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Pharmacokinetics urinary excretion and dosage regimen of levofloxacin following a single intramuscular administration in cross bred calves

机译:杂交牛犊单次肌内给药后左氧氟沙星的药代动力学尿排泄和剂量方案

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摘要

The pharmacokinetics and urinary excretion following single intramuscular administration of levofloxacin at a dose of 4 mg/kg was investigated in seven male cross bred calves. Appreciable plasma concentration of levofloxacin (0.38 ± 0.06 µg/ml) was detected at 1 min after injection and the peak plasma level of 3.07 ± 0.08 µg/ml was observed at 1 h. The drug level above MIC90 in plasma was detected up to 12 h after administration. Rapid absorption of the drug was also evident by the high value of the absorption rate constant (2.14 ± 0.24 /h). The overall systemic bioavailability of levofloxacin, after intramuscular administration, was 56.6 ± 12.4%. The high value of AUC (7.66 ± 0.72 mg . h/ml) reflected the vast area of body covered by drug concentration. Extensive distribution of the drug into various body fluids and tissues was noted by the high value of Vdarea (1.02 ± 0.05 l/kg). The high ratio of AUC/MIC (76.6 ± 7.25) obtained in this study indicated excellent clinical and bacteriological efficacy of levofloxacin in calves. The elimination half-life and MRT were 3.67 ± 0.4 h and 5.57 ± 0.51 h, respectively. The total body clearance (ClB) was 204.9 ± 22.6 ml/kg/h. On the basis of the pharmacokinetic parameters, a suitable intramuscular dosage regimen for levofloxacin in calves would be 1.5 mg/kg repeated at 12 h intervals.
机译:在七只雄性杂交犊牛中,对肌注左氧氟沙星单次肌肉注射4 mg / kg后的药代动力学和尿排泄进行了研究。注射后1分钟可测出左氧氟沙星的血浆浓度(0.38±0.06 µg / ml),在1 h时可观察到3.07±0.08 µg / ml的峰值血浆水平。给药后长达12小时,血浆中MIC90以上的药物水平被检测到。高吸收率常数值(2.14±0.24 / h)也证明了药物的快速吸收。肌肉注射后,左氧氟沙星的总体全身生物利用度为56.6±12.4%。高AUC值(7.66±0.72 mg。h / ml)反映了药物浓度覆盖的大面积区域。 Vdarea(1.02±0.05 l / kg)的高值表明了该药物在各种体液和组织中的广泛分布。这项研究中获得的高AUC / MIC比(76.6±7.25)表明左氧氟沙星在犊牛中具有出色的临床和细菌学功效。消除半衰期和MRT分别为3.67±0.4 h和5.57±0.51 h。总体清除率(ClB)为204.9±22.6 ml / kg / h。根据药代动力学参数,犊牛左氧氟沙星的合适肌内给药方案应为1.5 mg / kg,每12 h重复一次。

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