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Rotating-disk method for determining cutaneous metabolism.

L C Leung, H Y Ando

    Journal of Pharmaceutical Sciences
    |May 1, 1979
    PubMed
    Summary
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    This study developed an in vitro system to measure topical drug metabolism in guinea pig skin. The system quantified the rapid metabolism of vidarabine, an antiviral, aiding topical drug design.

    Area of Science:

    • Pharmacology
    • Dermatology
    • Biochemistry

    Background:

    • Topical drug formulation requires understanding skin permeation and metabolism.
    • Viable skin models are crucial for accurate in vitro assessment.
    • Vidarabine is an antiviral agent susceptible to cutaneous metabolism.

    Purpose of the Study:

    • To develop and validate an in vitro system for assessing cutaneous drug metabolism.
    • To quantify the metabolic rate of vidarabine in guinea pig skin.
    • To utilize the rotating disk method for evaluating drug diffusion and metabolism.

    Main Methods:

    • An in vitro system using viable guinea pig skin and a rotating disk was established.
    • The aqueous diffusion coefficient of vidarabine was determined using the capillary cell method.

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  • Skin samples were prepared, mounted on a disk, and incubated with vidarabine solution for metabolic analysis.

    • Main Results:

    • The rotating disk system was successfully standardized using benzoic acid.
    • Vidarabine was rapidly metabolized to 9-beta-D-arabinofuranosylhypoxanthine.
    • The calculated enzyme rate constant for vidarabine metabolism was 1.54 x 10(-1) sec-1.

    Conclusions:

    • The developed in vitro system effectively measures the metabolic component of viable skin.
    • This model provides valuable data for designing effective topical antiviral formulations.
    • Understanding cutaneous metabolism is essential for optimizing topical drug delivery and efficacy.