环孢素A亚微乳的制备及其性质考察  

Preparation and physic-chemical property of Cyclosporine submicroemulsion

作　　者：叶林茂[1] 苏冰[2] 王东凯[1] 李翔[1] 王雪丽[3] 温洪德[3] 刘丹丹[1] 

机构地区：[1]沈阳药科大学药学院,沈阳110016 [2]白求恩医科大学制药厂,长春130012 [3]沈阳军区总医院,沈阳110016

出　　处：《中国新药杂志》2009年第4期360-364,共5页Chinese Journal of New Drugs

摘　　要：目的:制备环孢素A亚微乳并对其性质进行考察。方法:本实验通过正交试验设计优选了环孢素A亚微乳的最佳处方及制备工艺,并通过粒径、Zeta电位、包封率的测定研究了环孢素A亚微乳的性质。结果:环孢素A亚微乳的最佳处方工艺组合为磷脂1.5%,泊洛沙姆188为0.3%,高速剪切乳化时间为6min,制备温度为70℃。所制备的乳剂Zeta电位为-29.5mV,平均粒径为140nm,包封率为98.30%和97.76%。结论:本实验制备的环孢素A亚微乳满足静脉注射用制剂要求。Objective：To prepare Cyclosporine （CsA） submicroemulsion and investigate its physic-chemical properties, nethods：Orthogonal experiment was designed to optimize the formulation and preparation condition of CsA submicroemulsion. The content of the preparation were determined by HPLC, and its properties such as particle size,Zeta potential, pH value and entrapment efficiency were studied. Results：The optimal formulation and preparation condition of CsA submicroemulsion were as follows：egg phospholipids 1.5% , poloxamer 188 0.3% , the high speed shearing emulsification time was 6 min and the preparation temperature was 70 ℃. The mean entrapment efficiency of 3 batches of CsA submicroemulsions was 98.30 % and 97.76% ,with Zeta potential of -29.5 mV and mean particle size of 140 nm. Conclusion：The prepared CsA submicroemulsion was up to the standards of intravenous injection preparations.

关 键 词：环孢素A 亚微乳 粒径 ZETA电位 包封率 

分 类 号：R943.4[医药卫生—药剂学] R979.5[医药卫生—药学]