Folate salts
AssigneeAprofol AG
InventorsMartin Ulmann, Gerd Wiesler, Arthur Bodenmüller, Markus Müller
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Abstract
The invention relates to crystalline folate salts. The salt consists of a folate anion and an organic cation. The folate anion is 5-methyl-(6S)-tetrahydrofolic acid, and the cation is an organic compound which is an alkanolamine selected from the group consisting of choline, N-methylaminoethanol, 2-amino-2-methylpropanol and 2-dimethylaminoethanol.
Claims15
-12. (canceled)
A crystalline folate salt comprising a tetrahydrofolic acid anion and an organic cation wherein the anion is 5-methyl-(6S)-tetrahydrofolic acid, and the cation is an organic compound wherein the organic compound is an alkanolamine selected from the group consisting of choline, 2-dimethylaminoethanol, N-methylaminoethanol, and 2-amino-2-methylpropanol.
The crystalline folate salt according to claim 1, wherein the folate salts have a solubility of higher than 2 weight-% (w/w) based on a total weight of a solution at 20° C. in organic solvents.
The crystalline folate salt according to claim 1, wherein the organic compound is di-choline.
The crystalline folate salt according to claim 1, wherein the organic compound is mono-2-dimethylaminoethanol.
The crystalline folate salt according to claim 1, wherein the organic compound is di 2-dimethylaminoethanol.
The crystalline folate salt according to claim 1, wherein the organic compound is di-N-methylaminoethanol.
The crystalline folate salt according to claim 1, wherein the organic compound is di-2-amino-2-methylpropanol.
The crystalline folate acid salt according to claim 1, wherein the tetrahydrofolic acid anion is 5-methyl-(6S)-tetrahydrofolic acid and the organic cation is di-choline.
The crystalline folate acid salt according to claim 1, wherein the tetrahydrofolic acid anion is 5-methyl-(6S)-tetrahydrofolic acid and the organic cation is mono-2-dimethylaminoethanol.
A pharmaceutical composition, comprising at least one folate salt according to claim 1, as a main active compound and at least a pharmaceutically acceptable excipient.
A food additive, a medicament, or a nutritional supplement comprising the crystalline folate salt according to claim 1, for use as a medicament, a food additive or a nutritional supplement, for the prevention and/or treatment of either deficiencies or disorders that are positively affected by the administration of tetrahydrofolic acid salt.
A method for preparing the crystalline folate salt according to claim 1, comprising crystallizing a folate salt comprising a tetrahydrofolic acid anion and an organic cation from an organic solvent comprising water in a range of 0.2 weight-% to 12 weight-% based on a weight of the organic solvent comprising the water.
A method of treating deficiencies or disorders that are positively affected by the administration of a tetrahydrofolic acid salt, comprising administering the crystalline folate salt according to claim 1 to a patient in need thereof.
A method of preventing deficiencies or disorders that are positively affected by the administration of a tetrahydrofolic acid salt, comprising administering the crystalline folate salt according to claim 1 to a patient in need thereof.
Dependencies are inferred from the claim text.