Quantitative Determination of Ginsenoside Rg1 in Rat Plasma by Ultrahigh Performance Liquid Chromatography-tandem Mass Spectrometry (UHPLC-MS/MS) and its Application in a Pharmacokinetics and Bioavailability Study

Abstract

Background: Ginsenoside Rg1 (Rg1) is the main active compound of ginseng herbs. Objective: The aim of this study is to develop a rapid, selective and sensitive ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method to determine the levels of Rg1 in rat plasma and investigate the pharmacokinetics and bioavailability of Rg1 in rats. Methods: Chromatographic separation was achieved on an UHPLC-MS/MS system with an UPLC BEH C18 column using an elution gradient of a mixture of acetonitrile and water (with 0.1% formic acid). The analytes were quantitatively determined by negative-mode electrospray tandem MS. Results: The linearity of the calibration curve was from 2 to 1,000 ng/mL (r ≥ 0.9956), and the lower limit of quantification was 2 ng/mL. The inter-day and intra-day precision were both lower than 12.0%, and the accuracy ranged from 90.6 to 109.7%. The recovery of the targets was higher than 87.0%, and the matrix effect at three different analyte concentrations were from 89.0 to 97.2%. The bioavailability of Rg1 was only 6.1% due to a poor oral absorption. Conclusion: This new quantitative method was found to be sensitive, rapid and selective, and was successfully used to study the pharmacokinetics of Rg1 after intravenous and oral administration in rats.

Pharmacokinetics of 10-Hydroxy Mesaconitine in Rat Plasma by Ultra-Performance Liquid Chromatography-Tandem Quadrupole Mass Spectrometry

“…Eliminating potential interferences is especially important for sample preparation [26][27][28]. e use of methanol-acetonitrile (1 : 1, v/v), acetonitrile, and methanol for precipitation protein was investigated.…”