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ANTIBIOTIC CONJUGATE AND ANTIBACTERIAL MEDICINAL AGENT BASED ON SAID CONJUGATE

机译:基于所述共轭物的抗菌共轭物和抗菌药物制剂

摘要

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
机译:领域:化学物质:含有羧基,硫酸根,羰基,醛基,氯离子或其他带负电荷基团的聚阴离子多糖与抗生素结合物,聚合物载体的分子质量(MM)为25至110 kDa。抗生素结合物是通过以1.0至4.5 Mrad的剂量暴露于加速电子流或伽马辐射中而获得的。使用的抗生素是异烟酰胺,莫西沙星或乙胺嘧啶。所使用的多糖是分子量为20至60 kDa的硫酸化葡聚糖,分子量为60至100 kDa的羧甲基化葡聚糖。所用的聚合物载体是分子量为2至10kDa的聚环氧乙烷或聚乙烯乙酸乙烯酯,胶原,明胶,聚尿烷或它们的混合物,每种所述聚合物载体的分子量为2至10kDa。抗菌药物包含上述抗生素结合物,也可以包含药学上可接受的添加剂。效果:获得抗生素结合物,其通过清除剂-受体依赖性内吞作用在巨噬细胞中具有高选择性积聚率,小剂量服用可延长治疗时间效果和降低的总体毒性。; 10 cl,4 dwg,9 tbl,9 ex

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