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C57BL/6小鼠单次皮下注射头孢维星的药代动力学

Pharmacokinetics of Single-bolus Subcutaneous Cefovecin in C57BL/6 Mice.

作者信息

Sanders Kevin L, Bas Esperanza, Cox Sherry K, Rothen Daniel E

机构信息

Division of Veterinary Resources, University of Miami, Miami, Florida.

The Ear Institute, University of Miami, Miami, Florida; ksanders@med. miami.edu.

出版信息

J Am Assoc Lab Anim Sci. 2017 Sep 1;56(5):558-561.

Abstract

Because of its extended half-life, cefovecin is a broad-spectrum cephalosporin antibiotic commonly used to treat dermatitis in dogs and cats. A single injection in dogs can yield an effective plasma concentration for as long as 14 d, depending on the strain of Staphylococcus and for as long as 7 d in cats for the treatment of Pasteurella multocida. In the laboratory animal setting, C57BL/6 mice are commonly affected with dermatologic conditions that make these animals unsuitable for experiments. Therefore, we performed this pharmacokinetic study to determine whether cefovecin would be of benefit in mice. Plasma levels of the drug were determined by HPLC. For this study, single-bolus subcutaneous dosages of 8 and 40 mg/kg were assessed. The results showed that the dosage of 40 mg/kg achieved a maximal plasma concentration of 411.54 μg/mL with a half-life of 0.84 h, whereas 8 mg/kg yielded 78.18 μg/mL and 1.07 h respectively. The pharmacokinetic results suggest that cefovecin is not suitable as a long-acting antibiotic after a single subcutaneous bolus injection in mice for the treatment of dermatitis or any other bacteria sensitive to this medication.

摘要

由于头孢维星的半衰期较长,它是一种广谱头孢菌素抗生素,常用于治疗犬猫的皮炎。在犬类中单次注射,根据葡萄球菌菌株不同,可产生长达14天的有效血浆浓度;在猫类中用于治疗多杀巴斯德菌时,可产生长达7天的有效血浆浓度。在实验动物环境中,C57BL/6小鼠通常会出现皮肤病况,这使得这些动物不适合用于实验。因此,我们进行了这项药代动力学研究,以确定头孢维星对小鼠是否有益。通过高效液相色谱法测定药物的血浆水平。在本研究中,评估了8和40mg/kg的单次皮下推注剂量。结果显示,40mg/kg的剂量达到了最大血浆浓度411.54μg/mL,半衰期为0.84小时,而8mg/kg分别产生了78.18μg/mL和1.07小时的结果。药代动力学结果表明,在小鼠单次皮下推注注射后,头孢维星不适合作为长效抗生素用于治疗皮炎或对该药物敏感的任何其他细菌感染。

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