替加环素脂质体的制备工艺研究  

Study on preparation technology of tigecycline liposomes

作　　者：徐艳艳[1] 郑丽君 张霞燕[1] 吴振波[1] 朱延焱[1] 王海翔 田吉来 XU Yanyan;ZHENG Lijun;ZHANG Xiayan;WU Zhenbo;ZHU Yanyan;WANG Haixiang;TIAN Jilai(The Central Hospital of Lishui City,Lishui 323000,China;College of Technology,China Pharmaceutical University,Nanjing 210009,China;School of Medicine&Holistic Integrative Medicine,Nanjing University of Chinese Medicine,Nanjing 210023,China)

机构地区：[1]丽水市中心医院,浙江丽水323000 [2]中国药科大学工学院,江苏南京211198 [3]南京中医药大学医学院·整合医学学院,江苏南京210023

出　　处：《药学研究》2021年第11期730-734,770,共6页Journal of Pharmaceutical Research

基　　金：浙江省自然科学基金资助项目(No.LY18H300007、LYY19H280004);丽水市高层次人才培养资助项目(No.2018RC06);中华医学会临床药学分会-吴阶平医学基金会科研基金资助项目(No.LCYX-Q014)。

摘　　要：目的本试验采用薄膜分散法制备替加环素脂质体。方法以胆脂比、药脂比、水化温度为影响因素,以包封率及载药量为考察指标,通过单因素试验和响应曲面试验设计法,研究替加环素脂质体的最优制备工艺。结果替加环素脂质体的最佳制备工艺为:水化温度60℃、药脂比1∶30、胆脂比1∶5,在此条件下制备的替加环素脂质体的包封率为73.07%,载药量为3.00%。结论所选工艺可用于制备替加环素脂质体。Objective To prepare tigecycline liposomes by thin film dispersion method.Methods The optimal preparation process of tigecycline liposome was studied by single factor test and response surface methodology(RSM)with encapsulation efficiency and drug loading as indexes.The cholesterol-lipid ratio,drug-lipid ratio and hydration temperature as influencing factors were used to optimize process.Results The optimal process of preparation of tigecycline liposome was as follows:hydration temperature 60℃,drug-lipid ratio 1∶30,cholesterol-lipid ratio 1∶5.Under these conditions,the encapsulation efficiency and drug loading capacity of tigecycline liposome were 73.07%and 3.00%,respectively.Conclusion The optimizes process can be used to prepare tigecycline liposome.

关 键 词：替加环素 脂质体 薄膜分散法 大豆磷脂 胆固醇 

分 类 号：R944.9[医药卫生—药剂学]