ARIPIPRAZOLE EXTENDED RELEASE MICROSPHERE AND A METHOD OF ITS PRODUCTION Russian patent published in 2023 - IPC A61K9/52 A61K9/50 A61K31/496 A61K47/34 A61P25/18 

FIELD: medicine.

SUBSTANCE: group of inventions discloses a microsphere with prolonged release of aripiprazole containing aripiprazole and a copolymer of lactide and glycolide, where the intrinsic viscosity of the copolymer of lactide and glycolide is 0.2–0.55 dl/g, the average molecular weight of the copolymer of lactide and glycolide is 20,000–40,000, the partition coefficient of the lactide-glycolide copolymer is 1.0–3.0, and the molar ratio of lactide to glycolide in the lactide-glycolide copolymer is 50:50 to 75:25; the average particle size of the microsphere is less than 20 μm, and the content of aripiprazole is 65–80% of the total weight of the microsphere. The group of inventions also relates to a method of producing a microsphere with prolonged release of aripiprazole and to a suspension for obtaining an anti-schizophrenia agent. Besides, the average microsphere particle size of less than 20 µm provides pain relief during administration, and the aripiprazole sustained release microsphere is characterized by small particle size, high medicinal product loading, high yield and high degree of sphericity. EFFECT: rapid achievement of an effective concentration of the medicinal product at an early stage of administration without the effect of explosive release.

10 cl, 11 dwg, 8 tbl, 20 ex