辛伐他汀缓释片制备及体外释放研究

Preparation and Study on Release Rate in Vitro for Sustained-release Tablets of Simvastatin

关键词:  辛伐他汀  凝胶骨架缓释片  羟丙基甲基纤维素  释放度

Key words:  simvastatin  gel matrix sustained-release tablets  hydroxypropyl methyl cellulose  release rate

摘要:

目的 制备辛伐他汀凝胶骨架缓释片，对影响药物释放的因素进行考查。方法 采用紫外分光光度法测定其体外释放度，应用湿法制粒压片法制备缓释片，以羟丙基甲基纤维素(HPMC)为骨架材料，考察了HPMC规格、用量及其它辅料对药物释放的影响，并进行了正交实验优化及处方和制备方法的验证。结果 辛伐他汀缓释片的体外释放受HPMC规格、HPMC用量、粘合剂种类的影响，选择HPMC(K15M)为骨架材料，其与主药质量比为1.5∶1，所制缓释片能持续释药12 h，批间重现性良好。结论 该制剂处方合理，制备方法可行，具有良好的缓释效果。

Abstract:

OBJECTIVE To prepare gel matrix sustained-release tablets of simvastatin and examine the factors affecting drug release rates. METHODS Assay the release rates in vitro by UV spectrophotometry, prepare the sustained-release tablets by wet granulation squash method with hydroxypropyl methyl cellulose (HPMC) as matrix material, examine the impact on the release rates with the specification and quantity of HPMC and other excipients, optimize the formulation with orthogonal test method and validate the preparation method. RESULTS The specification and quantity of HPMC and the kind of adhesive can impact on the release rates in vitro. When the proportion of HPMC (K15M) as matrix material to simvastatin is 1.5∶1, the release of the sustained-release tablets can stably last 12 hours, and the release rates in batches have good reproducibility. CONCLUSION The formulation is appropriate, the preparation method is feasible, and the sustained-release tablets has good and stable release rate.