Add time:07/27/2019         Source:sciencedirect.com

TRITICONAZOLE (cas 131983-72-7) with an asymmetrical carbon atom has two enantiomers and is a broad-spectrum systemic fungicide, but its disposition in animals is unclear. In this study, a chiral analytical method of LC–MS/MS was developed and validated for the assay of triticonazole enantiomers in rat plasma and tissues. There were no endogenous interferences in the blank plasma and tissues of rats. R-(−)- and S-(+)-triticonazole peaks were separated entirely. The calibration curves were linear from 25 to 2500 ng/mL of each enantiomer. The accuracy, precision, and stability met the requirements of bioanalysis. Therefore, this method is enantioselective, accurate, precise, sensitive and reliable, and has been successfully applied to analyze R-(−)- and S-(+)-triticonazole in rat plasma and to study the toxicokinetics of triticonazole enantiomers in rats. After single oral administration of 50 mg/kg racemate triticonazole to rats, the AUC (0-∞) and Cmax of R-(−)-triticonazole were 3.5 and 3.6 times higher than that of S-(+)-triticonazole, respectively. The content of S-(+)-triticonazole was higher in the kidney whilst R-(−)-triticonazole was higher in the brain and small intestine. The results showed that the toxicokinetics and tissues distribution of triticonazole enantiomers in rats have stereoselective differences.

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