复方盐酸二甲双胍肠溶缓释微丸的制备-药学与临床研究.DOC

复方盐酸二甲双胍肠溶缓释微丸的制备* 宦立娟，郑春丽，朱家壁**，刘建平** 中国药科大学药物制剂研究所，南京210009 摘 要 目的：制备复方盐酸二甲双胍肠溶缓释微丸，并考察制剂体外释放特性。方法：利用底喷式流化床包衣设备，以空白丸芯、羟丙基甲基纤维素、单硬脂酸甘油酯、Eudragit NE30D、Eudragit?L100-55等制备盐酸二甲双胍肠溶缓释微丸；羟丙基甲基纤维素等制备盐酸吡格列酮胃溶微丸。结果：制备的盐酸二甲双胍肠溶缓释微丸肠液中缓慢释放12h，盐酸吡格列酮胃溶微丸在人工胃液中30 min溶出85%以上。结论：优选出复方盐酸二甲双胍肠溶缓释微丸的制备工艺，该制备工艺简单易行，重现性好，有望应用于工业化生产。 关键词 盐酸二甲双胍；肠溶缓释微丸；盐酸吡格列酮；累积释放度；流化床包衣*基金项目 *基金项目 江苏省普通高校研究生科研创新计划项目CXZZ13_0327 作者简介 宦立娟，女，硕士生，研究方向：药物新制剂与新技术 Email:huanlijuan2008@126.com **通讯作者 朱家壁，男，教授，博士生导师，研究方向：药剂学、药物动力学 Email:zhujiabi001@; 刘建平，女，教授，博士生导师，研究方向：新型给药系统和生物药剂学 Email:jianpingliu1293@163.com 收稿日期 修回日期 中图分类号 文献标志码 文章编号 Preparation of Compound Metformin Hydrochloride Enteric-coated and Sustained-release Pellets* HUAN Li-juan, ZHENG Chun-li, ZHU Jia-bi**, LIU Jian-ping** Pharmaceutical Research Institution, China Pharmaceutical University, Nanjing 210009, China ABSTRACT Objective: To develop the compound metformin hydrochloride enteric–coated and sustained-release pellets and also study its in vitro drug release. Method: The fluid-bed coating equipment was used to prepare pellets. The metformin hydrochloride enteric–coated and sustained-release pellets were prepared with Eudragit NE30D, Eudragit??L100-55, HPMC-E5 and glycerylmonostearate(GMS).HPMC-E5 was used to prepare pioglitazone hydrochloride pellets. Results: The prepared metformin hydrochloride enteric–coated and sustained-release pellets in vitro slowly released 12 hours. Pioglitazone hydrochloride pellets dissolved more than 85% in the artificial gastric juice in 30 minutes. Conclusions: We prepared the preferred preparation of compound metformin hydrochloride enteric–coated and sustained-release pellets. The prepared process is simple and reproducible. It can be used in industrial production. KEY WORDS Metformin hydrochloride; Sustained-release pellets; Pioglitazone hydrochloride; Cumulative release; Fluid-bed coating 复方缓控释制剂对于慢性疾病的治疗具有重要的意义。本文以盐酸二甲双胍和盐酸吡格列酮为模型药物，研究制备