文档介绍：刘欣,薛红梅,王建明*,高月娟
(黑龙江中医药大学中医药研究院,黑龙江哈尔滨 150040)
摘要:目的用丙烯酸树脂水分散体包衣技术制备pH敏感-时间控释型盐酸小檗碱结肠定位包衣片,评价其体外释药特性。方法采用滚转包衣机多层薄膜包衣技术制备结肠定位包衣片,以羟丙甲纤维素HPMC作为隔离层,pH敏感型丙烯酸树脂Eudragit L30D-55与Eudragit S100混合包衣液作为肠溶层,渗透型丙烯酸树脂Eudragit RL30D和EudragitRS30D混合液作为缓释层,以柠檬酸三乙酯作为增塑剂,滑石粉作为抗粘剂,通过正交实验进行处方优化,研究包衣片在模拟人体胃肠道环境中的释药速率。结果最佳包衣处方:%;肠溶层组成Eudragit L30D-55:S100(1:5),包衣增重4%;缓释层组成(1:1),包衣增重2%。·L-1盐酸溶液中2小时无药物释放,%,,12小时内药物释放量在70%左右,累积释药百分率高于标示量的80%。结论水分散体包衣技术制备结肠定位包衣片工艺合理可行,有良好的开发和应用前景。
关键词:盐酸小檗碱;结肠定位包衣片;丙烯酸树脂水分散体
Study on the preparation of colon-specific delivery system for pH and time-controlled coated tablets of berberine hydrochloride and its in vitro release
LIU Xin, XUE Hong-Mei ,WANG Jian-Ming, GAO Yue-Juan
(Academy of Traditional Chinese Medicine, Heilongjiang University of Chinese Medicine, Harbin 150040, China)
Abstract: Objective To prepare a colon-specific delivery system for pH-dependent and time-contolled coated tablets of berberine hydrochloride with acrylic resin water dispersion coating technique , and the drug release in vitro was evaluated. Methods The berberine hydrochloride colon-specific targeting coated tablets were prepared by a sugar coater, with multi-layer coating technology, using HPMC as sealing-coat layer, Eudragit L30D-55/S100 as enteric-dissolved layer, and Eudragit RL30D/RS30D as sustained-release layer, usi