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单剂量磷霉素钠每日一次静脉注射和肌肉注射在牛体内的药代动力学,给药3天。

Intravenous and intramuscular pharmacokinetics of a single-daily dose of disodium-fosfomycin in cattle, administered for 3 days.

作者信息

Sumano L H, Ocampo C L, Gutierrez O L

机构信息

Departamento de Fisiología y Farmacología, Facultad de Medicina Veterinaria y Zootecnia, Universidad Nacional Autónoma de México, Coyoacán, México City, México.

出版信息

J Vet Pharmacol Ther. 2007 Feb;30(1):49-54. doi: 10.1111/j.1365-2885.2007.00812.x.

Abstract

Pharmacokinetic parameters of fosfomycin in cattle were determined after administration of buffered disodium fosfomycin either intravenously (i.v.) or intramuscularly (i.m.) at a dose of 20 mg/kg/day for 3 days. Calculated concentrations at time zero and maximum serum concentrations were 34.42 and 10.18 mug/mL, respectively. The variables determined, the elimination half-life of the drug remained unchanged during the 3 days ( = 1.33 +/- 0.3 h for the i.v. route and = 2.17 +/- 0.4 h for the i.m. route). Apparent volumes of distribution suggest moderated distribution out of the central compartment (V(darea) = 673 mL +/- 27 mL/kg and V(dss) = 483 +/- 11 mL/kg). Bioavailability after i.m. administration was 74.52%. Considering fosfomycin as a time-dependent antibacterial drug, plasma concentration vs. time profiles obtained in this study, suggest that clinically effective plasma concentrations of fosfomycin could be obtained for up to 8 h following i.v. administration and approximately 10 h after i.m. injection of 20 mg/kg, for susceptible bacteria. In addition to residue studies in milk and edible tissues, a series of clinical assessments, using fosfomycin at 20 mg/kg b.i.d. or t.i.d. are warranted before this antibacterial drug should be considered for use in cattle.

摘要

以20mg/kg/天的剂量静脉注射(i.v.)或肌肉注射(i.m.)缓冲磷霉素二钠3天,测定了牛体内磷霉素的药代动力学参数。计算得出的零时间浓度和最大血清浓度分别为34.42和10.18μg/mL。所测定的变量中,药物的消除半衰期在3天内保持不变(静脉注射途径为1.33±0.3小时,肌肉注射途径为2.17±0.4小时)。表观分布容积表明药物从中枢室向外分布适中(V(darea)=673mL±27mL/kg,V(dss)=483±11mL/kg)。肌肉注射后的生物利用度为74.52%。将磷霉素视为时间依赖性抗菌药物,本研究中获得的血浆浓度与时间曲线表明,对于敏感细菌,静脉注射20mg/kg后长达8小时以及肌肉注射后约10小时可获得临床有效的磷霉素血浆浓度。除了在牛奶和可食用组织中的残留研究外,在考虑将这种抗菌药物用于牛之前,还需要进行一系列临床评估,以20mg/kg的剂量每日两次或三次使用磷霉素。

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