哈西奈德脂质体制备方法的选择及其含量与包封率的测定  

Selection of Preparation Method and Determination of Content and Entrapment Efficiency of Halcinonide Liposome

作　　者：李志平[1] 梁庆[1] 刘文彬[2] 王晖[2] 

机构地区：[1]广东省皮肤性病防治中心药剂科,广东广州510500 [2]广东药学院中药药理学教研室,广东广州510006

出　　处：《今日药学》2011年第6期332-334,共3页Pharmacy Today

基　　金：广东省医学科研项目(编号:A2010110)

摘　　要：目的选择制备哈西奈德脂质体的方法并测定其含量与包封率。方法采用注入法、冻融法、薄膜分散法制备哈西奈德脂质体;用超速离心法分离游离药物;高效液相色谱法测定含量与包封率。结果冻融法、注入法、薄膜分散制备的脂质体哈西奈德含量分别为99.23%±0.13%,98.37%±0.19%,99.36%±0.16%;包封率分别为83.17%±2.21%,77.19%±1.37%,87.28%±1.49%。在选定的色谱条件下,哈西奈德与辅料能完全分离,在4~40 mg/L范围内,药物浓度与峰面积呈良好线性关系（r=0.999 9）,平均回收率为101.02%,RSD为0.64%。结论薄膜分散法制备的脂质体包封率较高;超速离心-高效液相色谱法操作简便、准确、重复性好,可用于测定哈西奈德脂质体的含量和包封率。Objective To select the preparation method of halcinonide liposome,and determine the content and entrapment efficiency of it.Methods Halcinonide liposome was prepared with injection method,freeze-thaw method,and film hydration method.The free drug was isolated with the ultracentrifugation.The content and encapsulation efficiencies were determined by HPLC.Results The content of halcinonide liposome preparated with freeze-thaw method,injection method,film hydration method was 99.23%±0.13%,98.37%±0.19%,99.36%±0.16%,respectively.The encapsulation efficiencies of halcinonide liposome preparated with freeze-thaw method,injection method,film hydration method was 83.17%±2.21%,77.19%±1.37%,87.28%±1.49%,respectively.Halcinonide had a good linearity within the range of 4～40 mg/L（r=0.999 9）.The average recovery rate was 101.02%,RSD=0.64%.Conclusion The drug-loading efficiency and encapsulation efficiencies of halcinonide liposome preparated with film hydration method are better than that of other methods.The ultracentrifugation-HPLC method is convenient,accurate,repeatable,and suitable for determination of the content and entrapment efficiency of halcinonide liposome.

关 键 词：哈西奈德 脂质体 注入法 冻融法 薄膜分散法 包封率 

分 类 号：R943[医药卫生—药剂学]