Characterization of ibuprofen microparticle and improvement of the dissolution

Pharm Dev Technol. 2017 Feb;22(1):63-68. doi: 10.3109/10837450.2016.1163386. Epub 2016 Apr 7.

Abstract

The objective of this study was to prepare ibuprofen (IBP) microparticles by pH-change method and enhance the dissolution rate in vitro. Tween80 and Cremophor RH40 were selected as stabilizers to change the microparticles morphology. The microparticles were evaluated by dissolution profiles and characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (XRD), laser particle size analyzer, scanning electron microscope (SEM) and Fourier transform infrared spectroscopy (FTIR). IBP microparticle prepared with surfactants showed a significant increase in dissolution rate (more than three times within 10 min) and an obvious decrease in mean particle size. The morphology of microparticles was obviously changed. XRD and DSC results revealed that the crystalline state of the untreated IBP and the prepared IBP microparticles were similar. The crystallinity of microparticles produced might be lightly reduced by adding surfactants in preparation process. All results showed that it was useful to prepare high dispersion microparticle by adding surfactants in the preparation process for improving the dissolution.

Keywords: Cremophor RH40; Tween 80; dissolution; ibuprofen; microparticle.

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / chemistry*
  • Calorimetry, Differential Scanning
  • Crystallization
  • Excipients / chemistry*
  • Ibuprofen / chemistry*
  • Particle Size
  • Polyethylene Glycols / chemistry
  • Polysorbates / chemistry
  • Powder Diffraction
  • Solubility
  • Spectroscopy, Fourier Transform Infrared
  • Surface-Active Agents / chemistry
  • X-Ray Diffraction

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Excipients
  • Polysorbates
  • Surface-Active Agents
  • cremophor
  • Polyethylene Glycols
  • Ibuprofen