SODIUM BENZOATE COCRYSTALS AND THEIR USE Russian patent published in 2022 - IPC C07C63/08 C07C57/10 C07C57/44 C07D213/55 

FIELD: medicine.

SUBSTANCE: invention relates to a method for producing cocrystals for their use in the treatment and/or reduction in the risk of a psychoneurological disorder (for example, psychotic disorders, depressive disorders or Alzheimer’s disease) or disorder of glucose or lipid metabolism (for example, obesity, diabetes, hypercholesterolemia, hypertension or hyperlipidemia). The method for producing cocrystal of a sodium benzoate compound and a co-component is described, in which (a) the co-component is sorbic acid, the molar ratio of the sodium benzoate compound and sorbic acid in cocrystal is 1:2, and cocrystal is characterized by powder X-ray diffractogram containing characteristic peaks at following values of an angle 2θ: 4.8, 7.4, 8.2, 8.4, 14.5, 17.4, 19.3, 19.7, 22.1, 22.8, 23.4, 25.5, 25.9, 27.3 and 30.6, when determining using Cu Kα radiation and an incident beam path provided with a divergence slit of 0.2 mm and 0.02 mm scattering screen; (b) the co-component is sorbic acid, the molar ratio of the sodium benzoate compound and sorbic acid in cocrystal is 1:1, and cocrystal is characterized by powder X-ray diffractogram containing characteristic peaks at following values of an angle 2θ: 4.9, 5.7, 7.4, 8.2, 9.1, 11.4, 13.0, 14.9, 16.1, 16.9, 17.5, 17.8, 18.3, 20.0, 21.5, 22.5, 22.8, 23.4, 24.8, 25.5, 27.2, 27.6, 28.5, 29.7, 30.5, 31.5, 32.5, 36.0, 37.0, 39.1, 40.0, 41.0 and 43.2, when determining using Cu Kα radiation and an incident beam path provided with a divergence slit of 0.2 mm and 0.02 mm scattering screen; or (c) the co-component is nicotinic acid, the molar ratio of the sodium benzoate compound and nicotinic acid in cocrystal is 1:1, and cocrystal is characterized by powder X-ray diffractogram containing characteristic peaks at following values of an angle 2θ: 6.5, 11.1, 13.1, 15.5, 16.7, 17.5, 18.4, 19.7, 20.3, 20.7, 21.2, 21.6, 22.3, 22.8, 24.4, 24.8, 25.9, 26.9, 28.0, 28.7, 29.2, 30.0, 30.6, 31.6, 32.3, 33.6, 34.1, 35.8, 36.3, 37.2, 38.3, 39.1, 39.9, 41.2, 41.8 and 42.8, when determining using Cu Kα radiation and an incident beam path provided with a divergence slit of 0.2 mm and 0.02 mm scattering screen. The method includes following stages: (i) mixing of the sodium benzoate compound and the co-component in a solvent at a temperature of 40-110°C to form a saturated solution, wherein the sodium benzoate compound and the co-component are in a molar ratio from 1:10 to 10:1, where the solvent is methanol; (ii) heating and mixing of the solution at a temperature of 70-150°C to provide the formation of cocrystal; or (ii) cooling of the solution to a room temperature; addition of a primer of cocrystal of the sodium benzoate compound and the co-component in the resulting solution to form a mixture; placement of the mixture at a room temperature to provide the formation of cocrystal; and (iii) collection of cocrystal formed at the previous stage.

EFFECT: obtaining cocrystals for use in medicine.

2 cl, 22 dwg, 5 ex