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Dissolution systems for chloramphenicol tablet bioavailability.

H Ogata, T Shibazaki, T Inoue

    Journal of Pharmaceutical Sciences
    |June 1, 1979
    PubMed
    Summary
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    Chloramphenicol (I) tablet bioavailability correlates with dissolution rates at pH 4. Food intake improved the bioavailability of a poorly performing tablet formulation (F).

    Area of Science:

    • Pharmacokinetics
    • Pharmaceutical Sciences

    Background:

    • Chloramphenicol (I) bioavailability is crucial for effective treatment.
    • Understanding the relationship between in vitro dissolution and in vivo performance is essential for drug formulation.

    Purpose of the Study:

    • To investigate the correlation between chloramphenicol (I) tablet bioavailability and in vitro dissolution rates.
    • To assess the impact of food on the bioavailability of chloramphenicol (I) tablets and powder.

    Main Methods:

    • Five chloramphenicol (I) tablet formulations were evaluated for bioavailability.
    • Dissolution rates were determined using multiple methods across different pH levels.
    • Oral administration of 500 mg chloramphenicol (I) to five subjects in a crossover design.
    • Urinary excretion was used to determine bioavailability parameters.

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    Main Results:

    • One tablet formulation (F) exhibited significantly lower bioavailability compared to others.
    • Dissolution rates at pH 1.2 did not correlate with bioavailability rank.
    • Tablet F demonstrated pH-dependent dissolution, with good correlation at pH 4.
    • Food did not affect chloramphenicol (I) powder bioavailability.
    • Tablet F's poor fasting bioavailability improved significantly when taken with food.

    Conclusions:

    • In vitro dissolution at pH 4 is a better predictor of chloramphenicol (I) tablet bioavailability than at pH 1.2.
    • Food intake can enhance the bioavailability of specific chloramphenicol (I) tablet formulations.
    • Formulation and administration conditions significantly influence chloramphenicol (I) bioavailability.