Document Detail


Studies of chitosan/organic acid/Eudragit RS/RL-coated system for colonic delivery.
MedLine Citation:
PMID:  18835342     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Prednisolone (PDS) beads were coated sequentially with (i) innermost hydrophobic layer of Eudragit RS/RL, (ii) middle drug release-triggering layer of chitosan, organic acid and Eudragit RS/RL, and (iii) outermost enteric coating layer. Continuous dissolution studies were carried out in artificial gastric fluid (pH 1.2), followed by intestinal fluid (pH 6.8), and finally in colonic fluid (pH 4 and 6) with and without beta-glucosidase. While drug release was prevented in the gastric and small-intestinal fluids, a continuous release was observed in the colonic fluid. Succinic acid provided the fastest rate of release in the colonic fluid compared to citric, tartaric or malic acid. A combined mechanism of drug release is proposed, which considers the swelling of chitosan and Eudragit RS/RL in the presence of succinic acid possibly via electrostatic interaction between the amine groups of chitosan/quaternary ammonium groups of Eudragit RS/RL and the carboxyl groups of succinic acid in aqueous medium. The results of plasma pharmacokinetic studies in Sprague-Dawley rats showed that the developed system provided a significant delay (T(max) 9.3 h) in the absorption profile of PDS compared with simple enteric-coated (T(max) 4 h) or powder (T(max) 1 h) formulation that was taken as proof for the colon-targeted delivery.
Authors:
Karanjit Kaur; Kwonho Kim
Publication Detail:
Type:  Journal Article     Date:  2008-09-13
Journal Detail:
Title:  International journal of pharmaceutics     Volume:  366     ISSN:  0378-5173     ISO Abbreviation:  Int J Pharm     Publication Date:  2009 Jan 
Date Detail:
Created Date:  2008-12-29     Completed Date:  2009-04-07     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7804127     Medline TA:  Int J Pharm     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  140-8     Citation Subset:  IM    
Affiliation:
Drug Delivery Systems Research Laboratory, College of Pharmacy and Allied Health Professions, St. John's University, Queens, NY 11439, USA.
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MeSH Terms
Descriptor/Qualifier:
Acrylic Resins / chemistry
Animals
Anti-Inflammatory Agents / administration & dosage,  pharmacokinetics
Chitosan / chemistry*
Colon / metabolism
Drug Carriers / chemistry*
Drug Delivery Systems*
Excipients / chemistry
Hydrogen-Ion Concentration
Male
Polymers / chemistry
Prednisolone / administration & dosage*,  pharmacokinetics
Rats
Rats, Sprague-Dawley
Solubility
Succinic Acid / chemistry
Time Factors
Chemical
Reg. No./Substance:
0/Acrylic Resins; 0/Anti-Inflammatory Agents; 0/Drug Carriers; 0/Excipients; 0/Polymers; 110-15-6/Succinic Acid; 33434-24-1/Eudragit RS; 50-24-8/Prednisolone; 51822-44-7/Eudragit RL; 9012-76-4/Chitosan

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


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