WO2020219062A1 - Methods and compositions to reduce staining for antibacterial oral care compositions - Google Patents
Methods and compositions to reduce staining for antibacterial oral care compositions Download PDFInfo
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- WO2020219062A1 WO2020219062A1 PCT/US2019/029256 US2019029256W WO2020219062A1 WO 2020219062 A1 WO2020219062 A1 WO 2020219062A1 US 2019029256 W US2019029256 W US 2019029256W WO 2020219062 A1 WO2020219062 A1 WO 2020219062A1
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- oral care
- care composition
- weight
- metal chelator
- acid
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/43—Guanidines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/55—Phosphorus compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
Definitions
- Oral care composition commonly include a variety of antibacterial and/or antimicrobial agents to promote oral hygiene and health.
- Chlorhexidine (CHX) is often the antimicrobial agent of choice as it combines superior anti-plaque and anti-gingivitis properties with an excellent safely profile.
- CHX is also known to lead to the staining or discoloration of dental surfaces.
- the oral care composition may include about 5 weight % or less metal chelator, based on a total weight of the oral care composition.
- the oral care composition may include about 1 weight % or less metal chelator, based on a total weight of the oral care composition.
- the oral care composition may include about 0.5 weight % or less metal chelator, based on a total weight of the oral care composition.
- the oral care composition may include about 0.01 weight % to about 0.5 weight % chlorhexidine, based on a total weight of the oral care composition.
- the metal chelator may include glutamic acid.
- the metal chelator may include aspartic acid.
- the metal chelator may include at least one of glutamic acid, aspartic acid,
- ATMP aminotris(methylenephosphonic acid)
- polyaspartic acid polyaspartic acid
- imminodisuccinic acid imminodisuccinic acid
- the metal chelator may be an iron chelator and may have a higher iron affinity than chlorhexidine.
- the metal chelator may have a Fe 3+ binding constant of 10 or more.
- the oral care composition may be applied to a tooth surface, and an amount of staining of the tooth surface by the oral care composition may be less than an amount of staining by a similar oral care composition without the effective amount of a metal chelator.
- the oral care composition may be applied at least daily, and the amount of staining may be less after at least one of 1 day, 2 days, 1 week, 2 weeks, 3 weeks, 4 weeks, 1 month, and 2 months of application, when compared to a similar oral care composition without the effective amount of the metal chelator.
- the one or more metal chelators may include at least one of glutamic acid, aspartic acid, aminotris(methylenephosphonic acid) (ATMP), polyaspartic acid, and imminodisuccinic acid.
- At least one of the one or more metal chelators may have a Fe 3+ binding constant of 10 or more, 11, or more, or 12 or more.
- the oral care composition may include about 5 weight % or less of the one or more metal chelators, based on a total weight of the oral care composition.
- an oral care composition including from about 0.01 weight % to about 0.20 weight % chlorhexidine, based on a total weight of the oral care composition; and an effective amount of metal chelator.
- the metal chelator may be an iron chelator with a higher iron affinity than chlorhexidine and the metal chelator may have a Fe 3+ binding constant of about 10 or more, 11 or more, or 12 or more.
- the metal chelator may include at least one of glutamic acid, aspartic acid,
- ATMP aminotris(methylenephosphonic acid)
- polyaspartic acid polyaspartic acid
- imminodisuccinic acid imminodisuccinic acid
- the oral care composition may further include one or more additional oral care ingredients selected from: a carrier, a humectant, surfactants, polymers, thickeners, antioxidants, preservatives, flavoring agents, sweeteners, colorants, pH modifiers, anti-calculus agents, fluoride sources, and wherein all the ingredients of the oral care composition may be orally acceptable.
- additional oral care ingredients selected from: a carrier, a humectant, surfactants, polymers, thickeners, antioxidants, preservatives, flavoring agents, sweeteners, colorants, pH modifiers, anti-calculus agents, fluoride sources, and wherein all the ingredients of the oral care composition may be orally acceptable.
- the term“of” is an inclusive operator, and is equivalent to the term “and/or,” unless the context clearly dictates otherwise.
- the term“based on” is not exclusive and allows for being based on additional factors not described, unless the context clearly dictates otherwise.
- the recitation of“at least one of A, B, and C,” includes implementations containing A, B, or C, multiple examples of A, B, or C, or combinations of A/B, A/C, B/C, A/B/B/ B/B/C, A/B/C, etc.
- the meaning of“a, ”“ an,” and“the” include plural references.
- the meaning of“in” includes“in” and“on.”
- first, second, etc. may be used herein to describe various elements, these elements should not be limited by these terms. These terms are only used to distinguish one element from another.
- a first object, component, or step could be termed a second object, component, or step, and, similarly, a second object, component, or step could be termed a first object, component, or step, without departing from the scope of the invention.
- the first object, component, or step, and the second object, component, or step are both, objects, component, or steps, respectively, but they are not to be considered the same object, component, or step.
- the term“if’ may be construed to mean“when” or“upon” or“in response to determining” or“in response to detecting,” depending on the context.
- any numerical range of values herein are understood to include each and every number and/or fraction between the stated range minimum and maximum, as well as the endpoints.
- a range of 0.5% to 6% would expressly include all intennediate values of, for example, 0.6%, 0.7%, and 0.9%, all the way up to and including 5.95%, 5.97%, and 5.99%, among many others.
- CHX has a strong ability to bind to teeth and gum surfaces, which enhances its effectiveness as an antimicrobial.
- CHX also has an affinity to complex with metals, such as iron.
- staining may be, at least partially, caused by the complexing of CHX with metals as it binds to teeth surfaces.
- the source of metal can be from diet or from blood, especially for sufferers of gingivitis who are prone to bleeding from the gums.
- the inventors have surprisingly discovered a method of reducing the staining associated with oral care compositions including chlorhexidine, including providing an effective amount of a metal chelator with the oral care composition.
- the oral care composition includes an effective amount of a metal chelator.
- the term“effective amount” refers to an amount of a compound or composition sufficient to significantly induce a positive benefit, preferably an oral health benefit, but low enough to avoid serious side effects, i.e., to provide a reasonable benefit to risk ratio, within the sound judgment of a person having ordinary skill in the art.
- the oral care composition may include an amount of metal chelator effective to reduce an amount of staining caused by the use of CHX.
- the oral care composition may include an amount of metal chelator effective to reduce an amount of staining caused by the use of CHX as compared to an oral care composition not including the effective amount of metal chelator.
- an amount of staining of the tooth surface by the oral care composition including the effective amount of metal chelator is less than an amount of staining by a similar oral care composition without the effective amount of a metal chelator.
- the oral care composition may be applied at least daily for 2 weeks. In other implementations, the oral care composition is applied at least daily for 2 days, 3 days, 4, days, 1 week, 2 weeks, 3 weeks, 4 weeks, 1 month, or 2 months.
- the metal chelator is an iron chelator.
- the metal chelator has a higher metal affinity than CHX.
- the iron chelator may have a higher iron binding constant than CHX in order to prevent metal ions from binding with the CHX.
- Fe 3+ may be the main form of free iron (Fe) present in the mouth.
- the metal chelator has a higher Fe 3+ binding constant than CHX.
- the metal chelator has a higher affinity for Fe 3+ than CHX.
- Table 1 is an exemplary listing of metal chelators according to implementations of the present disclosure.
- the iron chelators illustrated in Table 1 have a higher affinity for iron than CHX, as evidenced by their high Fe 3+ bonding constants (logK).
- ATMP is aminotris(methylenephosphonic acid).
- Example 1 illustrates the ability of exemplary metal chelators to reduce CHX- based staining.
- the metal chelators of Table 1 were tested in a bovine enamel model to evaluate their ability to reduce CHX-based staining.
- a bovine enamel model was used to mimic CHX staining.
- the bovine teeth samples were kept hydrated until use.
- Baseline (L*, a*, and b*) measurements were taken of the samples before treatment using a spectroshade.
- the samples were then placed in a solution representing each of the treatments of Table 2 and then in artificial saliva. This cycle of soaking in the treatment and in artificial saliva was then repeated 14 times for each sample, with spectroshade measurements taken every two cycles immediately after soaking in the artificial saliva step (the samples were dabbed dry before measurements). Control samples soaked in FeC13 alone and FeC13 + CHX solutions were also done.
- Table 2 illustrates the AW* for two representative metal chelators of Table 1. The more positive the value of AW*, the darker the tooth color is.
- Aminotris(methylenephosphonic acid) (ATMP) and Imminodi succinic acid (IDA) decreased the amount of teeth staining caused by CHX when exposed to an iron solution.
- ATMP performed better at every cycle compared to IDA. While not bound in theory, the inventors believe this may be due to the chemical structure of ATMP having phosphonate compared to the carboxylic acids present in the other metal chelators.
- an oral care composition may include chlorhexidine and an effective amount of a metal chelator.
- the oral care composition may include from about 0.01 weight % to about 0.50 weight % chlorhexidine, based on the total weight of the oral care composition.
- the oral care composition may include from about 0.01 weight % to about 0.2 weight % chlorhexidine.
- the oral care composition may include 0.5 weight % or less, 0.4 weight % or less, 0.3 weight % or less, 0.2 weight % or less, or 0.1 weight % or less, chlorhexidine.
- the metal chelator may include one or more metal chelators.
- the metal chelator may include at least one of glutamic acid, aspartic acid, aminotris(methylenephosphonic acid) (ATMP), polyaspartic acid, and imminodisuccinic acid.
- the metal chelator includes glutamic acid.
- the metal chelator includes aspartic acid.
- the metal chelator may include polyphosphates, such as sodium tripolyphosphate (STPP) and tetrasodium pyrophosphate.
- STPP sodium tripolyphosphate
- tetrasodium pyrophosphate tetrasodium pyrophosphate
- the oral care composition may include 5.0 weight % or less metal chelator, based on the total weight of the oral care composition.
- the oral care composition may include from about 0.10 weight % to about 5.0 weight % metal chelator, from about 0.50 weight % to about 5.0 weight % metal chelator, from about 1.0 weight % to about 5.0 weight % metal chelator, from about 1.50 weight % to about 5.0 weight % metal chelator, from about 2.0 weight % to about 5.0 weight % metal chelator, from about 2.50 weight % to about 5.0 weight % metal chelator, and/or from about 3.0 weight % to about 5.0 weight % metal chelator.
- the oral care composition may include 4.50 weight % or less, 4.0 weight % or less, 3.50 weight % or less, or 3.0 weight % or less, metal chelator.
- the metal chelator may have a higher metal affinity than CHX.
- the metal chelator may have a higher iron affinity than CHX.
- the metal chelator may be an iron chelator and may have a Fe 3+ binding constant (logK) of 10 or more.
- the iron chelator may have a Fe 3+ binding constant (logK) of 11 or more, 12 or more, 13 or more, 14 or more, 15 or more 16 or more, 17 or more, and/or 18 or more.
- at least one metal chelator may have a high Fe 3+ binding constant.
- a Fe 3+ binding constant (logK) of 10 or more, 11 or more, or 12 or more.
- the oral care composition may be substantially liquid in character, such as a mouthwash or rinse, and may include additional ingredients common to liquid oral care compositions, such as carriers, humectants, surfactants, polymers, thickeners, antioxidants, preservatives, flavoring agents, sweeteners, colorants, pH modifiers, anti-calculus agents, and fluoride sources.
- additional ingredients common to liquid oral care compositions such as carriers, humectants, surfactants, polymers, thickeners, antioxidants, preservatives, flavoring agents, sweeteners, colorants, pH modifiers, anti-calculus agents, and fluoride sources.
- All ingredients used in the oral care compositions described herein may be orally acceptable.
- “Orally acceptable” means an ingredient which is present in the composition as described in an amount and form which does not render the composition unsafe, unpalatable, or otherwise unsuitable for use in the oral cavity.
- the additional ingredients should not substantially inhibit the efficacy of the antibacterial agent (chlorhexidine) or metal chelators described herein.
- the oral care composition includes an orally acceptable carrier.
- an “orally acceptable carrier” refers to a material or combination of materials that are safe for use in the oral care compositions of the present disclosure while retaining significant efficacy for the antibacterial agent(s).
- the carrier is specifically selected to ensure that there is no substantially reduction in efficacy for the antibacterial agent(s).
- the oral care composition may be aqueous or non-aqueous, or may include a mixture of liquids as the carrier.
- the carrier may be water, and the water may be deionized and free of organic impurities.
- Water may make up the balance of the oral care composition and may include from about 10 weight % to about 90 weight %, e.g., from about 40 weight % to about 70 weight % water, based on the total weight of the oral care composition. This amount of water may include free water which is added plus that amount which is introduced with other materials, such as with sorbitol or any other components of the oral care composition.
- the carrier may be a water-alcohol mixture.
- the ratio of water to alcohol may be in the range of from about 1:1 to about 20:1, preferably from 3:1 to 20:1, and most preferably about 17:3, by weight.
- the total amount of water alcohol mixture may be from about 70 weight % to about 99.9 weight %, based on the total weight of the oral care
- the pH of the oral care composition may be from about 4.5 to about 9, and typically, from about 5.5 to 8.
- the pH of the oral care composition is preferably in the range of from about 6 to about 8.0.
- the oral care composition may include one or more humectants.
- Humectants may reduce evaporation and lower water activity. Certain humectants may impart desirable sweetness or flavor to the compositions.
- the humectant may be a mixture of humectants, such as glycerin and sorbitol, and a polyhydric alcohol, such as propylene glycol, butylene glycol, hexylene glycol, polyethylene glycol.
- the oral care composition may include from 15 weight % to 70 weight % or from 30 weight % to 65 weight % humectant, based on a total weight of the oral care composition.
- the oral care composition may include one or more surfactants.
- the surfactants may enhance a stability of the oral care composition, help clean the oral cavity surfaces through detergency, and provide foam upon agitation.
- suitable surfactants may function as a surface active agent, emulsifier, and/or foam modulator. Any orally acceptable surfactant, most of which are anionic, nonionic, cationic, or amphoteric, may be used. A combination of surfactants may also be used.
- the surfactants may include anionic surfactants.
- water-soluble salts of higher fatty acid monoglyceride monosulfates such as the sodium salt of the monosulfated monoglyceride of hydrogenated coconut oil fatty acids, such as sodium N-methyl N-cocoyl taurate, sodium cocomo-glyceride sulfate; higher alkyl sulfates, such as sodium lauryl sulfate; higher alkyl-ether sulfates, such as sodium laureth-2 sulfate; higher alkyl aryl sulfonates, such as sodium dodecyl benzene sulfonate (sodium lauryl benzene sulfonate); higher alkyl sulfoacetates, such as sodium lauryl sulfoacetate (dodecyl sodium sulfoacetate), higher fatty acid esters of 1,2 dihydroxy propane sulfonate,
- the anionic surfactant may be selected from sodium lauryl sulfate and sodium ether lauryl sulfate.
- the anionic surfactant may be present in an amount which is effective, e.g., >0.001% by weight of the formulation, but not at a concentration which would be irritating to the oral tissue, e.g., 1%, and optimal concentrations depend on the particular formulation and the particular surfactant.
- the anionic surfactant may be present at from about 0.03 weight % to about 0.5 weight % based on the total weight of the oral care composition.
- the surfactants may include cationic surfactants, such as derivatives of aliphatic quaternary ammonium compounds having one long alkyl chain containing 8 to 18 carbon atoms, such as lauryl trimethylammonium chloride, cetyl pyridinium chloride, cetyl
- trimethylammonium bromide di-isobutylphenoxyethyldimethylbenzylammonium chloride, coconut alkyltrimethylammonium nitrite, cetyl pyridinium fluoride, and mixtures thereof.
- the surfactants may include nonionic surfactants, such as compounds produced by the condensation of alkylene oxide groups (hydrophilic in nature) with an organic hydrophobic compound which may be aliphatic or alkylaromatic in nature.
- nonionic surfactants include, but are not limited to, the Pluronics, polyethylene oxide condensates of alkyl phenols, products derived from the condensation of ethylene oxide with the reaction product of propylene oxide and ethylene diamine, ethylene oxide condensates of aliphatic alcohols, long chain tertiary amine oxides, long chain tertiary phosphine oxides, long chain dialkyl sulfoxides and mixtures of such materials.
- the oral care composition may include a nonionic surfactant selected from polaxamers (e.g., polaxamer 407), polysorbates (e.g., polysorbate 20), polyoxyl hydrogenated castor oils (e.g., polyoxyl 40 hydrogenated castor oil), and mixtures thereof.
- a nonionic surfactant selected from polaxamers (e.g., polaxamer 407), polysorbates (e.g., polysorbate 20), polyoxyl hydrogenated castor oils (e.g., polyoxyl 40 hydrogenated castor oil), and mixtures thereof.
- the surfactants may include zwitterionic surfactants, such as derivatives of aliphatic quaternary ammonium, phosphomium, and sulfonium compounds, in which the aliphatic radicals can be straight chain or branched, and wherein one of the aliphatic substituents contains 8 to 18 carbon atoms and one contains an anionic water-solubilizing group, e.g., carboxy, sulfonate, sulfate, phosphate or phosphonate.
- zwitterionic surfactants such as derivatives of aliphatic quaternary ammonium, phosphomium, and sulfonium compounds, in which the aliphatic radicals can be straight chain or branched, and wherein one of the aliphatic substituents contains 8 to 18 carbon atoms and one contains an anionic water-solubilizing group, e.g., carboxy, sulfonate, sulfate, phosphate or phosphonate
- Illustrative examples of the surfactants suited for inclusion into the oral care composition include, but are not limited to, sodium alkyl sulfate, sodium lauroyl sarcosinate,
- cocoamidopropyl betaine and polysorbate 20 and combinations thereof.
- the oral care composition includes from about 0.1% to about 5.0% surfactant based on a total weight of the oral care composition.
- the oral care composition includes from about 0.3 weight % to about 3.0 weight % surfactant or from about 0.5 weight % to about 2.0 weight % surfactant.
- the oral care compositions may include one or more polymers or polymeric agents, such as polyethylene glycols, polyvinylmethyl ether maleic acid copolymers, polysaccharides (e.g., cellulose derivatives, for example caiboxymethyl cellulose, or polysaccharide gums, for example xanthan gum or carrageenan gum).
- polysaccharides e.g., cellulose derivatives, for example caiboxymethyl cellulose, or polysaccharide gums, for example xanthan gum or carrageenan gum.
- Acidic polymers for example polyacrylate gels, may be provided in the form of their free acids or partially or fully neutralized water soluble alkali metal (e.g., potassium and sodium) or ammonium salts.
- the oral care composition may include synthetic anionic polymeric polycarboxylates, such as 1:4 to 4:1 copolymers of maleic anhydride or acid with another polymerizable ethylenically unsaturated monomer, preferably methyl vinyl ether/maleic anhydride having a molecular weight (M.W.) of 30,000 to 3,000,000, most preferably 30,000 to 800,000.
- synthetic anionic polymeric polycarboxylates such as 1:4 to 4:1 copolymers of maleic anhydride or acid with another polymerizable ethylenically unsaturated monomer, preferably methyl vinyl ether/maleic anhydride having a molecular weight (M.W.) of 30,000 to 3,000,000, most preferably 30,000 to 800,000.
- Gantrez e.g., AN 139 (M.W. 500,000), AN 119 (M.W. 250,000) and S-97 Pharmaceutical Grade (M.W.
- Other usable polymers include those such as the 1 : 1 copolymers of maleic anhydride with ethyl acrylate, hydroxyethyl methacrylate, N-vinyl-2-pyrollidone, or ethylene, the latter being available for example as Monsanto EMA No. 1103, M.W. 10,000 and EMA Grade 61, and 1 : 1 copolymers of acrylic acid with methyl or hydroxyethyl methacrylate, methyl or ethyl acrylate, isobutyl vinyl ether or N-vinyl-2-pyrrolidone.
- olefinic monomers are aciylic, methacrylic, ethacrylic, alpha-chloroacrylic, crotonic, beta-acryloxy propionic, sorbic, alpha-chlorsorbic, cinnamic, beta-styrylacrylic, muconic, itaconic, citraconic, mesaconic, glutaconic, aconitic, alpha-phenylacrylic, 2-benzyl acrylic, 2-cyclohexylaciylic, angelic, umbellic, fumaric, maleic acids and anhydrides.
- Other different olefinic monomers are aciylic, methacrylic, ethacrylic, alpha-chloroacrylic, crotonic, beta-acryloxy propionic, sorbic, alpha-chlorsorbic, cinnamic, beta-styrylacrylic, muconic, itaconic, citraconic, mesaconic, glutaconic, acon
- copolymerizable with such carboxylic monomers include vinylacetate, vinyl chloride, dimethyl maleate and the like. Copolymers contain sufficient carboxylic salt groups for water-solubility.
- a further class of usable polymeric agents includes a composition containing
- homopolymers of substituted acrylamides and/or homopolymers of unsaturated sulfonic acids and salts thereof in particular where polymers are based on unsaturated sulfonic acids selected from acrylamidoalykane sulfonic acids such as 2-acrylamide 2 methylpropane sulfonic acid having a molecular weight of 1,000 to 2,000,000.
- unsaturated sulfonic acids selected from acrylamidoalykane sulfonic acids such as 2-acrylamide 2 methylpropane sulfonic acid having a molecular weight of 1,000 to 2,000,000.
- Another useful class of polymeric agents includes polyamino acids, particularly those containing proportions of anionic surface-active amino acids such as aspartic acid, glutamic acid and phosphoserine.
- the oral care composition may include thickening agents or thickeners.
- Orally acceptable thickening agents may be used to provide a desirable consistency or to stabilize or enhance the performance of the oral care composition.
- the thickening agent may include carboxyvinyl polymers, carrageenan, hydroxyethyl cellulose and water soluble salts of cellulose ethers such as sodium carboxymethyl cellulose and sodium carboxymethyl hydroxyethyl cellulose.
- Natural gums, such as karaya, gum arabic, and gum tragacanth can also be used.
- Colloidal magnesium aluminum silicate or finely divided silica can be used as component of the thickening composition to further improve the composition's texture.
- the oral care composition may include from about 0.5 weight % to about 5 weight %, based on the total weight of the oral care composition.
- the oral care composition may include one or more additional antibacterial agents or preservatives.
- the preservatives improve an antimicrobial characteristic of the oral care composition to improve storage life or prevent decay.
- the one or more additional antibacterial agents or preservatives are non-metal.
- the one or more antibacterial agents or preservatives include at least one of sodium benzoate, methyl paraben, ethyl paraben, triclosan, stannum salts, and combinations thereof.
- the oral care composition may include an effective amount of antibacterial agents or preservatives.
- the oral care composition may include an amount of antibacterial agents or preservatives effective to reduce spoilage of the oral care composition during storage or use.
- the oral care composition may include one or more flavoring agents.
- Useful flavoring agents include any material or mixture of materials operable to enhance the taste of the oral care composition. Any orally acceptable natural or synthetic flavoring agent may be used, such as flavoring oils, flavoring aldehydes, esters, alcohols, similar materials, and combinations thereof.
- Flavoring agents include vanillin, sage, maijoram, parsley oil, spearmint oil, cinnamon oil, oil of wintergreen (methyl salicylate), peppermint oil, clove oil, bay oil, anise oil, eucalyptus oil, citrus oils, fruit oils and essences including those derived from lemon, orange, lime, grapefruit, apricot, banana, grape, apple, strawberry, cherry, pineapple, etc., bean- and nut-derived flavors such as coffee, cocoa, cola, peanut, almond, etc., adsorbed and encapsulated flavorants, and mixtures thereof. Also encompassed within flavoring agents herein are ingredients that provide fragrance and/or other sensory effect in the mouth, including cooling or warming effects.
- Such ingredients include menthol, menthyl acetate, menthyl lactate, camphor, eucalyptus oil, eucalyptol, anethole, eugenol, cassia, oxanone, x-irisone, propenyl guaiethol, thymol, linalool, benzaldehyde, cinnamaldehyde, N-ethyl-p-menthan-3-carboxamine, N,2,3-trimethyl-2-isopropylbutanamide, 3- l-menthoxypropane-l,2-diol, cinnamaldehyde glycerol acetal (CGA), methone glycerol acetal (MGA) and mixtures thereof.
- the oral care composition includes from about 0.01% to about 1% flavoring agents based on a total weight of the oral care composition.
- the oral care composition may also include one or more sweeteners.
- Sweeteners among those useful herein include orally acceptable natural or artificial, nutritive or non-nutritive sweeteners. Such sweeteners include dextrose, polydextrose, sucrose, maltose, dextrin, dried invert sugar, mannose, xylose, ribose, fructose, levulose, galactose, com syrup (including high fructose com syrup and com syrup solids), partially hydrolyzed starch, hydrogenated starch hydrolysate, sorbitol, mannitol, xylitol, maltitol, isomalt, aspartame, neotame, saccharin and salts thereof, sucralose, dipeptide-based intense sweeteners, cyclamates, dihydrochalcones and mixtures thereof. Some implementations may include one or more sweeteners. In some implementations, the oral care composition includes from about 0.005%
- the oral care composition may include colorants.
- Colorants such as dyes or pigments, may be food color additives presently certified under the Food Drug & Cosmetic Act for use in food and ingested drugs, including dyes such as FD&C Red No. 3 (sodium salt of
- the oral care composition may also include one or more pH modifying agents.
- the pH modifying agents among those useful herein include acidifying agents to lower pH, basifying agents to raise pH and buffering agents to control pH within a desired range.
- any orally acceptable pH modifying agent may be used, including without limitation carboxylic, phosphoric and sulfonic acids, acid salts (e.g., monosodium citrate, disodium citrate, monosodium malate, etc.), alkali metal hydroxides such as sodium hydroxide, carbonates such as sodium carbonate, bicarbonates, sesquicarbonates, borates, silicates, phosphates (e.g., monosodium phosphate, tri sodium phosphate, pyrophosphate salts, etc.), imidazole and mixtures thereof.
- One or more pH modifying agents are optionally present in a total amount effective to maintain the composition in an orally acceptable pH range.
- the oral care composition includes from about 0.01% to about 10% pH modifier agents based on a total weight of the oral care composition.
- the oral care composition may include one or more anti-calculus or calcium chelating agents able to complex calcium found in the cell walls of the bacteria. Binding of this calcium weakens the bacterial cell wall and augments bacterial lysis.
- Another group of agents suitable for use as calcium chelating or anti-calculus agents are soluble pyrophosphates salts.
- the pyrophosphate salts may be any of the alkali metal pyrophosphate salts, such as tetra alkali metal pyrophosphate, dialkali metal diacid pyrophosphate, trialkali metal monoacid pyrophosphate, and mixtures thereof, wherein the alkali metals are sodium or potassium.
- the pyrophosphate salts may be useful in both their hydrated and unhydrated forms.
- the oral care composition may include an effective amount of pyrophosphate salts.
- the oral care composition may include one or more fluoride ion sources, e.g., soluble fluoride salts.
- fluoride ion-yielding materials may be employed as sources of soluble fluoride.
- suitable fluoride ion-yielding materials include, but are not limited sodium fluoride, potassium fluoride, sodium monofluorophosphate, sodium fluorosilicate, ammonium fluorosilicate, amine fluoride, ammonium fluoride, and combinations thereof.
- the fluoride ion source may include stannous fluoride, sodium fluoride, sodium
- the fluoride salts are preferably salts wherein the fluoride is covalently bound to another atom, e.g., as in sodium monofluorophosphate, rather than merely ionically bound, e.g., as in sodium fluoride.
- the oral care composition may include an amount of fluoride ion sources sufficient to release up to about 0.13 weight %, preferably from about 0.0013 weight % to about 0.1 weight %, and most preferably about 0.0013 weight % to about 0.05 weight % fluoride ions, based on the total weight of the oral care composition.
- Table 3 illustrates a mouthwash according to some implementations of the present disclosure.
- the exemplary composition described in Table 3 may be prepared according to conventional methods known to those skilled in the art.
- the exemplary composition described in Table 3 may be prepared according to conventional methods known to those skilled in the art.
- the exemplary composition described in Table 3 may be prepared according to conventional methods known to those skilled in the art.
- the exemplary composition described in Table 3 may be prepared according to conventional methods known to those skilled in the art.
- the exemplary composition described in Table 3 may be prepared according to conventional methods known to those skilled in the art.
- the exemplary composition described in Table 3 may be prepared according to conventional methods known to those skilled in the art.
- compositions are prepared to prevent CHX-caused staining when the oral care composition is applied to teeth, especially when applied to teeth surfaces at least daily, for a period of at least one of 1 day, 2 days, 1 week, 2 weeks, 3 weeks, 4 weeks, 1 month, and 2 months.
- Table 4 illustrates the effects of a metal chelator on CHX-caused staining when incorporating into an oral care composition including CHX according to implementations of the present disclosure.
- Table 4 illustrates the AW* for 5 oral care compositions containing CHX and measured similarly as described above. The more positive the value of AW*, the darker the tooth color is.
- Oral Care Composition #1 is a commercially available antimicrobial oral rinse with 0.12% chlorhexidine gluconate.
- Oral Care Compositions #2-#5 are the same as Oral Care Composition #1 except they include the specified amounts (by weight) of a metal chelator.
- the addition of a metal chelator reduces an amount of CHX- based staining.
- the addition of glutamic acid and aspartic acid to an oral care composition containing CHX significantly reduced the amount of CHX- staining as evidenced by the reductions in the AW* value.
- Addition of 0.2 weight % glutamic acid and 1 weight % aspartic acid were the best performers when combined with a CHX- containing commercially available oral care rinse (0.12% chlorhexidine gluconate).
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Abstract
Description
Claims
Priority Applications (6)
Application Number | Priority Date | Filing Date | Title |
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AU2019442626A AU2019442626B2 (en) | 2019-04-26 | 2019-04-26 | Methods and compositions to reduce staining for antibacterial oral care compositions |
EP19731371.1A EP3941430A1 (en) | 2019-04-26 | 2019-04-26 | Methods and compositions to reduce staining for antibacterial oral care compositions |
CA3137935A CA3137935A1 (en) | 2019-04-26 | 2019-04-26 | Methods and compositions to reduce staining for antibacterial oral care compositions |
CN201980095358.8A CN113677316A (en) | 2019-04-26 | 2019-04-26 | Methods and compositions for reducing staining of antibacterial oral care compositions |
MX2021012778A MX2021012778A (en) | 2019-04-26 | 2019-04-26 | Methods and compositions to reduce staining for antibacterial oral care compositions. |
PCT/US2019/029256 WO2020219062A1 (en) | 2019-04-26 | 2019-04-26 | Methods and compositions to reduce staining for antibacterial oral care compositions |
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PCT/US2019/029256 WO2020219062A1 (en) | 2019-04-26 | 2019-04-26 | Methods and compositions to reduce staining for antibacterial oral care compositions |
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PCT/US2019/029256 WO2020219062A1 (en) | 2019-04-26 | 2019-04-26 | Methods and compositions to reduce staining for antibacterial oral care compositions |
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EP (1) | EP3941430A1 (en) |
CN (1) | CN113677316A (en) |
AU (1) | AU2019442626B2 (en) |
CA (1) | CA3137935A1 (en) |
MX (1) | MX2021012778A (en) |
WO (1) | WO2020219062A1 (en) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2023138996A1 (en) * | 2022-01-19 | 2023-07-27 | Unilever Ip Holdings B.V. | Oral care composition |
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ITMI20100149A1 (en) * | 2010-02-02 | 2011-08-03 | Ilaria Lastri | COMPOSITION FOR ORAL HYGIENE CONTAINING CLOREXIDINE AND A SYSTEM TO PREVENT THE FORMATION OF DARK PIGMENTS ON THE SURFACE OF TEETH AND ORAL MUCOSA. |
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US20180043190A1 (en) * | 2016-08-11 | 2018-02-15 | Colgate-Palmolive Company | Oral Care Compositions |
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US10123953B2 (en) * | 2012-06-21 | 2018-11-13 | The Procter & Gamble Company | Reduction of tooth staining derived from cationic antimicrobials |
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2019
- 2019-04-26 CA CA3137935A patent/CA3137935A1/en active Pending
- 2019-04-26 WO PCT/US2019/029256 patent/WO2020219062A1/en unknown
- 2019-04-26 EP EP19731371.1A patent/EP3941430A1/en active Pending
- 2019-04-26 CN CN201980095358.8A patent/CN113677316A/en active Pending
- 2019-04-26 AU AU2019442626A patent/AU2019442626B2/en active Active
- 2019-04-26 MX MX2021012778A patent/MX2021012778A/en unknown
Patent Citations (9)
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FR2281107A1 (en) * | 1974-08-09 | 1976-03-05 | Procter & Gamble | COMPOSITIONS BASED ON BIS-BIGUANIDE DELAYING THE APPEARANCE OF THE DENTAL PLATE |
WO1993016681A1 (en) * | 1992-02-29 | 1993-09-02 | Smithkline Beecham Plc | Compositions |
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WO2023138996A1 (en) * | 2022-01-19 | 2023-07-27 | Unilever Ip Holdings B.V. | Oral care composition |
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CA3137935A1 (en) | 2020-10-29 |
EP3941430A1 (en) | 2022-01-26 |
CN113677316A (en) | 2021-11-19 |
MX2021012778A (en) | 2021-11-18 |
AU2019442626A1 (en) | 2021-10-28 |
AU2019442626B2 (en) | 2023-04-27 |
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