Study of transportation of rupatadine fumarate in Caco- 2 cell

Objective To make use of a probe drug to study the transfer characteristics of rupatadine fumarate in Caco-2 cell model in vitro. Methods The effect of P-gp inhibitor verapamil on the apparent permeability ratio of rupatading fumarate in Caco-2 cell was explored by a complete Caco-2 cell monolayer model,which evaluated by the trans epithellal electric resistance( TEER) value and activity of alkaline phosphatase. Results The TEER value was over 500 Ω·cm2. The activity of alkaline phosphatase in day 22 was more than twice of the day 15. The monolayer model was dense and complete,and can be used to transport experiment. The apparent permeability ratio of rupatadine fumarate was 5. 44,while it decreased to 1. 34 when verapamil existed. Conclusion The rupatadine fumarate was active transport in Caco-2 model. Rupatadine fumarate was a substrate of P-gp.