Development and Evaluation of Cocoa Butter Taste Masked Ibuprofen Using Supercritical Carbon Dioxide

AAPS PharmSciTech. 2021 Mar 14;22(3):106. doi: 10.1208/s12249-021-01962-7.

Abstract

Masking the unpleasant taste of the pharmaceutically active ingredients plays a critical role in patient acceptance, particularly for children. This work's primary objective was the preparation of taste-masked ibuprofen microparticles using cocoa butter with the assistance of supercritical fluid technology. Microparticles were prepared by dissolving ibuprofen in melted cocoa butter at 40 °C. The solution was then introduced into a supercritical fluid unit and processed at 10 MPa CO2 pressure for 30 min. The product was collected after depressurizing the system. The effect of the drug to cocoa butter ratio and the supercritical fluid units' configuration on product quality was evaluated and compared with the sample prepared by a conventional method. Physicochemical characterization of the prepared product, including particle size, crystallinity, entrapment efficiency, in vitro drug release, and product taste using a human volunteer panel was conducted. The produced microparticles were in the range of 1.42 to 15.28 μm. The entrapment efficiency of the formulated microparticles ranged from 66 to 81%. The drug:polymer ratio, the configuration of the supercritical fluid unit, and the method of preparation were found to have a critical role in the formulation of ibuprofen microparticles. Taste evaluation using human volunteers showed that microparticles containing 20% drug and processed with supercritical fluid technology were capable of masking the bitter taste of ibuprofen. In conclusion, the dispersion of ibuprofen in cocoa butter using supercritical fluid technology is a a promising innovative method to mask the bitter taste of ibuprofen.

Keywords: cocoa butter; ibuprofen; solid dispersion; supercritical fluid technology; taste masking.

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
  • Carbon Dioxide / chemistry*
  • Chromatography, Supercritical Fluid / methods*
  • Dietary Fats / administration & dosage
  • Dietary Fats / chemical synthesis*
  • Dietary Fats / pharmacokinetics
  • Drug Development / methods*
  • Humans
  • Ibuprofen / administration & dosage
  • Ibuprofen / chemical synthesis*
  • Ibuprofen / pharmacokinetics
  • Particle Size
  • Taste / drug effects*
  • Taste / physiology
  • X-Ray Diffraction / methods

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Dietary Fats
  • Carbon Dioxide
  • cocoa butter
  • Ibuprofen