Sun Changquan Calvin
Pfizer Global Research and Development, 7000 Portage Road, Portage, MI 49001, USA.
Int J Pharm. 2006 Aug 17;319(1-2):114-20. doi: 10.1016/j.ijpharm.2006.03.044. Epub 2006 Apr 7.
PHA-739521 is an experimental compound that exhibits polymorphism. The two anhydrous crystal forms, I and II, are characterized using powder X-ray diffractometry, thermal analyses, moisture sorption gravimetry. Both Forms I and II are non-hygroscopic and are stable to compaction pressure. The melting temperature is about 152 degrees C for Form I and 168 degrees C for Form II. Forms I and II are enantiotropically related where Form I is more stable below a transition temperature of approximately 70 degrees C. Crystallization behavior of this compound from solutions and during heating is also studied. Information obtained is used to design an appropriate crystallization process to successfully manufacture desired polymorph at large scale.
PHA - 739521是一种具有多晶型现象的实验性化合物。使用粉末X射线衍射法、热分析和吸湿重量法对两种无水晶体形式I和II进行了表征。I型和II型均不吸湿，且对压制压力稳定。I型的熔点约为152℃，II型为168℃。I型和II型是互变异构相关的，其中I型在约70℃的转变温度以下更稳定。还研究了该化合物在溶液中以及加热过程中的结晶行为。所获得的信息用于设计合适的结晶工艺，以成功大规模生产所需的多晶型物。
