Title:
Stand-alone or enhancer composition for oral care
Kind Code:
A1


Abstract:
A biological tissue care composition, such as an oral care composition, for enhancing the effects of whitening compositions. A solvent and surfactant is used with an alkaline builder and an optional saponifier. A method of use of such a composition includes use as a tooth cleaning composition. Alternatively the composition may be used as a stand-alone cleaning composition.



Inventors:
Giniger, Martin S. (New York, NY, US)
Application Number:
11/356316
Publication Date:
09/07/2006
Filing Date:
02/15/2006
Primary Class:
International Classes:
A61K8/46
View Patent Images:
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Primary Examiner:
ROBERTS, LEZAH
Attorney, Agent or Firm:
Peter B. Scull (Denver, CO, US)
Claims:
Accordingly, what is claimed is:

1. An enhancer composition for oral use in connection with a discrete tooth whitening composition, the enhancer composition comprising a solvent; an alkaline builder; and a dual surfactant system comprising a detergent and foaming/wetting agent.

2. The enhancer composition of claim 1, wherein the solvent is a primary cleaning solvent selected from one of more of ethanol and water.

3. The activation composition of claim 1 wherein the alkaline builder is potassium hydroxide.

4. The activation composition of claim 1, wherein the detergent is sodium lauryl sulfate.

5. The activation composition of claim 1, wherein the foaming/wetting surfactant is Pluronic F68.

6. The activation composition of claim 1, wherein a pH measure of the enhancer composition is approximately 9.0.

7. The activation composition of claim 1 further comprising an acid compound to reduce a pH measure of the activation composition to one or both of an effective and biologically compatible level.

8. The activation compound of claim 7, wherein the acid compound comprises tartaric acid.

9. The enhancer composition of claim 1 further comprising a saponifier.

10. The enhancer composition of claim 9, wherein the saponifier is one or both of potassium hydroxide or sodium citrate.

11. The enhancer composition of claim 1 further comprising a chelator.

12. The enhancer composition of claim 11, wherein the chelator is disodium EDTA.

13. The enhancer composition of claim 1, further comprising an oxidizing agent.

14. The enhancer composition of claim 13, wherein the oxidizing agent is hydrogen peroxide.

15. The enhancer composition of claim 13, wherein the concentration of the hydrogen peroxide is one or both of no more than about 5% and less than about 2%.

16. The enhancer composition of claim 1, wherein the enhancer composition is a non-viscous liquid with viscosity below 5.0 cps.

17. The enhancer composition of claim 1 further comprising any one or more of the following ingredients: an antibacterial agent, ethanol, menthol, eucalyptol, thiamine, methyl salicylate, cetylpyridium chloride, calcium nitrate, fluoride, zinc chloride, potassium nitrate, aloe, carnauba wax, sanguinaria extract, papain, sodium laurel sulfate, a coloring agent, sodium saccharin, sodium citrate, carbamide peroxide, calcium peroxide, glyceryl peroxide, benzoyl peroxide, peppermint oil, cinnamon oil, an acid compound, a stain removing agent, a gelling agent, and a flavoring agent.

18. The enhancer composition of claim 1, wherein other ingredients may be added so that the enhancer composition is adapted to become incorporated into one or more of the following other oral compositions: toothpastes, dual phase dentifrices, mouth rinses, topical fluoride compositions, tooth sealants, cosmetic dental bonding agents, acid etchants, dental prophylaxis pastes, stand alone whitening compositions, dual component whitening compositions, triple component tooth whitening systems four component tooth whitening systems, peroxide-free whitening systems, light activated whitening systems, chairside whitening systems, custom tray whitening compositions, paint-on whiteners, whitening strips, whitening pens, whitening compositions contained with in crushable ampoules, oral hydrogel delivery systems, denture cleaners, periodontal therapies, or powered dentifrice delivery systems including one or more of non-viscous liquids, thickened liquids, gels, pastes or solid forms.

19. A method of use of an enhancer composition of claim 1, comprising: delivering the enhancer composition onto a tooth surface with one of a cotton-tipped or foam-tipped swab.

20. A method of use according to claim 19 wherein the cotton-tipped or foam-tipped swab is adapted to be operable with or as part of a swab tube dispenser.

21. A skin whitening composition wherein the active ingredients include one or more of a solvent; an alkaline builder; and a dual surfactant system comprising a detergent and foaming/wetting agent.

Description:

BACKGROUND

The present invention relates to improvements in biological care compositions, and more particularly relates to a composition for enhancing the effects of tooth whitening compositions.

Many oral care tooth whitening compositions, and their associated methods of delivery, have been described and commercialized, yet numerous significant issues remain. Limitations of current art whitening compositions include: (1) reliance on a single dominant mechanism of action, involving decomposition of a strong oxidizer, that only inefficiently lightens one class of stains over relatively long treatment times; (2) a limited ability to physically remove stain molecules, especially deep seated ones; (3) a propensity to have high osmotic pressures which lead to tooth dehydration and subsequent inducement of transient dentinal hypersensitivity; and (4) almost universal reliance on carbomer-like thickener carrier vehicles that scavenge some active free radicals and limit surface penetration ability.

Prior art in other aspects of dentistry have shown that penetration ability is a major aspect of creating efficacy. Prior art has shown that active ingredients such as fluoride or triclosan (an anti-gingivitis agent), work best with enhanced ability to penetrate between teeth, or into the nooks and crannies on/of teeth, to provide their benefits to those oral features. Tooth whitening compositions also optimally require high penetration ability to reach and treat deep-seated tooth stains that have typically accumulated over many years.

The structure of enamel adds to the difficulty of treating tooth stains, because of its tightly packed crystalline structure and the high amount of electronegativity that is caused by incorporated enamel fluoride ions. Negatively charged teeth have a propensity to attract cationic stain molecules which unfortunately are also the most likely types of stain molecules to be colored and unaesthetic. Furthermore the enamel structure of a tooth is dense, but porous, in a deeply striated manner. Tightly packed enamel rods are arranged in a roughly parallel configuration, and over time, staining agents and discoloring substances permeate between the enamel rods and discolor the tooth, sometimes all the way through to the dentin. As the stains penetrate deeper into the enamel, between the densely packed rods, the activity of whitening compositions become increasingly reliant on carrier vehicle surface tensions and the ability of the active to penetrate into the enamel. Thus depth of tooth stains, in combination with electrostatic charges that further bind stains, make the challenge of efficiently and reliably whitening teeth even more difficult. The current art of whitening compositions rarely make mention of or address these issues.

A further limiting factor not well addressed in current art of oral care tooth whitening compositions is the lack of a multi-purpose active formulation strategy. This shortcoming ultimately causes current art whitening compositions to have unpredictable effectiveness, because they cannot lighten the broad spectrum of possible tooth stains that are present on teeth. The literature shows that there are many substances that have the ability to “stain” or reduce the “whiteness” of one's teeth including foods, medicines, job-related chemicals, air pollutants, food pigments, tobacco byproducts, and the like. These products can be organic or inorganic, hydrophilic, dry or oily. Oxidizer-reliant tooth whitening compositions are mostly limited to the lightening of some organic stains, and do not account very well for the other classes of stains.

The current art has also not overcome long treatment times that remain an unavoidable issue when oral compositions primarily rely on oxidizer chemistry. This is because the fundamental requirement for compositions that lighten teeth with oxidizing agents is prolonged contact time and the number of exposure cycles. To overcome this limitation formulations have opted for high concentrations of caustic oxidizers which further has the potential to cause tooth sensitivity. For maximum whitening, a long treatment time with a highly concentrated bleaching composition has generally been recommended.

Furthermore, a review of the current art shows a common reliance on moderately or highly viscous carrier, further limiting efficacy, and further enhancing susceptibility to tooth sensitivity. Carbomers such as carbopol and similar polymeric, carbon-based thickeners are almost universally chosen for tooth whitening compositions because: (1) they can enhance substantivity of the active within the wet oral environment; (2) they are generally regarded as safe; (3) they have very familiar and flexible chemical properties making compositions easier to formulate; and (4) because their adhesiveness and rheology are needed to help contain caustic peroxygen actives to the enamel surface. However use of thickening agents also causes unintended, undesirable effects on the safety and efficacy. This is because: 1) thickness, in general, causes high surface tensions and low wetting ability that prevents penetration of the active to reach deep seated stains; 2) thickness and density, in general, causes the osmotic pressure to be shifted such that the carrier gels tend to dehydrate the tooth, causing odontoblast cell processes to be drawn into dentinal tubules, further contributing to tooth sensitivity; and, 3) they have carbon bonded atomic structure that is somewhat similar in structure to stain molecules with high omnipresence and proximity to the oxidizer actives causing the scavenging of active free radicals, and further reducing efficacy.

Thus it is clear that these extant methods are not efficient, not rapid acting, not free of significant untoward side effects and are not able to truly clean teeth. This suggests that any new oral care composition that has a chemical formulation, that can enhance all other oral care whitening compositions so that they do not solely rely on or require strong oxidizers for activity, and works so rapidly and safely that thickened carrier vehicles are not required and as a result: (1) reduces the time required to achieve satisfactory efficacy levels; (2) increases patient comfort; (3) achieves more complete and longer lasting stain removal and (4) works via multiple chemical mechanisms to increase the reliability of the treatment outcome, should be highly useful, novel and desirable.

SUMMARY OF THE INVENTION

Stand-alone and/or enhancer compositions are described here which may be used alone or which may be used prior to or concomitantly with any discrete whitening composition. The compositions may include in preferred embodiments: an alcoholic cleaning solvent, one or more or a combination of neutral and anionic surfactants, one or more alkaline builders and optional saponifiers, chelating agents, additional optional solvents, glossing agent(s) and/or oxidizing agent(s).

An advantage may be in that the compositions hereof are not reliant on oxidizing agents or carbomer-like thickeners. Tooth whitening is enhanced by the ability of the compositions to deeply penetrate and either thereby whiten or remove most tooth stains using a multi-functional solvent/surfactant/alkaline builder approach known in prior art to the textile and related industries, but heretofore not applied in dentistry. As a result of this multi-factorial and true whitening and/or cleaning approach, the compositions hereof may have the ability to cause deeper, much more rapid and true whitening and/or removal of a majority of organic, inorganic, hydrophobic and/or hydrophilic tooth stains, rather than slowly lightening merely some organic stains. A further improvement may be a reduction in associated transient dentinal hypersensitivity. These may be achieved by shifting the mechanism of action away from caustic and slow acting oxidizing agents, and furthermore utilizing a non-viscous carrier instead of associated carbomer-thickened carrier matrices. A cleaning chemistry that may provide one or more of a superior whitening result in less time, and/or a virtual elimination of associated transient dentinal hypersensitivity, may thus be achieved.

In a preferred embodiment, the enhancing composition may contain a combination of ingredients that may work together to rapidly remove unwanted tooth stains. The enhancing composition may also include certain ingredients that may boost the effectiveness of discrete whitening gel oxidizing agents. The current composition ingredients may also prevent tooth dehydration. Low concentration saponifiers, peroxygens, and chelating agents may optionally be, but preferably are added to further round out the multi-factorial cleaning strategy, although in no way are they a necessity. These ingredients may help with some oily stains, prevent free calcium ions from inhibiting the anionic detergents, and may help to lighten any organic stain molecules that may have been resistant to the chemical cleaning strategy employed by multi-factorial cleaning mechanisms of the present invention.

The stand-alone and/or enhancing compositions may be non-viscous, liquid compositions, with viscosity typically under 5.0 cps. Using one preferred method of application, the enhancer liquid may be applied to the facial surfaces of the dentition, just before the application of any discrete whitening compound. This may be preferably done by using a specially designed, mildly abrasive, highly absorbent, foam-tipped swab tube container/applicator described in a simultaneously-filed U.S. patent application Ser. No. ______, filed Feb. 15, 2006, entitled APPLICATION AND/OR CARRYING DEVICES FOR ORAL CARE COMPOSITIONS, attorney docket number 281-006-USP. In another embodiment these compositions could be in the form of a mouth rinse, swished forcefully around all teeth for twenty seconds by the user to coat tooth surfaces and to help loosen tooth plaque and debris. In still another embodiment, the tooth cleaning liquid could be incorporated into a prophylaxis or prophy paste used for cleaning teeth by a dental professional just prior to a professional tooth whitening treatment or even as a stand-alone whitening treatment. In yet another embodiment a tooth cleaner composition hereof may be easily added into a dentifrice causing that dentifrice to have superior tooth whitening ability and may be especially useful when brushed onto teeth just prior to application of a whitening strip, a paint-on whitening gel or an at-home bleaching composition contained with a custom tray. Furthermore, an enhancer composition hereof may be applied in series or in parallel with the discrete whitener composition it may be intended to enhance.

The whitening effect that may be delivered rapidly and safely by the stand-alone or enhancer solution may be caused by a combination of ingredients designed to work together to remove many if not all species of extrinsic and intrinsic tooth stains. As such it may utilize a variety of different classes of solvents, surfactants and alkaline builders and other ingredients: as for example, 1) a solvent, particularly a highly pure, residue-free dissolving solvent such as HPLC grade de-ionized water; 2) an orally acceptable cleaning alcoholic solvent, that may assist penetration and may have the ability to dissolve most stains and break up thickened gels; 3) an orally acceptable anionic surfactant or detergent that may bind most cationic colored stains found on teeth; 4) an alternative surfactant or surface wetting and high foaming agent to allow deep penetration and foaming-lifting of loosened stains; 5) an alkaline builder that may assist the surfactant/detergent to bind stains and also may work to help cause decomposition of any oxidizers, if used; and 6) an optional saponifier to bind and dissolve hydrophobic oily stains.

Good stain cleaning and/or enhancing whitening solutions hereof may have complex and/or varied activities as shown in FIGS. 1 and 2 (descriptions in further detail below). The activity may be include a series of events whereby the tooth surface is wetted, which then allows better penetration of stain removers and stain lightening free radicals between the enamel rods. Tooth whitening may then be achieved by rendering the tooth free of colored stains via a series of steps that may include: stain loosening, stain decomposition, dissolution, foaming suspension of the tooth stain above the enamel surface, and dispersement to prevent re-deposition of stains. Any especially tenacious stains may then be optionally lightened by the optionally included oxidizing agent. Additional ingredients can be added or deleted to make a special purpose tooth cleaner for inclusion in any number of oral care products including tooth paste, tooth whitening systems, mouth rinses, prophylaxis pastes, tooth bonding agents, caries prevention systems, as well as many other oral care compositions.

BRIEF DESCRIPTION OF THE DRAWINGS

FIG. 1 is a schematic diagram of whitening and/or cleaning of a tooth stain according hereto;

FIG. 2 is a schematic diagram of an exemplary series of steps for whitening and/or cleaning of a tooth stain;

FIG. 3 is a schematic diagram alkaline builder activity;

FIG. 4 is a schematic diagram of chelator activity;

FIG. 5 is a schematic diagram of a method of application;

FIG. 6 is a flow diagram of a method of manufacture;

FIG. 7 is a flow diagram of a method of use;

FIG. 8 is a table of data regarding whitening; and,

FIG. 9 is a table of data regarding sensitivity.

DETAILED DESCRIPTION

The detailed description set forth herein is intended as a description of several exemplary compositions for enhancing the effectiveness of tooth whitening and/or other oral care compounds according to the present invention and is not intended to represent the only forms in which such compositions may be prepared or utilized. The description sets forth features of and steps for preparing and using the preferred enhancer compositions of the present invention. It is to be understood, however, that the same or equivalent ingredients may be incorporated in different embodiments of the invention to allow it to be used as a stand-alone whitener or to allow it to be incorporated into mouth rinse, dentifrice, prophylaxis paste, enamel and dentin bonding systems, caries prevention tooth sealants, desensitizing treatments and many other oral care products. Furthermore there are many compositions that may accomplish the same functions or achieve the same results and such compositions are also intended to be encompassed within the spirit and scope of this description.

The present invention, at a minimal level of complexity may employ one or two or more different liquid solvents, a surfactant, typically including one each of a neutral and an anionic surfactant, and an alkaline builder to enhance detergent activity. Although not previously used in dentistry in the combinations described nor for the purposes intended herein, surfactants, solvents, alkaline builders and chelators are well known in the art of fabric and textile cleaning and may be readily understood in translation from that field to the present one of oral care. Choices of particular solvents, surfactants and/or alkaline builders in use in oral care should also be based on safe oral administration and on the physical properties desired for the compositions being prepared. The amounts of chelators, alkaline builders, surfactants and solvents may be adjusted if necessary to compensate for any additional active agents which might be incorporated herein or used herewith, such as peroxide-based whitening agents. The sum amount of all the cleaning chemicals added into various embodiments of the current invention comprise from about 8% to about 90%, and preferably from about 10% to about 40% by weight of the oral composition, the balance preferably being de-ionized water, preferably, high performance liquid chromatography (HPLC) de-ionized water.

Solvents may be beneficial for stain removal and/or for rapid tooth whitening and they may moreover serve many purposes in the present invention. For example, the solvent may: (1) dissolve the other ingredients of this overall composition (2) enhance penetration of actives to the tooth surface (3) break up the stain molecule into smaller pieces that are more easily dissolved and suspended; (4) break the bond between the stain and the tooth surface; and (5) provide a medium in which stain can be suspended and carried away from the surface. Some schematics of solvent action are shown in FIGS. 1 and 2.

There are many solvents that work to remove stains. Water is in fact the oldest, least expensive and most widely used cleaning solvent known to man, although it is slow and inefficient for that purpose. However water will typically be present in compositions described herein because it may be used to: (1) dissolve the hydrophilic ingredients of the present invention (2) prevent dehydration of enamel caused by any whitener, if used; (3) help dilute and dissolve the thickener used by any whitener, if used; and (4) to assist in overall tooth cleaning.

De-ionized, HPLC grade water is preferred as an aqueous solvent medium for the creation of a tooth cleaning composition according hereto. The reason for preferring HPLC grade de-ionized water is because it may minimize contamination of the cleaning solution from trace minerals that might be found in other waters that ultimately could inhibit detergent action. Another advantage of using HPLC de-ionized water as the carrier solvent is that it may evaporate with little or no residue after delivering cleaning agents to the target surface to be cleaned. Other embodiments can use standard de-ionized water and still other embodiments may use distilled and filtered water.

In addition to water, it may be desirable to add other cleaning solvents. An ideal cleaning solvent would preferably be water miscible, forming a hydrophilic co-solvent system with water. As used in an enhancer composition for use with whiteners, the solvent chosen might also have a further preferable ability break down any present peroxide gel. The orally acceptable solvents that can be used to create a co-solvent system for use in the present invention include ethanol, dehydrated ethyl alcohol, glycerol, propylene glycol, or one of the orally acceptable polyethylene glycols. For superior tooth cleaning ability, the recommended solvents should be one or more orally acceptable hydrophilic or hydrophobic solvents, such as orange oil, ethyl alcohol, propylene glycol, polyethylene glycol 400 or polyethylene glycol 600. A preferred embodiment utilizes a combination hydrophobic/hydrophilic approach and may specifically use dehydrated ethyl alcohol or ethanol and orange oil. For example, the ethyl alcohol can be present in the range of about 0.5% to about 15%, and preferably between about 5% and about 10% and most preferably about 8.5%. Since orange oil is only slightly miscible, it can be present in the range of about 0.01% to about 0.5%, and preferably between about 0.08% and about 1% and most preferably between about 0.1% and about 0.2% by weight of the oral care composition.

Surfactants are also preferably used herein, and these can play a variety of roles from actually attaching to and/or assisting in the removal of the stain particles from a tooth surface, to providing a foaming and lifting activity for moving the stain particle into the solvent to carry it away. Following this, a dual neutral and charged surfactant approach may also be desirable. Neutral surfactants can cause foaming and surface wetting, while charged surfactants can bind to stains and increase solubility. As described further, added alkaline builders may further enhance these actions, helping to remove the most adherent tooth stains (see also FIG. 3).

As mentioned, the oral care compositions described herein may typically include an alkaline building agent that aids the surfactant/detergent in binding and removing tooth stain from highly negatively charged enamel surfaces. The alkaline builder should also preferably have sufficient capacity to decompose an oxidizing agent that could be included in any of these compositions or used in conjunction with these compositions. Such alkaline building agents, as used herein, refer to agents that can be used to adjust the pH of the compositions to a range of about pH 7.1 to about pH 10. An oral care composition used to decompose an optional whitening agent ideally should have a pH of from about 8.8 to about 9.2. If a whitening agent is included in the composition of matter the pH should ideally range from about 7.1 to about 8.0 and further stabilized with sodium EDTA which may also serve as a water softener and/or chelator.

An ideal alkaline builder may also have the ability to saponify oily tooth stains. Possible orally acceptable alkaline builders include alkali metal hydroxides, carbonates, sesquicarbonates, borates, silicates, phosphates, imidazole, and mixtures thereof. Specific alkaline building agents may include monosodium phosphate, trisodium phosphate, sodium hydroxide, potassium hydroxide, alkali metal carbonate salts, sodium bicarbonate, pyrophosphate salts, and sodium citrate. The preferred embodiment uses Sodium Bicarbonate, Sodium Hydroxide, or Potassium Hydroxide in combination with Sodium Citrate. Sodium or Potassium Hydroxide should ideally be used at a level of from about 0.01% to about 10%, with the preferred embodiment from about 1% to about 3%. Sodium Citrate should ideally be used at a level of from about 0.01% to about 5%, with a preferred embodiment from about 0.1% to about 0.5%. by weight of the oral care composition.

Oral surfactants useful in the present invention may include both nonionic and anionic surfactants. Any asymmetrical molecule dissolved in water will make at least a weak surfactant. Such weak surfactants may not normally be effective foaming agents, but the effectiveness can be improved if an alternatively available foaming dispenser is used. Asymmetrical molecules as contemplated herein may include those that contain a hydrophilic and a hydrophobic segment. One end of the molecule is thus polar in nature and dissolves in water, while the other end is nonpolar in nature, avoids water, and dissolves in oil and other nonpolar compounds. When in water, their polar ends of these surfactant molecules are oriented toward the water molecules, while the non-polar ends attract non-polar molecules. The non-polar ends of the surfactant molecules lift stain molecules from the tooth surface by loosening the molecules, breaking them up, and holding them onto the asymmetric molecules, allowing them to be washed away with the water. Oral surfactants which may be employed include block co-polymers of polyoxyethylene and polyoxypropylene such as the Pluronics. Other oral surfactants may include soluble alkyl sulfonates having 10 to 18 carbon atoms, such as sodium lauryl sulfate, and sulfates of monoglycerides of fatty acids having 10 to 18 carbon atoms or sarcosinates (including salts and derivatives) such as sodium-N-lauroyl sarcosinate. Mixtures of anionic and nonionic surfactants may be preferably used in many implementations.

Nonionic surfactants may include, but are not limited to, compounds comprising hydrophilic (having an affinity for water) and hydrophobic components (lacking an affinity for water). These surfactants may be produced by the condensation of alkylene oxide groups, which are hydrophilic in nature, with an organic hydrophobic compound, which may be aliphatic or alkyl-aromatic in nature. Examples of suitable nonionic surfactants include low viscosity poloxamers, e.g., poloxamer 188 (under trade name Pluronic), low viscosity hydroxyethyl cellulose, polysorbates, polyoxyethylene sorbitan esters (under trade name Tweens), fatty alcohol ethoxylates, polyethylene oxide condensates of alkyl phenols, products derived from the condensation of ethylene oxide with the reaction product of propylene oxide and ethylene diamine, ethylene oxide condensates of aliphatic alcohols, long chain tertiary amine oxides, long chain tertiary phosphine oxides, long chain dialkyl sulfoxides, and mixtures thereof. Anionic and other amphoteric surfactants may include, but are not limited to, derivatives of aliphatic secondary and tertiary amines in which the aliphatic component may be a straight chain or branched. One of the aliphatic substituents may contain from about 8 to about 18 carbon atoms and one may contain an anionic water-solubilizing group, e.g., carboxylate, sulfonate, sulfate, phosphate, phosphonate, betaines (e.g., cocamidopropyl betaine), and mixtures thereof. Many of these nonionic and amphoteric surfactants are disclosed in U.S. Pat. No. 4,051,234, which is hereby incorporated herein by reference in its entirety. Furthermore surfactants may also be included in the oral care activation compositions in solid form. Solid form surfactants may include, for example, sodium carbonate anhydrous, sodium bicarbonate, potassium iodide, and mixtures thereof. Exemplary surfactants may also include at least some difunctional block copolymer surfactants, e.g., those having terminal groups of primary hydroxyl groups, and groups comprising a hydrophobic and a hydrophilic segment. Examples include Pluronic F68, Pluronic F88, and mixtures thereof. In the preferred enhancer embodiment, Pluronic F68 is preferably used as the wetting and foaming agent. The amount of Pluronic F68 used in the oral care enhancer composition may be in a range from about 0.1% to about 2.0% by weight and most preferably in the range of about 0.5% and about 1.0%. Furthermore, in a preferred enhancer embodiment, sodium lauryl sulfate (SLS) or cocamidopropyl betaine may preferably be used as stain binding detergent. The amount of SLS used in the oral care enhancer composition may be in a range from about 0.1% to about 2.0% by weight and most preferably in the range of about 0.5% and about 1.0%. Furthermore, in the preferred embodiment the amount of detergent and neutral surfactant should be used in roughly equivalent amounts.

The present preferred composition also contains a basic saponification agent that has the ability to convert oily tooth stains into a kind of soap which is then easily dissolved and carried away from the tooth. Saponifying agents could serve as an excellent buffer for the enhancer composition. If used in this manner it should have the further ability to maintain and buffer the pH of the alkaline builders described hereabove such that the enhancer composition pH is in the range of about pH 7.0 to about pH 10. More typically, the enhancer embodiment should have a pH of from about 8.0 to about 10.0, and preferably from about 8.25 to about 9.0. The possible range of saponifying buffering agents include alkali metal hydroxides, carbonates, sesquicarbonates, borates, silicates, phosphates, imidazole, and mixtures thereof. Specific buffering agents include monosodium phosphate, trisodium phosphate, sodium benzoate, benzoic acid, sodium hydroxide, potassium hydroxide, alkali metal carbonate salts, sodium carbonate, imidazole, pyrophosphate salts, citric acid, and sodium citrate. Preferred saponifying buffering agents would be those that control the pH in the target alkaline range without affecting taste, odor or the cleaning ability of the composition of matter. Preferred saponifying buffering agents may include acetic acid, sodium acetate, citric acid, sodium citrate, benzoic acid and sodium benzoate. A preferred embodiment uses sodium citrate because of it has an excellent ability to saponify susceptible tooth stains. It ideally should be used at a level from about 0.01% to about 5%, with the preferred embodiment from about 0.1% to about 0.5%. by weight of the oral care composition.

Although not necessary, oxidizing agents may be optionally included as an oral care active in the present invention. In the case of an enhancer composition a small level could be included as an immediately available sink of oxidizing agents that would be used to further enhance the overall whitening activity during the initial minutes of the combined whitening treatment, prior to the carrier gel liquification. These optionally included whitening should have the property of decomposition under alkaline conditions. Such substances are selected from the group consisting of peroxides, metal chlorites, perborates, percarbonates, peroxyacids, persulfates, and combinations thereof. Suitable peroxide compounds include hydrogen peroxide, urea peroxide, calcium peroxide, carbamide peroxide, and mixtures thereof. In one embodiment the peroxide compound is carbamide peroxide. Suitable metal chlorites include calcium chlorite, barium chlorite, magnesium chlorite, lithium chlorite, sodium chlorite, and potassium chlorite. Additional bleaching substances may be sodium hypochlorite and chlorine dioxide. In one embodiment the chlorite is sodium chlorate. The preferred embodiment uses hydrogen peroxide as the whitening agent. The level of any of these substances is dependent on desirability of adding a stain lightening function to the tooth cleaning function of the composition of matter described hereabove. The oxidizer may use oxygen or chlorine respectively so long as that molecule is capable of providing to bleach the stain. This level generally used in compositions of the present invention are from about 0% to about 10%, preferably about 0% to about 5%.

The composition of the present invention can also include other active ingredients, such as peroxide photo-activators. The addition of peroxide photo-activators can also increase the photobleaching efficiency of the foamable compositions of the present invention. Suitable peroxide photo-activators include those with lower oxidative state transition metal salt. The metal salt may catalyze the bleaching action of the peroxide to produce faster effective bleaching at lower peroxide concentrations. The preferred transition metals are those of lower atomic numbers including lower atomic number transition metals such as those ranging from atomic number 21 to 30. Also, those with lower oxidative states may be more preferred, including, e.g., Iron(II), manganese(II), cobalt(II), copper(II) and mixtures thereof, and most preferably Iron(II), as in a ferrous gluconate. When used, only a very small amount of the transition metal salt is needed, for example, from about 0.01% by weight to about 4% by weight, further for example, from about 0.03% by weight to about 2% by weight, and even further for example, from about 0.04% to about 1% by weight. The peroxide photo-activator can also include alkali salts such as potassium iodide, potassium chloride, sodium iodine, sodium chloride and combinations thereof.

Amorphous calcium compounds such as amorphous calcium phosphate (ACP), amorphous calcium phosphate fluoride (ACPF) and amorphous calcium carbonate phosphate (ACCP) amorphous calcium carbonate phosphate (ACCP), and amorphous calcium carbonate phosphate fluoride (ACCPF) can be used in re-mineralizing teeth. These amorphous compounds are disclosed in U.S. Pat. Nos. 5,037,639, 5,268,167, 5,437,857, 5,562,895, 6,000,341, and 6,056,930, the disclosure of each of which hereby being incorporated by reference in its entirety.

In addition to or as an alternative to amorphous calcium compounds, amorphous strontium compounds such as amorphous strontium phosphate (ASP), amorphous strontium phosphate fluoride (ASPF), amorphous strontium calcium phosphate (ASCP), amorphous strontium calcium carbonate phosphate (ASCCP), amorphous strontium carbonate phosphate fluoride (ASCPF) and amorphous strontium calcium carbonate phosphate fluoride (ASCCPF) may be included for use in re-mineralization, as noted above. Such compounds are disclosed in U.S. Pat. No. 5,534,244, the content of which hereby incorporated by reference in its entirety.

For example, the whitening compound may include a source of phosphate and the second component may include a source of calcium or strontium. For example, the source of phosphate in the first component includes monosodium phosphate (NAH2PO4), disodium phosphate, tetrapotassium pyrophosphate and relatives thereof. As introduced above, the whitening component may include a source of calcium or strontium, which combines with phosphate to form the various amorphous calcium and/or strontium phosphates. The source of phosphate may be, for example, present in an amount of from about 0.2% to about 5% by weight. The source of calcium, strontium, or combinations thereof may include a calcium salt, a strontium salt, and thereof, further for example, a calcium salt such as calcium nitrate, in an amount of from about 0.25% by weight to about 1.5% by weight. The source of phosphate and the source of calcium, strontium or mixture can combine to form calcium phosphate. When applied to the teeth, the calcium phosphate can precipitate onto the surface of the teeth where it may be incorporated into hydroxyapatite, assisting in remineralization of the tooth enamel, as discussed in U.S. Pat. Nos. 5,037,639; 5,268,167; 5,460,803; 5,534,244; 5,562,895; 6,000,341; and 6,056,930 noted above.

In practice, it may in some embodiments be preferred to include as much phosphate as possible, as the phosphate salt further acts to adjust the pH of the first component. The pH of the system is from, for example, about 5 to about 10.0, or for a further example, from about 5.5 to about 9.0.

Note also, the fluoride-containing amorphous compounds described here may also be used in fluoridating teeth. Otherwise, as mentioned, fluorides may be added separately and then, many, if not all of the above amorphous compounds or solutions which form the amorphous compounds, when applied either onto or into dental tissue, particularly in the presence of fluoride, may operate to promote fluoridation. Such fluoridation or other mineralization may serve to assist in prevention and/or repair of dental weaknesses such as dental caries, exposed roots and dentin sensitivity.

The activation composition of the present invention can also include other active ingredients, such as de-sensitizing-agents and/or antimicrobial or antibacterial agents. Even with improved efficiency and shorter treatment time, some patients may still experience sensitivity from tooth whitening compositions. Inclusion of desensitizing agents in the activation composition allows time for desensitization of the oral tissue before the application of the whitening compound. Suitable desensitizing agents can include Eugenol and/or alkali nitrates such as potassium nitrate, sodium nitrate, and lithium nitrate and other potassium salts such as potassium chloride and potassium bicarbonate. The desensitizing agent may make up to about 3% to 5% percent by weight of the activation composition. Eugenol may also act as an antimicrobial or antibacterial agent.

Further additives may include calcium nitrate and/or sodium mono and/or dibasic hydrate. These compounds may be added to lower the viscosity of the activation composition and provide a composition that has greater ability to penetrate recesses and interstices of the dentition. Such additives may also improve the stability of the activation composition. Potassium nitrate may alternatively and/or additionally be added to achieve desired viscosity effects.

In addition, optional additives including emulsifiers, flavorings, coloring agents, anti-plaque agents, anti-staining compounds, excipients such as emollients, preservatives, other types of stabilizers such as antioxidants, chelating agents, tonicity modifiers (e.g., sodium chloride, manitol, sorbitol, or glucose), spreading agents, pH adjusting agents and water soluble lubricants, e.g., propylene glycol, glycerol, or polyethylene glycol may be included in the activation composition. The concentration of each may easily be determined by a person skilled in the art. Lecithin, a natural emulsifier found in soy and other plants, and gum arabic, which comes from the sap of certain species of acacia trees, can be added for use as an emulsifier, dispersant, and/or wetting agent. Suitable preservatives may include benzalkonium chloride, parabens, chlorhexidine acetate, chlorhexidine gluconate, sorbic acid, potassium sorbitol, chlorbutanol, and phenoxyethanol. Suitable emollients such as those used for topical applications are, for example, di-n-octyl ether, fatty alcohol polyalkylene glycol ether, 2-ethylhexyl palmitate, and isopropyl fatty acid esters.

An exemplary formula for an activation composition according to the present invention is presented in Table 1 below. Water may be used as a carrier solvent for the remaining ingredients. Dehydrated alcohol and orange oil are other solvents. Potassium hydroxide is incorporated in this example as a main alkaline builder and pH modifier. Other optional ingredients which may provide certain functionalities may include tartaric acid to adjust the final pH of the composition to a biologically compatible level and hydrogen peroxide which may initiate a secondary stain lightening process. Pluronic F68 is used as the neutral wetting and foaming agent responsible for lifting and dispersing stain molecules above the tooth surface. Sodium lauryl sulfate as anionic detergent remover. Sodium saccharin and sucralose are used as sweeteners, sodium citrate for saponification, pH buffering and improved oral sensation. Wintergreen and peppermint oil are for flavor and scent, as well as for their excellent solvent properties. The ethanol may also be used as an antibacterial preservative agent. Color can be optionally added for visual interest.

TABLE 1
Chemical/
IUPAC
IngredientAmount“real name”SourcePurpose
HPLC deionized80%De-ionizedSpectrumsolvent
water (H2O)waterChemical(carrier)
Dehydrated15.5%DehydratedSpectrumsolvent
ethanolalcoholChemical(cleaning)
Hydrogen2.0%SameAutofinaoptional
peroxidewhitening
(H2O2) (30%)agent
potassium0.1%SameSpectrumalkaline
hydroxideChemicalbuilder en-
(KOH)hancement
of deter-
gent action
Pluronic F680.5%poloxamerBASFneutral
188surfactant
wetting
and foaming
agent
sodium laurel0.5%SameSpectrumDetergent
sulfate (SLS)Chemicalstain
remover
sodium0.3%SameSpectrumsweetener
saccharinChemical
Sucralose0.2%splendaSpectrumsweetener
Chemical
sodium citrate0.7gSameSpectrumsaponifica-
(Na3C6H5O7)Chemicaltion oral
sensation
and pH
modifyer
orange oil0.1%SameSpectrumsolvent
Chemical(cleaning)
Methyl0.3%wintergreenS&Sflavor,
salicylateoilFlavorsscent, sta-
bilizer and
solvent
tartaric0.1gSameSpectrumpH modifier
acid (C4H6O6)Chemical

Table 1

The ingredients of Table 1 including the exemplary activation composition may be mixed according to the exemplary method depicted in FIG. 6. Initially, approximately 0.1 g of potassium hydroxide may be completely dissolved in 55 ml of de-ionized water (step 105). The dissolution of potassium hydroxide is an exothermic process that may heat the solution. Next, approximately 0.5 g of poloxamer 188 may be dissolved in the H2O—KOH mixture (step 110). The generation of heat may be advantageous because heat may be beneficial for the dissolution of the poloxamer 188. Application of additional heat to the mixture may assist in completely dissolving the poloxamer 188. The mixture of H2O, KOH, and poloxamer 188, which may be referred to as Mixture 1, may be set aside.

A second mixture, Mixture 2, may be prepared by dissolving approximately 0.3 g of sodium saccharin and 0.2 g of sucralose in 18 ml of water (step 115). Mixture 2 may be completed by dissolving approximately 0.7 g of sodium citrate into the water-sodium saccharin solution (step 120). Mixture 1 may then be combined with Mixture 2 (step 125). Next, approximately 6.7 g of 30% hydrogen peroxide solution may be slowly introduced to the combination of Mixture 1 and Mixture 2 to form Mixture 3 (step 130). Mixture 3 may then be set aside.

Another mixture, Mixture 4, may be created by dissolving approximately 0.3 g of methyl salicylate and 0.1 g of orange oil in approximately 16 g of ethanol (step 135). Several drops of a coloring additive, for example, food coloring, may be optionally added to Mixture 4 to provide visual interest to the activation composition (step 140). In the ingredients depicted in Table 1, approximately two drops of food coloring may be added to Mixture 4.

Next, Mixture 4 may be slowly added to Mixture 3 to form Mixture 5 (step 145). Finally, approximately 0.1 g of tartaric acid may be added to Mixture 5 (step 150) to adjust the basic pH of Mixture 5 downward to a biologically compatible level, for example, between about 8.5 and about 9.5, with a target pH of about 8.8. The mixture of the ingredients in Table 1 according to the steps set forth in FIG. 1 may thus result in a 100 ml volume of an exemplary composition for standalone use or pretreatment of dentition before application of a discrete tooth whitening composition. The increase in pH created by the activation composition may enhance the effectiveness of the discrete tooth whitening compound.

Although certain steps for combining the ingredients identified in Table 1 are indicated in FIG. 6 and the accompanying discussion above, it should be recognized that additional or alternative ingredients described above may also be included or substituted in the activation composition. Further, the steps depicted in FIG. 6 are merely exemplary and other variations for mixing ingredients of the activation composition are possible and contemplated.

The enhancer composition may be applied to a user's dentition in any of a variety of ways. For example, if the activation composition has a low viscosity, the enhancer composition may be provided in the form of a mouth rinse or through the use of a foam-tipped swab as shown in FIG. 5. At a higher viscosity, for example, in the form of a gel or paste. The activation composition may be in the form of a toothpaste and applied with a standard tooth brush. The activation composition may also be applied with a prophy cup if supplied as a prophylaxis paste. If the activation composition is applied with a swab (e.g., the activation composition is a gel), the swab may be formed of a foam material rather than other materials. Foam may be more structurally sound and uniformly absorptive as compared to cotton swabs or other materials. Foam also may be resistant to breaking down and does not permanently deform.

FIGS. 5 and 7 depict exemplary professional tooth whitening processes including steps of enhancer application using a supplied swab tube dispenser. First, the teeth may be cleaned and a shade guide may be used to determine initial tooth shade. In the next steps, the soft tissues may bee protected with cotton and a paint on rubber dam. The following next three steps demonstrate the correct method of opening the swab tube dispenser. After the dispenser is opened, a swab containing the enhancer composition may be swiped across the facial surface of each tooth that is intended to be whitened. A professional tooth whitening composition containing approximately 20% hydrogen peroxide may be applied to the teeth. A bleaching light may be then activated and the enhancer/bleaching gel mixture may be left on the patient's teeth for typically no more than about 5 minutes. After the first cycle is completed the whitening mixture may be evacuated and wiped off, new enhancer composition may be applied followed by new bleaching gel. After about 5 minutes, the mixture may be removed and a third cycle may be commenced similar to cycles 1 and 2. After only a total of only about 15-21 minutes, the teeth are rinsed, the treatment may be completed by matching a shade guide. Data shown in FIG. 8 show that 8 shades of whitening can be achieved in a procedure that may be completed in 21 minutes instead of the traditional 90 to 120 minutes. Furthermore data shown in FIG. 9 that the enhancer composition has a highly significant ability to eliminate the transient dentinal hypersensitivity typically associated with tooth whitening treatments. FIG. 9 shows that while most commercial whiteners cause some level of tooth sensitivity, when used in combination with the enhancer composition, the sensitivity levels drop to near zero.

When used in the above format as a pre-whitening activator to enhance the activity of any whitening gel, it is likely that the whitening gel will likely be distributed apart from the composition(s) described herein, though it could simply be packaged therewith.

In a further alternative, other organic or human tissue may be conditioned using compositions hereof. For example, melanin is an organic carbon-bonded molecule and is subject to whitening in much the same manner as organic tooth stain molecules. Darker skin pigmentation is caused by the over expression or accumulation of melanin in the skin. As a result, the application of an activated mild whitener composition, containing an oxidizing agent will work to make the skin appear whiter on a temporary basis. The resultant whitening is temporary as the epithelium and melanin are replaced on a daily basis. However to the extent that persons may want an instant temporary method of appearing cosmetically lighter, this method is one possible solution. The ability to modify the appearance of pigment content in the skin, to promote an even-looking skin tone and a more youthful appearance, is highly desired in many of the world's societies. Many people desire to modify their skin tone, to reduce aging spots, melasma, etc., or for purely cosmetic reasons. In fact, in the Far East, a lighter skin tone is desirable and is associated with higher socioeconomic status.

Therefore, the present invention, in an alternate embodiment may be used as a skin whitening composition which can be effectively used as a topical agent and which would cause rapid skin lightening. For this application, the preferred peroxygen would be benzoyl peroxide, and all other oxidizers, such as nitrogen oxide or sodium chlorite present should be preferably reduced by 50% or more in the overall composition. Furthermore, the composition of the invention described herein can be optionally combined with tyrosinase inhibitors, and/or melanin cell synthesis inhibitors, along with skin exfoliating agents, which are all useful in topically applied cosmetic skin whitening formulations described in the current art.

The above specification, examples and data shown in FIGS. 8 and 9 below, provide a complete description of the structure, process, and use of exemplary embodiments of the invention. Although various embodiments of this invention have been described above with a certain degree of particularity, or with reference to one or more individual embodiments, those skilled in the art could make numerous alterations to the disclosed embodiments without departing from the spirit or scope of this invention. Other embodiments are therefore contemplated. It is intended that all matter contained in the above description and shown in the accompanying drawings shall be interpreted as illustrative only of particular embodiments and not limiting. Changes in detail or structure may be made without departing from the basic elements of the invention as defined in the following claims.