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中文摘要：
【目的】研究中华绒螯蟹血淋巴中左氧氟沙星的抗嗜水气单胞菌（Aeromonas hydrophila）活性,为防治水产动物细菌性败血症提供参考。【方法】按15.00 mg/kg的剂量对中华绒螯蟹进行肌肉注射左氧氟沙星,分别于药前和给药后（0.083~160 h）的13个时间点采集血淋巴,每个时间点取4只蟹,然后进行体外与体内抗菌药效试验,运用3P97和Kinetica 4.4软件对半体内数据进行处理后,通过药动学—药效学（PK-PD）同步模型确定给药方案。【结果】左氧氟沙星在普通营养肉汤和未给药血淋巴中对嗜水气单胞菌HN08的MIC均为1.00μg/m L。对中华绒螯蟹进行肌肉注射给药后,Cmax为86.86μg/m L,吸收半衰期t1/2（α）为2.39 h,消除半衰期t1/2（β）为48.94 h,滞后时间TL为0 h,即左氧氟沙星在中华绒螯蟹血淋巴中符合开放型二室模型。在半效应室内,EC50为10.61 h,AUC0~24/MIC血淋巴为25.37 h,Cmax/MIC血淋巴为35.92h。通过PK-PD同步模型分析,得出临床使用左氧氟沙星防治中华绒螯蟹细菌性败血症的给药剂量为5.41~21.08mg/kg。【结论】左氧氟沙星在较长时间内对嗜水气单胞菌HN08产生较强抑制作用,且呈浓度依赖性杀菌特点,在中华绒螯蟹体内的药代动力学符合二室模型。针对中华绒螯蟹细菌性败血症的最佳给药方案：以5.41 mg/kg的剂量,每天肌肉注射给药1次可达到预防目的;以21.08 mg/kg的剂量,每天肌肉注射给药1次可达到治疗目的。
英文摘要：
[Objective]The present experiment was conducted to investigate the antibacterial activity of levofloxacin on Aeromonas hydrophila in Enocheir sinensis hemolymph in order to provide references for treatment and prevention of bacterial haemorrhagic septicemia in apuatic animals. [Method]Through intramuscular injection of 15.00 mg/kg dose levofloxacin on E. sinensis, their hemolymph were collected at 13 time points of before and after drug administration （0.083-160 h） with four crabs each. The antimicrobial efficacies in vitro and in vivo of levofloxacin were determined, and then its ex vivo data were analyzed by using 3P97 and Kinetica 4.4 softwares. Through constructing pharmacokinetics/ pharmacodynamics （PK-PD） synchronization model, the comprehensive dose regimen was investigated. [ Result ] The MIC of levofloxacin on A. hydrophila HN08 in ordinary nutrient broth and non-administered hemolymph were both 1.00 μg/mL. After intramuscular injection on E. sinensis, Cmax was 86.86 μg/mL, the absorption half-life [t1/2 （α）] 2.39 h, the elimination half-life [t1/2 （13）] 48.94 h and the lag time （TL） 0 h. Therefore, levofloxacin in hemolymph of E. sinensis was accorded with two-compartment open model. In the semi-effect compartment, EC50 was 10.61 h, AUC0-24/MIChemolyuph 25.37 h and Cmax/MIChemolyuph 35.92 h. Levofloxacin of 5.41-21.08 mg/kg was the clinical administration dosage of prevention and treatment bacterial haemorrhagic septicemia by analyzing PK-PD synchronization model. [Conclusion]Levofloxacin has a strong inhibitory effect on A. hydrophila HN08 for a long time and shows concentration-dependent bactericidal feature. Levofloxacin in E. sinensis hemolymph was accorded with two-compartment model. Therefore, aiming at haemorrhagic septicemia of E. sinensis, the best recommended clinical dosing regimenin is intramuscular injection of 5.41 mg/kg dose once a day for prevention, and intramuscular injection of 21.08 mg/kg dose once a day for treatment.
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