NICOTINE-POLACRILEX-LOZENGES-Taj-Pharmaceuticals by TAJ API

NICOTINE POLACRILEX LOZENGES Author: Madhura Joshi M.S.(Pharm)

Taj Pharmaceuticals Ltd India | Taj Pharma | Taj Pharmaceuticals Mumbai, Company Overview of Taj Pharmaceuticals Limited |Taj Pharmaceuticals Limited Taj Pharmaceutical an Industrial conglomerate, having diversified interest in Pharmaceuticals and healthcare, Chemicals, API and Agro commodities mainly offers unique opportunities for all its associates to grow in capacity as one of a significant part in curing lives worldwide and building a disease-free nation. Taj Pharma is having more than 600+ brands in different divisions and multiple subsidiaries to meet up most of the requirements of buyers in our industry along with a very efficient staff management capacity.

TABLE OF CONTENTS • • • • • • • • • •

About Taj Pharma About Nicotine Polacrilex About API: Nicotine Composition of Nicotine Polacrilex Lozenges Available Nicotine formulations in market Indication Method of Administration Pharmacokinetics of Nicotine Polacrilex Lozenges Conclusion Future prospects

ABOUT TAJ PHARMA • Taj Pharmaceuticals Limited manufactures and distributes medicines.

• The company’s products include prescription solutions, lifesaving drugs, anti-cancer drugs, veterinary products, consumer brands, and CNS drugs. • It focuses on medicines of anemia, anxiety disorders, cancer/oncology, ear infections, heart failure, hepatitis, HIV/AIDS, influenza, non-Hodgkin’s lymphoma, obesity, osteoporosis, Parkinson’s disease, pneumonia, transplantation, and common diseases. • Taj Pharmaceuticals Limited was founded in 2004 and is headquartered in Mumbai, India

ABOUT NICOTINE POLACRILEX • Nicotine Polacrilex is the nicotine bound to an ion-exchange resin (polymethacrilic acid such as Amberlite IRP64 known as Polacrilex). • Polacrilex polymer in lozenges, helps release the nicotine in a sustained manner so that maximum amount of nicotine is released and absorbed in buccal mucosa. • To mask the taste, generally flavors are added, for example; mint flavored Nicotine Polacrilex lozenges.

ABOUT NICOTINE • Plant derived Alkaloid • Cholinergic drug • Addictive CNS stimulant, causing ganglionic stimulation in low doses and ganglionic blockage in high doses.

Ref: https://pubchem.ncbi.nlm.nih.gov/compound/Nicotine

ABOUT NICOTINE REPLACEMENT THERAPY (NRT) • Over 35 million cigarette addicts try to quit smoking each year, but only 7% of them could reach till their 1 year anniversary of smoking cessation. • According to survey, 70% of cigarette smokers are willing to quit smoking.

• To help them achieve this, Nicotine Replacement Therapy (NRT) has made available OTC in different dosage forms such as chewable gums, lozenges, transdermal patches etc. • Pharmacists can help these patients in choosing the right medication and its method of administration. Ref: https://www.pharmacytimes.com/publications/issue/2010/august2010/otcfocussmokingcessation-0810

COMPOSITION Active ingredient in each lozenge: â&#x20AC;˘ Nicotine Polacrilex 4 mg (If smoking of first cigarette is within 30 minutes of waking up) â&#x20AC;˘ Nicotine Polacrilex 2 mg (if smoking of first cigarette is after 30 minutes of waking up)

Image Ref: https://images-na.ssl-images-amazon.com/images/I/71TZDPvFC6L._SL1000_.jpg Ref: https://www.webmd.com/drugs/2/drug-75256-77/nicotine-polacrilex-buccal/nicotine-gum-buccal/details

FINISHED PRODUCT MARKET Brand name

Strengths available

Nicorette Gum

2,4 mg

Habitriol Patch Nicoderm CQ patch

Step 1: 21 mg Step 2: 14 mg Step 3: 7 mg

Commit Lozenges Nicorette Mini Lozenges

2,4 mg

Examples of OTC NRT Products By Dosage Form

â&#x20AC;˘ These are the available OTC products of Nicotine Replacement Therapy (NRT) which includes gums, patches and lozenges. â&#x20AC;˘ Bupropion (Zyban) and Varenicline (Chantix) are two FDA approved non-nicotine medications used by people to quit smoking. Ref: https://www.drugabuse.gov/publications/drugfacts/cigarettes-other-tobacco-products

INDICATION â&#x20AC;˘ When one quits smoking, the nicotine levels are dropped quickly causing severe withdrawal symptoms. Nicotine in tobacco is an important part of cigarette addiction. â&#x20AC;˘ This medication helps quit smoking by replacing nicotine in cigarettes. These lozenges are Nicotine Replacement Therapy (NRT).

METHOD OF ADMINISTRATION • Lozenges must be used when there is urge of smoking. • For the first 6 weeks, use one lozenge every 1-2 hours (9 lozenges per day minimum). Gradually reduce the dose as per need or urge of smoking. • Eating or drinking within 15 minutes of lozenge administration should be avoided. No chewing or swallowing of lozenges.

Ref: https://www.webmd.com/drugs/2/drug-75256-77/nicotine-polacrilex-buccal/nicotine-gum-buccal/details10

PHARMACOKINETICS Lozenges erodes as a result of chewing or physical abrasion

In the presence of moisture (i.e. saliva) nicotine is released from ion-exchange resin (polacrilex)

Free nicotine available is easily get absorbed in the oral mucosa

Salt ions replace the nicotine in the resin

Sodium carbonate and potassium bicarbonate in the saliva at alkaline condition, keeps the nicotine as a free base

Ref: Jae H. Choi, Carolyn M. Dresler, Michele R. Norton, Kenneth R. Strahs, Pharmacokinetics of a nicotine polacrilex lozenge, Nicotine & Tobacco Research Volume 5, Number 5 (October 2003) 635â&#x20AC;&#x201C;644

CONCLUSION • Nicotine Polacrilex lozenges are useful in the Nicotine Replacement Therapy (NRT). • Along with proper counseling and patient’s will, quitting cigarette smoking can be achieved with these lozenges. • Lozenges offer patient compliance due to different flavors and ease of administration. • Use of Polacrilex polymer have increased the buccal absorption of nicotine than chewing gums.

FUTURE PROSPECTS • Efforts can be made in the direction of more patient compliance by making the formulation available in different flavors and colors. • Also, use of mesh like polymers to trap the nicotine in more concentration in orally administered dosage forms with more emphasis on release of medication ‘on the go’. • Nicotine formulation in orally dispersible tablets can improve the patient compliance.