Pharmacokinetic behaviors and oral bioavailability of oridonin in rat plasma

作     者：Wen XU~2 Jin SUN~2 Ting-ting ZHANG~2 Bo MA~2 Sheng-miao CUI~3 Da-wei CHEN~2 Zhong-gui HE~(2,4)2 Department of Pharmaceutics,School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China 3 Department of Pharmacy,Guangdong Pharmaceutical University,Guangzhou 510006,China 

作者机构：DepartmentofPharmaceuticsSchoolofPharmacyShenyangPharmaceuticalUniversityShenyang110016China DepartmentofPharmacyGuangdongPharmaceuticalUniversityGuangzhou510006China 

出 版 物：《Acta Pharmacologica Sinica》 (中国药理学报(英文版))

年 卷 期：2006年第27卷第12期

页      面：1642-1646页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 1002[医学-临床医学] 10[医学] 100602[医学-中西医结合临床] 

基　　金：Project supported by the Natural Science Foundation of Liaoning Province China(№20052058). 

主　　题：oridonin pharmacokinetics intravenous oral bioavailability intraperitoneal injections rats 

摘      要：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.