丹皮酚-羟丙基-β-环糊精包合物的制备及处方工艺优化

Preparation of Paeonol-HP-β-cyclodextrin Inclusion Compound and Its Prescription Technology Optimization

目的:制备丹皮酚-羟丙基-β-环糊精(PAE-HP-β-CD)包合物,优化其处方工艺。方法:采用冷冻干燥法制备PAE-HP-β-CD包合物并进行验证。以包合率为指标,主药-辅料投料比、包合时间、包合温度与搅拌速度为因素,采用星点设计-响应面法优化其处方工艺。结果:制备的PAE-HP-β-CD包合物发生了物相转变。最优处方工艺为主药-辅料投料比3.39∶1、包合温度50℃、包合时间3.2 h、搅拌速度350 r/min;所制得包合物的包合率测得值(87.46%)与预测值(89.12%)的相对误差为1.86%(n=6)。结论:成功制得PAE-HP-β-CD包合物,且其处方工艺稳定可行。

OBJECTIVE： To prepare paeonol-HP-β-cyclodextrin （PAE-HP-β-CD） inclusion compound and to optimize its pre- scription technology. METHODS： PAE-HP-β-CD was prepared by freeze drying method and validated. Using inclusion rate as in- dex, main drug-accessory ratio, inclusion time, inclusion temperature and stirring speed as factors, the preparation technology was optimized by central composite design-response surface methodology. RESULTS： Prepared PAE-HP-β-CD underwent phase transfor- mation. The optimal inclusion technology was as follows as main drug-accessory ratio of 3.39 ： 1, inclusion temperature of 50℃, inclusion time of 3.2 h, stirring speed of 350 r/min. Relative error between measured value （87.46%） and predicted value （89.12%） of inclusion rate was 1.86% （n=6）. CONCLUSIONS： PAE-HP-β-CD inclusion compound is prepared successfully, and its prescriotion technology is stable and feasible.