Background: Alpiniae oxyphyllae Fructus (AOF), a traditional Chinese medicine (TCM), is widely
used in the treatment of urinary, gastrointestinal and neurologic diseases in China. Although terpenoids are the
main active ingredients of AOF, there are few researches on their pharmacokinetics and metabolism.
Methods: In this study, a sensitive, rapid, accurate and novel ultra high performance liquid chromatography tandem
mass spectrometry (UPLC-MS/MS) method was established to evaluate the pharmacokinetic behavior of
five terpenoids (oxyphyllenodiol B, (4S*,5E,10R*)-7-oxo-tri-nor-eudesm-5-en-4β-ol, 7-epi-teucrenone, (+)-
(4R,5S,7R)-13-hydroxynootkatone, (E)-labda-12,14-dien-15(16)-olide-17-oic acid) in rats after oral administration
of AOF extracts. 27 metabolic metabolites of the five terpenoids were identified by ultra high performance
liquid chromatography -Q Exactive hybrid quadrupole-orbitrap high-resolution accurate mass spectrometry
(UHPLC-Q-Orbitrap HRMS) based on precise mass and fragment ions.
Results: The established pharmacokinetic analysis method showed good linearity over a wide concentration
range, and the lower quantitative limit (LLOQ) ranged from 0.97 to 4.25 ng/mL. Other validation parameters
were within the acceptable range. In addition, 27 metabolites were identified in plasma, urine and feces samples,
and the metabolic pathways of five terpenoids were mainly focused on glucoside conjugation, dehydration,
desaturation and glycine conjugation.
Conclusion: This is the first study on the pharmacokinetics and metabolism of five terpenoids in AOF, illuminating
the disposal process of terpenoids in vivo. It was expected that the results of this study would provide
some references for the apprehension of the action mechanism and the further pharmacological study of five terpenoids