阿立哌唑在Caco-2细胞单层模型中的跨膜转运

本文研究了阿立哌唑（aripiprazole）在Caco-2细胞模型中的跨膜转运特征。一种体外培养的人小肠上皮细胞模型 —— Caco-2细胞模型应用于阿立哌唑的跨膜转运研究。评价了时间、供给液浓度、pH值、温度及P-糖蛋白抑制剂对阿立哌唑跨膜转运的影响。采用高效液相色谱法检测药物浓度。结果表明阿立哌唑主要通过被动扩散的机制转运，同时兼有载体介导转运。阿立哌唑的转运量与时间、pH值、温度成正相关。表观渗透系数P_app值随供给液浓度升高而增大，10 μg·mL^-1时趋向饱和，之后随阿立哌唑浓度的增加而逐渐减小。P-糖蛋白抑制剂环孢菌素-A显著增加阿立哌唑的跨膜转运。

Transport of aripiprazole across Caco-2 monolayer model

This study aimed to investigate the transport characteristics of aripiprazole.  A human intestinal epithelial cell model Caco-2 cell in vitro cultured had been applied to study the transport of aripiprazole.  The effects of time, concentration of donor solutions, pH, temperature and P-glycoprotein inhibitor on the transport of aripiprazole were investigated.  The determination of aripiprazole was performed by HPLC.  It is concluded that aripiprazole is transported through the intestinal mucosa via a passive diffusion mechanism primarily, coexisting with a carrier-mediated transport.  The transport of aripiprazole is positively correlated to transport time, pH, and temperature.  P_app increased with donor concentrations up to 10 μg·mL^-1, and then decreased for higher concentrations.  The P-glycoprotein inhibitor cyclosporine A significantly enhanced the transport amount of aripiprazole.