摘要
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。
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 : choles- terol = 7 : 1; pH of PBS was 5.6, the temperature of the hydration was 401Z . 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.
出处
《中国药房》
CAS
CSCD
北大核心
2007年第19期1479-1481,共3页
China Pharmacy