Effect of respiratory tract disease on pharmacokinetics of tilmicosin in rats.

Laboratory animal science Pub Date : 1999-06-01

S Modric, A I Webb, M Davidson

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Abstract

Background and purpose: In rats, murine respiratory mycoplasmosis is caused by Mycoplasma pulmonis. Tilmicosin, a macrolide antibiotic, has good tissue penetration and reaches high concentration in the lungs. Therefore, a model for studying the effects of disease on pharmacokinetics of tilmicosin was developed, using LEW rats.

Methods: Seventy-two LEW rats were assigned at random to two groups: one group was inoculated with M. pulmonis, and the other served as an uninoculated control group. On postinoculation day 31, all rats received a single dose of tilmicosin (20 mg/kg of body weight, subcutaneously).

Results: Concentration of tilmicosin in the lungs of both groups of rats was significantly higher than serum tilmicosin concentration at all times. Infected rats had significantly higher lung tilmicosin concentration than did noninfected rats. No correlation was found between pH of the lungs and tilmicosin concentration in the lungs in either treatment group, nor did treatment have any effect on pH of the muscle.

Conclusion: Tilmicosin accumulates in the lungs, and infection/inflammation further improves its tissue penetration.

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呼吸道疾病对替尔米考星在大鼠体内药动学的影响。

背景与目的:大鼠呼吸道支原体病是由肺支原体引起的。替尔米考辛是一种大环内酯类抗生素，具有良好的组织穿透性，在肺部可达到高浓度。因此，我们以LEW大鼠为研究对象，建立了疾病对替米考星药代动力学影响的模型。方法:将72只LEW大鼠随机分为两组，一组接种肺支原体，另一组为未接种对照组。接种后第31天，所有大鼠均皮下注射单剂量替米考星(20mg /kg体重)。结果:两组大鼠肺组织中tilmicosin浓度均显著高于血清中tilmicosin浓度。感染大鼠的肺替米考星浓度明显高于未感染大鼠。在两组治疗中均未发现肺pH值与肺中tilmicosin浓度之间的相关性，治疗也未对肌肉pH值产生任何影响。结论:替米考星在肺部蓄积，感染/炎症进一步促进其组织渗透。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Laboratory animal science

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