CO-CRYSTAL OF KETOPROFEN CONTAINING ITS COMPOSITIONS, A METHOD OF ITS PRODUCTION AND USE Russian patent published in 2023 - IPC C07C57/30 C07C59/84 C07C51/41 

Abstract RU 2802975 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a method of obtaining form 1 of the ketoprofen-lysine co-crystal characterized by an x-ray pattern with characteristic peaks at 16.3; 17.5; 17.6; 17.7; 19.6; 19.7° 2-theta ± 0.20°, where the ratio of the quantities of ketoprofen and lysine molecules is 1:1, including: a) preparing a saturated solution of ketoprofen; b) mixing a saturated solution of ketoprofen with lysine; where the ratio of equivalents of ketoprofen in saturated solution and lysine is from 3:1 to 1:1; where the solvent used for the saturated solution of ketoprofen is selected from alcohols, where the said alcohols are selected from the group consisting of the following: 1-butanol, 1-propanol, 2-butanol, 2-propanol, 1-pentanol and benzyl alcohol; esters, where these esters are selected from the group consisting of the following: ethyl acetate, methyl acetate, propyl acetate; amide, where the said amide is N,N-dimethylacetamide; a ketone, where the said ketone is 4-methyl-2-pentanone; aromatic solvents, where these aromatic solvents are selected from the group consisting of the following: toluene, benzonitrile, p-xylene; a halogenated solvent, wherein the said halogenated solvent is dichloromethane; and their mixtures; and where the ratio of the mass of lysine (mg) to the volume (ml) of a saturated solution of ketoprofen is from 5 mg/ml to 60 mg/ml.

EFFECT: method has been developed for obtaining form 1 of the ketoprofen-lysine co-crystal, which is highly crystalline and can be used in medicine as an effective agent for the treatment of pain and inflammatory diseases.

2 cl, 17 dwg, 13 tbl

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RU 2 802 975 C2

Authors

Aramini, Andrea

Bianchini, Gianluca

Lillini, Samuele

Dates

2023-09-05Published

2019-12-20Filed