公开(公告)号：US06471955B1

公开(公告)日：2002-10-29

申请号：US09050042

申请日：1998-03-30

申请人： Samuel J. Tremont ,  Denis Forster ,  Ricky L. Fenton ,  Yinong Ma

发明人： Samuel J. Tremont ,  Denis Forster ,  Ricky L. Fenton ,  Yinong Ma

IPC分类号： A61K3175

CPC分类号： A61K31/5575 ,  A61K47/58 ,  A61K47/6927 ,  Y10S514/926 ,  Y10S514/927

摘要： This invention provides a method of preparing a polymeric delivery system for active ingredients having enhanced site specific release performance characteristics. The delivery system is formed either by attaching the active ingredient to a linker through an acid-sensitive covalent bond, then forming a covalent bond between the linker and a portion of the subunits of a crosslinked polystyrene polymer, or by attaching a linker to a portion of the subunits of a crosslinked polystyrene polymer, then attaching the active ingredient to the polymer-linker combination through an acid-sensitive covalent bond. The invention also provides a delivery system comprising an active ingredient covalently bonded through an acid-sensitive covalent bond to a linker, which is in turn covalently bonded to a portion of subunits of a crosslinked polystyrene polymer. The invention further provides a method for treatment or prevention of gastric ulcers using a delivery system capable of delivering prostaglandin or prostacyclin drugs, especially misoprostol.

摘要翻译： 本发明提供了制备具有增强的位点特异性释放性能特征的活性成分的聚合物递送系统的方法。 递送系统通过将活性成分通过酸敏感共价键连接到接头上，然后在接头与交联聚苯乙烯聚合物的一部分亚单位之间形成共价键，或通过将接头连接到部分 的交联聚苯乙烯聚合物的亚基，然后通过酸敏感共价键将活性成分连接到聚合物 - 连接体组合。 本发明还提供了一种递送系统，其包含通过酸敏感共价键共价结合至接头的活性成分，其接触共价键合到交联聚苯乙烯聚合物的一部分亚单位。 本发明还提供了使用能够递送前列腺素或前列环素药物，特别是米索前列醇的递送系统来治疗或预防胃溃疡的方法。