溶解度
候选药物
多态性(计算机科学)
重量分析
组合化学
溶剂
化学
药物开发
药物发现
药品
材料科学
有机化学
药理学
医学
基因型
基因
生物化学
作者
Jonathan M. Miller,Benjamin M. Collman,Landon Ray Greene,David J.W. Grant,A. C. Blackburn
摘要
The thermodynamically most stable polymorph under ambient conditions is almost without exception the most desirable crystalline form for development by a pharmaceutical company. It is, therefore, beneficial to discover and to characterize this polymorph at the earliest possible stage of development. A screen for discovering the stable polymorph of a pharmaceutical compound early in the drug discovery–development process is developed and described. In this screen, a small amount of compound is suspended in a diverse group of solvents for two weeks in an effort to crystallize the most stable polymorph. The solubility of the compound in each solvent utilized in the stable polymorph screen is also simultaneously determined using a simple gravimetric method. Ritonavir and an early development candidate (Pfizer compound A) are used as model compounds to demonstrate the utility of the screen for finding the stable polymorph early in the drug discovery–development process.
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