COMPOUND AND COMPOSITION FOR USE IN THE TREATMENT OF PREMENSTRUAL SYNDROME AND/OR PREMENSTRUAL DYSPHORIC DISORDER

Abstract

This invention pertains to a compound and a composition for use in the treatment of premenstrual syndrome and/or premenstrual dysphoric disorder.

Claims

1. Compound for use in the treatment of premenstrual syndrome and/or premenstrual dysphoric disorder, the said compound being magnesium N-acetyl-taurinate.

2. Compound for use according to claim 1, the said magnesium N-acetyl-taurinate is magnesium N-acetyl-taurinate dihydrate comprising two intrinsic water molecules.

3. Compound for use according to claim 1, the said compound is in an orally administrable form, for example in the form of a tablet, pill, capsule, medication, soluble powder, oily solution, an effervescent tablet or soft capsule.

4. Compound for use according to claim 1, the said compound being administered at a rate of 1 to 2 capsules per day for adults, adolescents or children.

5. Composition for use in the treatment of premenstrual syndrome and/or premenstrual dysphoric disorder, the said composition comprising magnesium N-acetyl-taurinate.

6. Composition for use according to claim 5, characterised in that the said magnesium N-acetyl-taurinate is magnesium N-acetyl-taurinate dihydrate comprising two intrinsic water molecules.

7. Composition for use according to claim 5, in which the said magnesium N-acetyl-taurinate or the said magnesium N-acetyl-taurinate dihydrate comprising two intrinsic water molecules is present up to 40 to 60% by weight with respect to the total weight of the composition.

8. Composition for use according to claim 5, which also comprises taurine up to 10 to 15% by weight with respect to the total weight of the composition.

9. Composition for use according to claim 5, which also comprises at least an additional magnesium compound selected in the group comprising magnesium salts of amino acids, magnesium citrate, magnesium gluconate, magnesium lactate, magnesium malate, magnesium taurate, magnesium bisglycinate, magnesium glycerophosphate, magnesium threonate, magnesium pidolate, their derivatives and mixtures.

10. Composition for use according to claim 5, which also comprises magnesium up to 8 to 15% by weight with respect to the total weight of the composition.

11. Composition for use according to claim 5, also comprising at least one pharmaceutically acceptable excipient, preferably four pharmaceutically acceptable excipients, selected in the group comprising glyceryl behenate, sucrose stearate, microcrystalline cellulose, magnesium stearate, silicon dioxide, pea maltodextrin and their mixtures.

12. Composition for use according to claim 5, the said composition being in the form of a medicine or a dietary supplement or a drink.

13. Composition for use according to claim 5, the said composition is in an orally administrable form, for example in the form of a tablet, pill, capsule, medication, soluble powder, oily solution, an effervescent tablet or soft capsule.

14. Composition for use according to claim 5, the said composition being administered at a rate of 2 to 3 capsules per day.

15. A method of treating premenstrual syndrome and/or premenstrual dysphoric disorder, the method comprising administrating to a subject magnesium N-acetyl-taurinate.

16. The method according to claim 15, wherein the subject is a subject suffering from or diagnosed with premenstrual syndrome and/or premenstrual dysphoric disorder.

17. The method according to claim 15, wherein the magnesium N-acetyl-taurinate is magnesium N-acetyl-taurinate dihydrate comprising two intrinsic water molecules.

Description

[0028] Other embodiments of the compound according to the invention are indicated in the appended claims.

[0029] This invention also pertains to a composition for use in the treatment of premenstrual syndrome and/or premenstrual dysphoric disorder.

[0030] Advantageously, in a composition according to the invention, the said magnesium N-acetyl-taurinate is magnesium N-acetyl-taurinate dihydrate comprising two intrinsic water molecules.

[0031] In the context of this invention, the terms “two intrinsic water molecules” mean that the two water molecules are inherent to the magnesium N-acetyl-taurinate dihydrate, i.e. that ‘they are an integral part of the magnesium N-acetyl-taurinate dihydrate, unlike hydration water that could be absorbed or adsorbed by this compound.

[0032] Magnesium N-acetyl-taurinate dihydrate (C8H20MgN2O10S2) is a magnesium vector and magnesium analogue of taurine that has a molecular weight of 392.677 g/mol, two water molecules (H2O) being intrinsic to the magnesium N-acetyl-taurinate dihydrate molecule.

[0033] Particularly speaking, magnesium N-acetyl-taurinate dihydrate is what is produced and marketed under the ATAMg® trademark by the company Synapharm Industrial Synthesis.

[0034] The molecular weight of magnesium N-acetyl-taurinate dihydrate is 392.677 g/mol and differs from that of non-dihydrate magnesium N-acetyl-taurinate (C8H16MgN2O8S2) that is 356.656 g/mol. This form, which is not dihydrated, is mainly described in the FR2384751 document where magnesium N-acetyl-taurinate is obtained by mixing magnesia, taurine, water and acetic acid before two successive drying steps, one under vacuum at 100° C. and the other with a drying solvent, so as to obtain crystals.

[0035] It was also determined that the two intrinsic water molecules are responsible for the formation of a stable complex by establishing bonds between the two intrinsic water molecules and the magnesium present in the magnesium N-acetyl-taurinate dihydrate compound. More particularly, magnesium bonds with the Nacetyl-taurine and water through non-covalent bonds of the metal ligand coordination bonds type.

[0036] The formation of such a complex is particularly advantageous as the latter ensures increased stability of the compound: the magnesium remains fixed (trapped) to the complex.

[0037] Advantageously, the magnesium N-acetyl-taurinate or the magnesium N-acetyl-taurinate dihydrate comprising two intrinsic water molecules is present up to 40 to 60% by weight with respect to the total weight of the composition.

[0038] In a particularly advantageous form, the composition according to the invention also includes taurine up to 10 to 15% by weight with respect to the total weight of the composition.

[0039] Advantageously, the composition according to the invention also comprises at least an additional magnesium compound selected in the group comprising magnesium salts of amino acids, magnesium citrate, magnesium gluconate, magnesium lactate, magnesium malate, magnesium taurate, magnesium bisglycinate, magnesium glycerophosphate, magnesium threonate, magnesium pidolate, their derivatives and mixtures.

[0040] Preferably, according to the invention, the composition also includes magnesium up to 8 to 15% by weight with respect to the total weight of the composition.

[0041] In addition, in a particular embodiment, the composition also comprises at least one amino acid, for example threonine.

[0042] Preferably, the said at least one amino acid is glycine present up to 10 to 15% by weight with respect to the total weight of the composition.

[0043] Advantageously, the said at least one amino acid is threonine present up to 10 to 15% by weight with respect to the total weight of the composition.

[0044] In a particular form, according to the invention, the composition also comprises at least one vitamin selected in the group consisting of vitamin B1, B2, B6 and their mixtures.

[0045] Advantageously, according to the invention, the said at least one vitamin is vitamin B1 present up to 0.05 to 0.1% by weight with respect to the total weight of the composition.

[0046] Preferably, the said at least one vitamin is vitamin B2 present up to 0.05 to 0.1% by weight with respect to the total weight of the composition.

[0047] In a particularly advantageous embodiment, according to the invention, the said at least one vitamin is vitamin B6 present up to 0.05 to 0.15% by weight with respect to the total weight of the composition.

[0048] Advantageously, the composition also comprises at least one pharmaceutically acceptable excipient, preferably four pharmaceutically acceptable excipients, selected in the group comprising glyceryl behenate, sucrose stearate, microcrystalline cellulose, magnesium stearate, silicon dioxide, pea maltodextrin and their mixtures.

[0049] In a particular form, the composition according to the invention is in the form of a medicine.

[0050] Preferably, the composition according to the invention is in the form of a food supplement.

[0051] Advantageously, the composition according to the invention is in the form of a drink.

[0052] In a particularly advantageous embodiment according to the invention, the composition is in an orally administrable form, for example in the form of a tablet, pill, capsule, medication, soluble powder, oily solution, an effervescent tablet or soft capsule.

[0053] Moreover, in a particular embodiment, the composition according to the invention is administered at a rate of 2 to 3 capsules per day.

[0054] Other embodiments of the composition according to the invention are indicated in the appended claims.

[0055] This invention has been described in relation to specific embodiments, which have a purely illustrative value and should not be considered as limiting. Generally, it will be obvious to those skilled in the art that this invention is not limited to the examples illustrated and/or described above.

[0056] The use of the verbs “comprise”, “include”, “consist of”, or any other variant, as well as their conjugations, can in no way exclude the presence of elements other than those mentioned herein.

[0057] The use of the indefinite article “a”, “an”, or the definite article “the”, to introduce an element does not exclude the presence of a plurality of these elements.