Department of Chemistry and Pharmaceutical Sciences, University of Ferrara, Ferrara, Italy.
Department of Life Sciences and Biotechnology, University of Ferrara, Ferrara, Italy.
Drug Discov Today. 2017 Aug;22(8):1134-1138. doi: 10.1016/j.drudis.2017.01.010. Epub 2017 Jan 24.
Poorly soluble and/or permeable molecules jeopardize the discovery and development of innovative medicines. Pharmaceutical co-crystals, formed by an active pharmaceutical substance (API) and a co-crystal former, can show enhanced dissolution and permeation values compared with those of the parent crystalline pure phases. It is currently assumed that co-crystallization with pharmaceutical excipients does not affect the pharmacological activity of an API or, indeed, might even improve physical properties such as solubility and permeability. However, as we highlight here, the biological behavior of co-crystals can differ drastically with respect to that of their parent physical mixtures.
水溶性差和/或渗透性差的分子会危及创新药物的发现和开发。药物共晶是由活性药物物质 (API) 和共晶形成剂形成的,与母体晶相纯物质相比,其溶解和渗透值可得到提高。目前认为,与药用辅料共晶化不会影响 API 的药理活性,甚至可能改善溶解度和渗透性等物理性质。然而,正如我们在这里强调的那样,共晶的生物学行为相对于其母体物理混合物可能会有很大的不同。