优福定脂质体的处方与工艺优化

目的:优化优福定脂质体的处方和制备工艺。方法:采用薄膜分散-冷冻干燥法制备优福定脂质体,以主药替加氟和尿嘧啶包封率为指标,应用正交试验优化其处方和制备工艺;考察其体外释放度并与普通片剂进行比较。结果:所得优化处方为磷脂与药物的重量比16∶1,磷脂与胆固醇的重量比7∶1,pH5.6的磷酸盐缓冲液为水合递质,水化温度为40℃。在此条件下,替加氟和尿嘧啶的平均包封率分别为(46.6±2.01)%、(48.7±1.49)%;脂质体的体外释放符合一级动力学方程,具有缓释作用。结论:优化得到的优福定脂质体处方工艺简便,稳定。

Optimization of Formula and Preparation Technique of UFT Liposomes

OBJECTIVE:To optimize the formula and preparation technique of UFT(tegafur/uracil)liposomes.METHODS:The liposomes were prepared by the film hydration-freeze drying technique;and the entrapment efficiencies of UFT(tegafur/uracil)liposomes were taken as parameters,the formula and preparation technique of the liposomes were optimized by orthogonal design;the in vitro drug release behavior of liposome was compared with that of the common market tablet.RESULTS:The optimum formula were as follows:the ratio between drugs and Lecithin was 16∶1;lecithin∶cholesterol=7∶1;pH of PBS was 5.6,the temperature of the hydration was 40℃.Under this condition,the average entrapment efficiency for tegafur was(46.6±2.01)% and that for uracil was(48.7±1.49)%.The release rule in vitro of liposome was in conformity with the first order kinetic equation,and the release behaviors of liposome has slow-release.CONCLUSION:The preparation technique for UFT liposomes is simple and stable.