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WO1999012517A1 - Preparations permettant de blanchir les dents - Google Patents

Preparations permettant de blanchir les dents Download PDF

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Publication number
WO1999012517A1
WO1999012517A1 PCT/US1998/018309 US9818309W WO9912517A1 WO 1999012517 A1 WO1999012517 A1 WO 1999012517A1 US 9818309 W US9818309 W US 9818309W WO 9912517 A1 WO9912517 A1 WO 9912517A1
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WO
WIPO (PCT)
Prior art keywords
weight
alkali metal
pyrophosphate
teeth
composition
Prior art date
Application number
PCT/US1998/018309
Other languages
English (en)
Inventor
Michael Cash
Gregory Davis
Indrajit Desai
Geoffrey C. Forward
Teresa Layer
Peter S. Mcconville
Original Assignee
Smithkline Beecham Corporation
Smithkline Beecham Plc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Smithkline Beecham Corporation, Smithkline Beecham Plc filed Critical Smithkline Beecham Corporation
Priority to AU93009/98A priority Critical patent/AU9300998A/en
Publication of WO1999012517A1 publication Critical patent/WO1999012517A1/fr

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Classifications

    • 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
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/81—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
    • A61K8/817—Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by a single or double bond to nitrogen or by a heterocyclic ring containing nitrogen; Compositions or derivatives of such polymers, e.g. vinylimidazol, vinylcaprolactame, allylamines (Polyquaternium 6)
    • A61K8/8176—Homopolymers of N-vinyl-pyrrolidones. Compositions of derivatives of such polymers
    • 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
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/24—Phosphorous; Compounds thereof
    • 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
    • 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
    • A61Q11/02—Preparations for deodorising, bleaching or disinfecting dentures
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/59—Mixtures

Definitions

  • This invention relates to an oral hygiene composition and methods for whitening of and preventing staining on natural teeth and dental prostheses.
  • the whitening is achieved through the use of an alkali metal tripolyphosphate at about between 0.5 to 10 percent by weight in combination with at least one alkali metal pyrophosphate salt at about 0.1 to 10 percent by weight.
  • Whitening and stain- prevention are achieved through the use of an alkali metal tripolyphosphate at about between 0.5 to 10 percent by weight in combination with at least one alkali metal pyrophosphate salt at about 0.1 to 10 percent by weight, and polyvinyl pyrrolidone ("PVP") at about 0.1 to 10 percent by weight in a dentally acceptable carrier. Any orally acceptable presentation, or one suitable for dental prostheses, can be utilized in this invention.
  • Over-the-counter teeth whitening preparations have been developed to address the cosmetic preference of many to restore luster to tooth enamel discolored by surface entrapped materials. While all dentifrices and mouthwashes contain some cleaning and polishing agents, some enamel deposits become intractable to being fully removed by these agents under normal use conditions. Also, these preparations may not be formulated with the amount or type of agent required to fully remove the amount of stains and discoloration which build up due to excessive exposure to various staining agents. For example, smokers often develop discolored enamel because the tars and particulate in exhaled cigarette smoke collect on the teeth. Further, a number of comestibles, such as tea, or some medicinal agents, can stain or discolor tooth enamel.
  • Harsher abrasives also known as polishing agents, than those used in typical non-whitening toothpaste preparations, are employed in this approach. Most, if not all of these preparations are toothpastes, gels or powder dentifrices. Brushing or similar scrubbing or polishing action is required as a complement to successful stain removal. Examples of such products are Smokers Topol made by Topol-Dep Corporation and marketed to smokers and tea drinkers as a means for removing stains caused thereby.
  • Oxidizing agents represent one of the most widely distributed and utilized agent in oral preparations; all of these products being pastes or gels. Urea peroxide, hydrogen peroxide or calcium peroxide are the most commonly used oxidizing agents in these products. These treatments require some time to achieve good results; typically one and one-half to eight days, or two to three months, depending on the peroxide source and its concentration.
  • Proteolytic enzymes are the catalyst of choice, particularly papain.
  • a second active such as a citric acid salt has been used by at least one manufacturer.
  • These products are presented in a paste or gel formulation. The products are claimed to whiten teeth by removing the plaque which has entrapped the stain.
  • European Patent Application EP 248936A discloses a cleaning tablet for dentures comprising two layers, each with a different composition, characterized by a change in the pH from acidic to alkaline during the dissolving process of the tablet in water.
  • the first layer contains 25-35% NaHCO3 as the carbon dioxide producing agent, and, inter alia, 3-15% disodium pyrophosphate.
  • the second layer contains 25-45% sodium perborate monohydrate, 25-35% potassium monopersulphate as an oxidzing agent, and mter alia, 7-18% sodium tripolyphosphate.
  • the advantage asserted is that the tablet shows a characteristic pH swing from acidic to alkaline and a greater generation of oxygen than commercially available two-phase tablets.
  • the advantage of this particular formulation is alleged to be that the astringent taste of the pyrogenic silica is effectively suppressed, providing a dentifrice with a good mouth feel.
  • U.S. Patent 4,913,895 issued April 3, 1990, to Lion Corp., discloses an oral hygiene composition alleged to have a synergistic antibacterial effect against Actinomyces viscosus, a plaque-forming bacteria causing calculus formation and periodontal disease.
  • the composition contains 0.1 to 10% by weight of component
  • PCT/US94/09185 published February 23, 1995, relates to a composition for whitening teeth and dentures containing sodium tripolyphosphate and a reducing agent such as Vitamin C.
  • PCT/US94/14662 published June 29, 1995, relates to a composition for whitening teeth and dentures containing STP alone; STP combined with peroxides; STP combined with enzymes (papain); and STP combined with peroxides and enzymes.
  • U.S. Patent 5,538,714 issued July 23, 1996, to Pink et al., describes a method of reducing the adherence of oral bacteria to tooth enamel comprising applying to the tooth enamel a composition containing an anti-adherence effective amount of PVP.
  • GB 739,936, published November 2, 1955 discloses compositions containing both chlorophyll and water-soluble polyvinyl pyrrolidone for inhibiting or preventing the formation of greenish stains associated with chlorophyll on certain absorbant materials such as cellulose, animal and synthetic fibers.
  • GB 741,315, published November 30, 1955, discloses dentifrices containing polyvinyl pyrrolidone as a stain remover, particularly for tar-like stains.
  • Calculus is a deposit, comprising an organic and an inorganic portion, forming on the surfaces of teeth at the gingival margin.
  • the inorganic portion consists mainly of calcium phosphate arranged in a hydroxy-apatite crystal lattice structure, whereas the organic portion consists of desquamated epithelial cells, leukocytes, food debris and various types of microorganisms. As the calculus develops it becomes visibly white or yellowish in color or it may become stained by some extraneous agency.
  • This invention provides a unique alternative to tooth whitening and stain prevention. It utilizes an alkali metal tripolyphosphate salt in combination with at least one alkali metal pyrophosphate salt, and PVP, to effect stain removal, whiten tooth enamel, and prevent future staining of the teeth. If tooth whitening or the removal of stains from teeth are desired alone, without the prevention of stain buildup, a useful composition of the invention is an alkali metal tripolyphosphate salt in combination with at least one alkali metal pyrophosphate salt.
  • the use of one or more of an alkali metal pyrophosphate in combination with sodium tripolyphosphate showed significant increases in whitening effect over the whitening effect of sodium tripolyphosphate when used alone as a whitening agent.
  • the use of one or more of an alkali metal pyrophosphate in combination with sodium tripolyphosphate and PVP showed significant increases in stain prevention and whitening effect over the whitening effect of sodium tripolyphosphate when used alone as a whitening agent.
  • compositions for preventing, reducing or removing surface deposited stains from natural teeth and dental prostheses comprising a dentally acceptable preparation comprising about 1 to 10% by weight of a water soluble alkali metal tripolyphosphate in combination with about 0.5 to 10% by weight of at least one alkali metal pyrophosphate salt and about 0.1 to 10% by weight of PVP.
  • this invention relates to a method for preventing, reducing or removing surface deposited stains from natural teeth and dental prostheses which method comprises contacting teeth or dental prostheses with a whitening effective amount of the instant dentally acceptable composition, in particular, a composition comprising at least about 1 to 10% by weight of a water soluble alkali metal tripolyphosphate in combination with about 0.5 to 10% by weight of at least one alkali metal pyrophosphate salt and about 0.1 to 10% by weight of PVP.
  • This invention also comprises compositions and a method for whitening or removing surface deposited stains from natural teeth and dental prostheses comprising contacting the teeth or dental prostheses with a dentally acceptable preparation comprising about 1 to 10% by weight of a water soluble alkali metal tripolyphosphate in combination with about 0.5 to 10% by weight of at least one alkali metal pyrophosphate salt.
  • Fig. 1 and Fig. 1 A depict graphically a comparison of the increase in L value obtained with varying concentrations of a combination of disodium pyrophosphate and sodium tripolyphosphate versus sodium tripolyphosphate alone.
  • Fig. 2 and Fig. 2A depict graphically a comparison of the increase in L value obtained with varying concentrations of a combination of tetrapotassium pyrophosphate and sodium tripolyphosphate versus sodium tripolyphosphate alone.
  • Fig. 3 depicts graphically an increase in L value obtained with a combination of sodium tripolyphosphate and disodium pyrophosphate compared with the increase in L value of sodium tripolyphosphate alone and disodium pyrophosphate alone.
  • Figs. 4-8 depict, in chart format, the data used to prepare Figs. 1, 1A, 2 and 2A.
  • Fig. 9 depicts data obtained from a stain prevention study to determine the stain-preventing properties of various toothpastes and solutions.
  • Fig. 10 depicts data from a soaking study to examine whitening effects of various formulations.
  • alkali metal pyrophosphate salts in particular, tetrasodium pyrophosphate and tetrapotassium pyrophosphate each in combination with sodium tripolyphosphate ("STP"), are highly effective whitening agents.
  • STP sodium tripolyphosphate
  • PVP is a highly effective stain prevention agent, particularly when used in a toothpaste matrix which gives suprisingly better stain prevention results than when compared with PVP in solution.
  • an oral composition purported to be effective in inhibiting or retarding the formation of dental calculus without adversely affecting tooth structure
  • the composition comprises from 0.5 to 10% by weight of an alkali metal pyrophosphate salt in combination with from about 1 to 10% by weight of an alkali metal tripolyphosphate and a carrier suitable for use in the oral cavity, the pH being in the range from 6.5 to 10.
  • stain or “staining” are used interchangeably with discoloration and generally mean that the surface of the enamel (or prostheses) has taken on some unwanted or unnatural coloration distinct from the color of the underlying enamel.
  • stain removal is used herein to mean removing stain which is periodically deposited on the tooth surface. Stain removal is effectuated by the whitening agents of this invention, i.e., STP and the alkali metal pyrophosphates, which in combination give enhanced whitening results when compared with STP alone.
  • stain prevention is used herein to mean inhibit or reduce the build-up of stain on the tooth surface.
  • PVP is a known complexing/sequestering agent for tannins. Tannins from various food sources causes staining of teeth. PVP, in a toothpaste matrix with a detergent such as sodiumlaurylsulfate (SLS), forms a film on the tooth surface and is thus retained on the tooth. Therefore, by using the inventive composition, and contacting the tooth surface therewith, stains introduced into the oral cavity might actually be sequestered by the PVP remaining as a film on the tooth surface, and not adhere to the tooth surface. As the PVP is sloughed-off the tooth surface, the sequestered stain is taken with it.
  • SLS sodiumlaurylsulfate
  • One active component of this invention comprises a water soluble alkali metal tripolyphosphate.
  • the sodium form of this salt is preferred, although the potassium or mixed sodium and potassium salts could be used as an embodiment as well. All physical forms of the salt can be used, e.g., a hydrate or the dehydrated form. STP is available from Monsanto Corp. or Sigma Chemical.
  • tripolyphosphate salt will be between about 0.5 and 10% by weight of the preparation.
  • a preferred amount of said salt is between about 5% and 7.5% by weight.
  • a composition for use in whitening human teeth and dental prostheses comprising tetrasodium pyrophosphate, tetrapotassium pyrophosphate, STP and PVP.
  • a composition for use in preventing stain build-up on human teeth and dental prostheses comprising tetrasodium pyrophosphate, tetrapotassium pyrophosphate, STP and PVP.
  • a composition for use in whitening human teeth and dental prostheses comprising at least one alkali metal pyrophosphate and STP.
  • the disodium pyrophosphate salt (available from Monsanto Corp. or Sigma Chemical, and also known as disodium dihydrogen pyrophosphate) is incorporated into the formulation in the range between about 0.1 and 10% by weight of the preparation, suitably between about 0.75 and 10% by weight, preferably between about 2.0 and 6.0% by weight, and most preferably about 1.0 to 2.0% by weight.
  • Disodium pyrophosphate in combination with STP is a preferred whitening composition.
  • a particularly preferred whitening composition of the invention comprises about 1.0 to 2.0% disodium pyrophosphate and 5 to 7.5% STP.
  • the tetrasodium pyrophosphate salt (available from Monsanto Corp. or Sigma Chemical) is incorporated into the formulation in the range between about 0.1 and 10% by weight of the preparation, suitably between about 0.75 and 10% by weight, preferably between about 0.75 and 4.0% by weight, and most preferably about 0.75 to 2.0% by weight.
  • the tetrapotassium pyrophosphate salt (available from FMC Corporation, and also known as tetrapotassium salt diphosphoric acid) is incorporated into the formulation in the range between about 0.1 and 10% by weight of the preparation, preferably 1.0 and 10% by weight, more preferably between about 1.0 and 4.0% by weight, and most preferably between 1.0 and 3.0% by weight.
  • a particularly preferred whitening composition of the invention comprises about 3.0 to 4.0% tetrapotassium pyrophosphate and 5 to 7.5% STP.
  • PVP suitable for use in the present invention preferably has an average molecular weight in the range 5,000 to 100,000.
  • a suitable grade of PVP with an average molecular weight of 50,000 is available commercially from BASF Corporation and is known as Povidone K30.
  • PVP is incorporated into the formulation in the range between about 0.1 to 10% by weight, preferably between about 0.5 to 5.0% by weight and most preferably between about 0.5 to 2.0% by weight.
  • the alkali metal pyrophosphate salt portion of the instant composition can be either a single pyrophosphate salt, or a combination of pyrophosphate salts.
  • a particularly preferred composition of the invention comprises about 0.75 to 2.0% tetrasodium pyrophosphate, 1.0 to 3.0% tetrapotassium pyrophosphate, 5 to 7.5% STP and 0.5 to 2.0% PVP.
  • the most preferred embodiment of this invention comprises about 2% tetrapotassium pyrophosphate, 0.91 % tetrasodium pyrophosphate, 5% STP and 1% PVP.
  • the whitening and stain preventing compositions may be presented in any of the conventional formulations such as a dentifrice, including a toothpaste, a mouthwash or a formulation that is chewed or sucked by the user such as a lozenge or a chewing gum. These formulations will be presented so that they are safe for use in the oral cavity and will not have a deleterious effect if accidentally swallowed.
  • the oral care art has developed a substantial body of formulation types and has identified and tested a large list of ingredients useful in these formulations. Confecting or manufacturing these preparations, and their safe packaging and storage is also well documented.
  • the formulation as used should have a pH of between about 7.0 to 9.0.
  • Optimum cleaning results are achieved with a pH of about 8 with reference to how the formulation is used for brushing teeth in the mouth.
  • a toothpaste preparation will usually be diluted in the mouth by about 1 plus 2 or 1 plus 3 volumes of water/saliva while brushing.
  • a paste or gel for example, optimized for whitening will be formulated to achieve a pH between about 7 and 9 when it is being actually used to brush or treat teeth.
  • An acid or base may be used to adjust the pH of the preparation; the choice is within the skill of the art concerned with oral preparations.
  • formulations for toothpastes, liquid pastes, gels and toothpowders suitable for this invention will contain the usual carriers, binders, surfactants, humectants, coloring agents, pigments, antiplaque agents, anti-bacterial agents, bioadhesive-type agents, abrasives, anticaries agents, flavorings, sweeteners, bulking agents, and the like.
  • Suitable abrasives for use in the present invention include precipitated silica, plastics particles, alumina, calcium carbonate, and zinc orthophosphate, insoluble metaphosphates and calcium pyrophosphate. Pyrogenic silicas are not claimed as a useful silica for the instant invention. Silica is an especially preferred abrasive for use herein.
  • Silica abrasives are well known and commercially available, generally having an average particle size ranging between about 0.1 to about 30 microns, such as from about 5 to about 15 microns.
  • Silica dental abrasives useful in the present invention include those marketed by the J.M. Huber Corporation under the trade name ZeofreeTM (Zeodent 113) and the silica xerogels marketed by the W.R. Grace and Company, Davison Chemical Division under the trade name 'Syloid'.
  • ZeofreeTM ZeofreeTM
  • U.S. Patent 3,358,230 and U.S. Patent 3,862,307 describe silica dental abrasives useful in the toothpaste compositions according to the present invention.
  • the silica abrasive may also be a naturally occurring amorphous silica such as diatomaceous earth. Suitable forms of diatomaceous earth are those marketed under the trade mark 'Celite' by Johns-Manville Products Corporation, for instance 'Celite Superfine Superfloss'.
  • the selected abrasive should be compatible with the phosphate actives, as well as any additives which may be actives as well, such as fluoride ions and antibacterial agents.
  • the selection of an abrasive can be influenced by the consequence of combining a particular abrasive with another additive. For example, if fluoride ions and calcium pyrophosphate ions are to be included in these preparations the pyrophosphate should be converted from its ⁇ -phase to its ⁇ -phase by heating the ⁇ -phase to 700°- 900°C as per the teachings of U.S. Patent 3,112,247. Also certain quaternary ammonium-based antibacterial agents may not be compatible with some silica abrasives.
  • Plastics dental abrasives are well known and are described in, for example, GB 939 230, GB 995 351, GB 1 055 784, and U.S. Patent 3,151,027.
  • Alumina abrasives are well known and commercially available.
  • the alumina abrasive may be treated with a solution of a surface-treating agent which may be an alkali metal silicate, hydrogen peroxide, an acid or an organophosphorus compound, of which an alkali metal silicate is especially preferred, as described in U.S. Patent 4,781,982 (to Aluminum Company of America).
  • a calcium carbonate abrasive is preferably used in conjunction with an ionic agent to suppress the formation of free calcium ions, such as an alkali metal carbonate or bicarbonate, or mixture thereof, as described in EP 0092 929 (to Beecham Group p.l.c).
  • Abrasive concentrations can cover a very broad range.
  • abrasive ranging in concentration from 5 to 80% by weight depending on the abrasive.
  • a secondary concentration range is that of 10 to 50% depending on the abrasive selected.
  • silica is employed in amounts between 5 and 30% by weight.
  • a source of fluoride ion may be included in the instant composition.
  • Fluoride ion sources are numerous. For example, see U.S. Patent 3,535,421 listing numerous salts useful in the dental arts. While any one of these sources could be used, sodium fluoride, stannous fluoride and sodium monofluorophosphate are considered the preferred ion sources in most dentifrices. Fluoride ions are routinely added into dentifrices in an amount sufficient to provide up to 3500 ppm, preferably 1100 ppm of the fluoride ion.
  • the fluoride ion source should be adjusted upward in an amount sufficient to provide a concentration of up to about 3500 ppm, but preferably 1100 ppm, in the product as used.
  • the orally acceptable vehicle may comprise other components such as, flavorings, coloring agents, sweeteners, humectants, thickening agents, binders and surfactants. Binders and thickening agents can be added to assure physical integrity in pastes, gels and liquid pastes.
  • Preferred thickening and binding agents include for example natural and synthetic gums such as xanthan and acacia gums, carageenans, alginates, cellulose ethers and esters such as carboxy methyl cellulose, polyoxyalkyl polymers such as the Pluronics polymers, certain polymers exemplified by the carboxy vinyl polymers (Gantrez and the like), and silica.
  • a thickening silica is ZeofreeTM 153, which is a precipitated synthetic amorphous silica.
  • Binders are usually added in amounts ranging between 0.1 and 5.5% by weight.
  • Humectants are added to gels and pastes to prevent their drying out on exposure to air. In addition, they impart a "moist" feel to the mouth when brushing. Some humectants, e.g., sorbitol, are perceived as sweet. Examples of compounds useful as humectants in dentifrices are the polyhydric alcohols such as glycerin, sorbitol, propylene glycol and polyethylene glycols. A preferred humectant system consists of glycerin, sorbitol (usually 70% sorbitol/water) and polyethylene glycol, which is present in an amount of about 25-45%, preferably 37-40% of the total composition. In pastes and gels one to three humectants are usually used in amounts between about 10 and 80%. Preferably the humectants are used in amounts between about 20 and 50% of the total composition.
  • the orally acceptable vehicle may optionally comprise surfactants, sweetening agents, flavoring agents, anticaries agents (in addition to a fluoride ion source provided as a phosphatase enzyme inhibitor), anti-plaque agents, anti-bacterial agents such as triclosan or cetyl pyridinium chloride, tooth desensitizing agents, coloring agents and pigments.
  • Surfactants normally are added to dentifrices to assist with removing debris.
  • Useful surfactants include the water-soluble salts of alkyl sulfates having from 10 to 18 carbon atoms in the alkyl moiety, such as sodium lauryl sulfate, but other anionic surfactants may also be used, e.g., non-ionic, zwitter-ionic, cationic and amphoteric surfactants. These compounds, and those which are most useful in the dental arts, are well documented in the literature. Reference is made to U.S. Patent 4,822,599 for a detailed listing of useful surfactants. Surfactants are available through a number of commercial manufacturers or can be made by well documented processes.
  • Surfactants are normally used in amounts between about 0.5 and 5% by weight in pastes and gels but may be used at higher concentrations in some dental powders. Surfactants can also be used as gelling agents. Taste is provided by adding a small amount of a flavoring agent to the composition. Numerous minty flavored agents are available for use in dentifrices. It is well known in the art how to select a flavoring agent which will be acceptable to consumers. Flavoring agents are routinely used at levels of between about 0.1 to 5% by weight. Dyes, lakes and titanium dioxide are routinely used in the dentifrice arts for imparting color to the composition. When titanium dioxide is the coloring agent, a white paste or powder is obtained. These materials are widely available and are well known to the dental artisan.
  • Coloring agents are usually present in concentrations ranging between 0.0001 and 5%.
  • Sweeteners are routinely added to increase consumer acceptability. Artificial sweeteners are used today to avoid the cariogenic potential of most sugars and other sweetening agents. Examples of non-cariogenic sweeteners now in routine use are saccharin, aspartame, D-tryptophan, dihydrochalcones, cyclamates, xylitol and acesulfame.
  • Sweeteners comprise about 0.1 to 5% by weight of the formulation. Appliques can provide an effective means for removing stains as per this invention. These can be prepared in the form of a doughy or tacky material which can be readily molded to conform to the teeth.
  • the active(s) can be formulated as a mouthwash or mouth rinse as well.
  • a mouth wash or rinse will contain up to 95% water, up to 30 % alcohol, flavor, polyhydric alcohols, anti-caries agents, plaque removing agents, sweeteners, dyes and lakes, and a preservative in some instances, and sufficient water to make volume.
  • the active could also be incorporated into currently existing formulations such as Cepacol (Lakeside Pharmaceuticals), Plax, (Pfizer), Scope (Procter & Gamble), and the like.
  • a soaking and cleaning solution for dental pieces can also be prepared with the combination of active ingredients. It is contemplated that such preparations would contain water, a surfactant, an effervescing agent, and other optional ingredients. Dental prostheses would be removed and placed in a solution containing the tripolyphosphate salt and pyrophosphate salt, and soaked for several hours, then either brushed with a recommended dentifrice or simply rinsed and reinserted into the mouth.
  • a toothpaste composition of the present invention suitably contains from about 10 to about 80% humectant, from about 0.25 to about 5% detergent, from 0 to about 5% sweeteners and flavoring agents together with water and an effective amount of binding and thickening agents, such as from about 0.1% to about 12%, to provide the toothpaste of the invention with the desired stability and flow characteristics.
  • Conventional manufacturing techniques are employed to prepare a whitening toothpaste with the inventive active combination.
  • Toothpaste compositions of the present invention may also be prepared in the form of a clear gel or a paste of a uniform color or in the form of a striped toothpaste. A suitable apparatus for filling toothpaste tubes with striped toothpaste is described in GB 962 757.
  • toothpastes of different colors are fed through separate tubes of a bundle of tubes that is inserted into a toothpaste container and gradually moved relative to the container as the container is filled.
  • the toothpaste of the invention is used in a conventional manner by applying the toothpaste to the teeth.
  • Most dentists and researchers recommend brushing one's teeth for at least three minutes per brushing to achieve maximum results, although compliance with this standard is not universal.
  • a similar standard is recommended for the instant pastes and gels, although it is expected that non-compliance will still provide the desired results with regular use, i.e., daily use.
  • Example 1 Formulation of Tooth Whitening/Stain-Preventing Toothpaste A whitening and stain-preventing toothpaste representative of what may be prepared for the practice of this invention was prepared as per the ingredient profile and percentages in Tables I and ⁇ .
  • Example 2 Formulation of Tooth Whitening Toothpaste A whitening toothpaste representative of what may be prepared for the practice of this invention was prepared as per the ingredient profile and percentages in Tables III and IV.
  • Example 5 & 6 Formulation of Whitening Gum A whitening gum representative of what may be prepared for the practice of this invention was prepared as per the ingredient profile and percentages in Tables Ul and lV.
  • Tooth whitening was measured by the following soaking experiment procedure:
  • Bovine teeth were sourced from abattoirs. They were cut from jaws and sorted and selected to have initial L-values between 50 and 75 by comparison with standards provided. The teeth were immediately placed in thymol /water (1 to 100) and after shipment stored in a fridge.
  • the teeth were de-pulped with the help of a stainless steel barb, made by the Beutelrock Company, and purchased through Victor Dental of Clifton, NJ.
  • a barb was inserted into the base of the tooth, twisted, and the pulp pulled out when the barb was removed. (Note: it may require several tries for complete removal).
  • Jet acrylic powder and Jet acrylic liquid, made by Lang Dental Manufacturing
  • plastic 100 mL beakers plastic 100 mL beakers
  • bottle (mounting) caps each 3.5 cm in diameter by 1.5 cm deep
  • stainless steel spatula The acrylic was stored in the freezer along with plastic beakers.
  • a beaker was taken out of the freezer, into which 9.0 grams of acrylic powder was weighed. To the powder was added 3.1 mL of acrylic liquid. The mixture was stirred until uniform. Do not over-stir, as this causes the acrylic to set- up prematurely. This mixture was divided into four mounting caps and packed down using a stainless steel spatula.
  • Example 7 Efficacy of an STP/DP Combination in an In-Vitro Stain Model
  • STP alkali metal tripolyphosphate
  • DP sodium dihydrogen pyrophosphate
  • the teeth were washed with demonized water and allowed to air dry prior to being mounted into Ecotrin lids using an acrylic polymer, such as jet acrylic powder and jet acrylic liquid from Lang Dental Manufacturing.
  • the teeth were mounted in the center of the lid such that the front of each individual tooth was exposed without there being any resin on the tooth surface.
  • the mounted teeth were stored in a desiccator which had a relative humidity of 100%.
  • the teeth Prior to use, the teeth were removed from the desiccator and allowed to air dry for 45 minutes. The teeth were numbered and then scribed so as to identify, for measurement purposes, ten equal positions on each tooth surface. The presoak L values (average of ten readings per tooth) were determined using a colorimeter (Hunter Labs).
  • the teeth were arranged five per cell, so that teeth having similar L value averages were located in the same cell. This ensured that there was a similar baseline for each solution measured.
  • the teeth were then stored in test solutions for various time points, typically
  • Test solutions comprising STP (Monsanto Corp.) (1.25% w/w), DP (Albright & Wilson) (2% w/w) and STP/DP (1.25/2% w/w, respectively) were prepared in USP grade water. The pH of the test solutions were adjusted to pH 9 with sodium hydroxide.
  • Figs. 1, 1A, 2, 2A and 3 The results of the soaking studies are graphically illustrated in Figs. 1, 1A, 2, 2A and 3. Based upon these results, preferred embodiments of this invention are a composition with about 1.0 to 2.0% disodium pyrophosphate and 5 to 7.5% STP, or a composition with about 3.0 to 4.0% tetrapotassium pyrophosphate and 5 to 7.5% STP.
  • Fig. 10 supports the conclusion that formulation A is a preferred embodiment for a whitening and stain preventing dentifrice. Each of these particular compositions achieves maximum whitening, above that achieved by a composition with 10% STP alone as the whitening agent.
  • the color of the human enamel substrate was measured using a Minolta chromameter.
  • the substrate was then subjected to the following treatment cycle:
  • DI is used herein to mean deionized water
  • This cycle was repeated 7 times in total; the substrate color was then rerecorded using the Minolta chromameter.
  • Fig. 9 Changes in color of the human substrate were calculated by subtracting initial chromameter readings from final chromameter data.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Cosmetics (AREA)

Abstract

Cette invention a trait à des compositions visant à empêcher la formation de taches et à blanchir les dents ainsi que les prothèses dentaires. Ces compositions renferment un sel tripolyphosphate de métal alcalin hydrosoluble associé à un sel pyrophosphate de métal alcalin et, éventuellement, de la pyrrolidone polyvinylique.
PCT/US1998/018309 1997-09-09 1998-09-03 Preparations permettant de blanchir les dents WO1999012517A1 (fr)

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AU93009/98A AU9300998A (en) 1997-09-09 1998-09-03 Tooth whitening preparations

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US5831897P 1997-09-09 1997-09-09
US5831597P 1997-09-09 1997-09-09
US60/058,315 1997-09-09
US60/058,318 1997-09-09
US7807198P 1998-03-16 1998-03-16
US60/078,071 1998-03-16

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Cited By (24)

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US6500408B2 (en) * 2001-01-27 2002-12-31 Jc Technologies, Inc. Enamel-safe tooth bleach and method for use
KR100383918B1 (ko) * 2000-09-15 2003-05-14 주식회사 엘지생활건강 치아 미백용 코팅제
US6682722B2 (en) 2001-09-19 2004-01-27 The Procter & Gamble Company Oral compositions providing enhanced overall cleaning
US6702999B2 (en) 2001-05-15 2004-03-09 The Procter & Gamble Co. Oral care compositions
US6706277B2 (en) 2001-05-15 2004-03-16 The Procter & Gamble Company Confectionery compositions
US6726897B2 (en) 2001-05-15 2004-04-27 The Procter & Gamble Co. Confectionery compositions
WO2005058264A1 (fr) * 2003-12-08 2005-06-30 Cadbury Schweppes Plc Composition de confiserie solide et orale de blanchiment des dents
WO2010068474A2 (fr) 2008-11-25 2010-06-17 The Procter & Gamble Company Compositions d'hygiène bucco-dentaire contenant de la silice fondue
EP2415473A1 (fr) 2006-11-10 2012-02-08 The Procter & Gamble Company Compositions d'hygiène buccale contenant des combinaisons d'agents antibactériens et de modulation de réponse hôte
CN102369013A (zh) * 2009-04-02 2012-03-07 高露洁-棕榄公司 包含焦磷酸四钾的口腔护理组合物
WO2014071284A2 (fr) 2012-11-05 2014-05-08 The Procter & Gamble Company Silice précipitée traitée thermiquement
EP2734194A1 (fr) * 2011-07-20 2014-05-28 Ranir LLC Formulations de soin buccal
EP2099416A4 (fr) * 2006-12-22 2015-05-27 Douglas Anderson Composition dentaire anti-tartre et son procédé d'utilisation
US9326924B1 (en) 2015-02-26 2016-05-03 Johnson & Johnson Consumer Inc. Compositions comprising combinations of organic acids
US9326925B1 (en) 2015-02-26 2016-05-03 Johnson & Johnson Consumer Inc. Compositions comprising combinations of organic acids
EP3017806A1 (fr) 2014-11-04 2016-05-11 The Procter and Gamble Company Compositions de soins bucco-dentaires anti-tartre fournissant une prévention contre la cristallisation
EP3017807A1 (fr) 2014-11-04 2016-05-11 The Procter and Gamble Company Compositions de soins bucco-dentaires anti-tartre fournissant une prévention contre la cristallisation
WO2016138217A1 (fr) 2015-02-26 2016-09-01 Johnson & Johnson Consumer Inc. Compositions comprenant des combinaisons d'acides organiques
WO2019112868A1 (fr) 2017-12-07 2019-06-13 Johnson & Johnson Consumer Inc. Composition de soins buccaux
US20190175478A1 (en) * 2017-12-13 2019-06-13 Colgate-Palmolive Company Dentifrice Comprising Zinc - Amino Acid Complex
WO2019112869A1 (fr) 2017-12-07 2019-06-13 Johnson & Johnson Consumer Inc. Compositions de soins buccodentaires
WO2019145794A1 (fr) * 2018-01-24 2019-08-01 Basf Se Composition de soin buccal anti-taches
US20220143073A1 (en) * 2020-11-12 2022-05-12 Ariel Lenharo Oral compositions for post-dental implants
US11471388B2 (en) 2018-11-07 2022-10-18 The Procter & Gamble Company Oral care compositions comprising medium length polyphosphates

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EP0397452A2 (fr) * 1989-05-08 1990-11-14 Beecham Inc. Compositions dentifrices contre le tartre possédant une longue durée de conservation
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WO1997045096A1 (fr) * 1996-05-31 1997-12-04 Smithkline Beecham Corporation Compositions

Cited By (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100383918B1 (ko) * 2000-09-15 2003-05-14 주식회사 엘지생활건강 치아 미백용 코팅제
US7862801B2 (en) 2001-01-27 2011-01-04 Ultradent Products, Inc. Adhesive dental bleaching compositions comprising polyvinylpyrrolidone
US9782338B2 (en) 2001-01-27 2017-10-10 Ultradent Products, Inc. Adhesive dental bleaching compositions containing polyvinylpyrrolidone
US7128899B2 (en) 2001-01-27 2006-10-31 Ultradent Products, Inc. Bleaching device comprising a barrier layer and a bleaching composition comprising polyvinylpyrrolidone
US8852560B2 (en) 2001-01-27 2014-10-07 Ultradent Products, Inc. Adhesive dental bleaching compositions containing polyvinylpyrrolidone
US6500408B2 (en) * 2001-01-27 2002-12-31 Jc Technologies, Inc. Enamel-safe tooth bleach and method for use
US6702999B2 (en) 2001-05-15 2004-03-09 The Procter & Gamble Co. Oral care compositions
US6706277B2 (en) 2001-05-15 2004-03-16 The Procter & Gamble Company Confectionery compositions
US6726897B2 (en) 2001-05-15 2004-04-27 The Procter & Gamble Co. Confectionery compositions
US6682722B2 (en) 2001-09-19 2004-01-27 The Procter & Gamble Company Oral compositions providing enhanced overall cleaning
CN1303969C (zh) * 2001-09-19 2007-03-14 宝洁公司 提供增强的整体清洁效果的口腔组合物
CN1889917B (zh) * 2003-12-08 2010-08-11 吉百利控股有限公司 固体口用牙齿增白糖果组合物
US8388938B2 (en) 2003-12-08 2013-03-05 Cadbury Holdings Limited Solid oral tooth whitening confectionary composition
WO2005058264A1 (fr) * 2003-12-08 2005-06-30 Cadbury Schweppes Plc Composition de confiserie solide et orale de blanchiment des dents
EP2415473A1 (fr) 2006-11-10 2012-02-08 The Procter & Gamble Company Compositions d'hygiène buccale contenant des combinaisons d'agents antibactériens et de modulation de réponse hôte
EP2099416A4 (fr) * 2006-12-22 2015-05-27 Douglas Anderson Composition dentaire anti-tartre et son procédé d'utilisation
WO2010068474A2 (fr) 2008-11-25 2010-06-17 The Procter & Gamble Company Compositions d'hygiène bucco-dentaire contenant de la silice fondue
EP2995351A1 (fr) 2008-11-25 2016-03-16 The Procter and Gamble Company Compositions de soin buccal anti-sensibilité contenant de la silice fondue
CN102369013A (zh) * 2009-04-02 2012-03-07 高露洁-棕榄公司 包含焦磷酸四钾的口腔护理组合物
EP2734194A1 (fr) * 2011-07-20 2014-05-28 Ranir LLC Formulations de soin buccal
EP2734194A4 (fr) * 2011-07-20 2015-04-22 Ranir Llc Formulations de soin buccal
WO2014071284A2 (fr) 2012-11-05 2014-05-08 The Procter & Gamble Company Silice précipitée traitée thermiquement
WO2016073535A1 (fr) 2014-11-04 2016-05-12 The Procter & Gamble Company Compositions anti-tartre pour soins bucco-dentaires destinées à prévenir la cristallisation
EP3017806A1 (fr) 2014-11-04 2016-05-11 The Procter and Gamble Company Compositions de soins bucco-dentaires anti-tartre fournissant une prévention contre la cristallisation
EP3017807A1 (fr) 2014-11-04 2016-05-11 The Procter and Gamble Company Compositions de soins bucco-dentaires anti-tartre fournissant une prévention contre la cristallisation
WO2016073534A1 (fr) 2014-11-04 2016-05-12 The Procter & Gamble Company Compositions anti-tartre pour soins bucco-dentaires destinées à prévenir la cristallisation
US9872491B2 (en) 2015-02-26 2018-01-23 Johnson & Johnson Consumer Inc. Compositions comprising combinations of organic acids
WO2016138217A1 (fr) 2015-02-26 2016-09-01 Johnson & Johnson Consumer Inc. Compositions comprenant des combinaisons d'acides organiques
WO2016138211A1 (fr) 2015-02-26 2016-09-01 Johnson & Johnson Consumer Inc. Compositions comprenant des combinaisons d'acides organiques
US9326924B1 (en) 2015-02-26 2016-05-03 Johnson & Johnson Consumer Inc. Compositions comprising combinations of organic acids
US9326925B1 (en) 2015-02-26 2016-05-03 Johnson & Johnson Consumer Inc. Compositions comprising combinations of organic acids
WO2016138214A1 (fr) 2015-02-26 2016-09-01 Johnson & Johnson Consumer Inc. Compositions comprenant des combinaisons d'acides organiques
WO2019112869A1 (fr) 2017-12-07 2019-06-13 Johnson & Johnson Consumer Inc. Compositions de soins buccodentaires
WO2019112868A1 (fr) 2017-12-07 2019-06-13 Johnson & Johnson Consumer Inc. Composition de soins buccaux
US20190175478A1 (en) * 2017-12-13 2019-06-13 Colgate-Palmolive Company Dentifrice Comprising Zinc - Amino Acid Complex
CN111432784A (zh) * 2017-12-13 2020-07-17 高露洁-棕榄公司 包含锌-氨基酸络合物的洁齿剂
WO2019145794A1 (fr) * 2018-01-24 2019-08-01 Basf Se Composition de soin buccal anti-taches
CN111629708A (zh) * 2018-01-24 2020-09-04 巴斯夫欧洲公司 防牙渍口腔护理组合物
US12042555B2 (en) 2018-01-24 2024-07-23 Basf Se Anti-stain oral care composition
US11471388B2 (en) 2018-11-07 2022-10-18 The Procter & Gamble Company Oral care compositions comprising medium length polyphosphates
US20220143073A1 (en) * 2020-11-12 2022-05-12 Ariel Lenharo Oral compositions for post-dental implants
US11419889B2 (en) * 2020-11-12 2022-08-23 Ariel Lenharo Oral compositions for post-dental implants

Also Published As

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AU9300998A (en) 1999-03-29
AR015437A1 (es) 2001-05-02

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