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Formulation and development of novel control release transdermal patches of carvedilol to improve bioavailability for the treatment of heart failure
Institution:1. Department of cardiology, Xiangya hospital central south university, Changsha, Hunan 410008, China;2. Institute of clinical pharmacology, Central South University, Changsha, Hunan 410005, China
Abstract:The main aim of this study is to optimize and evaluate transdermal patch of Carvedilol by the use of different polymer and different permeation enhancers which help to release drug in controlled action and thereby increase the bioavailability of the drug. Main objective was to avoid first pass metabolism of Carvedilol. Transdermal patches were developed by solvent evaporation method. The combination of Eudragit RS-100 as rate controlling polymer and Span 80 as a permeation enhancer was found to be ideal formulation (Formulation F7) with maximum drug release i.e. 100.29 ± 0.44 % within 12 h. Formulation F7 showed maximum bioavailability and showed maximum drop of BP at 6 h. From this study the conclusion was, transdermal patch of Carvedilol which contains Eudragit RS-100 polymer and Span 80 as penetration enhancer produced sustained and continued drug release.
Keywords:Heart failure  Carvedilol  Eudragit  Transdermal patch  Span 80  Control release
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