公开(公告)号：WO2012148252A3

公开(公告)日：2012-12-20

申请号：PCT/MX2012000043

申请日：2012-04-20

申请人： INST DE INVESTIGACION EN QUIMICA APLIC S A DE C V ,  LARA OCHOA JOSE MANUEL FRANCISCO

发明人： LARA OCHOA JOSE MANUEL FRANCISCO

IPC分类号： C07D417/12 ,  A61K31/155 ,  A61K31/4015 ,  A61K31/4439 ,  A61P3/10 ,  C07C279/26 ,  C07D207/38

CPC分类号： C07C279/26 ,  C07D207/27

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.

摘要翻译： 本发明涉及在一种情况下使用抗糖尿病剂格列美脲作为拮抗剂获得的两种新的基于二甲双胍的化合物，并且在另一种情况下使用抗糖尿病剂吡格列酮作为拮抗剂获得。 所得到的光谱以及其物理化学性质的评估表明，在固态下，两种化合物都对应于由离子力和氢键类型的相互作用所吸引的离子共晶。 已经显示离子共晶体的物理化学性质具有较好的固有溶解速率和相对于前体对映体的溶解度的改善; 这些性质可以有利地影响新型活性成分的生物利用度。 所述改进的新型活性成分配制在口服固体药物组合物例如片剂或囊片中，其具有优于现有商业片剂的优点。 因此，含有这些新型活性成分的片剂为控制II型糖尿病患者的血糖水平提供了改善的治疗。