Significant solubility of carbon dioxide in Soluplus® facilitates impregnation of ibuprofen using supercritical fluid technology

Pharm Dev Technol. 2018 Sep;23(7):697-705. doi: 10.1080/10837450.2017.1315135. Epub 2017 Apr 13.

Abstract

Treatment of Soluplus® with supercritical carbon dioxide allows promising applications in preparing dispersions of amorphous solids. Several characterization techniques were employed to reveal this effect, including CO2 gas sorption under high pressure and physicochemical characterizations techniques. A gravimetric method was used to determine the solubility of carbon dioxide in the polymer at elevated pressure. The following physicochemical characterizations were used: thermal analysis, X-ray diffraction, Fourier transform, infrared spectroscopy and scanning electron microscopy. Drug loading of the polymer with ibuprofen as a model drug was also investigated. The proposed treatment with supercritical carbon dioxide allows to prepare solid solutions of Soluplus® in less than two hours at temperatures that do not exceed 45 °C, which is a great advantage to be used for thermolabile drugs. The advantages of using this technology for Soluplus® formulations lies behind the high sorption capability of carbon dioxide inside the polymer. This will ensure rapid diffusion of the dissolved/dispersed drug inside the polymer under process conditions and rapid precipitation of the drug in the amorphous form during depressurization accompanied by foaming of the polymer.

Keywords: Soluplus; amorphous; dispersions; ibuprofen; supercritical fluid.

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage*
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Carbon Dioxide / chemistry*
  • Crystallization
  • Diffusion
  • Drug Carriers / chemistry*
  • Drug Compounding / methods
  • Drug Liberation
  • Ibuprofen / administration & dosage*
  • Ibuprofen / chemistry
  • Polyethylene Glycols / chemistry*
  • Polyvinyls / chemistry*
  • Solubility

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Drug Carriers
  • Polyvinyls
  • polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer
  • Carbon Dioxide
  • Polyethylene Glycols
  • Ibuprofen