Systemic exposure of quercetin after administration of feng-liao-chang-wei-kang granules to rats.
OBJECTIVE
The objective of this study was to observe the systemic exposure of quercetin (QCT) including its free and total concentration in rat blood samples following a single p.o. dose of feng-liao-chang-wei-kang granules (FLCWKG).


METHODS
Six male rats were given the FLCHKG and the serial blood samples were collected. Fully or partially validated LC/MS/MS methods were developed to analyze the resulting biosamples. Various pharmacokinetic (PK) parameters were estimated from the plasma concentration versus time data using non-compartmental methods.


RESULTS
Both methods for analysis of the free and total QCT plasma concentration are sensitive, specific, accurate and reliable. The PK parameters of free QCT after administration of FLCWKG, in comparison with total concentration, show a lower C(max) (32.4±8.2 ng/ml versus 164±49 ng/ml), a lower AUC(0→∞) (39.3±6.9 ng/ml h versus 313±16 ng/ml h), a shorter T(max) (0.17±0.00 h versus 0.83±1.01 h) and a similar t(1/2) (3.90±0.88 h versus 3.10±1.94 h), MRT(0→t) (2.27±0.10 h versus 2.86±0.41 h).


CONCLUSIONS
Free QCT was quickly absorbed from gastrointestinal tract and circulated in blood at quite low concentration. The circulating flavonoids originating from this formula were dominantly conjugated derivatives.
Department of Pharmacy, Hainan Medical College, Hainan Provincial Key Laboratory of R&D of Tropical Herbs, Xueyuan Road No. 3, Haikou 571101, China.
Junqing
J
Zhang
Xia
X
Liu
Naiguang
N
Fu
Mingsheng
M
Liu
Yinfeng
Y
Tan
D000818:Animals; D001774:Blood Chemical Analysis; D002681:China; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D020834:Ethnopharmacology; D008297:Male; D008516:Medicine, Chinese Traditional; D010946:Plants, Medicinal / Q000737:chemistry; D028502:Polygonum / Q000737:chemistry; D011794:Quercetin / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D031995:Saxifragaceae / Q000737:chemistry; D053719:Tandem Mass Spectrometry
D004365:Drugs, Chinese Herbal; D011794:Quercetin