草苔虫内酯冻干脂质体的制备及质量评价  

Preparation and quality evaluation of bryostatins freeze-dried liposomes

作　　者：俞园媛[1] 陈建明[1] 

机构地区：[1]第二军医大学药学院药剂学教研室,上海200433

出　　处：《第二军医大学学报》2006年第11期1254-1257,共4页Academic Journal of Second Military Medical University

基　　金：上海市科委中药现代化专项基金(05DZ19714-4)~~

摘　　要：目的：制备草苔虫内酯冻干脂质体，建立该脂质体的质量标准。方法：采用经典的旋转薄膜分散法制备草苔虫内酯脂质体，以氯仿为脂质溶媒，旋转蒸发挥干有机溶剂，水化后探针超声乳化，加入支撑剂后冻干即得。采用反相高效液相色谱法（RP—HPLC）测定草苔虫内酯冻干脂质体的含量，以Agilent C18为色谱柱，以甲醇一水75：25（0～38min），73．7：26．3（38～45min），79：21（45～48min）为流动相；柱温为25℃；流速为1.5ml／min；紫外检测波长为228nm。采用Zetasizer粒径测定仪测定脂质体粒径；采用离心超滤法测定脂质体的包封率。结果：草苔虫内酯冻干脂质体粒径大小均匀，平均粒径0．423μm；RP-HPLC法测定，在44～220μg／ml浓度范围内线性关系良好，r=0．9998；日内和日间精密度均良好（RSD〈2％）；高、中、低（88、110、132μg／ml）3个浓度的回收率分别为100．8％、98．4％、100．9％；最低检测限4．4ng；最低定量限为17．6ng；脂质体包封率达98．68％。结论：本制备方法适于制备草苔虫内酯脂质体，所建立的分析方法准确可靠，重现性好、操作简便、专属性强，符合质量测定要求。Objective：To prepare bryostatins freeze-dried liposomes and to establish a quality standard for the liposomes. Methods： Film dispersion technique was used to encapsulate bryostatins with liposomes. Chloroform was taken as the solvent and was volatilized by revolving. Emulsification was performed with the probe after hydration, then the supporting agent was added for freeze drying. An RP-HPLC method was developed to determine the freeze-dried liposome content. The separation was performed with a Agilent C18 Column and the mobile phase was methanol-water in gradient elution 75 ： 25 （0-38 min）, 73.7 , 26.3（38-45 min）, 79 ： 21（45-48 min） by a flow rate of 1.5 ml/min, with the UV detector set at 228 nm. Zetasizer was used to determine the size of liposomes and the entrapment efficiency was determined with centrifugal ultrafilter. Results： The freeze-dried liposomes were homogeneous and the mean diameter was 0. 423 μm. The standard curve was linear over the range of 44-220 μg/ml, r=0. 999 8. The intra-day and inter-day RSDs were less than 2.0%. The recoveries of the high, middle and low concentrations （88, 110, and 132 μg/ml） were 100.8% , 98.4% , and 100.9% , respectively. The detection limit was 4.4 ng, the quantitation limit was 17.6 ng, and the entrapment efficiency was 98.68%. Conclusion, The film dispersion technique is suitable for preparation of bryostatins liposomes. The method in this study is easy-to-use, accurate, and with good repeatability.

关 键 词：草苔虫内酯 脂质体 含量 包封率 

分 类 号：R944.9[医药卫生—药剂学]