The present invention belongs to the field of pharmaceutical industry and relates to a process for preparing a pharmaceutical composition comprising a pharmaceutically active ingredient (API) that is poorly soluble in water, preferably ezetimibe, a pharmaceutical composition obtained according to said process, to a dosage form comprising said pharmaceutical composition and to the use of said dosage forms for the treatment of hypercholesterolemia. The process comprises the steps of providing a suspension comprising API and excipient(s), subjecting it to a high energy input treatment and processing it by high shear granulation, fluid bed granulation, spray drying or lyophilisation.La présente invention appartient au domaine de l'industrie pharmaceutique et concerne un procédé de préparation d'une composition pharmaceutique comprenant un principe pharmaceutiquement actif (API) qui est médiocrement soluble dans l'eau ; une composition pharmaceutique obtenue selon ledit procédé ; une forme posologique comprenant ladite composition pharmaceutique et l'utilisation desdites formes posologiques pour le traitement de l'hypercholestérolémie.