Solubility of eflucimibe in supercritical carbon dioxide with or without a co‐solvent

Martial Sauceau (1) , Jean‐jacques Letourneau (1) , Bernard Freiss (2) , Dominique Richon (3) , Jacques Fages (1)

1 Poudres et procédés - Ecole des Mines Albi-Carmaux
2 Centre de R&D Pierre Fabre - Centre de Recherche Pierre Fabre
3 École des Mines de Paris

Eflucimibe is a drug, which displays hypocholesterolemic and anti‐atherosclerotic properties in animal models. The solubility of eflucimibe in supercritical carbon dioxide has been investigated with an apparatus based on an analytical open circuit method. Solubility values have been measured at 308.15 and 318.15 K in the pressure range 8‐30 MPa. Solubility appears to be an increasing function of both temperature and pressure. The two co‐solvents investigated, ethanol and dimethylsulphoxide, are found to significantly enhance the solubility. Solubility data are reported for the 308.15 K isotherm at different total pressures and different solvent/co‐solvent ratios. The observed co‐solvent effects can be explained not only by density effects, but by the effect of molecular interactions on the basis of compound solubility parameters.

Mots clés: Eflucimibe solubility; specific interactions; co‐solvent effect; supercritical carbon dioxide; Supercritical carbon dioxide; Co-solvent effect; Specific interactions

Domaines: Génie des procédés; Génie chimique; Pharmacie galénique

Martial Sauceau, Jean‐jacques Letourneau, Bernard Freiss, Dominique Richon, Jacques Fages. Solubility of eflucimibe in supercritical carbon dioxide with or without a co‐solvent. Journal of Supercritical Fluids, 2004, 31 (2), pp.133-140. ⟨10.1016/j.supflu.2003.11.004⟩. ⟨hal-01668424⟩