Aqueous caffeine dosage forms

• US 5,900,416 A
• Filed: 02/01/1996
• Issued: 05/04/1999
• Est. Priority Date: 02/01/1996
• Status: Expired due to Term

• Current Assignee: Anthea Enterprises Incorporated
• Original Assignee: Anthea Enterprises Incorporated
• Inventors: Markson, Stephen A.
• Primary Examiner(s): Cook, Rebecca
• Application Number:
  US08/595,366
• Time in Patent Office: 1,188 Days
• Field of Search: 514/264
• US Class Current: 424/728
• 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 31/44 Non condensed pyridines; Hydrogenated derivatives thereof
• CPC Class Codes: A61K 31/52 Purines, e.g. adenine
• CPC Class Codes: A61K 31/522 having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• CPC Class Codes: A61K 47/22 Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones

Abstract

Aqueous caffeine solutions containing a co-solubilizing agent selected from niacinamide, nicotinic acid and mixtures thereof present at a level up to the maximum concentration soluble in water and in a weight ratio to caffeine less than 1.50:1, wherein the caffeine is present up to the maximum level between about 2 and about 20 percent by weight that is water-soluble in combination with the co-solubilizing agent and the solution is buffered to a pH less than about 6. Methods for preparing the aqueous caffeine solutions of the present invention are also disclosed.

Claims

1. A caffeine oral dosage form comprising:

an aqueous solution of between

about 2 and about 20 percent by weight of caffeine;

niacinamide present in a weight ratio to said caffeine of between about 0.25;

1 and about 1.50;

1;

a buffering agent present in an amount effective to buffer said solution to a pH of between about 4 and about 6; and

an amount of an artificial sweetener effective to mask the taste of the caffeine.

2. The caffeine oral dosage form of claim 1, which is buffered to a pH less than about 5.

3. The caffeine oral dosage form of claim 2, which is buffered to a pH of about 4.3.

4. The caffeine oral dosage form of claim 1, wherein said buffering agent is an acidulent selected from the group consisting of citric acid, ascorbic acid and hydrochloric acid.

5. The caffeine oral dosage form of claim 1, wherein said buffering agent is an alkalizing agent selected from the group consisting of sodium hydroxide, sodium bicarbonate, potassium hydroxide and potassium bicarbonate.

6. The caffeine solution of claim 1, further comprising one or more essential vitamins other than niacinamide or nicotinic acid at a level soluble in said aqueous solution up to an amount effective to provide the minimum Recommended Daily Allowance of said vitamin in a 4.0 mL quantity of said aqueous solution.

7. The caffeine oral dosage form of claim 6, wherein said vitamin is selected from the group consisting of ascorbic acid, folic acid, an A vitamin, a D vitamin, an E vitamin, pyridoxine and thiamine.

8. The caffeine oral dosage form of claim 1, further comprising an effective amount of an analgesic, topical anesthetic anti-allergen or stimulant capable of being effectively absorbed through the skin or mucus membrane.

9. The caffeine oral dosage form of claim 8, comprising an analgesic selected from the group consisting of acetyl salicylic acid, acetaminophen, ibuprofen, ketoprofen and menthol.

10. The caffeine oral dosage form of claim 8, comprising a topical anesthetic selected from the group consisting of procaine, lidocaine, benzocaine, holocaine and dibucaine or an acid addition salt thereof.

11. The caffeine oral dosage form of claim 8, comprising an anti-allergen or stimulant selected from the group consisting of ginseng, epinephrine, ephedrine, pseudoephedrine, norephedrine and norepinephrine or an acid addition salt thereof.

12. The caffeine oral dosage form of claim 1, wherein said artificial sweetener is aspartame at an amount of between about 0.10 and about 1.0 percent by weight.

13. The caffeine oral dosage form of claim 1 further comprises one or more natural or artificial flavoring agents selected of the group consisting of vanillin, wintergreen, peppermint oil, orange oil, lemon oil, licorice, sassafras, natural and artificial cherry flavor, natural vanilla extract, ethylene vanillin, coffee extract, chocolate extract, artificial chocolate flavoring and cocoa extract.

28. The oral dosage form of claim 1, wherein said artificial sweetener is selected from the group consisting of saccharine, cyclamate, acesulfame K, aspartame and alatame.

14. A caffeine oral dosage form comprising, an aqueous solution of between about 2 and about 20 percent by weight of caffeine;

nicotinic acid present in a weight ratio to said caffeine between about 0.25;

1 and about 1.50;

1;

an alkaline buffering agent in an amount effective to both buffer said solution to a pH of between about 4 and about 6 and to facilitate taste marking; and

an artificial sweetener effective to mask the taste of the caffeine.

15. The oral dosage form of claim 14, which is buffered to a pH less than about 5.

16. The oral dosage form of claim 15, which is buffered to a pH of about 4.3.

17. The oral dosage form of claim 14, wherein said nicotinic acid is present at a level up to about 1.67 percent by weight and said caffeine is present at a level up to about 2.30 percent by weight.

18. The oral dosage form of claim 14, wherein said alkaline buffering agent is selected from the group consisting of sodium hydroxide, sodium bicarbonate, potassium hydroxide and potassium bicarbonate.

19. The oral dosage form of claim 14, further comprising one or more essential vitamins at a level soluble in said aqueous solution up to about an amount effective to provide the minimum Recommended Daily Allowance of said vitamin in a 4.0 mL quantity of said aqueous solution.

20. The oral dosage form of claim 19, wherein said vitamin is selected from the group consisting of ascorbic acid, folic acid, and A vitamin, a D vitamin, an E vitamin, pyridoxine and thiamine.

21. The oral dosage form of claim 19, further comprising an effective amount of an analgesic, topical anesthetic, anti-allergen or stimulant capable of being effective absorbed through the skin or mucous membrane.

22. The oral dosage form of claim 21, comprising an analgesic selected from the group consisting of acetyl salicylic acid, acetaminophen, ibuprofen, ketoprofen and menthol.

23. The oral dosage form of claim 21, comprising a topical anesthetic selected from the group consisting of procaine, lidocaine, benzocaine, holocaine and dibucaine or an acid addition salt thereof.

24. The oral dosage form of claim 21, comprising an anti-allergen or stimulant selected from the group consisting of ginseng, epinephrine, ephedrine, pseudoephedrine, norephedrine and norepinephrine, or the acid addition salt thereof.

25. The oral dosage form of claim 14, wherein said artificial sweetener is selected from the group consisting of saccharine, cyclamate, acesulfame K, aspartame and alatame.

26. The oral dosage form of claim 25, wherein said artificial sweetener is aspartame at a level of between about 0.10 and about 1.0 percent by weight.

27. The caffeine solution of claim 14, further comprising one or more natural or artificial flavoring agents selected from the group consisting of vanillin, wintergreen peppermint oil, orange oil, lemon oil, licorice, sassafras, natural and artificial cherry flavor, natural vanilla extract, ethylene vanillin, coffee extract, chocolate extract, artificial chocolate flavoring and cocoa extract.