Oral care compositions comprising chlorite

Technical area

The present invention relates to oral care compositions, including therapeutic mouthwashes and Mouth sprays comprising an effective amount of chlorite ion. These Invention further relates to the use of a Chloritionenquelle in the manufacture of such oral care compositions for treating or prevention of bad breath as well as for bleaching teeth with Humans or other animals.

Hinterergrund of the department

halitosis and discoloration the teeth are generally undesirable states, the many people concern. First is the foul smell the oral cavity also known as halitosis or bad breath. It is generally estimated, that in the US 20-90 million People suffering from halitosis. It is generally assumed that the cause For this State to the presence of anaerobic bacteria, especially gram-negative anaerobic bacteria, is due in the mouth. These bacteria produce volatile Sulfur compounds (volatile sulfur compounds, VSC) which are known to halitosis cause.

On the art is known that bad breath is caused by three chemical compounds. More specifically, these compounds hydrogen sulfide (HSH), methyl mercaptan (CH₃SH) and dimethyl sulfide (CH₂-S-CH₃). These compounds arising from the degradation of epithelial cells and bacteria in the oral cavity. More accurate the polypeptide chains consist of Epithelzellwände of a series of amino acids including cysteine and methionine which sulfur side chains. The dying microorganisms or epithelial cells has the degradation of polypeptide chains to the amino acids components thereof, especially cysteine ​​and methionine, the consequence. cysteine ​​and Methionine are precursors for the Formation of VSCs.

On the art is also known that bad breath not only from rear dorsum but resulting also from periodontal pockets. also a person with gingivitis or periodontitis stronger halitosis own by degraded epithelial cells. Epithelial cells are faster terminated if inflammation is available. Therefore, there remains a large number of dead Epithelial cells in the oral cavity and is bad for the odorous compounds degraded.

Moreover VSCs change the epithelial barrier, which the penetration of the barrier by antigenic substances possible. For example, wear VSCs as hydrogen sulfide and Methylcarptan Dimethyl sulfide to the penetration of bacterial toxins through the Epithelial barrier into the underlying basal membrane and the underlying Connective tissue at. Rizzo A., Peridontics 5 (1967), 233-236; ng W. and Tonzetich J., J. Dental Research 63 (7) (1984), 994-997; Solis-Gaffar MC, Fischer and TJ Gaffar A., ​​J. Soc. Cosmetic Chem. 30 (1979), 241-247. Thereafter bacterial toxins, bacteria and viruses into the underlying Gingival tissue penetrate directly beside the Subcuticularraum and then the underlying connective tissue affected. A reduction in the VSCs reduced tissue permeability for oral toxins and bacteria.

general diseases can also contribute to bad breath. These disorders include oral carcinomas, Diabetes, liver and kidney abnormalities, medications which the oral environment change, ENT problems such as chronic sinusitis, tonsillitis and inflamed adenoids one. Gastrointestinal problems not contribute to chronic bad breath in, although this is a widespread Acceptance. The determination and diagnosis of halitosis can with the Halimeter (InterScan) done. The Halimeter is a gas analysis sensor, which the volatile Sulfur compound measured in the breath.

Of further periodontal disease is also an undesirable condition which occurs very frequently. Periodontal disease is a major cause of tooth loss in adults, which begins at the age of 12 years. At the age of 15 years is 1 possible that 4 of 5 persons already suffering from gingivitis and possibly At least 4 out of 10 people suffering from periodontitis.

periodontitis befalls the attachment apparatus, ie, the surrounding and supporting tissues, which a enclose tooth (Ie, the periodontal ligament, the gingiva, and the alveolar bone). Gingivitis and periodontitis are inflammatory diseases of the gums or the deeper periodontal tissues.

it is well-known that periodontal disease with the accumulation of plaque on the teeth as<?page 3?>is soziiert. The teeth covered with a proteinaceous material saliva (pellicle) and thereafter adhere to streptococci to this covering. Gingivitis results from the dental plaque, and periodontitis is caused by infection, which which in the periodontal pocket or space between Gum and the tooth root spread.

moreover consumers are keen to make their teeth whiter. consumer consider people with whiter tooth as people with more confidence and better social Acceptance.

comprise teeth both an inner dentin layer and an outer hard enamel layer. The enamel layer protects the inner dentin layer and live tissue and serves as the contact surface for mastication of solid food. The enamel layer is generally transparent and has a slightly off-white color. It is also believed, that they is porous, since the hydroxyapatite crystals, from which the tooth is melting, microscopic hexagonal rods form or prisms having microscopic pores or channels between them. As Result of this porous structure can anfärbende Agents and discoloring substances, such as antibiotics, anfärbende Materials containing foods, coffee, cola, tea, tobacco, etc., penetrate the enamel and change its surface so as to yellow or brownish colored appears.

Although good oral hygiene, such as by brushing the teeth with a cleansing dentifrice is reached, may contribute to the incidence of Flekken, gingivitis, to reduce dental plaque, periodontal and / or halitosis, prevent or they do not necessarily eliminate their occurrence. microorganisms contributing both to the initiation and progression of gingivitis, Dental plaque, periodontal and / or halitosis at. To avoid these conditions treat or must these microorganisms therefore by any other means than a simple mechanical cleaning can be suppressed. It should also the simple mechanical cleaning not quite enough to all types of stains remove and / or the teeth to bleach.

Therefore is a big Part of the research on the development of therapeutic Compositions have been aligned, in which the suppression of Microorganisms are effective. The research had the goal effective bleaching compositions to develop. Part of this Research has focused on oral care compositions, chlorine dioxide or chlorine dioxide generating compounds include. Chlorine dioxide is a very strong oxidant and is known as a known broad-spectrum antibiotic.

Of the Prior art discloses compositions and methods that use chlorine dioxide for the treatment of various oral care conditions. Most of these references in the prior art teaching, that the Release of chlorine dioxide for the provision of effectiveness is necessary. This is in contrast to the present invention, which differs from the release Chlorite in the oral cavity concentrated to provide efficacy. compositions and method of the present invention are specifically and been purposely developed to the production of chlorine dioxide in to avoid or minimize the compositions.

Of the Prior art teaches a variety of methods to chlorine dioxide release in Oral Care Compositions in the oral cavity. For example . Teach the US Patents Nos 4,689,215, issued August 25, 1987; 4,837,009, issued June 6, 1989; 4,696,811, issued September 29, 1987 4,808,389, issued February 28, 1989; 4,786,492, issued November 22, 1988; 4,788,053, issued November 29, 1988; 4,792,442, issued on 20 December 1988; 4,818,519, issued April 4, 1989; 4,851,21, issued July 25, 1989; 4,855,135, issued August 8, 1989 4,793,989, issued December 27, 1988; 4,886,657, issued December 12, 1989; 4,889,714, issued December 26, 1989; 4,925,656, issued May 15, 1990; 4,975,285, issued December 4, 1990; 4,978,535, issued on 18 December 1990; 5,200,171, issued May. 6 April 1993; 5,348,734, issued September 20, 1994; 5,618,550, issued April 8, 1997 and 5,489,435, issued February 6, 1996 all to Perry A. Ratcliffe, oral care compositions and methods of treatment using stabilized chlorine dioxide.

More References in the prior the technique which the production and release of chlorine dioxide with activator compounds such as Bronsted acids, reducing Sugar activators, etc. teach include: US Patent Nos 5,281,412,. Lukacovic et al., Issued January 25, 1994, The Procter &amp; Gamble Co .; 5,110,652, Kross et al., Issued March 31, 1992 Alcide Corporation; 5,019,402, Kross et al., Issued on 28. May 1991 Alcide; 4,986,990, Davidson et al., Issued January 22, 1991 Alcide; 4,891.216, Kross et al., Issued on&lt;?page 4?&gt;January 2, 1990, Alcide; 4,330,531, Alliger, issued May 18, 1982;<patcit><text>DE 2,329,752</text></patcit>, Published on December 13, 1973 National Patent Development Corp .; <patcit><text>EP 287.074</text></patcit>, Kross et al. Published, October 19, 1988, Alcide; <patcit><text>EP 565.134</text></patcit>, Kross et al., Published October 13, 1993 Alcide; and WO / 95/27472, Richter published on 19 October 1995; and WO 96/04235, Montgomery, published on 5 February 1998th

More References in the prior art relating Chlordioxidzusammensetzungen include: GB 2,289,841, Mehmet published on 12 June 1995, Janina International; GB 2,290,233, Drayson et al., published On 20 December 1995, Medical Express Limited; WO 96/25916, Van Den Bosch et al. Published, on 29 August 1996, Diamond White; <patcit><text>JP 054.311</text></patcit>, Tsuchikura, published on March 28, 1985; <patcit><text>JP 105.610</text></patcit>, Tsuchikura published June 11, 1985; and WO / 89/03179, Partlow et al., published on April 20, 1989, New Generation Products.

The above references prior the art have not recognized that the release of chlorite ion even in the oral cavity for the Efficacy in various oral care conditions ensures. Since the references according to the state art focused on the release of chlorine dioxide for efficacy can have the compositions and methods of treatment according to the prior of the art have various disadvantages. For example, chlorine dioxide Compositions comprising aesthetic Disadvantages as a "chlorine" flavor and -smell (Eg as in the pool) have. In addition, chlorine dioxide comprehensive Compositions due to the strong oxidizing power of chlorine dioxide certain stability disadvantages, particularly in oral care formulations possess.

Therefore are the above-mentioned Compositions according to the state the art for the treatment and / or prevention of gingivitis, plaque, Periodontitis and / or bad breath or for bleaching of the teeth is not completely been satisfactory. Therefore, for these purposes additional effective compositions and methods of treatment desirable.

how mentioned above, The present invention relates to the release of chlorite ion in the oral cavity for a Effectiveness. The present invention is designed expressly so that the generation of chlorine dioxide or chlorous acid is avoided or minimized in the compositions. The present invention therefore relates to oral care compositions comprising chlorite ion, wherein no) (or only a very small proportion of) chlorine dioxide or chlorous acid is produced or in the oral care compositions at the time is the application available. also The present invention relates to oral care compositions, comprising chlorite ion with relatively alkaline pHs at pH values ​​above 7.6, whereby no) (or only a very small proportion of) chlorine dioxide or chlorous acid is produced or in the oral care compositions at the time is the application available. Further, compositions of the invention include at least a minimum amount of chlorite ion for effectiveness. These compositions and method (the present invention) are effective even if any) (or only a very small proportion of) chlorine dioxide or chlorous acid is generated or is present in these compositions.

The This invention has the purpose of compositions for the treatment or preventing conditions such as bad breath in people or other animals through the use of an effective amount of chlorite ion to provide, with no) (or produces only a very small proportion of) chlorine dioxide or chlorous acid is or in the oral care composition at the time of application is available. The pH of the final composition is alkaline, ie, greater than pH 7.6.

The present invention also has the purpose, compositions for Teeth bleaching in humans or other animals through the use of an effective provide amount of chlorite ion wherein no) (or only a very small proportion of) chlorine dioxide or chlorous acid is generated or in the oral care composition is present at the time of application. The pH of the final composition is alkaline, ie, greater than 7.6.

The This invention further relates to oral care compositions, including therapeutic rinses, particularly mouthwashes, and oral sprays. These compositions comprise a minimum effective Amount of chlorite.

These Compositions are in the killing of bacteria and / or of change of bacterial metabolism, and / or effective for a period of time to to suppress the growth of microorganisms, which topically treatable Infections and diseases of the oral cavity such as plaque, gingivitis, Periodontitis and / or bad breath, cause. These compositions are also in the bleaching &lt;?page 5?&gt;the teeth effective.

Summary the invention

The present invention relates to mouthwashes and oral sprays for oral care, full: <ul><li>(A) a safe and effective amount, preferably a minimum effective amount of chlorite ion; and</li><li>(B) a pharmaceutically-acceptable topical, oral carrier;</li></ul>in which the proportion of chlorine dioxide or chlorous acid in the final composition less than 1 ppm; and wherein the pH of the final composition is greater than 7.6. More preferably, the pH of the composition is greater than the sixth

Detailed Description of the Invention

The This invention relates to compositions for the treatment or preventing bad breath and whitening teeth at Humans and other animals by topical application of a safe and effective amount of chlorite ion to the oral cavity.

By "safe and effective Amount "as herein used is an amount of chlorite meant that sufficient is to modify the condition to be treated significantly (positively) or to give the desired causing bleaching result but which is small enough to serious Side effects (at a reasonable Benefit / risk ratio) within the scope of sound medical / dental review to prevent. The safe and effective amount of chlorite ion varies with the individual to be treated State (eg for inducing a bleaching or for treating bad breath), the age and physical condition of the patient to be treated, the severity of Condition, the duration of treatment, the nature of concurrent Therapy, the specific form (ie, salt) of the chlorite source employed and the individual vehicles, administered by the chlorite will.

By "oral care composition" or "oral composition" as used herein, is meant a product which is not intentionally for the purpose of swallowed systemic administration of therapeutic agents is, but in the oral cavity for one sufficient period of time is left, to substantially all of the tooth surfaces and / or Mucosal tissues of the mouth for the purpose of oral activity so to be contacted:

Chloritionenquelle

The present invention includes Chlorite ion as an essential ingredient in the inventive compositions and procedures. The chlorite ion can be of any type chlorite be derived. Examples include alkali metal chlorites, alkaline earth metal chlorites and any other transition metals, inner Übergangsmetallchlorite and / or polymeric salts. are water-soluble chlorite preferred. Examples of suitable metal chlorites include calcium chlorite, Barium chlorite, magnesium chlorite, lithium chlorite, sodium chlorite and potassium chloride a. Sodium chlorite and potassium chlorite are preferred. sodium chlorite is particularly preferred. Mixtures of two or more chlorite can also be used.

Without to be bound by any theory, the present inventors at that chlorite an antimicrobial Akitivität, especially selectivity for Gram-negative anaerobic bacteria, for Oral care compositions provide.

For inventive mouthwash compositions is the fraction of the chlorite ion is greater than 0.04 wt .-%, preferably greater than 0.075 wt .-%, more preferably greater than 0.15 wt .-% of the composition.

To the Teeth bleaching the compositions comprise preferably 0.75 wt .-% of bis 6 Composition of chlorite.

in the Associated with a reduction or elimination of halitosis see the inventive compositions a long-lasting breath protection against, for example, longer than about 3 hours.

preferably the compositions comprise from 0.04 to 6%, of chlorite ion, based weight &lt;?page 6?&gt;of the composition, for the treatment or prevention bad breath and for a more than about 3 hours lasting respirator.

chlorite are available as sodium from various suppliers. Sodium chlorite is commercially available as a powder or in the form of flakes technical grade and as an aqueous, liquid Concentrate available in a range of concentrations. examples for Sources of sodium chlorite include sodium chlorite, a which available from Aragonesas and from Vulcan. These sources have also generally not more than 4% sodium chlorate on. preferably the ratio of chlorite to chlorate is greater than 8: 1 and generally about 20: 1.

preferably Chloritionenquelle, the high purity, eg 70% or greater. Further are compositions of the invention preferably substantially free of Hypochloritmetallsalzen or Hypochlorite ion, dichloroisocyanurate, or salts thereof.

preferably the proportion of chlorite by gradient separation of inorganic and organic acid anions using a Pac ASII ion exchange column, available from Dionex Corporation, Sunnyvale, CA, measured.

The finished compositions of the present invention comprise less than 1 ppm of chlorine dioxide or chlorous acid.

For biphasic Compositions the level of chlorine dioxide or chlorous Acid within measured about 2 to 3 minutes after mixing together the two phases.

analytical methods to measure the proportions of chlorine dioxide or chlorous acid in the compositions of the invention are known in the art. For example: Clesceri LS, Greenberg AE and Trussell RR, Standard Methods for the Examination of Water and Wastewater, 17th Edition, American Public Health Association, Washington, DC, 1989, pp 4-75 to 4-83; Aieta EM, Roberts PV and Hernandez M., J. Am. Waterworks Assoc. 76 (1) (1984), pp 64-70; Pfaff JD and Brockhoff CA, J. Am.

Water Works Assoc. 82 (4) (1990), pp 192-195; Gordon G., Cooper W. J., Rice G. and Pacey GE, J. Am. Water Works Assoc. 80 (9) (1988), S. 94-108); Harp DL, Klein RL and Schoonover DJ, J. Am. Waterworks Assoc. 3 (7) (1981), pp 387-389; Gordon G., Cooper WJ, Rice RG and Pacey GE, Am. Water Works Assoc. Res. Foundation, Denver, Colo., 1987, S. 815th

Of the pH of the final composition (either a single phase or a two-phase composition) of the present invention is greater than 7.6, more preferably greater than 8. preferably the pH of the final composition of 8 to 12; more preferably, the pH 10th

For mouthrinse compositions the pH of the final composition is greater than 7.6, preferably greater than 8. Preferably, The pH of the final composition 8 to 12; more preferably, the pH 10th

For biphasic Compositions is the pH after mixing the two measured phases and is not based on the pH of a single phase prior to mixing.

pharmaceutical acceptable excipients

By "pharmaceutically acceptable Excipient "or" pharmaceutically acceptable, oral carrier ", as used herein, are one or more compatible solid or liquid filler diluents or encapsulating meant that for topical, oral administration are suitable. "Compatible" with, as used herein, is meant that the Components of the composition are miscible in a manner so that no Interaction which the stability and / or efficacy A composition for treating or preventing halitosis, Dental plaque, gingivitis and periodontitis and for whitening teeth in accordance with the compositions and methods of the present invention would be significantly reduced.

The carrier or excipient the present invention may the usual and conventional Components of toothpastes (including gels and gels for subgingival Application), mouth rinses, Mouth sprays, chewing gums, and lozenges (including breath mints for a fresh &lt;?page 7?&gt;including respiratory) detailed as follows will be described.

The compositions of the invention can dual phase compositions or single phase compositions be. The chlorite ion is relatively reactive and will react with certain carriers or excipients, which are generally used in oral care compositions. by virtue of this reactivity are the preferred compositions of the present invention therefore two-phase compositions. These compositions comprise a first phase and a second phase, wherein <ul><li>(A) the first phase comprising the chlorite ion, and</li><li>(B) the second phase comprises a pharmaceutically-acceptable topical, oral vehicle includes and no chlorite comprises.</li></ul>

These two-phase compositions comprise two phases, wherein chlorite ion is introduced into a first phase, said second phase of the must be kept separated. The first phase comprising chlorite ion can additionally pharmaceutically acceptable topical, oral carrier include which are compatible with chlorite ion. preferably includes the first phase in addition to chlorite (s) (or more) compatible binder (s), Humectants, buffers and / or preservatives. preferably includes the second phase, which comprises no chlorite, a flavoring agent, a surfactant, fluoride ions and / or an abrasive.

Usually each phase in these two phase compositions in a separate container or in a single container with two compartments contain.

In front the use of a two-phase composition by the consumer , the two phases by coextrusion of the two separate phases, preferably in a volume ratio of 1: 1, combined, and the composition is preferably immediately after manufacture, ie, within about 5 minutes, is used.

The two phases can However, about 1 minute to about 1 hour before use, or during the Use of the composition are combined.

Phase Two containers in U.S. Patents Nos. 5,052,590, Ratcliffe, issued on October 1 1991 and 4,330,531, Alliger, issued May 18, 1982 discloses.

in another preferred embodiment, is the chlorite until immediately prior to use substantially anhydrous. For example, a mouthwash solution is immediately before use by solving in water of a substantially anhydrous concentrate of chlorite manufactured to the required application concentration.

The Choice of a carrier to be used is substantially determined by the path over which the composition in the oral cavity is to be introduced.

If a mouthwash to be used is selected, a "mouth rinse carrier" as for example in US Pat. No. 3,988,433 to Benedict disclosed (eg water, Flavorings and sweeteners, etc.). Similarly Way is chosen, a "mouth spray carrier" if a mouth spray is to be used. The compositions of the invention for the preparation of suitable carrier are known in the art sufficient. Your choice depends on secondary Considerations like taste, cost, and shelf stability, etc. from.

The compositions of the invention are mouthwashes including Oral sprays. Components of such mouthwashes and mouth sprays typically include one or more of the following one: water (about 45 to about 95%), ethanol (from about 0 to about 25%), a humectant (from about 0 to about 50%), a surfactant (from about 0.01 to about 7%), a flavoring agent (About 0.04 to about 2%), a sweetening agent (About 0.1 to about 3%) and a colorant (About 0.001 to about 0.5%). Such mouthwashes and mouth sprays may also one or more of an anticaries agent (from 0.05 to 0.3% as fluoride ion), and Anticalculus agents include (about 0.1 to about 3%).

Other preferred compositions of the present invention are dental solutions. Components of such dental solutions conclude generally one or more of the following one: water (About 90 to about 99%), preservative (from about 0.01 to about 0.5%), a thickener &lt;?page 8?&gt;(About 0 to about 5%), a flavoring agent (About 0.04 to about 2%), a sweetening agent (About 0.1 to about 3%) and a surfactant (from about 0 to about 5%).

The compositions of the invention are preferably substantially free of organic solvents. The compositions of the invention are also preferably essentially free of peroxy compounds.

carrier or Oral care excipient types, which in the compositions according to the invention may be included, together with specific examples, are:

Foaming agents (Surfactants)

Suitable foaming agents include those which sufficiently stable are and a big produce a foam pH range. Foaming agents include nonionic, anionic, amphoteric, cationic, zwitterionic and synthetic Detergents, and mixtures thereof. Many suitable nonionic and amphoteric surfactants are disclosed in US Pat. No. 3,988,433 to Benedict and US Patent 4,051,234, issued September 27, 1977 discloses; and many suitable nonionic surfactants are in Agricola et al., US Patent 3,959,48, issued May 25, 1976..

a.) Nonionic and amphoteric surfactants

Nonionic Surfactants useful in the compositions according to the invention are able are generally defined as compounds produced by the condensation of alkylene oxide groups (hydrophilic in nature) with an organic hydrophobic compound, aliphatic or alkyl-aromatic in nature may be prepared. Examples of suitable nonionic include surfactants Poloxamers (sold under the trade name Pluronic), polyoxyethylene sorbitan esters (Sold under the trade name Tween), fatty alcohol ethoxylates, Polyethylene oxide condensates of Alkylphenoien selected from the condensation of ethylene oxide with the reaction product of propylene oxide and ethylenediamine derived product, ethylene oxide condensates of aliphatic alcohols, long chain tertiary Amine oxides, long chain tertiary Phosphine oxides, dialkyl sulfoxides and mixtures of such long chain Materials.

The useful in this invention amphoteric surfactants can be broadly described as derivatives of aliphatic secondary and tertiary Amines in which the aliphatic radical can be straight or branched can, and wherein one of the aliphatic substituents contains from about 8 to contains about 18 carbon atoms, and one contains an anionic water-solubilizing group, for example carboxylate, Sulfonate, sulfate, phosphate, or phosphonate. Other suitable amphoteric Surfactants are betaines, cocamidopropyl accurate. mixtures of amphoteric surfactants can also be used.

The present composition can typically be a nonionic Surfactant, an amphoteric surfactant or a combination of a nonionic and amphoteric surfactant each at a level of about 0.025 to about 5%, preferably about 0.05 to about 4%, and most preferably about 0.1 to about 3% comprise.

b.) Anionic surfactants

Here in useful include anionic surfactants the water-soluble Salts of alkyl sulfates having from 8 to 20 carbon atoms in the alkyl radical (Eg, sodium alkyl sulfate) and the water-soluble salts of sulfonated monoglycerides of fatty acids with 8 to 20 carbon atoms. Sodium lauryl sulfate and sodium coconut monoglyceride sulfonates are examples of anionic surfactants of this type. Other suitable anionic surfactants are sarcosinates such as sodium lauroyl, taurates, sodium lauryl, Sodium lauroyl, Natriumlaurethcarboxylat and sodium dodecylbenzenesulfonate. Mixtures of anionic surfactants can also be used. The present composition typically comprises an anionic Surfactant in a proportion of about 0.025 to about 9%, preferably about 0.05 to about 7%, and most preferably about 0.1 to about 5%.

fluoride ions

The present invention may also include free fluoride ions. Preferred free fluoride ions can by sodium fluoride, tin (II) fluoride, indium, and sodium monofluorophosphate be provided. Sodium fluoride is the most preferred free fluoride ion. Norris et al., US Patent 2,946,725 issued,&lt;?page 9?&gt;at the July 26, 1960, and Widder et al., US Patent 3,678,154, issued on July 18, 1972, disclose such salts as well as others.

The present composition may 50 ppm to 3,500 ppm and preferably 500 ppm to 3000 ppm of free fluoride ions contained.

flavorings and sweeteners

flavorings can also be added to the compositions. Suitable flavorings conclude Wintergreen oil, peppermint oil, spearmint oil, clove bud oil, menthol, Anethole, methyl salicylate, eucalyptol, cassia, 1-menthyl acetate, sage, Eugenol, parsley oil, Oxanon, alpha-Irison, marjoram, lemon, orange, Propenylguaethol, Cinnamon, vanillin, thymol, linalool, Zimtaldehydglycerolacetal, known as CGA, and mixtures thereof. Flavorings are generally in the co compositions at levels of from about 0.001 to about 5 wt .-% of the composition.

Usable sweeteners conclude Sucrose, glucose, saccharin, dextrose, levulose, lactose, mannitol, sorbitol, Fructose, maltose, xylitol, saccharin salts, thaumatin, aspartame, D-tryptophan, Dihydrochalcones, acesulfame and cyclamate salts, especially sodium cyclamate and sodium saccharin, and mixtures thereof. A composition contains preferably about 0.1 to about 10% of these agents, preferably from about 0.1 to about 1 wt .-% of the composition.

In addition to the flavors and sweeteners can Coolant, the salivation-promoting Means, heating means and narcotics used as optional ingredients in the inventive compositions will. These agents are present in the compositions at a level from about 0.001 to about 10 wt .-%, preferably about 0.1 to about 1 wt .-%, of the composition.

The coolant Any of a large its wide variety of materials. Such materials include carboxamides, Menthol, ketals, diols, and mixtures thereof. Preferred coolant in the present compositions are the Paramenthancarboxyamidmittel such as N-ethyl-p-menthane-3-carboxamide, known commercially as "WS-3"; N, 2,3-trimethyl-2-isopropylbutanamide known as "W-23"; and mixtures . thereof Further preferred coolant are selected from the group consisting of menthol, 3-1-menthoxypropane-1,2-diol, known as TK-10 manufactured by Takasago; Menthonglycerolacetal, known as MGA, manufactured by Haarmann and Reimer; and menthyl lactate, known as Frescolat^®Manufactured by Haarmann and Reimer. The terms menthol and menthyl as used herein, conclude right- and left-handed isomers of these compounds and racemic Mixtures thereof. TK-10 is described in US Pat. No. 4,459,425, Amano et al., issued 10/07/84, describes. WS-3 and other agents are in US Pat. No. 4,136,163, Watson et al., issued January 23, 1979..

Preferred slime formation promotional Agent of the present invention include Jambu^®, produced by Takasago, a. Preferred warming agents include capsicum and nicotinate esters, such as benzyl a. Preferred drugs conclude Benzocaine, lidocaine, clove bud oil and ethanol.

Anticalculus agent

The present invention includes also an anticalculus agent a, preferably a pyrophosphate ion source, which is derived from a pyrophosphate salt. The in the present useful compositions close pyrophosphate the Dialkalimetallpyrophosphatsalze, Tetraalkalimetallpyrophosphatsalze and mixtures thereof. Disodium dihydrogen pyrophosphate (Na₂H₂P₂O₇), Tetrasodium pyrophosphate (Na₄P₂O₇) And pyrophosphate (K₄P₂O₇) thereof in the unhydrated as well as hydrated forms are the preferred species. compositions according to the invention to co may be the pyrophosphate salt in one of three ways: primarily solved mainly unsolved or as a mixture of dissolved and undissolved Pyrophosphate.

compositions comprising predominantly dissolved Pyrophosphate refer to compositions where at least A pyrophosphate ion source in an amount sufficient, provide at least about 1.0% free pyrophosphate ions. The Amount of free pyrophosphate ions may be from about 1 to about 15%, preferably about 1.5 to about 10%, and most preferably about 2 to about 6% be. Free pyrophosphate ions may vary depending on the pH of the composition be in a variety of protonated states.

&lt;?page 10?&gt;

compositions comprising mainly unsolved Pyrophosphate refer to compositions containing no more than about 20% of the total pyrophosphate salt dissolved in the composition, preferably less than about 10% of the total pyrophosphate salt dissolved , Contained in the composition. The Tetranatriumpyrophosphatsalz is the preferred pyrophosphate salt in these compositions. Tetrasodium pyrophosphate may be in the anhydrous salt form or decahydrate form or in any other species which in solid form in the dentifrice compositions is stable, present. The salt is in solid particle form thereof, which correspond to the crystalline and / or amorphous state thereof can, wherein the particle size of the salt preferably is sufficiently small to aesthetically during use acceptable and readily soluble to be.

The compositions may a mixture of dissolved and unresolved Pyrophosphate salts include. Each of the above mentioned pyrophosphate salts may be used.

The Pyrophosphate salts are in Kirk &amp; Othmer, Encyclopedia of Chemical Technology, Third Edition, Volume 17, Wiley-Interscience Publishers (1982), detail described.

Optional Means, which, instead of or in combination with the pyrophosphate salt may be used conclude such known materials as synthetic anionic polymers, including Polyacrylates and copolymers of maleic anhydride or maleic acid and Methyl vinyl ether (eg Gantrez) as described for example in US Patent 4,627,977 to Gaffar et al., The disclosure of which herein incorporated by reference in its entirety; as well as Polyaminopropansulfonsäure (AMPS), zinc citrate trihydrate, Polyphosphates (eg tripolyphosphate; hexametaphosphate), diphosphonates (Eg EHDP; AHP), polypeptides (such as polyaspartic and polyglutamic acids), and Mixtures thereof.

Alkali Metal Bicarbonate

The present invention may also include an alkali metal bicarbonate salt. Alkali metal bicarbonate are soluble in water and tend unless stabilized, carbon dioxide in a aqueous system release. Sodium bicarbonate, also known as baking soda, is the preferred alkali metal bicarbonate salt. The present compositions can about 0.5 to about 30%, preferably about 0.5 to about 15%, and most preferably about 0.5 to about 5% of a Alkalimetallbicarbonatsalzes contain.

Various supports

The in the preparation of commercially suitable oral compositions Water used should preferably be of low ion content exhibit and free of organic contamination be en. water includes generally from about 5 to about 70 wt .-%, and preferably about 20 to about 50 wt .-% of the composition herein. These amounts of water conclude free of water, which in addition to the water with other materials as with sorbitol, added added becomes.

titania can also be added to the present composition. Titanium dioxide is a white Powder for opacity the compositions contributes. Antimicrobial anti-plaque agents can also optionally in oral Compositions exist. Such agents may, but are not limited to, triclosan; 5-chloro-2- (2,4-dichlorophenoxy) phenol, as described in The Merck Index, 11th edition (1989). S. 1529 (Entry no. 9573), in US Patent No., 3,506,720 and European Patent Application . No. 0,251,591 of Beecham Group, PLC, published January 7, 1988; Chlorhexidine (Merck Index, No. 2090th); Alexidine (Merck Index, no. 222); Hexetidine (Merck Index, No. 4624th); Sanguinarine (Merck Index, No. 8320). Benzalkonium chloride (Merck Index, No. 1066th); salicylanilide (Merck Index, No. 8299th); Domiphene bromide (Merck Index, No. 3411th); Cetylpyridinium (CPC) (Merck Index, No. 2024th); Tetradecylpyridinium chloride (TPC); N-tetradecyl-4-ethylpyridinium chloride (TDEPC); octenidine; delmopinol, Octapinol and other Piperidinoderivate; Nicinzubereitungen; Zinc / Zinnionenmittel; Antibiotics such as Augmentin, amoxicillin, tetracycline, doxycycline, Minocycline, and metronidazole; and analogs and salts of the above antimicrobial anti-plaque agents lock in. If present, the antimicrobial anti-plaque agent about 0.1 to about 5 wt .-% of the inventive compositions.

Anti-inflammatories agent can in the oral compositions of the present invention to be available. Such means may, but are not limited to, anti-inflammatory non-steroidal compounds such as aspirin, ketorolac, flurbiprofen, ibuprofen, naproxen, indomethacin, Aspirin, ketoprofen, piroxicam and meclofenamic acid, and mixtures thereof lock in. If present, the anti-inflammatory agents such as 0.001 to about 5 wt .-% of the Composition of the invention&lt;?page 11?&gt;gen. Ketorolac is described in U.S. Patent 5,626,838, issued May 6, 1997,.

Other optional agents include -synthetische, anionic polymeric polycarboxylates, which in Form of the free acids neutralized thereof or partially or preferably fully, water-soluble Alkali metal (eg potassium and preferably sodium) or ammonium salts be used and in US Patent No. 4,152,420 to Gaffar. US Patent No. 3,956,480 to poet et al .; US Patent No. 4,138,477 to Gaffar. US Pat. No. 4,183,914 to Gaffar et al .; and US Pat. No. 4,906,456 to Gaffar et al. disclosed. Preferred are 1: 4 to 4: 1 copolymers of maleic anhydride or maleic acid with another polymerizable ethylenically unsaturated Monomer, preferably methyl vinyl ether (methoxyethylene) with a Molecular weight (MW) of about 30,000 to about 1,000,000. These Copolymers, for example as Gantrez AN 139 (MW 500,000), AN 119 (MW 250,000) and preferably S-97 pharmaceutical grade (MW 70,000) available from GAF Corporation.

The present invention can also optionally selective H₂antagonists including in US Patent 5,294,433, Singer et al., issued March 15, 1994 disclosed compounds include.

Use of the composition

A safe and effective amount of the inventive compositions and / or the chlorite ion can topically applied to the mucosal tissue of the oral cavity, on the gingival tissue of the oral cavity and / or on the surface the teeth for the treatment or prevention of the above mentioned diseases or conditions of the Oral cavity over several conventional Paths are applied. For example, the gingival or Mucosal tissue with a solution (For example, a mouthwash or a mouth spray) containing chlorite, are rinsed.

The Concentration of chlorite ion in the composition according to the invention depends on of the type of composition, which is used to chlorite ion be applied to the gingival / mucosal tissue and / or teeth, as well as by the differences in the efficacy of the compositions in contact with the tissue and teeth, and also of the generally Amount used of the composition. The concentration may also depend on the / the disease to be treated or condition.

The mouthwash for use in the oral cavity has a concentration of chlorite ion in the range of 0.04 to 0.2 wt .-%, and still more preferably 0.1 to 0.2 wt .-% of the composition on. Preferably mouth rinse compositions of the invention set 3.75 to 22.5 mg chlorite in the oral cavity free when about 15 ml of flush be used.

mouth sprays Chloritionenkonzentrationen preferably have from 0.15 to 0.2 Wt .-%, and still more preferably 0.75 to 2 wt .-% of the composition on.

For biphasic Compositions give the above concentrations of chlorite the concentration of chlorite ion after the mixing together of the two phases again, which usually immediately before the application is carried out by the consumer.

A safe and effective amount of chlorite ion is preferably applied to the gum / mucosal tissue and / or the teeth by rinsing with a mouthwash, preferably for at least about 10 seconds, preferably about 20 seconds to about 10 minutes, more preferably about 30 seconds to about 60 seconds, applied. The method often involves expectoration of overriding Portion of the composition following such contact. The frequency is of such contact preferably from about once per week to about four times per day, more preferably from about thrice per week to about three times per day, more more preferably from about once per day to about twice per day. The Period of such treatment typically ranges from about one Day to a lifetime. For particular oral care diseases or conditions the duration of treatment depends on the severity of / of being treated oral disease or condition the individual release form employed and the patient's response the starting treatment. If a release in the gingival pockets required is, as in the treatment of periodontal disease, can be connected to a mouthwash the periodontal pocket using a syringe or Water injection apparatus be issued. These devices are known in the art. Devices of this type include "Water Pik" by Teledyne Corporation on. After rinsing , the individual rinsing moving the mouth back and forth to the tongue back and other gums and mucosal surfaces to cover. additionally can a toothpaste, an abrasive-free gel, a tooth gel &lt;?page 12?&gt;etc. with a brush on the tongue surface applied and other gingival and mucosal tissues of the oral cavity will.

To the Teeth bleaching in the oral cavity is a safe and effective amount of chlorite ion is preferably with or without an oral care device such as a toothbrush, a the composition containing shell, plastic strips (as hereinafter disclosed), etc., on the surface the teeth applied: for mouthwashes or oral sprays preferably at least about 10 seconds, preferably about 20 seconds to about 10 minutes, more preferably about 30 seconds to about 60 seconds. The method often involves expectoration of most of the composition of the after such contact, preferably followed by rinsing, such as with water. The frequency is of such contact preferably from about once per week to about four times per day, more preferably from about thrice per week to about three times per day, more more preferably from about once per day to about twice per day. The Period of such treatment typically ranges from about one Day to a lifetime. The subject may be the application optionally repeat to his teeth to bleach. The duration of treatment is preferably about 3 weeks to about 3 months, but may vary depending on the severity of the tooth discoloration being treated, the individual release form employed and the patient's response less to the treatment or longer be.

The following examples further describe preferred embodiments within the scope of the present invention.

all used herein percentages are based on the weight composition is, unless otherwise indicated.

Examples

The following examples are by conventional methods by mixing represents following ingredients:

example 1: Two-phase mouthwash <img img-content="tb" img-format="tif" he="74" wi="158" file="00170001.tif" />

example 2: Single-phase mouthwash <img img-content="tb" img-format="tif" he="37" wi="132" file="00170002.tif" />

&lt;?page 13?&gt;

example 3: Dry powder for a mouthwash reconstitution <img img-content="tb" img-format="tif" he="50" wi="132" file="00180001.tif" />&lt;!--footnotes removed--&gt;

example 4: Dry powder for a mouthwash reconstitution <img img-content="tb" img-format="tif" he="51" wi="132" file="00180002.tif" />&lt;!--footnotes removed--&gt;

The listed above the dry ingredients are added in any order and mixed until a homogeneous mixture. dye for providing a coloring after the addition of water to the dry mixture are optional.

Production of the finished Mouthwash:

example 3: 1.874 g of dry powder mixture in a small Dosage cup with a lid and added with 15 ml of H₂O mixed. The cup is shaken vigorously until the solids dissolve. The mixture is used to purge used and spat.

example 4: 1.874 g of dry powder mixture in a small Dosage cup with a lid and added with 15 ml of H₂O mixed. The cup is shaken vigorously until the solids dissolve. The mixture is used to purge used and spat.