紫杉醇口服自乳化给药系统的处方研究

Preparation of paclitaxel self-emulsifying drug delivery system

通过对油相、水、乳化剂、助乳化剂的选择和配比优化,成功地将紫杉醇包埋在乳液中,由伪三元相图得到相应的微乳区域,并结合自乳化速率、粒径、Zeta电位及紫杉醇溶解性能的研究,来筛选处方,最终确立微乳的较优配方为:十四酸异丙酯∶(聚氧乙烯蓖麻油∶正丁醇))(3∶7(4∶1)).并以简便、快捷的高效液相色谱法(HPLC)测定紫杉醇在微乳中的含量.制备的紫杉醇微乳液为泛乳光的澄清透明液体,透射电镜下观察为球状液滴,平均粒径均小于50 nm.

The recipe of paclitaxel microemulsion formation was optimized by studying the pseudo- ternary phase diagram, the micro-emulsifying rate, Zeta potential and particle size. Paelitaxel was successfully embedded in the SEDDS microemulsion, and the optimized prescription was isopropyl myristate as oil, Cremophor-EL as surfactant, Butyl alcohol as co-surfactant （with the surfaetant ： Co-surfactant ratio 4 ： 1, oil ： （surfactant ＋ Co-surfactant） ratio 3 ： 7）. The HPLC method was established to determine the concentration of paclitaxel in SEDDS. The prepared microemulsions were kinds of clarity solution and they presented small spherical drops under electron microscopy, with the average diameter less than 50 nm after diluting with water.