Department of Physical Chemistry, A.M. Butlerov Institute of Chemistry, Kazan Federal University, 420008, Kremlevskaya, 18, Kazan, Russia.
Universitat Rostock, Institute of Physics, Albert-Einstein_str. 23-24, Rostock, DE 18051, Germany.
J Pharm Sci. 2024 May;113(5):1257-1264. doi: 10.1016/j.xphs.2023.12.001. Epub 2023 Dec 7.
Production and evaluation of the kinetic stability of the amorphous forms of active pharmaceutical ingredients are among the current challenges of modern pharmaceutical science. In the present work, amorphous forms of several sulfonamides were produced for the first time using Fast Scanning calorimetry. The parameters, characterizing the glass-forming ability of the compounds, i.e. the critical cooling rate of the melt and the kinetic fragility, were determined. The cold crystallization kinetics was studied using both isothermal and non-isothermal approaches. The results of the present study will contribute to the development of approaches for producing amorphous forms of rapidly crystallizing active pharmaceutical ingredients.
生产和评估活性药物成分无定形形式的动力稳定性是现代药物科学的当前挑战之一。在本工作中,首次使用快速扫描量热法生产了几种磺胺类药物的无定形形式。确定了表征化合物成玻璃能力的参数,即熔体的临界冷却速率和动力学脆性。使用等温和非等温方法研究了冷结晶动力学。本研究的结果将有助于开发生产快速结晶活性药物成分的无定形形式的方法。