MX2008007467A - Abrasive system for oral care compositions - Google Patents

Abstract

Oral compositions comprising a first and a second abrasive are provided. The first abrasive preferably has an Einlehner hardness of greater than about 5 mg loss per 100,000 revolutions, and the second abrasive preferably has an Einlehner hardness of less than about 5 mg loss per 100,000 revolutions. A ratio of the first abrasive to the second abrasive ranges from about 1:1.6 to about 1.6:1, and the first and second abrasives are preferably present in the oral composition at an amount of about 13%to about 21%by weight, respectively. The pellicle cleaning ratio of the oral composition is greater than 100 and the radioactive dentin abrasiveness is preferably less than 200, and in certain embodiments, preferably less than about 175. Methods of using the oral compositions are also provided.

Description

ABRASIVE SYSTEM FOR COMPOSITIONS FOR ORAL CARE CROSS REFERENCE TO RELATED REQUEST The present application claims the benefit of U.S. Provisional Patent Application No. 60 / 752,340, filed December 21, 2005, which is hereby incorporated by reference in its entirety.

BACKGROUND OF THE INVENTION The abrasives in the oral compositions clean the contaminated tissue (debride) and physically rub the outer surface of the teeth. This rubbing action removes the organic biofilm (ie the film) on the surface of the teeth and is mainly composed of saliva proteins, bacteria and bacterial byproducts. It can be stained and discolored by food, such as coffee, tea and red fruits, as well as tobacco smoke, cationic compounds and chromogenic bacteria. Said physical removal of the stained film is a simple and effective means to eliminate stains and discoloration of the surface, which are undesirable and which occur daily. Moreover, said physical removal of the film also removes the bacterial plaque on the surface of the film. film, which minimizes the potential of gingivitis, periodontitis and caries formation. However, oral compositions, such as toothpastes, should not have such high abrasiveness that it could result in potential damage to enamel or tissues. Therefore, it is desirable to develop oral compositions that optimize the cleaning and / or polishing efficacy of the oral composition, while at the same time minimizing harmful abrasivity to avoid potential damage to oral surfaces.

BRIEF SUMMARY OF THE INVENTION In various embodiments, the present invention relates to an oral composition comprising: a first abrasive having an Einlehner hardness greater than about 5 mg loss per 100,000 revolutions; Y a second abrasive that has a hardness of Einlehner less than about 5 mg loss per 100,000 revolutions; wherein the ratio of the first abrasive to the second abrasive is from about 1: 1.6 to about 1. 6: 1, and wherein the oral composition has a film removal ratio (PCR) of greater than about 100 and an abrasion of radioactive dentin (RDA) of less than about 200.

In various embodiments, the present invention relates to an oral composition comprising: a first abrasive comprising silica, having an Einlehner hardness of greater than about 5 mg of loss per 100,000 revolutions and an absorption oil of less than about 90 cm 3/100 g; Y a second abrasive comprising silica, having an Einlehner hardness less than about 5 mg loss per 100,000 revolutions and an absorption oil greater than about 90 cm 3/100 g; wherein the first abrasive is present in an amount of about 13% to about 21% by weight and the second abrasive is present in an amount of about 13% to about 21% by weight of the composition.

In various embodiments, the present invention relates to an oral composition comprising: a first abrasive comprising silica and having an absorption oil of less than about 90 cm 3/100 g and an Einlehner hardness greater than about 5 mg of loss per 100,000 revolutions; Y a second abrasive comprising silica and having an absorption oil of greater than about 90 cm 3/100 g and an Einlehner hardness of less than about 5 mg of loss per 100,000 revolutions; wherein a ratio of the first abrasive to the second abrasive is from about 1: 1.6 to about 1.6: 1, and a total amount of the first and second abrasives present in the oral composition is greater than about 25% by weight of the composition; and wherein the oral composition has a film removal ratio of greater than about 100 and an abrasion of the radioactive dentin of less than about 200.

In various embodiments, the present invention provides methods for increasing the delivery of a active ingredient in an oral composition to an oral surface, comprising: introducing an oral composition into an oral cavity, wherein the oral composition comprises the active ingredient, a first abrasive and a second abrasive, wherein the first and second abrasives each comprise silica and each is present in an amount of about 13% to about 21% by weight, wherein the oral composition has a film removal ratio of greater than about 100 and an abrasion of the radioactive dentin of less than about 200. The composition is contacted with the oral surface. The supply of the active ingredient in the oral composition is greater than in a comparative composition having an abrasive comprising silica and a film removal ratio of less than about 100; Y contacting the composition with the oral surface, wherein the supply of the active ingredient is greater than in a comparative composition having an abrasive comprising silica and a film removal ratio of less than about 100.

In various embodiments, the present invention is directed to a composition for oral care comprising: a first abrasive having an Einlehner hardness greater than about 10 mg loss per 100,000 revolutions; Y a second abrasive having an Einlehner hardness of less than about 10 mg of loss per 100,000 revolutions wherein the ratio of the first abrasive to the second abrasive is from about 1: 1.6 to about 1.6: 1, and wherein the oral composition has a film removal ratio (PCR) greater than about 100 and an abrasion of the radioactive dentin ( RDA) less than about 200.

DETAILED DESCRIPTION OF THE INVENTION As used herein, all measurement levels described herein are by weight of the total composition, unless otherwise indicated. In addition, all references cited herein are incorporated herein by reference in their entireties. However, in case of contradiction between any of the definitions of the present description and those of a cited reference, those of the present description will prevail.

In various embodiments, an oral composition having a first abrasive and a second abrasive is provided. The selection of the abrasive for the present oral compositions may include the type of abrasive, the fineness (particle size), the particle size distribution and the amount of abrasive, in order to ensure that the tooth enamel is not excessively worn during the normal use of the composition, but clean and / or polished enough. In the context of oral care, the effectiveness of the abrasive can be expressed on the basis of the level of cleaning or abrasion of the dentifrice, namely, the rate of film removal (PCR) or the abrasion of radioactive dentin (RDA), respectively . Methods for performing PCR and RDA are described, for example, in U.S. Patent Nos. 5,939,051 and 6,290,933.

In commonly accepted conventional practice, the RDA values for an oral composition are generally kept below 250 to avoid damaging enamel or dentin with repeated use. However, in order to achieve higher PCR, you should normally increase the amount and hardness of abrasives, which is conventionally known to increase the RDA. For example, it has been observed that when the RDA value of a dentifrice composition exceeds certain values, such as, for example, above about 100 to about 115, the dentifrice does not necessarily exhibit a corresponding increase in its cleansing ability. It has been a challenge to formulate oral compositions having a PCR greater than about 80 or 90 but retaining an RDA below 250, more preferably below 200.

However, in certain embodiments of the present invention, an oral composition has been obtained with a PCR of more than 100, which at the same time has an RDA of less than 200. In certain embodiments, the RDA is less than or equal to approximately 175. , while retaining a PCR that exceeds approximately 100. In certain embodiments, the RDA is less than 165. In this respect, the oral compositions of the present invention provide superior efficacy in terms of cleaning and / or polishing, while at the same time they achieve a conveniently low RDA that minimizes the potential damage caused to enamel or dentin.

The present compositions can achieve cleaning and / or polishing of the tooth surface. The abrasives for cleaning and / or polishing can be classified according to different physical parameters. As one skilled in the art will appreciate, a single kind of abrasive normally performs at least some of the cleaning and polishing simultaneously. However, in the art, the particles are generally categorized according to the predominant effect they have on an objective oral surface.

As used herein, the term "cleaning" generally refers to the removal of contaminants, dirt, impurities and / or foreign matter on a target surface. For example, in the context of oral surfaces, in which the surface is tooth enamel, cleaning can remove at least part of a film or stain, such as plaque, film or tartar biofilm. As used herein, the term "polishing" generally refers to a finishing or refining process that makes the surface smoother and / or glossier. Polishing and cleaning can also provide shine to the surface where stain removal occurs, for example, whitening of the tooth surface.

Generally, "polishing abrasives" are those that contain relatively small particles of high hardness, while abrasives with relatively large particle sizes and low hardness are considered "abrasive" Moreover, the behavior exhibited by the abrasive when interacting with the surface indicates how well it will polish (or "smooth") the surface, since a desirable polishing agent generally degrades into smaller and smaller fragments as the contact with the surface advances, the smoothing behavior is related to the ease with which an abrasive is divided into smaller and smaller particle sizes and is generally believed to be based on the crystalline form of the abrasive particles, the lines of cleavage and friability, for example.

Therefore, an abrasive is generally categorized on a gradient that ranges from the softest abrasives for cleaning to the hardest polishing abrasives. In certain embodiments, a method for cleaning and / or polishing an objective oral surface comprises contacting the surface with an oral composition comprising a first abrasive and a second abrasive. The first abrasive of the composition can be a species other than the second abrasive, which means that each abrasive can have a different effect on the target surface, for example, it can be in a different category in the abrasive gradient. In this way, any amount of abrasives can be selected. Accordingly, the first abrasive can be a relatively low abrasive for cleaning and the second abrasive can be an abrasive for relatively high cleaning. The first abrasive can be an abrasive for cleaning and the second abrasive can be an abrasive for polishing. It should be noted that the oral compositions optionally comprise a plurality of different abrasive species and are not limited to the first and second abrasives only.

Among the other parameters that are also useful for categorizing the abrasivity of the particles are included, for example, hardness. The hardness can be expressed by several different tests known to those skilled in the art, including the hardness tests of Einlehner, Knoop, Vickers and Rockwell, as well as the Mohs hardness scale. A particularly useful method for evaluating abrasive particles is the hardness value of Einlehner. The hardness value of Einlehner is obtained using an Einlehner At-1000 abrasion instrument to measure the softness of the abrasive particle as follows: a Fourdrinier bronze wire sieve is weighed and exposed to the action of a suspension of the abrasive (for example, a 10% aqueous suspension of the abrasive) for a certain number of revolutions. The hardness value is expressed as milligrams of weight lost from the Fourdrinier wire sieve per 100,000 revolutions. Thus, in certain embodiments, the oral composition comprises a first abrasive having a hardness of Einlehner greater than about 5 mg of loss per 100,000 revolutions and a second abrasive having an Einlehner hardness of less than about 5 mg of loss per 100,000 revolutions. In certain embodiments, the first abrasive has an Einlehner hardness greater than about 10 mg loss per 100,000 revolutions and a second abrasive having an Einlehner hardness less than about 10 mg loss per 100,000 revolutions.

When the first particle has a hardness of Einlehner superior to 5 mg of loss per 100,000 revolutions, can exert a function mainly of polishing when it comes in contact with an oral surface. When the second particle has a hardness of Einlehner less than about 5 mg of loss per 100,000 revolutions, it can exert a function mainly of cleaning, since it is a softer particle. In certain embodiments, the second particle has a hardness greater than about 10 mg of loss per 100,000 revolutions, and in other embodiments, greater than about 15 mg of loss per 100,000 revolutions.

In certain embodiments, the first abrasive is a cleaning abrasive having a hardness less than or equal to that of the oral surface to be treated, and the second abrasive is an abrasive for polishing that has a hardness greater than or equal to that of the oral surface that will be treated.

The structure of an abrasive particle can also reflect abrasiveness; a relatively low structure tends to have a higher abrasiveness and a relatively high structure abrasive tends to have a lower abrasiveness. The structure of the particles may be indicated by the absorption of linseed oil or dibutyl phthalate (DBP) every 100 grams. The oil absorption values can be measured using the rubbing method ASTM D281.

In certain embodiments, the first abrasive has an oil absorption structure of less than about 90 cm3 / 100 g, and the second abrasive has an oil absorption structure of greater than about 90 cm3 / 100 g. In various embodiments, a particle of the first abrasive has an absorption structure of less than about 80 cm3 / 100 g, less than about 70 cm3 / 100 g, or less than about 60 cm3 / 100 g. In various embodiments, a particle of the second abrasive has an oil absorption greater than about 100 cm3 / 100 g, or greater than about 110 cm3 / l00 g.

The particle size can be an indicator of the cleaning and / or polishing efficiency of an abrasive. In certain embodiments, the first abrasive has a first particle size, and the second abrasive has a second particle size. In certain embodiments, the first particle size is smaller than the second particle size. The average particle size can be measured by a particle size analyzer Malvern, Model Mastersizer S, Malvern Instruments, Inc. (Southborough, Massachusetts, United States). A neon-helium gas laser beam is projected through a transparent cell containing the abrasive suspended in an aqueous solution. The light rays that impinge on the particles are scattered at angles that are inversely proportional to the particle size. The photodetector array measures the amount of light at various predetermined angles. The electric signals proportional to the light flux values measured by a microcomputation system are then processed with respect to a predicted dispersion pattern from theoretical particles, as defined by the refractive indexes of the sample and the aqueous dispersant for determine the particle size distribution of the abrasive subject.

In various embodiments, the first abrasive has an average particle size of less than about 11 μm, or less than about 10 μm. For example, Examples of suitable abrasives have an average particle size of about 7 μm to 11 μm. Some abrasives have particle sizes less than about 5 μm. In various embodiments, the second abrasive has an average particle size greater than about 8 μm, or greater than about 10 μm. In some embodiments, the second abrasive may have an average particle size of about 8 μm to about 14 μm.

In certain embodiments, the composition is safe for oral use in humans or other animals, and any orally and cosmetic suitable abrasive that meets the above requirements can be selected for an oral composition. Suitable abrasives include, without limitation: silica, silicate, silicone, alumina (including calcined aluminum oxide), aluminosilicates, such as bentonite, zeolite, kaolin, and mica, siliceous or diatomaceous earth, pumice, calcium carbonate, bone cuticular, insoluble phosphates, composite resins, such as melamine resin, phenolic resin, and urea-formaldehyde resin, polycarbonate, silicon carbide, boron carbide, microcrystalline wax, microcrystalline cellulose, including combinations of colloidal microcrystalline cellulose and carboxymethylcellulose, available in the trade under the trade name AVICEL® of FMC Biopolymer (Philadelphia, Pennsylvania, United States) and its combinations and derivatives.

As used herein, "mica" refers to any of a group of hydrated aluminum silicate minerals with plaque morphology and perfect basal excision. (micaceous) The mica can be, for example, mica in layers, mica in pieces or mica in flakes, as exemplified by micas of the muscovite, biotite or phlogopite type. Among the insoluble phosphates useful as abrasives include orthophosphates, polymetaphosphates and pyrophosphates. Illustrative examples include dicalcium orthophosphate dihydrate, dicalcium phosphate dihydrate, calcium hydrogen phosphate, calcium pyrophosphate, calcium β-pyrophosphate, tricalcium phosphate, calcium metaphosphate, potassium metaphosphate, and sodium metaphosphate.

Synthetic silicas include silica gels and precipitated silicas which are prepared by neutralization of aqueous silicate solutions with a strong mineral acid. In the preparation of silica gel, a silica hydrogel is formed which is then generally washed to reduce the salt content. The washed hydrogel can be milled to the desired size, or otherwise dried, finally to the point where the structure no longer changes as a result of size reduction. When such synthetic silicas are prepared, the objective is to obtain abrasives that provide maximum cleaning (ie, removal of stained film) with minimal damage to tooth enamel and other oral tissues.

Abrasives comprising silica are particularly useful in certain embodiments of the present invention. There has been significant difficulty in the past in the use of a silica-based abrasive with high concentrations within an oral composition, due to chemical and physical instability in the oral composition when provided in high concentrations, issues of mouthfeel, and excessive abrasive quality reflected by high RDA values. However, silica is a particularly attractive option as an abrasive, and cleans and / or effectively polishes oral surfaces. In addition, it is relatively inert and compatible with other ingredients in the oral composition and is relatively inexpensive. Accordingly, in certain embodiments of the present invention, the first and second abrasives comprise silica each. In some embodiments, the first abrasive is selected from a smaller and harder abrasive, eg, a better cleaning and / or polishing abrasive, and the second abrasive is a typical cleaning abrasive. In certain embodiments, the oral compositions may comprise a particularly effective combination of abrasive particle species.

Abrasive materials useful for preparing oral compositions include high cleaning, low structure silica abrasives, such as those marketed under the trade name SYLODENT® X A or SYLODENT® 783 from Davison Chemical Division of W. R. Grace & Co. (Balti ore, Maryland, United States). SYLODENT® XWA 650 is a silica hydrogel composed of colloidal silica particles.

Examples of silica hydrogels comprise colloidal silica particles with an average particle size, in various embodiments, from about 3 μm to about 12 μm, or about 5 μm to about 10 μm, with a pH from about 4 to about 10, or about 6 to about 9 measured as 5% by weight of slurry. The XWA 650 particles contain about 10% to about 35% by weight of water, have an average particle size of about 5 μm to about 12 μm, an Einlehner hardness greater than or equal to about 5 to about 20 mg of loss per 100,000 revolutions, an oil absorption of less than about 90 cm 3/100 g, for example between about 40 cm 3/100 g and about 90 cm 3/100 g. The abrasives have a surface area of Brunauer, Emmett and Teller (BET) of about 100 to about 700 m2 / g. XWA 650 has a brightness of 96.8 of tecnidina. Said abrasives are discussed in U.S. Patent No. 6,290,933 to Durga et al.

Another useful high cleaning abrasive is sold as SYLODENT® XWA 300 and is a silica hydrogel containing about 10% to about 25% water by weight, wherein the average particle size is about 2 μm to about 4 μm. The particles have a BET surface in the range of 150 to 400 m2 / g of silica. The abrasive XWA 300 has an oil absorption lower than 90 cm3 / 100 g of silica; and a pH, in a suspension 5% w / w in boiled water (without C02) demineralized, equal to or greater than 8.5. Said abrasives are analyzed, for example, in U.S. Patent No. 5,939,051 to Santalucia et al.

In other embodiments, a high-cleaning silica for the present invention comprises a silica product, wherein the particles are from about 5% to about 35% by weight of water, with an average particle size of from about 7 μm to about 11 μm. , a hardness of Einlehner of about 12 to about 19 and an oil absorption value of about 50 cm3 / 100 g to about 65 cm3 / 100 g. A BET surface is from about 100 to about 700 m2 / g of silica. A brightness greater than about 95 is generally reported tecnidina. Said silica product is commercially available as ZEODENT® 105 from J. M. Huber (Havre de Grace, Maryland, United States).

Other useful abrasives include typical silica cleaning abrasives, such as precipitated silicas with an average particle size of up to about 20 μm, generally at about 8 to about 14 μm, with an oil absorption structure of greater than about 90 to about 110. cm3 / l00 g; for example, ZEODENT®115, commercialized by J. M. Huber, with a pH of 5% of the particles of approximately 6.5-7.5 and a hardness of Einlehner of approximately 2 to 4 mg of loss per 100,000 revolutions. The gloss of said silica particle is greater than about 95. In certain embodiments, said cleaning abrasives comprise the second abrasive of the oral composition.

In certain embodiments, the oral composition is in the form of a dentifrice that is a clear or transparent gel. There, a colloidal silica abrasive, such as those sold under the trademark SYLOID® as SYLOID® 72 and SYLOID® 74 or under the trademark SANTOCEL® 100 as alkali metal alumina silicate complexes, may be particularly useful, since These abrasives have refractive indices close to refractive indexes of gel-liquid agent systems (including water and / or humectant) commonly used in dentifrices.

In various embodiments, a first and a second abrasive are combined in an oral composition to provide unexpectedly superior cleaning performance, unanticipated softness (relatively low abrasiveness), and aesthetically acceptable oral care compositions. In various embodiments, the ratio of the first abrasive to the second abrasive is from about 1: 1.6 to about 1.6: 1. For example, in certain embodiments, a ratio of the first abrasive to the second abrasive is approximately 1: 1. In certain embodiments, the respective amount of the first abrasive and the second abrasive present in an oral composition are about 13 to about 21% by weight of the oral composition. In some embodiments, the amount of the first abrasive is about 15% to about 19%, and the amount of the second abrasive is about 15% to about 19% by weight of the oral composition. In certain embodiments, the first abrasive is present at approximately 17% by weight and the second abrasive is present at approximately 17% by weight of the oral composition. In various embodiments, the total amount of the abrasive, including the first and second abrasives, is greater than about 25%, greater than about 30%, or greater than about 35% by weight of the oral composition.

In some embodiments, an oral composition comprises a first abrasive having an Einlehner hardness greater than about 5 mg loss per 100,000 revolutions and a second abrasive having an Einlehner hardness less than about 5 mg loss per 100,000 revolutions. In addition, the oral composition has a PCR of greater than about 100 and an RDA of less than about 200. In certain embodiments, the RDA is less than about 175.

In certain embodiments, the first abrasive has an oil absorption of less than about 90 cm3 / 100 g, and the second abrasive has an oil absorption greater than about 90 cm3 / 100 g. In certain embodiments, the total amount of the abrasives is greater than about 30%. In various embodiments, the first abrasive and the second abrasive are present in amounts of about 13% to about 21%, about 15% to about 19%, or about 17% each by weight of the total composition. In various embodiments, the first and second abrasives optionally comprise silica.

In certain embodiments, an oral composition comprises a first abrasive comprising silica, having an Einlehner hardness of greater than about 5 mg of loss per 100,000 revolutions, and an oil absorption of less than about 90 cm3 / l00 g; and a second abrasive comprising silica having an Einlehner hardness less than about 5 mg loss per 100,000 revolutions, and an oil absorption greater than about 90 cm 3/100 g.

The oral composition also comprises a second abrasive comprising silica and having an oil absorption greater than about 90 cm3 / 100 g and an Einlehner hardness of less than about 5 mg of loss per 100,000 revolutions.

In other embodiments, methods are provided for increasing the provision of an active ingredient in an oral composition on an oral surface. In various embodiments, the method comprises introducing an oral composition into an oral cavity containing the oral surface, wherein the oral composition comprises the active ingredient, a first abrasive and a second abrasive. In certain embodiments, the first and second abrasives each comprise silica and each is present in an amount of about 13% to about 21% by weight. The oral composition has a PCR greater than about 100 and one RDA less than about 200. The oral composition is contacted with the oral surface. Unexpectedly it has been found that the supply of the active ingredient is greater for this oral composition, when compared to a comparative composition having an abrasive comprising silica but having a PCR of less than about 100, as will be discussed in more detail below.

In particular embodiments, the active ingredient comprises a non-ionic antibacterial ingredient, for example a halogenated diphenyl ether such as triclosan, which will be discussed in more detail below. In some embodiments, the first abrasive has an oil absorption of less than about 90 cm 3/100 g and an Einlehner hardness greater than about 5 mg of loss per 100,000 revolutions, and the second abrasive has an oil absorption greater than about 90 cm 3 / l00 g and a hardness of Einlehner less than about 5 mg loss per 100,000 revolutions. In addition, the oral composition may comprise an efficacy enhancing copolymer, such as, for example, a copolymer of polyvinyl methylether and maleic anhydride, such as the commercially available GANTREZ® products sold by ISP Corporation of Wayne, NJ, and / or a anticaries active agent, which will be analyzed in more detail below.

The oral compositions may also comprise an orally acceptable carrier. The conventional ingredients that can be used to form the carriers of oral care compositions are known to the person skilled in the art. The specific composition of the carrier depends on the intended use of the composition. The carrier can be a liquid phase, semi-solid, or solid. The oral compositions may be in the form of a dentifrice (including toothpastes, tooth powders, and preventative pastes), confections (including gums, beads, and chew), film, paint gels, or any other form known to those skilled in the art. art when abrasives are used. The selection of specific carrier components depends on the form of the product of interest.

In certain embodiments, the oral composition is in the form of a dentifrice and the exemplary carrier is substantially semisolid or solid. The carrier can be aqueous, that is, it can comprise from about 5% to about 95% water. In other embodiments, the carrier is substantially non-aqueous. The carrier optionally comprises, for example, active ingredients for oral care, surfactants such as surfactants, emulsifiers and foam modulators, viscosity modifiers and thickeners, humectants, diluents, fillers, additional pH modifying agents, colorants, preservatives, solvents, and combinations thereof. It is understood that, while the general attributes of each of the above categories of materials may differ, there are some common attributes and any given material may serve multiple purposes within two or more of these material categories. As will be recognized by one skilled in the art, oral compositions optionally include other materials in addition to those components previously described, including for example, emollients, humidifiers, oral-feel agents, and the like. Examples of suitable carriers for oral compositions are discussed in U.S. Patent Nos. 6,669,929 to Boyd et al., 6,379,654 to Gebreselassie et al., And 4,894,220 to Nabi et al.

Active ingredients for oral care include, for example, antibacterial active agents, anticalculus agents, anti-caries agents, anti-inflammatory agents, anti-sensitizing agents, enzymes, nutrients, and the like. Useful assets herein are optionally present in the compositions of the present invention in safe and effective amounts which are sufficient to have the desired therapeutic or preventive effect in the human or an animal subject lower than that which the active agent is administered, without side effects undue adverse effects (such as toxicity, irritation or allergic response), in proportion to a reasonable risk / benefit ratio when used in the manner according to the invention. The specific safe and effective amount of the active agent will vary with factors such as the condition being treated, the physical condition of the subject, the nature of the concurrent therapy (if any), the specific active agent used, the specific dosage form, the carrier employee and the desired dosage regimen. Active ingredients useful for treating such conditions include those discussed in U.S. Patent Publication 2003/0206874 to Doyle et al. Active ingredients among those of use herein are also discussed in U.S. Patent 6,290,933 to Durga et al. And U.S. Patent 6,685,921 to Lawlor.

Any suitable fluoride ion source may be present in the oral composition, such as those discussed in U.S. Patent No. 5,080,887 to Gaffar et al. Sources of fluoride ions, acid phosphatases and inhibitors of the pyrophosphatase enzyme are well known in the art as anticaries agents. A fluoride ion source can be slightly soluble in water or can be completely soluble in water. It is characterized by its ability to release fluoride ions in water and by the freedom from unwanted reaction with other compounds in the oral preparation. Examples of such sources are salts and inorganic metal compounds and / or ammonium fluoride such as, for example: sodium fluoride, potassium fluoride, ammonium fluoride, calcium fluoride; a copper fluoride, such as cuprous fluoride; zinc fluoride, barium fluoride; sodium fluorosilicate, ammonium fluorosilicate, sodium fluorozirconate; and sodium monofluorophosphate, aluminum mono- and di-fluorophosphate and fluorinated calcium and sodium pyrophosphate. The fluoride source can also be an amine fluoride such as olaflur (N '-octadecyltrimethylenediamine-N, N, N' -tris (2-ethanol) -dihydrofluoride).

The amount of source that provides fluoride depends in a certain way on the type of source, its solubility and the oral type or preparation, but will be present in a non-toxic amount, generally from about 0.001% to about 3.0% in the preparation. In a toothpaste preparation, for example, dental gel, toothpaste (including cream), dental powder or dental tablet, an amount of that source which releases up to about 5,000 ppm of F-ion by weight of the preparation is considered satisfactory. Any appropriate minimum amount can be used from that source, but in various embodiments an amount is sufficient to release about 300 to 2,000 ppm, about 500 to about 1,800 ppm or about 800 to about 1,500 ppm of fluoride ion.

The oral composition optionally comprises an anti-tartar composition such as, for example, one or more of the anti-tartar compositions mentioned in U.S. Patent No. 5,292,526 to Gaffar, et al. In certain embodiments, the anti-tartar composition includes one or more polyphosphates. The anti-tartar composition may include at least one total or partially neutralized alkali metal or ammonium tripolyphosphate or hexametaphosphate salt present in the oral composition in an effective anti-tartar amount. The anti-tartar active agent may also include at least one soluble, linear molecularly dehydrated polyphosphate salt, effective in an anti-tartar amount. The anti-tartar active agent may also include a mixture of potassium and sodium salts, at least one which is present in an anti-tartar effective amount as a polyphosphate tartaric acid agent. The anti-tartar active agent may also contain an effective anti-tartar amount of an effective molecularly anti-tartar polyphosphate salt tartar present in a mixture of sodium and potassium salts. The ratio of potassium to sodium in the composition can be up to less than 3: 1. The polyphosphate may be present in the oral composition in various amounts, such as an amount wherein the weight ratio of polyphosphate ion to antibacterial agent varies from an excess of 0.72: 1 to less than 4: 1, or where the weight ratio of agent antibacterial enhancer to polyphosphate ion ranges from about 1: 6 to about 2.7: 1, or wherein the weight ratio of the antibacterial enhancer to polyphosphate varies from about 1: 6 to about 2.7: 1. Other useful anti-tartar agents include polycarboxylate polymers and polyvinylmethyl ether / maleic anhydride copolymers (PVM / MA), such as GANTREZ®.

Another active agent useful in toothpaste compositions of the present invention are antibacterial agents that are present in amounts of about 0.001 to about 3.0% by weight of the oral composition. A non-limiting list of additional compounds for oral care includes nonionic antibacterial agents, including phenolic and bisphenolic compounds, such as halogenated diphenylethers, including triclosan (2,4,4'-trichloro-2'-hydroxy diphenylether, triclocarban (3 , 4, 4-trichlorocarbanilide), as well as 2-phenoxyethanol, esters of benzoate and carbanilides. A halogenated diphenyl ether, such as triclosan, may be present in an amount of about 0.3% by weight of the oral composition, for example.

Suitable surfactants are those that are reasonably stable over a wide pH range. These compounds are known in the art, and include non-detergent soapy anionic (for example, sodium lauryl sulfate (SLS), N-myristoyl and N-palmitoyl sarcosine), non-ionic (for example, Polysorbate 20 (polyoxyethylene 20 sorbitan monolaurate, TWEEN 20) and Polysorbate 80 (polyoxyethylene 20 sorbitan monooleate, ® TWEEN 80), Poloxamer 407, available under the trademark PLURONICF F127 from BASF, Florham Park, New Jersey, United States), cationic, suteionic (for example, cocamidopropylbetaine and lauramidopropylbetaine) and amphoteric organic synthetics. Examples of suitable active agents for use in oral compositions are discussed in, for example, U.S. Patent Nos. 4,894,220 to Nabi et al., 6,555,094 to Glandorf et al., And 6,706,256 to Lawlor, among others. In certain embodiments, one or more surfactant agents are present in the oral composition of the present invention in the range of about 0.001% to about 5%, or from about 0.5% to about 2.5%.

Optional thickeners for use in oral compositions include natural and synthetic gums and colloids, such as carrageenan (Irish moss), xanthan gum, sodium carboxymethylcellulose, starch, polyvinylpyrrolidone, hydroxyethylpropylcellulose, hydroxybutylmethylcellulose, hydroxypropylmethylcellulose and hydroxyethylcellulose. Inorganic thickeners include amorphous silica compounds that work as thickening agents and include colloidal silica compounds available under the trademarks such as Cape-sil fumed silica manufactured by Cabot Corporation and distributed by Lenape Chemical (Bound Brook, N. J, United States); ZEODENT® 165 by JM Huber Chemicals, and Sylox 15, also known as SYLODENT® 15, available from Davison Chemical Division of WR Grace Corp. In certain embodiments, the thickening agent is present in the dentifrice composition in amounts of about 0.1 to about 10% by weight, or from about 0.5 to about 4% by weight.

The orally acceptable carrier vehicle used to prepare the dentifrice composition optionally comprises a humectant. The humectant may be glycerin, sorbitol and xylitol, propylene glycol of a molecular weight in the range of about 200 to about 1,000; or other moisturizers and mixtures of them. The concentration of the humectant typically totals approx. the 5 to approx. 70% by weight of the oral composition. Water is typically present in an amount of at least about 10% by weight, and in general about 25 to 70% by weight of the oral composition.

The synthetic anionic linear polycarboxylates are effective enhancing agents for optional use in oral compositions having certain active ingredients, including antibacterial active agents, anticalculus or other active agents in the oral composition. Such anionic polycarboxylates are generally used in the form of their free acids or water-soluble alkali metal salts totally or partially neutralized (eg, potassium and preferably sodium) or ammonium salts. The "synthetic" and "linear" concepts do not include known thickeners or gelling agents comprising carboxymethylcellulose and other cellulose derivatives and natural gums, nor carbopoles with reduced solubility due to cross-links.

The copolymers are preferably 1: 4 to 4: 1 copolymers of maleic anhydride or maleic acid with another unsaturated monomer which can be polymerized with ethylene, preferably methyl vinyl ether (methoxylene) having a molecular weight (P.M.) from about 30,000 to about 1,000,000. A useful copolymer is methyl vinyl ether / maleic anhydride. Examples of these copolymers of ISP Corporation can be obtained under the trade name GANTREZ®, p. ex. , AN 139 (P.M. 1,100,000), AN 119 (P.M. 200,000); S-97 Pharmaceutical Grade (P.M. 1,500,000), AN 169 (P.M. 2,000,000), and AN 179 (P.M. 2,400,000); wherein the preferred copolymer is S-97 Pharmaceutical Grade (P.M. 1,500,000). When it exists, the anionic polycarboxylate is used in effective amounts to achieve the desired increase in the efficacy of any active antibacterial, antibacterial agent or other active agent included in the composition of the dentifrice. In different embodiments, a synthetic anionic polycarboxylate is included in the oral composition at about 0.001 to about 5%, or about 0.1 to about 2.0% of the oral composition.

The oral composition of the present invention can be prepared by any of the methods known in the art to combine ingredients to produce compositions for oral care. Examples of these methods that can be used are indicated on p. ex. , U.S. Patent No. 6,403,059 to Martin et al .; Clinical Pharmacology for Dental Professionals (Mosby-Year Book, Inc., 3rd ed., 1989); Mosby's Dental Hygiene: Concepts, Cases and Competencies, (Daniel, S. and Harfst, S. eds., Elsevier Science Health Science Div. 2002); and Ernest W. Flick, Cosmetic and Toiletry Formulations, 2nd ed.

The present invention provides methods and processes for using the oral compositions of the present invention to clean and / or polish oral surfaces. In addition, the oral compositions optionally treat and inhibit oral conditions, such as inflammatory conditions, dental plaque and dental plaque. Oral compositions can apply the individual in any way known in the art; for example, by introducing the oral composition into the oral cavity of the individual using a suitable applicator or delivery device, such as a brush, a dental strip, a sheet, syringe, tape, pill or any other known applicator or delivery device. in art. The compositions can be used in prophylactic methods and processes in order to help and maintain oral health, appearance, maintain systemic health, and the like. The oral compositions can be applied repeatedly to the individual for a number of days according to a particular treatment scheme to treat and / or inhibit the formation of spots, plaque, calculus or tartar. The instructions indicated in the treatment scheme may be supplied in the commercial package together with the product, in the manner offered and retained commercially.

The present invention is further illustrated through the following non-limiting examples.

EXAMPLE I A tooth composition according to the present invention, which presents the ingredients indicated for the DENTÍFRICO 1 in TABLE I is prepared according to the following method: sodium saccharin, sodium benzoate, sodium monofluorophosphate and any other salts are dispersed in water and mixed on a conventional stirrer under stirring. Moisturizers are added, p. ex. , glycerin and sorbitol, to the water mixture under agitation. Organic thickeners are added, such as sodium carboxymethylcellulose, carrageenan and some polymers, such as GANTREZ®.

The resulting mixture is stirred until a homogeneous gel phase is formed. The mixture is then transferred to a high speed vacuum mixer; in which the abrasives are added. The mixture is then stirred at high speed for 5 to 30 minutes, under a vacuum of about 20 to 50 mm Hg, preferably about 30 mmHg. Weigh the flavoring oil and then add triclosan to the flavoring oil. Flavoring oil and flavonoid are added to the mixture. Surfactants, such as sodium lauryl sulfate (SLS) are loaded into the mixer. The resulting product is a homogeneous, semi-solid, extrudable paste or gel product. The resulting dentifrice can be applied by a brush or other applicator on the oral surfaces.

The toothpastes A and B are comparative examples and are prepared in the same manner as described above for Toothpaste 1.

Table I EXAMPLE II The PCR and RDA data are shown in TABLE II for the toothpaste 1 prepared according to the present invention, in comparison with the toothpastes A and B.

The RDA is determined according to the method recommended by the American Dental Association as indicated by Hefferren, Journal of Dental Research, Volume 55, Issue 4, July-August 1976, p. 563-573, and is described in the Patents Americans No. 4,340,583, 4,420,312 and 4,421,527 all from Wason.

PCR, as described above, is an in vitro method used to measure the effectiveness of removing tea or coffee stains on teeth from a standard. The PCR values referred to herein were obtained from a modification of the method described in "In Vitro Removal of Stain with Dentifrice", G. K. Stookey, et al J. Dental Research, 61, 123-9 (1982). The modification of the PCR method used herein is described in U.S. Patent Nos. 5,658,553 and 5,651,958 both from Rice. In this modification a transparent film material is first applied to a bovine tooth, which is then dyed with a combination of film material and tea, coffee and FeCl3, where in the original method described by Stookey et al., Are applied both, the film and the spot simultaneously.

Table II Toothpaste B is a typical formulation of oral composition that has a combination of silica with high cleaning power (XWA 650) and silica of a regular cleaning power (ZEODENT® 115) in 10% by weight, respectively. The dentifrice B is the control with a PCR of approximately 85 and an RDA of 138. As can be seen, in toothpaste A, the silica with high cleaning power (XWA 650) is increased by 20% while the silica is removed of regular cleaning power (ZEODENT® 115). For toothpaste A, the RDA increases to 180, but the CRP only increases to approximately 98. In comparison, toothpaste 1 presents 17% of both, the high cleaning power silica (XWA 650) and the regular silica cleaning power (ZEODENT® 115), but the RDA is only 163, while the PCR is greater than 100 (around 108). Thus, the combination of abrasives in toothpaste 1 provides an unexpectedly low RDA (with an increase of only 18% compared to toothpaste B) while achieving a 27% increase in CRP compared to toothpaste B. In comparison, the toothpaste A shows an increase in RDA of more than 30% and an increase in CRP of only 15%, compared to dentifrice B.

It has been discovered, therefore, that the desired elevated PCR values for a composition can be achieved toothpaste, while the RDA values are significantly lower than expected.

EXAMPLE III An in vitro polishing analysis is performed with the dentifrice 1, dentifrice B, a dentifrice prepared according to TABLE III below and the toothpaste C indicated, and a whitening dentifrice obtainable in the market, designated dentifrice D. The dentifrice C is prepared in the same manner as described above for the dentifrice 1 in EXAMPLE I, and contains 20% by weight of the silica of regular cleaning power, ZEODENT® 115. The dentifrice D can be obtained commercially as CREST® bleached toothpaste Procter &Gamble dual action vaccine from Cincinnati, OH, and is believed to contain the ingredients sodium fluoride at 0.243%, glycerin, hydrated silica, water, sorbitol, sodium hexametaphosphate (for tartar control / spot prevention), propylene glycol, flavoring, PEG-12, cocamidopropyl betaine, SLS, CARBOMER® 956, sodium saccharin, Poloxamer 407, polyethylene oxide, xanthan gum, sodium hydroxide, cellulose gum, sodium hydroxide, titanium dioxide and dyes Blue 1 and Yellow 5.

Table III Table IV shows the polishing analysis of the in vitro medium of these dentifrices. The maximum brightness of the opaque dental surface is determined by means of a reflectometer specially adapted to detect changes in the degree of polish of the enamel surface. The reflectometer was constructed in such a way that the enamel is exposed to a polarized beam of light, and the amount of light reflected from the enamel surface is determined by a photoelectric cell, which in turn activates a galvanometer. The smoother the enamel surface, the smaller the diffusion and absorption of the light, and therefore, the higher the value read by the galvanometer.

After determining the maximum reflection of the opaque surface of the tooth, the tooth is brushed with the toothpaste to be evaluated. Then the enameled surface is rinsed with water to remove the residual particles of the cleaning and polishing agent, and the reflectance of the enameled surface is measured again, placing the tooth in exactly the same position as that used to perform the "opaque" reading. The absolute change in the amount of reflectance between the opaque enameled surface and the polished surface is considered as a measure of the degree of polishing obtained during the treatment. The total brushing period is around 30,000 movements. The results in TABLE IV are expressed in terms of the average increase in the gloss of the enamel types.

Toothpaste C is a conventional toothpaste that has 20% abrasive silica of regular cleaning power and is selected as the control to calculate the percentage increase in average brightness increase. It can be seen that the dentifrice 1 shows the greatest increase in average increase in polish.

TABLE IV EXAMPLE IV The average absorption of triclosan in a hydroxyapatite disk is indicated in TABLE V. The dentifrices 1, B, and C are compared with respect to the absorption levels of triclosan. Absorption of the active ingredient triclosan is ensured by using hydroxyapatite disks (HAP) which can be obtained from Clarkson Chromatography Products, Inc., which are coated with saliva (SCHAP), as an in vi tro model for human teeth. It was found that this in vitro model is correlated to the delivery and in vivo retention of antibacterial agents on oral surfaces.

In order to determine the delivery and retention of triclosan to a SCHAP disk from a dentifrice containing triclosan and an anionic copolymer of the present invention, ie the AMPS terpolymer and the VCAP copolymer, the SCHAP discs are treated with compositions of solution of dentifrice identified in TABLE I above. The amounts of toothpaste solution used to contact the discs simulate in vivo proportions of surface to volume that were found in the mouth, to partially stimulate the brushing condition. After incubation for 30 minutes at 37 ° C, the SCHAP disks were removed from the dentifrice solution and washed three times with water. The increase in absorption of triclosan on the SCHAP discs of dentifrices 1, B, and C are indicated in TABLE V, below.

Table V The results in TABLE V show that the supply and retention of triclosan in SCHAP discs of dentifrice 1 are substantially higher than in any of the comparative examples of dentifrices B and C. Thus, these compositions provide methods of a greater supply of an active ingredient in an oral composition to an oral surface.

EXAMPLE V Various samples (A-E) were prepared and tested in accordance with the present invention. Sample A represents silica that is not highly clean. Samples B-E represent various high-cleaning silica compositions. All were tested with an Einlehner Abrasive Analysis. The samples were dispersed at 10% w / v (100 g diluted to a volume of 1000 ml) and run in duplicate in an Einlehner AT 1000. The results are shown in Table 6 below: TABLE VI

Claims (27)

1. An oral composition comprising: a first abrasive that has a hardness of Einlehner greater than about 5 mg of loss per 100,000 revolutions; Y a second abrasive having an Einlehner hardness of less than about 5 mg of loss per 100,000 revolutions; wherein the ratio of the first abrasive to the second abrasive is from about 1: 1.6 to about 1.6: 1, and wherein the oral composition has a film removal ratio of greater than about 100 and an abrasion of the radioactive dentin of less than about 200. .

2. The composition as claimed in clause 1, characterized in that the abrasion of the radioactive dentin is less than about 175.

3. The composition as claimed in clause 1, characterized in that the first abrasive has a absorption oil less than about 90 cm3 / l00 g and the second abrasive has an absorption oil greater than about 90 cm3 / 100 g.

4. The composition as claimed in clause 1, characterized in that the first abrasive has an average particle size of less than about 11 μm and the second abrasive has an average particle size greater than about 8 μm.

5. The composition as claimed in clause 1, characterized in that the ratio of the first abrasive to the second abrasive is about 1: 1.

6. The composition as claimed in clause 5, characterized in that the first abrasive is present in an amount of about 17% by weight and the second abrasive is present in an amount of about 17% by weight in the oral composition.

7. The composition as claimed in clause 1, characterized in that a total amount of the first and second abrasives in the oral composition is greater than about 30% by weight of the composition.

8. The composition as claimed in clause 1, characterized in that the first abrasive is present in an amount of about 13% to about 21% by weight and the second abrasive is present in an amount of about 13% to about 21% by weight of the oral composition.

9. The composition as claimed in clause 1, characterized in that the first abrasive is present in an amount of about 15% to about 19% by weight and the second abrasive is present in an amount of about 15% to about 19% by weight of the oral composition.

10. The composition as claimed in clause 1, characterized in that the first abrasive and the second abrasive each comprise silica.

11. An oral composition comprising: a first abrasive comprising silica, having an Einlehner hardness of greater than about 5 mg of loss per 100,000 revolutions and an absorption oil of less than about 90 cm 3/100 g; Y a second abrasive comprising silica, having an Einlehner hardness less than about 5 mg loss per 100,000 revolutions and an absorption oil greater than about 90 cm 3/100 g; wherein the first abrasive is present in an amount of about 13% to about 21% by weight and the second abrasive is present in an amount of about 13% to about 21% by weight of the composition.

12. The composition as claimed in clause 11, characterized in that the first abrasive is present in an amount of about 15% to about 19% by weight and the second abrasive is present in an amount of about 15% to about 19% by weight of the oral composition.

13. The composition as claimed in clause 12, characterized in that the first abrasive is present in an amount of about 17% by weight and the second abrasive is present in an amount of about 17% by weight of the oral composition.

14. The composition as claimed in clause 11, characterized in that the oral composition has a film removal ratio of greater than about 100 and an abrasion of the radioactive dentin of less than about 200.

15. The composition as claimed in clause 14, characterized in that the abrasion of the radioactive dentin is less than about 175.

16. The composition as claimed in clause 11, characterized in that a total amount of the first and second abrasives in the oral composition is greater than about 30%.

17. The composition as claimed in clause 11, characterized in that the first abrasive has an average particle size of less than about 11 μm, and the second abrasive has an average particle size greater than about 8 μm.

18. An oral composition comprising: a first abrasive comprising silica and having an absorption oil of less than about 90 cm3 / 100 g and a hardness of Einlehner greater than about 5 mg loss per 100,000 revolutions; Y a second abrasive comprising silica and having an absorption oil of greater than about 90 cm 3/100 g and an Einlehner hardness of less than about 5 mg of loss per 100,000 revolutions; wherein a ratio of the first abrasive to the second abrasive is from about 1: 1.6 to about 1.6: 1, and a total amount of the first and second abrasives present in the oral composition is greater than about 25% by weight of the composition; and wherein the oral composition has a film removal ratio of greater than about 100 and an abrasion of the radioactive dentin of less than about 200.

19. The composition as claimed in clause 18, characterized in that the ratio of the first abrasive to the second abrasive is about 1: 1.

20. The composition as claimed in clause 18, characterized in that the first abrasive is present in an amount of about 17% by weight and the second abrasive is present in an amount of about 17% by weight in the oral composition.

21. A method for increasing the delivery of an active ingredient in an oral composition to an oral surface comprising: introducing an oral composition into an oral cavity, wherein the oral composition comprises the active ingredient, a first abrasive and a second abrasive, wherein the first and second abrasives each comprise silica and each is present in an amount of about 13% to about 21% by weight, wherein the oral composition has a film removal ratio of greater than about 100 and an abrasion of radioactive dentin of less than about 200; Y contacting the composition with the oral surface, wherein the supply of the active ingredient is greater than a comparative composition having an abrasive comprising silica and a film removal ratio of less than about 100.

22. The method as claimed in clause 21, characterized in that a proportion of the first abrasive to the second abrasive is from about 1: 1.6 to about 1.6: 1.

23. The method as claimed in clause 21, characterized in that the active ingredient comprises a halogenated diphenyl ether.

24. The method as claimed in clause 21, characterized in that a ratio of the first abrasive to the second abrasive is from about 1: 1.6 to about 1.6: 1.

25. The method as claimed in clause 21, characterized in that the first abrasive has an absorption oil of less than about 90 cm3 / 100 g and an Einlehner hardness greater than about 5 mg of loss per 100,000 revolutions, and the second abrasive has an absorption oil greater than about 90 cm3 / 100 g and an Einlehner hardness less than about 5 mg loss per 100,000 revolutions.

26. An oral composition comprising: a first abrasive having an Einlehner hardness greater than about 10 mg loss per 100,000 revolutions; Y one second . abrasive that has a hardness of Einlehner less than approximately 10 mg of loss per 100,000 revolutions; wherein the ratio of the first abrasive to the second abrasive is from about 1: 1.6 to about 1.6: 1, and wherein the oral composition has a film removal ratio greater than about 100 and an abrasion of the radioactive dentin less than about 200.

27. The oral composition as claimed in clause 21, characterized in that the composition further comprises a polycarboxylate polymer or polyvinylmethyl ether / maleic anhydride copolymer (PVM / MA).