适温条件下氟苯尼考在罗非鱼体内的药物动力学

Pharmacokinetics of florfenicol in tilapia fed diet containing the drug

采用HPLC-MS-MS方法,研究了给罗非鱼Oreochromis niloticus×O.caureus单次口服(12 mg/kg)氟苯尼考后其体内的药代谢规律。结果表明:氟苯尼考在罗非鱼体内吸收迅速,1 h后血液和肌肉中的药浓度均超过1.0μg/mL(mg/kg),能够有效杀灭绝大多数水产病菌,Tmax和Cmax分别为5.05 h、6.67μg/mL和6.80 h、8.49 mg/kg,维持有效药物浓度(以MIC=1.0μg/mL计)以上的时间大于50 h,组织滞留时间较长;血液和肌肉中的t1/2β分别为11.18 h和12.67 h,药时曲线下面积分别为148.8μg/(mL.h)和225.2 mg/(kg.h);氟苯尼考在血液中的吸收和消除速率均快于肌肉,但最高药物浓度较肌肉中低。在本试验条件下,给药59 h后罗非鱼各组织中的药物含量均低于美国FDA(1 mg/kg)及加拿大标准(0.8 mg/kg),说明氟苯尼考具有良好的应用价值。

The metabolism and elimination of florfenicol in tilapia（Oreochromis niloticus×O.caureus） following oral treatment at a dose of 12 mg/kg body mass were studied at 28 ℃ by a HPLC-MS-MS method.Results showed that the florfenicol was rapidly absorbed by tilapia 1 h after administration,and more than 1.0 μg florfenicol/mL（lethal to majority of the aquatic bacteria） was found in the tissues.There were Tmax of 5.05 h and Cmax of 6.75 μg/mL in the blood,Tmax of 6.80 h,and Cmax of 8.49 mg/kg in the muscles,and the maintenance of effective concentrations（MIC=1.0 μg/mL） beyond 50 h.The drug had longer retention time,with t1/2β of 11.18 h in blood and 12.67 h in the muscle,which AUC were 148.8 μg/（mL·h）,and 225.2 mg/（kg·h）.There were more rapid absorption and elimination in the blood than those in the muscle where there was higher Cmax.The fish had lower concentration of the florfenicol in the blood and muscles than the standards of U.S.FDA（1 mg/kg） and the Canadian（0.8 mg/kg） 59 h after oral administration.Therefore,florfenicol had great value for the control of diseases in fish.