Wang Chenguang, Hu Shenye, Sun Changquan Calvin
Pharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USA.
Pharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USA.
Int J Pharm. 2017 Oct 30;532(1):435-443. doi: 10.1016/j.ijpharm.2017.08.100. Epub 2017 Aug 26.
Salt formation has been extensively used to improve drug properties, including solubility, stability and mechanical properties. A sweet salt of metformin with acesulfame, prepared though an anion exchange reaction, showed superior properties over the commercial hydrochloride salt. These included both remarkable improvement of taste and significant enhancement in tabletability, which is explained by the different crystal structures and lower hardness as measured by nanoindentation. The relationship among crystal structure, mechanical properties and tabletability was rationalized through an energy framework analysis. This approach led to the successful development of an orally disintegrating tablet product containing 60% of metformin-acesulfame salt by direct compaction.
盐形成已被广泛用于改善药物性质，包括溶解性、稳定性和机械性能。通过阴离子交换反应制备的二甲双胍与乙酰磺胺酸钾的甜盐，表现出优于市售盐酸盐的性能。这些性能包括味道的显著改善和可压性的显著提高，这可以通过不同的晶体结构以及通过纳米压痕测量的较低硬度来解释。通过能量框架分析使晶体结构、机械性能和可压性之间的关系合理化。这种方法通过直接压片成功开发出了一种含有60%二甲双胍 - 乙酰磺胺酸钾盐的口腔崩解片产品。
