5-氨基水杨酸pH依赖-时间控制型结肠定位微丸的制备与体外释放研究  

Study on preparation and release of 5-aminosalicylic colon-specific delivery pellets controlled by pH and time of in vitro

作　　者：刘群[1] 李晓华[1] 杨金荣[1] 房志仲[1] 

机构地区：[1]天津医科大学药学院药剂教研室,天津300070

出　　处：《天津医科大学学报》2008年第1期34-37,共4页Journal of Tianjin Medical University

摘　　要：目的:制备pH依赖-时间控制型5-氨基水杨酸(5-ASA)结肠定位微丸给药系统。方法:以Eudragit NE30D为时间控释包衣内层,Eudragit S100为pH控释外层,柠檬酸三乙酯为增塑剂,采用流化床喷雾包衣技术,制备pH依赖-时间控制型微丸。采用释放度测定法考察影响药物释放的各种因素。结果:包衣增重是影响药物释放的关键因素,在模拟人体胃肠道pH变化条件下,微丸释放基本符合释放要求,显示了良好的结肠定位效果。结论:通过调整内外层包衣厚度可制备5-氨基水杨酸结肠定位给药微丸。Objective： To prepare a colon-specific delivery system for pH and time controlled pellets of 5-aminosalicylic （5-ASA）. Methods： The delivery system for 5-ASA pellets was prepared using a fluid bed coater, with Eudragit NE30D as inner layer for time control, Eudragit S100 as out layer for pH control and triethyl citrate added to the dispersion as the plasticizer. In vitro the release rates of the 5-ASA pellets were investigated to evaluate the factors which influence the release behaviors of the pellets. Results： The release rates were decided by the thickness of the coating layer, The data of release in Vitro showed that it met the requirement of the colon-specific pellets. Conclusion： The pH and time controlled pellets for 5-ASA colon-specific delivery can be prepared by regulating the thickness of the outer and inner coating layer.

关 键 词：5-氨基水杨酸 口服结肠定位释药 微丸 pH-时间控制 

分 类 号：R574.62[医药卫生—消化系统] R944.9[医药卫生—内科学]