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用非离子表面活性剂制备5-氟尿嘧啶(5-Fu)囊泡,并对其进行了小鼠体内药动学和组织分布的研究.采用薄膜分散法制备5-Fu的类脂囊泡,以5-Fu水溶液为对照,尾静脉注射自制5-Fu囊泡和5-Fu水溶液,利用高效液相色谱法检测血浆和各组织中的5-Fu浓度,利用统计学方法计算了5-Fu在小鼠体内的药动学参数及小鼠的组织分布参数.与注射水溶液组相比,5-Fu囊泡组MRT值延长,AUC0～t值增加.组织分布结果显示:5-Fu囊泡在肝、肾中AUC值显著增加;5-Fu囊泡明显延长了5-Fu在体内的作用时间,比普通水溶液具有一定的缓释和提高生物利用度的作用.
5-Fluorouracil (5-Fu) vesicles were prepared with non-ionic surfactant, and their pharmacokinetics and tissue distribution were studied in vivo.The 5-Fu lipid vesicles were prepared by thin-film dispersion method, 5-Fu aqueous solution was used as a control. 5-Fu vesicles and 5-Fu aqueous solution were injected through the tail vein. The 5-Fu concentration in plasma and each tissue was detected by high performance liquid chromatography. The pharmacokinetic parameters in mice and the tissue distribution parameters in mice.Compared with the water injection group, the MRT value of 5-Fu vesicle group was prolonged and the AUC0 ~ t value was increased.The distribution of 5-Fu vesicles was Liver and kidney AUC values increased significantly; 5-Fu vesicles significantly prolong the role of 5-Fu in vivo time, compared with ordinary aqueous solution has a certain degree of sustained release and improve bioavailability.