盐酸巴马汀在Caco-2细胞中的吸收机制研究

Absorption mechanism of palmatine chloride across Caco-2 cell monolayer mode

摘要:

摘要：目的：研究盐酸巴马汀在Caco-2细胞模型中的吸收机制。方法：用Caco-2细胞单层模型研究盐酸巴马汀的双向转运，并考察时间、药物浓度、抑制剂、pH值及温度对盐酸巴马汀吸收的影响。用高效液相色谱法检测药物浓度，计算其表观渗透系数。结果：盐酸巴马汀在Caco-2细胞模型中，从单层细胞层顶端到基底端的转运大于基底端到顶端的转运，随时间和浓度的增加，药物吸收呈饱和趋势，且P-gp抑制剂维拉帕米、pH值和温度对它的转运有影响。结论：盐酸巴马汀在Caco-2细胞模型中的吸收主要是由载体介导的主动转运，且该主动转运的载体位于Caco-2细胞单层的顶端。

Abstract:

Abstract:Objective: to investigate the absorption mechanism of palmatine chloride by using Caco-2 monolayer mode1.Methods: Caco-2 cell monolayer model was used to investigate the bi-directional transport of palmatine chloride. The effect of time, drug concentration, temperature, pH and inhibitors on the absorption of palmatine chloride was studied. Drug concentration was measured by HPLC and the apparent permeability coefficients (Papp) were calculated. Results: The apical to basolateral permeability (Papp) of palmatine chloride was bigger than the basolateral to apical permeability(Papp).Transport of palmatine chloride was time and concentration dependent, and it was also effected by P-glycoprotein inhibitor, pH and temperature. Conclusion:The absorption of palmatine chloride in Caco-2 cell model was an active transportation mediated by transporter, which mainly located in the apical side of Caco-2 cell monolayer.