摘要
采用乳化法制备青蒿酯多层脂质体,脂质体带正电荷时其包裹率明显高于中性或带负龟荷时。类脂中胆固醇含量及加入α-生育酚对包裹率均无明显影响,最佳处方组成的包裹率为13.63±0.09%。采用冷冻干燥技术可获得稳定性较好的脂质体冻干品,且其结构粒径均无明显变化。通过微孔滤膜压滤,能有效地除去94%以上的游离药物。比较了青蒿酯及其脂质体在动物体内的抗疟作用,结果表明,后者对鼠疟原虫的抑制率明显地高于前者。
The encapsulation efficiency(EE)of positively charged artesunate
liposomes prepared by emulsification was much higher than those of neutral and
negatively charged liposomes.The content of cholesterol and α-tocopherol had no
significant effect on EE.The best formulation afforded EE of 13.63±0.09%.
The multilamellar structure and vesicle size were not changed apparently after
freeze-drying.More than 94% of free artesunate was removed from liposomes by
millipore filter membrane separation.Comparative test in mice proved that the
liposomes had greater efficacy against malaria than artesunate itself.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
1992年第2期62-72,共11页
Chinese Journal of Pharmaceuticals
关键词
青蒿酯
脂质体
乳化法
冷冻干燥
artesunate
liposome
emulsification method
freeze-drying
