Triboelectrification and dissolution property enhancements of solid dispersions

Int J Pharm. 2015 May 15;485(1-2):306-16. doi: 10.1016/j.ijpharm.2015.03.013. Epub 2015 Mar 12.

Abstract

The use of solid dispersion techniques to modify physicochemical properties and improve solubility and dissolution rate may result in alteration to electrostatic properties of particles. Particle triboelectrification plays an important part in powder processing, affecting end product quality due to particle deposition and powder loss. This study investigates the use of glucosamine hydrochloride (GLU) in solid dispersions with indomethacin. Solvents selected for the preparation of the dispersions were acetone, acetone-water, ethanol and ethanol-water. Solid state characterizations (DSC, FTIR and XRPD) and dissolution were conducted. Dispersions were subjected to charge using a custom built device based on a shaking concept, consisting of a Faraday cup connected to an electrometer. All dispersions improved the dissolution rate of indomethacin. Analysis showed the method of preparation of the dispersion induced polymorphic forms of the drug. Indomethacin had a high propensity for charging (-411 nC/g). GLU had a very low charge (-1 nC/g). All dispersions had low charges (-1 to 14 nC/g). Acetone as a solvent, or in combination with water, produced samples with an electronegative charge in polarity. The same approach with ethanol produced electropositive charging. The results show the selection of solvents can influence powder charge thereby improving powder handling as well as dissolution properties.

Keywords: Electrostatics; Indomethacin; Polymorphism; Solid dispersions; Triboelectrification; d-Glucosamine HCl.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetone / chemistry
  • Calorimetry, Differential Scanning
  • Chemistry, Pharmaceutical
  • Crystallography, X-Ray
  • Equipment Design
  • Ethanol / chemistry
  • Glucosamine / chemistry*
  • Indomethacin / chemistry*
  • Kinetics
  • Microscopy, Electron, Scanning
  • Models, Chemical
  • Powder Diffraction
  • Powders
  • Solubility
  • Solvents / chemistry
  • Spectroscopy, Fourier Transform Infrared
  • Static Electricity
  • Surface Properties
  • Technology, Pharmaceutical / instrumentation
  • Technology, Pharmaceutical / methods*
  • Water / chemistry

Substances

  • Powders
  • Solvents
  • Water
  • Acetone
  • Ethanol
  • Glucosamine
  • Indomethacin