Anadón Arturo, Martínez Maria Aranzazu, Martínez Marta, Ríos Alba, Caballero Virginia, Ares Irma, Martínez-Larrañaga Maria Rosa
Department of Toxicology and Pharmacology, Faculty of Veterinary Medicine, Universidad Complutense de Madrid, Madrid, Spain.
J Agric Food Chem. 2008 Nov 26;56(22):11049-56. doi: 10.1021/jf802138y.
Chickens were used to investigate plasma disposition of florfenicol after single intravenous (i.v.) and oral dose (20 mg kg-1 body weight) and to study residue depletion of florfenicol and its major metabolite florfenicol-amine after multiple oral doses (40 mg kg-1 body weight, daily for 3 days). Plasma and tissue samples were analyzed using a high-performance liquid chromatography (HPLC) method. After i.v. and oral administration, plasma concentration-time curves were best described by a two-compartment open model. The mean [ +/- standard deviation (SD)] elimination half-life (t1/2beta) of florfenicol in plasma was 7.90 +/- 0.48 and 8.34 +/- 0.64 h after i.v. and oral administration, respectively. The maximum plasma concentration was 10.23 +/- 1.67 microg mL-1, and the interval from oral administration until maximal concentration was 0.63 +/- 0.07 h. Oral bioavailability was found to be 87 +/- 16%. Florfenicol was converted to florfenicol-amine. After multiple oral dose (40 mg kg-1 body weight, daily for 3 days), in kidney and liver, concentrations of florfenicol (119.34 +/- 31.81 and 817.34 +/- 91.65 microg kg-1, respectively) and florfenicol-amine (60.67 +/- 13.05 and 48.50 +/- 13.07 microg kg-1, respectively) persisted for 7 days. The prolonged presence of residues of florfenicol and florfenicol-amine in edible tissues can play an important role in human food safety, because the compounds could give rise to a possible health risk. A withdrawal time of 6 days was necessary to ensure that the residues of florfenicol were less than the maximal residue limits or tolerance established by the European Union.
使用鸡来研究单剂量静脉注射（i.v.）和口服（20 mg/kg体重）氟苯尼考后的血浆处置情况，并研究多次口服剂量（40 mg/kg体重，每日一次，共3天）后氟苯尼考及其主要代谢产物氟苯尼考胺的残留消除情况。使用高效液相色谱（HPLC）法分析血浆和组织样本。静脉注射和口服给药后，血浆浓度-时间曲线最适合用二室开放模型描述。静脉注射和口服给药后，氟苯尼考在血浆中的平均[±标准差（SD）]消除半衰期（t1/2β）分别为7.90±0.48小时和8.34±0.64小时。最大血浆浓度为10.23±1.67μg/mL-1，口服给药至最大浓度的时间间隔为0.63±0.07小时。口服生物利用度为87±16%。氟苯尼考转化为氟苯尼考胺。多次口服剂量（40 mg/kg体重，每日一次，共3天）后，在肾脏和肝脏中，氟苯尼考（分别为119.34±31.81和817.34±91.65μg/kg-1）和氟苯尼考胺（分别为60.67±13.05和48.50±13.07μg/kg-1）的浓度持续7天。氟苯尼考和氟苯尼考胺在可食用组织中残留时间的延长对人类食品安全可能具有重要影响，因为这些化合物可能会带来健康风险。需要6天的休药期以确保氟苯尼考的残留量低于欧盟规定的最大残留限量或耐受量。
