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KMID : 0043319980210020174
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Archives of Pharmacal Research
1998 Volume.21 No. 2 p.174 ~ p.178
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Synthesis and Evaluation of 5-Aminosalicyl-glycine as a Potential Colon-specific Prodrug of 5-Aminosalicylic Acid
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Jung Yun-Jin
Lee Jeoung-Soo
Kim Hak-Hyun
Kim Young-Mi
Han Suk-Kyu
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Abstract
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As a new colon-specific prodrug of 5-aminosalicylic acid (5-ASA), 5-aminosalicyl-glycine (5-ASA-Gly) was prepared by a simple synthetic route in good yield. Apparent partition coefficients of 5-ASA-Gly were lower than those of 5-ASA, which determined in/pH 6.8 buffer or n-octanol/pH 6.8 buffer system. Stability of 5-ASA-Gly by peptidases was investigated by incubation of 5-ASA-Gly with the homogenates of tissue and contents of stomach, proximal small intestine or distal small intestine of rats at . 5-ASA was not detected, indicating that the prodrug was stable in the upper intestine. The amount of 5-ASA liberated from incubation of the prodrug in cecal or colonic contents of rats was about 65% or 27% in 8 hrs, respectively, which indicated that the prodrug activation took place more readily in the rat cecum whose bacterial counts are high like human colon. Results from in vitro experiments suggested 5-ASA-Gly as a promising candidate of a colon-specific prodrug of 5-ASA.
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KEYWORD
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5-Aminosalicyl-glycine, Colon-specific prodrug of 5-aminosalicylic acid, Ulcerative colitis, Crohn`s disease, Inflammatory bowel disease
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