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
| Title | Year | Author | Number | 
|---|---|---|---|
| PHARMACEUTICAL COMPOSITION OF 4-(3-ETHOXY-4-HYDROXYBENZYL)-5-OXO-5,6-DIHYDRO-4H-[1,3,4]-THIADIAZIN-2-(2,4-DIFLUOROPHENYL) CARBOXAMIDE IN CRYSTALLINE FORM , AND USE THEREOF AS ANTIBACTERIAL AGENT FOR TREATING ACUTE, RECURRENT AND CHRONIC INFECTIONS | 2020 | 
 | RU2737087C1 | 
| APPLICATION OF 4-(3-ETHOXY-4-HYDROXYBENZYL)-5-OXO-5,6-DIHYDRO-4H-[1,3,4]-THIADIAZINE-2-(2,4-DIFLUOROPHENYL)-CARBOXAMIDE TO SUPPRESS INFECTION, CAUSED BY ANTIBIOTIC-RESISTANT PSEUDOMONAS AERUGINOSA STRAINS, AND METHOD OF SUPPRESSION OF THIS INFECTION | 2016 | 
 | RU2624846C1 | 
| METHOD FOR PRODUCTION OF POLYMORPHOUS FORM OF 4-(3-ETHOXY-4-HYDROXYBENZYL)-N-(2,4-DIFLUORPHENYL)-5-OXO-5,6-DIHYDRO-4H-1,3,4-THIADIZINE-2-CARBOXAMIDE | 2022 | 
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| MODIFIED NUTRIENT MEDIUM FOR ACCUMULATION OF PSEUDOMONAS AERUGINOSA (BONDE MEDIUM) | 2024 | 
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Authors
Dates
2021-03-01—Published
2020-07-10—Filed