JP2024506028A - Hydrating oral care compositions containing peroxide - Google Patents

Abstract

A hydrating oral care composition comprising peroxide and water. A hydrating dentifrice composition comprising peroxide and water. A hydrating oral care composition comprising peroxide and water that is capable of releasing at least about 1% peroxide within 120 seconds. A hydrating oral care composition comprising peroxide and water that is capable of releasing at least about 15% peroxide within 15 minutes.

Description

The present invention relates to hydratable oral care compositions comprising peroxide and water. The present invention relates to hydratable dentifrice compositions comprising peroxide and water.

Oral care compositions, such as dentifrice compositions, contain fluoride, peroxide, and/or abrasives to clean teeth, prevent cavities, and maintain the aesthetics and health of the oral cavity, including teeth and gums. May contain agents.

To achieve high whitening effectiveness, it may be desirable to have dentifrice compositions that include relatively high concentrations of peroxide, such as at least about 1%, at least about 3%, or at least about 3.5%. . However, it is difficult to formulate dentifrice compositions containing relatively high concentrations of peroxide because peroxide can react with other dentifrice ingredients such as fluoride, metal ions, and abrasives. obtain. One approach to the formulation challenges associated with peroxide may be to package the peroxide separately and/or apply the peroxide from a separate whitening composition. However, consumer compliance may be lower if the peroxide needs to be applied from a separate composition. Therefore, it may be advantageous to provide peroxide in dentifrice compositions with other ingredients such as fluoride.

Another approach to the formulation challenges associated with peroxides may be to formulate the peroxides as adducts and/or complexes in a non-aqueous chassis. However, anhydrous compositions can lead to dehydration of oral care surfaces that can contribute to sensitivities, such as tooth sensitivity. Additionally, peroxide complexation may lower the amount of peroxide available to provide health and cosmetic benefits. Accordingly, there is a need for improved hydrating oral care compositions, such as improved hydrating dentifrice compositions containing uncomplexed peroxide.

Disclosed herein is an oral care composition comprising: (a) about 1% to about 5% peroxide, by weight of the oral care composition; and (b) water; The care composition releases at least about 1% peroxide within about 120 seconds according to a peroxide release method.

Disclosed herein are hydratable oral care compositions comprising (a) about 1% to about 5% peroxide, by weight of the oral care composition; and (b) water. The oral care composition releases at least about 1% peroxide into the user's oral cavity within about 120 seconds of initial application to the oral cavity.

Disclosed herein is an oral care composition comprising: (a) about 1% to about 5% peroxide, by weight of the oral care composition; and (b) water; The care composition releases at least about 15% peroxide within about 15 minutes of minimal application according to a peroxide release method.

Disclosed herein are hydratable oral care compositions comprising (a) about 1% to about 5% peroxide, by weight of the oral care composition; and (b) water. The oral care composition releases at least about 15% peroxide into the user's oral cavity within about 15 minutes of initial application to the oral cavity.

Disclosed herein is a dense oil-in-water emulsion comprising (a) a hydrophobic phase, (b) an aqueous phase, and (c) a peroxide, wherein the dense oil-in-water emulsion is , releases at least about 1% peroxide within about 120 seconds according to a peroxide release method.

Disclosed herein is a dense oil-in-water emulsion comprising (a) a hydrophobic phase, (b) an aqueous phase, and (c) a peroxide, wherein the dense oil-in-water emulsion is , releases at least about 1% peroxide into the user's oral cavity within about 120 seconds of initial application to the oral cavity.

Disclosed herein are: (a) a peroxide; (b) at least about 5% water by weight of the oral care composition; (c) a fluoride and/or abrasive; An oral care composition.

Disclosed herein is a method of delivering peroxide to the oral cavity of a user, the method comprising: (a) directing the user to apply any of the disclosed oral care compositions to the oral cavity; (b) instructing a user to continue applying the oral care composition to the oral cavity for at least 120 seconds.

Described herein is a method of delivering a majority of peroxide to a user's oral cavity instead of a sink, the method comprising: (a) having the user apply any of the disclosed oral care compositions to the oral cavity; (b) instructing the user to continue applying the oral care composition to the oral cavity for at least 120 seconds; and (c) instructing the user to spit out the oral care composition. A method comprising: instructing a person to:

Figure 2 shows peroxide release over time in compositions A, B, C, and D.

The present invention is directed to hydratable oral care compositions comprising peroxide and water. Without wishing to be bound by theory, it is believed that peroxide stabilized by complexation and placed within an anhydrous chassis increases the amount of peroxide available to provide health and cosmetic benefits. It is thought that it can be reduced. Additionally, anhydrous compositions can be dehydrating, presenting additional sensitivity challenges.

Surprisingly, it has been found that peroxide in compositions containing water has a high peroxide release rate and can moisturize the oral cavity. Without wishing to be bound by theory, it is believed that peroxides can be incorporated into compositions containing water by minimizing reactivity with the remaining ingredients in oral care compositions containing abrasives. It will be done.

DEFINITIONS To more clearly define the terms used herein, the following definitions are provided. Unless otherwise stated, the following definitions are applicable to this disclosure. When a term is used in this disclosure but is not specifically defined herein, the definition does not conflict with any other disclosure or definition that applies to this specification; Definitions from the IUPAC Compendium of Chemical Terminology, 2nd Ed (1997) may be applied unless they obscure or render impossible any claims to which they apply.

The term "oral care composition," as used herein, refers to a composition that, in the normal course of use, is not intended to be swallowed for the purpose of systemic administration of a particular therapeutic agent, but rather to the surface of the teeth or the oral cavity. Includes products that are retained in the oral cavity for a sufficient period of time to contact tissue. Examples of oral care compositions include dentifrices, tooth gels, subgingival gels, mouth rinses, mousses, foams, mouth sprays, lozenges, chewable tablets, chewing gum, tooth whitening strips, floss and floss coatings, bad breath. Includes prophylactic dissolving strips, or denture care or adhesive products. Oral care compositions may also be incorporated into strips or films for application or attachment directly to oral surfaces.

As used herein, the term "dentifrice composition" includes dental or subgingival paste, gel, or liquid formulations, unless otherwise indicated. The dentifrice composition may be a single phase composition or a combination of two or more separate dentifrice compositions. The dentifrice composition may be in any desired form, such as deep stripes, superficial stripes, multilayers, paste surrounded by gel, or any combination thereof. Each dentifrice composition in a dentifrice containing two or more separate dentifrice compositions may be contained within physically separate compartments of the dispenser and dispensed simultaneously.

"Active substances and other ingredients" useful herein may be classified or described herein by their cosmetic and/or therapeutic effects, or their desired mode of action or function. However, the active substances and other ingredients useful herein may in some cases provide more than one cosmetic and/or therapeutic benefit or function or act in more than one mode of action. It should be understood that Accordingly, the classification herein is implemented for convenience and is not intended to limit the components to the specifically defined functions or actions listed.

The term "orally acceptable carrier" includes one or more compatible solid or liquid excipients or diluents suitable for topical oral administration. The term "compatible" as used herein means that the components of a composition are mixed without interacting in a manner that substantially reduces the stability and/or effectiveness of the composition. It means that you can. The carrier or excipient of the present invention can include the usual and conventional components of mouthwashes or mouthrinses, as described more fully below. Carrier materials for mouthwashes or mouthrinses typically include, but are not limited to, water, alcohol, humectants, surfactants, and flavoring, sweetening, coloring, and/or Contains one or more of the following tolerability modifiers, such as cooling sensation agents.

As used herein, the term "substantially free of" means that a composition contains no more than 0.05%, preferably no more than 0.01%, more preferably no more than 0.01% of the total weight of such composition. Refers to the presence of .001% or less of the indicator.

As used herein, the term "essentially free of" means that the indicator has not been intentionally added to the composition or is preferably not present in an analytically detectable concentration. means. This is meant to encompass compositions in which the indicator is present only as an impurity among other intentionally added substances.

The term "oral hygiene regimen" or "regimen" refers to two or more distinct treatment steps for oral health, such as using toothpaste, mouthrinse, floss, toothpicks, sprays, mouth irrigators, and massagers. It can be a term for

As used herein, the term "total water content" refers to both free water and water bound by other ingredients in the oral care composition.

For the purposes of this invention, a reasonable molecular weight (MW) to be used is that of the material added when preparing the composition, for example if the chelating agent is citric acid, sodium citrate or For citric acid species that may be supplied as other salt forms, the MW used is the molecular weight of the particular salt or acid added to the composition, ignoring any water of crystallization that may be present. It is.

Although compositions and methods are described herein in terms of "comprising" various components or steps, the compositions and methods also include "comprising" various components or steps, unless otherwise specified. It can also be "consisting essentially of" or "consisting essentially of."

As used herein, the word "or" when used as a conjunction of two or more elements is meant to include the elements individually and in combination, e.g. or Y or both.

As used herein, the articles "a" and "an" shall refer to one or more of the claimed or described materials, e.g., "oral care composition" or "bleaching agent." be understood.

Unless otherwise specified, all measurements referred to herein are performed at approximately 23° C. (ie, room temperature).

Generally, groups of elements are designated using the numbering scheme shown in the version of the Periodic Table of the Elements published in Chemical and Engineering News, 63(5), 27, 1985. In some instances, a common name assigned to the group may be used to indicate a family of elements, such as alkali metals for Group 1 elements, alkaline earth metals for Group 2 elements, etc. It will be done.

Several types of ranges are disclosed in this invention. When a range of any kind is disclosed or claimed, all possibilities that such range could reasonably include include the endpoints of the range and any subranges and combinations of subranges subsumed therein. It is intended that each number individually disclosed or claimed.

The dentifrice composition can be in any suitable form, such as solid, liquid, powder, paste, or combinations thereof. Oral care compositions include dentifrices, tooth gels, subgingival gels, mouth rinses, mousses, foams, mouth sprays, lozenges, chewable tablets, chewing gum, tooth whitening strips, floss and floss coatings, and solutions for preventing bad breath. It can be a strip, or a denture care or adhesive product. The components of the dentifrice composition can be incorporated into a film, strip, foam, or fiber-based dentifrice composition.

The oral care compositions described herein include a peroxide and a peroxide-compatible abrasive, such as calcium pyrophosphate. Additionally, the oral care compositions may include other optional ingredients, as described below. The following section headers are provided for convenience only. In some cases, one compound may be included within one or more sections. For example, stannous fluoride can be a tin compound and/or a fluoride compound.

Peroxide The oral care composition includes peroxide. The peroxide can include any suitable peroxide source, such as a solubilized peroxide compound and/or a solid peroxide source. Suitable peroxides include solid peroxides, hydrogen peroxide, urea peroxide, calcium peroxide, benzoyl peroxide, sodium peroxide, barium peroxide, inorganic peroxides, hydroperoxides, organic peroxides, Examples include polyvinylpyrrolidone-peroxide complexes, crosslinked polyvinylpyrrolidone-peroxide complexes, and/or combinations thereof.

Without wishing to be bound by theory, peroxide compounds that are stabilized by complex formation with stabilizing compounds such as cross-linked polyvinylpyrrolidone-peroxides may exhibit effects such as whitening effects when applied to the oral cavity. It is believed that the availability to provide oral health benefits is low. Thus, peroxides may include solubilized peroxide compounds such as aqueous hydrogen peroxide.

In addition, the oral care composition is designed to maximize the amount of peroxide remaining after a defined period of time after initially mixing the oral care composition, for example, through the selection of other ingredients of the oral care composition. can be designed. Suitable oral care compositions include at least about 75%, at least about 80%, at least about 85%, at least about 90% remaining in the oral care composition when the oral care composition is stored at 50° C. for 10 days; Oral care compositions include about 90% to about 99%, or about 88% to about 99% hydrogen peroxide. Other suitable oral care compositions include at least about 75%, at least about 80%, at least about 85%, at least about 90% remaining in the oral care composition when the oral care composition is stored at 50°C for 20 days. %, at least about 95%, about 90% to about 99%, or about 88% to about 99% hydrogen peroxide.

The oral care composition comprises about 0.01% to about 20%, about 0.01% to about 10%, about 1% to about 5%, at least about 1%, by weight of the oral care composition. , at least about 2%, at least about 3%, at least about 3.5%, at least about 4%, or more than 3% by weight peroxide.

Without wishing to be bound by theory, the peroxides described herein may be present even if unbound or uncomplexed by other ingredients in the oral care composition; and/or may be minimally stabilized. Additionally, it is not bound, non-complexed, and/or only minimally stabilized to other ingredients in the oral care composition, such as amphiphilic polymers and/or other thickening agents. Oral care compositions containing no peroxide have higher peroxide release rates than compositions with peroxide adducts such as polyvinylpyrrolidone-peroxide and/or other sources of bound peroxide. It is thought that it can be brought about. Desirable oral care compositions include at least about 10%, at least about 15%, at least about 25%, at least about 35%, at least about 50%, at least about 60%, at least about 70%, at least about 75%, at least about 80%, at least about 90%, at least about 95%, about 10% to about 95%, about 25% to about 75%, about 20% to about 95%, about 35% to about 90%, about 40% to about 95%, about 50% to about 90% , and oral care compositions having a peroxide release of about 60% to about 99%.

Abrasives The oral care compositions may include abrasives, such as peroxide-compatible abrasives. Abrasives may be added to oral care formulations to help remove surface stains from teeth. The abrasive may include a calcium abrasive, a silica abrasive, a carbonate abrasive, a phosphate abrasive, an alumina abrasive, other suitable abrasives, and/or combinations thereof.

Calcium abrasives can include calcium carbonate, dicalcium phosphate, tricalcium phosphate, calcium orthophosphate, calcium metaphosphate, calcium pyrophosphate, calcium polyphosphate, calcium hydroxyapatite, and combinations thereof.

Calcium abrasives may include calcium carbonate. The calcium-containing abrasive can be selected from the group consisting of finely ground natural chalk, ground calcium carbonate, precipitated calcium carbonate, and combinations thereof.

Calcium abrasives may include calcium pyrophosphate. Without wishing to be bound by theory, it is believed that certain sources of calcium pyrophosphate may be sufficiently compatible with peroxides used in peroxide-containing oral care compositions. Calcium pyrophosphate has at least three polymorphic forms: alpha (α), beta (β), and gamma (γ). Unexpectedly, it has been found that calcium pyrophosphate with a higher proportion of gamma phase is more compatible with peroxides such as hydrogen peroxide. Suitable sources of calcium pyrophosphate include at least about 0.75, at least about 0.8, at least about 0.9, at least about 1, about 0.75 to about 1.5, about 0.9 to about 1.5 , or a ratio of gamma phase calcium pyrophosphate to beta phase calcium pyrophosphate from about 1 to about 1.5.

Without wishing to be bound by theory, it is believed that polishing agents containing large amounts of soluble metal ions are less compatible with peroxides due to the reactivity between the peroxides and metal ions. Accordingly, suitable abrasive sources, such as calcium pyrophosphate, provide less than about 0.001%, less than about 0.00075%, less than about 0.0006%, less than about 0.0005%, or about It can constitute less than 0.0001% by weight. Additionally, the abrasive can be free, substantially free, or essentially free of soluble metal ions. Examples of trace metal ions that may be present in abrasives and have been previously reported to induce peroxide decomposition include Cr, Mn, Fe, Co, Ni, Cu, Mo, and/or Or a combination thereof.

As described herein, it has also been unexpectedly found that abrasives having a slurry pH of about 5.4 to about 7 are more compatible with peroxide. Slurry pH was determined by making a 1:3 abrasive:water slurry and measuring the pH.

Carbonate abrasives can include sodium carbonate, sodium bicarbonate, calcium carbonate, strontium carbonate, and/or combinations thereof.

The phosphate abrasive can include calcium phosphate, sodium hexametaphosphate, dicalcium phosphate, tricalcium phosphate, calcium orthophosphate, calcium metaphosphate, calcium polyphosphate, polyphosphate, pyrophosphate, and/or combinations thereof.

Silica abrasives can include fused silica, fumed silica, precipitated silica, hydrated silica, and/or combinations thereof.

Alumina abrasives can include polycrystalline alumina, calcined alumina, uncalcined alumina, fused alumina, wet ground alumina, hydrated alumina, and/or combinations thereof.

Other suitable abrasives include diatomaceous earth, barium sulfate, wollastonite, perlite, polymethyl methacrylate particles, Tospearl, and combinations thereof.

The oral care composition comprises about 0.01% to about 30%, about 0.01% to about 15%, about 0.01% to less than 15%, about 1% by weight of the oral care composition. % to about 30%, about 1% to less than 15%, about 1% to about 12%, or about 0.01% to about 10% by weight of the abrasive.

The oral care composition can have a pellicle cleansing ratio (PCR) of at least about 75, at least about 90, at least about 100, from about 75 to about 250, or from about 100 to about 250.

The oral care composition can have a relative dentin polishing efficiency of up to about 250, up to about 150, from about 70 to about 150, or from about 50 to about 250.

Alumina The oral care composition may include alumina as an abrasive. Alumina may be the sole abrasive or may be used in combination with other abrasives as described herein. Since the abrasiveness of alumina can be higher than silica, smaller amounts of alumina abrasive can be added.

Oral care compositions comprising alumina can have a hard tissue safety value (REA) of at least about 15, at least about 20, at least about 25, or at least about 40.

Oral care compositions comprising alumina have a pellicle cleaning ratio (PCR) of at least about 75, at least about 100, about 75 to about 250, about 50 to about 175, about 50 to about 150, or about 65 to about 155. It is possible.

Oral care compositions that include alumina can have a relative dentin abrasion efficiency (RDA) of less than about 150, less than about 125, less than about 100, or less than about 90.

Without wishing to be bound by theory, it is believed that alumina may react with peroxides and/or fluorides. Accordingly, desirable alumina abrasives include those that are compatible with peroxides and/or fluorides. Suitable oral care compositions include at least about 75%, at least about 80%, at least about 85%, at least about 85% remaining in the oral care composition when the oral care composition is stored at 40° C. for 30 and/or 60 days. Oral care compositions include about 90%, at least about 95%, about 90% to about 99%, or about 88% to about 99% hydrogen peroxide.

Other suitable oral care compositions include peroxide and alumina and after 30 and/or 90 days at 40° C. less than about 10%, less than about 5%, less than about 4%, less than about 3% , about 0.5% to about 10%, about 0.5% to about 5%, or about 0.1% to about 5%. Without wishing to be bound by theory, it is believed that alumina is unexpectedly stable for alumina, and the amount of peroxide lost to peroxide decomposition and/or degradation is minimal.

Other suitable oral care compositions include peroxide, fluoride, and alumina, and after 30 and/or 90 days at 40° C. less than about 20%, less than about 18%, less than about 15%; Oral care compositions having a % fluoride loss of less than about 10%, less than about 5%, about 0.5% to about 10%, about 0.5% to about 20%, or about 0.1% to about 15%. Things can be mentioned. Without wishing to be bound by theory, it is believed that alumina and peroxide are unexpectedly stable with certain fluoride sources and only minimal loss of fluoride is observed.

Other suitable oral care compositions include peroxide and alumina, at least about 5%, at least about 10%, at least about 15%, at least about 20% for 30 days and/or 90 days at 40°C. , at least about 25%, at least about 35%, at least about 50%, at least about 75%, at least about 100%, about 5% to about 125%, about 5% to about 50%, or about 1% to about 75%. Oral care compositions having a % viscosity increase of . Without wishing to be bound by theory, it is believed that the combination of alumina and peroxide is unexpectedly stable, making it less likely that metastable peroxide compositions are commonly observed due to peroxide decomposition. It is believed that the decrease in viscosity can be minimized.

The oral care composition may contain about 0.01% to about 10%, about 0.01% to about 5%, about 0.1% to about 5%, about 0.01% to about 5%, about 0.1% to about 5%, by weight of the oral care composition. 0.01% to about 3%, or about 0.01% to about 1% by weight alumina.

Water The oral care compositions of the present invention can be dentifrice compositions that are anhydrous, low water content formulations, or high water content formulations. In total, the oral care composition comprises 0% to about 99%, about 5% to about 60%, about 5% to about 75%, about 20% or more, about 30% by weight of the composition. % or more, about 50% or more, up to about 45%, or up to about 75% by weight water. Preferably the water is USP water.

Oral care compositions of the present invention may include water. Without wishing to be bound by theory, the inclusion of water in oral care compositions provides greater availability of peroxide to provide oral health benefits such as whitening while hydrating the oral cavity. It is thought that this can lead to One option for stabilizing peroxide is to provide complexed peroxide in the anhydrous dentifrice composition, while simultaneously adding moisture to the oral cavity by selecting other ingredients in the oral care composition. It is believed that peroxide can be delivered more effectively while providing

In high water content dentifrice formulations, the dentifrice composition contains from about 45% to about 75% water by weight of the composition. Highly hydrated dentifrice compositions may include from about 45% to about 65%, from about 45% to about 55%, or from about 46% to about 54% water, by weight of the composition. Water may be added directly to the high water content dentifrice formulation and/or may be included in the composition by including other ingredients.

In low water content dentifrice formulations, the dentifrice composition contains from about 5% to about 45% water, or from about 10% to about 45%, by weight of the composition. Low water content dentifrice compositions may contain from about 10% to about 35%, from about 15% to about 25%, or from about 20% to about 25% water, by weight of the composition. Water may be added directly to the low water content dentifrice formulation and/or may be included in the composition by including other ingredients.

In anhydrous dentifrice formulations, the dentifrice composition contains less than about 10% water by weight of the composition. Anhydrous dentifrice compositions contain less than about 5%, less than about 1%, or 0% water by weight of the composition. Water may be added directly to the anhydrous formulation and/or may be included in the dentifrice composition by including other ingredients.

The dentifrice compositions also contain other orally acceptable agents such as alcohols, humectants, polymers, surfactants, and tolerability-improving agents, such as flavoring agents, sweetening agents, coloring agents, and/or cooling agents. A carrier material may be included.

Oral care compositions may also be mouthrinse formulations. Mouth rinse formulations may contain about 75% to about 99%, about 75% to about 95%, or about 80% to about 95% water.

Amphiphilic Polymers Oral care compositions can include amphiphilic polymers. Amphiphilic polymers may be included as peroxide compatible thickeners. Amphiphilic polymers can include polymers that have hydrophobic portions and hydrophilic portions. For example, a polymer can include a macromolecule that includes a hydrophilic backbone and hydrophobic subunits. This may allow the amphiphilic polymer to remain soluble in water while preventing strong interactions with peroxides.

It is believed that peroxide can be effectively delivered into the aqueous chassis if the other components are designed to minimize reactivity with the peroxide, as described herein. . Therefore, it is desirable that amphiphilic polymers do not react strongly with peroxides. Therefore, it is desirable that the amphiphilic polymer not form an isolable complex with the peroxide.

Amphiphilic polymers may include polymers that are at least partially and/or completely soluble in water.

Suitable amphiphilic polymers include 2-acrylamido-2-methylpropanesulfonic acid (AMPS) polymers, copolymers, crosspolymers, or combinations thereof. In one example, the oral care composition may contain polyacrylate crosspolymer-6 (commercially available as SepIMax™ ZEN from SEPPIC S.A., a subsidiary of Air Liquide Group, Puteaux Cedex, France). .

The oral care composition comprises about 0.01% to about 10%, about 0.1% to about 5%, about 1% to about 10%, or about 1% by weight of the oral care composition. It may contain up to about 5% by weight of amphiphilic polymer.

Alkyl Alcohols Oral care compositions may include alkyl alcohols. Without wishing to be bound by theory, it is believed that the addition of an alkyl alcohol in combination with an amphiphilic polymer can result in an oral care composition having an unexpectedly high viscosity.

Alkyl alcohols can include compounds having an alkyl functional group and an alcohol functional group. The alkyl functionality can be straight chain, branched, cyclic, or a combination thereof. Alkyl alcohols can include primary alcohols, secondary alcohols, and/or tertiary alcohols.

Alkyl alcohols can be represented by the general formula C _n H _2n+1 OH, where n can be any integer from 1 to 30, 10 to 20, or 10 to 25.

Specific examples of alkyl alcohols include 1-heptacosanol, 1-hexacosanol, 1-nonacosanol, 1-octacosanol, 1-tetracosanol, docosanol, heneicosan-1-ol, pentacosan-1-ol, and tricosan-1-ol. alcohol, 1,4-butanediol, 1-heptanol, 1-hexanol, 1-nonanol, 1-octanol, 1-pentanol, 1-propanol, 2,4-dichlorobenzyl alcohol, 2-ethylhexanol, 3-nitro Benzyl alcohol, allyl alcohol, anisyl alcohol, arachidyl alcohol, benzyl alcohol, cetyl alcohol, cinnamyl alcohol, crotyl alcohol, furfuryl alcohol, isoamyl alcohol, neopentyl alcohol, nicotinyl alcohol, perillyl alcohol, phenethyl alcohol, Mention may be made of propargyl alcohol, salicyl alcohol, stearyl alcohol, tryptophol, vanillyl alcohol, veratrol alcohol, and/or combinations thereof. Alkyl alcohols may include stearyl alcohol, cetyl alcohol, and/or combinations thereof.

The alkyl alcohol can be a commercially available mixture of alkyl alcohols, such as Lanette® W (available from BASF, Florham Park, NJ), which contains a 45:45:10 ratio of cetyl alcohol:stearyl alcohol:sodium lauryl sulfate. can be provided by.

The oral care composition comprises about 0.01% to about 10%, about 0.1% to about 5%, about 1% to about 10%, or about 1% by weight of the oral care composition. It may contain up to about 5% by weight alkyl alcohol.

The combination of amphiphilic polymers and alkyl alcohols can result in oral care compositions with unexpectedly high viscosities. Suitable amphiphilic polymer:alkyl alcohol ratios are at least about 0.25, at least about 0.5, at least about 0.75, at least about 1, about 0.25 to about 5, about 0.5 to 1. 5, or about 1.

The oral care composition can have a viscosity of at least about 5 cP, at least about 10 cP, at least about 20 cP, about 5 cP to about 20 cP, or about 1 cP to about 25 cP.

pH
The pH of the disclosed compositions can be from about 4 to about 10, from about 4 to about 7, from about 4 to about 8, or from about 7 to about 10.

Fluoride The oral care composition may include fluoride, which may be provided by a fluoride ion source. The fluoride ion source contains one or more fluoride ions, such as stannous fluoride, sodium fluoride, potassium fluoride, fluorinated amines, sodium monofluorophosphate, zinc fluoride, and/or mixtures thereof. Compounds can be included.

The fluoride ion source and the tin ion source can be the same compound, such as stannous fluoride, which is capable of producing tin and fluoride ions. Additionally, the fluoride ion source and the tin ion source can be separate compounds, such as when the tin ion source is stannous chloride and the fluoride ion source is sodium monofluorophosphate or sodium fluoride.

The fluoride ion source and the zinc ion source can be the same compound, such as zinc fluoride, which is capable of producing zinc ions and fluoride ions. Additionally, the fluoride ion source and the zinc ion source can be separate compounds, such as when the zinc ion source is zinc phosphate and the fluoride ion source is stannous fluoride.

The fluoride ion source may be essentially free or free of stannous fluoride. Thus, oral care compositions may include sodium fluoride, potassium fluoride, fluorinated amines, sodium monofluorophosphate, zinc fluoride, and/or mixtures thereof.

The oral care composition can include a fluoride ion source that can provide about 50 ppm to about 5000 ppm, preferably about 500 ppm to about 3000 ppm of free fluoride ions. To deliver the desired amount of fluoride ions, the fluoride ion source can be present in the oral care composition in amounts ranging from about 0.0025% to about 5%, from about 0.01% to about 5%, by weight of the oral care composition. Present in an amount of about 10%, about 0.2% to about 1%, about 0.5% to about 1.5%, or about 0.3% to about 0.6% by weight. obtain. Alternatively, the oral care composition may contain less than 0.1%, less than 0.01%, essentially free, substantially free, or free of a fluoride ion source. Good too.

Metals The oral care compositions described herein can include metals, which can be provided by a metal ion source that includes one or more metal ions. The metal ion source may include or be added to a tin ion source and/or a zinc ion source, as described herein. Suitable metal ion sources include metals such as, but not limited to, Sn, Zn, Cu, Mn, Mg, Sr, Ti, Fe, Mo, B, Ba, Ce, Al, In and/or mixtures thereof. Examples include compounds having ions. The metal ion source can be any compound containing a suitable metal and any associated ligands and/or anions.

Suitable ligands and/or anions that can be paired with the metal ion source include acetate ion, ammonium sulfate ion, benzoate ion, bromide ion, borate ion, carbonate ion, chloride ion, citrate ion, Gluconate ion, glycerophosphate ion, hydroxide ion, iodide ion, oxalate ion, oxide ion, propionate ion, D-lactate ion, DL-lactate ion, orthophosphate ion, pyrophosphate ion, sulfate ion, Examples include, but are not limited to, nitrate ions, tartrate ions, and/or mixtures thereof.

The oral care composition comprises from about 0.01% to about 10%, from about 1% to about 5%, or from about 0.5% to about 15% metal and/or metal ion source by weight. obtain.

Tin The oral care compositions of the present invention can include tin, which can be provided by a tin ion source. The stannous ion source is any suitable compound capable of providing stannous ions in the oral care composition and/or capable of supplying stannous ions to the oral cavity when the oral care composition is applied to the oral cavity. obtain. The tin ion sources include stannous fluoride, stannous chloride, stannous bromide, stannous iodide, stannous oxide, stannous oxalate, stannous sulfate, stannous sulfide, and fluoride. It may include one or more tin-containing compounds such as stannic, stannic chloride, stannic bromide, stannic iodide, stannic sulfide, and/or mixtures thereof. The stannous ion source may include stannous fluoride, stannous chloride, and/or mixtures thereof. The tin ion source may also be a fluoride-free tin ion source, such as stannous chloride.

The oral care composition may contain from about 0.0025% to about 5%, from about 0.01% to about 10%, from about 0.2% to about 1%, about 0.01% to about 1%, by weight of the oral care composition. It may include 4% to about 1% by weight, or about 0.3% to about 0.6% by weight of tin and/or a tin ion source. Alternatively, the oral care composition may be essentially free, substantially free, or free of tin.

Zinc The oral care compositions of the present invention may include zinc, which may be provided by a source of zinc ions. Zinc ion sources include zinc fluoride, zinc lactate, zinc oxide, zinc phosphate, zinc chloride, zinc acetate, zinc hexafluorozirconate, zinc sulfate, zinc tartrate, zinc gluconate, zinc citrate, zinc malate, and zinc. One or more zinc-containing compounds may be included, such as glycinate, zinc pyrophosphate, zinc metaphosphate, zinc oxalate, and/or zinc carbonate. The zinc ion source can be a fluoride-free zinc ion source such as zinc phosphate, zinc oxide, and/or zinc citrate.

Zinc and/or a source of zinc ions can be present in the total oral care composition from about 0.01% to about 10%, from about 0.2% to about 1%, from about 0.4% by weight of the dentifrice composition. It may be present in an amount from about 1% to about 1% by weight, or from about 0.3% to about 0.6% by weight. Alternatively, the oral care composition may be essentially free, substantially free, or free of zinc.

Polyphosphates Oral care compositions can include polyphosphates, which can be provided by a polyphosphate source. The polyphosphate source may include one or more polyphosphate molecules. Polyphosphates are a class of materials obtained by dehydration and condensation of orthophosphates to yield linear and cyclic polyphosphates of various chain lengths. Therefore, polyphosphate molecules are generally identified by the average number of polyphosphate molecules (n), as described below. Polyphosphates are generally understood to consist of two or more phosphate molecules arranged primarily in a linear configuration, although some cyclic derivatives may also be present.

Preferred polyphosphates contain an average of two or more phosphate groups such that surface adsorption at an effective concentration produces sufficient unbound phosphate functionality, which enhances the anionic surface charge as well as the hydrophilic character of the surface. It has the following. Preferred in the present invention are those having the formula: XO(XPO ₃ ) _n It is a linear polyphosphate with a Alkaline earth metal cations, such as calcium, are not preferred because of their tendency to form insoluble fluoride salts from aqueous solutions containing fluoride ions and alkaline earth metal cations. Accordingly, the oral care compositions disclosed herein may be free or substantially free of calcium pyrophosphate.

Some examples of suitable polyphosphate molecules include, for example, pyrophosphate (n=2), tripolyphosphate (n=3), tetrapolyphosphate (n=4), soda phosphate (n=6), Mention may be made of hexaphospolyphosphate (n=13), benefospolyphosphate (n=14), hexametaphosphate, also known as Glass H (n=21). Polyphosphates can include polyphosphate compounds manufactured by FMC Corporation, ICL Performance Products, and/or Astaris.

The oral care composition may contain from about 0.01% to about 15%, from about 0.1% to about 10%, from about 0.5% to about 5%, from about 1% to about 1%, by weight of the oral care composition. It may include up to about 20%, or about 10% by weight of the polyphosphate source. Alternatively, the oral care composition may be essentially free, substantially free, or free of polyphosphate.

Orthophosphate Oral care compositions can include orthophosphate, which can be provided by an orthophosphate source. Orthophosphate sources include salts containing orthophosphate anions, salts containing phosphate anions (H ₂ PO ₄ ⁻ , HPO ₄ ²⁻ , and PO ₄ ³⁻ ), phosphoric acid compounds, which decompose to orthophosphate under various conditions. and/or another suitable orthophosphate source.

The oral care composition may contain from about 0.01% to about 15%, from about 0.1% to about 10%, from about 0.5% to about 5%, from about 1% to about 1%, by weight of the oral care composition. It may contain up to about 20%, or about 10% by weight orthophosphate. Alternatively, the oral care composition may be essentially free, substantially free, or free of orthophosphate.

Surfactants Oral care compositions may include one or more surfactants. Surfactants can be used to make the composition more cosmetically acceptable. Surfactants are preferably detersive materials that impart detersive and foaming properties to the composition. Suitable surfactants include safe and effective amounts of anionic, cationic, nonionic, zwitterionic, amphoteric and betaine surfactants, such as sodium lauryl sulfate, sodium lauryl isethionate, lauroyl methyl ise. Sodium thionate, sodium cocoyl glutamate, sodium dodecylbenzenesulfonate, lauroyl sarcosinate, myristoyl sarcosinate, palmitoyl sarcosinate, alkali metal salts or ammonium salts of stearoyl sarcosinate and oleoyl sarcosinate, polyoxyethylene sorbitan monostearate, Sodium salt, potassium salt, and ethanolamine salt of polyoxyethylene sorbitan isostearate and polyoxyethylene sorbitan laurate, sodium lauryl sulfoacetate, N-lauroyl sarcosine, N-lauroyl sarcosine, N-myristoyl sarcosine, or N-palmitoyl sarcosine , polyethylene oxide condensates of alkylphenols, cocoamidopropyl betaine, lauramidopropyl betaine, palmityl betaine, sodium cocoyl glutamate, and the like. Sodium lauryl sulfate is a preferred surfactant. The oral care composition comprises one or more surfactants, each containing from about 0.01% to about 15%, from about 0.3% to about 10%, or about 0.3% by weight of the oral care composition. % to about 2.5% by weight.

Surprisingly, it has been found that additional amounts of anionic surfactants such as alkyl sulfate surfactants and/or sodium lauryl sulfate can result in increased peroxide stability. Accordingly, desirable compositions include at least about 1.5%, greater than 1.5%, from about 1.5% to about 10%, or from 1.5% to about 10% by weight of the oral care composition. % of anionic surfactant.

Amino Acids Oral care compositions can include amino acids. Amino acids can include one or more amino acids, peptides, and/or polypeptides, as described herein.

Amino acids are organic compounds that contain an amine functionality, a carboxyl functionality, and a side chain (R in Formula II) specific to each amino acid, as in Formula II. Suitable amino acids include, for example, amino acids with positive or negative side chains, amino acids with acidic or basic side chains, amino acids with polar uncharged side chains, amino acids with hydrophobic side chains, and/or A combination of these can be mentioned. Suitable amino acids include, for example, arginine, histidine, lysine, aspartic acid, glutamic acid, serine, threonine, asparagine, glutamine, cysteine, selenocysteine, glycine, proline, alanine, valine, isoleucine, leucine, methionine, phenylalanine, tyrosine, Also included are tryptophan, citrulline, ornithine, creatine, diaminobutanoic acid, diaminopropionic acid, salts thereof, and/or combinations thereof.

Suitable amino acids include compounds set forth in Formula I, naturally occurring or synthetically derived. Amino acids can be zwitterionic, neutral, positively charged, or negatively charged, based on the R group and the environment. The charge of amino acids and whether certain functional groups can interact with tin under certain pH conditions will be well known to those skilled in the art.

Suitable amino acids include one or more basic amino acids, one or more acidic amino acids, one or more neutral amino acids, or combinations thereof.

The oral care composition may contain about 0.01% to about 20%, about 0.1% to about 10%, about 0.5% to about 6%, or about 1% by weight of the oral care composition. It may contain from % to about 10% by weight of amino acids.

As used herein, the term "neutral amino acids" includes naturally occurring neutral amino acids, such as alanine, asparagine, cysteine, glutamine, glycine, isoleucine, leucine, methionine, phenylalanine, proline, serine, threonine , tryptophan, tyrosine, and valine, as well as biologically acceptable amino acids with isoelectric points ranging from pH 5.0 to 7.0. Biologically preferred and acceptable neutral amino acids have a single amino and carboxyl group in the molecule, or have similar or substantially similar physicochemical properties but with altered side chains. These functional derivatives, such as functional derivatives having . In a further embodiment, the amino acid is at least partially water soluble and provides a pH of less than 7 in an aqueous solution of 1 g/1000 mL at 25°C.

Accordingly, neutral amino acids suitable for use in the present invention include alanine, aminobutyric acid, asparagine, cysteine, cystine, glutamine, glycine, hydroxyproline, isoleucine, leucine, methionine, phenylalanine, proline, serine, taurine, threonine, Examples include, but are not limited to, tryptophan, tyrosine, valine, salts thereof, or mixtures thereof. Preferably, the neutral amino acids used in the compositions of the invention may include asparagine, glutamine, glycine, salts thereof, or mixtures thereof. Neutral amino acids are 5.0, or 5.1, or 5.2, or 5.3, or 5.4, or 5.5, or 5.6, or 5.7 in an aqueous solution at 25°C. , or 5.8, or 5.9, or 6.0, or 6.1, or 6.2, or 6.3, or 6.4, or 6.5, or 6.6, or 6.7 , or 6.8, or 6.9, or 7.0. Preferably, the neutral amino acid is selected from proline, glutamine, or glycine, more preferably in its free form (ie, uncomplexed). When the neutral amino acid is in its salt form, it is known in the art that suitable salts are pharmaceutically acceptable salts that are considered physiologically acceptable in the amounts and concentrations provided. Examples include known salts.

Humectants The oral care compositions may include one or more humectants, low concentrations of humectants, or no humectants. Humectants not only add body or "mouthfeel" to an oral care composition or dentifrice, but also serve to prevent the dentifrice from drying out. Suitable humectants include polyethylene glycol (in various different molecular weights), propylene glycol, glycerin (glycerol), erythritol, xylitol, sorbitol, mannitol, butylene glycol, lactitol, hydrolyzed hydrogenated starch, and/or mixtures thereof. can be mentioned. The oral care compositions each contain 0 to about 70%, about 5% to about 50%, about 10% to about 60%, or about 20% to about 80% by weight of the oral care composition. Concentrations may include one or more humectants.

Thickeners Oral care compositions may include one or more thickeners in addition to the amphiphilic polymer and alkyl alcohol, as described herein. Thickeners can be useful in oral care compositions to provide a gelatin structure that stabilizes the dentifrice and/or toothpaste against phase separation. Suitable thickeners include polysaccharides, polymers, and/or silica thickeners.

Thickeners may include one or more polysaccharides. Some non-limiting examples of polysaccharides include starch; glycerites of starch; gums such as gum karaya (gum sterculia), gum tragacanth, gum arabic, gum gati, gum acacia, xanthan gum, guar gum, and cellulose gum; aluminum silicate. Magnesium (Veegum); carrageenan; sodium alginate; agar; pectin; gelatin; cellulose compounds such as cellulose, microcrystalline cellulose, carboxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxymethylcellulose, hydroxymethylcarboxypropylcellulose, methylcellulose, ethylcellulose, and sulfated cellulose; natural and synthetic clays, such as hectorite clay; and mixtures thereof.

Other polysaccharides suitable for use herein include carrageenan, gellan gum, locust bean gum, xanthan gum, carbomer, poloxamer, modified cellulose, and mixtures thereof. Carrageenan is a polysaccharide derived from seaweed. There are multiple types of carrageenan that can be distinguished by their seaweed source and/or by the degree and location of sulfation. Thickeners can include κ-carrageenan, modified κ-carrageenan, ι-carrageenan, modified ι-carrageenan, λ-carrageenan, and mixtures thereof. Carrageenans suitable for use herein include those commercially available from FMC Company under the series name "Viscarin", including, but not limited to, Viscarin TP 329, Viscarin TP 388, and Viscarin TP 389. can be mentioned.

Thickeners may include one or more polymers. The polymers include polyethylene glycol (PEG), polyvinylpyrrolidone (PVP), polyacrylic acid, at least one acrylic acid, in varying weight percentages of the oral care composition, and in varying ranges of average molecular ranges. It can be a polymer derived from monomers, a copolymer of maleic anhydride and methyl vinyl ether, a crosslinked polyacrylic acid polymer. Alternatively, the oral care composition may be free, essentially free, or substantially free of maleic anhydride and methyl vinyl ether copolymer.

Thickeners may include one or more inorganic thickeners. Some non-limiting examples of suitable inorganic thickeners include colloidal magnesium aluminum silicate, silica thickeners. Useful silica thickeners include, for example, amorphous precipitated silicas, such as, by way of non-limiting example, ZEODENT® 165 silica. Other non-limiting silica thickeners include ZEODENT® 153, 163, and 167, and ZEOFREE® 177 and 265 silica products, all available from Evonik Corporation, and AEROSIL®. Examples include fumed silica.

The oral care composition may contain one or more of the following: 0.01% to about 15%, 0.1% to about 10%, about 0.2% to about 5%, or about 0.5% to about 2%. It can contain a sticky agent.

Dicarboxylic Acids Oral care compositions can include dicarboxylic acids. Dicarboxylic acids include compounds with two carboxylic acid functional groups. The dicarboxylic acid may include a compound defined by Formula II or a salt thereof.

R can be null, alkyl, alkenyl, allyl, phenyl, benzyl, aliphatic, aromatic, polyethylene glycol, polymer, O, N, P, or combinations thereof.

Dicarboxylic acids include oxalic acid, malonic acid, succinic acid, glutaric acid, adipic acid, pimelic acid, suberic acid, azelaic acid, sebacic acid, undecanedioic acid, dodecanedioic acid, brassylic acid, thapsic acid, Japanese acid, and ferrogenic acid. , exetolic acid, malic acid, tartaric acid, salts thereof, or combinations thereof. Dicarboxylic acids include monoalkali metal oxalates, dialkali metal oxalates, monopotassium monohydrogen oxalate, dipotassium oxalate, monosodium monohydrogen oxalate, disodium oxalate, titanium oxalate, and/or oxalic acid. Suitable salts of dicarboxylic acids may be included, such as other metal salts. Dicarboxylic acids may also include hydrates of dicarboxylic acids and/or hydrates of salts of dicarboxylic acids.

Oral care compositions can include about 0.01% to about 10%, about 0.1% to about 15%, about 1% to about 5%, or about 0.0001 to about 25% dicarboxylic acid.

Other Ingredients Oral care compositions may contain various ingredients such as flavoring agents, sweeteners, colorants, preservatives, buffering agents, or other ingredients suitable for use in oral care compositions, as described below. may contain other ingredients.

Flavoring agents may also be added to the oral care compositions. Suitable flavoring agents include wintergreen oil, peppermint oil, spearmint oil, clove bud oil, menthol, anethole, methyl salicylate, eucalyptol, cassia, 1-menthyl acetate, sage, eugenol, parsley oil, oxanone, alpha - irisone, marjoram, lemon, orange, propenylguetol, cinnamon, vanillin, ethylvanillin, heliotropin, 4-cis-heptenal, diacetyl, methyl para-tert-butylphenylacetate, and mixtures thereof. Cooling agents may also be part of the flavor system. Preferred cooling agents for the present compositions are para-menthane carboxamide agents such as N-ethyl-p-menthane-3-carboxamide (commercially known as "WS-3"), or N-(ethoxy carbonylmethyl)-3-p-menthanecarboxamide (commercially known as "WS-5"), and mixtures thereof. Flavor systems are generally used in the compositions at concentrations of about 0.001% to about 5% by weight of the oral care composition. These flavoring agents generally include aldehydes, ketones, esters, phenols, acids, and mixtures of aliphatic, aromatic, and other alcohols.

Sweeteners may be added to the oral care compositions to impart a pleasant taste to the product. Suitable sweeteners include saccharin (as saccharin sodium, saccharin potassium or saccharin calcium), cyclamate (as sodium salt, potassium salt or calcium salt), acesulfame K, thaumatin, neohesperidin dihydrochalcone, ammoniated glycyrrhizin, dextrose, lebulose, Includes sucrose, mannose, sucralose, stevia, and glucose.

Colorants may be added to improve the aesthetic appearance of the product. Suitable colorants include, but are not limited to, colorants approved by appropriate regulatory agencies such as the FDA and colorants listed in the European Food and Drug Directive, pigments such as _TiO2 , and dyes such as FD&C and D&C dyes.

Preservatives may also be added to oral care compositions to prevent bacterial growth. Suitable preservatives approved for use in oral compositions, such as methylparaben, propylparaben, benzoic acid, and sodium benzoate, can be added in safe and effective amounts.

Titanium dioxide may also be added to the compositions of the invention. Titanium dioxide is a white powder that adds opacity to the composition. Titanium dioxide generally comprises about 0.25% to about 5% by weight of the oral care composition.

Desensitizers, healing agents, other caries prevention agents, chelating agents/sequestering agents, vitamins, amino acids, proteins, other anti-plaque/anti-calculus agents, opacifying agents, antibiotics, anti-enzymes, enzymes, Other ingredients such as pH adjusting agents, oxidants, antioxidants, etc. can be used in the oral care compositions.

Hydrable Oral Care Compositions The oral care compositions can be hydratable oral care compositions. Suitable hydratable oral care compositions deliver large amounts of peroxide and/or other suitable active agents while imparting water or without removing moisture from the oral cavity upon exhalation of the oral care composition. can do. Suitable oral care compositions also include oral care compositions that, upon spitting of the oral care composition into the sink, can deliver a large portion of the active agent contained therein, such as peroxide, to the oral cavity rather than to the sink. obtain.

Suitable oral care compositions include dentifrice compositions, toothpaste compositions, and/or dense oil-in-water emulsions.

Multiphasic Oral Compositions Oral care compositions can include multiphasic oral compositions. Multiphasic oral compositions include multiphasic compositions such as U.S. Patent Application Publication No. 2018/0133121, U.S. Patent Application No. 10,849,729, and/or U.S. Patent Application Publication No. 10,780,032. , each of which is incorporated herein by reference in its entirety.

Suitable multiphase oral compositions include water-in-oil emulsions, oil-in-water emulsions, soluble particle dispersions in a hydrophobic phase, dense oil-in-water emulsions, and/or dense water-in-oil emulsions. . In particular, as described in Tables 5 and 6, dense oil-in-water emulsions have high peroxide release rates.

Conventional oil-in-water emulsions are multiphase compositions with a discontinuous hydrophobic phase and a continuous aqueous phase. Stable oil-in-water emulsions can be prepared by combining a small amount of a hydrophobic phase with a large amount of an aqueous phase. Conventional oil-in-water emulsions are discontinuous droplets of a hydrophobic phase suspended and/or stabilized within a continuous aqueous phase. Because the hydrophobic and aqueous phases are immiscible, generally only a small amount of the hydrophobic phase can be stabilized within the aqueous phase before macroscopic separation occurs.

High internal phase emulsions can be either oil-in-water or water-in-oil emulsions, in which there is a large amount of internal discontinuous phase by volume or weight of the multiphase composition compared to conventional emulsions. do. A high internal phase emulsion may have more internal discontinuous phases by total volume or weight of the multiphase composition than external continuous phases by volume or weight of the multiphase composition. However, the stability of high phase emulsions can prove difficult. High internal phase emulsions may undergo visible separation during mixing or during storage of the high internal phase emulsion prior to use by the consumer.

The dense emulsions described herein can be unexpectedly stable high internal phase emulsions. As the concentration of discontinuous phases in a high internal phase emulsion increases, the regions of discontinuous phases crowd together with the regions of continuous phase between them, and the regions of continuous phase between them They can be dense enough to be able to deform each other in areas. If both the continuous phase and the discontinuous phase are liquids, the emulsion may at least partially transition to a semi-solid structure when migration due to crowding occurs. The dense emulsions described herein can be prepared by adding the discontinuous phase to the continuous phase in portions, or by gradual addition, or by slow addition. Simply combining the entire discontinuous phase into a continuous phase does not necessarily result in a dense emulsion.

Multiphase oral care compositions and/or dense oil-in-water emulsions may include a hydrophobic phase, an aqueous phase, an active agent such as a peroxide, and optionally an emulsifier.

Aqueous Phase The aqueous phase may be at least partially continuous, essentially continuous, or preferably continuous. The multiphasic oral care compositions and/or dense oil-in-water emulsions contain from about 0.01% to about 25% by weight or volume, about 1% by weight of the multiphasic oral care compositions and/or dense oil-in-water emulsions. or from about 2.5% to about 20% by weight or volume, or preferably from about 5% to about 15% by weight or volume of the aqueous phase.

The aqueous phase may also include other water-soluble solvents such as, for example, polyalkylene glycols with humectants having a molecular weight of about 200 to about 20,000, or combinations thereof. Suitable humectants generally include edible polyhydric alcohols such as glycerin, sorbitol, xylitol, butylene glycol, and propylene glycol, and mixtures thereof. The aqueous phase may include at least about 10%, at least about 20%, or at least about 30% water by weight or volume of the aqueous phase. Multiphasic oral compositions may include an aqueous solution of a bleaching agent, such as hydrogen peroxide, optionally including an emulsifier.

Hydrophobic Phase Multiphase oral care compositions and/or dense oil-in-water emulsions may include a hydrophobic phase. The hydrophobic phase may be at least partially discontinuous, essentially discontinuous, or preferably discontinuous.

The multiphasic oral care composition may contain from about 75% to about 99% by weight or volume, from about 80% to about 97.5% by weight or volume of the multiphasic oral care composition or dense oil-in-water emulsion. , more than about 80% by weight or volume, more than about 90% by weight or volume, or preferably from about 85% to about 95% by weight or volume of the hydrophobic phase.

The density of the hydrophobic phase described herein is about 0.8 g/cm ³ to about 1.0 g/cm ³ , about 0.85 g/cm ³ to about 0.95 g/cm ³ , or about 0.9 g/cm 3 / ^cm3 , or any other numerical value that is narrower and falls within such broader numerical range, as if all such narrower numerical ranges were expressly recited herein. It can be a range.

The hydrophobic phase may include a non-toxic oil, such as a non-toxic edible oil. The hydrophobic phase may include non-toxic edible oils, saturated or unsaturated fatty alcohols, aliphatic hydrocarbons, long chain triglycerides, fatty acid esters, and combinations thereof. The hydrophobic phase may also include silicones, polysiloxanes, and mixtures thereof. The hydrophobic phase may preferably be selected from mineral oil, petrolatum, and combinations thereof.

Emulsifiers Multiphase oral care compositions and/or dense oil-in-water emulsions may include one or more emulsifiers. Depending on the design of the multiphase oral care composition, the hydrophobic phase may have emulsifying properties. Thus, the emulsifier and the hydrophobic phase may contain the same compound.

The multiphasic oral care compositions and/or dense oil-in-water emulsions described herein may be from about 0.001% to about 20%, by weight of the multiphasic oral care composition or dense oil-in-water emulsion, from about 0.00% to about 20%, by weight of the multiphasic oral care composition or dense oil-in-water emulsion. 0.1% to about 10%, up to about 10%, up to about 5%, or preferably from about 0.1% to about 10% by weight of emulsifier.

Classes of surfactants useful as emulsifiers include nonionic, anionic, cationic, amphoteric, polymeric, synthetic emulsifiers, and mixtures thereof. Many suitable nonionic and amphoteric surfactants are disclosed in U.S. Pat. No. 3,988,433, U.S. Pat. No. 4,051,234; , U.S. Pat. No. 3,959,458.

Emulsifiers may include polysorbates, alkyl sulfates, Lipowax® D, or combinations thereof. Suitable polysorbate compounds include polysorbates 20, 40, 60, 80, or combinations thereof, such as Tween® 20, 40, 60, 80, or combinations thereof.

Emulsifiers include natural emulsifiers such as acacia, gelatin, lecithin, and cholesterol, finely dispersed solids such as colloidal clay, bentonite, vegum (magnesium aluminum silicate), and salts of fatty acids, sorbitan trioleate, sorbitan tristearate, sucrose distearate. sulfates, such as propylene glycol monostearate, glycerol monostearate, propylene glycol monolaurate, sorbitan monostearate, sorbitan monolaurate, polyoxyethylene-4-lauryl ether, sodium lauryl sulfate, dioctyl sodium sulfosuccinate, Glyceryl esters, polyoxyethylene glycol esters and ethers, sulfonates such as diethylene glycol monostearate, PEG 200 distearate, and sorbitan monopalmitate and their polyoxyethylene derivatives, polyoxyethylene glycol esters such as monostearate, Polysorbate 80 Synthetic emulsifiers such as sorbitan fatty acid esters, such as ethoxylated sorbitan monooleate (supplied by Spectrum and others), as well as combinations thereof, may be included.

The emulsifier may be a surfactant that is non-reactive with bleaching agents. For example, surfactants that are non-reactive with bleach may contain substantially no hydroxy groups, nitrogen groups, and linkages, double or triple covalent bonds between adjacent carbon atoms, metals such as Zn, or combinations thereof. It does not have to be included in

Peroxide Release Suitable oral care compositions include those that have significant peroxide release into the oral cavity. Suitable compositions include compositions A and B listed in Table 6. Other suitable compositions include at least about 0.25%, at least about 0.5%, at least about 1%, at least about 1.5%, at least about 2.5%, at least about 5% after 2 minutes; and/or oral care compositions having a % peroxide diffusion of at least about 10%. Other suitable compositions include oral care compositions that have a % peroxide diffusion after 15 minutes of greater than 13%, at least about 15%, at least about 25%, or at least about 45%.

Other suitable compositions include at least about 0.25%, at least about 0.5%, at least about 1%, at least about 1.5%, at least about Oral care compositions that release 2.5%, at least about 5%, and/or at least about 10% peroxide into the user's oral cavity are included. Other suitable compositions include delivering more than 13%, at least about 15%, at least about 25%, or at least about 45% peroxide to the user's oral cavity within about 15 minutes of initial application to the oral cavity. oral care compositions that are released into the body.

Without wishing to be bound by theory, it is also believed that compositions with high percent peroxide diffusion according to the peroxide release rate method described herein release large amounts of peroxide into the oral cavity.

The invention is further illustrated by the following examples, which should not be construed as imposing a limitation on the scope of the invention in any way. After reading this description, various other embodiments, modifications, and equivalents thereof may occur to those skilled in the art without departing from the spirit of the invention or the scope of the appended claims. .

Peroxide Release A 15 mL dialysis cell (2K MWCO, Slide-A-Lyzer G2 Dialysis Cassette) was filled with WFI MilliQ water (16 grams) and the cap was secured. The test product was applied to one side of the cassette and the entire cell membrane surface was covered at the depth defined by the cell's plastic housing by leveling the applied product with a spatula. A piece of Parafilm was applied over the product composition to protect it during cassette mixing during sampling. The cell was placed vertically or horizontally with the product facing down on a tared balance. After application of the product, a timer was started and samples of the WFI MilliQ water in the cassette were taken at specified time points.

At each defined sampling point, the cell was removed, inverted twice 180°, the lid was removed, and the sample (0.3-0.50 g) was aspirated with a pipette. After sampling, the dialysis cell was returned to the balance until the next sample was required. Each sample was analyzed for peroxide percentage as outlined below.

Peroxide was measured using a Reflectoquant RQ Flex peroxide test strip reader (Millipore Sigma) with both 0.2-0.20 mg/L (604) and 100-1000 mg/L (609) test strips (Supelco). Calibration was performed using a standard solution as follows.
0.2-20.0mg/L strip:
1. Five grams of 35% hydrogen peroxide was diluted with WFI MilliQ water to a total of 500 grams.
2. One gram of (1) was diluted using WFI MilliQ water to a total weight of 500 grams.
3. Two drops of (2) were applied to the 0.2-20.0 mg/L test strip for 5 seconds and excess solution was dabbed on a paper towel.
4. The test strip was inserted into the RQ Flex 10 loaded with the 0.2-20.0 mg/L test strip program and the measurements were recorded. Note that the total strip development and programming is 15 seconds. 5. 2 grams of solution (1) was diluted to 500 grams with WFI MilliQ water and steps (3) and (4) were repeated.
100-1000mg/L strip:
1. 0.5 grams of 35% hydrogen peroxide was diluted with USP water to a total of 500 grams.
2. Two drops of (1) were applied to the 0.2-20.0 mg/L test strip for 10 seconds and excess solution was dabbed on a paper towel. The strip was developed by letting it sit for an additional 50 seconds.
3. The test strip was inserted into the RQ Flex 10 with the 100-1000 mg/L test strip program remaining for 10 seconds and the reading recorded. Note that the total strip deployment and programming was approximately 60 seconds for this test strip.
4. One gram of 35% hydrogen peroxide was diluted with WFI MilliQ water to a total of 500 grams.
5. The test strip was inserted into the RQ Flex 10 loaded with the 100-1000 mg/L test strip program and the measurements were recorded.

Sample analysis 1. Apply two drops from a given test sample time point to a test strip of either 0.2-20.0 mg/L or 100-1000 mg/L, followed by development time and analysis steps as defined above. (a3-a4 and b2-b3).
2. The diffused peroxide concentration defined the appropriate strip to use. If the concentration exceeded the concentration range of the respective strip, serial dilutions were performed to bring the concentration within range.

Peroxide release rates were determined for the four compositions. Composition A in Table 1 and Composition B in Table 2A are compositions of the present invention. Composition C and Composition D in Table 3 are commercial products sold by Colgate-Palmolive Company. Composition C is Colgate Optic White Renewal Toothpaste and is sold as containing 3% hydrogen peroxide by weight. Composition D is Colgate Optic White Overnight, also sold as containing 4% hydrogen peroxide by weight.

Table 1 shows the formulation of Composition A, a dense oil-in-water emulsion. Composition A was made by mixing an aqueous solution of polysorbate 20, water, sucralose, and H ₂ O ₂ in a 20 gallon premix tank. The premix mixture was transferred to a 400 L container and stirred while slowly adding mineral oil over 30 minutes. The flavor was then added and the batch was stirred for 5 minutes. An oil-in-water emulsion was formed during this step and the composition developed a lotion-like semi-solid consistency.

^１Ｓｅｐｉｍａｘ Ｚｅｎ（商標）
^２セチルアルコール：ステアリルアルコール：ＳＬＳ（４５：４５：１０）

¹ Sepimax Zen(trademark)
² Cetyl alcohol: Stearyl alcohol: SLS (45:45:10)

Table 2A shows the formulation of Composition B, a dentifrice composition containing fluoride, 4% by weight peroxide, water, and an abrasive. The release of peroxide into the dialysis cell is shown in Table 5 and further shown in FIG.

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^２セチルアルコール：ステアリルアルコール：ＳＬＳ（４５：４５：１０）

¹ Sepimax Zen(trademark)
² Cetyl alcohol: Stearyl alcohol: SLS (45:45:10)

Table 2B shows various exemplary compositions containing different amounts of amphiphilic polymer (1.25% to 2.25% by weight) and alkyl alcohol (0.75% to 1.25% by weight). show. Examples 1-6 include sodium monofluorophosphate (1.14% by weight), sodium lauryl sulfate (1.4% by weight), calcium pyrophosphate (10% by weight), and hydrogen peroxide (4% by weight) .

Table 3 shows the ingredients listed on the box of the comparative commercial products Composition C, Colgate Optic White Renewal toothpaste, and Composition D, Colgate Optic White Overnight whitening pen.

Table 4 shows an example of the procedure utilized to calculate the amount of peroxide (ppm) in a dialysis cell. As shown in Table 4, Composition A yielded 717 ppm peroxide after 120 seconds, 1525 ppm peroxide after 300 seconds, and 3263 ppm peroxide after 900 seconds. Using the same method of quantification shown in Table 4, concentrations in the dialysis cell were determined using Composition B, Composition C, and Composition D at various times.

Table 5 shows the peroxide concentration of each dialysis cell after loading Compositions AD after specified times. As shown in Table 5, Composition A and Composition B resulted in 717 ppm and 150 ppm hydrogen peroxide, respectively, in the dialysis cell after 120 seconds. Compositions C and D resulted in less than 1 ppm and 2 pm peroxide, respectively, in the dialysis cell after 120 seconds. Additionally, Composition A and Composition B resulted in 3263 ppm and 1529 ppm peroxide, respectively, in the dialysis cell after 900 seconds. Composition C and Composition D resulted in 219 ppm and 252 ppm peroxide, respectively, in the dialysis cell after 900 seconds. Thus, membranes loaded with Composition A and Composition B, both containing hydrogen peroxide in solution, resulted in increased delivery of hydrogen peroxide across the membrane.

Table 6 shows the relative amount of peroxide diffused into the dialysis cell after a specified period of time. 9.3-10.8% of the total amount of peroxide in Composition A diffused into the dialysis cell after 2 minutes. 49% of the total amount of peroxide in Composition A diffused into the dialysis cell after 15 minutes. 1.5% of the total amount of peroxide in Composition B diffused into the dialysis cell after 2 minutes. 16% of the total amount of peroxide in Composition B diffused into the dialysis cell after 15 minutes. In contrast, 0.001% and 0.13% of Composition C and Composition D diffused into the dialysis cell after 2 minutes, and 2.5% and 13% of Composition C and Composition D diffused into the dialysis cell after 2 minutes. Diffused into the dialysis cell after 15 minutes.

Therefore, compositions such as toothpaste compositions and dense oil-in-water emulsion compositions containing peroxide and water resulted in increased diffusion of peroxide into the dialysis cell. Surprisingly, as shown in Table 6 for Composition A and Composition B, peroxide in compositions containing water has a high peroxide release rate and can moisturize the oral cavity. discovered. Without wishing to be bound by theory, it is believed that peroxides can be incorporated into compositions containing water by minimizing reactivity with the remaining ingredients in oral care compositions containing abrasives. It will be done.

Without being bound by theory, as shown in Table 6 for Composition C and Composition D, peroxides stabilized by complexation and placed within an anhydrous chassis have health and cosmetic benefits. It is believed that a lower amount of peroxide can be made available to provide. Additionally, anhydrous compositions can be dehydrating, presenting additional sensitivity issues.

The dimensions and values disclosed herein are not to be understood as being strictly limited to the precise numerical values recited. Instead, unless otherwise indicated, each such dimension is intended to mean both the recited value and a functionally equivalent range surrounding that value. For example, a dimension disclosed as "40 mm" is intended to mean "about 40 mm."

All documents cited herein, including any patents or patent applications that are cross-referenced or related, and any patent applications or patents to which this application claims priority or benefit, are excluded or qualified. is incorporated herein by reference in its entirety unless explicitly stated otherwise. Citation of any document shall not be construed as prior art to any invention disclosed or claimed herein, alone or in combination with any other reference(s). In some cases, no such invention shall be deemed to teach, suggest or disclose any such invention. Further, if any meaning or definition of a term in this document conflicts with any meaning or definition of the same term in a document incorporated by reference, the meaning or definition given to that term in this document shall control. shall be

Although particular embodiments of the invention have been illustrated and described, it will be apparent to those skilled in the art that various other changes and modifications can be made without departing from the spirit and scope of the invention. It is therefore intended that the appended claims cover all such changes and modifications that fall within the scope of this invention.

Claims (24)

A hydrating oral care composition comprising:
(a) about 1% to about 5% peroxide by weight of the oral care composition;
(b) about 5% to about 75% water by weight of the oral care composition;
An oral care composition, wherein the oral care composition releases at least about 1% peroxide within about 120 seconds according to a peroxide release method. The peroxide is hydrogen peroxide, urea peroxide, carbamide peroxide, calcium peroxide, sodium peroxide, zinc peroxide, sodium percarbonate, polyvinylpyrrolidone-hydrogen peroxide complex, cross-linked polyvinylpyrrolidone-hydrogen peroxide. complexes, or combinations thereof, preferably the peroxide comprises hydrogen peroxide, or more preferably the oral care composition comprises at least about 1%, at least about 1% by weight of the oral care composition. 2. The oral care composition of claim 1, comprising 3%, or at least about 3.5% by weight of said peroxide. The oral care composition comprises an abrasive, preferably the abrasive comprises silica, alumina, a calcium abrasive, or a combination thereof, more preferably the calcium abrasive comprises calcium carbonate, calcium phosphate, pyro. 3. The oral care composition of claim 1 or 2, comprising calcium phosphate, or a combination thereof, or wherein the alumina comprises calcined alumina, uncalcined alumina, or a combination thereof. The oral care composition comprises fluoride, preferably the fluoride comprises sodium fluoride, stannous fluoride, sodium monofluorophosphate, amine fluoride, or more preferably a combination thereof. An oral care composition according to any one of claims 1 to 3, wherein the fluoride comprises sodium monofluorophosphate. The oral care composition comprises a metal, preferably the metal comprises tin, zinc, copper, or a combination thereof, or more preferably the tin comprises stannous chloride, stannous fluoride, or a combination thereof, and/or the zinc comprises zinc lactate, zinc oxide, zinc phosphate, zinc citrate, zinc chloride, or a combination thereof. Oral care compositions as described. The oral care composition comprises amino acids, preferably the amino acids are arginine, histidine, lysine, aspartic acid, glutamic acid, serine, threonine, asparagine, glutamine, cysteine, selenocysteine, glycine, proline, alanine, valine, isoleucine. , leucine, methionine, phenylalanine, tyrosine, tryptophan, citrulline, ornithine, creatine, diaminobutanoic acid, diaminopropionic acid, salts thereof, or combinations thereof. care composition. The oral care composition comprises an anionic surfactant, preferably the oral care composition comprises at least about 1.5% or more than 1.5% anionic surfactant by weight of the oral care composition. Oral care composition according to any one of claims 1 to 6, wherein the anionic surfactant comprises a sodium alkyl sulfate surfactant. The oral care composition comprises an amphiphilic polymer, preferably the amphiphilic polymer does not form an isolable complex with the peroxide, more preferably the amphiphilic polymer comprises: or even more preferably, the amphiphilic polymer comprises a 2-acrylamido-2-methylpropanesulfonic acid polymer, copolymer, crosspolymer, or a combination thereof. , the oral care composition according to any one of claims 1 to 7. The oral care composition comprises a dentifrice composition, a toothpaste composition, an emulsion composition, or a combination thereof, and preferably the emulsion composition is an oil-in-water emulsion, a water-in-oil emulsion, or a combination thereof. Or more preferably, the oil-in-water emulsion comprises a dense oil-in-water emulsion. A dense oil-in-water emulsion,
(a) a hydrophobic phase;
(b) an aqueous phase;
(c) peroxide;
The dense oil-in-water emulsion is a dense oil-in-water emulsion that releases at least about 1% peroxide within about 120 seconds according to a peroxide release method. The peroxide is hydrogen peroxide, urea peroxide, carbamide peroxide, calcium peroxide, sodium peroxide, zinc peroxide, sodium percarbonate, polyvinylpyrrolidone-hydrogen peroxide complex, cross-linked polyvinylpyrrolidone-hydrogen peroxide. complexes, or combinations thereof, preferably said dense oil-in-water emulsion comprises at least about 1%, at least about 3%, or at least about 3.5% by weight of said dense oil-in-water emulsion. 11. A dense oil-in-water emulsion according to claim 10, comprising a peroxide. A dense oil-in-water emulsion according to claim 10 or 11, wherein the hydrophobic phase comprises petrolatum. A dense oil-in-water emulsion according to any one of claims 10 to 13, wherein the dense oil-in-water emulsion comprises an emulsifier, preferably the emulsifier comprises a polysorbate, an alkyl sulfate, or a combination thereof. 10. The dense oil-in-water emulsion comprises fluoride, preferably the fluoride comprises sodium fluoride, sodium monofluorophosphate, amine fluoride, stannous fluoride, or a combination thereof. The dense oil-in-water emulsion according to any one of items 1 to 13. The dense oil-in-water emulsion comprises a metal, preferably the metal comprises zinc, tin, copper, or a combination thereof, more preferably the zinc comprises zinc phosphate, zinc oxide, zinc citrate, 15. According to any one of claims 10 to 14, comprising zinc lactate, zinc chloride, or a combination thereof, and/or the tin comprises stannous chloride, stannous fluoride, or a combination thereof. The dense oil-in-water emulsion described. Use of an oral care composition for delivering peroxide to the oral cavity, comprising:
The oral care composition comprises:
(a) about 1% to about 5% peroxide by weight of the oral care composition;
(b) about 5% to about 75% water by weight of the oral care composition;
Use wherein the oral care composition releases at least about 1% peroxide within about 120 seconds according to a peroxide release method. The peroxide is hydrogen peroxide, urea peroxide, carbamide peroxide, calcium peroxide, sodium peroxide, zinc peroxide, sodium percarbonate, polyvinylpyrrolidone-hydrogen peroxide complex, cross-linked polyvinylpyrrolidone-hydrogen peroxide. complexes, or combinations thereof, preferably the peroxide comprises hydrogen peroxide, or more preferably the oral care composition comprises at least about 1%, at least about 1% by weight of the oral care composition. 17. The use according to claim 16, comprising 3%, or at least about 3.5% by weight of said peroxide. The oral care composition comprises an abrasive, preferably the abrasive comprises silica, alumina, a calcium abrasive, or a combination thereof, more preferably the calcium abrasive comprises calcium carbonate, calcium phosphate, pyro. 18. The use according to claim 16 or 17, comprising calcium phosphate, or a combination thereof, or wherein the alumina comprises calcined alumina, uncalcined alumina, or a combination thereof. The oral care composition comprises fluoride, preferably the fluoride comprises sodium fluoride, stannous fluoride, sodium monofluorophosphate, amine fluoride, or more preferably a combination thereof. 19. The use according to any one of claims 16 to 18, wherein the fluoride comprises sodium monofluorophosphate. The oral care composition comprises a metal, preferably the metal comprises tin, zinc, copper, or a combination thereof, or more preferably the tin comprises stannous chloride, stannous fluoride, or a combination thereof, and/or the zinc comprises zinc lactate, zinc oxide, zinc phosphate, zinc citrate, zinc chloride, or a combination thereof. Use as described. The oral care composition comprises amino acids, preferably the amino acids are arginine, histidine, lysine, aspartic acid, glutamic acid, serine, threonine, asparagine, glutamine, cysteine, selenocysteine, glycine, proline, alanine, valine, isoleucine. , leucine, methionine, phenylalanine, tyrosine, tryptophan, citrulline, ornithine, creatine, diaminobutanoic acid, diaminopropionic acid, salts thereof, or combinations thereof. . The oral care composition comprises an anionic surfactant, preferably the oral care composition comprises at least about 1.5% or more than 1.5% anionic surfactant by weight of the oral care composition. 22. Use according to any one of claims 16 to 21, wherein the anionic surfactant comprises a sodium alkyl sulphate surfactant. The oral care composition comprises an amphiphilic polymer, preferably the amphiphilic polymer does not form an isolable complex with the peroxide, more preferably the amphiphilic polymer comprises: or even more preferably, the amphiphilic polymer comprises a 2-acrylamido-2-methylpropanesulfonic acid polymer, copolymer, crosspolymer, or a combination thereof. , the oral care composition according to any one of claims 16 to 22. The oral care composition comprises a dentifrice composition, a toothpaste composition, an emulsion composition, or a combination thereof, and preferably the emulsion composition is an oil-in-water emulsion, a water-in-oil emulsion, or a combination thereof. or more preferably, the oil-in-water emulsion comprises a dense oil-in-water emulsion.

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