GB2317339A - Dentifrice composition containing a curcuminoid - Google Patents

Abstract

The composition contains up to 10% of a curcuminoid ie. a curcumin anologue or derivative or a preparation of the plant Curcuma longa and up to 0.35 % fluoride in combination with one or more of an anticalulus agent an antimicrobial agent or an antiplaque agent and one or more carrier materials.

Description

TECHNICAL FIELD The present invention relates to oral compositions for the prevention and treatment of dental caries, periodontal diseases such as gingivitis and periodontitis, and other oral diseases, comprising a curcuminoid such as curcurnin or its derivatives, analogues, or preparations of the plant Curcuma longa or other curcumin-containing plants, a fluoride ion source, and a safe and effective amount of at least one oral active such as an anti calculus agent, antimicrobial/antiplaque agent, antibacterial agent, and the like. The present invenfion also relates to methods for using said compositions.

BACKGROUND OF THE INVENTION While separate compositions for the prevention and treatment of dental caries or periodontal diseases of the soft tissues of the oral cavity have been known for some time, the same can not be said for a single composition for preventing and treating both dental caries and periodontal disease. Periodontal disease is an inflammatory disorder of the supporting tissue of the teeth and one of the most difficult problems in dentistry. It is the major cause of tooth loss in adults over 35 years of age. The two most common periodontal diseases are chronic gingivitis and chronic destructive periodontitis.

Gingivitis is an inflammation of the gingiva, characterized by swelling, redness, changes in normal contours, watery exudate, and bleeding. It is often caused by the infection of the gingiva by bacterial plaque, calculus, and/or mechanical injury.

Left untreated, gingivitis usually results in the formation of periodontal pockets, wherein the bacteria in the plaque attack the periodontium (periodontal tissues supporting the teeth), causing a chronic inflammation of the periodontium known as periodontitis or pyorrhea. In advanced stages of periodontitis, the bacteria eventually erode the bone surrounding the teeth, often resulting in the loss of the affected teeth.

Current therapies for gingivitis and/or periodontitis include improved oral hygiene to eliminate supragingival plaque and calculus, professional prophylaxis to eliminate subgingival calculus, and/or surgery.

Curcumin (diferuloylmethane) is a naturally occurring compound obtained from the rhizomes of Curcuma longa plants. It is a major component of turmeric and commonly used as a spice (curry) and coloring agent for foods, drugs, and cosmetics.

For example, Futagami, et al. disclose, in Japanese Kokoku Patent Application No.

56-27489, adsorbing curcumin onto polysaccharide, polysaccharide derivative, protein, or gel, in an oral hygiene composition, to produce a color change according to the pH of the composition as an indicator that the composition has been in the mouth for a sufficient amount of time to fulfill the purpose of hygienic cleansing of the oral cavity. Curcumin has also been shown to possess anti-inflammatory and antioxidant properties, certain anti-mutagenic and anti-carcinogenic properties, the ability to reduce serum lipid peroxides and cholesterol, and has even been shown to have some efficacy in inhibiting certain aspects relating to the human immunodeficiency virus (HIV). Katyuzhanskaya, et al. disclose, in USSR Inventor's Certificate No.

1132945, incorporating extracts of turmeric or ginger into toothpaste compositions for improved anti-inflammatory effect on tissues of the oral cavity and treatment of certain diseases of the mucous membranes of the oral cavity and marginal periodontosis. Both of these compositions, however, have proven somewhat unsatisfactory.

The present inventor has discovered oral compositions, having improved efficacy and aesthetics, which fulfills the long felt need for a single oral composition which provides the prevention and treatment of dental caries, periodontal diseases such as gingivitis and periodontitis, and other diseases of the oral cavity. The compositions of the present invention comprise a curcuminoid such as curcumin, its derivatives, analogues, or preparations of the plant Curcuma longa or other curcumin-containing plants, a fluoride ion source, and a safe and effective amount of at least one oral active such as an anticalculus agent, antimicrobiaVantiplaque agent, antibacterial agent, and the like.

It is therefore, an object of the present invention to provide oral compositions for the prevention and treatment of dental caries, periodontal diseases such as gingivitis and periodontitis, and other diseases of the oral cavity, comprising a curcuminoid such as curcurnin, its derivatives, analogues, or preparations of the plant Curcuma longa or other curcumin-containing plants, a fluoride ion source, and a safe and effective amount of at least one oral active such as an anticalculus agent, antimicrobial/antiplaque agent, antibacterial agent, and the like.

It is a further object of the present invention to provide methods for the prevention and treatment of dental caries, periodontal diseases such as gingivitis and periodontitis, and other diseases of the oral cavity, using oral compositions comprising a curcuminoid such as curcurnin, its derivatives, analogues, or preparations of the plant Curcuma longa or other curcumin-containing plants, a fluoride ion source, and a safe and effective amount of at least one oral active such as an anticalculus agent, antimicrobiaVantiplaque agent, antibacterial agent, and the like.

All percentages and ratios used herein are by weight, and all measurements made at 250C, unless otherwise specified.

SUMMARY OF THE INVENTION The present invention provides novel oral compositions and methods for prevention and/or treatment of dental caries and periodontal and other diseases of the oral cavity.

The oral compositions of the present invention comprise: a.) from about 0.001% to about 10% by weight, of a curcuminoid such as curcumin, curcumin derivatives, analogues, preparations of the plant Curcuma longa or other curcumin-containing plants, and mixtures thereof; b.) from about 0.005% to about. 0.35% of fluoride ion from a soluble fluoride ion source; c.) a safe and effective amount of at least one oral active such as an anticalculus agent, antimicrobial/antiplaque agent, antibacterial agent, and the like; d. from about 79% to about 98% of one or more orally-acceptable carrier materials; and e. additional antidental caries agents and anti-inflammatory agents.

The present invention also provides methods for the prevention and treatment of dental caries, periodontal diseases such as gingivitis and periodontitis, and other oral diseases, using oral compositions comprising a curcuminoid such as curcumin, its derivatives, analogues, or preparations of the plant Curcuma longa or other curcumin-containing plants, a fluoride ion source, and a safe and effective amount of at least one oral active such as an anticalculus agent, antimicrobiaUantiplaque agent, antibacterial agent, and the like.

DETAILED DESCRIPTION OF THE INVENTION The phrase "safe and effective amount", as used herein, means an amount of a substance high enough to provide a significant positive modification of 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. A safe and effective amount of the substance will vary with the particular condition being treated, the severity of the condition, the duration of the treatment, the nature of concurrent therapy, and like factors.

The terms "treat" and "treatment", as used herein, mean to attempt to slow the progress of or to reverse the symptoms of the condition being addressed.

The terms "effective" and "efficacy", as used herein, mean successful treatment resulting in slowing, halting, or reversing the adverse condition being addressed.

The phrase "orally-acceptable carrier material", as used herein, denotes a carrier which results in a composition which is administered topically to the oral cavity, held therein for a period of time, and then is largely expectorated rather than being swallowed. Such compositions include toothpastes, tooth gels, tooth powders, mouthwashes, mouthsprays, prophylaxis pastes, dental treatment solutions, and the like.

The phrase "topical application", as used herein, means applied so as to contact exposed surfaces of the oral cavity with a composition or compound administered to the exposed surfaces of the oral cavity, preferably by swishing around in the mouth or brushing onto the teeth and/or over oral surfaces, or administered so as to inject or specifically insert into interior cavities, e.g., periodontal pockets, within the oral cavity. Application may also be accomplished by painting the composition or compound onto the oral cavity tissue afflicted with periodontal disease with a swab, gauze, sponge, or cotton ball. The composition or compound is then preferably largely expectorated, except when injected or inserted into interior cavities or swabbed onto the oral cavity tissue afflicted with periodontal disease.

The term "compatible", as used herein, means that the components of the compositions 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.

The term "curcuminoid", as used herein, means curcumin, e.g., (E,E)-1,7 bis(4-hydroxy-3 -methoxyphenyl)-l ,6-heptadiene-3 ,5-dione or diferuloylmethane, its derivatives, analogues, and preparations of the plant Curcuma longa or other curcumin-containing plants and having the basic general formula:

Typical derivatives and/or analogues of curcumin and/or preparations of the plant Curcuma longa or other curcumin-containing plants useful in the present invention include, but are not limited to, p-hydroxycinnamoyl(feruloyl)methane, p,p' dihydroxydicinnamoylmethane, desmethoxycurcumin, bis-desmethoxycurcumin, sodium curcuminate, diacetylcurcumin, triethylcurcumin, and tetrahydrocurcumin.

The essential, as well as optional components of the compositions of the present invention, are described in the following paragraphs.

Oral Compositions The compositions according to the present invention comprise a curcuminoid such as curcumin or its derivatives, analogues, or preparations of the plant Curcuma longa or other curcumin-containing plants, a soluble fluoride ion source, and a safe and effective amount of at least one oral active comprising anticalculus agents, antimicrobial/antiplaque agents, antibacterial agents, and the like. The compositions of the present invention may also comprise additional antidental caries agents and anti-inflammatory agents.

Curcuminoid The first essential component of the present invention is curcumin, its derivatives, analogues, or preparations of the plant Curcuma longa or other curcumin-containing plants. Typical derivatives and/or analogues of curcumin and/or preparations of the plant Curcuma longa or other curcumin-containing plants useful in the present invention include, but are not limited to, phydroxycinnamoyl(feruloyl)methane, p,p'-dihydroxydicinnamoylmethane, desmethoxycurcumin, bis-desmethoxycurcumin, sodium curcuminate, diacetylcurcumin, triethylcurcumin, and tetrahydrocurcumin. Preferred for use herein is curcumin. Turmeric may also be useful in the compositions of the present invention.

Typically, curcumin is present in the compositions of the present invention from about 0.001% to about 10%, preferably from about 0.01% to about 7%, more preferably from about 0.05% to about 3%, and most preferably from about 0.1% to about 0.5% by weight, of the total composition.

Fluoride Ion Source The second essential component of the present invention is a water-soluble fluoride ion source. The number of such fluoride ion sources is great and includes those disclosed in U.S. Patent No. 2,946,735 issued July 26, 1960 to Norris, et al., U.S. Patent No. 3,535,421 issued October 20, 1970 to Briner & Widder, and U.S.

Patent No. 3,678,154 issued July 18, 1972 to Widder, et al., all of which are incorporated herein by reference. Preferred fluoride ion source materials include: sodium fluoride, potassium fluoride, indium fluoride, stannous fluoride, and sodium monofluorophosphate and mixtures thereof. Sodium fluoride is the preferred fluoride ion source. The amount of the fluoride ion source in the oral compositions of the present invention, if present, is preferably sufficient to provide from about 0.005% to about 0.35%, more preferably from about 0.05% to about 0.3% of fluoride ions in the compositions.

Oral Actives The third essential component of the present invention is a safe and effective amount of at least one oral active comprising anticalculus agents, antimicrobial/antiplaque agents, antibacterial agents, and the like. Additional antidental caries agents and anti-inflammatory agents may also be useful in the compositions of the present invention.

Anticalculus Agents: The compositions of the present invention may comprise one or more anticalculus agents, on the condition that they are compatible with the other components of the compositions. Typical examples of such anticalculus agents include, but are not limited to, pyrophosphates or polyphosphates such as those disclosed in U.S. Patent No. 4,590,066 issued to Parran & Sakkab on May 20, 1986; polyacrylates and other polycarboxylates such as those disclosed in U.S. Patent No.

3,429,963 issued to Shedlovsky on February 25, 1969 and U.S. Patent No. 4,304,766 issued to Chang on December 8, 1981; and U.S. Patent No. 4,661,341 issued to Benedict & Sunberg on April 28, 1987; polyepoxysuccinates such as those disclosed in U.S. Patent No. 4,846,650 issued to Benedict, Bush & Sunberg on July 11, 1989; ethylenediaminetetraacetic acid as disclosed in British Patent No. 490,384 dated February 15, 1937; nitrilotriacetic acid and related compounds as disclosed in U.S.

Patent No. 3,678,154 issued to Widder & Briner on July 18, 1972; polyphosphonates as disclosed in U.S. Patent No. 3,737,533 issued to Francis on June 5, 1973, U.S.

Patent No. 3,988,443 issued to Ploger, Schmidt, Dunker & Gloxhuber on October 26, 1976 and U.S. Patent No. 4,877,603 issued to Degenhardt & Kozikowski on October 31, 1989; all of these patents are incorporated herein by reference. Mixtures of the above-identified anticalculus agents may also be useful. If present, the anticalculus agents generally comprise from about 0.2% to about 13%, preferably from about 0.4% to about 6% of the compositions of the present invention.

The soluble alkali metal pyrophosphate ion source used in the present compositions can be any of the alkali metal pyrophosphate salts. Specific salts include tetra alkali metal pyrophosphate, dialkali metal diacid pyrophosphate, trialkali metal monoacid pyrophosphate and mixtures thereof, wherein the alkali metals are sodium or potassium. The salts are useful in both their hydrated and unhydrated forms. [Pyrophosphate salts are described in more detail in Kirk & Othmer, Encyclopedia of Chemical Technologv, Second Edition, Volume 15, Interscience Publishers (1968), incorporated herein by reference in its entirety The amount of tetrasodium pyrophosphate salt useful in these compositions is any amount effective for tartar control and is generally enough to provide at least about 1.0% P207-4, preferably from about 1.5% to about 10%, more preferably from about 3.0% to about 6%, by weight of the compositions. It is to be appreciated that the level of P2074 is that amount capable of being provided to the composition (i.e., the theoretical amount at an appropriate pH) and that other pyrophosphate forms (e.g., HP207-3) may be present when a final product pH is established. As is well recognized in the art, P2074 means ions in solution and such ions have different degrees of protonation depending on the pH of the composition as indicated.

Optional tartar control agents include such known materials as synthetic anionic polymers [including polyacrylates and copolymers of maleic anhydride or acid and methyl vinyl ether (e.g., Gantrez), as described for example in U.S. Patent 4,627,977 to Gaffar et al., the disclosures of which are incorporated herein by reference in their entirety; as well as, e.g., polyamino propane sulfonic acid (AMPS)], zinc citrate trihydrate, polyphosphates (e.g., tripolyphosphate; hexametaphosphate), diphosphonates (e.g., EHDP; AHP), polypeptides (such as polyaspartic and polyglutamic acids), and mixtures thereof.

Antimicrobial/Antiplaque Agents The compositions of the present invention may comprise one or more antimicrobial/antiplaque agents, on the condition that they are compatible with the other components of the compositions. Typical examples of such antimicrobiaVantiplaque agents include, but are not limited to, Triclosan, 5-chloro-2 (2,4-dichlorophenoxy)-phenol, as described in The Merck Index, 10th ed. (1976), p.

1381; U.S. 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.

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. 8299); domiphen bromide (Merck Index, No.

3411); cetylpyridinium chloride, (CPC) (Merck Index, No. 2024); tetradecylpyridinium chloride, (TPC); N-tetra-decyl-4-ethylpyridinium chloride (TDEPC); octenidine; delmopinol, octapinol, and other piperidino derivatives; nicin preparations; zinc/stannous ion agents; antibiotics such as augmentin, amoxicillin, tetracycline, doxycycline, minocycline, and metronidazole; and peroxides, such as cylium peroxide, hydrogen peroxide, and magnesium monoperthalate and its analogs as described in U.S. Patent No. 4,670,252; and analogs, salts of the above antimicrobial antiplaque agents, and mixtures thereof. If present, the antimicrobial antiplaque agents generally comprise from about 0.1% to about 5% by weight of the compositions of the present invention.

Other antimicrobial/antiplaque agents comprise copper bis-glycinate, stannous salts, and/or mixtures thereof.

Copper bis-glycinate can be purchased as the salt or formed in-situ by using appropriate salts of copper and glycine. Suitable copper compounds which supply copper ions are, in principle, all copper compounds being toxicologically harmless, compatible with mucous membranes and, to some extent, water-soluble.

The inorganic copper salts which may be used include, but not limited to, copper chloride and the dihydrate thereof copper fluoride and the dihydrate thereof; copper fluorosilicate and the hexahydrate thereof copper sulphate and the pentahydrate thereof; copper nitrate and the tri- and hexa-hydrates thereof and the less popular copper salts, such as copper bromide; copper metaborate; copper bromate; copper chlorate; copper iodate; and copper fluorophosphate. Suitable sources of glycine include, but are not limited to, glycine; sodium glycinate; potassium glycinate; and glycine hydrochloride. "Copper bis-glycinate" as the term is used herein includes ratios of copper and glycine differing somewhat from one part copper to two parts glycine. The ratios of copper to glycine which are most useful herein are as follows: preferred from about 1:1.5 to about 1:3.5; more preferred from about 1:1.8 to about 1:3.0; most preferred from about 1:1.8 to about 1:2.4.

Copper bis-glycinate is typically used in an amount sufficient to provide from about 1 to about 8000, preferably from about 25 to about 6000, most preferably from about 50 to about 4000 ppm copper ions. For dentifrices the preferred levels are from about 400 to about 6000 ppm, and most preferably from about 800 to about 4000 ppm. For rinses the preferred levels are from about 25 to about 1000 ppm, and more preferably from about 100 to about 500 ppm. For chewing gums the levels may be as low as about 1 ppm copper. Typical dentifrice compositions comprising copper bisglycinate are disclosed in U.S. Patent No. 5,389,360, issued February 14, 1995, to Mobley, et al., which is incorporated herein by reference in its entirety.

Stannous fluoride is a staple item of commerce and can be purchased as the salt or formed in-situ by using appropriate salts of stannous and fluoride. Suitable salts include, but are not limited to, stannous chloride and sodium fluoride. Stannous fluoride is typical used at levels of from about 0.05% to about 1.1%, preferably from about 0.4% to about 0.95% of the compositions of the present invention.

Stannous gluconate is a known stannous chelate and may be provided to the present composition as a chelate or as separate soluble stannous and gluconate salts and the chelate formed in-situ such as with stannous fluoride. Such salts include stannous chloride and sodium gluconate. Stannous gluconate is typically present in the present compositions at a level of from about 0.1% to about 11%, preferably from about 2% to about 4% of the compositions of the present invention Typical dentifrice compositions comprising stannous salts are disclosed in U.S. Patent No. 5,338,537, issued August 8. 1994, to White, et al., which is incorporated herein by reference in its entirety.

Antibacterial Agents The compositions of the present invention may comprise one or more antibacterial agents, on the condition that they are compatible with the other components of the compositions. Typical examples of such antibacterial agents include, but are not limited to, noricationic and substantially water insoluble antibacterial agents. An antibacterial agent which is substantially water insoluble as described herein means that its solubility is less than about 1% by weight in water at 250C and may be even less than about 0.1%. If an ionizable group is present, solubility is determined at a pH at which ionization does not occur.

Typical examples of noncationic water insoluble antimicrobial agents useful in the present dental compositions include halogenated diphenyl ethers (excluding 2',4,4'-trichloro-2-hydroxy-diphenyl ether), phenolic compounds including phenol and its homologs, mono and poly-alkyl and aromatic halophenols, resorcinol and its derivatives, bisphenolic compounds and halogenated salicylanilides, benzoic esters, and halogenated carbanilides. Antibacterial agents can be present in an effective antiplaque amount, typically about 0.01% to about 5% by weight of the compositions.

Anti-Inflammatorv Agents: The compositions of the present invention may comprise one or more additional anti-inflammatory agents, on the condition that they are compatible with the other components of the compositions. Typical examples of such antiinflammatory agents include, but are not limited to, aspirin, acetaminophen, ibuprofen, naproxen, indomethacin, piroxicam, meclofenamate sodium, tenidap, tebufelone, benoxaprofen, flurbiprofen, ketoprofen, ketorolac, etodolac, fenoprofen, fenbufen, indoprofen, pirprofen, carprofen, oxaprozin, pranoprofen, miroprofen, tioxaprofen, suprofen, alminoprofen, tiaprofen, their pharmaceutically-acceptable salts, and mixtures thereof. The typical concentrations of anti-inflammatory agents in the dental compositions of the present invention are from about 0.004% to about 20%, preferably from about 0.02% to about 4%, more preferably from about 0.04% to about 2%, and most preferably from about 0.2% to about 0.8% of the compositions of the present invention.

Orally-Acceptable Carrier Materials: In preparing the present dental compositions, it is desirable to add one or more carrier materials to the compositions. Such materials are well known in the art and are readily chosen by one skilled in the art based on the physical and aesthetic properties desired for the composition being prepared. Carrier materials typically comprise from about 79% to about 98%, preferably from about 89% to about 98%, by weight of the compositions.

The compositions of the present invention, such as toothpastes, typically contain some thickening material and/or binders to provide a desirable consistency.

Preferred thickening agents are carboxyvinyl polymers (such as polyacrylic acids cross-linked with polyallyl sucrose or polyallyl pentaerythritol), carrageenan, hydroxyethyl cellulose and water soluble salts of cellulose ethers such as sodium carboxymethyl cellulose, sodium carboxymethyl hydroxyethyl cellulose, and mixtures thereof. Natural gums such as gum karaya, xanthan gum, gum arabic, and gum tragacanth can also be used. Colloidal magnesium aluminum silicate or finely divided silica can be used as part of the thickening agent to further improve texture.

Thickening materials and/or binders can be used in an amount from about 0.1% to about 5% by weight of the total composition.

It is also desirable to include some humectant material in the compositions of the present invention to keep the composition from hardening upon exposure to air and give mouthwash and toothpaste compositions a moist feel to the mouth. Certain humectants can also impart a desirable sweetness or flavor to the compositions.

Suitable humectants include polyethylene glycol, sorbitol, glycerin, xylitol, other edible polyhydric alcohols, and mixtures thereof, at a level of from about 0% to about 70%, preferably from about 2% to about 55%, by weight of the compositions herein.

Titanium dioxide may also be added to the present compositions. Titanium dioxide is a white powder which adds pigment to the compositions. Titanium dioxide generally comprise from about 0.25% to about 1% by weight of the compositions.

Water may also be present in the compositions of the present invention.

Water employed in the preparation of commercially suitable oral compositions should preferably be deionized and free of organic impurities. Water generally comprises from about 2% to about 99%, preferably from about 20% to about 95%, by weight of the dental compositions herein. When in the form of toothpastes, the compositions preferably are from about 2% to about 45%, more preferably from about 30% to about 40%, water, while mouthwashes are preferably from about 45% to about 95%, more preferably from about 75% to about 90%, water. These amounts of water include the free water which is added plus that which is introduced with other materials such as with sorbitol.

The pH of the present compositions is preferably adjusted through the use of buffering agents. Buffering agents, as used herein, refer to agents that can be used to adjust the pH of the compositions to a range of about pH 7 to about pH 9. These agents include mono and trisodium phosphate, sodium hydroxide, sodium carbonate, tris(hydroxymethyl)aminomethane, tetra and disodium pyrophosphate and tetrapotassium pyrophosphate. Citric acid and sodium citrate are preferred at a level of from about 0.5% to about 10% by weight ofthe present compositions.

An abrasive polishing material may also be included in the toothpaste compositions. The abrasive polishing material contemplated for use in the compositions of the present invention can be any material which does not excessively abrade dentin. These include, for example, silicas including gels and precipitates, calcium carbonate, dicalcium orthophosphate dihydrate, calcium pyrophosphate, tricalcium phosphate, calcium polymetaphosphate, insoluble sodium polymetaphosphate, hydrated alumina, and resinous abrasive materials such as particulate condensation products of urea and formaldehyde, and others such as disclosed by Cooley et al. in U.S. Patent 3,070,510, December 25, 1962, incorporated herein by reference. Mixtures of abrasives may also be used.

Silica dental abrasives of various types are preferred because of their unique benefits of exceptional dental cleaning and polishing performance without unduly abrading tooth enamel or dentin. The silica abrasive polishing materials useful herein, as well as other abrasives, generally have an average particle size ranging between about 0.1 and 30 microns, preferably 5 and 15 microns. The silica abrasive can be precipitated silica or silica gels such as the silica xerogels described in Pader et al., U.S. Patent 3,538,230, issued March 2, 1970 and DiGiulio, U.S. Patent 3,862,307, June 21, 1975, both incorporated herein by reference. Preferred are the silica xerogels marketed under the tradename "Syloid" by W. R. Grace & Company, Davison Chemical Division. 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. Patent 4,340,583, July 29, 1982, incorporated herein by reference. The abrasive in the toothpaste compositions described herein is preferably present at a level of from about 6% to 70% by weight of the compositions.

Sodium bicarbonate can also be added to the present compositions. Sodium bicarbonate, also known as baking soda, is a household product with a variety of uses including use in dentifrices and mouthrinses. It is a white powder that is soluble in water and unless stabilized, tends to release carbon dioxide in an aqueous system.

The present compositions can contain from about 1% to about 50%, sodium bicarbonate by weight of the composition.

The present compositions can also contain solubilizing agents. Suitable solubilizing agents are used to solubilize the anticalculus agents, antidental caries agents, antimicrobial/antiplaque agents, antibacterial agents, anti-inflammatory agents, and do not adversely affect the activity of the anti calculus agents, antidental caries agents, antimicrobiaVantiplaque agents, antibacterial agents, anti-inflammatory agents used in the compositions. Solubilizing agents useful in the present compositions include propylene glycol, dipropylene glycol, methyl cellosolve, ethyl cellosolve, olive oil, castor oil, amyl acetate, ethyl acetate, glyceryl tristearate and benzyl benzoate. Preferred is propylene glycol. Solubilizing agents are typically used at a level of from about 0.05% to about 10% by weight of the compositions.

Flavoring agents can also be added to the present compositions. Examples of flavoring agents useful in the present invention include oil of peppermint, oil of sassafras, clove bud oil, peppermint, menthol, anethole, thymol, methyl salicylate, eucalyptol, cassia, 1-menthyl acetate, sage, eugenol, parsley oil, oxanone, oil of wintergreen, alpha-irisone, oil of spearmint, marjoram, lemon, orange, propenyl guaethol, cinnamon, and mixtures thereof. Flavoring agents are generally used in toothpastes at levels of from about 0.001% to about 5% by weight of the composition.

Sweetening agents can be added to the present compositions. These include aspartame, acesulfame, sodium saccharin, dextrose, sucrose, lactose, maltose, xylitol, levulose, sodium cyclamate and mixtures thereof. Various coloring agents may also be incorporated in the present dental compositions. Sweetening agents and coloring agents are generally used in toothpastes at levels of from about 0.005% to about 5% by weight of the composition.

A preferred nonessential component of the compositions of the present invention is a cooling agent or a combination of cooling agents. Suitable cooling agents are those described in U.S. Patent 4,136,163, January 23, 1979, to Watson et al., U.S. Patents~4,032,661 and 4,230,688, June 28, 1977 and October 28, 1980, respectively, to Rowsell et al. and U.S. Patent 5,266,592, November 30, 1993 to Grub et al., all of which are herein incorporated by reference. Particularly preferred cooling agents include N-ethyl-p-menthane-3-carboxamide taught by the above incorporated U.S. Patent 4,136,163 and N,2,3-trimethyl-2-isopropylbutanamide which is taught by the above incorporated U.S. Patent 4,230,688. Another particularly preferred cooling agent is 3-1 -menthoxypropane 1,2-diol. This material is described in detail in U.S. Patent 4,459,425, July 10, 1984 to Amano et al. and incorporated herein by reference.

The compositions of the present invention may also comprise one or more surfactants. Suitable surfactants are those which are reasonably stable and preferably form suds through the pH range of the compositions. Surfactants useful as sudsing agents may be soaps, and anionic, nonionic, cationic, zwitterionic and amphoteric organic synthetic detergents, and compatible mixtures thereof. Surfactants of these types are described more fully in U.S. Patent No. 3,959,458 issued to Agricola, Briner, Granger & Widder on May 25, 1976, incorporated herein by reference. Such surfactants are generally present in the compositions of the present invention at a level of from about 0% to about 10%, preferably from about 0.2% to about 5%.

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.

The compositions of the present invention may comprise one or more nutrients, on the condition that they are compatible with the other components of the compositions. Typical examples of such nutrients include, but are not limited to, folate, retinoids (Vitamin A), Vitamin C, Vitamin E and zinc. If present, the nutrients generally comprise from about 0.001% to about 10% by weight of the compositions of the present invention.

The present compositions can be in the form of a mouth rinse or liquid dentifrice where conventional mouth rinse components comprise the carrier materials of the present invention. Mouth rinses and liquid dentifrices generally comprise from about 20:1 to about 2:1 of a water ethyl alcohol or alcohol free solution, and preferably other ingredients such as flavors, sweeteners, humectants, and surfactants such as those mentioned above. The humectants, such as glycerin and sorbitol give a moist feel to the mouth. Generally on a weight basis, the mouth rinses and liquid dentifrices of the present invention comprise from about 0% to about 60% ethyl alcohol, from about 0% to about 20% humectant, from about 0% to about 2% surfactant, from about 0% to about 0.5% sweetening agent, from about 0% to about 0.3% flavoring agent and the balance water. Other optional components described herein for use in toothpaste products are also useful in the mouth rinse and liquid dentifrice compositions.

Method of Treatment The present invention also relates to a method for preventing and treating periodontal diseases such as gingivitis and periodontitis, and other diseases of the oral cavity in a human or lower animal in need of such treatment. Said method comprises administering to a human or lower animal in need of such treatment the compositions of the present invention.

Examples The following examples further describe and demonstrate embodiments within the scope of the present invention. These examples are given solely for the purpose of illustration and are not to be construed as a limitation of the present invention as many variations thereof are possible without departing from the spirit and scope.

Examples 1-4 Given below are four dentifrice Examples representative of the present invention.

Weight % Component Ex. 1 Ex. 2 Ex. 3 Ex. 4 Sorbitol (70% Solution) 61.827 51.827 31.763 47.891 Glycerin -- 10.000 10.000 10.198 Glycine 0.218 0.262 -- - Curcumin 0.5 0.5 1.0 0.1 Copper (II) Sulfate-5H2O 0.360 0.360 -- - Sodium Fluoride 0.243 0.243 -- - Sodium Alkyl Sulfate (28% Solution) -- 4.000 4.000 4.000 Sodium Lauroyl Sarcosinate (28% Solution) 4.000 Stannous Fluoride -- -- 0.454 0.454 Sodium Gluconate -- -- 8.328 0.632 Stannous Chloride -- -- 1.5 Stannous Pyrophosphate -- -- -- 1.040 AHP -- -- 1.5 - Sodium Hydroxide -- -- 0.75 0.200 Hydroxy Ethyl Cellulose -- -- 0.75 - Magnesium Alumina Silicate -- -- -- 0.408 Saccharin 0.130 0.130 0.455 0.200 Titanium Dioxide 0.525 0.525 1.0 0.525 FD & C Blue 0.050 0.050 -- 0.051 Silica 20.000 20.000 20.000 20.000 Carboxy Methyl Cellulose 0.750 -- -- 1.050 Xanthan Gum -- 0.475 0.5 - Carbopol 956* -- 0.300 -- - Flavor 0.900 0.900 1.0 0.851 Water Q.S. Q.S. Q.S. Q.S.

*Carboxyvinyl polymer offered by B. F. Goodrich Company.

Examole S The following is a toothpowder representative of the present invention.

Component WeiNt Curcumin 0.500 Stannous Fluoride 0.454 Stannous Chloride Dihydrate 1.500 Sodium Gluconate 2..082 Silica 73.264 Sodium Sulfate 20.000 Sodium Lauryl Sulfate 1.000 Flavor 1.000 Sodium Saccharin 0.200 Examok 6-7 The following are topical toothgels representative of the present invention.

Weight % Component Ex.6 Ex.7 Curcumin 0.500 0.500 Stannous Fluoride 0.454 0.454 Stannous Chloride Dihydrate 1.141 2.200 Sodium Gluconate 1.750 2 500 Glycerin 92.855 50.000 Sorbitol (70% Solution) -- 42.146 Sodium Carboxymethyl Cellulose 0.600 - Hydroxyethyl Cellulose -- 0.500 Flavor 1.000 1.000 Sodium Saccharin 0.200 0.200 Sodium Alkyl Sulfate (27.9%) 2.000 1.000 Elamnies S11 Given below are four mouthrinse Examples representative of the present invention.

Weight % Component Ex. 8 Ex 9 Ex. 10 Ex. 11 Curcumin 0.100 0.100 0.100 0.100 Stannous Fluoride 0.100 0.100 0.100 0.100 Stannous Chloride Dihydrate -- 0.550 0.550 - Copper (11) Sulfate-5H2O 0.100 -- -- 0.100 Ethanol 16.250 10.000 15.000 - Na Gluconate -- 0.690 -- - Dibasic Na Phosphate Heptahydrate -- -- 0.480 - Monobasic Na Phosphate Monohydrate -- -- 1.820 Sorbitol (70%) -- 10.000 - Sorbitan Diisostearate -- 0.200 -- - Na Hydroxide -- 0.020 -- - Polysorbate 80* 0.120 -- 0.330 0.100 Polyethylene Glycol -- -- -- 0.300 Propylene Glycol -- -- -- 10.000 Glycerin 10.000 -- 12.000 12.000 Glycine 0.060 -- -- - Saccharin 0.060 0.050 0.080 0.060 Sodium Benzoate -- -- -- 0.420 Benzoic Acid -- 0.050 -- 0.075 Color Solution -- 0.020 -- 0.020 Flavor 0.150 0.150 0.150 0.100 Water Q.S. Q.S. Q.S. Q.S.

*Polyoxyethylene (20) sorbitan monooleate.

What is claimed is:

Claims (4)

1. An oral composition comprising: a.) from about 0.001% to about 10% of a curcuminoid; b.) from about 0.005% to about 0.35% of fluoride ion from a fluoride ion source; c.) a safe and effective amount of at least one oral active selected from the group consisting of anticalculus agents, antimicrobial agents, antiplaque agents, antibacterial agents, and mixtures thereof d.) from about 79% to about 98% of one or more carrier materials.

2. An oral composition according to Claim 1 wherein said curcuminoid is selected from the group consisting of curcumin, curcumin derivatives, curcumin analogues, preparations of the plant Curcuma longa or other curcumin-containing plants, and mixtures thereof.

3. An oral composition according to Claim 2 wherein said anticalculus agent is selected from the group consisting of pyrophosphates, polyphosphates, polyphosphonates, polyacrylates and other polycarboxylates, polyepoxysuccinates, ethylenediaminetetraacetic acid, nitrilotriacetic acid and related compounds, their pharmaceutically-acceptable salts, and mixtures thereof; antimicrobial agent is selected from the group consisting of Triclosan, 5-chloro-2 (2,4-dichlorophenoxy)-phenol, chlorhexidine, alexidine, hexetidine, sanguinarine, benzalkonium chloride, salicylanilide, domiphen bromide, cetylpyridinium chloride, tetradecylpyridinium chloride, N-tetra-decyl-4-ethylpyridinium chloride, octenidine, delmopinol, octapinol, and other piperidino derivatives, nicin preparations, zinc/copper/stannous ion agents, their pharmaceutically-acceptable salts, and mixtures thereof, antibacterial agent is selected from the group consisting of halogenated diphenyl ethers, phenolic compounds, mono- and poly alkyl and aromatic halophenols, resorcinol and its derivatives, bisphenolic compounds and halogenated salicylanilides, benzoic esters, halogenated carbanilides, their pharmaceutically-acceptable salts, and mixtures thereof.

4. An oral composition according to Claim 2 further comprising an additional anti inflammatory agent selected from the group consisting of aspirin, acetaminophen, ibuprofen, naproxen, indomethacin, piroxicam, meclofenamate sodium, tenidap, tebufelone, benoxaprofen, flurbiprofen, ketoprofen, ketorolac, etodolac, fenoprofen, fenbufen, indoprofen, pirprofen, carprofen, oxaprozin, pranoprofen, miroprofen, tioxaprofen, suprofen, alminoprofen, tiaprofen, their pharmaceutically-acceptable salts, and mixtures thereof.

An oral composition according to Claim 1 wherein said fluoride ion source is selected from the group consisting of sodium fluoride, potassium fluoride, indium fluoride, sodium monofluorophosphate, and mixtures thereof.

An oral composition according to Claim 5 wherein said fluoride ion source is sodium fluoride.

An oral composition according to Claim 1 wherein said oral composition is selected from the group consisting of a toothpaste, tooth gel, toothpowder, mouthwash, mouthspray, prophylaxis paste, dental treatment solution, and mixtures thereof.

An oral composition according to- Claim 7 wherein said oral composition is selected from the group consisting of a toothpaste, tooth gel, toothpowder, and mixtures thereof.

An oral composition according to Claim 8 wherein said oral composition is a toothpaste.

A method for preventing and treating gingivitis, periodontitis, and other diseases of the oral cavity comprising the topical application to the oral cavity of a human or lower animal in need of such treatment of a safe and effective amount of a composition according to Claim 1.

A method for preventing and treating gingivitis, periodontitis, and other diseases of the oral cavity comprising the topical application to the oral cavity of a human or lower animal in need of such treatment of a safe and effective amount of a composition according to Claim 4.