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KMID : 0370219980420010005
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Yakhak Hoeji
1998 Volume.42 No. 1 p.5 ~ p.11
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Synthesis and Properties of 5-Aminosalicyl-L-Aspartic Acid and 5-Aminosalicyl-L-glutamic Acid as Colon-Specific Prodrugs of 5-Aminosalicylic Acid
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정연진/Jung YJ
이정수/김학현/김영미/김대덕/한석규/Lee JS/Kim HH/Kim YM/Kim DD/Han SK
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Abstract
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5-Aminosalicyl-L-aspartic acid (5-ASA-Asp) and 5-aminosalicyl-L-glutamic acid (5-ASA-Glu) were synthesized as new colon-specific prodrugs of 5-aminosalicylic acid (5-ASA), their apparent partition coefficients, and the extent of conversion in the homogenates of tissue and contents of various G.I. Tract segments of rats were evaluated. These prodrugs were stable in the homogenate of tissue and contents of stomach, proximal small intestine (PSI) or distal small intestine (DSI). Release of 5-ASA from 5-ASA-Asp after incubation with the cecal and colonic contents for 8hrs at 37oC was 18%, and 8%, respectively. No significant conversion of prodrug was observed in the cecal and colonic contents of rats pretreated with kanamycin sulfate, which indicated that microbial enzymes were responsible for the cleavage of these prodrugs.
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KEYWORD
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