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目的制备5-氟尿嘧啶-蛇葡萄素复方脂质体并建立同时测定2种药物含量的紫外分光光度法。方法紫外分光光度法确定5-氟尿嘧啶和蛇葡萄素的测定条件。比较几种脂质体的制备方法,以包封率和粒径为指标,确定最优制备方法;采用正交设计进行优化处方和制备工艺。结果采用紫外分光光度法测定5-氟尿嘧啶和蛇葡萄素,2种药物的加样回收率均在99%~102%之间。以薄膜分散超声法为制备方法,以单因素考察结合正交设计优选出的最佳处方和制备工艺,主药∶卵磷脂=1∶20,卵磷脂∶胆固醇=4∶1,磷脂浓度50 g.L 1;维生素E的用量为5%,磷酸盐缓冲溶液pH为7.4。5-氟尿嘧啶和蛇葡萄素的包封率分别为(44.79±1.55)%和(75.47±0.91)%(n=3);复方脂质体的粒径为(142±3.6)nm。5-氟尿嘧啶和蛇葡萄素的体外12 h累积释放率分别为43.05%和60.24%。结论将5-氟尿嘧啶和蛇葡萄素同时包封于脂质体制备成复方脂质体,所采用的制备工艺简单可行,重复性好,包封率较高。建立的紫外分光光度法可同时测定复方脂质体中的5-氟尿嘧啶和蛇葡萄素含量。
OBJECTIVE To prepare 5-fluorouracil-amylopsin liposome and establish a UV spectrophotometry method for simultaneous determination of two drugs. Methods UV spectrophotometric determination of 5 - fluorouracil and snake grape prime determination of the conditions. The preparation methods of several liposomes were compared, and the optimal preparation method was determined by the entrapment efficiency and particle size. The orthogonal design was used to optimize the formulation and preparation process. Results UV spectrophotometry was used to determine 5-fluorouracil and snake grape. The recoveries of two drugs were between 99% and 102%. The main prescriptions were lecithin = 1:20, lecithin: cholesterol = 4:1, phospholipid concentration 50 gL 1, the amount of vitamin E was 5% and the pH value of phosphate buffer solution was 7.4. The encapsulation efficiency of fluorouracil and amylopsine were (44.79 ± 1.55)% and (75.47 ± 0.91)% (n = 3), respectively. The size of compound liposomes was (142 ± 3.6) nm. The cumulative 12-h cumulative release rates of 5-fluorouracil and sphingosine were 43.05% and 60.24%, respectively. Conclusion Both 5-fluorouracil and sphingosine are encapsulated in liposomes to prepare liposomes. The preparation process is simple, feasible and reproducible, and the entrapment efficiency is high. The UV spectrophotometry was established to determine the contents of 5-fluorouracil and sphingosine in the compound liposomes simultaneously.