恩诺沙星及其代谢产物在南美白对虾体内药代动力学研究

Pharmacokinetics of enrofloxacin and its residue ciprofloxacin in Penaeus vannamei

目的研究恩诺沙星(enrofloxacin,ENR)及其代谢产物环丙沙星(ciprofloxacin,CIP)在虾体内的组织分布和药物代谢随时间的变化规律。方法在(26±2)℃的养殖水温下,以30 mg/(kg·bw)的投喂剂量对南美白对虾进行单次投喂药饵给药,采用高效液相色谱-串联质谱技术(high performance liquid chromatographytandem mass spectrometry,HPLC-MS/MS)进行测定ENR与CIP的含量,其药-时数据通过DAS 2.0动力学软件分析。结果 ENR在南美白对虾体内药时数据符合一级吸收二室模型,而其代谢产物CIP在南美白对虾体内象不符合房室模型。ENR在肝胰腺和肌肉中的最快达峰时间(T_(peak))为1和8 h,达峰浓度(C_(max))分别为24451.2和14212.1μg/kg;药时曲线下面积分别为971766.2和116847.4μg/(L·h);消除半衰期(t1/2β)分别为59.5和33.6 h。CIP在肝胰腺和肌肉中的最快达峰时间(T_(peak))为8和20 h;达峰浓度(C_(max))分别为598.8和4566.6μg/kg。肝胰腺和肌肉的ENR残留量低于最大残留限量(maximum residual limit,MRL)分别为384 h和480 h,而肝胰腺和肌肉中的CIP分别从288和480 h开始低于检出限。结论在(26±2)℃养殖水温下,以30 mg/(kg·bw)剂量对南美白对虾进行单次投饵给药时,建议休药期不得低于20 d。

Objective To investigate the pharmacokinetics of enrofloxacin （ENR） and its metabolic residue ciprofloxacin （CIP） in Penaeus vannamei with time variation. Methods Under the water temperature of （264-2）℃, Penaeus vannamei were fed by single feeding bait delivery in 30 mg/（kg·bw）. The contents of ENR and CIP were determined by high performance liquid chromatography-tandem mass spectrometry （HPLC-MS/MS）. The drug-time data were analyzed by DAS 2 dynamic software. Results The data of ENR in Penaeus vannamei were consistent with the first-order absorption two compartment model, while its metabolite CIP in Penaeus vannamei was not consistent with the atrioventricular model. The peak time （Tpeak） of ENR in hepatopancreas and muscle was 1 and 8 h, the peak concentrations （Cmax） were 24451.2 and 14212.1 μg/kg, respectively. The area under curve were 971766.2 and 116847.4 μg/（L·h）, while the elimination half-life （t1/2β） were 59.5 and 33.6 h, respectively. The peak time （Tpeak） of CIP in hepatopancreas and muscle was 8 and 20 h, while the peak concentrations （Cmax） were 598.8 and 4566.6 μg/kg, respectively. The ENR residues in the hepatopancreas and muscles were lower than the maximum residual limits （MRLs）, which were 384 h and 480 h, respectively. The CIP content in the hepatopancreas and muscles began to be lower than the limit of detection from 288 and 480 h, respectively. Results Under the water temperature of （26±2）℃, when the Penaeus vannamei is fed by single feeding bait delivery in 30 mg/（kg·bw）, the withdrawal period should not be less than 20 d.