N-[5-(AMINOSULPHONYL)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2-PYRIDINYL)PHENYL]ACETAMIDE MESYLATE MONOHYDRATE HAVING SPECIFIC PARTICLE SIZE DISTRIBUTION RANGE AND SPECIFIC SURFACE AREA RANGE FOR USE IN PHARMACEUTICAL FORMULATIONS Russian patent published in 2017 - IPC C07D417/12 A61K31/4439 A61K31/10 A61K45/06 A61K9/16 A61K31/4402 A61P31/22 

FIELD: chemistry.

SUBSTANCE: present invention relates to a crystalline monohydrate of N-[5-(aminosulphonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide monomethanesulphonic acid of following formula

,

where particles of monohydrate of N-[5-(aminosulphonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide monomethanesulphonic acid have particle size ranging from 1 to 500 mcm, particle size distribution, which is determined in d (0.1) from 2 to 100 mcm, d(0.5) from 30 to 210 mcm and d(0.9) from 70 to 400 mcm, and specific surface area less than 1.0 m²/g. Invention also relates to a pharmaceutical composition for treating or preventing infectious diseases, containing crystalline particles of monohydrate of N-[5-(aminosulphonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide monomethanesulphonic acid, where particles of monohydrate of N-[5-(aminosulphonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide monomethanesulphonic acid have particle size ranging from 1 to 500 mcm, particle size distribution, which is determined in d(0.1) from 2 to 100 mcm, d(0.5) from 30 to 210 mcm and d(0.9) from 70 to 400 mcm, and specific surface area less than 1.0 m²/g, together with at least one pharmaceutically acceptable carrier, inert filler, solvent and/or diluent.

EFFECT: novel form is characterised by improved properties in relation to stability and bioavailability.

13 cl, 9 dwg, 10 tbl, 7 ex