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In this work, a sensitive and selective ultra-performance liquid chromatography–tandem mass spectrometry (UPLC–MS/MS) method was developed and fully validated for determination of jaceosidin in rat plasma. Avicularin was used as the internal standard (IS), and protein precipitation by acetonitrile was used to prepare samples. Chromatographic separation was achieved on a UPLC BEH C18 column (2.1 mm × 100 mm, 1.7 μm) with 0.1% formic acid and acetonitrile as the mobile phase with gradient elution. An electrospray ionization (ESI) source was applied and operated in positive ion mode; multiple reaction monitoring (MRM) mode was used for quantification. Calibration plots were linear throughout the range 2–500 ng Ml-1 for jaceosidin in rat plasma. Relative standard deviation (RSD) of intra-day and inter-day precision was less than 12%. The accuracy of the method was between 88.7% and 109.7%. Mean recoveries of jaceosidin in rat plasma ranged from 65.4% to 77.9%. The developed UPLC–MS/MS method was successfully applied to pharmacokinetic study of jaceosidin after intravenous administration of 2 mg kg-1 in rats. We could find that the jaceosidin rapidly eliminated, the t1/2 was 0.7 ± 0.3 h, and clearance (CL) was 22.4 ± 3.0 L h-1 kg-1.
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