摘要
目的:优化伏立康唑磺丁基醚-β-环糊精包合物的制备工艺。方法:以包合时间、包合温度、伏立康唑与磺丁基醚-β-环糊精投料比3个因素为考察对象,利用Box-Behnken响应面优化法探究包合率受到上述三因素三水平的交互影响,建立模型进行二次多项式拟合。优化得到的包合物采用TLC及1HNMR进行初步验证。结果:确立了伏立康唑包合物制备最优条件为:包合温度30℃,包合时间1. 25 h,磺丁基醚-β-环糊精与伏立康唑投料比3∶1。此条件下制备包合物的包合率为96. 57%。TLC及1HNMR均证实了该包合物的形成。结论:优化了伏立康唑包合物的制备工艺,为工业化生产奠定了实验基础。
Objective: To optimize the preparation process of voriconazole sulfobutyl ether-β-cyclodextrin inclusion compound.Methods: Taking the inclusion time,inclusion temperature and ratio of voriconazole to sulfobutyl ether-β-cyclodextrin as the investigation factors,a Box-Behnken response surface optimization method was used to explore the inclusion rate affected by the above three factors with three levels of interaction. A model was established for the second polynomial fitting. The optimal inclusion compound was verified by TLC and1 HNMR preliminarily. Results: The optimal preparation conditions of voriconazole inclusion compound were as follows:the inclusion temperature was 30℃,the inclusion time was 1. 25 h,and the ratio of sulfobutyl ether-β-cyclodextrin to voriconazole was 3 ∶ 1. The inclusion rate of the prepared inclusion compound under the above optimal conditions was(96. 57) %. TLC and1 HNMR both confirmed the formation of the inclusion compound. Conclusion: The preparation process of voriconazole inclusion compound is optimized,which lays the experimental basis for industrial production.
作者
何文
卢朝薇
He Wen;Lu Zhaowei(Department of Pharmacy,Renmin Hospital of Wuhan University,Wuhan 430060,China;School of Pharmaceutical Sciences,Wuhan University)
出处
《中国药师》
CAS
2018年第12期2242-2246,共5页
China Pharmacist
作者简介
通讯作者:何文Tel:15342223266E-mail:hwzxd@163.com
