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Optimization of pellets containing solid dispersion prepared by extrusion/spheronization using central composite

Gurinder Singh1, Roopa S Pai, V Kusum Devi

  • 1Department of Pharmaceutics, Al-Ameen College of Pharmacy, Bangalore, Karnataka, India.

Journal of Young Pharmacists : JYP
|November 1, 2012
PubMed
Summary
This summary is machine-generated.

This study developed furosemide solid dispersion pellets using extrusion/spheronization to enhance bioavailability. Optimized pellets demonstrated sustained drug release for 12 hours, improving therapeutic outcomes.

Keywords:
Central composite designdesirability functionfurosemidesolid dispersionsustained release pellets

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Area of Science:

  • Pharmaceutical Technology
  • Drug Delivery Systems
  • Biopharmaceutics

Background:

  • Furosemide, a Class IV drug, exhibits poor water solubility and low bioavailability due to first-pass metabolism and a short half-life.
  • Oral administration of furosemide is limited by its pharmacokinetic profile, necessitating formulation strategies for improved efficacy.

Purpose of the Study:

  • To prepare and evaluate furosemide solid dispersion (SD) pellets for oral administration using extrusion/spheronization.
  • To optimize pellet formulation and process parameters for enhanced drug release and bioavailability.
  • To investigate the drug release kinetics and mechanism of the developed furosemide pellets.

Main Methods:

  • Furosemide solid dispersion was prepared with Eudragit L-100 using a solvent evaporation method.
  • Pellets containing the solid dispersion were fabricated via extrusion/spheronization.
  • A 2-factor, 3-level central composite design and desirability function approach were employed for process optimization.
  • In vitro drug release studies and kinetic modeling (zero-order, Higuchi) were performed.

Main Results:

  • Optimized pellets containing furosemide solid dispersion (PSD) achieved 88.52 ± 0.69% drug release over 12 hours in a sustained manner.
  • Extrusion/spheronization process parameters significantly influenced pellet properties and drug release.
  • Drug release from PSD followed zero-order and Higuchi's kinetics, indicating diffusion-controlled release.

Conclusions:

  • Furosemide solid dispersion pellets prepared by extrusion/spheronization effectively enhance drug solubility and provide sustained release.
  • The optimized formulation improves the drug release profile, offering a promising approach for oral furosemide delivery.
  • This formulation strategy addresses furosemide's pharmacokinetic limitations, potentially leading to improved therapeutic efficacy.