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- Title
Inhibition of Monocarboxylate Transporter-Mediated Absorption of Valproic Acid by Gegen-Qinlian-Tang.
- Authors
Liu, Hsueh-Jung; Yu, Chung-Ping; Hsieh, Yow-Wen; Tsai, Shang-Yuan; Hou, Yu-Chi
- 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.
- Subjects
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
- Publication
American Journal of Chinese Medicine, 2013, Vol 41, Issue 2, p369
- ISSN
0192-415X
- Publication type
Article
- DOI
10.1142/S0192415X13500274