INJECTABLE COMPOSITIONS OF PROLONGED ACTION OF SALTS OF KETAMINE PAMOATE Russian patent published in 2024 - IPC A61K9/08 A61K9/10 A61K31/135 A61K47/02 A61K47/10 A61K47/14 A61K47/18 A61K47/20 A61K47/22 A61K47/34 A61K47/38 A61P23/00 A61P25/00 A61P25/24 A61P29/00 

FIELD: chemistry; pharmaceutics.

SUBSTANCE: group of inventions relates to chemistry and pharmaceutics, specifically to a sustained-release pharmaceutical composition, as well as to a method of treating a disease or pathological condition selected from a disease of the central nervous system, depression, anti-inflammatory action, pain, and to an anaesthesia method, wherein said methods involve administering to a subject the disclosed pharmaceutical composition which demonstrates a sustained release profile maintained for 72 hours after administration. Disclosed pharmaceutical composition contains a crystalline or amorphous form of a pamoate salt of ketamine, having a stoichiometric ratio of ketamine to pamoate of 2:1, and a pharmaceutically acceptable carrier thereof, selected N-methyl-2-pyrrolidone, dimethylsulfoxide, N, N-dimethylacetamide, polyethylene glycol 4000, polysorbate 80, sodium carboxymethyl cellulose, sodium chloride, polylactic acid, copolymer of lactic acid and glycolic acid and any combination thereof, where the pamoate salt of ketamine is selected from S-, R- or R, S-ketamine pamoate, wherein said crystalline form is represented by a powder X-ray diffraction pattern comprising one or more values of 2θ selected from 6.0, 10.7, 11.6, 12.0, 13.0, 14.7, 15.0, 22.2, 25.2 and 30.3 (±0.2 2θ).

EFFECT: group of inventions provides a prolonged release profile of ketamine without undesirable initial bursts, as well as high bioavailability and reduced risks of systemic side effects.

14 cl, 45 dwg, 28 tbl, 24 ex