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Pharmacokinetics and tissue distribution of 8,9‐epoxy brevifolin in rats, a hepatoprotective constituent isolated from Phyllanthus simplex Retz by liquid chromatography coupled with mass spectrometry method
Author(s) -
Niu Xiaofeng,
Li Weifeng,
He Langchong
Publication year - 2008
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.608
Subject(s) - pharmacokinetics , chromatography , chemistry , bioavailability , detection limit , distribution (mathematics) , oral administration , liquid chromatography–mass spectrometry , pharmacology , mass spectrometry , in vivo , medicine , biology , mathematical analysis , mathematics , microbiology and biotechnology
8,9‐Epoxy brevifolin (EBF) is a novel compound isolated from Phyllanthus simplex Retz ( P. simplex ) and has been demonstrated to possess a hepatoprotective effect. The purposes of the present study were to examine the in vivo pharmacokinetics and tissue distribution of EBF in rats using a liquid chromatography coupled with mass spectrometry quantitative detection method (LC‐MS/MS), with luteolin‐7‐O‐glucoside being employed as an internal standard (IS). The method was validated within the concentration range 20–15 000 ng/ml, and the calibration curves were linear with correlation coefficients of >0.999. The limit of quantitation (LOQ) for EBF was 20 ng/ml. The intra‐assay accuracy and precision ranged from 98.7% to 100.2% and 2.19% to 6.25%, respectively, while the inter‐assay accuracy and precision ranged from 97.5% to 100.3% and 3.35% to 7.28%, respectively. The method was further applied to assess the pharmacokinetics and oral bioavailability of EBF after intravenous and oral administration in rats. The oral bioavailability of EBF was 12.46 ± 2.31%. In the tissue distribution assay, its concentration was higher in the heart (13.2 ± 0.24 µg/g) and liver (14.5 ± 0.19 µg/g) than in other tissues. Copyright © 2008 John Wiley & Sons, Ltd.