Oral care compositions comprising ascorbic acid derivatives

Abstract

The oral care compositions described herein comprise an ascorbic acid derivative as a tooth whitening agent. The oral care compositions described herein are stable until use, affordable, safe, easy to use, and do not require special equipment or trained personnel to apply.

Description

Technical Field

[0001] In one aspect, this disclosure relates to oral care compositions for whitening teeth. In one aspect, the oral care compositions described herein contain ascorbic acid derivatives as teeth whitening agents. In another aspect, the oral care compositions described herein are stable until use, reasonably priced, safe, easy to use, and do not require special equipment or trained personnel for application. Background Technology

[0002] Food, tobacco, drugs, and beverages such as coffee, tea, and red wine stain teeth over time. Teeth whitening can be achieved by using teeth whitening products. Over the years, oral care compositions and methods for whitening teeth have been developed. Some of the most common oral care compositions used for teeth whitening contain peroxide derivatives. Peroxide compounds can bleach teeth, remove stains, and kill cariogenic bacteria. However, the lack of compound stability, cost, and roughness on teeth and gums represent drawbacks of the available methods. Consumers are increasingly turning to “natural” ingredients in their oral care products. “Natural” ingredients should be understood as “naturally derived” and “naturally sourced” ingredients.

[0003] Therefore, there is a clear need for natural oral care compositions for teeth whitening that are stable until use, reasonably priced, safe, easy to use, and do not require special equipment or trained personnel to apply. Summary of the Invention

[0004] This disclosure relates to oral care compositions for whitening teeth. The oral care compositions of this disclosure contain a reducing agent as a teeth whitening agent. Conventional whitening agents are thought to act as oxidizing agents (accepting electrons) to bleach tooth stains. Unbound by theory, ascorbic acid and its derivatives are capable of bleaching tooth stains by acting as reducing agents (losing electrons). In some aspects, the oral care compositions described herein contain a whitening agent in a buffered oral care composition that provides protection against tooth erosion.

[0005] In one aspect, the oral care compositions of this disclosure do not contain bleaching agents or whitening agents such as hydrogen peroxide or hydrogen peroxide sources, such as urea peroxide, or metal chlorites or peroxide salts or complexes (e.g., peroxyphosphate, peroxycarbonate, perborate, peroxysilicate), or persulfates (e.g., calcium peroxyphosphate, sodium perborate, sodium percarbonate, sodium peroxyphosphate and potassium persulfate), or hydrogen peroxide polymer complexes (e.g., peroxide-polyvinylpyrrolidone polymer complexes).

[0006] In one aspect, the oral care composition of this disclosure comprises an ascorbic acid derivative as a whitening agent. Ascorbic acid is a natural, water-soluble vitamin, commonly known as vitamin C. Ascorbic acid exists as two enantiomers, usually expressed as "l" (for "levorotatory") and "d" (for "devorotatory"). The "l" isomer is the most commonly encountered isomer. Ascorbic acid is also known as L(+)-ascorbic acid or l-ascorbic acid.

[0007] In one aspect, the oral care composition of this disclosure comprises an ascorbic acid derivative selected from: L-ascorbic acid, calcium ascorbate, L-calcium ascorbate dihydrate, magnesium ascorbate, potassium ascorbate, magnesium L-ascorbate phosphate (also known as magnesium ascorbate phosphate or magnesium ascorbate phosphate salt), L-ascorbic acid 2-phosphate sesquimagnesium salt hydrate, (+)L-ascorbate sodium, dehydro-L-(+)-ascorbic acid Dimers, sodium ascorbate phosphate (also known as: sodium ascorbate phosphate, sodium l-ascorbate phosphate, 2-phosphoryl-L-ascorbate trisodium salt, L-ascorbate 2-phosphate trisodium salt or L-ascorbate-2-phosphate sodium salt), ascorbate-2-glucoside, dipalmitoyl ascorbate, ascorbate methylsilanol pectate, stearate ascorbate, disodium ascorbate sulfate, 6-palmitoyl ascorbate and combinations thereof.

[0008] In one embodiment, the oral care composition of this disclosure is selected from the following forms: toothpaste, dental cleaning agent, mouthwash, mouth rinse liquid, topical oral gel, and denture cleaner. In another embodiment, the oral care composition of this disclosure is selected from the following forms: dental strips, beads, toothpaste strips, ointments, dental floss, chewing gum, lozenges, and tooth powder.

[0009] In another aspect, the oral care compositions of this disclosure may comprise anti-plaque agents, anti-gingivitis agents, anti-malodor agents, anti-tartar agents, anti-calculus agents, anti-erosion agents, and / or combinations thereof. Optionally, the oral care compositions of this disclosure may comprise abrasives, surfactants, viscosity and rheology modifiers, humectants, sweeteners, flavoring agents, colorants, preservatives, and / or combinations thereof. Optionally, the oral care compositions of this disclosure comprise water. Optionally, the oral care compositions of this disclosure may comprise pigments, opacifiers, polymer complexes, surfactants, bicarbonates, pH adjusters, foam adjusters, thickeners, antibacterial agents, anti-caries agents, fluoride ion sources, stannous ion sources, zinc ion sources, and / or combinations thereof.

[0010] In one aspect, the compositions of this disclosure contain a relatively large amount of sodium stearate. Without being bound by theory, a relatively large amount of sodium stearate can help toothpaste change color, which can occur in the presence of ascorbic acid derivatives (e.g., sodium ascorbate phosphate or sodium and 6-palmitoyl ascorbate).

[0011] In another aspect, any of the compositions of this disclosure, such as composition 1.0 and below, can be used in methods for removing surface enamel stains (e.g., non-intrinsic stain removal). In one aspect, without being bound by theory, the phosphate on the ascorbic acid derivative can help remove stains from the enamel surface, while the fatty acid chain can help anchor the derivative to the surface to perform this task. Detailed Implementation

[0012] It should be understood that the foregoing general description of this disclosure and the following detailed description are both exemplary and illustrative only, and not intended to limit the claimed disclosure.

[0013] As used herein, unless otherwise specified, the use of the singular includes the plural. As used throughout, the term "range" is used as a shorthand to describe each value within the range and each individual value. Any value within the range may be chosen as the endpoint of the range. As used herein, the use of "compound comprising several isomers or stereoisomers" includes all isomer forms of the compound.

[0014] Unless otherwise stated, all percentages of oral care composition components given in this specification are based on the weight of 100% of the total oral care composition or formulation.

[0015] As used herein, "oral care composition" means a composition whose intended use includes oral care, oral hygiene, and / or oral appearance, or whose intended method of use includes application to the oral cavity, and refers to a palatable and safe composition for topical application to the oral cavity and for providing benefits to the teeth and / or oral cavity. Therefore, the term "oral care composition" specifically excludes compositions that are highly toxic, unpalatable, or otherwise unsuitable for application to the oral cavity. In some embodiments, the oral care composition is not intended to be swallowed but is retained in the oral cavity for a duration sufficient to affect the intended utility. Oral care compositions disclosed herein can be used in non-human mammals such as companion animals (e.g., dogs and cats) and can be used in humans. In some embodiments, oral care compositions disclosed herein are intended for human use. Oral care compositions include, for example, dental floss and mouthwash. In some embodiments, this disclosure provides mouthwash formulations.

[0016] As used in this article, "orally acceptable" means a material that is safe and palatable at relevant concentrations used in oral care preparations such as mouthwash or dental floss.

[0017] As used herein, “orally acceptable carrier” means any carrier that can be used to formulate the oral care compositions disclosed herein. An orally acceptable carrier is harmless to mammals at the amounts disclosed herein when it remains in the mouth without being swallowed for a duration sufficient to allow effective contact with the tooth surface as required herein. Generally, orally acceptable carriers are harmless even if unintentionally swallowed. Suitable orally acceptable carriers include, for example, one or more of the following: water, thickeners, buffers, humectants, surfactants, abrasives, sweeteners, flavoring agents, pigments, dyes, cariogenic agents, antimicrobial agents, whitening agents, desensitizing agents, vitamins, preservatives, enzymes, and mixtures thereof.

[0018] Oral care compositions are further defined as products that, during normal use, are retained in the oral cavity for a duration sufficient to substantially contact all tooth surfaces and / or oral tissues for the purpose of oral activity, rather than for the purpose of systemic application of a specific therapeutic agent intended to be swallowed. Examples of such oral care compositions include, but are not limited to, toothpaste, dental cleaning agents, mouthwash, mouth rinse liquid, topical oral gels, denture cleaners, dental strips, beads, varnishes, dental floss, toothpaste strips, chewing gum, lozenges, tooth powder, etc.

[0019] As used herein, the term "toothpaste" refers to a paste, gel, or emulsion applied to a toothbrush to clean teeth. It should be understood that toothpaste, for example, is typically diluted with water upon use, while mouthwash is typically not.

[0020] As used herein, unless otherwise stated, the term "dental cleaning agent" refers to a paste, gel, or liquid formulation. A dental cleaning agent composition may be in any desired form, such as deep streaks, surface streaks, multilayers, a paste surrounded by a gel, or any combination thereof. Alternatively, an oral care composition may be a two-phase formulation dispensed from a spaced-apart dispenser.

[0021] As used herein, the terms "mouthwash" or "mouth rinse liquid" refer to oral care compositions that are substantially liquid in nature, such as sprays or rinses. In such formulations, the oral care composition typically has an aqueous phase comprising water or a mixture of water and alcohol. Furthermore, in several embodiments, the oral care composition comprises a humectant and a surfactant as described below. Typically, the weight ratio of water to alcohol is in the range of 1:1 to 20:1, preferably 3:1 to 10:1, and more preferably 4:1 to 6:1. The total amount of the water and alcohol mixture in this type of formulation is typically 70% to 99.9% by weight of the formulation. In several embodiments, the alcohol is typically ethanol or isopropanol.

[0022] As used herein, the term "topical oral gel" refers to a mixture prepared and immediately transferred into a retainer (e.g., for use with a retainer whitening gel), and which a person can wear for a sustained period of time. Teeth in contact with the mixture will be treated. For use with a retainer, the mixture may be in the form of a low-viscosity liquid or gel. In some embodiments, the whitening agent of this disclosure is formulated in a crosslinked copolymer comprising polyacrylic acid (… In an oral care composition of polymers, glycerin and water.

[0023] As used herein, the term "ointment" refers to a stock solution or mixture of stock solution and water applied to teeth as an ointment formulation, for example, wherein a gel can remain on the teeth for an extended period of time for effective treatment. When the oral care composition is in the form of a gel or ointment, the oral care composition of this disclosure is a viscous liquid, preferably a gel, which maintains its consistency during storage so that the product can be applied to the tooth surface with a soft applicator pen or brush. In some embodiments, the whitening agent of this disclosure is formulated in an oral care composition comprising a hydrophobic copolymer, said hydrophobic copolymer including at least one of: octylacrylamide / acrylate / butylaminoethyl methacrylate copolymer, VA / butyl maleate / isoborneol acrylate copolymer, acrylate / tert-butylacrylamide copolymer, polyvinylpyrrolidone / vinyl acetate copolymer, triacontylpolyvinylpyrrolidone copolymer, acrylate / dimethylaminoethyl methacrylate copolymer (by name) (for sale), 2-methyl-2-acrylate-2-methylpropyl ester with 2-acrylic acid and N-(1,1,3,3-tetramethylbutyl)-2-acrylamide polymer (as named) (sales) and / or a combination thereof.

[0024] As used herein, the term "denture cleaner" refers to a cleaning agent used on dentures when they are removed from the mouth. As used herein, the term "tooth strip" refers to a disposable strip placed directly on the teeth containing an enamel-safe whitening gel. As used herein, the term "tooth powder" refers to a powder used for cleaning teeth. As used herein, the term "toothpaste strip" refers to toothpaste dispensed in strip form. As used herein, the term "active ingredient" refers to a compound that provides benefit or improvement to a target tissue when applied to that tissue. Active ingredients can be delivered in any form of oral care preparation, such as toothpaste, clear paste, gel, mouthwash, powder, cream, tooth strip, spray, chewing gum, or any other form known in the art. The terms "active ingredient" and "reagent" are used interchangeably in this disclosure. As used herein, "teeth" refers to natural teeth, dentures, dental plates, fillings, dental caps, crowns, bridges, dental implants, and any other hard-surface dental prosthesis permanently or temporarily fixed in the oral cavity. As used herein, “whitening” refers to a change in the visual appearance of teeth, wherein the teeth have a lighter hue. As used herein, “apply” means any method of placing the oral care composition of this disclosure into contact with the tooth surface.

[0025] As used herein, those skilled in the art will understand that "ascorbate" may be referred to by several names in the literature. As used herein, "ascorbic acid derivatives" in this disclosure include all isomers, diastereomers, and enantiomers of the compounds cited.

[0026] whitening agent

[0027] This disclosure provides oral care compositions comprising a whitening agent containing an ascorbic acid derivative. Typically, the ascorbic acid derivative of this disclosure can be selected from any of the following: L-ascorbic acid, calcium ascorbate, L-calcium ascorbate dihydrate, magnesium ascorbate, potassium ascorbate, magnesium L-ascorbate phosphate, sesqui-magnesium L-ascorbate 2-phosphate hydrate, sodium (+)L-ascorbate, dehydro-L-(+)-ascorbic acid dimer, sodium ascorbate phosphate, ascorbate-2-glucoside, dipalmitoyl ascorbate, ascorbate methylsilanol pectate, stearate ascorbate, disodium ascorbate sulfate, and 6-palmitoyl ascorbate.

[0028] In one aspect, the ascorbic acid derivative of this disclosure is sodium ascorbate phosphate and 6-palmitate ascorbate. In another aspect, the content of the ascorbic acid derivative in the oral care composition is from 0.5% to 5% by weight of the total weight of the oral care composition. In some aspects, the content of the ascorbic acid derivative in the oral care composition is about 0.5% by weight, or about 0.75% by weight, or about 1% by weight, or about 1.25% by weight, or about 1.5% by weight, or about 1.75% by weight, or about 2% by weight, or about 2.25% by weight, or about 2.5% by weight, or about 2.75% by weight, or about 3% by weight, or about 3.25% by weight, or about 3.5% by weight, or about 3.75% by weight, or about 4% by weight, or about 4.25% by weight, or about 4.5% by weight, or about 4.75% by weight, or about 5% by weight of the total weight of the oral care composition.

[0029] In one embodiment, this disclosure provides an oral care composition for whitening teeth, wherein the composition comprises a whitening agent selected from sodium ascorbate phosphate, 6-palmitate ascorbate, and combinations thereof. In another embodiment, this disclosure provides an oral care composition for whitening teeth, wherein the composition comprises a whitening agent of sodium ascorbate phosphate in an amount of 0.5% to 5% by weight relative to the total oral care composition.

[0030] In one embodiment, this disclosure provides an oral care composition for whitening teeth, wherein the oral care composition comprises a whitening agent as sodium ascorbate phosphate, for example, wherein the amount of sodium ascorbate phosphate is from about 1.0% by weight to about 3.0% by weight relative to the total oral care composition. In another embodiment, this disclosure provides an oral care composition for whitening teeth, said oral care composition comprising a whitening agent as sodium ascorbate phosphate in an amount of about 1.5% by weight relative to the total oral care composition.

[0031] In one embodiment, this disclosure provides an oral care composition for whitening teeth, the oral care composition comprising, in an amount of about 2.5% by weight relative to the total oral care composition, a whitening agent of sodium ascorbate phosphate.

[0032] In one embodiment, this disclosure provides an oral care composition for whitening teeth, the oral care composition comprising a whitening agent of 6-palmitoyl ascorbate in an amount of 0.5% to 5% by weight relative to the total oral care composition. In one embodiment, this disclosure provides an oral care composition for whitening teeth, the oral care composition comprising a whitening agent of 6-palmitoyl ascorbate in an amount of about 1.5% by weight relative to the total oral care composition. In one embodiment, this disclosure provides an oral care composition for whitening teeth, the oral care composition comprising a whitening agent of 6-palmitoyl ascorbate in an amount of about 2.5% by weight relative to the total oral care composition. In one embodiment, this disclosure provides an oral care composition for whitening teeth, the oral care composition comprising a whitening agent of 6-palmitoyl ascorbate in an amount of 1.0% to 3.0% by weight relative to the total oral care composition.

[0033] In one aspect, the oral care compositions of this disclosure are free of peroxides or chemical whitening agents that are not ascorbic acid derivatives.

[0034] In some embodiments, the oral care composition of this disclosure includes a whitening agent, wherein the whitening agent comprises ascorbate.

[0035] For example, in one aspect, the oral care composition of this disclosure comprises one or more ascorbic acid salts selected from: calcium ascorbate, calcium l-ascorbate dihydrate, magnesium ascorbate, potassium ascorbate, magnesium L-ascorbate phosphate, sesqui-magnesium L-ascorbate 2-phosphate hydrate, sodium (+)L-ascorbate, dehydro-l-(+)-ascorbate dimer, sodium ascorbate phosphate, ascorbate dipalmitoate, ascorbate methylsilanol pectate, ascorbate stearate, disodium ascorbate sulfate, and 6-palmitoate ascorbate.

[0036] In some embodiments, the oral care composition of this disclosure comprises a whitening agent, wherein the whitening agent comprises an ascorbic acid derivative selected from: L-ascorbic acid, calcium ascorbate, calcium l-ascorbate dihydrate, magnesium ascorbate, potassium ascorbate, magnesium L-ascorbate phosphate, sesqui-magnesium L-ascorbate 2-phosphate hydrate, sodium (+)L-ascorbate, dehydro-l-(+)-ascorbic acid dimer, sodium ascorbate phosphate, ascorbate-2-glucoside, dipalmitoyl ascorbate, ascorbate methylsilanol pectate, stearate ascorbate, disodium ascorbate sulfate, and 6-palmitoyl ascorbate.

[0037] In some embodiments, the oral care composition of this disclosure comprises a whitening agent, wherein the whitening agent comprises sodium ascorbate phosphate. In some embodiments, the oral care composition of this disclosure comprises a whitening agent and comprises an orally acceptable carrier, wherein the whitening agent comprises sodium ascorbate phosphate.

[0038] In some embodiments, the oral care composition of this disclosure comprises sodium ascorbate phosphate, an orally acceptable carrier, and further comprises one or more ingredients selected from: pH adjusters, anti-erosion agents, foaming agents, thickeners, flavoring agents, antibacterial agents, desensitizing agents, anti-caries agents, fluoride ion sources, anti-tartar agents, abrasives, anti-spotting agents, polymer complexes, surfactants, humectants, and / or combinations thereof.

[0039] In some embodiments, the oral care composition of this disclosure includes a whitening agent, wherein the whitening agent comprises 6-palmitoyl ascorbate.

[0040] In some embodiments, the oral care composition of this disclosure comprises a whitening agent and an orally acceptable carrier, wherein the whitening agent comprises 6-palmitoyl ascorbate.

[0041] In some embodiments, the oral care composition of this disclosure comprises a whitening agent and an orally acceptable carrier, wherein the whitening agent comprises 6-palmitoyl ascorbate, and wherein the oral care composition further comprises one or more ingredients selected from: pH adjusters, anti-erosion agents, foaming agents, thickeners, flavoring agents, antibacterial agents, desensitizing agents, anti-caries agents, fluoride ion sources, anti-tartar agents, abrasives, anti-spotting agents, anti-tartar agents, polymer complexes, surfactants, humectants, and / or combinations thereof.

[0042] In some further embodiments, this disclosure provides a method of delivering an oral care composition of this disclosure using an applicator, wherein the applicator is a pen and the pen is stored within an oral care appliance. In some embodiments, the pen is removed from the oral care appliance before the oral care composition is applied to the teeth. In some embodiments, the oral care composition can be applied to the teeth after brushing. In some embodiments, the oral care composition can be applied to the teeth after brushing with an oral care appliance.

[0043] In one embodiment, this disclosure also provides a method for whitening a tooth surface using an oral care composition according to this disclosure. In one embodiment, this disclosure provides a method for whitening a tooth surface, the method comprising applying a safe and effective amount of the oral care composition of this disclosure to the tooth surface, wherein the oral care composition comprises a whitening agent and wherein the whitening agent comprises an ascorbic acid derivative.

[0044] In one embodiment, this disclosure provides a method for whitening tooth surfaces, the method comprising applying a safe and effective amount of the oral care composition of this disclosure to the tooth surface, wherein a whitening agent and an orally acceptable carrier are present, and wherein the whitening agent comprises an ascorbic acid derivative.

[0045] In another embodiment, this disclosure provides a method for whitening tooth surfaces, the method comprising applying an effective amount of the oral care composition described herein to the oral cavity of a subject in need of such treatment.

[0046] In another embodiment, this disclosure provides a method for whitening tooth surfaces, the method comprising: contacting the tooth surface with an oral care composition of this disclosure for a duration sufficient to whiten the tooth surface.

[0047] In another embodiment, this disclosure provides a method for whitening tooth surfaces, the method comprising: contacting the tooth surface with an oral care composition containing a whitening agent, wherein the whitening agent is an ascorbic acid derivative.

[0048] In another embodiment, this disclosure provides a method for whitening tooth surfaces using an oral care composition comprising a whitening agent, wherein the whitening agent is an ascorbic acid derivative selected from: L-ascorbic acid, calcium ascorbate, calcium l-ascorbate dihydrate, magnesium ascorbate, potassium ascorbate, magnesium L-ascorbate phosphate, sesqui-magnesium L-ascorbate 2-phosphate hydrate, sodium ascorbate, dehydro-l-(+)-ascorbic acid dimer, sodium ascorbate phosphate, ascorbate-2-glucoside, dipalmitoyl ascorbate, ascorbate methylsilanol pectate, stearate ascorbate, disodium ascorbate sulfate, 6-palmitoyl ascorbate, and / or combinations thereof.

[0049] In another embodiment, this disclosure relates to a method of whitening tooth surfaces using an oral care composition containing a whitening agent, wherein the whitening agent is an ascorbic acid derivative, and wherein the oral care composition does not contain other whitening agents, such as peroxides, percarbonates, peracids, persulfate derivatives, and / or combinations thereof.

[0050] In another embodiment, this disclosure provides a method for whitening tooth surfaces using an oral care composition comprising a whitening agent, wherein the whitening agent is an ascorbic acid derivative, and wherein the oral care composition further comprises one or more oral-acceptable carriers.

[0051] In another embodiment, this disclosure provides a method for whitening tooth surfaces, the method comprising: contacting the tooth surface with an oral care composition, wherein the oral care composition comprises a whitening agent, wherein the whitening agent is an ascorbic acid derivative, and wherein the composition further comprises one or more ingredients selected from: abrasives, anti-staining agents, anti-tartar agents, anti-calculus agents, polymer complexes, surfactants, humectants, pH adjusters, foam adjusters, thickeners, flavoring agents, antibacterial agents, desensitizing agents, anti-caries agents, fluoride ion sources, anti-erosion agents, and / or combinations thereof.

[0052] In another embodiment, this disclosure is a method of whitening tooth surfaces using an oral care composition, wherein the oral care composition comprises a whitening agent and wherein the whitening agent is an ascorbic acid derivative, and wherein the composition further comprises one or more of the following: a fluoride ion source, a zinc ion source, a stannous ion source and / or a combination thereof.

[0053] In another embodiment, this disclosure provides a method for whitening tooth surfaces using an oral care composition, wherein the oral care composition comprises a whitening agent, and wherein the whitening agent is an ascorbic acid derivative selected from 6-palmitoyl ascorbate, sodium ascorbate phosphate, and combinations thereof.

[0054] In yet another embodiment, the method described herein may include direct application of an oral care composition, including rinsing, spraying, and brushing. In some embodiments, applying the oral care composition includes using an application device that helps maintain contact between the ascorbic acid derivative whitening agent and the tooth surface for a sufficient time to allow whitening. Suitable application devices include dental trays, dental pieces, dental floss, fibers, sheets, strips, and cleaning bands. Dental strips comprise polymers, natural and synthetic woven materials, nonwoven materials, foils, paper, rubber, and / or combinations thereof. In one embodiment, the oral care composition of this disclosure is applied using a “smearing” technique. A small application device, such as a brush or spatula, is coated with the oral care composition of this disclosure and placed on the tooth surface.

[0055] In one embodiment, the oral care composition of this disclosure is selected from the following forms: dental cleaning agents (e.g., toothpaste), mouthwash, mouth rinse liquid, topical oral gel, denture cleaner, dental strips, beads, varnishes, dental floss, tablets, strips, toothpaste strips, chewing gum, tablets, and tooth powder.

[0056] In one embodiment, the oral care composition of this disclosure comprises one or more ascorbic acid derivatives and also comprises a fluoride ion source.

[0057] In one embodiment, the oral care composition of this disclosure comprises one or more ascorbic acid derivatives and also comprises a zinc ion source.

[0058] In one embodiment, the oral care composition of this disclosure comprises one or more ascorbic acid derivatives and also comprises a stannous ion source.

[0059] Oral care composition ingredients

[0060] In one embodiment, in addition to ascorbic acid derivatives (e.g., 6-palmitoyl ascorbate, sodium ascorbate phosphate), the oral care composition of this disclosure may also contain at least one abrasive agent. The abrasive acts as a polishing agent within the oral care composition. In some embodiments, the abrasive agent includes, but is not limited to, silica (in the form of silica gel, hydrated silica, perlite, high-cleaning silica, core-shell silica, or precipitated silica), alumina, insoluble phosphates, calcium carbonate, resin abrasives such as urea-formaldehyde condensate, dicalcium phosphate, calcium pyrophosphate, calcium carbonate, sodium bicarbonate, alumina, dicalcium orthophosphate dihydrate, calcium orthopyrophosphate, tricalcium phosphate, polymetaphosphate, insoluble sodium polymetaphosphate, and precipitated calcium carbonate. The average particle size of the abrasive is typically from about 0.1 μm to about 30 μm, for example, from about 1 μm to about 20 μm or from about 5 μm to about 15 μm. In some embodiments, one or more abrasives are present in an amount from about 0.1% by weight to about 60% by weight of the total weight of the oral care composition. In some embodiments, the abrasive is calcium pyrophosphate. In some embodiments, calcium pyrophosphate is present in an amount from about 5% by weight to about 50% by weight of the total weight of the oral care composition. In some embodiments, the abrasive is named Perlite. 25P perlite for sale. In some embodiments, the abrasive is core-shell silica. In some embodiments, the abrasive is precipitated calcium carbonate. In some embodiments, the oral care composition of this disclosure comprises an abrasive containing cellulose, such as non-colloidal microcrystalline cellulose, colloidal microcrystalline cellulose, and / or combinations thereof.

[0061] In one embodiment, in addition to ascorbic acid derivatives (e.g., 6-palmitate ascorbate, sodium ascorbate phosphate), the oral care composition of this disclosure may also contain at least one antiscalant. In some embodiments, the antiscalant includes tetrasodium pyrophosphate (TSPP), disodium pyrophosphate (SAPP), sodium tripyrophosphate (STPP), sodium hexametaphosphate (SHMP), or zinc citrate.

[0062] In some embodiments, one or more antispot agents are present in an amount of about 0.1% by weight to about 60% by weight of the total weight of the oral care composition.

[0063] In one embodiment, in addition to ascorbic acid derivatives (e.g., 6-palmitoyl ascorbate, sodium ascorbate phosphate), the oral care composition of this disclosure may also contain at least one surfactant. The surfactant serves to enhance the stability of the oral care composition and generate foam during agitation, which ensures oral cleaning. In some embodiments, the surfactant includes anionic surfactants, nonionic surfactants, or amphoteric surfactants.

[0064] Suitable anionic surfactants include, but are not limited to, C 8-20 Water-soluble salts of alkyl sulfates, C 8-20 Sulfonated monoglycerides of fatty acids, sarcosine salts, taurine salts, etc. Illustrative examples of these and other classes include sodium cocoyl monoglyceride sulfonate, sodium stearate, and sodium lauryl sarcosine (as named...). 30-B (sold), lauryl glucoside, sodium lauroyl hydroxyethyl sulfonate (by name) (WHSP sales), sodium lauryl ether carboxylate, sodium lauryl sulfate (same as sodium dodecyl sulfate or SLS or SDS), and sodium dodecylbenzene sulfonate.

[0065] Suitable nonionic surfactants include, but are not limited to, poloxamer, polyoxyethylene sorbitan esters, fatty alcohol ethoxylates, alkylphenol ethoxylates, tertiary amine oxides, tertiary phosphine oxides, and dialkyl sulfoxides. Suitable amphoteric surfactants include, but are not limited to, C-type surfactants with anionic groups (e.g., carboxyl, sulfate, sulfonate, phosphate, phosphonate). 8-20 Derivatives of aliphatic secondary and tertiary amines, or cocamidopropyl betaine, alkyl betaine, and alkylamide betaine.

[0066] In some implementations, the surfactant is named as The product sold is a mixture of sodium cocoamphoacetate and glycerin, lauryl glucoside, sodium cocoyl glutamate, and sodium lauryl glucocarboxylate. In some embodiments, the surfactant is sodium carboxymethyl cellulose, sodium stearate, lauryl glucoside, polyanionic cellulose, sodium lauroyl hydroxyethyl sulfonate, sodium lauryl sarcosinate, sodium cocoyl glutamate, cocamidopropyl betaine, and / or combinations thereof. In some embodiments, one or more surfactants may be present in a total amount of about 0.01% by weight to about 20.00% by weight of the total weight of the oral care composition. In some embodiments, one or more surfactants may be present in a total amount of about 1.8% by weight to about 2% by weight of the total weight of the oral care composition. In some embodiments, one or more surfactants may be present in a total amount of about 1.9% by weight to about 2% by weight of the total weight of the oral care composition. In some embodiments, one or more surfactants may be present in a total amount of about 2% by weight of the total weight of the oral care composition.

[0067] In one embodiment, in addition to ascorbic acid derivatives (e.g., 6-palmitate ascorbate, sodium ascorbate phosphate), the oral care composition of this disclosure may also contain at least one thickener. In some embodiments, the thickener includes, but is not limited to: carbomer (also known as carboxyvinyl polymer), carrageenan (also known as Irish moss, and more particularly carrageenan (I-carrageenan)), high molecular weight polyethylene glycol (e.g. Available from The Dow Chemical Company), cellulose polymers such as hydroxyethyl cellulose, carboxymethyl cellulose (CMC) and its salt—sodium CMC, polyanionic cellulose, natural gums such as gum arabic, xanthan gum, thickening silica, gum arabic and astragalus gum, microcrystalline cellulose, colloidal magnesium aluminum silicate, and colloidal silica, pyrolytic silica and / or combinations thereof.

[0068] In some embodiments, the thickener is thickening silica or xanthan gum and / or a combination thereof. In some embodiments, the thickener is present in a total amount of about 0.1% by weight to about 90% by weight of the total weight of the oral care composition. In some embodiments, one or more optional thickeners are present in a total amount of about 1% by weight to about 50% by weight of the total weight of the oral care composition. In some embodiments, one or more optional thickeners are present in a total amount of about 5% by weight to about 35% by weight of the total weight of the oral care composition.

[0069] In one embodiment, in addition to ascorbic acid derivatives (e.g., 6-palmitoyl ascorbate, sodium ascorbate phosphate), the oral care composition of this disclosure may also contain at least one humectant. In some embodiments, the humectant includes polyols such as vegetable-refined glycerin, amorphous sorbitol, xylitol, or low molecular weight polyethylene glycol (PEG) or polyoxyethylene. In some embodiments, the humectant is amorphous sorbitol, vegetable glycerin, or polyoxyethylene glycol and / or combinations thereof. High molecular weight PEGs are suitable, including those with an average molecular weight of about 200,000 to about 7,000,000, for example, about 500,000 to about 5,000,000 or about 1,000,000 to about 2,500,000. One or more PEGs are optionally present in a total amount of about 0.1% to about 10% of the total weight of the oral care composition, for example, about 0.2% to about 5% by weight or about 0.25% to about 2% by weight.

[0070] The oral care compositions of this disclosure may contain at least one adhesive. The adhesive serves to ensure that the oral care composition remains on the oral cavity surface. In some embodiments, the adhesive includes binders, film-forming materials, viscosity enhancers, hydrophilic organic polymers, hydrophobic organic polymers, silicone resins, silicone adhesives, silica, and / or combinations thereof. The adhesive is preferably present at a level of about 0.01% to about 75% by weight, and optionally about 1% to about 40% by weight of the total weight of the oral care composition.

[0071] In one embodiment, in addition to an ascorbic acid derivative (e.g., 6-palmitoyl ascorbate, sodium ascorbate phosphate), the oral care composition of this disclosure may also comprise at least one hydrophobic polymer carrier, and wherein the oral care composition is water-free. As applied to polymers and as used herein, hydrophobic or water-insoluble means a substantially non-aqueous polymer with a water solubility of less than one gram per 100 grams of water at 25°C. In some embodiments, the composition of this disclosure comprises at least one hydrophobic polymer carrier and at least one whitening agent, wherein the hydrophobic polymer carrier is a silicone pressure-sensitive adhesive, and wherein the whitening agent is an ascorbic acid derivative. For example, the ascorbic acid derivative may be present in the oral care composition in an amount ranging from about 0.5% by weight to about 5.0% by weight relative to the total weight of the oral care composition.

[0072] In several embodiments, the hydrophobic polymer is compatible with at least one whitening agent described herein (e.g., 6-palmitoyl ascorbate, sodium ascorbate phosphate). In some embodiments, the hydrophobic polymer is selected as a carrier to produce a teeth whitening oral care composition having a viscosity ranging from about 1,000 cPs to about 900,000 cPs, for example, from about 10,000 cPs to about 900,000 cPs or from about 10,000 cPs to about 100,000 cPs. One class of hydrophobic polymers that can be used according to certain exemplary embodiments includes siloxane polymers, which are also commonly referred to in the art as “organosilicon” polymers, such as silicone pressure-sensitive adhesives (PSA). In some embodiments disclosed herein, the hydrophobic polymer in the carrier is one in which the whitening agent can be dispersed and is known in the art. For example, the silicone polymer may be commercially available. In several embodiments, the silicone-based hydrophobic polymer is a polyorganosiloxane, such as polydimethylsiloxane. In one embodiment, the oral care composition disclosed herein may further comprise cropovidone (poly[N-vinyl-2-pyrrolidone]) as an adhesion enhancer. Cropovidone may be present in the oral care composition in an amount ranging from about 10% by weight to about 30% by weight relative to the total weight of the teeth whitening oral care composition, for example, from about 15% by weight to about 25% by weight, or from about 18% by weight to about 25% by weight of the total weight of the oral care composition. In another embodiment, the oral care composition disclosed herein may further comprise an N-vinyl heterocyclic polymer. The N-vinyl heterocyclic polymer is derived from an N-heterocyclic vinyl monomer or a specific monomer such as an N-vinylimide or an N-vinyllactam. A preferred polymer is poly[N-vinyl-poly-2-pyrrolidone](PVP).

[0073] In another embodiment, the oral care composition of this disclosure may contain at least one antioxidant. In some embodiments, the antioxidant may be selected from: butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), vitamin A, carotenoids, quercetin, rutin, catechins, water-soluble vitamin E (trolox), vitamin E, flavonoids, polyphenols, ascorbic acid, 2,4-dihydroxybenzoic acid, m-methoxybenzoic acid, m-hydroxybenzoic acid, p-hydroxybenzoic acid, 3,4-dihydroxybenzoic acid, stannous compounds, potassium metabisulfite or sodium metabisulfite, butylated hydroxytoluene (BHT), ammonium sulfate, herbal antioxidants, chlorophyll, melatonin and / or combinations thereof.

[0074] In another embodiment, the oral care composition of this disclosure may comprise at least one anti-erosion agent selected from: sodium fluoride, arginine, arginine phosphate, arginine hydrochloride, arginine bicarbonate, sodium monofluorophosphate, potassium citrate, titanium phosphate, zinc oxide, zinc citrate, zinc citrate trihydrate, zinc lysine chloride complex, and zinc arginine chloride complex. The anti-erosion agent or combination thereof may be present in the oral care composition in an amount ranging from about 0.2% by weight to about 10.0% by weight, relative to the total weight of the oral care composition.

[0075] In another embodiment, the oral care composition of this disclosure may contain at least one preservative selected from: benzyl alcohol, chlorhexidine, benzoic acid, benzoate, quaternary ammonium compounds (e.g., benzalkonium chloride).

[0076] In another embodiment, the oral care composition of this disclosure may comprise at least one antimicrobial agent selected from: triclosan (5-chloro-2-(2,4-dichlorophenoxy)phenol); 8-hydroxyquinoline and its salts; zinc and stannous ion sources, such as zinc citrate, zinc sulfate, zinc glycinate, sodium zinc citrate, and stannous pyrophosphate; copper(II) compounds, such as copper(II) chloride, copper(II) fluoride, copper(II) sulfate, and copper(II) hydroxide; phthalic acid and its salts, such as magnesium monopotassium phthalate; sanguisorbin; and quaternary ammonium compounds, such as alkylpyridine chloride. Hexadecylpyridine chloride (CPC), CPC combined with zinc and / or enzymes, tetradecylpyridine chloride and N-tetradecyl-4-ethylpyridine chloride Biguanides, such as chlorhexidine digluconate, hexetine, oteninidine, and alexicon; halogenated bisphenol compounds, such as 2,2'-methylenebis-(4-chloro-6-bromophenol); benzalkonium chloride; salicylanilide, domiphen bromide; iodine; sulfonamides; biguanides; phenolic resins; piperidine derivatives, such as dimopiperol and octopiol; magnolia extract; grape seed extract; thymol; eugenol; menthol; geraniol; carvacrol; citral; eucalyptol; catechol; 4-allyl catechol; hexylresorcinol; methyl salicylate; antibiotics, such as octomenine, amoxicillin, tetracycline, doxycycline, minocycline, metronidazole, neomycin, kanamycin, and clindamycin; and / or combinations thereof.

[0077] In another embodiment, the oral care composition of this disclosure may comprise at least one anti-tartar (anti-calculus) agent selected from: phosphates and polyphosphates (e.g., pyrophosphates), polyaminopropanesulfonic acid (AMPS), polyolefin sulfonates, polyolefin phosphates, bisphosphonates such as aziridine-2,2-bisphosphonates (e.g., aziridine-2,2-bisphosphonic acid), N-methylaziridine-2,3-bisphosphonic acid, ethane-1-hydroxy-1,1-bisphosphonic acid (EHDP) and ethane-1-amino-1,1-bisphosphonate, phosphonyl alkane carboxylic acids, and salts of any of these agents, such as their alkali metal salts and ammonium salts. Available inorganic phosphates and polyphosphates include sodium dihydrogen phosphate, disodium hydrogen phosphate and trisodium phosphate, sodium tripolyphosphate, sodium tetrapolyphosphate, monosodium pyrophosphate, disodium pyrophosphate, trisodium pyrophosphate and tetrasodium pyrophosphate, sodium trimetaphosphate, sodium hexametaphosphate and / or combinations thereof, wherein sodium may optionally be replaced by potassium or ammonium. Anti-tartar agents comprise polycarboxylate polymers and polyvinyl methyl ether / maleic anhydride (PVME / MA) copolymers, for example, available from ISP, Wayne, NJ and Gantrez. TM Those trademarks obtained. In another embodiment, the oral care composition of this disclosure comprises one or more anti-tartar agents present in an effective total amount, for example, from 0.01% to 50% by weight of the total oral care composition, such as from 0.05% to 25% by weight, or from 0.1% to 15% by weight.

[0078] In another embodiment, the oral care composition of this disclosure may comprise at least one stannous ion source. Stannous ions may act as periodontal actives, anti-tartar agents, anti-caries agents, or tooth desensitizers. In some embodiments, the stannous ion source may be selected from: stannous fluoride, other stannous halides such as stannous chloride dihydrate, organic carboxylic acid stannous salts such as stannous formate, stannous acetate, stannous gluconate, stannous lactate, stannous tartrate, stannous oxalate, stannous malonate, and stannous citrate, stannous ethylene glyoxide, and / or combinations thereof.

[0079] In another embodiment, the oral care composition of this disclosure may comprise at least one fluoride ion source. Fluoride ions can act as an anti-caries agent. In some embodiments, the fluoride ion source may be selected from: fluorides and monofluorophosphates of potassium, sodium, and ammonium, sodium monofluorophosphate, stannous fluoride, indium fluoride, and / or combinations thereof.

[0080] In another embodiment, the oral care composition of this disclosure may contain at least one zinc ion source. Zinc ions can act as an antiodor agent. In some embodiments, the zinc ion source may be selected from: zinc oxide, zinc citrate, zinc chloride, zinc acetate, zinc lactate, zinc salicylate, zinc sulfate, zinc phosphate, zinc tartrate, and zinc nitrate, and / or combinations thereof.

[0081] In another embodiment, the oral care composition of this disclosure may comprise at least one colorant source. In some embodiments, the colorant source may be selected from pigments, dyes, lakes, and agents that impart a particular gloss or reflectivity, such as pearlescent agents. In many embodiments, the colorant is operable to provide a white or light-colored coating on the tooth surface, act as an indicator of the location on the tooth surface where the oral care composition has been effectively contacted, and / or alter the appearance of the oral care composition, particularly its color and / or opacity, thereby enhancing its appeal to consumers.

[0082] In another embodiment, the oral care composition of this disclosure may contain at least one flavoring agent. For example, the oral care composition of this disclosure may contain 0.1% to 2.0% by weight of a flavoring agent based on the total weight of the oral care composition. In some embodiments, the flavoring agent may be any material and / or combination of materials operable to enhance the flavor of the oral care composition, such as any orally acceptable natural or synthetic flavoring agent (e.g., flavoring oils, flavoring aldehydes, esters, alcohols, similar materials, and / or combinations thereof). Flavoring agents include vanillin, sage, marjoram, parsley oil, spearmint oil, cinnamon oil, wintergreen oil (methyl salicylate), peppermint oil, clove oil, laurel oil, anise oil, eucalyptus oil, citrus oil, fruit oils and flavorings (including those derived from lemon, mandarin orange, lime, grapefruit, apricot, banana, grape, apple, strawberry, cherry, pineapple), flavoring agents derived from legumes and nuts (e.g., coffee, cocoa, kola nut, peanut, almond), adsorbed and encapsulated flavoring agents, and / or combinations thereof. Also included in the flavoring agents described in this article are ingredients that provide additional sensory effects in the mouth, including cooling or warming effects.

[0083] In another embodiment, the oral care composition of this disclosure may contain at least one sweetener. The oral care composition of this disclosure may contain 0.1% to 2.0% by weight of a sweetener based on the total weight of the oral care composition. In some embodiments, the sweetener includes dextrose, sucrose, polydextrose, maltose, dextrin, dry invert sugar, mannose, xylose, ribose, fructose, levulose, galactose, corn syrup, partially hydrolyzed starch, hydrogenated starch hydrolysate, sorbitol, mannitol, xylitol, maltitol, isomaltitol, aspartame, neotame, saccharin and its salts, sucralose, dipeptide-based potent sweeteners, cyclohexylsulfamic acid salts, dihydrochalcone, stevia, saccharified stevia glucoside, and / or combinations thereof.

[0084] In another embodiment, the oral care composition of this disclosure may include at least one mouthfeeling agent. In some embodiments, the mouthfeeling agent includes a material that imparts a desired texture or other sensation during use of the oral care composition of this disclosure.

[0085] In another embodiment, the oral care composition of this disclosure may contain at least one pH adjuster. The function of the pH adjuster is to maintain the oral care composition within an orally acceptable pH range. In some embodiments, the pH adjuster includes an acidifier that lowers the pH, an alkalizer that raises the pH, and a buffer that controls the pH within a desired range. Orally acceptable pH adjusters include carboxylic acids, phosphoric acids and sulfonic acids, acid salts, monosodium citrate, disodium citrate, monosodium malate, alkali metal hydroxides such as sodium hydroxide, carbonates such as sodium carbonate, bicarbonates, sesquicarbonates, borates, silicates, phosphates, monosodium phosphate, trisodium phosphate, pyrophosphate, imidazole, and / or combinations thereof. The oral care composition of this disclosure may contain a viscosity modifier. The function of the viscosity modifier is to ensure that the oral care composition is homogeneous. In some embodiments, the viscosity modifier includes mineral oil, petrolatum, clay and organically modified clay, silica, and / or combinations thereof.

[0086] In another embodiment, the oral care composition of this disclosure may contain at least one foam modifier. The function of the foam modifier is to generate foam upon mixing, which facilitates the dispersion of the oral care composition in the oral cavity. In some embodiments, the foam modifier includes sodium lauroyl sarcosinate, sodium lauroyl sulfate powder, and polyethylene glycol (PEG) (also known as polyoxyethylene). High molecular weight PEGs are suitable, including those with an average molecular weight of about 200,000 to about 7,000,000, for example, about 500,000 to about 5,000,000 or about 1,000,000 to about 2,500,000. One or more PEGs are optionally present in a total amount of about 0.1% by weight to about 10% by weight, for example, about 0.2% by weight to about 5% by weight or about 0.25% by weight to about 2% by weight of the total weight of the oral care composition.

[0087] In another embodiment, the oral care composition of this disclosure may comprise at least one saliva stimulant. The saliva stimulant functions to prevent dry mouth. In some embodiments, the saliva stimulant includes food acids such as citric acid, lactic acid, rilalic acid, succinic acid, ascorbic acid, adipic acid, fumaric acid, and tartaric acid, and / or combinations thereof.

[0088] In another embodiment, the oral care composition of this disclosure may contain at least one breath freshener. In some embodiments, the breath freshener includes zinc salts such as zinc gluconate, zinc citrate, and zinc chlorite, α-ionone, and / or combinations thereof.

[0089] In another embodiment, the oral care composition of this disclosure may contain at least a desensitizing agent. In some embodiments, the desensitizing agent includes potassium citrate, potassium chloride, potassium tartrate, potassium bicarbonate, potassium oxalate, potassium nitrate, strontium salts, and / or combinations thereof.

[0090] In another embodiment, the oral care composition of this disclosure may comprise at least one nutrient agent. In some embodiments, the nutrients include vitamins, minerals, amino acids, and / or combinations thereof. Vitamins include vitamin D, thiamine, riboflavin, calcium pantothenate, niacin, folic acid, nicotinamide, pyridoxine, cyanocobalamin, para-aminobenzoic acid, bioflavonoids, and / or combinations thereof. Nutritional supplements include amino acids, arginine, L-tryptophan, L-lysine, methionine, threonine, L-carnitine and L-carnitine, lipophilic substances, choline, inositol, betaine and linoleic acid, fish oil (including its components such as omega-3 (N-3) polyunsaturated fatty acids, eicosapentaenoic acid, and docosahexaenoic acid), coenzyme Q10, and / or combinations thereof. The oral care composition of this disclosure may contain neutral amino acids selected from alanine, GABA, asparagine, cysteine, cystine, glutamine, glycine, hydroxyproline, isoleucine, leucine, methionine, phenylalanine, proline, serine, taurine, threonine, tryptophan, tyrosine, valine and / or combinations thereof; preferably selected from glycine, asparagine, glutamine and / or combinations thereof; and wherein the neutral amino acids are present in an amount of 0.1% to 5% by weight of the total weight of the oral care composition.

[0091] In another embodiment, the oral care composition of this disclosure may contain at least one anti-inflammatory agent. In some embodiments, the anti-inflammatory agent includes steroidal agents such as fluocinolone acetonide and hydrocortisone, and nonsteroidal anti-inflammatory agents (NSAIDs) such as ketorolac, flurbiprofen, ibuprofen, naproxen, indomethacin, diclofenac, etodoxacin, indomethacin, sulindac, tometetin, ketoprofen, fenprofen, piroxicam, nabumetone, aspirin (ASPMN), diflunisal, meclofenamic acid, mefenamic acid, hydroxyphenylbutazone, and phenylbutazone and / or combinations thereof.

[0092] In some embodiments, the oral care composition of this disclosure may contain at least one ingredient selected from: humectants, abrasives, surfactants, thickeners, foam modifiers, anti-spotting agents, preservatives, anti-erosion agents, anti-plaque agents, sweeteners, water, and combinations thereof.

[0093] In some embodiments, the oral care composition of this disclosure may comprise 0.10 wt% to 70 wt% of at least one humectant, about 0.10 wt% to about 60 wt% of at least one abrasive, 0.01 wt% to 20 wt% of at least one anionic surfactant, 0.01 wt% to 20 wt% of at least one nonionic surfactant, 0.01 wt% to 20 wt% of at least one amphoteric surfactant, 0.10 wt% to 90 wt% of at least one thickener, 0.10 wt% to 10 wt% of at least one foaming agent, 0.10 wt% to 60 wt% of at least one antiscalant, 0.20 wt% to 1 wt% of at least one preservative, 0.10 wt% to 10 wt% of at least one anti-erosion agent, 0.01 wt% to 5 wt% of at least one anti-plaque agent, 0.10 wt% to 2 wt% of at least one sweetener and / or combinations thereof, wherein the weights are based on the total weight of the composition.

[0094] In some embodiments, the oral care composition of this disclosure may contain 0.10% to 70% by weight, or 0.10% to 1% by weight, or 1% to 5.5% by weight, or 5.5% to 20% by weight, or 20% to 40% by weight, or 40% to 46% by weight, or 45% to 53% by weight, or 50% to 60% by weight, or 61.00% to 68.00% by weight, relative to the total oral care composition, at least one moisturizer.

[0095] In some embodiments, the oral care composition of this disclosure may contain 0.10% to 60% by weight, or about 0.10% to 10% by weight, or 5% to 7.5% by weight, or about 10.00% to 15.00% by weight, or 15.00% to 21.00% by weight, or 21.00% to 35.00% by weight, or 7.00% to 17.00% by weight, or 35.00% to 51.00% by weight, or 51.00% to 60.00% by weight, relative to the total oral care composition, at least one abrasive.

[0096] In some embodiments, the oral care composition of this disclosure may contain 0.01% to 20% by weight, or 0.01% to 0.7% by weight, or 0.45% to 0.7% by weight, or 0.7% to 1% by weight, or 1.00% to 10% by weight, or 10% to 15.5% by weight, or 4.2% to 5% by weight, or 15.5% to 20% by weight, relative to the total oral care composition, at least one anionic surfactant.

[0097] In some embodiments, the oral care composition of this disclosure may contain 0.01% to 20% by weight, or 0.01% to 0.05% by weight, or 0.04% to 1% by weight, or 1% to 3% by weight, or 3% to 5% by weight, or 5% to 7% by weight, or 7% to 14% by weight, or 14% to 20% by weight, relative to the total oral care composition, at least one nonionic surfactant.

[0098] In some embodiments, the oral care composition of this disclosure may contain 0.01 wt% to 20 wt%, or 0.01 wt% to 1.00 wt%, or 1.00 wt% to 1.6 wt%, or 1.5 wt% to 2 wt%, or 2 wt% to 2.6 wt%, or 2.5 wt% to 3 wt%, or 3 wt% to 5 wt%, or 5 wt% to 7 wt%, or 7 wt% to 14 wt%, or 14 wt% to 20 wt% of at least one amphoteric surfactant, relative to the total oral care composition.

[0099] In some embodiments, the oral care composition of this disclosure may comprise, relative to the total oral care composition, 0.1 wt% to 90 wt%, or 0.1 wt% to 5.5 wt%, or 5.5 wt% to 7.5 wt%, or 7.5 wt% to 15.5 wt%, or 1.5 wt% to 5.5 wt%, or 0.2 wt% to 0.5 wt%, or 0.4 wt% to 1.5 wt%, or 1.5 wt% to 2.5 wt%, or 2.5 wt%. At least one thickener in amounts of up to 3.5 wt%, or 3.5 wt% to 5 wt%, or 5 wt% to 5.5 wt%, or 5.5 wt% to 7 wt%, or 7 wt% to 8 wt%, or 7.2 wt% to 12.8 wt%, or 15.5 wt% to 35.5 wt%, or 35.5 wt% to 55.5 wt%, or 55.5 wt% to 75.5 wt%, or 75.5 wt% to 85.5 wt%, or 85.5 wt% to 90 wt%.

[0100] In some embodiments, the oral care composition of this disclosure may contain 0.10% to 10% by weight, or 1% to 2% by weight, or 2% to 3.5% by weight, or 3.5% to 5% by weight, or 5% to 6% by weight, relative to the total oral care composition. The oral care composition of this disclosure may contain 0.1% to 60% by weight, or 0.1% to 0.45% by weight, or 0.45% to 5.45% by weight, or 5.45% to 10.65% by weight, or 10.65% to 20.85% by weight, or 20.85% to 40% by weight, or 40% to 50% by weight, or 50% to 60% by weight, relative to the total oral care composition.

[0101] In some embodiments, the oral care composition of this disclosure may contain at least one preservative in 0.20% to 1% by weight, or 0.2% to 0.45% by weight, or 0.45% to 0.55% by weight, or 0.55% to 0.85% by weight, or 0.85% to 1% by weight, relative to the total oral care composition.

[0102] In some embodiments, the oral care composition of this disclosure may contain at least one anti-erosion agent in 0.10 wt% to 10 wt%, or 0.55 wt% to 0.85 wt%, or 0.10 wt% to 0.2 wt%, or 0.2 wt% to 0.5 wt%, or 0.2 wt% to 0.35 wt%, or 0.35 wt% to 0.65 wt%, or 0.65 wt% to 0.85 wt%, or 0.85 wt% to 1 wt%, relative to the total oral care composition.

[0103] In some embodiments, the oral care composition of this disclosure may contain, relative to the total oral care composition, at least one anti-plaque agent in amounts of 0.01% to 50% by weight, or 0.01% to 0.5% by weight, or 0.5% to 1% by weight, or 1% to 5% by weight, or 5% to 10% by weight, or 10% to 20% by weight, or 20% to 30.2% by weight, or 30.2% to 40% by weight, or 40% to 50% by weight.

[0104] Relative to the total oral care composition, the oral care composition of this disclosure may contain at least one sweetener in 0.10% to 2% by weight, or 0.1% to 0.4% by weight, or 0.4% to 1% by weight, or 1% to 1.2% by weight, or 1.2% to 1.7% by weight, or 1.7% to 2% by weight.

[0105] It should be understood that although the general properties of each of the above categories of materials may differ, there may be some common properties, and any given material can be used for multiple purposes in two or more of the materials in such categories.

[0106] In some embodiments, the oral care composition is anhydrous. Anhydrous means less than 5% by weight of water, optionally less than 4% by weight, less than 3% by weight, less than 2% by weight, less than 1% by weight, less than 0.5% by weight, less than 0.1% by weight, down to 0% by weight of water.

[0107] In some embodiments, the oral care composition of this disclosure contains 60% to 90% by weight of water based on the total weight of the oral care composition. In some embodiments, the oral care composition contains 65% to 85% by weight of water based on the total weight of the oral care composition. In some embodiments, the oral care composition contains 70% to 80% by weight of water based on the total weight of the oral care composition. In some embodiments, the oral care composition contains 10% to 22% by weight of water based on the total weight of the oral care composition. In some embodiments, the oral care composition contains 5% to 30% by weight of water based on the total weight of the oral care composition.

[0108] The oral care compositions disclosed herein may comprise a variety of agents that are active in protecting and enhancing the strength and integrity of tooth enamel and tooth structure and / or reducing bacteria and associated caries and / or gingival disease. The effective concentration of the active ingredient used herein will depend on the specific reagent and delivery system used.

[0109] Therefore, in one aspect, this disclosure provides an oral care composition (composition 1.0) for whitening tooth enamel to a thickness greater than 0.1, wherein the oral care composition comprises an effective amount of an ascorbic acid derivative.

[0110] The derivatives described herein are selected from: L-ascorbic acid, calcium ascorbate, L-calcium ascorbate dihydrate, magnesium ascorbate, potassium ascorbate, magnesium L-ascorbate phosphate, sesqui-magnesium L-ascorbate 2-phosphate hydrate, sodium (+)L-ascorbate, dehydro-L-(+)-ascorbic acid dimer, sodium ascorbate phosphate, ascorbate-2-glucoside, dipalmitoyl ascorbate, ascorbate methylsilanol pectate, stearate ascorbate, disodium ascorbate sulfate, 6-palmitoyl ascorbate, and combinations thereof. (For example, the amount of the ascorbic acid derivative is sufficient to increase the ΔW of the enamel by at least 0.3 times relative to the non-peroxide reference standard).

[0111] For example, composition 1.0 also includes the following:

[0112] 1.1 Composition 1.0, wherein the amount of said ascorbic acid derivative is sufficient to increase the ΔW of said tooth enamel by at least 0.3 times relative to a non-peroxide reference standard.

[0113] 1.2 Composition 1.0 or 1.1, wherein the amount of said ascorbic acid derivative is sufficient to increase the ΔW of said enamel by 0.3 to 4 times (e.g., about 0.5 times) (e.g., about 2.5 times) relative to the non-peroxide reference standard.

[0114] 1.3 Any of the foregoing compositions, wherein the ascorbic acid derivative is present in an amount of 1% to 5% by weight (e.g., 1% to 3% by weight) (e.g., about 1% by weight) (e.g., about 1.5% by weight) (e.g., about 2% by weight) (e.g., about 2.5% by weight) (e.g., about 3% by weight) of the total composition.

[0115] 1.4 Any of the foregoing compositions, wherein the ascorbic acid derivative is selected from: sodium ascorbate phosphate, 6-palmitate ascorbate, and combinations thereof.

[0116] 1.5 Any of the foregoing compositions, wherein the ascorbic acid derivative is sodium ascorbate phosphate (e.g., 1 wt% to 5 wt% (e.g., 1 wt% to 3 wt% (e.g., about 1 wt% (e.g., about 1.5 wt% (e.g., about 2 wt% (e.g., about 2.5 wt% (e.g., about 3 wt% (e.g.)).

[0117] 1.6 Any of the foregoing compositions, wherein the ascorbic acid derivative is 6-palmitoyl ascorbate (e.g., 1 wt% to 5 wt% (e.g., 1 wt% to 3 wt% (e.g., about 1 wt% (e.g., about 1.5 wt% (e.g., about 2 wt% (e.g., about 2.5 wt% (e.g., about 3 wt% (e.g.)).

[0118] 1.7 Any of the foregoing compositions comprises a stannous ion source.

[0119] 1.8 The aforementioned composition, wherein the stannous ion source is selected from: stannous fluoride, stannous chloride, stannous pyrophosphate, stannous formate, stannous acetate, stannous gluconate, stannous lactate, stannous tartrate, stannous oxalate, stannous malonate, stannous citrate, stannous glyoxylate, and combinations thereof.

[0120] 1.9 Any of the foregoing compositions, wherein the stannous ion source comprises stannous fluoride.

[0121] 1.10 Any of the foregoing compositions, wherein the stannous ion source comprises stannous fluoride in an amount of 0.1 wt% to 2 wt% (0.1 wt% to 0.6 wt%) (e.g., about 0.454 wt%) of the total composition weight.

[0122] 1.11 Any of the foregoing compositions, wherein the stannous ion source comprises stannous fluoride in an amount of 50 ppm to 25,000 ppm (e.g., 750 ppm to 7,000 ppm, e.g., 1,000 ppm to 5,000 ppm, e.g., about 4,500 ppm, e.g., about 4,540 ppm).

[0123] 1.12 Any of the foregoing compositions, wherein the composition comprises stannous fluoride and stannous pyrophosphate.

[0124] 1.13 Any of the foregoing compositions, wherein the composition comprises stannous fluoride and stannous chloride.

[0125] 1.14 Any of the foregoing compositions, wherein the amount of one or more stannous ion sources is from 0.1% to 5% by weight of the total composition.

[0126] 1.15 Any of the foregoing compositions, wherein the composition comprises a zinc ion source, and wherein the zinc ion source comprises one or more zinc salts selected from the group consisting of zinc citrate, zinc oxide, zinc phosphate, zinc lactate, zinc sulfate, zinc silicate, zinc gluconate, and combinations thereof.

[0127] 1.16 Any of the foregoing compositions, wherein the composition comprises a zinc ion source, and wherein the zinc ion source comprises zinc oxide.

[0128] 1.17 Any of the foregoing compositions, wherein the composition comprises a zinc ion source, and wherein the zinc ion source comprises zinc citrate.

[0129] 1.18 Any of the foregoing compositions, wherein the composition comprises a zinc ion source, and wherein the zinc ion source comprises zinc oxide and zinc citrate.

[0130] 1.19 Any of the foregoing compositions, wherein the ratio of the amount of zinc oxide (e.g., wt%) to the amount of zinc citrate (e.g., wt%) is from 1.5:1 to 4.5:1 (e.g., 2:1, 2.5:1, 3:1, 3.5:1 or 4:1).

[0131] 1.20 Any of the foregoing compositions, wherein the amount of zinc citrate is from 0.25% to 0.75% by weight (e.g., 0.5% by weight) based on the weight of the oral care composition, and zinc oxide may be present in an amount from 0.75% to 1.25% by weight (e.g., 1.0% by weight).

[0132] 1.21 Any of the foregoing compositions, wherein zinc citrate is about 0.5% by weight.

[0133] 1.22 Any of the foregoing compositions, wherein the zinc oxide is about 1.0% by weight.

[0134] 1.23 Any of the foregoing compositions, wherein zinc citrate is about 0.5% by weight and zinc oxide is about 1.0% by weight.

[0135] 1.24 Any of the foregoing compositions, wherein the composition comprises a zinc ion source, and wherein the zinc ion source comprises zinc phosphate (e.g., wherein the zinc phosphate is a pre-formed salt of zinc phosphate) (e.g., zinc phosphate hydrate) (e.g., 0.5% to 4% by weight of zinc phosphate) (e.g., about 1.0% by weight of zinc phosphate).

[0136] 1.25 The aforementioned composition, wherein the zinc phosphate is added as a pre-formed salt.

[0137] 1.26 Any of the foregoing compositions, wherein the composition comprises a zinc ion source, and wherein the zinc ion source comprises zinc lactate.

[0138] 1.27 Any of the foregoing compositions, wherein the amount of zinc ion source is from 0.1% to 5% by weight of the total composition (e.g., 0.1% to 5% by weight of zinc phosphate of the total composition).

[0139] 1.28 Any of the foregoing compositions, comprising an effective amount of a fluoride ion source.

[0140] 1.29 The aforementioned composition, wherein the amount of the fluoride ion source is from 0.01% to 5% by weight relative to the weight of the oral care composition, for example, from 0.05% to 4% by weight, or from 0.1% to 3% by weight, or from 0.2% to 2% by weight, or from 0.3% to 1% by weight, or from 0.3% to 0.5% by weight, or about 0.32% by weight (e.g., 0.32% by weight).

[0141] 1.30 Any one of the foregoing compositions, wherein the fluoride source is selected from: sodium fluoride, potassium fluoride, calcium fluoride, zinc fluoride, zinc ammonium fluoride, lithium fluoride, ammonium fluoride, stannous fluoride, stannous fluorozirconate, sodium monofluorophosphate, potassium monofluorophosphate, laurylamine hydrofluoride, diethylaminoethyloctylamide hydrofluoride, dialcyldimethylammonium fluoride, hexadecylpyridine fluoride, dilaurylmorpholine fluoride. Stannous fluoride of sarcosine, potassium fluoride of glycine, hydrofluoric acid of glycine, fluorinated amines and combinations thereof.

[0142] 1.31 The aforementioned composition, wherein the fluoride ion source comprises sodium fluoride (e.g., 0.2% to 2% by weight of sodium fluoride).

[0143] 1.32 Any of the foregoing compositions, wherein the fluoride ion source comprises stannous fluoride (e.g., 0.1% to 2% by weight of stannous fluoride in the total composition).

[0144] 1.33 Any of the foregoing compositions, wherein the fluoride ion source comprises sodium monofluorophosphate.

[0145] 1.34 Any of the foregoing compositions, wherein the composition comprises 10% by weight or more, for example, 10% to 90%, or 10% to 80%, or 10% to 70%, or 10% to 60%, or 10% to 50%, or 10% to 40%, or 10% to 30%, or 15% to 30%, 15% to 40%, 20% to 40%, 20% to 35%, or 20% to 50%, or 30% to 35%, or about 25% to about 30% water by weight of the composition.

[0146] 1.35 Any of the foregoing compositions further comprising an organic buffer system, wherein the buffer system comprises a carboxylic acid and one or more conjugate base salts thereof, such as alkali metal salts thereof (e.g., citric acid and sodium citrate).

[0147] 1.36 Any of the foregoing compositions, wherein the composition comprises, as measured by the combined amount of the organic acid and any conjugate base salt (e.g., citric acid and sodium citrate), in an amount of 0.1% to 5.0% by weight of the composition; for example, in an amount of 0.5% to 4.0%, or 1.0% to 3.0%, or 1.5% to 3.0%, or 1.0% to 2.4%, or 1.0% to 2.0%, or 1.0% to 1.5%, or about 1.2% by weight of the composition, an organic acid buffer system.

[0148] 1.37 Any of the foregoing compositions, wherein the oral care composition further comprises an abrasive, such as a silica abrasive, a calcium abrasive, and other abrasives disclosed herein.

[0149] 1.38 Any of the foregoing compositions further comprising one or more humectants as described herein, such as those selected from sorbitol, glycerin, xylitol and propylene glycol, or combinations thereof, such as a combination of sorbitol and glycerin.

[0150] 1.39 Any of the preceding compositions, wherein the zwitterionic surfactant comprises cocamidopropyl betaine (e.g., in an amount of 0.1% to 5% by weight) (e.g., about 0.6% by weight).

[0151] 1.40 Any of the foregoing compositions further comprising an effective amount of one or more alkali metal phosphates, such as orthophosphate, pyrophosphate, tripolyphosphate, tetraphosphate or higher polyphosphate.

[0152] 1.41 The aforementioned composition, wherein the alkali metal phosphate comprises tetrasodium pyrophosphate or tetrapotassium pyrophosphate, for example, in an amount of 0.5% to 5% by weight of the composition, such as 1% to 4% by weight, or about 2% to 4% by weight, or about 1% to 2% by weight, or about 1.5% by weight, or about 2% by weight, or about 4% by weight.

[0153] 1.42 The aforementioned composition, wherein the alkali metal phosphate comprises sodium tripolyphosphate or potassium tripolyphosphate, for example, in an amount of 0.5% to 6% by weight of the composition, for example, 1% to 4%, or 2% to 3%, or about 3% by weight.

[0154] 1.43 Any of the foregoing compositions, in addition to the ascorbic acid derivative, further comprises a whitening agent.

[0155] 1.44 Any of the foregoing compositions, wherein the oral care composition is in the form of: dental cleaning agent (e.g., toothpaste or oral gel), powder (e.g., tooth powder), cream, mouthwash, strip or gel (e.g., chewing gum).

[0156] 1.45 Any of the preceding compositions, wherein the pH of the composition is 6 to 9, for example 6.5 to 8, or 6.5 to 7.5, or about 7.0.

[0157] 1.46 Any of the preceding compositions, wherein the composition is a single-phase composition (e.g., not a biphase composition).

[0158] 1.47 Any of the foregoing compositions, wherein the composition is substantially free of or contains no more than four phosphate groups.

[0159] 1.48 Any of the foregoing compositions, wherein the composition is substantially free of or contains no more than three phosphate groups.

[0160] 1.49 Any of the foregoing compositions, wherein the composition is substantially free of or contains no hexametaphosphate (e.g., sodium hexametaphosphate).

[0161] 1.50 Any of the foregoing compositions, wherein the composition, when applied to the oral cavity, for example by rinsing, optionally in conjunction with brushing, is effective in (i) reducing or inhibiting the formation of caries, (ii) reducing, repairing, or inhibiting precarious lesions of the enamel, for example, as detected by quantitative light-induced fluorescence (QLF) or electrical caries measurement (ECM), (iii) reducing or inhibiting tooth demineralization and promoting tooth remineralization, (iv) reducing tooth hypersensitivity, (v) reducing or inhibiting gingivitis, (vi) promoting the healing of ulcers or wounds in the mouth, (vii) reducing the level of acid-producing bacteria, (viii) thereby increasing the relative level of arginine-degrading bacteria, (ix) inhibiting the formation of microbial biofilms in the oral cavity, and (x) increasing and / or maintaining the pH of dental plaque at at least pH after a sugar challenge. At a level of 5.5, (xi) reduce plaque buildup, (xii) treat, alleviate, or reduce dry mouth, (xiii) clean teeth and the oral cavity, (xiv) reduce erosion, (xv) prevent staining and / or whiten teeth, (xvi) make teeth immune to cariogenic bacteria; and / or (xvii) promote overall health, including cardiovascular health, for example by reducing the potential for systemic infections originating from oral tissues.

[0162] 1.51 Any of the foregoing compositions, wherein the composition further comprises a polymer selected from: carboxymethyl cellulose (in free form or salt, such as sodium salt), gum (such as xanthan gum, carrageenan, or gum arabic), polyethylene glycol (such as polyethylene glycol 200, 400, 600, or 800, or mixtures thereof), and combinations thereof, such as a mixture of sodium carboxymethyl cellulose, xanthan gum, and polyethylene glycol 600.

[0163] 1.52 Any of the foregoing compositions, wherein the polymer comprises sodium carboxymethyl cellulose.

[0164] 1.53 Any of the foregoing compositions, wherein the polymer comprises xanthan gum.

[0165] 1.54 Any of the foregoing compositions, further comprising a silica thickener and / or silica abrasive.

[0166] 1.55 The aforementioned composition, wherein the oral care composition comprises an additional anionic surfactant selected from: water-soluble salts of monoglycerides of higher fatty acids (e.g., sodium salts of monosulfated glycerides of hydrogenated coconut fatty acids, such as sodium N-methyl N-cocoyl taurate), sodium monoglyceride sulfate of coconut oil, and higher alkyl ether sulfates (e.g., having the formula CH3(CH2)). m CH2(OCH2CH2) nOSO3X, where m is 6 to 16, for example 10, n is 1 to 6, for example 2, 3 or 4, and X is Na or K, for example sodium lauryl ether-2-sulfate (CH3(CH2)). 10 CH2(OCH2CH2)2OSO3Na), higher alkyl aryl sulfonates such as sodium dodecylbenzenesulfonate (sodium laurylbenzenesulfonate), higher alkyl sulfonates (such as sodium lauryl sulfoacetate (sodium dodecyl sulfoacetate)), higher fatty acid esters of 1,2-dihydroxypropane sulfonate, sulfocolaurate (N-2-ethyllaurate potassium sulfoacetamide), sodium lauryl sulfate, sodium stearate and sodium lauryl sarcosinate.

[0167] 1.56 Any of the foregoing compositions, wherein the composition comprises an amino acid.

[0168] 1.57 The aforementioned composition, wherein the amino acid is a basic amino acid (e.g., arginine).

[0169] 1.58 Any of the foregoing compositions, wherein the amino acid is a basic amino acid provided in the form of a dipeptide or tripeptide comprising arginine or lysine or a salt thereof.

[0170] 1.59 Any of the foregoing compositions, wherein the basic amino acid comprises arginine or lysine, and wherein the arginine or lysine is present in an amount corresponding to 1% to 15% of the total composition weight, for example 3% to 10% by weight, for example about 1.5%, 4%, 5% or 8%, wherein the weight of the basic amino acid is calculated in free form.

[0171] 1.60 Any of the preceding compositions, wherein the amino acid comprises 0.1% to 6.0% by weight (e.g., about 1.5% by weight) (e.g., about 5% by weight) of arginine in the total composition, wherein the weight of arginine is calculated in free form.

[0172] 1.61 Any of the foregoing compositions, wherein the amino acid is about 1.5% by weight of arginine in the total composition, wherein the weight of arginine is calculated in free form.

[0173] 1.62 Any of the foregoing compositions, wherein the amino acid is 4.5% to 8.5% by weight (e.g., about 5.0% by weight) of arginine in the total composition, wherein the weight of the basic amino acid is calculated in free form.

[0174] 1.63 Any of the foregoing compositions, wherein the amino acid is about 5.0% by weight of arginine in the total composition, and wherein the weight of the basic amino acid is calculated in free form.

[0175] 1.64 Any of the preceding compositions, wherein the amino acid is L-arginine.

[0176] 1.65 Any of the foregoing compositions, wherein the amino acid is arginine in its free form.

[0177] 1.66 Any of the foregoing compositions, wherein the amino acid is arginine or lysine in salt form, either partially or entirely.

[0178] 1.67 The aforementioned composition, wherein the amino acid is arginine phosphate, arginine hydrochloride, or arginine bicarbonate.

[0179] 1.68 Any of the aforementioned compositions, comprising an amphoteric surfactant.

[0180] 1.69 The aforementioned composition, wherein the zwitterionic surfactant is a betaine zwitterionic surfactant (e.g., 0.1% to 5% by weight of the total composition) (e.g., 0.2% to 1% by weight of the total composition) (e.g., about 0.6% by weight of the total composition).

[0181] 1.70 The aforementioned composition, wherein the betaine zwitterionic surfactant is C8-C16 aminopropyl betaine (e.g., cocamidopropyl betaine).

[0182] 1.71 The aforementioned composition, wherein the C8-C16 aminopropyl betaine is cocamidopropyl betaine.

[0183] 1.72 The aforementioned composition, wherein the cocamidopropyl betaine is present in an amount of 0.5% to 4% by weight of the total composition.

[0184] 1.73 The aforementioned composition, wherein the cocamidopropyl betaine is 0.1% to 3% by weight of the total composition.

[0185] 1.74 The aforementioned composition, wherein the cocamidopropyl betaine is 0.1% to 1% by weight (e.g., about 0.6% by weight) of the total composition.

[0186] 1.75 Any of the preceding compositions, wherein the composition comprises cocamidopropyl betaine and sodium methylcocoyl taurate in a weight % ratio (e.g., weight %) of 0.1:1 to 1:1 (e.g., 0.1:1, 0.2:1, 0.3:1, 0.4:1 or 0.5:1) (e.g., 0.3:1).

[0187] 1.76 Any of the foregoing compositions, wherein the oral care composition is free of sodium lauryl sulfate.

[0188] 1.77 Any of the preceding compositions, wherein the composition comprises:

[0189] Zinc phosphate;

[0190] ·Stin fluoride;

[0191] • Sodium ascorbate phosphate and / or 6-palmitate ascorbate; and

[0192] • Oral-acceptable carriers.

[0193] 1.78 Any of the foregoing compositions, wherein the composition comprises:

[0194] Zinc phosphate;

[0195] ·Stin fluoride;

[0196] Arginine;

[0197] • Sodium ascorbate phosphate and / or 6-palmitate ascorbate; and

[0198] • Oral-acceptable carriers.

[0199] 1.79 Any of the preceding compositions, wherein the composition comprises:

[0200] ·Stin fluoride;

[0201] • Zinc citrate and / or zinc lactate and / or zinc oxide (e.g., zinc lactate) (e.g., zinc citrate and zinc oxide);

[0202] • Sodium ascorbate phosphate and / or 6-palmitate ascorbate; and

[0203] • Oral-acceptable carriers.

[0204] 1.80 Any of the preceding compositions, wherein the composition comprises:

[0205] Zinc oxide;

[0206] Zinc citrate;

[0207] ·Stin fluoride;

[0208] • Sodium ascorbate phosphate and / or 6-palmitate ascorbate; and

[0209] • Oral-acceptable carriers.

[0210] 1.81 Any of the preceding compositions, wherein the composition comprises:

[0211] ·Stin fluoride;

[0212] ·Stene chloride;

[0213] • Zinc citrate or zinc lactate;

[0214] • Sodium ascorbate phosphate and / or 6-palmitate ascorbate; and

[0215] • Oral-acceptable carriers.

[0216] 1.82 Any of the preceding compositions, wherein the composition comprises:

[0217] ·Stin fluoride;

[0218] ·Stene chloride;

[0219] • One or more zinc salts selected from zinc oxide, zinc citrate, zinc lactate, and combinations thereof; (e.g., zinc lactate) (e.g., zinc citrate and zinc oxide) (e.g., zinc citrate and zinc lactate) (e.g., zinc lactate and zinc oxide);

[0220] • Sodium ascorbate phosphate and / or 6-palmitate ascorbate; and

[0221] • Oral-acceptable carriers.

[0222] 1.83 Any of the foregoing compositions, wherein the composition comprises:

[0223] • 0.5% to 4% by weight of zinc phosphate in the composition;

[0224] • 0.1% to 2% by weight of stannous fluoride in the composition;

[0225] • 1% to 5% by weight (e.g., about 1.5% by weight) (e.g., about 2.5% by weight) of sodium ascorbate phosphate or 6-palmitate ascorbate in the composition; and

[0226] • Oral-acceptable carriers.

[0227] 1.84 Any of the preceding compositions, wherein the composition comprises:

[0228] • 0.1% to 2% by weight of stannous fluoride in the composition;

[0229] • 0.25% to 0.75% by weight of zinc citrate in the composition;

[0230] • 1% to 5% by weight (e.g., about 1.5% by weight) (e.g., about 2.5% by weight) of sodium ascorbate phosphate and / or 6-palmitate ascorbate in the composition; and

[0231] • Oral-acceptable carriers.

[0232] 1.85 Any of the foregoing compositions, wherein the composition comprises:

[0233] • 0.5% to 1.5% by weight of zinc oxide in the composition;

[0234] • 0.25% to 0.75% by weight of zinc citrate in the composition;

[0235] • 0.1% to 2% by weight of stannous fluoride in the composition;

[0236] • 1% to 5% by weight (e.g., about 1.5% by weight) (e.g., about 2.5% by weight) of sodium ascorbate phosphate and / or 6-palmitate ascorbate in the composition; and

[0237] • Oral-acceptable carriers.

[0238] 1.86 Any of the foregoing compositions, wherein the composition comprises:

[0239] • 0.1% to 2% by weight of stannous fluoride in the composition;

[0240] • 0.1% to 2% by weight of stannous chloride in the composition;

[0241] • 0.1% to 2% by weight of zinc citrate in the composition;

[0242] • 1% to 5% by weight (e.g., about 1.5% by weight) (e.g., about 2.5% by weight) of sodium ascorbate phosphate and / or 6-palmitate ascorbate in the composition; and

[0243] • Oral-acceptable carriers.

[0244] 1.87 Any of the preceding compositions, wherein the composition comprises:

[0245] • 0.1% to 2% by weight of stannous fluoride in the composition;

[0246] • 0.1% to 2% by weight of stannous chloride in the composition;

[0247] • One or more zinc salts in an amount of 0.5% to 5%, wherein the zinc salt is selected from: zinc oxide, zinc citrate, zinc lactate, and combinations thereof (e.g., zinc lactate) (e.g., zinc citrate and zinc oxide) (e.g., zinc citrate and zinc lactate) (e.g., zinc lactate and zinc oxide);

[0248] • 1% to 5% by weight (e.g., about 1.5% by weight) (e.g., about 2.5% by weight) of sodium ascorbate phosphate and / or 6-palmitate ascorbate in the composition; and

[0249] • Oral-acceptable carriers.

[0250] 1.88 Any of the preceding compositions, wherein the composition comprises:

[0251] • 0.5% to 4% by weight of zinc phosphate in the composition;

[0252] • 0.1% to 2% by weight of stannous fluoride in the composition;

[0253] • 1% to 5% by weight (e.g., about 1.5% by weight) (e.g., about 2.5% by weight) of sodium ascorbate phosphate and / or 6-palmitate ascorbate in the composition;

[0254] • 0.5% to 10% by weight (e.g., about 1.5% by weight) (e.g., about 5% by weight) of arginine in the composition, wherein the amount of arginine is calculated in free form; and

[0255] • Oral-acceptable carriers.

[0256] 1.89 Any of the preceding compositions, wherein the composition comprises:

[0257] • 0.5% to 4% by weight of zinc phosphate in the composition;

[0258] • 0.1% to 2% by weight of stannous fluoride in the composition;

[0259] • 0.1% to 2% by weight of stannous pyrophosphate in the composition;

[0260] • 1% to 5% by weight (e.g., about 1.5% by weight) (e.g., about 2.5% by weight) of sodium ascorbate phosphate and / or 6-palmitate ascorbate in the composition; and

[0261] • Oral-acceptable carriers.

[0262] 1.90 Composition 1.0 to 1.89 further comprises 0.1% to 5% by weight of cocamidopropyl betaine in the total composition.

[0263] 1.91 Any of the foregoing compositions, wherein the composition does not contain any sodium lauryl sulfate.

[0264] 1.92 Any one of compositions 1.0 to 1.90, wherein said composition is substantially free of sodium lauryl sulfate.

[0265] 1.93 Any of the foregoing compositions, wherein the oral care composition is a dental cleaning agent (e.g., toothpaste or oral gel), powder (e.g., tooth powder), cream, mouthwash, strip, or gum (e.g., chewing gum).

[0266] 1.94 Any of the foregoing compositions further comprises a preservative selected from benzyl alcohol, methylisothiazolinone (“MIT”), sodium bicarbonate, lauryl alcohol, and polyphosphates.

[0267] 1.95 Any of the foregoing compositions, comprising nitric acid or a water-soluble nitrate (e.g., potassium nitrate).

[0268] 1.96 The aforementioned composition, wherein the water-soluble nitrate is selected from alkali metal or alkaline earth metal nitrates, or zinc nitrate, silver nitrate or ammonium nitrate.

[0269] 1.97 The aforementioned composition, wherein the water-soluble nitrate is an alkali metal nitrate or an alkaline earth metal nitrate.

[0270] 1.98 The aforementioned composition, wherein the nitrate is selected from lithium nitrate, sodium nitrate, potassium nitrate, magnesium nitrate, and calcium nitrate.

[0271] 1.99 The aforementioned composition, wherein the nitrate is potassium nitrate.

[0272] 1.100 Any of the foregoing compositions, wherein the oral care composition is free of or substantially free of sodium lauryl sulfate.

[0273] 1.101 Any of the preceding compositions, wherein the oral care composition comprises an effective amount of a taurine surfactant, wherein the taurine surfactant is represented by formula (1):

[0274]

[0275] Where R1 is a saturated or unsaturated straight-chain or branched alkyl chain with 6 to 18 carbon atoms, R2 is H or methyl, and M is M. + It can be H, sodium, or potassium (e.g., sodium methylcocoyl taurate).

[0276] 1.102 The aforementioned composition, wherein R1 is a saturated or unsaturated straight-chain or branched alkyl chain having 8 to 14 C atoms.

[0277] 1.103 The aforementioned composition, wherein the taurine surfactant comprises one or more surfactants selected from the group consisting of: potassium cocoyl taurate, potassium methyl cocoyl taurate, sodium hexanoyl methyl taurate, sodium cocoyl taurate, sodium lauroyl taurate, sodium methyl cocoyl taurate (SMCT), sodium methyl lauroyl taurate, sodium methyl myristoyl taurate, sodium methyl oleoyl taurate, sodium methyl palmitoyl taurate, sodium methyl stearyl taurate, and combinations thereof.

[0278] 1.104 Any of the foregoing compositions, wherein the taurine surfactant comprises sodium methylcocoyl taurate (e.g., 1% to 5% by weight of sodium methylcocoyl taurate) (e.g., about 2% by weight of sodium methylcocoyl taurate).

[0279] 1.105 Any of the foregoing compositions, wherein the oral care composition comprises sodium stearate (e.g., 1% to 5% by weight of the composition) (e.g., 1.5% to 3% by weight) (e.g., 1.75% to 2.5% by weight) (e.g., 1.75% to 2.25% by weight) (e.g., about 2% by weight) (e.g., 2% to 5% by weight) (e.g., 2.5% to 4.5% by weight) (e.g., 2.75% to 4.25% by weight) (e.g., 3% to 4.25% by weight) (e.g., about 4% by weight).

[0280] 1.106 Any of the foregoing compositions, wherein the oral care composition is free of other whitening agents, said other whitening agents including peroxides, percarbonates, peroxysilicates, persulfate derivatives and / or combinations thereof.

[0281] 1.107 Any of the foregoing compositions, wherein the oral care composition is in the form of toothpaste, dental cleaning agent, mouthwash, mouth rinse liquid, topical oral gel, denture cleaner, dental strips, beads, toothpaste strips, ointments, dental floss, tablets, chewing gum, lozenges and tooth powder.

[0282] 1.108 Any of the preceding compositions, wherein the oral care composition comprises sodium stearate in an amount of 0.1% to 4% by weight relative to the total composition.

[0283] 1.109 The aforementioned composition, wherein the amount of sodium stearate is 0.4% to 1.6% by weight of the silicate relative to the total composition.

[0284] 1.110 The aforementioned composition, wherein the amount of sodium stearate is 0.5% to 1.5% by weight of the silicate relative to the total composition.

[0285] 1.111 The aforementioned composition, wherein the amount of sodium stearate relative to the total composition is about 0.5% by weight, about 0.75% by weight, about 1% by weight, about 1.25% by weight, or about 1.5% by weight.

[0286] Composition 1.0 and below, etc., are used in the method described herein.

[0287] This disclosure also provides a method (method 1.0) for whitening the tooth surface of a patient in need (e.g., extrinsic whitening), wherein the method includes contacting the tooth surface in the patient in need with an oral care composition comprising an ascorbic acid derivative (e.g., any one of composition 1.0 and below) for a duration sufficient to whiten the tooth surface.

[0288] 1.1 Method 1.0, wherein the patient in need of this method has gingival irritation or is at risk of gingival irritation.

[0289] 1.2 Method 1.0 or 1.1, wherein the patient in need of this method has weak enamel and / or is at risk of having weak enamel.

[0290] 1.3 Any of the foregoing methods, wherein the patient in need suffers from one or more gastric symptoms.

[0291] 1.4 The aforementioned method, wherein the one or more gastric symptoms are tooth erosion (e.g., enamel erosion) caused by the presence of gastric acid (e.g., stomach acid) in the oral cavity (e.g., an increase or elevation in the amount of stomach acid).

[0292] 1.5 The aforementioned method, wherein the tooth erosion caused by the presence of gastric acid (e.g., enamel erosion) is the subject's enamel erosion caused by calcium loss.

[0293] 1.6 Any of the foregoing methods, wherein the patient suffers from a gastric disease, the gastric disease increases the amount of gastric acid in the patient's oral cavity (and / or prolongs the time the oral cavity is exposed to gastric acid), and wherein the gastric disease is selected from: duodenal ulcer, gastric ulcer, gastroesophageal reflux disease (GERD), corrosive esophagitis, weakly reactive gastroesophageal reflux disease (weakly reactive symptomatic gastroesophageal reflux disease), bulimia nervosa, pathological gastrointestinal hypersecretionary disease (pathological gastrointestinal hypersecretionary disease), Zhuo-Ellison syndrome, heartburn, and hyperacidity dyspepsia.

[0294] 1.7 The aforementioned method, wherein the gastric disease is gastroesophageal reflux disease (GERD).

[0295] 1.8 Any of the foregoing methods, further comprising the condition that the patient is at risk of tooth erosion.

[0296] 1.9 Any of the foregoing methods, further comprising the condition that the patient is at risk of gingivitis.

[0297] This disclosure also provides a method (method 2.0) for increasing the color stability of an oral care composition containing an ascorbic acid derivative, wherein the method comprises adding sodium stearate (e.g., wherein the composition contains sodium ascorbate phosphate or 6-palmitoate ascorbate) to the composition of any of the following compositions, wherein the sodium stearate reduces the yellowing variable in the oral care composition relative to a reference oral care composition containing sodium ascorbate phosphate or 6-palmitoate but not sodium stearate.

[0298] In some embodiments, the application of any of composition 1.0 and below is part of a method for treating or reducing enamel discoloration.

[0299] In another aspect, any of the compositions 1.0 and below can be used in a method of whitening the surface of tooth enamel to remove extrinsic staining.

[0300] In one aspect, this disclosure contemplates the use of any of the disclosed compositions (e.g., any of compositions 1.0 and below, etc.) in any of the methods described herein (e.g., methods 1.0 and below, etc. or methods 2.0 and below, etc.).

[0301] As used herein, “staining” refers to discoloration of the tooth surface caused by the adsorption or absorption of a staining agent on or within the surface, or by the reaction of the tooth surface material (e.g., enamel) with a staining or non-staining agent in contact with the surface. In one aspect, staining is caused by exposure to tobacco smoke, chewing tobacco, tea, and / or coffee.

[0302] Manufacturing method

[0303] The oral care compositions of this disclosure are prepared by any of a variety of methods, which include adding and mixing the components of the oral care composition in a suitable container equipped with a mixer. In one embodiment, ascorbic acid derivatives, humectants, surfactants, and carriers are mixed to form a homogeneous mixture. Additional components, such as flavoring agents, coloring agents, or sweeteners, may be added at any time during the mixing process, and in many embodiments, such components are preferably added last or near last.

[0304] Example

[0305] The following embodiments are for illustrative purposes only and are not intended to limit the scope of this disclosure in any way, nor should they be construed as limiting the scope of this disclosure in any way. Those skilled in the art will understand that variations and modifications can be made to the following embodiments without departing from the spirit or scope of this disclosure.

[0306] As will be apparent to those skilled in the art, the individual isomer forms can be obtained by separating the mixture in a conventional manner. For example, in the case of diastereomeric isomers, chromatographic separation can be employed.

[0307] The following compounds were used in the examples:

[0308]

[0309] Several alkaline toothpastes containing various main ingredients were formulated as described in the table below. To evaluate the whitening efficacy of reducing agents, a series of reducing agents were added to the alkaline toothpastes at different weight percentages. The pH of the toothpaste samples was adjusted as needed to maintain a pH between 5 and 11 using 1M sodium hydroxide (NaOH) and 1M hydrochloric acid (HCl). The whitening efficacy of these toothpaste samples was determined in standard brushing studies, as described below in Example 1. In each study, the whitening efficacy was compared with alkaline toothpastes and whitening toothpastes containing more conventional whitening agents such as peroxides and / or abrasives.

[0310] Example 1. Standard Toothbrushing Study

[0311] Purchase individual bovine enamel teeth mounted in resin blocks and brush them with abrasive paste until the initial "L" value is 56 to 68. Prepare dental trays for the brushing machine, with each tray consisting of six teeth mounted using 3D-printed dental trays. Perform baseline optical measurements of the bovine teeth using a spectrophotometer and load the dental trays onto the brushing machine.

[0312] The toothbrush was placed on the brushing machine by removing the head of the manual toothbrush from its handle. A slurry consisting of test toothpaste and artificial saliva in a 1:1 weight ratio was prepared and added to each tooth tray. The teeth were brushed for two minutes at 120 strokes per minute and a pressure of 250 grams. After brushing was stopped, the slurry was removed and any remaining toothpaste was rinsed off with deionized water. The brushing treatment was repeated a total of 14 times, with measurements taken every two cycles. The teeth were then gently patted with a paper towel to remove excess liquid, and measurements were taken using a spectrophotometer. Six teeth were tested per unit. The “L,” “a,” and “b” values ​​were determined and used to calculate the whiteness change “ΔW” for each tooth after treatment. According to the International Committee of Illumination (CIE), the “L,” “a,” and “b” values ​​provide a digital representation of a three-dimensional color space, where “L” represents the lightness axis, “a” represents the red-green axis, and “b” represents the yellow-blue axis. All “ΔW” values ​​were averaged over the teeth in the same treatment. A lower "ΔW" means whiter teeth.

[0313]

[0314] ΔW*=W* 经处理的 -W* 基线

[0315] Anova-Tukey statistical analysis was performed to examine the statistical differences with the buffer alone (p<0.05 was declared significant).

[0316] Example 2. Evaluation of reducing agents as whitening agents in toothpaste

[0317] Prepare alkaline toothpaste A without colorants according to Table 1.

[0318] Table 1: Toothpaste A

[0319]

[0320]

[0321]

[0322] Based on the total weight of the toothpaste sample, various reducing agents were added to toothpaste A at a rate of 2.5% by weight, and the pH was adjusted as needed.

[0323] Table 2: Toothpaste sample A containing reducing agent

[0324]

[0325] The whitening effect of toothpaste sample A was determined in a standard brushing study, as described in Example 1. The ΔW values ​​are listed in Table 3.

[0326] Table 3: ΔW values ​​of toothpaste sample A containing reducing agent

[0327]

[0328] "a” TP A is toothpaste A as defined in Table 1.

[0329] "b” Toothpaste A containing 2.5% by weight L-ascorbic acid

[0330] "c” Toothpaste A containing 2.5% by weight of (+)-L-ascorbic acid sodium

[0331] "d” Toothpaste A contains 2.5% by weight of sodium ascorbate phosphate.

[0332] "e” Toothpaste A contains 2.5% by weight of 6-palmitate ascorbate.

[0333] "f” Toothpaste A contains 2.5% citric acid by weight.

[0334] "g” Toothpaste A contains 2.5% by weight citric acid + 2.5% by weight L-ascorbic acid.

[0335] "h” Toothpaste A containing 2.5% by weight TCEP

[0336] The ΔW data shown in Table 3 indicate that ascorbate: sodium ascorbate phosphate and 6-palmitate ascorbate provided whitening efficacy when added to toothpaste A: Sample 3 and Sample 4, respectively. Based on these results, the whitening efficacy of 6-palmitate ascorbate was further investigated in different alkaline toothpaste formulations.

[0337] Example 3.6 Evaluation of ascorbic acid palmitate as a whitening agent

[0338] Prepare alkaline toothpaste B without flavoring agents or coloring agents according to Table 4.

[0339] Table 4: Toothpaste B

[0340]

[0341]

[0342] 6-Palmyl ascorbate was added to alkaline toothpaste B in varying amounts, and the pH of the sample was adjusted as needed.

[0343] Table 5: Toothpaste Sample B containing 6-palmitoyl ascorbate

[0344]

[0345] The whitening efficacy of toothpaste sample B was determined in a standard brushing study as described in Example 1. In addition to alkaline toothpaste B, two other toothpaste samples were used as controls: toothpaste C and toothpaste D. Toothpaste C contains dicalcium phosphate dihydrate, and toothpaste D contains 0.1% hydrogen peroxide as a whitening agent. ΔW values ​​are listed in Table 6.

[0346] Table 6: ΔW values ​​of toothpaste sample B containing 6-palmitate ascorbate

[0347]

[0348] "a” TP B is the toothpaste B specified in Table 4.

[0349] "b” TP C is a toothpaste containing dicalcium phosphate dihydrate.

[0350] "c” TP D is a toothpaste containing 0.1% by weight of H2O2.

[0351] "d” Toothpaste B contains 1.0% by weight of 6-palmitate ascorbate.

[0352] "e” Toothpaste B contains 3.0% by weight of 6-palmitate ascorbate.

[0353] "f” Toothpaste B contains 5.0% by weight of 6-palmitate ascorbate.

[0354] The ΔW data in Table 6 indicate that all toothpaste samples containing 6-palmitoyl ascorbate had an impact on whitening efficacy. The formulations of toothpaste "C" and toothpaste "D" are as follows:

[0355] Table 6a – Toothpaste C

[0356]

[0357] Table 6b – Toothpaste D

[0358]

[0359] Example 4. Evaluation of sodium ascorbate phosphate as a whitening agent

[0360] Based on the results obtained in Table 3, the whitening effect of sodium ascorbate phosphate was further investigated. Toothpaste samples were prepared by adding different amounts of sodium ascorbate phosphate to alkaline toothpaste B in Table 4. The pH value of the samples was adjusted as needed.

[0361] Table 7: Toothpaste Sample B containing sodium ascorbate phosphate

[0362]

[0363] The whitening effect of toothpaste sample B was determined in a standard brushing study, as described in Example 1. In addition to alkaline toothpaste B, two other toothpaste samples were used as controls: toothpaste C and toothpaste D. The ΔW values ​​are listed in Table 8.

[0364] Table 8: ΔW values ​​of toothpaste sample B containing sodium ascorbate phosphate

[0365]

[0366] "a” TP B is the toothpaste B specified in Table 4.

[0367] "b” TP C is a toothpaste containing dicalcium phosphate dihydrate.

[0368] "c” TP D is a toothpaste containing 0.1% by weight of H2O2.

[0369] "d” Toothpaste B contains 0.5% by weight of sodium ascorbate phosphate.

[0370] "e” Toothpaste B contains 1.0% by weight of sodium ascorbate phosphate.

[0371] "f” Toothpaste B contains 1.5% by weight of sodium ascorbate phosphate.

[0372] "g” Toothpaste B contains 3.0% by weight of sodium ascorbate phosphate.

[0373] "h” Toothpaste B contains 5.0% by weight of sodium ascorbate phosphate.

[0374] The ΔW data in Table 8 indicate that all toothpaste samples containing sodium ascorbate phosphate have an impact on whitening efficacy.

[0375] Prepare colorant-free alkaline toothpaste B1 according to Table 8A. Add 1.5% by weight of sodium ascorbate phosphate to alkaline toothpaste B1.

[0376] Table 8A: Toothpaste B1

[0377]

[0378]

[0379] Example 5. Further evaluation of sodium ascorbate phosphate as a whitening agent

[0380] Based on the results obtained in Tables 3 and 8, the whitening effect of sodium ascorbate phosphate was further investigated. Alkaline toothpaste E was prepared according to Table 9.

[0381] Table 9. Toothpaste E

[0382]

[0383]

[0384] Toothpaste samples were prepared by adding different amounts of sodium ascorbate phosphate to alkaline toothpaste E. The pH of the samples was adjusted as needed.

[0385] Table 10: Toothpaste Sample E containing sodium ascorbate phosphate

[0386]

[0387]

[0388] The whitening efficacy of the toothpaste samples in Table 10 was determined in a standard brushing study as described in Example 1. The only variation was the initial "L" value, which ranged from 59 to 66. The brushing treatment was repeated a total of 14 times, with measurements taken every 5 cycles. Alkaline toothpaste E was used as a control. The ΔW values ​​are listed in Table 11.

[0389] Table 11: ΔW values ​​of toothpaste sample E containing sodium ascorbate phosphate

[0390]

[0391] "a” TP E is the toothpaste E defined in Table 9.

[0392] "b” Toothpaste E containing 0.5% by weight of sodium ascorbate phosphate

[0393] "c” Toothpaste E containing 2.75% by weight of sodium ascorbate phosphate

[0394] "d” Toothpaste E containing 5.0% by weight of sodium ascorbate phosphate

[0395] The ΔW data in Table 11 indicate that all toothpaste samples containing sodium ascorbate phosphate have an impact on whitening efficacy.

[0396] Example 6. Further evaluation of sodium ascorbate phosphate as a whitening agent

[0397] To further investigate the effect of sodium ascorbate phosphate on whitening, alkaline toothpaste F was prepared according to Table 12.

[0398] Table 12. Toothpaste F

[0399]

[0400]

[0401] Toothpaste samples were prepared by adding different amounts of sodium ascorbate phosphate to alkaline toothpaste F. The pH of the samples was adjusted as needed and is shown in Table 13.

[0402] Table 13: Toothpaste sample F containing sodium ascorbate phosphate

[0403]

[0404] The brushing study was conducted as previously described in Example 1. The only changes were the starting “L” from 57.3 to 66.3, the number of teeth per unit being twelve, and the measurements being taken at the 4th, 8th, and 14th cycles to maintain consistency with the standard brushing study design relative to the factorial study design.

[0405] Table 14: ΔW values ​​of toothpaste sample F containing sodium ascorbate phosphate

[0406]

[0407] "a” TP F is the toothpaste F defined in Table 12.

[0408] "b” Toothpaste F containing 0.5% by weight of sodium ascorbate phosphate

[0409] "c” Toothpaste F containing 1.5% by weight of sodium ascorbate phosphate

[0410] "d” Toothpaste F containing 2.5% by weight of sodium ascorbate phosphate

[0411] "e” Toothpaste F containing 3.5% by weight of sodium ascorbate phosphate

[0412] "f” Toothpaste F containing 5.0% by weight of sodium ascorbate phosphate

[0413] The ΔW data in Table 14 show that the dosage of sodium ascorbate phosphate has a significant impact on the whitening effect.

[0414] Adding sodium ascorbate phosphate to an alkaline toothpaste formulation resulted in an observable yellow color in the toothpaste composition. To overcome this color problem, surfactants were added to the alkaline toothpaste formulation in combination with sodium ascorbate phosphate. Table 15 describes an alkaline toothpaste formulation in which sodium ascorbate phosphate and surfactants were added. Three surfactants, sodium stearate, sodium cocoyl glutamate, and sodium lauroyl hydroxyethyl sulfonate, were screened, individually and in different combinations with / without sodium ascorbate phosphate. The color of the final toothpaste formulation was determined, as listed in Table 16.

[0415] Table 15: Alkaline Toothpaste G

[0416]

[0417]

[0418] Table 16 describes the samples whose colors were tested using a spectrophotometer.

[0419] Table 16: L* and b* values ​​of toothpaste sample G containing sodium ascorbate phosphate and surfactant

[0420]

[0421]

[0422] "a” Sodium cocoyl glutamate

[0423] "b” Sodium lauroyl hydroxyethyl sulfonate

[0424] Alkaline toothpaste samples G containing / without sodium ascorbate phosphate and different amounts and combinations of surfactants were prepared, and their colors were evaluated, as shown in Table 16. The L*, a*, and b* values ​​of these samples are listed in Table 16. A higher b* value indicates a more yellow color, while a lower value indicates a more blue color. A higher L* value indicates a whiter sample compared to a lower L* value, which indicates a darker sample. As can be observed in Table 16, samples without sodium stearate but containing sodium ascorbate phosphate tend to have higher b* values, indicating a more yellow color. Samples containing both sodium stearate and sodium ascorbate phosphate tend to have relatively lower b* values, indicating a less yellow color.

Claims

1. An oral care composition for whitening tooth enamel, wherein the oral care composition is a dentifrice and comprises: sodium ascorbyl phosphate in an amount of 1% to 5% by weight of the total composition; one or more pyrophosphates and one or more tripolyphosphates; sodium cocoyl glutamate; and sodium stearate in an amount of 0.1% to 4% by weight relative to the weight of the total composition.

2. The oral care composition of claim 1, wherein the sodium ascorbyl phosphate is in an amount sufficient to increase the tooth enamel's AW by at least 0.3 times greater relative to a non-peroxide reference standard.

3. The oral care composition of claim 1 or 2, wherein the sodium ascorbyl phosphate is in an amount sufficient to increase the tooth enamel's AW by 0.3 times to 4 times greater relative to a non-peroxide reference standard.

4. The oral care composition of claim 1 or 2, comprising an effective amount of a fluoride ion source.

5. The oral care composition of claim 1 or 2, wherein the oral care composition comprises an abrasive.

6. The oral care composition of claim 1 or 2, comprising one or more humectants selected from sorbitol, glycerin, xylitol, and propylene glycol, or combinations thereof.

7. The oral care composition of claim 1 or 2, comprising an anionic surfactant.

8. The oral care composition of claim 1 or 2, comprising a zwitterionic surfactant.

9. The oral care composition of claim 1 or 2, further comprising an effective amount of one or more alkali metal phosphates.

10. The oral care composition of claim 1 or 2, comprising an amino acid, wherein the amino acid is a basic amino acid.

11. The oral care composition of claim 1 or 2, comprising a stannous ion source.

12. The oral care composition of claim 11, wherein the stannous ion source comprises stannous fluoride.

13. The oral care composition of claim 1 or 2, wherein the composition comprises a zinc ion source, and wherein the zinc ion source comprises one or more zinc salts selected from the group consisting of zinc citrate, zinc oxide, zinc phosphate, zinc lactate, zinc sulfate, zinc silicate, zinc gluconate, and combinations thereof.

14. The oral care composition of claim 1 or 2, wherein the composition comprises a taurinate surfactant, wherein the taurinate surfactant is selected from the group consisting of potassium cocoyl taurate, potassium methyl cocoyl taurate, sodium hexanoyl methyl taurate, sodium cocoyl taurate, sodium lauroyl taurate, sodium methyl cocoyl taurate (SMCT), sodium methyl lauroyl taurate, sodium methyl myristoyl taurate, sodium methyl oleoyl taurate, sodium methyl palmitoyl taurate, sodium methyl stearoyl taurate, and combinations thereof.

15. The oral care composition of claim 9, wherein the alkali metal phosphate is an orthophosphate, a tetraphosphate, or a higher polyphosphate.

16. A method for whitening a tooth surface, wherein the method comprises contacting the tooth surface with the oral care composition of any one of claims 1 to 15 in a patient in need thereof for a duration sufficient to whiten the tooth surface.

17. A method for increasing the color stability of an oral care composition comprising an ascorbic acid derivative, wherein the method comprises adding sodium stearate to the composition of any one of claims 1 to 15, wherein the sodium stearate decreases the amount of yellowing in the composition relative to a reference oral care composition comprising sodium ascorbyl phosphate but not sodium stearate.

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