Transport of aripiprazole across Caco-2 monolayer model / 药学学报

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 microg x mL(-1), and then decreased for higher concentrations. The P-glycoprotein inhibitor cyclosporine A significantly enhanced the transport amount of aripiprazole.