Solid-state study of polymorphic drugs: carbamazepine
Solid-state study of polymorphic drugs: carbamazepine
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DOI：
10.1016/s0731-7085(00)00262-4
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发表时间：
2000-08-01
影响因子：
3.4
通讯作者：
Tommasini, S
中科院分区：
文献类型：
--
作者：
Rustichelli, C;Gamberini, G;Tommasini, S
化合物的多晶型具有不同内部晶格的固体晶相；在药物中，由于多型性和伪多晶性而导致的差异会影响生物利用度和有效的临床使用。本工作的目的是获得抗惊厥药物卡马西平的不同多态修饰，并利用典型的结构敏感分析技术，如FT-IR光谱、XRPD和DSC对其进行表征。进一步的研究还进行了热台傅里叶变换红外热显微镜，这使得在加热过程中的多形形态的可见和光谱表征。我们的结果证实了无水卡马西平存在三种不同的晶型：晶型III，商业晶型，晶型I，加热晶型III和晶型II，从乙醇溶液中结晶。在固态性质方面，在多晶型之间检测到了显著的差异。此外，热台红外热显微镜证明了它的分析潜力，以表征药物的多态。(C)2000 Elsevier Science B.V.保留所有权利。
Polymorphs of a compound have solid crystalline phases with different internal crystal lattices; in pharmaceuticals, differences due to polymorphism and pseudopolymorphism can affect bioavailability and effective clinical use. The aim of this work was to obtain the different polymorphic modifications of the anticonvulsant drug, carbamazepine, and to characterise them by means of typical structure-sensitive analytical techniques, such as FT-IR spectroscopy, XRPD and DSC. Further investigations were also performed by Hot Stage FT-IR thermomicroscopy, which permitted the visible and spectroscopic characterisation of the polymorphic forms during heating. Our results confirm the existence of three different polymorphic forms for anhydrous carbamazepine: Form III, the commercial one, Form I, obtained by heating Form III and Form II, crystallised from ethanolic solution. Substantial differences were detected among the polymorphs with regard to solid-state properties. Moreover, Hot Stage FT-IR thermomicroscopy proved its analytical potential to characterise the drug's polymorphism. (C) 2000 Elsevier Science B.V. All rights reserved.