METFORMIN-BASED IONIC CO-CRYSTALS

摘要

The invention relates to two novel metformin-based compounds obtained using the antidiabetic agent glimepiride as a contra-ion in one case and using the antidiabetic agent pioglitazone as a contra-ion in the other case. The resulting spectroscopy, as well as an evaluation of the physicochemical properties thereof, indicate that, in the solid state, both compounds correspond to ionic co-crystals attracted by ionic forces and interactions of the hydrogen bond type. The physicochemical properties of the ionic co-crystals have been shown to have better intrinsic dissolution rates and improved solubilities in relation to those of the precursor contra-ions; properties that can impact favourably on the bioavailability of the novel active principles. Said improved novel active principles are formulated in oral solid pharmaceutical compositions such as tablets or caplets that have advantages over existing commercial tablets. Consequently, tablets containing these novel active principles provide an improved treatment for controlling blood glucose levels in patients with type II diabetes.