SOLID DISPERSION of 4- (3-ETHOXY-4-HYDROXIBENZIL) -5-OXO-5,6-DIHYDRO-4H- [1,3,4] -THIADIAZINE-2- (2,4-DIFLUOROPHENYL) -CARBOXAMIDE FOR PRODUCING PHARMACEUTICAL FORMULATION AND METHOD OF TREATMENT OF CHRONIC INFECTIOUS DISEASES Russian patent published in 2021 - IPC A61K31/549 A61K47/30 A61P31/04 

Abstract RU 2743927 C1

FIELD: pharmaceutical industry and medicine.

SUBSTANCE: invention relates to chemical and pharmaceutical industry and medicine, in particular to solid dispersion for production of pharmaceutical formulations. It comprises the active ingredient 4- (3-ethoxy-4-hydroxybenzyl) -5-oxo-5,6-dihydro-4H- [1,3,4] -thiadiazine-2- (2,4-difluorophenyl) -carboxamide and at least one pharmaceutically acceptable polymer, which is contained in a solid dispersion at a mass ratio of the active substance to the polymer from 1: 1 to 1:10, while the active substance is contained in amorphous form or in amorphous form with an admixture of microcrystalline and crystalline phases. The invention also relates to a method for treatment of chronic infections of the respiratory system caused by Pseudomonas aeruginosa antibiotic-resistant strains. The method comprises the use of the specified solid dispersion in an effective therapeutic dose for humans in an amount of 1 to 4 milligrams per kilogram body weight (mpk) equivalent to the active ingredient.

EFFECT: technical result consists in obtaining a solid dispersion with increased bioavailability in comparison with the active substance in crystalline form and therapeutic efficiency in relation to infections caused by Pseudomonas aeruginosa antibiotic-resistant strains.

8 cl, 9 ex, 13 tbl, 18 dwg

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RU 2 743 927 C1

Authors

Zigangirova Nailia Akhatovna

Lubenets Nadezhda Leonidovna

Zolotov Sergei Anatolevich

Luiksaar Sergei Igorevich

Zaiakin Egor Sergeevich

Zakhoda Oleg Iurevich

Sheremet Anna Borisovna

Soloveva Anna Vladimirovna

Gintsburg Aleksandr Leonidovich

Dates

2021-03-01Published

2020-07-10Filed