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Bioavailability of disopyramide in normal volunteers using unbound concentration

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Summary

The pharmacokinetics of disopyramide were determined in 10 healthy volunteers after a 300 mg oral dose and again after a 2mg/kg i.v. dose.

The unbound clearance was 599 ml/min and the unbound renal clearance 310 ml/min. The terminal elimination rate constant of unbound drug was 0.180 h−1 after the i.v. dose and 0.203 h−1 after the oral dose. The absorption rate constant was 0.53−1 and the maximum peak concentration occurred after 3.2 h. The bioavailability was 0.809 using the area under the unbound plasma concentration time curve.

Although a saturable plasma protein binding was found in all subjects the bioavailability using the total concentration, in contrast to theoretical expectations, showed the same value (0.813) as the unbound concentrations.

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Author notes

  1. J. Braun

    Present address: Institut für Nephrologie, Universität Erlangen-Nürnberg 4. Medizinische Klinik, Kontumazgarten 14-18, D-8500, Nürnberg 80, Federal Republic of Germany

Authors and Affiliations

  1. IBMP, Institute for Biomed. and Pharm. Research, Nürnberg, FRG

    F. Sörgel

  2. Carl-Korth-Institute and Institute of Forensic Pathology, University of Erlangen-Nürnberg, Erlangen, FRG

    W. P. Gluth

  3. Department of Pharmacy, University of California, San Francisco, USA

    S. Øie

Authors
  1. J. Braun
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  2. F. Sörgel
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  3. W. P. Gluth
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  4. S. Øie
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Braun, J., Sörgel, F., Gluth, W.P. et al. Bioavailability of disopyramide in normal volunteers using unbound concentration. Eur J Clin Pharmacol 32, 625–629 (1987). https://doi.org/10.1007/BF02456000

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  • DOI: https://doi.org/10.1007/BF02456000

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