星点设计-效应面法优化钩藤碱缓释片处方

Optimizaton on recipe of rhynchophylline sustained release tablet by central composite design and response surface methodology

目的优化钩藤碱缓释片处方,为该制剂的工业化生产提供参考。方法在单因素考察的基础上以释放度为指标,采用星点设计-效应面法,考察骨架材料羟丙甲基纤维素(HPMC)、阻滞剂乙基纤维素(EC)、黏合剂聚乙烯吡咯烷酮(PVP)的质量比对释放度的影响,筛选钩藤碱缓释片最优处方。结果最优处方:钩藤碱:9.5%,HPMC:19%,EC:7%,PVP:2.2%,淀粉:61.5%,滑石粉:0.8%,按优化后的处方工艺制备的钩藤碱缓释片无突释效应且12 h释放度>84%。结论钩藤碱缓释片处方合理,能满足缓释制剂的要求,可为制剂工业化提供参考。

Objective To optimize the recipe of rhynchophylline sustained release tablet in order to provide a reference for industrial production of the formulation. Method With the release degree as index,the influences of single factors on the release,such as hydroxypropyl methyl cellulose（HPMC）used as an skeleton materials,ethyl cellulose（EC）as blockers and the mass fraction of polyvinylpyrrolidone（PVP）as adhesive,were evaluated to screen the optimal preparation by central composite design and response surface methodology based on the single factor investigation. Result The optimal preparation was as follows：rhynchophylline 9.5%,HPMC：19%,EC：7%,PVPP：2.2%,starch：61.5% and talcum powder：0.8%. The sustained release tablet prepared by the optimized recipe of rhynchophylline had no sudden release effect and the release degree in 12 h was more than 84%. Conclusion The optimized recipe is reasonable and meets the requirements of sustained release formulation,which means it can provide a reference for industrial production of the formulation.