Transport of aripiprazole across Caco-2 monolayer model.
- Author:
Juan WU
1
;
Xian-Yi SHA
;
Xiao-Ling FANG
Author Information
1. School of Pharmacy, Fudan University, Shanghai, 200032, China.
- Publication Type:Journal Article
- MeSH:
ATP-Binding Cassette, Sub-Family B, Member 1;
antagonists & inhibitors;
Antipsychotic Agents;
administration & dosage;
pharmacokinetics;
Aripiprazole;
Biological Transport;
drug effects;
Caco-2 Cells;
Cyclosporine;
pharmacology;
Dose-Response Relationship, Drug;
Humans;
Hydrogen-Ion Concentration;
Piperazines;
administration & dosage;
pharmacokinetics;
Quinolones;
administration & dosage;
pharmacokinetics;
Temperature;
Time Factors
- From:
Acta Pharmaceutica Sinica
2009;44(2):188-191
- CountryChina
- Language:English
-
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.
