瑞巴派特在大鼠胃肠道的吸收动力学研究

Absorption Kinetics of Rebamipide in Rat Gastrointestinal Tract

目的研究瑞巴派特在体胃肠道吸收动力学的特征。方法采用大鼠胃部定时取样和单向肠灌流技术,HPLC法测定瑞巴派特的含量,对瑞巴派特在大鼠胃部和不同肠段吸收进行研究。结果在0~120 min,大鼠胃部吸收呈线性吸收规律,120 min后胃中平均吸收率为28.47%;瑞巴派特在不同肠段的净累计吸收量为十二指肠〉空肠〉回肠〉结肠,并与瑞巴派特吸收速率常数Ka顺序保持一致;瑞巴派特在20~100μg·mL^-1对小肠吸收速率常数Ka无影响。结论瑞巴派特为全胃肠道吸收药物,以胃和十二指肠为主要吸收部位,提示瑞巴派特可以设计制成缓控释制剂。

Objective To investigate the absorption kinetics of rebamipide in the gastrointestinal tract of rats. Methods Samples taken from rat stomachs at a definite time and single-pass perfusion were used to study the absorption mechanism of rebamipide in rats. HPLC was used to determine the concentration of rebamipide. The absorption rate of rebamipide in the stomach and different intestine segments in rats was also determined. Results Between 0 and 120 min,the absorption rate of rebamipide showed a linear absorption pattern and after 2 hours it was 28. 47 % in the stomach. The cumulative absorption of rebamipide in each intestinal segment was as follows：duodenum colon ileum jejunum,which was consistent with the order of Ka value. Also,rebamipide had no effect on Ka value of duodenum in the examined drug concentration range. Conclusion Rebamipide can be well absorbed in the whole intestine,especially in the stomach and duodenum. It can be processed into a sustainedrelease preparation.