5-아미노살리실산의 結腸標的性 프로드럭 : 덱스트란-5-(4-에톡시카르보닐페닐아조)살리실산 에스테르

• 영문명: Dextran-5-(4-ethoxycarbonylphenylazo)salicylic Acid Ester as a Colon-specific Prodrug of 5-Aminosalicylic Acid
• 발행기관: 대한약학회
• 저자명: 정연진(Yun Jin Jung) 이정수(Jeoung Soo Lee) 김윤택(Yun Taek Kim) 김영미(Young Mi Kim) 김대덕(Dae Duk Kim) 한석규(Suk Kyu Han)
• 간행물 정보: 『약학회지』제42권 제1호 (1998년), 31~38쪽, 전체 8쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1998.01.31

영문 초록

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-ethoxycarbonylphenylazo) 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.

키워드

Colon-specific delivery 5-aminosalicylic acid prodrug dextran inflammatory bowel disease.