FIELD: chemistry.
SUBSTANCE: invention relates to a method for the production of a crystalline form of citrate of A 5-(2,4-diaminopyrimidine-5-yloxy)-4-isopropyl-2-methoxy-benzenesulfonamide, which is characterized by the presence of an X-ray powder diffraction profile obtained using Kα-radiation of copper, having peaks at values of 2Θ of 9.38 ± 0.20, 11.69 ± 0.20, 14.41 ± 0.20, 16.22 ± 0.20, 19.54 ± 0.20, 21.14 ± 0.20, and 26.31 ± 0.20 degrees. The method is carried out by a) addition of ethanol to a form of a free base of A 5-(2,4-diaminopyrimidine-5-yloxy)-4-isopropyl-2-methoxy-benzenesulfonamide to form a solution; b) addition of citric acid to the solution of the stage a) to form a suspension; c) mixing of the suspension of the stage b); and d) drying of the mixed suspension of the stage c) by filtration at reduced pressure.
EFFECT: crystalline form of citrate of A 5-(2,4-diaminopyrimidine-5-yloxy)-4-isopropyl-2-methoxy-benzenesulfonamide, having improved water solubility, without showing signs of disproportioning and wetting due to absorption of moisture from the air.
1 cl, 17 dwg, 16 tbl, 20 ex
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