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Pharmacokinetic profile of a novel slow release preparation of molsidomine

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Summary

A novel slow release preparation containing 24 mg molsidomine has been investigated in 6 healthy subjects.

Individual concentration/time-profiles after the tablet showed two separate concentration peaks at 2.2 h and 15.0 h. The relative bioavailability of the slow release preparation in comparison to an aqueous solution of molsidomine was 0.67.

The in vivo dissolution profile revealed either a progressive decrease in dissolution velocity caused by altered physico-chemical conditions in the ileum and the colon or a progressive reduction in the absorption constant. In all subjects deconvolution revealed a punctual increase in absorption about 15 h post-dose, coinciding with the second peak of the concentration/time-profile.

Therapeutic plasma levels of molsidomine (> 5 ng · ml−1 were not maintained over 24 h by this slow release formulation.

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Authors and Affiliations

  1. Department of Clinical Pharmacology, Johann Wolfgang Goethe-University, Frankfurt

    S. Rietbrock, B. Keller-Stanislawski & P. Thürmann

  2. Hoechst AG, Frankfurt/M., FRG

    S. Rietbrock & D. Brockmeier

Authors
  1. S. Rietbrock
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  2. B. Keller-Stanislawski
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  3. P. Thürmann
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  4. D. Brockmeier
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Rietbrock, S., Keller-Stanislawski, B., Thürmann, P. et al. Pharmacokinetic profile of a novel slow release preparation of molsidomine. Eur J Clin Pharmacol 43, 273–276 (1992). https://doi.org/10.1007/BF02333022

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  • DOI: https://doi.org/10.1007/BF02333022

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