This study investigates the pharmacokinetic interactions between quercetin and amlodipine in rats. Twelve male Sprague-Dawley rats were randomly assigned into two groups: amlodipinegroup (1 mg/kg of amlodipine) and quercetin (20 mg/kg/day for 7 days) + amlodipine (1 mg/kg) group. Plasma concentrations of amlodipine were determined by using a sensitive and reliable LC-MS/MS method. The effects of quercetin on the metabolic stability of amlodipine were investigated by using rat liver microsome incubation systems. The results indicated that when the rats were pretreated with quercetin, the C-max of amlodipine increased from 13.78 +/- 3.57 to 19.96 +/- 4.56 mu g/L (p < 0.05), the T-max increased from 4.04 +/- 1.15 to 5.89 +/- 1.64 h (p < 0.05), and the AUC(0-t) increased by approximately 104% (p < 0.05), which suggested that the pharmacokinetic behavior of amlodipine was affected after oral co-administration of quercetin. Additionally, the metabolic half-life was prolonged from 35.2 +/- 6.5 to 56.8 +/- 11.7 min (p < 0.05) with the pretreatment of quercetin. It can be speculated that the drug-drug interaction between quercetin and amlodipine might occur, which might have resulted from inhibiting the metabolism of amlodipine by quercetin when they were co-administered.
[1]Yidu Cent Hosp Weifang, Dept Pharm, Weifang 262500, Shandong, Peoples R China.
[2]Linyi Cent Blood Stn, Linyi 276000, Peoples R China.
[3]Shanghai Univ TCM, Peoples Hosp 7, Dept Endocrinol, Shanghai 200137, Peoples R China.
(8.0+极速模式)