【摘要】 目的:制备5-氟尿嘧啶(5-Fu)口服微乳,并考察其在大鼠肠吸收的作用。方法:以肉豆蔻酸异丙酯为油相、单辛/癸酸甘油酯为乳化剂,借助伪三元相图法对不同5-Fu微乳处方进行评价;用外翻肠囊法制备肠吸收离体模型,考察5-Fu微乳的吸收部位和促吸收效果。结果:选择肉豆蔻酸异丙酯-单辛/癸酸甘油酯-无水乙醇-水(Km=1∶2)体系作为5-Fu微乳的载药体系;与其溶液比较,5-Fu微乳可明显改善药物的肠吸收,小肠中后段是其最佳吸收部位,90min时累积吸收率微乳是溶液的3倍。结论:所制备的5-Fu微乳性质稳定、肠吸收效果良好。更多还原

【Abstract】 OBJECTIVE: To prepare 5-fluorouracil(5-Fu) microemulsion and to investigate the intestinal absorption of 5-Fu microemulsion in rats. METHODS: The formulation of 5-Fu microemulsion was optimzied using pseudo-ternary phase diagrams with isopropyl myristate (IPM) as oil phase and ODO-L as surfactant; the intestinal absorption ex vivo model was prepared using everted intestinal sac method to investigate the absorption sites and absorption efficiency of 5-Fu microemulsion in rats. RESULTS: IPM/ODO-L/EtOH/H2O (Km=1∶2) was selected as the delivery system of 5-Fu; as compared with 5-Fu solution, the intestinal absorption of 5-Fu microemulsion was significantly improved and the middle and lower segments of rat’s intestine were the best sbsorption sites for 5-Fu microemulsion and the accumulative aborption rates of 5-Fu microemulsion at 90 min was 3-fold that of 5-Fu solution. CONCLUSION: The prepared 5-Fu microemulsion is stable in quality and well-absorbed in rats’ intestine.更多还原