Miniaturization of powder dissolution measurement and estimation of particle size

Chem Biodivers. 2009 Nov;6(11):1796-811. doi: 10.1002/cbdv.200900082.

Abstract

The objective was to investigate the applicability and limitations of an approach for estimating particle size from powder dissolution measurement using as little as 50 microg of sample in 1 ml of buffer solutions. The powder dissolution profiles of five sparingly-soluble drugs (hydrochlorothiazide, phenazopyridine hydrochloride, 2-naphthoic acid, indomethacin, and dipyridamole) were evaluated with a novel biexponential spherical particle equation and also the Wang-Flanagan spherical particle non-sink equation. The results were compared to particle sizing based on measured specific surface area by the Brunauer-Emmett-Teller (BET) method, and also based on Coulter counting. With the exception of hydrochlorothiazide, the model compounds indicated some agglomeration in the dissolution media. The dry-state specific surface area was larger than expected from either the Coulter method or the powder-dissolution data, especially for phenazopyridine hydrochloride. The particle radii estimated by the powder dissolution method ranged from 10 to 68 microm, with equilibrium solubilities spanning from 5 microg/ml (dipyridamole) to 911 microg/ml (hydrochlorothiazide). Powder dissolution data collected with the miniaturized apparatus can be used to determine particle size, with estimated values agreeing reasonably with those measured by the Coulter counter method.

MeSH terms

  • Algorithms
  • Chemistry, Pharmaceutical / methods*
  • Hydrogen-Ion Concentration
  • Kinetics
  • Microspheres
  • Miniaturization
  • Models, Chemical
  • Particle Size
  • Pharmaceutical Preparations / chemistry*
  • Powders*
  • Solubility
  • Surface Properties
  • Technology, Pharmaceutical
  • Ultraviolet Rays
  • Viscosity

Substances

  • Pharmaceutical Preparations
  • Powders