前列地尔微乳处方及制备工艺的优化  

Optimization of Preparation of Alprostadil Microemulsions

作　　者：刘洁[1] 杨亚妮[1] 何军[1] 卞玮[1] 李晓燕[1] 

机构地区：[1]中国医药工业研究总院药物制剂国家工程研究中心,上海200437

出　　处：《中国医药工业杂志》2015年第6期586-591,共6页Chinese Journal of Pharmaceuticals

基　　金：上海市科委2012年度"科技创新行动计划"纳米科技专项:前列地尔固态纳米乳工程化制备技术研究及安全性评价(12nm0502500)

摘　　要：结合预试验结果，首先确定前列地尔微乳的处方组成，再通过星点设计．效应面法和绘制电导率一含水量曲线，确定了前列地尔微乳处方中各组分的优化用量；最后以粒径和药物含量为指标，优化了微乳制备时的搅拌速度、时间和温度等工艺参数。结果表明，前列地尔微乳优化处方为：Solutol HS 158％、蛋黄卵磷脂2％、中链甘油三酸酯4％、甘油6％和水80％；制备时搅拌的速度、温度和时间分别为300r／min、30℃和0．5h。照上述优化处方制备的3批前列地尔微乳粒径均约23～25nm，且离心稳定性好。Based on the result of pre-test, the compositions of alprostadil microemulsions were decided. The amounts of these compositions were optimized by central composite design-response surface methodology and drawing the profiles of conductivity-water content. The process parameters, such as stirring speed, temperature and time, were optimized with particle size and drug content as indexes. The results showed that the optimal microemulsions were composed of 8% Solutol HS 15, 2% lecithin, 4% medium chain triglyceride, 6% glycerol and 80% water, and were prepared at 30 ℃ with the stirring speed of 300 r/min and for 0.5 h. The mean diameters of three batches of alprostadil microemulsion prapared according to the above results were all in the range of 23 - 25 nm, and all samples demonstrated good centrifugal stability behaviors.

关 键 词：前列地尔 微乳 星点设计-效应面法 电导率-含水量曲线 

分 类 号：R944.9[医药卫生—药剂学]