DOSAGE FORMS IN FORM OF CAPSULES Russian patent published in 2024 - IPC A61K31/445 A61K47/10 A61K47/14 A61K47/38 A61K9/48 A61P9/10 A61P17/00 A61P25/28 A61P29/00 A61P37/06 

FIELD: medicine; pharmaceutics.

SUBSTANCE: group of inventions relates to the field of pharmaceutics, namely to solid solution capsule formulations for treating patients suffering from diseases that respond to C5a receptor modulation, method of making a solid solution capsule formulation, a single dose capsule for treating patients suffering said diseases, and to a kit for treating patients suffering said diseases. Solid solution capsule formulation for treating patients suffering from diseases which respond to modulation of the C5a receptor, containing compound 1 in the form of a free base in its neutral form or in the form of a pharmaceutically acceptable salt:

and a carrier containing at least one nonionic surfactant selected from the group consisting of polyoxyethylene 40 castor oil, macrogol-40-glycerol hydroxystearate, macrogol-glycerol ricinoleate, macrogol-15-hydroxystearate, polyoxyethylene 60 of castor oil, polyoxyethylene 60 of hydrogenated castor oil, polyoxyethylene 100 of hydrogenated castor oil, polyoxyethylene 200 of castor oil and polyoxyethylene 200 of hydrogenated castor oil, and at least one water-soluble solubiliser selected from the group consisting of PEG-1500, PEG-1540, PEG-2000, PEG-3000, PEG-3350, PEG-4000, PEG-6000, PEG-8000, poloxamer 188, poloxamer 237, poloxamer 338 and poloxamer 407, where compound 1 is from 1 to 3% by weight of the total weight of the contents of said capsule with solid solution, total weight of carrier includes ratio of at least one non-ionic surfactant and at least one water-soluble solubiliser from 30:70 to 65:35, and the content of carrier is 97–99% by weight of the total weight of the content of the capsule with the solid solution. Method of making a capsule formulation with a solid solution of the above composition, wherein said method includes: (a) melting the carrier, (b) combining the molten carrier obtained in step (a) with compound 1 to form a drug solution, (c) encapsulating the drug solution in a capsule shell, and (d) cooling the encapsulated drug solution to form a solid solution capsule containing compound 1. Solid solution capsule formulation for treating patients suffering from the above diseases, containing compound 1 in the form of a free base, in its neutral form or in the form of a pharmaceutically acceptable salt and a carrier containing at least one nonionic surfactant selected from the group consisting of polyoxyethylene 40 castor oil, macrogol-40-glycerol hydroxystearate, macrogol-glycerol ricinoleate, macrogol-15-hydroxystearate, polyoxyethylene 60 of castor oil, polyoxyethylene 60 of hydrogenated castor oil, polyoxyethylene of 100 of hydrogenated castor oil, polyoxyethylene 200 of castor oil and polyoxyethylene 200 of hydrogenated castor oil, equal to at least 10, and at least one water-soluble solubiliser selected from the group consisting of PEG-1500, PEG-1540, PEG-2000, PEG-3000, PEG-3350, PEG-4000, PEG-6000, PEG-8000, poloxamer 188, poloxamer 237, poloxamer 338 and poloxamer 407, where compound 1 is from 1 to 3% by weight of the total weight of the contents of said capsule with solid solution, total weight of carrier contains ratio of at least one non-ionic surfactant and at least one water-soluble solubiliser in ratio from 30:70 to 65:35, and content of carrier is 97–99% by weight of total weight of contents of said capsule with solid solution, wherein said solid solution capsule composition is made in accordance with said method. Single-dose capsule for treating patients suffering from the above diseases, containing 2.6–25.2 mg of compound 1 in the form of a free base, in its neutral form and a carrier of the above composition, with the above content of compound 1 and the carrier by weight of the total weight of the contents of the capsule formulation, with said content of the nonionic surfactant and the water-soluble solubiliser in the total weight of the carrier. Kit for treating patients suffering the above diseases, containing one or more of the above capsules with a solid solution or one or more of the above capsules with a single dose.

EFFECT: said group of inventions enables to obtain pharmaceutical compositions which meet the requirements of manufacturability, stability, bioavailability and pharmacokinetics, suitable for oral administration to humans or other animals.

26 cl, 11 dwg, 15 tbl, 12 ex