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    • 专利摘要:
    Summary "Stable Fluoride-containing Zinc Oral Care Compositions" Described herein are oral care compositions comprising a zinc ion source, a fluoride ion source, and a basic amino acid; along with methods for producing and using them.
    公开号:BR112015012918B1
    申请号:R112015012918
    申请日:2012-12-05
    公开日:2018-10-30
    发明作者:Rege Aarti；F Suriano David；A Stranick Michael；Sullivan Richard
    申请人:Colgate Palmolive Co；
    IPC主号:
    专利说明:

    (54) Title: COMPOSITION FOR ORAL CARE, USE OF A BASIC AMINO ACID AND USE OF A SOURCE OF ZINC IONS, A SOURCE OF FLUORIDE IONS AND A BASIC AMINO ACID (73) Holder: COLGATE-PALMOLIVE COMPANY. Address: 300 PARK AVENUE, NEW YORK, UNITED STATES OF AMERICA (US), 10022 (72) Inventor: AARTI REGE; DAVID F. SURIANO; RICHARD SULLIVAN; MICHAEL A. STRANICK
    Validity Term: 20 (twenty) years from 12/05/2012, subject to legal conditions
    Issued on: 10/30/2018
    Digitally signed by:
    Liane Elizabeth Caldeira Lage
    Director of Patents, Computer Programs and Topographies of Integrated Circuits
    1/37
    COMPOSITION FOR ORAL CARE, USE OF A BASIC AMINO ACID AND USE OF A SOURCE OF ZINC IONS, A SOURCE OF FLUORIDE IONS AND A BASIC AMINO ACID.
    BACKGROUND [001] Dental erosion involves demineralization and damage to the dental structure due to acid attack from non-bacterial sources. Erosion is found initially in the enamel and, if left unchecked, can progress to the underlying dentin. Dental erosion can be caused or subjected to corrosion directed by acidic food and drinks, exposure to chlorinated pool water and gastric acid regurgitation. Tooth enamel is a negatively charged surface, which naturally tends to attract positively charged ions such as hydrogen and calcium ions, while resisting negatively charged ions, such as fluoride ions. Depending on the relative pH of the surrounding saliva, tooth enamel will lose or gain positively charged ions such as calcium ions. Usually saliva has a pH between 7.2 and 7.4. When the pH is lowered and the hydrogen ion concentration becomes relatively high, the hydrogen ions will replace the calcium ions in the enamel,
    forming phosphate hydrogen (acid phosphoric), which damage the enamel and create a porous surface, type sponge rough. If the saliva remains acidic during a period prolonged, So can does not occur to remineralization, and the tooth goes continue to lose minerals , making the tooth weaken and
    finally ask for the structure.
    [002] There is a need for improved products for the
    2/37 treatment and reduction of erosion.
    [003] Heavy metal ions, such as zinc, are resistant to acid attack. Zinc is above hydrogen in the electrochemical series, so the metallic zinc in an acidic solution will react to release hydrogen gas as the zinc passes into the solution to form di-cations, Zn 2+ . Zinc has been shown to have antibacterial properties in plaque and cavity studies.
    [004] Soluble zinc salts, such as zinc citrate, have been used in toothpaste compositions, but have several disadvantages. Free zinc ions can react with fluoride ions to produce zinc fluoride, which is insoluble and thus reduces the availability of both zinc and fluoride. In addition, the zinc ions in solution impart an unpleasant astringent taste, so formulations that provide effective levels of zinc, and also have acceptable organoleptic properties, have been difficult to achieve. Finally, the zinc ions will react with anionic surfactants such as sodium lauryl sulfate, thus interfering with foaming and cleaning.
    SUMMARY [005] It has now been found that formulations that comprise zinc ions in conjunction with fluoride have greater stability when combined with a basic amino acid, for example, arginine or lysine. The basic amino acid appears to inhibit the formation of water-insoluble zinc fluoride, thereby increasing the availability of both zinc and fluoride. The available zinc assists in protecting against erosion, reducing
    3/37 bacterial colonization and development of biofilm, and providing accentuated shine to the teeth, while the fluoride helps to strengthen the enamel and reduce the formation of cavities. The formulations, moreover, have no poor taste and mouthfeel and poor foaming and cleaning associated with conventional zinc-based oral care products.
    [006] The invention thus provides compositions for oral care, for example, dentifrices, which comprise a source of zinc ions, a source of fluoride ions, and a basic amino acid. The compositions can optionally further comprise a phosphate source. The compositions can be formulated from a toothpaste base or conventional mouthwashes, for example, comprising abrasives, for example, silica abrasives, surfactants, foaming agents, vitamins, polymers, enzymes, humectants, thickeners, antimicrobial agents, preservatives , flavors, dyes, and / or combinations thereof. For example, in one embodiment, the invention provides a toothpaste comprising about 1% zinc citrate, about 5% arginine, about 5% alkali phosphate salts, and about 1450ppm fluoride, in one base of abrasive silica toothpaste.
    [007] The invention further provides methods of using the compositions of the invention to reduce and inhibit enamel acid erosion, clean teeth, reduce biofilm and bacterially generated plaque, reduce gingivitis, inhibit tooth decay and cavity formation, and reducing dentin hypersensitivity, comprising brushing teeth with a composition of the invention.
    4/37 [008] Other areas of applicability of the present invention will become apparent from the detailed description provided hereinafter. It should be understood that the detailed description and specific examples, while indicating the preferred embodiment of the invention, are intended for purposes of illustration only and are not intended to limit the scope of the invention.
    DETAILED DESCRIPTION [009] The following description of the preferred mode (s) is merely exemplary in nature and is in no way intended to limit the invention, its application or uses.
    [010] The invention therefore provides, in a first embodiment, a composition for oral care, for example, a mouthwash or a toothpaste, which comprises a source of zinc ions, a source of fluoride ions, and a basic amino acid (Composition 1), for example:
    1.1. composition 1, wherein the source of zinc ions is selected from zinc citrate, zinc sulfate, zinc silicate, zinc lactate, zinc phosphate, zinc oxide, and combinations thereof, for example, in an effective amount , for example, providing an amount of effective zinc inhibition erosion, for example, 0.005-5% zinc, for example, 0.01-0.05% of a mouthwash or 0.1-3% of a dentifrice, for example, a dentifrice comprising 1-3% zinc citrate;
    1.2. composition 1 in the form of a dentifrice, which further comprises an abrasive, for example, an effective amount of a silica abrasive, for example, 10-30%, for example, about 20%;
    5/37
    1.3. composition 1 in the form of a mouthwash;
    1.4. any of the foregoing compositions, wherein fluorine is present in an effective amount of tooth decay inhibition, for example, 500-3000 ppm fluorine;
    1.5. any of the foregoing compositions, wherein fluoride is a salt selected from stannous fluoride, sodium fluoride, potassium fluoride, sodium monofluorophosphate, sodium fluorosilicate, ammonium fluorosilicate, amine fluoride (for example, N'octadecyltrimethylendiamine-N , Ν, Ν'-tris (2-ethanol) difluorohydrate), ammonium fluoride, titanium fluoride, hexafluorosulfate, and combinations thereof;
    1.6. any of the foregoing compositions, wherein the basic amino acid is present in an amount sufficient to inhibit the formation of zinc fluoride precipitate, for example, about 0.5% to about 20% by weight of the total weight of the composition, from about 0.5% by weight to about 10% by weight of the total weight of the composition, for example, about 1.5% by weight, about 3.75% by weight, about 5% by weight, or about 7.5% by weight of the total weight of the composition in the case of a dentifrice, or, for example, about 0.5-2% by weight, for example, about 1% in the case of a mouthwash;
    1.7. any of the foregoing compositions, wherein the basic amino acid is selected from f;
    1.8. any of the foregoing compositions, wherein the basic amino acid is present in an amount sufficient to increase the pH of the formulation to greater than 8, for example, at pH 8.5-10, for example, about pH 99.5;
    6/37
    1.9. any of the foregoing compositions comprising an effective amount of one or more alkali metal phosphate salts, for example, sodium, potassium or calcium salts, for example, selected from dibasic alkaline phosphate and alkali metal pyrophosphate salts, for example, alkali metal phosphate salts selected from dibasic sodium phosphate, dibasic potassium phosphate, dicalcium phosphate dihydrate, calcium pyrophosphate, tetrasodium pyrophosphate, tetrapotassium pyrophosphate, sodium tripolyphosphate, and mixtures of any two or more of these, for example, in an amount of 1-20%, for example, 2-8%, for example, about 5%, by weight of the composition;
    1.10. any of the foregoing compositions comprising, buffering agents, for example, sodium phosphate buffer (for example, monobasic sodium phosphate and disodium phosphate). Any of the foregoing compositions comprising a humectant, for example, selected from glycerin, sorbitol, propylene glycol, polyethylene glycol, xylitol, and mixtures thereof, for example, comprising at least 20%, for example, 2040%, for example , 25-35% glycerin;
    1.12. any of the foregoing compositions comprising one or more surfactants, for example, selected from anionic, cationic, zwitterionic, and non-ionic surfactants, and mixtures thereof, for example, comprising an anionic surfactant, for example, a surfactant selected from lauryl sulfate sodium, sodium lauryl ether sulfate, and mixtures thereof, for example, in an amount of about 0.3% to about
    7/37
    4.5% by weight, for example, 1-2% sodium lauryl sulfate (SLS); and / or a zwitterionic surfactant, for example, a betaine surfactant, for example, cocamidopropyl betaine, for example, in an amount of about 0.1% to about 4.5% by weight, for example, 0.5- 2% cocamidopropyl betaine;
    1.13. any of the foregoing compositions further comprising a viscosity-modifying amount of one or more of the polysaccharide gums, for example, xanthan or carrageen gum, silica thickener, and combinations thereof;
    1.14. any of the foregoing compositions comprising fragments or strips of gum;
    1.15. any of the foregoing compositions further comprising flavorings, perfumes and / or dyes;
    1.16. any of the foregoing compositions comprising an effective amount of one or more antibacterial agents, for example, comprising an antibacterial agent selected from halogenated diphenyl ether (for example, triclosan), herbal extracts and essential oils (for example, rosemary extract , tea extract, magnolia extract, thymol, menthol, eucalyptol, geraniol, carvacrol, citral, hinoquitol, catechol, methyl salicylate, epigallocatechin gaiate, gaiato, gallic acid, miswak extract, hawthorn extract), antiseptic antiseptics (for example, chlorhexidine, alexidine or octenidine), quaternary ammonium compounds (for example, cetylpyridinium chloride (CPC), benzalkonium chloride, tetradecylpyridinium chloride (TPC), N-tetradecyl-4-ethylpyridinium chloride (TDEPC) ,
    8/37 phenolic antiseptics, hexetidine, octenidine, sanguinarine, povidone iodine, delmopinol, salifluor, metal ions (eg zinc salts, eg zinc citrate, tin salts, copper salts, iron salts), sanguinarine , propolis and oxygenating agents (eg hydrogen peroxide, sodium peroxyborate or buffered peroxycarbonate), phthalic acid and the salts thereof, monopertallic acid and the salts thereof and esters, ascorbyl stearate, oleoyl sarcosine, sulfate
    alkyl, sulfosuccinate of dioctyl, salicylanilide, bromide of domifene, delmopinol, octapinol and others derivatives of piperidine, preparations in nicine, salts of chlorite; and mixtures of any From previous; per example, understanding the triclosan or chloride
    cetylpyridinium;
    1.17. any of the foregoing compositions comprising an antibacterially effective amount of triclosan, for example, 0.1-0.5%, for example, about 0.3%;
    1.18. any of the foregoing compositions further comprising a bleaching agent, for example, one selected from the group consisting of peroxides, metal chlorites, perborates, percarbonates, peracids, hypochlorites, and combinations thereof;
    1.19. any of the foregoing compositions which further comprises hydrogen peroxide or a source of hydrogen peroxide, for example, urea peroxide or a peroxide salt or complex (for example, such as peroxyphosphate, peroxycarbonate, perborate, peroxysilicate, or persulfate salts) , for example, peroxyphosphate
    9/37 calcium, sodium perborate, sodium carbonate peroxide, sodium peroxyphosphate, and potassium persulfate);
    1.20. any of the foregoing compositions further comprising an agent that interferes with or prevents bacterial attachment, for example, solbrol or chitosan;
    1.21. any of the foregoing compositions further comprising a source of calcium and phosphate selected from (i) calcium-glass complexes, for example, calcium sodium phosphosilicates, and (ii) protein-calcium complexes, for example, calcium caseinaphosphate phosphopeptide amorphous;
    1.22. any of the foregoing compositions further comprising a soluble calcium salt, for example, selected from calcium sulfate, calcium chloride, calcium nitrate, calcium acetate, calcium lactate, and combinations thereof.
    1.23. any of the foregoing compositions further comprising a physiologically or orally acceptable potassium salt, for example, potassium nitrate or potassium chloride, in an amount effective to reduce dentin sensitivity;
    1.24. any of the foregoing compositions, further comprising an anionic polymer, for example, a synthetic anionic polymeric polycarboxylate, for example, wherein the anionic polymer is selected from 1: 4 to 4: 1 of anhydride or maleic acid copolymers with another monomer polymerisable ethylenically unsaturated; for example, where the anionic polymer is a methyl vinyl ether / maleic anhydride (PVM / MA) copolymer, having an average molecular weight (MW) of about 30,000 to about 1,000,000, for example
    10/37 example, about 300,000 to about 800,000, for example, wherein the anionic polymer is about 1-5%, for example, about 2%, of the weight of the composition;
    1.25. any of the foregoing compositions further comprising a breath freshener, perfume or flavoring;
    1.26. any of the foregoing compositions, wherein the pH of the composition is either acidic or basic, for example, from pH 4 to pH 5.5 or from pH 8 to pH 10;
    1.27. any of the foregoing compositions, which is a toothpaste, wherein the composition comprises:
    0.5-2.5%, for example, about 1% or about 2% zinc citrate;
    1- 10%, for example, about 5% L-arginine (free base);
    2- 8%, for example, about 5% of alkaline phosphate salts, for example, selected from dibasic sodium phosphate, dibasic potassium phosphate, dicalcium phosphate dihydrate, calcium pyrophosphate, tetrasodium pyrophosphate, tetrapotassium pyrophosphate, sodium tripolyphosphate, and mixtures of any two or more of these;
    700-2000 ppm, for example, about 1450ppm of fluoride, for example, 0.3-0.4%, for example, about 0.32% of sodium fluoride;
    on an abrasive silica toothpaste base;
    1.28. any of the foregoing compositions comprising substantially the same ingredients as in test formulation A or B in Example 1 below, for example, comprising the ingredients listed in amounts within a range of +/- 5% of the indicated values;
    11/37
    1.29. any of the foregoing compositions effective after application to the oral cavity, for example, with a brush, to (i) reduce tooth hypersensitivity, (ii) to reduce the accumulation of plaque, (iii) reduce or inhibit demineralization and promote remineralization of the teeth, (iv) inhibit the formation of microbial biofilms in the oral cavity, (v) reduce or inhibit gingivitis, (vi) promote the healing of wounds or cuts in the mouth, (vii) reduce the levels of bacteria producing acid, (viii) to increase the relative levels of non-plaque and / or non-cariogenic bacteria, (ix) reduce or inhibit the formation of dental caries, (x) reduce, repair or inhibit pre-carious enamel lesions, for example example, as detected by quantitative light-induced fluorescence (QLF) or measurement of electrical caries (ECM), (xi) treating, relieving or reducing dry mouth, (xii) cleaning teeth and oral cavity, (xiii) reducing erosion , (xiv) whiten teeth; and / or (xv) promoting systemic health, including cardiovascular health, for example, through the potential reduction of systemic infection through oral tissues;
    1.30. a composition obtained or obtainable by combining the ingredients as established in any of the foregoing compositions.
    [011] The invention further provides the use of a basic amino acid, for example, arginine, to increase the release of fluoride in an oral care composition, for example, a toothpaste, which comprises a source of zinc ions and a source of ions fluoride.
    [012] The invention also provides methods of using the compositions of the invention, to increase zinc levels
    12/37 on the enamel and to treat, reduce or control the incidence of enamel erosion, comprising applying a composition as described above, for example, any of Composition 1, and following, to the teeth, for example, by brushing . In several embodiments, the invention provides: (i) reduction of hypersensitivity of the teeth, (ii) reduction of plaque accumulation, (iii) reduction or inhibition of demineralization and promotion of remineralization of teeth, (iv) inhibition of biofilm formation microbial in the oral cavity, (v) reduction or inhibition of gingivitis, (vi) promoting healing of wounds or cuts in the mouth, (vii) reducing levels of acid-producing bacteria, (viii) increasing the relative levels of non-forming bacteria plaque and / or non-cariogenic, (ix) reduction or inhibition of the formation of dental caries, (x), reduction, or inhibition of the repair of pre-carious enamel lesions, for example, as detected by quantitative light-induced fluorescence ( QLF) or electrical caries measurement (ECM), (xi) treatment, relief or reduction of dry mouth, (xii) cleaning of teeth and oral cavity, (xiii) reduction of erosion, (xiv) teeth whitening; (xv) reduction of tartar accumulation, and / or (xvi) promotion of systemic health, including cardiovascular health, for example, through the potential reduction of systemic infection through oral tissues, including the application of any of Compositions 1, and following, as described above, for the oral cavity of a person in need of it, for example, brushing one's teeth one or more times a day with any of Compositions 1, and following. The invention further provides Compositions 1, and following, for use
    13/37 in any of these methods.
    [013] Active Agents: The compositions of the invention may comprise various agents that are active to protect and enhance the strength and integrity of the enamel and dental structure and / or to reduce bacteria and associated tooth decay and / or gum disease. The effective concentration of the active ingredients used here will depend on the particular agent and the delivery system used. It is understood that a toothpaste, for example, will typically be diluted with water through use, while a mouthwash will typically not be. Thus, an effective concentration of active ingredient in a toothpaste will normally be 5-15x greater than that needed for a mouthwash. The concentration will also depend on the exact salt or polymer selected. For example, when the active agent is supplied in the form of salt, the counterion will affect the weight of the salt, so that if the counterion is heavier, more salt by weight, it will be necessary to provide the same concentration of active ion. in the final product. Arginine, when present, can be present at levels of, for example, about 0.1 to about 20% by weight (expressed as free base weight), for example, about 1 to about 10% by weight from a consumer toothpaste or about 7 to about 20% by weight for a professional treatment or prescription product. Fluoride when present can be present at levels of, for example, about 25 to about 25,000 ppm, for example, about 750 to about 2000 ppm for a consumer toothpaste, or about 2000 to about 25,000 ppm of a professional treatment or prescription product. Levels of antibacterial agents will
    14/37 vary in the same way, with levels used in toothpaste being, for example, about 5 to about 15 times greater than that used in mouthwash. For example, a triclosan toothpaste can contain about 0.3% by weight of
    Triclosan.
    [014] Fluoride ion source: Oral care compositions may further include one or more sources of fluoride ions, for example, soluble fluoride salts. A wide variety of fluoride ion-producing materials can be used as sources of soluble fluoride in the present compositions. Examples of suitable fluoride ion producing materials are found in US Patent No. 3,535,421, by Briner et al .; US patent no. 4,885,155, by Parran, Jr. et al. and US Patent No. 3,678,154, by Widder et al. Representative sources of fluoride ions include, but are not limited to, stannous fluoride, sodium fluoride, potassium fluoride, sodium monofluorophosphate, sodium fluorosilicate, ammonium fluorosilicate, amine fluoride, ammonium fluoride, and combinations thereof. . In certain embodiments, the source of fluoride ions includes stannous fluoride, sodium fluoride, sodium monofluorophosphate, as well as mixtures thereof. In certain embodiments, the oral care composition of the invention may also contain a source of fluoride ions or fluoride-providing ingredient in sufficient quantities to provide about 25 ppm to about 25,000 ppm fluoride ions, generally at least about 500 ppm , for example, about 500 to about 2000 ppm, for example, about 1000 to about 1600 ppm, for example, about 1450 ppm. The appropriate level of fluoride will
    15/37 depend on the particular application. A toothpaste for general consumer use would typically have about 1000 to about 1500 ppm, with pediatric toothpaste having slightly less. A toothpaste or coating for professional application could have as much as about 5,000 or even about 25,000 ppm of fluoride. The sources of fluoride ions can be added to the compositions of the invention at a level of about 0.01 by weight to about 10% by weight; in some embodiments, from about 0.1% by weight to about 1.2% by weight; in other embodiments, from about 0.3% by weight to about 1% by weight, and in other embodiments, from about 0.5% by weight to about 0.8% by weight of the composition in another embodiment. The weights of fluoride salts to provide the appropriate level of fluoride ions will, of course, vary according to the weight of the salt counterion.
    [015] Amino acids: In some embodiments, the compositions of the present invention comprise an amino acid. In particular embodiments, the amino acid can be a basic amino acid. By basic amino acid means the naturally occurring basic amino acids, such as arginine, lysine and histidine, as well as any basic amino acid having a carboxyl group and an amino group in the molecule, which is soluble in water and provides an aqueous solution with a pH of about 7 or greater. Consequently, basic amino acids include, but are not limited to, arginine, lysine, citrulline, ornithine, creatine, histidine, diaminobutanoic acid, diaminoproprionic acid, salts thereof or combinations thereof. In a particular embodiment, the basic amino acids are selected from
    16/37 arginine, citrulline, and ornithine. In certain embodiments, the basic amino acid is arginine, for example, 1-arginine, or a salt thereof. In other embodiments, the amino acid is quaternized, that is, the amino group is further substituted to form a quaternary ammonium radical, which can form an internal salt with the carboxyl group, for example, betaine (Ν, N, N-trimethylglycine ).
    [016] In various embodiments, the amino acid is present in an amount of about 0.5% by weight to about 20% by weight of the total weight of the composition, from about 0.5% by weight to about 10% by weight of the total weight of the composition, for example, about 1.5% by weight, about 3.75% by weight, about 5% by weight, or about 7.5% by weight of the total weight of the composition in the case of a toothpaste, or for example, about 0.5-2% by weight, for example, about 1% in the case of a mouthwash.
    [017] Abrasives: The compositions of the invention, for example, Composition 1 and following, include silica abrasives, and may comprise additional abrasives, for example, a calcium phosphate abrasive, for example, tricalcium phosphate (Ca3 (PO 4 ) 2) r hydroxyapatite (Caio (PO 4 ) 6 (OH) 2 ), or dicalcium phosphate dihydrate (CaHPO 4 .2H2O, also sometimes referred to here as DiCal) or calcium pyrophosphate; calcium carbonate abrasive; or abrasives, such as sodium metaphosphate, potassium metaphosphate, aluminum silicate, calcined alumina, bentonite or other siliceous materials or combinations thereof.
    [018] Other silica abrasive polishing materials useful here, as well as other abrasives, generally have a
    17/37 average particle size ranging between about 0.1 and about 30 pm, about between 5 and about 15 pm. The silica abrasives can be either precipitated silica or silica gels, such as the silica xerogels described in US Patent No. 4,291,291. 3,538,230, by Pader et al. and US Patent No. 3,862,307, by Digiulio. Private silica Xerogels are marketed under the trade name Syloid® by W.R. Grace & Co., Davison Chemical Division. Precipitated silica materials include those marketed by J.M. Huber Corporation under the trade name Zeodent®, including silica under the designation Zeodent 115 and 119. These silica abrasives are described in US Patent No. 4,340,583, from Wason. In certain embodiments, abrasive materials useful for practicing oral care compositions according to the invention include silica gels and precipitated amorphous silica having an oil absorption value of less than about 100 cc / 100 g of silica and na range of about 45 cc / 100 g to about 70 cc / 100 g of silica. Oil absorption values are measured using the ASTA Rub-out Method D281. In certain embodiments, silicas are colloidal particles with an average particle size of about 3 pm to about 12 pm and about 5 to about 10 pm. Low oil absorption silica abrasives particularly useful in the practice of the invention are marketed under the trade name Sylodent XWA® by Davison Chemical Division of W.R. Grace & Co., Baltimore, Md. 21203. Sylodent 650 XWA®, a silica hydrogel, composed of colloidal silica particles having a water content of 29% by weight ranging from about 7 to about 10 pm in diameter , and an oil absorption of less
    18/37 of about 70 cc / 100 g of silica is an example of a silica abrasive with low oil absorption useful in the practice of the present invention.
    [019] Foaming agents: The oral care compositions of the invention may also include an agent for increasing the amount of foam that is produced when the oral cavity is brushed. Illustrative examples of agents that increase the amount of foam include, but are not limited to, polyoxyethylene and certain polymers including, but not limited to, alginate polymers. Polyoxyethylene can increase the amount of foam and foam thickness generated by the oral care support component of the present invention. Polyoxyethylene is also commonly known as polyethylene glycol (PEG) or polyethylene oxide. The polyoxyethylenes suitable for this invention will have a molecular weight of about 200,000 to about 7,000,000. In one embodiment, the molecular weight will be about 600,000 to about 2,000,000 and in another mode about 800,000 to about 1,000,000. Polyox® is the trade name for high molecular weight polyoxyethylene produced by Union Carbide. Polyoxyethylene can be present in an amount of about 1% to about 90%, in one embodiment about 5% to about 50% and in other embodiments about 10% to about 20%, by weight, of the component carrier of the oral care element of the oral care compositions of the present invention. When present, the amount of foaming agent in the oral care composition (i.e., a single dose) is about 0.01 to about 0.9%, by weight, about 0.05 to about 0 , 5% by weight, and other
    19/37 embodiments about 0.1 to about 0.2% by weight.
    [020] Surfactants: Compositions useful in the present invention may contain anionic surfactants, for example:
    i. water-soluble salts of higher fatty acid monoglyceride monosulfates, such as the sodium salt of the monoglyceride monoglyceride of hydrogenated coconut oil fatty acids, such as sodium N-methyl-Ncocoyl-taurate, sodium cocomonoglyceride sulfate;
    ii. higher alkyl sulfates, such as sodium lauryl sulfate;
    iii. higher alkyl ether sulfates, for example, of the formula CH3 (CH2) mCH2 (OCH2CH2) nOSO 3 X, where m is 6-16, for example, 10, n is 1-6, for example, 2, 3 or 4 and X is Na or K, for example, sodium lauride-2 sulfate (CH 3 (CH 2 ) 1st CH 2 (OCH 2 CH 2 ) 2 OSO 3 Na);
    iv. higher alkyl aryl sulfonates such as sodium dodecyl benzene sulfonate (sodium lauryl benzene sulfonate);
    v. upper alkyl sulfoacetates, such as sodium lauryl sulfoacetate (sodium dodecylsulfoacetate), higher fatty acid esters of 1,2-dihydroxypropanesulfonate, sulfocolaurate (sulfoacetamide N2-ethyl potassium laurate) and sodium lauryl-sarcosinate.
    [021] By higher alkyl is meant, for example, Cg-30 alkyl. In particular modalities, the anionic surfactant is selected from sodium lauryl sulfate and sodium lauryl ether sulfate. The anionic surfactant can be present in an amount that is effective, for example,> 0.01% by weight of the formulation, but not at a concentration that
    20/37 would be irritating to oral tissue, for example, <10%, and optimal concentrations depend on the particular formulation and the particular surfactant. For example, the concentrations used or a mouthwash are typically on the order of a tenth of that used for a toothpaste. In one embodiment, the anionic surfactant is present in a toothpaste of about 0.3% to about 4.5% by weight, for example, about 1.5%. The compositions of the invention can optionally contain mixtures of surfactants, for example, comprising anionic surfactants and other surfactants which can be anionic, cationic, zwitterionic or nonionic. Generally, surfactants are those that are reasonably stable over a wide pH range. Surfactants are described more fully, for example, in US Patent No. 3,959,458, by Agrícola et al; US patent no. 3,937,807, by Haefele; and
    US patent no. 4,051,234, by Gieske et al. In certain embodiments, the anionic surfactants useful for this invention include the water-soluble salts of alkyl sulfates having from about 10 to about 18 carbon atoms in the alkyl radical and the water-soluble salts of sulfonated fatty acid monoglycerides having about of about 18 carbon atoms. Sodium lauryl sulfate, sodium lauroyl sarcosinate and coconut sodium monoglyceride sulfonates are examples of anionic surfactants of this type. In a particular embodiment, the composition of the invention, for example, Composition 1 and following, comprises sodium lauryl sulfate.
    [022] The surfactant or mixtures of surfactants
    21/37 compatible can be present in the compositions of the present invention in about 0.1% to about 5.0%, in other embodiments, about 0.3% to about 3.0% and in other embodiments, about from 0.5% to about 2.0% by weight of the total composition.
    [023] Tartar control agents: In various embodiments of the present invention, the compositions comprise an anti-calculus (tartar control) agent. Suitable anticalculation agents include, without limitation, phosphates and polyphosphates (e.g., pyrophosphates), polyaminopropanesulfonic acid (AMPS), hexametaphosphate salts, zinc citrate trihydrate, polypeptides, polyolefin sulfonates, polyolefin phosphates. The invention can thus comprise phosphate salts, in addition to zinc phosphate. In particular embodiments, these salts are salts of alkaline phosphates, that is, salts of alkali metal hydroxides or alkaline earth hydroxides, for example, sodium, potassium or calcium salts. Phosphate, as used herein, encompasses orally acceptable mono- and polyphosphates, for example, Pi- 6 phosphates, for example, monomeric phosphates, such as monobasic, dibasic or tribasic phosphate; dimeric phosphates, such as pyrophosphates; and multimeric phosphates, for example, sodium hexametaphosphate. In particular examples, the selected phosphate is selected from alkaline dibasic phosphate and alkaline pyrophosphate salts, for example, selected from sodium dibasic phosphate, potassium dibasic phosphate, dihydrated dicalcium phosphate, calcium pyrophosphate, tetrasodium phosphate tetra-phosphate, pyrophosphate , sodium tripolyphosphate, and mixtures of
    22/37 any two or more of these. In a particular embodiment, for example, the compositions comprise a mixture of tetrasodium pyrophosphate (Na 4 P2O 7 ), calcium pyrophosphate (Ca2PzO 7 ), and dibasic sodium phosphate (Na2HPO 4 ), for example, in quantities of about 3 -4% of dibasic sodium phosphate and about 0.2-1% of each of the pyrophosphates. In another embodiment, the compositions comprise a mixture of tetrasodium pyrophosphate (TSPP) and sodium tripolyphosphate (STPP) (Na 5 P30io), for example, in proportions of TSPP about 1-2% and STPP about 7% about 10%. Such phosphates are supplied in an amount effective to reduce enamel erosion, to aid teeth cleaning, and / or to reduce the accumulation of tartar on the teeth, for example, in an amount of 2-20%, for example, about 5-15%, by weight of the composition.
    [024] Flavoring agents: The oral care compositions of the invention may also include a flavoring agent. Flavoring agents that are used in the practice of the present invention include, but are not limited to, essential oils, as well as various flavoring aldehydes, esters, alcohols, and the like. Examples of essential oils include mint, peppermint, wintergreen, sassafras, cloves, sage, eucalyptus, marjoram, cinnamon, lemon, lime, grape and orange oils. Also useful are chemicals like menthol, carvone and anethole. Certain modalities use peppermint and peppermint oils. The flavoring agent can be incorporated into the oral composition at a concentration of about 0.1 to about 5% by weight, for example, about 0.5 to
    23/37 about 1.5% by weight.
    [025] Polymers: Compositions for invention may also include polymers to adjust the viscosity of the formulation to the solubility of other ingredients. Additional polyethylene glycols, (eg, oral cellulose derivatives of additional care to or accentuate the
    Such polysaccharide polymers, for example, carboxymethylcellulose, example gums, xanthan gum or acids, for example, gels supplied in the form of
    in polysaccharides or by gum carrageenan). Polymers in polyacrylate, can be their free acids or metals
    partially soluble or fully neutralized water-soluble (eg, potassium and sodium) or ammonium salts.
    [026] Silica thickeners, which form polymeric structures or gels in an aqueous medium, may be present. Note that these silica thickeners are physically and functionally distinct from the particulate silica abrasives also present in the compositions, since the silica thickeners are very finely divided and offer little or no abrasive action. Other thickening agents are polymers of carboxyvinyl, carrageenan, hydroxyethylcellulose and water soluble salts of cellulose ethers such as sodium carboxymethyl cellulose and sodium carboxymethyl hydroxyethyl cellulose. Natural gums such as karaya gum, gum arabic, and tragacanth gum can also be incorporated. Colloidal magnesium and aluminum silicate can be used as a component of the thickening composition to further improve the texture of the composition. In certain embodiments, the thickening agents in an amount of about 0.5% to about
    24/37
    5.0% by weight of the total composition is used.
    [027] The compositions of the invention can include an anionic polymer, for example, in an amount of about 0.05 to about 5%. Such agents are generally known for use in dentifrice, although not for this particular application, those useful in the present invention are disclosed in US Patents. No. 5,188,821 and 5,192,531; and include synthetic anionic polymeric polycarboxylates, such as 1: 4 to 4: 1 of anhydride or maleic acid copolymers with another polymerisable ethylenically unsaturated monomer, preferably methyl vinyl ether / maleic anhydride having a molecular weight (PM) of about 30,000 to about 1,000,000, more preferably, about 300,000 to about 800,000. These copolymers are available, for example, as Gantrez. , for example, AN 139 (P.M.
    500,000), AN 119 (PM 250,000) and, preferably, Pharmaceutical Grade S-97 (PM 700,000) available from ISP Technologies, Inc., Bound Brook, NJ 08805. Accenting agents when present are present in quantities ranging from about 0.05 to about 3% by weight. Other operative polymers include those such as maleic anhydride 1: 1 copolymers with ethyl acrylate, hydroxyethyl methacrylate, N-vinyl-2-pyrrolidone, or ethylene, the latter being available, for example, as Monsanto EMA No. 1103, PM 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. Generally suitable are ethylenically unsaturated or olefinically polymerized carboxylic acids which contain a double bond
    25/37 activated carbon-to-carbon olefin and at least one carboxyl group, that is, an acid containing an olefinic double bond that readily works in polymerization because of its presence in the monomer molecule, either in the alpha-beta position in relation to a carboxyl group or as part of a terminal methylene group. Illustrative of such acids are acrylic, methacrylic, ethacrylic, alpha-chloroacrylic, crotonic, beta-acryloxypropionic, sorbic, alpha-chlorosorbic, cinnamic, beta-styrene acrylic, muconic, itaconic, citraconic, mesaconic, glutaconic, alpha-phenylacrylic, 2benzylacrylic, 2-cyclohexyl-acrylic, angelic, umbelic, fumaric, and maleic. Other olefinic monomers other than copolymerizable with these carboxylic monomers include vinyl acetate, vinyl chloride, dimethyl maleate and the like. Copolymers contain groups of sufficient carboxylic salts for solubility in water. Another class of polymeric agents includes a composition containing the acrylamide homopolymers and / or unsaturated sulfonic acid homopolymers and substituted salts thereof, in particular, where the polymers are based on unsaturated sulfonic acids selected from acrylamidoalonic sulfonic acids such as 2-acid - sulfonic methylpropane 2 having a molecular weight of about 1,000 to about 2,000,000, described in U.S. Pat. US No. 4,842,847, of June 27, 1989 by Zahid. Another useful class of polymeric agents includes polyamino acids that contain proportions of amino acids active on an anionic surface, such as aspartic acid, glutamic acid and phosphoserine, for example, as disclosed in US Patent No. 4,866,161 of
    26/37
    Sikes et al.
    [028] Water: Oral compositions can comprise significant levels of water. The water used in the preparation of commercial oral compositions must be deionized and free of organic impurities. The amount of water in the compositions includes free water that is added plus the amount that is introduced with other materials.
    [029] Humectants: Within certain modalities of oral compositions, it is also desirable to incorporate a humectant to prevent the composition from hardening on exposure to air. Certain humectants can also impart desirable sweetness or taste to toothpaste compositions. Suitable humectants include edible polyhydric alcohols such as glycerin, sorbitol, xylitol, propylene glycol, as well as other polyols and mixtures of these humectants. In one embodiment of the invention, the main humectant is glycerin, which can be present at levels greater than 25%, for example, 25-35% to about 30%, with
    5% or less of other humectants.
    [030] Other optional ingredients: In addition to the components described above, the embodiments of this invention may contain a variety of optional toothpaste ingredients, some of which are described below. Optional ingredients include, for example, but are not limited to, adhesives, foaming agents, flavoring agents, sweetening agents, additional anti-plaque agents, abrasives and coloring agents. These and other optional components are further described in US Patent No. 5,004,597, by Majeti; US Pat. 3,959,458 by Agrícola et al. and US Patent No. 3,937,807, by Haefele,
    27/37 all of which are incorporated by reference.
    [031] As used throughout this document, ranges are used as an abbreviation to describe each and every value within the range. Any value within the range can be selected as the end of the range. In addition, all references cited herein are hereby incorporated by reference in their entirety. In the event of a conflict between a definition in the present disclosure and a cited reference, the present disclosure shall prevail.
    [032] Unless otherwise stated, all percentages and quantities expressed here and elsewhere in the specification should be understood as referring to weight percentages. The quantities given are based on the weight of the active material.
    EXAMPLES
    Example 1 [033] Test dentifrices comprising 1% and 2% zinc citrate in combination with 5% arginine, 1450 ppm fluoride, phosphates and are prepared, together with control dentifrices that do not comprise zinc or none. arginine, and the stability of the formulations, in particular, the availability of zinc and fluoride, is measured after accelerated aging, as follows:
    TABLE 1
    Ingredient A, 1% Zinc B. 2% C. Without D. Without PEG600 3.00 3.00 3.00 3.00 CMC-7 0.65 0.65 0.65 0.75 Xanthan 0.20 0.20 0.20 0.20 Sorbitol 28.4 27.4 29.4 28.4 Glycerin 20, 0 20, 0 20, 0 20, 0 Saccharin 0.30 0.30 0.30 0.30
    28/37
    TSPP 0.50 0.50 0.50 0.50 Cu Phosphate 0.25 0.25 0.25 0.25 Dibasic Phosphate 3.50 3.50 3.50 3.50 Na fluoride 0.32 0.32 0.32 0.32 Water QS QS QS QS Ti02 0.50 0.50 0.50 0.50 Abrasive Silica 8.00 8.00 8.00 8.00 Silica thickener 8.00 8.00 8.00 8.00 L-Arginine 5.00 5.00 5.00 SLS 1.50 1.50 1.50 1.50 Brighter K91-5661 flavoring 1.20 1.20 1.20 1.20 Zinc Citrate 1.00 2.00 1.00 ROOM TEMPERATUREHOME % Arginine (4.5 - 5.5) 4.90 4.90 4.90 F1 (1250 - 1500 ppm) 1490 1490 1460 1390 % Zinc (0.5 - 0.35) 0.09 0.14 0.08 pH (6.5 - 8.0) Cosmetic Good Good Good 1 Month @ 49 ° C % Arginine (4.5 - 5.5) 4.80 4.80 4.70 F1 (1250 - 1500 ppm) 1480 1500 1480 1330 % Zinc (0.5 - 0.35) 0, 06 0.09 pH (6.5 - 8.0) Cosmetic Good Good Good 1 Month @ 40 ° C % Arginine (4.5 - 5.5) 4.90 4.80 4.70 F1 (1250 - 1500 ppm) 1420 1410 1480 1320 % Zinc (0.5 - 0.35) 0.10 0.10 pH (6.5 - 8.0) Cosmetic Good Good Good 1 Month @ -4 ° C % Arginine (4.5 - 5.5) 5.00 5.00 4.90 F1 (1250 - 1500 ppm) 1430 1470 1500 1370 % Zinc (0.5 - 0.35) 0.07 0.13 pH (6.5 - 8.0) Cosmetic Good Good Good 2 Months @ 49 ° C % Arginine (4.5 - 5.5) 4.70 4.70 4.60
    29/37
    F1 (1250 - 1500 ppm) 1480 1410 1460 1380 % Zinc (0.5 - 0.35) 0, 06 0.10 pH (6.5 - 8.0) Cosmetic Good Good Good 2 Months @ 40 ° C % Arginine (4.5 - 5.5) 4.90 4.80 4.70 F1 (1250 - 1500 ppm) 1420 1470 1510 1290 % Zinc (0.5 - 0.35) 0.10 0.11 pH (6.5 - 8.0) Cosmetic Good Good Good 2 Months @ -4 C % Arginine (4.5 - 5.5) 5.00 4.90 5.00 F1 (1250 - 1500 ppm) 1440 1440 1450 1280 % Zinc (0.5 - 0.35) 0.08 0.13 pH (6.5 - 8.0) Cosmetic Good Good Good 3 Months @ 49 ° C % Arginine (4.5 - 5.5) 4.70 4.80 4.50 F1 (1250 - 1500 ppm) 1470 1470 1480 % Zinc (0.5 - 0.35) 0, 06 0.08 pH (6.5 - 8.0) Cosmetic Good Good Good 3 Months @ 40 ° C % Arginine (4.5 - 5.5) 4.80 4.80 4.70 F1 (1250 - 1500 ppm) 1470 1480 1430 % Zinc (0.5 - 0.35) 0.09 0.13 pH (6.5 - 8.0) Cosmetic Good Good Good 3 Months @ -4 ° C % Arginine (4.5 - 5.5) 5.00 4.90 4.90 F1 (1250 - 1500 ppm) 1430 1430 1430 % Zinc (0.5 - 0.35) 0.12 0.18 pH (6.5 - 8.0) Cosmetic Good Good Good
    [034] As will be noted, Formulation D, a zinc formulation without arginine, has significantly less fluoride available than formulations with arginine,
    30/37 probably due to the interaction of zinc ions and fluoride, but formulations with 1% and 2% zinc citrate and arginine have approximately the same levels of fluoride available as the formulation without zinc citrate, even after aging at low or high temperatures, which suggests that the presence of arginine increases the availability of fluoride in combination with zinc.
    Example 2 [035] The ability of test and control formulations to provide fluoride and zinc for enamel is measured using electron spectroscopy, for chemical analysis (ESCA, also known as X-ray photoelectron or XPS spectroscopy). ESCA is a surface analysis technique used to obtain chemical information on the surfaces of solid materials. The material characterization method uses an x-ray beam to excite a solid sample resulting in the emission of photoelectrons. An energy analysis of these photoelectrons provides both elemental and chemical information about the bond on a sample surface. The relatively low kinetic energy of the photoelectrons gives ESCA a sampling depth of approximately 30 Å. ESCA is used to analyze the mineral content of the enamel before and after using the test vs control toothpaste on polished and etched enamel substrates prepared and treated as described in the previous examples, which confirms that zinc is released to the surface of the enamel and that zinc remains on the surface, even after acid challenges, as well as
    31/37 confirming the effective fluoride release.
    [036] The ESCA data for the enamel samples treated with the various Zn / arginine / phosphate anti-erosion pastes from Example 1 are shown in Table 2 below, which defines the detected elements and their respective atomic concentrations. All samples are analyzed after each polishing, engraving and treatment step. For simplicity, only the average composition for all samples is presented for the polished surfaces and subjected to directed corrosion. In all cases, three to four separate areas are analyzed for each sample. For the treated samples, the compositions of the individual areas, as well as the average composition for each sample are presented.
    [037] C and N are detected in the polished samples and subjected to directed corrosion from organic surface compounds. Ca and P are detected from hydroxylapatite (PAH) in the enamel, with typical P / Ca ratios for the enamel surfaces. The average P / Ca ratio for surfaces subjected to directed corrosion is slightly less than for polished surfaces, indicating that a reduction in the phosphate surface in relation to Ca occurs after the directed corrosion. A low level of Zn is detected for the polished surfaces, which is removed by directed corrosion. Fluorine is also detected for both polished surfaces and subjected to targeted corrosion at low levels. A low level of Na is also observed. In general, the compositions of enamel surfaces that are polished and subjected to directed corrosion are typical for bovine enamel.
    32/37 [038] C and N are detected on the surfaces of all samples treated from organic surface compounds. The C levels for everyone, but for the sample treated without zinc, are higher than for surfaces subjected to directed corrosion, due to the presence of residual organic materials, most likely from the pastes. The levels of N are also higher for the treated samples in relation to the surfaces subjected to directed corrosion. For samples treated with pastes containing arginine, it is possible that some N is due to arginine on the surfaces. Thus, SIMS analysis is conducted on all treated blocks to determine arginine deposition. The peak of the molecular ion of arginine at 175 amu is detected only for the sample treated with the paste without Zn. This example also exhibited the highest N level of ESCA of all treated samples. Thus, for this example, the higher concentration of N determined by ESCA is, at least in part, due to the presence of arginine on the surface. The peak of the arginine molecular ion is not observed for the other samples treated with arginine containing pastes. Arginine may still be present in these samples, but at levels below the SIMS detection limit. The concentration of N in ESCA for the sample treated with arginine - free paste is similar to those presented for the remaining samples treated with arginine pastes. Thus, the increase in N on these enamel surfaces may also be due to other sources of arginine.
    [039] Ca and P are also detected on the surface of the samples, from the PAH in the enamel. P / Ca ratios
    33/37 for treated samples are higher than for surfaces subjected to directed corrosion, indicating an excess of phosphate in relation to Ca. For all samples, Na concentrations are also significantly higher than for the submitted enamel corrosion. The higher levels of phosphate and Na on the treated samples suggest that Na phosphate from the paste was deposited on the enamel surfaces. Si is also detected in low amounts in the treated enamels, due to residual silica from the pastes.
    [040] For enamel samples treated with zinc-containing pastes, high levels of zinc are observed on the surface. As with previous studies, Zn / Ca ratios provide the best means for comparing zinc absorption on enamel surfaces. The Zn / Ca ratios for enamel treated with pastes containing zinc citrate are all the same. Thus, the data suggest that neither arginine nor doubling the zinc citrate concentration has any noticeable effect on zinc absorption.
    [041] ESCA zinc peak positions can provide information on the chemical status of zinc on enamel surfaces. The zinc peak positions for all samples treated with zinc containing pastes are the same. This suggests that the zinc present in all samples is of a similar chemical form. In addition, the peak zinc positions for samples treated with zinc paste are the same as those for base zinc on the surfaces of the polished enamel. The base zinc inherently present in the enamel is probably under the
    34/37 form of a zinc HAP. Thus, the data suggest that zinc
    in the treated enamel can also be in the shape of a PAH zinc. [042] F, in the form of fluoride is detected at surface of all treated samples with the folder in
    enamel. The relative fluoride absorption between samples is also best determined using the F / Ca ratios. The data indicate that the enamel treated without zinc, pastes with 1% and 2% zinc citrate had similar F / Ca ratios, which suggests similar F absorption. The enamel treated with zinc citrate without arginine exhibited slightly lower F / Ca ratios, although we noticed some variation.
    [043] ESCA results indicate that zinc deposition occurs for enamel treated with pastes containing either zinc citrate or zinc phosphate. The deposition of zinc is greater for the paste containing zinc phosphate compared to zinc citrate pastes. The data also suggest that zinc may be present on the surface as a zinc HAP. Elevated fluoride levels are also observed for all treated pulp samples.
    [044] The detailed results of the analysis are shown in Table 2 (below).
    TABLE 2
    Analysis of enamel ESCA - Zn Anti-erosion Paste / Arginine / PO </ NaF Sample Atomic Percentage Reason ç 0 N Here P Zn At F Si P / Ca Zn / Ca F / Ca Polished - all 5 samples average 23.84 49.56 0.58 14.39 11.04 0.09 0.42 0.10 - 0.77 0.007 0.007
    35/37
    Targeted corrosion - all 5 samplesaverage 31.88 44.05 0.46 13.22 9.75 0.00 0.51 0.13 - 0.74 0.000 0.010 1% Zn citrate withoutArginine treated 40.57 36.10 0.82 8.78 8.32 0.54 3.35 0.48 1.05 0.95 0.062 0.055 43.35 34.21 0.99 8.49 7.94 0.55 3.08 0.50 0.88 0.94 0.065 0.059 44.50 33, 64 1.00 8.47 7.82 0.53 2.88 0.49 0.67 0.92 0.063 0.058 average 42.81 34.65 0.94 8.58 8.03 0.54 3.10 0.49 0.87 0.94 0.063 0.057 1% Zn Citrate withArginine treated 43.06 37.74 0.93 6.23 6.11 0.33 2.88 0.45 2.27 0.98 0.053 0.072 42, 48 36.77 0.74 7.25 6.84 0.45 2.50 0.51 2.43 0.94 0.062 0.070 ★ 38.71 37.10 0.82 8.14 8.00 0.47 3.99 0.51 1.15 0.98 0.058 0.063 average 41.42 37.20 0.83 7.21 6, 98 0.42 3.12 0.49 1.95 0.97 0.058 0.068 2% Zn Citrate withArginine treated 47.28 31.68 1.19 7.15 7.42 0.39 2.42 0.49 1.15 1.04 0.055 0.069 42.77 34.84 1.21 8.22 8.43 0.55 2.60 0.55 0.83 1.03 0.067 0.067 43.07 34.28 1.26 7.94 8.22 0.51 3.12 0.52 1.08 1.04 0.064 0.065 average 44.37 33.60 1.22 7.77 8.02 0.48 2.71 0.52 1.02 1.03 0.062 0.067
    [045] As these data show, formulations comprising zinc and arginine release fluoride at nearly 20% higher levels than the formulation comprising zinc without arginine (F / Ca 0.057 ± 0.0016 vs. 0.068 ± 0.0038 to 1 % zinc citrate and 0.067 ± 0.0016 for 2% zinc citrate), which is consistent with the data in the previous example that these formulations provide higher levels of available fluoride.
    Example 3 [046] The dentifrice A of Example 1 containing 1% zinc citrate, together with arginine and fluoride, shows superior efficacy for the acid challenge compared to controls.
    36/37 [047] An in vitro method is used to determine the protective enamel activity of the prototype formulations of Example 1. Enamel substrates (N = 6/8 per cell) are prepared by incorporating bovine incisors into the resin based on methacrylate and polishing with carbide sandpaper 600 and 1200 consecutively. Care is taken not to penetrate the dentin layer when polishing the enamel to a mirror finish. Before testing, all enamel substrates are preconditioned with 5% citric acid for 30 seconds. Half a side of each
    with ribbon resistant acid to as one control in surface. 0 ally the products alternated in
    1-minute product treatment periods with 2 min acid exposure periods according to the daily follow-up of T-C-C-C-C-T (T = product treatment, C = acid challenge). The acid challenge is performed with a 1% aqueous solution of citric acid (not buffered), adjusted to pH = 3.8 with NaOH. All enamel substrates are kept in a sterile artificial saliva solution at 37 ° C, while not undergoing treatment or challenge. This regime is conducted for a total of five days, at the end of which a microhardness analysis is used to guarantee the amount of lost enamel due to erosion on each enamel substrate on protected and exposed surfaces. The change in percentage hardness is calculated. Without treatment, using deionized water instead of test toothpaste, the percentage change in hardness is very high, approaching 80%, and only slightly reduced with treatment with a toothpaste
    37/37 without zinc (Formulation C), but is greatly reduced by treatment with Formulation A of Example 1
    TABLE 3
    Water Dl Formulation C Formulation A Average% reduction in 78.28 70.16 46.44 Standard deviation 9.15 15.74 9.26
    1/3
    权利要求:
    Claims (3)
    [1]
    1 to 8% arginine;
    1 to 3% zinc citrate;
    1. Composition for oral care characterized by the fact that it comprises:
    from 0.05 to 5%, by weight, of a source of zinc ions comprising zinc citrate;
    a source of fluoride ions in an amount effective to provide 500 to 5000 ppm of fluoride, where the source of fluoride is sodium fluoride, and 0.1 to 10% by weight of arginine.
    [2]
    2 to 8% alkaline phosphate salts, selected from dibasic sodium phosphate, dibasic potassium phosphate, dicalcium phosphate dihydrate, tetrasodium pyrophosphate, tetrapotassium pyrophosphate, calcium pyrophosphate, sodium tripolyphosphate, and a combination of two or more of these;
    700 to 2000 ppm fluoride;
    on a silica abrasive toothpaste base.
    11. Composition according to any one of claims 1 to 10, characterized in that it is for use in the treatment or reduction of dental enamel erosion.
    12. Use of a basic amino acid, characterized by the fact that it is to increase the release of fluoride in an oral care composition that comprises a source of zinc ions and a source of fluoride ions.
    13. Use of a source of zinc ions, a source of fluoride ions and a basic amino acid, characterized by being in the preparation of a composition as defined
    Petition 870180061012, of 07/16/2018, p. 9/13
    2/3
    8. Composition, in a deal with any an of claims 1 to 7, characterized by the fact in what further comprises a or more sources ions zinc in addition to citrate zinc. 9. Composition, in a deal with any an of
    claims 1 to 8, characterized by the fact that the pH of the composition is basic.
    10. Composition according to any one of claims 1 to 9, characterized by the fact that it comprises:
    2. Composition according to claim 1, characterized by the fact that it is in the form of a toothpaste comprising an abrasive.
    3. Composition according to claim 1 or 2, characterized by the fact that the amount of zinc is 0.5 to 4% by weight.
    4. Composition, in wake up with any an of claims 1 to 3, characterized by the fact in what comprises one or more abrasives, one or more humectants it is a or more surfactants. 5. Composition, in wake up with any an of claims 1 to 4, characterized by the fact in what further comprises a amount effective one or more salts alkaline phosphate. 6. Composition, in wake up with any an of claims 1 to 5, characterized by the fact in what
    it further comprises an effective amount of one or more antibacterial agents.
    Composition according to any one of claims 1 to 6, characterized in that it further comprises a bleaching agent.
    Petition 870180061012, of 07/16/2018, p. 8/13
    [3]
    3/3 in any one of claims 1 to 10, for the treatment or reduction of dental enamel erosion, which treatment comprises the administration of the composition in the oral cavity of an individual in need thereof.
    Petition 870180061012, of 07/16/2018, p. 10/13
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    同族专利:
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    US20190038531A1|2019-02-07|
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    HK1215159A1|2016-08-19|
    CN108078798A|2018-05-29|
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    AU2012396294A1|2015-05-28|
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    KR20150092255A|2015-08-12|
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    TW201438748A|2014-10-16|
    US20150313813A1|2015-11-05|
    WO2014088572A1|2014-06-12|
    PH12015501186A1|2015-08-17|
    PH12015501186B1|2015-08-17|
    EP2928440A1|2015-10-14|
    CA2890537A1|2014-06-12|
    EP2928440B2|2019-12-18|
    TW201626978A|2016-08-01|
    AR093792A1|2015-06-24|
    IL238841D0|2015-06-30|
    ZA201503925B|2017-07-26|
    IN2015DN03990A|2015-10-02|
    CN104822362A|2015-08-05|
    EP3195850A1|2017-07-26|
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    法律状态:
    2018-04-10| B15K| Others concerning applications: alteration of classification|Free format text: AS CLASSIFICACOES ANTERIORES ERAM: A61K 8/27 , A61K 8/44 , A61Q 11/00 , A61K 8/21 Ipc: A61K 8/21 (2006.01), A61K 8/27 (2006.01), A61K 8/4 Ipc: A61K 8/21 (2006.01), A61K 8/27 (2006.01), A61K 8/4 |
    2018-04-17| B07A| Technical examination (opinion): publication of technical examination (opinion)|
    2018-08-07| B09A| Decision: intention to grant|
    2018-10-30| B16A| Patent or certificate of addition of invention granted|Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 05/12/2012, OBSERVADAS AS CONDICOES LEGAIS. |
    优先权:
    申请号 | 申请日 | 专利标题
    PCT/US2012/067994|WO2014088572A1|2012-12-05|2012-12-05|Fluoride-stable zinc containing oral care compositions|
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