星点设计——效应面法优化布洛芬缓释片的处方

Optimization of Ibuprofen sustained-release tablets by central composite design response surface methodology

目的采用星点设计——效应面法优化布洛芬缓释片的处方。方法以布洛芬为主药,乙基纤维素(ethyl cellulose,EC)为不溶性骨架缓释材料,聚乙烯吡咯酮(PVP K30)为致孔剂,滑石粉为润滑剂,采用粉末直压法制备布洛芬骨架缓释片。以布洛芬含量、EC与PVPK30的比值为考察因素,以1 h、6 h、12 h累积释放度为效应值优化该处方。结果按优化后的处方制备的布洛芬缓释片释放度为1小时10.54%,6小时61.63%,12小时100.75%,累积释放度与理论值的偏差较小,说明该模型具有良好的预测性。结论最终确定布洛芬缓释片每片的处方为:布洛芬170 mg、乙基纤维素7 mg、PVP K3021 mg、滑石粉2 mg。该处方应用本设计方法能实现多指标的同步优化,所建立的模型具有良好的预测性,可用于处方优化。

Objective:To optimize the formulation of sustained-release Ibuprofen tablets by central composite design-response surface method.Methods:Ibuprofen matrix sustained-release tablets were prepared with ibuprofen as the main drug,ethyl cellulose(EC)as insoluble matrix sustained-release material,polyvinyl pyrrolidone(PVP K30)as porogen and talcum powder as lubricant.The content of ibuprofen and the ratio of EC to PVP were used as the factors,and the cumulative release of ibuprofen at 1 h,6 h and 12 h were used as the response value to optimize the formulation.Results:the optimized formulation exhibited accumulative drug release as follows:10.54%in one hour,61.63%in six hours,100.75%in twelve hours,the deviation between the cumulative release rate and the theoretical value were small,which showed that the model had good predictability.Conclusion:The final formulation is as follows:170 mg of ibuprofen,7 mg of ethyl cellulose,21 mg of PVP K30 and 2 mg of talcum powder.Central composite design-response surface method can optimize multiple indexes simultaneously,which can be used for prescription optimization.