恩诺沙星在三疣梭子蟹主要组织中的代谢动力学

Pharmacokinetics of enrofloxacin in main tissues Portunus trituberculatus

应用反相高效液相色谱法(RP-HPLC)研究了三疣梭子蟹(portunus trituberculatus)经口灌10 mg/kg恩诺沙星后体内的药代动力学规律。结果表明口灌给药后,三疣梭子蟹肝胰腺、肌肉和血淋巴组织中的恩诺沙星达峰速度快,肝胰腺和血淋巴在给药24h都有双峰现象出现。恩诺沙星在肝胰腺、肌肉、血淋巴中的Cmax分别为11.235μg/g、0.850μg/g和0.858μg/g,Vd/F为7.954 L/kg、10.367 L/kg和0.345 L/kg。t1/2β分别为283.361 h、47.869 h和17.681 h,AUC分别为245.618μg/g.h、24.753μg/g.h和20.111μg/g.h。给药后5 min在肝胰腺中即可检测到恩诺沙星的代谢产物环丙沙星,而肌肉和血淋巴在给药后2 h才能检测到,其含量均处于较低水平。用3P97软件对各组织中的药时数据进行房室模型拟合,结果显示:三疣梭子蟹口灌给药后,恩诺沙星在血淋巴、肌肉和肝胰腺中的代谢过程均符合一级吸收二室开放模型,而环丙沙星不能用房室模型来描述。

The pharmacoknetics of enroflxacin in Portunus trituberculatus were investigated after oral administration of enrofloxacin（ENR） at single dose of 10 mg/kg by reverse-phase high performance liquid chromatography（RP-HPLC）.The level of enrofloxacin in three tissues reached the maximum concentration（Cmax） quickly,the double peak were observed in the hepatopancrea and hemolymph（24 h）.The maximal concentration of enrofloxacin in hepatopancrea,muscle and hemolymph was 11.235 g/g,0.850 g/g and 0.858 g/g,respectively.The apparent volume of distribution（Vd/F） was 7.954 L/kg,10.367 L/kg and 0.345 L/kg,respectively.The elimination half-life（t1/2β） was 283.361 h,47.869 h and 17.681 h,respectively.The area under the curve（AUC） was 245.618μg/g·h,24.753μg/g·h and 20.111μg/g·h,respectively.Ciprofloxacin,the main active metabolite of enrofloxacin,was detected in hepatopancrea after administration shortly（5 min）,while detected at 2 h in muscle and hemolymph showing relatively low levels.Enroflxacin concentrations versus time data were analyzed by one-,two-or three-compartment open model on Practical Pharmacokinetics Program（3P97）.The results demonstrated that enrofloxacin in three tissues from P.trituberculatus was well described by a two-department open model with first-order absorption,but ciprofloxacin in tissues could not be described by a one-or two-compartment open model.