Chewable tablet containing lysine

• US 20030138484A1
• Filed: 09/25/2002
• Published: 07/24/2003
• Est. Priority Date: 10/23/2001
• Status: Active Grant

• Current Assignee: Pharmaton S.A. (C.H. Boehringer Sohn AG & Co. KG)
• Original Assignee: Boehringer Ingelheim International GmbH (C.H. Boehringer Sohn AG & Co. KG)
• Inventors: David Marocchi, Michael, Cappellini, Claudia, Gianesello, Valter
• Granted Patent: US 7,070,804 B2
• Time in Patent Office: Days
• US Class Current: 424/465
• CPC Class Codes: A23L 33/15 Vitamins
• CPC Class Codes: A23L 33/175 Amino acids
• CPC Class Codes: A23V 2002/00 Food compositions, function of food ingredients or processes for food or foodstuffs
• CPC Class Codes: A23V 2250/063 Lysine
• CPC Class Codes: A23V 2250/1578 Calcium
• CPC Class Codes: A23V 2250/1588 Copper
• CPC Class Codes: A23V 2250/1592 Iron
• CPC Class Codes: A23V 2250/161 Magnesium
• CPC Class Codes: A23V 2250/1642 Zinc
• CPC Class Codes: A23V 2250/70 Vitamins
• CPC Class Codes: A23V 2250/702 Vitamin A
• CPC Class Codes: A23V 2250/704 Vitamin B
• CPC Class Codes: A23V 2250/708 Vitamin C
• CPC Class Codes: A23V 2250/7106 Vitamin D3
• CPC Class Codes: A23V 2250/712 Vitamin E
• CPC Class Codes: A23V 2250/718 Vitamin PP
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/07 Retinol compounds, e.g. vitamin A retinoic acids A61K31/203
• CPC Class Codes: A61K 31/198 Alpha-amino acids, e.g. alanine or edetic acid [EDTA] betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00
• CPC Class Codes: A61K 31/355 Tocopherols, e.g. vitamin E
• CPC Class Codes: A61K 31/375 : Ascorbic acid, i.e. vitamin C; Salts thereof
• CPC Class Codes: A61K 31/4415 : Pyridoxine, i.e. Vitamin B6 pyridoxal phosphate A61K31/675
• CPC Class Codes: A61K 31/51 : Thiamines, e.g. vitamin B1
• CPC Class Codes: A61K 31/525 : Isoalloxazines, e.g. riboflavins, vitamin B2
• CPC Class Codes: A61K 31/593 : 9,10-Secocholestane derivatives, e.g. cholecalciferol, i.e. vitamin D3

Abstract

A tablet with enhanced compliance by humans, in particular children and/or juveniles, comprising:

(a) a vitamin;

(b) lysine or a pharmaceutically acceptable salt thereof;

(c) a sweetener; and

(d) a pharmaceutically or dietetically acceptable carrier.

Claims

1. A tablet comprising:

(a) a vitamin;

(b) lysine or a pharmaceutically acceptable salt thereof;

(c) a sweetener; and

(d) a pharmaceutically or dietetically acceptable carrier.

2. The tablet according to claim 1, further comprising a mineral.

3. The tablet according to claim 1, further comprising a flavoring agent capable of masking the flavor of lysine.

4. The tablet according to claim 2, further comprising a flavoring agent capable of masking the flavor of lysine.

5. The tablet according to claim 1, wherein the vitamin is selected from the group consisting of:

β

-carotene, vitamin A palmitate, vitamin B₁ nitrate, vitamin B₂, vitamin B₆ hydrochloride, vitamin B₁₂, vitamin C, vitamin D₃, vitamin E acetate, folic acid, vitamin H, and vitamin PP.

6. The tablet according to claim 2, wherein the vitamin is selected from the group consisting of:

β

-carotene, vitamin A palmitate, vitamin B₁ nitrate, vitamin B₂, vitamin B₆ hydrochloride, vitamin B₁₂, vitamin C, vitamin D₃, vitamin E acetate, folic acid, vitamin H, and vitamin PP.

7. The tablet according to claim 3, wherein the vitamin is selected from the group consisting of:

β

-carotene, vitamin A palmitate, vitamin B₁ nitrate, vitamin B₂, vitamin B₆ hydrochloride, vitamin B₁₂, vitamin C, vitamin D₃, vitamin E acetate, folic acid, vitamin H, and vitamin PP.

8. The tablet according to claim 4, wherein the vitamin is selected from the group consisting of:

β

-carotene, vitamin A palmitate, vitamin B₁ nitrate, vitamin B₂, vitamin B₆ hydrochloride, vitamin B₁₂, vitamin C, vitamin D₃, vitamin E acetate, folic acid, vitamin H, and vitamin PP.

9. The tablet according to claim 1, wherein the vitamin is a mixture of vitamins consisting essentially of:

0.4 mg to 0.8 mg of β

-carotene, 500 IU to 1500 IU of vitamin A palmitate, 0.3 mg to 1.0 mg of vitamin B₁ nitrate, 0.3 mg to 1.0 mg of vitamin B₂, 0.3 mg to 1.0 mg of vitamin B₆ hydrochloride, 0.4 μ

g to 1.0 μ

g of vitamin B₁₂, 15 mg to 40 mg of vitamin C, 100 IU to 300 IU of vitamin D₃, 3.0 mg to 9.5 mg of vitamin E acetate, 20 μ

g to 80 fig of folic acid, 10 μ

g to 25 μ

g of vitamin H, and 4 mg to 10 mg of vitamin PP per unit dosage.

10. The tablet according to claim 2, wherein the vitamin is a mixture of vitamins consisting essentially of:

0.4 mg to 0.8 mg of β

-carotene, 500 IU to 1500 IU of vitamin A palmitate, 0.3 mg to 1.0 mg of vitamin B₁ nitrate, 0.3 mg to 1.0 mg of vitamin B₂, 0.3 mg to 1.0 mg of vitamin B₆ hydrochloride, 0.4 μ

g to 1.0 μ

g of vitamin B₁₂, 15 mg to 40 mg of vitamin C, 100 IU to 300 IU of vitamin D₃, 3.0 mg to 9.5 mg of vitamin E acetate, 20 μ

g to 80 μ

g of folic acid, 10 μ

g to 25 μ

g of vitamin H, and 4 mg to 10 mg of vitamin PP per unit dosage.

11. The tablet according to claim 3, wherein the vitamin is a mixture of vitamins consisting essentially of:

0.4 mg to 0.8 mg of β

-carotene, 500 IU to 1500 IU of vitamin A palmitate, 0.3 mg to 1.0 mg of vitamin B₁ nitrate, 0.3 mg to 1.0 mg of vitamin B₂, 0.3 mg to 1.0 mg of vitamin B₆ hydrochloride, 0.4 μ

g to 1.0 μ

g of vitamin B₁₂, 15 mg to 40 mg of vitamin C, 100 IU to 300 IU of vitamin D₃, 3.0 mg to 9.5 mg of vitamin E acetate, 20 μ

g to 80 μ

g of folic acid, 10 μ

g to 25 μ

g of vitamin H, and 4 mg to 10 mg of vitamin PP per unit dosage.

12. The tablet according to claim 4, wherein the vitamin is a mixture of vitamins consisting essentially of:

0.4 mg to 0.8 mg of β

-carotene, 500 IU to 1500 IU of vitamin A palmitate, 0.3 mg to 1.0 mg of vitamin B₁ nitrate, 0.3 mg to 1.0 mg of vitamin B₂, 0.3 mg to 1.0 mg of vitamin B₆ hydrochloride, 0.4 μ

g to 1.0 μ

g of vitamin B₁₂, 15 mg to 40 mg of vitamin C, 100 IU to 300 IU of vitamin D₃, 3.0 mg to 9.5 mg of vitamin E acetate, 20 μ

g to 80 μ

g of folic acid, 10 μ

g to 25 μ

g of vitamin H, and 4 mg to 10 mg of vitamin PP per unit dosage.

13. The tablet according to claim 2, wherein the mineral is selected from the group consisting of:

manganese (II) gluconate, copper (II) carbonate, calcium phosphate, ferrous (II) fumarate, zinc oxide, and magnesium oxide.

14. The tablet according to claim 4, wherein the mineral is selected from the group consisting of:

manganese (II) gluconate, copper (II) carbonate, calcium phosphate, ferrous (II) fumarate, zinc oxide, and magnesium oxide.

15. The tablet according to claim 6, wherein the mineral is selected from the group consisting of:

manganese (II) gluconate, copper (II) carbonate, calcium phosphate, ferrous (II) fumarate, zinc oxide, and magnesium oxide.

16. The tablet according to claim 8, wherein the mineral is selected from the group consisting of:

manganese (II) gluconate, copper (II) carbonate, calcium phosphate, ferrous (II) fumarate, zinc oxide, and magnesium oxide.

17. The tablet according to claim 10, wherein the mineral is selected from the group consisting of:

manganese (II) gluconate, copper (II) carbonate, calcium phosphate, ferrous (II) fumarate, zinc oxide, and magnesium oxide.

18. The tablet according to claim 12, wherein the mineral is selected from the group consisting of:

manganese (II) gluconate, copper (II) carbonate, calcium phosphate, ferrous (II) fumarate, zinc oxide, and magnesium oxide.

19. The tablet according to claim 2, wherein the mineral is a mixture of minerals consisting essentially of:

0.2 mg to 0.8 mg of copper (II) carbonate, 150 mg to 300 mg of dicalcium phosphate anhydrous, 8.0 mg to 20 mg of ferrous (II) fumarate, 4 mg to 9 mg of zinc oxide, and 12 mg to 28 mg of magnesium oxide.

20. The tablet according to claim 4, wherein the mineral is a mixture of minerals consisting essentially of:

0.2 mg to 0.8 mg of copper (II) carbonate, 150 mg to 300 mg of dicalcium phosphate anhydrous, 8.0 mg to 20 mg of ferrous (II) fumarate, 4 mg to 9 mg of zinc oxide, and 12 mg to 28 mg of magnesium oxide.

21. The tablet according to claim 6, wherein the mineral is a mixture of minerals consisting essentially of:

0.2 mg to 0.8 mg of copper (II) carbonate, 150 mg to 300 mg of dicalcium phosphate anhydrous, 8.0 mg to 20 mg of ferrous (II) fumarate, 4 mg to 9 mg of zinc oxide, and 12 mg to 28 mg of magnesium oxide.

22. The tablet according to claim 8, wherein the mineral is a mixture of minerals consisting essentially of:

0.2 mg to 0.8 mg of copper (II) carbonate, 150 mg to 300 mg of dicalcium phosphate anhydrous, 8.0 mg to 20 mg of ferrous (II) fumarate, 4 mg to 9 mg of zinc oxide, and 12 mg to 28 mg of magnesium oxide.

23. The tablet according to claim 10, wherein the mineral is a mixture of minerals consisting essentially of:

0.2 mg to 0.8 mg of copper (II) carbonate, 150 mg to 300 mg of dicalcium phosphate anhydrous, 8.0 mg to 20 mg of ferrous (II) fumarate, 4 mg to 9 mg of zinc oxide, and 12 mg to 28 mg of magnesium oxide.

24. The tablet according to claim 12, wherein the mineral is a mixture of minerals consisting essentially of:

0.2 mg to 0.8 mg of copper (II) carbonate, 150 mg to 300 mg of dicalcium phosphate anhydrous, 8.0 mg to 20 mg of ferrous (II) fumarate, 4 mg to 9 mg of zinc oxide, and 12 mg to 28 mg of magnesium oxide.

25. The tablet according to claim 1, wherein lysine or a pharmaceutically acceptable salt thereof comprises (L)-lysine monohydrochloride.

26. The tablet according to one of claims 2 to 24, wherein lysine or a pharmaceutically acceptable salt thereof comprises (L)-lysine monohydrochloride.

27. The tablet according to one of claims 1 to 24, wherein lysine or a pharmaceutically acceptable salt thereof consists essentially of 10 mg to 100 mg of (L)-lysine monohydrochloride.

28. The tablet according to claim 1, wherein the sweetener is selected from the group consisting of:

calcium saccharinate, ammonium cyclamate, ammonium glycirhizinate, aspartame, glucose, and glucitols.

29. The tablet according to claim 25, wherein the sweetener is selected from the group consisting of:

calcium saccharinate, ammonium cyclamate, ammonium glycirhizinate, aspartame, glucose, and glucitols.

30. The tablet according to claim 3, wherein the flavoring agent is selected from the group consisting of:

natural citrus or orange flavor.

31. The tablet according to claim 4, wherein the flavoring agent is selected from the group consisting of:

natural citrus or orange flavor.

32. The tablet according to claim 3, wherein:

the sweetener consists essentially of 1.0 mg to 10.0 mg of aspartame, 5.0 mg to 50.0 mg of glucose syrup, and 200 mg to 800 mg of sorbitol, and the flavoring agent comprises 5.0 mg to 50.0 mg of natural orange flavor.

33. The tablet according to claim 4, wherein:

the sweetener consists essentially of 1.0 mg to 10.0 mg of aspartame, 5.0 mg to 50.0 mg of glucose syrup, and 200 mg to 800 mg of sorbitol, and the flavoring agent comprises 5.0 mg to 50.0 mg of natural orange flavor.

34. The tablet according to claim 1, wherein a pharmaceutically or dietetically acceptable carrier is selected from the group consisting of:

diluents, excipients, sticking agents, buffering agents, bulk agents, lubricating agents, and colorants.

35. A tablet comprising:

(a) a mixture of vitamins consisting essentially of;

0.4 mg to 0.8 mg of β

-carotene, 500 IU to 1500 IU of vitamin A palmitate, 0.3 mg to 1.0 mg of vitamin B₁ nitrate, 0.3 mg to 1.0 mg of vitamin B₂, 0.3 mg to 1.0 mg of vitamin B₆ hydrochloride, 0.4 μ

g to 1.0 μ

g of vitamin B₁₂, 15 mg to 40 mg of vitamin C, 100 IU to 300 IU of vitamin D₃, 3.0 mg to 9.5 mg of vitamin E acetate, 20 μ

g to 80 μ

g of folic acid, 10 μ

g to 25 μ

g of vitamin H, and 4 mg to 10 mg of vitamin PP,

(b) a mixture of minerals consisting essentially of 0.2 mg to 0.8 mg of copper (II) carbonate, 150 mg to 300 mg of dicalcium phosphate anhydrous, 8.0 mg to 20 mg of ferrous (II) fumarate, 4 mg to 9 mg of zinc oxide and 12 mg to 28 mg of magnesium oxide,

(c) 10 mg to 100 mg of (L)-lysine monohydrochloride per unit dosage,

(d) a mixture of sweeteners and flavoring agents comprising;

1.0 mg to 10.0 mg of aspartame, 5.0 mg to 50.0 mg of glucose syrup, 200 mg to 800 mg of sorbitol, and 5.0 mg to 50.0 mg of natural orange flavor;

(e) a pharmaceutically or dietetically acceptable carrier,

wherein the tablet weighs 500 mg to 2000 mg.

36. A method of improving the physiological state of a human comprising administering orally to the human an effective amount of a tablet which can be chewed or sucked comprising:

(a) a vitamin;

(b) lysine or a pharmaceutically acceptable salt thereof;

(c) a sweetener; and

(d) a pharmaceutically or dietetically acceptable carrier.

37. The method according to claim 36, wherein the tablet further comprises a mineral.

38. The method according to claim 36, wherein the tablet further comprises a flavoring agent capable of masking the flavor of lysine.

39. The method according to claim 37, wherein the tablet further comprises a flavoring agent capable of masking the flavor of lysine.

40. A method of improving the development and growth of a child or juvenile comprising administering orally to the child or juvenile an effective amount of a tablet which can be chewed or sucked comprising:

(a) a vitamin;

(b) lysine or a pharmaceutically acceptable salt thereof;

(c) a sweetener; and

(d) a pharmaceutically or dietetically acceptable carrier.

41. The method according to claim 40, wherein the tablet further comprises a mineral.

42. The method according to claim 40, wherein the tablet further comprises a flavoring agent capable of masking the flavor of lysine.

43. The method according to claim 41, wherein the tablet further comprises a flavoring agent capable of masking the flavor of lysine.