In China, Yinchenzhufu decoction (YCZFD) has been used to treat cholestatic liver disease in clinical practice for hundreds of years. Nonvolatile components in YCZFD, their composition, components absorbed in blood, and pharmacokinetic characteristics have been clarified. However, information about its volatile components is limited. The aim of the present study was to identify the components of the volatile oil (VO) of YCZFD, quantify the major volatile components in YCZFD, and reveal their pharmacokinetic characteristics. In YCZFD, 85 components representing 95.36% of the total oil composition were identified by gas chromatography-mass spectrometry. Next, 11 highly abundant components were quantified in YCZFD and YCZFD VO. Finally, a sensitive headspace solid-phase dynamic extraction-chromatography-quadruple mass spectrometry method for determining 8 volatile components in rat plasma was established and applied to compare the pharmacokinetics of YCZFD and YCZFD VO after oral administration in rats. These volatile components were rapidly absorbed and eliminated, and they presented highly different exposure levels. The area under the concentration-time curves of some volatile components in YCZFD was higher than that in YCZFD VO. The results showed that the water extract of YCZFD increased the exposure of volatile components. Our study provides valuable information for understanding the potential effective components of YCZFD.
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