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    • 2. 发明申请
    • Temperature and Ph Sensitive Block Copolymer and Polymeric Hydrogels Using the Same
    • 温度和Ph敏感嵌段共聚物和聚合物水凝胶使用它
    • US20080293827A1
    • 2008-11-27
    • US11815960
    • 2006-03-31
    • Doo Sung LeeMin Sang KimJe Sun YouHuynh Dai PhuBong Sup KimMinh Khanh Nguyen
    • Doo Sung LeeMin Sang KimJe Sun YouHuynh Dai PhuBong Sup KimMinh Khanh Nguyen
    • A61K47/32C08L71/00C08G65/08
    • C08G65/33306C08G65/331C08G65/3322C08G65/3324C08G73/028C08G81/00C08L53/00C08L67/00C08L71/02C08L2203/02C08L2205/05C08L2666/02C08L2666/18
    • Disclosed is a block copolymer formed by coupling the following components with each other: (a) a copolymer (A) of a polyethylene glycol (PEG) type compound with a biodegradable polymer; and (b) at least one oligomer (B) selected from the group consisting of poly(β-amino ester) and poly(amido amine). A method for preparing the same block copolymer, and a polymeric hydrogel type drug composition comprising the temperature and pH-sensitive block copolymer and a physiologically active substance that can be encapsulated with the block copolymer are also disclosed. The multiblock copolymer is obtained by copolymerization of a pH-sensitive poly(β-amino ester) and/or poly(amido amine) type oligomer, a hydrophilic and temperature-sensitive polyethylene glycol type compound and a hydrophobic and biodegradable polymer. Therefore, the block copolymer can form a polymeric hydrogel structure due to its amphiphilicity resulting from the combination of a hydrophilic group and a hydrophobic group in the copolymer and ionization characteristics depending on pH variations, and thus can be used as a drug carrier for target-directed drug delivery depending on pH variations in the body.
    • 公开了通过将以下组分彼此偶联而形成的嵌段共聚物:(a)聚乙二醇(PEG)型化合物与可生物降解聚合物的共聚物(A) 和(b)至少一种选自聚(β-氨基酯)和聚(酰氨基胺)的低聚物(B)。 还公开了制备相同嵌段共聚物的方法和包含温度和pH敏感性嵌段共聚物的聚合物水凝胶型药物组合物和可以用嵌段共聚物包封的生理活性物质。 多嵌段共聚物通过pH敏感的聚(β-氨基酯)和/或聚(酰氨基胺)型低聚物,亲水和温度敏感的聚乙二醇型化合物和疏水和可生物降解的聚合物共聚获得。 因此,嵌段共聚物由于其在共聚物中的亲水基团和疏水基团的组合引起的两亲性而形成聚合物水凝胶结构,并且根据pH变化而具有电离特性,因此可以用作靶向的药物载体, 定向药物递送取决于体内的pH变化。
    • 6. 发明授权
    • Temperature and pH-sensitive block copolymer having excellent gel strength
    • 具有优异凝胶强度的温度和pH敏感性嵌段共聚物
    • US08586087B2
    • 2013-11-19
    • US12061322
    • 2008-04-02
    • Doo Sung LeeKasala DayanandaBong Sup Kim
    • Doo Sung LeeKasala DayanandaBong Sup Kim
    • A61K9/00
    • A61K9/0024A61K47/34C08G18/3293C08G18/4277C08G18/428C08G18/73C08G2210/00C08G2230/00
    • An amphiphilic pentablock copolymer that is temperature- and pH-sensitive and has superior and sustained gel strength, includes (a) a hydrophilic triblock copolymer that is temperature-sensitive and that is a copolymer of a poly(ethylene glycol)-based compound and a biodegradable polymer that is one or more polymer selected from the group consisting of polylactide, polyglycolide, polycaprolactone, poly(caprolactone-lactide) random copolymer, poly(caprolactone-glycolide) random copolymer, poly(lactide-glycolide) random copolymer, and mixtures thereof; coupled with (b) a polyurethane-based oligomer (PU) that is pH sensitive and that includes a diisocyanate compound represented by a Formula as follows: OCN—(CH2)n—NCO, where n is an integer of 4 to 10, polymerized with a diol compound having a tertiary amine on a main chain thereof that is one or more of 1,3-bis{1-(2-hydroxyethyl) -4-pyridyl}propane and 1,4-bis(2-hydroxyethyl)piperazine, and is represented by Formulae as follows: where R and R′ are alkyl groups of 1 to 8 carbon atoms, respectively.
    • 具有温度和pH敏感性并具有优异和持续的凝胶强度的两亲性五嵌段共聚物包括(a)温度敏感的亲水性三嵌段共聚物,并且是聚(乙二醇)基化合物和 一种或多种选自聚丙交酯,聚乙交酯,聚己内酯,聚(己内酯 - 丙交酯)无规共聚物,聚(己内酯 - 乙交酯)无规共聚物,聚(丙交酯 - 乙交酯)无规共聚物及其混合物的聚合物的生物可降解聚合物 ; 与(b)pH敏感的聚氨酯类低聚物(PU)结合,并且包括由下式表示的二异氰酸酯化合物:OCN-(CH 2)n -NCO,其中n为4至10的整数,聚合 与主链上具有叔胺的二醇化合物是1,3-双{1-(2-羟乙基)-4-吡啶基}丙烷和1,4-双(2-羟乙基)哌嗪中的一种或多种 并且由式如下表示:其中R和R'分别为1-8个碳原子的烷基。