| Pharmacokinetic behaviors and oral bioavailability of oridonin in rat plasma | |
| Alternative Title | Pharmacokinetic 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 Publication | ACTA PHARMACOLOGICA SINICA
 |
| ISSN | 1671-4083 |
| Volume | 27Issue:12Pages:1642-1646 |
| 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 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 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 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. |
| Keyword | RABDOSIA-RUBESCENS SIGNAL PATHWAYS CELLS oridonin pharmacokinetics intravenous oral bioavailability intraperitoneal injections rats |
| Indexed By | CSCD |
| Language | 英语 |
| CSCD ID | CSCD:2618176 |
| Citation statistics | |
| Document Type | 期刊论文 |
| Identifier | http://ir.imr.ac.cn/handle/321006/150909 |
| Collection | 中国科学院金属研究所 |
| Affiliation | 1.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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