Formulation and biopharmaceutical evaluation of transdermal patch containing benztropine

International Journal of Pharmaceutics
Nguyen Thien HaiSang-Cheol Chi

Abstract

Benztropine (BZ) is a potent muscarinic receptor antagonist that has been used for the treatment of Parkinson disease. However, the oral administration of BZ is often limited because of its many dose-related side effects. In this study, BZ was formulated into drug-in adhesive (DIA) patches in an attempt to overcome these problems. The effects of the formulation factors including pressure-sensitive adhesive (PSA), enhancer, the loading amount of the drug and patch thickness on the skin permeation of the drug were evaluated using excised rat skin. The optimized patch contained 10% BZ in Duro-Tak 2525 as a PSA at a thickness of 100 microm. The pharmacokinetic characteristics of the optimized DIA patch were determined after the transdermal application to rabbits. The calculated relative bioavailability of BZ in the DIA patch was 54% compared to the oral administration of BZ mesylate. This suggests that the transdermal application of BZ in a DIA patch may be used for the treatment of Parkinson disease.

Citations

Apr 3, 2010·Archives of Pharmacal Research·Robhash Kusam SubediHoo-Kyun Choi
Feb 18, 2012·Drug Development and Industrial Pharmacy·Geeta AggarwalS L Hari Kumar
Dec 17, 2011·Expert Opinion on Drug Delivery·Francesco CilurzoPaola Minghetti
Dec 30, 2011·Drug Development and Industrial Pharmacy·L I SolerJ Domenech
Oct 16, 2012·Journal of Controlled Release : Official Journal of the Controlled Release Society·Amit AlexanderDulal Krishna Tripathi
Aug 17, 2011·International Journal of Pharmaceutics·Robhash Kusam SubediHoo-Kyun Choi
May 19, 2009·International Journal of Pharmaceutics·Ligang ZhaoChangshu Ren
Jul 10, 2012·International Journal of Pharmaceutics·Chun-Woong ParkEun-Seok Park
Dec 31, 2014·European Journal of Drug Metabolism and Pharmacokinetics·Subham BanerjeeVijay Veer

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