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Ranitidine kinetics in normal subjects.

N P Chau, P Y Zech, N Pozet

    Clinical Pharmacology and Therapeutics
    |June 1, 1982
    PubMed
    Summary
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    Ranitidine absorption and elimination were studied in healthy subjects. Oral ranitidine (150 mg) showed approximately 50% absorption with a zero-order kinetic profile, indicating consistent drug uptake.

    Area of Science:

    • Pharmacokinetics
    • Drug Metabolism and Disposition

    Background:

    • Ranitidine is a widely used H2 receptor antagonist for treating acid-related gastrointestinal disorders.
    • Understanding the pharmacokinetic profile of ranitidine is crucial for optimizing therapeutic efficacy and safety.

    Purpose of the Study:

    • To characterize the pharmacokinetic parameters of oral and intravenous ranitidine in healthy subjects.
    • To determine the absorption kinetics and bioavailability of oral ranitidine.
    • To compare urinary clearance of ranitidine following different administration routes.

    Main Methods:

    • Seven healthy subjects received a 1-mg/kg IV bolus injection and a 150-mg oral tablet of ranitidine, with at least a one-week interval between doses.
    • Plasma concentrations of ranitidine were measured over time to determine pharmacokinetic parameters.

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  • Urinary excretion of unchanged ranitidine was quantified following both administration routes.

    • Main Results:

    • Ranitidine exhibited a plasma half-life of approximately 2.5 hours.
    • Oral ranitidine demonstrated an absorption of about 50% of the administered dose, following zero-order kinetics (75 mg absorbed over 5 hours at 15 mg/hr).
    • Total body clearance was 10.1 ml/min/kg, with similar urinary clearance observed for both IV and oral routes (6.4 vs. 6.9 ml/min/kg).

    Conclusions:

    • Oral ranitidine is effectively absorbed with consistent zero-order kinetics.
    • The elimination and urinary excretion pathways of ranitidine are comparable regardless of the administration route (oral vs. IV).
    • These findings provide valuable insights into ranitidine's pharmacokinetic behavior in humans.