【2017年整理】盐酸小檗碱结肠定位包衣片的制备工艺和体外释放研究.docVIP

盐酸小檗碱结肠定位包衣片的制备工艺和体外释放研究 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：隔离层增重1.2%；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%。包衣片在0.1moL·L-1盐酸溶液中2小时无药物释放，在pH6.8的磷酸盐缓冲液中3小时药物释放低于10%，在pH7.8的磷酸盐缓冲液中呈缓慢释放，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, using triethyl citrate as plasticizer and talc powder as antisticking agent. An optimal prescription was obtained by orthogonal design. The drug dissolusion rate in vitro was studied in simulating gastrointestinal circumstances. Results The result of orthogonal experiment showed that combination of Eudragit L30D-55/S100 was 1:5, coating weight was 4%; combination of Eudragit RL30D/RS was 1:1, coating weight was 2%, were the optimal formulation. There was no drug released in 0.1moL·L-1 hydrochloric acid solution for 2 hours. In pH6.8 phosphate buffer, dissolution