Oral care composition

Abstract

Disclosed is an oral care composition comprising: an uncharged polar amino acid, a charged polar amino acid, a water-insoluble and / or slightly soluble calcium source wherein the amount of calcium source is present in a weight ratio to the total amount of uncharged polar amino acid and charged polar amino acid of 1: 10 to 20: 1, and wherein the amount of calcium source is less than the total amount of uncharged polar amino acid and charged polar amino acid based on the total weight of the composition, and wherein the amount of water-insoluble and / or slightly soluble calcium source is less than the total amount of water-insoluble and / or slightly soluble calcium source is less than the total amount of water-insoluble and / or slightly soluble calcium source. The composition comprises less than 0.005% by weight of other amino acids in addition to uncharged polar amino acids and charged polar amino acids.

Description

Technical Field

[0001] The present invention relates to an oral care composition, such as toothpaste, tooth powder, chewing gum, mouthwash, slurry, etc. The present invention particularly relates to an oral care composition comprising certain amino acids and a calcium source. The present invention also relates to the use of such a composition for remineralizing an individual's teeth and / or preventing or reducing dental caries in an individual and / or reducing the sensitivity of an individual's teeth. Background Art

[0002] Teeth include dentin covered with an outer layer of enamel. Teeth are constantly attacked by chemical and physical forces, including bacteria-derived acids and mechanical abrasion, which lead to demineralization and weakening of the enamel and underlying dentin. Enamel is composed of hydroxyapatite crystals that create a porous surface. The erosion of enamel needs to be stopped or at least delayed to maintain good oral health. Fluoride is commonly used in oral care products to combat caries. The resulting fluorapatite composition is harder than the original hydroxyapatite composition and is more resistant to acid attack.

[0003] Tooth hypersensitivity is a temporary, painful sensation that affects up to 20% of the adult population. It is associated with tooth demineralization and the loss of enamel or cementum, exposing the underlying dentin. The dentin of a tooth normally contains channels called tubules that provide flow between the inner pulp region of the tooth and the outer root surface. The cause of tooth hypersensitivity may be related to demineralization, which results in increased tubule exposure and dentin permeability. The most common causes of demineralization of enamel or dentin are friction, abrasion, gum recession, and erosion. When the root surface is exposed, the dentinal tubules are also exposed.

[0004] The currently accepted theory for tooth hypersensitivity is the fluid dynamic theory, which is based on the idea that open, exposed dentinal tubules allow fluid to flow through the tubules. This flow stimulates nerve endings in the dental pulp. Clinical replicas of sensitive teeth viewed in a SEM (scanning electron microscope) show varying numbers of open or partially closed dentinal tubules.

[0005] Over the years, people have been trying to treat tooth hypersensitivity. One approach is to reduce the excitability of the nerves in sensitive teeth by using "nerve-depolarizing agents" containing strontium ions, potassium salts (such as potassium nitrate, potassium bicarbonate, potassium chloride, etc.). These nerve depolarizing agents work by interfering with the nerve conduction of painful stimuli to make the nerves less sensitive.

[0006] Another approach is to use "tubule blockers" that completely or partially occlude the tubules, such as polystyrene beads, apatite, polyacrylic acid, the mineral hectorite clay, etc. These tubule blockers work by physically blocking the exposed ends of the dentinal tubules, thereby reducing the movement of dentinal fluid and reducing the irritation associated with shear stress as described by fluid dynamic theory.

[0007] US 9,717,929 B2 (COLGATE-PALMOLIVE COMPANY) discloses an oral care composition for reducing tooth hypersensitivity, comprising an effective amount of a basic amino acid in free or salt form; and an effective amount of calcium silicate particles, wherein the calcium silicate particles have an average diameter of less than 5 microns, wherein the particles have a d50 of 2 to 5 μm and a d90 of 5 to 10 μm and a cumulative volume percentage of at least 50% at 3.95.

[0008] There remains a need to develop an oral care composition that is more effective in remineralizing teeth and / or preventing or reducing caries and / or sealing dentinal tubules to reduce tooth sensitivity. Summary of the invention

[0009] In a first aspect, the present invention relates to an oral care composition comprising:

[0010] a) uncharged polar amino acids;

[0011] b) charged polar amino acids;

[0012] c) a water-insoluble and / or slightly soluble calcium source;

[0013] wherein the amount of the calcium source to the total amount of the uncharged polar amino acid and the charged polar amino acid is present in a weight ratio (c:(a+b)) of 1:10 to 20:1; and

[0014] Wherein, based on the total weight of the composition, the composition comprises less than 0.005 wt % of other amino acids other than the uncharged polar amino acids and the charged polar amino acids.

[0015] In a second aspect, the present invention relates to a packaged oral care product comprising the oral care composition of the first aspect of the present invention.

[0016] In a third aspect, the present invention relates to a method for remineralizing a tooth of an individual and / or preventing or reducing dental caries of an individual and / or reducing the sensitivity of a tooth of an individual, comprising the step of applying a composition of any embodiment of the first aspect to at least one surface of a tooth of the individual. The method is preferably used for non-therapeutic benefits.

[0017] All other aspects of the invention will become more readily apparent by consideration of the following detailed description and examples. DETAILED DESCRIPTION

[0018] Except in the examples, or where otherwise explicitly indicated, all numbers in this description indicating amounts of material or reaction conditions, physical properties of materials and / or use may optionally be understood as modified by the word "about".

[0019] Unless otherwise indicated, all amounts are by weight of the final composition.It should be noted that in specifying any range of values, any particular upper value can be associated with any particular lower value.

[0020] For the avoidance of doubt, the word "comprising" is intended to mean "including" but not necessarily "consisting of" or "composed of." In other words, the listed steps or options do not have to be exhaustive.

[0021] The disclosure of the invention found herein is deemed to cover all embodiments found in the claims to be multiply dependent on each other, irrespective of the fact that the claims can be found without multiple dependency or redundancy.

[0022] Where features are disclosed with respect to a particular aspect of the invention (eg, a composition of the invention), such disclosure is also considered applicable, mutatis mutandis, to any other aspect of the invention (eg, a method of the invention).

[0023] For the purposes of the present invention, "soluble" and "insoluble" refer to the solubility of a source (e.g., a calcium source) in water at 25°C and atmospheric pressure. "Soluble" refers to a source that dissolves in water to give a solution with a concentration of at least 0.1 mol / liter. "Insoluble" refers to a source that dissolves in water to give a solution with a concentration of less than 0.001 mol / liter. Thus, "slightly soluble" is defined to mean a source that dissolves in water to give a solution with a concentration greater than 0.001 mol / liter and less than 0.1 mol / liter.

[0024] For purposes of the present invention, "remineralization" refers to the production of calcium phosphate on teeth in situ (i.e., in the oral cavity) to reduce tooth sensitivity, the potential for tooth decay, regenerate tooth enamel, and / or improve tooth appearance by whitening by producing this new calcium phosphate. Preferably, the new calcium phosphate layer on the teeth is 10 nm to 20 microns, more preferably 75 nm to 10 microns, and most preferably 150 nm to 5 microns thick, including all ranges subsumed therein.

[0025] Amino acids are organic molecules composed of a basic amino group (–NH2) and an acidic carboxyl group (–COOH) and an organic side chain that is unique to each amino acid. So far, 20 amino acids are known to exist in the standard genetic code, and others are found in a few bacteria (e.g., selenocysteine, pyrrolysine, ornithine). These 20 amino acids include alanine, arginine, asparagine, aspartic acid, cysteine, glutamine, glutamic acid, glycine, histidine, isoleucine, leucine, lysine, methionine, phenylalanine, proline, serine, threonine, tryptophan, tyrosine, and valine.

[0026] Amino acids can be divided into two groups: nonpolar amino acids and polar amino acids. Polar amino acids have hydrophilic side chains, which can be further divided into three groups: uncharged (neutral) polar amino acids, positively charged polar amino acids, and negatively charged polar amino acids.

[0027] Uncharged polar amino acids suitable for use in the present invention include, for example, serine, tyrosine, threonine, cysteine, asparagine, glutamine or a mixture thereof, preferably serine, tyrosine, cysteine ​​or a mixture thereof. Tyrosine is particularly preferred.

[0028] The composition preferably comprises 0.01 to 15 wt %, more preferably 0.1 to 10 wt %, even more preferably 0.5 to 8 wt % and most preferably 1 to 5 wt % of the composition of an uncharged polar amino acid, based on the total weight of the composition, and including all ranges subsumed therein.

[0029] Suitable positively charged polar amino acids include lysine, arginine, histidine, ornithine or a mixture thereof, preferably, the positively charged polar amino acid includes or is lysine. Suitable negatively charged polar amino acids include aspartic acid, glutamic acid or a mixture thereof, preferably, the negatively charged polar amino acid includes or is glutamic acid.

[0030] Preferably, the charged polar amino acid suitable for use in the present invention is a positively charged polar amino acid, which includes lysine, arginine, histidine, ornithine or a mixture thereof, more preferably lysine.

[0031] It is also preferred that the charged polar amino acid suitable for the present invention is a combination of a positively charged polar amino acid and a negatively charged polar amino acid. The combination preferably comprises a weight ratio of 10:1 to 1:20, more preferably 5:1 to 1:10 of positively charged polar amino acid and negatively charged polar amino acid.

[0032] In the composition, preferably, the charged polar amino acid is present in an amount of 0.01 to 15 wt %, more preferably 0.1 to 10 wt %, even more preferably 0.5 to 8 wt % and most preferably 1 to 5 wt % of the composition, based on the total weight of the composition, and including all ranges subsumed therein.

[0033] The weight ratio of uncharged polar amino acids to charged polar amino acids in the composition is preferably from 1:15 to 15:1, more preferably from 1:10 to 10:1 and most preferably from 1:5 to 5:1.

[0034] The total amount of uncharged polar amino acids and charged polar amino acids in the oral care composition is preferably from 0.1 to 20 wt %, more preferably from 1 to 15 wt %, even more preferably from 2 to 10 wt % and most preferably from 3 to 8 wt % of the composition, based on the total weight of the oral care composition, and including all ranges subsumed therein.

[0035] It is particularly preferred that the uncharged polar amino acid is tyrosine and the charged polar amino acid is lysine.

[0036] The oral care composition of the present invention is substantially free of other amino acids, except for the uncharged polar amino acids and charged polar amino acids contained in the composition. As used herein, "substantially free" means less than 0.005 wt%, preferably less than 0.001 wt%, more preferably less than 0.0005 wt%, even more preferably 0 to 0.0005 wt%, including all ranges contained therein, based on the total weight of the composition. Preferably, the composition of the present invention does not contain other amino acids, except for the uncharged polar amino acids and charged polar amino acids contained in the composition.

[0037] Water-insoluble and / or slightly soluble calcium sources suitable for use in the present invention are limited to the extent that they can be used in the mouth. Illustrative but non-limiting examples of water-insoluble and / or slightly soluble calcium sources that can be used in the present invention include, for example, calcium carbonate, hydroxyapatite, tricalcium phosphate, calcium-poor hydroxyapatite (Ca9(HPO4)(PO4)5OH), dicalcium phosphate, dehydrated dicalcium phosphate, octacalcium phosphate, tetracalcium phosphate, calcium glycerophosphate, calcium lactate, calcium aluminate, calcium oxalate, calcium oxide, carboxymethylcellulose calcium, calcium alginate, calcium hydroxide, calcium sulfate, calcium salts of citric acid, or mixtures thereof. Preferably, the water-insoluble and / or slightly soluble calcium source includes calcium carbonate, hydroxyapatite, tricalcium phosphate, or mixtures thereof. Hydroxyapatite is most preferred.

[0038] It is also preferred that the water-insoluble and / or slightly soluble calcium source comprises or is calcium carbonate. Preferably, the calcium carbonate has a D50 particle size of 5 microns or less, more preferably 0.01 to 3 microns and most preferably 0.01 to 1.5 microns. Suitable calcium carbonate is commercially available from Omya, for example, under the trade name OMYACARE HP 900OG.

[0039] Preferably, the water-insoluble and / or sparingly soluble calcium source is present in an amount of 0.1 to 60 wt %, more preferably 0.5 to 55 wt %, even more preferably 1 to 50 wt % and most preferably 3 to 40 wt % of the composition, based on the total weight of the composition, and including all ranges subsumed therein.

[0040] In the composition, the amount of calcium source to the total amount of uncharged polar amino acids and charged polar amino acids is present in a weight ratio of 1:10 to 20:1, preferably 1:5 to 15:1, more preferably 1:3 to 13:1, even more preferably 1:1 to 10:1, including all ratios subsumed therein.

[0041] The composition may include a phosphate source. Preferably, the phosphate source is dissolved in water to obtain a phosphate ion concentration of at least 0.1 mol / L at room temperature and atmospheric pressure. Illustrative examples of the types of phosphate sources suitable for use in the present invention include trisodium phosphate, monosodium phosphate, disodium hydrogen phosphate, ammonium phosphate, diammonium hydrogen phosphate, monoammonium phosphate, tripotassium phosphate, monopotassium phosphate, dipotassium hydrogen phosphate, mixtures thereof, and the like.

[0042] The phosphate source may be present in the range of 0.1 to 30 wt %, preferably 0.5 to 20 wt %, more preferably 1 to 15 wt % of the composition, based on the total weight of the composition, and including all ranges subsumed therein.

[0043] The calcium source and the phosphate source may be present in a weight ratio of 1:10 to 30:1, preferably 1:5 to 20:1, more preferably 1:3 to 15:1.

[0044] Preferably, the composition is an aqueous composition. The water content is at least 1.5 wt %, preferably at least 5 wt %, more preferably at least 10 wt % of the composition. Preferably, the water content is 1.5 to 95 wt %, more preferably 5 to 90 wt %, and most preferably 10 to 90 wt % of the composition, based on the total weight of the composition, and including all ranges subsumed therein.

[0045] Typically, the composition has a pH of 5.5 to 10.5, more preferably 6.0 to 10 and most preferably 6.5 to 9.0. When 5 parts by weight of the composition are uniformly dispersed and / or dissolved in 20 parts by weight of pure water at 25°C, the pH of the composition can be measured. Specifically, the pH can be measured by manually mixing 5 g of the composition with 20 mL of water for 30 seconds and then immediately testing the pH with an indicator or a pH meter. Alternatively, the pH of the composition can be directly measured with a pH meter.

[0046] The composition of the present invention may also include a physiologically acceptable carrier. The carrier preferably includes at least a surfactant, a thickener, a wetting agent or a combination thereof.

[0047] Preferably, the composition comprises a surfactant. Preferably, the composition comprises at least 0.01%, more preferably at least 0.1%, most preferably from 0.5 to 7% of a surfactant by weight of the composition. Suitable surfactants include anionic surfactants, such as C8-C 18 Sodium, magnesium, ammonium or ethanolamine salts of alkyl sulfates (e.g. sodium lauryl sulfate), C8-C 18 Sodium, magnesium, ammonium or ethanolamine salts of alkyl sulfosuccinates (e.g. sodium dioctyl sulfosuccinate), C8-C 18 Sodium, magnesium, ammonium or ethanolamine salts of alkyl sulfoacetates (e.g. sodium lauryl sulfoacetate), C8-C 18 Sodium, magnesium, ammonium or ethanolamine salts of alkyl sarcosinates (e.g. sodium lauryl sarcosinate), C8-C 18 The surfactants include sodium, magnesium, ammonium or ethanolamine salts of alkyl phosphates (which may optionally contain up to 10 ethylene oxide and / or propylene oxide units) and sulfated monoglycerides. Other suitable surfactants include nonionic surfactants, such as optionally polyethoxylated fatty acid sorbitan esters, ethoxylated fatty acids, esters of polyethylene glycol, ethoxylates of fatty acid monoglycerides and diglycerides, and ethylene oxide / propylene oxide block polymers. Other suitable surfactants include amphoteric surfactants, such as betaines or sulfobetaines. A mixture of any of the above materials can also be used. More preferably, the surfactant includes or is an anionic surfactant. Preferred anionic surfactants are sodium lauryl sulfate and / or sodium dodecylbenzene sulfonate. Most preferably, the surfactant is sodium lauryl sulfate, sodium cocosulfate, cocamidopropyl betaine, sodium methyl cocoyl taurate or a mixture thereof.

[0048] Thickeners may also be used in the present invention. Illustrative examples of the types of thickeners that may be used in the present invention include sodium carboxymethylcellulose (SCMC), hydroxyethylcellulose, methylcellulose, ethylcellulose, tragacanth, gum arabic, karaya gum, sodium alginate, carrageenan, guar gum, xanthan gum, Irish moss, starch, modified starch, silica-based thickeners including silica aerogels, magnesium aluminum silicate (e.g., Veegum), carbomer (cross-linked acrylates), and mixtures thereof.

[0049] Typically, xanthan gum and / or sodium carboxymethylcellulose and / or carbomer are preferred. When using carbomer, those with a weight average molecular weight of at least 700,000 are desired, and those with a molecular weight of at least 1,200,000 are preferred, and those with a molecular weight of at least about 2,500,000 are most preferred. Mixtures of carbomers may also be used herein.

[0050] In a particularly preferred embodiment, the carbomer is Synthalen PNC, Synthalen KP or a mixture thereof. It is described as a high molecular weight and cross-linked polyacrylic acid and is identified via CAS number 9063-87-0. These types of materials are commercially available from suppliers such as Sigma.

[0051] In another particularly preferred embodiment, the sodium carboxymethylcellulose (SCMC) used is SCMC 9H. It is described as a sodium salt of a cellulose derivative having carboxymethyl groups bonded to the hydroxyl groups of the glucopyranose backbone monomers and is identified via CAS number 9004-32-4. It is commercially available from suppliers such as Alfa Chem.

[0052] In another particularly preferred embodiment, the thickener is xanthan gum.

[0053] Thickeners generally comprise from 0.01 to about 10 wt %, more preferably from 0.1 to 9 wt %, most preferably from 0.1 to 5 wt %, of the composition based on the total weight of the composition, and including all ranges subsumed therein.

[0054] Suitable humectants are preferably used in the oral care compositions of the present invention, and include, for example, glycerol, sorbitol, propylene glycol, dipropylene glycol, diglycerol, triacetin, mineral oil, polyethylene glycol (preferably PEG-400), alkanediols such as butylene glycol and hexylene glycol, ethanol, pentylene glycol or mixtures thereof. Glycerol, polyethylene glycol, sorbitol or mixtures thereof are preferred humectants.

[0055] The wetting agent may be present in a range of 10 to 90 wt % based on the weight of the composition. More preferably, the carrier wetting agent comprises 25 to 80 wt %, most preferably 30 to 60 wt %, of the composition based on the total weight of the composition, and including all ranges contained therein.

[0056] The composition may include a fluoride source. Preferred fluoride sources include sodium fluoride, stannous fluoride, potassium fluoride, sodium monofluorophosphate, sodium fluorosilicate, ammonium fluorosilicate, amine fluoride, ammonium fluoride or a mixture thereof. Preferably, the fluoride source is stannous fluoride, sodium fluoride, sodium monofluorophosphate or a mixture thereof. Sodium monofluorophosphate is particularly preferred. Based on the gross weight of the composition, the fluoride source may be present at a level of 0.01% to 10% by weight of the composition, more preferably 0.03% to 5% by weight, and most preferably 0.1% to 2% by weight, and including all ranges contained therein.

[0057] The composition may include an abrasive, such as calcium carbonate, silicon dioxide and aluminum oxide. Based on the total weight of the composition, the abrasive may be present in a range of 0.01% to 60% by weight, more preferably 0.1% to 30% by weight, and most preferably 1% to 15% by weight of the composition, and including all ranges contained therein. When the abrasive is calcium carbonate, the total amount of water-insoluble and / or slightly soluble calcium source and calcium carbonate abrasive is preferably 0.1 to 60%, more preferably 0.5 to 55%, even more preferably 1 to 50%, most preferably 3 to 40%.

[0058] In addition to the amino acids contained in the composition, the composition of the present invention may contain a variety of other ingredients commonly used in the art to enhance physical properties and performance. These ingredients include sunscreens, colorants, antimicrobial agents, anti-inflammatory agents, anti-caries agents, plaque buffers, vitamins, plant extracts, desensitizers, anticalculus agents, biomolecules, spices, protein materials, preservatives, pH regulators, sweeteners, polymeric compounds, buffers and salts for buffering the pH and ionic strength of the composition, and mixtures thereof.

[0059] These ingredients generally collectively comprise less than 20% by weight of the composition, preferably from 0.0 to 15% by weight of the composition, most preferably from 0.01 to 12% by weight of the composition, and including all ranges subsumed therein.

[0060] The oral care composition of the present invention can be used in a method for remineralizing individual teeth and / or preventing or reducing individual caries and / or reducing the sensitivity of individual teeth. Preferably, the method is non-therapeutic. Additionally or alternatively, the present invention relates to an oral care composition for remineralizing individual teeth and / or preventing or reducing individual caries and / or reducing the sensitivity of individual teeth. Additionally or alternatively, the present invention relates to the use of an oral care composition for remineralizing individual teeth and / or preventing or reducing individual caries and / or reducing the sensitivity of individual teeth, which use is preferably non-therapeutic. Additionally or alternatively, the present invention relates to the use of an oral care composition in the manufacture of a medicament for remineralizing individual teeth and / or preventing or reducing individual caries and / or reducing the sensitivity of individual teeth.

[0061] Oral care composition can be any form common in the art. Preferred forms are dentifrice, toothpaste, gel, mouthwash, medicine, oral film, slurry, chewing gum and lozenge, more preferably toothpaste or gel. When the oral care composition is toothpaste or gel, it usually has a viscosity of about 30,000 to 180,000 mPa.s (centipoise), and preferably 60,000 to 170,000 mPa.s (centipoise), and most preferably 65,000 to 165,000 mPa.s (centipoise), the viscosity is obtained at room temperature (25 ° C) with a Brookfield viscometer (spindle number 93 / 94) at a speed of 5 rpm for 1 minute. Usually the composition will be packaged. The composition can be packaged in conventional plastic laminates, metal tubes or single-chamber dispensers in the form of toothpaste or gel. It can be applied to the tooth surface by any physical means, such as a toothbrush, fingertips or by an applicator directly to sensitive areas. The composition may be packaged as a liquid mouthwash in a bottle, sachet or other convenient container.

[0062] The composition can be effective even when used in an individual's daily oral hygiene routine. For example, the composition can be brushed onto the teeth. The composition can, for example, be in contact with the teeth for a period of 1 second to 20 hours. More preferably, 1 second to 10 hours, even more preferably 10 seconds to 1 hour, and most preferably 30 seconds to 5 minutes. The composition can be used daily, for example, once, twice, or three times per day by an individual.

[0063] The following examples are provided to facilitate the understanding of the present invention. These examples are not provided to limit the scope of the claims.

[0064] Example

[0065] Example 1

[0066] The compositions were prepared as shown in Table 1. All ingredients are expressed as weight percent of the total formulation.

[0067] Table 1

[0068]

[0069] a. Available from Omya International AG under the trade name HP 900-OG is commercially available micro chalk (CaCO3) with a particle size of 0.85 microns.

[0070] b. Hydroxyapatite C73-08, commercially available from Budenheim, Co., Germany.

[0071] method

[0072] Brushing solution

[0073] To evaluate the effect of sealing dentinal tubules, fresh slurries were prepared by mixing toothpaste with deionized (DI) water or sodium phosphate solution for 40 seconds and used immediately.

[0074] Human dentin discs were etched with 6% citric acid for 2 minutes, and then they were treated with different slurries by brushing according to the same protocol. 16 human dentin discs were divided into 8 groups (n=2). The dentin discs were brushed with slurry under a toothbrush-equipped brushing machine. The load of brushing was 170g+ / -5g, and the automatic brushing was operated at a speed of 150rpm. After brushing for 1 minute, the dentin disc was soaked in the slurry for 1 minute. The dentin disc was then placed in 50mL DI water and stirred for 10 strokes at 150rpm on a flat oscillator. The disc was then soaked in simulated oral fluid (SOF) for at least 6 hours under 37°C and 60.0rpm shaking water bath conditions. Afterwards, the dentin disc was brushed with slurry by machine using the same procedure as in the first step. Brushing was repeated 2 times in one day, and then the dentin disc was kept overnight (>12 hours) in SOF in a shaking water bath at 37°C to simulate the oral environment. After 3 days of brushing, the dentin samples were characterized using a scanning electron microscope (SEM, Hitachi S-4800, Japan).

[0075] Prepare simulated oral fluid by combining the ingredients in Table 2:

[0076] Table 2

[0077] Element Amount / g NaCl 16.07 <![CDATA[NaHCO3]]> 0.7 KCl 0.448 <![CDATA[K2HPO4·3H2O]]> 3.27 <![CDATA[MgCl2·6H2O]]> 0.0622 1M HCl 40mL <![CDATA[CaCl2]]> 0.1998 <![CDATA[Na2SO4]]> 0.1434 Buffer Adjust pH to 7.0 water Remaining volume up to 2L

[0078] Scoring criteria for tubule closure

[0079] Regardless of the original shape of the dentin disc, a square (having a size of 4 mm × 4 mm) was selected and an image was captured at 30x magnification. Within the square, 5 points (each having a size of 150 μm × 150 μm, one in the middle and one in each corner) were selected and observed at 1000x magnification. The closure of the tubules was evaluated according to the criteria described in Table 3. Two dentin discs of each test group were measured.

[0080] Table 3

[0081] score Tubule closure 0 All dentinal tubules are open. 1 <20% of dentinal tubules are completely occluded. 2 Between 20% and 50% of the dentinal tubules are completely occluded. 3 Between 50% and 80% of the dentinal tubules are completely occluded. 4 Between 80% and 100% of the dentinal tubules are completely occluded. 5 All dentinal tubules were completely occluded.

[0082] result

[0083] SEM images of the dentin disks were taken 3 days after brushing. The images were analyzed and scored. The results are reported in Table 4.

[0084] Table 4

[0085]

[0086] From the results, it can be seen that after 3 days of brushing, Sample 4 according to the present invention provides better tubule sealing efficacy than Sample 3 containing only calcium carbonate. Similarly, Sample 6 according to the present invention provides better tubule sealing efficacy than Sample 5.

[0087] It can also be seen from the results that Sample 6 according to the present invention provides better tubule sealing efficacy than Sample 7 containing only the uncharged polar amino acid tyrosine and Sample 8 containing only the charged polar amino acid lysine.

Claims

1. An oral care composition comprising: a) uncharged polar amino acids; b) charged polar amino acids; c) a water-insoluble and / or slightly soluble calcium source; wherein the amount of the calcium source to the total amount of the uncharged polar amino acid and the charged polar amino acid is present in a weight ratio (c:(a+b)) of 1:10 to 20:1; and Wherein, based on the total weight of the composition, in addition to the uncharged polar amino acid and the charged polar amino acid, the composition comprises less than 0.005 wt % of other amino acids.

2. An oral care composition according to claim 1, wherein the amount of calcium source to the total amount of uncharged polar amino acids and charged polar amino acids is present in a weight ratio of 1:5 to 15:1, preferably 1:3 to 13:

1.

3. An oral care composition according to claim 1 or claim 2, wherein the total amount of uncharged polar amino acids and charged polar amino acids in the composition is from 0.1% to 20%, preferably from 1% to 15%.

4. An oral care composition according to any one of the preceding claims, wherein the uncharged polar amino acid and the charged polar amino acid are present in the composition in a weight ratio of 1:15 to 15:1, preferably 1:10 to 10:

1.

5. The oral care composition according to any one of the preceding claims, wherein the uncharged polar amino acid comprises serine, tyrosine, threonine, cysteine, asparagine, glutamine or a mixture thereof, preferably serine, tyrosine, cysteine ​​or a mixture thereof, more preferably tyrosine.

6. An oral care composition according to any one of the preceding claims, wherein the charged polar amino acid is a combination of a positively charged polar amino acid and a negatively charged polar amino acid.

7. The oral care composition according to claim 6, wherein the positively charged polar amino acid comprises lysine, arginine, histidine, ornithine or a mixture thereof, preferably lysine.

8. The oral care composition according to claim 6, wherein the negatively charged polar amino acid comprises aspartic acid, glutamic acid or a mixture thereof, preferably glutamic acid.

9. The oral care composition according to any one of claims 1 to 5, wherein the charged polar amino acid is a positively charged polar amino acid, and the positively charged polar amino acid comprises lysine, arginine, histidine, ornithine or a mixture thereof, preferably lysine.

10. An oral care composition according to any preceding claim, wherein the uncharged polar amino acid is tyrosine and the charged polar amino acid is lysine.

11. An oral care composition according to any one of the preceding claims, wherein the water-insoluble and / or slightly soluble calcium source comprises calcium carbonate, hydroxyapatite, tricalcium phosphate, calcium-poor hydroxyapatite (Ca9(HPO4)(PO4)5OH), dicalcium phosphate, dehydrated dicalcium phosphate, octacalcium phosphate, tetracalcium phosphate, calcium glycerophosphate, calcium lactate, calcium aluminate, calcium oxalate, calcium oxide, carboxymethylcellulose calcium, calcium alginate, calcium hydroxide, calcium sulfate, calcium salt of citric acid or a mixture thereof, preferably calcium carbonate, hydroxyapatite, tricalcium phosphate or a mixture thereof.

12. An oral care composition according to any preceding claim, wherein the water-insoluble and / or sparingly soluble calcium source is present in an amount of 0.1 to 60 wt%, preferably 0.5 to 55 wt%, of the composition.

13. An oral care composition according to any preceding claim, wherein the composition additionally comprises a phosphate source.

14. An oral care composition according to any preceding claim, wherein the composition is an aqueous composition.

15. Method for remineralizing teeth of an individual and / or preventing or reducing dental caries and / or reducing the sensitivity of teeth of an individual, comprising the step of applying a composition according to any one of the preceding claims to at least one surface of a tooth of the individual.

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