The Effect of Apigenin on Pharmacokinetics of Imatinib and Its Metabolite N-Desmethyl Imatinib in Rats

Abstract EN

The purpose of this study was to determine the effect of apigenin on the pharmacokinetics of imatinib and N-desmethyl imatinib in rats.

Healthy male SD rats were randomly divided into four groups: A group (the control group), B group (the long-term administration of 165 mg/kg apigenin for 15 days), C group (a single dose of 165 mg/kg apigenin), and D group (a single dose of 252 mg/kg apigenin).

The serum concentrations of imatinib and N-desmethyl imatinib were measured by HPLC, and pharmacokinetic parameters were calculated using DAS 3.0 software.

The parameters of AUC(0-t), AUC(0−∞), Tmax, Vz/F, and CLz/F for imatinib in group B were different from those in group A (P<0.05).

Besides, MRT(0−t) and MRT(0−∞) in groups C and D differed distinctly from those in group A as well.

The parameters of AUC(0-t) and Cmax for N-desmethyl imatinib in group C were significantly lower than those in group A (P<0.05); however, compared with groups B and D, the magnitude of effect was modest.

Those results indicated that apigenin in the short-term study inhibited the metabolism of imatinib and its metabolite N-desmethyl imatinib, while in the long-term study the metabolism could be accelerated.