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 - ∞), T max, V z / F, and CL z / 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 C max 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. © 2013 Xian-yun Liu et al.
Liu, X. Y., Xu, T., Li, W. S., Luo, J., Geng, P. W., Wang, L., … Hu, G. X. (2013). The effect of apigenin on pharmacokinetics of imatinib and its metabolite N-desmethyl imatinib in rats. BioMed Research International, 2013. https://doi.org/10.1155/2013/789184