恩诺沙星及其代谢物在俄罗斯鲟多组织中的 代谢及消除研究

Metabolic and elimination rules of enoxacin and its metabolites in Acipenser gueldenstaedtii

中文关键词:  俄罗斯鲟  口灌给药  恩诺沙星  代谢与消除  休药期

英文关键词:Acipenser gueldenstaedtii  oral administration  enrofloxacin  metabolism and elimination  withdrawal time

中文摘要:

      目的 研究恩诺沙星及其代谢产物环丙沙星在俄罗斯鲟中的代谢及消除规律, 制定恩诺沙星在俄罗斯鲟体内的休药期。方法 在水温12~15 ℃条件下, 以60 mg/(kg?bw)剂量对体重为(750±50) g的健康俄罗斯鲟灌服恩诺沙星, 灌服后的0~3360 h内不间断采样, 使用高效液相色谱-串联质谱仪测定各组织内恩诺沙星及其代谢产物含量。结果 灌药后, 恩诺沙星在俄罗斯鲟鳃、血浆、肌肉、肝脏、肾脏、皮肤中达峰时间Tmax分别为0.25、9、12、12、18、24 h; 肾脏、肝脏、皮肤、肌肉、鳃、血浆达峰浓度Cmax分别为31.863、23.435、21.434、18.640、10.342、2.599 mg/kg; 消除半衰期以皮肤最大t1/2为394.431 h、血浆最小为129.6 h。鳃中药物浓度有2个峰值, 第1次达峰时, 血浆中药物浓度远低于鳃, 推测与受试鱼进食习惯或组织结构有关。代谢产物环丙沙星代谢及消除趋势与恩诺沙星大致相同, 血浆最早达峰, Tmax为12 h, 达峰浓度以肝脏和肾脏较高, Cmax分别为6.876 mg/kg和5.648 mg/kg。结论 从水产品质量安全角度应用本研究结果: 以皮肤和肌肉作为可食性组织, 恩诺沙星和环丙沙星残留总量不超过0.1 mg/kg至少需要100 d。

英文摘要:

      Objective To investigate the metabolism and elimination of enrofloxacin and its metabolite ciprofloxacin in Russian sturgeon, and establish the resting period of enrofloxacin in the Acipenser gueldenstaedtii. Methods At the water temperature of 12?15 ℃, Acipenser gueldenstaedtii weighted (750±50) g were fed by oral administration in 60 mg/(kg?bw), and then the samples were collected during 0~3360 h. The content of enrofloxacin and its metabolites in tissues were determined by high performance liquid chromatography-tandem mass spectrometer (HPLC–MS). Results The time of peak concentration (Tmax) of the gill, blood, muscle, liver, kidney and skin was 0.25, 9, 12, 12, 18, 24 h after oral administration respectively, and the maximum enrofloxacin concentration (Cmax) of the kidney, liver, skin, muscle, gill and blood was 31.863, 23.435, 21.434, 18.640, 10.342, 2.599 mg/kg, respectively. The elimination half-life (t1/2) in skin was the largest with the value of 394.431 h and the t1/2 in blood was the minimum with the value of 129.6 h. The drug concentration in the gills had 2 peaks, and at the first peak, the drug concentration in the plasma was far lower than that in the gills, which was speculated to be related to the feeding habit or tissue structure of the tested fish. The metabolism and elimination trend of ciprofloxacin were similar to that of enrofloxacin, Tmax of the blood with value of 12 h was the minimum, the Cmax of liver and kidney with value of 6.876 mg/kg and 5.648 mg/kg was the largest. Conclusion Application of the results of this study from aquatic product quality safety perspective: using skin and muscle as edible tissues, it needs not less than 100 days when the total residual amount of enrofloxacin and ciprofloxacin is not more than 0.1 mg/kg.