去氢骆驼蓬碱脂质体冻干剂粉的制备工艺优选  

Optimization of Preparation Process for Freeze-dried Powder of Harmine Liposome

作　　者：朱爱军[1] 陈维良[1] 杜昆泽[1] 贝永燕[1] 黄倩[2] 张学农[1] 

机构地区：[1]苏州大学药学院,09级本科生江苏苏州215123 [2]苏州医药科技学校,江苏苏州215009

出　　处：《抗感染药学》2013年第1期19-23,共5页Anti-infection Pharmacy

基　　金：国家自然基金资助项目(编号:81273463);江苏省科技支撑计划(BE2011670);国家大学生创新性试验计划课题资助(111028533;微机编号5731503311)

摘　　要：目的:制备含有不同冻干保护剂的N-三甲基壳聚糖(TMC)包衣去氢骆驼蓬碱脂质体(TMC-HM-LP)的冻干粉,并筛选其最佳制备工艺。方法:用"薄膜分散-pH梯度法"制备去氢骆驼蓬碱脂质体,并采用孵育包衣法、低温高速离心法和结合高效液相色谱(HPLC)定量方法测定其包衣脂质体的包封率;以其冻干粉的外观在冻干前和复溶后脂质体的粒径、包封率作为对比指标,优选出最佳的冻干工艺以及冻干保护剂的种类及比例。结果:以葡萄糖-乳糖-甘露醇(2:1:0.5)作为冻干保护剂,通过"分步预冻"的方法和-80℃冷冻干燥技术得到的TMC-HM-LP外观良好,冻干前后粒径和包封率变化较小。结论:采用冷冻干燥技术并结合冻干保护剂的优选,可显著提高包衣脂质体的稳定性。Objective:To prepare freeze-dried powder of N-trimethyl chitosan(TMC)-coated harmine liposome(TMC-HM-LP) containing different lyoprotectants for searching the optimization of preparation process.Methods:Harmine liposome was obtained through film dispersion-pH gradient method,and then coated by TMC through incubation.Encapsulation efficiency was measured by high-speed centrifuge method and quantificational technique of high performance liquid chromatography(HPLC).The appearance of freeze-dried powder,particle size and encapsulation efficiency before and after lyophilization were compared so as to optimize the process and lyoprotectants together with their ratios.Results:With an appropriate mass ratio of glucose-lactose-mannitol(2:1:0.5) and by the method of stepped pre-freezing before lyophilization,the obtained lyophilized product was of satisfactory appearance and less difference of particle size and encapsulation efficiency before and after lyophilization.Conclusion:The stability of prepared coated liposome was increased with the aid of adopting lyophilization technique and optimizing the lyoprotectants.

关 键 词：氢骆驼蓬碱 脂质体 冷冻干燥 保护剂 冻干粉 稳定性 

分 类 号：R943[医药卫生—药剂学]