5-아미노살리실산의 결장표적성 프로드럭 : 5-아미노살리실-L-글루타민산과 5-아미노살리실-L-아스파틸산의 합성 및 성상

• 영문명: Synthesis and Properties of 5-Aminosalicyl-L-Aspartic Acid and 5-Aminosalicyl-L-glutamic Acid as Colon-specific Prodrugs of 5-Aminosalicylic Acid
• 발행기관: 대한약학회
• 저자명: 정연진(Yun Jin Jung) 이정수(Jeoung Soo Lee) 김학현(Hak Hyun Kim) 김영미(Young Mi Kim) 김대덕(Dae Duk Kim) 한석규(Suk Kyu Han)
• 간행물 정보: 『약학회지』제42권 제1호 (1998년), 5~11쪽, 전체 7쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1998.01.31

영문 초록

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.

키워드

5-Aminosalicyl-L-aspartic acid 5-Aminosalicyl-L-glutamic acid Colon-specific prodrug 5-aminosalicylic acid Ulcerative colitis Crohn's disease Inflammatory bowel disease.