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2. 发明申请

WO2009135799A3 METHOD FOR EVALUATING THE SOLUBILITY OF A CRYSTALLINE SUBSTANCE IN A POLYMER 审中-公开
标题翻译：评估聚合物中晶体物质的溶解性的方法
公开(公告)号：WO2009135799A3
公开(公告)日：2010-01-28
申请号：PCT/EP2009055233
申请日：2009-04-29
申请人： ABBOTT GMBH & CO KG , ZHANG GEOFF G Z , YU LIAN , TAO JING , SUN YE , MAEGERLEIN MARKUS
发明人： ZHANG GEOFF G Z , YU LIAN , TAO JING , SUN YE , MAEGERLEIN MARKUS
IPC分类号： G01N33/15 , G01N25/48
CPC分类号： G01N33/15 , G01N25/4866
摘要： A viable strategy to enhance the bioavailability of poorly soluble drugs is to use amorphous solids in place of the more commonly used crystalline solids in pharmaceutical formulations. However, amorphous solids are physically meta-stable and tend to revert back to their crystalline counterpart. An effective approach to stabilizing an amorphous drug against crystallization is to disperse it in a polymer matrix. The drug's solubility in the chosen polymer defines the upper limit of drug loading without any risk of crystallization. Measuring the solubility of a drug in a polymer has been a scientific and technological challenge because the high viscosity of polymers makes achieving solubility equilibrium difficult and because pharmaceutically important drug/polymer dispersions are glasses, which undergo structural relaxation over time. The invention provides a method based on Differential Scanning Calorimetry (DSC) for measuring the solubility of crystalline drugs in polymeric matrices. The method relies on the detection of the dissolution endpoint of a drug/polymer mixture prepared by cryomilling.
摘要翻译：提高难溶性药物的生物利用度的可行策略是使用无定形固体代替药物制剂中更常用的结晶固体。然而，无定形固体物理上是元稳定的，并且倾向于回复到它们的结晶对应物。稳定无定形药物抗结晶的有效方法是将其分散在聚合物基质中。药物在所选聚合物中的溶解度限定了药物负载的上限，而没有结晶的风险。测量药物在聚合物中的溶解度已经是科学和技术挑战，因为聚合物的高粘度使得难以实现溶解度平衡，并且因为药物重要的药物/聚合物分散体是随时间经历结构松弛的玻璃。本发明提供了一种基于差示扫描量热法（DSC）测量结晶药物在聚合物基质中的溶解度的方法。该方法依赖于通过冷冻法制备的药物/聚合物混合物的溶解终点的检测。

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