Enantioselective metabolism of quizalofop-ethyl in rat

Liang, Wang, Liu, Shen, Liu, Jia, Zhou (2014) Enantioselective metabolism of quizalofop-ethyl in rat PLoS One (IF: 2.9) 9(6) e101052
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Abstract

The pharmacokinetic and distribution of the enantiomers of quizalofop-ethyl and its metabolite quizalofop-acid were studied in Sprague-Dawley male rats. The two pairs of enantiomers were determined using a validated chiral high-performance liquid chromatography method. Animals were administered quizalofop-ethyl at 10 mg kg(-1) orally and intravenously. It was found high concentration of quizalofop-acid in the blood and tissues by both intragastric and intravenous administration, and quizalofop-ethyl could not be detected through the whole study which indicated a quick metabolism of quizalofop-ethyl to quizalofop-acid in vivo. In almost all the samples, the concentrations of (+)-quizalofop-acid exceeded those of (-)-quizalofop-acid. Quizalofop-acid could still be detected in the samples even at 120 h except in brain due to the function of blood-brain barrier. Based on a rough calculation, about 8.77% and 2.16% of quizalofop-acid were excreted through urine and feces after intragastric administration. The oral bioavailability of (+)-quizalofop-acid and (-)-quizalofop-acid were 72.8% and 83.6%.

Links

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4071037
http://www.ncbi.nlm.nih.gov/pubmed/24964043
http://dx.doi.org/10.1371/journal.pone.0101052

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