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    • 126. 发明授权
    • Pure polyanhydride from dicarboxylic acid and coupling agent
    • 来自二羧酸和偶联剂的纯聚酐
    • US4916204A
    • 1990-04-10
    • US80332
    • 1987-07-31
    • Abraham J. DombRobert S. LangerEyal RonSteven GiannosRohit KothariEdith Mathiowitz
    • Abraham J. DombRobert S. LangerEyal RonSteven GiannosRohit KothariEdith Mathiowitz
    • A61K31/335A61K31/365A61K31/39C08G67/04C08G69/08C08G69/10
    • A61K31/335A61K31/365A61K31/39C08G67/04C08G69/08C08G69/10Y10S514/863
    • A method for synthesizing polyanhydrides in solution using coupling agents and a removable acid acceptor to effect a one-step polymerization of dicarboxylic acids. As used in the method, these coupling agents include phosgene, diphosgene, and acid chlorides. Insoluble acid acceptors include insoluble polyamines and crosslinked polyamines such as polyethyleneimine and polyvinylpyridine and inorganic bases such as K.sub.2 CO.sub.3, Na.sub.2 CO.sub.3, NaHCO.sub.3, and CaCO.sub.3. The only byproduct formed is a removable hydrochloric acid-acid acceptor.Examples are provided of the polymerization of highly pure polyanhydrides using phosgene, diphosgene or an acid chloride as the coupling agent, in combination with either an insoluble acid acceptor or a soluble acid acceptor in a solvent wherein the polymerization byproduct or polymer is insoluble.A particularly important application of these polyanhydrides is in the formation of drug delivery devices containing bioactive compounds. The method is also useful in the polymerization of dicarboxylic acids including heat liable dipeptides of glutamic or aspartic acid.
    • 使用偶联剂和可除去的酸受体在溶液中合成聚酐以进行二羧酸的一步聚合的方法。 如该方法所用,这些偶联剂包括光气,双光气和酰氯。 不溶性酸受体包括不溶性多胺和交联聚胺如聚乙烯亚胺和聚乙烯吡啶以及无机碱如K 2 CO 3,Na 2 CO 3,NaHCO 3和CaCO 3。 形成的唯一副产物是可除去的盐酸酸受体。 提供了使用光气,双极光或酰氯作为偶联剂的高纯度聚酐与在溶剂中的不溶性酸受体或可溶性酸受体组合的聚合反应,其中聚合副产物或聚合物是不溶的。 这些多酸酐的特别重要的应用是形成含有生物活性化合物的药物递送装置。 该方法也可用于二羧酸的聚合,包括谷氨酸或天冬氨酸的热应答二肽。