Compositions forming fluoride mouthrinse when combined with water

Abstract

The disclosure provides tablets for a mouthrinse containing fluoride, an effervescent agent comprising an acid and a base, a water soluble lubricant, a binder, and a sensory modifying agent. The tablets are free of preservatives and free et alcohol. In certain embodiments, the effervescent agent contains citric acid and sodium bicarbonate. The water soluble lubricant may include polyethylene glycol (PEG), potassium sorbate, sodium benzoate, calcium sorbate, PEG with one or more of trisodium citrate, calcium ascorbate, and mixtures thereof. The binder may include sodium carboxymethyl cellulose, mannitol, polyvinylpolypyrrolidone, microcrystalline cellulose, colloidal silicon dioxide, and combinations thereof.

Description

COMPOSITIONS FORMING FLUORIDE MOUTHRINSE WHEN COMBINED WITH WATERFIELD OF THE INVENTION

[0001] This disclosure relates to effervescent tablets containing fluoride or other compositions containing fluoride that generate a fluoride mouthrinse when combined with water.BACKGROUND OF THE INVENTION

[0002] Fluoride is a mineral known to strengthen tooth enamel, reduce tooth decay, and can also reduce cavities. It protects tooth enamel against acid attacks and is known to repair initial stages of tooth decay.

[0003] Because of its benefits, fluoride mouthrinses are often used as part of a dental hygiene regimen. These mouthrinses are typically sold in liquid form and as such require packaging that needs to be recycled after use. These rinses also necessitate the bottling and transport of a large amount Of water. In addition, due to being in liquid forms mouthrinses are subject to the Transportation Security Administration’s limit for liquids in carry-ons on airplanes.

[0004] Effervescent tablets containing fluoride reduce waste, are far more sustainable, and avoid the ISA’s liquid limits. However, such tablets must be carefully designed to be suitable for human consumption and to preserve the effectiveness of fluoride.

[0005] Fprexample, U.S. Patent No. 4,267,164 discloses effervescent stannous fluoride tablets. These tablets require malic acid and alkali metal bicarbonate in a weight ratio of about 3:2. Malic acid is not preferred. Malic acid has been associated with certain side effects such as headaches, diarrhea, nausea, and irritations. In addition to containing the bicarbonate base, all the examples of these tablet formulations also contain carbonate. Furthermore, depending on the formulation, stannous fluoride Containing formulations have the potential to stain teeth. In addition, stannous fluoride was known to have an unpleasant taste.

[0006] U.S. Patent Na 6,811 ,793 discloses effervescent compositions containing stevia, a water soluble binder, a water soluble lubricant, an active agent, and an effervescent agent. The effervescent agent that includes an acid and a base, both of which may be present in an amount from about 10% w / w to about 60% w / w. The compositions can also contain from about 10% w / w to about 60% w / w ofone or more binder, with from about 25% w / w toIabout 40% w / w being preferred. Suitable active agents include vitamins, amino acids, pharmaceutical agent, minerals, and dietary supplements. Fluoride is notincluded in the list of suitable active agents.[60071 What is needed are compositions containing an anticaries active ingredient (such as e.g., fluoride) as that do not stain teeth or contain components that have undesirable side effects such as headaches, diarrhea, nausea, and irritations.SUMMARY OF THE INVENTION f0OO8] Otho* features and advantages of the invention will be apparent from the detailed description and examples that follow.

[0009] This disclosure is directed to compositions containing an anticaries active ingredient (such as e.g., fluoride) and a sensory modifying agent that generate a mouthrinse (such as e.g., a fluoride mouthrinse) when combined with water. Tn particular, this disclosure is directed to a composition comprising an anticaries active ingredient and a sensory modifying agent that dissolves in water.

[0010] In certain embodiments, the anticaries active ingredient is fluoride. The composition can also include a water-soluble lubricant. Tn some embodiments, the composition contains a water-soluble lubricant selected from polyethylene glycol (PEG), potassium sorbate, sodium benzoate, calcium sorbate, PEG with one or more of trisodium citrate, calcium ascorbate, and mixtures thereof.

[0011] In other embodiments, the sensory modifying agent is a sensate, a taste modifying agent, or a combination thereof. For example, the sensory modifying agent is a senate that imparts a cooling sensation. Examples of such sensates include (lR,2S,5R)-N-ethyl-2- isopropyl-5- methylcyclohexanecarboxamide, (IR2S,5R)-N~(4-(<yanomethyl)phenyi)-2- isopropyl-5-metbylcyclohexanecarboxamide, and (!R,2S,5R)-2-isopropyl-5- methyl-N-(2- (pyridin-2-yl)ethyl)cyclohexanecarboxamide, menthyl lactate, 2-isopropyl-N,2,3- trimethylbutanamide, and (lR,2S,5R)-2-isopropyl-5-methyl-N-(2-(pyridin-2- yl)ethyl)cyclohexanecarboxamide, and a combination thereof. In other embodiments, the sensate imparts a cooling sensation, awarming sensation, a burning sensation, and / or a tingling sensation.

[0012] In alternate embodiments, the composition further includes a binder selected from sodium carboxymethyl cellulose, mannitol, polyvinylpolypyrrolidonc, microcrystalline cellulose, colloidal silicon dioxide, and combinations thereof. In some embodiments, the binder is sodium carboxymethyl cellulose, polyvinylpolypyrrolidone, and mannitol.2

[0013] The compositions may be in various forms. For example, the composition can be formulated as an effervescent powder, a non-effervescent powder , a compressed tablet, an effervescent tablet, a non-effervescent tablet, a non-effervescent powder, or a water free liquid concentrate.(0014] One aspect of foe disclosure is directed to effervescent tablets containing fluoride, an effervescent agent having an acid and a base component, a binder, and a sensory modifying agent. The effervescent tablets of the disclosure are preservative free <Le., they do not include any added preservative). The tablets of the disclosure are also alcohol free (f,e., they do not contain an alcohol as a tablet and / orwhen dissolved in water), in certain embodiments, the tablets also include a colorant, a bullring agent, and / or a lubricant (e.g., a water soluble lubricant^(0015] One embodiment is an effervescent tablet containing: fluoride; an effervescent agent containing an acid and a base in a ratio of acid:base (% w / w) of 1: 1.1 to 1 : 1.7; a lubricant including polyethylene glycol (PEG), potassium sorbate, sodium benzoate, calcium sorbate, PEG with one or more of trisodium citrate, calcium ascorbate, and mixtures thereof; a binder selected from sodium carboxymethyl cellulose, mannitol, polyvinylpolypyrrolidone, microcrystaliine cellulose, colloidal silicon dioxide, and combinations thereof; and a sensory modifying agent In some embodiments of flte tablet, foe binder is sodium carboxymefoyl cellulose^ polyvinylpolypyrrolidone, and mannitol. (0016 j In another embodiment the tablet contains: an anticaries active ingredient; an effervescent agent comprising an acid and a base in a ratio of acidbase (% w / w) of 1:9 to 1 :3; a water-soluble lubricant selected from polyethylene gfycpl (PEG), potassium sorbate, sodium benzoate, calcium sorbate, PEG with one or more of trisodium citrate, calcium ascorbate, and mixtures thereof; a binder selected from sodium carboxymethyl cellulose, mannitol, polyvinylpolypyrrolidone, microcrystaliine cellulose, colloidal silicon dioxide, and combinations thereof, and a taste modifyingagent.

[0017] to one embodiment, flte fluoride is sodium fluoride. In certain embodiments, foe tablet contains fluoride, acid, and base in a ratio of fluoride:acid:base of 1 :1.5:12 to 1 :3: 17.

[0018] The effervescait agent can include citric acid as foe acid and / or bicarbonate as the base. In one embodiment, the bicarbonate is sodium bicarbonate.(0019] In certain embodiments, the sodium carboxymethyl cellulose in foe binder is croscahnellose sodium. In other embodiments, the binder includes polyvinylpolypyrrolidone, mannitol and croscarmellose sodium. In some embodiments, the3PEG is PEG 4800, PEG 6000, and / or PEG 8000. to other embodiments, the PEG is PEG 6000.(0020| to certain embodiments, the binder contains sodium carboxymethyl cellulose, mannitol, and a mixture of microcrystalline cellulose and colloidal silicon dioxide, to other embodiments, the binder only contains sodium carboxymethyl cellulose, mannitol, and a mixture of microcrystalline cellulose and colloidal silicon dioxide, to one embodiment, the binder contains, croscarmellose sodium, mannitol and a mixture of microcrystalline cellulose and colloidal silicon dioxide.[6021 J to some embodiments, die sensory modifying agent is a sensate, a taste modifying agent, or a combination thereof, to one embodiment, the taste modifying agent includes a sweetener and / or a flavoring agent to one embodiment the taste modifying agent includes mint flavor (such as e.g., arvensis mint flavor). In another embodiment, the taste modifying agent includes sweet wintetgreen flavor, peppermint, spearmint, cinnamon, bubblegum, and / or fruit flavors. Alternatively, toe taste modifying agent includes a sweetener such as e.g., sucralose, stevia, xylitol, neotame, sugar alcohols, saccharines.]0022| In other embodiments, the tablet contains more than 20% w / w of the binder, to another embodiment, the tablet contains: from about 0.1% w / w to about 10% w / w of fluoride (e.g., sodium fluoride); from about 15% w / w to about 60% w / w of toe acid; from about 15% w / w to about 60% w / w of toe base; from about 1% w / w to about 10% w / w of the water soluble lubricant; from about 10% w / w to about 50% w / w of the binder, and / or from about 0.1% w / w to about 10% w / w of the sensory modifying agent (e.g.. a sensate, a taste modifying agent, or a Combination thereof), to other embodiments, the tablet contains, from about 0.1% w / w to about 10% w / w of sodium fluoride; from about 30% w / w to about 85% w / w of the effervescent agent; from about 1% W / w toabout 10% w / w of the water soluble lubricant; from about 10% w / w to about 50% w / w of the binder, and / or from about 0.1% w / w to about 10% w / w of the sensory modifying agent.{0023] to another embodiment, toe tablet contains from about 0.1% to about 10% w / w of PEG, from about 0.1% w / w to about 10% w / w of sodium carboxymetoyl cellulose, and / or from about 20% w / w to about 50% w / w mannitol.[0024| In one embodiment the effervescent tablet contains: fluoride; an effervescent agent comprising an acid and a base in a ratio of acickbase (% w / w) of 1 :9 to 1 :3; a water- soluble lubricant selected from polyethylene glycol (PEG), potassium sorbate, sodium benzoate, calcium sorbate, PEG with one or more of trisodium citrate, calcium ascorbate,4and mixtures thereof; a binder selected from sodium carboxymethyl cellulose, mannitol, polyvinylpolypyrrolidonc, and combinations thereof; and a sensory modifying agent |0625| In an alternate embodiment, the effervescent tablet only contains: fluoride; an acid and a base in a ratio of acid to base (% w / w) of 1 :9 to 1 :3; PEG; a binder consisting of sodium carboxymethyl cellulose, mannitol, and a poly vinylpolypyrrolidone; and a sensory modifying agent In another embodiment the tablet only contains: from about 1% w / w to about 10% w / w offluoridr, from about 15% w / w to about 60% w / w of the acid; from about 15% w / w to about 60% w / w of the base; from about 1% w / w to about 10% w / w of the water soluble lubricant; from about 10% w / w to about 50% w / w of the binder; and / or from about 0.1% w / w to about 10% w / w of the sensory modifying agent In these embodiments of the tablet the tablet contains or only contains: sodium fluoride; sodium bicarbonate; citric acid; a binder consisting of PEG 6000, sodium carboxymethyl cellulose, croscarmellose sodium, mannitol, and a mixture of microcrystalline cellulose and colloidal silicon dioxide; and a sensory modifying agent in furflier embodiments, the tablet contains from about 0.1% w / w to about 10% w / w of sodium fluoride; from about 30% w / w to about 85%w / w of the effervescent agent; from about l%w / w to about 10% w / w of PEG; from about 10% w / w to about 50% w / w of the binder; and / or from about 0.1% w / w to about 10% w / W of Are sensory modifying agent, wherein the binder i$ mannitol and croscarmellose sodium,(0026| In certain embodiments, the sum of the % w / w of the fluoride, the % w / w of the effervescent agent, the % w / w of the binder, and the % w / w of the sensory modifying agent in the tablet is 100 % w / w.{0027] In some embodiments, the tablet is preservative-free. In other embodiments, the tablet is alcohol-free. In further embodiments, bicarbonate is the only base.(0028] Another embodiment of the disclosure is a container containing the effervescent tablets of the disclosure. Yet another embodiment is a blister package containing the effervescent tablets of the disclosure. The disclosure also includes a dose cup and a tablet of the disclosure, a container of the disclosure or a blister package of the disclosure. Hie kit also includes instructions for mixing with water.DETAILED DESCRIPTION

[0029] Generally, the disclosure provides a fluoride mouthrinse in an effervescent tabid which will be added to water, ideally about 10 ml of water. In an embodiment of the5invention, a dosing cup may be provided. The consumer wilt allow the product to dissolve and then use as usual for a 10ml dose of fluoride mouthrinse..

[0030] These effervescent fluoride containing tablets do not stain teeth and do not contain components that have undesirable side effects such as headaches, diarrhea, nausea, and irritations.(0031j Accordingly, this disclosure provides effervescent tablets containing fluoride. These tablets generate a fluoride mouthrinse when combined with water. The disclosure includes the tablets packaged in containers or blister packages as well as kits. The kits may include a dose cup,[003?| Without being bound by theory, the tablets of the disclosure save space, minimize waste, and allow for improved portability when compared to conventional bottles containing a mouthrinse. The tablets are also very sustainable in eliminating the bottling and transporting of water for a mouth rinse.

[0033] In certain embodiments, the tablets are designed to be added to 10 ml of water. After the tablets dissolve, they are to be swished in the mouth for 60 seconds and then spit out. The tablets of the disclosure provide several benefits including but not limited to: fluoride for strengthening teeth and restoring enamel; more environmentally friendly than large plastic bottles; recyclable container (smaller than conventional packaging); TSA approved size; and alcohol free.[0034| Furthermore, the tablets of the disclosure when packaged are in a smaller padcage than conventional liquid mouthwashes. Due to the smaller package, they are easier to carry and store, and provide a significant reduction in carbon emissions and countertop clutter.

[0035] Ute tablets of the disclosure are more sustainable, shelf stable, preservative free, portable, and do not impact the efficacy of fluoride.[00361 The general description and the following detailed description are exemplary and explanatory only and are not restrictive of the invention, as defined in the appended claims. Other aspects of the present invention will be apparent to those skilled in the art in view of the detailed description of the invention as provided herein.[0037 j For clarity of disclosure, and not by way of limitation, die detailed description of the invention is divided into subsections that describe or illustrate certain features, embodiments, or applications of the present invention.6Definitions

[0038] Unless defined otherwise, al! technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs. Although any methods and materials similar or equivalent to those described herein can also be used in the practice or testing of the present invention, representative illustrative methods, and materials are now described.

[0039] All publications and patents cited in tins specification are herein incorporated by reference as if each individual publication or patent were specifically and individually indicated to be incorporated by reference and are incorporated herein by reference to disclose and describe the methods and / or materials in connection with which the publications are cited. The citation of any publication is for its disclosure prior to the filing date and should not be construed as an admission that the present invention is not entitled to antedate such publication by virtue of prior invention. Further, the dates of publication provided may be different from the actual publication dates, which may need to be independently confirmed.

[0040] It is noted that, as used herein and in the appended claims, the singular forms “a,” “an,” and “the” include plural referents unless the context dearly dictates otherwise. It is further noted that the claims may be drafted to exclude any optional element As such, this statement is intended to serve as antecedent basis fin* use of such exclusive terminology as “solely,” “only** and the like in connection with the recitation of claim elements, or use of a “negative” limitation.[0041 j Each of the individual embodiments described and illustrated herein has discrete components and features which may be readily separated from or combined with the features of any of the other several embodiments without departing from the scope or spirit of the present invention. Any recited method can be carried out in the order of events recited or in any other order which is logically possible.

[0042] As used herein, the term “about” when referring to a measurable value such as an amount, a temporal duration, and the like, is meant to encompass variations of =20% or* 10%, more preferably * 5%, even more preferably * 1%, and still more preferably * 0.1% from the specified value, as such variations are appropriate to perform the disclosed methods and formulate the disclosed compositions.

[0043] It is also to be understood that the terminology used herein is for the purpose of describing particular embodiments only and Is not intended to be limiting.7

[0044] Throughout tills specification, unless the context requires otherwise, the word “comprise* or variations such as “comprises” or “comprising,” will be understood to imply the inclusion of a stated integer or group of integers but not the exclusion of any other integer or group of integers.]0045] As used herein, the term “consisting of” excludes any element, step, or ingredient nof specified in the claim element|0046] Before certain embodiments are described in greater detail, it is to be understood that this invention is not limited to certain embodiments described, as such may, of course, vary. It is also to be understood that the terminology used herein is for the purpose of describing certain embodiments only, and is not intended to be limiting, since the scope of the present invention will be limited only by the appended claims.(0047] Where a range of values is provided, it is understood that each intervening value, to the tenth of the unit of the lower limit unless the context dearly dictates otherwise, between the upper and lower limit of that range and any other Mated or intervening value in that stated range, is encompassed within the invention. The upper and lower limits of these smaller ranges may independently be included in the smaller ranges and are also encompassed within the invention, subject to any specifically excluded limit in the stated range. Where the stated range includes one or both of the limits, ranges excluding either or both of those included limits are also included in the invention.

[0048] It is also to be understood that the terminology used herein is for the purpose of describing particular embodiments only and is not intended to be limiting.(0049] A “subject” or “patient,” as used therein, may be a human or non-human mammal. Non-human mammals include, for example, livestock and pete, such as ovine, bovine, porcine, canine, feline and murine mammals. Preferably, the subject is a human.(0050] Ranges: throughout this disclosure, various aspects of die invention can be presented in a range format, ft should be understood that the description in range format is merely for convenience and brevity and should not be construed as an inflexible limitation on the scope of the invention. Accordingly, the description of a range should be considered to have specifically disclosedall die possible subranges as well as individual numerical values within that range. For example, description of a range such as from I to6 should be considered to have specifically disclosed subranges Mich as from 1 to 3, from I to 4, from 1 to 5, from 2 fo 4, from 2 to 6, from 3. to 6 etc., as well as individual numbers within that range, for example, 1, 2, 2.7, 3, 4, 5, 5.3, and 6. This applies regardless of the breadth of the range.8(00511 As used herein, and as well-understood in the art, “treatment” is an approach for obtaining beneficial or desired results, including clinical results. For purposes of this invention, beneficial or desired clinical results include, but are not limited to, alleviation or amelioration of one or more symptoms, diminishment of extent of disease, stabilized (Ze., not worsening) state of disease, preventing spread of disease, delay or slowing of disease progression, amelioration or palliation of the disease state, and remission (whether partial or total), whether detectable or undetectable. “Treatment” can also mean prolonging survival as compared to expected survival if not receiving treatmentCompositions and Tablets Generatine M 'CLGoLmbrinse when combined with Water{0052 ] Tliis disclosure is directed to compositions and tablets that generate a mouthrinse when combined with water. Specifically, this disclosure is directed to compositions containing an anticaries active ingredient (such as e.g., fluoride) and a sensory modifying agent that dissolve in water, i.e.» generate a mouthrinse (such as eg., a fluoride mouthrinse) when combined with water.[0053, Accordingly, one embodiment of the disclosure a composition containing an anticaries active ingredient ami a sensory modifying agent that dissolves in water. The composition forms a mouthrinse when combined with water.[0054| The composition can be formulated as an effervescent powder, a non-effervescent powder, a compressed tablet, an effervescent tablet, a non-effervescent tablet, a liquid concentrate, or a water free liquid concentrate.10055) lb certain embodiments, the compositions arc preservative-free and / or alcohol free. In other embodiments, die composition dissolves in water in five minutes or less more, preferably in two minutes or less.|0056| The composition can contain a variety of other components including but not limited to a water soluble lubricant, a sensory modifying agent, a binder, a colorant, and / or a bulking agent.[0057| In some embodiments of die disclosure, the anticaries active ingredient is an active ingredient as defined in 21 C.F.R. § 355.10. In certain embodiments, the anticaries active ingredient is fluoride, such as eg., sodium fluoride.(00581 The fluoride may be present in an amount from about 0.1% w / w to about 0.8% w / w, alternatively from about 0.1 % w / w to about 10% w / w, alternatively from about 0.05% w / w to about 0,5% w / w. alternatively from about 0.1 % w / w to about 0,4% w / w, alternatively from about 0.1 % w / w to about 10% w / w, alternatively from about 0.2% w / w9to about 6% w / w; alternatively from about 02% w / w to about 4% w / w, 1% w / w to about 9% W / w, alternatively from about 1% w / w to about 8% w / w, from about 1% w / w to about 7% w / w. alternatively from about 1% w / w to about 6% w / w, alternatively from about 2% to about 8%, alternatively from about 2% w / w to about 6% w / w, alternatively from about 2% to about 6% w / w, alternatively from about 4% w / w to about 6% w / w. In certain embodiments, the fluoride is sodium fluoride (which may be present in the amounts specified above). In some embodiments, the compositions contain from about 1% w / w to about 10% w / w, alternatively from about 1% w / w to about 9% w / w, alternatively from about 1% w / wto about 8% w / w, from about 1% w / w to about 7% w / w, alternatively from about 1 % w / w to about 6% w / w, alternatively from about 2% to about 8%, altemati vely from about 2% w / w to about 6% w / w, alternatively from about 2% to about 6% w / w, alternatively from about 4% w / w to about 6% w / w of sodium fluoride.

[0059] in certain embodiments of the disclosure, the composition contains a water soluble lubricant In certain embodiments, tire water soluble lubricant is polyethylene glycol (PEG), potassium sorbate, sodium benzoate, calcium sorbate, PEG with one or more of trisodium citrate, calcium ascorbate, or mixtures thereof. In an embodiment, the water soluble lubricant is PEG. In one embodiment, the polyethylene glycol has a molecular weight of 6000 (PEG 6000). In alternate embodiments, the PEG has a molecular weight of 4800 (PEG 4800) or 8000 (PEG 8000).(0060) In other embodiments, the composition contains a binder, in certain embodiments, the binder is selected from sodium carboxymetbyl cellulose, mannitol, polyvinylpolypyrrolidone, microcrystalline cellulose, colloidal silicon dioxide, and combinations thereof. In certain embodiments, the binder contains sodium carboxymethyl cellulose, mannitol, and polyvinylpolypyrrolidone. In other embodiments, the binder only contains sodium carboxymetbyl cellulose, mannitol, and a polyvinylpolypyrrolidone ( / .&, no other component is added to the binder).

[0061] In certain embodiments, the sodium carboxymetbyl cellulose is croscarmellose sodium. Accordingly, in one embodiment, the binder contains croscarmellose sodium, marmitol. and polyvinylpolypyrrolidone. In other embodiments, the binder only contains croscarmellose sodium, mannitol, and polyvinylpolypyrrolidone.

[0062] In yet another embodiment, the microciystalline cellulose and colloidal silicon dioxide are a mixture of microcrystalline cellulose and colloidal silicon dioxide (&g.» ProsoIvS SMCC).10[0063| to some embodiments, the sensory modifying agent is a sensate, a taste modifying agent, or a combination thereof, to one embodiment, the sensory modifying agent is a taste modifying agent that contains a sweetener and / or a flavoring agent to certain embodiments and consistent with toe definition of “a" above, the compositions contain more than one sensory modifying agent For example, in certain embodiments, the compositions contain more than one sensate and more than one flavoring agent(0064] A variety of different flavoring agents may be used, to certain embodiments, toe flavoring agent is a fruit flavor (e.g., apple, grape, strawberry, watermelon). Other suitable flavoring agents include but are not limited to mint, cinnamon, and bubble gum. In one embodiment, the flavoring agent is a mint (such as e.g., arvensis mint flavor), to another embodiment, the flavoring agent also includes a sweet Wintergreen flavor.(0065] to other embodiments, the sweetener is sucralose. A variety of sweeteners and / or flavoring agents are suitable, to one embodiment, the sweetener is stevia^ aspartame, acesulfame potassium, cyclamate salts, neotame, sugar alcohols and saccharin.

[0666] to one embodiment, the sensory modifying agent is a sensate that imparts a cooling sensation. Examples of suitable cooling compounds include but are not limited to (1 R,2S,5R)-N-etoyl-2-isopr6pyl-5- methylcyclohexanecarboxamide, (1 R,2S,5R)-N~(4- (cyanomethyl)phenyl)-2- isopropyl-5-methylcyclohexanecarboxamide, and (lR,2S,5R)-2- isopropyl-5- methyl-N-(2-(pyridin-2-yl)ethyl)cyclohexanecarboxamide, menthyl lactate, 2- isopropyl-N,2,3- trimethylbutanamide, and ( IR^S^R)-2-isopropyl-5-methyl-N-(2-(pyridin- 2- yl)ethyl)cyclohexanecarboxamide. Other suitable cooling compounds are disclosed in WO 2009 / 140783, the disclosure of which is incorporated by reference as it pertains to cooling compounds, to other embodiments, toe sensory modifying agent is a sensate that imparts a warming, burning, or tingling sensation.|0067] to certain embodiments, the composition contains from about 1% w / w to about 10% w / w, alternatively from about 2 % w / w to about 9 % w / w, alternatively from about 2 % w / w to about 8 % w / w of a water soluble lubricant (such as e.g.. PEG).

[0068] In some embodiments, the composition contains from about 20% w / w to about 60%>w / w, alternatively, from about 20% w / w to about 55% w / w, from about 25% w / w to about 40% w / w of the binder. In other embodiments, the composition contains from about , 10% w / w to about 50% w / w, alternatively from about from about 10% w / w to about 40% w / w, alternatively from about from about 15% w / w to about 35% w / w of a binder selected from sodium carboxymethyl cellulose, mannitol, polyvinylpolypyrrolidone, microcrystalline cellulose, colloidal silicon dioxide, and combinations thereof.11{0069J In alternate embodiments, the composition contains more than 20% w / w, alternatively more than 22% w / w, alternatively more than 24% w / w, alternatively more than 26% w / w, alternatively more than 48% w / w of the binder.[06701 In other embodiments, the composition contains from about 0.1% w / w to about 9% w / w, alternatively from about 1% w / w to about 8% w / w, alternatively from about 1% w / w to about 7% w / w of PEG (e.g., PEG 4800, PEG 6000, and / or PEG 8000). In further embodiments, the composition contains from about 0.1% w / w to about 9% w / w, alternatively from about 1% w / w to about 8% w / w, alternatively from about 0.8% w / w to about 5% w / w of sodium carboxymethyl cellulose (e.g., croscarmellose sodium). In further embodiments, the composition contains Oom about 10% w / w to about 50% w / w, alternatively from about 15% w / w to about 45% w / w, alternatively from about 15% w / w to about 35% w / w of mannitol.[00711 In yet further embodiments, the composition can also contain from about 0.1% w / w to about 10% w / w, alternatively from about 1.5% w / w to about 9% w / w, alternatively from about 2% w / w to about 8% w / w of mixture of microcrystalline cellulose (MCC) and colloidal silicon dioxide (CSD) (eg., Prosolv® SMCC).[0072} In other embodiments, the compositions contain from about 0.1 % w / w to about 9% w / w, alternatively from about 0.5% W / w to about 8% w / w, alternatively from about 2% w / w to about 7% w / w, alternatively from about 0.1% w / w to about 40% w / w, alternatively from about 0.01% w / w to about 50% w / w of the sensory modifying agent. In further embodiments, the sensory modifying agent contains from about 0.01 % w / w to about 2% w / w, alternatively from about 0.2% w / w to about 1.5% w / w, alternatively from 0.5% w / w to about 1.5% w / w of a sweetener (e.g., sucralose) and / or from about 0.1% w / w to about 7% w / w, alternatively from about 0.5% w / w to about 6.5% w / w, alternatively from about 1% w / w to about 6% w / w of a flavoring agent (e.g., mint) (by w / w of die composition). [0073[ One aspect of the disclosure is directed to effervescent tablets that contain fluoride. Generally, the effervescent tablets contain fluoride,an effervescent agent having an acid and a base component, a water soluble lubricant, a binder, and a sensory modifying agent The effervescent tablets of the disclosure are preservative free (i.e., they do not include any added preservative). The tablets of the disclosure are also alcohol free (i.e., they do not contain an alcohol as a tablet and / or when dissolved in water). The tablets can also contain a colorant and / or a bulking agent[0674} Accordingly, in certain embodiments of the disclosure, the compositions are effervescent tablets. The effervescent tablets can have any of the features described above.12In some embodiments, the effervescent tablets contain of the anticaries active ingredient (such as e.g-, fluoride), an effervescent agent having an acid and a base component, a water soluble lubricant, a binder, and a sensory modifying agent.[00751 The effervescent agent may contain an acid and a base in a ratio of acid:base (% w / w) of 1:9 to 1:3, alternatively 1:8 to 1:4, alternatively 1:7 to 1:5. In some embodiments, the effervescent agent contains citric acid as the acid. Other suitable acids include but are not limited to tartaric acid, malic acid, fumaric acid, adipic acid, acid citrates, and / or succinic acid.

[0076] In certain embodiments, the tablet contains fluoride, acid, and base in a ratio of fluoride:acid:base of 1:1.5:12 to 1:3:17, alternatively in a ratio of 1:1.8:13 to 1:3.4:16, alternatively in a ratio of 1:1.9: 12 to 1:3:15. In other embodiments, die ratio of acid:base in effervescent agent is 1:9 to 1:3, alternatively 1:8 to 1 :4, alternatively 1:7 to 1:5.[0077| In other embodiments, the effervescent agent contents bicarbonate (such as e.g., sodium bicarbonate) as the base. Other suitable bases include but are not limited to sodium carbonate, potassium carbonate, sodium bicarbonate, potassium bicarbonate, calcium bicarbonate, magnesium carbonate, sodium glycocarbonate, and / or carboxy lysine.[0078| In alternate embodiments, the effervescent agent contains citric acid as the acid and bicarbonate (such as e.g., sodium bicarbonate) as the base, to yet alternate embodiments, the effervescent agent contains bicarbonate (such as e.g., sodium bicarbonate) as the only base (r.e.. no other base is present in the effervescent agent), in a farther embodiment, the effervescent agent contains citric acid as the only acid and bicarbonate (such as e.g., sodium bicarbonate) as the only base (£<?., no other add or base is present in die effervescent agent), to one embodiment, sodium bicarbonate is the only base. (0079| to some embodiments, the effervescent tablet contains: an anticaries active ingredient: an effervescent agent comprising an acid and a base in a ratio of acid:base (% w / w) of 1 :9 to 1:3; a water-soluble lubricant selected from polyethylene glycol (PEG), potassium sorbate, sodium benzoate, calcium sorbate, PEG with ohe or more of trisodium citrate, calcium ascorbate, and mixtures thereof; a binder selected from sodium earboxymethyl cellulose, mannitol, polyvinylpolypyrrolidone, microcrystalline cellulose, colloidal silicon dioxide, and combinations thereof; and a taste modifying agent (0086| In one embodiment, the effervescent tablet contains: fluoride (e.g., sodium fluoride); an effervescent agent comprising an acid and a base in a ratio of acid:base (% w / w) of 1 :9 to 1 :3; a water-soluble lubricant selected from polyethy lene glycol (PEG), potassium sorbate, sodium benzoate, calcium sorbate, PEG with one or more of trisodium13citrate, calcium ascorbate, and mixtures thereof; a binder selected from sodium carboxymethyl cellulose, mannitol, poly vinylpolypyrrolidone, microcrystalline cellulose, colloidal silicon dioxide, and combinations thereof; and a sensory modifying agent In another embodiment, the effervescent tablet contains: sodium fluoride; an effervescent agent comprising citric acid and a bicarbonate base in a ratio of acid:base (% w / w) of 1 :9 to 1 :3; a binder containing PEG, sodium carboxymethyl cellulose, mannitol, and a combination of microcrystalline cellulose and colloidal silicon dioxide; and a sensory modifying agent In yet another embodiment, die effervescent tablet contains: sodium fluoride; an effervescent agent comprising citric acid and sodium bicarbonate in a ratio of acidibase (% w / w) of 1:9 to 1 :3; PEG 6000; a binder containing polyvinylpolypyrrolidone, croscarmellose sodium, and mannitol; and a sensory modifying agent(0081 j The acid and the base may be present ht an amount of from about 1% w / w to about 60% w / w of the acid and / or inan amount of from about 15% w / w to about 65% w / w of the base.[00821 la certain embodiments, the effervescent agent contains from about 1% w / w to about 60% w / w, alternatively from about to 5% to about 20% w / w; alternatively, from about 3% w / w to about 50% W / w, alternatively from about 5% w / w to about 35% w / w of the acid (w / w of the tablet). In other embodiments, the effervescent agent contains from about 1 % w / w to about 60% w / w, alternatively from about to 5% to about 20% w / w; alternatively, from about 3% w / w to about 50% w / w, alternatively from about 5% w / w to about 35% w / w of citric acid (w / w of the tablet).(0083 j In other embodiments^ die effervescent agent contains from about 15% w / w to about 65% w / w, altematively from about 20% w / w to about 60% w / w, alternatively from about 35% w / w to about 55% w / w of the base (w / w of the tablet). In further embodiments, the effervescent agent contains from about 15% w / w to about 65% w / w, altematively from about 20% w / w to about 60% w / w, altematively from about 35% w / w to about 55% w / w of bicarbonate (e,g., sodium bicarbonate) (w / w of the tablet).(0084| In additional embodiments, the effervescent agent contains from about 1 % w / w to about 60% w / w, altematively from about to 5% to about 20% w / w; altematively from about 3% w / w to about 50% w / w, altematively from about 5% w / w to about 35% w / w of die acid and from about 15% w / w to about 65% w / w, altematively from about 20% w / w to about 60% w / w, altematively from about 35% w / w to about 55% w / w of the base (w / w of the tablet). Altematively, the effervescent agent contains from about 1% w / w to about 60% w / w, altematively from about to 5% to about 20% w / w; alternatively from about 3% w / w to 14about 50% w / w, alternatively from about 5% w / w to about 35% w / w of Citric acid and from about 15% w / w to about 65% w / w, alternatively from about 20% w / w to about 60% w / w, alternatively from about 35% w / w to about 55% w / w of bicarbonate (e.g., sodium bicarbonate) (w / w of the tablet).

[0085] In some embodiments, the composition is an effervescent tablet that contains:• from about 1% w / w to about 10% w / w, alternatively from about 1% w / w to about 9% w / w. alternatively from about 1% w / w to about 8% w / w, fiom about 1% w / wto about 7% w / w, alternatively fiom about 1% w / w to about 6% w / w, alternatively from about 2% to about 8%, alternatively from about 2% w / w to about 6% w / w, alternatively fiom about 2% to about 6% w / w, alternatively from about 4% w / w to about 6% w / w of fluoride sodium fluoride):• from about 1% w / wto about 60% w / w, alternatively fiom about to 5% to about 20% w / w; alternatively, from about 3% w / w to about 50% w / w, alternatively from about 5% w / wto about 35% w / w acid (e.g., citric acid); from about 15% w / w to about 65% w / w, alternatively from about 20% w / w to about 60% w / w, alternatively fiom about 35% w / w to about 55% w / w of base (e.g., sodium bicarbonate);. from about 0.1% w / w to about 9% w / w, alternatively from about 1% w / w to about 8% w / w, ahematively from about 1% w / w to about 5% w / w of PEG (e.g., PEG 4800. PEG 6000, and / or PEG 8000);• from about 0.1% w / w to about 9% w / w, alternatively fiom about 1% w / w to about 8% w / w, alternatively fiom about 1% w / w to about 5% w / w of sodium carboxymethyl cellulose (e.g., croscarmellose sodium);• from about 10% w / w to about 50% w / w, alternatively fiom about 15% w / w to about 45% w / w, ahematively from about 15% w / w to about 35% w / w of mannitol; and / or• from about 0.1% w / w to about 9% w / w, alternatively from about 0.5% w / w to about 8% w / w, alternatively fiom about 2% w / w to about 7% w / w of a sensory modifying agentThe sensory modifying agent may contain from about 0.01% w / wto about 2% w / w, alternatively from about 0.2% w / w to about 1.5% w / w, altemati vely from 0.5% w / w to about 15% vtfw of a sweetener (e.g., sucralose) and / or from about 0.1% w / w to about 7% w / w, alternatively from about 0.5% w / w to about 6.5% w / w, ahematively from about 1% w / w to about 6% w / w of a flavoring agent (e.g., mint) (by w / w of the composition).

[0086] In other embodiments, the effervescent tablet contains:15• from about 1% w / w to about 10% w / w, alternatively Brom about 1% w / w to about 9% w / w, alternatively from about 1% w / w to about 8% w / w, from about 1 % w / w to about 7% w / w, alternatively from about 1% w / w to about 6% W / w, alternatively Brom about 2% to about 8%, alternatively from about 2% w / w to about 6% w / w, alternatively from about 2% to about 6% w / w, alternatively from about 4% w / w to about 6% w / w of sodium fluoride;• from about 1% w / w to about 60% w / w, alternatively from about to 5% to about 20% w / w; alternatively, from about 3% w / w to about 50% w / w, alternatively from about 5% w / w to about 35% w / w of citric acid;• from about 15% w / w to about 65% w / w, alternatively from about 20% w / w to about 60% w / w, alternatively from about 35% w / w to about 55% w / w of sodium bicarbonate;• from about 0.1% w / w to about 9% w / w, alternatively from about 1% w / w to about 8% w / w, alternatively from about 1% w / w to about 5% w / w of PEG 6000;• from about 0.1% w / w to about 9% w / w, alternatively from about 1% w / w to about 8% w / w, alternatively from about 1% w / w to about 5% w / w of croscarmellose sodium;• from about 10% w / w to about 50% w / w, alternatively from about 15% w / w to about 45% w / w, alternatively from about 15% w / w to about 35% w / w of mannitol; and• from about 0. 1 % w / w to about 9% w / w, alternatively from about 0.5% W / w to about 8% w / w, alternatively from about 2% w / w to about 7% w / w of a sensory modifying agent.The sensory modifying agent may contain from about 0.01% w / w to about 2% w / w, alternatively from about 0.2% w / w to about 1.5% w / w, alternatively from 0.5% w / w to about 1.5% w / w of a sweetener sucralose) and / or from about 0.1% w / w to about 7% w / w, alternatively from about 0.5% w / w to about 6.5% w / w, alternatively from about 1 % w / w to about 6% w / w of a flavoring agent (e.g„ mint) (by w / w of the tablet).(0087| In certain embodiments, the tablets of the disclosure are stable for at least two years.(0088| One embodiment of the disclosure is an effervescent tablet containing: sodium fluoride; an effervescent agent having an acid and a base in a ratio of acid:base (% w / w) of 1.9 to l .3 a water soluble lubricant selected from polyethylene glycol (PEG), potassium sorbate, sodium benzoate, calcium sorbate, PEG with one or more of trisodium citrate, calcium ascorbate, and mixtures thereof; a binder selected from sodium carboxymethy! cellulose, mannitol, polyvinylpolypyrrolidone, microcrystalline cellulose, colloidal silicon dioxide, and combinations thereof; and a taste modifying agent The tablet can also contain16a variety of other components. In one embodiment, the tablet contains a colorant, In One embodiment, the effervescent agent contains citric acid and sodium bicarbonate. In another embodiment, the effervescent agent contains citric acid and sodium bicarbonate, with citric acid and sodium bicarbonate being the only acid and the only base, respectively. In certain embodiments, the taste modifier includes a sweetener and a flavoring agent, such as e.g., sucralose and mint. In certain embodiments, the binder is croscarmellose sodium and mannitol. Other embodiments, citric acid is the only acid. In further embodiments, sodium bicarbonate is the only base.(0089) Another embodiment of the disclosure is an effervescent tablet containing: sodium fluoride; citric acid and sodium bicarbonate in a ratio (% w / w) of 1:7 to 1 :5 as an effervescent agent; PEG (eg., PEG6000); mannitol; croscarmellose sodium; polyvinylpolypyrrolidone; and a taste modifying agent. An alternate embodiment of the disclosure is an effervescent tablet containing: sodium fluoride; citric add and sodium bicarbonate in a ratio (% w / w) of 1 :9 to 1 :3 as an effervesced agent; PEG (eg., PEG6000); mannitol; croscarmellose sodium; polyvinylpolypyrrolidone; and a taste modifying agent. Yet another embodiment is an effervescent tabletcontaining: sodium fluoride; citric add and sodium bicarbonate in a ratio (% w / w) of 1:8 to 1:4 as ah effervescent agent; PEG (eg., PEG6000); mannitol; croscarmellose sodium; polyvinylpolypyrrolidone; and a taste modifying agent(0090 j Exemplary embodiments of effervescent tablets of the disclosure are shown in the Tables below. Any amount for one component (eg, anticaries agent) may be combined withany of the other amounts listed for any other component in any other embodiment (eg., water soluble lubricant).Component Embodiment Al Embodiment Bl Embodiment Cl an anticaries active from about 0.1% from about 0.2% from about 02% ingredient (eg., fluoride w / w to about 10% w / w to about 6% w / w to about 4% (sodium fluoride)) w / w w / w w / w effervescent agent from about 30% from about 35% from about 35% w / w to about 85% w / w to about 80% w / w to about 60% w / w w / w w / w a water soluble lubricant from about 1% from about 2 % from about 2 % selected from w / w to about 10% w / w to about 9 % w / w to about 8 % polyethylene glycol w / w w / w w / w (PEG), potassium Sorbate, sodium benzoate, calcium17Component Embodiment Al Embodiment Bl Embodiment Cl sorbate, PEG with one or more of trisodium citrate, calcium ascorbate, and mixtures thereof a binder selected from from about 10% from about 10% from about 15% sodium carboxymethyl w / w to about 50% w / w to about 40% w / w to about 35% cellulose, mannitol, w / w w / w w / w polyvinylpolypyrrolidone, microcrystalline cellulose, colloidal silicon dioxide, and combinations thereof a senstory modifying from about 0.1% from about 0.5% from about 1%' agent w / w to about 10% W / w to about 7% w / w to about 6 % w / w w / wRatio of acid:base in 1.9 to 13 1:8 to 1:4 1:7 to 1:5 effervescent agentRatioof 1:1.5:12 to 1:3:17 l:1.8:13to 1:1.9:12 to 1:3:15 fluoride:acid:base 1:3.4:16Component Embodiment A2 Embodiment B2 Embodiment C2 an anticaries active from about 0.1% from about 0.2% from about 6.2% ingredient (e.g., fluoride w / w to about 10% w / w to about 6% w / w to about 4% (sodium fluoride)) w / w w / w w / w effervescent agent from about 30% from about 35% from about 35% w / w to about 85% w / w to about 80% w / w to about 60% w / w w / w w / w a water soluble lubricant from about 1% from about 2 % from about 2 % selected from w / w to about 10% w / w to about 9 % W / w to about 8 % polyethylene glycol w / w w / w w / w (PEG), potassium sorbate, sodium benzoate, calcium sorbate, PEG with one or more of trisodium citrate, calcium ascorbate, and mixtures thereof18Component Embodiment A2 Embodiment 82 Embodiment C2 sodium carboxymethyl from about 10% from about 10% from abodt 15% cellulose, mannitol, and w / w to about 50% w / w to about 40% w / w to about 35% polyvinylpolypyrrolidone, w / w w / w w / w a sensory modifying from about 0.1% from about 0.5% from about 1% agent w / w to about 10% w / w to about 7% w / w to about 6 % w / w w / wRatio of acid:base in ).9to l3 1:8 to .1:4 1:7 to 1:5 effervescent agentRatio of 1:1.5:12 to 1:3:17 l:1.8:13to l:1.9:12 to l:3:15 fluoride;acid:base 13.4:16Component Embodiment A3 Embodiment 83 Embodiment C3 fluoride (sodium from about 0.1% from about 0.2% from about 0.2% fluoride) w / w to about 10% w / w to about 6% w / w to about 4% w / w . w / w w / w effervescent agent (citric from about 30% from about 35% from about 35% acid and sodium w / w to about 85% w / w to about 80% w / w to about 60% bicarbonate) w / w w / w w / wPEG (PEC 4800, PEG from about 1% from about 2% from about 2 % 6000, or PEG 8000) w / w to about 10% w / w to about 9 % w / w to about 8 % w / w w / w w / w mannitol, from about 10% from about 10% from about 15% polyvinylpolypyrrolidone w / w to about 50% w / w to about 40% w / w to about 35% and croscarmellose w / w w / w w / w sodium a sensory modifying from about 0.1% from about 0.5% from about 1% agent w / w to about 10% W / w to about 7% w / w to about 6 % w / w w / wRatio of acid.'base in 1.9 to 13 1:8 to 1:4 1:7 to 1:5 effervescent agentRatio of 1:1.5:1210 1:3:17 1:1.8:13 to 1:1.9:12 to 1:3:15 fluoride:acid:base 1:3.4:16[00911 In some embodiments, the compositions of die disclosure can also contain a colorant.19.{0092] Iti other embodiments, the effervescent tablets of the disclosure are formulated so that die tablets when dissolved in water result in a 0.02-percent or 0.05-percent aqueous solution containing sodium fluoride with a pH of from about 5.5 to about 8.5, alternatively about approximately 7.Containers eitd tits{0093] Another aspect of the disclosure is directed to containers, packaging, and / or kits containing the compositions or effervescent tablets of the disclosure.{0094] In certain embodiments, compositions, or tablets are individually wrapped, for example in a sachet or blister package. In other embodiments, the composition or tablets are loose packed such as for example in a multi-pill container (eg., a bottle, carton, or pouch).(009SJ One embodiment of the disclosure is directed to a container containing the effervescent tablets of the disclosure. In one embodiment, the container is a pill bottle. The container may also include a label with instructions for use.{0896] Another embodiment of the disclosure is directed to a blister package containing effervescent tablets of the disclosure. One embodiment is a blister package arranged in rows and columns each containing an effervescent tablet of the disclosure.{0997] Another embodiment of the disclosure is directed to kits containing the blister packagers or the containers described above. The kits include a dose cup. The dose cup is calibrated for a suitable amount of water to dissolve the tablets of die disclosure (such as e.g., 10 mUtablet). The kit may also include instructions for mixing the tablets with water.

[0098] In certain embodiments, the kit includes instructions for mixing the tablets with water to result in a 0.02-percent or 0.05-percent aqueous solution containing sodium fluoride with a pH of approximately 7. In other embodiments, the instructions are in compliance with 21 C.F.R. § 355.10.{0099] The disclosure is also directed to using the compositions of the disclosure, such as e.g. , the tablets of the disclosure, to improve oral and / or dental health. In one embodiment, die method includes providing the tablets of the disclosure, adding a suitable amount of water (such as e.g., about 10 ml) to allow the tablets to disintegrate and dissolve, aid then rinsing the mouth of a patient In certain embodiments, the tablets when dissolved form a200,02 -percent or 0,05-percent aqueous solution containing; sodium fluoride with a pH of approximately 7.[0100| Other embodiments ate directed to use of a liquid composition containing die tablets of the disclosure to improve oral and / or dental health.[01011 Without furflier description, it is believed that one of ordinary skill in the art can, using tiie preceding description and the following illustrative examples, make and utilize the present invention and practice the claimed methods. The following working examples therefore specifically point out tiie preferred embodiments of the present invention, and are hot to be construed as limiting in any way tiie remainder of the disclosure.EMBODIMENTS[0102| The invention provides also the following non-limiting embodiments.[01031 Embodiment 1 is a composition comprising an anticaries active ingredient and a sensory modifying agent that dissolves in water.[0104} Embodiment! is the composition of embodiment 1, wherein the composition forms a mouthrinse when combined with water.[0105| Embodiment 3 is the composition of embodiments 1 and 2, wherein tiie anticaries active ingredient is fluoride.[0106| Embodiment 4 is the composition of any one of embodiments 1 to 3 further comprising a water-soluble lubricant.[0107} Embodiment 5 is the composition of any one of embodiments I to 4. wherein the sensory modifying agent is a senrate, a taste modifying agent, ora combination thereof.[0108} Embodiment 6 is the composition of embodiment 5 wherein die sensory modifying agent is a senate that imparts a cooling sensation, a warming sensation, a burning sensation, and / or tingling sensation.[0109} Embodiment 7 is the composition of embodiment 6, wherein the senate is (lR,2S,5R)-N-ethyl-2-isopropyl-5- methylcyclohexanecarboxamide, (1R,2S,5R)-N~(4- (cyanomethyl)phenyl)-2- isopropyl-5-methylcyclohexanecarboxamide, and (lR,2S,5R)-2- isopropyl-5- methyl-N-(2-(pyridin-2-yl)ethyl)cyclohexanecarboxamide, menthyl lactate, 2- isopropyl-N,2,3- trimethylbutanamide, and (IR,2S,5R)-2-isopropyl-5-methyl-N-(2-(pyridin- 2- yl)ethyl)cyclohexanecaiboxamide, and a combination thereof.(0110} Embodiment 8 is tiie composition of any one of embodiments 1 to 7. wherein the composition further comprises a tinder selected from sodium carboxymethyl cellulose,21mannitol, polyvinylpolypyrrolidone, microcrystallint; cellulose, colloidal silicon dioxide, and combinations thereof.(0111) Embodiment 9 is the composition of my one of embodiments 1 to 8, wherein the composition further comprises a water-soluble lubricant selected from polyethylene glycol (PEG), potassium sorbate, sodium benzoate, calcium sorbate, PEG with one or more of trisodium citrate, calcium ascorbate, and mixtures thereof.(0112) Embodiment 10 is the composition of any one of embodiments I to 9, wherein the composition is formulated as an effervescent powder, a non-effervescent powder, a compressed tablet, an effervescent tablet, a iron-effervescent tablet, a liquid concentrate, or a water free liquid concentrate.(0113) Embodiment 11 is the composition of embodiment 1 , wherein the composition is an effervescent tablet comprising: an anticaries active ingredient; an effervescent agent comprising an acid and a base in a ratio of addibase (% w / w) of 1 :9 to 1 :3; a water-soluble lubricant selected from polyethylene glycol (PEG), potassium sorbate, sodium benzoate, calcium sorbate, PEG with one or more of trisodium citrate, calcium ascorbate, and mixtures thereof; a binder selected from sodium carboxymetbyl cellulose, mannitol, polyvinylpolypyrrolidone, microcrystalline cellulose, colloidal silicon dioxide, and combinations thereof; and a taste modifying agent.(6114) Embodiment 12 is the composition of embodiment 11, wherein the composition is an effervescent table comprising: fluoride; an effervescent agent comprising an acid and a base in a ratio of acid:base (% w / w) of 1 :9 to J :3; a water-soluble lubricant selected from polyethylene glycol (PEG), potassium sOrbate, sodium benzoate, calcium sorbate, PEG with one or more of trisodium citrate, calcium ascorbate, and mixtures thereof, a binder selected from sodium carboxymethyl cellulose, manhitoL polyvinylpolypyrrolidone, and combinations thereof; and a sensory modifying agent16115) Embodiment 13 is the composition of embodiment 12, wherein the fluoride is sodium fluoride.(0116) Embodiment 14 is the canposition of any one ofembodiments 11 to 13, wherein tfie composition comprises fluoride, acid, and base in a ratio of fluoride;acid:baseof 1:1.5:12 to 1:3:17.(0117) Embodiment 15 is the composition ofany one ofembodiments 11 to 14, wherein the effervescent agent comprises citric acid.(0118) Embodiment 16 is the canposition of any one of embodiments 11 to 15 whereto the effervescent agent comprises bicarbonate.22

[0119] Embodiment 17 is the composition of embodiment 16, wherein the bicarbonate is sodium bicarbonate.[0120 j Embodiment 18 is the composition of embodiment 17, wherein bicarbonate is the only base.[01211 Embodiment 19 is the composition of any one of embodiments 8 to 18, wherein the sodium carboxymethyl cellulose in the binder is croscarmellose sodium.

[0122] Embodiment 20 is the composition of any one of embodiments 11 to 19, wherein the sensory modifying agent is a sensate, a taste modifying agent, or a combination thereof. [0123| Embodiment 21 is the composition of embodiment 20 wherein the sensory modifying agent is a senate that imparts a cooling sensation, a warming sensation, a burning sensation, and / or tingling sensation.[0124 j Embodiment 22 is the composition of embodiment 21 , wherein the senate is (1 R.2S,5R)-N-ethyl-2-isopropyl-5- methylcyclohexanecarboxamide, ( 1 R,2S,5R)-N~(4- (cyanomethyl)phenyl)-2- isopropyl-5-methylcyclohexanecarboxamide, and (lR,2S,5R)-2- isopropyl-5- methyl-N-(2-(pyridin-2-yl)ethyl)cyclohexanecarboxamide, menthyl lactate, 2- isopropyl-N.2,3- trimethylbutanamide, and (IR3S3R)-2-isopropyl-5-methyl-N-(2-(pyridin- 2- yl)ethyl)cyclohexanecarboxamide, and a combination thereof.

[0125] Embodiment 23 is the composition of any one of embodiments 11 to 22, wherein the composition forms a mouthrinse when combined with water.

[0126] Embodiment 24 is the composition of any one of embodiments 8 to 23, wherein the binder is sodium carboxymethyl cellulose, mannitol and polyvinylpolypyrrolidone. (0127) Embodiment 25 is the composition of any one of embodiments 9 to 24, wherein the water soluble lubricant is PEG.[0128| Embodiment 26 is the composition of embodiment 25, wherein the PEG is PEG 4800, PEG 6000, or PEG 8000.[0129) Embodiment 27 is the composition of embodiment 26, wherein the PEG is PEG 6000.[0130| Embodiment 28 is the composition of any one of embodiments 25 to 27, wherein the composition comprises from about 0.1% w / w to about 10% w / w of PEG.[01311 Embodiment 29 is the composition Of embodiment 1 , wherein the composition is an effervescent tablet comprising: sodium fluoride; an effervescent agent having an add and a base in a ratio of acid:base (% w / w) of 1.9 to 1.3; a water-soluble lubricant selected from polyethylene glycol (PEG), potassium sorbate, sodium benzoate, calcium sorbate, PEG with one or more of trisodium citrate, calcium ascorbate, and mixtures thereof; a binder selected23from sodium carboxymethyl cellulose, mannitol, polyvinylpolypyrrolidone, microcrystalline cellulose, colloidal silicon dioxide, and combinations thereof; and a sensory modifying agent.[0132| Embodiment 30 is the composition of embodiment 29, wherein the effervescent agent comprises citric acid and sodium carbonate.[0133| Embodiment 31 is the composition Of embodiment 30, wherein citric acid is the only acid and wherein sodium carbonate is the only base in the effervescent agent.[0134, Embodiment 32 is the composition ofany one of embodiments 30 to 31, wherein die water soluble lubricant is PEG.

[0135] Embodiment 33 is the composition of any one of embodiments 30 to 32, wherein the binder comprises croscarmeilose sodium and mannitol.,0136, Embodiment 34 is the composition of anyone embodiments 30 to 33, wherein the composition comprises: from about 0.1% w / w to about 10% w / w of sodium fluoride; from about 30% w / w to about 85% w / w of the effervescent agent; from about 1 % w / w to about 10% w / w of the water soluble lubricant; from about 10% w / w to about 50% w / w of tire binder; and / orfrom about 0.1% w / w to about 10% w / w of tire sensory modifying agent. (0137, Embodiment 35 is the composition of embodiment I , wherein the composition is an effervescent tablet comprising: sodium fluoride; citric acid and sodium bicarbonate in a ratio (% w / w) of 1 ;7 to 1 :5 as an effervescent agent; PEG; mannitol; croscarmeilose sodium; and a sensory modifying agent[0138, Embodiment 36 is the canposition of embodiment 35, wherein the PEG is PEG 6000.

[0139] Embodiment 37 is the canposition of embodiments 35 and 36, wherein the composition comprises; from about 0.1% w / w to about 10% w / w of sodium fluoride; from about 30% w / w to about 85% w / w of the effervescent agent; from about 1% w / w to about 10% w / w of PEG; from about 10% w / w to about 50% w / w of die binder; and / or from about 0.1% w / w to about 10% w / w of the sensory modifying agent, wherein the binder is mannitol and croscarmeilose sodium.,0140] Embodiment 38 is the composition ofany one of embodiments 1 to 37. wherein die composition is preservative-free.

[0141] Embodiment 39 is the composition of any one of embodiments 1 to 38, wherein die composition is alcohol-free.

[0142] Embodiment 40 is the canposition of any one of embodiments 1 to 39, wherein the composition dissolves in water in two minutes or less.24(01431 Embodiment 41 is a container comprising the composition tablet of any one of embodiments 1 to 40.(0144) Embodiment 42 is a blister package comprising the composition of any one of embodiments 1 to 40.(0145) Embodiment 43 is the blister package of embodiment 42, wherein the composition is a tablet(O146| Embodiment 44 is a kit comprising a dose cup and a canposition of any one of embodiments 1 to 40, a container of embodiment 42 or a blister package of embodiment 44. (0147] Embodiment 45 is the kit of embodiment 44 further comprising instructions fpr mixing with water.25

Claims

CLAIMSWhat is claimed is*.

1. A composition comprising an anticaries active ingredient and a sensory modifying .. agent that dissolves in water.

2. The composition of claim 1 , wherein the composition forms a mouthrinse when combined with water.

3. The composition of claims 1 and 2, wherein the anticaries active ingredient is fluoride.

4. The composition of any one of claims 1 to 3 further comprising a water-soluble lubricant5. The composition of any one of claims 1 to 4, wherein the sensory modifying agent is a sensate, a taste modifying agent, or a combination thereof.& The composition of claim 5, wherein the sensory modifying agent is a senate that imparts a cooling sensation, a warming sensation, a burning sensation, and / or tingling sensation.

7. The composition of claim 6. wherein the sensate is ( I RJ2S,5R)-N-ethyl-2-isopropyl-5- methylcyclohexanecarboxamide, (lR,2S,5R)-N~(4-(cyanomethyl)phenyl)-2- isopropyl- 5-methylcyclohcxanecarboxamide, and (lR^2S,5R)-2-isopropyl-5- methyI-N-(2-(pyridin-2- yl)ethyl)cyclohexanecarboxamide, menthyl lactate, 2-isopropyl-N,2.3- trimethylbutanamide, and ( lI<2S.5R)-2-isopropyl-5-methyl-N-(2-(pyridin-2- yl)ethyl)cyclohexanecarboxamide, and a combination thereof.

8. The composition of any one of claims 1 to 7, wherein the composition further comprises a binder selected from sodium carboxymethyl cellulose, mannitol, polyvinylpolypyrrolidone, microcrystalline cellulose, colloidal silicon dioxide, and combinations thereof.

9. The composition of any one of chums 1 to & wherein the composition further comprises a water-soluble lubricant selected from polyethylene glycol (PEG), potassium26sorbate, sodium benzoate, calcium sorbate, PEG with one or more of trisodium citrate, calcium ascorbate, and mixtures thereof.

10. The composition of any one of claims I to 9, wherein the composition is formulated as ah effervescent powder, a non-effervescent powder, a compressed tablet, an effervescent tablet, a non-effervescent tablet, a liquid concentrate, or a water free liquid concentrate.

11. The composition of claim I , wherein the composition is an effervescent tablet comprising: an anticaries active ingredient; an effervescent agent comprising an add and a base in a ratio of acidtbase (% w / w) of T:9 to l:3; a water-soluble lubricant selected from polyethylene glycol (PEG), potassium sorbate, sodium benzoate, calcium sorbate, PEG with one or more of trisodium citrate, calcium ascorbate, and mixtures thereof; a binder selected from sodium carboxymetiiyl cellulose, mannitol, polyvinylpolypyrrolidone, microcrystalline cellulose, colloidal silicon dioxide, and combinations thereof; and a taste modifying agent.

12. The composition of claim 11, wherein the composition is an effervescent tablet comprising: flubride; an effervescent agent comprising an acid and a base in a ratio of acidtbase (% w / w) of 1:9 to 1:3; a water-soluble lubricant selected from polyethylene glycol (PEG), potassium sorbate, sodium benzoate, calcium sorbate, PEG with one or more of trisodium citrate, calcium ascorbate, and mixtures thereof; a binder selected from sodium carboxymethyl cellulose, mannitol, polyvinylpolypyrrolidone, and combinations thereof; and a sensory modifying agent2713. The composition of claim 12, wherein toe fluoride is sodium fluoride,14. The composition of any one of claims 11 to 13, wherein toe composition comprises fluoride, acid, and base in a ratio of fluoride:acid:base of 1:1.5:12 to 1:3:17.

15. The composition of any one of claims 11 to 14, wherein the effervescent agent comprises citric acid.

16. The composition of any one of chums 11 to 15 wherein the effervescent agent comprises bicarbonate.

17. The composition of claim 16, wherein the bicarbonate is sodium bicarbonate.

18. The composition of claim 17, wherein bicarbonate is the only base.

19. The composition of any one of claims 8 to 18, wherein tire sodium carboxymethyi cellulose in the binder is croscarinellose sodium.

20. The composition of any one of claims 11 to 19, wherein the sensory modifying agent is a sensate. a taste modifying agents or a combination thereof.

21. The composition of claim 20 wherein the sensory modifying agent is a senate that impels a cooling sensation, a warming sensation, a burning sensation, and / or tingling sensation.

22. The composition of claim 21, wherein toe sensate is (lR2S,5R)-N-ethyl-2- isopropyl-5- methylcyclohexanecarboxamide, (lR2S,5R)-M~(4-(cyanomethyl)phenyl)-2- isopropyl-5-methylcyclohexanecarboxamide, and ( 1 R2S.5R)-2-isopropyl-5- methy l-N-(2- (pyridin-2-yl)ethyl)cyclohexanecaTboxamide, menthyl lactate, 2-isopropyl-N2,3- trimethylbutanarnide, and (lR2S^5R)-2-isopropyl-5-methyl-N-(2-(pyridin-2- yl)ethyl)cyclohexanecarboxamide, and a combination thereof.23, •_ The composition of arty one of claims 11 to 22, wherein toe composition forms a mouthrinse when combined with water.

24. The Composition of any one of claims 8 to 23, wherein toe binder is sodium carboxymethyi cellulose, mannitol and polyvinylpoiypyrrolidone.

25. The composition of any one of claims 9 to 24, wherein the water soluble lubricant isPEG.2826. The composition of claim 25, wherein die PEG is PEG 4800, PEG 6000, or PEG8000.

27. The composition of claim 26, wherein die PEG is PEG 6000128. The canposition of any one of claims 25 to 27, wherein the composition comprises from about 0.1% w / w to about 10%w / w ofPEG.

29. The composition of claim 1 , wherein Ute composition is an effervescent tablet comprising: sodium fluoride; ati effervescent agent having an acid and a base in a ratio pf acid:base (% w / w) of 1.9 to 1.3; a water-soluble lubricant selected from polyethylene glycol (PEG), potassium sorbate, sodium benzoate, calcium sorbate, PEG with one or more Of trisodium citrate, calcium ascorbate, and mixtures thereof; a binder selected from sodium carboxymethyl cellulose, mannitol, polyvinylpolypyrrolidone, microcrystalline cellulose, colloidal silicon dioxide, and combinations thereof; and a sensory modifying agent30. The composition of claim 29, wherein the effervescent agent comprises citric acid and sodium carbonate.

31. The composition of claim 30, wherein citric acid is the only acid and wherein sodium carbonate is the only base in the effervescent agent.

32. The composition of any one of claims 30 to 31, wherein die water soluble lubricant is PEG.

33. The composition of any one of claims 30 to 32, wherein tire binder comprises croscarmellose sodium and mannitol.34, The composition of any one claims 30 to 33, wherein the composition comprises: from about 0.1% w / w to about 10% w / w of sodium fluoride;29from about 30% w / w to about 85% w / w of the effervescent agent; from about 1% w / w to about 10% w / w of the water soluble lubricant; from about 10% w / w to about 50% w / w of the binder; and / or from about 0.1% w / w to about 10% w / w of the sensory modifying agent.

35. The composition of claim 1, wherein the composition is an effervescent tablet comprising: sodium fluoride; citric acid and sodium bicarbonate in a ratio (% w / w) of 1 :7 to 1 :5 as an effervescent agent;$EG; mannitol; croscarmellose sodium; and a sensory modifying agent36. The composition of claim 35, wherein the PEG is PEG 6000.

37. The composition of claims 35 and 36, wherein the composition comprises: from about 0.1% w / w to about 10% w / w ofsodium fluoride; from about 30% w / w to about 85% w / w of the effervescent agent; from about 1% w / w to about 10% w / w of PEG; from about 10% w / w to about 50% w / w of toe binder; and / or from about 0.1 % w / w to about 10% w / w of toe sensory modifying agent, wherein the binder Is mannitol and croscarmellose sodium.

38. The composition of any one of claims I to 37, wherein the composition is preservative-free.

39. The composition of any one of claims 1 to 38, wherein the composition is alcohol- free.3040. The composition of any one of claims 1 to 39, wherein the composition dissolves in water in two minutes or less.

41. A container comprising the composition tablet of any one of claims I to 40.

42. A blister package comprising the composition of any one of claims 1 to 40.

43. The blister package of claim 42, wherein the composition is a tablet.

44. A Itifc comprising adose cup and a composition of any one of claims 1 to 40, a container of claim 42 or a blister package of claim 44.

45. The kit of claim 44 further comprising instructions for mixing with water.31

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