伊维菌素小单室脂质体工艺配方优化及质量分析

为获得高包封率的伊维菌素小单室脂质体,本研究对其制备工艺进行了优化,并选取超声波频率、超声时间、卵磷脂与胆固醇质量比、伊维菌素与卵磷脂质量比各因素进行正交交互作用考察,同时利用反相高效液相色谱法对各工艺配方组合下伊维菌素小单室脂质体的包封率进行了测定。结果显示,伊维菌素小单室脂质体的制备最佳配方和工艺组合为超声波频率200 kHz,超声时间6 min,伊维菌素与大豆卵磷脂质量比为1:10。经过优化组合,得到了较高品质的伊维菌素小单室脂质体,平均载药量达到(92.35±0.61)%,药物品质优良,且制备工艺简单可行。

Optimizing Process and Formula and Analyzing Quality for IvermectinSingle Unilamellar Vesicles

To obtain high entrapment rate of ivermectin single unilamellar vesicles.The study was aim to optimizing preparation process of ivermectin single unilamellar vesicles;we had selected some factors such as ultrasonic frequency,ultrasonic time,mass ratio of lecithin to cholesterol and mass ratio of ivermectin to lecithin to design orthogonal test L8(27),and we used RP-HPLC to determine the entrapment rate of ivermectin single unilamellar vesicles under every combination of process and formula.The results showed the optimal process and formula combination of ivermectin single unilamellar vesicles were as follows: the ultrasonic frequency was 200 kHz,the ultrasonic time was 6 minutes and the mass ratio of ivermectin to lecithin was 1∶10.We have obtained high qualitative ivermectin single unilamellar vesicles by optimization,the loading rate reach(92.35±0.61)%,the quality of drug is fine,the preparation process are simple and feasible.