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Factors Influencing Drug Absorption: Pharmaceutical Parameters01:28

Factors Influencing Drug Absorption: Pharmaceutical Parameters

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Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
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Development and evaluation of febuxostat solid dispersion through screening method.

Jeong Sun Sohn1, Jin-Seok Choi2

  • 1College of General Education, Chosun University, Gwangju 61452, Republic of Korea.

Saudi Pharmaceutical Journal : SPJ : the Official Publication of the Saudi Pharmaceutical Society
|August 10, 2023
PubMed
Summary

This study developed a novel Febuxostat solid dispersion (SD) formulation to enhance drug solubility and dissolution. The optimized Febux-SD formulation significantly improved in vitro drug release and is expected to increase bioavailability.

Keywords:
Dissolution (%)FebuxostatIn vitro drug releaseIn vitro permeabilityMeglumineStability

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems

Background:

  • Febuxostat is a BCS Class II drug with poor aqueous solubility, limiting its therapeutic efficacy.
  • Enhancing Febuxostat solubility and dissolution is crucial for improving its bioavailability.

Purpose of the Study:

  • To develop an improved Febuxostat formulation with increased in vitro dissolution and drug release using a screening method.
  • To investigate the potential of solid dispersion technology for Febuxostat solubilization.

Main Methods:

  • A screening approach was employed to select optimal solubilizers, pH agents, and carriers.
  • Solvent evaporation method was utilized for the preparation of Febuxostat-SD formulations.
  • In vitro dissolution, drug release, and permeability studies were conducted and compared to a commercial Feburic® tablet.

Main Results:

  • The optimal Febuxostat-SD formulation (SD3) demonstrated significantly higher dissolution rates across various pH conditions compared to Feburic®.
  • In vitro drug release and permeability of the SD3 formulation were markedly improved.
  • The SD3 formulation exhibited good stability over a 6-month period with altered physicochemical properties.

Conclusions:

  • The development of a novel Febuxostat-SD formulation using meglumine was successfully achieved.
  • The enhanced dissolution profile of the Febuxostat-SD formulation suggests potential for improved in vivo bioavailability in subsequent animal and human studies.