烟酸诺氟沙星预混剂在罗氏沼虾体内药代动力学及残留消除规律

Pharmacokinetics and residue elimination of niacin norfloxacin premix in Macrobrachium rosenbergii

采用混饲口灌方式给药罗氏沼虾,通过有机萃取及固相萃取等方法提纯净化各组织样本,利用超高效液相色谱(UPLC)法测定样本中药物的浓度,研究烟酸诺氟沙星预混剂在罗氏沼虾体内的药代动力学及残留规律。结果发现,混饲口灌烟酸诺氟沙星预混剂(20 mg/kg体重)后,罗氏沼虾肝胰腺符合药代动力学一级吸收二室开放模型,主要动力学参数如下:达峰时间Tpeak为2.905 h,最大峰浓度Cmax为328.12μg/mL,分布半衰期T1/2α为2.178 h,消除半衰期T1/2β为10.058 h;连续5 d混饲口灌烟酸诺氟沙星预混剂(20 mg/kg体重)后,药物在肝胰腺、血液、肌肉组织的残留低于50μg/kg所需的时间分别为12、4、5 d。

To determine the parameters of pharmacokinetics and residue elimination of niacin norfloxacin premix in Macrobrachium rosenbergii, the M. rosenbergii were fed with niacin norfloxacin premix by oral perfusion, the tissue samples were purified by organic extraction and solid phase extraction. Tile concentrations of niacin norfloxacin were measured by ultra performance liquid chromatography （UPLC）. The results showed that, after M. rosenbergii were oral perfused with niacin norfloxacin premix （20 mg/kg body weight）, the hepatopancreas complied pharmacokinetic two-compartment model with first order absorption. The main pharmacokinetic parameters were as follows： the peak time （Tpeak） was 2.905 h, the maximum peak concentration （Cmax ） was 328.12 μg/mL, the distribution half-life （T1/2α） was 2.178 h, the elimination half-life （T1/2β） was 10.058 h; and after continuous oral perfusion with niacin norfloxaein premixes（20 mg/kg body weight） for 5 days, drug residues time when its concentration less than 50 μg/kg in hepatopanereas, muscle, blood tissue were 12 d, 4 d, 5 d, respectively.