【摘要】 目的以星点设计-效应面法筛选并优化硝苯地平缓释微丸包衣处方,量化Eudragit RL/RS用量及比例与释放度之间的关系,为硝苯地平缓释微丸胶囊的研究提供参考。方法采用层积上药法制备含药丸芯,流化床包衣制备缓释微丸。以释放度作为考察指标,将Eudragit RL/RS比例和包衣增重为自变量,采用星点设计-效应面法优化包衣处方,并对模型进行验证。结果包衣液中Eudragit RL/RS的配比、包衣增重量对释放度影响显著。二次方模型是描述指标与因素之间的最佳模型。当Eudragit RL/RS的包衣增重量为15%,Eudragit RL/RS的配比为4:6时,制备的硝苯地平缓释微丸能维持12 h持续释药,释药速率实测值与预测值的偏差<10%。结论星点设计-效应面法可用于硝苯地平缓释微丸包衣处方的优化,所建模型具有较好的预测能力和实用性。更多还原

【Abstract】 Objective To prepare nifedipine sustained release pellets with blends of Eudragit RL and Eudragit RS as sustained coating material and optimize the coatine formulation with central composite design-response surface methodology. Methods The core pellets, which contained the drug, were prepared by suspension layering. The pellets were coated with a fluidized bed coating equipment. Drug release from the coated pellets were used as responses and central composite design-response surface methodology was applied to optimize sustained coating formulation, namely Eudragit RL/RS ratio and polymer load(weight gain), which were based on single factor tests. Results The single factor study indicated that the ratio and weight gain of Eudragit RL/RS greatly affected the in vitro drug release. The relationship between dependent and independent variables was best fitted to second-order polynomial equation. Nifedipine sustained-release pellets were successfully prepared which showed 12 h release in vitro when the ratio and weight gain of Eudragit RL/RS were 15% and 4 :6, respectively, and its observed values agree well with model predicted values. Conclusion The central composite design-response surface methodology can be applied to optimize the coating formulation for nifedipine sustained-release pellets, and the models constructed in this study was proved to be feasible.更多还原