Pharmacokinetics of arctigenin nanoemulsion in rats / 中国药学杂志

ABSTRACT

OBJECTIVE: To develop an HPLC method for the determination of arctigenin in rat plasma and study the pharmacokinetics of arctigenin nanoemulsion. METHODS: The plasma samples were extracted by ethyl acetate. The determination was carried out on an Agilent C18 column (4.6 mm × 250 mm, 5 μm) with the mobile phase consisting of methanol-0.2% phosphoric acid (5248, V/V) and the UV detection wavelength was set at 280 nm. Quercetin was selected as internal standard. Arctigenin nanoemulsion was administered to rats by intravenous injection at a dose of 4 mg · kg-1. The plasma concentration of arctigenin at different time points was determined by the established HPLC method. The pharmacokinetic parameters were processed by DAS2.1 software. RESULTS: The calibration curve of arctigenin had acceptable linearity in the range of 0.1-10 mg · L-1 in rat plasma(r=0.9992). The lower limit of quantitation (LLOQ) was estimated to be 0.1 mg · L-1 and the lower limit of detection (LLOD) was estimated to be 0.03 mg · L-1. The mean extraction recovery rates of arctigenin QC samples at low, medium and high concentration levels were all a-bove 85%. The intra-day and inter-day precisions were less than 6%. The pharmacokinetics of arctigenin in rats after intravenous injection were fitted to a two-compartment model and the half-lives of α phase and β phase were (0.134 ± 0.085) and (1.471 ± 0.164) h, respectively. CONCLUSION: The HPLC method is simple, rapid and accurate. It can be used for monitoring the plasma concentration of arctigenin and its pharmacokinetic study. After intravenous administration of arctigenin nanoemulsion, arctigenin is rapidly distributed into tissues, but the elimination is slow.