吴 娟 沙先谊 方晓玲. 阿立哌唑在Caco-2细胞单层模型中的跨膜转运J. 药学学报, 2009,44(2): 188-191.
引用本文: 吴 娟 沙先谊 方晓玲. 阿立哌唑在Caco-2细胞单层模型中的跨膜转运J. 药学学报, 2009,44(2): 188-191.
TUN Juan, Sha-Xian-Yi, Fang-Xiao-Ling. Transport of aripiprazole across Caco-2 monolayer modelJ. 药学学报, 2009,44(2): 188-191.
Citation: TUN Juan, Sha-Xian-Yi, Fang-Xiao-Ling. Transport of aripiprazole across Caco-2 monolayer modelJ. 药学学报, 2009,44(2): 188-191.

阿立哌唑在Caco-2细胞单层模型中的跨膜转运

Transport of aripiprazole across Caco-2 monolayer model

  • 摘要:

    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Papp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。

     

    Abstract:

    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.  Papp 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.

     

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