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多次肌肉注射后螺旋霉素在牛体内的药代动力学及组织残留

Pharmacokinetics and tissue residues of spiramycin in cattle after intramuscular administration of multiple doses.

作者信息

Sanders P, Guillot P, Dagorn M, Moulin G, Delépine B, Mourot D

机构信息

Laboratoire des Médicament Vétérinaires, Centre National d'Etudes Vétérinaires et Alimentaires, Ministère de l'Agriculture et de la Forêt, La Haute Marche-Javené, Fougères, France.

出版信息

Am J Vet Res. 1994 Mar;55(3):358-62.

PMID:8192258
Abstract

Pharmacokinetic variables of spiramycin and its distribution in muscle, liver, kidney, and injection sites were studied in 18 mixed-sex 1-year-old calves to assess drug withdrawal time after 2 IM administrations of 100,000 IU of spiramycin/kg of body weight at 48-hour intervals. Presence of a compound, other than spiramycin I (ie, neospiramycin), was observed in tissues used for withdrawal time determination. High concentrations observed at the injection sites decreased slowly to maximal residue limit with half-life of 109.5 hours for neospiramycin and 77.5 hours for spiramycin. At 14 days, neospiramycin concentrations were higher in kidney than in liver and half-life was different between these 2 tissues. Two methods of withdrawal time determination were used and the part of the samples without residue detected, in the calculation, was discussed. Withdrawal time of 35 days can be proposed on the basis of average daily intake determined for spiramycin, with concentration at injection sites representing 10% of the whole muscle concentration.

摘要

对18头1岁的混种小牛进行了研究,以评估间隔48小时两次肌肉注射100,000 IU螺旋霉素/千克体重后药物的停药时间,研究内容包括螺旋霉素的药代动力学变量及其在肌肉、肝脏、肾脏和注射部位的分布。在用于确定停药时间的组织中观察到了除螺旋霉素I(即新螺旋霉素)以外的一种化合物。注射部位观察到的高浓度缓慢下降至最大残留限量,新螺旋霉素的半衰期为109.5小时,螺旋霉素的半衰期为77.5小时。在第14天时,肾脏中新螺旋霉素的浓度高于肝脏,且这两个组织的半衰期不同。使用了两种确定停药时间的方法,并讨论了计算中未检测到残留的样本部分。根据所测定的螺旋霉素平均日摄入量,可提出35天的停药时间,注射部位的浓度占整个肌肉浓度的10%。

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