SOLID ORAL FORMULATIONS AND CRYSTALLINE FORMS OF APOPTOSIS PROTEIN INHIBITOR Russian patent published in 2018 - IPC C07D417/04 A61K31/427 A61K9/20 A61K9/28 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: present invention relates to a pharmaceutical composition inhibiting an apoptosis protein comprising, as an active ingredient, a crystalline hemihydrate form H_A (S)-N-((S)-1-cyclohexyl-2-{(S)-2-[4-(4-fluorobenzoyl)thiazol-2-yl]pyrrolidine-1-yl}-2-oxoethyl)-2-methylaminopropionamide characterized by the formula (I), in an amount of more than 100 mg and pharmaceutically acceptable excipients. Crystalline hemihydrate form H_A of compound (I) is characterized by a powder X-ray diffraction pattern comprising three or more values of 2θ, selected from the group consisting of 8.3 ± 0.2, 9.5 ± 0.2, 13.5 ± 0.2, 17.3 ± 0.2, 18.5 ± 0.2 and 18.9 ± 0.2 at room temperature. Composition of the invention further comprises a surfactant, an acid, an antioxidant.

(I).

EFFECT: technical result is an oral pharmaceutical composition with a high content of active agent.

24 cl, 18 dwg, 17 ex, 10 tbl