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Related Experiment Videos

An evaluation of ibuprofen bioinversion by simulation.

A J Romero1, R J Rackley, C T Rhodes

  • 1Department of Pharmaceutics, University of Rhode Island, Kingston.

Chirality
|January 1, 1991
PubMed
Summary
This summary is machine-generated.

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This study simulated ibuprofen enantiomer plasma concentrations to understand drug disposition. Systemic bioinversion, where (R)-ibuprofen converts to (S)-ibuprofen in the body, best explains ibuprofen

Area of Science:

  • Pharmacokinetics
  • Drug Metabolism
  • Chiral Therapeutics

Background:

  • Ibuprofen exists as two enantiomers, (R)-ibuprofen and (S)-ibuprofen, with differing pharmacological activities.
  • Understanding the disposition of these enantiomers is crucial for optimizing ibuprofen therapy.
  • Bioinversion, the conversion of one enantiomer to another, plays a significant role in drug metabolism.

Purpose of the Study:

  • To simulate plasma concentrations of ibuprofen enantiomers using a pharmacokinetic model.
  • To compare simulated and literature data for S/R ratios to determine the predominant bioinversion pathway.
  • To evaluate different methods for calculating the fraction of (R)-ibuprofen bioinverted to (S)-ibuprofen.

Main Methods:

  • Utilized a pharmacokinetic model to simulate plasma concentrations of ibuprofen enantiomers.

Related Experiment Videos

  • Performed numerical simulations using STELLA software to analyze bioinversion cases.
  • Compared simulated area under the curve (AUC) ratios with literature values for different administration scenarios.

    • Main Results:

    • Simulated S/R AUC ratios for racemic ibuprofen ranged from 4.0 (presystemic) to 1.66 (systemic) bioinversion.
    • Literature S/R AUC ratios for racemic ibuprofen averaged 1.53 ± 0.2, supporting systemic bioinversion.
    • Simulated and literature data for administration of (-)-(R)-ibuprofen also supported systemic bioinversion.

    Conclusions:

    • Systemic bioinversion is the primary pathway for ibuprofen disposition in humans.
    • Different equations for estimating the fraction of (R)-ibuprofen to (S)-ibuprofen bioinversion yield inconsistent results from literature data.
    • Bioavailability of (+)-(S)-ibuprofen may be comparable between a 150 mg dose of the pure enantiomer and a 200 mg dose of the racemate.