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The Pharmacokinetics, Bioavailability, and Excretion Studies of α-Cyperone in Rats by UHPLC-QQQ-MS/MS
Ye Shang1, Yameng Zhu1, Kaili Zhang1
1State Key Laboratory of Chinese Medicine Modernization, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China.
None:
α-Cyperone (C15H22O), a critical bioactive sesquiterpene, serves as a representative chemical compound of Cyperi Rhizoma-a classical functional food. To investigate the pharmacokinetic characteristics of α-cyperone, a quantified method was developed in plasma, bile, urine, and feces by ultra-high-performance liquid chromatography tandem triple quadrupole mass spectrometry (UHPLC-QQQ-MS/MS). After being validated, the developed method was applied in a plasma pharmacokinetic study as well as biliary, urinary, and fecal excretion kinetics studies. It revealed poor absolute bioavailability (F = 1.36%) and rare excretion (total cumulative excretion = 0.022%) of α-cyperone, which suggested extensive first-pass metabolism. This study provided crucial insight into explaining the in vivo process and promoting the further development of α-cyperone.
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