申请人:Pharmacia Corporation
公开号:US06471955B1
公开(公告)日:2002-10-29
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.
本发明提供了一种制备聚合物释放系统的方法,该系统具有增强的特定部位释放性能特征。该释放系统通过将活性成分通过酸敏感的共价键连接到连接物上,然后在交联聚苯乙烯聚合物的部分亚基上形成共价键,或通过将连接物连接到交联聚苯乙烯聚合物的部分亚基上,然后通过酸敏感的共价键将活性成分连接到聚合物-连接物组合上形成。本发明还提供了一种释放系统,该系统包括通过酸敏感的共价键共价键连接到连接物上的活性成分,连接物再与交联聚苯乙烯聚合物的部分亚基共价键连接。本发明还提供了一种使用能够释放前列腺素或前列环素药物的释放系统,特别是米索前列醇,用于治疗或预防胃溃疡的方法。