@article{APS3657,
author = {Wen Xu and Jin Sun and Ting-ting Zhang and Bo Ma and Sheng-miao Cui and Da-wei Chen and Zhong-gui He},
title = {Pharmacokinetic behaviors and oral bioavailability of oridonin in rat plasma},
journal = {Acta Pharmacologica Sinica},
volume = {27},
number = {12},
year = {2016},
keywords = {},
abstract = {Aim: To study the intravenous and oral pharmacokinetic behavior of oridonin and its extent of absolute oral bioavailability in rats.
Methods: Oridonin was administered to rats via iv (5, 10 and 15 mg/kg), po (20, 40 and 80 mg/kg) or ip administration (10 mg/kg). The concentrations of oridonin in rat plasma were determined by a high performance liquid chromatography with electrospray ionization mass spec-trometric detection (HPLC/ESI-MS) method and the pharmacokinetic parameters were determined by non-compartmental analysis.
Results: The plasma concentration of oridonin after intravenous administration decreased polyexponentially, and the pharmacokinetic parameters of oridonin were dose-independent within the examined range. Oridonin was absorbed rapidly after oral gavage with a tmax of less than 15 min; the extent of absolute bioavailability of oridonin following oral administration was 4.32%, 4.58% and 10.8%. The extent of absolute bioavailability of oridonin following intraperitoneal administration was 12.6%.
Conclusion: First order rate pharmacokinetics were observed for oridonin within the range of iv doses, while the extent of absolute oral bioavailability was rather low and dose-dependent. The low and dose-dependent extent of oral bioavailability may be due to the saturation of first-pass effects.},
issn = {1745-7254}, url = {http://www.chinaphar.com/article/view/3657}
}