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不同输注速率下利福平及去乙酰利福平在结核病患者中的药代动力学

Pharmacokinetics of rifampicin and desacetylrifampicin in tuberculous patients after different rates of infusion.

作者信息

Houin G, Beucler A, Richelet S, Brioude R, Lafaix C, Tillement J P

出版信息

Ther Drug Monit. 1983;5(1):67-72. doi: 10.1097/00007691-198303000-00005.

Abstract

Four rates of rifampicin infusion ranging from 3.3 to 15 mg/min in 12 tuberculous patients were studied. Blood samples (n = 10) were drawn during infusion and 8 h later. Urine samples were collected in six fractions during a 24-h period. Rifampicin and desacetylrifampicin were measured by high-pressure liquid chromatography. Results show that the maximum plasma concentrations increase linearly for each dose with the rate of infusion, and that the amounts excreted in the urines are highly dependent on the administered dose. Simulation of plasma concentrations after different dosage regimens shows that a double rate of infusion--20 mg min-1 during 1 h and then 200 mg h-1--allows plasma concentrations to be quickly reached and maintained at a 20 mg L-1 level, far higher than the minimum inhibitory concentrations of most germs.

摘要

对12例结核病患者研究了4种利福平输注速率,范围为3.3至15毫克/分钟。在输注期间和8小时后采集血样(n = 10)。在24小时内分6份收集尿样。通过高压液相色谱法测定利福平和去乙酰利福平。结果表明,每种剂量的最大血浆浓度随输注速率呈线性增加,且尿中排泄量高度依赖于给药剂量。不同给药方案后血浆浓度的模拟显示,双倍输注速率——1小时内20毫克/分钟,然后200毫克/小时——可使血浆浓度迅速达到并维持在20毫克/升水平,远高于大多数细菌的最低抑菌浓度。

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