目的:研究祖师麻甲素在Caco-2细胞模型中的吸收特性,为其及祖师麻给药途径的选择和剂型的合理设计提供依据。方法:采用Caco-2细胞单层模型研究祖师麻甲素的摄取和跨膜转运,采用HPLC法检测药物浓度,计算其表观渗透系数,考察时间、温度、pH值、药物浓度以及P-gp抑制剂对祖师麻甲素吸收的影响。结果:祖师麻甲素以被动扩散为主要方式被细胞摄取和转运。药物的摄取与时间、温度和浓度呈正相关,不受媒介pH值的影响。祖师麻甲素从Basolateral-Apical方向转运要稍快于相反方向。随着药物浓度的增加,比值呈降低趋势,但变化不大。P-gp抑制剂维拉帕米对祖师麻甲素的转运无显著性影响。结论:祖师麻甲素是以被动扩散为主要方式被小肠上皮细胞摄取和转运,此过程不受P-gp的外排作用。 OBJECTIVE: To study the absorption characteristics of ZGPA in Caco-2 cell model and provide the basis for its selection and rational design of dosage form. Methods: Caco-2 cell monolayer model was used to study the uptake and transmembrane transport of GPs. The drug concentration was measured by HPLC and the apparent permeability coefficient was calculated. The effects of time, temperature, pH, drug concentration and P-gp Effects of Inhibitors on the Absorption of Megan A in Gentiana. Results: Zujian A was absorbed and transported by cells mainly by passive diffusion. Drug uptake was positively correlated with time, temperature and concentration, independent of media pH. Zyphospene translocates slightly faster in the opposite direction from the Basolateral-Apical direction. With the increase of drug concentration, the ratio showed a downward trend, but little change. Verapamil, a P-gp inhibitor, had no significant effect on the translocation of epinephrine. CONCLUSION: ZGPA is taken up and transported by small intestine epithelial cells mainly by passive diffusion, and this process is not affected by the efflux of P-gp.