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磷霉素在兔血清和间质组织液中的药代动力学线性关系。

Linearity of the pharmacokinetics of phosphomycin in serum and interstitial tissue fluid in rabbits.

作者信息

Fernández Lastra C, Mariño E L, Dominguez-Gil A

出版信息

Arzneimittelforschung. 1986 Oct;36(10):1518-20.

PMID:3814213
Abstract

A study was carried out on the access and residence of (-)(1R,2S)-1,2-epoxypropylphosphonic acid (phosphomycin) in interstitial tissue fluid produced experimentally by subcutaneous implantation of spiral steel cages after administration of doses of 20, 30 and 60 mg/kg of the antibiotic to rabbits. The levels reached by the drug in serum and interstitial tissue fluid (ITF) were determined by a microbiological plate diffusion method. The elimination half-lives of phosphomycin ranged between 1.16 and 1.57 h. These values are similar to those found for the disappearance half-lives from ITF. Phosphomycin reached maximum concentrations in ITF between 31.95 and 80.37 micrograms/ml. Linear relationships were established between the (AUC) 0 infinity in serum, the (AUC) 0 infinity in ITF and Cmax in ITF and the doses studied, revealing the non-dose-dependent kinetics of phosphomycin. The linearity of phosphomycin kinetics was checked in serum and ITF by applying the superposition principle.

摘要

对家兔分别给予20、30和60mg/kg剂量的抗生素(-)(1R,2S)-1,2-环氧丙基膦酸(磷霉素)后,通过皮下植入螺旋形钢笼产生实验性间质组织液,对磷霉素在该组织液中的进入和留存情况进行了研究。采用微生物平板扩散法测定药物在血清和间质组织液(ITF)中达到的水平。磷霉素的消除半衰期在1.16至1.57小时之间。这些值与从ITF中消失的半衰期值相似。磷霉素在ITF中的最大浓度在31.95至80.37微克/毫升之间。血清中的(AUC)0至无穷大、ITF中的(AUC)0至无穷大以及ITF中的Cmax与所研究的剂量之间建立了线性关系,揭示了磷霉素的非剂量依赖性动力学。通过应用叠加原理,在血清和ITF中检验了磷霉素动力学的线性。

相似文献

1
Linearity of the pharmacokinetics of phosphomycin in serum and interstitial tissue fluid in rabbits.磷霉素在兔血清和间质组织液中的药代动力学线性关系。
Arzneimittelforschung. 1986 Oct;36(10):1518-20.
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Arzneimittelforschung. 1987 Aug;37(8):927-9.
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引用本文的文献

1
Fosfomycin: Uses and potentialities in veterinary medicine.磷霉素:在兽医学中的用途及潜力
Open Vet J. 2014;4(1):26-43. Epub 2014 Mar 16.
2
Distribution and antimicrobial activity of fosfomycin in the interstitial fluid of human soft tissues.磷霉素在人体软组织间质液中的分布及抗菌活性
Antimicrob Agents Chemother. 2000 Oct;44(10):2728-32. doi: 10.1128/AAC.44.10.2728-2732.2000.