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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 formulation and preparation process of Youfuding liposomes. Methods: The liposomes of Youfuding were prepared by membrane dispersion and freeze-drying method. The encapsulation efficiency of tegafur and uracil as the main drug was taken as an index. The orthogonal test was used to optimize the formulation and preparation process. Ordinary tablets for comparison. Results: The optimized formulation was phospholipid-drug weight ratio of 16: 1, phospholipid to cholesterol weight ratio of 7: 1, pH5.6 phosphate buffer hydrated mesotrons, hydration temperature of 40 ℃. Under these conditions, the average entrapment efficiencies of tegafur and uracil were (46.6 ± 2.01)% and (48.7 ± 1.49)%, respectively. The in vitro release of liposomes was consistent with the first-order kinetic equation with sustained release. Conclusion: The optimized formulation of UFIDA liposomes is simple and stable.