PHARMACEUTICAL COMPOSITION CONTAINING PROLONGED RELEASE MICROSPHERES CONTAINING GPP-1 ANALOGUE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF Russian patent published in 2025 - IPC A61K9/14 A61K38/26 A61K47/56 A61K47/61 A61P3/04 A61P3/10 A61P25/16 A61P25/28 B01F21/00 B01F23/00 B01D1/00 

FIELD: medicine; pharmaceutics.

SUBSTANCE: group of inventions relates to a pharmaceutical composition for preventing or treating diabetes mellitus, type 2 diabetes mellitus, obesity, non-alcoholic steatohepatitis, Alzheimer's disease or Parkinson's disease, containing a prolonged release microsphere containing a free base of semaglutide and a biodegradable polymer, in which the free base of semaglutide is from 3% to 15% by weight in terms of semaglutide, referred to the total weight of the microsphere, biodegradable polymer contains two types of polylactide-co-glycolide (PLGA), said two types of PLGA independently have molar ratio of repeating units of lactide: glycolide from 65:35 to 75:25 and characteristic viscosity from 0.32 dl/g to 0.44 dl/g, where the sustained-release microsphere is prepared by a production method comprising a step of dissolving a free base of semaglutide and two types of PLHA in an organic solvent to prepare a solution containing a free base of semaglutide and a polymer, and a step of adding a solution containing a free base of semaglutide and a polymer to an aqueous phase (continuous phase) containing a surfactant, to prepare an emulsion, in which the continuous phase pH is 5 or less, the prolonged release microsphere releases the semaglutide free base for 1 to 2 months, and the sustained-release microsphere is prepared for injection, and also relates to methods of producing the sustained-release microsphere.

EFFECT: group of inventions provides creating an injectable composition with excellent semaglutide activity when administered, but with inhibition of the initial excessive release of semaglutide and at the same time with the release thereof for 1 to 2 months in an effective concentration with inhibition of lethal side effects and minimization of pain and inflammatory response in the patient at the injection site of the composition.

18 cl, 5 dwg, 5 tbl, 43 ex