ANTIBIOTIC CONJUGATE AND ANTIBACTERIAL MEDICINAL AGENT BASED ON SAID CONJUGATE Russian patent published in 2009 - IPC C08B37/00 A61K31/74 A61K31/765 A61K31/715 

FIELD: chemistry.

SUBSTANCE: antibiotic conjugate with polyanion polysaccharide, containing carboxy, sulphate, carbonyl, aldehyde, choride or other negatively charged groups, and a polymer carrier have molecular mass (MM) of 25 to 110 kDa. The antibiotic conjugate is obtained through exposure in a stream of accelerated electrons or gamma-radiation in doses of 1.0 to 4.5 Mrad. The antibiotic used is isoniaside, moxifloxacin or pyrimethamine. The polysaccharide used is sulphated dextran with molecular mass of 20 to 60 kDa, carboxymethylated glucan with molecular mass of 60 to 100 kDa. The polymer carrier used is polyethylenoxide with molecular mass of 2 to 10 kDa or polyethylenevinylacetate, collagen, gelatin, polyurathane or their mixture with molecular mass of each of the said polymer carriers of 2 to 10 kDa. Antibacterial medicinal agent contains the said antibiotic conjugate and can also contain pharceutically acceptable additives.

EFFECT: obtaining antibiotic conjugate, which has high rate of selective accumulation in macrophages through scavenger-receptor-dependent endocytosis, high therapeutic effectiveness when taken in small doses, prolonged effect and reduced overall toxicity.

10 cl, 4 dwg, 9 tbl, 9 ex