MXPA97010224A - Oral compositions having accelerated effects of whitening of dien - Google Patents

Abstract

The present invention relates to a two-component whitening dentifrice composition comprising a first component containing a peroxygen compound such as hydrogen peroxide and a second component of dentifrice containing a complex manganese coordination compound such as manganese gluconate. , which activates the peroxygen compound and accelerates the release of active oxygen for a rapid whitening action, the first and second components are kept separate from each other until they are supplied for application to the dient.

Description

ORAL COMPOSITIONS FEARING ACCELERATED EFFECTS OF BLEACHING OF TEETH.

Antecedents of the Invention 1. Field of the Invention This invention relates generally to an oral composition, which when applied on the surface of the teeth acts to whiten the teeth and more particularly to an oral composition for whitening the teeth which is more effective than the existing available products. for the consumer. 2. Previous Art A tooth is composed of an inner dentin layer and an outer hard enamel layer that is the protective layer of the tooth. The enamel layer of a tooth is naturally opaque white or a slightly discolored color. It is this layer of enamel that can stain or discolor. The enamel layer of a tooth is composed of hydroxyapatite mineral crystals that create a somewhat porous surface. It is believed that this porous nature of the enamel layer is what allows staining agents and bleaching substances to permeate enamel and discolor the tooth.

Many substances that a person confronts or contacts with a daily basis can "stain" or reduce the "whiteness" of one's teeth. In particular, food, tobacco products and fluids such as tea and coffee tend to stain one's teeth. These products or substances tend to accumulate on the enamel layer of the teeth and form a film on the teeth. These staining and coloring substances can then permeate the enamel layer. This problem occurs gradually over many years, but imparts noticeable discoloration to the enamel of one's teeth.

Oral compositions for home use, which contain 1-3% by weight of concentrations of peroxygen compound such as hydrogen peroxide, are available on the market and when applied to the teeth effect bleaching of the spots. However, these compositions are considered to have a slow bleaching effect.

Exemplary oral compositions containing peroxygen compounds for bleaching teeth include those of U.S. Patent Nos. 5,302,374, 5,279,816, 4,988,450; No. 4,980,152, United States of America No. 4,839,156, and United States of America No. 3,657,417.

U.S. Patent No. 5,279,816, discloses an oral composition for bleaching teeth containing dissolved peracetic acid suspended in a vehicle. U.S. Patent No. 5,302,374 describes the generation of a peracetic acid within a toothpaste by combining water, acetylsalicylic acid and a water-soluble alkali metal percarbonate.

The patent of the United States of America No. 4,988,450 and United States of America No. 3,657,417 describes the formulation of oxygen-releasing compositions for bleaching teeth using anhydrous gels or pastes.

U.S. Patent No. 4,980,152 discloses an aqueous oral gel composition comprising about 0.5 to about 10% by weight of urea peroxide or 0.01 to 2% by weight of a compound providing fluoride.

U.S. Patent No. 4,839,156 describes a thickened oral gel composition Pluronic-hydrogen peroxide containing water.

U.S. Patent No. 4,405,599 discloses a toothpaste containing a combination of oxidising agents of sodium perborate and calcium peroxide, the cleaners of dicalcium phosphate, calcium carbonate and magnesium carbonate, the humectant of sorbitol, the thickeners of cellulose gum and corn starch, and an anionic detergents.

U.S. Patent No. 3,988,433 describes oral compositions containing peroxyacids and diperoxyalkyl acids having alkylene groups containing 5-11 carbon atoms, which remove stains from teeth.

In those applications where the oral compositions are designed for the domestic use of teeth whitening, it is essential that the peroxide gelation components react rapidly since the user will normally wish to limit the time at which the whitening composition is in contact with the teeth. To accomplish this, the Applicant has recognized the desirability of accelerating the breakdown of the peroxygen compounds and the release of active oxygen into the oral cavity to effect faster whitening of the teeth.

Synthesis of the Invention According to the present invention there is provided an oral peroxygen composition for accelerated bleaching of the teeth wherein a non-mixed two-component composition composed of (a) a first component containing a water-soluble peroxygen compound is provided. in an orally acceptable vehicle and (b) a second unmixed component containing a compound of manganese coordination complex in an orally acceptable vehicle in an amount effective to activate the peroxygen compound and accelerate the release of active oxygen, the two phases being combined shortly before application to the teeth wherein the manganese compound interacts with the peroxygen constituent to accelerate the breakdown and rapid release of active oxygen from the peroxygen compound, such rapid release being effective for whitening the teeth when leaving the stay on the teeth for a while Po limited.

The present invention offers the advantages that the active oxygen is generated rapidly and in large quantities thus facilitating convenient and effective domestic use by the consumer as well as professional use by a dentist.

Detailed description of the invention Peroxygen compounds useful in the oral compositions of the invention include hydrogen peroxide, peroxydiphosphate, urea peroxide, metal peroxides such as calcium peroxide, sodium peroxide, strontium peroxide, magnesium peroxide. , and the salts of perborate, persilicate, perphosphate and percarbonate such as sodium perborate, potassium persilicate and sodium percarbonate. The most suitable peroxygen compound for this invention is hydrogen peroxide.

Manganese coordination complexes suitable for use as activator compounds in the practice of the present invention include a complex of manganese (III) and a multidentate ligand supplied by a complexing agent such as the activating compounds that are known in the art and are fully described in U.S. Patent No. 4,728,455, the disclosure of which is incorporated herein by reference.

Preferred activators to be used to accelerate the breakdown of the peroxygen compounds and the release of the active oxygen according to the practice of the present invention include a complex of manganese (III) and a multidentate ligand supplied by a carboxylic acid complexing agent. hydroxy containing at least 5 carbon atoms, including hydroxy hexonic acids such as gluconic acid, gulonic acid, idonic acids such as glucuronic acid, galacturonic acid and mannuronic acid, heptonic hydroxy acids such as acid glucoheptanoic acid and sugars such as saccharic acid and isosaccharic acid. A more preferred compound is Mn (III) gluconate.

Other useful manganese coordination complex compounds suitable for use in the practice of the present invention include the manganese complexes of the formula.

Ln Mm X where Mn is manganese in the oxidation state +3 or +4; n and m are integers from 1 to 4; X represents a coordination or bridge species that coordinates with manganese and is selected from H20, OH ", 02", SH., And the alkyl and aryl groups having from 1 to 20 carbon atoms. L is a ligand having at least two nitrogen, phosphorus, oxygen or sulfur atoms coordinating with manganese.

Examples of the ligands suitable for the formula of the manganese complexes of the formula are more fully described in U.S. Patent No. 5,194,416, such description is incorporated herein by reference. Preferred examples of L in the above-indicated formula include: 1, 4, 7-triazacyclonanone; 1,4,7-triazacyclodocane, 1,4-triazacyclohexane, 1,5,9-triazacyclodecane, 1,4,7-trimethyl-1, 1,4,7-triazacyclonanone, 1,4,7-trimethyl- l, 1,4,7-triazacyclodocane, 1,4,8-trimethyl-1,1,4,8-triazacyclohexane, 1, 5, 9-trimethyl-1, 1,5,9-triazacyclododecane, tris (pyridine), 2-yl) methane, tris (pirasol-l-yl) methane, tris (imidazol-2-yl) methane, tris (pyridin-2-yl) borate, tris (imidazol-2-yl) phosphine, 1, 1, l-tris (methylamino) ethane, Bis (pyridin-2-yl-methyl) amine, Bis (triazol-1-yl-methyl) amine and Bis (imidazol-2-yl-methyl) amine.

The amount of peroxygen compound incorporated in the first component of the two-component oral composition of the present invention will vary depending on its intended use. For use by professionals trained in office treatments, the concentration of peroxygen compound incorporated in the oral composition can vary from about 5 to about 30% by weight. For domestic use, such high concentrations of the peroxygen compounds can not surely be made by the typical consumer and therefore the useful range of the peroxygen compound when the oral composition is in paste, gel or rinse is between 0.1 to 3.0% by weight. The preferred range is between about 0.5 to about 2.0% by weight.

The amount of manganese complex activating compound present in the second component of the two-phase bleaching oral composition of the present invention will vary depending on the amount of peroxygen compound incorporated in the first component. When the oral bleaching composition is to be used by trained professionals and the first component contains relatively high concentrations of a peroxygen compound, for example, from 5 to 35% by weight, the amount of the manganese activating compound incorporated into the second component will vary from between 0.1 to 3% by weight and preferably between 0.25 to 1.75% by weight. For home use oral compositions in which the concentration range of the peroxygen compound in the first component of the oral composition is between about 0.1 to about 3.0% by weight, the lowest concentrations, for example, between about 0.001 to about 0.3% by weight of the manganese activator are included in the second component and about 0.025 to about 0.15 percent by weight of the activator are preferably used.

The vehicle used to prepare the individual components of the oral composition of the present invention is essentially the same for both components and includes water and a suitable humectant such as glycerin, propylene glycol, polyethylene glycol, or any suitable mixture thereof. A mixture of glycerin and polyethylene glycol is preferred as the humectant in the practice of the present invention.

In the proportion of vehicle in each of the dentifrice components of the present invention is generally within the range of from about 40 to about 80 percent by weight of the paste or gel dentifrice component of this invention and preferably from about 50 to 65 percent by weight of the tooth component.

A surfactant is used in the preparation of the components of the oral composition of the present invention to aid in the complete dispersion of the composition through the oral cavity when applied thereto as well as to improve cosmetic acceptability and detersive properties and foaming of the composition. Among the surfactants useful in the practice of the present invention are the salts of the higher alkyl sulfates and the alkyl sulfates having from 8 to 18 carbon atoms in the alkyl group such as sodium lauryl sulfate and sodium phosphate. sodium lauryl, sulfoacetate lauryl sodium, salts of sulfonated monoglycerides of higher fatty acids, such as coconut monoglyceride sulfate or other suitable sulfonated monoglycerides of fatty acids of 10 to 18 carbon atoms, the salts of the amides of higher fatty acids , for example, acids of 12 to 16 carbon atoms, with lower aminoliphatic acids, such as sodium N-methyl-N-palmitoyl tauride, sodium N-laurolo-N-myristoyl- and N-palmitoyl sarcosinates.; the salts of the esters of such fatty acids with isothionic acid or with glycerol ßonosulfate, such as the solution salt of monosulphated ßonoglyceride of the hydrogenated coconut oil fatty acids.

The surfactant is included in the vehicles of the components of the oral composition of the present invention at a concentration of from about 0.5 to about 3.0% by weight and preferably from about 1.0 to about 2.0% by weight.

To prepare the dentifrice components, the polishing agents are incorporated into both components of the present invention and the preferred polishing agents are silicon materials, such as silica, which have a main particle size of up to about 20 microns. A preferred silica is a precipitated amorphous hydrous silica, such as Sorbosil AC-35 marketed by Crosfield Chemicals or Zeodent 115 of J.M. Huber Company but other polishing agents can also be used, including sodium metaphosphate, potassium ßetaphosphate, tricalcium phosphate, calcium phosphate dihydrate, anhydrous dicalcium phosphate, calcium pyrophosphate, magnesium orthophosphate, trimagnesium phosphate, alumina trihydrate, aluminum silicate, sirconium silicate, alumina and calcined window.

The polishing agent is present in the dentifrice compositions of the present invention at a concentration of from about 10 to about 30 percent by weight and preferably from 15 to about 25 percent by weight.

The inorganic thickeners can be included in the dentifrices of the present invention and include smoked silicas such as Cabosil available from Cabot Corporation, and thickener silicas including those available from .R. Grace designated Sylox 15.

Organic thickeners such as natural and synthetic gums and colloids can also be incorporated into the dentifrice compositions of the present invention. Examples of such thickeners include carrageenan (Irish moss), xanthan gum and sodium carboxymethyl cellulose, starch, polyvinyl pyrrolidone, hydroxyethylpropyl cellulose, hydroxybutyl methyl cellulose, hydroxypropyl methyl cellulose and hydroethyl cellulose.

The inorganic or organic thickener may be incorporated into dentifrice components of the present invention at a concentration of from about 0.05 to about 2% by weight and preferably from about 0.1 to about 1.5% by weight.

The fluoride-providing salts having anticaries efficacy can also be incorporated into the oval compositions of the present invention and are characterized by their ability to release fluoride bonds in water. It is preferred to employ a water-soluble salt fluoride that provides about 10-5000 ppm of fluoride ion and preferably about 1000-1500 ppm of fluoride ion. Among these materials are the water-soluble alkali metal salts, for example, potassium fluoride, sodium mono-phosphate phosphate and sodium fluorosilicate. Sodium fluoride and sodium monoflorophosphate with preferred fluoride salts.

Salts having an anticalculus efficacy including water soluble salts, such as dialkali or tetraalkali metal pyrophosphate salts such as Na4P207 (TSPP) K4P207, Na2K2P207, Na2H2P207 and K2H2P207, long chain polyphosphate, such as cyclic sodium hexametaphosphate and phosphate such as sodium trimetaphosphate as well as the alkali metal tripolyphosphates such as sodium tripolyphosphate (STPP) and potassium tripolyphosphate can be incorporated in the dentifrice compositions of the present invention preferably at a concentration of about 0.5 to about 8.0% by weight.

A marbled toothpaste product is obtained in accordance with the practice of the present invention wherein the dyes of contrasting colors are incorporated into each of the tooth components used in the practice of the present invention, the dyes being pharmacologically and physiologically non-toxic when use in the suggested quantities. The colorants used in the practice of the present invention include both pigments and dyes.

The pigments used in the practice of the present invention include non-toxic water-insoluble inorganic pigments such as titanium dioxide and chromium oxide greens, ultramarine and pink blues and ferric oxides as well as water-insoluble dye lacquers. prepared by aluminum or calcium salts of extension of FD &C dyes on alumina, such as the lacquer FD &C Green No. 1, the lacquer FD &C Blue No. 2, the lacquer FD &C R &D No. 30 and the lacquer of FD &C No. Yellow 15. The pigments have a particle size in the range of 5-1000 microns, preferably 250-500 microns and are present in a concentration of 0.5 to 3% by weight.

The dyes used in the practice of the present invention are uniformly distributed throughout the dentifrice component and are generally food color additives currently certified under the food, drug and cosmetic law for use in drugs and ingested foods, including dyes such as FD &C Red No. 3 (sodium salt of tetraiodofluoroesaine), FD &C Yellow No.5 (sodium salt of 4p-sulfophenylazo-1-p-sulfophenyl-5-hydroxypyrasole-3 carboxylic acid), FD &C Yellow No 6 (sodium salt of p-sulfophenylazo B-naptol-6-monosulfonate), FD &C Green No. 3 (disodium salt of 4 { [4- (N-ethyl-p-sulfobenzylamino) -phenyl] - (4-hydroxy-2-sulfoniunphenyl-methylene.) - [lN-ethyl-Np-sulfobenzyl) -? - 3,5-cyclohexadienimine] FD &C Blue No. 1 (disodium salt of dibenzyl diethyldiane inotriphenylcarbinol trisulphonic acid) , FD &C Blue No. 2 (sodium disulfonic acid salt of indigotin) and mixtures thereof in various s proportions.

The concentration of dye for most effective result in the present invention is present in the dentifrice composition in an amount of from about 0.005% to about 2% by weight.

It is preferred that the colorant included in one of the dentifrice components be a pigment such as Ti02 and that the colorant distributed through the vehicle of the other dentifrice component be a dye and that the dye be a different color from the pigment included in the first toothpaste component. To avoid bleaching of the dye by the constituent of the peroxygen compound it is critical that the peroxygen compound is not included in the dentifrice component in which a peroxygen-sensitive dye ingredient is included.

Any suitable sweetening or flavoring material can also be employed. Examples of suitable flavoring constituents are flavor oils, for example, oils of peppermint, peppermint, clove, sage, eucalyptus, marjoram, cinnamon, lemon and orange and methyl salicylate. Suitable sweetening agents include sucrose, lactose, maltose, sorbitol, sodium cyclamate, perillartin and zacarine sodium. Suitably, the flavor and sweetener agents can together comprise from 0.01% to 5% or more of the preparations.

Various other materials may be incorporated within the components of the composition of this invention. Non-limiting examples thereof include preservatives, silicones and chlorophyll compounds, vitamins, such as vitamins B6, B12, C, E and K, antibacterial agents such as chlorohexidene, allogenated diphenylethers such as triclosan, desensitizing agents such as potassium nitrate and potassium citrate and mixtures thereof. These auxiliaries are incorporated into the components of the oral composition in amounts which do not adversely affect the desired properties and characteristics, and are selected and used in appropriate amounts, depending on the particular type of component involved.

To prepare a peroxygen compound containing a paste or toothpaste component of the present invention, humectants, for example, propylene glycol, glycerin, polyethylene glycol ingredients, sweetener and water are dispersed in a conventional mixer until the mixture becomes a homogeneous gel phase. In the gel phase, a pigment such as Ti02 and tartar control agents such as tetrasodium pyrophosphate or sodium tripolyphosphate or both and agents against fluoride caries such as monofluorophosphonate are added. These ingredients are mixed until a homogeneous phase is obtained. After the thickener, the polishing agent, the peroxygen compound, the flavor and the surfactant ingredients are added and the ingredients are mixed at a higher speed under vacuum of about 20-100 mm Hg. The resulting product is an extrudable, semi-solid, homogeneous paste product.

To prepare the second dye-containing component, an identical procedure to that described above is employed except that the ink ingredients and activator compounds are incorporated in the initial mixture of humectants and sweetener and the Ti02 and the peroxygen compound are omitted from the formula of the toothpaste component.

To prepare a rinse composition the various ingredients are mixed together in water in a conventional manner.

In the package of the oral composition of the present invention for sale, any convenient means for effecting separation of the peroxygen compound from the activating components before use may not be used. For example, in the packaging of dentifrice components, a single container can be divided into compartments so that the peroxygen-containing tooth component and the activator-containing component are housed in separate compartments and are simultaneously stocked for a common application to a toothbrush. teeth and do not mix until they are applied to the teeth. Alternatively, the peroxygen-containing component and the activator-containing component can be housed in separate containers from which the respective phases are dispensed to be combined just before use.

The following examples are further illustrative of the present invention but it is understood that the invention is not limited thereto. All the amounts and proportions mentioned herein and in the appended claims are by weight.

Example 1 Table 1 Dentifrice Composition of Dual Component To prepare component 1, water, glycerin, propylene glycol, polyethylene glycol 600 and sodium saccharin ingredients were dispersed in a conventional mixer until the mixture became a solution, which was smooth in appearance, producing a homogeneous gel phase in which the MFP, TSPP, STPP and Ti02 were added by mixing to prepare a dispersion. The dispersion was transferred to a vacuum mixer, and the silicon agents, hydrogen peroxide, sodium carbonate and flavor were added and mixed for 10 to 30 minutes at a high speed under a vacuum of about 50 mm. Hg, to obtain a homogeneous mixture. The resulting product was a paste with a satisfactory flavor and white color.

Component 2 was prepared in the same manner as was used for component 1, except that the dye FD &C was replaced by the pigment Ti02 and the manganese gluconate was replaced by the hydrogen peroxide. The resulting product was a gel with a satisfactory flavor and was green.

To test the bleaching efficacy of the components of toothpaste 1 and 2, the human teeth stained naturally and stained with a broth essentially coffee, tea, ucine, microbiological means and a chromogenic microorganism. The stained teeth selected for the test showed the same amount of discoloration. To test the bleaching efficiency of the gel, the teeth were immersed in two grams of a mixture of equal amounts of components 1 and 2 at 37 ° C. Before immersion the color of the teeth was measured with a Minolta Chromameter in which L * is a measure of the eye's response to light and darkness, and b * is a measure of the yellowish, a * is a measure of the bluish ones. The higher the value L * and the lower the value of b *, the teeth will appear whiter.

The whiteness index was calculated using the following question: ? E = (? L *) 2 + (? B *) 2] 12 The higher it is? The greater the bleaching effect observed.

The teeth remained submerged in the mixed components for 15 minutes. The bleaching index (? E) of submerged teeth is summarized in Table II given below.

For comparison purposes, the procedure of Example 1 was repeated except that component 2 did not contain manganese gluconate. This comparative composition was designated as composition "Cl" of the bleaching index of the comparative composition Cl is also summarized in Table II given below.

Example 2 to 5 The procedure of Example I was repeated except in separate dentifrice components urea peroxide (Example 2), sodium percarbonate (Example 3) calcium peroxide (Example 4) and peroxydiphosphate (Example 5) were replaced by the peroxide of hydrogen in Example 1. The dual component compositions of Examples 2-5 were also tested for bleaching efficacy following the test procedure of Example 1.

For comparison purposes, the product used to prepare the compositions of Examples 2-5 was repeated with the exception that the manganese gluconate activating ingredient included in component 2 was not included. The color measurements, these designated comparative compositions C2 to C ,, are also included in Table II given below. Table II The ΔE values reported in Table II indicate that activating manganese gluconate essentially increases the bleaching efficiency of the peroxygen compound, hydrogen peroxide, urea peroxide, sodium percarbonate, calcium peroxide compounds and of peroxydiphosphate in the order of about 1.5 to 8 times.

Claims (14)

1. A method for whitening stained or discolored teeth in the oral cavity which comprises applying to the teeth a two component whitening composition, which will whiten stained or discolored teeth, when applied to these, the composition being composed of a first component containing in a vehicle a safe amount of an effective peroxygen compound for teeth whitening, and a second component containing a compound of manganese coordination complex in a vehicle, the manganese compound being present in the vehicle in an effective amount for activating the peroxygen compound, first and second components being kept separate from each other until they are supplied for application to the teeth, supplying and mixing the components maintained separately so that the manganese compound of the second component interacts with the compound of peroxygen of the first component so the rompim of the peroxygen compound and the release of the active oxygen is accelerated and then the mixed components are allowed to remain on the teeth for a sufficient time to effect a rapid bleaching of the same.

2. The method as claimed in clause 1, characterized in that the peroxygen compound is hydrogen peroxide.

3. The method as claimed in clause 1, characterized in that the peroxygen compound is urea peroxide.

4. The method as claimed in clause 1, characterized in that the peroxygen compound is sodium percarbonate.

5. The method as claimed in clause 1, characterized in that the peroxygen compound is calcium peroxide.

6. The method as claimed in clause 1, characterized in that the peroxygen compound is peroxydiphosphate.

7. The method as claimed in clause 1, characterized in that the manganese coordination complex compound is a manganese gluconate.

8. A two-component whitening dentifrice composition which exhibits rapid bleaching of stained or discolored teeth, which composition comprises a first component of dentifrice containing a peroxygen compound and a second component of dentifrice containing a complex compound of manganese coordination, The first and second dentifrices are kept separate from one another until they are filled for application to the teeth requiring the removal of the stain and discoloration.

9. The composition as claimed in clause 8, characterized in that the peroxygen compound is hydrogen peroxide.

10. The composition as claimed in clause 8, characterized in that the peroxygen compound is urea peroxide.

11. The composition as claimed in clause 8, characterized in that the peroxygen compound is sodium percarbonate.

12. The composition as claimed in clause 8, characterized in that the peroxygen compound is calcium peroxide.

13. The composition as claimed in clause 8, characterized in that the peroxygen compound is peroxydiphosphate.

14. The composition as claimed in clause 8, characterized in that the peroxygen compound is manganese gluconate.