Pharmacokinetics of Naringin and its Metabolite Naringenin in Rats after Oral Administration of Rhizoma Drynariae Extract Assayed by UPLC-MS/MS

AimTo investigate the pharmacokinetics of naringin and naringenin in rats after oral administration of Rhizoma Drynariae extract.MethodsThe extract of Rhizoma Drynariae were refluxed with 50% ethanol for 1 h and dissolved with 50% PEG 400, and then administered to the rats. Naringin and naringenin were extracted from rat plasma by means of liquid-liquid extraction (LLE) with ethyl acetate. Paracetamol was used as the internal standard (IS). The analysis was carried out on an ACQUITY UPLC™ BEH C18 column with acetonitrile-0.4% acetic acid (80: 20, V/V) as mobile phase at a flow rate of 0.25 mL·min−1. The detection was carried out via negative electrospray ionization (ESI) mass spectrometry with multiple-reaction monitoring (MRM). The quantification was performed using the transitions of m/z 578.4→270.7 for naringin, m/z 270.7→150.7 for naringenin and m/z 149.9→106.6 for paracetamol (IS), respectively.ResultsAfter oral administration of Rhizoma Drynariae extract to rats, the mean Cmax of naringin and naringenin was (2.56 ± 0.77) × 103 ng·mL−1 and 222 ± 45 ng·mL−1, the Tmax was 0.67 ± 0.20 h and 8.0 ± 1.3 h, the AUC0-t was calculated to be (3.23 ± 0.54) × 103 ng·mL−1·h and (1.57 ± 0.37) × 103 ng·mL−1·h, the AUC0-∞ was calculated to be (3.29 ± 0.54) × 103 ng·mL−1·h and (1.79 ± 0.43) × 103 ng·mL−1·h. The t½ was 4.1 ± 0.8 h for naringin, and another small peak could be seen at 8h in the plasma concentration–time profile of naringin.ConclusionThe developed UPLC-MS/MS method was conformed to the criteria for the analysis of biological samples according to the guidance of FDA. The results of pharmacokinetic study on naringin and its active metabolite naringenin would be a suitable reference in clinical application for Rhizoma Drynariae.