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蛋白质结合对体外模型中头孢噻肟模拟血管内和血管外动力学的影响。

Effect of protein binding on simulated intravascular and extravascular kinetics of cefotaxime in an in vitro model.

作者信息

Peterson L R, Van Etta L L, Fasching C E, Gerding D N

出版信息

Antimicrob Agents Chemother. 1984 Jan;25(1):58-61. doi: 10.1128/AAC.25.1.58.

Abstract

The simulated intravascular and extravascular kinetics of cefotaxime were studied in an in vitro model to evaluate the effect of antibiotic protein binding in the "intravascular" and "extravascular" space. Intravascular fluid consisted of either phosphate-buffered saline, which has no cefotaxime binding, or 3% bovine albumin, which has 63% cefotaxime binding. Extravascular spaces were filled with phosphate-buffered saline, 1.5% bovine albumin (46.6% cefotaxime binding), or 3% bovine albumin. Cefotaxime (80 mg per dose) was infused every 3 h for eight doses, and intravascular and extravascular drug concentrations were measured after doses one and eight. The corresponding intravascular and extravascular spaces were at (phosphate-buffered saline) or approaching (3% bovine albumin) equilibrium by dose eight. There were marked differences in drug concentrations achieved in the various extravascular spaces, but all could be explained on the basis of differing amounts of albumin present and the resultant differences in cefotaxime binding.

摘要

在体外模型中研究了头孢噻肟的模拟血管内和血管外动力学,以评估抗生素蛋白结合在“血管内”和“血管外”空间中的作用。血管内液体由无头孢噻肟结合的磷酸盐缓冲盐水或有63%头孢噻肟结合的3%牛白蛋白组成。血管外空间填充有磷酸盐缓冲盐水、1.5%牛白蛋白(46.6%头孢噻肟结合)或3%牛白蛋白。每3小时输注一剂头孢噻肟(每剂80毫克),共输注8剂,在第1剂和第8剂后测量血管内和血管外药物浓度。到第8剂时,相应的血管内和血管外空间处于(磷酸盐缓冲盐水)或接近(3%牛白蛋白)平衡状态。在各个血管外空间中达到的药物浓度存在显著差异,但所有差异都可以根据存在的白蛋白量不同以及由此导致的头孢噻肟结合差异来解释。

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