泻心汤中药效成分的吸收机制与相互作用

Investigation of the absorption mechanism and interactions among active components in Xiexin decoction

目的研究泻心汤药中效成分黄芩苷、大黄酸、盐酸小檗碱在Caco-2细胞单层模型的吸收机制和相互作用。方法采用Caco-2细胞单层模型研究黄芩苷、大黄酸、盐酸小檗碱由绒毛面(AP侧)到基底面(BL侧)的转运过程,采用HPLC法测定药物在BL侧的累积量,通过计算表观渗透系数(Papp),比较配伍前后药物Papp的差别,探讨药物的跨细胞转运机制和相互作用。结果泻心汤药效成分黄芩苷、大黄酸、盐酸小檗碱在考察的浓度范围内皆以被动扩散为主要跨细胞转运方式,配伍前后药物的Papp无统计学差异。结论泻心汤中药效成分跨细胞转运方式为被动扩散,在转运过程中,药物之间无影响。

OBJECTIVE To investigate the absorption mechanism and interactions among active components in Xiexin decoction（baicalin,rhein and berberine hydrochloride） by Caco-2 cell monolayer model.METHODS The transport process of baicalin,rhein and berberine hydrochloride from apical side（AP） to basolateral side（BL）was studied,the cumulative amount in the basolateral side was measured by HPLC,then the apparent permeability coefficient（Papp）was calculated and the Papp values before and after compatibility was compared to discuss the drug transport mechanism and interaction.RESULTS The absorption and transport of active components in Xiexin decoction（baicalin,rhein and berberine hydrochloride） was passive diffusion as the dominating process in Caco-2 cell monolayer model.There was no significanl different between the Papp values before and after compatibility.CONCLUSION The absorption and transport of active components in Xiexin decoction was passive diffusion as the dominating process,and there was no drug interaction between baicalin,rhein and berberine hydrochloride when they transported from apical side to basolateral side.