Evaluation in vitro of Cecum and Colon-specific Drug Delivery System of 4-aminosalicylic Acid-maltoside

VernacularTitle:4-氨基水杨酸麦芽糖苷盲结肠定位给药系统的体外评价
Author: Guoli WU ; Feifei LI ; Ruiling LIU ; Tingli QU ; Xia LI ; Zhengbao ZHAO
Publication Type:Journal Article
Keywords: 4-aminosalicylic acid-maltoside; Cecum and colon-specific drug delivery system; Rat; Ulcerative colitis; Cumula-tive release
From: China Pharmacy 2015;(25):3485-3487
CountryChina
Language:Chinese
Abstract: OBJECTIVE:To investigate the characteristics of cecum and colon-specific drug delivery system of 4-aminosalicyl-ic acid-maltoside (4-ASA-Mal) in vitro. METHODS:With the cumulative release rate of 4-ASA as the index,HPLC was em-ployed to observe the delivery of 4-ASA-Mal (equivalent to 250 μg/ml 4-ASA) in the buffer solutions of different pH (1.2,6.8 and 7.4)and in the aqueous contents in different parts(stomach,small intestine,cecum and colon)of normal rats and the rat mod-els of ulcerative colitis. RESULTS:4-ASA-Mal was hardly released in the buffer solutions of different pH. 12 h cumulative release rates were less than 8% in the aqueous contents in the stomachs and small intestines of normal rats and rat models,and were 55%and 81% in the aqueous contents in the cecum and colons of normal rats,and 55% and 74% in the aqueous contents in the cecum and colons of model rats with ulcerative colitis. CONCLUSIONS:4-ASA-Mal can release a lot of 4-ASA in aqueous contents in ce-cum and colon,targeting cecum and colon in vitro.