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Preparation and investigation of mefenamic acid - polyethylene glycol - sucrose ester solid dispersions

Ibolya Fülöp, Árpád Gyéresi, Lóránd Kiss

    Acta Pharmaceutica (Zagreb, Croatia)
    |December 19, 2015
    PubMed

    Insights

    This study enhanced mefenamic acid (MA) solubility using solid dispersions. While solubility increased, drug penetration across intestinal cells did not significantly change.

    Area of Science:

    • Pharmaceutical Sciences
    • Drug Delivery Systems

    Background:

    • Mefenamic acid (MA), a common non-steroidal anti-inflammatory drug (NSAID), exhibits adverse effects partly due to poor water solubility.
    • Improving MA's solubility is crucial for enhancing its absorption and bioavailability.

    Purpose of the Study:

    • To enhance the water solubility of mefenamic acid (MA).
    • To investigate the impact of solid dispersions on MA's solubility, absorption, and bioavailability.

    Main Methods:

    • Solid dispersions of MA were prepared using the melting method with polyethylene glycol 6000 and various sucrose esters (D-1216, P-1670, S-1670).
    • X-ray diffraction was used to confirm the absence of MA crystals in the prepared products.
    • Dissolution tests in artificial intestinal juice and permeability studies using Caco-2 cell layers were conducted.

    Main Results:

    • Solid dispersions successfully rendered mefenamic acid amorphous, eliminating crystalline MA.
    • The product containing 10% D-1216 demonstrated approximately a threefold increase in MA's water solubility.
    • Apparent permeability coefficient across Caco-2 cells remained high, with no significant increase observed despite enhanced solubility.

    Conclusions:

    • Solid dispersions effectively increased mefenamic acid's water solubility.
    • While solubility was enhanced, the formulation additives did not further improve drug penetration across intestinal epithelial cells.

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