Chistyakov Dmitry, Sergeev Gleb
Belozersky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, 119992 Moscow, Russia.
Department of Chemistry, M. V. Lomonosov Moscow State University, 119991 Moscow, Russia.
Pharmaceutics. 2020 Jan 1;12(1):34. doi: 10.3390/pharmaceutics12010034.
Among the significant problems of modern pharmacology are the low solubility and bioavailability of drugs. One way to resolve this problem is to obtain new polymorphic forms of drugs with improved physicochemical properties. Various approaches have been developed with this aim, including the preparation of co-crystals, the use of nanoparticles, or the use of compounds in the form of a salt. A promising direction in pharmacology concerns the production of new stable polymorphic structures. In this mini-review, we consider certain aspects of drug polymorphism, methods for the synthesis of polymorphs, and the stability, size, and transformation of crystalline polymorphs. Moreover, we summarize our results from several studies demonstrating the problems associated with the synthesis of new polymorphous modifications based on inert gases and cryotemperatures. The results indicate that the problems specific to drug polymorphisms have only been partly resolved, are of current interest, and require further development.
现代药理学的重大问题之一是药物的低溶解度和生物利用度。解决这一问题的一种方法是获得具有改善物理化学性质的药物新多晶型物。为此已开发出各种方法,包括制备共晶体、使用纳米颗粒或以盐的形式使用化合物。药理学中一个有前景的方向是生产新的稳定多晶型结构。在本综述中,我们考虑了药物多晶型的某些方面、多晶型的合成方法以及晶体多晶型的稳定性、尺寸和转变。此外,我们总结了几项研究的结果,这些研究证明了基于惰性气体和低温合成新多晶型变体所涉及的问题。结果表明,药物多晶型特有的问题仅得到部分解决,目前仍受到关注,需要进一步发展。