Effect of protective colloids on the induction of polymorphic changes in indomethacin agglomerates after solvent evaporation from o/w emulsions

Abstract

Indomethacin (IMC) agglomerates were prepared by the solvent evaporation process from o/w emulsions containing different protective colloids in the external aqueous solution. The types of protective colloids inducing the polymorphic transformation of IMC in the agglomerates without wall material were investigated. The composition and its polymorphs were evaluated from the X-ray diffraction patterns, IR spectra and DSC thermograms. The results indicate that when pectin, beta-cyclodextrin, sodium alginate or sodium dodecyl supphase acted as a protective colloid, the respective IMC agglomerates consisted only of the alpha form of IMC. When gelatin or hydroxypropyl methylcellulose was used as a protective colloid, the amorphous, alpha and gamma forms as well as methylene chloride solvates of IMC were found in the IMC agglomerates. There was only methylene chloride solvate of IMC with a small amount of amorphous form in the IMC agglomerates prepared from albumin as a protective colloid, while IMC agglomerates prepared from methylcellulose, polyvinyl alcohol or biosoluble polymer consisted of the mixture of amorphous and alpha forms, and methylene chloride solvate of IMC. When polyvinyl pyrrolidone was applied to act as a protective colloid, the mixture of methylene chloride solvate and gamma form of IMC with less quantity of amorphous form was found in its IMC agglomerates. This strongly suggests that the composition of IMC agglomerates prepared from the solvent evaporation process was significantly influenced by the type of protective colloids used.

Keywords::

• Protective Colloid Indomethacin Agglomerate Polymorphism Solvent-evaporation