Pfizer Global Research and Development has submitted a patent for a varenicline transdermal patch that would hopefully hit the market in 2008.
Varenicline is a highly potent compound such that dosage forms are necessarily highly diluted with excipients...providing for such desirable features as controlling the drug dissolution...either fast dissolving or slow dissolving in a controlled-release system as described in co-pending applications U.S. Patent Publication No. 2003-0180360 A1 , published Sept. 25, 2003, and Serial No. 10/848,464, filed May 18, 2004.[...]There are advantages of delivering varenicline in the form of a transdermal composition.
- Relative to an oral dosage form such as a tablet or capsule delivery of varenicline via a transdermal composition would be a preferred choice by patients who have difficulty in swallowing tablets, capsules or other solids.
- The tablet dosage form of varenicline has shown, in some instances, a certain level of nausea in patients. There is a need to reduce these side effects.
- A gradual release of the varenicline dosage form such as would be the case from a transdermal composition might prove to be useful towards reducing the incidence of nausea and enhance the desirability of the drug to a larger patient population requiring its use.
- Finally, it is likely to assume there would be a higher compliance rate if a patient could apply a transdermal patch that delivers therapeutically useful levels of active ingredient over the course of a day or a longer period of time versus taking a once or twice daily tablet or capsule with water.


FYI - Pfizer have just opened a trial of the patch formulation of varenicline - We are covering it in our monthly analysis of nicotinic therapeutics, UpdatesPlus-Nicotinic Receptors. The patch formulation looks particularly interesting - in particular it has the potential to reduce the rate of adverse effects - they are actiually looking at nausea in the study.