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Pharmacokinetics and pharmacodynamics of methyl proscillaridin in healthy man

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Summary

The aim of this study was to obtain data about the pharmacological properties of a new glycoside derivative in man. Plasma concentrations and ECG parameters were measured after oral and intravenous administration of a single dose of 1.2 mg methyl proscillaridin in 16 healthy volunteers, using a strictly randomized, two-period change-over design. Glycoside concentrations were measured using a modified86Rb-erythrocyte-assay. QT-duration, corrected for frequency (QTc), was the principal variable measured in the ECG. By either route, there was a maximum plasma level after 1 hour, which had decreased to a minimum at 3 hours, followed by a second peak at 4 to 10 hours (orally>iv). From 10 to 72 hours the concentrations decreased with a median t 1/2 of 23.3 hours (iv) and 33.0 hours (orally). Comparison of the ratio of plasma concentrations following oral and iv administration resulted in a bioavailability of 69 % using the 48 hour plasma levels, and 59 % using the areas under the concentration-time curves. The mean QTc was maximally shortened to 28 msec at 1 hour after iv and to 19 msec at 10 hours after the oral dose. A distinct similarity between time-concentration and time-QTc curves was seen after the initial distribution phase, both after oral and intravenous administration. The new derivative shows a rapid elimination. Its bioavailability is reasonably high.

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Authors and Affiliations

  1. Abteilung Pharmakologie, Sektion Cardiologie und Angiologie des Zentrums für Innere Medizin und Kinderheilkunde, Universität Ulm, Bundeswehrkrankenhaus Ulm, Germany

    G. G. Belz & H. Schreiter

  2. Institut für Medizinische Dokumentation, Statistik und Datenverarbeitung der Universität Heidelberg, Federal Republic of Germany

    G. K. Wolf

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  1. G. G. Belz
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  2. H. Schreiter
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  3. G. K. Wolf
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Belz, G.G., Schreiter, H. & Wolf, G.K. Pharmacokinetics and pharmacodynamics of methyl proscillaridin in healthy man. Eur J Clin Pharmacol 10, 101–108 (1976). https://doi.org/10.1007/BF00609467

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  • DOI: https://doi.org/10.1007/BF00609467

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