响应曲面法优化长春西汀β-环糊精两亲性聚合物胶束的制备工艺  

Optimization of the Vinpocetine β-cyclodextrin Amphiphilic Copolymer Micelle Preparation Technology by Response Surface Methodology

作　　者：于丽萍[1] 黄淑玲[1] 刘意[2] 夏自花 任嘉琳 林翠翠 杨帆[1] 

机构地区：[1]广东药学院药科学院,广州510006 [2]广东药学院医药化工学院,广州510006

出　　处：《海峡药学》2016年第5期6-10,共5页Strait Pharmaceutical Journal

基　　金：广东省科技计划项目(编号:2013B021800091);广州市科技局科技重大专项(编号201300000046和201508010036);广州市科技计划项目(编号:201508010036)

摘　　要：目的采用响应曲面法优化设计长春西汀β-环糊精两亲性聚合物(VIP/β-CD-〔P(AA-co-MMA)-b-PNVP〕4)胶束的制备工艺。方法根据单因素考察结果,以挥发速度、挥发时间、药物用量、甲醇用量为自变量,以胶束中VIP的载药量为考察指标,采用响应曲面法设计优化载药胶束的制备工艺条件,模拟得到VIP/β-CD-〔P(AA-co-MMA)-b-PNVP〕4胶束中载药量的二次回归方程模型,确定制备胶束的最佳工艺组合。结果最佳组合工艺为挥发速度1148r·min-1,挥发时间2.3h,药物用量0.056g,甲醇用量34m L,采用该工艺制备的VIP/β-CD-〔P(AA-coMMA)-b-PNVP〕4胶束的平均载药量为24.14%。结论响应曲面法对优化设计VIP/β-CD-〔P(AA-co-MMA)-b-PNVP〕4胶束的制备工艺有实际指导价值。OBJECTIVE Response surface methodology is used to design the preparation technology of VIP / β-CD-〔P（ AA-co-MMA）-b-PNVP〕4micelle. METHODS Based on the single-factor results,the quadratic regression model for the drug loadings in the VIP / β-CD-〔P（ AA-co-MMA）-b-PNVP〕4micelle was established about the independent variables（ volatilization speed,volatilization time,the dosage of model drug,methanol dosage） and the investigation target（ the drug loading of VIP in the micelle） through response surface methodology to design the preparation technology of drug-loaded micelles. Then determine the optimal process combination for preparing the micelles. RESULTS The best combination of four factors was evaporation rate 1148r·min- 1,volatile time 2. 3h,dosage of drug 0. 056 g,the amount of methanol 34 m L. The average drug loading of VIP / β-CD-〔P（ AA-co-MMA）-bPNVP〕4micelles was 24. 14%. CONCLUSION It was worthy to design the preparation technology of VIP / β-CD-〔P（ AA-co-MMA）-b-PNVP〕4micelle by response surface methodology.

关 键 词：响应曲面法 β-环糊精两亲性聚合物 胶束 长春西汀 

分 类 号：R94[医药卫生—药剂学]