RAPIDLY DISSOLVING PHARMACEUTICAL FORM OF INDOMETHACIN AND METHOD FOR PRODUCTION THEREOF (VARIANTS) Russian patent published in 2022 - IPC A61K31/345 A61K33/10 A61K47/10 A61K47/12 A61K47/58 

FIELD: pharmaceuticals.

SUBSTANCE: group of inventions relates to medicine, namely, to a rapidly dissolving pharmaceutical form of indomethacin in the form of an effervescent granulate or a tablet, including indomethacin, polyvinyl pyrrolidone (PVP) with a molecular weight of 11,000±9,000, a granulating agent, an effervescent pair - acidic and basic components, and a glidant excipient, with the following ratio of components, wt.%: indomethacin 0.40 to 3.00, PVP-11,000±9,000 0.10 to 30.00, granulating agent 0.01 to 10.00, basic component 20.00 to 75.00, acidic component 20.00 to 75.00, glidant 0.50 to 3.00; also relates to a method for producing rapidly dissolving pharmaceutical forms of indomethacin in the form of effervescent granulate or a tablet containing no components with crystallisation water, characterised by the fact that the organic solvent is divided into two parts, in one part, a mixture of indomethacin and polyvinyl pyrrolidone with a molecular weight of 11,000±9,000 is dissolved, wherein from 1 to 100 parts of the solvent is taken per 1 part of the mixture at a temperature of 95±5°C, the resulting solution is used to granulate the powder of the basic component, in the other part of the organic solvent, a 1 to 10% solution of the granulating agent is prepared at a temperature of 95±5°C, the resulting solution is used to granulate the powder of the acidic component, the resulting basic and acidic granulates are powdered with the gildant, mixed in the ratio required to achieve a pH of 6.0±0.5 when dissolving the pharmaceutical form in water, tableted or packaged into sealed packages, and also relates to a method for producing rapidly dissolving pharmaceutical forms of indomethacin in the form of an effervescent granulate containing at least one component containing crystallisation water, characterised by the fact that a mixture of indomethacin and polyvinyl pyrrolidone with a molecular weight of 11,000±9,000 is dissolved in an organic solvent, wherein from 1 to 100 parts of the solvent is taken per 1 part of the mixture at a temperature of 95±5°C, the resulting solution is used to granulate the powder of the basic component, a 1 to 10% solution of the granulating agent is prepared in water at a temperature of 95±5°C, the resulting solution is used to granulate the powder of the acidic component, the resulting basic and acidic granulates are powdered with the gildant and packaged separately into sealed packages in the ratio required to achieve a pH of 6.0±0.5 when dissolving the pharmaceutical form in water.

EFFECT: group of inventions ensures development of a composition of rapidly dissolving effervescent granules and tablets of indomethacin, characterised by increased solubility and high release of indomethacin from the PF (99±1%), providing a therapeutically effective concentration of indomethacin in a solution in less than 5 minutes (within a time interval of 2.5±0.5 min).

19 cl, 1 dwg, 3 tbl, 15 ex