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

1 . A medicinal combination for the treatment of diabetes, combining a biguanide, as a first medicament, and an agent for transporting said biguanide, as a second medicament, said combination comprising:

(a) a therapeutically active quantity of the biguanide; and

(b) a quantity of the transporting agent, previously determined to potentiate the therapeutic activity of the biguanide.

2 . The medicinal combination as claimed in claim 1 , wherein the biguanide and the transporting agent are in an equimolar quantity.

3 . The medicinal combination as claimed in claim 1 , wherein the biguanide is metformin.

4 . The medicinal combination as claimed in claim 1 , wherein the transporting agent is a biogenic amine.

5 . The medicinal combination as claimed in claim 1 , wherein the biguanide and/or the transporting agent are in a form suitable for their controlled release respectively.

6 . The medicinal combination as claimed in claim 5 , chemically put together for the controlled release of at least biguanide, wherein said medicinal combination is an active compound of general formula

capable of restoring at least the entity A by cleavage, in vivo, of the corresponding attachment between A′ and V′, wherein:

V is a biogenic vectorization compound, of general formula X-R-Y, where:

R represents an aliphatic, cyclic or alicyclic, saturated or unsaturated hydrocarbon chain of 2 to 10 carbon atoms, which is optionally substituted with C1 to C5 alkyl groups and/or hydroxyl groups, and

X and Y are each a free acid, amine or alcohol function; and

A and C are two respectively different active principles, namely the biguanide and the transporting agent, one of which comprises a chemical function complementary to the function X, capable of reacting with the function X so as to give an ionic A′-V′ or covalent A′-V′ attachment which can be cleaved in vivo, and the other of which comprises a chemical function complementary to the function Y, capable of reacting with the function Y so as to give an ionic V′-C′ or covalent V′-C′ attachment which can be cleaved in vivo.

7 . The medicinal combination as claimed in claim 6 , wherein the V′-C′ or V′-C′ attachment can be cleaved in vivo, and said active compound is also capable of restoring the entities V and C by said cleavage in vivo.

8 . The medicinal combination as claimed in claim 7 , A being metformin, wherein the metformin is attached to the biogenic vectorization compound by salification of the terminal primary amine function of the metformin.

9 . The medicinal combination as claimed in claim 7 , wherein, when C is arginine, the arginine is attached to the biogenic vectorization compound V using an acylation reaction.

10 . The medicinal combination as claimed in claim 6 , wherein V is selected from the group consisting of oxalic, malonic, succinic, glutaric, adipic, pimelic, suberic, azelaic, sebactic, malic, isatic and phthalic acids.

11 . A method for treating diabetes, comprising administering an active compound of general formula

as claimed in claim 6 .

12 . A process for preparing an active compound as claimed in claim 6 , comprising the following steps:

(a) reaction by condensation and/or salification of the biogenic vectorization compound V with one of the active principles A or C,

(b) reaction by condensation and/or salification of the product of the reaction according to (a) with the other active principle C or A,

wherein:

the active compound is represented by formula III:

13 . A pharmaceutical composition comprising at least one active compound as claimed in claim 6 , in combination with one or more compatible and pharmaceutically acceptable vehicles, diluents, excipients or adjuvants.

14 . The pharmaceutical composition as claimed in claim 13 , which makes it possible to adjust a daily dose in humans of between approximately 0.2 g and approximately 1 g of said active compound, to one or more doses.

15 . A medicinal combination as claimed in claim 1 , wherein said combination is for treatment of type 2 diabetes.

16 . A medicinal combination as claimed in claim 1 , wherein said biguanide is an N-dimethylbiguanide.

17 . A medicinal combination as claimed in claim 4 , wherein said biogenic amine is selected from the group consisting of arginine, putrescine, cadaverine, spermidine and spermine.

18 . A medicinal combination as claimed in claim 17 , wherein said biogenic amine is L-arginine.

19 . A medicinal combination as claimed in claim 10 , wherein V is succinic acid.