Peroxymonosulfate dentifrice composition for stubborn stains

Abstract

The present invention relates to a peroxymonosulfate dentifrice composition for stubborn stains. A solid oral care composition, such as a tablet or powder, comprises an alkali metal peroxymonosulfate as an effective bleaching agent for bleaching stubborn stains, such as smoke and coffee stains.

Description

[0001] This application is a divisional application of a Chinese patent application filed on August 11, 2016, with application number "201680088342.0" and invention name "Permonosulfate toothpowder composition for stubborn stains". Technical Field

[0002] The present invention relates to peroxymonosulfate dentifrice compositions for stubborn stains. Background Art

[0003] Products currently available for tooth whitening contain a variety of different ingredients, and the primary active ingredient is often a peroxide source, such as hydrogen peroxide. The use of peroxide agents can present difficulties in formulation and long-term stability of the resulting compositions. Therefore, there is a need for alternative bleaching agents with improved stability and tolerability.

[0004] A particularly challenging use of existing tooth whitening agents is to remove cigarette stains. Cigarette stains are caused by the nicotine and tar present in tobacco products, including cigarettes and cigars, as well as chewing tobacco. Although nicotine itself does not stain strongly, oxidation caused by air can cause dark yellow or even brown stains that are difficult to remove. When tobacco is inhaled or placed in the mouth, nicotine and tar are deposited in the oral cavity. These chemicals penetrate into the microscopic openings in the tooth enamel, causing the tooth surface to become severely yellowed / brown over time as these chemicals oxidize. Similarly, coffee stains and stains caused by chewing betel nut are also problematic. Existing tooth whitening compositions are difficult to bleach these types of stubborn stains.

[0005] Persulfate and its salts (persulfates) are powerful oxidizing and detergent agents. They are currently used for a variety of consumer purposes, including denture cleaning. The most common peroxymonosulfate oxidant is potassium peroxymonosulfate, commonly known as MPS.

[0006] Potassium monopersulfate has limited use in tooth whitening compositions due to its instability in aqueous solutions, particularly at or above neutral pH. In fact, potassium monopersulfate is known to degrade even in the presence of small amounts of water and heat. Formulating potassium monopersulfate as a triple salt mixture of potassium peroxymonosulfate, potassium bisulfate, and potassium sulfate (2KHSO5·KHSO4·K2SO4) enhances the stability of the oxidant. However, there remains a need for improved MPS formulations for use in stable oral care products to treat stubborn stains, such as cigarette and coffee stains. Summary of the Invention

[0007] The present disclosure provides solid oral care compositions, e.g., tablets or powders, comprising an alkali metal permonosulfate as an effective oxidant for bleaching stubborn tooth stains. In some embodiments, the permonosulfate is sodium permonosulfate or potassium permonosulfate. In some embodiments, the permonosulfate is potassium permonosulfate, which is optionally presented as a ternary salt mixture of potassium permonosulfate, potassium hydrogen sulfate, and potassium sulfate (2KHSO5·KHSO4·K2SO4). In some embodiments, the composition is combined with water or an aqueous solution (e.g., an oral care solution) for use by consumers in bleaching stubborn stains. Once the tooth powder is dissolved or suspended in water or an aqueous solution, the consumer can use the resulting liquid as a conventional toothpaste. The present disclosure provides compositions and methods of use.

[0008] Further areas of applicability of the present disclosure will become apparent from the detailed description provided hereinafter.It should be understood that the detailed description and specific examples, while indicating the preferred embodiment of the invention, are intended for purposes of illustration only and are not intended to limit the scope of the invention. DETAILED DESCRIPTION

[0009] The following description of the preferred embodiment is merely exemplary in nature and is in no way intended to limit the invention, its application, or uses.

[0010] As used throughout, ranges are used as a shorthand way of describing each value within the range. Any value within a range can be selected as the end of the range. In addition, all references cited herein are hereby incorporated by reference in their entirety. In the event of a conflict between a definition in this disclosure and a definition in a cited reference, the present disclosure controls.

[0011] Unless otherwise specified, all percentages and amounts expressed here and elsewhere in the specification should be understood to refer to percentages by weight. The amounts given are based on the active weight of the material.

[0012] Open-ended terms such as "comprising" and "including" mean "including." In this description, unless otherwise specified, the use of the singular also includes the plural. For example, "lubricant" also covers the case where more than one lubricant is used.

[0013] In one aspect, the present disclosure provides a solid oral care composition, such as a dentifrice, for reducing and / or removing stubborn tooth stains, including stains caused by exposure to tobacco smoke, chewing tobacco, betel nut, and coffee.

[0014] The solid composition of the present disclosure includes a tooth whitening effective amount of an alkali metal peroxymonosulfate. Specific examples of such salts are sodium peroxymonosulfate, potassium peroxymonosulfate, and lithium peroxymonosulfate. In some embodiments, the solid composition of the present disclosure is a tooth powder.

[0015] In one embodiment, the peroxymonosulfate is potassium peroxymonosulfate (also known as potassium monoperoxysulfate or MPS). Potassium peroxymonosulfate can be present as a triple salt mixture of potassium peroxymonosulfate, potassium bisulfate, and potassium sulfate (2KHSO5·KHSO4·K2SO4). This triple salt is commercially available as and For example, It is approximately 47 wt% potassium peroxymonosulfate (KHSO5).

[0016] In one embodiment, the compositions of the present disclosure are effective in improving tooth whitening when used twice daily in a mouthwash or toothpaste for about three months, as compared to a control mouthwash or toothpaste in the absence of permonosulfate.

[0017] Peroxymonosulfate salts have limited stability in aqueous solutions and are therefore best stored as dry (e.g., anhydrous) powders. Preferably, the solid compositions (e.g., tablets, granules, or powders) are individually packaged and sealed into unit dose packages. In some embodiments, the solid compositions can be stored in airtight, moisture-proof packaging, such as pouches, sealed foil bags, blister packs, desiccant-covered tubes, and the like.

[0018] The solid compositions of the present disclosure may have a low water content (e.g., substantially anhydrous, or anhydrous). As used herein, the terms "low water content," "water content," and "water" refer to the total water concentration including any free water and all water contained in any ingredient. In various embodiments of the compositions, the amount of water is less than 4% by weight, or less than 3% by weight, or less than 2% by weight, or less than 1% by weight, or less than 0.5% by weight, or less than 0.1%. For example, the minimum amount of water may be about 0.0001%, such as in the range of 0.0001% to 4% by weight, or 0.0001% to 0.5% by weight, or 0.0001% to 0.1% by weight.

[0019] The solid compositions of the present disclosure can be in various forms, including, for example, powders (eg, free-flowing granules), tablets, caplets (tablet-type), granules, pellets, wafers, films, and beads.

[0020] The amount of permonosulfate such as sodium persulfate or potassium permonosulfate in the solid composition of the present invention can effectively reduce or remove stubborn tooth stains, especially smoke stains and / or coffee stains. According to the gross weight of the composition, the amount of permonosulfate is generally from about 0.1% to about 50%, such as from about 0.75% to about 40% in one embodiment, from about 1% to about 20% in another embodiment, and from about 1% to about 10% in another embodiment. In a particular embodiment, the composition may include 0.5% to 10% by weight, 1% to 10% by weight, 2% to 8% by weight, 4% to 6% by weight, or about 5% by weight of permonosulfate. As used herein, when referring to a triple salt mixture, this amount refers only to the amount of permonosulfate (i.e., HSO5 salt, such as NaHSO5 or KHSO5).

[0021] The compositions of the present disclosure may optionally include one or more desiccants, such as hygroscopic desiccants. Examples of desiccants include, but are not limited to, phosphates, pyrophosphates and other polyphosphates, calcium lactate, calcium lactophosphate, double salts of calcium lactate, and mixtures thereof. Other desiccants include silica gel and precipitates, alumina, and mixtures thereof. Specific examples include, but are not limited to, dicalcium orthophosphate dihydrate, calcium pyrophosphate, tricalcium phosphate, calcium polymetaphosphate, insoluble sodium polymetaphosphate, potassium metaphosphate, tricalcium phosphate, trimagnesium phosphate and magnesium orthophosphate, hydrated alumina, aluminum silicate, zirconium silicate, bentonite, sodium sulfate, magnesium sulfate, calcium sulfate, beta-calcium pyrophosphate, or calcium carbonate. Pyrophosphates may also be used as anticalculus agents or as buffers in the present invention. Pyrophosphates suitable for the compositions of the present invention include dialkali metal pyrophosphates, tetraalkali metal pyrophosphates, and mixtures thereof. Disodium dihydrogen pyrophosphate, tetrasodium pyrophosphate, and tetrapotassium pyrophosphate in their unhydrated and hydrated forms are preferred species. In various embodiments, the amount of desiccant in the total composition is from about 0.1 wt % to about 60 wt %, from about 1 wt % to about 30 wt %, from about 1 wt % to about 10 wt %, or from about 1 wt % to about 5 wt %, or about 2%, about 3%, about 4%, or about 5%.

[0022] In some embodiments, the compositions of the present disclosure contain an abrasive. Examples of abrasives include, but are not limited to, calcium carbonate (precipitated or natural), sodium carbonate, sodium chloride, sodium bicarbonate, silicon dioxide, arginine bicarbonate, calcium phosphate, calcium pyrophosphate, dicalcium phosphate, zinc oxide, calcined alumina, or a combination thereof. In some embodiments, the abrasive is calcium carbonate, such as natural calcium carbonate, precipitated calcium carbonate, or a combination thereof. The composition may include one or more abrasives in an amount of 10% to 90% by weight of the composition, for example, 30-90%, or 50-90%, or 60-90%, or 70-90%, or 80-90%, or 85-90%, or about 86%.

[0023] In some embodiments, the compositions of the present disclosure contain a buffer. Examples of buffers include anhydrous carbonates such as sodium carbonate, sesquicarbonates, bicarbonates such as sodium bicarbonate, silicates, bisulfates, phosphates such as monopotassium phosphate and dipotassium phosphate, citrates, pyrophosphates (sodium and potassium salts), and combinations thereof. When the composition is dissolved in water, a mouthwash base, or a toothpaste base, the amount of buffer is sufficient to provide a pH of about 5 to about 9, preferably about 6 to about 8, and more preferably about 7. Typical amounts of buffer are about 5% to about 35%, in one embodiment about 10% to about 30%, and in another embodiment about 15% to about 25%, based on the total weight of the composition.

[0024] In some embodiments, the solid composition of the present invention contains a disintegrant. Disintegrants include natural starches such as corn starch and potato starch, directly compressible starches such as starch 1500, and as well as Modified starches such as carboxymethyl starch and sodium starch glycolate are available, as well as starch derivatives such as amylose. Other examples include cross-linked polyvinyl pyrrolidone, such as POLYPLASDONE and KOLLIDON The obtained crospovidone; modified cellulose, such as can be used as e.g. PHARMACEL and NYMCEL Cross-linked sodium carboxymethylcellulose obtained; alginic acid and sodium alginate; microcrystalline cellulose, e.g. and can be used as, for example IRP-88 obtained methacrylic acid divinylbenzene copolymer salt. Other examples of disintegrants include light silicic anhydride, calcium silicate, magnesium metasilicatealuminate and carboxymethyl cellulose. In the present invention, each of them can be used alone, or two or more of them can be used together. The typical amount of disintegrant is about 0.5% to about 20% by weight of the total weight of the composition, in one embodiment about 1% to about 5%, and in another embodiment about 1% to about 3%.

[0025] Composition of the present disclosure optionally contains the binding agent compatible with oxidant, preferably polymeric binding agent, and described binding agent increases the volume of composition, and when being in tablet form, helps each component of composition to be kept together.The example of suitable polymeric binding agent comprises for example starch, natural gum (for example, xanthan gum), cellulose gum, microcrystalline cellulose, maltodextrin, methylcellulose, cellulose ether, sodium carboxymethyl cellulose, ethyl cellulose, gelatin, Polyethylene Glycol, polyvinyl pyrrolidone, pectin, alginate, polyacrylamide, polyvinyl oxazolidone, polyvinyl alcohol and its mixture.Described binding agent also can comprise one or more non-polymer adhesives, for example dextrose, lactose, sucrose, sorbitol, mannitol, xylitol etc.Usually, binding agent is present in composition with the amount of about 10 % by weight to about 60 % by weight, about 15 % by weight to about 50 % by weight or about 25 % by weight to about 40 % by weight.

[0026] The solid composition of the present disclosure is optionally an effervescent composition. As used herein, the term "effervescent composition" means a composition that releases bubbles when in contact with water or an aqueous solution. When the solid composition of the present invention is an effervescent composition, it comprises an effervescent agent. Preferably, the effervescent agent is an effervescent couple comprising an acid and a base. When in contact with water, for example, when a composition such as a powder, granules or tablets is placed in a glass of water, the effervescent couple is activated. Water releases the acid and base and causes the acid and base to react with each other to produce carbon dioxide gas, which carbonates the aqueous composition.

[0027] The example of the acid that can be used for effervescent composition comprises citric acid, ascorbic acid, malic acid, adipic acid, tartaric acid, fumaric acid, succinic acid, acid sodium pyrophosphate, lactic acid, cyclamic acid and its acid salt and acid anhydride, and its mixture.The example of available acid anhydride comprises citraconic anhydride, glucono-D-lactone and succinic anhydride.The example of available acid salt comprises potassium hydrogen tartrate, acid citrate, sodium dihydrogen phosphate, disodium dihydrogen phosphate, sodium bisulfite and its combination.When effervescent, acid is present in the composition with the amount of about 10 % by weight to about 60 % by weight, about 15 % by weight to about 50 % by weight or about 25 % by weight to about 40 % by weight.

[0028] Preferably, the alkali of the effervescent composition is capable of producing carbon dioxide. Examples of suitable alkali carbonates include sodium bicarbonate, sodium carbonate, sodium sesquicarbonate, potassium carbonate, potassium bicarbonate, calcium carbonate, magnesium carbonate, magnesium oxide, sodium glycine carbonate, L-lysine carbonate, arginine carbonate, zinc carbonate, zinc oxide, and mixtures thereof. When effervescent, the alkali is present in the composition in an amount of about 10 % by weight to about 60 % by weight, about 15 % by weight to about 50 % by weight, or about 25 % by weight to about 40 % by weight.

[0029] The composition of the present disclosure optionally contains a lubricant. Various lubricants are suitable for use in the composition, including water-dispersible, water-soluble, water-insoluble lubricants and combinations thereof. Examples of available water-soluble lubricants include sodium benzoate, polyethylene glycol, L-leucine, adipic acid and combinations thereof. The composition may also include a water-insoluble lubricant, including, for example, stearates (such as magnesium stearate, calcium stearate and zinc stearate), oils (such as mineral oil, hydrogenated and partially hydrogenated vegetable oils and cottonseed oil) and combinations thereof. Other water-insoluble lubricants include, for example, animal fat, polyoxyethylene monostearate, talc and combinations thereof. When the composition is in tablet form, the composition preferably includes a sufficient amount of lubricant so that the composition can be shaped into tablets and discharged from a high-speed tablet press in tablet form. Typically, the amount of lubricant in the composition is about 1 wt % to about 15 wt %, about 1 wt % to about 12 wt %, about 2 wt % to about 10 wt % or about 3 wt % to about 8 wt %. In one embodiment, the composition comprises sodium benzoate in an amount of about 1 wt% to about 3 wt% and polyethylene glycol in an amount of about 1 wt% to about 5.5 wt%.

[0030] In addition to the permonosulfate salt, the solid composition of the present invention may optionally contain a whitening agent. Whitening agents are generally materials that can effectively whiten the tooth surface to which they are applied, and include reagents such as hydrogen peroxide and urea peroxide. In various embodiments, the composition of the present invention may optionally include a peroxide whitening agent, including a peroxide compound. A peroxide compound is an oxidizing compound that includes a divalent oxygen-oxygen group. Peroxide compounds include peroxides and hydroperoxides, such as hydrogen peroxide, alkali metal and alkaline earth metal peroxides, organic peroxides, peroxyacids, pharmaceutically acceptable salts thereof, and mixtures thereof. Alkali metal and alkaline earth metal peroxides include lithium peroxide, potassium peroxide, sodium peroxide, magnesium peroxide, calcium peroxide, barium peroxide, and mixtures thereof. Organic peroxides include urea peroxide (also known as urea hydroperoxide), glyceryl hydroperoxide, alkyl hydroperoxides, dialkyl peroxides, alkyl peroxyacids, peroxyesters, diacyl peroxides, benzoyl peroxide, and monoperoxyphthalate, and mixtures thereof. Peroxyacids and their salts include organic peroxyacids such as alkyl peroxyacids, as well as monoperoxyphthalates and mixtures thereof, and inorganic peroxyacid salts, such as persulfates, dipersulfates, percarbonates, perphosphates, perborates and persilicates of alkali metals and alkaline earth metals such as lithium, potassium, sodium, magnesium, calcium and barium, and mixtures thereof. In various embodiments, peroxide compounds include hydrogen peroxide, urea peroxide, sodium percarbonate and mixtures thereof. In some embodiments, the peroxide compound includes hydrogen peroxide. In some embodiments, the peroxide compound consists essentially of hydrogen peroxide. In some embodiments, non-peroxide whitening agents can be provided. Among those whitening agents available herein, the whitening agent includes non-peroxide compounds, such as chlorine dioxide, chlorite and hypochlorite. Chlorite and hypochlorite include chlorite and hypochlorite of alkali metals and alkaline earth metals such as lithium, potassium, sodium, magnesium, calcium and barium. Non-peroxide whitening agents also include colorants, such as titanium dioxide and hydroxyapatite. Optionally, one or more additional whitening agents are present in a tooth whitening effective total amount.In some embodiments, the composition further comprises an activator, such as tetraacetylethylenediamine.

[0031] The solid compositions may optionally further comprise other ingredients such as flavoring agents; fillers; fluoride sources; surfactants; preservatives such as sodium benzoate and potassium sorbate; coloring agents including, for example, dyes and pigments; and sweeteners.

[0032] Examples of fluoride sources include sodium fluoride, sodium monofluorophosphate, zinc fluoride, stannous fluoride, amine fluoride, etc. The fluoride source generally comprises 0.1% to 5% by weight of the composition, such as 0.1% to 2%, or 0.1% to 1%, or 0.5% to 1%, or about 0.75%.

[0033] Examples of surfactants that can be used are sodium lauryl sulfate, sorbitan fatty acid esters, polyoxyethylene (20) sorbitan monooleate (polysorbate 80 or Tween 80), polyethylene glycol fatty acid esters, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene alkyl ethers, polyoxyethylene polyoxypropylene alkyl ethers, polyoxyethylene polyoxypropylene block copolymers, polyoxyethylene alkylphenyl ethers, polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitol fatty acid esters, and polyoxyethylene glycerol fatty acid esters. In the present invention, each of these can be used alone, or two or more thereof can be used together. Typical amounts of surfactants are from about 0.5% to 10%, in one embodiment from 1% to 5%, in another embodiment from 2% to 4%, or about 3%, based on the total weight of the composition.

[0034] Examples of fillers are crystalline cellulose, ethyl cellulose, dextrin, various cyclodextrins (α-cyclodextrin, β-cyclodextrin and γ-cyclodextrin), sodium sulfate and its derivatives and pullulan.

[0035] Available flavoring agents include natural and synthetic flavoring sources, including, for example, volatile oils, synthetic flavoring oils, flavoring fragrances, oils, liquids, oleoresins, and extracts derived from plants, leaves, flowers, fruits, stems, and combinations thereof. Suitable flavoring agents include, for example, lemon oils, such as lemon, orange, grape, lime, and grapefruit; fruit essences, such as apple, pear, peach, grape, strawberry, raspberry, cherry, plum, pineapple, apricot, and other fruit flavors. Other available flavoring agents include, for example, aldehydes and esters (e.g., benzaldehyde (cherry, almond)), citral (i.e., α-citral (lemon, lime)), neral (i.e., β-citral (lemon, lime)), decanal (orange, lemon), aldehyde C-8 (citrus fruit), aldehyde C-9 (citrus fruit), aldehyde C-12 (citrus fruit), tolualdehyde (cherry, almond), 2,6-dimethyloctanal (unripe fruit), 2-dodecenal (citrus, tangerine), and mixtures thereof.

[0036] Suitable colorants include, for example, food, drug, and cosmetic (FD&C) colors, including, for example, dyes, lakes, and certain natural and derived colorants. Useful lakes include dyes absorbed on aluminum hydroxide and other suitable carriers.

[0037] Suitable sweeteners include stevia, sugars (e.g., sucrose, glucose, invert sugar, fructose, ribose, tagatose, sucralose, maltitol, erythritol, xylitol, and mixtures thereof), saccharin and its various salts (e.g., sodium and calcium salts of saccharin), cyclamate and its various salts, dipeptide sweeteners (e.g., aspartame), acesulfame potassium, dihydrochalcone, glycyrrhizin, and sugar alcohols (including, for example, sorbitol, sorbitol syrup, mannitol, and xylitol), and combinations thereof.

[0038] It should be understood that while the general properties of each of the above-mentioned classes of materials may differ, there may also be some common properties, and any given material may be used for multiple purposes in two or more of these classes of materials. All ingredients in a composition may have functions other than their primary function and may contribute to the overall properties of the composition, including its stability, efficacy, consistency, mouthfeel, flavor, odor, etc. For example, a binder may also act as a disintegrant, and vice versa.

[0039] Solid compositions of the present invention can be manufactured by techniques known in the art. Documents disclosing techniques for preparing solid compositions of the present invention include: U.S. Patents 4,886,669, 6,106,861, 6,596,311, 6,743,443, 6,811,793, 7,501,409, 7,815,897, 8,377,995, and U.S. Patent Application 2005 / 0169986, all of which are incorporated herein by reference in their entirety. Typically, the composition and optional components can be kneaded, filled in a mold, and subjected to compression molding using an organic solvent. The organic solvent can be an alcohol, such as methanol, ethanol, propanol, isopropanol, etc. The kneading and granulation operations performed by adding such adjuvants for preparing the formulation and by adding such solvents can be performed using conventionally used equipment. For example, a fluidized bed granulator, a tumbling granulator, an extrusion granulator, or a spray drying dryer can be used. Solid compositions can also be prepared by freeze drying.

[0040] Powders may be prepared by combining the ingredients and optionally calcium carbonate and, if desired, further orally acceptable additives and mixing in a conventional manner.

[0041] The powdered composition of the present disclosure can be made by comminuting the granular material (and optionally sieving) to an individual particle size having an average diameter of about 0.1 to about 1 mm, about 1 to about 500 microns, about 1 to about 250 microns, about 1 to about 150 microns, about 5 to about 100 microns, about 6 to about 35 microns, about 6 to about 13 microns. In one embodiment, the orally edible microparticles are comminuted such that in a bed having a volume of at least 125 cubic millimeters, at least 99% of the individual particles in the bed have an individual calcium carbonate particle size of about 1 to about 150 microns.

[0042] The granules can be prepared by any known method for preparing granules, such as dry granulation, layered granulation, impregnation granulation, and the like.

[0043] For dry granulation, the mixture of ingredients and optional additives is granulated by passing through a roller compactor, a roller granulator, or the like.

[0044] For layered granulation, a mixture similar to the above is added to a rolling inactive carrier while spraying a binder solution to adhere the mixture to the carrier using a centrifugal fluidized bed granulator, etc. Examples of the inactive carrier used in this method include crystals of sugars or inorganic salts, such as crystalline lactose, crystalline cellulose, crystalline sodium chloride, etc., and spherical particles, such as spherical particles of crystalline cellulose (brand name: Avicel SP, Asahi Kasei Corporation), spherical particles of crystalline cellulose and lactose (brand name: Nonpareil-NP-5 and NP-7, Freund Co., Ltd.), spherical particles of purified white sugar (brand name: Nonpareil-103, Freund Co., Ltd.), spherical particles of lactose and α-starch, etc.

[0045] For impregnation granulation, a solution containing potassium permonosulfate and other ingredients at appropriate concentrations is mixed with a porous carrier so that a sufficient amount of the solution remains in the carrier's cavities, and then dried to remove the solvent. Examples of usable porous carriers include magnesium aluminum silicate (trade name: Neusiline, Fuji Chemical Industry Co., Ltd.) and calcium silicate (Florite, Eisai Co., Ltd.). Examples of solvents include ethanol and methanol.

[0046] In another aspect, the present disclosure provides a method for bleaching teeth to remove or reduce stubborn stains, comprising mixing a solid oral care composition as described herein (e.g., any one of compositions 1 or 1.1-26) into water, a mouthwash base, or a toothpaste base, optionally until the composition dissolves, and then applying the composition to the teeth. The composition can be applied to the teeth in the form of a solution or suspension. As a solution, such as a mouthwash, the composition can be used as an irrigant. As a suspension, such as a paste, the composition can be applied to the teeth with a toothbrush or similar device.

[0047] In another aspect, the present disclosure provides the use of a solid oral care composition as described herein (e.g., any one of compositions 1 or 1.1 to 26) for removing or reducing stubborn tooth stains, such as smoke stains and / or coffee stains. Such uses may comprise mixing the solid oral care composition into water, a mouthwash base, or a toothpaste base, optionally until the composition is dissolved or homogenized, and then applying the composition to the teeth. The composition can be applied to the teeth as a solution, a suspension, or a paste. As a solution, such as a mouthwash, the composition can be used as a rinse. As a suspension, such as a paste, the composition can be applied to the teeth by a toothbrush or similar device.

[0048] The term "mouthwash" or "mouth rinse" generally refers to a liquid formulation used to rinse the surfaces of the oral cavity and provide the user with a feeling of oral cleanliness and freshness. A mouthwash is an oral composition that is not intended to be swallowed for the purpose of systemic administration of a therapeutic agent, but is instead applied to the oral cavity, used to treat the oral cavity, and subsequently expectorated. Mouthwash compositions will typically contain an aqueous continuous phase.

[0049] A typical mouthwash composition is composed of a liquid carrier such as water, a humectant such as glycerol, sorbitol, or propylene glycol, a surfactant such as Pluronics or sodium lauryl sulfate, a sweetener such as sodium saccharin or xylitol, a flavoring agent, a coloring agent, and a preservative such as potassium sorbate or sodium benzoate. The composition may also contain a buffering agent (e.g., sodium phosphate) capable of buffering to a final pH of 6.5 to 8, an anticaries agent (e.g., sodium chloride), and an antibacterial agent (e.g., cetylpyridinium chloride).

[0050] A solid oral care composition (Composition 1) for removing or reducing stubborn tooth stains (eg, smoke stains and / or coffee stains) is provided, comprising a tooth whitening effective amount of an alkali metal salt of peroxymonosulfate.

[0051] 1.1. Composition 1, wherein the peroxymonosulfate is sodium peroxymonosulfate, potassium peroxymonosulfate, lithium peroxymonosulfate, or a combination thereof;

[0052] 1.2. Composition 1 or 1.1, wherein the peroxymonosulfate is potassium peroxymonosulfate;

[0053] 1.3. Composition 1.2, wherein the potassium peroxymonosulfate is a triple salt of potassium peroxymonosulfate, potassium bisulfate, and potassium sulfate, optionally wherein the triple salt comprises about 47% to 50% by weight of potassium peroxymonosulfate, e.g., 47% or 50% by weight of potassium peroxymonosulfate;

[0054] 1.4. Any of the preceding compositions, wherein the composition comprises an effective amount of a peroxymonosulfate salt, which comprises from 0.1% to 50% by weight of the composition, e.g., from 0.75% to 40%, or from 1% to 20%, or from 1% to 10%, or from 0.5% to 10%, or from 1% to 10%, or from 2% to 8%, or from 4% to 6%, or about 5% by weight of the composition;

[0055] 1.5. Any of the preceding compositions, further comprising an abrasive, optionally wherein the abrasive comprises 10% to 95%, e.g., 30% to 95%, or 50% to 95%, or 60% to 95%, or 70% to 95%, or 80% to 95%, or 85% to 95%, or 85% to 90%, or about 86%, by weight of the composition;

[0056] 1.6. Composition 1.5, wherein the abrasive is selected from the group consisting of calcium carbonate (precipitated or natural), sodium carbonate, sodium chloride, sodium bicarbonate, silica, arginine bicarbonate, calcium phosphate, calcium pyrophosphate, dicalcium phosphate, zinc oxide, calcined alumina, or combinations thereof;

[0057] 1.7. Composition 1.5 or 1.6, wherein the abrasive is natural calcium carbonate, precipitated calcium carbonate, or a mixture thereof;

[0058] 1.8. Any of the foregoing compositions, further comprising a desiccant;

[0059] 1.9. Composition 1.8, wherein the desiccant is selected from the group consisting of calcium lactate, calcium lactophosphate, double salts of calcium lactate, phosphates, pyrophosphates, polyphosphates, orthophosphates, metaphosphates, silica, alumina, bicarbonates, polymetaphosphates, aluminum silicate, zirconium silicate, bentonite, and combinations thereof;

[0060] 1.10. Any of the preceding compositions, wherein the desiccant comprises pyrophosphate, alumina, sodium bicarbonate, or a combination thereof;

[0061] 1.11. Any of the preceding compositions, wherein the desiccant comprises an alkali metal salt of pyrophosphate, such as tetrasodium pyrophosphate or tetrapotassium pyrophosphate;

[0062] 1.12. Any of the preceding compositions, wherein the composition is in tablet, powder, or granule form and packaged in an anhydrous environment;

[0063] 1.13. Any of the preceding compositions, wherein the composition is packaged in a single-use container, including a tin, tube, or sachet;

[0064] 1.14. Any of the preceding compositions, wherein the composition contains no water or contains less than 4% water by weight, or less than 3% water by weight, or less than 2% water by weight, or less than 1% water by weight, or less than 0.5% water by weight, or from about 0.0001% water to about 4% water by weight, or from about 0.0001% water to about 0.5% water by weight, or from about 0.0001% water to about 0.1% water, or from about 0.001% water to about 4% water by weight;

[0065] 1.15. Any of the preceding compositions, wherein the desiccant is present in an amount of about 0.1% to about 60%, about 1% to about 30%, about 1% to about 10%, or about 1% to about 5%, or about 2%, or about 3%, or about 4%, or about 5% by weight of the total composition;

[0066] 1.16. Any of the preceding compositions comprising a disintegrant selected from the group consisting of natural starches, e.g., corn starch, potato starch; directly compressible starches, e.g., starch 1500; modified starches, e.g., carboxymethyl starch and sodium starch glycolate; starch derivatives, e.g., amylose; cross-linked polyvinyl pyrrolidone, e.g., crospovidone; modified cellulose, e.g., cross-linked sodium carboxymethyl cellulose; alginic acid; sodium alginate; microcrystalline cellulose; methacrylic acid-divinylbenzene copolymer salt; light silicic anhydride; calcium silicate; magnesium aluminometasilicate; carboxymethyl cellulose; and mixtures thereof;

[0067] 1.17. Any of the preceding compositions comprising a binder, wherein the binder is selected from the group consisting of starch, natural gums (e.g., xanthan gum), cellulose gum, microcrystalline cellulose, maltodextrin, methylcellulose, cellulose ethers, sodium carboxymethylcellulose, ethylcellulose, gelatin, polyethylene glycol, polyvinyl pyrrolidone, pectin, alginates, polyacrylamides, polyvinyl oxazolidinone, polyvinyl alcohol, and mixtures thereof;

[0068] 1.18. Composition 1.17, wherein the binder is present in the composition in an amount from 10% to about 60% by weight, or from about 15% to about 50% by weight, or from about 25% to about 40% by weight;

[0069] 1.19. Any of the preceding compositions, further comprising a buffering agent selected from the group consisting of anhydrous carbonates, such as sodium carbonate, sesquicarbonates, bicarbonates, such as sodium bicarbonate, silicates, bisulfates, citrates, phosphates, such as monopotassium phosphate and dipotassium phosphate, or combinations thereof, in an amount from about 5.0% to about 35%, or from about 10% to about 30%, or from about 15% to about 25%, based on the total weight of the composition;

[0070] 1.20. Any of the preceding compositions, wherein the composition is effervescent and comprises an effervescent acid and an effervescent base;

[0071] 1.21. Composition 1.20 wherein the effervescent acid is citric acid, ascorbic acid, malic acid, adipic acid, tartaric acid, fumaric acid, succinic acid, sodium acid pyrophosphate, lactic acid, caproic acid, citraconic anhydride, glucono-D-lactone, succinic anhydride, potassium bitartrate, acid citrate, sodium dihydrogen phosphate, disodium dihydrogen phosphate, sodium bisulfite, and combinations thereof, and is present in the composition in an amount from 10% to about 60%, from about 15% to about 50%, or even from about 25% to about 40% by weight;

[0072] 1.22. Composition 1.20 or 1.21, wherein the effervescent base is sodium bicarbonate, sodium carbonate, sodium sesquicarbonate, potassium carbonate, potassium bicarbonate, calcium carbonate, magnesium carbonate, magnesium oxide, sodium glycine carbonate, L-lysine carbonate, arginine carbonate, zinc carbonate, zinc oxide, and mixtures thereof, and is present in the composition in an amount from 10% to about 60%, or from about 15% to about 50%, or from about 25% to about 40%, by weight;

[0073] 1.23. Any of the preceding compositions, further comprising a lubricant in an amount of about 1 wt % to about 15 wt %, or about 1 wt % to about 12 wt %, or about 2 wt % to about 10 wt %, or about 3 wt % to about 8 wt %;

[0074] 1.24. Any of the preceding compositions, comprising an additional whitening agent;

[0075] 1.25. Any of the preceding compositions further comprising one or more flavoring agents, one or more fillers, one or more surfactants, one or more coloring agents, or any combination of two or more thereof.

[0076] 1.26. Any of the preceding compositions which is a dentifrice.

[0077] Examples

[0078] Exemplary embodiments of the present disclosure will be described with reference to the following examples, which are included for purposes of illustration and not limitation of the scope of the invention.

[0079] In the examples and other descriptions of the present invention, chemical symbols and terms have their common and customary meanings. Unless otherwise indicated, temperatures are in degrees Celsius. Amounts of components are expressed as weight percent based on the stated standard; if no other standard is stated, the total weight of the composition is used. Various names of chemical components include those listed in the CTFA International Cosmetic Ingredient Dictionary (Cosmetics, Toiletry and Fragrance Association, Inc., 7th Edition, 1997).

[0080] Example 1: Bleaching of tobacco active substances

[0081] Loose tobacco leaf was soaked in the water 24 hours, filtered to produce yellow-brown solution then, it is diluted with 0.1M phosphate buffer (pH 7.5), until the absorbance at the 405nm place is between 0.75 and 1.0 on the Perkin-Elmer Envision multi-plate reader. This tobacco solution of 5mL is added in one group of scintillation vials. Bleach is added in each bottle: add Caroat to 5%w / v (about 2.5%w / v KHSO ), Caroat to 10%w / v (about 5%w / v KHSO ), or hydrogen peroxide (HP) to 5%w / v (using 35%w / v hydrogen peroxide solution). In 30 minutes process, measure the absorbance of every kind of solution at the 405nm place. The reduction of absorbance is indicated to the bleaching of the tobacco active substance of painting.

[0082] Table 1

[0083]

[0084] The results showed that both 2.5% w / v MPS and 5% w / v MPS were superior to 5% hydrogen peroxide in bleaching active agents from tobacco leaves with stained teeth.

[0085] Example 2: MPS is more effective than hydrogen peroxide in removing smoke stains from cattle incisors

[0086] The incisors are individually mounted in a resin block and dyed with a tobacco solution. The incisors are then brushed with a grinding paste until the initial L value is between 60 and 65 (see below). The mounted incisors are then placed in a tray and inserted into an automatic toothbrush machine, where a commercial toothbrush head is used to brush the incisors. Under a pressure of 0.25 kg, the teeth are brushed at 120 times per minute for two minutes. A slurry consisting of a test dentifrice and artificial saliva in a 1:1 weight ratio is used for brushing. After brushing is complete, the remaining dentifrice is rinsed with distilled water, the teeth are gently dipped in dry water, and then spectral measurement is performed. This cycle is repeated 14 times.

[0087] The change in whiteness was calculated using the parameter W*, which is a measure of whiteness and is calculated as: W* = ((a* - 0) 2 +(b*-0) 2 +(L*-100) 2 ) 1 / 2 The whiteness change ΔW* is then calculated as: ΔW*=W*treatment--W*baseline. An increase in the ΔW* value indicates a progressive whitening of the teeth and, therefore, a bleaching of stubborn smoke stains.

[0088] An MPS-based dentifrice according to the present invention was compared to a matching placebo containing no MPS. The results are shown in Table 2 below. The experiment showed that the MPS-based dentifrice bleached significantly better smoke stains on bovine tooth enamel than the placebo containing no MPS. The composition of the MPS-based dentifrice is shown in Table 4 below.

[0089] Table 2: External scrubbing (MPS vs. placebo)

[0090] deal with 0 2 4 6 8 10 12 14 5% MPS 0.00 2.62 3.81 3.81 5.20 6.88 7.11 8.23 Placebo 0.00 0.92 1.21 2.06 2.59 2.84 3.23 3.70

[0091] Additionally, a 5% MPS-based dentifrice was also compared side-by-side with a 2% hydrogen peroxide dentifrice (in the same procedure as above). The results are shown in Table 3 below. The experiments showed that the MPS-based dentifrice produced significantly better bleaching of smoke stains on bovine tooth enamel than the hydrogen peroxide-based dentifrice.

[0092] Table 3: In vitro scrubbing (MPS and hydrogen peroxide)

[0093] deal with 0 2 3 4 6 8 9 10 12 14 5% MPS 0.00 2.62 3.81 3.81 5.20 6.88 7.11 8.23 2% HP 0.00 0.74 1.43 2.30 3.20 3.01

[0094] The compositions of the MPS-based dentifrice and its matching placebo are shown in Table 4 below.

[0095] Table 4: MPS-whitening powder and matching placebo (% w / w)

[0096]

[0097] The composition of the 2% hydrogen peroxide dentifrice is shown below in Table 5. The cross-linked polyvinylpyrrolidone-hydrogen peroxide complex used was approximately 18% hydrogen peroxide by weight.

[0098] Table 5: HP dentifrice (% w / w)

[0099] Whitening Wetting agent 52.7％ polymer 11.75％ Anti-tartar agents 1.90％ Sodium monofluorophosphate 0.76％ Silicon dioxide 1.75％ calcium pyrophosphate 15.00％ Flavorings, colorings, preservatives 3.14％ Sodium lauryl sulfate 2.00％ Hydrogen peroxide-cPVP complex 11.00％ total 100％

[0100] The present invention has been described with reference to illustrative examples, but it should be understood that the present invention is not limited to the disclosed embodiments. Changes and modifications that may be made by those skilled in the art after reading this specification are also within the scope of the present invention, which is defined in the appended claims.

Claims

1. A toothpaste comprising a toothpaste base and a solid oral care composition, wherein the solid oral care composition comprises 2 to 8 weight percent of potassium permonosulfate and 70 to 90 weight percent of an abrasive, wherein the abrasive is selected from the group consisting of calcium carbonate, calcium phosphate, calcium pyrophosphate, dicalcium phosphate, and combinations thereof.

2. The toothpaste according to claim 1, wherein the potassium peroxymonosulfate is provided in the form of a triple salt of potassium peroxymonosulfate, potassium hydrogensulfate and potassium sulfate.

3. The toothpaste of claim 2, wherein the triple salt comprises 47 to 50 wt% potassium peroxymonosulfate.

4. Toothpaste according to any one of claims 1 to 3, wherein the abrasive is selected from calcium pyrophosphate, dicalcium phosphate and combinations thereof.

5. A toothpaste according to any one of claims 1 to 3, wherein the solid oral care composition comprises 4 to 6 wt% potassium peroxymonosulfate.

6. The toothpaste of claim 5, wherein the solid oral care composition comprises 5 wt% potassium peroxymonosulfate.

7. The toothpaste according to any one of claims 1 to 3, wherein the solid oral care composition is granulated to have a particle size of 1 to 150 microns.

8. A method of bleaching teeth to remove or reduce stubborn stains, comprising applying a toothpaste according to any one of claims 1 to 7 to the teeth.

9. The method of claim 8, wherein the stubborn stain is a smoke stain.

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