INJECTABLE ISOXAZOLINE PHARMACEUTICAL COMPOSITIONS AND THEIR USE Russian patent published in 2023 - IPC A61K9/14 C07D261/04 A61K31/42 A61P33/00 

FIELD: pharmaceuticals.

SUBSTANCE: group of inventions relates to an injectable pharmaceutical composition containing particles of an isoxazoline compound of formula (I)

Formula (I)

where R¹ represents halogen; n is 2; R² represents CF₃; T represents a 6-membered ring which is optionally substituted with one or more Y radicals; Y represents methyl; Q represents X-NR³R⁴; X represents CO; R³ represents CH₂-C(O)NHCH₂CF₃; R⁴ represents either hydrogen or a salt thereof, and a pharmaceutically acceptable excipient, wherein the isoxazoline compound has a volume-weighted particle size distribution D50 measured by a static light scattering instrument, from 50 microns to 150 microns, where the isoxazoline compound is suspension in the composition, also refers to a method for treating or preventing infestation of an animal, comprising administering to an animal in need thereof an effective amount of an injectable pharmaceutical composition, also relates to a kit for treating or preventing infestation of an animal, wherein the kit comprises two or more containers of a) a solid crystalline isoxazoline compound; b) a carrier medium containing a pharmaceutically acceptable excipient capable of forming a suspension with compound a); and c) instructions for combining the solid crystalline isoxazoline compound with a vehicle prior to injection, wherein for the solid crystalline isoxazoline compound, the particle size D50 is 75 microns to 130 microns and the particle size D10 is 30 microns to 50 microns, and also applies to a method of treating or preventing infestation of an animal with parasites, comprising administering a kit to an animal requiring it.

EFFECT: group of inventions provides a composition that demonstrates the desired bioavailability and duration of action, while causing minimal irritation at the injection site.

23 cl, 7 ex, 9 tbl, 4 dwg