Crystal polymorphism in a carbamazepine derivative: oxcarbazepine.
Crystal polymorphism in a carbamazepine derivative: oxcarbazepine.
复制标题
卡马西平衍生物的晶体多态性：奥卡西平。
DOI：
10.1002/jps.21873
复制
发表时间：
2010
影响因子：
3.8
通讯作者：
Matzger,AdamJ
中科院分区：
文献类型：
--
作者：
Lutker,KatieM;Matzger,AdamJ
卡马西平（carbamazepine，一种用于治疗癫痫的抗惊厥药）的晶体多态性已经被发现了几十年，但这种现象直到最近才因其酮衍生物奥卡西平（oxcarbazepine， OCB）而引起注意。本文证明了OCB至少具有三种无水多晶型。虽然所有的形式在形态上相似，使得光学显微镜很难区分晶体修饰，但粉末x射线衍射，拉曼光谱和热显微镜显示出明显的差异。这些技术提供了一种区分三种多态的有效方法。本文首次报道了OCB的II型晶体结构，并在低温下重新确定了I型的晶体结构。值得注意的是，形式II的分子构象和晶体排列都与2007年的盲预测非常吻合。©2009 Wiley-Liss, Inc. and American Pharmacists Association [J] . pharmaceutical science, 99:794 - 803,2010
Although crystal polymorphism of carbamazepine (CBZ), an anticonvulsant used to treat epilepsy, has been known for decades, the phenomenon has only recently been noted for its keto-derivative oxcarbazepine (OCB). Here it is demonstrated that OCB possesses at least three anhydrous polymorphs. Although all forms are morphologically similar, making differentiation between crystal modifications by optical microscopy difficult, powder X-ray diffraction, Raman spectroscopy, and thermomicroscopy show distinctive differences. These techniques provide an efficient method of distinguishing between the three polymorphs. The crystal structure of form II of OCB is reported for the first time and the structure of form I has been redetermined at low temperature. Remarkably, both the molecular conformation and crystal packing of form II are in excellent agreement with the blind prediction made in 2007. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 99:794–803, 2010