辣椒素大鼠不同肠段在体给药药代动力学

摘要

Objective To validate the correlation between in vitro and in vivo absorption of capsaicin, and study the distribution of capsaicin in tissue after oral administration. Methods In situ closed loop method was used to measure the absorption of capsaicin from different intestine segments of rats. Concentrations of capsaicin in rat plasma were examined by LC-MS/MS and pharmacokinetic parameters were calculated by the software WinNonlin. Results The AUC0-240min and Cmax of capsaicin absorbed from colon were higher than those of ileum and jejunum. However, there was no statistic difference. Conclusion In the primary study, we realized that permeability of capsaicin across the colonic mucosa is remarkably higher than that across jejunal or ileac mucosa in mucosal-to-serosal direction. However, there′s no statistical difference for the absorption of capsaicin across different intestinal regions by in situ assay. These results suggest the correlation between in vitro and in situ method is worth further study.%目的：通过在体环境下对辣椒素经不同肠段的吸收情况进行检测来验证体外实验与体内实验的相关性。方法采用在体肠封闭实验研究辣椒素经不同肠断的吸收情况，辣椒素的血药浓度检测采用已经建立的LC-MS/MS 检测方法，并计算各种药代动力学参数。结果辣椒素经不同肠段吸收后，在结肠的浓度时间曲线下面积（AUC0鄄240min）和最高血浆浓度（Cmax）的平均值大于回肠和空肠，但无统计学差异。结论体内研究结果并没有出现体外研究中所呈现的具有显著性的结肠特异性吸收特性，体外研究和体内研究的完全相关性仍然是值得进一步探究。