白花前胡丁素在人结肠腺癌细胞系细胞模型上的吸收转运特征研究

The absorption and transport characteristics of praeruptorin in Caco-2 cell model

目的研究白花前胡丁素在人结肠腺癌细胞系(Caco-2)细胞模型上的转运特征。方法利用Caco-2单层细胞模型研究白花前胡丁素的双向转运,采用高效液相色谱(HPLC)法测定药物的转运量,计算其表观渗透系数(Papp),并考察时间和药物质量浓度对其转运的影响。结果白花前胡丁素在Caco-2细胞模型上的双向转运量在120min内均随时间与浓度的增加而增大,其从肠腔侧(AP)向基底侧(BL)和从BL向AP的Papp介于2.0×10-6cm/s～5.0×10-6cm/s,Papp(BL-AP)/Papp(AP-BL)<1.5。结论白花前胡丁素为吸收较差的药物,主要以被动扩散方式经肠道吸收。

Objective To investigate the transport characteristics of praeruptorin in Caco-2 cell model.Methods The Caco-2 cell monolayer model was used to investigate the bidirectional transport of praeruptorin.The transport amount of drug was determined by HPLC method and calculated its apparent permeability coefficients（Papp）.The impact of time and drug concentration on the bidirectional transport was then evaluated.Results The transport amount of praeruptorin was increased in the Caco-2 cell model within 120 min along with the increases of time and drug concentration.The Papp values for apical（AP） to basolateral（BL） or BL to AP were between 2.0×10-6 cm/s and 5.0×10-6 cm/s,with Papp（BL-AP） /Papp（AP-BL） less than 1.5.Conclusion Praeruptorin was a drug with relatively bad absorption,which absorbed mainly by passive diffusion approach through intestinal tract.