| Synthesis and properties of dextran-5-aminosalicylic acid ester as a potential colon-specific prodrug of 5-aminosalicylic acid. | |
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MedLine Citation:
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PMID: 9875428 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Dextran-5-aminosalicylic acid ester (dextran-5-ASA) was synthesized as a colon-specific prodrug of 5-aminosalicylic acid (5-ASA) which is active against inflammatory bowel diseases. Chemical stability of dextran-5-ASA in the bath of pH 1.2 or 6.8 was investigated at 37 degrees C for 6 hrs, and 5-ASA was not released on such conditions. Depolymerization (%) of dextran-5-ASA by dextranase with the degree of substitution (DS) of 18, 23, or 30 was 92, 62 or 45 in 8 hrs respectively, but was not affected by the MW of dextran (9,000, 40,600, 80,200 or 580,000). Distribution of 5-ASA in dextran, determined by gel filtration chromatography, appeared to be relatively uniform. Incubation of dextran-5-ASA (DS 18) in cecal contents of rats released 20% (28 g) and 35% (49 g) of 5-ASA in 8 hrs and 24 hrs, respectively, but no 5-ASA was liberated from small intestinal contents. |
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Authors:
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Y J Jung; J S Lee; H H Kim; Y T Kim; Y M Kim |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Archives of pharmacal research Volume: 21 ISSN: 0253-6269 ISO Abbreviation: Arch. Pharm. Res. Publication Date: 1998 Apr |
Date Detail:
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Created Date: 1999-02-04 Completed Date: 1999-02-04 Revised Date: 2003-11-14 |
Medline Journal Info:
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Nlm Unique ID: 8000036 Medline TA: Arch Pharm Res Country: KOREA |
Other Details:
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Languages: eng Pagination: 179-86 Citation Subset: IM |
Affiliation:
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College of Pharmacy, Pusan National University, Korea. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Aminosalicylic Acids
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chemical synthesis*,
pharmacokinetics Animals Buffers Calibration Cecum / metabolism Chromatography, High Pressure Liquid Colon / metabolism* Dextrans / chemical synthesis*, pharmacokinetics Male Mesalamine / chemical synthesis*, pharmacokinetics Prodrugs / chemical synthesis*, pharmacokinetics Rats Rats, Sprague-Dawley Spectrophotometry, Ultraviolet Stomach / metabolism |
| Chemical | |
Reg. No./Substance:
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0/Aminosalicylic Acids; 0/Buffers; 0/Prodrugs; 0/dextran-5-aminosalicylic acid; 89-57-6/Mesalamine; 9004-54-0/Dextrans |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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