| Studies of chitosan/organic acid/Eudragit RS/RL-coated system for colonic delivery. | |
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MedLine Citation:
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PMID: 18835342 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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Karanjit Kaur; Kwonho Kim |
Publication Detail:
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Type: Journal Article Date: 2008-09-13 |
Journal Detail:
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Title: International journal of pharmaceutics Volume: 366 ISSN: 0378-5173 ISO Abbreviation: Int J Pharm Publication Date: 2009 Jan |
Date Detail:
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Created Date: 2008-12-29 Completed Date: 2009-04-07 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 7804127 Medline TA: Int J Pharm Country: Netherlands |
Other Details:
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Languages: eng Pagination: 140-8 Citation Subset: IM |
Affiliation:
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Drug Delivery Systems Research Laboratory, College of Pharmacy and Allied Health Professions, St. John's University, Queens, NY 11439, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Acrylic Resins
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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:
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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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