吲达帕胺大鼠在体胃、小肠的吸收动力学研究

目的研究吲达帕胺在大鼠胃、小肠的吸收特性。方法采用大鼠在体方式 ,对吲达帕胺进行了大鼠胃、小肠的吸收动力学实验。结果大鼠胃部为吲达帕胺的不良吸收部位 ,2h的吸收百分率为 9 8% ;胆管结扎与不结扎对吸收速率无明显影响 ;吲达帕胺在小肠各部位吸收良好 ,吸收速率常数按十二指肠、空肠、回肠、结肠顺序依次下降 ,吸收速率常数分别为 0 1 5 6、0 1 4 0、0 1 30、0 0 73h-1。药物在肠道的吸收呈现一级吸收动力学 ,吸收机制为被动吸收。结论结肠的吸收速率常数大约是小肠段的十分之三 ,提示适于制备日服一次 ( 2 4h)缓释给药系统。

Studies on the absorption kinetics of indapamide in rats's stomachs and intestines

Objective This paper is to study the absorption of indapamide in rats' stomachs and intestines. Methods The absorption kinetics are obtained by using the in situ perfusion method in rats. Results It showed that the stomach was the worse absorption segment, the absorption percent after 2 hours was 9.8%;There was no marked difference of the absorption rate constants between rats with or without ligated bile duct; the small intestine was the best absorption segment, the absorption rate constants were 0 156,0 140,0 131,0 073h -1 respectively at duodenum,jejunum,ileum and colon. The absorption mechanism of indapamide was studied at different concentrations and no saturation phenomenon occurred. At the same time the absorption rate constant value was kept unchanged. The results indicated that the absorption of indapamide complied with the passive transport mechanism and first order kinetics.Conclusions The results indicated that indapamide could be prepared and processed into a sustained release dosage form.