Pharmacokinetic behaviors and oral bioavailability of oridonin in rat plasma

IMR OpenIR

	Pharmacokinetic behaviors and oral bioavailability of oridonin in rat plasma
其他题名	Pharmacokinetic behaviors and oral bioavailability of oridonin in rat plasma
	Xu Wen 1; Sun Jin 1; Zhang TingTing 1; Ma Bo 1; Cui ShengMiao 1; Chen DaWei 1; He ZhongGui 1
	2006
发表期刊	ACTA PHARMACOLOGICA SINICA
ISSN	1671-4083
卷号	27 期号:12 页码:1642-1646
摘要	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 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.
其他摘要	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 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.
关键词	RABDOSIA-RUBESCENS SIGNAL PATHWAYS CELLS oridonin pharmacokinetics intravenous oral bioavailability intraperitoneal injections rats
收录类别	CSCD
语种	英语
CSCD记录号	CSCD:2618176
引用统计
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/150909
专题	中国科学院金属研究所
作者单位	1.中国科学院金属研究所 2.Guangdong Pharmaceut University
推荐引用方式 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.