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目的研究穿心莲内酯在Caco-2细胞单层模型中的吸收机制。方法观察穿心莲内酯在Caco-2细胞模型中的双向转运,考察时间、药物浓度、温度和抑制剂对穿心莲内酯吸收的影响。用LC/MS/MS检测药物浓度,计算其表观渗透系数(Papp)。结果穿心莲内酯在Caco-2细胞模型中,随时间和浓度的增加,药物吸收呈饱和趋势,且受温度和碘乙酰胺影响,但不受外排抑制剂维拉帕米和MK-571的影响。结论穿心莲内酯在Caco-2细胞中的吸收主要是由载体介导的主动转运。
Objective To study the absorption mechanism of andrographolide in Caco-2 monolayer model. Methods The bidirectional transport of andrographolide in Caco-2 cell model was observed. The effects of time, drug concentration, temperature and inhibitor on the andrographolide uptake were investigated. The drug concentration was measured by LC / MS / MS and its apparent permeability coefficient (Papp) was calculated. Results Andrographolide showed a trend of saturation in the Caco-2 cell model with time and concentration, and was affected by temperature and iodoacetamide but not by the efflux inhibitors verapamil and MK-571 influences. Conclusion The absorption of andrographolide in Caco-2 cells is mainly mediated by carriers.