5-氨基水杨酸结肠定位给药pH与时间同时控释小丸的制备与体外释放  

Preparation of colon-specific delivery system for pH and time-controlled pellets of 5-aminosalicylic acid and its in vitro release

作　　者：徐彦[1] 齐宪荣[1] 

机构地区：[1]北京大学药学院药剂学系,北京100083

出　　处：《中国新药杂志》2004年第2期129-133,共5页Chinese Journal of New Drugs

摘　　要：目的:用水分散体包衣技术制备5-氨基水杨酸(5-ASA)结肠定位小丸给药系统。方法:以EudragitRL30D作为时间控释包衣内层,Eudragit S水分散体作为pH控释外层,三乙酸甘油酯为增塑剂,使用流化床包衣设备,制备pH值与时间同时控释的小丸,用释放度测定法研究小丸在不同pH介质中的释放度。结果:小丸在模拟胃酸情况下不释药,在变换pH 7.5条件下9h内释药完全。Eudragit S层保证小丸安全通过胃;而药物释放速度是由丸心、Eudragit RL30D时间控释层来控制。利用小肠相对恒定的转运时间(3-4h)和小肠末端高pH(7-8),及不同Eudragit 聚合物的pH性质制备了较可靠的多剂量结肠给药系统。结论:通过调整内外层包衣厚度可制备5-ASA结肠定位释放小丸。Objective:To prepare a colon-specific delivery system for pH and time controlled pellets of 5-aminosalicylic acid (5-ASA) with water dispersion coating technique. Methods: The delivery system for 5-ASA pellets was prepared using a fluid bed coater, with Eudragit RL30D as inner layer for time control, Eudragit S aqueous dispersion as outer layer for pH control and glycerol triacetate as plasticizer. The in vitro release rates of the 5-ASA pellets were studied in medium of different pH by dissolution apparatus. Results :The ASA pellets did not release in simulated gastric fluid and completely released within 9h as the pH of the fluid changed to 7.5. The Eugragit S outer layer of the pellets can ensure it pass safely through stomach and the Eudrgit RL30D inner layer can control its release time. Colon-specific delivery system for multi-dosages of 5-ASA pellets could be prepared by virtue of constant delivery time through small intestine, the high pH value at its end and the properties of the Eu-dragit polymers. Conclusion: The pH and time-controlled pellets of 5-ASA with specific site of release could be prepared by regulating the thickness of the outer and inner coating layer.

关 键 词：5-氨基水杨酸 pH与时间控释小丸 结肠定位给药 优特奇 水分散体 

分 类 号：R944.9[医药卫生—药剂学] R971.1[医药卫生—药学]