PREPARATION AND DISSOLUTION CHARACTERISTICS OF SEVERAL FAST-RELEASE SOLID DISPERSIONS OF GRISEOFULVIN

A marked increase of dissolution rates and attainments of supersaturation of griseofulvin were found when dispersed in the matrices of polyethylene glycol (PEG) 4000, 6000, 20,000, pentaerythritol, pentaerythrityl tetraacetate, and citric acid by the fusion or solvent methods. The exact physical nature of these dispersion system are not determined. It is believed, however, that some griseofulvin is molecularly and/or colloidally dispersed in the PEG polymers due to their highly viscous and supercooling effect which will retard the nucleation and growth of griseofulvin precipitation during the solidification process. Pentaerythritol and pentaerythrityl tetraacetate which are globular compounds with the high degree of deformation of crystal lattice allowed are believed to form limited or complete solid solutions with griseofulvin. The melt of griseofulvin‐citric acid mixture is highly viscous. It required several days of standing at 37° in order to transform to a form (glassy) which could then be pulverized. The resultant glass solution is believed to represent a new class of physical modification of drugs exhibiting strikingly fast dissolution rate of griseofulvin. Copyright © 1969 Wiley‐Liss, Inc., A Wiley Company