Department of Pharmacy, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark.
Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH-4123 Allschwil, Switzerland.
Int J Pharm. 2017 Apr 15;521(1-2):232-238. doi: 10.1016/j.ijpharm.2017.02.042. Epub 2017 Feb 21.
The glass forming ability (GFA), i.e. the ease of amorphization of drugs, is mostly investigated using the critical cooling rate upon melt quenching to generate an amorphous product via the thermodynamic pathway. However, amorphous materials can also be prepared via the kinetic pathway by milling. In this case, the time required to generate an amorphous product is called the minimal milling time. This study investigates the correlation of the GFA between these two pathways. Eighteen compounds were chosen and their GFA was investigated by determining the critical cooling rate and the minimal milling time. It was observed that drugs, which turned amorphous upon cooling from the melt at slow cooling rates also had a low minimal milling time and vice versa. It was found that the GFA of the studied set of drugs was inherent and independent of the preparation method. It can be concluded that a drug with low critical cooling rate will also have a low minimal milling time and is thus a good glass former.
玻璃形成能力（GFA），即药物非晶化的容易程度，主要通过熔体淬火时的临界冷却速率来研究，以通过热力学途径生成非晶产物。然而，通过研磨也可以通过动力学途径制备非晶材料。在这种情况下，生成非晶产物所需的时间称为最小研磨时间。本研究调查了这两种途径之间的 GFA 相关性。选择了十八种化合物，并通过确定临界冷却速率和最小研磨时间来研究它们的 GFA。结果表明，在缓慢冷却速率下从熔体冷却时变为非晶态的药物也具有低的最小研磨时间，反之亦然。研究发现，所研究的药物集的 GFA 是固有且独立于制备方法的。可以得出结论，具有低临界冷却速率的药物也将具有低的最小研磨时间，因此是良好的玻璃形成剂。
