尼美舒利缓释片处方优化研究

Optimization of the Formula of Nimesulide Sustained-release Tablets

目的:优化尼美舒利缓释片的处方。方法:采用正交试验设计,以体外累积释放度为指标,以载药材料羟丙基甲基纤维素(HPMC)、乳糖、聚乙烯吡咯烷酮(PVP)K30无水乙醇溶液的处方用量作为影响因素,设计正交试验筛选缓释片的最佳处方,并进行处方验证试验。结果:优化处方为:HPMC100mg、乳糖50mg、5%PVPK30无水乙醇溶液3mL;以此处方制备的3批缓释片在12h累积释放度约为97%,未出现时滞、突释等现象,体外释药动力学符合零级方程。结论:尼美舒利缓释片处方合理,具有良好的缓释效果。

OBJECTIVE： To optimize the formula of Nimesulide sustained-release tablets. METHODS： The formula of Nimesulide sustained-release tablets was optimized by orthogonal design with accumulative release rate in vitro as index, and the amount of HPMC, lactose and PVP（K30） absolute alcohol solution as factors. Validation test was also conducted. RESULTS： The opti- mized formula was as follows： HPMC 100 mg, lactose 50 mg, 5% PVP K30 absolute alcohol solution 3 mL. The rate of in vitro accumulative drug release of 3 batches of samples was about 97% within 12 h, and there wash＇ t time-lag or sudden release phe- nomenon. The drug release in vitro could be well fitted with the zero-order equation. CONCLUSION： The formula of Nimesulide sustained-release tablets is reasonable. The prepared sustained-release tablets show well effect in vitro.