Improved rate of absorption of a novel oral transmucosal dosage form of nicotine in human subjects

Authors:
Vikas Agarwal and Derek Moe

Presenter:
Vikas Agarwal
Associate Director, Formulation Development, CIMA Labs Inc. Minnesota, USA

Abstract
Nicotine Polacrilex was formulated in a proprietary dosage form for buccal/sublingual administration. The tablets incorporate effervescence and pH modifying agents that enhance the absorption of nicotine. This 2 mg nicotine dosage form incorporating effervescence (OV) was compared with a non-effervescent dosage form (Control) and an existing commercial lozenge (Commit ®) in a cross-over pharmacokinetic study in human subjects (n = 23).

Results: The mean nicotine peak and overall exposure of the given OV treatment were higher compared to the control and reference. The mean ratios (AUC0-tmax[ref] and AUC0-tmax) of the OV was almost double compared to the control and reference. The tmax of the OV tablet shorter than the control and reference, and the Cmax was double.

Conclusions: Improved rate of absorption was seen from the effervescent tablet. Nicotine exposure comparable to existing commercial strengths can be achieved at half the dose which might lead to decreased incidence of gastrointestinal side-effects associated with Nicotine. Compared to existing commercial products, the organoleptic experience of the dosage form was better due to the smaller size of the effervescent tablet (1/5th) which allowed for discreet placement in the buccal cavity and use of the effervescent ingredients inhibited the taste of nicotine in the oral cavity.

Source of funding: Self – Company funds.

Declaration of interest: I have a commercial interest in the product being evaluated.

About the presenter
Vikas Agarwal is currently the Associate Director of Formulation Development at CIMA LABS. His group is responsible for formulation and process development of products spanning CIMA’s existing and new drug delivery technologies in the area of Orally Disintegrating Dosage Forms, Oral Transmucosal Delivery of small molecules and macromolecules and Solubility enhancement. Dr. Agarwal has a Ph.D. from Texas Tech University Health Sciences Center and a B.Pharm. and Masters of Pharmacy from Birla Institute of Technology and Science. He is currently pursuing a Certificate of Innovation Studies at the University of Minnesota.