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The pharmacokinetics of furazlocillin in healthy humans

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Abstract

The pharmacokinetics of the novel acylureidopenicillin furazlocillin, 6-[D-2-(3-furfurylidenamino-2-oxo-imidazolidine-1-carboxamido)-2-(4-hydroxyphenyl)-acetamido]-penicillanic acid and of its penicilloic acid derivative were investigated in five healthy male volunteers after intravenous administration of 2 and 4 g dosages. The volunteers were either in a lying or sitting position throughout the duration of the studies. The concentrations of the drug in plasma and urine were measured by two different methods in parallel: a microbiological assay and a newly developed high pressure liquid chromatography method. The latter method was also applicable for quantitation of the penicilloic acid derivative in these biological fluids. The drug's plasma protein binding (66%) and apparent red cell-plasma partition coefficient (0.055) were concentration independent. The pharmacokinetics of the drug were first order only at the lower dose level The apparent half lives of three distinguishable phases were, respectively, 4\((t_{1/2_1 } )\), 18\((t_{1/2_2 } )\), and 64\((t_{1/2_z } )\).

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Authors and Affiliations

  1. Abteilung Pharmakologie, Biozentrum der Universität, Basel, Switzerland

    Peter H. Hinderling

  2. Abteilung für Klinische Pharmakologie, Medizinische Universitätsklinik, Heidelberg, FRG

    Ursula Gundert-Remy

  3. Bayer AG, Pharmaforschungszentrum, Wuppertal, FRG

    Dietrich Förster & Wolfgang Gau

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  1. Peter H. Hinderling
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  2. Ursula Gundert-Remy
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  3. Dietrich Förster
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  4. Wolfgang Gau
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Hinderling, P.H., Gundert-Remy, U., Förster, D. et al. The pharmacokinetics of furazlocillin in healthy humans. Journal of Pharmacokinetics and Biopharmaceutics 11, 5–30 (1983). https://doi.org/10.1007/BF01061765

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  • DOI: https://doi.org/10.1007/BF01061765

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