HUT72041A - Oral compositions containing antiplaque, anticalculus agents - Google Patents

Description

Oral preparations containing anti-plaque and anti-calcifying agents

THE PROCTER & GAMBLE COMPANY, CINCINNATI, Ohio, US

inventors:

MONTGOMERY Rónáid Earl, CINCINNATI, Ohio, US

PYRZ Joseph Wasyl, N. WALES, Pennsylvania, US

COYLE-REES Margaret Mary, CINCINNATI, Ohio, US

Date of filing: 06.12.1993

Priorities: December 18, 1992 (07 / 993,336) US

11.16.1993. (08 / 148,776) US

International Application Number: PCT / US93 / 11787

International Publication Number: WO 94/14407

The present invention relates to oral care compositions, such as toothpastes and oral care solutions, which are useful in the treatment and prevention of plaque formation, scaling and gingivitis, and mouth odor.

Oral microbes are breeding sites for colonization and reproduction. Within the mouth, the gums, lips, mucous membranes, palate, tongue and teeth are all capable of colonizing and multiplying bacteria. Teeth are unique elements of the oral cavity that typically proliferate bacteria and their by-products (plaques) on their hard, non-detachable surfaces and primarily in the areas and gaps adjacent to them.

Plaque is a coarse, sticky substance made from tooth that is made up of saliva, bacteria, and food residue, and sticks firmly to the tooth in irregular and discontinuous spots. Within a few hours after brushing, an animal-derived mucous coating is formed on the tooth, consisting mainly of protein. In the mucous membrane, various oral bacteria settle and produce a plaque on their growth. The mucus coating adheres to a carbohydrate food residue, which is digested by some types of plaque - forming bacteria. Digestion results in the formation of plaque-related by-products and acids that cause tooth enamel. Bacterial by-products formed in the oral cavity can produce a foul-smelling gas formation and, as a result, may produce a smell of the mouth.

Plaque oral bacterium is embedded in a number of grams of insoluble polysaccharide extracellular matrices · ························································· · · · · · · · · ·

It consists of a positive and gram negative microorganism which adheres firmly to the gripping other mouth surfaces. The bacterial colonization resulting in plaque formation follows an ecological pattern whereby some pioneer aerobic species, mostly gram-positive streptococci, settle on the enamel surfaces. The plaque then grows through the complex stages of microbiological development. Tooth-protected surfaces, such as gaps and gingival spaces, often contain mature plaques that contain anaerobes. Saliva and gingival fluid are one of the sources of substances involved in plaque formation.

If plaque is not removed or prevented, it is embedded with mineral salts containing calcium and phosphate and causes tartar or tar deposits on the teeth. The tartar is white or yellowish in color and may be discarded or discolored by external agents. Tartar is less visible than plaque and is much more difficult to remove from the tooth. Toxins in plaque and tartar can irritate the gingival tissues surrounding the scaly teeth and cause inflammation and destruction of the gums and thus other complications.

Zinc is a known anti-scaling agent, but zinc-containing formulations are also astringent and have an unpleasantly bitter taste. The negative aesthetic effect of the zinc cation, like the chemical and biological effects, is a function of the amount used; at higher concentrations results in a worse aesthetic effect, thus improving efficiency by increasing the free zinc concentration at the expense of aesthetics. · · · · · · · · · · · · · · · · · ·· happens. Due to the relationship between efficacy and aesthetics described above, the use of zinc in oral care products is limited.

Pyrophosphate is also an anti-tartar anti-tartar agent that inhibits the increase in pyrophosphate concentration.

However, it has been found that careful formulation of zinc and pyrophosphate-containing formulations can enhance the zinc content of the oral care compositions and thereby enhance the anti-tartar effect without increasing the negative aesthetic effect of the formulation.

In our work, it has been found that the efficacy and aesthetic effects of zinc-containing preparations are separable properties. Formulating zinc with a citrate and a pyrrole compound so that the molar ratio of zinc: cifrate to zinc: pyrrole is certain, prevents the negative aesthetic effect typically associated with the use of zinc ions.

It is an object of the present invention to provide a composition for the prevention of tooth decay in the oral cavity.

Another object of the present invention is to provide a composition for preventing plaque formation in the oral cavity.

It is a further object of the present invention to provide a method of preventing tooth decay in the oral cavity.

* · E ··

It is a further object of the present invention to provide a method for preventing plaque formation in the oral cavity.

The present invention relates to a composition for the treatment or prevention of plaque, tartar and gum inflammation or mouth odor comprising:

(a) (i) a source of zinc containing a safe and effective amount of zinc ions;

(ii) a source of citrate ion; and (iii) one or more anti-scaling agents, which may be pyrophosphate, phosphonate, diphosphate, or a pharmaceutically acceptable linear condensed polyphosphate of formula (P _n 0 (3n + 1)) < ^{n + 2} ) wherein n is 2 to 21;

in the composition, the molar ratio of zinc to citrate is at least about 1: 1 and the molar ratio of zinc to pyrrole is at least about 1: 1; and

b) a pharmaceutically acceptable carrier for topical treatment of the mouth.

The invention also relates to a method of treating or preventing the formation of plaque, tartar and gum inflammation or mouth odor, wherein said composition is applied to the oral cavity of a human or other mammal.

As used herein, the term "pharmaceutically acceptable carrier" suitable for topical treatment of the mouth refers to solid or liquid filler diluents suitable as carriers for the active ingredient of the present invention, which when in contact with the oral cavity of humans or inferior mammals. They are, for example, non-toxic, incompatible, unstable, irritant, allergy-inducing, and the benefit-risk ratio is sufficiently high.

The composition containing the active ingredient of the invention is suitable for topical treatment of the oral cavity. Preferably, these formulations are to be kept in the mouth for a period of time and not swallowed but spit out. Examples of such compositions are mouthwashes, mouthwashes, mouth sprays, dentifrices, toothpastes, gels, toothpastes, preventive pastes, liquids and chewing gums, which will be described in more detail below. Preferred compositions are toothpastes and mouthwashes.

As used herein, the term pyro compound refers to pyrophosphate, phosphonate, diphosphate and pharmaceutically acceptable polyphosphates, including, for example, ( ^p n ° (3n + 1)) ( ^{n + 2} ) 'linear fused polyphosphate wherein n is An integer from 2 to 21.

As used herein, the term free pyro compound refers to a pyro compound which does not form a bond or chelate with the zinc transition metal.

As used herein, the term free zinc refers to zinc cations of hydrated water, such as Zn (H2O) g ²⁺ .

The percentages used in this specification are by weight unless otherwise stated.

The amount of pyrrole compound and citrate is determined by the ratio of zinc in the oral care composition.

The molar ratio of citrate to zinc is at least about 7 · ··· 1: 1; and the pyrrole compound has a molar ratio of zinc to zinc of at least about 1: 1. The zinc: citrate molar ratio is preferably from about (1: 1) to (1:20), more preferably from about (1: 1) to (1: 4) and most preferably about (1) : 1) - - (1: 3). The molar ratio of zinc to pyrrole compound is preferably from about (1: 1) to (1: 20), more preferably from about (1: 1) to (1: 8), and most preferably from about (1: 1.5) to (1: 6) ). Also preferred is a molar ratio of zinc: citrate to pyruvate in which the sum of the molar ratios of citrates to pyrroles is from 2 to 9, more preferably from 3 to 9, based on one mole of zinc.

The amount of zinc useful in the compositions of the present invention is from about 0.005 to 5% by weight, preferably from about 0.03 to 3% by weight, and more preferably from about 0.05 to 2% by weight. The amount of zinc used in the toothpastes is preferably about 0.1 to 2% by weight and more preferably about 0.25 to 1% by weight. The amount of zinc used in mouthwashes, mouthwashes, mouth sprays and dentifrice solutions is preferably from about 0.005% to about 1% by weight, and more preferably from about 0.05% to about 0.5% by weight.

The amount of citrate anion useful in the compositions of the present invention is from about 0.015% to about 25% by weight. The amount of citrate anion used in toothpastes is preferably about 0.2 to 17% by weight, more preferably about 0.7 to 12% by weight, and most preferably about 1.5 to 5% by weight. The amount of citrate anion used in mouthwashes, mouthwashes, mouth sprays and dentifrice solutions is preferably from about 0.01% to about 12% by weight, more preferably from about 0.1% to about 6% by weight, and most preferably from about 0.15% to about 1%.

The amount of piroanion useful in the compositions of the invention is from about 0.015% to about 25% by weight. The amount of pyroanion used in toothpastes is preferably from about 0.25 to about 16% by weight, and more preferably from about 0.6 to about 11% by weight. The amount of piroanion used in mouthwashes, mouthwashes, mouth sprays and dentifrice solutions is preferably from about 0.01% to about 11% by weight, and more preferably from about 1% to about 5% by weight.

Suitable sources of zinc ions include zinc oxide, zinc halides, zinc strong acid complexes, zinc nitrate, zinc perchlorate, zinc sulfate, and zinc organic acid derivatives such as zinc lactate, tartrate, citrate salts, zinc citrate trihydrate and sodium zinc citrate. Not applicable sources of zinc are zinc ethylene diamine tetraacetate (ZnEDTA) and zinc nitrilotriacetate (ZnNTA). Preferred sources of zinc ions are zinc oxide (ZnO) and zinc nitrate, and ZnO is more preferred.

Suitable sources of citrate ions include zinc citrate, citric acid, citric acid alkaline metal salts, particularly sodium citrate and potassium citrate, and pharmaceutically acceptable hydrated and dehydrated salts of any of the foregoing, and any mixture thereof.

Suitable sources of pyrroles include those described in U.S. Patent Nos. 4,885,155, 3,678,154, 3,737,522, and 4,627,977. Suitable pyrrole sources include, for example, tetrasodium pyro9 phosphate, disodium dihydrogen pyrophosphate (λ2¾P2O7)> tetra-potassium pyrophosphate (K4P2O7); phosphates, such as linear fused polyphosphates of the formula ^Mn (n + 2) PnO (3n + 1) wherein M is sodium or potassium and n is an integer from 2 to 21; phosphonates and diphosphonates such as EHDP (ethane-1-hydroxy-1,1-diphosphonate) and AHP (azacycloheptane-2,2-diphosphonic acid); pharmaceutically acceptable alkali metal salts of pyrophosphates, polyphosphates, phosphonates and diphosphonates; and appropriate mixtures of the above compounds. Preferred pyrroles are pyrophosphate ions; and preferred polyphosphate ions are those compounds of the general formula described above wherein n is 6, 13 and 21. Preferred solubility alkali metals are sodium and potassium; mixtures of alkali metal salts may also be used.

Although the pH of the oral care compositions of the present invention is critical, it can be varied to some extent. The pH of the oral care compositions is preferably from about 6 to about 9, more preferably from about 6.25 to about 8.75, and most preferably from about 7.5 to about 8.5.

In preparing the compositions of the invention, the conditions for the addition of the components must be optimized so that the pH of the mixture is added to the components. never fall below the formulation pH.

A safe and effective amount as used herein is that amount of the compound or composition that is typically positive to the lesion being treated and does not yet cause a serious side effect within the scope of the treatment (the benefit / risk ratio is appropriate). The compound or • · · · «· _ ·? ·· * · ♦ · 4 ··

W · · 4 · · · · ♦ · ♦ · · · 4 ··· safe and effective amounts of, for example, the nature of the lesion being treated, the age and physical condition of the subject, the severity of the lesion, the duration of treatment and the nature of concurrent treatment. , depending on the nature of the compound or composition employed and the pharmaceutically acceptable carrier employed.

As used herein, the term composition refers to the composition obtained after the addition of various additives used in the compositions of the invention.

The carrier components used in the oral care compositions of the present invention for topical treatment of the mouth of the human or inferior organism should be compatible with each other, with other components, in particular the active ingredients. The term "compatible" as used herein means that the components may be admixed without interfering with the efficacy of the oral care composition under normal conditions of use.

Suitable carriers for topical application to the mouth are those which provide the desired properties of mouthwashes, mouthwashes, mouth sprays, dentifrices, toothpastes, toothpastes, toothpastes, preventive pastes, liquids and chewing gums. Suitable carriers for topical administration of the mouth in the compositions of the present invention are well known in the art. Such components are, for example, anti-caries, anti-plaque agents, anti-tartar agents, abrasives, surfactants, flavorings, sweeteners, binders, wetting agents, thickeners, buffers, preservatives, paints, dyes, ethanol.

Suitable carriers for topical administration of the mouth in the compositions of the present invention optionally contain water. The water used in commercially available compositions should preferably be of low ionic strength and free from organic contamination. The compositions of the invention preferably contain from about 2% to about 99% by weight water, and more preferably from about 20% to about 95% by weight water. Preferably, toothpastes contain from about 2% to about 80% by weight, more preferably from about 30% to about 60% by weight of water, and mouthwashes preferably contain from about 45% to about 99% by weight of water.

The toothbrush used in the compositions of the present invention for topical treatment of the mouth may be of many different materials. The material actually used must be compatible with the particular formulation and not be sanded. Examples of such materials are silicas, including gels and precipitates, calcium carbonate, dicalcium orthophosphate dihydrate, calcium phosphate, tricalcium phosphate, calcium polymetaphosphate, insoluble sodium polymetaphosphate, hydrated alum, such as urea and formaldehyde condensation products, and such materials as described in U.S. Patent 3,070,510. Mixtures of abrasives may also be used.

Different types of silica abrasive materials, without damaging tooth enamel or tooth decay, have very good cleaning and polishing properties. They are therefore very advantageous in the compositions of the invention.

The silica and other abrasives used in the composition of the present invention have an average particle size of from about 0.1 to about 30 µm, preferably from about 5 to about 15 µm. The silica abrasive may be precipitated silica or silica gel. Examples of such materials are the silica xerogels described in U.S. Patent Nos. 3,538,230 and 3,862,307. Preferred are W.R. Grace and Company, Syloid silica xerogels from Davidson Chemical Division. Preferred precipitated silica materials are, for example, J.M. Zeodent under the trade name of Huber Corporation, with Zeodent 119 being particularly preferred. For a detailed description of these silica abrasives, see U.S. Patent No. 4,340,583.

Mixtures of abrasives may also be used. When the oral care composition is a toothpaste, the composition has an abrasive concentration of about 6 to 70% by weight, and preferably about 15 to 50% by weight. For tooth powders, larger amounts of up to 90% by weight may be used.

Flavoring agents may also be added to the compositions of the present invention for improved taste. Suitable flavoring agents include menthol, gaulter oil, peppermint oil, marjoram oil, safflower bay oil and clove oil. The amount of flavoring agent used in the compositions of the invention is generally from 0% to about 3% by weight, preferably from about 0.04% to 2% by weight.

Dyes may also be added to the compositions of the present invention to enhance their appearance. Dyes, when used, are typically present in an amount of from about 0.001% to about 0.5% by weight.

Sweetening agents may also be added to the compositions of the present invention for improved taste. Suitable sweeteners include, for example, aspartame, acesulfame, saccharin salts, dextrose, glucose, levulose thaumatin, D-tryptophan, dihydrocalcones and cyclamate salts. Saccharine salts are preferred. The sweetener content of the compositions of the invention is generally from 0% to 6% by weight, preferably from about 0.005% to 5% by weight.

Oral compositions also contain a surfactant. A wide range of pH stable and foaming surfactants, such as non-soap anionic, nonionic, cationic, dual ionic and amphoteric synthetic organic detergents and compatible mixtures thereof, are well suited. Most of these are described in U.S. Patent Nos. 4,051,234 and 3,959,458. The surfactant concentration of the compositions of the invention is typically from 0% to about 20% by weight, preferably from about 0.1% to about 4% by weight, more preferably from about 1% to about 4%. Surfactants may also be used as suitable solubilizers to keep poorly soluble components such as certain flavoring agents in solution. Polysorbates and poloxamers are well suited for this purpose.

Nonionic surfactants in the formulation pH range are preferred.

It is also desirable to use binders and / or thickeners for the oral care agents of the present invention, in particular to achieve the desired consistency of toothpastes. Examples of such materials are natural gums such as karaya gum, gum arabic, tragacanth gum; polysaccharide gums such as xanthan gum; and other natural materials such as seaweed; chemically modified natural substances such as cellulose esters, such as carboxymethyl cellulose (CMC), hydroxyethyl cellulose (HEC) and hydroxypropyl cellulose (HPC); synthetic binders such as polyvinylpyrrolidone; water soluble cellulose ether salts such as sodium carboxymethyl cellulose and sodium salt of carboxymethyl hydroxyethyl cellulose. They are less desirable, but carboxy vinyl polymer binders may also be used. Colloidal magnesium or fine silica may also be used as part of the thickener used to further improve the texture of the composition. Suitable binders and mixtures thereof can greatly improve the properties of the compositions of the invention. Chemically modified celluloses such as CMC and HEC are preferred binders. The binder and thickener in the compositions of the invention will generally be from about 0.1 to about 10% by weight, preferably from about 0.25 to about 7.5% and more preferably from about 0.5 to about 3.5% by weight.

The carriers used in the compositions of the invention for topical treatment of the mouth may optionally be a wetting agent

may also contain. The wetting agent prevents air hardening of toothpaste and promotes wet taste of mouthwash and toothpaste formulations. The amount of wetting agent, based on pure wetting agent, is generally from 0% to about 70% by weight of the composition, preferably from about 2% to 55% by weight. Suitable wetting agents for use in the compositions of the present invention include glycerol, sorbitol, xylitol, polyethylene glycol and propylene glycol, in particular sorbitol and glycerol.

Toothpaste compositions of the present invention may also include opacifying agents to provide an opalescent appearance. Such materials include, for example, magnesium aluminum silicate. The amount of opacifying agent is generally from 0% to about 4% by weight, preferably from about 0.5% to 3% by weight of the composition.

Other optional components of the compositions of the invention are preservatives. Preservatives prevent microbes from developing in the formulations. Suitable preservatives include methyl paraben, propyl paraben, benzoates and ethanol. In the case of an ethanol preservative, the amount used is generally from 0% to about 35% by weight, preferably from about 5% to 15% by weight of the composition. Other preservatives will generally be present in an amount of from about 0% to about 5%, preferably from about 0.1% to about 2% by weight of the composition.

Optionally, anti-microbial anti-plaque agents may be added to the oral care compositions of the present invention. An example of such material is The

Merek Index, 11th Ed. (1989), p. 15,420, 2,4,4'-trichloro-2'-hydroxydiphenyl ether, triclosan

(Indicator: 9573), chlorhexidine (ref. 2090), alexidine (Indicator: 222), hexetidine (ref. 4624), sanguinarine (precursor: 8320), Benzalkonium chloride (ref. 1066),

lycyl anilide (ref. 8299), domifenium bromide (ref.:

3411), cetylpyridinium chloride (CPC) (ref. 2024), tetra decylpyridinium chloride (TPC), N-tetradecyl-4-ethylpyridinium

chloride (TDEPC), ectenidine, delmopinol, octapinol and other piperidine derivatives, nicin formulations, antibiotics such as augmentin, amoxicillin, tetracycline, doxycycline, minocycline and metronidazole, peroxides such as cilium peroxide, monohydrate, as well as its analogs as disclosed in U.S. Patent No. 4,670,252 and anti-microbial anti-plaque agents as described above. Anti-microbial plaque inhibitors, when used, are added to the compositions of the invention in an amount of from 0% to about 6% by weight, preferably from about 0.1% to about 5% by weight.

The oral care compositions of the present invention may also contain bleaching agents. Inorganic oxidizing agents such as hydrogen peroxide, alkali metal peroxides and superoxides may be used as bleaching agents; organic oxidizing agents such as monoperoxyphthalates and perbenzoic acid derivatives. These bleaching agents, when used, are added in an amount of from 0% to about 6% by weight, preferably from about 1% to 5% by weight, of the compositions of the invention.

Nutrient-compatible nutrients such as folate, retinoids (vitamin A), vitamin C and vitamin E may also be added to the oral care compositions of the present invention. These, when used, are added in an amount of from about 0.001% to about 10% by weight of the composition.

Other optional additives that may be used include a safe and effective amount of a source of fluorine, typically a water-soluble fluoride compound. The water-soluble fluoride compound is typically added in an amount such that the concentration of fluoride is from about 0.0025% to about 5% by weight, preferably from about 0.005% to about 2% by weight. Preferred sources of fluoride are sodium fluoride, acidified phosphate fluoride and sodium monofluorophosphate. Such salts are described, for example, in U.S. Patent 3,678,154.

Preferred compositions of the present invention are toothpastes, in particular toothpastes. These toothpastes generally contain about 10 to 50% by weight of tooth sanding agent, about 0.5 to 10% by weight of surfactant, about 0.1 to 5% by weight of thickening agent, about 10 to 55% by weight of wetting agent, about 0.04 to 2% by weight and by weight containing about 0.1% to about 3% by weight of sweetener, about 0.01% to about 0.5% by weight of coloring agent, and about 2% to about 45% by weight of water.

Other preferred embodiments of the compositions of the present invention are mouthwashes, mouthwashes, and mouth sprays. These mouthwashes and mouth sprays contain from about 45% to about 90% water, from about 0% to about 25% ethanol, from about 0% to about 50% wetting agent, from about 0.01% to about 7% by weight. a surfactant, from about 0.04% to about 2% by weight of a flavoring agent, from about 0.1% to about 3% by weight of a sweetener, and from about 0.001% to about 0.5% by weight of a coloring agent. These compositions may also contain from about 0.1% to about 5% by weight of an anti-plaque agent.

Further representative compositions of the present invention are dental solutions. Such formulations will generally contain from about 90% to about 99% water, from about 0.01% to about 0.5% preservative, from about 0% to about 5% thickening agent, from about 0.04% to about 2% flavoring agent. containing from about 0.1% to about 3% by weight of a sweetener and from about 0% to about 5% by weight of a surfactant.

In another aspect of the present invention, a composition comprising a safe and effective amount of an active ingredient is used to treat or prevent mouth odor, plaque, scaling, and gingivitis. The formulations used are as defined above.

In such methods, a safe and effective amount of an active ingredient, typically a

an oral care composition. The effective amount of the active ingredient in the composition will generally be at least about 0.001 g. Teeth and other tissues in the oral cavity are exposed to the active ingredient.

When the oral care composition is a toothpaste, the application device, such as a toothbrush, typically comprises about 0.3 g to about 15 g, preferably about 0.5 g to about 15 g, and more preferably about 1 g to about 2 g. The application device is then contacted with the oral cavity surfaces such that the oral care composition is in contact with the oral cavity surfaces, particularly the gingiva. The application device may further enhance the treatment of the tooth surface with an oral care composition, such as brushing. The application preferably ranges from about 15 seconds to 10 minutes, more preferably from about 30 seconds to 3 minutes, and more preferably from about 1 minute to 2 minutes. After application, the toothpaste residue is removed from the oral cavity with a suitable liquid, typically water, by rinsing the oral cavity and spitting out the liquid.

When the oral care composition is a mouthwash, typically about 1 to 20 ml, preferably about 2 to 15 ml, and most preferably about 10 to 15 ml, of plaque inhibiting mouthwash is administered into the oral cavity. The mouthwash is rotated in the oral cavity for about 10 seconds to 10 minutes, preferably for about 15 seconds to 3 minutes, and more preferably for about 30 seconds to 2 minutes, so that the mouthwash is well distributed across the oral cavity tissue. The mouthwash is then spit out of the mouth.

The frequency of application is preferably from about 3 times a week to four times a day, more preferably from about once a day to twice a day. The duration of treatment is typically from about 1 day to a lifetime.

The following examples illustrate the invention in more detail. The examples are provided for illustrative purposes only, are not intended to limit the scope of the invention, and any modification or modification of the invention is intended to be within the scope of the invention.

The formulations of the present invention are prepared by methods conventionally used in the preparation of oral care compositions.

- Examples 11:

In the following examples, toothpaste compositions of the invention are prepared by conventional methods. The composition of the formulations is set out in the following table, and the numbers given for the composition are by weight. During manufacture, each formulation is maintained at a pH of at least 7.5.

Example

component 1 2 3 4 5 6 sorbitol 21,17 21,17 14.2 18.3 21,17 31 65 PEG-8 3 3 3 3 3 - Citric acid 0, 69 0.34 0.51 0.51 1, 03 Irish 46 Sodium citrate 4.84 2.42 3, 63 3, 63 7.25 3 68 Zinc nitrate - - - - - 2, 97

Zinc sulphate

1, 61

Zinc chloride 1.36 - - - 1.36 - tetrapotassium pyrophosphate (60% aqueous solution) 5.08 12.71 10, 16 7.62 2.54 11.87 disodium -dihidrogén- pyrophosphate 1.33 ' 3.32 2, 65 1, 99 0, 66 - tetrasodium pyrophosphate 1.28 3, 19 2.55 1.91 0, 64 - Sodium fluoride 0.24 0.24 0.24 0.24 0.24 0.24 Sodium- -szacharid 0.46 0.46 0.46 0.46 0.46 0.46 Titanium dioxide 0.5 0.5 0.5 0.5 0.5 0.5 Silicon dioxid22 22 22 22 22 22 Glycerol 9 9 9 9 9 9 Carboxymethyl -cellulose 1 1 0.75 - 0.75 0.75 xanthan gum - - 0.75 0.75 0.75 0.75 Hydroxyethyl -cellulose - - - 0.75 - - Natra-lauryl -sulfate (27.9% aqueous solution) 4 4 4 4 4 4 Flavoring agent 1.1 1.1 1.1 1.1 1, 1 1, 1

Water

100% additional quantity

• * «

The pH of the suspension is 7.1 to 7.3

Example

component

10 11

S zorbit 31, 65 31, 65 14.2 31, 65 31, 65 PEG-8 Citric acid (you are anhydrous 3 3 3 3 3 monohydrate) 1.44 0, 91 0.73 0, 88 2, 94 Sodium citrate 3.23 0, 144 4, 62 - - Zinc Oxide tetrapotassium pyrophosphate (60% aqueous 0.81 .407 0.81 0.374 0, 13 solution) disodium -dihidrogén- 3.3 5.09 25.33 4.22 pyrophosphate tetrasodium 1.28 pyrophosphate 2.66 6, 65 1.33 - - Sodium fluoride Sodium- 0.24 0.24 0.24 0.24 0.24 -szacharid 0.46 0.46 0.25 0.25 0.46 Titanium dioxide 0.5 0.5 0.5 0.5 0.5

• · 4

Silicon-

-dioxide 22 22 22 22 22 Glycerol 2.25 2.25 8 2.25 2.25 Carboxymethyl -cellulose 0.5 0.5 0.75 0.75 xanthan gum 0.4 0.4 0.75 0.75 0.75 Hydroxyethyl -cellulose - - 0.75 - Natra-lauryl -sulfate (27.9% aqueous solution) 4 4 4 4 4 Flavoring agent 1.1 1.1 1 1 1 KOH / HCl and water: PH 7.5 8.0 8.0 8.0 8.5 with

100% additional quantity

The pH of the suspension is 7.5 to 8.5

-16. examples:

In the following examples, mouthwash and mouthwash compositions of the invention are prepared by conventional methods. The composition of the formulations is shown in the following table, and the figures given for the composition are expressed as a percentage by weight. During manufacture, each formulation is maintained at a pH of at least 7.5.

Example

component 12 13 14 15 16 Glycerol 10 10 10 10 10 ethanol 10 10 10 10 10 Sodium citrate 0.41 3, 84 - - 1.28 Citric acid - - 11, 40 3, 80 - Zinc chloride - 1.36 - - - Zinc Oxide 0,081 - 1, 63 0, 81 0.41 tetrapotassium pyrophosphate (60% aqueous solution) 1.10 - - 5, 51 1.1 tetrasodium pyrophosphate - - - 2, 66 0.27 Sodium- tripolyphosphate - - 7.36 - 0, 37 disodium -dihidrogén- pyrophosphate - 6, 66 - - 0.22 Sodium lauryl -sulfate 0.4 0.4 0.4 0.4 0.4 Sodium- -szacharid 0.03 0.03 0.03 0.03 0, 03 0.03 Flavoring agent 0.22 0.22 0.22 0.22 0.22 0.22 KOH / HCl and water: pH 7.5 8.5 with 8.5 with 7.5 8.0

100% additional quantity

Of course, any modified version of the compositions of the present invention is within the scope of the invention.

Claims (9)

Claims An oral care composition for treating or preventing plaque, tartar and gingivitis or mouth odor, characterized in that it comprises: (a) (i) a source of zinc containing a safe and effective amount of zinc ions; (ii) a source of citrate ion; and (iii) one or more anti-scaling agents, which may be pyrophosphate, phosphonate, diphosphate or a pharmaceutically acceptable linear condensed polyphosphate (Pn ° (3n + 1)) ( ^{n + 2} ) wherein n is 2- from 21 to 21; in the composition, the molar ratio of zinc to zircrate is at least about 1: 1 and the molar ratio of zinc to pyrrole is at least about 1: 1; and b) a pharmaceutically acceptable carrier for topical treatment of the mouth. Composition according to claim 1, characterized in that the molar ratio of zinc to citrate ions is from 1: 1 to 1: 20, preferably from 1: 1 to 1: 5, and more preferably from 1: 1. ) - - (1: 4), molar ratio of cyclones to anti-scaling agent (1: 1) - - (1:20), preferably (1: 1) - (1: 8) and more preferably (1: 1) - (1: 5). Composition according to any one of claims 1 or 2, characterized in that the composition has a pH of from 9 to 9, preferably from 7.5 to 8.5 and a molar ratio of citrate ions to anti-tartar agent. the amount ranges from 3 to 9. Composition according to any one of claims 1 to 3, characterized in that a toothpaste in which the pharmaceutically acceptable carrier for topical treatment of the mouth preferably contains a tooth-grinding material. Composition according to any one of claims 1 to 4, characterized in that it contains from 0.1 to 2% by weight, preferably from 0.25 to 1% by weight, of zinc ions. Composition according to any one of claims 1 to 3, characterized in that a mouthwash, wherein the pharmaceutically acceptable carrier for topical treatment of the mouth preferably comprises a wetting agent, ethanol and a nonionic surfactant. Composition according to any one of claims 1 to 3 and 6, characterized in that it contains from 0, 005 to 0.5% by weight of zinc ion. 8. 1 - composition according to any claim 7, wherein said inhibiting calculus deposition agent is pyrophosphate, EHDP, AHP or a (P _n O (3 _n + l)) ^{(n +} 2) ^- linear condensed polyphosphates of the formula - wherein n is 6, 13 or 21 - preferably pyrophosphate. A composition according to any one of claims 1 to 8, characterized in that it contains sufficient sources of fluoride to provide a fluorine concentration of 0.0025 to 5% by weight.