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Aim:To study the intravenous and oral pharmacokinetic behavior of oridonin andits extent of absolute oral bioavailability in rats.Methods:Oridonin was adminis-tered to rats via iv(5,10 and 15 mg/kg),po(20,40 and 80 mg/kg)or ip administra-tion(10 mg/kg).The concentrations of oridonin in rat plasma were determined bya high performance liquid chromatography with electrospray ionization mass spec-trometric detection(HPLC/ESI-MS)method and the pharmacokinetic parameterswere determined by non-compartmental analysis.Results:The plasma concen-tration of oridonin after intravenous administration decreased polyexponentially,and the pharmacokinetic parameters of oridonin were dose-independent withinthe examined range.Oridonin was absorbed rapidly after oral gavage with a t(max)ofless than 15 min;the extent of absolute bioavailability of oridonin following oraladministration was 4.32%,4.58% and 10.8%.The extent of absolute bioavailabilityof oridonin following intraperitoneal administration was 12.6%.Conclusion:Firstorder rate pharmacokinetics were observed for oridonin within the range of ivdoses,while the extent of absolute oral bioavailability was rather low and dose-dependent.The low and dose-dependent extent of oral bioavailability may be dueto the saturation of first-pass effects.
Aim: To study the intravenous and oral pharmacokinetic behavior of oridonin and extent extent of absolute oral bioavailability in rats. Methods: Oridonin was adminis-tered to rats via iv (5,10 and 15 mg / kg), po (20,40 and 80 mg / kg) or ip administra tion (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 parameterswere determined by non-compartmental analysis. Results: The plasma concen-tration of oridonin after intravenous administration decreased polyexponentially, and the pharmacokinetic parameters of oridonin were dose-independent withinthe examined range. Oridonin was absorbed rapidly after oral gavage with at (max) ofless than The extent of absolute bioavailability of oridonin following oraladministration was 4.32%, 4.58% and 10.8%. The extent of absolute bioavailability of oridonin following intraperitoneal administration was 12. 6% .Conclusion: Firstorder rate pharmacokinetics were observed for oridonin within the range of ivdoses, while the extent of absolute oral bioavailability was rather low and dose-dependent. The low and dose-dependent extent of oral bioavailability may be dueto the saturation of first -pass effects.