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2. 发明申请

US20050201974A1 Bioadhesive polymers with catechol functionality 审中-公开
标题翻译：具有儿茶酚功能的生物粘合剂聚合物
公开(公告)号：US20050201974A1
公开(公告)日：2005-09-15
申请号：US11009327
申请日：2004-12-09
申请人： Marcus Schestopol , Jules Jacob , Ryan Donnelly , Thomas Ricketts , Avinash Nangia , Edith Mathiowitz , Ze'ev Shaked
发明人： Marcus Schestopol , Jules Jacob , Ryan Donnelly , Thomas Ricketts , Avinash Nangia , Edith Mathiowitz , Ze'ev Shaked
IPC分类号： A61K9/00 , A61K9/20 , A61K31/74 , C08F8/32 , C08G63/91 , C09J135/00 , C09J167/00 , C09J167/04 , C09J201/06
CPC分类号： C08F8/32 , A61K9/0004 , A61K9/006 , A61K9/0065 , A61K9/204 , A61K9/2077 , A61K9/2081 , A61K9/2086 , C08G63/91 , C08G63/912 , C09J167/00 , C09J167/04 , C08F222/06
摘要： Polymers with improved bioadhesive properties and methods for improving bioadhesion of polymers have been developed. A compound containing an aromatic group which contains one or more hydroxyl groups is grafted onto a polymer or coupled to individual monomers. In one embodiment, the polymer is a biodegradable polymer. In another embodiment, the monomers may be polymerized to form any type of polymer, including biodegradable and non-biodegradable polymers. In some embodiments, the polymer is a hydrophobic polymer. In the preferred embodiment, the aromatic compound is catechol or a derivative thereof and the polymer contains reactive functional groups. In the most preferred embodiment, the polymer is a polyanhydride and the aromatic compound is the catechol derivative, DOPA. These materials display bioadhesive properties superior to conventional bioadhesives used in therapeutic and diagnostic applications. These bioadhesive materials can be used to fabricate new drug delivery or diagnostic systems with increased residence time at tissue surfaces, and consequently increase the bioavailability of a drug or a diagnostic agent. In a preferred embodiment, the bioadhesive material is a coating on a controlled release oral dosage formulation and/or forms a matrix in an oral dosage formulation.
摘要翻译：已经开发了具有改进的生物粘附性质的聚合物和改善聚合物生物粘附的方法。含有含有一个或多个羟基的芳族基团的化合物被接枝到聚合物上或与单独的单体偶联。在一个实施方案中，聚合物是可生物降解的聚合物。在另一个实施方案中，单体可以聚合以形成任何类型的聚合物，包括可生物降解和不可生物降解的聚合物。在一些实施方案中，聚合物是疏水性聚合物。在优选的实施方案中，芳族化合物是儿茶酚或其衍生物，并且聚合物含有反应性官能团。在最优选的实施方案中，聚合物是聚酐，芳族化合物是邻苯二酚衍生物DOPA。这些材料显示出比用于治疗和诊断应用的常规生物粘合剂优越的生物粘附性。这些生物粘附材料可用于制造具有增加的组织表面停留时间的新药物递送或诊断系统，并因此提高药物或诊断剂的生物利用度。在优选的实施方案中，生物粘附材料是在控释口服剂量制剂上的涂层和/或在口服剂量制剂中形成基质。

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