Martínez María-Aránzazu, Ares Irma, Rodríguez José-Luis, Martínez Marta, Martínez-Larrañaga María-Rosa, Isea Gerardo, Anadón Arturo
Department of Toxicology and Pharmacology, Faculty of Veterinary Medicine, Universidad Complutense de Madrid, Madrid, Spain.
Front Vet Sci. 2017 May 24;4:77. doi: 10.3389/fvets.2017.00077. eCollection 2017.
The pharmacokinetics of pefloxacin after single 10 mg/kg BW intravenous (IV) and oral doses were studied in healthy broiler chickens. For 24 h, serial blood samples were obtained after IV and oral administration. Concentrations of pefloxacin and its major metabolite -demethyl pefloxacin (norfloxacin) were measured by use of high-performance liquid chromatography. The plasma concentrations-time data were found to fit a two-compartment open model. For pefloxacin, the elimination half-life () was 8.44 ± 0.48 and 13.18 ± 0.82 h after IV and oral administration, respectively. After single oral dose, pefloxacin was rapidly absorbed with an absorption half-life () and of 0.87 ± 0.07 and 2.01 ± 0.12 h, respectively. Maximum plasma concentration () was 4.02 ± 0.31 µg/mL. Oral bioavailability of pefloxacin was found to be 70 ± 2%. Pefloxacin was converted to -demethyl pefloxacin (norfloxacin). This metabolite represented 5% of the parent drug plasma concentrations. The maximal plasma concentration () of -demethyl pefloxacin (norfloxacin) was calculated as 0.19 ± 0.01 mg/mL. The of -demethyl pefloxacin after oral pefloxacin administration was 10.93 ± 0.80 h. The results indicate that an oral dose of 10 mg pefloxacin/kg BW, every 24 h, should be effective in treatment of the most systemic infections in poultry.
在健康肉鸡中研究了单次静脉注射(IV)和口服10mg/kg体重培氟沙星后的药代动力学。静脉注射和口服给药后24小时内,采集系列血样。使用高效液相色谱法测定培氟沙星及其主要代谢产物去甲基培氟沙星(诺氟沙星)的浓度。血浆浓度-时间数据符合二室开放模型。对于培氟沙星,静脉注射和口服给药后的消除半衰期(t1/2)分别为8.44±0.48小时和13.18±0.82小时。单次口服给药后,培氟沙星迅速吸收,吸收半衰期(t1/2ka)和达峰时间(tmax)分别为0.87±0.07小时和2.01±0.12小时。最大血浆浓度(Cmax)为4.02±0.31μg/mL。培氟沙星的口服生物利用度为70±2%。培氟沙星转化为去甲基培氟沙星(诺氟沙星)。该代谢产物占母体药物血浆浓度的5%。去甲基培氟沙星(诺氟沙星)的最大血浆浓度(Cmax)计算为0.19±0.01mg/mL。口服培氟沙星后去甲基培氟沙星的t1/2为10.93±0.80小时。结果表明,每24小时口服10mg培氟沙星/kg体重应能有效治疗家禽的大多数全身感染。