A validated LC–MS/MS assay for the simultaneous determination of periplocin and its two metabolites, periplocymarin and periplogenin in rat plasma: Application to a pharmacokinetic study

• A method for the determination of periplocin and its two metabolites is established.
• The lower limits of quantitation of the analytes were lower than 1 ng/mL.
• The main pharmacokinetic parameters of the two metabolites in rats were reported.

A sensitive and reliable LC–MS/MS method was developed and validated for the simultaneous determination of periplocin and its two metabolites (periplocymarin and periplogenin) in rat plasma using psoralen as the internal standard (IS). After liquid–liquid extraction with ethyl acetate, chromatographic separation was performed on a C18 column with a 13 min gradient elution using 0.1% formic acid and acetonitrile as mobile phase at a flow rate of 0.3 mL/min. The detection was accomplished on a tandem mass spectrometer via an electrospray ionization (ESI) source by multiple reaction monitoring (MRM) in the positive ionization mode. The lower limits of quantitation (LLOQs) for periplocin, periplocymarin and periplogenin were 0.5, 1 and 0.1 ng/mL, respectively. The mean recoveries of the analytes and IS were higher than 67.7%. The proposed method was successfully applied to evaluating the pharmacokinetic studies of periplocin and its metabolites (periplocymarin and periplogenin) in rats after a single oral administration of periplocin at 50 mg/kg.

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