Pharmacokinetic study of puerarin in rat serum by liquid chromatography tandem mass spectrometry

Abstract A highly sensitive and specific atmospheric pressure chemical ionization liquid chromatography–tandem mass spectrometry method was developed for serum pharmacokinetic studies of puerarin in rats. Chromatography was carried out on a reversed‐phase Phenomenex Synergi 4 µm Fusion‐RP80 column (150 × 2.0 mm i.d.) using a mobile phase consisting of acetonitrile–water (10:90, v/v) in 10 m m NH 4 OAc with a flow rate of 0.2 mL/min. Puerarin was analyzed in the multiple reaction monitoring mode with a precursor/product ion transition of m/z 415/267. The method was demonstrated to be specific and sensitive, and a linear response was observed over a range of 2–5000 ng/mL in rat serum. The validated method was successfully applied to the characterization of the pharmacokinetics of puerarin in rat serum after oral administration to spontaneously hypertensive rats. The blood concentration–time profile of puerarin showed a rapid initial increase, reaching a maximum and then declining within 1 h. Puerarin could not be detected after 24 h. The main pharmacokinetic parameters for puerarin after oral administration were as follows: C max (3.54 ± 2.03 mg/L), T max (0.68 ± 0.37 h), AUC 0−t (7.29 ± 3.79 mg h/L), AUC 0−∞ (9.17 ± 4.87 mg h/L), T 1/2 (1.7 ± 0.6 h), CL/F (7.24 ± 4.27 L/h/kg) and V/F (17.88 ± 13.55 L/h/kg). Copyright © 2007 John Wiley & Sons, Ltd.