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Medicinal association of a biguanine and a carrier, for example metformin and arginine

a biguanine and carrier technology, applied in the field of medicine combination, can solve the problem of low bioavailability

Inactive Publication Date: 2007-11-15
INOPHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention relates to a medicinal set for the treatment of diabetes, particularly type 2 diabetes, which includes a biguanide and a transporting agent. The biguanide is metformin, which is currently used in the treatment of diabetes but has side effects and bioavailability issues. The invention proposes the use of an amine or polyamine with a structure similar to metformin, such as L-arginine, as a transporter for metformin, which can increase its bioavailability and improve its therapeutic effects. The invention also provides a method for cleaving the attachment between the biguanide and the transporting agent in vivo. The medicinal set has been found to be effective in treating diabetes in animal models.

Problems solved by technology

This low bioavailability explains the bothersome side effect of metformin, namely diarrhea.

Method used

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  • Medicinal association of a biguanine and a carrier, for example metformin and arginine
  • Medicinal association of a biguanine and a carrier, for example metformin and arginine
  • Medicinal association of a biguanine and a carrier, for example metformin and arginine

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Embodiment Construction

[0044] The expression “biguanide” is understood to mean in particular N-dimethylbiguanides, substituted or otherwise, and for example metformin, but also other pharmaceutical compounds, for example buformin or fenformin.

[0045] Preferably, the biguanide is metformin.

[0046] The expression “simultaneous administration” is intended to mean the administration, in a single dose, of the two active principles, it being understood that the simultaneous administration allows the release, in the organism, of the two active principles simultaneously or in sequence.

[0047] The term “biogenic” is intended to mean a chemical compound which is of natural or unnatural origin and / or is metabolizable and / or is biodegradable and / or is atoxic with respect to the human or the animal, at a physiological dose.

[0048] The term “transporter” is intended to mean a molecule or substance which allows the transfer of another molecule across a barrier, either by forming an attachment, or without forming an atta...

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Abstract

A medicinal combination for the treatment of diabetes, in particular of type 2 diabetes, combining a biguanide, in particular an N-dimethylbiguanide, as a first medicament, and an agent for transporting the said biguanide, as a second medicament, said combination comprising: e [sic] a therapeutically active quantity of the biguanide f [sic] and a quantity of transporting agent, previously determined to potentiate the therapeutic activity of the biguanide according to (a).

Description

[0001] This is a Divisional of application Ser. No. 10 / 465,997, filed Oct. 3, 2003, which in turn is a National Stage Application of PCT / FR01 / 04235, filed Dec. 31, 2001, which in turn claims the benefit of French Patent Application No. 00 / 17332, filed Dec. 29, 2000. The entire disclosure of the prior applications is hereby incorporated by reference herein in their entirety.FIELD OF THE INVENTION [0002] The present invention relates to a medicinal combination of two active principles, having, jointly, a complementary and / or synergistic action, this being for the treatment of diabetes, in particular of type 2 diabetes. [0003] The expression “complementary action” is intended to mean the pharmacological action of two different compounds making it possible to act on the same pathology via two respectively different pharmacological mechanisms, for example the combined use of two antidiabetic agents, such as a biguanide and a sulfonylurea. [0004] The expression “synergistic action” is int...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/155A61K31/195A61K47/48A61P3/10A61P5/00A61P9/00C07C279/22C07C279/26
CPCA61K31/155A61K31/195A61K47/48023A61K2300/00A61K47/54A61P3/10A61P5/00A61P9/00
Inventor RAPIN, JEAN-ROBERTHALBITTE, DOMINIQUE
Owner INOPHARM
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