Escudero E, Fernández-Varón E, Marín P, Espuny A, Nájera M D, Cárceles C M
Departamento de Farmacología, Facultad de Veterinaria, Universidad de Murcia, Campus de Espinardo, 30071 Murcia, Spain.
Res Vet Sci. 2006 Dec;81(3):366-72. doi: 10.1016/j.rvsc.2006.01.006. Epub 2006 Mar 10.
The pharmacokinetics of azithromycin after intravenous and intramuscular injection at a single dose rate of 10mg/kg bodyweight were investigated in rabbits by using a modified agar diffusion bioassay for determining plasma concentrations. The plasma creatine kinase activity was determined after i.m. administration for the evaluation of the tissue tolerance. The elimination half-lives of azithromycin after intravenous and intramuscular administration were 24.1 and 25.1h, respectively. After intramuscular administration mean peak plasma concentration was 0.26+/-0.01 mg/L and bioavailability was 97.7%. Plasma CK activity rose sharply within 8h after i.m. injection of azithromycin; activity returned to pre-treatment level by 48-72 h post-treatment. The transient rise in serum CK activity indicates some degree of muscle tissue damage at the injection site.
通过使用改良的琼脂扩散生物测定法测定血浆浓度，研究了体重为10mg/kg的单次剂量静脉注射和肌肉注射后阿奇霉素在兔体内的药代动力学。肌肉注射给药后测定血浆肌酸激酶活性，以评估组织耐受性。静脉注射和肌肉注射后阿奇霉素的消除半衰期分别为24.1小时和25.1小时。肌肉注射后平均血浆峰浓度为0.26±0.01mg/L，生物利用度为97.7%。肌肉注射阿奇霉素后8小时内血浆CK活性急剧上升；治疗后48-72小时活性恢复到治疗前水平。血清CK活性的短暂升高表明注射部位存在一定程度的肌肉组织损伤。
