诺氟沙星在大菱鲆体内药代动力学及残留消除规律

Studies on pharmacokinetics and the elimination regularity of norfloxacin residues in Scophthalmus maximus

利用高效液相色谱法分别测定了单次和多次混饲口灌大菱鲆诺氟沙星(NFLX)后鱼体主要组织中的NFLX含量。通过MCP-KP药动学程序对NFLX在大菱鲆体内的药代动力学及残留消除规律进行了分析研究。结果表明,以30mg/kg的剂量单次混饲口灌大菱鲆,NFLX在大菱鲆体内的达峰时间(Tmax)为2h,血、鳃、肾脏、肝脏、肌肉的达峰浓度(Cmax)分别为:8.365、7.519、1.871、6.485和4.060μg/g;NFLX在组织中的消除半衰期(T1/2)由小到大依次为:肝脏8.18h<肌肉12.39h<鳃丝15.29h<血液23.22h<肾脏23.25h。连续5d以30mg/kg的剂量混饲口灌大菱鲆,消除半衰期(T1/2)由小到大依次为:肌肉74.88h<血液98.16h<肝脏186.43h<鳃192.12h<肾脏200.45h。以上研究表明,诺氟沙星在大菱鲆体内的吸收较为迅速,有利于疾病的预防和治疗用药。在组织中以肾脏中的残留最为显著。使用诺氟沙星进行大菱鲆疾病的预防和治疗时,至少停药30d后方可上市销售。

The contents of NFLX in turbot （Scophthalmus maximus） were determined with High Performance Liquid Chromatography. By using MCP-KP practical pharmacokinetics software, the pharmacokinetics and the elimination regularity of NFLX residues in turbot were investigated. The results showed that the peak time of NFLX （T ） was about 2 h after oral administration at the dose of 30 mg/kg NFLX. The peak content （Cmax） and elimination half life （T1/2） were 8. 365 μg/ml and 23.22 h in blood, 7. 519 μg/g and 15.29 h in gill, 1. 871 μg/g and 23.25 h in kidney, 6. 485 μg/g and 8.18 h in liver, and 4. 060 μg/g and 12.39 h in muscle, respectively. After 5d oral administration at the dose of 30 mg/kg NFLX, T1/2was in the sequence of muscle （74. 88 h） 〈 blood （98. 16h） 〈 liver （186. 43h） % gill （192. 12h） 〈 kidney （200.45h）. The analysis revealed that turbot absorbed NFLX rather rapidly, and that kidney was the highest in NFLX residue among the main tissues of turbot. It is suggested that turbot come into the market at least 30d after ceasing utilization of the drug when NFLX is used for disease prevention and treatment.