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INTERNATIONAL JOURNAL OF PHARMACEUTICAL RESEARCH

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IJPR included in UGC-Approved List of Journals - Ref. No. is SL. No. 4812 & J. No. 63703

Published by : Advanced Scientific Research
ISSN
0975-2366
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IJPR 9[3] July - September 2017 Special Issue

July - September 9[3] 2017

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Transdermal film of Simvastatin to Avoid Pre-systemic Metabolism: Formulation and Characterization

Author: PRAVEEN R, DEEPAK SETHI, PRP VERMA
Abstract: The aim of the present study was to formulate and evaluate transdermal films containing simvastatin which has low bioavailability due to high first-pass metabolism. The films were prepared with mixture of different grades of Eudragit® (RL100:RS100, RLPO:RSPO and RLPM:RSPM each in the ratios of 100:00, 80:20, 60:40, 50:50, 40:60, 20:80, 00:100) using solvent casting method on mercury. Solvent mixture of dichloromethane and methanol (4:6) was used with dibutyl phthalate (20%w/w of polymer) as plasticizer. Drug-polymer interaction was investigated using FT IR and DSC. The prepared films were evaluated for thickness, weight variation, folding endurance and drug content, which produced satisfactory results with low standard deviation. The moisture absorption, water vapour transmission rate and percent drug release were highest in the formulations containing higher proportion of Eudragit® RL type (A1, B1, and C1). Among them, C1, with Eudragit® RLPO, showed highest percent drug release in 24 hours, may be due to the polymer being highly permeable with high number of quarternary ammonium groups. Release kinetic studies revealed a good fit to the Higuchi model indicating that the drug release mechanism was diffusion.
Keyword: Polymeric film, Eudragit®, Simvastatin, Drug delivery, Dissolution
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