Scalemic mixtures preparation for optimized composition of ibuprofen solid dosage forms

Abstract

The stable and metastable phase diagrams between the sinister and the rectus ibuprofen enantiomers were established by means of thermal analysis and X-ray powder diffraction experiments as a function of temperature. The results obtained allow proving for the first time the existence, for the stable system, of a solid solution by mixing the racemic ibuprofen with one of its enantiomers for low concentration of the enantiomer. Since the rectus ibuprofen is a non-active pharmaceutical agent which can be partially bio-converted into the sinister enantiomer, the present work offers a new approach for scalemic mixtures preparation in order to improve the benefit/risk ratio related to ibuprofen solid dosage form administration.

Keywords: Drug-drug interaction; Enantiomeric mixtures; Phase diagram; Racemate; Solid solution; Thermal behavior; X-ray pattern.