基于响应曲面法优化粉末直压工艺制备杠柳多苷片

Preparation of Periploca sepium periplosides tablets by optimizing powder direct compression process based on response surface methodology

目的:基于响应曲面法优化粉末直压工艺制备杠柳多苷片。方法:以杠柳多苷为原料,在单因素筛选的基础上,采用Box-Behnken设计,以乳糖与微晶纤维素(MCC)的比例、二氧化硅用量、硬脂酸镁用量作为试验因素,考察其对片剂硬度、崩解时限、脆碎度、片重差异以及黏冲情况的影响,并采用响应曲面法研究杠柳多苷片的最佳制剂处方。结果:利用Design Expert软件拟合模型分析,获得最佳的制剂辅料处方为:乳糖与MCC配比1∶2,二氧化硅用量1%,硬脂酸镁用量1%。验证实验显示,3批样品的实验评分与预测评分接近。结论:优化得到的制剂处方可明显改善物料流动性差和黏冲等问题,制得的片剂符合质量要求且外观较好。

Objective: To prepare Periploca sepium periplosides(PePs) tablets by optimizing powder direct compression process based on response surface methodology. Methods: PePs was used as the raw material. Based on the single factor screening, Box-Behnken design was performed. The ratio of lactose to microcrystalline cellulose(MCC), the amount of silicon dioxide and the amount of magnesium stearate were taken as the test factors, and their effects on tablet hardness, disintegration time, friability, tablet weight difference and viscosity were investigated. And the response surface methodology was used to study the best preparation formula of PePs tablets. Results: Using Design Expert software for fitting model and analysis, the obtained best formula of excipients was as follows: the ratio of lactose to MCC was 1∶2, the amount of silicon dioxide was 1%, the amount of magnesium stearate was 1%. Verification experiments showed that the experimental scores of three batches of samples were close to the predicted scores. Conclusion: The optimized preparation formula can obviously improve the poor fluidity and viscosity of materials, and the obtained tablets meet the quality requirements with good appearance.