1. Inhibition of Monocarboxylate Transporter-Mediated Absorption of Valproic Acid by Gegen-Qinlian-Tang.
- Author
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Liu, Hsueh-Jung, Yu, Chung-Ping, Hsieh, Yow-Wen, Tsai, Shang-Yuan, and Hou, Yu-Chi
- Subjects
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CHINESE medicine , *ANALYSIS of variance , *ANIMAL experimentation , *ANISOTROPY , *CELL lines , *CROSSOVER trials , *FLUORIMETRY , *HIGH performance liquid chromatography , *DRUG-herb interactions , *MEDICINAL plants , *MOLECULAR structure , *RATS , *RESEARCH funding , *STATISTICS , *T-test (Statistics) , *VALPROIC acid , *DATA analysis , *DATA analysis software , *DESCRIPTIVE statistics , *FLUORESCENT dyes - Abstract
Valproic acid (VPA), an anti-epileptic drug with a narrow therapeutic index, is a substrate of the monocarboxylate transporter (MCT). In this study, we investigated the effect of Gegen-Qinlian-Tang (GQT), a Chinese Medicine prescription containing Puerariae Radix (PR), Scutellariae Radix (SR), Coptidis Rhizoma (CR) and Glycyrrhizae Radix (GR), on the pharmacokinetics of VPA, as a probe drug of MCT, in rats and the underlying mechanism. Sprague-Dawley rats were orally administered VPA with and without GQT in crossover design. The serum concentrations of VPA were determined by a fluorescence polarization immunoassay. The results showed that coadministration with 2.0 and 4.0 g/kg of GQT remarkably decreased the Cmax of VPA by 72% and 74% and reduced the 0-t by 63% and 53%, respectively. The mechanism study using Caco-2 cells revealed that the uptake function of MCT was inhibited by GQT and each component herb. In conclusion, the MCT-mediated absorption of VPA was significantly decreased by GQT and its component herbs. [ABSTRACT FROM AUTHOR]
- Published
- 2013
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