Hernandez Esther, Rey Raquel, Puig Mariona, Garcia Maria Angeles, Solans Carlos, Bregante Miguel Angel
Department of Pharmacology and Physiology, Faculty of Veterinary Science, University of Zaragoza, Miguel Servet 177, Zaragoza 50013, Spain.
Vet J. 2005 Sep;170(2):237-42. doi: 10.1016/j.tvjl.2004.06.003.
The pharmacokinetics of amoxicillin (Amx) were determined in pigs following intravenous (IV) administration of a single dose of 15 mg/kg and a single dose of 15 mg/kg of a new oral formulation (Amx-FP containing 10% amoxicillin). Residue studies were performed to determine residues in edible tissues of healthy pigs after chronic oral administration of Amx-FP at a daily dose of 15 mg/kg for five consecutive days. After IV administration, the plasma concentration was characteristic of a two-compartment open model. The main pharmacokinetic variables were: t(1/2lambda(n)), MRT=90.1 min, V(darea)=0.81 L/kg and Cl(b)=3.9 mL/kg/min. After single oral administration the main pharmacokinetic variables were: C(max)=758 mug/L, t(max)=347 min and Cl(b/f)=3.7 mL/kg/min for Amx-FP. The oral bioavailability (F) was calculated at 11% for Amx-FP. Based on maximum residue levels (MRL) for AMX in pigs established at 50 microg/kg for all tissues, the withdrawal times of AMX in muscle and skin plus fat were estimated (95% tolerance limit and 95% confidence) to fall below the MRL after a withdrawal period of seven days. Levels of AMX in the liver and kidneys were estimated to fall below the MRL after a withdrawal period of four days.
在猪身上静脉注射15mg/kg单剂量阿莫西林（Amx）以及口服15mg/kg单剂量的一种新口服制剂（含10%阿莫西林的Amx-FP）后，测定了阿莫西林的药代动力学。进行了残留研究，以确定连续5天每天口服15mg/kg Amx-FP的健康猪可食用组织中的残留情况。静脉注射后，血浆浓度符合二室开放模型特征。主要药代动力学变量为：t(1/2lambda(n))、平均滞留时间（MRT）=90.1分钟、稳态分布容积（V(darea)）=0.81L/kg以及清除率（Cl(b)）=3.9mL/kg/分钟。单次口服给药后，Amx-FP的主要药代动力学变量为：最大血药浓度（C(max)）=758μg/L、达峰时间（t(max)）=347分钟以及口服清除率（Cl(b/f)）=3.7mL/kg/分钟。计算得出Amx-FP的口服生物利用度（F）为11%。基于猪所有组织中阿莫西林最大残留限量（MRL）设定为50μg/kg，估计阿莫西林在肌肉、皮肤加脂肪中的停药时间（95%耐受限和95%置信度）在停药7天后低于MRL。估计肝脏和肾脏中的阿莫西林水平在停药4天后低于MRL。
