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Central composite designed ezetimibe solid dispersion for dissolution enhancement: synthesis and in vitro evaluation.

Neelam Sharma1, Sukhbir Singh1

  • 1Chitkara College of Pharmacy, Chitkara University, Punjab, India.

Therapeutic Delivery
|November 9, 2019
PubMed
Summary

This study enhanced ezetimibe (EZ) solubility and dissolution using a modified solvent evaporation technique to create solid dispersions (EZSD). The EZSD formulation significantly improved drug release compared to pure ezetimibe.

Keywords:
ezetimibegelucire 50/13polyvinyl pyrollidone K30rotary evaporatorsolvent evaporation technique

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Area of Science:

  • Pharmaceutical Technology
  • Drug Delivery Systems
  • Physical Pharmacy

Background:

  • Ezetimibe (EZ) is a BCS class II drug with poor aqueous solubility, limiting its oral bioavailability.
  • Developing effective formulations to enhance EZ's solubility and dissolution is crucial for therapeutic efficacy.

Purpose of the Study:

  • To improve the aqueous solubility and dissolution rate of ezetimibe.
  • To produce ezetimibe solid dispersions (EZSD) using a modified solvent evaporation technique.

Main Methods:

  • Utilized gelucire 50/13 and polyvinyl pyrollidone K30 as carriers for ezetimibe solid dispersions.
  • Employed a modified solvent evaporation technique with a rotary evaporator.
  • Applied central composite design to optimize carrier concentrations and analyze their impact on drug release.

Main Results:

  • Ezetimibe aqueous saturation solubility increased 25-fold in the optimized EZSD formulation.
  • Cumulative drug release of optimized EZSD reached 87.54% within 1 hour, compared to 24.67% for pure ezetimibe.
  • The formulation demonstrated a significant enhancement in both solubility and dissolution profiles.

Conclusions:

  • The modified solvent evaporation technique is a promising method for manufacturing ezetimibe solid dispersions.
  • EZSD formulations effectively enhance the solubility and dissolution of ezetimibe, potentially improving its therapeutic performance.