5-Fu大鼠在体肠道吸收动力学和结肠吸收促进剂的研究

Studies on the absorption kinetics of fluorouracil and effect of colon penetration enhancers using perfusion method in rats

目的 研究氟脲嘧啶 ( 5 Fu)在大鼠肠道的吸收动力学 ,选择合适的结肠吸收促进剂。方法 进行大鼠在体灌流肠吸收实验 ,研究 5 Fu在小肠和结肠的吸收情况 ,并分别考察枸橼酸钠和聚山梨酯 (吐温 80 ) 80对结肠吸收的促进作用。结果 5 Fu在小肠和结肠的吸收速率分别为 10 .6 6± 4 .38× 10 -2 ·h-1,0 .72± 0 .5 3× 10 -2 ·h-1;含 1%枸橼酸钠或吐温 80的溶液结肠灌流后测得吸收速率分别为 2 .2 3± 1.0 3× 10 -2 ·h-1,1.70± 0 .5 5× 10 -2 ·h-1,经统计学检验 ,二者能显著提高结肠吸收速率。结论 5 Fu在结肠段吸收速率较小肠小 ,枸橼酸钠和吐温 80对 5Fu在结肠的吸收有显著促进作用 ,枸橼酸钠的促进作用优于吐温 80。

OBJECTIVE To explore the absorption kinetics of fluorouracil in various intestinal segments, and select apposite colon penetration enhancers. METHOD The absorption kinetics was investigated using perfusion method in rats. Effect of 1% sodium citrate or 1% tween 80 were investigated by way of perfused in colon. RESULTS It was showed that fluorouracil could be absorbed absorption in small intestine and colon, and the permeability rate constants were 10.66±4.38×10 -2 ·h -1 and 0.72±0.53×10 -2 ·h -1 , respectively. With 1% sodium citrate or 1% tween 80 and in colon, the permeability rate constants were 2.23± 1.03 ×10 -2 ·h -1 and 1.70±0.55×10 -2 ·h -1 , respectively. CONCLUSION Fluorouracil is absorbed more in small intesine than in colon. Sodium citrate and tween 80 can remarkably increase the absorption of fluorouracil in colon. The enhancement of sodium citrate is batter than tween 80.