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目的:采用Caco-2细胞模型研究獐牙菜苦苷转化产物獐牙菜新素{(Z)-5-ethylidene-8-hydroxy-3,4,5,6,7,8-hexahydro-1H-pyrano[3,4-c]pyrid ine-1-one,EHPO}的吸收机制。方法:以Caco-2细胞单层作为吸收研究模型,分别考察给药浓度、环境、pH以及加入维拉帕米后对EHPO双向跨膜转运的影响。通过HPLC测定药物浓度,计算表观渗透系数(Papp)。结果:在Caco-2细胞模型中,给予不同剂量的EHPO后,双向Papp几乎相等。在所试验浓度范围内EHPO的Papp基本保持恒定,pH值、维拉帕米对其跨膜转运有一定的影响。结论:在Caco-2细胞模型中,EHPO主要以被动扩散方式较快的被吸收。
OBJECTIVE: To study the transformation of swertiamarin, a product of swertiamarin, using the Caco-2 cell model. {(Z)-5-ethylidene-8-hydroxy-3,4,5,6,7,8-hexahydro-1H- The absorption mechanism of pyrano[3,4-c]pyridine-1-one, EHPO}. METHODS: Caco-2 cell monolayer was used as an absorption model to study the effect of concentration, environment, pH and the addition of verapamil on bidirectional transmembrane transport of EHPO. The drug concentration was determined by HPLC and the apparent permeability coefficient (Papp) was calculated. Results: In the Caco-2 cell model, two-way Papps were almost equal after different doses of EHPO. In the tested concentration range, the Papp of EHPO remained basically constant, and pH and verapamil had a certain influence on transmembrane transport. Conclusion: In the Caco-2 cell model, EHPO is rapidly absorbed by passive diffusion.