PHARMACEUTICAL COMPOSITIONS FOR INJECTIONS AND USE THEREOF Russian patent published in 2024 - IPC A61K9/14 A61K31/42 A61K31/365 A61P33/00 

FIELD: veterinary science.

SUBSTANCE: group of inventions relates to a veterinary composition for injections for treating or preventing infection of animals with parasites, comprising a) moxidectin microspheres containing 50–99 wt.% of glycerol tristearate and 0.01–10 wt.% of antioxidant; and b) isoxazoline compound particles of formula (I)

where the compound of formula (I) is fluralaner, and where the moxidectin microspheres and the isoxazoline compound particles are suspended in an aqueous carrier containing: a suspending agent, where the suspending agent is selected from sodium carboxymethyl cellulose, polyvinylpyrrolidone and methylcellulose, a wetting agent, where the wetting agent is a poloxamer, a preservative and water, where the moxidectin microspheres and/or the isoxazoline compound particles have a volume-weighted particle size distribution D50, measured by a static light scattering method, from about 25 mcm to about 250 mcm, as well as to a kit for treating or preventing infection of animals with parasites, which includes: a) a first container containing a solid mixture of particles of an isoxazoline compound of formula (I) and moxidectin microspheres, and b) a second container with an aqueous carrier containing a suspending agent, a wetting agent, a preservative and water; and c) instructions for diluting moxidectin microspheres and isoxazoline compound particles with an aqueous carrier before subcutaneous injection into an animal, also relates to a method for preparing a veterinary composition for injections, comprising the steps of: a) preparation of particles of isoxazolines of formula (I); b) preparing moxidectin microspheres by melting glycerol tristearate and adding moxidectin and an antioxidant, and obtaining microspheres by spraying on a rotating disc and sieving; c) loading the moxidectin microspheres obtained in step b), together with the isoxazoline particles obtained in step a), into a first container; d) preparing an aqueous carrier by dissolving auxiliary substances, including suspending agents, wetting agents and preserving agents, in water and filling a second container; e) diluting the solids by transferring the aqueous carrier from the second container d) into the first container c) and shaking to form a ready-to-use suspension, and also relates to a method of using a kit for treating or preventing parasite infestation in an animal, comprising administering to the animal the reconstituted suspension prepared by the method by subcutaneous injection.

EFFECT: group of inventions provides the development of a composition having prolonged antiparasitic efficacy, which is safe to use, which has physical and chemical stability and which is safe for the animal after administration without side effects, especially unacceptable irritation of the injection site.

14 cl, 3 dwg, 5 tbl, 5 ex