洛伐他汀-β-环糊精包合物的制备和评价  

Preparation and Evaluation of Lovastatin-β-cyclodextrin Inclusion Compound

作　　者：刘会芳[1] 赵燕燕[2] 杜光玲[2] 谢奇明[3] 梁兴华[3] 

机构地区：[1]河北大学卫生职业技术学院,河北保定071000 [2]河北大学医学实验中心,河北保定071000 [3]河北大学药学院,河北保定071000

出　　处：《中国现代应用药学》2009年第2期127-130,共4页Chinese Journal of Modern Applied Pharmacy

基　　金：河北省科技攻关项目(42761220);河北省中医药管理局资助项目(05015);河北大学人才引进项目(y2004039);河北大学自然科学基金资助项目(2005Y08)

摘　　要：目的优选洛伐他汀-β-环糊精(β-CD)包合物的制备工艺,提高洛伐他汀的溶出速率和生物利用度。方法用饱和溶液法制备包合物,并用正交设计法对洛伐他汀与β-CD摩尔比(A)、温度(B)、搅拌时间(C)、速度(D)四因素进行优化,得出洛伐他汀-β-环糊精包合物的最佳制备条件。结果根据包合物收率和药物利用率,得出洛伐他汀-β-环糊精最佳包合条件为:洛伐他汀:β-环糊精为1:3,包合温度为50℃,包合时间为3h,搅拌速度为300r.min-1。结论该包合工艺可提高洛伐他汀的溶出速率,工艺简便易行。OBJECTIVE To optimize the preparation technology for the inclusion compound of lovastatin-β-cyclodextrin and improve its solubility and bioavailability. METHODS The inclusion compound was prepared with the saturated solution method, and anorthogonal test was used to optimize four factors： LT： β-CD, temperature, stirring time and speed. And the conditions for the technology of preparation was obtained. RESULTS According to the inclusion compound yield and the drug utilization rate. The optimal condition for the inclusion compound of the drug were： lovastatin： β-cyclodextrin = 1： 1; time for inclusion： 5 h; Inclusion temperature： 60 ℃; stirring time： 300 r·min^-1. CONCLUSION This inclusion technology could improve the solubility of lovastatin in the inclusion compound. And this optimized process is simple and efficient.

关 键 词：洛伐他汀 Β-环糊精 包合物 正交设计 

分 类 号：R943.4[医药卫生—药剂学]