Document Detail

Design and evaluation of pH modulated controlled release matrix systems for colon specific delivery of indomethacin.
MedLine Citation:
PMID:  18972836     Owner:  NLM     Status:  MEDLINE    
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 canbe ideal for site specific delivery of drugs to colon with controlled release profile.
L F A Asghar; S Chandran
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Die Pharmazie     Volume:  63     ISSN:  0031-7144     ISO Abbreviation:  Pharmazie     Publication Date:  2008 Oct 
Date Detail:
Created Date:  2008-10-31     Completed Date:  2008-12-09     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9800766     Medline TA:  Pharmazie     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  736-42     Citation Subset:  IM    
Formulation Development & Pharmacokinetic Laboratory, Pharmacy Group, Birla Institute of Technology & Science, Pilani, India.
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MeSH Terms
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*
Polymethacrylic Acids
Reproducibility of Results
Spectrophotometry, Ultraviolet
Reg. No./Substance:
0/Anti-Inflammatory Agents, Non-Steroidal; 0/Delayed-Action Preparations; 0/Polymethacrylic Acids; 25086-15-1/methylmethacrylate-methacrylic acid copolymer; 53-86-1/Indomethacin; 9004-34-6/Cellulose; 9004-57-3/ethyl cellulose

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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