恩诺沙星在黑鲪体内的药物代谢动力学研究

Pharmacokinetics of enrofloxacin in Sebastodes fuscescens

研究了单剂量灌服给药方式下,黑鲪肌肉和血液中恩诺沙星(EF)及其代谢产物环丙沙星(CF)的代谢动力学规律。结果表明:18℃条件下,黑鲪单次灌服剂量20mg.kg-1EF后,其肌肉和血液中的药物代谢动力学房室模型符合二房室模型,吸收半衰期t1/2ka分别为2.015和2.173h,分布半衰期t1/2α分别为3.267和2.908h,消除半衰期t1/2β分别为31.416和23.675h,达峰时间Tmax均为4h,峰值分别为10.250和2.765μg.mL-1。代谢物环丙沙星在黑鲪肌肉和血液中符合一房室模型,一级吸收速率常数Ka分别为0.422和0.501h-1,一级消除速率常数K分别为2.568和0.028h-1,吸收半衰期t1/2ka分别为1.644和1.384h,消除半衰期t1/2β分别为2.734和1.927h,达峰时间分别为4和6h,峰值分别为0.496和0.030μg.mL-1。建议18℃条件下休药期大于35d。

In this article, Sebastodes fuscescens was treated orally with enrofloxacin （EF） via stomach tube at a single dose of 20 mg＇kg-1 at 18 ℃. Concentration of the drugs in muscle and blood was determined by high performance liq- uid chromatography （HPLC）. The concentration - time data were analyzed with DAS2. 0. The results were as follows： the EF in muscle and blood concentration -time data were best described by two -compartment model; the absorption half-life time were 2.015 h and2. 173 h, the distribution half-life （t1/2α） were 3.267 h and 2.908 h, the elimination half- life （t1/2β） were 31. 416 h and 23. 675 h ,the time of peak concentration （Tmax ） was 4 h, the maximum EF concentration （ Cmax ） were 10. 250 μg .mL-1 and 2. 765 μg .mL-1. Ciprofloxacin （CF） and, the metabolite of enrofloxacin, can be detected in muscle and blood of Sebastodes fuscescens . The values of main pharmacokinetics parameters Ka, K, t1/2ka, t1/2, Tmax, Cmax were as follows： 0.501 and 0. 422 h -1,0. 036 and 2. 253 h-1, 1. 384 and 1. 644 h, 2. 734 h and 1 927 h, 4h and 6h, 0.496 and 0. 030 μg mL-1. Base on those data, it was suggested that the consecutive days should be above 35 d at 18 ℃.