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Comparative dissolution studies for mefenamic acid-polyethylene glycol solid dispersion systems and tablets

G Owusu-Ababio1, N K Ebube, R Reams

  • 1College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee 32307, USA.

Pharmaceutical Development and Technology
|September 22, 1998
PubMed
Summary
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Solid dispersions of mefenamic acid (MFA) significantly enhance drug dissolution. Formulating these dispersions into tablets maintained the improved dissolution rates, potentially reducing doses for poorly soluble drugs.

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Materials Science

Background:

  • Mefenamic acid (MFA) is a practically water-insoluble non-steroidal anti-inflammatory drug.
  • Enhancing the dissolution rate of poorly soluble drugs is crucial for improving their bioavailability and therapeutic efficacy.
  • Solid dispersion technology offers a promising approach to overcome solubility challenges.

Purpose of the Study:

  • To enhance the dissolution of mefenamic acid (MFA) via solid dispersion systems.
  • To compare the dissolution profiles of unformulated solid dispersions versus formulated tablet dosage forms.
  • To investigate the impact of formulation components and processing on MFA dissolution.

Main Methods:

  • Preparation of binary (MFA/polyethylene glycol 3350) and ternary (MFA/polyethylene glycol 3350/Tween 20) solid dispersions using the melt method.

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  • Characterization techniques included dissolution studies, scanning electron microscopy (SEM), and powder X-ray diffraction (PXRD).
  • Formulation of dispersions into tablets and comparison with uncompressed mixtures and pure MFA.

    • Main Results:

    • Reduced MFA content in binary dispersions (down to 5% w/w) increased dissolution rate threefold compared to pure MFA.
    • Ternary systems incorporating Tween 20 further enhanced MFA dissolution, achieving a sevenfold increase at MFA/PEG/TW 4.7:93:2.3 (% w/w).
    • SEM indicated increased particle size, while PXRD showed decreased crystallinity of dispersions. Tablet compression did not negatively impact dissolution from dispersions.

    Conclusions:

    • Solid dispersions, particularly ternary systems with PEG and Tween 20, significantly improve mefenamic acid dissolution.
    • Formulating these enhanced dispersions into tablets preserves the improved dissolution characteristics.
    • This approach holds potential for reducing the dosage of poorly water-soluble drugs like MFA when formulated as tablets.