Design and evaluation of pH modulated controlled release matrix systems for colon specific delivery of indomethacin

Indomethacin, a potent non steroidal anti-inflammatory drug (NSAID), is indicated for the local treatment of colorectal carcinoma. The aim of the present study was to design and investigate various matrix systems for controlled and site specific delivery of indomethacin to the colon. Various pH sens...

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Veröffentlicht in:Pharmazie 2008-10, Vol.63 (10), p.736-742
Hauptverfasser: Asghar, L. F. A., Chandran, S.
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Chandran, S.
description Indomethacin, a potent non steroidal anti-inflammatory drug (NSAID), is indicated for the local treatment of colorectal carcinoma. The aim of the present study was to design and investigate various matrix systems for controlled and site specific delivery of indomethacin to the colon. Various pH sensitive and hydrophobic polymers were investigated for their effect on drug release and site specificity. Effect of proportion of Eudragit L100 and Eudragit S100 in matrix either alone or in combination was evaluated. Effect of hydrophobic non-swellable polymer ethyl cellulose on the release pattern of drug from the Eudragit bases was also investigated. Matrix tablets prepared with Eudragit showed pH dependent release profile with the formulations of Eudragit L100 showing faster rate of drug release than Eudragit S100 in alkaline pH. The release profile from matrix tablets containing Eudragit L100 and Eudragit S100 in combination or with ethyl cellulose correlated well with the relative proportion of the two polymer types in the matrix base. Selected formulations when evaluated in simulated gastric fluid pH without enzymes showed negligible to low drug release (less than 10%) in the first 4-6 h followed with controlled release for 14-16 h. It was concluded that pH sensitive matrix bases in combination with a hydrophobic polymer like ethyl cellulose can be ideal for site specific delivery of drugs to colon with controlled release profile.
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subjects Anti-Inflammatory Agents, Non-Steroidal - administration & dosage
Cellulose - analogs & derivatives
Chemistry, Pharmaceutical
Chemistry, Physical
Colon - metabolism
Delayed-Action Preparations
Drug Delivery Systems
Drug Stability
Drug Storage
Hydrogen-Ion Concentration
Indomethacin - administration & dosage
Kinetics
Polymethacrylic Acids
Reproducibility of Results
Solubility
Spectrophotometry, Ultraviolet
title Design and evaluation of pH modulated controlled release matrix systems for colon specific delivery of indomethacin
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