FABRICATION, DEVELOPMENT AND CHARACTERIZATION OF CARVEDILOL TRANSDERMAL PATCHES: AN EMPIRICAL STUDY

Abstract

Carvedilol is a nonselective beta-adrenergic blocking agent and is employed for the treatment of hypertension. Carvedilol is subjected to considerable first-pass metabolism when it is administered orally. Transdermal preparation of carvedilol was prepared to achieve a sustained effect and to reduce the dose size & dosing frequency as compared to multiple oral dosing and also developed to minimize first pass metabolism. Various polymers such as Ethyl cellulose, PVP K-30, HPMC K15M and Carbopol 934 were selected on the basis of their adhering property and nature of non toxicity, to develop transdermal film of carvedilol. The patches fabricated by EC and Carbopol (F-5 and F-6) were showed very good folding endurance compared to patches containing PVP K-30 and HPMC K15M. Based on physicochemical and in-vitro permeation studies, F-3 and F-5 were chosen as the best formulations. Among these two patches, F-5 film was found to have maximum in vitro permeation, maximum steady state flux and maximum permeability coefficient of drug.

Key words: Transdermal patch, Carvedilol, ethylcellulose, PVP K-30, HPMC K15M and Carbopol 934