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Molecules 2014, 19(5), 5538-5549; doi:10.3390/molecules19055538
Article

Pharmacokinetics, Tissue Distribution, Excretion and Plasma Protein Binding Studies of Wogonin in Rats

, , , , , ,  and *
Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, 24# Tongjiaxiang, Nanjing 210009, Jiangsu, China The authors contributed equally to this work.
* Author to whom correspondence should be addressed.
Received: 31 March 2014 / Revised: 24 April 2014 / Accepted: 25 April 2014 / Published: 29 April 2014
(This article belongs to the Section Natural Products)
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Abstract

Wogonin is a natural anticancer candidate. The purpose of this study was to explore the pharmacokinetic profiles, tissue distribution, excretion and plasma protein binding of wogonin in Sprague—Dawley rats. A rapid, sensitive, and specific LC-MS/MS method has been developed for the determination of wogonin in different rat biological samples. After i.v. dosing of wogonin at different levels (10, 20 and 40 mg/kg) the elimination half-life was approximately 14 min, the AUC0-∞ increased in a dose disproportional manner from 112.13 mg/L·min for 10 mg/kg to 758.19 mg/L·min for 40 mg/kg, indicating a non linear pharmacokinetic profile. After i.g. dosing at 100 mg/kg, plasma levels of wogonin peaked at 28 min with a Cmax value of 300 ng/mL and a very low oral bioavailability (1.10%). Following i.v. single dose (20 mg/kg), wogonin was detected in all examined tissues (including testis) with the highest levels in kidney and liver. Approximately 21% of the administered dose was excreted as unchanged drug (mainly via non-biliairy fecal route (16.33%). Equilibrium dialysis was used to evaluate plasma protein binding of wogonin at three concentrations (0.1, 0.5 and 2 µg/mL). Results indicated a very high protein binding degree (over 90%), reducing substantially the free fraction of the compound.
Keywords: flavonoids; excretion; LC-MS/MS; Scutellaria baicalensis Georgi; wogonin flavonoids; excretion; LC-MS/MS; Scutellaria baicalensis Georgi; wogonin
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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Talbi, A.; Zhao, D.; Liu, Q.; Li, J.; Fan, A.; Yang, W.; Han, X.; Chen, X. Pharmacokinetics, Tissue Distribution, Excretion and Plasma Protein Binding Studies of Wogonin in Rats. Molecules 2014, 19, 5538-5549.

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