紫杉醇静脉注射脂肪乳配方及制备工艺的考察

Study of the Formulas and Preparation Technology of Intravenous Fat Emulsion Containing Paclitaxel

考察三种紫杉醇脂肪乳配方的时间及温度稳定性、制备工艺对其粒径的影响以及测定脂肪乳中紫杉醇的浓度,光子相关光谱法（PCS）测试结果表明,以单一F-68作为乳化剂的脂肪乳粒径为235±15nm,PDI为0.2±0.1,Zeta电位为-35±10mV,在室温（25℃）下放置60d粒径变化不明显,较含有92%、98%蛋黄卵磷脂的脂肪乳稳定;随着高压均质压力升高,脂肪乳的粒径减小,高压均质循环次数对粒径几乎无影响;4000r/min条件下离心15min不分层,说明脂肪乳具有良好的离心稳定性。高效液相色谱（HPLC）结果表明,脂肪乳中紫杉醇的浓度为0.291mg/mL,提高初始加入量后浓度可达0.673mg/mL。

Compare the time and temperature stability among three formulas of fat emulsion containing Paclitaxel, and study the influence of the preparation technology on the size and determine the concentration of the Paclitaxel in the fat emulsion. The PCS test revealed that the size of the fat emulsion of F-68 was 235 ± 15 nm with the polydispersity （PDI） ranged from 0.2 ± 0.1 and the Zeta potential was-35 ± 10 mV. The change of the size of the F-68 formula was not significant at room temperature （25℃） over 60 days, which implied this formula had better stability than the 92% yolk lecithin plus F-68 formula and the 98% yolk lecithin plus F-68 formula. The size of the fat emulsion decreased with the increasing of the homogenization pressure. However, it didn＇t change a lot with the additional number of the homogenization cycles. The centrifugal study showed that fat emulsion could have good centrifugal stability under 4000r/min, 15min conditions. The HPLC result showed the concentration of the Paclitaxel in the fat emulsion was 0.291mg/mL and it could reach 0.673 mg/mL by increasing the initial loading.