. True or False: Lipid composition is not an important factor in the properties of biological membranes.

13. Which mechanism of drug transport across biological membranes can be a carrier mediated process, saturable, and structurally selective for drug?

A. Facilitated Diffusion B. Passive Diffusion C. Transcellular Diffusion D. Paracellular Transport E. Phagocytosis 14. Which of the following dosage regimens would maximize the amount of calcium absorbed for biological action in a patient? Calcium is absorbed from the gastrointestinal tract through active transport mechanisms. Assume the rate of calcium transport across gastrointestinal membranes is typically saturated with a single dose of 350mg. a) 250 mg PO Q3H b) 500 mg PO Q6H c) 1000 mg PO Q12H d) 2000 mg PO Q24H e) 4000 mg PO Q24H 15. Which of the following properties has the greatest influence for drug movement across biological membranes by passive diffusion?

A. Large concentration gradient across a membrane B. Large molecular weight C. Poor membrane permeability D. Strong molecular polarity E. Structural mimic of an endogenous biological compound

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 14 ‐ Questions Mathematical questions 1. The total surface area of a drug undergoing dissolution was 5.0 cm2. The diffusion coefficient if this drug in the release medium is 9.0 x 10‐6 cm2sec‐1. The diffusion layer thickness was 5.0 x10‐3 cm when it was stirred at 50 rpm in the dissolution medium. The solubility of the drug in the dissolution medium was 0.25 mg/mL. Calculate the dissolution of the drug assuming sink condition (Concentration of the drug in the release medium is less than 15% of its solubility).

2. A solid drug with an initial weight of 1 gram was subjected to dissolution study in 1000mL of a dissolution medium. After 2 hours of dissolution studies, the weight of dissolved material was found to be 0.51 gram. Using Hixson‐Crowell law determine the cube root dissolution rate constant for this drug.

3. A compressed tablet contains 81 mg of an active drug and disintegrate in 10 minutes in water. 60% of the granules dissolved in the release medium during a dissolution study in 20 minutes. Determine the cube root dissolution rate constant for this drug.

Theoretical Questions 1. Which of the following metabolism reactions does not belong to Phase II metabolism a. Glucuronidation b. Sulfation c. Oxidation d. Methylation e. Glutathione conjugation 2. Absorption of most orally administered compounds occurs in: a. Rectum b. Mouth c. Small intestine d. Stomach e. Colon 3. True or False: The uneven presences of transporters in in various segment of the GI tract also contribute to the different absorption rate in different GI segments.

4. True or False: Many drugs with low aqueous solubility and either high membrane permeability or extensive metabolism have increased absorption with food intake referred to as “negative food effect” 5. True or False: Ketoconazole, an antifungal agent, is a known CYP inhibitor that will inhibit the metabolism of many co‐administered medications.

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

6. Oral bioavailability of poorly soluble drug can be improved by: i. reducing particle size ii. forming a salt or co‐crystals with higher solubility iii. developing amorphous or lipid formulations a. I. only b. II only c. III only d. I and II only e. I, II and III only 7. Identify the physiological factor that affect dissolution of a solid drug a. Particle size b. Salt form of the drug c. Disintegrant in the formulation d. GI motility e. Polymorphism 8. The effect of food on drug absorption is generally influenced by I. Drug solubility II. Membrane permeability III. Metabolism a.

I only b.

II only c.

III only d.

I and II only e.

I,II and III 9. Co‐administration of which of the following liquid will not affect the absorption of Allegra and its bioavailability a. Water b. Grapefruit juice c. Orange juice d. Grapefruit and orange juice combination e. None of the above

10. True or False: The drug absorption is a homogeneous and simple process.

11. True or False: There is no absorption process for drugs that are administered directly into systemic circulation.

12. True or False: First‐pass metabolism can affect oral absorption of drugs.

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 15 - Questions Theoretical Questions 1. True or False: Different routes of drug administration results in varied rates and extents of drug absorption and distribution.

2. The choice of route of administration depends on: I. Drug and formulation in which the drug is present II. Patient factors III. FDA decision and mandate a. I only b. II only c. III only d. I and II only e. I, II and III 3. Identify the administration route that uses both ears as the administration route a. Ophthalmic b. Rectal c. Intravenous d. Vaginal e. Auricular 4. The rate and extent of drug absorption depends on: i.

Drug properties ii.

Formulation iii.

Anatomical, physiological and pathological characteristics a. I only b. II only c. III only d. I and II only e. I, II and III 5. Identify the route of administration which is not considered as a parenteral route a. Intravenous b. Subcutaneous c. Rectal d. Intradermal e. Intramuscular

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

6. Identify the route which has the greatest bioavailability a. Intravenous b. Subcutaneous c. Rectal d. Oral e. Ophthalmic 7. Parenteral preparation should be I. Expensive II. Sterile and non-immunogenic III. Pyrogen free a. I inly b. II only c. III only d. II and III only e. I, II, and III 8. Identify the route which guarantees complete bioavailability a. Intramuscullar b. Intravenous c. Intra dermal d. Intraperitoneal e. subcutaneous 9. Identify the fact that is not related to IV route of administration a. used when rapid drug effect is desired b. when drug has a limited and unpredictable absorption c. when oral bioavailability high and oral route is preferred d. when patient cannot receive via other route e. trained individual needed for administration 10. True or False: The rate of drug absorption after IM administration is influenced by the formulation properties and the perfusion rate at the site of injection.

11. The most important advantage of IM administration as compared to IV injections is: a. large volume can be injected b. the bioavailability is better in the case of IM c. the wide variety of formulation that can be administered to the muscle d. no trained individual needed for administration e. sterility is not an issue in the case of IM 12. True or False: IM route can be used for sustained release of some drugs.

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

13. True or False: In formulation, the word “topical” means the same as “transdermal” 14. True or False: Buffering of an ophthalmic formulation is not an important formulation factor used to optimize ocular drug absorption.

15. True or False: Corneal penetration of drugs from ophthalmic solution can be affected by binding of drugs to proteins like albumin, globulin and lysozyme in the tears.

16. Which is not true for an ophthalmic formulation? a. be sterile b. be hypertonic c. non-immunogenic d. be pyrogen free e. have no allergenic response 17. Function of tears are as follows EXCEPT a. bath the corneal surface b. make the applied ophthalmic product pyrogen free c. provide nutrition for the cornea d. to protect against bacterial infection e. clear cell debris and foreign substances 18. Which preservative with an appropriate concentration is used as a preservative in ophthalmic solutions? a. methylparaben 1% b. propyl paraben 1% c. both methyl and propyl paraben at a concentration of 1% each d. Benzalkonium chloride at a concentration of 0.01% e. Benzalkonium chloride at a concentration of 1% 19. True or False: The ear is a highly perfused organ and is used for systemic drug absorption following topical instillation of otic drug products.

20. Identify the false statement a. auricular drug administration is unlikely to encounter mucous membrane b. Otic solution need not be pyrogen free c. Otic solution need not be sterile d. tonicity is not an issue for otic solutions e. Otic solution can be used in the eye 21. The average pH of the nasal cavity ranges from: a. 6.2-6.4 b. 1.0-2.0 c. 7-4-7-8 Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

d. 8-8.4 e. none of the above 22. True or False: Nasal drug administration can be utilized for systemic drug delivery as well as local drug effects.

23. Which of the following routes of administration will not be able to avoid first-pass metabolism? a.) b.) c.) d.) e.)

Intramuscular injection Intravenous injection Nasal aerosol Oral tablet None of the above

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 16 - Questions Mathematical Questions 1

Determine the appropriate total daily dose of the extended release tablet formulation that will produce an equivalent physiologic response to the conventional tablet formulation described below.

Conventional Tablet (CT)

Extended Release Tablet (ERT)

Salt Factor

90%

87%

Bioavail ability

78%

62%

Total Daily Dose

325 mg

?

Refer to the following information for questions 2-3 A drug company has formulated a generic version of a brand name antibiotic suspension. As part of the generic drug approval process, a bioavailability study was conducted in order to compare different formulations. ࢓ࢍൈࢎ࢘

Formulation

Dose ሺ࢓ࢍሻ

AUC ቀ

IV Solution (Brand)

100

6,743.9

Oral Tablet (Brand)

350

10,445.2

Oral Suspension (Brand)

500

12,818.6

Oral Suspension (Generic)

450

10,972.7

ࡸ

ቁ

2.

What is the relative bioavailability of the generic drug suspension?

3.

What is the absolute bioavailability of the generic drug suspension?

4.

What is the 24-hour AUC for the following drug product? Note: following a single intravenous dose, tabulated concentration and time values were obtained.

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Time (hr) 0 6 12 18 24

Concentration (µg/mL) 359.2 84.3 19.8 4.6 1.1

Theoretical Questions 1.

Which of the following statements best describes the area under the curve for a medication? a.) It is a measure of total exposure to the drug b.) It is a parameter with units of mg/L c.) It is equivalent to the bioavailability of a drug d.) It is the maximum observed drug concentration e.) It is the time at which the maximal drug concentration is observed

2.

Which oral formulation would likely have the most delayed tmax value? a. A quick dissolving tablet with a high amount of disintegrant b. A sugar coated tablet c. A tablet that uses a water-soluble lubricant d. An effervescent tablet e. An enteric coated tablet

3.

Which of the following factors is the most likely to decrease the gastric emptying rate? a) Eating a large meal b) Light exercise c) Lying on the right side d) Medications that induce gastric spasticity e) Standing

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

4. A study was conducted comparing different oral formulations of a drug. The resulting concentration versus time profile was included for comparison of the formulations. Identify the statement that is more appropriate to describe the resulting concentration versus time profile.

a) Formulation A contains a polymorphic form with the lowest observed aqueous solubility b) Formulation A contains the smallest average drug particle size c) Formulation B contains the highest amount of disintegrant in the formulation d) Formulation C contains a salt form with the highest aqueous solubility e) Formulation C contains the lowest amount of lipophilic lubricant 5. In the determination of bioequivalence studies, the FDA allows 80-120% tolerances around which key pivotal pharmacokinetic parameters: a. b. c. d. e.

Bioavailability and total drug exposure Time to reach maximal concentrations and bioavailability Time to reach maximal concentrations and maximum drug concentration Total drug exposure and the maximum drug concentration Total drug exposure and the bioavailability

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

6.

Plasma concentration of a same dose of a drug is administered by different routes as indicated below. Identify the route which will produce the highest initial plasma concentration a.) b.) c.) d.) e.)

Oral Intravenous injection IM injection Rectal suppository Transdermal

7. The absolute bioavailability of an oral medication is calculated such that the denominator of the equation uses data from:

a) The brand name drug product because it is assumed to be completely bioavailable b) The brand name drug product because it is the established reference product c) The intravenous form of the drug because it is assumed to be completely bioavailable d) The intravenous form of the drug because it is the established reference product e) None of the above 8.

A patient is successfully managing hypertension with the use of oral verapamil.

While reviewing a new prescription for oral levofloxacin for the treatment of a lung infection, the pharmacist identifies that levofloxacin is a substrate of Pglycoprotein while verapamil is a known inhibitor of P-glycoprotein. Which of the following drug-drug interactions and effects is the most likely consequence if no change is made to the prescribed therapy? (NOTE: hypertension is elevated blood pressure and levofloxacin is a fluoroquinolone antibiotic. Also assume that drug adverse events are directly related to the systemic drug concentration.)

a.) Less levofloxacin will be absorbed which will then cause decreased antibacterial effects and decreased adverse events b.) Less verapamil will be absorbed which will then cause an elevation in blood pressure and decreased adverse events c.) More levofloxacin will be absorbed which will then cause increased antibacterial effects and increased adverse events Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

d.) More verapamil will be absorbed which will then cause a lowering of blood pressure and increased adverse events e.) Noting will be affected by co-administration of oral levofloxacin 9. According to the BCS classification, a drug with high solubility and high permeability is classified as: a) BCS Class I b) BCS class II c) BCS class III d) BCS Class IV e) None of the above 10. True or False: Generic drug products filling an abbreviated new drug application can utilize BCS classification in support of requests for waiver of BE studies against the then marketed innovator or brand drug product.

11. True or False: Dosage form design factors do not affect the rate and extent of drug release and bioavailability.

12. Food intake can affect drug absorption by many factors that may include: i. Interacting with dosage form ii. Affecting GI Physiology iii. Influencing gastric pH a. Only i is correct b. Only ii is correct c. Only iii is correct d. All factors i, ii, and iii e. None of the factors i, ii, and iii.

13. True or False: Drug-excipient complexes that do not readily dissociate at the site of absorption can lead to altered or reduced bioavailability

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

14. In a Bioequivalence study design which of the following elements is generally discouraged (a) Crossover design (b) Parallel group design (c) Subject is randomly selected (d) Washout period is allowed for complete elimination of the drug (e) Subjects are double blinded 15. A correlation describing a relationship between rate and extent of drug release in vitro with rate and extent of drug absorption is termed as:

(a) Therapeutic equivalent (b) Therapeutic index (c) Pharmaceutical alternative (d) IVIVC (e) Pharmaceutical equivalent

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

15-d

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 1 - Answers Numerical Questions:

1. d 2. b 3. b 4. a 5. b 6. b 7. b 8. c 9. d 10. a 11. b 12. b 13. d 14. d 15. d 16. c 17. b 18. c 19. d 20. c 21. c 22. c 23. d 24. b 25. a 26. c 27. d 28. b 29. d 30. f 31. c Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Theoretical questions:

1. a 2. c 3. b 4. d

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Answers – Chapter 2 Numerical Questions: 1.

2.

3.

4.

5.

c d c a Go = -4.36 kJ

Use the equation: Go =

Ho – T So

H° = 28.05 kJ So = 108.7 J/K = 0.1087 kJ/K T = 273.17 + 25 = 298.17 K The dissolution of NH4NO3 in water is spontaneous because the value of Go is negative.

Theoretical questions:

1. a 2. b 3. a 4. b 5. b 6. d 7. a 8. d 9. b 10. b 11. b 12. b 13. c 14. a 15. a Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

16. a 17. a 18. d 19. a 20. a 21. d

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Answers – Chapter 3 Numerical Questions: 1. A

Use the equation, Surface tension,

Where:  = surface tension, d = inner diameter of the capillary tube = 0.1 cm, h = height to which the liquid rises in the capillary tube = 1.63 cm,  = density of the liquid = 1.1120 g/cm3 and, g = acceleration due to gravity (981 cm/sec2).

2. C

The moles of sucrose = 1.0 g/342 g/mole= 0.0029 moles 100 mL = 0.1 L Therefore,

= 0.0029/0.1 = 0.029 mole/L

Osmotic pressure, p =

=

x 0.0821

x 298.16 K = 0.71 atm.

3. d Solution: 20 mL of a solution containing 0.25 g of apomorphine hydrochloride = 1.25% apomorphine hydrochloride In this problem, first the freezing point depression by 1.25% apomorphine hydrochloride should be calculated Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

The freezing point depression by 1.25% apomorphine hydrochloride = 1,25% x 0.08 degree/% = 0.1 degree Therefore, the amount of NaCl is required to decrease the freezing point by (0.52-0.1 = 0.420) 0.420 which can be calculated as shown below: The amount of NaCl needed to decrease the freezing point of 20 mL solution by 0.52 degree =

Therefore, # of g of NaCl required to lower the freexing point of 20 mL solution by 0.42 degree =

4. a Solution: On the basis of given E value in the question: 0.18 g of NaCl = 1 g of anhydrous dextrose Hence, 0.9 g of NaCl = Therefore, 5 g of dextrose in 100 mL solution i.e. 5% would be isotonic.

5. b Solution: Step 1: 0.25 g of Procaine HCl = Sodium chloride equivalent, E x 0.25 g = 0.21 x 0.25 g = 0.0525 g NaCl Step 2: The

amount

of

NaCl

needed

to

make

30

mL

solution

isotonic

The amount of NaCl needed to make 30 mL solution containing 0.25 g of procaine HCl isotonic = Step 2- Step 1 = 0.27 g – 0.0525 g = 0.2175 g NaCl = 0.218 g NaCl 6. a Solution: On the basis of v value, the following statement is true: 7.7 mL solution containing 0.3 g of calcium lactate would be isotonic

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

=

Hence, 100 mL solution containing

7. b 8. a 9. d

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Theoretical questions:

1. a 2. a 3. c 4. b 5. a 6. b 7. b 8. b 9. d 10. c 11. d 12. b 13. a 14. a 15. a 16. a

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 4 - Answers Numerical Questions: 1. b According to H-H equation, for a buffer consisted of a weak acid and its salt: which can be re-arranged for ratio of salt to acid

=

Therefore, the ratio of salt to acid = 1.74:1

2. d Solution: Use the following equation:

pH = 5.8 pkw = 14 pKb = pkw – pka pka = 4.8 On substituting the above values, % ionization = 9.09% Hence, % of unionized form = 100 -9.09 = 10.91% 3. d Solution:

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

4. b Solution:

If the total amount of compound A is 4 g, 3 g could be in hexane.

Hence, when the total amount of compound A is 5 g,

could be in

hexane.

5. A Solution:

Minimum blood or saline flow rate needed to prevent precipitation of the administered drug =

Therefore, the rate greater than 8.33 mL/min would be needed to prevent precipitation.

Theoretical questions:

1. d 2. c 3. b 4. a 5. a

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 5 - Answers Numerical Questions: 1. b The 1st order reaction can be expressed by the following equation: which can be re-arranged for time as shown below:

Where, C0 = initial concentration, Ct = concentration at any time which is equal to 0.95 C0 because there is 5% degradation = 1st order rate constant

Using Ct = 0.95 C0 in the above equation,

2. c 3. a Solution: The following equation represents 1st order kinetics: which can be re-arranged as shown below:

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Use

= 0.02 M

Use any from the following table: Time (Hr) (M)

2

5

9

14

18

0.1806

0.1542

0.1262

0.0962

0.0778

Substittuting these values in the equation, the rate constant for different times (it is good to discard the beginning first time) can be calculated which mean = 0.052 hr.

4. c Solution:

Use

Where

= 0.052 h-1

5. d Solution: First, calculate the rate constant using the following equation:

Use,

= 12.0 x 10-3 M,

The calculated value of

= 9.2 x 10-3 M, and t = 24 months would be equal to 0.011 h-1

Now using the following equation calculate the time, t:

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Using

= 0.7

and

= 0.011 h-1, the calculated value of t = 32.4 months

Theoretical questions:

1. d 2. d 3. a 4. c 5. a 6. b 7. a 8. b 9. a 10. b 11. d 12. a 13. b 14. d 15. a 16. c 17. b 18. a 19. a 20. a 21. b 22. a 23. b 24. b 25. a

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Answers Numerical: 64,000 ⋯

1. Use the equation

⋯

 

where mole fraction of each component

4

10,000

can be used instead of its number of molecule.

6

100,000 6

2. The equation Can be written as log  log

4

64,000

 log

Therefore, a plot of log  and log M would be a straight line where intercept = log K and constant “a” = slope.

The linear regression analysis of log  and logM gives the following equation: log  = 0.1749M -0.6633 Therefore a = 0.175 and K = antilog (-0.6633) = 0.217

3. [η] = k Ma Viscosity = 0.34 dl/g k = 1.27 x 10-3 g/dl M = 3.24 x 103 0.34 = 1.27 x 10-3 g/dl (3.24 x 103 )a Ln (0.34) = Ln(1.27 x 10-3) + a Ln (3.24 x 103) -1.0788 = -6.6687 + a (8.08) a = (-1.0788+6.6687)/8.08 = 0.69 1

Theoretical 1. d 2. b 3. a 4. a 5. d 6. b 7. a 8. b 9. b 10. a 11. a 12. c 13. d 14. c 15. c 16. a 17. b

2

Answers – Chapter 7 Mathematical Questions 1(a) Partition coefficient calculation. = .

= 11.25

.

(b) The drug is more lipophilic since its partition to lipophilic solvent octanol is 11.25 as compared to water (1).

2.

Angle of repose of the powder is 38.7ºC 3.

=

Bulk density = Tap density =

=

= 1.2 g/cc

= 1.29 g/cc

Q4.

18 V=

.

Theoretical Questions 2.d 3.b 4.d 5.e 6.e 7.e 8.c 9.a 10.b 11.a 12.a 13.e 14.b 15.b 16.a 17.c 18.c 19. a-II, b-I, c-IV, d-V, e-III Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

.

=

.

= 0.00029 cm/sec

Chapter 8 - Answers Mathematical Questions 1.

dM 760 mg = = 12.67 mg/ sec dt 60 sec

dM DSC s = (assuming sink condition) = h dt

D = k = dissolutio n rate constant h

 12.67

mg mg = k x 0.28 x 104 cm2 x 15 3 sec cm

 k = 3.02 x 10-4 cm/ sec 2 (a). The dissolution rate can be given by Noyes Whitney equation as shown below:

1.75 x 10

= 2.5x10 0.35 1.25 10 1.22

2.1 10

/

(b) Since the surface area is directly proportional to the dissolution rate a tenfold increase in surface area will increase the dissolution rate ten times. So the new dissolution rate is: 1.22 10

12.2

/

(c) In order to find out the sink condition one has to determine the concentration of the drug in the release medium and its relation to the saturated solubility. If it is below 15% of the solubility then the dissolution is carried out under sink condition.

Therefore, (2.1 x 10-4mg/mL)/(0.35 mg/mL) x 100 = 0.6% Since this concentration is very low, less than even 1% of solubility, the dissolution was carried out under sink condition.

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Theoretical Questions

1. c 2. c 3. c 4. b 5. d 6. a 7. a 8. c 9. d 10. b 11. e 12. a 13. e 14. d 15. b 16. b 17. d 18. a 19. c

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Answers – Chapter 9 Mathematical questions 1. v



2.

d 2 (  s  o ) g 18

(5 x10 4 ) 2 x(0.90  1.05) x981 18 x0.5 v = -4.1x 10-6 cm/sec 24 hour = 86, 400 seconds -v = 0.35 cm/day

HLB values are additive.

Let A has a HLB of 8 and B has a HLB of 12.0 Optimum HLB value required = 9.0 %A required 

%A



100(OptimumHLB  HLBB ) ( HLB A  HLBB )

100(9  12)  300   75% 4 8  12

%B required  100% - 75% = 25% 25% of 20 mL = 5 mL Therefore, the blend should contain 5 mL of B and 15 mL of surfactant A. 3.

Optimum HLB value =12 Total amount of surfactants that can be used = 5% (v/v) Total volume of emulsion = 100 mL Therefore, volume of surfactant to be used = 5% (v/v) x 100mL = 5 mL Span 80, HLB = 4.3 Tween 20, HLB =16. 7 x = optimum HLB = 12

Let it be A Let it be B



100( x  HLB B ) 100(12  16.7)  ( HLB A  HLBB ) (4.3  16.7)



100(4.7)  38%  12.4

%A

38% of 5 mL = 1.9 mL = 2 mL Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Volume of B = 5-2 = 3 mL Therefore, the blend should contain 2 mL of Span 80 and 3 mL of Tween 20.

4.

Original volume in (V0) mL Ultimate volume of (Vu) the sediment Sedimentation Vu F = volume (F) V0

Suspension 1 100

Suspension 2 100

Suspension 3 100

50

100

150

0.5

1

1.5

Theoretical Questions

1. b 2. b 3. e 4. b 5. a 6. c 7. c 8. a 9. a 10. e 11. d 12. b 13. a 14. b 15. d 16. c 17. d 18. c 19. e 20. e 21. d 22. c 23. b

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 10 - Answers 1. B 2. C 3. A 4. D 5. E 6a.) The device and equipment needed for drug administration AccuNeb-any nebulizer could work, but a specific air-jet nebulizer and compressor are recommended.

Ventolin HFA-pMDI EasyHaler Salbutamol-passive DPI device a. The breathing requirements necessary for optimal drug deposition in the lungs AccuNeb-slow regular tidal breathing Ventolin HFA-slow, steady, deep inspiration EasyHaler Salbutamol-rapid, deep inspiration b. The mental cognition and physical dexterity needed to properly selfadminister the drug AccuNeb- can be administered using a face mask to any type of patient Ventolin HFA-patient must have high cognition and coordination to time breathing with actuation and regulate inspiration in time with actuation.

EasyHaler Salbutamol-patient must have high cognition and coordination to prime the dose, keep the device oriented properly, and inspire accurately. c. The excipients and their function in the formulation These formulations are very simple. There are only excipients to control pH and tonicity for the AccuNeb, a propellant without any other excipient for the Ventolin HFA, and only lactose as a carrier particle for the EasyHaler. None of the formulations have flavors or other functional excipients.

7. The Easyhaler Salbutamol® DPI device. It requires a deep, rapid inspiration that is normally impaired in patients suffering an acute asthma attack.

8. The discussion could include the requirements for biocompatible and nonimmunogenic excipients in the lung. The excipients used are to promote Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

biocompatibility (nebulized solution), aerosolize the dose (pMDI), and carry the very small dose (DPI) in an inspiration.

9. F 10. T 11. F 12. F 13. B,C,E 14. A,C,F 15. C 16. A,D,F 17. B,C,E 18. B,D,F 19. C 20. A 21. C 22. A 23. D 24. D 25. B 26. D.

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 11 - Answers Mathematical Questions 1 Permeability = Where,

DK h

D = diffusion coefficient K = partition coefficient h = thickness

P = 1.01 x 10-5 cm/sec D = 4.23 x 10-7 cm2/sec h = 0.085 K= ?

K =

Pxh 1.01 x 10 -5 x 0.085 (cm/ sec x cm) = D 4.23 x 10 -7 ( cm2 / sec )

K = 2.03 2 2

t lag =

h 6D

t lag = lag time = 50 minutes h = thickness of the skin = 0.085 cm D = Diffusivit y 2

2

(0.085 ) h = D = = 0.000024 Cm /min 6 x t lag 6 x 50 2

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

3.

DK h

P=

P = Permeability (cm/sec) D = Diffusion coefficient (cm2/sec) K = Partition coefficient h = thickness of membrane (cm) At steady state M = P.S.Cd(t - t L ) =

DK S.Cd(t - t L ) h

M = amount material crossed the membrane S = cross sectional area of the membrane Cd = concentration of drug in the donor side 

M = Q S 2

h 6D

 t lag = a)

Calculate the parameter DK and permeability

Q=

mmole 3.65 x 10 -3 mmoles M = 0.35 x 10 -3 = 2 2 10.36 cm S cm

= D.K. (

0.003 mmole/ cm3 47.5 ) [ 4.0 hr - ( )h] 0.085 cm 60 2

DK = 0.0031 b)

2

cm cm = 8.6 x 10-7 sec hr

Using the lagtime (tL), calculate the diffusion coefficient.

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

2

2

(0.085 ) cm h D= = 6 tL 6.475 min

2

2

= 25.4 x 10-6

cm min 2

cm sec

Or

D = 4.23 x 10-7

c)

Calculate the partition coefficient of the drug.

P=

DK h K

K =

=

Ph D

(1.0 x 10 -5 cm/ sec )(0.085 cm) 4.23 x 10 -7 cm2 / sec

K = 2.01

4.

3µ 3

1

Flux of nicotine is 1 µg/cm2.hr 5.

3

60 µ 60

Flux of nicotine is 0.33 µg/mm2. Min

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

6.

2

t lag =

h 6D

t lag = lag time = 36minutes h = thickness of the skin = 3mm D = Diffusivit y

= 0.042 mm2/min

Theoretical Questions 1. b 2. d 3. e 4. c 5. a 6. e 7. d 8. c 9. c 10. e 11. b

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Answers to Chapter 12 Mathematical questions 1.

Moles of the colloids = weight/mol wt = 1.0g/3000g/mole = 0.000333 moles V = volume = 100/1000 = 0.1 L Van't Hoff Equation:  = iCRT i = 1 for nonelectrolyte Temperature = 25◦C = 25 + 273 = 298◦K  x 0.1 = 0.000333 x 0.082 x 298  = 0.0814 atm 2.

a ~ ()/ (c’) a = 100 nm () = 10 dynes/cm c10-2 poise = dyne.sec/cm2

3. dm/dt = (A/h) Lp C A = 2.5 cm2 h = 0.03 cm Lp 2.5 x10-6 cm2/atm.hr C = 350 mg/cc 2.5 2 0.03

2.5 x10

= 18.23 mg/hr Theoretical questions 1. d 2. b 3. d 4. e 5. d 6. c 7. d 8. d Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

x 250

350

9. e 10. e 11. a 12. b 13. e 14. c 15. d 16. a

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 13 - Answers Mathematical Questions 1 Permeability P = Where, K = Partition coefficient = 3.0 D = Diffusion coefficient = 4.5 x 10-5 cm2/sec h = Thickness of the membrane = 0.09 cm P= P=

.

. .

. .

=

0.0015

/

2 Flux =

=

3.

Where: tlag = Lag time h = Thickness of the membrane D = Diffusion coefficient of the drug 10 = D=

0.42 mm2/min

Theoretical Questions 1. e 2. a 3. c 4. c 5. e 6. True 7. False 8. False 9. False 10. True 11. True 12. True 13. a Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

0.1

14. a 15. a

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 14 ‐ Answers Mathematical questions 1.

Under sink condition,

Diffusion coefficient = D = 9.0 x 10‐6 cm2sec‐1 Solubility of the drug = S = 0.25 mg/mL Thickness of the diffusion boundary layer = h = 5.0 x10‐3 cm C = concentration of the drug in the release medium at ay time dm/dt = Dissolution rate Surface area = A = 5.0 cm2 .

.

.

.

= 0.000225 mg/sec

2. /

/

m0 = 1 gram m = (1‐ 0.51 gram) = 0.49 gram t = 2hours = 2x60 = 120 min 11/3 – (0.49)1/3 = K x 2 K = 11/3 – (0.49)1/3 / 120 = (1‐0.799)/120 = 0.0017 (g)1/3 x min‐1

3. Compressed Tablet

Disintegration (granules)

m0 = 81 mg Forty percent of granules remained m = 0.4 x 81 = 32.4 mg remained Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Dissolution (in solution)

t = 20‐10. = 10 minutes (Assuming no dissolution during disintegration and granules are formed after complete disintegration) /

/

(81)1/3 – (32.4)1/3 = K x 10 4.327‐3.188 = K x 10 K = 1.139/10 = 0.1139 (mg)1/3 min‐1

Theoretical questions 1. c 2. c 3. True 4. False 5. True 6. e 7. d 8. e 9. a 10. False 11. True 12. True

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 15 - Answers 1. True 2. 9 3. e 4. e 5. c 6. a 7. d 8. b 9. c 10. True 11. c 12. True 13. False 14. False 15. True 16. b 17. b 18. d 19. False 20. e 21. a 22. True 23. d

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

Chapter 16 - Answers Mathematical Questions 1.

.

. .

. .

.

= 422.97

423 mg

2.

10972.7 450 12818.6 500

,

24.38 25.64

0.951 ≡ 95.1%

24.38 67.439

0.3615 ≡ 36.2%

GS = Generic Oral Suspension BS = Brand Oral Suspension 3.

10972.7 450 6743.9 100

,

4.

Time (hr) 0 6

Concentration (ug/mL) 359.2 84.3

12

19.8

18

4.6

24

1.1

∆ AUC

(359.2+84.3)/2 * (6) = 1330.5 (84.3+19.8)/2 * 6 = 312.3 (19.8+4.6)/2 * 6 = 73.2 (4.6+1.1)/2 * 6 =17.1

AUC = 1733.1 µg*hr/mL Theoretical Questions 1. a Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.

AUC (ug.hr/mL)

1330.5 1642.8 1716 1733.1

2. e 3. a 4. b 5. d 6. b 7. c 8. c 9. a 10. True 11. False 12. d 13. True 14. b

Alekha K. Dash, Somnath Singh, Justin Tolman: Pharmaceutics © 2014 Elsevier Inc.