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Disposition Kinetics of Levofloxacin in Sheep after Intravenous and Intramuscular Administration

机译:绵羊静脉注射和肌肉注射后左氧氟沙星的处置动力学

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摘要

The present study was planned to investigate the disposition kinetics of levofloxacin in plasma of female native Barky breed sheep after single intravenous (IV) and intramuscular (IM) administration of 4 mg/kg body weight. The concentrations of levofloxacin in the plasma were measured using high-performance liquid chromatography (HPLC) with a UV detector on samples collected at 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 4, 6, 8, 10, 12, 18, 24, 32, and 48 h after treatment. Following intravenous injection, the decline in plasma drug concentration was biexponential with half-lives of (t1/2α) 0.33 ± 0.12 h and (t1/2β) 3.29 ± 0.23 h for distribution and elimination phases, respectively. The volume of distribution at steady state V(d(ss)) was 0.86 ± 0.23 l/kg. After intramuscular administration of levofloxacin at the same dose, the peak plasma concentration (Cmax) was 3.1 ± 0.35 μg/mL and was obtained at 1.64 ± 0.29 h (Tmax), the elimination half-life (T1/2el) was 3.58 ± 0.30 h, and AUC was 20.24 ± 1.31 μg.h/mL. The systemic bioavailability was 91.35 ± 6.81 %. In vitro plasma protein binding was 23.74%. When approved therapy fails, levofloxacin may be used in some countries for therapy of food animals, however, that is not true in the US.
机译:本研究旨在研究左氧氟沙星在雌性本地Barky繁殖绵羊血浆中的单剂量静脉内(IV)和肌内(IM)施用4 mg / kg体重后的血浆中处置动力学。使用高效液相色谱(HPLC)和UV检测器测量在0、0.08、0.16、0.33、0.5、1、2、4、6、8、10、12、12收集的样品中血浆中左氧氟沙星的浓度治疗后18、24、32和48 h。静脉内注射后,血浆药物浓度的下降是双指数的,分布和消除阶段的半衰期分别为(t1 /2α)0.33±0.12 h和(t1 /2β)3.29±0.23 h。稳态V(d(ss))的分布体积为0.86±0.23ll / kg。肌注左氧氟沙星剂量相同后,血浆峰浓度(Cmax)为3.1±0.35μg/ mL,在1.64±0.29 h(Tmax)时获得,消除半衰期(T1 / 2el)为3.58±0.30 h,且AUC为20.24±1.31μg.h/ mL。全身生物利用度为91.35±6.81%。体外血浆蛋白结合率为23.74%。当批准的治疗失败时,左氧氟沙星可能会在某些国家/地区用于食用动物的治疗,但是在美国并非如此。

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  • 年度 2010
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  • 正文语种 {"code":"en","name":"English","id":9}
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