目的:研究环肽astin C在Caco-2细胞单层模型中的吸收机制。方法:研究astin C在Caco-2细胞单层模型中的双向转运,考察时间、药物浓度对astin C吸收的影响。采用高效液相色谱法检测astin C的浓度,计算其表观渗透系数(Papp)。结果:在Caco-2细胞单层模型中,astin C的吸收随着时间和浓度的增加药物吸收呈近似线性增加;Papp(A→B)明显大于Papp(B→A),存在方向差异性;astin C不是P-gp的底物。结论:Astin C在Caco-2细胞单层模型中的主要转运机制是AP侧膜转运蛋白所介导的主动转运。
Objective : To study the absorption mechanism of the astin C, a cyclopeptide, in Caco-2 cell monolayer model. Method: Caco-2 cell model was established to investigate the bidirectional transport of astin C. The influences of time and drug concentration on the absorption of astin C was observed. Drug concentration was measured by HPLC and the apparent permeability coefficients(Papp) was calculated. Results: The absorption of asitn C in Caco-2 cell monolayer was nearly linear increased in a time and concentration dependent manner. The value of Papp ( A→B ) was much greater than that of Papp (B-~A) indicating astin C was not a substrate of P-gp. Conclusion : The absorption of astin C in Caco-2 cell mon- olayers is an active transportation mediated by transporter in the AP side.