Expedited development of a high dose orally disintegrating metformin tablet
Salt formation has been intensively 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.