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Chronopharmacokinetic and bioequivalence studies of two formulations of trimipramine after oral administration in man

  • A. M. Bougerolle
  • J. L. Chabard
  • M. Jbilou
  • G. Dordain
  • A. Eschalier
  • O. Aumaitre
  • J. Gaillot
  • J. J. Piron
  • J. Petit
  • J. A. Berger
Original Papers

Summary

The bioavailability of two oral formulations of trimipramine, tablets and solution, was performed in twelve healthy volunteers, in a cross-over study. Each formulation was administered in the morning after a fasted period, and in the evening after a meal, in order to evaluate the role of both administration time and food consumption on the plasma kinetic parameters, under usual therapeutic conditions. A high interindividual variability of data was found.

First, the extent of bioavailability was identical for the two formulations but the rate of bioavailability seemed to be different, with the p.o. solution, being more rapidly absorbed (tmax=1.50 h).

The effect of administration time was more obvious for the solution as shown by a lower quantitative absorption as well as a delay in time to reach the maximal concentration.

Regardless of formulation and administration time, the ty1/2 β was about 10 hours and the mean MRT value was 11 hours.

Keywords

Trimipramine chronopharmacokinetic bioequivalence 

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Copyright information

© Springer-Verlag 1989

Authors and Affiliations

  • A. M. Bougerolle
    • 1
  • J. L. Chabard
    • 1
  • M. Jbilou
    • 1
  • G. Dordain
    • 2
  • A. Eschalier
    • 3
  • O. Aumaitre
    • 2
  • J. Gaillot
    • 4
  • J. J. Piron
    • 5
  • J. Petit
    • 1
  • J. A. Berger
    • 1
  1. 1.Groupe de Recherches en Biodynamique du médicamentLaboratoire de Chimie analytiqueClermont-FerrandFrance
  2. 2.Service de Neurologie, Hôpital NordCHRUClermont-FerrandFrance
  3. 3.Laboratoire de Pharmacologie médicale et INSERM U195Clermont-FerrandFrance
  4. 4.Département de BiodynamiqueInstitut de Biopharmacie Rhône-PoulencAntonyFrance
  5. 5.Département PsychotropesSPECIAParisFrance

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