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A NEW METFORMIN GLYCINATE SALT FOR BLOOD GLUCOSE CONTROL
专利权人:
发明人:
申请号:
EP08807218.6
公开号:
EP2303838B1
申请日:
2008.06.26
申请国别(地区):
EP
年份:
2013
代理人:
摘要:
In this invention, a new 1,1 -dimethylbiguanide Glycinate salt was synthesised, called metformin Glycinate. This salt exhibits advantages over other metformin salts. These advantages are due, in the first place, to the fact that the glycine counterion exhibits hypoglycaemic effects by itself. Moreover, this salt exhibits more rapid absorption, reaching higher plasma concentrations than those produced with metformin hydrochloride. The synthesis was synthesised from the Metformin Hydrochloride salt, where free Metformin was produced by releasing the hydrochloride counterion, using an ion-exchange column for this purpose the metformin base released was dissolved in an aqueous medium and, subsequently, glycine was added at ambient temperature under constant stirring subsequently, the resulting product is heated until a concentrated solution is produced, an organic solvent is added which does not react with the components present and wherein glycine is insoluble in order to create insolubility in the medium and favour crystallisation of the saturated medium all this in order to precipitate the excess glycine and then separate it by filtering the filtrate was concentrated again until precipitation of the metformin glycinate salt was achieved.Dans cette invention, un nouveau sel de 1,1 -diméthylbiguanide glycinate a été synthétisé, appelé metformine glycinate. Ledit sel présente des avantages sur dautres sels de metformine. Lesdits avantages sont dûs, en premier lieu, au fait que le contre-ion de glycine présente lui-même des effets hypoglycémiques. De plus, ledit sel présente une absorption plus rapide, atteignant des concentrations plasmatiques supérieures à celles produites avec du chlorhydrate de metformine. La synthèse est obtenue à partir du sel de chlorhydrate de metformine, la metformine libre étant produite par libération du contre-ion de chlorhydrate, à laide dune colonne échangeuse dions prévue à cet effet la metformine base libérée est dissoute dans un milieu a
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