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The fate of Drotaverine-Acephyllinate in rat and man II. Human pharmacokinetics of Drotaverine-14C-Acephyllinate

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Summary

Pharmacokinetics of Drotaverine-Acephyllinate, Chinoin was investigated in seven male volunteers using14C labelled drug. Drotaverine-Acephyllinate was administered at a 100 mg single oral dose. Measurements of total radioactivity showed that the drug was absorbed completely and was eliminated by renal and biliary routes. Within 72 hours 39.9 ± 9.9% and 47.1 ± 4.9% of the dose were recovered in the urine and faeces respectively. Experimental results were interpreted on the basis of a complex linear compartment model. The structural identifiability of the model was proved by computer analysis, and the pharmacokinetic parameters were determined.

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References

  1. Szentmiklósi P., Mészáros Z. (1973): Hung. Pat. 167. 246.

    Google Scholar 

  2. Mészáros Z., Szentmiklósi P., Czibula I. (1962): Hung. Pat. 150. 535.

    Google Scholar 

  3. Mészáros Z., Szentmiklósi P., Czibula I. (1965): USA Pat. 3. 337. 539.

    Google Scholar 

  4. Szentmiklósi P., Marton S. (1979): Practical significance of drug-equivalence in preclinical research. Acta Pharmaceutical Hungarica49, 50–53.

    Google Scholar 

  5. Zuidema J., Merkus F. (1978): Rapid method for the high-performance liquid-chromatographic determination of acephylline in human serum. J. Chromatography145. 489–491.

    Article  CAS  Google Scholar 

  6. Zuidema J., Hilbers H. (1980): Gas-liquid chromatographic determination of acephylline in urine. J. Chromatography 182(3–4), 445–7.

    CAS  Google Scholar 

  7. Zuidema J., Mercus F. (1980): Is acephylline a theophylline bronchodilator. Lancet, I. 1318–19.

    Google Scholar 

  8. Strolin-Benedetti M., Larne D., Oliver Ch., Bouvet P. (1978): Absorption and excretion of piperazine theophylline ethanoate-14C in the rat. Arzneimittelforsch.21, 662–664.

    Google Scholar 

  9. Belpaire F., Bogaert M., Rosseel M. (1975): Identification of metabolites in rat bile. Xenobiotica,5, No.7., 413–420.

    Article  CAS  PubMed  Google Scholar 

  10. Belpaire F., Bogaert M. (1975): Metabolism of papaverine. Species differences. Xenobiotica,5. No.7., 421–429.

    Article  CAS  PubMed  Google Scholar 

  11. Belpaire F., Bogaert M. (1975): Effect of phenobarbital 3-methylcholanthrene and SKF 525-A pre-treatment in vivo and in vitro. Xenobiotica,5, No.7., 431–438.

    Article  CAS  PubMed  Google Scholar 

  12. Belpaire F., Rosseel M., Bogaert M. (1978): Metabolism of paraverine. IV. Urinary elimination of papaverine metabolites in man. Xenobiotica, Vol.8.,5. 297–300.

    Article  CAS  PubMed  Google Scholar 

  13. Gyarmati L., Dávid A., Mészáros Z., Rácz I., Szentmiklósi P. (1975): Data on themetabolism of benzylisoquinoline derivatives. Pharmazie,30 (3). 1–4.

    Google Scholar 

  14. Magyar K., Lengyel M., Knoll J. (1978): Absorption, distribution and elimination of Drotaverine. Acta Physiologica Acad. Scie. Hung.,51/41, 401–411.

    Google Scholar 

  15. Simon G., Vargay Z., Winter M., Szüts T. (1979): The intestinal absorption and excretion of14C-drotaverine in rats. J. Drug Metab. Pharmacokinetics,4. 213–217.

    Article  CAS  Google Scholar 

  16. Vargay Z., Simon G., Winter M., Szüts T. (1980): Qualitative and quantitative determination of Drotaverine metabolites in rat bile. Eur. J. Drug Metab. Pharmacokinetics,5, 2 69–74.

    Article  CAS  Google Scholar 

  17. Szatmári I., Vargay Z., SimonG., Szüts T. (1981): Pharmacokinetics and metabolism of Depogen in rats. Drugs, Biochemistry and Metabolism of Action, pharmacokinetics and metabolism of drugs, Mátrafüred, Hungary, 5–8 May, 1981.

  18. Rutz-Coudray M., Balant L., Revillard G., Buri P. (1976): Pharmacokinetique de ladrotaverinechez l’homme. Pharm. Acta Helv.,51 (9), 258.

    CAS  Google Scholar 

  19. Koltai E., Banfi D., Engler J., Volford J., Mészáros Z. (1979): Syntheses of14C labelled drotaverinum hydrochloride. J. Labelled Compounds, XVI,2. 351–354.

    Article  Google Scholar 

  20. Gács I., Vargay Z., Dobis O. (1980): Hung. Pat. 177. 476.

    Google Scholar 

  21. Vajda S. (1981): Structural equivalenceof linear models and compartmental systems. Mathematical Biosciences,55. 39.

    Article  Google Scholar 

  22. Metzler C, Elfring G., McEwen A. (1976): A users manual for NONLIN and associated programs, rev. ed. The Upjohn Company, Kolamazoo, Mich.

    Google Scholar 

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Authors and Affiliations

  1. Chinoin Pharmaceutical and Chemical Works Ltd., Budapest, Hungary

    Vargay Z., Deutsch T., Szatmári I., SzÜts T. & Várkonyi P.

  2. National Institute of Oncology (Chin. Lab.), Ráth Gy. u. 5-7, H-1525, Budapest, Hungary

    Kerpel-Fronius S. & Eckhardt S.

Authors
  1. Vargay Z.
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  2. Deutsch T.
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  3. Szatmári I.
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  4. SzÜts T.
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  5. Várkonyi P.
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  6. Kerpel-Fronius S.
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  7. Eckhardt S.
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Vargay, Z., Deutsch, T., Szatmári, I. et al. The fate of Drotaverine-Acephyllinate in rat and man II. Human pharmacokinetics of Drotaverine-14C-Acephyllinate. European Journal of Drug Metabolism and Pharmacokinetics 9, 17–29 (1984). https://doi.org/10.1007/BF03189602

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  • DOI: https://doi.org/10.1007/BF03189602

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