Oral care composition

Abstract

Disclosed is an oral care composition comprising tetracalcium phosphate and a water soluble calcium source; wherein the water soluble calcium source comprises calcium chloride, calcium nitrate, calcium acetate, calcium lactate, calcium formate, calcium malate, calcium propionate, calcium butyrate, calcium bicarbonate, calcium glycerophosphate, calcium gluconate, calcium ascorbate, calcium glycinate, or mixtures thereof; and wherein the composition is an aqueous composition and the water content is at least 5% by weight of the composition.

Description

Technical Field

[0001] This invention relates to an oral care composition comprising tetracalcium phosphate and a water-soluble calcium source. The invention also relates to a method for remineralizing and / or reducing sensitivity and / or combating tooth erosion or caries by applying such a composition to an individual's oral cavity. Background Technology

[0002] Tooth erosion, cavities, and tooth sensitivity are common problems that can significantly impact oral health and quality of life. These dental issues are of great concern to consumers worldwide. Teeth consist of dentin, which is covered by a layer of enamel. Teeth face constant threats from chemical and physical forces, such as acids produced by bacteria and mechanical abrasion, leading to demineralization and weakening of the enamel and the underlying dentin. Enamel is composed of hydroxyapatite crystals, forming a porous surface. Tooth erosion begins in the enamel and can progress to the underlying dentin. It is important to prevent or slow down enamel erosion to maintain good oral health. Fluoride is commonly used in oral care products to combat tooth erosion or cavities. The resulting fluorapatite composition is harder and more resistant to acid erosion than the original hydroxyapatite composition.

[0003] Tooth hypersensitivity is a common dental condition characterized by sharp pain or discomfort in response to various stimuli such as hot or cold temperatures, sweet or acidic foods, or mechanical pressure. Tooth hypersensitivity occurs when the underlying dentin is exposed due to enamel erosion, gingival recession, or caries. The dentin of a tooth typically contains channels called tubules, which provide permeable flow between the internal pulp region of the tooth and the external root surface. When the root surface is exposed, the dentinal tubules are also exposed.

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

[0005] For many years, efforts have been made to treat tooth hypersensitivity. One approach involves using "nerve depolarizers" that contain strontium ions, potassium salts such as potassium nitrate, potassium bicarbonate, and potassium chloride to reduce the excitability of nerves in sensitive teeth. These nerve depolarizers work by interfering with the nerve conduction of painful stimuli, making the nerves less sensitive.

[0006] Another approach is to use "tubular sealants" that completely or partially block the tubules, such as polystyrene beads, apatite, polyacrylic acid, mineral lithium montmorillonite clay, etc. These tubular sealants work by physically sealing the exposed ends of the exposed dentinal tubules, thereby reducing dentin fluid flow and reducing stimulation associated with shear stress as described in fluid dynamics theory.

[0007] There is still a need for an improved oral care composition that can effectively remineralize tooth enamel and dentin, reduce tooth sensitivity, and combat tooth erosion or caries in individuals who require it. Summary of the Invention

[0008] In a first aspect, the present invention relates to an oral care composition comprising: a) Tetracalcium phosphate; b) Water-soluble calcium source; The water-soluble calcium source described herein comprises calcium chloride, calcium nitrate, calcium acetate, calcium lactate, calcium formate, calcium malate, calcium propionate, calcium butyrate, calcium bicarbonate, calcium glycerophosphate, calcium gluconate, calcium ascorbate, calcium glycinate, or mixtures thereof; and The composition is an aqueous composition, and the water content is at least 5% by weight of the composition.

[0009] 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.

[0010] In a third aspect, the present invention relates to a method for remineralizing and / or reducing sensitivity of an individual's teeth and / or combating tooth erosion or caries, comprising the step of applying a composition of any embodiment of the first aspect to the individual's oral cavity. The method is preferably for non-therapeutic benefits. In the context of this invention, the term "combating tooth erosion or caries" means preventing, inhibiting, reducing, and / or treating tooth erosion or caries.

[0011] All other aspects of the invention will become more readily apparent after considering the following detailed description and examples. Invention Details Unless explicitly stated in the examples or otherwise, all figures indicating the amount of material or reaction conditions, physical properties of the material and / or uses in this specification may optionally be understood to be modified by the word “about”.

[0013] Unless otherwise stated, all quantities are weight percentages of the final composition. It should be noted that when specifying any numerical range, any particular upper limit may be associated with any particular lower limit.

[0014] To avoid any doubt, the word "contains" is intended to mean "including," but not necessarily "composed of" or "consisting of." In other words, the steps or options listed do not need to be exhaustive.

[0015] The disclosure of this invention herein should be considered to cover all embodiments in which the claims are mutually dependent, regardless of whether the claims may be found to have no multiple dependent or redundant relationships.

[0016] When a feature is disclosed with respect to a specific aspect of the invention (e.g., a composition of the invention), such disclosure should also be considered applicable to any other aspect of the invention (e.g., a method of the invention) with the necessary modifications.

[0017] In the context of this invention, the term "remineralization" means the in-situ generation of calcium phosphate on teeth in the oral cavity to reduce the likelihood of tooth sensitivity, reduce tooth decay, regenerate enamel, and / or improve tooth appearance by whitening through the generation of such new calcium phosphate. Preferably, the thickness of the new calcium phosphate layer on the teeth is 10 nanometers to 20 micrometers, more preferably 75 nanometers to 10 micrometers, and most preferably 150 nanometers to 5 micrometers, including all of the ranges contained herein.

[0018] In the context of this invention, the term "oral care composition" refers to a composition delivered to the oral cavity surface. The composition may be a product that, during normal use, is not intended for systemic administration or intentional swallowing, but rather remains in the oral cavity for a sufficient time to contact substantially all tooth surfaces and / or oral tissues for oral activity purposes.

[0019] Examples of oral compositions include toothpaste or dental floss, mouthwash or mouthwash liquid, powder (e.g., tooth powder), tablets, mints, creams, strips or chewing gum (e.g., chewing gum), films, topical oral gels, oral serums, and denture cleaners. Typically, these compositions can be packaged. In toothpaste or gel form, the compositions may be packaged in conventional plastic laminated tubes, metal tubes, or single-compartment dispensers. These toothpaste or gel forms can be applied to the tooth surface by any physical means, such as a toothbrush, fingertips, or direct application to sensitive areas via an applicator. In liquid mouthwash form, the compositions may be packaged in bottles, sachets, or other convenient containers.

[0020] The compositions of the present invention are preferably used for cleaning oral surfaces. Therefore, the preferred product forms of the compositions of the present invention are those suitable for brushing and / or rinsing oral surfaces.

[0021] The compositions of the present invention are most preferably in the form of a dental floss or toothpaste. In the context of this invention, the term "dental floss" refers to an oral composition for cleaning the surfaces of the oral cavity. Such compositions are not intentionally swallowed for the purpose of systemic administration of a therapeutic agent, but are applied to the oral cavity for treatment and then spat out. Typically, such compositions are used in conjunction with a cleaning tool such as a toothbrush, usually by applying them to the bristles of the toothbrush and then brushing the accessible surfaces of the oral cavity. In the context of this invention, the term "toothpaste" means a paste or gel-like dental floss for use with a cleaning tool such as a toothbrush. Preferably, the dental floss / toothpaste is in a squeezeable semi-solid form, such as a cream, paste, or gel (or mixtures thereof).

[0022] Tetracalcium phosphate is an inorganic compound with the formula Ca4(PO4)2O, also known by the mineral name Hilgenstockite. Tetracalcium phosphate can be prepared by heating calcium hydroxide and calcium hydrogen phosphate dihydrate at high temperatures, or by reacting calcium oxide with phosphoric acid.

[0023] The oral care composition of the present invention preferably contains 0.1 to 80% by weight of tetracalcium phosphate based on the total weight of the oral care composition, more preferably 0.5 to 50%, even more preferably 1 to 30%, and most preferably 1.5 to 20%, including all of the ranges contained herein.

[0024] The water-soluble calcium sources applicable to this invention are limited only to their oral use. In the context of this invention, the term "water-soluble" means a source that dissolves in water to provide a concentration of at least 0.1 mol / L.

[0025] Examples of suitable water-soluble calcium sources include, but are not limited to, calcium chloride, calcium nitrate, calcium acetate, calcium lactate, calcium formate, calcium malate, calcium propionate, calcium butyrate, calcium bicarbonate, calcium glycerophosphate, calcium gluconate, calcium ascorbate, calcium glycinate, or mixtures thereof. Preferably, the water-soluble calcium source is calcium chloride, calcium nitrate, calcium glycinate, calcium glycerophosphate, calcium gluconate, or mixtures thereof. More preferably, the water-soluble calcium source is calcium glycinate, calcium glycerophosphate, calcium gluconate, or mixtures thereof.

[0026] The oral care composition of the present invention preferably contains 0.001 to 20% by weight of a water-soluble calcium source based on the total weight of the oral care composition, more preferably 0.01 to 15%, even more preferably 0.05 to 10%, and most preferably 0.1 to 5%, including all of the ranges contained herein.

[0027] Preferably, tetracalcium phosphate and a water-soluble calcium source are present in the oral care composition in a weight ratio of 1:20 to 80:1, more preferably 1:10 to 50:1, and most preferably 1:1 to 40:1.

[0028] The composition may comprise a phosphate source. The phosphate source provides phosphate ions to react with a calcium source to produce the in-situ reaction product calcium phosphate, a precursor for hydroxyapatite formation. Preferably, the phosphate source is dissolved in water at room temperature and atmospheric pressure to provide a phosphate ion concentration of at least 0.1 mol / L. Examples of phosphate sources suitable for this invention include trisodium phosphate, sodium dihydrogen phosphate, disodium hydrogen phosphate, ammonium phosphate, diammonium hydrogen phosphate, ammonium dihydrogen phosphate, tripotassium phosphate, potassium dihydrogen phosphate, dipotassium hydrogen phosphate, mixtures thereof, etc.

[0029] The phosphate source may be present in an amount ranging from 0.1% to 30%, preferably 0.5% to 20%, more preferably 1% to 15% by weight of the total composition, including all of the ranges contained herein.

[0030] The composition is an aqueous composition. The water content is at least 1.5% by weight of the composition, preferably at least 5%, more preferably at least 10%, even more preferably at least 15%, and most preferably at least 20%. Preferably, the water content is from 1.5% to 95% by weight of the composition, more preferably from 5% to 80%, even more preferably from 10% to 60%, still more preferably from 15% to 50%, and most preferably from 20% to 40%, based on the total weight of the composition, including all ranges contained therein.

[0031] Typically, the pH of the composition is from 5.5 to 10.5, more preferably from 6.0 to 10, and most preferably from 6.5 to 9.5. The pH of the composition can be measured 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. In particular, 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 pH meter, or the pH of the composition can be measured directly with a pH meter.

[0032] The compositions of the present invention may also contain a physiologically acceptable carrier. The carrier preferably contains at least a surfactant, a thickener, a humectant, or a combination thereof.

[0033] Preferably, the composition comprises a surfactant. More preferably, the composition comprises at least 0.01% surfactant based on the weight of the composition, more preferably at least 0.1%, and most preferably from 0.5% to 7%. Suitable surfactants include anionic surfactants, such as sodium, magnesium, ammonium, or ethanolamine salts of the following: C8 to C999. 18 Alkyl sulfates (e.g., sodium lauryl sulfate), C8 to C 18 Alkyl sulfosuccinates (e.g., sodium dioctyl sulfosuccinate), C8 to C 18 Alkyl sulfonates (e.g., sodium lauryl sulfonate), C8 to C 18 Alkyl sarcosine salts (e.g., sodium lauryl sarcosine), C8 to C 18Alkyl 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 dehydrated sorbitan esters, ethoxylated fatty acids, esters of polyethylene glycol, ethoxylated monoglycerides and diglycerides of fatty acids, and ethylene oxide / propylene oxide block polymers. Other suitable surfactants include amphoteric surfactants, such as betaine or sulfobetaine. Mixtures of any of the above materials may also be used. More preferably, the surfactant comprises 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 cocoyl sulfate, cocamidopropyl betaine, sodium methyl cocoyl taurate, or mixtures thereof.

[0034] Thickeners may also be used in this invention. Illustrative examples of types of thickeners that may be used in this invention include sodium carboxymethyl cellulose (SCMC), hydroxyethyl cellulose, methyl cellulose, ethyl cellulose, tragacanth gum, gum arabic, ark tartar 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 (crosslinked acrylates), and mixtures thereof.

[0035] Typically, xanthan gum and / or sodium carboxymethyl cellulose and / or carbomer are preferred. When using carbomer, those with a weight-average molecular weight of at least 700,000 are desirable, and those with a molecular weight of at least 1,200,000 are preferred, with those having a molecular weight of at least about 2,500,000 being most preferred. Mixtures of carbomer may also be used herein.

[0036] In a preferred embodiment, the carbomer is Synthalen PNC, Synthalen KP, or a mixture thereof. It is described as high molecular weight crosslinked polyacrylic acid and identified by CAS number 9063-87-0. These types of materials are commercially available from suppliers such as Sigma.

[0037] In another preferred embodiment, the sodium carboxymethyl cellulose (SCMC) used is SCMC 9H. It is described as a sodium salt of a cellulose derivative having a carboxymethyl group bonded to the hydroxyl group of the pyranose backbone monomer, and is identified by CAS number 9004-32-4. It is available from suppliers such as Alfa Chem.

[0038] In another preferred embodiment, the thickener is xanthan gum.

[0039] In another particularly preferred embodiment, the thickener is carrageenan. Suitable carrageenan includes ι-carrageenan and κ-carrageenan. Preferably, ι-carrageenan and κ-carrageenan are present in a weight ratio of 1:2 to 2:1. Preferably, the carrageenan present in the composition of the present invention consists of 33 to 66% by weight of ι-carrageenan and 33 to 66% by weight of κ-carrageenan. The total level of carrageenan is preferably 0.05 to 1% by weight of the composition, more preferably 0.08 to 0.5%, and most preferably 0.08 to 0.25%. ι-carrageenan or κ-carrageenan is commercially available, for example from CP Kelco.

[0040] The thickener preferably comprises 0.01 to 10% of the weight of the composition, more preferably 0.1 to 9%, and most preferably 0.1 to 5%, based on the total weight of the composition, including all ranges contained therein.

[0041] Suitable humectants are preferably used in the oral care compositions of the present invention, and they include, for example, glycerin, sorbitol, propylene glycol, dipropylene glycol, diglycerin, triacetyl, mineral oil, polyethylene glycol (preferably PEG-400), alkyl diols such as butylene glycol and hexanediol, ethanol, pentanediol, or mixtures thereof. Glycerin, polyethylene glycol, sorbitol, or mixtures thereof are preferred humectants.

[0042] The humectant may be present in an amount of 10 to 90% by weight of the composition. More preferably, the carrier humectant accounts for 25 to 80% by weight of the composition, most preferably 30 to 60%, based on the total weight of the composition, including all ranges contained therein.

[0043] The composition may contain a fluoride source. Preferred fluoride sources include sodium fluoride, stannous fluoride, potassium fluoride, sodium monofluorophosphate, sodium fluorosilicate, ammonium fluorosilicate, amine fluoride, ammonium fluoride, or mixtures thereof. Preferably, the fluoride source is stannous fluoride, sodium fluoride, sodium monofluorophosphate, or mixtures thereof. Sodium monofluorophosphate is particularly preferred. The fluoride source may be present in an amount of 0.01 to 10%, more preferably 0.03 to 5%, and most preferably 0.1 to 2% by weight of the total composition, including all ranges contained herein.

[0044] The composition may contain particulate abrasive materials, such as silica, alumina, calcium carbonate, trimetaphosphate, insoluble hexametaphosphate, etc., including agglomerated particulate abrasive materials. The abrasive may be present in an amount ranging from 0.01% to 60% by weight of the total composition, more preferably from 0.1% to 30%, and most preferably from 1% to 15% by weight, including all of the ranges contained herein.

[0045] Preferably, the composition (particularly toothpaste) comprises a silica-based abrasive. The preferred abrasive silica used in this invention is silica with a low refractive index. It can be used as the sole abrasive silica, or in combination with other abrasive silicas at low levels, such as those according to EP 236070. The low refractive index silica used as an abrasive in this invention is preferably silica with an apparent refractive index (RI) in the range of 1.41 to 1.47, preferably 1.435 to 1.445, and preferably has a weight average particle size between 5 and 15 mm and a particle size between 10 and 100 μm. 2 BET (nitrogen) surface area between / g and 70 to 150 cm² 3 Oil absorption per 100 g is required, but triboidal silica with a lower apparent refractive index can also be used. Typical examples of suitable low-refractive-index triboidal silica (e.g., RI between 1.435 and 1.445) are Tixosil 63 and 73 from Rhone Poulenc; Sident 10 from Degussa; Zeodent 113 from Zeofinn; Zeodent 124 and Zeodent 120 from Evonik; and Sorbosil AC 77 (RI approximately 1.440) from PQ Corporation. These silicas are typically present in amounts of 5 to 60% by weight in the composition, and typically 5 to 20% by weight.

[0046] In another preferred embodiment, the composition comprises a calcium carbonate abrasive. Natural calcium carbonate abrasives are typically finely ground limestone, which may optionally be refined or partially refined to remove impurities. The material preferably has an average particle size of less than 10 micrometers, for example 3-7 micrometers, such as about 5.5 micrometers. For example, small-particle silica may have an average particle size (D50) of 2.5-4.5 micrometers. Because natural calcium carbonate may contain a high proportion of relatively large d particles that are not carefully controlled, this can unacceptably increase friction; preferably no more than 0.01%, preferably no more than 0.004% by weight of particles cannot pass through a 325-mesh sieve. This material has a strong crystalline structure and is therefore much harder and more abrasive than precipitated calcium carbonate. The tap density of natural calcium carbonate is, for example, between 1 and 1.5 g / cc, for example about 1.2, such as about 1.19 g / cc. Natural calcium carbonate has various polymorphs, such as calcite, aragonite, and spherulite, with calcite being preferred for the purposes of this invention.

[0047] Precipitated calcium carbonate has a different crystal structure than natural calcium carbonate. It is generally more brittle and porous, thus exhibiting lower friction and higher water absorption. In the present invention, the particles are small, for example, with an average particle size of 1-5 micrometers, and for example, no more than 0.1%, preferably no more than 0.05% by weight, of the particles cannot pass through a 325-mesh sieve. The particles may, for example, have a D50 of 3-6 micrometers, such as 3.8-4.9 micrometers, for example, about 4.3 micrometers; a D50 of 1-4 micrometers, such as 2.2-2.6 micrometers, for example, about 2.4 micrometers; and a D10 of 1-2 micrometers, such as 1.2-1.4, for example, about 1.3 micrometers. The particles have relatively high water absorption, for example, at least 25 g / 100 g, for example, 30-70 g / 100 g.

[0048] The composition may contain a water-soluble or slightly water-soluble metal salt source, preferably a zinc source. Examples of suitable zinc sources include zinc chloride, zinc acetate, zinc gluconate, zinc sulfate, zinc fluoride, zinc citrate, zinc lactate, zinc oxide, zinc monoglyceride, zinc tartrate, zinc pyrophosphate, zinc maleate, or mixtures thereof; stannous sources such as stannous fluoride and stannous chloride are also preferred.

[0049] The composition may contain a polymer deposition aid. Preferably, the composition contains an anhydride polymer, particularly preferably a copolymer of maleic anhydride and methyl vinyl ether, wherein the anhydride moiety may be in a partially or completely hydrolyzed or alcoholic form. Preferred copolymers include Gantrez® polymers, for example: Gantrez S-95: Molecular weight 216,000; Free acid; Gantrez S-96: Molecular weight 700,000; Free acid; Gantrez S-97: Molecular weight 1,500,000; Free acid; and Gantrez MS-955: Molecular weight 1,060,000; Calcium / sodium salt.

[0050] A particularly preferred maleic acid and methyl vinyl ether copolymer has a molecular weight of 1,000,000 or greater, and a particularly preferred material is Gantrez S-97.

[0051] The composition may contain a teeth whitening agent. The whitening agent preferably contains green and / or blue pigments. In the context of this invention, pigment is generally understood as a hue / material that is insoluble in the relevant medium at a relevant temperature. This is the opposite of a soluble dye. In the context of this invention, "relevant medium" is a liquid medium in which the composition is used during brushing at an oral temperature of up to 37 degrees Celsius, i.e., human saliva. As a reasonable approximation, the relevant medium may be considered as water, and the relevant temperature may be considered as 25 degrees Celsius.

[0052] Preferably, the blue pigment is Pigment Blue 15, more preferably Pigment Blue 15:1, 15:2, 15:3, 15:4, 15:5 or 15:6, and most preferably 15:1. The preferred pigment is a blue pigment of phthalocyanine, CI No. 74160, Blue Covarine.

[0053] The preferred green pigment is phthalocyanine green, with phthalocyanine green CI-74260 being the most preferred.

[0054] Preferably, the total level of pigment in the composition is 0.01 to 3% of the weight of the composition, more preferably 0.02 to 2%.

[0055] The composition may comprise an oral care enzyme system, such as a hydrogen peroxide generating enzyme system (e.g., the oxidoreductase glucose oxidase), amylase, glucanase and / or polysaccharidease (optionally in the presence of a zinc ion providing compound and / or an 8-hydroxyquinoline derivative), lactoperoxidase, lactoferrin, lysozyme and mixtures thereof. A mixture of any of the above materials may also be used.

[0056] In addition to the specified components mentioned above, the compositions of the present invention may contain a variety of other components commonly found in the art to enhance physical properties and performance, such as: Antimicrobial agents, such as chlorhexidine, sanguisorbin extract, metronidazole, quaternary ammonium compounds such as cetylpyridinium chloride; cetylpyridinium chloride clay complex biguanides, such as chlorhexidine digluconate, hexamidine, oteninidine, alexiconidine; and halogenated bisphenol compounds, such as 2,2'-methylenebis-(4-chloro-6-bromophenol); Anti-inflammatory agents, such as ibuprofen, flurbiprofen, aspirin, indomethacin, etc. Anti-caries agents, such as sodium fluoride and stannous fluoride, amine fluoride, sodium monofluorophosphate, sodium tripolyphosphate and casein; Dental plaque buffers, such as urea, calcium lactate, calcium glycerophosphate, and strontium polyacrylate; Vitamins, such as vitamins A, C, D, B (preferably B3) and E; Plant extracts; Antioxidants that can be derived from plants, such as flavonoids, catechins, polyphenols and tannins, and mixtures thereof; Desensitizing agents, such as potassium citrate, potassium chloride, potassium tartrate, potassium bicarbonate, potassium oxalate, potassium nitrate, and strontium salts; Anti-tartar agents, such as alkali metal pyrophosphates, hypophosphite-containing polymers, organophosphonates, and phosphate citrates; Biomolecules, such as bacteriocins, antibodies, and enzymes; Spices, such as peppermint oil and spearmint oil; Protein materials, such as collagen; preservative; Sunscreen; Hyaluronic acid; Amino acids, such as arginine; Colorant; pH adjuster; Sweeteners; Flavoring agents; Polymer compounds that can enhance the delivery of active ingredients, such as antimicrobial agents, may also be included; Buffers and salts to buffer the pH and ionic strength of the oral care composition; and Other optional ingredients may include bleaching agents, peroxides such as potassium peroxybisphosphate, effervescent systems such as sodium bicarbonate / citric acid systems, color-changing systems, etc.

[0057] Such components typically and generally constitute less than 20% by weight of the composition, preferably 0.0 to 15% by weight, most preferably 0.01 to 12% by weight, including all ranges contained herein.

[0058] The oral care composition of the present invention can be used in methods for remineralizing and / or reducing sensitivity of individual teeth and / or combating tooth erosion or caries. The method includes applying the oral care composition of the present invention to the oral cavity of an individual in need, for example by brushing, for example once or more daily. Preferably, the method is non-therapeutic.

[0059] Additionally or alternatively, the present invention relates to oral care compositions for remineralizing and / or reducing sensitivity of individual teeth and / or combating tooth erosion or caries. Additionally or alternatively, the present invention relates to the use of oral care compositions for remineralizing and / or reducing sensitivity of individual teeth and / or combating tooth erosion or caries, said use preferably being non-therapeutic. Additionally or alternatively, the present invention relates to the use of oral care compositions in the preparation of medicaments for remineralizing and / or reducing sensitivity of individual teeth and / or combating tooth erosion or caries.

[0060] Additionally, applying the compositions of the present invention to an individual's oral cavity may provide one or more of the following benefits: reduced plaque buildup; inhibition of oral microbial biofilm formation; reduction or inhibition of gingivitis; promotion of healing of sores or incisions in the oral cavity; reduction of acid-producing bacteria levels; increase of the relative levels of non-cariogenic and / or non-plaque-forming bacteria; reduction, repair, or inhibition of early enamel caries; treatment, relief, or reduction of dry mouth; cleaning of teeth and the oral cavity; reduction of erosion; whitening of teeth; reduction of tartar buildup; and / or promotion of overall health, including cardiovascular health, for example by reducing the likelihood of systemic infections via oral tissues. This disclosure also provides compositions for any of the above methods.

[0061] The composition can be effective even when used as part of an individual's routine daily oral hygiene practices. For example, the composition can be brushed onto teeth. The composition can be in contact with teeth for a period of time, for example, from 1 second to 20 hours. More preferably, from 1 second to 10 hours, even more preferably from 10 seconds to 1 hour, and most preferably from 30 seconds to 5 minutes. The composition can be used daily, for example, by an individual once, twice, or three times a day.

[0062] The following examples are provided to facilitate understanding of the invention. These examples are not intended to limit the scope of the claims. Detailed Implementation

[0063] Example Example 1 This example demonstrates the sealing of dentinal tubules. The composition was prepared as shown in Table 1. All components are expressed as total amounts of the formulation and as levels of the active ingredient.

[0064] Table 1

[0065] method Fresh toothpaste slurry is prepared by mixing a toothpaste sample with water and used immediately.

[0066] Human dentin discs were etched with 6% citric acid for 2 minutes, then treated with different slurries using the same protocol after brushing. Ten human dentin discs were divided into five groups (n=2). The dentin discs were brushed under the slurry using a toothbrush-equipped brushing machine. The brushing load was 170 g + / - 5 g, and the automatic brushing was performed at 150 rpm. After brushing for 1 minute, the dentin discs were immersed in the slurry for 1 minute. The discs were then placed in 50 mL of deionized water and vibrated 10 times at 150 rpm on a flatbed shaker. The discs were then immersed in simulated oral fluid (SOF) at 37°C and 60.0 rpm in a vibrating water bath for at least 3 hours. Afterward, the dentin discs were brushed under the slurry using the same procedure as in step one. This brushing was repeated 3 times a day, and the dentin discs were then kept overnight (>12 hours) in SOF in a vibrating water bath at 37°C to simulate the oral environment. One day later, the dentin samples were characterized using a scanning electron microscope (SEM, Hitachi S-4800, Japan).

[0067] Simulated oral fluid is prepared by combining the components in Table 2: Table 2

[0068] Regardless of the original shape of the dentin disc, select a square (4mm x 4mm) and take an image at 30x magnification. Within this square, select five points (each 150 μm x 150 μm, one in the center and one at each corner) and observe them at 1000x magnification. Assess tubular closure according to the criteria described in Table 3. Measure both dentin discs in each test group.

[0069] Table 3

[0070] One day later (after 3 brushing sessions), SEM images of the dentin discs were taken. The images were analyzed and scored. The results are reported in Table 4.

[0071] Table 4

[0072] The results showed that sample 1 was more effective in sealing tubes compared to samples A, B, C, and D.

[0073] Example 2 This example demonstrates the microhardness variation of tooth enamel. The compositions were prepared as shown in Table 5. All components are expressed as a percentage by weight of the total formulation.

[0074] Table 5

[0075] Assessment of the decrease in surface microhardness (SMH) of tooth enamel Fresh toothpaste slurry was prepared by mixing 4 g of toothpaste sample with 8 mL of deionized (DI) water for 40 seconds and used immediately.

[0076] The surface microhardness (SMH) of tooth enamel was measured for 10 seconds using a Knoop indenter on a Struers Durascan microhardness tester under a load of 50 gf. Five indentations were made at each test point on different areas of each enamel block to avoid residual stress. To assess the microhardness of enamel, well-polished human enamel blocks were divided into five groups (n=5 per group) with similar baseline SMH values. The SMH of the human enamel blocks was measured and recorded as SMH. 基线 Human tooth enamel blocks were immersed in freshly prepared toothpaste slurry for 3 minutes, then placed in a demineralizing solution (Demin solution) at 37°C with gentle shaking for 4 hours, followed by rinsing with water. Afterward, the enamel blocks were immersed in a remineralizing solution (Remin solution) at 37°C with gentle shaking for 4 hours. The entire treatment within one day is called a one-day treatment cycle. The treatment was repeated for 7 days, and the SMH of the enamel blocks was measured and recorded as SMH. 处理 .

[0077] The demineralization solution consisted of 2 mM CaCl2, 2 mM KH2PO4, 75 mM acetic acid, and 0.1 mM Tris buffer, and the pH was adjusted to 4.6 with 1 M KOH.

[0078] The remineralization solution consisted of 1.5 mM CaCl2, 0.9 mM KH2PO4, 150 mM KCl and 20 mM HEPES, with the pH adjusted to 7.0 using NaOH.

[0079] The decrease in surface microhardness (SMH) of tooth enamel is calculated as follows: SMH decrease (%) = (SMH) 处理 -SMH 基线 ) × 100 / SMH 基线 The results are shown in Table 6.

[0080] Table 6

[0081] As shown in Table 6, the enamel blocks treated with Sample 2 exhibited higher acid resistance, indicating improved protection against acid erosion.

Claims

1. An oral care composition comprising: a) Tetracalcium phosphate; b) Water-soluble calcium source; The water-soluble calcium source described herein comprises calcium chloride, calcium nitrate, calcium acetate, calcium lactate, calcium formate, calcium malate, calcium propionate, calcium butyrate, calcium bicarbonate, calcium glycerophosphate, calcium gluconate, calcium ascorbate, calcium glycinate, or mixtures thereof; and The composition is an aqueous composition, and the water content is at least 5% by weight of the composition.

2. The oral care composition according to claim 1, wherein the water-soluble calcium source comprises calcium chloride, calcium nitrate, calcium glycinate, calcium glycerophosphate, calcium gluconate, or a mixture thereof.

3. The oral care composition according to claim 1 or 2, wherein the tetracalcium phosphate is present in an amount of 0.1 to 80% by weight of the composition, preferably in an amount of 0.5 to 50% by weight of the composition.

4. The oral care composition according to any one of the preceding claims, wherein the tetracalcium phosphate and the water-soluble calcium source are present in a weight ratio of 1:20 to 80:1, preferably in a weight ratio of 1:10 to 50:

1.

5. The oral care composition according to any one of the preceding claims, wherein the water-soluble calcium source is present in an amount of 0.001 to 20% by weight of the composition, preferably in an amount of 0.01 to 15% by weight of the composition.

6. The oral care composition according to any one of the preceding claims, wherein the composition further comprises a phosphate source.

7. The oral care composition according to any one of the preceding claims, wherein the composition further comprises a silica-based abrasive or a calcium carbonate abrasive.

8. The oral care composition according to any one of the preceding claims, wherein the composition further comprises a fluoride source.

9. The oral care composition according to any one of the preceding claims, wherein the composition further comprises a zinc source.

10. The oral care composition according to any one of the preceding claims, wherein the water content is at least 10% by weight of the composition, preferably at least 15%.

11. A method for remineralizing and / or reducing sensitivity and / or combating tooth erosion or caries in an individual, comprising the step of applying a composition according to any one of the preceding claims to the oral cavity of the individual.

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