Formulations of (S)-3-amino-6-methoxy-N-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)picolinamide

• Main Authors: DUBEY, Vivek, SANTOS, Paulo, THOMA, Hubert, TIAN, Xianbin, LOWALEKAR, Rohit
• Format: Patent
• Language: English
• Published: 27.01.2022
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

A pharmaceutical composition comprising a. (S)-3-amino-6-methoxy-N-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl) -5-(trifluoromethyl)picolinamide or a pharmaceutically acceptable salt, polymorph, or co-crystal thereof, b. sodium starch glycolate, and c. sodium stearyl fumarate. A pharmaceutical composition comprising a. (S)-3-amino-6-methoxy-N-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl) -5-(trifluoromethyl)picolinamide or a pharmaceutically acceptable salt, polymorph, or co-crystal thereof, b. crospovidone, and c. sodium stearyl fumarate. Said compositions for use in the treatment of bronchiectasis, chronic obstructive pulmonary disorder, cystic fibrosis, chronic bronchitis or asthma. A process for the manufacture of said compositions, comprising the steps of: (a) blending (S)-3-amino-6-methoxy-N-(3,3,3-trifluoro-2- hydroxy-2-methylpropyl)-5-(trifluoromethyl)picolinamide together with sodium starch glycolate to form a material, (b) wet milling the material to form a plurality of granules, (c) blending the granules with sodium stearyl fumarate and sodium starch glycolate to form a final blend, and (d) compressing the final blend into a tablet. A process for the manufacture of said compositions, comprising the steps of: (a) blending (S)-3-amino-6-methoxy-N-(3,3,3-trifluoro-2- hydroxy-2-methylpropyl)-5-(trifluoromethyl)picolinamide together with sodium starch glycolate to form a material, (b) wet milling the material to form a plurality of granules, (c) blending the granules with sodium stearyl fumarate and crospovidone to form a final blend, and (d) compressing the final blend into a tablet.