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[Biological availability].

E Weber, U Gundert-Remy

    Arzneimittel-Forschung
    |July 1, 1975
    PubMed
    Summary
    This summary is machine-generated.

    Drug bioavailability, the percentage reaching receptors for a biological effect, faces formulation and physiological challenges. Reliable prediction remains difficult due to limitations in in vitro and animal models.

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    Area of Science:

    • Pharmacology
    • Drug Development
    • Biopharmaceutics

    Context:

    • Bioavailability is crucial for drug efficacy, representing the drug percentage reaching the target site.
    • Oral drug administration requires rapid dosage form disintegration and active substance dissolution.
    • Physiological and pathological factors significantly influence drug bioavailability.

    Purpose:

    • To define bioavailability and outline challenges in its accurate prediction.
    • To highlight limitations of current in vitro and animal models for predicting human bioavailability.
    • To describe methods used for determining drug bioavailability.

    Summary:

    • Bioavailability quantifies the drug amount from a dosage form that reaches systemic circulation to exert a biological effect.

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  • Key factors influencing oral drug bioavailability include dosage form disintegration, active substance release, dissolution rate, intestinal absorption, and metabolism.
  • Current in vitro methods and animal studies offer limited predictive accuracy for human bioavailability due to species-specific physiological differences.

    • Impact:

    • Understanding bioavailability challenges aids in optimizing drug formulation and delivery systems.
    • Improved bioavailability prediction can reduce drug development timelines and costs.
    • Accurate bioavailability assessment is essential for establishing safe and effective drug dosages.