Pharmacokinetics and Bioavailability of Matrine in Rats by UPLC-MS/MS

Matrine has a wide range of biological activities, such as antibacterial, antiviral, anti-inflammatory, anti-tumor, immune regulation and protection of heart, liver, lung, kidney, brain, blood vessels, and positive muscle strength to the heart, as well as the pharmacological effects of elevated white blood cells, asthma, anti-ulcer, anti-fibrosis, and sedative, hypnotic, analgesic and other effects on central nervous system. In this study, we used UPLC-MS/MS to detect matrine in rat plasma, and investigated its pharmacokinetics in rats. Palmatine was utilized as an internal standard (IS), and acetonitrile precipitation method was used to process the plasma samples. Chromatographic separation was achieved using a UPLC BEH C18 column using mobile phase of acetonitrile-0.1 % formic acid with gradient elution. Electrospray ionization (ESI) tandem mass spectrometry in multiple reaction monitoring (MRM) mode with positive ionization was applied. The results indicated that within the range of 1-1000 ng/mL, linearity of matrine in rat plasma was acceptable (r > 0.995), and the lower limit of quantification (LLOQ) was 1 ng/mL. Intra-day and inter-day precision RSD of matrine in rat plasma were lower than 15%. Accuracy range was between 96.1 and 106.0 %, and matrix effect was between 91.1 and 94.8%. The method was successfully applied in the pharmacokinetics of matrine in rats after oral and intravenous administration. The absolute bioavailability of the matrine was 18.5% in rats.