羟喜树碱注射乳剂的制备及其灭菌稳定性研究

Preparation of Hydroxycamptothecin Emulsion for Inject and Its Stability After Sterilization

目的:制备羟喜树碱(HCPT)乳剂并考察不同油相、磷脂(PL)及灭菌条件对乳剂质量的影响。方法:采用高压均质法制备羟基喜树碱注射乳剂,考察不同种类油相、磷脂对乳剂包封率、粒径、ξ电位、游离脂肪酸和过氧化值的影响,采用正交试验优化处方,并选择最佳灭菌条件。结果:羟喜树碱乳剂的最佳处方为20%鱼油,2%PL-100M,制备温度80℃,均质压力700bar。所制备的乳剂平均粒径为190.6±20.1nm,包封率为89.4%,在121℃,15min灭菌条件下,乳剂的粒径、包封率、过氧化值和游离脂肪酸无明显变化。结论:羟喜树碱静脉鱼油乳剂包封率高、大小均匀并且能够耐受高压灭菌。

Objective： To study the effect of different Kinds of oil phase and phospholipids on the quality of hydroxycamptothecin （HCPT） emulsion, and to find the best sterilization condition for the emulsion. Method： High pressure homogenization method was used to prepare HCPT emulsion. The effects of different kinds of oil phase, phospholipids and sterilization methods on the quality of HCPT emulsion were evaluated. HCPT emulsion was investigated based on the parameters such as encapsulation efficiency （EN）, particle size, zeta potential, free fatty acids and peroxide value. Orthogonal design was used to optimize the experiment and the best sterilization condition was found. Result： The optimal formulation was consisted of 2% fish oil and 2% PL-100M. The preparation temperature was set at 80℃ and homogenization pressure was 700bar. The particle size and encapsulation efficiency were 190.6nm and 89. 4%, respectively. The mean particle size, EN%, free fatty acids and peroxide value had no obvious changes during 121℃, 15min sterilization. Conclusion： It is practical to prepare HCPT emulsion for injection with promising EN%, uniformal sizes. The emulsion is stable during high pressure sterilization.