METHOD FOR APPLICATION OF COPOLYMER OF DIMETHYLAMINOETHYLMETHACRYLATE, BUTYLMETHACRYLATE AND METHYL METHACRYLATE TO INCREASE SOLUBILITY AND/OR BIOAVAILABILITY OF ANTIRETROVIRAL ACTIVE PHARMACEUTICAL SUBSTANCE IN MANUFACTURE OF SOLID DISPERSION ON GRANULAR CARRIER Russian patent published in 2021 - IPC A61K31/34 A61K31/427 A61K31/505 A61K31/513 A61K31/536 A61K31/635 A61K47/32 A61P31/18 

FIELD: medicine.

SUBSTANCE: present invention relates to the field of medicine, namely to a method for manufacturing an oral antiretroviral therapeutic agent, characterized by the fact that when implementing the method: (a) an active pharmaceutical substance (APS) selected from a group of protease inhibitors consisting of amorphous darunavir, darunavir ethanolate, ritonavir, lopinavir, or reverse transcription inhibitors consisting of etravirine and efavirenz is mixed with a copolymer of dimethylaminoethylmethacrylate, butyl methacrylate and methyl methacrylate having a sequence of links according to formula (I):

where x=2, y=1, z=1 and the average weight mass Mw equal to 47 kDa, in the mass ratio of the APS : copolymer 1:(1-5) to obtain a mixture, (b) the mixture is dissolved in a solvent selected from ethyl absolute alcohol and tetrahydrofuran to obtain a solution, (c) the solution is sprayed in a fluidized bed installation on an acceptable granular carrier selected from microcrystalline cellulose, magnesium aluminosilicate, calcium phosphate, lactose, mannitol, hydroxypropyl cellulose, taken in the mass ratio of APS granular carrier 1:(1-3), to obtain a solid dispersion of APS on the granular carrier, (d) the solid dispersion of the APS on the granular carrier is dried until the residual solvent content is below the permissible level.

EFFECT: present invention provides obtaining of solid dispersions of antiretroviral APS on a granular carrier with a low content of impurities, good characteristics of bulk density, flowability, angle of natural slope and compressibility.

1 cl, 21 dwg, 33 ex