P物质多囊脂质体的制备工艺优化及相关性质考察  

Optimization of Preparation Technology and Property of Substance P Multivesicular Liposomes

作　　者：郭文治[1,2] 赖西南 王正国[1] 刘育杰[1] 黄晖[1] 王丽丽[1] 

机构地区：[1]第三军医大学大坪医院野战外科研究所/创伤、烧伤与复合伤国家重点实验室,重庆市400042 [2]北京军区总医院麻醉科,北京市100700

出　　处：《中国药房》2009年第10期767-769,共3页China Pharmacy

基　　金：国家重点基础研究规划基金资助项目(2005CB522603)

摘　　要：目的:优化P物质多囊脂质体的制备工艺,并考察其相关性质。方法:复乳法制备P物质多囊脂质体,以包封率为指标,磷脂与胆固醇的摩尔比(A)、超声乳化时间(B)、初乳与二相小的体积比(C)、辅助乳化剂的浓度(D)为因素进行正交试验设计,优化其制备条件;对优化条件所制脂质体进行包封率、粒径分布、体外释药性能、相转变温度和熔点的考察。结果:优化制备条件A为2:1,B为30 s,C为1:2,D为2%;所制多囊脂质体包封率可达85%,粒径分布为0.75～27.75μm,在生理盐水中释药t_(1/2)=11 h,可持续72 h释药,相转变温度为34℃,熔点为110℃。结论:所制P物质多囊脂质体包封率高,物理性能稳定,是一种较为理想的缓释制剂。OBJECTIVE： To optimize the preparation technology of substance P multivesicular liposomes （Depo-SP） and investigate its property. METHODS： Depo-SP was prepared by multiple emulsion method, with encapsulation efficiency taken as index, molar ratio of phospholipid to cholesterol （A）, ultrasound emulsification time （B）, volume ratio of colostrum to two-phase water （C） and coemulsifier concentration （D） as factors to design the orthogonal experiment for optimizing the preparation technology. The encapsulation efficiency, distribution of particle size, in vitro drug release profiles, phase transition temperature and melting point of the optimized preparation were determined. RESULTS： The optimized preparation conditions of Depo- SP were as follows： A = 2 ： 1, B = 30 s, C = 1 ： 2 and D = 2%. The encapsulation efficiency of the preparation reached 85% ; the particle size stood at 0.75-27.75 μm; the SP release in normal sodium was t 1/2 = 11 h and the sustained release maintained for 72 hours; the phase transition temperature was 34 12 and the melting point was 110 ℃.ONCLUSION： The prepared Depo-SP had high encapsulation efficiency and stable in physical property, and it is an ideal sustained release preparation.

关 键 词：P物质 多囊脂质体 制备 

分 类 号：R943[医药卫生—药剂学] R977[医药卫生—药学]