Oral compositions comprising a potassium salt for reducing dental nerve and dentin sensitivity

ES 2 248 015 T3

DESCRIPTION

Oral compositions comprising a potassium salt to reduce the sensitivity of the dental nerve and dentin.

Field of the invention

The present invention relates to detergent compositions useful in the fields of sanitary hygiene and cleaning of hard surfaces and fabrics.

Background of the invention

Sodium alkyl sulfate surfactants, for example sodium lauryl sulfate (SLS) are generally substantially incompatible with potassium-containing compounds because an insoluble potassium alkyl sulfate precipitate is formed when sodium alkyl sulfate is combined with a potassium salt. Although the solubility of SLS in water is about 10% on a gram basis, certain experiments indicate that the solubility of potassium lauryl sulfate is less than about 0.02%.

Thus, many aqueous SLS-containing compositions cannot contain a potassium salt which might otherwise be useful as an active ingredient. If the potassium salt and the SLS coexist in a composition, the utility of said potassium salt is not optimized since a portion of the potassium ion of the salt is being occupied in the insoluble potassium lauryl sulfate precipitate. Alternatively, if an ingredient in the composition is a potassium salt, nonionic surfactants can be used in place of SLS to prevent precipitation of potassium lauryl sulfate. However, such nonionic surfactants are, in many cases, not as effective as SLS as wetting or cleaning agents. For example, oral hygiene compositions that contain nonionic surfactants instead of SLS are not as effective in removing dental plaque. It would thus be beneficial in the fields of sanitary hygiene and cleaning of fabrics and surfaces if SLS could be combined with a potassium salt without forming an insoluble precipitate of potassium lauryl sulfate. WO 93/04663 describes dentifrices incorporating alkali metal pyrophosphate and sodium bicarbonate salts in amounts effective to inhibit stone formation on teeth. However, only low proportions of the pyrophosphate salts dissolve in these dentifrices. Document US 5,756,074 describes new compositions comprising an abrasive system comprising an alkali metal bicarbonate and a surfactant system comprising a non-ionic poly (hydroxypropyl ether) surfactant, characterized in that said surfactant system further comprises an alkali metal , alkaline earth metal or ammonium lauryl sulfate, particularly sodium lauryl sulfate or magnesium lauryl sulfate. The precipitated potassium salts form the basis of the abrasive system in these compositions.

Numerous potassium salts are useful in detergent compositions. Potassium pyrophosphate salts, for example, may have activity as builders in detergent compositions comprising a wetting agent such as SLS. However, the builder activity of the potassium pyrophosphate salt in such compositions may not be optimal due to the formation of the potassium lauryl sulfate precipitate described above. For example, US Patent 5,338,538 to Tricca et al. refers to liquid plaque loosening and removing compositions comprising SLS and a builder selected from alkali dimetal pyrophosphate salts, alkali tetrametal pyrophosphate salts, and mixtures thereof. The preferred pyrophosphate salts are disodium pyrophosphate and tetrasodium pyrophosphate. The ability to add potassium pyrophosphate salts to compositions such as those described in US Patent 5,338,538 may be useful. This is because potassium pyrophosphate salts can be more soluble than sodium pyrophosphate salts and therefore a higher pyrophosphate concentration could be achieved in solution. Furthermore, substituting some or all of the sodium pyrophosphate salt for potassium pyrophosphate would reduce the sodium content of the oral composition, which some consumers consider preferable.

On the other hand, many potassium salts possess therapeutic activities that are useful in compositions for sanitary hygiene. For example, various potassium salts are believed to possess activity in reducing dental nerve and / or dentin sensitivity. Such potassium salts could therefore be included in oral compositions designed for the treatment of sensitive teeth and gums. For example, US Patent 4,751,072 to Kim, relates to a procedure for reducing sensory nerve activity in hypersensitive teeth and desensitizing hypersensitive dentin that involves applying a selected potassium salt of potassium bicarbonate and potassium chloride. In addition, US Patent 5,403,577 to Friedman relates to a sustained release oral composition for treating and preventing dental hypersensitivity, comprising an anti-hypersensitivity agent selected from a group of active ingredients including potassium nitrate, bicarbonate potassium and potassium chloride. On the other hand, potassium ions are believed to block nerve conduction in vitro (Peackock, J. and Orchardson, R., 1995, J. Dent. Res. 74 (2): 634-641). However, the SLS present in such a sensitivity composition comprising a potassium salt can lead to the formation of the above insoluble potassium lauryl sulfate precipitate. DE 1,617,939 describes a toothpaste composition for sensitive teeth comprising potassium sulfate, SLS and oleyl methyltaurate, in which the molar reaction of oleyl methyltaurate to SLS is not greater than 1. US 5,849,267 discloses a desensitizing anti-scale dentifrice comprising potassium nitrate, SLS and surfactants which are outside the scope of the present invention. WO 93/25184 describes

ES 2 248 015 T3 as the desensitizing behavior of potassium nitrate can be improved by controlling the level of surfactant used.

Summary of the invention

The present invention provides an oral composition comprising:

a) from about 0.01% by weight to about 20% by weight of an active ingredient which is an orally acceptable soluble potassium salt;

b) from about 0.01% by weight to about 10% by weight of a (C-alkyl₈-C₂₄) sodium sulfate;

c) from about 0.01% by weight to about 20% by weight of an orally acceptable polar surfactant, said surfactant selected from the group consisting of a mono- or diester of fatty acid C₆-C₃₀ of ethoxylated sorbitan, a C fatty acid diester₆-C₃₀ polyethylene glycol, a sodium salt of a (acyl C₆-C₃₀ fatty) sarcosinate, an ester of (acyl C₆-C₃₀ fatty) of sarcosine acid, a sodium salt of (acyl C₆-C₃₀ fatty) taurate, a sodium salt of (acyl C₆ -C₃₀ fatty) methyltaurate, an ester of (acyl C₆-C₃₀ fatty) of taurine, an ester of (acyl C₆-C₃₀ fatty) acid methyltaurine, a (acyl C₆ -C₃₀ fatty) betaine and a chloride of (acyl C₆ -C₃₀ fatty) quaternary ammonium, dimethicone copolyols, phosphate esters of polydimethylsiloxane or copolyols of polydimethylsiloxane, phosphobetaines of polydimethylsiloxane or of copolyols of polydimethylsiloxane, taurates of polydimethylsiloxane or polydimethylsiloxane copolyols of polydimethylsiloxane or polydimethylsiloxylated polydimethylsiloxane copolyols, and polydimethylsiloxane or polydimethylsiloxylated polydimethylsiloxane copolyols polydimethylsiloxane; Y

d) an orally acceptable aqueous vehicle;

wherein the potassium salt is dissolved in the aqueous carrier and wherein the polar surfactant is added to the potassium salt mixture either prior to the addition of or in combination with the (C₈-C₂₄) sodium sulfate in a surfactant molar ratio of (c) to (C-alkyl)₈-C₂₄) sodium sulfate of (b) of greater than or equal to about 1: 1.

The present invention further provides an oral composition as mentioned above, suitable for loosening or removing plaque and / or stains present on dental surfaces, in which the soluble potassium salt of the composition comprises a potassium pyrophosphate salt in an amount effective, optionally in combination with other pyrophosphate salts, to remove or loosen plaque and / or stains when the composition is applied orally to a dental surface.

The present invention further provides an oral composition as mentioned above, suitable for reducing the sensitivity of the dental nerve and / or dentin, wherein the soluble potassium salt of the composition comprises a potassium salt that can reduce the sensitivity of the dental nerve. and / or dentin, in an amount effective to reduce the sensitivity of the dental nerve and / or dentin when the composition is applied orally to a dental surface.

The present invention further provides a process for inhibiting the formation of a potassium lauryl sulfate precipitate in an aqueous composition, comprising a soluble potassium salt and a sodium (C8-C24 alkyl) sulfate, said process comprising including a polar surfactant in said composition in an amount approximately equal to or greater than the amount of sodium (C8-C24 alkyl) sulfate in the composition, said polar surfactant comprising a hydrophobic portion selected from the group consisting of a C alkyl group₆-C₃₀ and a silicone polymer group.

The present invention further provides a method for loosening and / or removing dental plaque and / or stains, while reducing the sensitivity of the dental nerve and / or dentin in an oral cavity of a mammal, comprising administering into the oral cavity of said mammal an effective amount of an oral composition as described herein.

The present invention further provides a method for loosening and / or removing dental plaque and / or stains in an oral cavity of a mammal, comprising administering to the oral cavity of said mammal an effective amount of an oral composition as described in the present report.

Detailed description of the invention

The present invention provides an oral composition comprising a sodium alkyl sulfate and a potassium salt, said compositions further comprising a surfactant in order to inhibit the formation of a potassium lauryl sulfate precipitate.

As used herein, unless otherwise indicated, the term "oral composition" refers to a detergent composition, as defined above (having a detergent property as a primary or secondary function) useful for oral hygiene, which includes compositions for hygiene of the teeth and / or gums. Examples of detergent composition forms of the present invention may include gels, ointments, and liquids (mouthwashes). The term "gel" refers to a visually clear semisolid composition. The gels conform

ES 2 248 015 T3 to this invention can have various viscosities. One of ordinary skill in the art can also formulate the compositions of the present invention in other ways that are known in the art. Examples of such forms include, but are not limited to, creams, tablets, and granules.

Oral compositions of the present invention include, for example, dentifrices. A toothpaste is a composition, in the form such as a paste or gel, that comprises an abrasive, said composition being useful for removing and / or loosening plaque, debris and / or stains from the teeth and gums. Other oral compositions of the invention include mouthwashes, for example, oral rinses to treat oral malodour and rinses having as their primary function detergent properties to remove and / or loosen plaque. "Mouthwashes" are distinguished from toothpastes in that mouthwashes do not include an abrasive.

Unless otherwise indicated, the amounts of the ingredients and the solubilities expressed as percentages throughout the application refer to the amount by weight of said ingredient or solute compared to the total weight of the composition containing the ingredient or solute. For example, a composition comprising from about 0.01% by weight to about 20% by weight of an orally acceptable polar surfactant comprises from about one ten thousand to about two tenths of a gram of polar surfactant per gram of total composition ( i.e., from about one hundredth to about 20 grams of polar surfactant per 100 grams of total composition).

A composition of the present invention comprises a soluble potassium salt as an active ingredient. The term "active ingredient" refers, unless otherwise indicated, to any substance that possesses a therapeutic, hygienic or cosmetic activity in a detergent composition (eg, an oral composition) or possesses an activity that improves the aesthetic or sensory properties of the detergent composition, or possesses an activity that improves the detergent properties of the detergent composition. For example, certain potassium salts, such as potassium sorbate, possess bacteriostatic activity and therefore can be an active ingredient as they are useful in a detergent composition as a preservative. As another example, certain potassium salts, such as potassium pyrophosphate salts, have mineral chelating activity in water and can serve as active ingredients because they behave as builders, enhancing the ability of the sodium alkyl sulfate in the detergent composition to remove and loosen debris, such as plaque and / or stains. Other potassium salts, such as potassium nitrate and potassium chloride, can be an active ingredient because they can reduce the sensitivity of the dental nerve and / or dentin. Other potassium salts, for example, potassium phosphate, can be an active ingredient because it can buffer a detergent composition at a selected pH, for example, at about pH 7. Other potassium salts having particular properties known in the art may be selected as the active ingredient and compositions comprising such potassium salts form part of the present invention.

The term "orally acceptable" as used herein, unless otherwise indicated, refers to application in the oral cavity of a living animal. "Oral application" includes, but is not limited to, brushing the oral cavity and / or teeth in the oral cavity, rinsing the oral cavity, and gargling and spraying the oral cavity.

For the purposes of this application and unless otherwise indicated, a "soluble potassium salt" is any organic or inorganic potassium salt that is soluble in an aqueous solution. Preferably, the soluble potassium salt is any potassium salt that has a solubility greater than or equal to about 5% in water, indicating that a potassium salt composition (composed solely of water and the potassium salt) can contain at least about 0.05 grams of the potassium salt, or more, in solution. Thus, one hundred grams of an aqueous solution comprising a potassium salt having a solubility of at least 5% in water contains at least about 5 grams of the potassium salt and up to about 95 grams of water.

The active ingredient is present in the compositions of the present invention in an "effective amount", which means that the ingredient, that is, the soluble potassium salt, is present in the composition in an amount that is at least sufficient to provide the activity for which the potassium salt has been selected. An effective amount can be determined by one of ordinary skill in the art, for example, by preparing a series of pre-formulations, each comprising a different amount of the potassium salt, testing each of the previous formulations for activity of the potassium salt. potassium salt and determining the minimum amount of potassium salt necessary to provide the desired activity. Generally, the amount of the effective potassium salt for a cloth or hard surface cleaner ranges from about 0.1% to about 50% and for a sanitary hygiene composition ranges from about 0.1% to about twenty%.

Some specific examples of orally acceptable soluble potassium salts that can be used as an active ingredient in an oral composition of the present invention include potassium pyrophosphate salts such as dipotassium pyrophosphate, tetrapotassium pyrophosphate, tripotassium pyrophosphate and monopotassium pyrophosphate. Pyrophosphate salts have activity as builders and thus are useful in reducing or loosening plaque and / or stains present on dental surfaces. A composition of the present invention may comprise a combination of pyrophosphate salts, for example, a combination of potassium pyrophosphate salts, each of which has activity as a builder. The oral compositions of the present invention may further comprise, optionally, potassium pyrophosphate salts in combination with other pyrophosphate salts, such as, for example, pyrophospha4

ES 2 248 015 T3 to disodium or tetrasodium pyrophosphate, to remove or loosen plaque and / or stains when the composition is applied orally to a tooth surface.

Other specific examples of potassium salts that can be used in an oral composition of the present invention are potassium salts that are active in reducing the sensitivity of the dental nerve and / or dentin. Potassium salts possessing activity to reduce dental nerve and / or dentin sensitivity are known in the art, and any such potassium salt is useful in the present invention. Examples of potassium salts that are active in reducing dental nerve and / or dentin sensitivity include, but are not limited to, potassium nitrate, potassium citrate, potassium chloride, potassium oxalate, potassium bicarbonate, potassium phosphate, potassium phosphate. monobasic, dibasic potassium phosphate, tribasic potassium phosphate and potassium pyrophosphate salts. Mixtures of such salts can be used in the present invention. In a preferred embodiment, the potassium salt that can reduce the sensitivity of the dental nerve and / or dentin is potassium nitrate.

A composition of the present invention may comprise a mixture of soluble potassium salts. Each potassium salt in the mixture can have the same or similar activity (for example, each of them can have activity as a builder, improve the removal or detachment of residues and / or stains) or the potassium salts of the mixture they may have different activities (eg, one salt may have activity as a detergency builder and another salt in the mixture may have activity to reduce dental nerve sensation).

The amount of soluble potassium salt preferably ranges from about 0.01% by weight to about 20% by weight of a sanitary hygiene composition of the present invention. If the composition is a dentifrice, a preferred amount of the potassium salt in said dentifrice ranges from about 1% to about 10%. If the composition is a mouthwash, a preferred amount of the potassium salt in said mouthwash ranges from about 0.1% to about 5%.

In specific oral compositions of the present invention for removing and loosening plaque and stains, a potassium pyrophosphate salt is present in the composition in an effective amount, optionally in combination with other pyrophosphate salts as described above, providing at least about 0 , 3%, more particularly from about 0.3% to about 5% by weight of P₂OR₇⁴, based on the weight of the total composition. In order to provide this amount of P₂OR₇^-4, the compositions of this invention for loosening or removing plaque and / or stains from dental surfaces preferably contain from about 0.02% by weight to about 1% by weight of potassium pyrophosphate salt, based on the weight of the total composition .

With reference to the sodium alkylsulfate ingredient of the compositions of the present invention, the expression "(C₈-C₂₄) sodium sulfate ”refers to any (C₈-C₂₄) sodium sulfate or mixture of (alkyl C₈-C₂₄) sodium sulfates. The term "alkyl" as used herein refers to any hydrocarbon, saturated or unsaturated, and straight chain, branched or cyclic. The reference to a (C₈ -C₂₄) Specific sodium sulfate, such as SLS, includes both the (C₈-C₂₄) pure sodium sulfate, as well as the various qualities of (alkyl C₈-C₂₄) sodium sulfate containing relatively small amounts of different sodium (C8-C24 alkyl) sulfates. For example, the term "SLS" includes compositions of pure SLS in addition to the various grades of SLS which may contain other sodium alkyl sulfates which may generally have 10 to 14 carbon atoms in their alkyl portion and which may have in addition one or more unsaturated bonds in its alkyl portions. The (C alkyl₈-C₂₄) Sodium sulfates, such as SLS, are useful as a wetting agent, to loosen and / or remove debris and / or stains in detergent compositions. When sodium (C8-C24 alkyl) sulfate does not interact with a potassium salt ingredient, such as that provided by the present invention, a higher degree of residue and stain removal can be achieved. Examples of sodium (C8-C24 alkyl) sulfates that are useful in the present invention include, but are not limited to, SLS, sodium myristyl sulfate, sodium palmityl sulfate, sodium stearyl sulfate, palmitoleyl sulfate, sodium oleyl sulfate, sodium capryl sulfate, and sodium caprylylsulfate. The above-mentioned sodium (C8-C24 alkyl) sulfates comprise 12, 14, 16, 18, 16 (with an unsaturated carbon-carbon bond), 18 (with an unsaturated carbon-carbon bond), 10 and 8 carbons, respectively. An example of sodium alkyl sulfate having 24 carbon atoms that can be used in the present invention is Nervonyl sodium acid. Preferably, the compositions of the present invention comprise SLS.

Preferably, the amount of sodium (C8-C24 alkyl) sulfate in a composition of the present invention ranges from about 0.01% to about 10% by weight of the composition for a sanitary hygiene composition, from about 0.1 % to about 50% by weight for a hard surface cleaner and from about 0.1% to about 50% for a fabric cleaning composition. The amount of (C alkyl₈-C₂₄) sodium sulfate of a dentifrice of the present invention preferably ranges from about 0.1% to about 5% by weight of the composition. For a mouthwash, the amount of the ingredient (C8-C24 alkyl) sodium sulfate preferably ranges from about 0.02% by weight to about 2% by weight of the composition. More preferably, for a hard surface cleaner, the amount ranges from about 1% to about 50%, and more preferably, for a fabric cleaner, from about 1% to about 50%.

The polar surfactant used in the compositions of the present invention can be any polar surfactant comprising a hydrophobic portion selected from the group consisting of a C alkyl group.₆-C₃₀, being "alkyl"

ES 2 248 015 T3 as defined above, and a silicone polymer group. If the composition is for oral use or for application to the skin and / or hair of a live animal, then the surfactant should not cause harmful side effects to the animal when used as intended. Determination of acceptable surfactants for such uses is known in the art. For the purposes of this invention, a "polar" surfactant is a surfactant that comprises a hydrophilic group and a hydrophobic group. Polar surfactants can be anionic, cationic, nonionic, or amphoteric. One of ordinary skill in the art can determine whether a surfactant is polar.

A "silicone polymer group" is any group that comprises repeating units that comprise a silicon atom. In a preferred embodiment, a silicone polymer group comprises -Si (R¹) (R²) O- repetitive, where R¹ and R² of each unit, independently, equal or different, and each unit may have -SitR¹ ) (R² ) O in the silicone polymer group R groups¹ and / or R² the same or different, each being R¹ and R² a C alkyl₁ -C₆. Preferably, each of R¹ and R² in a silicone polymer group it is methyl or ethyl. More preferably, each R¹ and R² it is a methyl.

Polar surfactants comprising a hydrophobic portion that is a silicone polymer group may include, but are not limited to, dimethicone copolyols (i.e., ethoxylated and / or propoxylated polydimethylsiloxane polymers) and derivatives thereof, wherein the ethoxylated / propoxylated portion of the compounds is derivatized, such as polydimethylsiloxane phosphate esters, polydimethylsiloxane phosphobetaines, polydimethylsiloxane taurates, copolyols of acetylated polydimethylsiloxane and quaternary polydimethylsiloxane compounds. Surfactants comprising a silicone polymer group are also described, inter alia, in Imperante, J. et al., 1994, Cosmetics & Toiletries Vol. 108, no. 4, page 79, and in Imperante, J. et al. , 1994, Cosmetics & Toiletries Vol. 109, No. 3, page 81, which are incorporated herein by reference in their entirety.

Some specific examples of derivatized polydimethylsiloxane copolyols are sodium dimethicone acetylmethyltaurate copolyol, eg, PECOSIL ™ DCT (Phoenix Chemical Inc., Somerville, NJ); dimethicone myristyl ammonium chloride copolyol, eg, PECOSIL ™ SM-40, (Phoenix Chemical Inc. Somerville, NJ); and dimethicone phosphate copolyol, for example, PECOSIL ™ PS-100, PECOSIL ™ PS-150 and PECOSIL ™ PS-200, from Phoenix Chemical Inc., and SILPHOS ™ A100 (Siltech, Norcross, Georgia). As described above, other polydimethylsiloxane copolyols are known in the art and can be used in the present invention.

In another embodiment, the polar surfactant comprises a hydrophobic portion comprising a C6C alkyl group.₃₀. The alkyl group C₆-C₃₀ it can be saturated or unsaturated. Polar surfactants that comprise a hydrophobic portion constituted by a C alkyl group₆-C₃₀ can be determined by one of ordinary skill in the art. Examples of polar surfactants comprising a hydrophobic portion consisting of a C6-C30 alkyl group include, but are not limited to, ethoxylated sorbitan C6-C30 fatty acid mono- and diesters such as PEG-40 diisostearate (eg, EMSORB ™ 2726, PEG-40 Sorbitan Diisotearate (Henkel Corporation (Gulph Mills, PA)), PEG-2 sorbitan isostearate, and PEG-40 sorbitan laurate; C6-C30 fatty acid diesters of polyethylene glycol such as PEG-175 distearate and PEG-150 distearate (for example, LIPOPEG ™ 6000-DS (Lipo Chemicals Inc. (Paterson, NJ)); sodium salts of fatty acyl sarcosinates C₆-C₃₀ such as sodium lauroyl sarcosinate (for example, HAMPOSYL ™ L-30 (Hampshire (Lexington, Massachusetts)) and sodium cocoyl sarcosinate (for example, HAMPOSYL ™ C-30 (Hampshire); C fatty acyl esters₆-C₃₀ of acidic sarcosine such as lauroyl sarcosine (eg, HAMPOSYL ™ L (Hampshire) and oleoyl sarcosine (eg, HAMPOSYL ™ O (Hampshire)); sodium salts of C6-C30 fatty acyl taurates and methyl taurates such as sodium lauroyl taurate, methyl sodium cocoyl taurate (for example, a TAURANOL ™ WS series surfactant (Finetex Inc., Elmwood Park, New Jersey)) and sodium methyl oleoyl taurate (for example, a TAURANOL ™ M series surfactant (Finetex, Inc.) ); C fatty acyl esters₆-C₃₀ acid taurine and methyltaurine; (acyl C₆-C₃₀ fatty) betaines such as cocoamidopropyl betaine (eg, Betaine ZF TEGO ™ and Betaine E TEGO ™ (both from Goldschmidt Chemical Corp., Hopewell, Virginia)); and chlorides of (acyl C₆-C₃₀ fatty) quaternary ammonium such as dimethicone myristyl ammonium chloride copolyol (eg, PECOSIL ™ SM-40, supra). "PEG" in the following examples and throughout this application is an abbreviation for "polyethylene glycol." One of ordinary skill in the art will be able to determine other polar surfactants comprising a C6-C30 alkyl group.

In general, polar surfactants comprising a hydrophobic portion selected from the group consisting of a C₆-C₃₀ and a silicone polymer group can be found in texts known in the art such as The CTFA International Cosmetic Ingredient Dictionary (Cosmetics Tioleteries and Fragrances Association (Washington DC)), which is incorporated herein by reference in its entirety.

On the other hand, the following procedure can be used to select surfactants, such as those taken from The CTFA International Cosmetic Ingredient Dictionary above, for use in inhibiting the formation of a potassium lauryl sulfate salt in accordance with the present invention. The procedure is based on a three component system in water, surfactant, TKPP (tetrapotassium pyrophosphate) and SlS. The surfactant to be tested is weighed into 250 ml beakers in increasing increments of 0.5 g; that is, 0.5 g, 1.0 g, 2.0 g, 2.5 g, and so on. Then 90 ml of a TKPP solution is added and the solution is stirred to dissolve the surfactant. (If the surfactant tested is not soluble on its own in the TKPP solution on visual inspection, i.e. if the solution appears cloudy or a precipitate is observed, then other solvents such as alcohol can be included in each beaker to dissolve the surfactant). 10 ml of a 4.0% solution of SLS are then added with stirring. Since this is a one-tenth dilution, the final concentration of SLS in the beaker is 0.4%. The concentration of surfactant in the beaker is considered equal to the number of grams of surfactant in each beaker, without having

ES 2 248 015 T3 takes into account the concentration of surfactant that was originally added to the beaker. (Each surfactant is frequently tested as a 30% concentrate). The series of solutions is allowed to stand for at least four hours. The solution with a lower surfactant concentration that is clear is designated as the typical effective concentration. The typical effective concentration of neat surfactant can then be calculated by multiplying the typical effective concentration determined experimentally by the actual percentage of surfactant in the originally added surfactant concentrate.

In a specific embodiment, a composition of the present invention is an oral composition for reducing the sensitivity of the dental nerve and / or dentin in the form of a dentifrice, for example, a paste or a gel. Said composition may comprise potassium nitrate in an amount effective to reduce the sensitivity of the dental nerve and / or dentin when the composition is applied orally to a dental surface, preferably further including a soluble fluoride salt or a soluble monofluorophosphate salt in an effective amount to avoid cavities produced by caries.

In another embodiment, a composition of the present invention is an oral composition for removing or loosening plaque and / or stains from tooth surfaces in the form of a mouthwash, such as a pre-brush rinse or in the form of a dentifrice.

A preferred dentifrice of the present invention is in the form of a gel, with a "liquid gel" being especially preferred. A liquid gel refers to a gel, as defined above, of low viscosity, which is suitable for rinsing.

A mouthwash of the present invention is preferably in the form of a liquid gel or a liquid.

A specific dentifrice of the present invention to reduce the sensitivity of the dental nerve and / or dentin comprises:

(a) from about 1% to about 10% potassium nitrate;

(b) from about 0.1% to about 5% SLS;

(c) from about 0.1% to about 20% by weight of an orally acceptable polar surfactant, said surfactant selected from the group consisting of a C fatty acid mono- or diester₆-C₃₀ of ethoxylated sorbitan, a C fatty acid diester₆-C₃₀ polyethylene glycol, a sodium salt of a (acyl C₆-C₃₀ fatty) sarcosinate, an ester of (acyl C₆-C₃₀ fatty) of sarcosine acid, a sodium salt of (acyl C₆-C₃₀ fatty) taurate, a sodium salt of (acyl C₆ -C₃₀ fatty) methyltaurate, an ester of (acyl C₆-C₃₀ fatty) of taurine, an ester of (acyl C₆-C₃₀ fatty) acid methyltaurine, a (acyl C₆ -C₃₀ fatty) betaine and a chloride of (acyl C₆ -C₃₀ fatty) quaternary ammonium, dimethicone copolyols, phosphate esters of polydimethylsiloxane or copolyols of polydimethylsiloxane, phosphobetaines of polydimethylsiloxane or of copolyols of polydimethylsiloxane, taurates of polydimethylsiloxane polydimethylsiloxane or copolymeric polydimethylsiloxane copolyols, and polydimethylsiloxylated polydimethylsiloxane polydimethylsiloxyl compounds, and polydimethylsiloxane polyoxylated polydimethylsiloxane copolyols polydimethylsiloxane;

(d) from about 10% to about 60% by weight of a silica-based abrasive;

(e) an effective amount of a soluble fluoride salt; and (f) an orally acceptable aqueous vehicle;

wherein the potassium salt is dissolved in the aqueous carrier and wherein the polar surfactant is added to the potassium salt mixture either prior to the addition of or in combination with the (C₈-C₂₄) sodium sulfate in a molar ratio of polar surfactant to (C₈-C₂₄) sodium sulfate of greater than or equal to about 1: 1.

Another specific dentifrice of the present invention is in the form of a gel and is especially useful for removing or loosening plaque and / or stains from tooth surfaces. This toothpaste includes:

(a) from about 1% to about 10% of a soluble potassium salt selected from the group consisting of dipotassium pyrophosphate, tetrapotassium pyrophosphate, tripotassium pyrophosphate, monopotassium pyrophosphate, and combinations thereof;

(b) from about 0.1% to about 5% SLS;

(c) from about 0.1% to about 20% by weight of an orally acceptable polar surfactant, said surfactant selected from the group consisting of a C fatty acid mono- or diester₆-C₃₀ of ethoxylated sorbitan, a C fatty acid diester₆-C₃₀ polyethylene glycol, a sodium salt of a (acyl C₆-C₃₀ fatty) sarcosinate, an ester of (acyl C₆-C₃₀ fatty) of sarcosine acid, a sodium salt of (acyl C₆-C₃₀ fatty) taurate, a sodium salt of (acyl C₆ -C₃₀ fatty) methyltaurate, an ester of (acyl C₆-C₃₀ fatty) of taurine, an ester of (acyl C₆-C₃₀ fatty) acid methyltaurine, a (acyl C₆ -C₃₀ fatty) betaine and a chloride of (acyl C₆ -C₃₀ fatty) quaternary ammonium, dimethicone copolyols, phosphate esters of polydimethylsiloxane or of copolyols of polydimethylsiloxane, phosphobetaines of polydimethylsiloxane or of

ES 2 248 015 T3 polydimethylsiloxane copolyols, polydimethylsiloxane taurates or polydimethylsiloxane copolyols, acetylated polydimethylsiloxane copolyols, and quaternary compounds of polydimethylsiloxane or polydimethylsiloxane copolyols;

(d) from about 10% to about 60% by weight of a silica-based abrasive;

(e) an effective amount of a soluble fluoride salt; and (f) an orally acceptable aqueous vehicle;

wherein the potassium salt is dissolved in the aqueous carrier and wherein the polar surfactant is added to the potassium salt mixture either prior to the addition of or in combination with the (C₈-C₂₄) sodium sulfate in a molar ratio of polar surfactant to (C₈-C₂₄) sodium sulfate of greater than or equal to about 1: 1.

A specific mouthwash of the present invention to reduce the sensitivity of the dental nerve and / or dentin comprises:

(a) from about 0.1% to about 5% potassium nitrate;

(b) from about 0.02% to about 2% SLS;

(c) from about 0.1% to about 20% by weight of an orally acceptable polar surfactant, said surfactant selected from the group consisting of a C fatty acid mono- or diester₆-C₃₀ of ethoxylated sorbitan, a C fatty acid diester₆-C₃₀ polyethylene glycol, a sodium salt of a (acyl C₆-C₃₀ fatty) sarcosinate, an ester of (acyl C₆-C₃₀ fatty) of sarcosine acid, a sodium salt of (acyl C₆-C₃₀ fatty) taurate, a sodium salt of (acyl C₆-C₃₀ fatty) methyltaurate, an ester of (acyl C₆-C₃₀ fatty) of taurine, an ester of (acyl C₆-C₃₀ fatty) acid methyltaurine, a (acyl C₆-C₃₀ fatty) betaine and a chloride of (acyl C₆-C₃₀ fatty) quaternary ammonium, dimethicone copolyols, phosphate esters of polydimethylsiloxane or copolyols of polydimethylsiloxane, phosphobetaines of polydimethylsiloxane or of copolyols of polydimethylsiloxane, taurates of polydimethylsiloxane polydimethylsiloxane or copolymeric polydimethylsiloxane copolyols, and polydimethylsiloxylated polydimethylsiloxane polydimethylsiloxyl compounds, and polydimethylsiloxane polyoxylated polydimethylsiloxane copolyols polydimethylsiloxane; and (d) an orally acceptable aqueous vehicle;

wherein the potassium salt is dissolved in the aqueous carrier and wherein the polar surfactant is added to the potassium salt mixture either prior to the addition of or in combination with the sodium (C8-C24 alkyl) sulfate in a molar ratio of polar surfactant to (C alkyl₈-C₂₄) sodium sulfate of greater than or equal to about 1: 1.

Another specific mouthwash of the present invention especially useful for removing or detaching plaque and / or stains from dental surfaces comprises:

(a) from about 0.1% to about 5% of a potassium salt selected from the group consisting of dipotassium pyrophosphate, tetrapotassium pyrophosphate, tripotassium pyrophosphate, monopotassium pyrophosphate, and combinations thereof;

(b) from about 0.02% to about 2% SLS;

(c) from about 0.1% to about 20% by weight of an orally acceptable polar surfactant, said surfactant selected from the group consisting of an ethoxylated sorbitan C6-C30 fatty acid mono- or diester, a fatty acid diester C₆-C₃₀ polyethylene glycol, a sodium salt of a (acyl C₆-C₃₀ fatty) sarcosinate, a (C6-C30 fatty acyl) ester of sarcosine acid, a sodium salt of (C6-C30 fatty acyl) taurate, a sodium salt of (C6-C30 fatty acyl) methyltaurate, a (C6 acyl -C30 fatty) of taurine, a (C6-C30 fatty acyl) ester of acid methyltaurine, a (C-acyl₆-C₃₀ fatty) betaine and a chloride of (acyl C₆-C₃₀ fatty) quaternary ammonium, dimethicone copolyols, phosphate esters of polydimethylsiloxane or copolyols of polydimethylsiloxane, phosphobetaines of polydimethylsiloxane or of copolyols of polydimethylsiloxane, taurates of polydimethylsiloxane polydimethylsiloxane or copolymeric polydimethylsiloxane copolyols, and polydimethylsiloxylated polydimethylsiloxane polydimethylsiloxyl compounds, and polydimethylsiloxane polyoxylated polydimethylsiloxane copolyols polydimethylsiloxane; and (d) an orally acceptable aqueous vehicle;

wherein the potassium salt is dissolved in the aqueous carrier and wherein the polar surfactant is added to the potassium salt mixture either prior to the addition of or in combination with the sodium (C8-C24 alkyl) sulfate in a molar ratio of polar surfactant to (C alkyl₈-C₂₄) sodium sulfate of greater than or equal to about 1: 1.

Flavorings may optionally also be included in the compositions of the present invention. Flavorings can comprise synthetic chemicals, purified chemicals, natural extracts, or combinations thereof. Examples of flavorings that can be used include, but are not limited to, peppermint; spicata mint; wintergreen; clove; cinnamon; anise; sassafras; chewing gum; or aromas

ES 2 248 015 T3 of fruits such as lemon, orange, lime or cherry; or combinations thereof. An "amount of a flavor effective to provide flavor to a composition" for the purposes of this invention refers to any amount at which the flavor of the flavor can be savored by a subject using the oral composition comprising the flavor. One of ordinary skill can determine an amount of a flavoring effective to flavor a composition using known techniques. When determining the effective amount of any flavor, various factors known in the art can be considered, such as the type of flavor. Generally, the amount of flavoring that is effective ranges from about 0.001% to about 0.5% of a liquid composition according to the present invention and from about 0.25% to about 5% of a paste or gel herein. invention. Preferred amounts of a flavoring for a liquid range from about 0.01% to about 0.3% and for a paste or gel from about 0.5% to about 2.5%.

The present invention also provides oral compositions for reducing dental nerve and / or dentin sensitivity, which comprise particular flavorings, namely those that do not comprise a substantial amount of menthol. Such compositions are useful in that they do not aggravate sensitive dentin and / or dental nerves like oral compositions for sensitive teeth and / or gums comprising menthol-containing ingredients. In this aspect of the invention, the ingredient having activity to reduce the sensitivity of the dental nerve and / or dentin can be a potassium salt, for example potassium chloride, potassium nitrate, potassium bicarbonate or other potassium salt indicated above for having activity to reduce the sensitivity of the dental nerve and / or dentin, or may be one or more substances capable of reducing the sensitivity of the dental nerve and / or dentin, such as strontium chloride or other soluble strontium salt, or a soluble tin salt. Other substances that possess activity to reduce dental nerve and / or dentin sensitivity and are known in the art can be used in this aspect of the invention. The composition may comprise a combination of ingredients that reduce the sensitivity of the dental nerve and / or dentin. An "effective amount" of the ingredient that possesses activity to reduce dental nerve sensitivity and / or dentin, eg, potassium chloride, potassium nitrate, and potassium bicarbonate, is any amount that can reduce dental nerve sensitivity and / or dentin. dentin when the composition is applied orally to a tooth surface. Effective amounts of ingredients that reduce dental nerve and / or dentin sensitivity are known in the art and generally range from about 0.1% to about 20% by weight of the composition. A preferred amount of an ingredient that reduces dental nerve and / or dentin sensitivity ranges from about 0.05% to about 10%.

For the purposes of the present invention and unless otherwise indicated, a flavoring that "does not contain a substantial amount of menthol" is any flavoring that does not contain a sufficient amount of menthol to aggravate a sensitive dental nerve or sensitive dentin. when used in an oral composition in an amount effective to flavor the composition. One of ordinary skill in the art can determine a flavor that does not contain a sufficient amount of menthol to aggravate a sensitive dental nerve or sensitive dentin, for example, by oral application to a tooth surface of a composition comprising an amount of an effective flavor. to provide aroma to the composition, and to determine if the composition aggravates the sensitive nerve or dentin of the tooth, thereby determining whether the flavoring contains a sufficient amount of menthol to aggravate a sensitive dental nerve or sensitive dentin. Some flavors are generally known in the art to be non-menthol and such flavors will therefore not have to be tested to determine whether they can be used in the present invention. Other flavorings can be prepared so that they do not contain a substantial amount of menthol.

Processes for making flavors are known in the art and any such process can be used to make a flavoring for the present invention, provided that the flavoring does not contain a substantial amount of menthol. For example, certain mints, i.e. peppermint, are known to naturally comprise menthol, and therefore a peppermint flavoring must be dementorized or synthesized by mixing chemical compounds (excluding a substantial amount of menthol) in order to are useful in practicing this aspect of the present invention.

In one embodiment, the flavoring in the sensitivity compositions of this invention does not contain a peppermint flavoring. Examples of flavorings that are not peppermint flavorings include, but are not limited to, cloves; cinnamon; anise; sassafras; chewing gum; and fruit aromas, such as, but not limited to, lemon, orange, lime, and cherry.

However, in another embodiment, the flavor in the sensitivity compositions of the present invention is a peppermint flavor that does not comprise a substantial amount of menthol. Such flavors are preferred in the sensitivity compositions of the present invention since peppermint flavors are preferred by many consumers to other types of flavors. Some mints, like peppermint spicata, do not naturally contain menthol. However, peppermint, as described above, comprises menthol. Any peppermint-based flavoring, including peppermint used in a flavoring blend (eg, a peppermint plus peppermint blend) should be dementorized or prepared by mixing chemicals prior to use in this aspect of the present invention.

The term "dementorized" means that all or part of the menthol in a natural peppermint extract has been chemically removed. Dementing procedures are known in the art and generally involve cooling the crude oil obtained from the mentha arvensis plant from a temperature of approximately 40 ° C adjusted by

ES 2 248 015 T3 above 0 ° C for a period of about ten to about fourteen days and separate the crystals formed during this period, which essentially comprise menthol, from the residual oil (see, for example, Haarmann & Reimer (Springfield, New Jersey), Optamint-Freshness with taste to match). Any natural peppermint (naturally containing menthol, such as peppermint) used in accordance with the present invention should be sufficiently dementorized so that it does not contain a substantial amount of menthol so as not to unduly aggravate sensitive teeth.

However, preferably, peppermint, including peppermint, used in a composition of the present invention to reduce dental nerve and / or dentin sensitivity is synthesized by mixing chemical components, excluding a substantial amount of menthol, i.e., it is a "synthetic blend".

For the purposes of this invention, the term "synthetic blend" refers to a flavoring prepared by mixing chemicals. The synthetic mixture can comprise synthetic chemicals, purified chemicals, or combinations thereof. A "synthetic chemical compound" for the purposes of this invention and unless otherwise indicated, refers to a chemical compound that is synthesized from non-natural sources. However, synthetic chemical compounds can be chemically the same as those found in natural sources. On the other hand, a synthetic chemical compound can be a molecule that is not found in nature. For the purposes of this invention, unless otherwise indicated, a "purified chemical compound" is a chemical compound that has been substantially purified from a natural source such as a plant. Known methods of organic synthesis and purification can be employed to obtain the synthetic and purified chemical compounds for the synthetic mixtures of the present invention. Mixing synthetic and purified chemicals to obtain flavors that are synthetic mixtures is also known in the art.

A synthetic blend for use in the present invention may have a natural-like flavor, for example, a synthetic blend that has a minty flavor; or it may have a flavor not found in nature, for example a synthetic blend that has a wintergreen flavor or an orange-mint flavor. In general, synthetic blends, including peppermint flavors that are synthetic blends, are more preferable than natural extracts for use as flavors in the sensitivity compositions of the present invention.

As used herein and unless otherwise indicated, the terms "peppermint", "peppermint flavoring" and the like refer to flavorings that have a mint flavor, whether it is a mint flavor. natural or natural-like such as a peppermint flavor or spicata peppermint flavor, or a non-naturally occurring peppermint flavor like wintergreen flavor.

The orally acceptable aqueous vehicle for the detergent compositions of the present invention can be, for example, water or a mixture of water and an orally acceptable alcohol such as ethanol. A mouthwash of the present invention more specifically comprises from about 50% by weight to about 85% by weight of water, based on the total weight of the composition and, optionally, from about 5% to about 25% by weight of ethanol. However, not all compositions of this invention, including mouthwashes, comprise an alcohol and, in some cases, the absence of alcohol in such compositions is preferred to reduce the sensitivity of the dental nerve and / or dentin.

In certain compositions of the invention, especially those containing no alcohol or a low alcohol content, it may be desirable to include preservatives, for example benzoic acid, sodium benzoate, methyl paraben, propyl paraben, sorbic acid, potassium sorbate, or combinations thereof. . Other preservatives known in the art to be useful in detergent compositions can be used in the compositions of the present invention. The amount of preservative generally ranges from about 0% to about 2%, and preferably from about 0.01% to about 1%.

Examples of abrasives useful in dentifrices of the present invention include, but are not limited to, silica-based abrasives such as precipitated silica or silica gels, which preferably have a mean particle size ranging from about 0.1 to about 50 micrometers. Preferred silica-based abrasives include those marketed under the trademarks SYLODENT ™ or SYLOID ™, by WR Grace & Co., and those marketed under the trademark ZEODENT ™ by JM Huber Corp. Other suitable abrasives include, but are not limited to, β-phase calcium pyrophosphate, alumina, and calcium carbonate. Other abrasives can be used in the present invention. The amount of abrasive in a dentifrice composition ranges up to about 60% by weight, preferably from 10% by weight to 40% by weight.

The oral compositions of the present invention can optionally comprise humectants, which can impart a moist mouthfeel and, in some cases, can sweeten the compositions. Useful humectants in the oral compositions of the present invention include, but are not limited to, edible polyhydric alcohols such as glycerin, sorbitol, propylene glycol, xylitol, and cyclodextrins, including derivatives thereof. Other humectants known in the art can be used in the compositions of the present invention. Generally, a humectant is present in an amount of from about 0.1% to about 30% for mouthwashes and from about 10% to about 50% for toothpastes. If a humectant is included in a mouthwash of this invention, it is preferably present in an amount of from about 5% to about 25%.

ES 2 248 015 T3

The oral compositions of the present invention may further comprise an effective amount of a soluble fluoride salt, for example, sodium fluoride, potassium fluoride, or stannous fluoride; or a soluble monofluorophosphate salt such as sodium monofluorophosphate. An effective amount of a soluble fluoride salt or soluble sodium monofluorophosphate salt for a composition of the present invention is an amount that is effective to prevent cavities caused by caries, generally an amount sufficient to provide from about 50 ppm to about 2,500 ppm. ppm of fluoride ion to the composition; it being within the ability of one of ordinary skill in the art to determine such an effective amount. "Preventing cavities caused by cavities" means treating teeth so that they are less prone to cavities caused by cavities.

Optionally, the compositions of this invention may further comprise thickening and / or binding agents. Typical thickening agents include, but are not limited to, xanthan gum, carrageenan, carboxyvinyl polymers, carbomers, cellulose gums such as carboxymethyl cellulose, cellulose derivatives such as hydroxyethyl cellulose, and silicas. Thickeners are normally present in the compositions in an amount of up to about 20%. Xanthan gum is a preferred thickener for a mouthwash. Silica-based thickeners such as SYLOX can be used in toothpastes^TM (WR Grace & Co., Boca Raton, FL).

Examples of sweeteners that can optionally be included in the compositions of the present invention include, but are not limited to, saccharin, lactose, maltose, aspartame, acesulfame potassium (Nutrinova (Somerset, New Jersey, USA), sodium cyclamate, and polydextrose.

Coloring agents, including those acceptable for oral use, known in the art, may also be used in the compositions of the present invention. Generally, a coloring agent is present in a composition of this invention in an amount up to about 0.01%.

The compositions of the present invention may optionally contain other ingredients, for example fragrances, known in the art to be useful in detergent compositions for use in sanitary hygiene.

Stability of detergent compositions of the present invention at low temperatures can be determined by cooling a composition to about 1.66 ° C, storing the composition at that temperature for about seven days, and then evaluating the composition for the presence or absence of precipitate, such as crystals or flocculated material, after heating the cooled composition to a temperature of about room temperature. The stability of the compositions of the invention in time at room temperature can also be evaluated according to the previous criteria, that is, absence of precipitate such as crystals or flocculated material.

The following examples are provided solely to illustrate aspects of the present invention. The examples are not intended, and shall not be construed in this regard, to limit the invention set forth in the claims and described in more detail herein.

Example 1

Eight surfactants were formulated in mouthwashes (Formulations AH) in accordance with the present invention, as indicated in Table 1 below. The amounts of the ingredients in Table 1 are expressed in percent by weight, based on the total weight of the formulation. "TKPP" is tetrapotassium pyrophosphate and "TSPP" is tetrasodium pyrophosphate; thus, each formulation contains 1% by weight of pyrophosphate anion, P₂OR₇⁴, 75% of which is TKPP.

TABLE 1

<td>Ingredient</td><td>TO</td><td>B</td><td>C</td><td>D</td><td>AND</td><td>F</td><td>G</td><td>H</td>

<td>Part A</td><td></td><td></td><td></td><td></td><td></td><td></td><td></td><td></td>

<td>Water</td><td> 60,00</td><td> 60,00</td><td> 60,00</td><td> 60,00</td><td> 60,00</td><td> 60,00</td><td> 60,00</td><td> 60,00</td>

<td>Xanthan gum</td><td> 0,03</td><td> 0,03</td><td> 0,03</td><td> 0,03</td><td> 0,03</td><td> 0,03</td><td> 0,03</td><td> 0,03</td>

<td>TKPP</td><td> 1,42</td><td> 1,42</td><td> 1,42</td><td> 1,42</td><td> 1,42</td><td> 1,42</td><td> 1,42</td><td> 1,42</td>

<td>TSPP</td><td> 0,38</td><td> 0,38</td><td> 0,38</td><td> 0,38</td><td> 0,38</td><td> 0,38</td><td> 0,38</td><td> 0,38</td>

<td>Benzoic acid</td><td> 0,53</td><td> 0,53</td><td> 0,53</td><td> 0,53</td><td> 0,53</td><td> 0,53</td><td> 0,53</td><td> 0,53</td>

<td>Poloxamer 407</td><td> 0,30</td><td> 0,30</td><td> 0,30</td><td> 0,30</td><td> 0,30</td><td> 0,30</td><td> 0,30</td><td> 0,30</td>

<td>Benzoate Na</td><td> 0,37</td><td> 0,37</td><td> 0,37</td><td> 0,37</td><td> 0,37</td><td> 0,37</td><td> 0,37</td><td> 0,37</td>

<td>Saccharin Na</td><td> 0,03</td><td> 0,03</td><td> 0,03</td><td> 0,03</td><td> 0,03</td><td> 0,03</td><td> 0,03</td><td> 0,03</td>

<td>Sorbitol (70%)</td><td> 20,00</td><td> 20,00</td><td> 20,00</td><td> 20,00</td><td> 20,00</td><td> 20,00</td><td> 20,00</td><td> 20,00</td>

ES 2 248 015 T3

TABLE 1 (continued)

<td>Ingredient</td><td>TO</td><td>B</td><td>C</td><td>D</td><td>AND</td><td>F</td><td>G</td><td>H</td>

<td>Part b</td><td></td><td></td><td></td><td></td><td></td><td></td><td></td><td></td>

<td>Water</td><td> 7,0</td><td> 7,0</td><td> 7,0</td><td> 7,0</td><td> 7,0</td><td> 7,0</td><td> 7,0</td><td> 7,0</td>

<td>Alcohol (190 pf)</td><td> 7,0</td><td> 7,0</td><td> 7,0</td><td> 7,0</td><td> 7,0</td><td> 7,0</td><td> 7,0</td><td> 7,0</td>

<td>SLS</td><td> 0,4</td><td> 0,4</td><td> 0,4</td><td> 0,4</td><td> 0,4</td><td> 0,4</td><td> 0,4</td><td> 0,4</td>

<td>Surfactant *</td><td> 1,5</td><td> 1,5</td><td> 1,5</td><td> 1,0</td><td> 1,0</td><td> 1,0</td><td> 0,75</td><td> 0,5</td>

<td>Flavoring</td><td> 0,18</td><td> 0,18</td><td> 0,18</td><td> 0,15</td><td> 0,15</td><td> 0,15</td><td> 0,18</td><td> 0,18</td>

<td>Water</td><td>cs</td><td>cs</td><td>cs</td><td>cs</td><td>cs</td><td>cs</td><td>cs</td><td>cs</td>

<td>Total</td><td> 100</td><td> 100</td><td> 100</td><td> 100</td><td> 100</td><td> 100</td><td> 100</td><td> 100</td>

* The surfactant used in each formulation was:

Formulation A, HAMPOSYL L-30 (Lauroyl sarcosinate sodium);

Formulation B, EMSORB 2726 (PEG-40 sorbitan diisostearate);

Formulation C, Betaine ZF (Cocamidopropyl betaine / cocamidopropyl);

Formulation D, PECOSIL DCT, (sodium dimethicone acetylmethyltaurate copolyol); Formulation E, PECOSIL SM-40 (Dimethicone myristyl ammonium chloride copolyol); Formulation F, PECOSIL PS-100 (Dimethicone phosphate copolyol);

Formulation G, TAURANOL WS (ethanesulfonic acid, 20 (methylamino) -N-cocoacyl); and Formulation H, LIPOPEG 6000DS (PEG-150 distearate).

Formulations AH were generally prepared according to the following procedure:

Part A was prepared first: The xanthan gum was dispersed in 60% by weight of water and mixed for 15 minutes under high shear. Tetrapotassium pyrophosphate, tetrasodium pyrophosphate and benzoic acid were added to the xanthan gum dispersion and the resulting mixture was homogenized for 15 minutes or until dissolved. Poloxamer 407, sodium benzoate, sodium saccharin and sorbitol were added and the resulting mixture was homogenized; the resulting Part A was homogenized for 20 minutes.

Part B was prepared below: Sodium lauryl sulfate was dissolved in alcohol and 7% by weight of water; this mixture was then homogenized for 15 minutes or until the SLS dissolves. The surfactant * was added and the resulting mixture was homogenized for 10 minutes. The flavor was added and the resulting mixture was homogenized for 10 minutes. The remaining water was added and the resulting Part B was homogenized for 10 minutes.

Part B was slowly added to Part A and the mixture was homogenized for 20 minutes.

The pH of each final formulation ranged from about 7.0 to about 8.0.

Formulations AH above were still clear after about a year or more at room temperature.

Example 2

Formulation I below is an example of a mouthwash for reducing dental nerve and / or dentin sensitivity in accordance with the present invention. The pH of Formulation I is in the range of about 5.0 to about 7.0:

ES 2 248 015 T3

Formulation I

Ingredient% w / w

Water 60,010

Xanthan gum 0.035

Potassium nitrate 1,000

HAMPOSYL^TM L-30 (30.0%) 2,000

Sodium saccharin 0.030

Sorbitol (70%) 20,000

Aloe powder 0.250

Sodium salicylate 2,000

Disodium phosphate 0.025

Monosodium phosphate 0.100

Alcohol (190 mp) 7,000

Water 7,000

SLS 0.400

Flavoring 0.150

100,000%

Formulation I was prepared as follows: Xanthan gum was dispersed in 60.010% by weight of water and mixed for 15 minutes under high shear. KNO was added₃ and mixed until dissolved. Hamposyl L-30, sodium saccharin, sorbitol, aloe powder and sodium salicylate were added, the resulting mixture was homogenized for 20 minutes. Disodium phosphate and monosodium phosphate were added; the resulting mixture was homogenized for 10 minutes. In a separate container, the alcohol, 7.0% by weight water, SLS, and flavor were combined until the SLS dissolved. The alcohol / water / SLS / flavor mixture was added to the batch and mixed for 15 minutes.

Example 3

The following Formulation J is an example of a dentifrice according to the present invention in the form of a liquid gel, to reduce the sensitivity of the dental nerve and / or dentin.

Formulation J

Ingredient% w / w

Hydroxyethyl cellulose 1,000

PEG-8 3,000

Glycerin (99.5%) 10,000

Purified water 18,000

Potassium nitrate 5,000

Sodium fluoride 0.243

HAMPOSYL^TM L-30 (30%) 4,000

Xanthan gum 0.300

Sorbitol (70%) 35,451

Sodium saccharin 0.500

SYLODENT ™ 15 (Thickening Silica from WR Grace &amp; Co.) 8,000

SYLODENT ™ 750 (abrasive silica from WR Grace &amp; Co.) 10,000

Colorant (s) 0.006

SLS (30% solution) 3,000

Flavoring 1,500

100,000%

Formulation J was prepared as follows: Carboxyethylcellulose was dispersed in the PEG-8 and glycerin using a mixer. In a separate container, the KNO was dissolved₃ in the water and sorbitol and mixed until dissolved. NaF was added to the water mixture and mixing was continued for 25 minutes. The water / sorbitol / KNO phase₃/ NaF was added to the carboxyethylcellulose / PEG-8 / glycerin mixture and homogenized for 10 minutes. The xanthan gum was added slowly and mixed under high shear for 15 minutes. Hamposyl L-30, sodium saccharin, Sylodent 15, Sylodent 750, the dyes (FD&amp;C Blue No. 1 and D&amp;C Yellow No. 10) were added; the resulting mixture

ES 2 248 015 T3 was stirred until homogeneous. The aroma was dissolved in the SLS and mixed for 5 minutes. The aroma / SLS mixture was added to the batch and mixed for 10 minutes. The resulting gel was deaerated to remove trapped air bubbles.