Bioavailability of disopyramide in normal volunteers using unbound concentration |
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Authors: | PD Dr J Braun F Sörgel W P Gluth S Øie |
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Institution: | 1. Institut für Nephrologie, Universit?t Erlangen-Nürnberg 4. Medizinische Klinik, Kontumazgarten 14-18, D-8500, Nürnberg 80, Federal Republic of Germany 2. IBMP, Institute for Biomed. and Pharm. Research, Nürnberg, FRG 3. Carl-Korth-Institute and Institute of Forensic Pathology, University of Erlangen-Nürnberg, Erlangen, FRG 4. Department of Pharmacy, University of California, San Francisco, USA
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Abstract: | 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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Keywords: | disopyramide bioavailability saturable binding pharmacokinetics |
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