Open AccessPharmacokinetic behaviors and oral bioavailability of oridonin in rat plasma 1
Author(s) -
XU Wen,
SUN Jin,
ZHANG Tingting,
MA Bo,
CUI Shengmiao,
CHEN Dawei,
HE Zhonggui
Publication year - 2006
Publication title -
acta pharmacologica sinica
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.514
H-Index - 90
eISSN - 1745-7254
pISSN - 1671-4083
DOI - 10.1111/j.1745-7254.2006.00440.x
Subject(s) - bioavailability , pharmacokinetics , pharmacology , plasma concentration , plasma levels , chemistry , medicine
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.