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

Ther Deliv. 2019 Oct;10(10):643-658. doi: 10.4155/tde-2019-0063. Epub 2019 Nov 8.

Abstract

Aim: The current research is focused on increasing aqueous solubility and dissolution of BCS class II drug by using modified solvent evaporation technique to produce solid dispersions of ezetimibe (EZSD) using gelucire 50/13 and polyvinyl pyrollidone K30. Methodology & results: Central composite design analyzed the effect of gelucire 50/13 and polyvinyl pyrollidone K30 on the percentage of drug released in 5 and 30 min. Ezetimibe (EZ) aqueous saturation solubility (4.56 ± 0.94 μg/ml) was increased 25-fold in EZSD (115 ± 3.41 μg/ml). Cumulative drug release from EZ and optimized EZSD were observed 24.67 and 87.54% within 1 h, respectively. Conclusion: Manufacturing EZSD using modified solvent evaporation technique using rotary evaporator holds great promise for enhancing EZ's solubility and dissolution.

Keywords: ezetimibe; gelucire 50/13; polyvinyl pyrollidone K30; rotary evaporator; solvent evaporation technique.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chemistry, Pharmaceutical / methods
  • Drug Compounding / methods*
  • Drug Liberation
  • Excipients / chemistry*
  • Ezetimibe / chemistry
  • Ezetimibe / pharmacokinetics*
  • Fats / chemistry
  • Oils / chemistry
  • Polyethylene Glycols
  • Polyvinyls / chemistry
  • Pyrrolidinones / chemistry
  • Solubility
  • Solvents / chemistry
  • X-Ray Diffraction

Substances

  • Excipients
  • Fats
  • Oils
  • Polyvinyls
  • Pyrrolidinones
  • Solvents
  • Gelucire 50-13
  • Polyethylene Glycols
  • Ezetimibe