盐酸曲美他嗪缓释片的研制及其体外释药特性考察

摘要

Objective: To prepare trimetazidine hydrochloride (TMZ) sustained release tablets and to evaluate its release characteristics in vitro. Methods; Hydroxy propyl methyl cellulose (HPMC) was used as the main polymer, and wet-granulation method was used to prepare the tablets. The formulation was optimized by orthogonal design,using release rate as the evaluation parameter. The release rate at different time was used to fit the release equation and to determine the release characteristics. Results;The optimized prescription of the tablets was as follows; HPMC 90 mg,sodium carboxy methyl cellulose 30 mg,microcrystalline cellulose 60 mg,10% polyvinylpyrroli-dine-alcohol solution (w/v) q. S. ,magnesium stearate 2 nig;the release degree at 12 h was (98. 1 ±1.8)% , and the release profile was fitted with first order kinetic equation ( r =0. 994 2) ; pressure during preparation of the tablets influenced the release in a certain extent. Conclusion: This preparation method of TMZ sustained release tablets is simple and reproducible, which produces tablets with sustained release characteristics.%目的:研制盐酸曲美他嗪( TMZ)缓释片,并考察其体外药物释放特性.方法:以羟丙基甲基纤维素( HPMC)为主要骨架材料,采用湿法制粒压片法,制备TMZ缓释片；以释放度为评价指标,采用正交试验设计对处方进行优化；根据药物不同时间释放度,拟合释放度方程,确定释药特性.结果:TMZ缓释片的处方组成为:HPMC 90 mg,羧甲基纤维素钠30 mg,微晶纤维素60 mg,10％聚乙烯吡咯烷酮-乙醇溶液(w/v)适量,硬脂酸镁2 mg;12 h释放度为(98.1±1.8)％,体外释放曲线符合一级动力学方程(r =0.994 2)；压片力对药物释放有一定影响.结论:研制的TMZ缓释片制备工艺简单,重现性好,释药特性达到缓释要求.