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.
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Project supported by the Natural Science Foundation of Liaoning Province, China (No 20052058).
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Xu, W., Sun, J., Zhang, Tt. et al. Pharmacokinetic behaviors and oral bioavailability of oridonin in rat plasma. Acta Pharmacol Sin 27, 1642–1646 (2006). https://doi.org/10.1111/j.1745-7254.2006.00440.x
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DOI: https://doi.org/10.1111/j.1745-7254.2006.00440.x
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