MACOZINONE-BASED PHARMACEUTICAL COMPOSITION FOR TREATMENT OF TUBERCULOSIS INCLUDING MULTI- AND EXTENSIVELY DRUG-RESISTANT FORMS THEREOF Russian patent published in 2021 - IPC A61K9/26 A61K31/5415 A61K47/10 A61K47/26 A61K47/32 A61K47/38 A61K47/40 A61P31/06 

FIELD: medicine.

SUBSTANCE: group of inventions relates to the field of medicine and pharmaceuticals. The first object constitutes a gastroretentive swellable mucoadhesive tablet for controlled release of macozinone in the stomach and upper small intestine, constituting a combined system including a complex of macozinone or a pharmaceutically acceptable salt thereof in a therapeutically effective amount and cyclodextrin in form of granules coated with a layer of mucoadhesive polymer, wherein said layer includes a solubiliser, and pressed into a polymer matrix based on two hydrophilic soluble or one hydrophilic soluble and one insoluble swellable and mucoadhesive polymers, and an additional pharmaceutically acceptable excipient. The second object constitutes an application of the tablet for prevention and/or treatment of a disease caused by mycobacteria.

EFFECT: technical result of the invention is production of a gastroretentive tablet containing macozinone or a pharmaceutically acceptable salt thereof with modified release of an active substance with an increased relative bioavailability, providing long-term maintenance of a therapeutically significant concentration of an active substance in the body under conditions of a single oral administration, exhibiting high compliance and suitability for use in regimens of complex therapy of tuberculosis infection.

26 cl, 4 dwg, 11 tbl, 14 ex