正交试验优选二氢青蒿素脂质体的制备工艺.pdfVIP

正交试验优选二氢青蒿素脂质体的制备工艺 ＊ # 温 悦 ，孟德胜 ，毕小婷（第三军医大学大坪医院野战外科研究所药剂科，重庆市 400042） 中图分类号 R283.69；R283 文献标识码 A 文章编号 1001-0408（2010）43-4069-03 摘 要 目的：优选二氢青蒿素脂质体的制备工艺。方法：以大豆磷脂与胆固醇的质量比、脂质与药物的质量比、水合溶液的种类 为考察因素，以包封率为评价指标，利用正交试验优选制备工艺。结果：优选的工艺为采用薄膜-超声法，大豆磷脂与胆固醇的质 量比为5∶1，脂质与药物的质量比为5∶1，以0.9％NaCl 注射液为水合溶液。制得的脂质体形态均匀，包封率＞85％。结论：该制备 工艺和处方可以得到高包封率和稳定的二氢青蒿素脂质体。 关键词 二氢青蒿素；脂质体；包封率；质量评价；正交试验 Optimization of the Preparation Technology of Dihydroartemisinin Liposome by Orthogonal Test WEN Yue ，MENG De-sheng ，BI Xiao-ting （Dept. of Pharmacy ，Research Institute of Field Surgery ，Daping Hospital of Third Military Medical University ，Chongqing 400042，China ） ABSTRACT OBJECTIVE ：To optimize the preparation technology of dihydroartemisinin liposome. METHODS ：The preparation technology of dihydroartemisinin liposomes was optimized by orthogonal test with ratio of granulesten to cholesterol ，ratio of lipid to drugs and types of aqueous solution as factors and using encapsulation efficiency as index. RESULTS ：Film-ultrasound method was used to optimize the preparation method. The optimal preparation technology was as follows ：ratio of granulesten to cholesterol was 5∶1，ratio of lipid to drugs was 5∶1and 0.9％NaCl injection was used as aqueous solution. Prepared liposome was uniform in shape with encapsulation efficiency more than 85％. CONCLUSION ：The method can be used to prepare stable dihydroartemisinin liposome with high encapsulation efficiency. KEY WORDS Dihydroartemisinin ；Liposome ；Encapsulation efficiency ；Quality evaluation ；Orthogonal test 二氢青蒿素（dihydroartemisinin ，DHA ）是青蒿的提取物青 050106）；DHA （浙江义乌高登精细化工有限公司，批号： 蒿素及其衍生物在体内的活性代谢产物和有效成分，是一种 051028，纯度：99.3％）；其余试剂均为分析纯。 水溶性很好的青蒿素衍生物，其药理作用强度是青蒿素的4～ 2 方法与结果 [1] 8倍。研究表明 ，除有抗疟活性外，DHA 还可抑制细胞血管 2.1 制备方法选择 内皮