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头孢喹肟在罗非鱼体内的药代动力学
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摘要
为临床合理用药提供参考,研究在单次给药(10 mg/kg)途径下,头孢喹肟在罗非鱼体内的药代动力学。单剂量肌肉注射和腹腔注射给药后,高效液相色谱法(HPLC)测定血浆中头孢喹肟含量,并用Win Nonlin药动学软件的对实验数据进行了分析。结果表明:头孢喹肟在罗非鱼体内的药动学曲线符合二室开放模型。肌肉注射给药后,药物吸收和消除均较快,体内分布广泛。主要药动学参数为:T_(max)为0.14 h,T1/2ka为0.028h,T1/2b为5.81 h,Vd/F为0.41 L/kg,AUC为204.6μg h/mL。腹腔注射给药后,药物吸收和消除均较慢,体内分布广泛。T_(max)为0.17 h,T1/2ka为0.035 h,T1?2b为6.05h,Vd/F为0.33 L/kg,AUC为267.8μg·h/mL。通过测定头孢喹肟对30株感染罗非鱼体内分离的无乳链球菌的体外抑菌情况,得出其最小抑菌浓度(MIC)值在0.015-0.12μg/mL之间。鉴于以上结果可得出,每日10mg/kg剂量的头孢喹肟能够有效控制由大多数致病菌引起的罗非鱼感染。
The pharmacokinetics of cefquinome in tilapia(Oreochromis niloticus) after a single dose(10 mg/kg) was evaluated to provide references for clinical rational use of drugs. After intramuscular(i.m.) or intraperitoneal(i.p.) administration, the drug concentration in plasma was measured using the high performance liquid chromatography(HPLC), and analyzed by the compartment model of Win Nonlin software. The result was obtained that the concentrations versus time in plasma were well described by a two-department open model. After i.m.administration cefquinome, absorption and elimination were relatively faster and it was widely distributed throughout the body. The main pharmacokinetics parameters were T_(max) 0.14 h, T1/2ka0.028 h, T1/2b 5.81 h, Vd/F 0.41 L/kg, AUC 204.6 μg h/mL. Following i.p. injection, drug absorption and elimination were relatively slower and it was widely distributed throughout the body.
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