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1.发明申请Method for preparing a polymer micelle pharmaceutical preparation containing drug for injection 审中-公开制备含有注射用药物的聚合物胶束药物制剂的方法公开(公告)号：US20060057219A1
公开(公告)日：2006-03-16
申请号：US10515388
申请日：2003-05-21
CPC分类号： A61K31/557 , A61K9/1075 , A61K31/337 , A61K31/407 , A61K31/4745 , A61K31/519 , A61K31/704 , A61K31/7048 , A61K45/06
摘要： A production method of a preparation containing drug-encapsulating polymer micelles is provided, which comprises dissolving a hydrophilic-hydrophobic block copolymer and a sparingly water-soluble drug in a volatile organic solvent, then removing the solvent, and stirring the residue with water at a temperature not higher than 30° C. to dissolve the drug-encapsulating polymer micelles into the water.
摘要翻译： 提供含有药物包封的聚合物胶束的制备方法，其包括将亲水疏水性嵌段共聚物和微溶于水的药物溶解在挥发性有机溶剂中，然后除去溶剂，并在水中搅拌残留物 温度不高于30℃，将药物包封的聚合物胶束溶解到水中。
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2.发明申请Micellar preparation containing sparingly water-soluble anticancer agent and novel block copolymer 有权含微水溶性抗癌剂和新型嵌段共聚物的胶束制剂公开(公告)号：US20090156742A1
公开(公告)日：2009-06-18
申请号：US12322322
申请日：2009-01-30
IPC分类号： C08L53/00
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。
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3.发明申请Micellar preparation containing sparingly water-soluble anticancer agent and novel block copolymer 审中-公开含微水溶性抗癌剂和新型嵌段共聚物的胶束制剂公开(公告)号：US20060099265A1
公开(公告)日：2006-05-11
申请号：US10548998
申请日：2004-03-18
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。
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4.发明申请公开(公告)号：US20120141556A1
公开(公告)日：2012-06-07
申请号：US13358025
申请日：2012-01-25
IPC分类号： A61K9/00
CPC分类号： A61K47/36 , A61K9/1075 , A61K9/127 , A61K9/19 , A61K31/337 , A61K31/343 , A61K33/24 , A61K47/10 , A61K47/26
摘要： Provided are a composition for preparing a lyophilized preparation, comprising a drug-encapsulating polymer micelle and saccharides and/or polyethylene glycol as a stabilizing agent, a lyophilized preparation and a process for producing them. The lyophilized preparation thus provided is easily restructured to an aqueous preparation using an aqueous medium.
摘要翻译： 提供一种用于制备冻干制剂的组合物，其包含药物包封的聚合物胶束和作为稳定剂的糖和/或聚乙二醇，冻干制剂及其制备方法。 由此提供的冻干制剂使用水性介质容易地重组成含水制剂。
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5.发明授权Micellar preparation containing sparingly water-soluble anticancer agent and novel block copolymer 有权含微水溶性抗癌剂和新型嵌段共聚物的胶束制剂公开(公告)号：US07820759B2
公开(公告)日：2010-10-26
申请号：US12322322
申请日：2009-01-30
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。
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