PL202563B1 - Improved low−cost dentifrice composition - Google Patents

Abstract

An improved low-cost dentifrice composition comprises from about 6 % to about 70 % of an abrasive polishing material, from about 0.5 % to about 4.5 % of a thickener, from about 0.5 % to about 45 % of a hexahydric humectant, from about 0.05 % to about 2.5 % of an anti-cavity agent, and at least about 30 % of water. The composition comprises less than about 10 % dihydric and trihydric alcohols, and has a viscosity of from about 8 to about 100 BKU.

Description

Description of the invention

The present invention relates to a dentifrice composition. Good oral hygiene may be partially achieved by cleaning the teeth with an oral composition such as a dentifrice composition. The effect of dentifrice compositions in improving oral health is widely recognized as important, in particular by reducing the extent of tooth cavities and the deposition of plaque and tartar. These conditions are the result of plaque bacteria and can lead to diseases such as periodontitis and gingivitis. These conditions are currently the leading cause of adult loss of dentition. In addition, other oral diseases such as staining of the tooth enamel and bad odor (bad breath) can be reduced by brushing your teeth regularly with a dentifrice composition.

While many dentifrice compositions have been described, and many types of dentifrice and other oral care compositions are commercially available, there is still interest and a need for improved oral health promoting products. In addition, presently known dentifrice compositions may require expensive ingredients or an expensive manufacturing process. For these reasons, such compositions may be too expensive for certain areas or for certain consumer groups. Accordingly, it is desirable to improve the cost-effectiveness of such products without compromising their effectiveness, so that they can become increasingly accessible to consumers of different income levels and locations.

Previous economic dentifrice compositions typically contain an abrasive, a humectant, an aqueous solvent, at least 15% di- and trihydric alcohols, and a small amount of water. Dentifrice compositions containing the above ingredients are disclosed in US 5,320,830, EP 0331415, US 4,421,527 and US 5,089,255. However, such dentifrice compositions typically do not contain anti-caries agents because they are expensive. Accordingly, such cheap dentifrice compositions may not provide an adequate level of protection against caries. Moreover, they typically contain a lot of di- and trihydric alcohols, since it is commercially essential that the dentifrice composition has acceptable physical properties such as form and rheology. Consumers will typically require an acceptable dentifrice composition, e.g., lump-free, squeezable and relatively non-sticky.

Accordingly, there is a need for a tooth cleaning composition that provides satisfactory oral health benefits in a cost effective manner.

The present invention relates to a dentifrice composition comprising an abrasive polishing material, a thickening agent, a humectant, an anti-cavity agent, and water, characterized in that it comprises

A. 6% to 70% silica based abrasive polishing material;

B. from 0.5% to 4.5% of a thickening agent selected from the group consisting of carboxymethyl cellulose, carbomer, xanthan gum, and mixtures thereof;

C. from 0.5% to 45% of a humectant selected from the group consisting of sorbitol, xylitol, glucose, and mixtures thereof;

D. 0.05% to 2.5% of an anti-cavity agent selected from sodium fluoride; and

E. at least 30% water, the composition being free of di- and trihydric alcohols, and the composition having a viscosity of 0.8 to 10 Pa · s.

The composition according to the invention preferably contains 0.1% to 1% sodium fluoride, preferably at least 40% water, preferably 5% to 30% humectant.

The viscosity of the composition is preferably 1.5 to 8 Pa · s, more preferably the viscosity of the composition is 1.5 to 5 Pa /

The composition of the invention further comprises an excipient selected from the group consisting of a source of peroxide, a source of alkali metal bicarbonate, an anti-calculus agent, a surfactant, titanium dioxide, an antioxidant, a coloring agent, a perfume, a sweetener, a herbal agent, an antimicrobial agent and their mixtures.

It has now been found that the present invention can provide an effective, stable, less irritating composition that is both easy to manufacture and economical. Moreover, such an improved dentifrice composition provides oral health and / or a reduction in tooth loss that is comparable to, or better than, current dentifrice compositions. In addition, the flavor release, rheology, and / or form of an improved dentifrice composition may be comparable to, or better than, current dentifrice compositions.

All percentages, ratios and proportions in this application are based on the weight of the final dentifrice composition, unless otherwise specified. All temperatures are in degrees Celsius (° C) unless otherwise specified.

In the present application, alkyl means a hydrocarbon moiety which is straight or branched, saturated or unsaturated. Unless otherwise specified, alkyl moieties are preferably saturated or unsaturated with double bonds, preferably with one or two double bonds. The term alkyl includes the alkyl portion of acyl groups. In the present application, an effective amount means an amount of a compound or composition sufficient to significantly produce a beneficial effect, preferably a beneficial oral health effect, but an amount low enough to avoid serious side effects, i.e. to provide a reasonable benefit-risk ratio within the limits of in-depth sludge of a skilled specialist.

As used herein, a dentifrice composition means a composition whose physical form is a paste or gel composition, unless otherwise specified. The dentifrice composition may be in any desired aesthetic form, such as deep stripes, surface stripes, multi-layer forms, with a gel surrounding the paste, or any combination thereof. Alternatively, the dentifrice composition can be a two-phase system with two or more dentifrice compositions contained within a physically separate dispenser compartment and dispensed side by side.

In the present application, dihydric alcohol is a molecule that has two hydroxyl groups, and contains common humectants such as polyethylene glycol, propylene glycol, etc. In this application, trihydric alcohol is a molecule that has three hydroxyl groups, and it contains typical humectants such as glycerin. Dihydric alcohols and trihydric alcohols are collectively referred to in this application as dihydric and trihydric alcohols.

As used herein, dispenser means any pump, tube, or container suitable for dispensing a dentifrice composition.

As used herein, substantially free means that no such compound is intentionally added as an ingredient to a dentifrice composition. However, this term does not exclude the possibility that a small amount of such a compound may be present as an impurity, or in an amount that does not significantly affect the overall characteristics, cost, and / or durability of the dentifrice composition.

All ingredients such as active ingredients and other ingredients useful in this application can be classified or described according to their beneficial cosmetic and / or therapeutic effects or their postulated mode of action. However, it should be understood that the active ingredients and other ingredients useful in this application may, in some event, provide more than one cosmetic and / or therapeutic benefit or act through more than one mode of action. Thus, the classifications in this application are made for convenience and are not intended to limit the ingredient to the particular application or uses stated.

The abrasive polishing material useful in this application may be selected from any material that does not excessively rub the dentin. The abrasive / polishing material preferably has a calcium content of less than about 23%. Typical abrasive polishes include silicas including gels and deposits; aluminum oxides; phosphates including orthophosphates, polymetaphosphates, and pyrophosphates; and mixtures thereof. Particular preferred examples of the abrasive polishing material useful in this application include silicas (further described below), dicalcium orthophosphate dihydrate, calcium pyrophosphate, tricalcium phosphate, calcium polymetaphosphate, insoluble sodium polymetaphosphate, hydrated alumina, calcium beta-pyrophosphate, calcium carbonate resins, such as particulate urea formaldehyde condensation products, dicalcium phosphate, alumina trihydrate, insoluble sodium metaphosphate, and others, such as those disclosed by Cooley, et al. in US Patent 3,070,510, issued December 25, 1962. Mixtures may also be used. abrasives. While calcium carbonate may be used in this application, it is not preferred as it may be incompatible with the tooth defect agent as described below; thus, in a preferred embodiment, the dentifrice composition is substantially free of calcium carbonate.

PL 202 563 B1

Silica tooth brushing abrasives of various types are also highly advantageous due to their exceptional tooth cleaning benefits and polishing performance without excessively abrading tooth enamel or dentin. The silica abrasive polishes in this application, as well as other abrasive polishes, generally have an average particle size ranging between about 0.1 to about 30 microns, preferably from about 5 to about 15 microns, and exhibit good fluoride compatibility (i.e. to provide soluble fluoride ions). The abrasive polishing material can be precipitated silica or silica gels, such as the silica xerogels described in Pader, et al., US Patent 3,538,230, issued March 2, 1970, and DiGiulio, US Patent 3,862,307, issued January 21, 1975. Xerose is preferred. silica gels sold under the trade name Syloid by WR Grace & Company, Davison Chemical Division. Also preferred are precipitated silica type materials such as those sold by JM Huber Corporation under the trade name Zeodent, particularly silica designated Zeodent 119. The types of silica abrasive tooth brushing polishing materials useful in the dentifrice compositions of the present invention are described in more detail in: Wason, U.S. Patent 4,340,583, issued Jul. 29, 1982. The dentifrice composition includes abrasive polishing material in an amount of from about 6% to about 70%, preferably from about 10% to about 50%, and more preferably from about 15% to about 30%. % by weight of the dentifrice composition.

The thickening agent useful in this application acts as a binder to provide the desired consistency. Thickening agents useful in the present dentifrice composition may be selected from the group consisting of inorganic, gel-forming, thickening agent, cellulose-based thickening agent, natural plant gum thickening agent, bacterial-derived gum thickening agent, synthetic organic polymer of natural origin, mixed thickener and mixtures thereof. Preferred inorganic gel-forming thickening agents include precipitated silica, airgel silica, pyrogenic silica, colloidal magnesium aluminum silicate, and mixtures thereof. Preferred modified cellulose based thickeners include carboxymethyl cellulose, hydroxyethyl cellulose, hydroxymethyl carboxyethyl cellulose, hydroxypropyl cellulose, hydroxymethyl carboxypropyl cellulose, methyl cellulose, ethyl cellulose and mixtures thereof. Such thickeners are available from, e.g., Aqualon Co., Hopewell, VA, USA; Jiangmen Fenghua Fine Chemical Industry Co., Ltd., Jiangmen City, China; and Zhangjiagang Xinguang Chemical Factory, Zhangjiagang City, China. Preferred natural plant gum thickeners include Irish moss (carrageenan), tragacanth, gum arabic, ghatti gum, senegalese gum, locust bean gum, sodium alginate and mixtures thereof. A preferred bacterial resin based thickening agent is xanthan gum. Preferred synthetic organic polymer based thickeners include polyacrylate, polyvinylpyrrolidone, and mixtures thereof, in particular a cross-linked acrylic acid homopolymer such as a carbomer. Particularly preferred carbomers include those derived from the Carbopol series, in particular Carbopol 956, available from BF Goodrich Co., Calvert City, Kentucky, USA. Preferred mixed natural thickeners include agar-agar, pectin, gelatin, and mixtures thereof. From the standpoint of operation, economy, safety and cost, a particularly preferred thickening agent is carboxymethyl cellulose, carbomer, and mixtures thereof.

The thickening agent is present in an amount from about 0.5% to about 4.5%, preferably from about 0.5% to about 2.0%, and more preferably from about 0.8% to about 1.5% by weight of the composition to brushing teeth.

The present dentifrice composition includes a humectant which serves to prevent the toothpaste composition from hardening in the air, and typically imparting the desired sweet taste to the dentifrice composition. The humectant useful in this application has six or fewer hydroxyl groups and is typically, though not necessarily, a sugar or sugar derivative. The humectant can have a linear, branched, or cyclic backbone; and preferably the humectant has a cyclic backbone of about 6 carbon atoms. The humectant may also have one or more additional functional groups such as carboxylic acid, amine, amide, ester groups, and mixtures thereof. It is particularly preferred that the humectant is selected from the group consisting of sorbitol, xylitol, and glucose, and a mixture thereof, particularly preferably sorbitol. Such sugars can further reduce the cost of the formulation by reducing or eliminating the need for additional sweetener. Without wishing to be bound by theory, it is believed that these humectants, especially sorbitol, xylitol, glucose, and mixtures thereof, interact with those described above.

They are thickeners and provide excellent water binding capacity due to the presence and alignment of multiple hydroxyl groups in the molecule. Moreover, it is believed that such advantages do not exist if e.g. the content of only the humectant is increased. This synergistic effect in turn can reduce the need for a more expensive thickener and di- and trihydric alcohols, and further reduce formulation costs while maintaining acceptable rheological properties and formulations for the dentifrice composition. Such humectants are typically readily available, cost effective, safe in almost all cases, and are surprisingly stable when included in the present dentifrice composition.

Furthermore, it is believed that the high hydrophilicity of such humectants directly improves fragrance retention and fragrance release from oil-based fragrance systems and allows the use of less fragrance. Since the fragrance systems typically require advanced distillation and are expensive mixtures, the present dentifrice composition has significantly reduced formulation costs. Because oil-based fragrance systems are relatively insoluble in such a hydrophilic compound, more fragrance is directly perceived by the user of the dentifrice composition. In contrast, oil-based fragrance systems may be partially or fully soluble in dihydric and / or trihydric alcohols such as glycerin and polyethylene glycol which are common in dentifrice compositions; this in turn lowers the user's perception of the dentifrice composition, and can increase the cost of formulating a recipe by increasing the required amount of the fragrance included in the composition.

Without wishing to be bound by theory, it is believed that the combination of a humectant and thickener described in this application synergistically works to provide acceptable rheological, aesthetic, durability, and equivalent or better performance without the need for traditionally large amounts (e.g., 15). % or greater) of dihydric and trihydric alcohols. As noted above, such dihydric and trihydric alcohols are typically expensive, and thus reducing or eliminating such compounds can significantly reduce the cost of formulating dentifrice compositions. Accordingly, the dentifrice composition of the present invention typically comprises less than about 10%, preferably between 0% and about 5%, of di- and trihydric alcohols. It is particularly preferred that the dentifrice composition of the present invention does not contain di- and trihydric alcohols.

The humectant is typically present in an amount from about 0.5% to about 45%, preferably from about 5% to about 40%, and more preferably from about 10% to about 35% by weight of the dentifrice composition.

The reduction in formulation costs resulting from lowering or eliminating di- and trihydric alcohols allows the formulator more freedom to add to the dentifrice composition and / or increase the anti-cavity agent content without increasing the selling price. In certain countries and areas, this can increase the availability of goods to a significant proportion of the general population and improve effective oral health. The anti-cavity agent typically comprises a fluoride ion, preferably water-soluble. Fluoride ion sources are well known in oral care applications as anti-caries agents. For these purposes, fluoride ions are included in many oral care compositions, particularly in dental cleaning compositions such as toothpastes. Patents disclosing such dentifrice compositions include US Patent 3,538,230, issued November 3, 1970 to Pader, et al; U.S. Patent 3,689,637, issued September 5, 1972 to Pader; U.S. Patent 3,711,604, issued January 16, 1973 to Colodney, et al; U.S. Patent 3,911,104, issued October 7, 1975, assigned to Harrison; U.S. Patent No. 3,935,306, issued January 27, 1976 to Roberts, et al; and U.S. Patent 4,040,858, issued August 9, 1977 to Wason.

The use of fluoride ions in tooth enamel protects the teeth against decay. A wide variety of fluoride ion-forming materials can be used as a source of soluble fluoride in formulations immediately prior to use. Examples of suitable fluoride ion forming materials can be found in the patents: Briner et al; U.S. Patent 3,535,421; published October 20, 1970 and Widder, et al; U.S. Patent 3,678,154; dated July 18, 1972. A preferred fluoride ion source for use in this application

These include sodium fluoride, potassium fluoride, ammonium fluoride, sodium monofluorophosphate, tin (I) fluoride, and mixtures thereof. Sodium Fluoride is especially preferred, and is available from, e.g., Jinan Chemical Subfactory, Jinan City, Shandong Province, China. Preferably, the dentifrice composition provides from about 50 ppm to 10,000 ppm, particularly preferably from about 100 to 3000 ppm, of fluoride ions in compositions which come into contact with dental surfaces when used with the dispensing system of the present invention. Such fluoride ion measurements are typically performed on a 3: 1 slurry of water and dentifrice composition. Generally, the anti-cavity anti-cavity agent, preferably the fluoride ion anti-cavity agent, is present in an amount from about 0.05% to about 2.5%, preferably from about 0.1% to about 1%, and especially from about 0.1% to about 0.5% by weight. composition.

However, when an anti-cavity agent containing fluoride ions is used, interaction with incompatible materials such as calcium carbonate, which may exist as an abrasive polishing material, should be reduced. Accordingly, when a fluoride ion, and in particular sodium fluoride, is present, it is highly preferred that the dentifrice composition is substantially free of calcium carbonate. While fluoride ion containing anti-cavity agents are preferred, non-fluoride anti-cavity agents known in the art, such as monosodium phosphate monohydrate, are also useful in this application, either alone or in combination with an anti-cavity agent. containing a fluoride ion.

The dentifrice composition further comprises at least 30% water by weight of the dentifrice composition. As reported and measured in this application, water includes water from solutions (i.e., humectant solution, sweetener solution, surfactant solution, etc.) but not bound water (i.e., hydrates in ambient temperature). Prior to addition to dentifrice compositions, the water useful in this application is typically purified or distilled to remove contaminants.

The dentifrice composition may further contain one or more additives known in the art, preferably an additive compound selected from the group consisting of a di- or trihydric humectant, buffering agent, peroxide source, alkali metal bicarbonate source, anti-calculus agent, surfactant, titanium oxide, antioxidant, colorant, fragrance, sweetener, herbal agent, antimicrobial agent, and mixtures thereof.

The present invention may include up to 10% of a di- or trihydric humectant such as are conventionally used in dentifrice compositions. However, in a preferred embodiment, the dentifrice composition contains from 0% to about 5% di- and trihydric alcohols. It is particularly preferred that the dentifrice composition of the present invention is substantially free of di- and trihydric alcohols. Suitable humectants for use in the present invention include glycerin, polyethylene glycol, propylene glycol, edible polyhydric alcohols and mixtures thereof, particularly glycerin, polyethylene glycol, and mixtures thereof.

Typically the present composition comprises a buffering agent. When the dentifrice composition is a two-phase system, the buffering agent is present in both dentifrice compositions. Buffering agents, as used herein, refer to agents that can be used to adjust the pH of the composition to about pH 4 to about pH 10, preferably about pH 4 to about 8, and more preferably from about pH 5.5 to about pH 10. about 8. These agents include alkali metal hydroxides, carbonates, sesquicarbonates, borates, silicates, phosphates, imidazoles, and mixtures thereof. Particular buffering agents include monosodium phosphate, trisodium phosphate, sodium hydroxide, potassium hydroxide, alkali metal carbonates, sodium carbonate, imidazole, pyrophosphate salts, citric acid, and sodium citrate. The buffering agents are used in an amount of from about 0.01% to about 30%, preferably from about 0.1% to about 10%, and more preferably from about 0.3% to about 7% by weight. of this composition. Preferred buffering agents are monosodium phosphate, trisodium phosphate, pyrophosphate salts, citric acid, sodium citrate, and mixtures thereof. It has been surprisingly found that the dentifrice composition of the present invention does not require as high a level of buffering salts as traditional dentifrice compositions. Without wishing to be bound by theory, it is believed that this may result in reduced irritation to the gums and mouth of the user.

Pyrophosphate salts can be used as buffering agents. The pyrophosphate salts useful in the present compositions include di-alkali metal pyrophosphate salts, tetra-alkali metal pyrophosphate, and mixtures thereof. Sodium acid pyrophosphate, disodium dihydrogen pyrophosphate (Na2H2P2O7), tetrasodium pyrophosphate (Na4P2O7), and tetrapotassium pyrophosphate (K4P2O7) in the non-hydrated state as well as in the form of hydrates are the preferred agents. In the compositions of the present invention, the pyrophosphate salt can be present in three ways: predominantly dissolved: predominantly undissolved, or a mixture of dissolved and undissolved pyrophosphate.

Compositions containing predominantly dissolved pyrophosphate are compositions in which at least one source of pyrophosphate ion is present. Free pyrophosphate ions can be present in various protonated states depending on the pH of the composition.

Compositions containing predominantly undissolved pyrophosphate are compositions containing no more than about 20% of the total amount of pyrophosphate salt dissolved in the composition, preferably less than about 10% of the total amount of pyrophosphate salt dissolved in the composition. The tetrasodium pyrophosphate and tetrapotassium pyrophosphate salts are the preferred pyrophosphate salts in these compositions, with the tetrasodium pyrophosphate salt being particularly preferred. The tetrasodium pyrophosphate can be in the form of the anhydrous salt or in the form of the decahydrate salt, or in some other solid-state stable form in dentifrice compositions. The salt is in the form of solid particles which may be crystalline and / or amorphous in nature, with preferably small particle sizes of the salt which are aesthetically acceptable and readily soluble during use. The useful amount of pyrophosphate salt in the preparation of these compositions corresponds to any tartar control effective amount. Some or all of the tetrasodium pyrophosphate may be undissolved in the article and present as tetrasodium pyrophosphate particles. Pyrophosphate ions may also exist in different protonated states (eg. HP2O7 ^-3) depending on the pH of the composition and if part of the tetrasodium pyrophosphate is dissolved.

The compositions may also contain a mixture of dissolved and undissolved pyrophosphate salts. Any of the pyrophosphate salts mentioned above can be used. Pyrophosphate salts are described in detail in Kirk & Othmer, Encyclopedia of Chemical Technology, Third Edition, Vol. 17, Wiley-Interscience Publishers (1982).

The present invention may contain a peroxide source for the whitening effect. The peroxide source is selected from the group consisting of hydrogen peroxide, calcium peroxide, urea peroxide, and mixtures thereof. The preferred source of peroxide is urea peroxide. The amounts given below refer to the amount of the peroxide feed, although the peroxide source may contain other ingredients in addition to the peroxide feed. The present composition may contain from about 0.01% to about 10%, preferably from about 0.1% to about 5%, more preferably from about 0.2% to about 3%, most preferably from about 0.3% to about 5%. 0.8% peroxide source based on the weight of the composition.

The present invention may also contain alkali metal bicarbonate salts. The alkali metal bicarbonate salts are water soluble and, unless stabilized, tend to release carbon dioxide in the aqueous system. Sodium bicarbonate, known as baking soda, is the preferred salt - alkali metal bicarbonate. The alkali metal bicarbonate salt can also act as a buffering agent. The present composition may contain from about 0.5% to about 50%, preferably from about 0.5% to about 30%, particularly preferably from about 2% to about 20%, most preferably from about 5% to about 18% salt. - alkali metal bicarbonate based on the weight of the oral composition.

Anti-tartar agents known for use in dental care products include phosphates. Phosphates include pyrophosphates, polyphosphates, polyphosphonates, and mixtures thereof. Pyrophosphates are best known for dental care applications. Pyrophosphate and polyphosphate ions are delivered to the teeth from polyphosphate pyrophosphate salts. Pyrophosphate salts useful in the present compositions include di-alkali metal pyrophosphate salts, tetra-alkali metal pyrophosphate salts, and mixtures thereof. Sodium acid pyrophosphate, di-sodium dihydrogen pyrophosphate (Na2H2P2O7), tetrasodium pyrophosphate (Na2H2P2O7), and tetrapotassium pyrophosphate (K4P2O7), in both unhydrated and hydrated forms are the preferred compounds. Either of the mentioned pyrophosphate salts can be used, however the tetrasodium pyrophosphate salt is preferred. For example, sodium polyphosphate and triethanolamine polyphosphates are preferred.

Pyrophosphate salts are described in more detail in Kirk & Othmer, Encyclopedia of Chemical Technology, 3rd Ed., Vol. 17, Wiley-Interscience Publishers (1982). Other anti-tartar agents include the pyrophosphates or polyphosphates disclosed in US Patent 4,590,066 (issued to Parran and Saqqab on May 20, 1986); polyacrylates and other polycarboxylates such

PL 202,563 B1 as disclosed in US Patent 3,429,963 (issued to Shedlovski February 25, 1969) and US Patent 4,304,766 (issued to Chang on December 8, 1981); and U.S. Patent 4,661,341 (issued to Benedict and Sunberg on April 28, 1987); polyepoxy succinates such as those disclosed in US Patent 4,846,650 (issued to Benedict, Bush, and Sunberg on Jul 11, 1989); ethylenediaminetetraacetic acid as disclosed in British Patent No. 490,384 dated February 15, 1937; nitrilotriacetic acid and related compounds as disclosed in US Patent 3,678,154 (issued to Widder and Briner on Jul 18, 1972); polyphosphonates as disclosed in US Patent 3,737,533 (issued to Francis June 5, 1973), US Patent 3,988,443 (issued to Ploger, Schmidt-Dunker, and Gloxhuber on October 26, 1976) and US Patent 4,877,603 (issued to Degenhardt and Kozikowski 31 October, 1989). Anti-tartar phosphates include potassium and sodium pyrophosphates; sodium tripolyphosphate; diphosphonates such as ethane-1-hydroxy-1,1-diphosphonate, 1-azacyclo-heptane-1,1-diphosphonate, and linear alkyl diphosphonates; linear carboxylic acids; and sodium zinc citrate.

Anti-tartar agents may be used in place of or in combination with pyrophosphate, which include known substances such as synthetic anionic polymers, including polyacrylates and copolymers of maleic anhydride or acid with methylvinyl ether (e.g., Gantrez), as described in US Patent 4,627,977. (patent granted to Gaffar et al.); such as and, for example, polyaminopropanesulfonic 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.

The present compositions may further contain a surfactant, commonly referred to as a saponification agent. Suitable surfactants should be foaming and stable over a wide pH range. The surfactant can be anionic, non-ionic, amphoteric, zwitterionic, cationic, or mixtures thereof. Anionic surfactants useful in the present invention include water-soluble salts of alkyl sulfates having 8 to 20 carbon atoms in the alkyl substituent (e.g., sodium alkyl sulfate) and water-soluble salts of sulfonated fatty acid monoglycerides with 8 to 20 carbon atoms. Sodium lauryl sulfate and sodium coconut monoglyceride sulfonates are examples of anionic surfactants of this type. Sodium lauryl sulfate is available, e.g., from Rhodia Specialty Chemical Wuxi Company, Wuxi City, Jiangsu Province, China. Other suitable anionic surfactants are sarcosinates such as sodium lauroyl sarcosinate, taurates, sodium lauryl sulfoacetate, sodium lauroyl isethionate, sodium laureth carboxylate, and sodium dodecylbenzenesulfonate. Mixtures of anionic surfactants can also be used. Many suitable anionic surfactants are disclosed in Agricola, et al., US Patent 3,959,458, issued May 25, 1976. Nonionic surfactants that may be used in the compositions of the present invention may be broadly defined as compounds obtained by condensation of alkylene oxide groups. (hydrophilic in nature) with an organic hydrophobic compound, which may be aliphatic or alkylaromatic. Examples of suitable nonionic surfactants include poloxamers (sold under the trade name Pluronic), polyoxyethylenes, polyoxyethylene sorbitan esters (sold under the trade name Tweens), fatty alcohol ethoxylates, poly (ethylene oxide) alkylphenol condensates, ethylene oxide condensates with an oxide reaction product propylene with ethylene diamine, ethylene oxide condensates with aliphatic alcohols, long chain tertiary amine oxides, long chain tertiary phosphine oxides, long chain dialkyl sulfoxides, and mixtures thereof. The amphoteric surfactants useful in the present invention can be broadly described as derivatives of aliphatic secondary and tertiary amines in which the amino substituent can be straight or branched chain and wherein one of the aliphatic substituents contains from about 8 to about 18 carbon atoms and one contains an anionic group. rendering water soluble, e.g., carboxylic, sulfonic, sulfate, phosphate or phosphonate. Other suitable amphoteric surfactants are betaines, especially cocamidopropyl betaine. Mixtures of amphoteric surfactants can also be used. Many of the suitable nonionic and amphoteric surfactants are disclosed by Gieske et al. In US Patent 4,051,234, issued September 27, 1977. The present composition typically comprises one or more

The number of surfactants, each in an amount from about 0.25% to about 12%, preferably from about 1% to about 10%, and more preferably from about 1% to about 8% by weight. composition.

Titanium dioxide may also be added to the dentifrice composition. Titanium dioxide is a white powder that gives the compositions an opaque appearance. Generally, titanium dioxide comprises from about 0.1% to about 5% by weight. composition.

In general, the antioxidant is believed to be useful in and may be added to the present composition. Antioxidants are described in texts such as Cadenas and Packer, The Handbook of Antioxidants. © 1996, Marcel Dekker, Inc. Antioxidants that may be included in the oral care composition include (but are not limited to): vitamin E, ascorbic acid (vitamin C), uric acid, carotenoids, vitamin A, flavonoids, herbal antioxidants, melatonin, aminoindoles, acids lipoids and mixtures thereof. Vitamins E and C are preferred in an amount of from about 0.01% to about 0.10%, and preferably from about 0.01% to about 0.05%.

In addition, one or more coloring agents may be added to the present composition. The coloring agent may be in the form of an aqueous solution, preferably a 1% coloring agent in an aqueous solution. The color solutions generally make up from about 0.01% to about 5% by weight. composition.

Fragrance systems can also be added to the compositions. Suitable fragrance ingredients include tea oil, wintergreen oil, peppermint oil, mint oil, clove oil, menthol, anethole, methyl salicylate, eucalyptol, cinnamon oil, 1-menthyl acetate, sage oil, eugenol, parsley oil, oxanone, alpha irizon, marjoram, lemon, orange, propenylguetole, cinnamon, vanillin, ethylvanillin, heliotropin, 4-cis-heptenal, diacetyl, methyl-para-t-butylphenyl acetate and mixtures thereof. Non-limiting examples of commercially available perfume systems are sold under the trade names Smoothmint, Ultimint, and Icy Mint, available from International Flavors and Fragrances, USA & China. Refrigerants can also be part of the fragrance system. Preferred cooling agents in the present compositions are paramentan carboxamide based agents such as N-ethyl-p-menthane-3-carboxamide (commercially known as WS-3) and mixtures thereof.

The fragrance is generally used in the compositions in an amount of from about 0.001% to about 5% by weight. composition.

A sweetening agent such as saccharin, dextrose, sucrose, lactose, maltose, levulose, aspartame, sodium cyclamate, D-tryptophan, dihydrochalcones, acesulfame, and mixtures thereof can be added to the present composition. Sweetening agents are generally used in toothpastes in an amount of from about 0.005% to about 5% by weight. composition.

A herbal agent, including, but not limited to, gold strand extract, honeysuckle extract, and mixtures thereof may also be present in the compositions of the invention in an amount from about 0.01% to about 0.05%. Such herbal remedies are believed to provide antimicrobial efficacy.

While not required, traditional antibacterial agents may also be present in the dentifrice composition of the present invention. However, because they are expensive and the present invention shows surprising stability without the use of these agents, in a preferred embodiment the present invention does not contain traditional antimicrobial agents. A preferred traditional antibacterial agent is 5-chloro-2- (2,4-dichlorophenoxy) -phenol, commonly referred to as triclosan, and is described in The Merck Index. Ed. 11 (1989), p. 1529 (entry no. 9573), in US Patent 3506720, and in European Patent Application Beecham Group EP0251591, PLC, published Jan. 7, 1988. Other specific antibacterial agents include chlorhexidine, triclosan monophosphate, and essential oils including including thymol, geraniol, carvacrol, citral, hinokithiol, eucalyptol, and mixtures thereof. Triclosan and other agents of this type have been disclosed in Parran, Jr., et al., US Patent 5,015,466, issued May 14, 1991, and US Patent 4,894,220, issued Jan. 16, 1990 to Nabie, et al. These agents may be present in an amount from about 0.01% to about 1.5% by weight. composition.

In addition to such antibacterial agents, there are also water-insoluble non-cationic antibacterial agents, such as halogenated diphenyl ethers, phenolic compounds, including phenol and its homologues, mono- and polyalkyl and aromatic halophenols, resorcinol and its derivatives, biphenols and halogenated salicylanilides, esters and halogenated carbanilides. Water-soluble antibacterial agents include quaternary ammonium salts and bis-biguanide salts, etc. Triclosan monophosphate is also a suitable water-soluble antibacterial agent. Quaternary ammonium salts include those compounds where

One or two of the quaternary nitrogen substituents have a carbon chain (typically alkyl) from about 8 to about 20, typically from about 10 to about 18 carbon atoms, the remaining substituents (typically alkyl or benzyl) have a smaller number of carbon atoms, i.e. from about 1 to about 7 carbon atoms, typically methyl or ethyl groups. Examples of typical quaternary ammonium antibacterial agents are dodecyltrimethylammonium bromide, tetradecylpyridinium chloride, domidomiphene bromide, N-tetradecyl-4-ethylpyridinium chloride, dodecyldimethyl (2-phenoxyethyl) -ammonium-quaternimethylchloridimethylchloride, 5-phenylethyl ammonium chloride, 1,3-tetradecylpyridinium chloride. bis (2-ethylhexyl) -5-methylhexahydropyrimidine, benzalkonium chloride, benzethonium chloride and methylbenzethonium chloride. Other compounds are the bis [4- (R-amino) -1-pyridinium] alkanes disclosed by Bailey in US Patent 4,206,215, issued June 3, 1980. stannous salts such as stannous pyrophosphate and stannous gluconate, and other antibacterial agents such as as copper bisglycinate, copper glycinate, zinc citrate, and zinc lactate also can be present in the composition. Enzymes are also useful, including endoglycosidase, papain, dextranase, multanase, and mixtures thereof. Such measures were disclosed by Norris et al. in U.S. Patent 2,946,725, issued July 26, 1960, and Gieske et al. in US Patent 4,051,234, issued September 27, 1977, which is hereby incorporated by reference into this application.

Suitable for use in this application are antibacterial agents such as phthalic acid and its salts including, but not limited to, those disclosed in US Patent 4,994,262, issued February 19, 1991, preferably magnesium monopotassium phthalate, chlorhexidine (Merck Index, no. 2090), alexidine (Merck Index, no. 222; hexetidine (Merck Index, no. 4624); sanguinary (Merck Index, no. 8320); benzalkonium chloride (Merck Index, no. 1066); salicylanilide (Merck Index, no. no. 8299); domiphen bromide (Merck Index, no. 3411); cetylpyridinium chloride (CPC) (Merck Index, no. 2024; tetradecylpyridinium chloride (TPC); N-tetradecyl-4-ethylpyridinium chloride (TDEPC); octenidine; delmopinol , octapinol, and other piperidine derivatives; nicin preparations; zinc / tin (II) ionic agents; antibiotics such as augmentin, amoxicillin, tetracycline, doxycycline, minocycline and metronidazole; and analogs and salts of the above; methyl salicylate; hydrogen peroxide, metallic saltschlorite and mixtures thereof.

In order to achieve the desired effect in the practice of the present invention, e.g. whitening, breath freshening, anti-caries protection, pain relief, gum improvement, tartar control, etc., the user only needs to apply the present tooth cleaning composition to the tooth surface at the desired area. , in a human or animal. The compositions can also be applied to other surfaces of the oral cavity such as the gingiva or mucosa, although it is believed that greater benefits are obtained when the dentifrice composition is applied to the teeth. The dentifrice composition may contact the surface of the teeth and / or the oral cavity either directly or indirectly, but it is more preferred to apply the dentifrice composition directly. The dentifrice composition may be applied in any manner, but is preferably applied using a brush.

The dentifrice composition can be prepared using conventional materials and methods known in the art. For example, the humectant and any optional di- and trihydric alcohols may be added to the purified water, then homogenized in an anticaries mixer for 2 min. A sweetener, antimicrobial agent, and other adjuvants (other than the fragrance system, surfactant, and titanium oxide) can be added, and the mixture is homogenized for a further 10 min. The thickener and titanium oxide are then added to the mixture at a pressure of about 10-20 kPa for about 20 minutes to remove air bubbles. The surfactant and fragrance are added and homogenized under reduced pressure for 15 to 30 mins to give the final dentifrice composition. The dentifrice composition is then packaged into individual dispensers, e.g., toothpaste tubes, for shipping and sale.

The final dentifrice composition typically has a viscosity of from about 0.8 to about 10 Pas, preferably from about 1.5 to about 8 Pas, and more preferably from about 1.5 to about 5 Pas. The viscometer used is a Brookfield viscometer, Model 1/2 RVT (spring force 1/2), with a Brookfield "Helipath." The spindle is a typical "E series" T-shaped spindle. The viscometer is mounted on a Helipath stand and leveled with an alcohol level. The spindle E is attached and, after starting, the speed is set to 2.5 rpm. The viscosity is measured after 10 min, the temperature is constant at 25 ° C. Commercially acceptable dentifrice compositions typically have suitable rheological properties, good texture, pleasing aesthetic characteristics and a specific gravity greater than water, preferably from about 1 to 1.5 g / cm ³ , most preferably from about 1 g / cm 3. 1 to about 1.3 g / m ³ . Dentifrice compositions having the above viscosity and specific gravity are generally acceptable to the consumer.

Embodiments of the invention are given below.

T h e x l e d s 1-2

The following dentifrice compositions are prepared according to the method described above.

Ingredient Comparative example A. Example 1 Example 2 Sodium Fluoride, USP 0.25 0.25 0.25 Silica, precipitated (Zeodent 119) twenty twenty twenty Sorbitol 30.4 21 14 Purified Water * 29.4 53.85 60.8 Triclozan, USP 0.05 - 0.05 Carbopol 956 0.2 0.3 0.3 Sodium carboxymethyl cellulose 0.85 1 1 Sodium Saccharin, USP 0.15 0.25 0.25 Trisodium phosphate dodecahydrate 1.3 0.5 0.5 Sodium alkyl sulfate 2.1 1.8 1.8 Fragrance system 0.8 0.8 0.8 Titanium Dioxide, USP (Rutile) 0.5 0.25 0.25 Glycerine 10 - - Polyethylene glycol 4 - - TOTAL 100 100 100 Brookfield Viscosity (Belt) (10 min each) 1.3-3.7 1.8 1.5 pH 6.8-7.4 6.8 6.8 Soluble Fluoride Level (3: 1 suspension purified with water: dentifrice) 265-315 ppm 268 ppm 268 ppm Specific weight (g / cm ³ ) 1.32-1.38 1.2 1.2

* contains water from sorbitol solution, surfactant solution, etc.

Non-limiting examples of the dentifrice compositions of the invention are described in Examples 1 and 2, and comparative Example A is also provided. All three formulations have surprisingly good rheological properties and stability; however, the unit cost of the formulation of Comparative Example A is about 50% greater than the cost of the formulations of Examples 1 and 2. Furthermore, the compositions of Examples 1 and 2 have excellent stability although they contain more than 50% water. Moreover, the compositions of Examples 1 and 2 provide improved fragrance release (i.e. perception of fragrance), at the same level of fragrance content as Comparative Example A.

Surprisingly, after 1 month, the bacterial growth in Example 1 is comparable to that of Comparative Example A and Example 2, although there is no Triclosan in the composition of Example 1.

PL 202 563 B1

P r z o l a d y 3-4

The following dentifrice compositions are prepared according to the method described above.

Ingredient Example 3 Example 4 Sodium Fluoride, USP 0.243 0.243 Silica, precipitated (Zeodent 119) 22 21 Sorbitol thirty thirty Purified Water* 32.657 38.057 Carbopol 956 0.3 0.3 Sodium carboxymethyl cellulose 1 1.1 Sodium Saccharin, USP 0.25 0.25 Trisodium phosphate dodecahydrate 3 0.5 Monosodium phosphate 2 Sodium alkyl sulfate 7.5 7.5 Fragrance system 0.8 0.8 Titanium Dioxide, USP (Rutile) 0.25 0.25 TOTAL 100 100 Brookfield Viscosity (Belt) (10 min each) 2.1 1.8 pH 6.8 6.8 Soluble Fluoride Level (3: 1 Suspension: Purified Water: Dentifrice) 268 ppm 268 ppm Specific weight (g / cm ³ ) 1.29 1.22

* contains water from sorbitol solution, surfactant solution, etc.

Claims (6)

A dentifrice composition comprising an abrasive polishing material, a thickening agent, a humectant, an anti-cavity agent, and water, characterized in that it comprises A. 6% to 70% silica based abrasive polishing material; B. from 0.5% to 4.5% of a thickening agent selected from the group consisting of carboxymethyl cellulose, carbomer, xanthan gum, and mixtures thereof; C. from 0.5% to 45% of a humectant selected from the group consisting of sorbitol, xylitol, glucose, and mixtures thereof; D. 0.05% to 2.5% of an anti-cavity agent selected from sodium fluoride; and E. at least 30% water, the composition being free of di- and trihydric alcohols, and the composition having a viscosity of from 0.8 to 10 Pa · s. 2. A composition according to claim 1 The composition of claim 1, containing from 0.1% to 1% sodium fluoride. 3. A composition according to p. 5. The composition of claim 1, comprising at least 40% water. 4. A composition according to p. The composition of claim 1, comprising from 5% to 30% of a humectant. PL 202 563 B1 5. A composition according to p. The composition of claim 1, wherein the viscosity of the composition is from 1.5 to 8 Pa. S, preferably the viscosity of the composition is 1.5 to 5 Pa. S. 6. A composition according to p. The method of claim 1, further comprising an excipient selected from the group consisting of a source of peroxide, a source of alkali metal bicarbonate, an anti-calculus agent, a surfactant, titanium dioxide, an antioxidant, a colorant, a perfume, a sweetener, a herbal agent, an antimicrobial agent and mixtures thereof.