外翻肠囊法研究灵仙新苷肠吸收动力学

Intestinal absorption of clematichinenoside AR in rat everted gut sacs

目的:建立外翻肠囊模型测定灵仙新苷浓度,并研究其在大鼠小肠的吸收特征。方法:采用离体肠外翻模型进行肠吸收实验,串联质谱法测定灵仙新苷的含量,研究灵仙新苷在大鼠小肠的吸收部位和吸收机制。计算灵仙新苷的累计吸收量(Q)和吸收速率(J)。结果:灵仙新苷在大鼠的十二指肠、空肠和回肠均可进人肠囊(P>0.05),且浓度在检测的线性范围内;肠囊内灵仙新苷的Ka具有明显的浓度依赖关系,未观察到饱和现象;P-糖蛋白抑制剂维拉帕米未见对灵仙新苷的小肠吸收产生显著性影响。结论:灵仙新苷在大鼠小肠的不同肠段均有较好的吸收,吸收机制为被动转运。

Objective： To establish an everted gut sac method for determining clematichinenoside AR （C- AR） , and to investigate its intestinal absorptive characteristics. Methods： Rat everted gut sac was adopted and the sac fluid samples were collected at various time points after C-AR administration. C-AR was determined by LC-MS/ MS to investigate the site and mechanism of intestinal absorption. The accumulative absorption （Q） and the absorp- tion rate （J） of C-AR were calculated. Results： C-AR was detectable in the gut sac fluids from duodenum, jeju- num and ileum （P 〉 0.05）. The J of C-AR increased in jejunum with increasing of the concentration, and the ab- sorption was consistent with passive absorption. The absorption of C-AR was not significantly changed by P-glyco- protein inhibitor verapamil. Conclusion： C-AR is well absorbed in whole intestinal segments. Its absorption mech-