NOVEL COCRYSTALS OF AGOMELATINE, SYNTHESIS METHOD THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME Russian patent published in 2016 - IPC C07C231/12 C07C233/18 A61K31/165 A61P25/16 A61P25/18 A61P25/28 A61P3/00 C30B29/54 

FIELD: chemistry.

SUBSTANCE: invention relates to agomelatine co-crystall, which is characterised by that it consists of agomelatine, or N-[2-(7-methoxy-1-naphtyl)ethyl]acetamide of formula (I), and organic acid, which is in solid state at ambient temperature, which is selected from a steam-hydroxybenzoic acid, citric acid, oxalic acid, Gallic acid, maleic acid, malonic acid, glutaric acid, glycolic acid or ketoglutaric acid. Agomelatine co-crystall and organic acid are obtained by mixing two components in organic solvent in desirable proportions: 1 agomelatine equivalent at 0.25-4 mol equivalent of organic acid, than obtained solution is stirred and optionally is heated at temperature not exceeding boiling point of selected solvent, then mixture is cooled while stirring, and deposited co-crystall naturally or precipitates after absorption in second solvent, obtained precipitate is filtered and dried. Also co-crystall is obtained by combined grinding of two components. Also co-crystall is obtained by mixing two components in organic or aqueous-organic solvent, followed by freezing and drying at very low temperature. Alternative method of preparing co-crystall involves mixing powders agomelatine and said acid in mixer, and then mixture is extruded by extrusion in twin-screw mixers without matrix to obtain solid granulated product directly at extrusion device outlet. Agomelatine co-crystall and organic acid are applicable for preparing drugs for treating disturbed melatonin aergic system.

EFFECT: technical result is agomelatine co-crystalls permitting to modify rate of active ingredient dissolution.

19 cl, 13 ex