Patent Description:
Teeth comprise dentin overlaid with an outer layer of enamel. Teeth are under constant attack from chemical and physical forces, including bacteria-derived acids and mechanical wear, resulting in demineralization and weakening of enamel and the underlying dentin.

Tooth hypersensitivity is a temporary induced pain sensation that affects up to <NUM>% of the adult population. It is associated with tooth demineralization and the loss of either enamel or cementum to expose underlying dentin. The dentin of the tooth generally contains channels, called tubules, which provide for an osmotic flow between the inner pulp region of the tooth and the outer root surfaces. The cause of tooth hypersensitivity may be related to demineralization giving rise to increased exposure of tubules and permeability of the dentine. The most common causes of demineralization of the enamel or dentine are attrition, abrasion, gingival recession and erosion. When root surfaces are exposed, dentinal tubules are also exposed.

The currently accepted theory for tooth hypersensitivity is the hydrodynamic theory, based on the belief that open exposed dentinal tubules allow fluid flow through the tubules. This flow excites the nerve endings in the dental pulp. Clinical replica of sensitive teeth viewed in a SEM (scanning electron microscopy) reveal varying numbers of open or partially occluded dentinal tubules.

Efforts have been made over the years to treat tooth hypersensitivity. One approach is to reduce the excitability of the nerve in a sensitive tooth by using "nerve-depolarising agents" comprising strontium ions, potassium salts such as potassium nitrate, potassium bicarbonate, potassium chloride and the like. These nerve-depolarising agents function by interfering with neural transduction of the pain stimulus to make the nerve less sensitive.

Another approach is to use "tubule blocking agents" that fully or partially occlude tubules such as polystyrene beads, apatite, polyacrylic acid, mineral hectorite clay and the like. These tubule blocking agents function by physically blocking the exposed ends of the dentinal tubules, thereby reducing dentinal fluid movement and reducing the irritation associated with the shear stress described by the hydrodynamic theory.

<CIT>relates to a preparation that contains: at least one calcium compound, selected from calcium phosphate, calcium fluorides and calcium fluorophosphates and hydroxyl derivatives and carbonate derivatives of said calcium salts, calcium hydroxides and calcium oxides, said calcium compound being precipitated with at least one protein component, selected from proteins and protein hydrolysates; and at least one crosslinking agent for the protein component and/or non-set cement.

A variety of products have been developed in an attempt to treat tooth hypersensitivity and/or enhance tooth remineralization. But there still remains a need to develop an oral care composition which is more effective in remineralizing teeth and/or occluding dentinal tubules to reduce tooth sensitivity.

In a first aspect, the present invention is directed to an oral care composition comprising:.

wherein the phosphate source comprises trisodium phosphate, monosodium dihydrogen phosphate, disodium hydrogen phosphate, ammonium phosphate, diammonium hydrogen phosphate, ammonium dihydrogen phosphate, tripotassium phosphate, monopotassium dihydrogen phosphate, dipotassium hydrogen phosphate or a mixture thereof.

In a second aspect, the present invention is directed to a packaged oral care product comprising the oral care composition of the first aspect of this invention.

In a third aspect, the present invention is directed to a method for remineralizing and/or reducing sensitivity of teeth of an individual comprising the step of applying the oral care composition of any embodiment of the first aspect to at least one surface of the teeth of an individual. The method is preferably for non-therapeutic benefits.

In a fourth aspect, the present invention is directed to non-therapeutic use of the oral care composition of any embodiment of the first aspect for remineralizing and/or reducing sensitivity of teeth of an individual.

In a fifth aspect, the present invention is directed to use of the oral care composition of any embodiment of the first aspect in the manufacture of a medicament in remineralizing and/or reducing sensitivity of an individual.

All amounts are by weight of the final oral care composition, unless otherwise specified. It should be noted that in specifying any ranges of values, any particular upper value can be associated with any particular lower value.

"Soluble" and "insoluble" for the purpose of the present invention means the solubility of a source (e.g., like phosphate source) in water at <NUM> and atmospheric pressure. "Soluble" means a source that dissolves in water to give a solution with a concentration of at least <NUM> moles per litre. "Insoluble" means a source that dissolves in water to give a solution with a concentration of less than <NUM> moles per litre. "Slightly soluble", therefore, is defined to mean a source that dissolves in water to give a solution with a concentration of greater than <NUM> moles per litre and less than <NUM> moles per litre.

Now it has been found unexpectedly that an oral care composition comprising calcium silicate, casein phosphopeptide and a phosphate source can efficiently occlude dentinal tubules to provide excellent tubule blockage efficacy to reduce tooth sensitivity. In addition, such oral care composition can also provide enhanced tooth remineralization efficacy. "Remineralization" for the purpose of the present invention means in situ (i.e. in the oral cavity) generation of calcium phosphate on teeth (including layers on teeth from <NUM> to <NUM> microns, and preferably from <NUM> to <NUM> microns, and most preferably, from <NUM> to <NUM> microns thick including all ranges subsumed therein) to reduce the likelihood of tooth sensitivity, tooth decay, regenerate enamel and/or improve the appearance of teeth by whitening through the generation of such new calcium phosphate.

The calcium silicate suitable for use in the present invention comprises calcium oxide (CaO) and silica (SiO<NUM>) and is made up of varying proportions of CaO and SiO<NUM>. Preferably, the calcium silicate is insoluble, present as the composite material calcium oxide-silica (CaO-SiO<NUM>), which is described, for example, in international patent application published as <CIT>.

For a calcium silicate composite material, the atom ratio of calcium to silicon (Ca:Si) may be from <NUM>:<NUM> to <NUM>:<NUM>. The Ca:Si ratio is preferably <NUM>:<NUM> to <NUM>:<NUM>, and more preferably, from <NUM>:<NUM> to <NUM>:<NUM>, and most preferably, from about <NUM>:<NUM> to <NUM>:<NUM>. The calcium silicate may comprise mono-calcium silicate, bi-calcium silicate, or tricalcium silicate.

The calcium silicate may be crystalline or amorphous or even mesoporous. Preferably the calcium silicate is at least partially crystalline. When the calcium silicate is partially crystalline, it comprises calcium (Ca) and silicon (Si) in an atom ratio (Ca:Si) from <NUM>:<NUM> to <NUM>:<NUM>, more preferably from <NUM>:<NUM> to <NUM>:<NUM> and most preferably from <NUM>:<NUM> to <NUM>:<NUM>. It is particularly preferable that the calcium silicate is fully crystalline. The presence of crystallinity may be confirmed, for example, by x-ray diffraction. An example of the calcium silicate suitable for use in the present invention is commercially available under the trade name NYAD® M9000 from NYCO Minerals, Inc.

Preferably, the calcium silicate of the present invention is not hydrated. The calcium silicate which is not hydrated may comprise other components in addition to calcium oxide and silica, such as metal cations, anions and the like. It is preferable that the calcium silicate comprises calcium oxide, silica in an amount of at least <NUM>% by weight of the calcium silicate, more preferably at least <NUM>%, more preferably still at least <NUM>%, even more preferably at least <NUM>% and most preferably the calcium silicate consist of (or at least consist essentially of) calcium oxide, silica.

The calcium silicate may be hydrated. When the calcium silicate is hydrated, the calcium silicate hydrate comprises at least calcium oxide, silica and water. Compared with conventional calcium silicate which are not hydrated, the calcium silicate hydrate comprises the water of hydration in an amount of at least <NUM>% by weight of the calcium silicate hydrate, preferably at least <NUM>%, more preferably at least <NUM>%, even more preferably at least <NUM>% and most preferably at least <NUM>%. The water content is typically no greater than <NUM>% by weight of the calcium silicate hydrate, more preferably no greater than <NUM>%, even more preferably no greater than <NUM>% and most preferably no greater than <NUM>%. "Water of hydration" for the purpose of the present invention means water chemically combined with a substance in a way that it can be removed by heating without substantially changing the chemical composition of the substance. In particular, water which could only be removed when heated above <NUM>. The water loss is measured using thermo gravimetric analysis (TGA) with a Netzsch TG instrument. The TGA is conducted under an N<NUM> atmosphere with heating rate of <NUM> degree/min in the range of <NUM> to <NUM>.

It is preferable that the calcium silicate of the present invention is particulate which allows for maximum surface area for contact with dental tissue. Preferably the calcium silicate used in this invention has a particle size from <NUM> to <NUM> microns, more preferably from <NUM> to <NUM> microns, more preferably still from <NUM> to <NUM> microns and most preferably from <NUM> micron to <NUM> microns. "Particle size" for the purpose of the present invention means D50 particle size. The D50 particle size of a particulate material is the particle size diameter at which <NUM> wt% of the particles are larger in diameter and <NUM> wt% are smaller in diameter.

Typically, the oral care composition comprises from <NUM> to <NUM>% by weight of the calcium silicate, more preferably from <NUM> to <NUM>% and most preferably from <NUM> to <NUM>%, based on total weight of the oral care composition and including all ranges subsumed therein.

The casein phosphopeptide suitable for use in the present invention comprises multiple phosphoseryl residues, which may be made synthetically by chemical synthesis or genetic engineering or extracted from naturally occurring materials. Preferably, the casein phosphopeptide may be obtained by hydrolyzing or digesting (either chemical or proteolytic) a protein or by tryptic digestion of casein or other phosphor-acid rich proteins such as phosphitin, or by chemical or recombinant synthesis. It is preferred that the casein phospopeptide comprises the core sequence -Ser(P)-Ser(P)-Ser(P)-Glu-Glu-, where Ser(P) is a phosphoseryl residue.

The oral care composition typically comprises the casein phosphopeptide in an amount of from <NUM> to <NUM>% by weight of the composition, more preferably from <NUM> to <NUM>% and most preferably from <NUM> to <NUM>%, based on total weight of the oral care composition and including all ranges subsumed therein.

The oral care composition preferably comprises the calcium silicate and the casein phosphopeptide in a weight ratio from <NUM>:<NUM> to <NUM>:<NUM>, more preferably from <NUM>:<NUM> to <NUM>:<NUM> and most preferably from <NUM>:<NUM> to <NUM>:<NUM>, including all ratios subsumed therein.

The phosphate source used in this invention is limited only to the extent that the same may be used in a composition suitable for use in the mouth. Preferably the phosphate source is water soluble. The phosphate source suitable for use in this invention include trisodium phosphate, monosodium dihydrogen phosphate, disodium hydrogen phosphate, ammonium phosphate, diammonium hydrogen phosphate, ammonium dihydrogen phosphate, tripotassium phosphate, monopotassium dihydrogen phosphate, dipotassium hydrogen phosphate, mixtures thereof or the like.

The oral care composition preferably comprises the phosphate source in an amount of from <NUM> to <NUM>% by weight of the composition, preferably from <NUM> to <NUM>%, more preferably from <NUM> to <NUM>% and most preferably from <NUM> to <NUM>%, based on total weight of the oral care composition and including all ranges subsumed therein. In a preferred embodiment, the phosphate source is trisodium phosphate and monosodium dihydrogen phosphate at a trisodium phosphate to monosodium dihydrogen phosphate weight ratio of <NUM>:<NUM> to <NUM>:<NUM>, preferably <NUM>:<NUM> to <NUM>:<NUM>, and most preferably, from <NUM>:<NUM> to <NUM>:<NUM>, including all ratios subsumed therein. In another preferred embodiment, the phosphate source is or at least comprises monosodium dihydrogen phosphate.

Preferably, the oral care composition is an aqueous composition. The water content is at least <NUM>% by weight of the oral care composition, preferably at least <NUM>%, more preferably at least <NUM>%. It is preferable that the water content is from <NUM> to <NUM>% by weight of the oral care composition, more preferably from <NUM> to <NUM>% and most preferably from <NUM> to <NUM>%, based on total weight of the oral care composition and including all ranges subsumed therein.

Typically, the oral care composition has a pH from <NUM> to <NUM>, more preferably from <NUM> to <NUM>, and most preferably from <NUM> to <NUM>. The pH of oral care composition is measured when <NUM> parts by weight of the composition is uniformly dispersed and/or dissolved in <NUM> parts by weight pure water at <NUM>. In particular, the pH may be measured by manually mixing <NUM> oral care composition with <NUM> water for <NUM>, then immediately testing the pH with indicator or a pH meter.

The oral care composition of the present invention may also comprise a physiologically acceptable carrier. The carrier preferably comprises at least surfactant, thickener, humectant or a combination thereof.

Preferably the oral care composition comprises a surfactant. Preferably the composition comprises at least <NUM>% surfactant by weight of the composition, more preferably at least <NUM>% and most preferably from <NUM> to <NUM>%. Suitable surfactants include anionic surfactants, such as the sodium, magnesium, ammonium or ethanolamine salts of C<NUM> to C<NUM> alkyl sulphates (for example sodium lauryl sulphate), C<NUM> to C<NUM> alkyl sulphosuccinates (for example dioctyl sodium sulphosuccinate), C<NUM> to C<NUM> alkyl sulphoacetates (such as sodium lauryl sulphoacetate), C<NUM> to C<NUM> alkyl sarcosinates (such as sodium lauryl sarcosinate), C<NUM> to C<NUM> alkyl phosphates (which can optionally comprise up to <NUM> ethylene oxide and/or propylene oxide units) and sulphated 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 sulphobetaines. Mixtures of any of the above described materials may also be used. More preferably the surfactant comprises or is anionic surfactant. The preferred anionic surfactants are sodium lauryl sulphate and/or sodium dodecylbenzene sulfonate. Most preferably the surfactant is sodium lauryl sulphate, sodium coco sulfate, cocamidopropyl betaine, sodium methyl cocoyl taurate or mixtures thereof.

Thickener may also be used in this invention and is limited only to the extent that the same may be added to a composition suitable for use in the mouth. Illustrative examples of the types of thickeners that may be used in this invention include, sodium carboxymethyl cellulose (SCMC), hydroxyl ethyl cellulose, methyl cellulose, ethyl cellulose, gum tragacanth, gum arabic, gum karaya, sodium alginate, carrageenan, guar, xanthan gum, Irish moss, starch, modified starch, silica based thickeners including silica aerogels, magnesium aluminum silicate (e.g., Veegum), Carbomers (cross-linked acrylates) and mixtures thereof.

Typically, xanthan gum and/or sodium carboxymethyl cellulose and/or a Carbomer is/are preferred. When a Carbomer is employed, those having a weight-average molecular weight of at least <NUM>,<NUM> are desired, and preferably, those having a molecular weight of at least <NUM>,<NUM>,<NUM>, and most preferably, those having a molecular weight of at least about <NUM>,<NUM>,<NUM> are desired. Mixtures of Carbomers may also be used herein.

In an especially preferred embodiment, the Carbomer is Synthalen PNC, Synthalen KP or a mixture thereof. It has been described as a high molecular weight and cross-linked polyacrylic acid and identified via <NPL>. These types of materials are available commercially from suppliers like Sigma.

In another especially preferred embodiment, the sodium carboxymethyl cellulose (SCMC) used is SCMC <NUM>. It has been described as a sodium salt of a cellulose derivative with carboxymethyl groups bound to hydroxy groups of glucopyranose backbone monomers and identified via <NPL>. The same is available from suppliers like Alfa Chem.

In another especially preferred embodiment, the thickener is xanthan gum.

Thickener typically makes up from <NUM> to about <NUM>%, more preferably from <NUM> to <NUM>%, and most preferably, from <NUM> to <NUM>% by weight of the oral care composition, based on total weight of the composition and including all ranges subsumed therein.

When the oral care composition of this invention is a toothpaste or gel, the same typically has a viscosity from about <NUM>,<NUM> to <NUM>,<NUM> centipoise, and preferably, from <NUM>,<NUM> to <NUM>,<NUM> centipoise, and most preferably, from <NUM>,<NUM> to <NUM>,<NUM> centipoise, taken at room temperature (<NUM>) with a Brookfield Viscometer, Spindle No.<NUM>/<NUM> and at a speed of <NUM> rpm for <NUM> minute.

Suitable humectants are preferably used in the oral care composition of the present invention and they include, for example, glycerin, sorbitol, propylene glycol, dipropylene glycol, diglycerol, triacetin, mineral oil, polyethylene glycol (preferably, PEG-<NUM>), alkane diols like butane diol and hexanediol, ethanol, pentylene glycol, or a mixture thereof. Glycerin, polyethylene glycol, sorbitol or mixtures thereof are the preferred humectants.

The humectant may be present in the range of from <NUM> to <NUM>% by weight of the oral care composition. More preferably, the carrier humectant makes up from <NUM> to <NUM>%, and most preferably, from <NUM> to <NUM>% by weight of the composition, based on total weight of the composition and including all ranges subsumed therein.

The oral care composition may further comprise benefit agents that are typically delivered to human teeth and/or the oral cavity including the gums to enhance or improve a characteristic of those dental tissues. The benefit agents are present in the oral care composition in addition to the calcium silicate, the casein phosphopeptide and the phosphate source that are included in the composition.

Typically the benefit agent is selected from optical agents, biomineralization agents, adsorbing agents, anti-microbial agents, gum health agents, desensitizing agents, anti-calculus agents, freshness agents and mixtures thereof.

Optical agents may be selected from one or more of whitening agents and pearlescent agents. When the optical agent is a whitening agent, it is preferable that the whitening agent is a particulate whitening agent having a refractive index of from <NUM> to <NUM>. The refractive index is quoted at a temperature of <NUM> and a wavelength of <NUM>. Suitable materials to provide such a high refractive index are metal compounds and preferred are compounds where the metal is selected from zinc (Zn), titanium (Ti), zirconium (Zr) or a mixture thereof. Preferably, the metal compound is (or at least comprises) a metal oxide such as titanium dioxide (TiO<NUM>), zinc oxide (ZnO), zirconium dioxide (ZrO<NUM>) or a mixture thereof. Preferably, the particulate whitening agent is a composite particle. "Composite particle", as used herein, means a particle comprising a first component core and a second component coating wherein the core and coating are composed of different materials. Particularly suitable core materials are metal compounds and preferred are compounds where the metal is selected from zinc (Zn), titanium (Ti), zirconium (Zr) or a mixture thereof. Preferably, the metal compound is (or at least comprises) a metal oxide such as titanium dioxide (TiO<NUM>), zinc oxide (ZnO), zirconium dioxide (ZrO<NUM>) or a mixture thereof. The second component coating comprises material suitable to adhere to tooth enamel, dentin or both. Typically the coating material comprises the element calcium, and optionally, other metals like potassium, sodium, aluminium, magnesium as well as mixtures thereof whereby such optional metals are provided as, for example, sulphates, lactates, oxides, carbonates or silicates. Optionally, the coating material may be aluminium oxide or silica. In a preferred embodiment, the second component coating can comprise, for example, calcium phosphate, calcium gluconate, calcium oxide, calcium lactate, calcium carbonate, calcium hydroxide, calcium sulphate, calcium carboxymethyl cellulose, calcium alginate, calcium salts of citric acid, calcium silicate, mixture thereof or the like. Calcium silicate is particularly preferred. In an especially preferred embodiment, the particulate whitening agent is titanium dioxide coated with calcium silicate.

In another preferred embodiment, the whitening agent is a dye or a pigment or a combination of the two. The pigment according to the invention is a shade/material which is insoluble in the relevant medium, at the relevant temperature. This is in contrast to dyes which are soluble. The term "relevant medium", as used herein, refers to human saliva, the liquid medium in which the composition is used, at the temperature of the oral cavity during brushing of the teeth, i.e. up to <NUM>. The relevant medium may also be water and the relevant temperature to be <NUM>. Preferred pigment or dye for use in the present invention is violet or blue having a hue angle, h, in the CIELAB system of from <NUM> to <NUM> degrees, preferably from <NUM> to <NUM> degrees. When the whitening agent is a pigment, it is preferable that the pigment is violet or blue selected from one or more of those listed in the Colour Index International as pigment blue <NUM> through to pigment blue <NUM> and pigment violet <NUM> through to pigment violet <NUM>. Other suitable pigments are pigment ultramarine blue and ultramarine violet. While the preferred pigment is blue or violet, the same effect may be achieved through mixing pigments outside of this hue angle range.

For example, such a hue angle may also be obtained by mixing a red and green-blue pigment to yield a blue or violet shaded pigment. It is particularly preferred that the pigment is a blue pigment. A preferred class of blue pigments suitable for use in the invention are organic blue pigments such as phthalocyanine blue pigments. It is especially preferred that the pigment is phthalocyanine blue pigment selected from alpha copper phthalocyanines Pigment Blue <NUM>, Pigment Blue <NUM>:<NUM>, Pigment Blue <NUM>:<NUM>, Pigment Blue <NUM>:<NUM>, Pigment Blue <NUM>:<NUM>, Pigment Blue <NUM>:<NUM> and mixtures thereof. Most preferably the pigment is Pigment Blue <NUM>:<NUM>. A commercially available example is Cosmenyl Blue A4R from Clariant. When the whitening agent is a dye, it is preferable that the dye is a blue dye, more preferably FD&C Blue <NUM> or Patent Blue V.

In another preferred embodiment, the optical agent is a pearlescent agent. The term "pearlescent", as used herein, means an agent in the form of particles which reflects and partially transmits the incident light. Suitable pearlescent agent for use in the present invention includes mica, bismuth oxychloride or mixtures thereof. Preferably the pearlescent agent is formed by coating one or more metal oxide layers onto natural or synthetic mica flakes. Examples of suitable mica include, for example, muscovite, phlogopite, fluorophlogopite, biotite or mixtures thereof. Examples of suitable metal oxides include, for example, TiO<NUM>, Fe<NUM>O<NUM>, TiFe<NUM>O<NUM>, Fe<NUM>O<NUM>, Cr<NUM>O<NUM>, Al<NUM>O<NUM>, SiO<NUM>, ZrO<NUM>, ZnO, SnO<NUM>, CoO, Co<NUM>O<NUM>, VO<NUM>, V<NUM>O<NUM>, Sn(Sb)O<NUM>, titanium suboxides or mixtures thereof. One example of a preferred pearlescent agent is mica coated with TiO<NUM>.

Biomineralization agents for tooth enamel remineralization may be selected from one or more of calcium sources, biomolecules, proteinaceous materials, amorphous calcium phosphate, α-tricalcium phosphate, β-tricalcium phosphate, calcium silicate, calcium sulfate, calcium carbonate, calcium deficient hydroxyapatite Ca<NUM>-X(HPO<NUM>)X(PO<NUM>)<NUM>-X(OH)<NUM>-X, <NUM> ≤ x < <NUM>), dicalcium phosphate (CaHPO<NUM>), dicalcium phosphate dihydrate (CaHPO<NUM>·<NUM><NUM>O), hydroxyapatite (Ca<NUM>(PO<NUM>)<NUM>(OH)<NUM>), monocalcium phosphate monohydrate (Ca(H<NUM>PO<NUM>)<NUM>·H<NUM>O), octacalcium phosphate (Ca<NUM>H<NUM>(PO<NUM>)<NUM>·<NUM><NUM>O) and tetracalcium phosphate (Ca<NUM>(PO<NUM>)<NUM>O).

Adsorbing agents may be selected from one or more of boron nitride, porous silica, charcoal, layered silicate (e.g. montmorillonite, kaoline, clay), graphene and polymethyl methacrylate microsphere.

Anti-microbial agents may be selected from one or more of metal salts where the metal is selected from zinc, copper, silver or a mixture thereof, triclosan, triclosan monophosphate, triclocarban, curcumin, quaternary ammonium compounds, bisbiguanides and long chain tertiary amines, preferably zinc salts including zinc oxide, zinc chloride, zinc acetate, zinc ascorbate, zinc sulphate, zinc nitrate, zinc citrate, zinc lactate, zinc peroxide, zinc fluoride, zinc ammonium sulfate, zinc bromide, zinc iodide, zinc gluconate, zinc tartarate, zinc succinate, zinc formate, zinc phenol sulfonate, zinc salicylate, zinc glycerophosphate or a mixture thereof.

Desensitizing agents may be selected from one or more of potassium citrate, potassium chloride, potassium tartrate, potassium bicarbonate, potassium oxalate, potassium nitrate and strontium salts.

Anti-calculus agents may be selected from one or more of alkali-metal pyrophosphates, hypophosphite-containing polymers, organic phosphonates and phosphocitrates.

Gum health agents may be selected from one or more of anti-inflammatory agents such as ibuprofen, flurbiprofen, aspirin and indomethacin, plaque buffers, biomolecules, proteinaceous materials, vitamins such as Vitamins A,C and E, plant extracts and curcumin.

Freshness agents may be flavours selected from one or more of peppermint, spearmint, menthol, flora oil, clove oil and citrus oil.

The benefit agent is preferably selected from optical agents, biomineralization agents and mixtures thereof. In an especially preferred embodiment, the benefit agent is an optical agent, especially a whitening agent.

The oral care composition of the present invention may comprise a single benefit agent or a mixture of two or more benefit agents. Typically, the benefit agent is present in an amount from <NUM> to <NUM>%, and more preferably, from <NUM> to <NUM>%, and most preferably from <NUM> to <NUM>% by total weight of the oral care composition and including all ranges subsumed therein.

The oral care composition may additionally comprise a fluoride source. Preferred fluoride source includes 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 at a level from <NUM> to <NUM>%, more preferably from <NUM> to <NUM>% and most preferably from <NUM> to <NUM>% by weight of the oral care composition, based on total weight of the composition and including all ranges subsumed therein.

The oral care composition may additionally comprise abrasives. Preferred abrasives include silicas, aluminas, calcium carbonates, dicalcium phosphates, calcium pyrophosphates, hydroxyapatites, trimetaphosphates, insoluble hexametaphosphates or mixtures thereof, including agglomerated particulate abrasives. Calcium carbonate and silica are particularly preferred, especially silica. The abrasives may be present in the range of from <NUM> to <NUM>%, more preferably from <NUM> to <NUM>%, and most preferably from <NUM> to <NUM>% by weight of the oral care composition, based on total weight of the composition and including all ranges subsumed therein.

The oral care composition of the present invention may contain a variety of other ingredients which are common in the art to enhance physical properties and performance. These ingredients include preservatives, pH-adjusting agents, sweetening agents, polymeric compounds, buffers and salts to buffer the pH and ionic strength of the compositions, and mixtures thereof. Such ingredients typically and collectively make up less than <NUM>% by weight of the composition, and preferably, from <NUM> to <NUM>% by weight, and most preferably, from <NUM> to <NUM>% by weight of the composition, including all ranges subsumed therein.

In a preferred embodiment, the oral care composition is a monophase composition.

In another preferred embodiment, the oral care composition is a dual-phase composition comprising a calcium phase and a phosphate phase, wherein the calcium silicate is present in the calcium phase and the phosphate source and the casein phosphopeptide are present in the phosphate phase. The two phases are physically separate from one another by being in independent phases. The delivery of the two independent phases to the teeth may be simultaneous or sequential. In a preferred embodiment, the phases are delivered simultaneously.

Typically, the dual-phase composition is delivered by a dual-tube having a first compartment for calcium phase and a second compartment for phosphate phase, which allows for co-extrusion of the two phases.

In a preferred embodiment, such a dual-tube has one of the compartments surrounding the other. In such embodiments, one phase is present as a sheath, surrounding the other phase in the core. In an especially preferred embodiment, the core is the calcium phase and the sheath is the phosphate phase.

In another preferred embodiment, such a dual-tube has the two compartments side by side within the same tube. In such embodiments, the two phases are extruded from the tube as one, such extrusion being termed "contact extrusion". A pump head may be used in such a dual-tube for squeezing the two phases from the tube as one.

The dual-phase oral care composition may be a gel composition that comprises two independent gel phases, the first is the calcium phase and the second is the phosphate phase. The means of delivery may involve a cotton rod, or a tray, onto which the calcium phase and the phosphate phase are applied, prior to the tray being placed in contact with the teeth.

The oral care composition of this invention can be used in a method for remineralizing and/or reducing sensitivity of teeth of an individual. Preferably, the method is non-therapeutic. The oral care composition of this invention may additionally be used for remineralizing and/or reducing sensitivity of teeth of an individual, and/or used in the manufacture of a medicament in remineralizing and/or reducing sensitivity of an individual. Preferably, the use is non-therapeutic.

The oral care composition may be in any form common in the art, preferred forms are dentifrices, tooth pastes, gels, mouthwashes, medicaments, oral films, serums, chewing gums and lozenges. Typically the composition will be packaged. In tooth paste or gel form, the composition may be packaged in a conventional plastic laminate, metal tube or a single compartment dispenser. The same may be applied to dental surfaces by any physical means, such as a toothbrush, fingertip or by an applicator directly to the sensitive area. In liquid mouthwash form the composition may be packaged in a bottle, sachet or other convenient container.

The composition can be effective even when used in an individual's daily oral hygiene routine. For example, the composition may be brushed onto the teeth. The composition may, for example, be contacted with the teeth for a time period of one second to <NUM> hours. More preferably from <NUM> to <NUM> hours, more preferably still from <NUM> to <NUM> hour and most preferably from <NUM> to <NUM> minutes. The composition may be used daily, for example for use by an individual once, twice or three times per day.

The following examples are provided to facilitate an understanding of the present invention. The examples are not provided to limit the scope of the claims.

This example demonstrates the effect of calcium silicate and casein phosphopeptide on blockage of dentinal tubules. All ingredients are expressed by weight percent of the total formulation.

To evaluate the blockage efficacy of dentinal tubules, fresh slurries were prepared by mixing toothpaste with de-ionised (DI) water or sodium phosphate solution for <NUM> seconds and used immediately.

Human dentine discs were eroded by <NUM>% citric acid for <NUM> mins, then they were treated with different slurries via brushing following the same protocol. Eight human dentine discs were separated into four groups (n=<NUM>). The dentine discs were brushed with the slurry under a tooth brushing machine equipped with toothbrushes. The load of the tooth brushing was <NUM> +/-<NUM> and the automatic brushing operated at a speed of <NUM> rpm. After brushing for <NUM>, the dentine discs were soaked in slurry for <NUM>. Then the dentine discs were placed in <NUM> DI water and agitated on a flatbed shaker at <NUM> rpm for <NUM> strokes. The discs were then soaked in simulated oral fluid (SOF) for at least <NUM> hours under the condition of a shaking water bath at <NUM> and <NUM> rpm. After that, the dentine discs were brushed with the slurry by machine using the same procedure as in the first step. The brushing was repeated twice for one day, then the dentine discs were kept in SOF overnight (><NUM> hours) in a shaking water bath at <NUM> to mimic oral environment. The dentine samples were characterized by scanning electron microscopy (SEM, Hitachi S-<NUM>, Japan) after <NUM> days of brushings.

Simulated oral fluid was made by combining the ingredients in Table <NUM>:.

Regardless of the original shape of the dentine discs, a square (with a size of <NUM> x <NUM>) is selected and one image is captured under 30x magnification. Within this square, five spots (each with a size of <NUM> x <NUM>, one in the middle, and one in every corner) are selected and observed under 1000x magnification. The blockage of tubules is accessed following the standards described in Table <NUM>. The measurement is carried out for the two dentine discs of each test group.

SEM images of the dentine discs were taken after <NUM> days of brushings. The images were analyzed and scored. The results are reported in table <NUM> (error represents standard error for duplicate measurements).

It can be seen from the results that samples comprising additional casein phosphopeptide had significantly better tubule blockage efficacy compared to sample A.

This example demonstrated the effect of calcium source on blockage of dentinal tubules. All ingredients are expressed by weight percent of the total formulation.

The same protocol was used to evaluate the blockage of dentinal tubules as described in Example <NUM>. The dentine samples were brushed twice daily for three days.

Claim 1:
An oral care composition comprising:
a) calcium silicate;
b) casein phosphopeptide; and
c) a phosphate source;
wherein the phosphate source comprises trisodium phosphate, monosodium dihydrogen phosphate, disodium hydrogen phosphate, ammonium phosphate, diammonium hydrogen phosphate, ammonium dihydrogen phosphate, tripotassium phosphate, monopotassium dihydrogen phosphate, dipotassium hydrogen phosphate or a mixture thereof.