Sensitive and selective liquid chromatography-electrospray ionisation-mass spectrometry analysis of astragaloside-IV in rat plasma

Astragaloside-IV (3-O-beta-D-xylopyranosyl-6-O-beta-D-glueopyranosyl-cycloastragenol) is the major active constituent contained in Radix Astragali. This paper describes a rapid, sensitive and specific assay for quantitative determination of astragaloside-IV in rat plasma. After a liquid/liquid extraction (LLE) with n-butanol and high-performance liquid chromatography (HPLC) gradient separation with acetonitrile-NH4Cl solution (0.5 mu mol/L) as the mobile phase, the anions adduct [M + Cl](-) at m/z 819.4 of astragaloside-IV, and [M + Cl](-) at m/z 815.35 of internal standard (IS) digoxin were analyzed by electrospray ionisation-mass spectrometry (LC-ESI-MS) in selected ion monitoring (SIM) mode. Chromatographic separation was achieved in less than 9 min and calibration curve was linear over a concentration range of 2-200 ng/ml. The described assay method was successfully applied to the preclinical pharmacokinetic study of astragaloside-IV. After intragastric administration of astragaloside-IV to rats, Cmax and Tmax of astragaloside-IV were 134.73 +/- 39.86 ng/ml and 1.5 h, respectively, and the elimination half-life (t(1/2)) was 5.45 +/- 0.39 h. (c) 2005 Elsevier B.V. All rights reserved.