ALA and salt formulation
The addition of a salt to an ALA formulation that is dissolved in the mouth unexpectedly significantly reduces the degree of burning or irritation from ALA exposure during administration. This invention is particularly useful for an oral dissolved form of administration due to the extended time of ALA exposure that is possible with such formulations. The salt-inclusive formulations of the invention can increase efficacy of the ALA administration, reduce negative side effects, or both.
1 . An orally dissolvable tablet comprising (a) alpha-lipoic acid in a weight concentration of 12%-45% and (b) a physiologically acceptable salt wherein the weight concentration ratio of the salt to the alpha-lipoic acid in the tablet is in the range between 5% and 200%, wherein the tablet is non-chewable and adapted to be maintained in a recipient's mouth until fully dissolved within 10 minutes following administration.
2 . The orally dissolvable tablet of claim 1 , wherein the salt is an inorganic salt.
3 . The orally dissolvable tablet of claim 2 , wherein the salt comprises a sodium cation.
4 . The orally dissolvable tablet of claim 3 , wherein the salt is sodium chloride.
5 . The orally dissolvable tablet of claim 4 , wherein the tablet further comprises (1) one or more sugars, (2) one or more sugar substitutes, or (3) a combination of any thereof selected from dextrose, fructose, maltose, isomalt, a directly compressible co-crystallized mixture of about 3% maltodextrin and about 97% sucrose, wherein the one or more sugars, one or more sugar substitutes, or combination of any thereof makes up between about 31% and about 59% of the tablet.
6 . An orally administered and orally dissolving formulation comprising alpha-lipoic acid and a salt comprising a cation and an anion, wherein the formulation is non-chewable and is adapted to be maintained in a recipient's mouth until fully dissolved within 10 minutes following administration.
7 . The orally administered and orally dissolving formulation of claim 6 , wherein (1) the formulation is in the form of a compressed tablet, (2) the alpha-lipoic acid is non-polymerized, (3) the weight concentration of the alpha-lipoic acid in the formulation is in the range between 12% to 45%, and (4) the salt-to-alpha-lipoic acid weight concentration ratio is in the range between 5% to 200%.
8 . The orally dissolvable tablet of claim 1 , wherein the weight concentration ratio of the salt to the alpha-lipoic acid in the tablet is in the range between 20% and 200%.
9 . The orally dissolvable tablet of claim 5 , wherein the one or more sugars, one or more sugar substitutes, or combination of any thereof comprises a directly compressible co-crystallized mixture of about 3% maltodextrin and about 97% sucrose.
10 . The orally administered and orally dissolving formulation of claim 7 , wherein the weight concentration ratio of the salt to the alpha-lipoic acid in the tablet is in the range between 20% and 200%.
11 . The orally administered and orally dissolving formulation of claim 7 , wherein the weight concentration ratio of the salt to the alpha-lipoic acid in the tablet is in the range between 5% and 100%.
12 . The orally administered and orally dissolving formulation of claim 6 , wherein the salt is an inorganic salt.
13 . The orally administered and orally dissolving formulation of claim 6 , wherein the formulation further comprises (1) one or more sugars, (2) one or more sugar substitutes, or (3) a combination of any thereof selected from sucrose, dextrose, fructose, maltose, isomalt, a directly compressible co-crystallized mixture of about 3% maltodextrin and about 97% sucrose, or a combination of any thereof, and whereby the one or more sugars, one or more sugar substitutes, or combination of any thereof reduces the burning associated with the alpha-lipoic acid, increases the bioavailability of the alpha-lipoic acid, or both.
14 . An orally administered and orally dissolving formulation comprising alpha-lipoic acid and a salt comprising a cation and an anion, wherein the formulation is non-chewable and is adapted to be dissolved within 10 minutes following administration when maintained in a recipient's mouth.
15 . The orally administered and orally dissolving formulation of claim 14 , wherein the salt is an inorganic salt.
16 . The orally administered and orally dissolving formulation of claim 15 , wherein the inorganic salt is sodium chloride.
17 . The orally administered and orally dissolving formulation of claim 14 , wherein the formulation further comprises (1) one or more sugars, (2) one or more sugar substitutes, or (3) a combination of any thereof selected from sucrose, dextrose, maltose, isomalt, a directly compressible co-crystallized mixture of about 3% maltodextrin and about 97% sucrose, or a combination of any thereof wherein the one or more sugars, one or more sugar substitutes, or combination of any thereof is present in an amount of between about 31% and about 59%.
18 . The orally administered and orally dissolving formulation of claim 17 , wherein the one or more sugars, one or more sugar substitutes, or combination of any thereof comprises a directly compressible co-crystallized mixture of about 3% maltodextrin and about 97% sucrose.
19 . The orally dissolvable tablet of claim 1 , wherein the tablet further comprises sodium bicarbonate.
20 . The orally dissolvable tablet of claim 1 , wherein the tablet is adapted to be maintained in a recipient's mouth until fully dissolved within 3.5 minutes following administration.
21 . The orally administered and orally dissolving formulation of claim 6 , wherein the formulation further comprises sodium bicarbonate.
22 . The orally administered and orally dissolving formulation of claim 6 , wherein the formulation is adapted to be maintained in a recipient's mouth until fully dissolved within 3.5 minutes following administration.
23 . The orally administered and orally dissolving formulation of claim 14 , wherein the formulation further comprises sodium bicarbonate.
24 . The orally administered and orally dissolving formulation of claim 14 , wherein the formulation is adapted to be maintained in a recipient's mouth until fully dissolved within 3.5 minutes following administration.
25 . The orally dissolvable tablet of claim 1 , wherein the alpha lipoic acid and the physiologically acceptable salt are distributed in a homogeneous matrix formulation.