摘要
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-
出处
《中国新药杂志》
CAS
CSCD
北大核心
2014年第5期601-605,共5页
Chinese Journal of New Drugs
基金
江苏省中医药局科技项目(LB09059
LZ13145)
南京药学会-常州四药医院药学科研基金(2012YX012
2013YX005)
关键词
灵仙新苷
外翻肠囊法
药动学
吸收机制
clematichinenoside AR
everted gut sac
pharmacokinetics
absorption mechanism