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Related Experiment Videos

[Prolonged action preparation of cefaclor].

T Sakamoto, S Kawai, Y Doi

    The Japanese Journal of Antibiotics
    |March 1, 1985
    PubMed
    Summary

    A new prolonged action preparation of cefaclor (CCL) offers effectiveness with twice-daily dosing, matching conventional three-times-daily cefaclor. This development improves patient convenience by reducing administration frequency.

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    Area of Science:

    • Pharmaceutical Sciences
    • Drug Delivery Systems
    • Pharmacology

    Background:

    • Conventional cefaclor (CCL) preparations require multiple daily administrations, impacting patient compliance.
    • There is a need for extended-release formulations to improve cefaclor's therapeutic profile and patient adherence.

    Purpose of the Study:

    • To develop a prolonged-action formulation of cefaclor (CCL).
    • To achieve equivalent therapeutic effectiveness with a reduced dosing frequency (twice-daily) compared to conventional preparations (three-times-daily).

    Main Methods:

    • Investigated CCL absorption sites, developed enteric-coated granules for slow release, and optimized dissolution properties.
    • Formulated complex granules comprising 40% non-enteric coated and 60% enteric-coated granules (dissolving at pH 6).

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  • Evaluated bactericidal activity using comparative viable cell counts simulating plasma concentrations.

    • Main Results:

    • A prolonged-action preparation (S6472) was successfully developed using a specific ratio of coated and non-coated granules.
    • In vitro studies confirmed the desired dissolution profile for sustained release.
    • In vivo simulations demonstrated equivalent bactericidal activity between S6472 (375 mg b.i.d.) and conventional cefaclor (250 mg t.i.d.).

    Conclusions:

    • S6472 is a viable prolonged-action formulation of cefaclor.
    • The twice-daily administration of S6472 offers comparable efficacy to conventional cefaclor, enhancing patient convenience.
    • This formulation eliminates the need for daytime dosing, significantly benefiting patient compliance and treatment outcomes.