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1、中国农业科学2006,39(2):418-424ScientiaAgriculturaSinica甲磺酸达氟沙星在鲫体内药物动力学及残留研究11112111潘玉善，操继跃，方之平，王翔凌，潘黔生，丁方科，葛建，彭玉芬12(华中农业大学动物医学院，武汉430070；华中农业大学水产学院，武汉430070)摘要：【目的】研究甲磺酸达氟沙星(Danofloxacinmesylate,DFM)在鲫体内的药物动力学和残留消除规律。-1【方法】在试验水温20℃时，鲫以10mg·kgb.w的剂量单次经口灌服甲磺酸达氟沙星后，用液
2、－液提取、反相高效液相色谱法（RP-HPLC）测定血浆和组织中DFM的浓度。盐酸氧氟沙星做为内标。房室模型分析表明，其药物时间数据符合有吸收二室模型，吸收、分布迅速，但消除缓慢，半衰期（T1/2Ka、T1/2α、T1/2β）分别为0.63、4.96、-1-147.79h，最大血药浓度（Cmax）为3.23µg·ml，达峰时间（TP）为2.73h，药时曲线下面积（AUC）为154µg·h·ml。非房室模型分析表明，平均滞留时间（MeanResidenceTime,MRT）为58.56h。【结果】组织中药物浓度在测定时
3、间里均显著高于血浆（P＜s0.05），消除快慢依次为肾脏、肝胰脏、血浆、肌肉和皮肤，其消除半衰期分别为33、44、48、51、177h。与其它组织相比皮肤消除最慢，建议其作为DFM在鲫体内的残留靶组织。在20℃时,皮-1肤以100µg·kg为最高残留限量（maximumresiduelimit,MRL）建议休药期不低于23d。关键词：鲫；甲磺酸达氟沙星；药物动力学；休药期PharmacokineticsandResiduesofDanofloxacinMesylateinGoldfish(Carassiusaura
4、tusLinnaeus)11112PANYu-shan,CAOJi-yue,FANGZhi-ping,WANGXiang-ling,PANQian-sheng,111DIANGFang-ke,GEJian,PENGYu-fen12（CollegeofVeterinaryMedicine,HuazhongAgriculturalUniversity，Wuhan430070；CollegeofAquaculture,HuazhongAgriculturalUniversity,Wuhan430070)Abstract:
5、【Objectiveandmethod】Theplasmapharmacokineticsandtissueresiduesofdanofloxacinmesylate(DFM)were-1investigatedingoldfish,underexperimentalfieldconditionsat20℃aftersingleoralgavageadministration(10mg·kgb.w).Thedanofloxacinconcentrationsinplasmaandtissuessampleswer
6、edeterminedbyusingreversed-phasehighperformanceliquidchromatography（RP-HPLC）afterliquid-liquidextraction.Ofloxacinhydrochloridewasselectedasinternalstandard.Plasmaconcentration-timedataofDFMwerebestfittedusingatwo-compartmentalopenmodel,withabsorption,distribu
7、tionand-1eliminationhalf-lifeof0.63,4.96and47.79h,respectively.Themaximalplasmaconcentrationwas3.23μg·ml,peakingat2.73h-1afterdosing.Areaundertheplasmadrugconcentration-timecurvefrom0to∞was154μg·h·ml.Themeanresidencetime(MRT)was58.56husingnon-compartmentalanal
8、ysisbasedonstatisticalmomenttheory.【Results】TheresultsindicatedthattheconcentrationofDFMinkidney,liver,plasma,muscleandskinwassignificantlyhigherthanthatinplasma,witheliminationhal
