Metabolism and excretion kinetics of 14C-labeled and non-labeled difloxacin in pigs after oral administration, and antimicrobial activity of manure containing difloxacin and its metabolites.
Metabolism and excretion kinetics of 14C-labeled and non-labeled difloxacin in pigs after oral administration, and antimicrobial activity of manure containing difloxacin and its metabolites.
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DOI：
10.1016/j.envres.2008.12.007
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发表时间：
2009-04
影响因子：
8.3
通讯作者：
P. Sukul;M. Lamshöft;S. Kusari;S. Zühlke;M. Spiteller
中科院分区：
文献类型：
--
作者：
P. Sukul;M. Lamshöft;S. Kusari;S. Zühlke;M. Spiteller
氟喹诺酮类药物是兽药中最重要的抗生素之一。为此，通过给育肥猪使用14c标记和未标记的兽药来研究双氟沙星（DIF）及其代谢物的行为。在每天收集粪便后测定其排泄动力学。采用高分辨率质谱技术，发现主要代谢物为萨拉沙星（Sarafloxacin， SAR），另外还检出了3种微量代谢物。通过与真品的光谱和色谱数据对比，证实了DIF和SAR的鉴别。采用HR-MS/MS对3种微量代谢物进行鉴定。10天后，仅8.1%的给药放射性残留在猪体内，DIF占排泄放射性的95.9%。在粪便中检测和鉴定了99%以上的标记化合物。所有单一电解质的平均回收率为大于或等于94%。在10-10,000μg /kg粪便浓度范围内建立线性关系，相关系数大于或等于0.99。对一组标准病原菌对照进行体外抑菌活性试验，结果表明猪粪中残留的抗生素浓度足够高，具有抑菌活性。
Fluoroquinolones are amongst the most important antibiotics used in veterinary medicine. On this account the behavior of difloxacin (DIF) and its metabolites was investigated by administering the14C-labeled and non-labeled veterinary drug to fattening pigs. The excretion kinetics were determined after daily collection of manure. Sarafloxacin (SAR) was found to be the major metabolite, three further trace metabolites were also recovered, applying high-resolution (HR) mass spectrometric technique. The identification of DIF and SAR was confirmed by comparison with the spectroscopic and chromatographic data of the authentic references. The identification of the three trace metabolites was performed by HR-MS/MS. Only 8.1% of the administered radioactivity remained in the pig after 10 days and DIF accounted for 95.9% of the radioactivity excreted. More than 99% of the labeled compounds were detected and identified in the manure. The mean recoveries for all single electrolytes were ⩾94%. Linearity was established over concentration range 10–10,000μg/kg manure with a correlation coefficient ⩾0.99. By using in vitro antimicrobial activity tests against a group of standard pathogenic control strains, the results showed that the residual antibiotic concentrations in the manure of pigs are high enough to exhibit antibacterial activity.