Essentially sodium-free effervescent solid pharmaceutical compositions
Essentially sodium-free effervescent solid pharmaceutical compositions The present invention relates to an effervescent solid pharmaceutical composition, which is essentially free of sodium content, comprising: a therapeutically effective amount of an active pharmaceutical ingredient; one or more pharmaceutically acceptable alkaline earth metal carbonates or hydrogencarbonates in an amount from 1 to 31% by weight of the composition; and one or more pharmaceutically acceptable acids, pharmaceutically acceptable acid salts, or alternatively, a mixture thereof, in an amount from 2 to 62% by weight of the composition; together with one or more pharmaceutically acceptable excipients or carriers; wherein, the total content of the ion sodium in the effervescent solid pharmaceutical composition is equal to or lower than 1 mmol. It also relates to processes for its preparation and its use in therapy.
1 . An effervescent solid pharmaceutical composition comprising:
an active pharmaceutical ingredient, wherein the active pharmaceutical ingredient is lacosamide;
one or more of a pharmaceutically acceptable alkaline earth metal carbonate or hydrocarbonate thereof in an amount in a range from 1 to 31% by weight of the composition, wherein the one or more of the pharmaceutically acceptable alkaline earth metal carbonate or hydrocarbonate thereof comprise calcium carbonate or magnesium carbonate;
one or more of a pharmaceutically acceptable acid, a salt thereof, or a mixture thereof, in an amount in a range from 2 to 62% by weight of the composition, wherein the one or more of the pharmaceutically acceptable acid, the salt thereof, or the mixture thereof is at least one material selected from the group consisting of citric acid, malic acid, glycine hydrochloride, fumaric acid, tartaric acid, and glutamic acid; and
one or more of a pharmaceutically acceptable excipient or a pharmaceutically acceptable carrier,
wherein a total content of an ion sodium in the effervescent solid pharmaceutical composition is equal to or lower than 1 mmol,
wherein a molar ratio between the one or more of the pharmaceutically acceptable acid, the salt thereof, or the mixture thereof, and the one or more of the pharmaceutically acceptable alkaline earth metal carbonate or hydrocarbonate thereof, is in a range from 1.05:1 to 1.07:1, and
wherein the effervescent solid pharmaceutical composition is provided in a tablet formulation.
2 . The effervescent solid pharmaceutical composition according to claim 1 ,
wherein a disintegration time of the tablet formulation is equal to or less than 5 minutes, when the disintegration time is measured using a disintegration test of effervescent tablets established in the European Pharmacopoeia (Ph. Eur.), which comprises placing a tablet in a 250 mL beaker containing 200 mL of water R at 15-25° C., leaving numerous bubbles of a gas to evolve, and measuring a time when an evolution of the gas around the tablet or fragments thereof ceases and the tablet has disintegrated, being either dissolved or dispersed in the water so that no agglomerates remain.
3 . The effervescent solid pharmaceutical composition according to claim 1 , wherein the composition is free of sodium.
4 . The effervescent solid pharmaceutical composition according to claim 1 , wherein the active pharmaceutical ingredient is in a range from 0.5% to 60% by weight of the composition.
5 . The effervescent solid pharmaceutical composition according to claim 1 ,
wherein the amount of the one or more of the pharmaceutically acceptable alkaline earth metal carbonate or hydrocarbonate thereof is in a range from 2 to 28% by weight of the composition, and the amount of the one or more of the pharmaceutically acceptable acid, the salt thereof, or the mixture thereof is in a range from 4 to 56% by weight of the composition.
6 . The effervescent solid pharmaceutical composition according to claim 1 , wherein the one or more of the pharmaceutically acceptable acid, the salt thereof, or the mixture thereof comprises citric acid; and the one or more of the pharmaceutically acceptable alkaline earth metal carbonate or hydrocarbonate thereof comprises calcium carbonate.
7 . The effervescent solid pharmaceutical composition according to claim 1 , wherein a content of an alkaline earth metal is equal to or lower than 300 mg.
8 . The effervescent solid pharmaceutical composition according to claim 1 , wherein a content of calcium is equal to or lower than 180 mg, and a content of magnesium is equal to or lower than 50 mg.
9 . An effervescent solid pharmaceutical composition as defined in claim 1 , wherein the composition comprises the active pharmaceutical ingredient in an amount effective for treating a chronic disease; wherein the chronic disease is at least one disease selected from the group consisting of epilepsy; thromboembolic disorders; psychotic disorders; neurodegenerative disorders; allergic disorders; and chronic pain.
10 . The effervescent solid pharmaceutical composition according to claim 1 , wherein the lacosamide is present in an amount in a range from 2.5 to 10% by weight of the composition.