马来酸桂哌齐特胃内漂浮片制备及释药机制研究  

Study on Preparation and Release Mechanism of Cinepazide Maleate Intragastric Floating Tablets

作　　者：曾灿丽 何雄 贺莲 梁致红 刘娟 吴健民 刘达 张静 张华玲 Zeng Canli;He Xiong;He Lian;Liang Zhihong;Liu Juan;Wu Jianmin;Liu Da;Zhang Jing;Zhang Hualing(Kamp pharmaceutical Co.,Ltd.,Changsha 410205,China)

机构地区：[1]康普药业股份有限公司,湖南长沙410205

出　　处：《广东化工》2021年第11期33-35,共3页Guangdong Chemical Industry

基　　金：湖南常德市科技重大项目(常财企指2017(66))。

摘　　要：目的:制备马来酸桂哌齐特胃内漂浮片并研究其释药机制。方法:以粉末直压再包衣工艺制备漂浮片;以2 h、6 h、22 h累积释放度为指标,采用L9(34)正交试验设计优选漂浮片HPMC、碳酸钙、Eudragit L30D-55的用量;以平均累积释放率对时间分别以零级方程、一级方程和Higuchi方程、Peppas方程进行拟合,用相关系数(r)判断释放机制。结果:漂浮片HPLC、起泡剂碳酸钙、Eudragit L30D-55的用量分别为25%、5%、10%;起漂时间小于5 min,可以维持24 h持续释放;体外释药模型符合Higuchi动力学方程,通过骨架溶蚀进行释放。结论:经三批产品工艺验证,表明马来酸桂哌齐特胃内漂浮片工艺稳定,重现性好,具有缓释作用。Objective: To prepare cinepazide maleate intragastric floating tablets and study its release mechanism. Methods: Floating tablets were prepared by direct powder pressing and coating process. Taking the cumulative release at 2 h, 6 h and 22 h as indexes, the dosage of floating tablets by HPMC, calcium carbonate and Eudragit L30 D-55 was optimized by L9(34) orthogonal design. The average cumulative release rate was used to fit the time by zero-order equation, first-order equation, Higuchi equation and Peppas equation, respectively, and the correlation coefficient(r) was used to determine the release mechanism. Results: The dosage of floating tablet by HPLC, foaming agent calcium carbonate and Eudragit L30 D-55 were 25 %, 5 % and 10 %, respectively. The initial drift time is less than 10 min,and it can maintain continuous release for 24 h. The model of drug release in vitro accords with Higuchi kinetic equation. Conclusion: After three batches of product process verification, it is shown that cinepazide maleate intragastric floating tablet has stable process, good reproducibility and slow release effect.

关 键 词：马来酸桂哌齐特 胃内漂浮片 制备工艺 缓释 释放机制 

分 类 号：TQ[化学工程]