星点设计-效应面法优化双嘧达莫包合物制备工艺  

Optimization of preparation of dipyridamole-β-cyclodextrin inclusion complex by central composite design and response surface methodology

作　　者：李玉静[1] 

机构地区：[1]山东中医药大学第二附属医院药剂科,山东济南250001

出　　处：《中国医院药学杂志》2015年第2期129-132,共4页Chinese Journal of Hospital Pharmacy

摘　　要：目的:星点设计-效应面法优化双嘧达莫(DIP)-β-环糊精(β-CD)包合物制备工艺。方法:以饱和水溶液法制备DIP-β-CD包合物,采用星点设计优化制备工艺,以β-CD/DIP质量比、包合时间和包合温度为自变量,包合率为因变量,分别进行多元线性回归和二项式方程拟合,优选最佳处方工艺并进行验证。结果:二项式方程拟合度较高(r2=0.911 3,P<0.001),预测性好;效应面法优选最佳工艺条件为β-CD/DIP质量比5.7,包合时间5.5 h,包合温度50℃;最佳工艺验证偏差均<5%,所得包合物溶解度及释药速度均提高。结论:应用星点设计-效应面优化法能够精确有效地优化DIP-β-CD包合物制备工艺,且最优工艺稳定可行,可用于工业生产。OBJECTIVE To optimize the preparation of dipyridamole（DIP）-β-cyclodextrin（β-CD）inclusion（DIP-β-CD inclusion）complex by central composite design and response surface methodology.METHODS DIP-β-CD inclusion complex was prepared by using saturated aqueous solution method and the preparing method was optimized by central composite design.With the mass ratio ofβ-CD/DIP,inclusion time and temperature as the independent variables and the inclusion rate as the dependent variable,the binomial and linear equations were fitted respectively to the data,to choose and verify the best prescription process.RESULTS The correlation coefficient of second-order quadratic model was higher and the prediction was better（r2=0.911 3,P〈0.01）;The optimum conditions for preparation of DIP-β-CD inclusion complex were as follows：mass ratio ofβ-CD/DIP5.7,inclusion time 5.5 h,inclusion temperature at 50℃.The deviation between the results of the best craft verification test was less than 5%,and the solubility and release velocity were all improved for the obtained inclusion complex.CONCLUSION Central composite design and response surface methodology can precisely and effectively optimize the preparation of DIP-β-CD inclusion complex.The optimized process is stable and feasible,and can be used for the industrial production.

关 键 词：双嘧达莫(DIP) β-环糊精(β-CD) 包合率 星点设计 效应面 

分 类 号：R943[医药卫生—药剂学]