ORAL CARE PRODUCT AND METHODS OF USE AND MANUFACTURE THEREOF

• US 20090202451A1
• Filed: 03/28/2008
• Published: 08/13/2009
• Est. Priority Date: 02/08/2008
• Status: Active Grant

• Current Assignee: Colgate-Palmolive Company
• Original Assignee: Colgate-Palmolive Company
• Inventors: Sullivan, Richard J., Robinson, Richard Scott, Subramanyam, Ravi, Kohli, Rajnish, Wu, Donghui, Simon, Eric A., Santarpia, Ralph Peter III, Prencipe, Michael, Cummins, Diane, Wang, Qin, Christopoulou, Constantina, Morgan, Andre M., DePierro, Karen J., Tambs, Gary Edward, Mello, Sarita V., Zaidel, Lynette, Barnes, Virginia Monsul, Chopra, Suman, Leite, Sergio
• Granted Patent: US 9,682,027 B2
• Time in Patent Office: Days
• US Class Current: 424/50
• 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 8/25 Silicon; Compounds thereof
• CPC Class Codes: A61K 8/44 Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
• CPC Class Codes: A61P 1/02 Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: A61Q 11/00 Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

Abstract

This invention relates to oral care compositions comprising a basic amino acid or salt thereof, and a small particle fraction: and to methods of using and of making these compositions.

Claims

1. An oral care composition comprising

a. an effective amount of a basic amino acid in free or salt form;

b. a small particle fraction comprising at least about 5% of the formulation by weight, wherein the particles of the small particle fraction have a d50 of less than about 5 μ

m.

2. A composition according to claim 1 further comprising an effective amount of a soluble fluoride salt.

3. A composition according to claim 1 wherein the basic amino acid is arginine.

4. A composition according to claim 1 wherein the basic amino acid is partially or wholly in salt form selected from arginine bicarbonate, arginine hydrochloride, arginine phosphate, and combinations thereof.

5. A composition according to claim 1 comprising arginine bicarbonate.

6. A composition according to claim 1, wherein the small particle fraction comprises precipitated calcium carbonate having d50 of about 0.5- about 4 μ

m, silica having d50 of about 1- about 4, and mixtures thereof.

7. A composition according to claim 1, having a radioactive dentin abrasion (RDA) of about 30- about 130.

8. A composition according to claim 1, having a radioactive dentin abrasion (RDA) of about 30- about 70.

9. A composition according to claim 1, comprising at least about 20% of small particles having a d50 less than about 5 μ

m.

10. A composition according to claim 1, wherein the basic amino acid is arginine bicarbonate and which further comprises sodium monofluorophosphate and precipitated calcium carbonate.

11. A composition according to claim 1, wherein the salt of a basic amino acid is arginine bicarbonate and further comprises sodium monofluorophosphate and silica.

12. A composition according to claim 1, further comprising an anionic surfactant.

13. A composition according to claim 12 wherein the anionic surfactant is sodium lauryl sulfate.

14. A composition according to claim 1 further comprising an antibacterial agent.

15. A composition according to claim 14 wherein the antibacterial agent is triclosan.

16. A composition according to claim 1 further comprising an anionic polymer.

17. A composition according to claim 16 wherein the anionic polymer is a copolymer of methyl vinyl ether and maleic anhydride.

18. The composition according to claim 1, in the form of a toothpaste further comprising one or more of water, abrasives, surfactants, foaming agents, vitamins, polymers, enzymes, humectants, thickeners antimicrobial agents, preservatives, flavorings, colorings and/or combinations thereof.

19. A method comprising applying an effective amount of the oral care composition of claim 1 to the oral cavity of a subject in need thereof, to

a. reduce or inhibit formation of dental caries,

b. reduce, repair or inhibit pre-carious lesions of the enamel.

c. reduce or inhibit demineralization and promote remineralization of the teeth,

d. reduce hypersensitivity of the teeth.

e. reduce or inhibit gingivitis,

f. promote healing of sores or cuts in the mouth,

g. reduce levels of acid producing bacteria,

h. to increase relative levels of arginolytic bacteria,

i. inhibit microbial biofilm formation in the oral cavity,

j. raise and/or maintain plaque pH at levels of at least pH 5.5 following sugar challenge,

k. reduce plaque accumulation,

l. treat, reduce, relieve or alleviate dry mouth,

m. whiten teeth.

n. reduce erosion,

o. improve systemic health,

p. immunize teeth against cariogenic bacteria;

and/or

q. clean teeth and oral cavity.

20. The method of claim 19 to reduce hypersensitivity of the teeth.

21. An oral care composition comprising a basic amino acid, in free or salt form, and an abrasive material, the abrasive material including a small particle fraction comprising at least about 5 wt % of the total composition weight, wherein the particles of the small particle fraction have a d50 of less than 5 μ

m, for use in the treatment of sensitive teeth within an oral cavity of a subject.

22. An oral care composition according to claim 21 wherein the basic amino acid is present in an amount of from 0.1 to 20 wt % of the total composition weight.

23. An oral care composition according to claim 21 wherein the basic amino acid is present in an amount of from 1 to 10 wt % of the total composition weight.

24. An oral care composition according to claim 21 wherein the basic amino acid comprises arginine.

25. An oral care composition according to claim 21 further comprising an antibacterial agent in an amount of from 0.01 to 5 wt % of the total composition weight.

26. An oral care composition according to claim 25 wherein the antibacterial agent is present in an amount of from 0.01 to 1 wt % of the total composition weight.

27. An oral care composition according to claim 21 wherein the antibacterial agent is triclosan.

28. An oral care composition according to claim 21 further comprising a soluble fluoride salt in an amount of from 0.01 to 2 wt % of the total composition weight.

29. An oral care composition according to claim 21 further comprising a source of fluoride ions in an amount to provide 50 to 25,000 ppm by weight of fluoride ions in the total composition weight.

30. An oral care composition according to claim 28 wherein the soluble fluoride salt is selected from sodium fluoride, sodium monofluoropohosphate, and mixtures thereof.

31. An oral care composition according to claim 21 further comprising an anionic surfactant in an amount of from 0.01 to 10 wt % of the total composition weight.

32. An oral care composition according to claim 31 wherein the anionic surfactant is present in an amount of from 0.3 to 4.5 wt % of the total composition weight.

33. An oral care composition according to claim 31 wherein the anionic surfactant is selected from sodium lauryl sulfate, sodium laureth sulfate, and mixtures thereof.

34. An oral care composition according to claim 21 wherein the small particle fraction comprises at least about 20 wt % of the total composition weight.

35. An oral care composition according to claim 34 wherein the abrasive material is selected from calcium carbonate, silica, and mixtures thereof.

36. An oral care composition according to claim 34 wherein the abrasive material comprises from 15 to 70 wt % of the total composition weight.

37. An oral care composition comprising a basic amino acid, in free or salt form, and a small particle fraction comprising at least about 5% of the composition by weight, wherein the particles of the small particle fraction have a d50 of less than about 5 μ

m, for enhancing dentinal occlusion within an oral cavity of a subject.

38. An oral care composition according to claim 37 wherein the basic amino acid comprises arginine and is present in an amount of from 0.1 to 20 wt % of the total composition weight.

39. An oral care composition according to claim 37 further comprising an antibacterial agent comprising triclosan in an amount of from 0.01 to 5 wt % of the total composition weight.

40. An oral care composition according to claim 37 further comprising a soluble fluoride salt in an amount of from 0.01 to 2 wt % of the total composition weight.

41. An oral care composition according to claim 37 further comprising a source of fluoride ions in an amount to provide 50 to 25,000 ppm by weight of fluoride ions in the total composition weight.

42. An oral care composition according to claim 37 further comprising an anionic surfactant in an amount of from 0.01 to 10 wt % of the total composition weight, the anionic surfactant being selected from sodium lauryl sulfate, sodium laureth sulfate, and mixtures thereof.

43. An oral care composition according to claim 37 wherein the small particle fraction comprises at least about 20 wt % of the total composition weight.

44. An oral care composition according to claim 37 wherein the abrasive material is selected from calcium carbonate, silica, and mixtures thereof.

45. An oral care composition according to claim 37 wherein the abrasive material comprises from 15 to 70 wt % of the total composition weight.

46. Use of a basic amino acid, in free or salt form, in an oral care composition comprising a small particle fraction comprising at least about 5% of the composition by weight, wherein the particles of the small particle fraction have a d50 of less than about 5 μ

m, for enhancing dentinal occlusion within an oral cavity of a subject.

47. Use according to claim 46 wherein the basic amino acid is present in an amount of from 0.1 to 20 wt % of the total composition weight.

48. Use according to claim 46 wherein the basic amino acid comprises arginine.

49. Use according to claim 46 wherein the small particle fraction comprises at least about 20 wt % of the total composition weight.

50. Use according to claim 46 the abrasive material is selected from calcium carbonate, silica, and mixtures thereof.

51. Use according to claim 46 wherein the abrasive material comprises from 15 to 70 wt % of the total composition weight.

52. Use of a basic amino acid, in free or salt form, for the manufacture of a medicament which includes a small particle fraction comprising at least about 5% of the medicament by weight, wherein the particles of the small particle fraction have a d50 of less than about 5 μ

m, for enhancing dentinal occlusion within an oral cavity of a subject.

53. A method of treating sensitive teeth within an oral cavity, the method comprising treating the oral cavity of a subject with an oral care composition comprising a basic amino acid, in free or salt form, and a small particle fraction comprising at least about 5% of the composition by weight, wherein the particles of the small particle fraction have a d50 of less than about 5 μ

m, to enhance dentinal occlusion.