Advertisement

Comparative pharmacokinetics and bioavailability of two oral formulations of thiocolchicoside, a GABA-mimetic muscle relaxant drug, in normal volunteers

  • E. Perucca
  • P. Poitou
  • G. Pifferi
Article

Summary

The comparative pharmacokinetic and bioavailability profile of two different formulations (tablets and capsules) of thiocolchicoside was investigated in 8 healthy male volunteers after administration of single oral 8 mg doses. Plasma samples were assayed by a capillary gas chromatography — mass spectrometry (GC-MS) method following enzymatic hydrolysis of thiocolchicoside to its aglycone (3-demethylthiocolchicine) and no attempt was made to account for the possible occurrence of hydrolysis in vivo. Irrespective of the formulation used, the drug was rapidly absorbed from the gastrointestinal tract, peak levels of about 17 ng/ml being detected within 1 h in most subjects. Elimination was rapid, with mean MRT values of 5–6 h. All kinetic parameters showed considerable interindividual variability but none differed significantly between the two formulations. Relative to the tablet formulation, the oral bioavailability of the capsule formulation was 1.06 ± 0.39.

Keywords

Thiocolchicoside 3-demethylthiocolchicine muscle relaxant pharmacokinetics bioavailability 

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. 1.
    Janbroers J.M. (1987): Review of the toxicology, pharmaco-dynamics and pharmacokinetics of thiocolchicoside, a GABA-agonist muscle relaxant with antiinflammatory and analgesic actions. Acta Ther., 13, 221–250.Google Scholar
  2. 2.
    Capra C. (1970): Su alcune proprietá farmacologiche del tiocolchicoside. Fitoterapia, 41, 19–33.Google Scholar
  3. 3.
    Biziere K., Huguet F., Narcisse G., Breteau M. (1981): Affinity of thiocolchicoside and thocolchicoside analogues for the postsynaptic GABA receptor site. Eur. J. Pharmacol., 75, 167–168.CrossRefPubMedGoogle Scholar
  4. 4.
    Reynolds J.E.F. (ed.) (1993): Martindale — The Extra Pharmacopoeia. XXX Edn. Pharmaceutical Press, London, pp. 1210–1211.Google Scholar
  5. 5.
    Repertorio Farmaceutico Italiano. (1992): CEDOF Ed., Milan, pp. 1031–1032.Google Scholar
  6. 6.
    Marcel C., Rezvani Y., Revel M. (1990): Evaluation du thiocolchicoside en monothérapie dans le lumbago douloureux — Resultats d’une étude randomisée contre placebo. Presse Med., 19, 1133–1136.PubMedGoogle Scholar
  7. 7.
    Capra C. (1967): Attivita’ antinfiammatoria del tiocolchicoside. Fitoterapia, 38, 16–21.Google Scholar
  8. 8.
    Capra C. (1967): Attivita’ analgesica del tiocolchicoside. Fitoterapia, 38, 66–71.Google Scholar
  9. 9.
    Sandouk P., Bouvier d’Yvoire M., Chretien P., Tillement J.P., Schermann J.M. (1994): Single dose bioavailability of oral and intramuscular thiocolchicoside in healthy volunteers. Biopharm. Drug Dispos., 15, 87–92.CrossRefGoogle Scholar
  10. 10.
    Griffini A., Martinelli E.M., Pifferi G. (1988): Quantitation of thiocolchicoside in rat plasma and urine by capillary gas chromatography and selected ion monitoring. 11th International Mass Spectrometry Conference, Bordeaux, 29 August–2 September, FRA 19.Google Scholar
  11. 11.
    Sherman J.M., Boudet R., Pontikis R., Nam N.-H., Fournier E. (1980): A sensitive radioimmunoassay for colchicine. J. Pharm. Pharmacol., 32, 800–802.Google Scholar

Copyright information

© Springer-Verlag 1995

Authors and Affiliations

  • E. Perucca
    • 1
  • P. Poitou
    • 2
  • G. Pifferi
    • 3
  1. 1.Clinical Pharmacology Unit, Department of Internal Medicine and TherapeuticsUniversity of PaviaPaviaItaly
  2. 2.Laboratoires LederleRungisFrance
  3. 3.Institute of Pharmaceutical ChemistryUniversity of MilanMilanoItaly

Personalised recommendations