Abstract
Objective: To study the absorption characteristics of cetirizine in small intestine.Methods: Everted intestinal sacs were used to study the absorption characteristics of cetirizine in rats.The absorption values of cetirizine of various concentrations in different intestinal segments of rats were determined by HPLC method.The constant of absorption rate(Ka) and the apparent permeability coefficient were calculated.The influences of the P-glycoprotein(P-gp) inhibitor digoxin and the multidrug resistance-associated protein-2(Mrp-2) inhibitor probenecid on the intestinal absorption of cetirizine were investi-gated.Results: Cetirizine was well absorbed in every intestinal segment.The orders of Ka and the apparent permeability coefficient were jejunumduodenumcolonileum.The accumulative absorption amount had nonlinear relation with the concentrations of cetirizine.The absorption of cetirizine was accelerated at high concentration.The P-gp inhibitor digoxin significantly accelerated the absorption of cetirizine,while the Mrp-2 inhibitor probenecid had no significant effect.Conclusion: The transportation of cetirizine is mediated by P-gp.Attention should be paid to the influence of P-gp and its substrates on the pharmacokinetic process of cetirizine in clinical application.
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