A METHOD OF PREPARING A PHARMACEUTICAL CO-CRYSTAL COMPOSITION

摘要

The present invention relates to a method of preparing a pharmaceutical co-crystal composition, said method comprising the steps of: a. simultaneously contacting a supercritical or liquefied gas with solid particles of a pharmaceutically active component and with solid particles of a co-builder to form a co-crystallisation medium containing dissolved pharmaceutically active component and dissolved co-builder as well as solid particles of the pharmaceutically active component and solid particles of the co-builder; b. transforming the solid particles of the pharmaceutically active component and the solid particles of the co-builder into co-crystals of said pharmaceutically active component and said co-builder by keeping the supercritical or liquefied gas in a supercritical or liquid state until at least 80 wt. % of the pharmaceutically active component is incorporated in the crystal matrix of said co-crystals; and c. separating said co-crystals from the supercritical or liquefied gas wherein at least a fraction of the pharmaceutically active component and at least a fraction of the co-builder remain in an undissolved state during the co-crystallisation. The present method enables easy preparation of a pharmaceutical co-crystal composition containing virtually no solvent residue and can suitably be used to prepare co-crystals of highly labile pharmaceutically active components.