Pharmacokinetics and disposition of monoterpene glycosides, derived from Paeonia lactiflora roots (Chishao), after intravenous dosing of antiseptic XueBiJing injection in human subjects and rats

Acta Pharmacologica Sinica
Chen ChengChuan Li

Abstract

Monoterpene glycosides derived from Paeonia lactiflora roots (Chishao) are believed to be pharmacologically important for the antiseptic XueBiJing injection. This study was designed to characterize the pharmacokinetics and disposition of monoterpene glycosides. Systemic exposure to Chishao monoterpene glycosides was assessed in human subjects receiving an intravenous infusion and multiple infusions of XueBiJing injection, followed by assessment of the pharmacokinetics of the major circulating compounds. Additional rat studies were also performed. Membrane permeability and plasma-protein binding were assessed in vitro. A total of 18 monoterpene glycosides were detected in XueBiJing injection (content level, 0.001-2.47 mmol/L); the dose level of paeoniflorin was 85.5% of the total dose of monoterpene glycosides detected. In human subjects, unchanged paeoniflorin exhibited considerable levels of systemic exposure, with elimination half-lives of 1.2-1.3 h; no significant metabolite was detected. Oxypaeoniflorin and albiflorin exhibited low exposure levels, and the remaining minor monoterpene glycosides were negligible or undetected. Glomerular-filtration-based renal excretion was the major elimination pathway of paeoniflorin, which...Continue Reading

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Citations

Dec 22, 2017·International Journal of Molecular Sciences·Solomon Habtemariam
Jan 11, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Solomon Habtemariam
Mar 11, 2018·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Nating ZhangChuan Li
Nov 15, 2020·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Zi-Ying WangMin Li
Mar 2, 2021·Frontiers in Physiology·Zhengcan ZhouYuxin Feng

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