多西他赛热敏脂质体的制备及含量和包封率的测定  

Preparation of docetaxel-loaded thermosensitive liposomes and determination of its content and entrapment efficiency

作　　者：付盟[1,2] 龚伟[2] 张慧[2] 梅兴国[2] 

机构地区：[1]武汉工程大学化工与制药学院,武汉430073 [2]军事医学科学院毒物药物研究所,北京100850

出　　处：《军事医学》2012年第3期196-198,216,共4页Military Medical Sciences

基　　金：国家"973"计划资助项目(2009CB930305);国家重大新药创制科技重大专项资助项目(2009ZX09301-002)

摘　　要：目的制备多西他赛(DTX)热敏脂质体(docetaxel-loaded thermosensitive liposomes,DTL),建立其含量和包封率测定方法。方法采用薄膜分散法制备DTL并用高效液相色谱法(HPLC)测定脂质体中多西他赛的含量。采用高速离心法分离脂质体与游离药物并测定包封率。结果制备的DTL粒径均一,平均粒径为104 nm,相变温度为42.20℃。辅料和溶剂不干扰主药含量测定,线性范围为1.0～100.0μg/ml(r=1);多西他赛平均回收率为99.50%(RSD=0.65%)。药物在脂质体中的包封率大于98%。结论薄膜分散法可用于制备DTL。药物含量和包封率测定方法简便快速,准确可靠,专属性强。Objective To prepare docetaxel（DTX）-loaded thermosensitive liposomes（DTL） and establish a method for determination of the content and entrapment efficiency.Methods DTLs were prepared by the thin film hydration method.HPLC was used to determine drugs in DTL.The entrapment efficiency of DTL was determined,followed by high-speed centrifugation at 13 400×g for 15 min.Results DTLs appeared uniform and the mean particle size was 104 nm.The transition temperature（Tm） of DTL was 42.20 ℃.The excipients and solvents did not interfere with the assay.A good linear relationship was found between the peak area and the concentration of DTX in the range of 1.0-100.0 μg/ml（r= 1）.The average recovery was 99.50%（RSD=0.65%）.The entrapment efficiency of DTL exceeded 98%.Conclusion The thin fllm hydration method can be used for DTL preparation.The method is simple,accurate,reliable,sensitive and applicable for the determination of the content and entrapment efficiency of DTL.

关 键 词：多西他赛 脂质体 抗肿瘤药 热敏 HPLC 含量测定 包封率 

分 类 号：R944.9[医药卫生—药剂学] R979.1[医药卫生—药学]