EFFECT OF QUERCETIN ON THE PHARMACOKINETIC PROFILE OF ELETRIPTAN, A CYP3A SUBSTRATE, IN RAT MODEL

Quercetin is a plant flavonol that is available from both daily diet and nutraceuticals. Various studies report that Quercetin alters the pharmacokinetics of various drugs by mechanisms like p-glycoprotein (p-gp) inhibition or other unknown mechanisms. The study was undertaken to evaluate the effect of Quercetin on the pharmacokinetics of Eletriptan. A single dose in-vivo pharmacokinetic study was carried out in rat models. In this study, rats were treated with Quercetin (10 mg/kg) and Eletriptan (2 mg/kg) orally and blood samples were collected at various time points such as 0 (predose), 0.5, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 6.0, 8.0, 12, 24 h post-treatment. Plasma concentration of Eletriptan was estimated using the HPLC method. AUC (0-24) of Eletriptan has significantly (p<0.01) increased in the Eletriptan and Quercetin combination group 1451.98 ± 93.78*** (ng/ml/h) when compared to AUC (0-24) Eletriptan alone treated group 883.94 ± 77.25 (ng/ml/h). AUC0-∞ of Eletriptan has significantly (***p<0.001) increased in the combination group (1543.32 ± 182.39*** (ng/ml/h).) in comparison to AUC0-∞ of Eletriptan of Eletriptan – alone treated group (925.59 ± 78.73 (ng/ml/h)). In conclusion, the results obtained herein indicate that Quercetin is enhancing the bioavailability of Eletriptan by augmenting the exposure (AUC) of the Eletriptan when concomitantly administered by the oral route.