Tang Cheng, Zhang Yanjun, Zhang Tiejun, Tian Chengwang, Liu Changxiao
Pharmacy College, Tianjin Medical University, Tianjin 300070, China.
Zhongguo Zhong Yao Za Zhi. 2009 Sep;34(17):2258-60.
To investigate the intestinal absorption mechanism of swertiamain metabolite {(Z)-5-ethylidene-8-hydroxy-3,4,5,6,7,8-hexahydro-1H-pyrano [3,4-c]pyridine-1-one, EHPO}.
The time depended hi-directional transport of EHPO in Caco-2 monolayer model was investigated with the factors of concentration, pH and verapamil. EHPO concentration was measured by HPLC assay and the apparent permeability coefficients (Papp) were calculated.
In the this cell model, EHPO could be absorbed through Caco-2 soon. The P(app AP-BL) was equal to the P(app BL-AP), and Papp keep almost constant with the selected concentration investigated. But the Papp could be influenced by pH and verapamil (100 mg x L(-1)).
The absorption of EHPO in Caco-2 cell model is a passive one. And absorption of EHPO in the intestines is quite good.
研究獐牙菜苷代谢产物{(Z)-5-亚乙基-8-羟基-3,4,5,6,7,8-六氢-1H-吡喃并[3,4-c]吡啶-1-酮,EHPO}的肠道吸收机制。
在Caco-2单层模型中研究EHPO在浓度、pH值和维拉帕米因素影响下的时间依赖性双向转运。采用高效液相色谱法测定EHPO浓度,并计算表观渗透系数(Papp)。
在该细胞模型中,EHPO可很快被Caco-2吸收。P(app AP-BL)等于P(app BL-AP),在所研究的选定浓度范围内Papp几乎保持恒定。但Papp会受到pH值和维拉帕米(100 mg·L(-1))的影响。
EHPO在Caco-2细胞模型中的吸收为被动吸收。且EHPO在肠道中的吸收良好。