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EP0675706A1 - Compositions de soins bucco-dentaires contenant des agents antiplaque et antitartre - Google Patents

Compositions de soins bucco-dentaires contenant des agents antiplaque et antitartre

Info

Publication number
EP0675706A1
EP0675706A1 EP94903459A EP94903459A EP0675706A1 EP 0675706 A1 EP0675706 A1 EP 0675706A1 EP 94903459 A EP94903459 A EP 94903459A EP 94903459 A EP94903459 A EP 94903459A EP 0675706 A1 EP0675706 A1 EP 0675706A1
Authority
EP
European Patent Office
Prior art keywords
zinc
compositions
ions
composition
oral
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP94903459A
Other languages
German (de)
English (en)
Inventor
Ronald Earl Montgomery
Joseph Wasyl Pyrz
Margaret Mary Coyle-Rees
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Procter and Gamble Co
Original Assignee
Procter and Gamble Co
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 Procter and Gamble Co filed Critical Procter and Gamble Co
Publication of EP0675706A1 publication Critical patent/EP0675706A1/fr
Withdrawn legal-status Critical Current

Links

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
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/27—Zinc; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/365—Hydroxycarboxylic acids; Ketocarboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

Definitions

  • the subject invention relates to oral compositions, such as dentifrices and oral solutions, for the treatment or prevention of dental plaque, calculus and gingivitis, and mouth malodor.
  • the mouth is a habitat for microbial growth and colonization.
  • the gums, lips, oral mucosa (cheek), palate, tongue and teeth provide surfaces for the colonization and accumulation of bacteria.
  • Teeth are unique in the oral cavity because they have hard, non-shedding surfaces where bacteria and their products (dental plaque) can significantly accumulate, especially in approximal areas and along the gingival crevice.
  • Dental plaque is a rough sticky film on the teeth that is made up of saliva, bacteria and food particles which adheres tenaciously to teeth at points of irregularity or discontinuity.
  • salivary mucins consisting primarily of proteins
  • Various oral bacteria colonize the mucins and multiply, forming a layer of plaque.
  • Carbohydrate food debris adheres to the mucins and is digested by some types of plaque- causing bacteria. The digestion both produces by-products which add to the plaque, and produces acid which erodes tooth enamel.
  • the bacterial by-products produced in the oral cavity also include foul smelling gases which can result in malodor of the oral cavity.
  • the oral bacteria in dental plaque includes many gram positive and gram negative microorganisms embedded in an extracellular matrix of insoluble polysaccharides, firmly attached to teeth and other oral surfaces.
  • the colonization of bacteria to form dental plaque follows an ecological pattern where a few pioneer aerobic species, mostly gram-positive streptococci, colonize enamel surfaces. The plaque then progresses through stages of increasing microbial complexity. Mature plaques, often found in protected regions of the teeth, such as cracks, approximal regions and in the gingival crevice, typically contain anaerobes. Saliva and crevicular fluid are a source of nutrients for the dental plaque. Local conditions affect the metabolic activity and composition of dental plaque.
  • plaque may become embedded with mineral salts, containing calcium and phosphate, to form a hard crusty deposit, calculus or tartar, on the teeth.
  • Calculus may be white or yellowish in color or may be stained or discolored by extraneous agents. Calculus tends to be more unsightly than plaque and much more difficult to remove from the teeth.
  • the toxins in plaque and calculus can irritate the gingival tissues surrounding the coated teeth, causing inflammation and destruction of the gums which can lead to other complications.
  • Zinc is an anticalculus agent; however, compositions containing zinc generally taste astringent and unknowingly bitter. Like the chemical and biological activities, the negative aesthetics of the zinc cation are dose dependent: higher concentrations of zinc exhibit poorer aesthetics; therefore, increasing the concentration of free zinc tends to increase efficacy at the expense of aesthetics. This coupled behavior between efficacy and aesthetics has limited the utility of zinc in oral compositions. Pyrophosphate is also an anticalculus agent and, likewise, has an unpleasant taste which worsens with increased pyrophosphate concentration. By carefully formulating zinc and pyrophosphate-containing compositions, applicants have surprisingly found that the level of zinc in an oral composition can be increased, thus increasing the corresponding anticalculus effect, without greatly increasing the negative aesthetics of the composition.
  • compositions for impeding calculus formation in the oral cavity It is an object of the subject invention to provide compositions for impeding calculus formation in the oral cavity. It is also an object of the subject invention to provide compositions for impeding dental plaque formation in the oral cavity. It is a further object of the subject invention to provide methods for impeding calculus formation in the oral cavity.
  • This invention involves a composition for treating or preventing dental plaque, calculus and gingivitis, or malodor of the oral cavity, comprising:
  • This invention also involves methods for treating or preventing dental plaque, calculus and gingivitis, or malodor of the oral cavity, comprising administering to the oral cavity of a human or other animal such a composition.
  • the subject invention provides compositions effective against dental plaque formation, calculus formation, gingivitis, and mouth malodor.
  • “Pharmaceutically-acceptable topical oral carrier” denotes a carrier for the active compounds of the subject invention (hereinafter “Actives”) comprising solid or liquid filler diluents suitable for use in contact with the oral tissues of humans and lower animals without undue toxicity, incompatibility, instability, irritation, allergic response, and the like, commensurate with a reasonable benefit/risk ratio.
  • Actives active compounds of the subject invention
  • Such topical oral carrier when combined with Actives of the subject invention, results in a composition which is administered topically to the oral cavity.
  • Such compositions are held in the oral cavity for a period of time, and then largely expectorated rather than being swallowed.
  • compositions include mouthwashes, mouth rinses, mouth sprays, dental treatment solutions, toothpastes, dental gels, tooth powders, prophylaxis pastes, lozenges, chewing gums and the like and are more fully described hereinafter. Dentifrices and mouthwashes are the preferred compositions.
  • Polyro refers to pyrophosphate; phosphonate; diphosphonate; and pharmaceutically-acceptable polyphosphates including, but not limited to, linear condensed polyphosphates of the general formula: (P n O(3 n+1 ⁇ )( n+2 )"wherein n is an integer from 2 to
  • Free pyro refers to pyro that is not bound or chelated to the transition metal, zinc.
  • Free zinc refers to hydrated zinc cationic species, such as Zn(H2 ⁇ )6 2+ . As used herein, percentages listed are weight percentage of composition unless otherwise specified.
  • the amounts of pyro and citrate are expressed in terms of a ratio to the amount of zinc in the oral composition.
  • the amount of citrate relative to zinc is at least one when the molar amount of zinc is one (i.e. the molar, ratio of zincxitrate is at most about 1:1); and the amount of pyro relative to zinc is at least one when the molar amount of zinc is one (i.e. the molar ratio of zinc:pyro is at most about 1:1).
  • the zincxitrate ratio is from about 1:1 to about 1:20; more preferably from about 1:1 to about 1:4, more still preferably from about 1:1 to about 1:3.
  • a zinc: pyro ratio from about 1:1 to about 1:20 more preferably from about 1:1 to about 1:8, more preferably still from about 1:1.5 to about 1:6.
  • a zincxitrate.pyro ratio wherein the sum of the molar ratio amounts of citrate ions and pyro ions is from about 2 to about 9, more preferably from about 3 to about 9, when the ratio amount of zinc is 1.
  • the amount of zinc suitable for the purposes of the subject invention is from about 0.005% to about 5% Zn; more preferably from about 0.03% to about 3% Zn; more preferably still from about 0.05% to about 2% Zn.
  • the preferred amounts of zinc are from about 0.1% to about 2%, more preferably from about 0.25% to about 1%.
  • the preferred amount of zinc is from about 0.005% to about 1%, more preferably from about 0.05% to about 0.5%.
  • the amount of citrate anion suitable for the purposes of the subject invention is from about 0.015% to about 25% citrate.
  • the preferred amounts of citrate anion are from about 0.2 % to about 17%, more preferably from about 0.7% to about 12%, more preferably still from about 1.5% to about 5%.
  • the preferred amount of citrate anion is from about 0.01% to about 12%, more preferably from about 0.1% to about 6%, more preferably still from about 0.15% to about 1 %.
  • the amount of pyro anion suitable for the purposes of the subject invention is from about 0.015% to about 25% pyro.
  • the preferred amounts of pyro ion are from about 0.25% to about 16%, more preferably from about 0.6% to about 11%.
  • the preferred amount of pyro anion is from about 0.01 % to about 11 %, more preferably from about 0.1% to about 5%.
  • Suitable sources of zinc ions include zinc oxides, zinc halides, zinc-strong acid complexes, Zn(N03)2, Zn(CIO_ )2, ZnSO_ , and zinc- organic acids sources such as zinc lactate, tartrate, citrate salts, zinc citrate trihydrate and sodium zinc citrate.
  • Zinc sources that are unacceptable are zinc ethylenediaminetetraacetate (ZnEDTA) and zinc nitrilotriacetate (ZnNTA).
  • Preferred sources of zinc ions include zinc oxide (ZnO) and zinc nitrate; more preferred is ZnO.
  • Suitable sources of citrate ions include zinc citrate; citric acid; alkali metal salts of citric acid, especially sodium citrate and potassium citrate; pharmaceutically acceptable hydrated and dehydrated salts of any of the above; and mixtures of any of the above.
  • Suitable sources of pyro ions are disclosed in U.S. Pat. No.
  • Suitable pyro ion sources include tetrasodium pyrophosphate, sodium acid pyrophosphate (Na2H2P2 >7), tetrapotassium pyrophosphate (K4P2O7); phosphates including, but not limited to, linear condensed polyphosphates of the general an integer from 2 to 21; phosphonates and diphosphonates, such as EHDP (ethane-1-hydroxy-1,1-diphosphonate) and AHP (azacyclo- heptane-2,2-diphosphonic acid); pharmaceutically-acceptable alkali metal salts of pyrophosphates, polyphosphates, phosphonates and diphosphonates; and mixtures of any of the above.
  • EHDP ethane-1-hydroxy-1,1-diphosphonate
  • AHP azacyclo- heptane-2,2-diphosphonic acid
  • Preferred pyro ions are pyrophosphate ions; preferred polyphosphate ions are those of the above formula wherein n is 6, 13, and 21.
  • Preferred alkali metals are sodium and potassium for solubility reasons; mixtures of alkali metal salts are acceptable.
  • the pH of oral compositions of the subject invention is critical but can be varied to some extent.
  • the oral compositions are at a pH of from about 6 to about 9, more preferably from about 6.25 to about 8.75, more preferably still from about 7.5 to about 8.5.
  • the conditions for addition of each component should be optimized such that the pH of the mixture does not drop below formulation pH at any time during mixing the indredients.
  • safe and effective amount as used herein is meant an amount of compound or composition sufficient to induce a significant positive modification in the condition to be treated, but low enough to avoid serious side effects (at a reasonable benefit/risk ratio), within the scope of sound medical judgment.
  • the safe and effective amount of the compound or composition will vary with the particular condition being treated, the age and physical condition of the patient being treated, the severity of the condition, the duration of the treatment, the nature of concurrent therapy, the specific compound or composition employed, the particular pharmaceutically-acceptable carrier utilized, and like factors.
  • compositions of this invention are suitable for administration to the oral cavity of a human or lower animal and are compatible with one another and the other components, especially with the Actives, used in an oral composition of the subject invention.
  • compatible means that the components are capable of being co-mingled with one another, in a manner such that there is no interaction which would substantially reduce the efficacy of the oral composition under ordinary use conditions.
  • Preferred topical, oral carriers provide the desired characteristics for mouthwashes, mouth rinses, mouth sprays, dental treatment solutions, toothpastes, dental gels, toothpowders, prophylaxis pastes, lozenges, chewing gums, and the like.
  • the topical, oral carriers of the subject invention comprise components typically used in such compositions which are well known to a skilled practitioner. Such components include, but are not limited to, anticaries agents, antiplaque agents, anticalculus agents, dental abrasives, surfactants, flavoring agents, sweetening agents, binders, humectants, thickening agents, buffering agents, preservatives, coloring agents and pigments, ethanol and water.
  • Water is an optional component of the topical, oral carriers of the compositions of the subject invention.
  • Water employed in the preparation of the commercially suitable compositions should preferably be of low ion content and free of organic impurities.
  • Water preferably comprises from about 2% to about 99%, more preferably from about 20% to about 95% of the compositions of the subject invention.
  • the compositions preferably comprise from about 2% to about 80%, more preferably from about 30% to about 60%, water, while mouthwashes comprise preferably from about 45% to about 99%, more preferably from about 75% to about 98%, water.
  • Dental abrasives useful in the topical, oral carriers of the compositions of the subject invention include many different materials.
  • the material selected must be one which is compatible with the composition of interest and does not excessively abrade dentin.
  • These include, for example, silicas, including gels and precipitates, calcium carbonate, dicalcium orthophosphate dihydrate, calcium pyrophosphate, tricalcium phosphate, calcium polymeta-phosphate, insoluble sodium polymeta-phosphate, hydrated alumina, • and resinous abrasive materials such as particulate condensation products of urea and formaldehyde, and other materials such as those disclosed by Cooley et al. in U.S. Pat. No. 3,070,510, issued December 25, 1962, incorporated herein by reference. Mixtures of abrasives may also be used.
  • Silica dental abrasives of various types, can provide the unique benefits of exceptional dental cleaning and polishing performance without unduly abrading tooth enamel or dentin. For this reason they are preferred for use herein.
  • the silica abrasive polishing materials useful herein, as well as the other abrasives generally have an average particle size ranging between about 0.1 and 30 microns, preferably between about 5 and 15 microns.
  • the silica abrasive can be precipitated silica or silica gels such as the silica xerogels described in U.S. Pat. No. 3,538,230, issued March 2, 1970 to Pader et al., and in U.S. Pat. No. 3,862,307, issued June 21, 1975 to DiGiulio, both incorporated herein by reference.
  • Preferred precipitated silica materials include those marketed by the J. M. Huber Corporation under the tradename, Zeodent®, particularly the silica carrying the designation Zeodent 119®. These silica abrasives are described in U.S. Pat. No. 4,340,583, Wason, issued July 20, 1982, incorporated herein by reference.
  • abrasives may be used.
  • the amount of abrasive in the compositions described herein ranges from about 6% to about 70%, preferably from about 15% to about 50%, when the dentifrice is a toothpaste. Higher levels, as high as 90%, may be used if the composition is a tooth powder.
  • Flavoring agents can also be added to the oral compositions of the subject invention to make them more palatable. Suitable flavoring agents include menthol, oil of wintergreen, oil of peppermint, oil of spearmint, oil of sassafras, and oil of clove. Flavoring agents are generally included in the subject compositions in amounts of from 0% to about 3%, preferably from about 0.04% to about 2% by weight.
  • Coloring agents may be added to compositions of the subject invention to improve appearance. If present, coloring agents typically are included at levels of from about 0.001 % to about 0.5% by weight. Sweetening agents are also preferred in the compositions of the subject invention to make them more palatable. Sweetening agents which can be used include aspartame, acesulfame, saccharin salts, dextrose, glucose, levulose thaumatin, D-tryptophan, dihydrochalcones, and cyclamate salts. Saccharin salts are preferred. Sweetening agents are generally used in the subject compositions in amounts of from 0% to about 6%, preferably from about 0.005% to about 5% by weight.
  • Oral compositions can also contain a surfactant.
  • Suitable surfactants are those which are reasonably stable and form suds throughout a wide pH range, including nonsoap anionic, nonionic, cationic, zwitterionic and amphoteric organic synthetic detergents, and compatible mixtures thereof. Many of these suitable surfactants are disclosed in U.S. Pat. No. 4,051,234, issued to Gieske et al. on September 27, 1977, and in U.S. Pat. No. 3,959,458 issued to Agricola, Briner, Granger and Widder on May 25, 1976, both of which are incorporated herein by reference.
  • Surfactants are typically present in compositions of the subject invention at a level of from 0% to about 20%, preferably from about 0.1, more preferably from about 1% to about 4% by weight. Surfactants may also be used as solubilizing agents to help retain sparingly soluble components, e.g., some flavoring agents, in solutions. Surfactants suitable for this purpose include polysorbates and poloxamers. Preferred are surfactants which are non-ionic at the formulation pH of the compositions.
  • binders and/or thickening agents are natural gums such as gum karaya, gum arabic, and gum tragacanth; polysaccharide gums such as xanthan gum; and other natural products such as carrageenan; chemically modified natural products such as those based on cellulose esters, that is, carboxyimethylcellulose (CMC), hydroxyethylcellulose (HEC), and hydroxypropylcellulose (HPC); and synthetic binders such as polyvinylpyrrolidone; and water soluble salts of cellulose ethers such as sodium carboxymethyl cellulose and sodium carboxymethyl hydroxyethyl cellulose.
  • CMC carboxyimethylcellulose
  • HEC hydroxyethylcellulose
  • HPC hydroxypropylcellulose
  • synthetic binders such as polyvinylpyrrolidone
  • water soluble salts of cellulose ethers such as sodium carboxymethyl cellulose and sodium carboxymethyl hydroxyethyl cellulose.
  • Carboxyvinyl polymer binders are less desirable, but may be used. Colloidal magnesium aluminum silicate or finely divided silica can be used as part of the thickening agent to further improve texture. Blends and mixtures of the suitable binders may significantly improve the characteristics of compositions made therewith. Preferred binders are chemically modified celluloses such as CMC or HEC; more preferred is HEC. Binders and thickening agents are generally present in the compositions of the subject invention in amounts of from about 0.1% to 10%, preferably from about 0.25% to about 7.5%, more preferably from about 0.5% to about 3.5%.
  • humectant serves to keep toothpaste compositions from hardening upon exposure to air, and to give mouthwash and toothpaste compositions a moist feel to the mouth. Certain humectants can also impart desirable sweetness of flavor to mouthwash and toothpaste compositions.
  • the humectant on a pure humectant basis, generally comprises from 0% to about 70%, preferably from about 2% to about 55%, by weight of the compositions herein.
  • Suitable humectants for use in compositions of the subject invention include edible polyhydric alcohols such as glycerin, sorbitol, xylitol, polyethylene glycol, and propylene glycol, especially sorbitol and glycerin.
  • Opacifiers may also be used in toothpastes of the subject invention to render the toothpaste opaque.
  • Suitable opacifiers include titanium dioxide and some abrasives including, for example, magnesium aluminum silicate.
  • Opacifiers generally comprise from 0% to about 4%, preferably from about 0.5% to about 3% by weight of the compositions herein.
  • compositions of the subject invention are preservatives.
  • the preservatives prevent microbial growth in the compositions. Suitable preservatives include methylparaben, propylparaben, benzoates and ethanol. If the preservative is ethanol, it generally comprises from 0% to about 35% by weight, preferably from about 5% to about 15%, of the compositions herein. Other preservatives generally comprise from 0% to about 5% by weight, preferably from about 0.1% to about 2%, of the compositions herein.
  • Antimicrobial, antiplaque agents can also optionally be present in the oral compositions of the subject invention, on the condition that they are compatible with the Actives.
  • Such agents may include, but are not limited to, triclosan, 2,4,4 , -trichloro-2'-hydroxydiphenyl ether, as described The Merck Index. 11th Ed. (1989), p. 1520 (entry No. 9573); chlorhexidine, ..Merck Index. No. 2090); alexidine (Merck Index. No. 222); hexetidine (Merck Index. No. 4624); sanguinarine (Merck Index. No. 8320); benzalkonium chloride (Merck Index. No. 1066); salicylanilide (Merck Index. No.
  • the antimicrobial antiplaque agents may comprise from 0% to about 6%, preferably from about 0.1% to about 5% by weight of the compositions of the subject invention.
  • Bleaching agents can also be present in the oral compositions of the subject invention.
  • Suitable bleaching agents include organic and inorganic oxidizing agents such as hydrogen peroxide, alkali metal peroxides and superoxide and organic peroxides such as monoper-oxyphthalates and perbenzoic derivatives. If present, such bleaching agents may comprise from 0% to about 6%, preferably from about 1 % to about 5% by weight of the compositions of the subject invention.
  • Nutrients can also be present in the oral composition of the subject invention, on condition that they are compatible with the Actives. Such agents may include folate, retinoids (Vitamin A), Vitamin C, Vitamin E. If present, the nutrients generally comprise from about 0.001% to about 10% by weight of the compositions of the subject invention.
  • a fluoride ion source typically is in the form of a water-soluble fluoride compound.
  • This water-soluble fluoride compound is typically present in the compositions of the subject invention in an amount sufficient to give a fluoride concentration of from about 0.0025% to about 5.0% by weight, preferably from about 0.005% to about 2.0% by weight.
  • Preferred fluoride sources are sodium fluoride, acidulated phosphate fluoride, and sodium monofluorophosphate.
  • compositions of the subject invention are in the form of dentifrices, especially toothpastes.
  • Components of toothpastes generally include a dental abrasive (from about 10% to about 50%), a surfactant (from about 0.5% to about 10%), a thickening agent (from about 0.1% to about 5%), a humectant (from about 10% to about 55%), a flavoring agent (from about 0.04% to about 2%), a sweetening agent (from about 0.1% to about 3%), a coloring agent (from about 0.01 % to about 0.5%) and water (from about 2% to about 45%).
  • compositions of the subject invention are mouth rinses, mouthwashes and mouth sprays.
  • Components of such mouthwashes and mouth sprays include water (from about 45% to about 95%), ethanol (from 0% to about 25%), humectant (from 0% to about 50%), surfactant (from about 0.01% to about 7%), flavoring agent (from about 0.04% to about 2%), sweetening agent (from about 0.1% to about 3%), and coloring agent (from about 0.001% to about 0.5%).
  • Such mouth rinses, mouthwashes and mouth sprays may also include an antiplaque agent (from about 0.1% to about 5%).
  • Other preferred compositions of the present invention are dental solutions.
  • Components of such dental solutions generally include water (from about 90% to about 99%), preservative (from about 0.01% to about 0.5%), thickening agent (from 0% to about 5%), flavoring agent (from about 0.04% to about 2%), sweetening agent (from about 0.1 % to about 3%), and surfactant (from 0% to about 5%). 5 Methods of Use
  • Another aspect of the subject invention involves methods of treating or preventing mouth odor, dental plaque, calculus and gingivitis, by application of compositions comprising a safe and effective amount of Actives, to tissues of the oral cavity.
  • compositions of the subject invention typically by administering an oral composition of the subject invention, as described hereinabove, to the oral cavity.
  • an amount of composition comprising at least about 0.001 g
  • the oral composition is a toothpaste, typically from about 0.3 grams to about 15 grams, preferably from about 0.5 grams to about 5 grams, more preferably from about 1 to about 2 grams, of
  • toothpaste is applied to an applicating device e.g., a toothbrush.
  • the applicating device is then contacted with the oral cavity surfaces in a manner such that the oral composition is contacted with tissue of the oral cavity, especially the teeth and gums.
  • the applicating device may be further used to effect an even distribution of the oral composition to
  • the application preferably lasts for a period of from about 15 seconds to about 10 minutes, more preferably from about 30 seconds to about 3 minutes, more preferably still from about 1 minute to about 2 minutes.
  • the toothpaste residue is typically removed from the tooth surface by using j 30 a liquid acceptable to the oral cavity, typically water, to rinse and be expectorated from the oral cavity.
  • the oral composition is a mouthwash, typically from about 1 ml. to about 20 ml., preferably from about 2 ml. to about 15 ml., most preferably from about 10 ml. to about 15 ml., of liquid mouthwash
  • the oral cavity 35 containing the antiplaque Active is introduced to the oral cavity.
  • the liquid mouthwash is then agitated for from about 10 seconds to about 10 min., preferably from about 15 seconds to about 3 min., more preferably from about 30 seconds to about 2 minutes, within the oral cavity to obtain an improved distribution of the mouthwash over the tissue of the oral cavity.
  • the mouthwash is typically expectorated from the oral cavity.
  • Application frequency is preferably from about 3 times weekly to about 4 times daily, more preferably from about once daily to about 3 times daily, more preferably still from about once to about twice daily.
  • the period of such treatment typically ranges from about one day to a lifetime.
  • compositions of the subject invention can be made using methods which are commonly used to produce oral care products.
  • dentifrice compositions of the subject invention are made using conventional processes.
  • the numbers listed are weight percentages of the compositions.
  • EXAMPLES XII-XVI The following are examples of mouthwash and dental rinse compositions of the subject invention and are made using conventinal processes. The amounts listed are weight percentages of the compositions. During manufacture, the pH of the following compositions is maintained at a minimum of pH 7.5.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Inorganic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Emergency Medicine (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cosmetics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Cette invention concerne une composition utilisée dans le traitement et la prévention de la plaque dentaire, du tartre et de la gingivite ou de la mauvaise odeur de la cavité bucco-dentaire, et comprenant: (a) (i) une source d'une quantité inoffensive et efficace d'ions de zinc; (ii) une source d'ions de citrate; et (iii) un ou plusieurs agents antitartre sélectionnés à partir du groupe se composant de pyrophosphate, phosphonate, diphosphonate et de polyphosphates condensés linéaires pharmaceutiquement acceptables de la formule générale: (PnO(3n+1)(n+2)-, dans laquelle n est un nombre entier de 2 à 21; et dans laquelle le rapport molaire zinc:citrate est au plus d'environ 1:1; le rapport molaire de zinc:pyro est au plus d'environ 1:1; et (b) un excipient bucco-dentaire local pharmaceutiquement acceptable. Cette invention se rapporte également à des procédés de traitement ou de prévention de la plaque dentaire, du tartre, de la gingivite ou de la mauvaise odeur de la cavité bucco-dentaire et consistant à administrer dans la cavité bucco-dentaire d'un être humain ou d'un autre animal cette composition.
EP94903459A 1992-12-18 1993-12-06 Compositions de soins bucco-dentaires contenant des agents antiplaque et antitartre Withdrawn EP0675706A1 (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US99333692A 1992-12-18 1992-12-18
US14877693A 1993-11-16 1993-11-16
US148776 1993-11-16
PCT/US1993/011787 WO1994014407A1 (fr) 1992-12-18 1993-12-06 Compositions de soins bucco-dentaires contenant des agents antiplaque et antitartre
US993336 1997-12-19

Publications (1)

Publication Number Publication Date
EP0675706A1 true EP0675706A1 (fr) 1995-10-11

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EP94903459A Withdrawn EP0675706A1 (fr) 1992-12-18 1993-12-06 Compositions de soins bucco-dentaires contenant des agents antiplaque et antitartre

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JP (1) JPH08505843A (fr)
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AU5740094A (en) 1994-07-19
CN1095263A (zh) 1994-11-23
CZ156795A3 (en) 1996-01-17
CA2151913A1 (fr) 1994-07-07
BR9307688A (pt) 1999-09-08
HU9501784D0 (en) 1995-08-28
WO1994014407A1 (fr) 1994-07-07
HUT72041A (en) 1996-03-28
MX9400053A (es) 1994-07-29
JPH08505843A (ja) 1996-06-25

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