紫杉醇微乳的研究  

Studies on paclitaxel microemulsion

作　　者：阎家麒[1] 王惠杰[1] 童岩[1] 臧莹安[1] 王九一[2] 

机构地区：[1]郑州牧业工程高等专科学校,郑州450008 [2]河南省分析测试中心,郑州450003

出　　处：《中国药学杂志》2000年第3期173-176,共4页Chinese Pharmaceutical Journal

摘　　要：目的 :研究紫杉醇微乳的制备 ,稳定性和静注、口服的生物利用度。方法 :聚乙二醇 (EPC) ,紫杉醇和PEG DSPE的氯仿溶液在氮气流下减压成膜 ,加入经水化超声处理的玉米油 ,进一步超声处理后 ,通过微流化器使其微乳化。结果 :粒径 5 0～1 0 0nm ,包封率≥ 99.2 % ,兔绝对生物利用度 :静注 1 0 7.7% ,口服 2 2 .4%。结论 :本实验研究为开发紫杉醇新型静注和口服制剂提供了科学依据。OBJECTIVE:To study the preparation of microemulsion containing paclitaxel for both intravenous and oral administration,its stability and bioavailability.METHODS:Corn oil was hydrated and sonicated.EPC,paclitaxel and PEG DSPE were combined in CHCl 3.A thick lipid film was obtained after drying under a stream of N 2 and vacuum evacuation.The hydrated oil was added directly to the thin phospholipid film,vortexed and then sonicated.The mixture was passed through the Microfluidizer for microemulsified.RESULTS:The particle size was 50～100 nm,the encapsulation efficiency was ≥99.2% and the absolute bioavailability of intravenous and oral adminstration was 107.7% and 22.4%,respectively.CONCLUSION:This study developed a new formulation for paclitaxel.It will provide a scientific basis of the intravenous and oral administiation of paclitaxel.

关 键 词：紫杉醇 微乳 生物利用度 稳定性 

分 类 号：R979.1[医药卫生—药品]