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MICELLAR AGENT CONTAINING POORLY WATER-SOLUBLE ANTICANCER AGENT, ANTICANCER DRUG AND NOVEL BLOCK COPOLYMER
MICELLAR AGENT CONTAINING POORLY WATER-SOLUBLE ANTICANCER AGENT, ANTICANCER DRUG AND NOVEL BLOCK COPOLYMER
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机译：包含弱水溶性抗癌剂，抗癌药和新型嵌段共聚物的胶束剂
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摘要
FIELD: medicine; pharmacology.;SUBSTANCE: novel micellar preparation is invented, which contains the anticancer agent with increased water-solubility, and which provides its high concentration in blood after the intravenous injection. The micellar preparation is produced from block copolymer with the general formula (1): where. R1 identifies the atom-methyl group; R2 identifies the tri-methyl group; R3 identifies the methylen group; R4 identifies the acetyl group; R5 identifies the hydroxyl group, optionally substituted by aryl C2-8alcoxyl group, substituted C1-4alkylamino group or amino group, containing the residue of amino acid or peptide derivative; n has integral values from 5 to 1000, m has integral values from 2 to 300, and x has integral values from 1 to 300; provided, percentage of hydroxyl groups in R5 is from 0 to 99%, and x has value not more than m; and taxane anticancer agent at concentration from 0.1 to 50 weight% per total mass of the agent and block copolymer.;EFFECT: preparation has high medical activity and reduced side effects.;7 cl, 4 tbl, 3 ex
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机译：领域：医学;药理学：物质：发明了新的胶束制剂，其包含具有增加的水溶性的抗癌剂，并且在静脉内注射后在血液中提供其高浓度。胶束制剂由具有通式（1）的嵌段共聚物生产：<图像文件=“ 00000002.GIF” he =“ 15” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 139” />其中。 R1表示原子甲基。 R 2表示三甲基; R 3标识亚甲基; R4标识乙酰基; R5表示羟基，其任选地被芳基C 2-8 烷氧基，取代的C 1-4 烷基氨基或氨基取代，包含氨基酸或肽的残基衍生物; n具有5到1000的整数值，m具有2到300的整数值，x具有1到300的整数值;假设R5中羟基的百分比为0至99％，且x的值不大于m;紫杉烷类抗癌剂的浓度为试剂和嵌段共聚物总质量的0.1％至50％（重量）。;效果：该制剂具有很高的医疗活性，并减少了副作用。; 7 cl，4 tbl，3 ex
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