COMPOSITIONS AND METHODS FOR AGE RELATED EYE DISEASES COMPRISING HIGH CONCENTRATIONS OF VITAMINS

Abstract

The present disclosure describes compositions comprising a potent vitamin B complex and pharmaceutically acceptable salts of any of the foregoing. The compositions are useful in methods for treating conditions associated with a loss of visual acuity including, for example, age-related macular degeneration.

Claims

1. A composition for visual health comprising a vitamin complex comprising: vitamin B1, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing; vitamin B2, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing; vitamin B3, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing; vitamin B5, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing; vitamin B6, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing; vitamin B7, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing; vitamin B9, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing; and vitamin B12, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing.

2. The composition of claim 1, wherein the vitamin B1, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing comprises thiamin.

3. The composition of claim 1, wherein the vitamin B2, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing comprises riboflavin.

4. The composition of claim 1, wherein the vitamin B3, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing comprises nicotinic acid, niacinamide, or a combination of any of the foregoing.

5. The composition of claim 1, wherein the vitamin B5, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing comprises pantothenic acid.

6. The composition of claim 1, wherein the vitamin B6, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing comprises pyridoxine.

7. The composition of claim 1, wherein the vitamin B7, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing comprises biotin.

8. The composition of claim 1, wherein the vitamin B9, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing comprises folic acid and/or methyl tetrahydrofolate.

9. The composition of claim 1, wherein the vitamin B12, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing comprises cyanocobalamin.

10. The composition of claim 1, wherein the composition comprises 0.1 mg to 25.0 mg of thiamin or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B1.

11. The composition of claim 1, wherein the composition comprises 0.1 mg to 25.0 mg of riboflavin or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B2.

12. The composition of claim 1, wherein the composition comprises 1.0 mg to 300.0 mg of nicotinic acid and/or niacinamide or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B3.

13. The composition of claim 1, wherein the composition comprises 1.0 mg to 250.0 mg of pantothenic acid or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B5.

14. The composition of claim 1, wherein the composition comprises 25.0 mg to 200.0 mg of pyridoxine or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B6.

15. The composition of claim 1, wherein the composition comprises 0.01 mg to 1.0 mg of biotin or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B7.

16. The composition of claim 1, wherein the composition comprises 0.1 mg to 50.0 mg of folic acid and/or methyl tetrahydrofolate or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B9.

17. The composition of claim 1, wherein the composition comprises 0.25 mg to 3.0 mg of cyanocobalamin or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B12.

18. The composition of claim 1, wherein the composition comprises: 1.5 mg thiamin; 1.7 mg riboflavin; 20.0 mg nicotinic acid and/or niacinamide; 10.0 mg pantothenic acid; 50.0 mg pyridoxine; 0.03 mg biotin; 2.5 mg folic acid and/or methyl tetrahydrofolate; and 1.0 mg cyanocobalamin.

19. The composition of claim 1, wherein the composition is in the form of a tablet, capsule, soft gel, liquid, or powder.

20. The composition of claim 1, wherein the composition is in the form of an immediate release formulation or a modified release formulation.

21. The composition of claim 1, wherein at least one vitamin is from a natural source of said vitamin.

22. The composition of any one of claim 1, wherein at least one vitamin is from a synthetic source of said vitamin.

23. The composition of claim 1, wherein the composition comprises: 3.0 mg thiamin; 3.4 mg riboflavin; 40.0 mg nicotinic acid and/or niacinamide; 20 mg pantothenic acid; 50.0 mg pyridoxine; 0.06 mg biotin; 2.5 mg folic acid and/or methyl tetrahydrofolate; and 1.0 mg cyanocobalamin.

24. The composition of claim 1, wherein the composition comprises: 4.5 mg thiamin; 5.1 mg riboflavin; 60.0 mg nicotinic acid and/or niacinamide; 30.0 mg pantothenic acid; 50.0 mg pyridoxine; 0.09 mg biotin; 2.5 mg folic acid and/or methyl tetrahydrofolate; and 1.0 mg cyanocobalamin.

25. The composition of claim 1 wherein the composition is on a daily dosage basis.

26. A method of delaying the progression and/or onset of macular degeneration, the method comprising administering to a person in need thereof a composition comprising: vitamin B1, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing; vitamin B2, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing; vitamin B3, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing; vitamin B5, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing; vitamin B6, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing; vitamin B7, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing; vitamin B9, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing; and vitamin B12, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing.

27. The method of claim 26, wherein the composition comprises: 0.1 mg to 25.0 mg of thiamin or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B1; 0.1 mg to 25.0 mg of riboflavin or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B2; 1 mg to 300.0 mg of nicotinic acid and/or niacinamide or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B3; 1 mg to 250.0 mg of pantothenic acid or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B5; 25.0 mg to 200.0 mg of pyridoxine or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B6; 0.01 mg to 1.0 mg of biotin or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B7; 0.1 mg to 50.0 mg of folic acid and/or methyl tetrahydrofolate or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B9; and 0.25 to 3.0 mg of cyanocobalamin or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B12.

28. The method of claim 26, wherein the composition comprises: 1.5 mg thiamin; 1.7 mg riboflavin; 20.0 mg nicotinic acid and/or niacinamide; 10.0 mg pantothenic acid; 50.0 mg pyridoxine; 0.03 mg biotin; 2.5 mg folic acid and/or methyl tetrahydrofolate; and 1.0 mg cyanocobalamin.

29. The method of claim 26, wherein the composition comprises: 3.0 mg thiamin; 3.4 mg riboflavin; 40.0 mg nicotinic acid and/or niacinamide; 20.0 mg pantothenic acid; 50.0 mg pyridoxine; 0.06 mg biotin; 2.5 mg folic acid and/or methyl tetrahydrofolate; and 1.0 mg cyanocobalamin.

30. The method of claim 26, wherein the composition comprises: 4.5 mg thiamin; 5.1 mg riboflavin; 60.0 mg nicotinic acid and/or niacinamide; 30.0 mg pantothenic acid; 50.0 mg pyridoxine; 0.09 mg biotin; 2.5 mg folic acid and/or methyl tetrahydrofolate; and 1.0 mg cyanocobalamin.

31. A method for treating and/or preventing at least one disease, disorder, and/or condition associated with a loss of visual acuity, the method comprising administering to a subject a composition comprising: vitamin B2, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing; vitamin B3, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing; vitamin B5, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing; vitamin B6, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing; vitamin B7, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing; vitamin B9, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing; and vitamin B12, a prodrug thereof, and/or a pharmaceutically acceptable salt of any of the foregoing.

32. The method of claim 31, wherein the composition comprises: 0.1 mg to 25.0 mg of thiamin or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B1; 0.1 mg to 25.0 mg of riboflavin or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B2; 1.0 mg to 300.0 mg of nicotinic acid and/or niacinamide or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B3; 1 mg to 250.0 mg of pantothenic acid or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B5; 25.0 mg to 200.0 mg of pyridoxine or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B6; 0.01 mg to 1.0 mg of biotin or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B7; 0.1 mg to 50.0 mg of folic acid and/or methyl tetrahydrofolate or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B9; and 0.25 to 3.0 mg of cyanocobalamin or an equivalent amount of a prodrug, a pharmaceutically acceptable salt, and/or a pharmaceutically acceptable salt of a prodrug of vitamin B12.

33. The method of claim 31, wherein the composition comprises: 1.5 mg thiamin; 1.7 mg riboflavin; 20.0 mg nicotinic acid and/or niacinamide; 10.0 mg pantothenic acid; 50.0 mg pyridoxine; 0.03 mg biotin; 2.5 mg folic acid and/or methyl tetrahydrofolate; and 1.0 mg cyanocobalamin.

34. The method of claim 31, wherein the composition comprises: 3.0 mg thiamin; 3.4 mg riboflavin; 40.0 mg nicotinic acid and/or niacinamide; 20.0 mg pantothenic acid; 50.0 mg pyridoxine; 0.06 mg biotin; 2.5 mg folic acid and/or methyl tetrahydrofolate; and 1.0 mg cyanocobalamin.

35. The method of claim 31, wherein the composition comprises: 4.5 mg thiamin; 5.1 mg riboflavin; 60.0 mg nicotinic acid and/or niacinamide; 30.0 mg pantothenic acid; 50.0 mg pyridoxine; 0.09 mg biotin; 2.5 mg folic acid and/or methyl tetrahydrofolate; and 1.0 mg cyanocobalamin.

36. The method of claim 26, wherein the composition is administered daily to the subject in one, two, three, or four daily doses.

Description

PROPHETIC EXAMPLES

[0110] The following compositions can be prepared. The amounts in each composition are set forth on a daily dosage basis. Each composition can be formulated into two or more dosage units, which dosage units can be administered to a subject daily.

TABLE-US-00001 Active Ingredient Amount (mg) Vitamin B1 (Thiamin) 1.5 Vitamin B2 (Riboflavin) 1.7 Vitamin B3 (Nicotinic acid, and/or niacinamide) 20.0 Vitamin B5 (Pantothenic acid) 10.0 Vitamin B6 (Pyridoxine) 50.0 Vitamin B7 (Biotin) 0.03 Vitamin B9 (Folic acid and/or methyl tetrahydrofolate) 2.5 Vitamin B12 (Cyanocobalamin) 1.0

TABLE-US-00002 Active Ingredient Amount (mg) Vitamin B1 (Thiamin) 3.0 Vitamin B2 (Riboflavin) 3.4 Vitamin B3 (Nicotinic acid, and/or niacinamide) 40.0 Vitamin B5 (Pantothenic acid) 20.0 Vitamin B6 (Pyridoxine) 50.0 Vitamin B7 (Biotin) 0.06 Vitamin B9 (Folic acid and/or methyl tetrahydrofolate) 2.5 Vitamin B12 (Cyanocobalamin) 1.0

TABLE-US-00003 Active Ingredient Amount (mg) Vitamin B1 (Thiamin) 4.5 Vitamin B2 (Riboflavin) 5.1 Vitamin B3 (Nicotinic acid, and/or niacinamide) 60.0 Vitamin B5 (Pantothenic acid) 30.0 Vitamin B6 (Pyridoxine) 50.0 Vitamin B7 (Biotin) 0.09 Vitamin B9 (Folic acid and/or methyl tetrahydrofolate) 2.5 Vitamin B12 (Cyanocobalamin) 1.0

TABLE-US-00004 Active Ingredient Amount (mg) Vitamin B1 (Thiamin) 1.0 1.2 1.4 1.6 1.8 2.0 2.2 2.4 2.6 2.8 Vitamin B2 (Riboflavin) 1.2 1.4 1.6 1.8 2.0 2.3 2.5 2.7 3.0 3.2 Vitamin B3 (Nicotinic acid, 15.0 16.0 18.5 21.5 24.0 26.0 29.0 32.0 34.0 35.0 and/or niacinamide) Vitamin B5 (Pantothenic acid) 6.5 8.0 9.3 10.7 12.0 13.4 14.7 15.0 15.0 15.0 Vitamin B6 (Pyridoxine) 25.0 40.0 46.5 53.5 60.0 67.0 73.5 80.0 87.0 93.5 Vitamin B7 (Biotin) 0.02 0.02 0.03 0.03 0.04 0.04 0.04 0.05 0.05 0.06 Vitamin B9 (Folic acid and/or 1.5 2.0 2.3 2.7 3.0 3.0 3.0 3.0 3.0 3.0 methyl tetrahydrofolate) Vitamin B12 (Cyanocobalamin) 0.5 0.8 1.0 1.1 1.2 1.4 1.5 1.5 1.5 1.5

TABLE-US-00005 Active Ingredient Amount (mg) Vitamin B1 (Thiamin) 3.0 3.2 3.6 3.8 4.0 4.2 4.0 4.6 4.8 5.0 Vitamin B2 (Riboflavin) 3.4 3.6 4.1 4.3 4.5 4.7 4.9 5.0 5.0 5.0 Vitamin B3 (Nicotinic acid, 35.0 35.0 35.0 35.0 35.0 35.0 35.0 35.0 35.0 35.0 and/or niacinamide) Vitamin B5 (Pantothenic acid) 15.0 15.0 15.0 15.0 15.0 15.0 15.0 15.0 15.0 15.0 Vitamin B6 (Pyridoxine) 100.0 100.0 100.0 100.00 100.0 100.0 100.0 100.0 100.0 100.0 Vitamin B7 (Biotin) 0.06 0.06 0.07 0.08 0.08 0.08 0.08 0.10 0.10 0.10 Vitamin B9 (Folic acid and/or 3.0 3.0 3.0 3.0 3.0 3.0 3.0 3.0 3.0 3.0 methyl tetrahydrofolate) Vitamin B12 (Cyanocobalamin) 0.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5

[0111] A multivitamin combining the nutritional dietary ingredients listed above is prepared by including a vitamin B complex comprising vitamins B1, B2, B3, B5, B6, B7, B9, and B12.

[0112] A multivitamin combining the nutritional dietary ingredients listed above is stable for at least two years at about room temperature.