Abstract: Objective To develop a LC-MS/MS method for determination of astragalin in rat plasma and study its
pharmacokinetics in rats. Methods The analytical column was packed with ZORBAX SB-C18, and the mobile phase was
methanol-water containing 10 mmol/L ammonium acetate-formic acid (80∶20∶0.15, V/V/V). Quercetin was used as the internal
standard (IS). Multiple reaction monitoring (MRM) mode was employed, and the transition of m/z was m/z 449.1→m/z 287.1 for
astragalin, and m/z 301.1→m/z 151.1 for IS. Results A good liner relationship was obtained within the range of 1.00-1000 ng/ml
(r2=0.9929), and the lower limit of quantification of astragalin was 1.00 ng/ml in rat plasma. The extraction recoveries were all
above 93%. After oral administration of astragalin, the maximum plasma concentration of astragalin was 231.1±67.3 ng/ml and
the time to reach this value was 0.5±0.1 h, with a half-life of 3.9±1.3 h and an AUC0-∞ of 782.6±152.8 ng·h/ml. Conclusion The
method is highly sensitive, selective and rapid for determination of the concentration of astragalin in rat plasma to facilitates
the study of its pharmacokinetics.