丹皮酚-羟丙基-β-环糊精包合物的制备及处方工艺优化

摘要

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 prescription technology is stable and feasible.%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。