公开(公告)号：US20060099265A1

公开(公告)日：2006-05-11

申请号：US10548998

申请日：2004-03-18

申请人： Kazuhisa Shimizu ,  Toshitaka Murata ,  Katsuhiko Sagawa

发明人： Kazuhisa Shimizu ,  Toshitaka Murata ,  Katsuhiko Sagawa

IPC分类号： A61K9/14

CPC分类号： A61K9/1075 ,  A61K31/337 ,  A61K47/42

摘要： A novel micellar preparation in which the solubility of a sparingly water-soluble anticancer agent has been heightened and which after intravenous administration, enables a high blood concentration to be maintained. The preparation has high medicinal activity and/or is reduced in side effects. The micellar preparation is formed from a block copolymer represented by the following general formula (1): [wherein R1 represents hydrogen or C1-5 alkyl; R2 represents C1-5 alkylene; R3 represents methylene or ethylene; R4 represents hydrogen or C1-4 acyl; R5 represents hydroxyl, optionally substituted aryl C2-8 alkoxyl, substituted C1-4 alkylamino, or amino having a residue of either an amino acid or a peptide derivative; n is an integer of 5 to 1,000; m is an integer of 2 to 300; and x is an integer of 1 to 300; provided that the proportion of hydroxy in the R5's is 0 to 99% and x is not larger than m] and a sparingly water-soluble anticancer agent.

摘要翻译： 提高了微水溶性抗癌剂的溶解性的新型胶束制剂，并且在静脉内给药后能够维持高血药浓度。 该制剂具有高药用活性和/或副作用减少。 胶束制剂由以下通式（1）表示的嵌段共聚物形成：[其中R 1表示氢或C 1-5烷基; R 2表示C 1-5亚烷基; R3表示亚甲基或亚乙基; R 4表示氢或C 1-4 - 酰基; R5表示羟基，任选取代的芳基C 2-8烷氧基，取代的C 1-4烷基氨基或具有氨基酸或肽衍生物残基的氨基; n为5〜1000的整数。 m为2〜300的整数， x为1〜300的整数。 条件是R5中羟基的比例为0-99％且x不大于m]和少量水溶性抗癌剂。

公开(公告)号：US07820759B2

公开(公告)日：2010-10-26

申请号：US12322322

申请日：2009-01-30

申请人： Kazuhisa Shimizu ,  Toshitaka Murata ,  Katsuhiko Sagawa

发明人： Kazuhisa Shimizu ,  Toshitaka Murata ,  Katsuhiko Sagawa

IPC分类号： A61K47/48

CPC分类号： A61K9/1075 ,  A61K31/337 ,  A61K47/42

摘要： A novel micellar preparation in which the solubility of a sparingly water-soluble anticancer agent has been heightened and which after intravenous administration, enables a high blood concentration to be maintained. The preparation has high medicinal activity and/or is reduced in side effects. The micellar preparation is formed from a block copolymer represented by the following general formula (1): [wherein R1 represents hydrogen or C1-5 alkyl; R2 represents C1-5 alkylene; R3 represents methylene or ethylene; R4 represents hydrogen or C1-4 acyl; R5 represents hydroxyl, optionally substituted aryl C2-8 alkoxyl, substituted C1-4 alkylamino, or amino having a residue of either an amino acid or a peptide derivative; n is an integer of 5 to 1,000; m is an integer of 2 to 300; and x is an integer of 1 to 300; provided that the proportion of hydroxy in the R5's is 0 to 99% and x is not larger than m] and a sparingly water-soluble anticancer agent.

摘要翻译： 提高了微水溶性抗癌剂的溶解性的新型胶束制剂，并且在静脉内给药后能够维持高血药浓度。 该制剂具有高药用活性和/或副作用减少。 胶束制剂由下列通式（1）表示的嵌段共聚物形成：[其中R 1表示氢或C 1-5烷基; R2表示C1-5亚烷基; R3表示亚甲基或亚乙基; R4代表氢或C1-4酰基; R5表示羟基，任选取代的芳基C2-8烷氧基，取代的C1-4烷基氨基或具有氨基酸或肽衍生物残基的氨基; n为5〜1000的整数。 m为2〜300的整数， x为1〜300的整数。 条件是R5中羟基的比例为0-99％且x不大于m]和少量水溶性抗癌剂。