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Related Experiment Videos

Prednisone and prednisolone interconversion in the rabbit utilizing unbound concentrations.

M Hammarlund-Udenaes1, L Z Benet

  • 1Department of Pharmacy, School of Pharmacy, University of California, San Francisco.

Biopharmaceutics & Drug Disposition
|August 1, 1991
PubMed
Summary

This study investigated the pharmacokinetics of prednisolone (POH) and prednisone (PO) in rabbits. It found that while the conversion of POH to PO is dose-independent, the reverse conversion shows saturability, impacting drug disposition.

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Area of Science:

  • Pharmacology
  • Drug Metabolism
  • Pharmacokinetics

Background:

  • Prednisolone (POH) and prednisone (PO) are corticosteroids with distinct administration routes and metabolic pathways.
  • Understanding their disposition is crucial for optimizing therapeutic efficacy and minimizing adverse effects.

Purpose of the Study:

  • To characterize the pharmacokinetic disposition of unbound prednisolone (POH) and prednisone (PO) in rabbits.
  • To investigate the interconversion and dose-dependency of POH and PO pharmacokinetics.

Main Methods:

  • Intravenous infusions and bolus doses of POH and PO were administered to rabbits.
  • Plasma concentrations were analyzed using high-performance liquid chromatography (HPLC).
  • Unbound fractions were determined by equilibrium dialysis and computer modeling.

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Main Results:

  • The unbound fraction of POH was 3-15%, while PO ranged from 23-34% and showed nonlinearity in some rabbits.
  • Apparent unbound clearances for both POH and PO were dose-independent.
  • The conversion of POH to PO was 50-70% and dose-independent, whereas PO to POH conversion was saturable and dose-dependent.

Conclusions:

  • The disposition of unbound POH and PO in rabbits is largely dose-independent, despite saturable conversion of PO to POH.
  • The observed nonlinear conversion does not significantly alter the overall linear disposition of unbound POH.
  • These findings contribute to a better understanding of corticosteroid pharmacokinetics.