Serum concentrations and renal excretion in humans after oral administration of praziquantel — results of three determination methods — (original) (raw)

Summary

The concentration-time-course in serum as well as the urinary excretion of Praziquantel and metabolites were studied, in healthy volunteers, using the14C-labelled compound, at dose levels of 14 and 46 mg/kg. The analytical methods applied comprised determination of radioactivity (Praziquantel and metabolites in toto) as well as unmetabolized drug by two specific methods (gas liquid chromatography, fluorometry).

Depending on the dose, the concentration maximum of radioactivity in serum was observed 2 to 4 hrs after administration. In contrast, the concentration maximum of the unmetabolized drug was attained at 1 to 2 hrs after administration. Compared to the concentrations of14C-radioactivity, the concentrations of unmetabolized drug were smaller by a factor of about 102, indicating rapid and almost complete metabolism of Praziquantel.

The radioactivity was eliminated from serum with a half life of approx. 4 hours whereas the half life of unmetabolized drug was found to be approx. 1.5 hours.

On the basis of the radioactivity values, 84±3% of the 14 mg/kg dose and 80±6% of the 46 mg/kg dose were found to be excreted renally within 4 days. More than 90% of the renally excreted drug was recovered within the first 24 hours.

The excretion data indicate a virtually complete enteral absorption of the drug.

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Authors and Affiliations

  1. Institut für Pharmakokinetik der Bayer AG Wuppertal, Germany
    K. Patzschke, J. Pütter, L. A. Wegner, F. A. Horster & H. W. Diekmann
  2. Medizinische Kliniken der Universität Düsseldorf, Germany
    K. Patzschke, J. Pütter, L. A. Wegner, F. A. Horster & H. W. Diekmann
  3. Institut für experimentelle Arzneimittelforschung E. Merck in Grafing, Germany
    K. Patzschke, J. Pütter, L. A. Wegner, F. A. Horster & H. W. Diekmann

Authors

  1. K. Patzschke
  2. J. Pütter
  3. L. A. Wegner
  4. F. A. Horster
  5. H. W. Diekmann

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Patzschke, K., Pütter, J., Wegner, L.A. et al. Serum concentrations and renal excretion in humans after oral administration of praziquantel — results of three determination methods —.European Journal of Drug Metabolism and Pharmacokinetics 4, 149–156 (1979). https://doi.org/10.1007/BF03189418

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