5-氟尿嘧啶口服微乳的制备及其大鼠肠吸收作用研究  

Preparation and Intestinal Absorption Effect of 5-Fluorouracil Microemulsion in Rats

作　　者：李文浩[1] 何应[1] 

机构地区：[1]天津大学药物科学与技术学院,天津市300072

出　　处：《中国药房》2008年第7期501-503,共3页China Pharmacy

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。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（Kin = 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.

关 键 词：5-氟尿嘧啶 微乳 伪三元相图 肠吸收 

分 类 号：R979.1[医药卫生—药品] R965[医药卫生—药学]