title: Transport of aripiprazole across Caco-2 monolayer model.
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.
authors.affiliation: School of Pharmacy, Fudan University, Shanghai, 200032, China.
authors.forename: Juan
authors.initials: J
authors.lastname: Wu
authors.forename: Xian-Yi
authors.initials: XY
authors.lastname: Sha
authors.forename: Xiao-Ling
authors.initials: XL
authors.lastname: Fang
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors*; D014150:Antipsychotic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000068180:Aripiprazole; D001692:Biological Transport / Q000187:drug effects; D018938:Caco-2 Cells; D016572:Cyclosporine / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D006863:Hydrogen-Ion Concentration; D010879:Piperazines / Q000008:administration & dosage / Q000493:pharmacokinetics*; D015363:Quinolones / Q000008:administration & dosage / Q000493:pharmacokinetics*; D013696:Temperature; D013997:Time Factors
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D014150:Antipsychotic Agents; D010879:Piperazines; D015363:Quinolones; D000068180:Aripiprazole; D016572:Cyclosporine