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KMID : 0043319980210020179
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Archives of Pharmacal Research
1998 Volume.21 No. 2 p.179 ~ p.186
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Synthesis and Properties of Dextran-5-amonosalicyclic Acid Ester as a Potential Colon-specific Prodrug of 5-Aminosalicyclic Acid
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Jung Yun-Jin
Lee Jeoung-Soo
Kim Hak-Hyun
Kim Yun-Taek
Kim Young-Mi
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Abstract
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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 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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KEYWORD
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Dextran-5-aminosalicylic acid ester, Colon-specific delivery, 5-Aminosalicylic acid, Crohn`s disease, Ulcerative colitis, Inflammatory bowel disease
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