不同给药方式下培氟沙星在鲤体内的药代动力学研究

Pharmacokinetics of pefloxacin in common carp challenged by a single intramuscular injection and oral administration

在水温为18℃下,按10 mg/kg(体质量)对体质量为(200±30)g的福瑞鲤Cyprinus carpio单次肌肉注射和混饲口灌培氟沙星,于不同时间点采集鲤血浆、肌肉、肝胰脏、肾脏组织,经超高液相色谱法测定各组织中培氟沙星的浓度,并采用DAS 3.0药物代谢动力学软件的非房室模型统计矩方法分析药时数据。结果表明:混饲口灌给药和肌注给药后,培氟沙星的药时曲线下面积(AUC)分别为88.35、139.9 mg·h/L,达峰浓度(Cmax)分别为2.092、3.687 mg/L,达峰时间(Tmax)分别为4.0、0.5 h,消除半衰期(t1/2)分别为22.301、74.357 h,表观分布容积(Vd)分别为5.464、15.342 L/kg,总体清除率(CL)分别为0.170、0.143 L·kg/h。研究表明,肌肉注射给药较混饲口灌达峰时间短,达峰浓度高,半衰期长,生物利用度高。

The concentration of pefloxacin was determined in plasma, muscle, hepatopancreas and kidney of FFRC common carp Cyprinus carpio strain with body weight of （200±30）g challenged by a single intramuscular injection and oral administration at a dose of 10 mg/kg body weight by the ultrahigh performance liquid chromatography at water temperature of 18 ℃, and the data were analyzed by the non-compartmental analysis method of DAS 3 . 0 pharmacokinetic program software to establish a reasonable withdrawal period for pefloxacin in common carp. The Auc was found to be 88. 35 mg·h/L for oral administration and 139. 9 mg·h/L for the injection. The elimination half-life（t1/2） was found to be 22. 301 h after oral administration and 74. 357 h after injection,and the volume of distribution（Vd） 5. 464 L/kg for oral administration and 15. 342 L/kg for the injection. The peak concentration of the pefloxacin （Cmax） was 2. 092 mg/L for oral administration and 3. 687 mg/L for the injection, and the peak time （Tmax） 4. 0 h for oral administration and 0. 5 h for the injection. The total body clearance（CL） of pefloxacin was 0. 170 L·kg/h for oral administration and 0. 143 L·kg/h for the injection. It is concluded that more quickly ab-sorption, higher peak plasma concentration, higher bioavailability and faster elimination is observed in intramuscu-lar injection compared with the oral administration.