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首页> 外文期刊>Veterinary and Animal Science >Pharmacokinetic profile of enrofloxacin and its metabolite ciprofloxacin in Asian house geckos (Hemidactylus frenatus) after single-dose oral administration of enrofloxacin
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Pharmacokinetic profile of enrofloxacin and its metabolite ciprofloxacin in Asian house geckos (Hemidactylus frenatus) after single-dose oral administration of enrofloxacin

机译:巢穴麦克风(Hemidactylus Frenatus)巢口服寄生素巢穴(血红蛋白骨盆)巢氧基酯及其代谢产物环丙沙星的药代动力学谱

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The pharmacokinetics of enrofloxacin and its active metabolite ciprofloxacin were determined following oral administration in 21 Asian house geckos ( Hemidactylus frenatus ) at a dose of 10 mg/kg. Changes in enrofloxacin and ciprofloxacin plasma concentrations were quantified at regular intervals over 72 h (1, 2, 6, 12, 24, 48, and 72 h). Samples were analysed by high-pressure liquid chromatography (HPLC) and the enrofloxacin pharmacokinetic data underwent a two-compartment analysis. Due to the limited ciprofloxacin plasma concentrations above the lower limit of quantification (LLOQ), the ciprofloxacin data underwent non-compartment analysis and the half-life was determined by the Lineweaver-Burke plot and analysis. The enrofloxacin and ciprofloxacin mean half-lives ( t sub?/sub) were 0.95 h (α) / 24.36 h (β), and 11.06 h respectively, area under the curve (AUCsub0-24h/sub) were 60.56 and 3.14 μg/mL*h, respectively, maximum concentrations ( C submax/sub) were 12.31 and 0.24 μg/mL, respectively, and time required to reach the C submax/sub ( T submax/sub) were 1 and 2 h respectively. Enrofloxacin was minimally converted to the active metabolite ciprofloxacin, with ciprofloxacin concentrations contributing only 4.91% of the total fluoroquinolone concentrations (AUCsub0-24h/sub). Based on the pharmacokinetic indices when using susceptibility breakpoints when determined at mammalian body temperature it is predicted that single oral administration of enrofloxacin (10 mg/kg) would result in plasma concentrations effective against susceptible bacterial species inhibited by an enrofloxacin MIC ≤ 0.5 μg/mL in vitro, but additional studies will be required to determine its efficacy in vivo.
机译:在10mg / kg的剂量时,在21个亚洲房屋壁虎(Hemidactylus Frenatus)后测定苯甲酸苯甲酸和活性代谢物环丙沙星的药代动力学。以72小时(1,2,6,12,24,48和72h)定期定期定量苯甲酸辛辛和环丙沙星血浆血浆血浆浓度的变化。通过高压液相色谱(HPLC)分析样品,苯甲酸氧氟沙林药代动力学数据进行了两室分析。由于高于定量下限(LLOQ)的有限的环丙沙星血浆浓度(LLOQ),通过LINEWEAVER-BURKE图和分析确定了非隔室分析和半衰期的环丙沙星数据。富含氧氟沙星和环丙沙星平均半衰期(T β/ sub>)分别为0.95小时(α)/ 24.36h(β)和11.06小时,曲线下面积(AUC 0-24h < /亚>)分别为60.56和3.14μg/ ml * h,分别为12.31和0.24μg/ ml,分别为C MAX所需的时间(t max 分别为1和2 h。苯甲酸克洛克星最小化转化为活性代谢物环丙沙星,具有环氟苯胺浓度仅占总氟喹诺酮浓度的4.91%(AUC 0-24H )。基于药代动力学指数在哺乳动物体温下测定时使用易感性断裂点,预测富含氧氟沙星(10mg / kg)的单一口服施用将导致血浆浓度与富含氧氧氟沙星MIC≤0.5μg/ ml抑制的敏感细菌种类有效体外,但需要额外的研究来确定体内的疗效。

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