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Related Experiment Videos

The maximum pharmacodynamic effect as a response parameter: pharmacokinetic considerations.

C S Leopold1

  • 1Department of Pharmaceutical Technology, Heinrich-Heine-University, Düsseldorf, Germany. leopold@uni-duesseldorf.de

The Journal of Pharmacy and Pharmacology
|October 21, 1999
PubMed
Summary

Pharmacokinetic simulations reveal that drug penetration enhancement factors are accurately determined only under infinite dose conditions (zero-order kinetics). Finite doses (first-order kinetics) lead to misestimations in bioavailability and enhancement factor calculations.

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Area of Science:

  • Dermatopharmacology
  • Pharmacokinetics
  • Drug Delivery Systems

Background:

  • Cutaneous ointment formulations exhibit variable drug penetration enhancement.
  • Previous in vivo studies showed discrepancies in enhancement factor determination based on applied methods.
  • Differences in enhancement factors arise from formulation-dependent penetration.

Purpose of the Study:

  • To clarify discrepancies in enhancement factor determination for topical formulations.
  • To investigate the impact of drug penetration kinetics on bioavailability assessment.
  • To establish accurate methods for calculating enhancement factors and relative bioavailability.

Main Methods:

  • Pharmacokinetic simulations using an open one-compartment model.
  • Modeling with first-order or zero-order drug penetration kinetics and first-order elimination.

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  • Simulation of drug concentration-time profiles, dose-response, and activity-response curves.

    • Main Results:

    • Significant differences were observed between first-order and zero-order input kinetics in evaluating bioavailability and penetration.
    • First-order input kinetics (finite dose) resulted in misestimation of bioavailability and enhancement factors.
    • Zero-order input kinetics (infinite dose) provided accurate determination of these factors.

    Conclusions:

    • Accurate determination of bioavailability and drug penetration enhancement factors requires zero-order input kinetics (infinite dose conditions).
    • First-order input kinetics (finite dose conditions) leads to inaccurate assessments.
    • Simulation clarifies the critical role of drug input kinetics in evaluating topical formulation performance.