4-氨基水杨酸麦芽糖苷盲结肠定位给药系统的体外评价

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

目的:研究4-氨基水杨酸(4-ASA)麦芽糖苷(Mal)的体外盲结肠定位释药特征。方法:采用高效液相色谱法,以4-ASA的累积释放率为指标,分别考察4-ASA-Mal(相当于250μg/ml的4-ASA)在不同p H(1.2、6.8、7.4)缓冲液、正常大鼠和溃疡性结肠炎模型大鼠不同部位(胃、小肠、盲肠、结肠)内容物液中的释药行为。结果:4-ASA-Mal在不同p H缓冲液中几乎不释放;在正常和模型大鼠胃和小肠的内容物液中12 h的累积释放率均小于8%;在正常大鼠盲肠和结肠内容物液中12 h的累积释放率分别为55%和81%;在溃疡性结肠炎模型大鼠盲肠和结肠内容物液中12 h的累积释放率分别为55%和74%。结论:4-ASA-Mal可在体外盲结肠内容物液中定位大量释放4-ASA,具有盲结肠靶向性。

OBJECTIVE：To investigate the characteristics of cecum and colon-specific drug delivery system of 4-aminosalicylic acid-maltoside（4-ASA-Mal） in vitro. METHODS：With the cumulative release rate of 4-ASA as the index,HPLC was employed to observe the delivery of 4-ASA-Mal（equivalent to 250 μg/ml 4-ASA） in the buffer solutions of different p H（1.2,6.8and 7.4）and in the aqueous contents in different parts（stomach,small intestine,cecum and colon）of normal rats and the rat models of ulcerative colitis. RESULTS：4-ASA-Mal was hardly released in the buffer solutions of different p H. 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 cecum and colon,targeting cecum and colon in vitro.