Composition for oral cavity care, containing arginine and calcium carbonate

FIELD: chemistry.

SUBSTANCE: composition of preparation for teeth cleaning contains effective quantity of arginine in free form or in form of salt; abrasive substance, containing (i) natural sodium carbonate (NSC) with the average size of particles 3-7 mcm and moisture absorption 12-25 g/100 g and (ii) precipitated calcium carbonate (PCC) with the average particle size 1-5 mcm and water absorption higher than 25 g/100 g. Ratio of natural calcium carbonate to precipitated calcium carbonate constitutes from 1:2 to 1:3. Composition has pellicle cleaning ratio (PCR), at least, 70 and value of abrasivity of isotope-labelled dentin (RDA) lower than 140. Method of oral cavity care includes application of effective quantity of said composition in oral cavity of individual requiring it.

EFFECT: effective teeth cleaning and strengthening without injuring abrasive action, which makes it possible to apply it, in particular, for individuals with increased teeth sensitivity.

13 cl, 2 tbl, 2 ex

 

The technical field to which the invention relates

The present invention relates to compositions for caring for the oral cavity, containing the basic amino acid or its salt together with improved abrasive system based on the calcium carbonate containing natural calcium carbonate and precipitated calcium carbonate, and to methods of application and receipt of such compositions.

Background of the invention

Arginine and other basic amino acids have been proposed for use in the care of the oral cavity, and believe they have significant advantages in the fight against the formation of caries cavities and tooth sensitivity. Commercially available toothpaste on the basis of arginine, for example, such as toothpaste ProClude® or toothpaste DenClude®, contains arginine bicarbonate and precipitated calcium carbonate, but does not contain fluoride. I believe that the carbonate ion has charismaticism properties, and believe that calcium forms a complex with arginine, providing a protective effect.

Natural calcium carbonate (e.g. chalk or limestone) typically has a clearly defined crystal structure (providing that it is very hard). Typically, during production it is necessary to mill. Abrasive substances based on natural calcium carbonate provides good� teeth cleaning and stain removal, but they are also highly abrasive, so products based on natural calcium carbonate is considered as undesirable for individuals with sensitive teeth. Precipitated calcium carbonate is more refined and less abrasive, resulting in less pronounced damaging abrasion of the enamel, which is favorable for sensitive teeth, but, as a rule, it also provides less effective cleansing.

Thus, there is a need for a consistent product to care for the oral cavity, containing the basic amino acid and which have a beneficial effect minerals such as fluoride and calcium, which, in addition, contains provides effective cleansing optimized abrasive system without damaging abrasive ability, particularly for individuals with sensitive teeth.

Brief description of the invention

Now unexpectedly discovered that the combination of natural calcium carbonate and abrasive substances on the basis of vysokobarnogo precipitated calcium carbonate together with basic amino acid such as arginine, provide highly effective means for cleaning teeth, particularly for individuals with sensitive teeth.

Thus, the invention relates to compositions for caring for the oral cavity and JV�the event of their use, which are effective in suppressing or reducing the accumulation of plaque, lowering the levels of acid producing (cariogenic) bacteria, remineralizing teeth, suppression or reduction of gingivitis and reducing hypersensitivity of the teeth. The invention also relates to compositions and methods for cleaning the oral cavity and relates to improved methods of maintaining a healthy state of the oral cavity and/or General health, including the health of the cardiovascular system, for example, by reducing the total probability of infection through the tissues of the mouth.

Thus, the invention relates to compositions for caring for the oral cavity (the composition of the invention), for example, the dentifrice containing:

(a) an effective amount of basic amino acid in free form or in salt form, for example arginine bicarbonate;

(b) abrasive substance containing:

(c) natural calcium carbonate (NCC) with an average particle size of 3-7 μm, for example approximately 5.5 micrometers, and a moisture absorption 12-25 g/100 g, for example approximately 18 g/100 g; and

(d) precipitated calcium carbonate (PCC) with an average particle size of 1-5 micrometers, for example 2-3 micrometer, for example approximately 2.4 microns and water absorption of more than 25 g/100 g;

(e) an effective amount of a fluoride source, such as RA�do Sol fluorine, for example sodium monofluorophosphate.

The composition is effective for cleaning and strengthening the teeth without damaging abrasion, for example, individuals with sensitive teeth, for example, has a good ratio of plaque purification, for example at least 70, and low abrasion value isotopically labeled dentin, for example less than 140.

In some embodiments, the composition further comprises an anionic surfactant, such as sodium lauryl sulfate; an anionic polymer such as a copolymer of methyl vinyl ether and maleic anhydride; and/or antibacterial agent, such as triclosan.

In specific embodiments, the compositions according to the invention are in the form of tools for cleaning teeth, containing additional ingredients selected from one or more of water, abrasives, surfactants, foaming agents, vitamins, polymers, enzymes, humectants, thickeners, antimicrobial agents, preservatives, flavorings, colorings and/or combinations thereof.

Without intending to be bound by a particular theory, it is believed that the presence of small particles in the compositions of the arginine and calcium may contribute to the filling of microtubules, leading to hypersensitivity of the teeth, and helps vosstanovleniya damage the enamel and dentin.

In addition, it was discovered that the combination of fluoride and a basic amino acid such as arginine, in a product to care for the oral cavity in accordance with specific variants of implementation of the present invention provides an unexpected additional favorable action and qualitatively different from what can be observed using compositions comprising effective amounts of any compounds separately, in the maintenance of remineralization, restoration precariously damage and enhancing healthy state of the oral cavity. In addition, it was found that this effect can be further strengthened by the addition of fine abrasives that contains a combination of natural calcium carbonate and precipitated calcium carbonate, which may contribute to the filling of microfissure enamel and dentin microtubules.

Also unexpectedly discovered that the presence of basic amino acids reduces the adhesion of bacteria to the tooth surface, in particular when the basic amino acid is provided in combination with the anionic surface-active substance. The combination of the basic amino acids and anionic surfactants and/or anionic polymer, for example, PVM/MA also increases the delivery of antimicrobial agents, in particular triclosan.

Thus, the invention additional�but relates to methods (i) reducing or inhibiting the formation of dental caries, (ii) reduce, repair or suppression precariously damage to the enamel, e.g., as diagnosed by quantitative secondarywindow fluorescence (QLF) or the definition of caries from the electric resistance (ECM), (iii) a decrease or inhibition of demineralization and activation remineralization of the teeth, (iv) reduce hypersensitivity of the teeth, (v) reduction or suppression of gingivitis, (vi) promote healing of wounds or cuts in the mouth, (vii) lower levels of acid producing bacteria, (viii) to increase relative levels alginolyticus bacteria, (ix) inhibit the formation of microbial biofilms in the oral cavity, (x) raise and/or maintain the pH of dental plaque at levels of at least pH around 5.5 after exercise sugar, (xi) reduce plaque accumulation, (xii) reduce dry mouth, (xiii) reduce erosion, (xiv) whiten teeth, (xv) immunize or protect the teeth against cariogenic bacteria, (xvi) cleaning of the teeth and oral cavity and/or (xvii) improvement in the overall health, including the health of the cardiovascular system, for example, by reducing the total probability of infection through the tissues of the mouth, comprising applying the composition according to the invention in the oral cavity, for example the use of the compositions according to the invention in the oral cavity in need of an individual.

GI�training description

As used throughout, ranges are used as a shorthand for describing each and every part of the range values. Any value in the range can be selected as the final value of the range. In addition, all cited in the present description reference is fully included, therefore, by reference. In case of discrepancies in the description in the present description and the description of the cited references present description shall take precedence. In addition, the compositions and methods may include, essentially consist of or consist of the elements described in the present description.

Unless otherwise indicated, all percentages and quantities specified in the present description and in the description, should be understood as referring to mass percent. Given the amount determined in the calculation of the active mass of the substance. The enumeration of particular value in the present description is intended to indicate the value, plus or minus the degree of variability due to measurement errors. For example, the amount of 10% may include a 9.5% or 10.5%, giving a margin of error of measurement, which will take into account and understand the specialists in this field.

Thus, the invention comprises a composition for cleaning teeth (composition 1.0) containing:

(a) an effective amount of basic and�of inability in free form or in salt form, for example arginine bicarbonate;

(b) abrasive substance containing:

(i) natural calcium carbonate (NCC) with an average particle size of 3-7 μm, for example approximately 5.5 micrometers, and a moisture absorption 12-25 g/100 g, for example approximately 18 g/100 g; and

(ii) precipitated calcium carbonate (PCC) with an average particle size of 1-5 micrometers, for example 2-3 micrometer, for example approximately 2.4 microns and water absorption of more than 25 g/100 g; and

(c) an effective amount of a fluoride source, e.g., a soluble fluoride salt, for example sodium monofluorophosphate.

For example, the invention relates to any of the following songs:

1.0.1. The composition is 1.0 with a coefficient of cleansing plaque from at least 70 and value abrasion isotopically labeled dentin less than 140.

1.0.2. Composition 1.0 or 1.0.1, where the basic amino acid is an arginine, lysine, citrulline, ornithine, creatine, histidine, diaminobutane acid, diaminopropionic acid, their salts and/or combinations thereof.

1.0.3. Any of the preceding compositions, where the basic amino acid has the L-configuration.

1.0.4. Any of the preceding compositions in the form of salts of di - or Tripeptide containing a basic amino acid.

1.0.5. Any of the preceding compositions, where the basic amino acid is an arginine, such as L-argin�n

1.0.6. Any of the preceding compositions, where the basic amino acid is partially or wholly in salt form.

1.0.7. Any of the preceding compositions where the core contains the amino acid arginine phosphate.

1.0.8. Any of the preceding compositions, where the basic amino acid contains arginine hydrochloride.

1.0.9. Any of the preceding compositions where the core contains the amino acid arginine sulfate.

1.0.10. Any of the preceding compositions where the core contains the amino acid arginine bicarbonate.

1.0.11. Any of the preceding compositions wherein the salt of the basic amino acid is formed in situ in the composition by neutralizing the basic amino acid or salt acid.

1.0.12. Any of the preceding compositions wherein the salt of the basic amino acid is formed by the neutralization of the basic amino acid to form a preliminary mixture before combining with the fluoride salt.

1.0.13. Any of the preceding compositions, where the basic amino acid is contained in an amount corresponding to from 1% to 15% by weight of the total composition, where the weight of the basic amino acid is calculated for the form of the free base.

1.0.14. Any of the preceding compositions, where the basic amino acid is contained in an amount corresponding to from 8% to 10% by weight of the total composition, where the weight of the basic amino acids R�schityvat for the form of the free base.

1.0.15. Any of the preceding compositions where the ratio of natural calcium carbonate to be precipitated calcium carbonate is from 1:1 to 1:5, for example from 1:2 to 1:3, e.g. about 1:2,5.

1.0.16. Any of the preceding compositions, where natural calcium carbonate is a refined natural calcium carbonate.

1.0.17. Any of the preceding compositions, where natural calcium carbonate is a product of crushed limestone.

1.0.18. Any of the preceding compositions, where not more than 0.01%, preferably not more than 0,004% by weight of particles of natural calcium carbonate do not pass through 325 mesh.

1.0.19. Any of the preceding compositions, where the precipitated calcium carbonate has a D502.3 to 2.7 micrometers, D90The 3.7-5.0 micrometers and D101.1-1.5 micrometers.

1.0.20. Any of the preceding compositions, where natural calcium carbonate is contained in an amount of 5-20% by weight of the composition.

1.0.21. Any of the preceding compositions, where the precipitated calcium carbonate is contained in an amount of from 10% to 35% by weight of the composition.

1.0.22. Any of the preceding compositions, where natural calcium carbonate is contained in the amount of about 10%, and precipitated calcium carbonate contains approximately 25% by weight of the composition.

1.0.23. Any of the preceding compositions,where the source of fluoride is a soluble fluoride salt.

1.0.24. Any of the preceding compositions, where the source of fluoride is a soluble fluoride salt selected from tin fluoride, sodium fluoride, potassium fluoride, sodium monofluorophosphate, fertilitate sodium, fertilitate ammonium, amine fluoride (e.g., N'-octadecyltrimethylammonium-N,N,N'-Tris(2-ethanol)-dihydrofluoride), ammonium fluoride, titanium fluoride, hexaferrite and their combinations.

1.0.25. Any of the preceding compositions, where the source of fluoride is perforat.

1.0.26. Any of the preceding compositions, where the fluoride source is a sodium monofluorophosphate.

1.0.27. Any of the preceding compositions, where the source of fluoride is a fluoride salt in an amount of from about 0.1% wt. to 2 wt%. by weight of the total composition.

1.0.28. Any of the preceding compositions, where the source of fluoride is a fluoride salt contained in the amount of approximately 1.1% by weight of the composition.

1.0.29. Any of the preceding compositions, where the source of fluoride is a soluble fluoride salt provides fluoride ion in an amount of from about 50 to about 25,000 hours/million

1.0.30. Any of the preceding compositions, where the source of fluoride is a soluble fluoride salt provides fluoride ion in a quantity�hardness from about 750 to about 2000 hours/million

1.0.31. Any of the preceding compositions, where the composition comprises from about 1000 to about 1500 hours/million fluoride ion.

1.0.32. Any of the preceding compositions, where the composition contains approximately 1450 hours/million fluoride ion.

1.0.33. Any of the preceding compositions where the pH is in the range of 6 to 9, for example 6.5 to 7.4 or 7.5-9.

1.0.34. Any of the preceding compositions where the pH is in the range from 6.5 to 7.4.

1.0.35. Any of the preceding compositions where the pH is approximately neutral.

1.0.36. Any of the preceding compositions where the pH is 8.5 to 9.5.

1.0.37. Any of the preceding compositions, optionally containing means against the formation of stones.

1.0.38. Any of the preceding compositions, optionally containing means against the formation of stones, which is a polyphosphate, e.g., pyrophosphate, tripolyphosphate or hexametaphosphate, for example, in the form of sodium salt.

1.0.39. Any of the preceding compositions containing at least one surfactant.

1.0.40. Any of the preceding compositions containing at least one surfactant selected from sodium lauryl sulfate, cocamidopropylbetaine and their combinations.

1.0.41. Any of the preceding compositions containing anionic surface-activeelement, for example, selected from sodium lauryl sulfate, sodium Laureth and mixtures thereof.

1.0.42. Any of the preceding compositions comprising sodium lauryl sulfate in an amount of from 0.5 to 3% by weight of the composition.

1.0.43. Any of the preceding compositions containing at least one humectant.

1.0.44. Any of the preceding compositions containing at least one humectant selected from glycerin, sorbitol and their combinations.

1.0.45. Any of the preceding compositions containing at least one polymer.

1.0.46. Any of the preceding compositions containing at least one polymer selected from polyethylene glycols, copolymers polivinilovogo ether maleic acid, polysaccharides (e.g., cellulose derivatives such as carboxymethyl cellulose, or polysaccharide gums, for example xanthan gum or carrageenan) and their combinations.

1.0.47. Any of the preceding compositions containing strips or pieces of gum.

1.0.48. Any of the preceding compositions containing fragrance, perfume and/or dye.

1.0.49. Any of the preceding compositions containing water.

1.0.50. Any of the preceding compositions comprising an antibacterial agent.

1.0.51. Any of the preceding compositions comprising an antibacterial agent selected from a simple halog�kirovenego diphenyl ether (for example, triclosan), herbal extracts and essential oils (e.g. rosemary extract, tea extract, Magnolia extract, thymol, menthol, eucalyptus, geraniol, carvacrol, citral, hinokitiol, catechol, methyl salicylate, EGCG, EGCG, Galic acid, extract of miswak, extract of sea buckthorn (Hippophae rhamnoides), biguanidines antiseptics (e.g., chlorhexidine, alexidine or octenidine), Quaternary ammonium compounds (e.g., cetylpyridinium chloride (CPC), benzalkonium chloride, chloride tetradecylbenzene (TPC), chloride N-tetradecyl-4-ethylpyridine (TDEPC)), phenolic antiseptics, hexetidine treatment, octenidine, sanguinarine, povidone-iodine, delmopinol, soliflore, metal ions (e.g., zinc salts, e.g. zinc citrate, tin salts, copper salts, iron salts), sanguinarine, propolis and oxidizing agents (e.g. hydrogen peroxide, savefilename of peroxyborate or peroksikarbonat), phthalic acid and its salts, nonoperatively acid and its salts and esters, ascorbinsaeure, oleoresin, alkylsulfate, dioctylsulfosuccinate, salicylanilide, domiphen bromide, delmopinol, Octafinal and other piperidine derivatives, preparations Nizina, salts of the acid chloride and mixtures of any of the above compounds.

1.0.52. Any of the preceding compositions containing protivo�plateline connection for example, the inhibitor of at least one proinflammatory host of factors, metalloproteinases selected from the intercellular substance (MMP), cyclooxygenase (COX), PGE2interlekin 1 (IL-1), IL-1β-converting enzyme (ICE), transforming growth factor β1 (TGF-β1), inducible synthase nitric oxide (iNOS), hyaluronidase, in vitro, nuclear factor Kappa B (NF-kB) and kinases associated with the receptor of IL-1 (IRAK), for example, selected from aspirin, Ketorolac, flurbiprofen, ibuprofen, naproxen, indomethacin, aspirin, Ketoprofen, piroxicam, meclofenamic acid, nordihydroguaiaretic acid and mixtures thereof.

1.0.53. Any of the preceding compositions comprising an antioxidant, e.g., selected from the group consisting of coenzyme Q10, PQQ, vitamin C, vitamin E, vitamin A, anethole-ditation and mixtures thereof.

1.0.54. Any of the preceding compositions comprising triclosan.

1.0.55. Any of the preceding compositions comprising an antibacterial agent in amount of about 0.01 to about 5 wt%. by weight of the total composition.

1.0.56. Any of the preceding compositions comprising triclosan in the amount of approximately from 0.01 to about 1 percent by weight by weight of the total composition.

1.0.57. Any of the preceding compositions comprising triclosan in an amount from about 0.3% m�ssy of the total composition.

1.0.58. Any of the preceding compositions comprising triclosan and a source of ions of Zn2+, such as zinc citrate.

1.0.59. Any of the preceding compositions comprising a bleaching agent.

1.0.60. Any of the preceding compositions comprising a bleaching agent selected from a whitening active substances selected from the group consisting of peroxides, metal chlorite, perborates, percarbonates, peroxyketal, hypochlorite and combinations thereof.

1.0.61. Any of the preceding compositions further comprising hydrogen peroxide or a source of hydrogen peroxide such as urea peroxide or a salt or complex of a peroxide (for example, such salts as peroxyborate, peroxocarbonate, perborate, peroxisomal or persulfate; for example, proxyport calcium, sodium perborate, peroksikarbonat, peroxyborate sodium and potassium persulfate) or polymeric complexes of hydrogen peroxide, such as polymeric complexes of hydrogen peroxide-polyvinylpyrrolidone.

1.0.62. Any of the preceding compositions, optionally containing a source of calcium and phosphate selected from (i) complexes of calcium-glass, for example, nitrilotriacetic of calcium, and (ii) calcium-protein complexes, e.g., casein phosphopeptide-amorphous calcium phosphate.

1.0.63. Any of the preceding compositions, more�tive containing a soluble calcium salt, for example, selected from calcium sulfate, calcium chloride, calcium nitrate, calcium acetate, calcium lactate, and combinations thereof.

1.0.64. Any of the preceding compositions, optionally containing an agent that inhibits or prevents the attachment of bacteria, for example, Cabral or chitosan.

1.0.65. Any of the preceding compositions, optionally containing a physiologically acceptable potassium salt, e.g., potassium nitrate, potassium citrate or potassium chloride, in amounts effective to reduce tooth sensitivity.

1.0.66. Any of the preceding compositions comprising about 0.1% to about 7.5% of a physiologically acceptable potassium salt, e.g., potassium nitrate and/or potassium chloride.

1.0.67. Any of the preceding compositions, which when applied in the oral cavity, for example, with a brush, effectively provides (i) a decrease or inhibition of formation of dental caries, (ii) reduce, repair or suppression precariously damage to the enamel, e.g., as diagnosed by quantitative secondarywindow fluorescence (QLF) or the definition of caries from the electric resistance (ECM), (iii) a decrease or inhibition of demineralization and the activation of remineralization of the teeth, (iv) reduce hypersensitivity of the teeth, (v) a decrease or inhibition of gingivitis, (vi) accelerated�to the amount of healing wounds or cuts in the mouth, (vii) lower levels of acid producing bacteria, (viii) to increase relative levels alginolyticus bacteria, (ix) inhibition of formation of biofilms in the oral cavity, (x) raise and/or maintain the pH of dental plaque at levels of at least pH around 5.5 after exercise sugar, (xi) reduce plaque accumulation, (xii) reduce dry mouth, (xiii) cleaning of teeth and oral cavity (xiv) reduce erosion, (xv) whiten teeth; and/or (xvi) immunize or protect the teeth against cariogenic bacteria.

1.0.68. The composition is obtained or obtainable by combining the ingredients as described above in any of the preceding compositions.

1.0.69. Any of the preceding compositions, where the composition is a toothpaste.

1.0.70. Any of the preceding compositions, where the composition is a toothpaste, optionally containing one or more of one or more of water, abrasives, surfactants, foaming agents, vitamins, polymers, enzymes, humectants, thickeners, antimicrobial agents, preservatives, flavorings, colorings and/or combinations thereof.

1.0.71. Any of the preceding compositions containing:

(a) an effective amount of basic amino acid in free form or in salt form, for example arginine bicarbonate;

(b) abrasive substance containing:

(i) natural calcium carbonate (NCC) with an average particle size of 3-7 μm, for example approximately 5.5 micrometers, and a moisture absorption 12-25 g/100 g, for example approximately 18 g/100 g; and

(ii) precipitated calcium carbonate (PCC) with an average particle size of 1-5 micrometers, for example 2-3 micrometer, for example approximately 2.4 microns and water absorption of more than 25 g/100 g;

(c) an effective amount of a fluoride source, e.g., a soluble fluoride salt, for example sodium monofluorophosphate; and

(d) an anionic surfactant, such as sodium lauryl sulfate.

1.0.72. The dentifrice according to any one of the preceding embodiments containing:

(a) 3-15% wt./wt. of arginine bicarbonate;

(b) abrasive substance containing:

(i) 5-15% wt./wt. natural calcium carbonate (NCC) with an average particle size of 3-7 μm, for example approximately 5.5 micrometers, and a moisture absorption 12-25 g/100 g, for example approximately 18 g/100 g; and

(ii) 20-30% wt./wt. precipitated calcium carbonate (PCC) with an average particle size of 1-5 micrometers, for example 2-3 micrometer, for example approximately 2.4 microns and water absorption of more than 25 g/100 g; and

(iii) 0.1 to 2% wt./wt., for example, approximately 1.1% wt./wt. of sodium monofluorophosphate; and

(iv) about 0.5-3% wt./wt. sodium lauryl sulfate.

The�them, the invention relates to a toothpaste according to any of the preceding compositions 1.0-1.0.72 containing, wt.%:

Water
Humidifiers20-35
Thickeners and polymers0-5
Flavors and pigmentsOf 0.01-5
Buffers0-3
Soluble fluoride salt0,3-2
Bicarbonate arginine5-12
Abrasive a substance based on natural calcium carbonate5-15
Abrasive substance on the basis of precipitated calcium carbonate15-35
SurfactantOf 0.3-3

In another preferable embodiment of the, present invention relates to a method (method 2) improve the health of the oral cavity, comprising applying an effective amount of the oral composition of any of Varian�s implementation compositions 1.0-1.0.72 in the oral cavity in need of an individual, for example, method:

(a) reducing or inhibiting the formation of dental caries,

(b) reduce, repair or suppression prekrasnyh damage to the enamel, e.g., as diagnosed by quantitative secondarywindow fluorescence (QLF) or the definition of caries from the electric resistance (ECM),

(c) a decrease or inhibition of demineralization and activation remineralization of the teeth,

(d) reduce hypersensitivity of the teeth,

(e) reduction or suppression of gingivitis,

(f) accelerate healing of wounds or cuts in the mouth,

(g) lowering the levels of acid producing bacteria,

(h) the increase in relative levels alginolyticus bacteria

(i) inhibiting the formation of microbial biofilms in the oral cavity,

(j) improve and/or maintain the pH of dental plaque at levels of at least pH around 5.5 after exercise sugar,

(k) reduce plaque accumulation,

(l) reduce erosion,

(m) tooth whitening

(n) the better health,

(o) immunize or protect the teeth against cariogenic bacteria, and/or cleaning of the teeth and oral cavity.

Thus, the skilled practitioner in the field to care for the oral cavity may be seen that a surprising technical effect and advantage of enhanced closing defects of dentin sensitive teeth could�t be due to the composition and applying the composition to care for the oral cavity, for example, a toothpaste in accordance with one or more aspects of the invention, which is intended to provide combinations of active components or ingredients, and preferably their respective quantities in the composition.

The levels of active ingredients will vary depending on the nature of the delivery system and specific active substances. For example, the basic amino acid may be contained at levels, for example, from about 3 to about 112% wt. for toothpaste consumer or from about 7 to about 20 wt%. for a professional or prescription remedies medicinal purposes (amount expressed by weight of the free base). Fluoride may be contained at levels, for example, from about 750 to about 2000 hours/million for toothpaste consumer or from about 2000 to about 10000 hours/million for a professional or prescription remedies medicinal purposes. Levels of antibacterial agents will be in accordance with the specific agent and a composition, for example, toothpaste with triclosan may contain about 0.3 wt%. triclosan.

Measurement

RDA: RDA is an abbreviation abrasion isotopically labeled dentin, relative�th readings abrasive ability. Generally remote from human or cow teeth irradiated by neutron flux, placed in an environment of methylmethacrylate (bone glue), remove the enamel, inserted into a brushing machine, brush in accordance with the standards of the American dental Association (ADA) (standard toothbrush, pressure 150 g, 1500 movements, suspension water-toothpaste 4-to-1). Then measure and record the radioactivity of the wash water. For control experiment, the test is repeated with a standard toothpaste ADA, made of calcium pyrophosphate, where this measurement is taken for a value of 100 for relative calibration of the scale. See, for example, Hefferren, Journal of Dental Research, 55:4, 1976, 563-573 and U.S. patents Nos. 4340583, 4420312 and 4421527.

By PCR or the rate of purification of plaque determine the effectiveness of the means for brushing your teeth while removing plaque, for example as described in U.S. patent No. 5658553 and 5651958. As a rule, the substance for the purification of plaque applied to a cow's tooth, which is then stained with a combination of plaque forming substances and tea, coffee and FeCl3which is then treated with a composition, and the change in reflectivity of the surface of the tooth before and after treatment is the value of the PCR.

Essential amino acids

Essential amino acids that can be used in the compositions and methods of the invention include not only the basic amino acids of prirodoohoronnogo, such as arginine, lysine, and histidine, as well as any amino acid that contains a carboxyl group and an amino group in the molecule, which are water-soluble and provide an aqueous solution with a pH of about 7 or above.

Thus, the basic amino acids include, but are not limited to, arginine, lysine, citrulline, ornithine, creatine, histidine, diaminobutane acid, diaminopropionic acid, their salts or their combinations. In a specific embodiment of the basic amino acid selected from arginine, citrulline and ornithine. In certain embodiments, the basic amino acid is an arginine, such as L-arginine, or its salt.

The composition of the invention are intended for topical application in the oral cavity, and, thus, the salts for use in the present invention should be safe for such use provided in quantities and concentrations. Suitable salts include salts known in this area as pharmaceutically acceptable salts, which is generally considered a physiologically acceptable provided in quantities and concentrations. Physiologically acceptable salts include salts derived from pharmaceutically acceptable inorganic or organic acids or bases, such as additive, acid salts formed by acids which obra�comfort physiologically acceptable anion, for example hydrochloride or bromine salt, and additive salts of the bases formed with bases which form a physiologically acceptable cation, for example, such as derived from alkali metals such as potassium and sodium or alkaline earth metals such as calcium and magnesium. Physiologically acceptable salts can be obtained using known in the field of conventional methods, such as the interaction is sufficiently basic compound such as an amine with a suitable acid, providing a physiologically acceptable anion.

In various embodiments, the basic amino acid is contained in the amount of about 0.5 wt%. to about 20 wt%. by weight of the total composition, from about 1 wt%. up to about 10 wt%. by weight of the total composition, for example about 1.5 wt.%, approximately 3,75% wt., approximately 5% wt. or about 7.5 wt%. by weight of the total composition.

Sources of fluoride ion

Compositions for caring for the oral cavity may further comprise one or more sources of fluoride ion, such as a soluble fluoride salt. A wide range of substances, giving the fluoride ion can be used as sources of soluble fluoride in the present compositions. Examples of suitable substances, giving the fluoride ion can be found in U.S. patent No. 535421 addressed to Briner et al., U.S. patent No. 4885155 addressed to Parran Jr. et al. and U.S. patent No. 3678154 addressed to Widder et al., included in this description by reference.

Typical sources of fluoride ion include, but are not limited to, tin fluoride, sodium fluoride, potassium fluoride, sodium monofluorophosphate, forcricket sodium, forcricket ammonium, amine fluoride, ammonium fluoride, and combinations thereof. In certain embodiments, the source of fluoride ion comprises tin fluoride, sodium fluoride, sodium monofluorophosphate, and mixtures thereof.

In certain embodiments, the composition for caring for the oral cavity according to the invention may also contain a source of fluoride ions or fluoride ingredient in amounts sufficient to provide from about 25 hours/million up to 25,000 hours/million fluoride ions, generally at least about 500 hours/million, for example, from about 500 to about 2000 hours/million, for example, from about 1000 to about 1600 hours/million, for example, approximately 1450 hours/million the Appropriate level of fluoride will depend on the specific application. Toothpaste for conventional applications, typically contains from about 1000 to about 1500 hours/million, where children's toothpaste contains a lower number. The dentifrice or coating for professional application can contain up to Ali even up to 25,000 hours/million fluoride.

The sources of the fluoride ion can be added to the compositions according to the invention at the level of about 0.01 wt%. up to about 10 wt%. in one embodiment, implementation, or about 0.03 wt%. up to about 5 wt%. in another embodiment of implementation and approximately 0.1 wt%. to about 1 wt%. by weight of the composition in another embodiment of the implementation. Weight fluoride salts to provide the appropriate level of fluoride ion, obviously, vary depending on the mass of the counterion salt.

When the composition contains bicarbonate of calcium, sodium monofluorophosphate is preferred to sodium fluoride for reasons of stability.

Abrasives

Natural calcium carbonate can be found in rocks, such as chalk, limestone, marble and travertine. He is also the main component of the eggshell and shell species. Abrasive substance on the basis of natural calcium carbonate according to the invention, generally, is a micronized limestone, which can optionally be refined or partially refined to remove impurities. For use in the present invention the average particle size of the substance is less than 10 micrometers, for example from 3 to 7 micrometers, for example about 5.5 micrometers. Due to the fact that the natural calcium carbonate can�to keep a high proportion not thoroughly tested relatively large particles, which can suddenly increase the grinding capacity, preferably not more than 0.01%, preferably not more than 0,004 mass percent of the particles pass through a 325 mesh. Substance possesses strongly pronounced crystalline structure, and thus it is harder and more abrasive than precipitated calcium carbonate. The density of abrasion of the natural calcium carbonate is in the range of, for example, 1 to 1.5 g/cm3for example , about 1.2, for example, approximately 1.19 g/cm3. There are various natural polymorphs of calcium carbonate, such as calcite, aragonite and poterit where calcite is preferred for the purposes of the present invention. An example of a commercially available product, suitable for use in the present invention includes Vicron® 25-11 FG from GMZ.

Precipitated calcium carbonate typically produced by burning limestone to get calcium oxide (burnt lime), which then can be converted back to calcium carbonate by reaction with carbon dioxide in the water. Precipitated calcium carbonate has a crystalline structure different from that of natural calcium carbonate. As a rule, he is a looser and more porous, thus, has a lower abrasive capacity and higher water absorption. For use in the present invent�AI particles are small, for example, with an average particle size of 1-5 micrometers and contain, for example, not more than 0.1%, preferably not more than 0.05% by weight of particles that pass through 325 mesh. The particles can, for example, to have D903-6 micrometers, for example, 3,8-4,9, for example, about 4.3, D501-4 micrometer, for example, 2,2-2.6 micrometers, for example, approximately 2.4 micrometers, and D101-2 micrometer, for example, 1.2 to 1.4, for example, approximately 1.3 micrometer. The particles have a relatively high water absorption, for example, at least 25 g/100 g, for example, 30-70 g/100 g. Examples of commercially available products suitable for use in the present invention include, for example, Carbolag® 15 Plus from Lagos Industria Quimica.

In certain embodiments, the invention may contain additional calcium abrasives, for example, the abrasive substance on the basis of calcium phosphate, such as calcium triphosphate (Ca3(PO4)2), hydroxyapatite (Ca10(PO4)6(OH)2) or the dihydrate of calcium diphosphate (CaHPO4·2H2Oh, also sometimes referred to in the present description as DiCal) or calcium pyrophosphate, and/or abrasives on the basis of silica, such as precipitated silicates with an average particle size of approximately 20 microns, such as Zeodent 115®, manufactured by J. M. Huber, metaphosphate n�try, of potassium metaphosphate, aluminum silicate, calcined alumina, bentonite or other siliceous substances or their combinations. However, additional abrasives preferably not contained by a type and in such quantity that increase the RDA for cleaning teeth to levels that can damage sensitive teeth, for example, 130.

Foam funds

Compositions for caring for the oral cavity according to the invention may also contain a means for increasing the amount of foam that is formed during the cleaning of the oral cavity brush.

Illustrative examples of means that increase the amount of foam include, but are not limited to, polyoxyethylene and certain polymers, including, but not limited to, alginate polymers.

Polyoxyethylene can increase the amount of foam and the density of the foam formed by the component carrier to care for the oral cavity according to the present invention. Polyoxyethylene also commonly known as polyethylene glycol ("PEG") or polyethylene oxide. Suitable for the present invention polyoxyethylene have a molecular weight of approximately from 200,000 to about 7000000. In one of the embodiments the molecular weight is from about to about 600000 2000000, and in another embodiment, the implementation of from about 800000 approx�sideline to 1000000. Polyox® is a trade name of a high-molecular polyoxyethylene, manufactured by Union Carbide.

Polyoxyethylene may be contained in amounts of from about 1% to about 90%, in one embodiment, the implementation of from about 5% to about 50% and in another embodiment, the implementation of from about 10% to about 20% by weight of the component carrier compositions for caring for the oral cavity according to the present invention. The dosage of the foaming means in a composition for caring for the oral cavity (e.g., single dose) is about 0.01 to about 0.9 percent by weight, from about 0.05 to about 0.5% by weight and in another embodiment, the implementation of from about 0.1 to about 0.2% by mass.

Surfactants

Other means, not necessarily contained in a composition for caring for the oral cavity according to the invention, is a surface-active agent or mixture of compatible surfactants. Suitable surfactants are those which are sufficiently stable in a wide pH range, for example, anionic, cationic, nonionic or zwitterionic surfactants.

Suitable surfactants are described in more detail, for example, in U.S. patent �� 3959458 in the name of Agricola et al., U.S. patent No. 3937807 in the name Haefele and U.S. patent No. 4051234 addressed to Gieske et al., included in this description by reference.

In certain embodiments, suitable in the present description anionic surfactants include water soluble salts of alkylsulfate containing from about 10 to about 18 carbon atoms in the alkyl radical and the water-soluble salts of sulfonated monoglycerides of fatty acids containing from about 10 to about 18 carbon atoms. Sodium lauryl sulfate, lauroylsarcosine sodium and sodium salts of sulfonates of monoglycerides of coconut oil are examples of anionic surfactants of this type. You can also use a mixture of anionic surfactants.

In another embodiment, the implementation of suitable in the present invention cationic surfactants can be defined in a broad sense as derivatives of aliphatic Quaternary ammonium compounds containing one long-chain alkyl containing from about 8 to about 18 carbon atoms, such as lauryldimethylamine ammonium, cetylpyridinium chloride, bromide, cetyltrimethylammonium, ammonium, nitrite of cocoalkylamine, fluoride Camilleri�the action, and mixtures thereof.

Illustrative examples of cationic surfactants are the Quaternary ammonium fluorides described in U.S. patent No. 3535421 addressed to Briner et al., included in this description by reference. Certain cationic surfactants can also act as germicides in the compositions.

Illustrative examples of nonionic surfactants that can be used in the compositions according to the invention, can be defined in a broad sense as compounds produced by the condensation alkalinising groups (hydrophilic in nature) with an organic hydrophobic compound which may be aliphatic or alkyl of nature. Examples of suitable nonionic surfactants include, but are not limited to, pluronic, condensation products of polyethylene oxide and alkyl phenols, products derived from the condensation of ethylene oxide and the reaction product of propylene oxide and ethylene diamine, condensation products of ethylene oxide and aliphatic alcohols, oxides, long chain tertiary amine oxides, long chain tertiary phosphine, a long-chain diallylsulfide and mixtures of such substances.

In certain embodiments, suitable in the present invention the zwitterionic synthetic surfactants can� to determine in a broad sense as derivatives of aliphatic Quaternary ammonium, compounds of phosphonium and sulfone in which the aliphatic radical can contain unbranched or branched chain, and where one of the aliphatic substituents contains from about 8 to about 18 carbon atoms and one contains an anionic water-soluble group, e.g., carboxy, sulfonate, sulfate, phosphate or phosphonate. Illustrative examples suitable for introduction into the composition of surface-active substances include, but are not limited to, alkylsulfate sodium, lauroylsarcosine sodium, cocamidopropylbetaine and Polysorbate 20, and combinations thereof.

In a specific embodiment of the composition according to the invention contains anionic surfactants, such as sodium lauryl sulfate.

A surfactant or mixtures of compatible surfactants can be contained in the compositions of the present invention from about 0.1 percent to about 5.0 percent, preferably in another embodiment, the implementation of approximately 0.3% to about 3.0% and preferably in another embodiment, the implementation of from about 0.5 percent to about 2.0 percent by weight of the total composition.

Flavors

Compositions for caring for the oral cavity according to the invention may also contain flavoring. The flavors that are used in practical �the I mplementation of the present invention, include, but are not limited to, essential oils as well as various flavoring aldehydes, esters, alcohols, and similar substances. Examples of essential oils include oil curly mint, peppermint, Wintergreen, sassafras, clove, sage, eucalyptus, marjoram, cinnamon, lemon, lime, grapefruit and orange. Also useful are such chemicals as menthol, carvone, and anethole. In certain embodiments, use of peppermint oil and mint crispy.

Flavor is administered in the oral composition at a concentration of about 0.1 to about 5% by weight and about 0.5 to about 1.5 percent by weight. The dosage of flavoring in a separate dose of the composition to care for the oral cavity (e.g., single dose) is about 0.001 to about 0.05 percent by weight and in another embodiment, the implementation of from about 0.005 to about 0.015% by mass.

Chelating means

Compositions for caring for the oral cavity according to the invention may also optionally contain one or more chelating means forming complexes with calcium in the cell walls of bacteria. Linking with calcium weakens the cell wall of bacteria and increases the lysis of bacteria.

Another group of funds, suitable for use in qualities� chelating means in the present invention, is a soluble pyrophosphates. Used in the present compositions propogate salt can be any kind pyrophosphate alkali metal salts. In certain embodiments, salts include tetrapyrrolic alkali metal, dukely deerfoot alkali metal, acid tapirisat alkali metal and mixtures thereof, where the alkali metals are sodium or potassium. Salts are suitable for use both in hydrated and non hydrated forms. An effective amount of pyrophosphate salt useful in the present composition, generally sufficient for the formation of at least approximately 1.0 wt%. pyrophosphate ions, about 1.5 wt%. to about 6 wt.%, approximately 3.5 wt%. to about 6 wt%. such ions.

Polymers

Compositions for caring for the oral cavity according to the invention also optionally contain one or more polymers, such as polyethylene glycols, copolymers polivinilovogo ether maleic acid, polysaccharides (e.g., cellulose derivatives, e.g., carboxymethyl cellulose, or polysaccharide gums, for example xanthan gum or carrageenan). Acidic polymers, such as polyacrylate gels, can be in the form of their free acids or in a form partially or completely neutralized with�her a water soluble alkali metal (e.g., potassium and sodium) or ammonium. In certain embodiments, contains from 1:4 to 4:1 copolymers of maleic anhydride or acid with another polymerizable ethyleneamines monomer, for example, a simple methyl vinyl ether (methoxyethanol) with a molecular mass (MM) from about 30000 to about 1000000. These copolymers are available for example as Gantrez AN 139(MM OF 500,000), AN 119 (MM 250000) and S-97 pharmaceutical grade purity (MM 70000) from GAF Chemicals Corporation.

Other used polymers such as copolymers of 1:1 maleic anhydride with acrylate, hydroxyethylmethacrylate, N-vinyl-2-pyrrolidone or ethylene, where the latter are available, for example, as Monsanto EMA No. 1103, MM 10,000 and EMA grade 61, and copolymers of 1:1 acrylic acid with methyl methacrylate or hydroxyethylmethacrylate, methyl acrylate or ethyl, simple isobutylphenyl ether or N-vinyl-2-pyrrolidone.

Generally suitable are polymerized reinstatement or Ethylenediamine carboxylic acids containing an activated carbon-carbon olefinic double bond and at least one carboxyl group, i.e., an acid containing an olefinic double bond which is easily participates in polymerization because of its presence in the monomer molecule in the alpha-beta position relative to the carboxyl grupper as part of a terminal methylene grouping. Illustrative examples of such acids are acrylic, methacrylic, etakrinova, alpha florachilena, crotonic, beta-aryloxypropanolamine, sorbic, alpha-chlorobenzoate, cinnamic, beta-stellacreasy, Mukanova, taconova, Tarakanova, muzakaeva, glucagonoma, akonita, alpha phenylacrylate, 2-benzylacrylamide, 2-cyclohexylaniline, angelic, umbellata, fumaric, maleic acids and anhydrides. Other different olefinic monomers forming the copolymer with such carboxylic monomers include vinyl acetate, vinyl chloride, dimethylmaleic, etc., the Copolymers contain sufficient carboxylic salt groups for water solubility.

An additional class of polymeric means includes a composition containing homopolymers of substituted acrylamide free and/or homopolymers of unsaturated sulfonic acids and their salts, in particular when the polymers are based on unsaturated sulfonic acids selected from acrylamidophenylboronic acids such as 2-acrylamide-2-methylpropanesulfonic acid with a molecular weight of from about 1000 to about 2000000 described in U.S. patent No. 4842847, published on 27 June 1989, in the name Zahid included in this description by reference.

Another suitable class of polymeric means includes polyaminoamide, such that ka� containing proportional parts anionic surfactant-active amino acids, such as aspartic acid, glutamic acid and phosphoserine, as described in U.S. patent No. 4866161 in the name of Sikes et al., included in this description by reference.

Upon receipt of the compositions for the care of the oral cavity is sometimes necessary to add some thickening of the substance to achieve the desired consistency or to stabilize or enhance the characteristics of the composition. In certain embodiments, thickening funds are carboxyvinyl polymers, carrageenan, hydroxyethyl cellulose and water soluble salts of ethers of cellulose, such as carboxymethylcellulose sodium and sodium. You can also enter the natural gums, such as gum, gum karaya, gum Arabic and tragacanth gum. Colloidal magnesium aluminosilicate or finely divided silica can be used as a component of the thickening composition which further improves the texture of the composition. In certain embodiments, use thickening funds in the amount of from about 0.5 percent to about 5.0 percent by weight of the total composition.

Enzymes

Compositions for caring for the oral cavity according to the invention may also optionally contain one or more enzymes. Suitable enzymes include any of the available proteases, glucanohydrolase�, endoglycosidase, amylase, mutans, lipase and Mucins or their compatible mixtures. In certain embodiments, the enzyme is a protease, dextranase, endoglycosidase and athanasou. In other embodiments, the enzyme is a papain, endoglycosidase or a mixture of dextranase and atanazy. Additional enzymes suitable for use in the present invention are described in U.S. patent No. 5000939 in the name Dring et al., U.S. patent No. 4992420, U.S. patent No. 4355022, U.S. patent No. 4154815, U.S. patent No. 4058595, U.S. patent No. 3991177 and U.S. patent No. 3696191 included in this description by reference. The enzyme mixture of several compatible enzymes in the present invention is approximately from 0.002% to about 2.0% in one of the embodiments or from about 0.05 percent to about 1.5% in another embodiment, implementation, or in another embodiment, the implementation of from about 0.1 percent to about 0.5 percent.

Water

Water can also be contained in oral compositions according to the invention. The water used in the commercial oral compositions must be deionized and not contain organic impurities. Water is usually of the composition is adjusted to the final volume, and it contains from about 10% to about 90%, from about 20% to about 60% or approx�siteline from 10% to about 30% by weight of the oral compositions. The amount of water includes the free water which is added plus that amount which is introduced with other materials such as with sorbitol or any component of the invention.

Humidifiers

In certain embodiments, oral compositions also preferably enter the humidifier to prevent solidification of the composition when exposed to air. Certain humectants can also impart desirable romantic rogue or fragrance compositions tools for cleaning teeth. Humidifier based on pure moisturizer usually contains from about 15% to about 70% in one of the embodiments or from about 30% to about 65% in another embodiment, the implementation by weight of the composition for cleaning teeth.

Suitable humectants include edible polyhydric alcohols such as glycerin, sorbitol, xylitol, propylene glycol, and other polyols and mixtures of these humectants. In certain embodiments, it is possible to use a mixture of glycerin and sorbitol as a component of the humidifier of the toothpaste compositions of the present description.

In addition to the components described above embodiments of the present invention may contain a variety of optional ingredients for cleaning teeth, some of which are described below. Not�necessary ingredients include, for example, but not limited to, adhesives, foaming tools, flavors, sweeteners, additional funds against plaque formation, abrasives and dyes. These and other optional components are further described in U.S. patent No. 5004597 addressed Majeti, U.S. patent No. 3959458 in the name of Agricola et al. and U.S. patent No. 3937807 in the name Haefele, included in this description by reference.

Methods of obtaining

The compositions of the present invention can be obtained by methods that are conventional in the field of products for oral use.

In one illustrative embodiments of a composition for caring for the oral cavity is produced by neutralization or partial neutralization of arginine in a gel phase with acid, for example phosphoric acid, hydrochloric acid or carbonic acid, and stirring. Moisturizer, such as, for example, vitamins, plus fluoride are mixed separately. Then to the mixture humidifier adds abrasives and arginine. Then the mixture was injected surfactants and fragrances and the resulting slurry is formed into a product for cleaning teeth.

Use of the composition

The present invention in the aspect of its method involves applying to the oral cavity safe and effective amounts described in the present description composite�.

Compositions and methods according to the invention is suitable for a way to protect the teeth by facilitating recovery and remineralization, in particular to reduce or inhibit the formation of dental caries, reduce or inhibit the demineralization and activation remineralization of the teeth, reduce hypersensitivity of the teeth, and reduce, repair or suppression prekrasnyh damage to the enamel, e.g., as diagnosed by quantitative secondarywindow fluorescence (QLF) or the definition of caries from the electric resistance (ECM).

Quantitative light-induced fluorescence is a fluorescence in visible light, which can be used to detect early damage and to conduct surveillance for a long period of time progress or regress. Normal teeth fluoresce in visible light, demineralized teeth do not fluoresce or fluoresce only in lesser degree. The area of demineralization, you can quantify and monitor its progression. To induce autofluorescence of the teeth using blue laser light. Areas in which there is a loss of minerals, have a weaker fluorescence and appear darker in comparison with the surface of a healthy tooth. For the quantitative determination of fluorescence from white spot or area/volume associated with damage, use software. Typically, individuals with existing damage in the form of white patches are selected as the participants of the trial. The measurements were carried out in vivo on these teeth. In early clinical observations determine the area/volume of the damage. Reduction (improvement) of the region/volume of damage is determined at the end of 6 months of product use. Data is usually represented as the percentage of improvement compared with baseline.

Definition of caries from the electric resistance is a method used to measure the content of mineral substances of the tooth on the basis of electrical resistance. When measuring electrical conductivity using the fact that the fluid-filled tubules that open when demineralization and erosion of the enamel conduct electricity. Because the tooth loses minerals, its resistance to current flow decreases due to increased porosity. Thus, increasing the conductivity of the patient's teeth may indicate demineralization. Typically, research is conducted on the surfaces of the roots with the existing damage. The measurements were carried out in vivo on these teeth. Spend a change of electrical resistance before and after 6 months of treatment. In addition, conduct a classic assessment of carisporodol roots with the use of tactile samples. Hardness is classified on a scale: a tough, hard or soft. In this type of study, the results generally are in the form of electrical resistance (the higher the number, the better) ECM measurements and improve the rigidity of damage on the basis of tactile points of the sample.

Thus, the compositions according to the invention are suitable in the method of reducing prekrasnyh damage the enamel (as measured by QLF or ECM) compared with the composition not containing effective amounts of fluorine and/or arginine.

The compositions according to the invention are additionally suitable in methods to reduce harmful bacteria in the oral cavity, for example, reduction or inhibition of gingivitis, lowering the levels of acid producing bacteria, to increase relative levels alginolyticus bacteria, inhibiting the formation of microbial biofilms in the oral cavity, raise and/or maintain the pH of dental plaque at levels of at least pH around 5.5 after load of sugar, reduce the accumulation of plaque and/or cleaning of the teeth and oral cavity.

Finally, by increasing the pH in the oral cavity and inhibit pathogenic bacteria composition according to the invention are suitable for accelerating the healing of wounds or cuts in the mouth.

Improving the health of the mouth also has a beneficial effect on total �dorofee, because the tissues of the mouth can be a gateway for other infections. A good healthy condition of the oral cavity is associated with General health, including the health of the cardiovascular system. Compositions and methods according to the invention have a specific favourable action due to the fact that the essential amino acids, particularly arginine, are sources of nitrogen, which provides a path of NO synthesis and thus increases microcirculation in the tissues of the oral cavity. Providing a less acidic environment in the oral cavity also helps to reduce gastric distress and creates a less favorable environment for Heliobacter, which is associated with stomach ulcers. Arginine, in particular, is required for high expression of specific receptors of immune cells, such as T-cell receptors, thus, arginine may enhance the effectiveness of the immune response. Thus, the compositions and methods according to the invention is suitable for improving General health including the health of the cardiovascular system.

Compositions and methods of the invention can be included in compositions for oral care mouth and teeth such as toothpastes, transparent pastes, gels, rinses mouth, sprays and chewing gum.

As used throughout, ranges are used as a quick �of oznaczenia to describe each and every part of the range values. Any value in the range can be selected as the final value of the range. In addition, all cited in the present description reference is fully included, therefore, by reference. In case of discrepancies in the description in the present description and the description of the cited references, the present description shall take precedence. It should be understood that when describing the compounds, they can be described in terms of their ingredients, as is common in this area, despite the fact that these ingredients may react with each other in the present composition when it is received, stored and applied, and imply that the described formulations include such products.

The following examples further describe and demonstrate illustrative embodiments of within the scope of the present invention. Examples are given for illustration only and not meant to be limitations of the present invention, as many changes are possible without deviation from the essence and scope of the present invention. Various modifications of the invention addition to those shown and described in the present description, will be obvious to specialists in this field and are included in the attached claims.

Examples

Example 1 - Comparison of various grinding systems

Test different combinations of abrasive�x substances:

Composition A: Prophylactic paste:

31% Sylodent 756,

15% Vicron 25-11 (fine CaCO3natural source),

14% Vicron 41-8 (fine CaCO3),

10% arginine Bicarbonate

RDA: 230

Composition: detergent for sensitive teeth consumer

50% Vicron 25-11 (fine CaCO3),

7% Sylodent 15,

2% arginine Bicarbonate

RDA: 179

Receive an additional composition as shown in table 1, and measure the RDA and PCR.

Table 1
RDAPCR
C. 8% Arginine/15% PCC/25% HA PCC6662
D. 8% Arginine/35% Wolkem RNCC17888
E. 8% Arginine/35% Vicron 25-11 NCC176109
F. 8% Arginine/7% PCC/25% PCC HA/3% AC43 HCS17294
G. 8% Arginine/10% Vicron 25-11 NCC/25% HA PCC10287
H 8% Arginine/10% Wolkem RNCC/25% HA PCC98 81

The original lineup was augmented by the addition of 3% AC 43 of silicon dioxide of high purity or replacement abrasives HA PCC (precipitated calcium carbonate with high absorption) NCC (natural calcium carbonate), which led to RDA and more than 170 compared to RDA 110-130 commercially available toothpaste for sensitive teeth. Testing other classes NCC, including the RNCC (refined natural calcium carbonate) from Wolkem Inc. India, which does not provide sufficient efficiency of purification at lower concentrations. The best combination is Vicron 25-11 NCC FG with 10% by weight with an average particle size of about 5.5 micrometers in combination with Lagos PCC with high absorption at 25% by weight with average particle size (D50) approximately 2.4, the result of which was the composition, which had the best efficiency of purification and low RDA.

Example 2 - Optimized composition for cleaning teeth

Based on preliminary testing of various combinations of abrasive substances that has been optimized dentifrice (table 2), which provides good cleaning and stain removal, but low abrasive action:

Ingredient% wt.
Water� 25,225
70% Sorbitol23,000
Carboxymethylcellulose0,720
Xanthan gumIs 0.135
Acesulfame K0,400
Sucralose0,020
Sodium bicarbonate0,500
Sodium silicate0.800 to
Titanium dioxide0,500
The sodium monofluorophosphate1,100
Bicarbonate arginine10,000
NCC-Vicron 25-1110,000
PCC-high absorption25,000
Sodium lauryl sulfate (SLS)1,500
Flavoring1,100
Total100,000

1. Composition for cleaning teeth, containing:
(a) effective number of�of arginine in free form or in salt form;
(b) abrasive substance that contains:
(i) natural calcium carbonate (NCC) with an average particle size of 3-7 microns and water absorption 12-25 g/100 g; and
(ii) precipitated calcium carbonate (PCC) with an average particle size of 1-5 microns and water absorption of more than 25 g/100 g
where the composition has a ratio of plaque purification (PCR) of at least 70 and the abrasion value of the isotopically labeled dentin (RDA) of less than 140, and the ratio of natural calcium carbonate to be precipitated calcium carbonate is from 1:2 to 1:3.

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

3. A composition according to any one of claims. 1 and 2, where the arginine in free form or in salt form represents an arginine bicarbonate.

4. A composition according to any one of claims. 1 and 2, where arginine is contained in an amount corresponding to from 1% to 15% of the total weight of the composition, where the weight of arginine designed for the form of the free base.

5. A composition according to any one of claims. 1 and 2, where the ratio of natural calcium carbonate to be precipitated calcium carbonate is 1:2,5.

6. A composition according to any one of claims. 1 and 2, wherein the natural calcium carbonate is contained in an amount of 5-20% by weight of the composition, and precipitated calcium carbonate is contained in an amount of from 10 to 35% by weight of the composition.

7. A composition according to any one of claims. 1 and 2, where natural calcium carbonate� is contained in an amount of 10%, and precipitated calcium carbonate is contained in the amount of 25% by weight of the composition.

8. A composition according to any one of claims. 1 and 2, further comprising an anionic surfactant.

9. A composition according to any one of claims. 1 and 2, further comprising an antibacterial agent.

10. A composition according to any one of claims. 1 and 2, further comprising an anionic polymer.

11. A composition according to any one of claims. 1 and 2 in the form of toothpaste, further comprising one or more components selected from water, abrasives, surfactants, foaming agents, vitamins, polymers, enzymes, humectants, thickeners, antimicrobial agents, preservatives, flavors or colors.

12. A composition according to any one of claims. 1 and 2, containing the following ingredients, wt.%:

Humidifiers20-35
Thickeners and polymers0-5
Flavors and pigmentsOf 0.01-5
Buffers0-3
Soluble fluoride salt0,3-2
Bicarbonate arginine5-12
Abrasive substance on the basis of
natural calcium carbonate5-15
Abrasive substance on the basis of
precipitated calcium carbonate15-35
SurfactantOf 0.3-3
Waterelse

13. The way to care for the oral cavity comprising applying an effective amount of a composition according to any one of claims. 1-12 in the oral cavity in need of an individual for:
(a) reducing or inhibiting the formation of dental caries,
(b) reduce, repair or suppression prekrasnyh damage enamel,
c) a decrease or inhibition of demineralization and activation remineralization of the teeth,
(d) reduce hypersensitivity of the teeth,
(e) reduction or suppression of gingivitis,
(f) accelerate healing of wounds or cuts in the mouth,
(g) lowering the levels of acid producing bacteria,
h) increase relative levels alginolyticus bacteria,
(i) inhibiting the formation of microbial biofilms in the oral cavity,
(j) improve and/or maintain the pH of dental plaque at levels of at least pH �roughly 5,5 after load of sugar
k) reduce plaque accumulation,
l) to treat, reduce, mitigate or partial withdrawal symptoms dry mouth,
m) teeth whitening,
n) reduce erosion,
a) improve overall health and/or
p) cleaning of the teeth and oral cavity.



 

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13 cl, 1 dwg, 18 tbl, 64 ex

FIELD: chemistry.

SUBSTANCE: present invention refers to developing brewing products. According to the invention, a method for preparing an extract of polyphenols as a result of brewage involves the stages: contacting partially purified beer with resin, which adsorbs polyphenols; desorbing polyphenols adsorbed on the resin contacting with partially purified beer; adsorbing polyphenols on the second resin different from the first one; the above second resin is hydrophobic and non-ionic; and desorbing polyphenols adsorbed on the second resin with using an organic solvent; implementing the method is ethylacetate-free. The invention also refers to the method for preparing the extract of polyphenols as a result of brewage that involves the following stages: contacting partially purified beer with hydrophobic and non-ionic resin, which adsorbs polyphenols; and desorbing polyphenols adsorbed on the resin used at the previous stage of contacting with using the organic solvent; a desorption product contains at least 0.85 g of polyphenols per one gram of a dry matter. The invention also refers to the extract of polyphenols prepared by the above method and containing catechin, epicatechin, thyrozol and ferulic acid. The invention also refers to a cosmetic product, a functional food product, a food additive, which contain the above extract of polyphenols in an effective amount. Also the invention provides using the above cosmetic product for skin moistening and/or ageing prevention or delay, using the extract of polyphenols for producing an antioxidant composition.

EFFECT: invention provides preparing the extract of ethylacetate-free and high-purity polyphenols.

19 cl, 23 dwg, 22 tbl, 6 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to an oral care composition, methods for preparing and using it. The presented composition containing a pre-mix containing arginine in the free form or in the form of a salt, a soluble carbonate salt and arginine bicarbonate formed in situ when mixing arginine in the free form or in the form of a salt with the soluble carbonate salt. The method for preparing the composition involves preparing the pre-mix by mixing arginine in the free form or in the form of the salt and soluble carbonate salt. What is also presented is an oral care procedure involving coating the patient's oral cavity with an effective amount of the above composition.

EFFECT: using the group of inventions provides positive effects achieved by using the oral care composition containing arginine bicarbonate in a combination with a simplified process of preparation of this composition.

15 cl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the field of pharmaceutics and represents a composition for oral cavity care in the form of dental varnish, containing bioactive glass and fluoride, where the said fluoride is present in the composition in an amount of up to 5% by weight. An increased ionic release is observed for the dental varnish containing bioactive glass and fluoride.

EFFECT: invention provides the creation of compositions, containing bioactive glass, for which in case of applying fluoride in lower concentrations (lower than 900 mln-1) its efficiency is the same as for higher concentrations (900 - 1450 mln-1).

3 cl, 2 ex, 6 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to a compound with a woody note having structural formula I. In formula , the ring with 6 carbon atoms is saturated or has a double bond between carbon atoms C1 and C2 or between carbon atoms C1 and C6, R is selected from a C2-C5 alkyl or C2-C5 alkenyl group.

EFFECT: invention also relates to a fragrant composition containing said compound.

13 cl, 16 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I) : or a salt thereof, wherein R1 and R5 are independently selected from H, OH and alkoxy; R2-R4 and R6-R8 are independently selected from H, OH, F, Cl, Br and I; R9 and R10 are C2-C8 alkenyl; under the condition that at least one of R1, R5 and R7 is OH or alkoxy; at least one of R2-R4, R6 and R8 is F, Cl, Br or I; and R2 and R6 are Cl. The invention also relates to an antibacterial composition and treatment methods.

EFFECT: improved properties.

18 cl, 7 ex, 10 tbl

FIELD: medicine.

SUBSTANCE: method involves: a) preparing a polymer matrix film containing a water-soluble polymer and a hydrophobic/lipophilic additive and being substantially free from a poorly-soluble flavour; b) preparing a dental care base containing the poorly-soluble flavour; c) combining the polymer matrix film with the prepared base; and d) keeping the combined polymer matrix film and base for the period of time adequate to transfer an effective amount of the above flavour from the base of the dental care agent into the above polymer matrix film. That involves using the flavour specified in a certain list of poorly-soluble flavours (menthol, thyme oil, etc.), and one or more hydrophobic/lipophilic additives specified in a group of specific additives (Vaseline, silicone oil, etc.). The agent prepared by the above method has the same characteristics as the agents prepared by a common method, when the prepared films containing the flavour are added to the base of the dental care agent.

EFFECT: method provides such advantages as compared to the common method for preparing these agent, as a possibility to avoid using ethanol in preparing the film, otherwise required to solve the flavours if following the common method for preparing the film, as well as eliminating the flavour loss in heating during the film drying.

14 cl, 9 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: composition contains a) surface-active substances, including a salt of C10-16 alcohol ethoxylate sulphate, a betaine surface-active substance and alkylpolyglicoside, and b) a fatty C12-18 acid, constituting at least 15% of the total composition weight.

EFFECT: composition, possessing an increased viscosity and capable of producing a stable foam, is created.

10 cl, 1 tbl, 4 ex, 2 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, namely to a method for producing a preparation applicable for oral tissue regeneration. A method for producing a multi-component melatonine-containing preparation for oral tissue regeneration, involving incubating eggs, cooling them, performing homogenisation and ultramicrofiltration; the incubation procedure is performed for 5-6 days; the ultramicrofiltration procedure is added with 0.1% sodium benzoate; the prepared substance of embryo-egg mass is added with a second substance containing medical gelatine, sage and St. John's wort tea, melatonine, eucalyptus oil, glycerol and prepared according to certain procedure that is followed by mixing in a homogeniser; the produced mass is bottled, placed in a thermostat, cooled until film hardened; the films are cut in strips 1 cm wide and packed into plastic package. The multi-component melatonine-containing preparation for oral tissue regeneration.

EFFECT: preparation prepared by the method described above is effective for oral tissue regeneration.

3 cl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a method for producing antioxidant microcapsules: vitamin A, C, E, Q10, eleuterococcus, green tea extract or ginseng extract. A method for producing antioxidant microcapsules: vitamin A, C, E, Q10, eleuterococcus, green tea extract or ginseng extract consists in using carrageenan as a microcapsule coating with dissolving a certain amount of vitamin A, C, E, Q10, eleuterococcus, green tea extract or ginseng extract in dimethylsulphoxide and dispersing the produced mixture into the carrageenan suspension in butanol containing carrageenan in the presence of E472c, agitating in certain circumstances; adding benzene and water, filtering the produced suspension and drying at room temperature.

EFFECT: method provides simplifying and accelerating the microencapsulation process, reducing the process loss, higher weight yield.

7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the pharmaceutical industry, namely to an oral care composition and to a method for increasing the solubility of an active ingredient recovered from magnolia extract - tetrahydrohonokiol. The oral care composition contains an active ingredient recovered from the magnolia extract - tetrahydrohonokiol, propylene glycol and an orally acceptable carrier, in a certain amount.

EFFECT: content of the certain amount of propylene glycol in the oral care composition increases the solubility of tetrahydrohonokiol that leads to improving the effectiveness of its delivery and bioavailability.

3 cl, 8 tbl, 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to medicine, particularly to cosmetology, and describes a method for stabilising an anhydrous antiperspirant composition involving: (a) preparing a mixture of at least one substance having the antiperspirant action, containing a metal salt, and an anhydrous carrier for at least one substance possessing the antiperspirant action, wherein dissolved is at least one substance having the antiperspirant action, a carrier containing an eutectic mixture of carbamide and trimethylglycine; (b) heating this mixture for preparing the eutectic mixture of at least one substance having the antiperspirant action, and the anhydrous carrier.

EFFECT: invention can be used to reduce the body perspiration; the compositions can be applied by hands or with a package.

22 cl, 3 dwg, 2 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine and is intended for oral cavity care. Compositions include a multi-layered film and an orally acceptable carrier. The carrier contains the first flavouring agent, with the second flavour being contained in the present central layer of the multi-layered film, located between two external surface layers. The first and second flavouring agents can be similar or different. Each film layer can include a film-forming polymer, for instance, hydroxypropylmethylcellulose. The external layers can include a substance, modulating the release of the flavouring agent, for instance, polyvinylacetate or hydroxymethylcellulose. The carrier can be a means for teeth cleaning or a liquid for mouth rinsing.

EFFECT: obtaining the composition for oral cavity care.

22 cl, 3 dwg, 4 tbl, 11 ex

FIELD: medicine.

SUBSTANCE: vaseline-lanolin (2:1) based ointment 74.0 g is added with a 40% herbal alcoholate 25 ml of the following composition (in the mixture of a herbal raw material: alcohol base - 1:5), weight fractions: nodding catchfly herb - 3 weight fractions, pot marigold blossom - 1 weight fraction, spiraea herb - 1 weight fraction, with the ointment added with clove oil 1.0 ml. The prepared ointment is applied on inflamed periodontal and oral mucosal tissues for 20 minutes 2-3 times a day for 14 days; the patient is advised not to drink or eat for 1 hour.

EFFECT: method enables increasing clinical effectiveness by combining high antimicrobial, immunomodulatory, anti-allergic and keratoplastic activity and ease of use.

3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a compound of formula such as below , wherein Z is oxygen; Y is hydrogen or a sequence as follows: -O-C(R4)-V-(C=O)-R5; V is oxygen; R1 and R4 are identically or independently hydrogen or a C1-4 alkyl; R2 and R5 are identically or independently a C1-10 alkyl.

EFFECT: these compounds can be applicable in therapy for treating pathologies or disorders related to the presence of Propionibacterium acnes, eg acne-like skin disorders.

5 cl, 2 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed is emulsified composition for improvement of skin condition, which contains (A) 0.001-10 wt % of organic compound, which has two or more hydroxyl groups, inorganic value 220-450 and organic value 300-1000; (B) 0.001-10 wt % of organic compound, which has one hydroxyl group, inorganic value 100-200 and organic value 280-700; (C) 0.001-10 wt % of organic substance, represented by formula (2), in which R1 is C4-C30 hydrocarbon group; Z is methylene group, methane group or oxygen atom; X1, X2, X3 are hydrogen atom, hydroxyl group or acetoxy group; X4 is hydrogen atom, acetyl group or glyceryl group; each of R2 and R3 is hydrogen atom, hydroxyl group, hydroxymethyl group or acetoxymethyl group; R4 is C5-C60 hydrocarbon group; and R5 is hydrogen atom or hydrocarbon group, containing in total 1-30 carbon atoms; (D) (D) 0.00012-10 wt % of at least one compound, selected from group, consisting of non-ionic surface-active substance, which has polyoxyethylene group and HLB 10 or higher, ionic surface-active substance and sphingosine salt; (E) 0.003-15 wt % of at least one compound, selected from group, consisting of sugar alcohol, selected from group, consisting of erythritol, threitol, xylitol and mannitol, disaccharide and trisaccaride, and (F) water.

EFFECT: emulsion composition preserves water in skin for long time.

13 cl, 1 dwg, 18 tbl, 64 ex

FIELD: chemistry.

SUBSTANCE: present invention refers to developing brewing products. According to the invention, a method for preparing an extract of polyphenols as a result of brewage involves the stages: contacting partially purified beer with resin, which adsorbs polyphenols; desorbing polyphenols adsorbed on the resin contacting with partially purified beer; adsorbing polyphenols on the second resin different from the first one; the above second resin is hydrophobic and non-ionic; and desorbing polyphenols adsorbed on the second resin with using an organic solvent; implementing the method is ethylacetate-free. The invention also refers to the method for preparing the extract of polyphenols as a result of brewage that involves the following stages: contacting partially purified beer with hydrophobic and non-ionic resin, which adsorbs polyphenols; and desorbing polyphenols adsorbed on the resin used at the previous stage of contacting with using the organic solvent; a desorption product contains at least 0.85 g of polyphenols per one gram of a dry matter. The invention also refers to the extract of polyphenols prepared by the above method and containing catechin, epicatechin, thyrozol and ferulic acid. The invention also refers to a cosmetic product, a functional food product, a food additive, which contain the above extract of polyphenols in an effective amount. Also the invention provides using the above cosmetic product for skin moistening and/or ageing prevention or delay, using the extract of polyphenols for producing an antioxidant composition.

EFFECT: invention provides preparing the extract of ethylacetate-free and high-purity polyphenols.

19 cl, 23 dwg, 22 tbl, 6 ex

FIELD: medicine, oncology, amino acids.

SUBSTANCE: invention relates, in particular, to the development of an antitumor preparation based on natural substances. Invention relates to an amino acid preparation comprising at least one modified essential amino acid obtained by treatment of amino acid by ultraviolet radiation (UV) at wavelength 250-350 nm for 12-80 h at temperature 15-30oC or with ozone at temperature 15-25oC. The modified amino acid has no toxicity for health cells. Also, invention relates to a method for preparing such preparation. Invention provides the development of an antitumor preparation based on modified amino acids and expanded assortment of antitumor preparations being without cytotoxicity for normal cells.

EFFECT: valuable medicinal antitumor properties of preparation.

8 cl, 4 tbl, 2 dwg, 4 ex

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