Metformin glycinate for blood glucose control

a technology of glucose control and metformin, which is applied in the field of metformin glycinate salt, can solve the problems of affecting the industrial handling of solid compositions such as tablets, capsules, and gastric disorders with prolonged us

USRE46496E1Active Publication Date: 2017-08-01LAB SILANES S A DE
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Patent Information

Authority / Receiving Office
US · United States
Patent Type
Patents(United States)
Current Assignee / Owner
Publication Date
2017-08-01

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Abstract

The present invention relates to metformin glycinate salt and pharmaceutical compositions thereof for the treatment of diabetes mellitus. The method includes administration of the metformin glycinate salt by various routes selected from oral, intravenous injectable, intramuscular injectable, nasal, intraperitoneal, or sublingual, in order to achieve a reduction in blood glucose levels. The invention further relates to the synthesis of a new 1,1-dimethylbiguanide glycinate salt, called Metformin Glycinate. The resulting salt exhibits advantages over other metformin salts. These advantages are due, in the first place, to the fact that the glycine counterion exhibits hypoglycemic effects by itself. Moreover, the salt exhibits more rapid absorption, reaching higher plasma concentrations than those produced with metformin hydrochloride.
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Description

[0001] This application is a continuation-in-part application of PCT / IB2008 / 002665 filed on Jun. 26, 2008, published under WO2009 / 144527 on Dec. 3, 2009, all of the disclosure of which is incorporated herein by reference.TECHNICAL FIELD OF THE INVENTION

[0002] This invention relates to metformin glycinate salt, which exhibits superior hypoglycemic properties, greater bioavailability a particular, safe pharmacokinetics. The invention further relates to pharmaceutical compositions of metformin glycinate salt and the use of these compositions for the treatment of diabetes mellitus and other associated diseases.TECHNICAL BACKGROUND

[0003] The class of anti-diabetic drugs called biguanides originates from the Galega officinalis plant, which has been known for several centuries for its capacity to reduce the symptoms of diabetes mellitus. Metformin is a compound derived from biguanides that primarily acts by reducing hepatic gluconeogenesis, but also reduces glucose absorption at the gastroint...

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Embodiment Construction

[0037]Below, we specify a preferred embodiment, which is not intended to limit the synthesis of the metformin glycinate salt, which was synthesized 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 favor crystallization of the saturated medium; all of 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, this precipitate is washed and purified.

[0038]The ...