Pharmaceutical Composition with High-Potency Sweetener

• US 20070116829A1
• Filed: 11/02/2006
• Published: 05/24/2007
• Est. Priority Date: 11/23/2005
• Status: Abandoned Application

• Current Assignee: The Coca-Cola Company
• Original Assignee: The Coca-Cola Company
• Inventors: Prakash, Indra, DuBois, Grant
• Application Number:
  US11/555,991
• Publication Number:
  US 20070116829A1
• Time in Patent Office: Days
• US Class Current: 426/548
• CPC Class Codes: A23L 27/34 Sugar alcohols
• CPC Class Codes: A23L 27/36 Terpene glycosides
• CPC Class Codes: A23L 33/15 Vitamins
• CPC Class Codes: A23V 2002/00 Food compositions, function of food ingredients or processes for food or foodstuffs
• CPC Class Codes: A23V 2250/156 Mineral combination undefined extract A23V2250/1638
• CPC Class Codes: A23V 2250/262 Stevioside
• CPC Class Codes: A23V 2250/6402 Erythritol
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• CPC Class Codes: C07H 1/08 from natural products
• CPC Class Codes: C07H 15/24 Condensed ring systems having three or more rings

Abstract

The present invention relates generally to pharmaceutical compositions comprising non-caloric or low-caloric high-potency sweeteners and methods for making and using them. In particular, the present invention relates to different pharmaceutical compositions comprising at least one non-caloric or low-caloric natural and/or synthetic high-potency sweetener, at least one sweet taste improving composition, and a pharmaceutically active substance. The present invention also relates to pharmaceutical compositions and methods that can improve the tastes of non-caloric or low-caloric natural and/or synthetic,, high-potency sweeteners by imparting a more sugar-like taste or characteristic. In particular, the pharmaceutical compositions and methods provide a more sugar-like temporal profile, including sweetness onset and sweetness linger, and/or a more sugar-like flavor profile.

Claims

1. A pharmaceutical composition comprising;

a pharmaceutically active substance;

at least one high-potency sweetener; and

at least one sweet taste improving composition.

2. The pharmaceutical composition of claim 1, wherein the at least one high-potency sweetener comprises a natural high-potency sweetener selected from the group consisting of rebaudioside A, rebaudioside B, rebaudioside C, rebaudioside D, rebaudioside E, rebaudioside F, dulcoside A, dulcoside B, rubusoside, stevia, stevioside, mogroside IV, mogroside V, Luo Han Guo sweetener, siamenoside, monatin and its salts (monatin SS, RR, RS, SR), curculin, glycyrrhizic acid and its salts, thaumatin, monellin, mabinlin, brazzein, hernandulcin, phyllodulcin, glycyphyllin, phloridzin, trilobatin, baiyunoside, osladin, polypodoside A, pterocaryoside A, pterocaryoside B, mukurozioside, phlomisoside I, periandrin I, abrsoside A, cyclocarioside I, and combinations thereof.

3. The pharmaceutical composition of claim 1, wherein the at least one high-potency sweetener comprises a synthetic high-potency sweetener selected from the group consisting of sucralose, acesulfame potassium and other salts, aspartame, alitame, saccharin, neohesperidin dihydrochalcone, cyclamate, neotame, N—

[N-[3-(3-hydroxy-4-methoxyphenyl)propyl]-L-α

-aspartyl]-L-phenylalanine 1-methyl ester, N—

[N-[3-(3-hydroxy-4-methoxyphenyl)-3-methylbutyl]-L-α

-aspartyl]-L-phenylalanine 1-methyl ester, N—

[N-[3-(3-methoxy-4-hydroxyphenyl)propyl]-L-α

-aspartyl]-L-phenylalanine 1-methyl ester, salts thereof, and combinations thereof.

4. The pharmaceutical composition of claim 1, wherein the at least one sweet taste improving composition comprises a first sweet taste improving composition selected from the group consisting of carbohydrates, polyols, amino acids and their corresponding salts, polyamino acids and their corresponding salts, sugar acids and their corresponding salts, organic acids, inorganic acids, organic salts, inorganic salts, bitter compounds, flavorants, astringent compounds, polymers, proteins or protein hydrolysates, surfactants, emulsifiers, flavonoids, alcohols, and combinations thereof.

5. The pharmaceutical composition of claim 1, wherein the at least one sweet taste improving composition imparts a more sugar-like temporal profile to the pharmaceutical composition than the sweetener would have without the at least one sweet taste improving composition.

6. The pharmaceutical composition of claim 1, further comprising at least one second sweet taste improving composition different from the at least one first sweet taste improving composition and selected from the group consisting of carbohydrates, polyols, amino acids and their corresponding salts, polyamino acids and their corresponding salts, sugar acids and their corresponding salts, organic acids, inorganic acids, organic salts, inorganic salts, bitter compounds, flavorants, astringent compounds, polymers, proteins or protein hydrolysates, surfactants, emulsifiers, flavonoids, alcohols, and combinations thereof.

7. The pharmaceutical composition of claim 6, further comprising at least one third sweet taste improving composition different from the at least one first sweet taste improving composition and the at least one second sweet taste improving composition and selected from the group consisting of carbohydrates, polyols, amino acids and their corresponding salts, polyamino acids and their corresponding salts, sugar acids and their corresponding salts, organic acids, inorganic acids, organic salts, inorganic salts, bitter compounds, flavorants, astringent compounds, polymers, proteins or protein hydrolysates, surfactants, emulsifiers, flavonoids, alcohols, and combinations thereof.

8. The pharmaceutical composition of claim 1, wherein the at least one high-potency sweetener is rebaudioside A, stevioside, stevia, or combinations thereof.

9. The pharmaceutical composition of claim 8, wherein the at least one sweet taste improving composition comprises a polyol.

10. The pharmaceutical composition of claim 9, wherein the at least one polyol comprises erythritol.

11. The pharmaceutical composition of claim 9, wherein the at least one polyol comprises xylitol.

12. The pharmaceutical composition of claim 8, wherein the at least one sweet taste improving composition comprises at least one amino acid.

13. The pharmaceutical composition of claim 12, wherein the at least one amino acid comprises glycine, alanine, proline, hydroxyproline, glutamine, or combinations thereof.

14. The pharmaceutical composition of claim 8, wherein the at least one sweet taste improving composition comprises at least one polyamino acid.

15. The pharmaceutical composition of claim 14, wherein the at least one polyamino acid comprises poly-L-aspartic acid, poly-L-α

-lysine, poly-L-ε

-lysine, poly-L-α

-ornithine, poly-ε

-ornithine, poly-L-arginine, salts thereof, or combinations thereof.

16. The pharmaceutical composition of claim 8, wherein the at least one sweet taste improving composition comprises at least one inorganic salt.

18. The pharmaceutical composition of claim 16, further comprising at least one inorganic phosphate.

19. The pharmaceutical composition of claim 18, wherein the at least one inorganic phosphate comprises a sodium, potassium, calcium, or magnesium phosphate.

20. The pharmaceutical composition of claim 16, further comprising at least one inorganic chloride.

21. The pharmaceutical composition of claim 20, wherein the at least one inorganic chloride comprises a sodium, potassium, calcium, or magnesium chloride.

22. The pharmaceutical composition of claim 8, wherein the at least one sweet taste improving composition comprises at least one carbohydrate.

23. The pharmaceutical composition of claim 22, wherein the at least one carbohydrate comprises sucrose, high fructose corn syrup, glucose, or sucrose.

24. The pharmaceutical composition of claim 23, wherein the at least one carbohydrate is present in the pharmaceutical composition in an amount from about 10,000 ppm to about 80,000 ppm of the composition.

25. The pharmaceutical composition of claim 8, wherein the at least one sweet taste improving composition comprises at least one synthetic high-potency sweetener.

26. The pharmaceutical composition of claim 25, wherein the at least one synthetic high-potency sweetener comprises sucralose, acesulfame potassium or other salts, aspartame, alitame, saccharin, neohesperidin dihydrochalcone, cyclamate, neotame, N—

[N-[3-(3-hydroxy-4-methoxyphenyl)propyl]-L-α

-aspartyl]-L-phenylalanine 1-methyl ester, N—

[N-[3-(3-hydroxy-4-methoxyphenyl)-3-methylbutyl]-L-α

-aspartyl]-L-phenylalanine 1-methyl ester, N—

[N-[3-(3-methoxy-4-hydroxyphenyl)propyl]-L-α

-aspartyl]-L-phenylalanine 1-methyl ester, salts thereof, and combinations thereof.

27. The pharmaceutical composition of claim 25, wherein the at least one synthetic high-potency sweetener comprises saccharin or acesulfame potassium or other salts.

28. The pharmaceutical composition of claim 27, wherein the at least one synthetic sweetener is present in the pharmaceutical composition in an amount from about 10 ppm to about 100 ppm of the composition.

29. The pharmaceutical composition of claim 8, wherein the rebaudioside A comprises rebaudioside A in a purity greater than about 70% rebaudioside A by weight on a dry basis.

30. The pharmaceutical composition of claim 8, wherein the rebaudioside A comprises rebaudioside A in a purity greater than about 80% rebaudioside A by weight on a dry basis.

31. The pharmaceutical composition of claim 8, wherein the rebaudioside A comprises rebaudioside A in a purity greater than about 90% rebaudioside A by weight on a dry basis.

33. The pharmaceutical composition of claim 8, wherein the rebaudioside A comprises rebaudioside A in a purity greater than about 98% rebaudioside by weight on a dry basis.

34. The pharmaceutical composition of claim 8, wherein the rebaudioside A comprises rebaudioside A in a purity greater than about 99% rebaudioside by weight on a dry basis.

35. The pharmaceutical composition of claim 1, wherein the pharmaceutically active substance comprises a substance selected from the group consisting of antacids, reflux suppressants, antiflatulents, antidopaminergics, proton pump inhibitors, cytoprotectants, prostaglandin analogues, laxatives, antispasmodics, antidiarrhoeals, bile acid sequestrants, opioids, beta-receptor blockers, calcium channel blockers, diuretics, cardiac glycosides, antiarrhythmics, nitrates, antianginals. vasoconstrictors, vasodilators, peripheral activators, ACE inhibitors, angiotensin receptor blockers, alpha blockers, anticoagulants, heparin, antiplatelet drugs, fibrinolytics, anti-hemophilic factors, baemostatic drugs, hypolipidaemic agents, statins, hynoptics, anaesthetics, antipsychotics, antidepressants, anti-emetics, anticonvulsants, antiepileptics, anxiolytics, barbiturates. movement disorder drugs, stimulants, benzodiazepines, cyclopynolones, dopamnine antagonists, antihistamines, cholinergics, anticholinergics, emetics, cannabinoids, analgesics, muscle relaxants, antibiotics, aminoglycosides, anti-virals, anti-fungals, anti-inflammatories, anti-gluacoma drugs, sympathomimetics, steroids, ceruminolytics, bronchodilators, NSAIDS, antitussive, mucolytics, decongestants, corticosteroids, androgens, antiandrogens, gonadotropins, growth hormones, insulin, antidiabetics, thyroid hormones, calcitonin, diphosponates, vasopressin analogues, alkalizing agents, quinolones, anticholinesterase, sildenafil, oral contraceptives, Hormone Replacement Therapies, bone regulators, follicle stimulating hormones, luteinizings hormones, gamolenic acid, progestogen, dopamine agonist, oestrogen, prostaglandin, gonadorelin, clomiphene, tamoxifen, diethylstilbestrol, antileprotics, antituberculous drugs, antimalarials, anthelmintics, antiprotozoal, antiserums, vaccines, interferons, tonics, vitamins, cytotoxic drugs, sex hormones, aromatase inhibitors, somatostatin inhibitors, and combinations thereof.

36. The pharmaceutical composition of claim 1, further comprises an excipient material selected from the group consisting of antiadherents, binders, coatings, disintegrants, fillers, diluents, softeners, emulsifiers, flavoring agents, coloring agents, adjuvants, lubricants, functional agents, viscosity modifiers, bulking agents, olidiants, surface active agents, osmotic agents, diluents, and combinations thereof.

37. The pharmaceutical composition of claim 1, further comprising a bulk sweetener.

38. The pharmaceutical composition of claim 1, wherein the sweet taste improving composition functions as a hulk sweetener.

17. The pharmaceutical composition of claim 163 wherein the at least one inorganic salt comprises a sodium, potassium, calcium, or magnesium salt.

32. The pharmaceutical composition of claim 87 wherein the rebaudioside A comprises rebaudioside A in a purity greater than about 97% rebaudioside by weight on a dry basis.