SOLID DISPERSIONS COMPRISING 4-{[(2R, 3S, 4R, 5S)-4-(4-CHLORO-2-FLUORO-PHENYL)-3-(3-CHLORO-2-FLUORO-PHENYL)-4-CYANO-5-(2,2-DIMETHYL-PROPYL)-PYRROLIDINE-2-CARBONYL]-AMINO}-3- METHOXY -BENZOIC ACID AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME WITH IMPROVED BIOAVAILABILITY

• Main Authors: SHAH, NAVNIT HARGOVINDAS, ZHANG, YU-E, SANDHU, HARPREET K, MATCHETT, MICHAEL ALLEN, LOMUSCIO, STEVE, MA, HUA
• Format: Patent
• Language: English; French
• Published: 15.02.2022
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention relates to solid dispersions of poorly water soluble compounds, in particular 4-{[(2R, 3S, 4R, 5S)-4-(4-chloro-2-Fluorophenyl)-3-(3-chloro-2-Fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)-pyrrolidine-2-carbonyl]amino}-3- Methoxy-Benzoic Acid, formed by solvent co-precipitation or spray drying, resulting in improved bioavailability, safety and tolerability of said compounds. La présente invention concerne des dispersions solides de composés peu solubles dans l'eau, en particulier, le 4-{[(2R, 3S, 4R, 5S)-4-(4-chloro-2- fluorophenyl)-3-(3-chloro-2-fluorophenyl)-4-cyano-5-(2,2- dimethylpropyl)-pyrrolidine-2-carbonyl]amino}-3- acide méthoxybenzoïque, formé par coprécipitation de solvants ou séchage par atomisation, ce qui permet d'améliorer la biodisponibilité, la sécurité et tolérabilité de ces composés.