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KMID : 0370219980420010031
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Yakhak Hoeji
1998 Volume.42 No. 1 p.31 ~ p.38
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Dextran-5- ( 4-ethoxycarbonylphenylazo ) salicylic Acid Ester as a Colon-Specific Prodrug of 5-Aminosalicylic Acid
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정연진/Jung YJ
이정수/김윤택/김영미/김대덕/한석규/Lee JS/Kim YT/Kim YM/Kim DD/Han SK
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Abstract
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Dextran-5-(4-ethoxycarbonylphenylazo)salicylic acid ester(Dextran-5-ESA) was synthesized as a potential colon-specific prodrug of 5-aminosalicylic acid (5-ASA). No free 5-(4-eth oxycarbonylphenylazo) salicylic acid (5-ESA) was detected when the chemical stability of dextran-5-ESA was tested at pH 1.2, or pH 6.8 bath solution, Effects of the degree of substitution (DS) and molecular weight of dextran on the depolymerization by dextranase was investigated. Depolymerization(%) decreased with increasing DS, and was not affected by M.W. of dextran. The extent of prodrug conversion after incubation in the contents of various G.I. Tract segments of rats was evaluated. 5-ASA was released in the cecal contents, but not in the contents of proximal small intestine (PSI) or distal small intestine (DSI). No significant prodrug conversion was observed in the cecal contents of rats pretreated with kanamycin sulfate, which indicated that microbial enzymes were responsible for the cleavage of the prodrug.
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