关附壬素肠道吸收机理及最佳吸收部位研究

Study on the Intestinal Absorption Mechanism and the Best Absorption Segments of GFI

采用大鼠在体循环肠灌流吸收模型,以LC-MS法测定关附壬素（GFI）的含量来研究GFI的吸收机理及最佳吸收部位.结果表明,在整段肠回流实验条件下,在1~100 mg/L质量浓度范围内药物吸收量与质量浓度呈线性关系,无高质量浓度饱和现象,各质量浓度下的吸收速度常数无明显差异;P-糖蛋白抑制剂不影响GFI的肠吸收.在分段肠回流实验条件下,GFI在肠道各部位的吸收速度按十二指肠、空肠、回肠、结肠顺序下降.GFI在大鼠体内的吸收机制为被动扩散,十二指肠及空肠是最佳吸收部位.

Rat intestine reperfusion experiment was carried out and LC- MS method for determining the content of GFI was used to study the absorption mechanism of GFI and the best absorption area. When the concentration was raised from 1 to 100 mg / L,the uptake of GFI increased and did not appear saturable,whereas the absorption rate constants for the high dosage groups,middle dosage groups and low dosage groups were no significance. And there were different rates of absorption in different parts of intestine,the absorption rate constant was as follows： duodenum jejunum ileum colon. P-gp inhibitor had no effect on the absorption of GFI. The experiment results suggested that the absorption mechanism of GFI was mainly via passive diffusion,and the duodenum and jejunum were the best absorption segments of GFI.