The use of spray-drying to enhance celecoxib solubility

Drug Dev Ind Pharm. 2011 Dec;37(12):1463-72. doi: 10.3109/03639045.2011.587428. Epub 2011 Jun 27.

Abstract

The present research investigates the enhancement of the dissolution rate of celecoxib by using spray-drying to prepare a solid dispersion with various polymers, namely Kollicoat IR® (Kollicoat), polyvinyl alcohol (PVA) 22000, or polyethylene glycol 6000 (PEG). The investigated drug-to-polymer mass ratios were 1:1, 1:2, and 1:4 by weight. Hydroalcoholic or methylene chloride solvent systems were used. The obtained yields ranged from 65% to 78%, whereas the entrapment efficiencies were between 68% and 82%. The results revealed an increase in the dissolution rate of the prepared particles up to 200% within 20 min. The prepared particles were investigated using differential scanning calorimetry, scanning electron microscopy, X-ray diffraction, and Fourier transform infrared spectroscopy. The increased dissolution rate was attributed to hydrogen bond formation between celecoxib and each polymer together with the reduced size of the formed particles offering a greater overall surface area. It was concluded that spray-drying may be considered a successful one-step technique to improve the dissolution rate of celecoxib when using Kollicoat, PVA, or PEG as the carrier polymer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biological Availability
  • Celecoxib
  • Cyclooxygenase 2 Inhibitors / chemistry*
  • Desiccation / methods
  • Microscopy, Electron, Scanning
  • Particle Size
  • Polyethylene Glycols / chemistry
  • Polyvinyl Alcohol / chemistry
  • Polyvinyls / chemistry
  • Pyrazoles / chemistry*
  • Solubility
  • Spectroscopy, Fourier Transform Infrared
  • Sulfonamides / chemistry*
  • Surface-Active Agents / chemistry*

Substances

  • Cyclooxygenase 2 Inhibitors
  • Kollicoat IR
  • Polyvinyls
  • Pyrazoles
  • Sulfonamides
  • Surface-Active Agents
  • Polyethylene Glycols
  • Polyvinyl Alcohol
  • Celecoxib