POLYMORPHOUS AND PSEUDOPOLYMORPHOUS FORMS OF THE PHARMACEUTICAL COMPOUND Russian patent published in 2020 - IPC C07D471/08 A61K31/439 A61K31/4188 A61P31/04 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to an antibacterial pharmaceutical composition, containing an effective amount of the sodium salt of (1R,2S,5R)-7-oxo-6-sulphooxy-1,6-diazabicyclo[3.2.1]octane-2-carboxamide of formula (I) in a crystalline enantiomeric form, which is hydrated or anhydrous, and a pharmaceutically acceptable excipient, wherein said salt is found in its monohydrate pseudopolymorphic form "A", which has X-ray diffraction diagram with at least two characteristic peaks of about 8.5 +/− 0.5 degrees 2θ and about 15.3 +/− 0.5 degrees 2θ; or where said salt is in its dihydrate pseudopolymorphic form "E", which has X-ray diffraction diagram with five characteristic lines at 2θ (±0.5°) 13.65, 15.01, 15.38, 15.72, 19.42 and two characteristic lines at 15.01 and 24.57; or where said salt is in its polymorphous form "B", which has X-ray diffraction diagram with at least two characteristic peaks of about 13.0 +/− 0.5 degrees 2θ and about 16.5 +/− 0.5 degrees 2θ; or where said salt is in its polymorphous form "D", which has X-ray diffraction diagram with five characteristic lines at 2θ (±0.1°) 16.23, 17.44, 17.75, 18.53, 22.22 and characteristic line at 12.43.

EFFECT: obtaining a stable antibacterial pharmaceutical composition, containing an effective amount of sodium salt (1R,2S,5R)-7-oxo-6-sulphooxy-1,6-diazabicyclo[3_2_1]octane-2-carboxamide of formula (I), which ensures better retention of the active ingredient.

10 cl, 13 dwg, 12 ex