Preparation and Intestinal Absorption Effect of 5-Fluorouracil Microemulsion in Rats / 中国药房

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.