Pharmacokinetics, Activity, and Residue Elimination of R- and S-Diclazuril in Broiler Chickens.

Journal of Agricultural and Food Chemistry
Meiyu ZhangLimin He

Abstract

Diclazuril (DIC) is widely used as a racemic mixture to prevent and treat coccidiosis in farm animals, while the pharmacokinetics, bioactivity, and toxicity of DIC enantiomers are not known at all. This study first established a simple, sensitive, and reliable liquid chromatography tandem mass spectrometry method for separation of R-DIC and S-DIC and their analyses. Then, it was applied to investigate the stereoselective pharmacokinetics and residual elimination of individual enantiomers, and their anticoccidial activity was also evaluated in broiler chickens. The results indicated that the area under the concentration-time curve (AUC) and elimination half-life (t1/2β) were significantly different (p < 0.05) for two enantiomers in chicken plasma. The AUC and t1/2β of S-DIC were approximately 2 and 1.4 times those of R-DIC, respectively. The residual elimination of DIC enantiomers in chicken tissues was also stereoselective. The concentrations of S-DIC in chicken muscle and liver were greater than those of R-DIC, and it is the opposite in the kidney. There was no significant difference (p > 0.05) in the anticoccidial activity of racemate and enantiomers when a single enantiomer in feed was added above 0.5 mg kg-1. However, the a...Continue Reading

References

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Jul 23, 2016·Drug Design, Development and Therapy·Qian SunDequn Sun
May 7, 2019·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Meiyu ZhangLimin He

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Citations

May 22, 2021·ACS Infectious Diseases·Jinxin ZhengZhijian Yu

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