Box-Behnken效应面法优化多西他赛微乳注射液制备工艺.PDF

Box-Behnken 效应面法优化多西他赛微乳注射液制备工艺 1＊ 2# 果秋婷 ，张小飞 （1.咸阳职业技术学院医学系，陕西咸阳 712000；2.陕西中医学院药学院陕西省中药制药 重点学科，陕西咸阳 712046） + 中图分类号 R944.11 文献标志码 A 文章编号 1001-0408（2013）29-2742-04 DOI 10.6039/j.issn. 1001-0408.2013.29.20 摘 要 目的：优化微乳制备工艺，制备多西他赛微乳注射液。方法：采用高压均质法制备多西他赛微乳，以制备温度、均质压力 和均质次数为考察对象，以粒径分布、多分散系数和包封率为评价指标，采用Box-Behnken 效应面法优化多西他赛微乳的制备工 艺；采用Mastersizer 粒度仪测定微乳的粒径分布，考察多分散系数及Zeta 电位，透射电镜考察其形态。结果：多西他赛微乳优化工 5 艺为制备温度61 ℃，均质压力860×10 Pa ，均质次数7次；所得微乳的粒径为（221.6±13.4）nm ，多分散系数为0.092±0.003，Zeta 电位为－30.3mV ，包封率为（93.4±2.1）％；透射电镜显示微乳粒径均一，呈球状分布。结论：多西他赛微乳制备工艺采用 Box-Behnken 效应面法优化是有效、可行的。 关键词 多西他赛微乳注射液；制备；高压均质法；Box-Behnken 效应面法 Optimization of the Preparation Technology of Docetaxel Microemulsion Injection by Box-Behnken Design and Response Surface Method 1 2 GUO Qiu-ting ，ZHANG Xiao-fei （1.Dept. of Medicine ，Xianyang Vocational Technical College ，Shaanxi Xian- yang 712000，China ；2.College of Pharmacy ，Shaanxi University of TCM ，Shaanxi Key Disciplines of TCM Preparation ，712046，China ） ABSTRACT OBJECTIVE ：To optimize the preparation technology of microemulsion ，and to prepare Docetaxel microemulsion in- jection. METHODS ：Docetaxel microemulsion was prepared using high pressure homogenization. The preparation technology of Docetaxel microemulsion was optimized by Box-Behnken design and response surface method with preparation temperature ，homog- enization pressure and homogenization times as factors using particle size distribution ，polydispersity index and entrapment efficien- cy as index. The distribution of particle size ，polydispersion index and Zeta potential were determined by Mastersizer particle ana- lyzer ；the morphology of Docetaxel microemulsion was observed under TEM. RESULTS ：Optimized preparation technology was as