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Pharmacokinetic behaviors and oral bioavailability of oridonin in rat plasma
Alternative TitlePharmacokinetic behaviors and oral bioavailability of oridonin in rat plasma
Xu Wen1; Sun Jin1; Zhang TingTing1; Ma Bo1; Cui ShengMiao1; Chen DaWei1; He ZhongGui1
2006
Source PublicationACTA PHARMACOLOGICA SINICA
ISSN1671-4083
Volume27Issue:12Pages:1642-1646
AbstractAim: 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 t(max) 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.
Other AbstractAim: 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 spectrometric 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.
KeywordRABDOSIA-RUBESCENS SIGNAL PATHWAYS CELLS oridonin pharmacokinetics intravenous oral bioavailability intraperitoneal injections rats
Indexed ByCSCD
Language英语
CSCD IDCSCD:2618176
Citation statistics
Document Type期刊论文
Identifierhttp://ir.imr.ac.cn/handle/321006/150909
Collection中国科学院金属研究所
Affiliation1.中国科学院金属研究所
2.Guangdong Pharmaceut University
Recommended Citation
GB/T 7714
Xu Wen,Sun Jin,Zhang TingTing,et al. Pharmacokinetic behaviors and oral bioavailability of oridonin in rat plasma[J]. ACTA PHARMACOLOGICA SINICA,2006,27(12):1642-1646.
APA Xu Wen.,Sun Jin.,Zhang TingTing.,Ma Bo.,Cui ShengMiao.,...&He ZhongGui.(2006).Pharmacokinetic behaviors and oral bioavailability of oridonin in rat plasma.ACTA PHARMACOLOGICA SINICA,27(12),1642-1646.
MLA Xu Wen,et al."Pharmacokinetic behaviors and oral bioavailability of oridonin in rat plasma".ACTA PHARMACOLOGICA SINICA 27.12(2006):1642-1646.
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