Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
  • A61K8/4973—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
  • A61K8/498—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
  • A61K8/22—Peroxides; Oxygen; Ozone
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
  • A61K8/42—Amides
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
  • A61K2800/42—Colour properties
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
  • A61K2800/42—Colour properties
  • A61K2800/43—Pigments; Dyes
  • A61K2800/434—Luminescent, Fluorescent; Optical brighteners; Photosensitizers
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
  • A61K2800/48—Thickener, Thickening system
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
  • A61K2800/52—Stabilizers
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
  • A61K2800/81—Preparation or application process involves irradiation
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
  • A61N5/00—Radiation therapy
  • A61N5/06—Radiation therapy using light
  • A61N5/0601—Apparatus for use inside the body
  • A61N5/0603—Apparatus for use inside the body for treatment of body cavities
  • A61N2005/0606—Mouth
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
  • A61N5/00—Radiation therapy
  • A61N5/06—Radiation therapy using light
  • A61N5/0613—Apparatus adapted for a specific treatment
  • A61N5/062—Photodynamic therapy, i.e. excitation of an agent

Definitions

• Peroxide and peroxyaeid compounds such as hydrogen peroxide and carbamide peroxide, are useful as bleaching agents in teeth whitening compositions.
• Appropriate heat, light, or chemical sources can accelerate the release of oxygen radicals from the peroxide or peroxyaeid compounds,
• Tooth sensitivity .following treatment, and the time required for teeth whitening compositions (typically requiring about an hour of time or multiple applications or both), however, remains a significant drawback.
• the present disclosure provides compositions for teeth whitening comprising an oxidizing agent and at least one chromophore.
• the present disclosure provides a composition comprising an oxidizing agent and Eosin Y and Fluorescein.
• present disclosure provides a composition comprising an oxidizing agent and Eosin Y, Fluorescein and Rose Bengal
• the present disclosure provides a composition comprising an oxidizing agent and Eosia Y and Rose Bengal.
• the present disclosure provides a composition comprising an oxidizing agent and Fluorescein and Rose Bengal.
• die present disclosure provides a composition comprising an oxidizing agent and Eosia Y, Fluorescein and Brythrosine.
• the oxidizing agent comprises hydrogen peroxide or carbamide peroxide or both, in certain embodiments, the hydrogen peroxide content is less man or equal to 6% by weight of hydrogen peroxide in the composition. In other aspects, the carbamide peroxide content is less than or equal to 22% by weight of carbamide peroxide in fhe composition in ofher aspects, the total content of the oxidizing agent is equi valent to about 6% by weight of Iiydrogen peroxide content.
• the composition further comprises a stabilizing agent.
• the composition further comprises a thickening agent.
• the thickening agent comprises silicon dioxide and/or famed silica having a particle size less than one micron.
• the composition further comprises a hydrophilic gelling agent.
• the hydrophilic gelling agent comprises polypropylene glycol, polyethylene glycol, propylene glycol glycerol, or a large molecular weight polyol, or any combination thereof.
• the composition further comprises a base.
• the base comprises potassium hydroxide.
• the pH of the composition is between 2 and . In other embodiments, the pH of the composition is between 4 and 8, preferably between 6 and 7, more preferably 6,5.
• Eosin Y is present in an amount of 0.001 % to 1 % weight per weight of the composition.
• Fluorescein is present in an amount of 0.001 % to 1 % weight per weight of the composition.
• Rose Bengal is present in an amount of 0.001 % to 1 % weight per weight of the composition
• Erythrosin is present in an amount of 0.001 % to 1 % weight per weight of the composition.
• kits for preparin and/or applying any of the compositions of the present: disclosure comprises a first component comprising an oxidizing agent; and a second component comprising Eosin Y and Fluorescein.
• the kit comprises a first component comprising an oxidizing agent: and second component comprising Eosin Y, Fluorescein and Rose Bengal, In other embodiments, the kit comprises a first component comprising an oxidizing agent and a second component comprising Eosin Y and Rose Bengal, in other embodiments, fhe kit comprises a first component comprising an oxidizing agent and a second component comprising Fluorescein and Rose Bengal In other embodiments, the kit comprises a first component comprising an oxidizing agent and a second component comprising Eosi Y, Fluorescein and Erythrosme.
• the first and second components additionally comprise a hydrophi!rc gelling agent.
• the kit additionally comprises an applicator comprising a tooth brightening composition.
• the kit additionally comprises a gingival barrier composition, in some embodiments, the kit: further comprises instructions for using the kit apparatus for mixing together the first and second components, a light source, or information for assessing the efficacy of the composition.
• the present disclosure also provides a method for whitening teeth comprising applying a composition of the disclosiire to at least one tooth and exposing the composition applied to the at least one tooth to actinic light
• each tooth is exposed to actinic light for about 1-30 seconds. In other embodiments, each tooth is exposed to actinic Sight, for about 3-10 seconds. In other embodiments, each tooth is exposed to the actinic light for about 5- i t ) seconds.
• FIG. 2 illustrates the absorption and emission spectra of donor and acceptor chromophores. The spectral overlap between the absorption spectrum of the acceptor chromophobe and the emission spectrum of the donor chromophore is also shown.
• Figure 3 is a schematic of a j bionski diagram that illustrates the eoupied transitions involved between a donor emission and acceptor absorbanee.
• Figures 4a and 4b are absorbanee and emission spectra, respectively, of an embodiment of the composition of the present invention, which includes Eosin and Fluorescein (Example I).
• Figures 5a and 5b are absorbanee and emission spectra, respectively, of an embodiment of the composition of the present invention which includes Eosin and Fluorescein in a ⁇ 2% carbamide gel (Example 7).
• Figures 6a and 6b arc absorbanee and emission spectra, respectively, of an embodiment of the composition of the present invention which includes .Eosin and f luorescein in an aqueous solution (Example 8).
• Figures 7a and 7b are absorbance and emission spectra, respectively, of an embodiment of the composition of the present invention which includes Eosin, Fluorescein and Rose Bengal in a 12% carbamide gel (Example 9),
• Figures 8a and 8b are absorbance and emission spectra, respectively, of an embodiment of the composition of the present invention which includes Eosin and Fluorescein in an aqueous solution (Example 10).
• the term "about'" in the contex t of a gi ven value or range refers to a value or range that is within 20%, preferably within 10%, and more preferably within 5% of the given value or range.
• accelerating agent ' ' refers to any agent capable of accelerating and/or contri buting to the completion of radical generation.
• actinic light is intended to mean Sight energy emitted from a specific light source (e.g. lamp, LED, or laser) and capable of being absorbed by matter (e.g. the chromophore or photoactivator defined below), la a preferred embodiment, the actinic light is visible light.
• a specific light source e.g. lamp, LED, or laser
• the actinic light is visible light.
• photosensitive agent refers to any agent capable of absorbing actinic tight.
• the photosensitive agent undergoes photoexcitation and transfers its energy. This may be in the form of emitted light (e.g. fluorescence) and-'or energy transferred to molecules. This energy may initiate chemical reactions.
• Photosensitive agents ma enhance and/or accelerate the dispersion of light energy, or otherwise enhance and/or activate the decomposition of an oxidizing agent.
• a chromophore means a chemical compound or a part of a chemical compound, which when contacted by light irradiation, is capable of absorbing the Sight. The chromophore readily undergoes photoexcitation and then emits energy such as by transferring its energy to other -molecules or by emitting light.
• “Gelling agent” means an agent that thickens and stabilizes liquid solutions, emulsions and suspensions,
• Oxidant' ' or "oxidizing agent” means a chemical compound that readily transfers oxygen, atoms and oxidizes other compounds and also includes precursors of compounds capable of oxidizing other compounds.
• compositions for teeth whitening are provided.
• the present disclosure provides a. composition comprising an. oxidizing agent and a photosensitive agent (e.g., comprising one or more chromophores), which, when activated by light, disperses the light energy, leading to the photochemical activation of the oxidant contained in the composition; which may lead to the formation of oxygen radicals, such as singlet oxygen.
• a photosensitive agent e.g., comprising one or more chromophores
• the present disclosure provides a first composition and. a second composition, wherein the first composition comprises an oxidizing agent and the second composition comprises a photosensitive agent, (e.g., comprising one or snore chromophores), which, when mixed with the first composition and subsequently acti vated by light, disperses the light energy, leading to the photochemical activation of the oxidant contained in the mixture, which may lead to the formation of oxygen radicals, such as singlet oxygen.
• a photosensitive agent e.g., comprising one or snore chromophores
• the present disclosure provides a composition or compositions comprising a photosensitive agent (e.g. comprising one or more chromophores), which when exposed to light, can be activated to initiate chemical reactions.
• a photosensitive agent e.g. comprising one or more chromophores
• the composition, or compositions can react with oxidizing species in, on, or applied to, the teeth, to have a teeth whitening effect,
• the present disclosure provides a composition or compositions comprising a photosensitive agent, said photosensitive agent comprising at least two chromophores having a synergistic effect together.
• the at least chromophores can be activated on exposure to light to initiate chemical reactions.
• the chemical reactions may include oxidizing species in, on, or applied to, the teeth, to have a teeth whitening effect.
• compositions of the present disclosure may be described based on the components making up the composition. Additionally or alternatively, the compositions of the present disclosure have functional and structural properties and these properties may also be used to define and describe the compositions. Indi vidual components of the composition of the present disclosure are detailed as below ,
• the composition of the present disclosure may comprise one or more photosensitive agents, e.g., chromophores.
• the terra ''chromophore' * (used herein interchangeably with "photosensitizing agent”, or “photosensitizer” or “photoactivator”) is intended to mean a part or whole of a chemical compound capable of absorbing actinic light.
• the chromophore readily undergoes pliotoexcitation and may then transfer its energy to other molecules. The energy transferal may also be in the form of emitted l ight or fluorescence.
• Suitable chromophores can be fluorescent dyes (or stains), a! though other dye groups or dyes (biological and histological dyes, food colorings, carotenoids) can also be used. Combining chromophores may increase photo-absorption by the combined dye molecules and enhance absorption and photo-bioraodulation selectivity. This creates multiple possibilities of generating new photosensitive, and/or selective chromophores mixtures. Tims, in certain embodiments, compositions of the disclosure include more than one photoaetivator.
• a composition of the present disclosure comprises a first chromophore, which undergoes at least a partial photobleachmg upon application of light.
• photobieaching is meant a photochemical destruction of the chromophore, which can generall be visualized as a loss of colour.
• the first chromophore absorbs at a wavelength in the range of the visible spectrum, such as at wavelenglh of about 380-800 nm, 380-700, or 380-600 nm. in other embodiments, the first chromophore absorbs at a wavelength of about 200-800 nm, 200-700 nm, 200-600 nm or 200-500 nm. In one embodiment th first chromophore absorbs at a wavelength of about 200-600 mn.
• the first chroraophore absorbs Sight at a wavelength of about 200-300 nm, 250-350 am, 300-400 nm, 350-450 nm, 400-500 nm, 450-650 nm, 600-700 nm, 650-750 nm or 700-800 am.
• compositions disclosed herein may also include at least one additional chromophore.
• soch multichromophore compositions When soch multichromophore compositions are illuminated with light, energy transfer can occur between the chromophores.
• This process .known as resonance energy transfer, is a photophysicai process through which an excited 'donor' chromophore (also referred to herein as first chromophore) transfers its excitation energy to an 'acceptor' chromophore (also referred to herein as second chromophore).
• the efficienc and directedncss of resonance energy transfer depends on the spectral features of donor and acceptor chromophores.
• the Row of energy between chromophores is dependent on a spectral overlap reflecting the relative positioning and shapes of the absorption and emission spectra. More specifically, tor energy transfer to occur, the emission spectrum of the donor chroraophore must overlap with the absorption spectrum of the acceptor chromophore ( Figure 2 ⁇
• FIG. 3 is a Jablonski diagram that illustrates the coupled transitions involved between a donor emission and acceptor absorbance.
• the donor chromophore should have good abiiiiies to absorb photons and emit photons. Furthermore, the more overlap there is between the donor chromophore 's emission spectra and the acceptor chromophore's absorption spectra, the better a donor chromophore can transfer energy to the acceptor chromophore.
• the first chromophore may have an emission spectrum that overlaps at least about 80%, 50%, 40%, 30%, 20% or 1.0% with an absorption spectrum of the second chromophore
• the first cliromophore has an emission spectrum that overlaps at least about 20% with an absorption spectrum of the second chromophore.
• the first cliromophore has an emission spectrum that overlaps at least 1-10%, 5- 15%, 10-20%, 15-25%, 20-30%, 25-35%, 30-40%, 35-45%, 50-60%, 55-65% or 60-70% with an absorption spectrum of the second chromophobe.
• % spectral overlap means the % overlap of a donor chromophobe's emission wavelength range with an acceptor chromophobe's absorption wavelength rage, measured at spectral full width quarter maximiim (FWQM),
• FWQM full width quarter maximiim
• Figure 2 shows the normalized absorption and emission spectra of donor and acceptor chromophores.
• the spectral FWQM of the acceptor chromophore's absorption spectrum is from about 60 nm (5.1 nm to about 575 nm).
• the overlap of the donor chromophore 's spectrum with the absorption spectrum o the acceptor cliromophore is about 40 nm (from 515 nra to about 555 nm).
• the % overlap can be calculated as 40nm 60am x .100 ::: 66.6%.
• the second cliromophore absorbs at a wavelength in the range of the visible spectrum.
• the second chromophore has an absorption wavelength that is relatively longer than that of the first cliromophore within the range of abou t 50-250, 25- 150 or 10-100 nm.
• compositions of the present disclosure may .include, in addition to a first and second chromophore, a third, fourth, etc. claomophore.
• compositions including three chromophores not only is there spectra! overlap between the emission spectrum of the first chromophore and the absorption spectrum of the second chromophore, spectral overlap also exists between the emission spectrum of the second chromophore and the absorption spectrum of the third chromophore.
• the second chromophore has an emission spectrum that overlaps at least about 20% with an absorption spectrum of the third chromophore.
• the second chromophore has an emission spectrum that: overlaps at least 1-10%, 5-15%, 10-20%, 15- 25%, 20-30%, 25-35%, 30-40%, 35-45%, 50-60%, 55-65% or 60-70% with an absorption spectrum of the third chromophore.
• the third chromophore has an emission spectrum: that overlaps at least about 20% with an absorption spectrum of the fourth chromophore.
• the third chromophore has an emission spectrum that overlaps at least 1-10%, 5- 15%, 10-20%, 15-25%, 20-30%, 25-35%, 30-40%. 35-45%, 50-60%, 55-65% or 60-70% with an absorption spectrum of the fourth chromophore.
• the application of light to the compositions of the present disclosure results in cascade of energy transfer between the chromophores.
• a cascade of energy transfer provides photons that penetrate the dental tissue
• such a cascade of energy transfer is not accompanied by concomitant generation of beat
• the cascade of energy transfer does not .result in tissue damage suc as damage to the enamel of a tooth.
• the photosensitive agent or agents not only are capable of emitting light in the wavelength range from about 400 nm to about 570 nm, but also absorb light in the wavelength range from about 400 nm to about 570 nm.
• a photosensitive agent is activated by light in the wavelength range of from about. 400 nm to about 570 nm.
• the photosensitive agent absorbs light in the waveiength range of about 400 nm to about 570 nm.
• the photosensitive agent absorbs light at a wavelength between about 470 nm to about 550 nm. This embodiment therefore allows for the optimal absorption of energy from the actinic light and the optima! transmission through dentin and enamel.
• photosensitive agents of the present disclosure when exposed to actinic light, can accelerate the dispersion of light energy, which, consequently leads to a complete photochemical activation of the oxidizing agent within the composition. It is believed that a gel mass can transmit light in the wavelength range of about 400 nm to about 570 nm, so that when a photosensitive agent in the gel mass is exposed to actinic light, the dispersion of the light energy leads to an accelerated photochemical activation of the peroxide. Together, these embodiments allow for favourable absorption by the photosensitive agent of energy from the actinic light and the favourable transmission through the composition, dentin and enamel.
• Suitable chrotnophores that may be used as photosensitive agents in the tooth whitening compositions of the present disclosure include, but are not limited to, chlorophyll dyes, xanthenes dyes, methylene blue dyes and azo dyes,
• Exemplary chlorophyll dyes include but are not limited to chlorophyll a; chlorophyll b; oil soluble chlorophyll; baeterioehSorophyii a; baeteriochiorophyll b; bacteriochiorophy! c; baeteriochiorophyll d; protochSorophy!i; protochlorophyll a; amphophilic chlorophyll derivative I; and amphophilic chlorophyll derivative 2.
• Exemplary-' xanthene dyes include but are not limited to Eosin B (4 ⁇ S - dibromo,2',7'-dimtr- o-fluoreseein, dia ioo); eosin Y; eosin Y (2 4 , ,5',7 , eu-abromo-fluorese- eitt dianion); eosin (2 , ,4 , ,5',7 , -tetrabro.mo-fluoreseein, dianion); eosin (2 ⁇ 4 ⁇ 5 ⁇ ?Metrabrorao- fluoreseein, dianion) methyl ester; eosin (2 , ,4' J 5 , ,7 , -tetrabromo-fl " uorescei 5 monoanion) p- isopropyibenzyi ester; eosin derivative f2',7'
• dianion eosin derivative (trihromo-fluoreseein, dianion); eosin derivative (2 ⁇ 4V5',7'-tetracMor- ⁇ -fluorescein, dianion); eosin; eosin dieelylpyridimum chloride ion pair; crythrosm B (2 > > 4' > S , ,7 , - ⁇ c6raiodo-flvjoresccm !l dianion); erythrosin; erythrosin dianion; erythiosin S; fluorescein; fluorescein dianion; phloxiti B (2 , -4',5'J , -tetrabromo-3 s 4-5,6-tctnichloro-;fluorescein, dianion); phloxin B (tettiic oro-tetrabromo-fluorescein); phloxin
• Exemplary methylene blue derivatives include but are not limited to i- methyl methylene blue; 1 ,9-dimethyl methylene blue; methylene blue; methylene blue (1 ⁇ .); methylene blue (14 ⁇ ); methylene violet; bro omethylene violet; 4-iodo.raethylene violet; 1 ,9-din3 ⁇ 4thyl-3 ⁇ raethyl-amrao-7-die ⁇ hy!-a- raino-phenothiazme; and .1 ,9-dimethyl-3- dtethylamino-7-diburyl-amino-phenot- hiaziae.
• Exemplary azo (or diazo-) dyes include bitt are not limited to methyl violet, neutral red, para red (pigment red I ), amaranth (Azorubine S), Carmoisine (azorubine, food red 3, acid red 14), ailura red AC (FD&C 40), tartraxioe (FD&C Yellow 5), orange G (acid orange 10), Ponceau 4R (food red 7), methyl red (acid red 2), and murexide-ammonium purpura te.
• the one or more chromophores of the tooth whi ten ing composition disclosed herein can be independently selected from any of Acid black i. Acid blue 22, Acid blue 93, Acid fuchsin, Acid green. Acid green i. Acid green 5, Acid magenta. Acid orange 10, Acid red .26, Acid red 29, Acid red 44, Acid red 51, Acid red 66, Acid red 87, Acid red 91 , Acid red 92, Acid red 94, Acid red 101, Acid red 103, Acid roseine, Acid robin.
• Acid violet 19 Acid yellow 1 , Acid yellow 9, Acid yellow 23, Acid yellow 24, Acid yellow 36, Acid yellow 73, Acid yellow S, Aoridine orange, Acriftavrae, Alcian blue, A.iciati yellow, Alcohol soluble eosin.
• Ethyl violet Evans blue, Fast bine B, Fast green FCF, Fast, red B, Fast yellow, Fluorescein, Food green 3, Gal!ein, Gallamme blue, GalSoeyanin, Gentian violet, Haernatein, Haematine, HaematoxyHn, He!io fast rubm BB.L, .Helvetia blue, Hematein, Hematine, Hematoxylin, Hoffman's violet, Imperial red. Ingrain blue. Ingrain blue L Ingrain yellow 1 , INT, Kermes, Kermesic acid, Keraechtrot, Lac, Laccaic acid, Lauth's violet. Light green, Lissamme green SF, Luxol fast blue.
• Magenta 0, Magenta 1, Magenta 11, Magenta HI Malachite green, Manchester brown, Martins yellow, Mexbrorain, Mercurocltrome, Metanii yellow, Methylene azure A, Methylene azure B, Methylene azure C, Methylene blue, Methyl blue, Methyl green. Methyl violet. Methyl violet 2B, Methyl violet 10B, Mordant, blue 3, Mordant blue 10, Mordant blue 14, Mordant blue 23, Mordant blue 32, Mordant, blue 45, Mordant red 3, Mordant red 11, Mordan violet 25, Mordant violet 39 Naphthol blue black, Naphthol green B, Naphthol yellow S, Natural black 1, Natural red.
• Natural red 3 Natural red 4, Natural red 8, Natural red 16, Natural red 25, Natural red 28, Natural yellow 6, NBT, Neutral red, New fuchsia, Niagara blue 3B, Night blue, Nile blue, Nile blue A, Nile blue oxazoiie, Nile blue sulphate, Niie red, Nitro BT, Nitro bine fetrazolhim, Nuclear fast red.
• Oil red O Orange G, Orcein, Pararosanilm, Phloxmc B, Picric acid.
• Ponceau 2 Ponceau 6R, Ponceau B, Ponceau de Xylidine, Ponceau S, Primula, Purpurin, Pyronin B, Pyronin G, Pyronin Y, Rhodamine B, Rosanilin, Rose bengal.
• the composition includes Eosin Y as a first chromophore and Fluorescein as a second chromophore. It is believed that the combination of Eosin Y and Piuroreseein has a synergistic effect, it is further believed that because Eosin Y and Fluorescein reemit green light, that this green light can and may be further absorbed (or reabsorbed) by the chromophores so that light energy is not dissipated as in conventional compositions. This absorbed and re-emitted Light is thought to penetrate throughout the whitening composition, and also to be transmitted into the enamel and dentin.
• the composition includes Eosin Y as a first chromophore, fluorescein as a second chromophore, and Rose Bengal as a third chromophore. It is believed that the combination of Eosin Y, Fluorescein and Rose Bengal also has a synergistic effect,
• the composition includes Eosin Y and Rose Bengal; Fluorescein, Eosin Y and Erythrosine B; Fluorescein and Rose Bengal; Rose Bengal and Erythrosine .8; Fluorescein and Erythrosine B.
• Other synergistic chromophore combinations are also possible.
• O073 ⁇ By means of synergistic effects of the chromophorc combinations in the composition, the light absorption and emission amounts ma be increased, and the time to absorb and emit Hght energy reduced. Advantageously, this may translate to increased reactivity of the composition and faster teeth whitening.
• the amount of oxidizing agent in the compositions can be lowered, or even avoided, without compromising the efficacy of the composition.
• the treatment conditions need not be altered to achieve the same or better whitening results, such as time of exposure to Sight, power of light source used, wavelength of light used-
• use of synergistic combinations of chromophores in the final composition may allow the same or better whitening effects to he achieved using less oxidizing agent in the composition, and without necessitating a longer time of exposure to a light source or a higher power light source.
• a lowered oxidizing agent content may be associated with decreased gum and tooth sensitivity, decreased dehydration of the tooth, decreased hrittleness of the enamel, decreased decalcification of the enamel and longer lasting tooth whitening effects.
• the content of oxidizing agents such as hydrogen peroxide in teeth whitening compositions are also relevant from a regulatory perspective. For example, levels above 6% are not permitted by the European Commission (European Cosmetics Directive 767768/EEC and European Cosmetic Regulation EC 1.223/2009). Therefore, the use of 6% or less hydrogen peroxide, or a hydrogen peroxide equivalent, can be achieved by means of compositions of the present disclosure without compromising teeth whitening effects or necessitating longer treatment times.
• the composition of the present disclosure includes any of the chromophores listed above, or a combination thereof to promote tooth whitening.
• the chromophores can be included in a gel, powder, or liquid. j0077 ⁇ This is a distinct: application of these agents and differs from the use of chromophores as simple stains or as a catalyst for photo-polymerization,
• compositions of the disclosure may include an oxidant.
• Oxidants are chemical compounds that readily transfer oxygen atoms and oxidizes other compounds and also include precursors of compounds capable of oxidizing oilier compounds.
• Useful oxidizing agents that may be utilized in the compositions of the present disclosure preferably include peroxide, an alkali metal percarbonate, an alkali metal perborate, or a peroxyacid known in the art.
• Oxidizing agents include, but are not limited to, hydrogen peroxide, carbamide peroxide, calcium peroxide, magnesium peroxide, zinc peroxide, sodium percarbonate, potassium: percarbonate, potassium persulfate, sodium: persultate, ammonium persulfate, disodium monoperphosphafe, dipotassium roonoperphosphate , pamy acids, magnesium monoperoxyphthaiate, sodium perborate, chlorine dioxide, and sodium chlorite.
• Oxidants can be provided in powder, liquid or gel form.
• Oxidants may be inherent in the environment of the teeth and/or contacted with the compositions of the disclosure on application of the composition, to the teeth or oral environment. In some embodiments, oxidants can be applied to the teeth (teeth 'preconditioning') before application of present compositions including chromophores.
• compositions of the disclosure may also include a gelling agent, such as a hydrophihe gelling agent.
• the nature of the gelling agent prevents vaporization of the gel when exposed to actinic light thus improving hydration of the coated tooth area. Increased hydration of the teeth and surrounding tissues is associated with decreased discomfort and sensitivity.
• the gelling agent can include, for example, one or more modified starches and-'or glucose, hi some embodiments, the gelling agent further enhances the consistenc of the composition, facilitating the application to the tooth surface.
• the gelling agent can enhance the tratishtcency or transparency upon addition to the composition and/or upon activation by, e.g., actinic light, emitted light and/or heat. In one embodiment, it minimizes vaporization of the composition. Additionally or alternatively, the gelling and/or trans!ucency agent minimizes any thermal effects by absorbing any heat generated in the composition.
• the gelling agent may be selected from: any of synthetic or semi-synthetic polymeric materials, polyacrylate copolymers, cellulose derivatives and poiymethyi vinyl ether/nialeic anhydride copolymers.
• the gelling agent is a hydrophihe, high molecular weight (i.e., molar masses of more than about 5,000, and in some instances, more than about 10,000, or 100,000, or 1 ,000,000 and/or cross-linked poIyaerySie acid polymer.
• the gelling composition comprises a gelling agent this is a polyacrylic acid polymer has a viscosity in the range of about 20,000-100,000, 25,000- 90,000, 30,000-80,000, 30,000-70,000, 30,000-60,000, 25,000-40,000 cP.
• the gelling agent is a hydrophilic, high -molecular weight, and/or cross-linked polyacrylic acid polymer, where the polyacrylic acid polymer has a viscosity in the range of about 20,000-80,000 cP.
• the gelling agent comprises a carbomer.
• Carbomers are synthetic high molecular weight polymer of acrylic acid that are crosslinked with either altyisucrose or allyfethers of pentaerythruo! having a molecular weight of about 3 x 10*. The gelation mechanism depends on neutralization of the earboxylic acid moiety to form a soluble salt. The polymer is hydrophilic and produces sparkling clear gels when neutralized. Carbomer gels possess good thermal stability in that gel viscosity and yield value are essentially unaffected by temperature. Carbomer gels possess optimum rheological properties.
• Aqueous solution of Carbopol ⁇ is acidic in nature due to the presence of free carboxylic acid residues. Neutralization of this solution cross-links and gelatinizes the polymer to form a viscous integral structure of desired viscosity,
• Carboraers are available as fine white powders which disperse in water to form acidic colloidal suspensions (a 1% dispersion has approx. pH 3) of low viscosity. Neutralization of these suspensions using a base, for example sodium, potassium or ammonium hydroxides, low molecular weight amines and atkanolamines, results in the formation of clear translucent gels. Nicotine salts such as nicotine chloride form stable water-soluble complexes with carbomers at about pH 3,5 and are stabilized at an optimal pH of about 5.6.
• the carbomer is Carbopoi.
• Such polymers are commercially available from B.F. Goodrich under the designation Carbopoi® 420, 430, 475, 488, 493, 910, 934, 934P, 9 / IPNF, 974P NF, 980 NF, 981 NF and the like.
• Carbopoi s are versatile eontrolled-release polymers, as described by Brock (Pharmacotherapy, 14:430-7 (1994)) and Durrani (Pharmaceutical Res, (Supp.) 8:S-135 (1991)), and belong to a family of carbomers which are synthetic, high molecular weight, non-linear polymers of acrylic acid, crosslinked with polyaikenyl polyether.
• the carbomer is Carbopoi® 974P NF, 980 NF, 5984 EP, ETD 2020NF, LJltrez 10 NF, 934 NF, 934P NF or 940 NF, hi certain embodiments, the carbomer is Carbopoi® 980 NF, ETD, 2020 NF, U!trez 10 NF, or 940 NF.
• compositions of the present disclosure may also include a stabilizing agent.
• the stabilizing agent stabilizes the peroxide concentration in the composition for days, weeks, months, a year or several years, in some embodiments, the stabilizing agent not only stabilizes the oxidizing agent, but also is a pH modifier and/or stabilizer.
• the stabilizing agent is sodium acetate. In one embodiment, sodium acetate is added until the desired pH is attained.
• the stabilizing agent is selected from the group consisting of antioxidants such as sodium sulfite, metal chelators (e.g., EDTA), and stabilizers (e.g., tin salts, phosphoric acid, and tin sulphonates). in some embodiments, the stabilizing agent scavenges or otherwise isolates or removes from, solution, metal ions that can potentially destabilize the oxidizing agent.
• the pH of the composition is in or adjusted to the range of from about 4 to about 10. In alkaline conditions, with a pH from about 8 to about 10, the stronger free radical, perhydroxyl ions, can be generated. Perhydroxyl free radicals are capable of reacting not only with yellow and brown stains but even with grey chromophores situated deeper in the tooth structure.
• the pH of the composition is between about 5 and about 7, or between about 5 and about 6, or between about 6 and 7. In certain embodiments the pH is about 6 or 6,5.
• Suitable pH adjusting agents include, but are not limited to, sodium hydroxide, potassium hydroxide, ammonium hydroxide, sodium carbonate, potassium carbonate, TRIS, and trtetbanoiamine, or any other salt of an alkaline base which is safely used in the mouth.
• the pH adjusting agent is sodium perborate.
• a single component may act as a pH adjusting agent or as a stabilizing agent or may serve both functions, in one embodiment, sodium acetate acts as a pH adjusting agent and as a stabilizing agent, in further embodiments, the pH adjusting agent is of the group consisting of sodium bicarbonate, calcium bicarbonate, sodium carbonate and calcium carbonate.
• the composition can include a thickening agent to improve the ease of application of the composition to the teeth such thai even and effective coverage is more readily achieved.
• Suitable thickening agents include but. are not limited to mixed silica-aluminum oxides, oiethanolamine (e.g., Trolartime), and water soluble poly (ethylene oxide) resins (e.g., PolyoxTM).
• Suitable thickening agents also include amide starches.
• the photosensitive agent has particle size below about 2 microns or below about I micron.
• the agent has a particle size below about 0.8, 0.?, 0.6, 0.5, 0.4, 0,3, or 0.2 microns.
• the photosensitive agent has a particle size between about O.i and about 0.8, between about 0.2 and about 0.7, or between about 0.3 and about 0.6 microns.
• the thickening agent can include fumed silica and/or any other inert inorganic material that may be used as a carrier and can aid in the delivery of active oxygen to the tooth surface.
• Fumed silica of a small particle size e.g., between about 0.2 microtis and about 0,4 microns, can provide efficient dispersion of hydrogen peroxide and reflection of light energy within the oxidizing composition.
• the compositions of the disclosure include a reaction accelerator or accelerating agent
• the composition includes sodium perborate.
• Sodium perborate has selective reactivity with hydrogen peroxide in forming free radicals (reacts with water to release hydrogen peroxide).
• the use of one or more photosensitive agents e.g., sodium perborate
• acceleration of the reaction means that the composition can be removed more quickly than conventional compositions thereby decreasing exposure of the patient to the composition and resulting sensitivity and/or other damage to tissues and teeth.
• Another aspect of the disclosure provides methods for tooth whitening including applying a tooth whitening composition of the present disclosure to at least one tooth, and exposing the tooth whitening composition to actinic iight to activate the oxidizing agent and/or the ehro ophore.
• the composition may he any of the compositions described herein.
• the method for whitening the teeth ma he performed its a dentist's office or clinic under ordinary conditions.
• the composition can be mixed chair-side and applied to the surface of as many teeth as are desired to be whitened. The whole or part of the teeth may be treated. Alternatively, the composition can be provided without the need for mixing chair- side. For example, in a light-proof container to minimize activation of the chromophores. Thereafter, the composition can be exposed to actinic light to accelerate decomposition of the oxidizing agen t and the formation of free radicals. Premixes can be prepared with some or aft of the ingredients and then mixed chair-side and applied to the teeth.
• a carbamide peroxide gel premix and a ehromophore gel premix can be prepared and stored. The user then mixes the two premixes immediately prior to use. Additionally or alternatively, some or all of the remaining ingredients can also be separately premi ed and stored. Such premixes can he stored, e.g., for at least about one year.
• compositions of the disclosure can be used to whiten teeth discolored by any agent or disorder.
• the compositions may be used to whiten discoloration due to stains (e.g., tobacco, coffee, tea and/or food stains.), fluorosis, developmental disturbances, bacteria, genetics, tetracycline antibiotics, trauma, blood decomposition, pigments present during development of teeth, etc. Therefore, there is also provided use of a composition of the present disclosure to whiten teeth.
• any source of actinic Sight can be used to activate the oxidizing agent.
• Any type of halogen, LED or plasma arc lamp, or laser may be suitable.
• the primary characteristic of suitable sources of actinic light will be that they emit Sight in a wavelength (or wavelengths) appropriate for photosensitive the one or more photoaetivators present in the composition.
• an argon laser is used.
• a potassium-titanyl phosphate ( TP) laser e.g. a GrcenLtghtTM laser
• a LED photocurmg device is the source of the actinic light.
• the source of the actinic light is a source of light having a wavelength between about 200 to 600 nra. in another embodiment, the source of the actinic light is a source of visible light having a wavelength between about 400 and 600 urn. Furthermore, the source of actinic light should have a suitable power density.
• the actinic light is at a wavelength of about the absorption wavelength of the photosensitive agent in one embodiment, the actinic light has a wavelength in the range from about 470 nm to about. 550 am, In another embodiment, the actinic light has a wavelength in the range from about 470 am to about 520 nm. in a further embodiment, the actinic light has a wavelength of about 530 nm to about 535 nm
• the teeth are exposed to actinic light tor a total of less than 20 minutes, in another for less than 10 minutes, in another for less than 5 minutes, hi one embodiment the teeth are exposed to actinic light for less than 4, 3, 2, or 1 minute.
• the disclosure provides a method for whitening teeth at least 2 shades in about 1 minute. In some embodiments, there is no significant post-treatment sensitivity. In other embodiments, there is no post-treatment sensitivity. In yet other embodiments, the whitening effect does not diminish over time following treatment.
• the tooth whitening composition is applied and the tooth is exposed to multiple applications of actinic light, for a time of about 4 to about 6 seconds for each tooth per exposure.
• the tooth is exposed to actinic light at least two, three, four, five or six times, in some embodiments, a fresh application of the tooth whitening composition, is applied before each exposure to actinic light
• the total exposure to actinic light is less than about one minute. In other embodiments, the total exposure to actinic light is less than about 60, 40, 30, or 20 seconds.
• the tooth is whitened at least 7 shades, 6 shades, 5 shades, 4 shades, 3 shades, 2 shades or 1 shade.
• Shades can be determined before and after treatment using any of a number of shade guides, including, e.g., the VITA® (Vita Zahnfabrik H. Rauter GmbH & Co., KG), CHROMA SCOP#- (Ivoelar Vivadent, Inc.) or BIODENT (Dentsp!y intenational) shade guides.
• a shade taking system e.g., the ShadeEye CC Dental Chroma Meter, can be employed to determine shade before and/or after treatment
• the tooth is whitened at least two shades, three shades, four shades, fi ve shades, six shades or seven shades in less than about one minute of total exposure time to actinic light. In some embodiments, the tooth is whitened at least two shades, three shades, four shades, five shades, si shades or seven shades in less than about 40 seconds of total exposure time to actinic light, in some embodiments, the tooth is whitened at least two shades, three shades, tour shades, five shades, six shades or seven shades in less than about 30 seconds of total exposure time to actinic light. In some embodiments, the tooth is whitened at least two shades, three shades, four shades, five shades, six shades or seven shades in less than about 20 seconds or even less than about 10 seconds of total exposure time to actinic light
• the risk of transient inflammation of the pulp by percolation of the oxidizing agent is reduced, not significant and/or eiimmated.
• inflammation of the pulp is thought to be caused by percolation of the oxidizing agent into the pulp tissue, in some embodiments, the synergistic effect of the photosensitive agents, and the actinic light results in an instantaneous and complete photochemical reaction. Accordingly, exposure of the tooth, the pulp, and/or the surrounding tissues to the oxidizing agent and/or other components in the composition is dramatically reduced,
• the disclosure provides a method for tooth whitening comprising application of actinic light and a composition of the disclosure (any of the compositions described herein) to at least one tooth such that the tooth is whitened at least about two shades in less than about 10 minutes.
• the toot is whitened at least about two shades in less than about 5 minutes, less than about 4 minutes, less than about 3 minutes, less than about 2 minutes or in about 1 minute, in some embodiments, the teeth are whitened at least about 3 shades. 4 shade or 5 shades.
• kits for preparing and/or applying any of the compositions of the present disclosure may include a composition comprising an. oxidizin agent and at least one chromophore having an emission wavelength between abo ut 400 am and about 570 m
• the oxidizing agent may be present in an amount of about 0.0.1 % - 40%, 0.01 % - 1.0%, 0.5% - 10.0%, 5% - 15%, 10% - 20%, 15% - 25%, 20% - 30%, 15.0% - 25%, 20% - 30%, 25% ⁇ 35%, or 30% - 40% by weight to weight of the composition.
• the chromophore may be present in an amount of about 0.001-0.
• the first chromophore may be present in an amount of about 0.05-40% per weight of the composition, and a second, chromophore may be present in an amount of about 0.05-40% per weight of the composition, in certain embodiments, the first chromophore is present in an amount of about 0.001 -0.1%, 0.05- 1 %, 0.5-2%, 1 -5%, 2.5-7.5%, 5-10%, 7.5-12.5%, 10-15%, 12.5- 17.5%, 15- 20%.
• the second chromophobe is present in an amount of about 0.001-0.1%, 0.05-1%, 0.5-2%, 1-5%, 2.5-7.5%, 5-10%, 7.5- 12.5%, 10- 15%, 12.5-17.5%, 15-20%, 17.5-22.5%, 20-25%, 22.5-27.5%, 25-30%, 27.5- 32,5%, 30-35%, 32,5-37.5%, or 35-40% per weight of the composition.
• the amount of chromophore or combination of chromophores may be in the amount of about 0.05-40.05% per weight of the composition. In certain embodiments, the amount of chromophore or combination of chromophores may be in the amount of about 0.001 -0.1 %, 0.05-1%, 0.5-2%, 1 -5%, 2,5-7,5%, 5-10%, 7.5-12.5%, 10-15%, 12.5-17.5%, 15- 20%, 17.5-22.5%, 20-25%, 22.5-27.5%, 25-30%, 27.5-32.5%, 30-35%, 32.5-37.5%. or 35- 40 05% per weight of the composition
• the kit includes more than one composition, for example, a first and a second composition.
• the first composition may include the oxidizing agent and the second composition may include the chromophore having an emission wavelength between about 400 nm and about 570 nm.
• the oxidizing agent may be present in the first composition in an amount of about 0.01% - 1.0%, 0.5% - 10.0%, 5% - 1 %, 10% - 20%, 15% - 25%, 20% - 30%, 15.0% - 25%, 20% - 30%, 25% - 35%, 30% - 40% or 35 - 45% by weight to weight of the first composition.
• the chromophore may be present in the second composition in an amount of about 0,001-0.1%, 0.05-1%, 0.5-2%, 1-5%, 2.5-7.5%, 5- 10%, 7.5-12.5%, 10-55%, 12.5-17.5%, 15-20%, 17.5-22.5%, 20-25%, 22.5-27.5%, 25-30%, 27.5-32.5%», 30-35%, 32.5-37.5%, or 35-40% per weight of the second composition.
• the first chromophore may be present in an amount of about 0,05-40% per weight of the second composition
• a second chromophore may be present in an amount of about 0.05-40% per weight of the second composition.
• the first chromophore is present in an amount of about 0.001-0.1%, 0.05- 1%, 0.5-2% f 1-5%, 2.5-7.5%, 5- 10%, 7.5-12.5%, 10- 15%, 12,547,5%, 15-20%, 17.5-22.5%, 20-25%, 22.5-27.5%, 25-30%, 27.5-32.5%, 30-35%, 32.5-37.5%, or 35-40% per weight of the second composition, ht certain embodiments, the second chromophore is present in an amount of about 0.001 -0.1 %, 0.05-1 %, 0.5-2%, 1 -5%, 2.5-7.5%, 5- 10%, 7.5- 12.5%.
• the amount of chromophore or combination of chromophobes may be in the amount of about 0.05-40.05% per weight of the second composition, in certain embodiments, the amount of chromophore or combination of chromophores may be in the amount of about 0.001 -0.1%, 0,05-1 %, 0.5-2%, 1-5%, 2.5-7.5%, 5-10%, 7.5-1.2.5%, 10-15%, 12.5- 17.5%, 15-20%, 17.5-22.5%. 20-25%, 22.5-27.5%, 25- 30%, 27.5-32.5%, 30-35%, 32.5-37.5%, or 35-40.05% per weight of the second chromophore.
• the kit includes containers comprising the compositions of the present disclosure.
• the kit includes a first container comprising a first composition that includes the oxidizing agent, and a second container comprising a second composition that includes at least one chromophore.
• the containers may be light impermeable, air-tight and/or leak resistant.
• Exemplary containers include, but are not limited to, syringes, vials, or pouch.
• kits of the disclosure may also include directions for application. Additionally or alternatively, the kit can include apparatus for application (e.g., brushes or trays or both). The kit can also include charts or other information helpful in assessing the whitening effect desired and/or achieved by the methods and compositions of the disclosure. The kit ma also include a source of actinic light. The kit may also include a retractor for the hps, mouth, cheeks in order to expose the teeth for the treatmen
• a kit of the disclosure may also include an applicator or a dispenser containing a tooth brightening composition.
• the tooth brightening composition may be used to pre-treat the teeth before the whitening treatment and/or to treat the teeth after the whitening treatment.
• the tooth brightening composition may include a low concentration of an oxidizing agent, such as hydrogen peroxide.
• the applicator may conveniently be substantially pen-shaped, and configured to include a reservoir containing the brightening composition tn fluid communication with an applicator tip for delivering the brightening composition to the teeth.
• Embodiments herein are directed to compositions comprising an oxidizing agent and at least one chroraophore.
• the compositions described herein are preferentially used for teeth whitening.
• the oxidizing agent is selected from hydrogen peroxide, carbamide peroxide and a combination thereof. In some embodiments, the oxidizing agent is carbamide peroxide. In some embodiments, the carbamide peroxide comprises about 22% or less of the composition by weight, in some embodiments, the oxidizing agent comprises about 17.97% of the composition by weight,
• the chromophore is selected from eosin Y, .fluorescein, and a combination thereof, in some embodiments, the eosin Y comprises between about 0.001 % to about 1 % of the composition by weight, in some embodiments, fluorescein comprises between about 0.001 % to about 1% of the composition by weight, in some embodiments, the eosin Y comprises about 0.02% of the composition by weight. In some embodiments, fluorescein comprises about 0,01% of the composition by weight. In some embodiments, the eoshi Y comprises about 0.016% of the composition by weight In some embodiments, fluorescein comprises about 0.005% of the composition by weight.
• the composition further comprises a stabilizing agent.
• the stabilizing agent is a metal chelator, in some embodiments, the metal chelator is sodium EDTA. In some embodiments, the sodium EDTA comprises about 0.13% of the composition by weight.
• the composition farther comprises a gelling agent.
• the gelling agent comprises a hydrophilic gelling agent.
• the ' hydrophilic gelling agent is selected from polypropylene glycol, polyethylene glycol, propylene glycol, glycerol, or a large molecular weight polyoi, and any combination thereof.
• the hydrophilic gelling agent is propylene glycol
• the propylene glycol comprises about 3.1.1 % of the composition by weight
• the gelling agent comprises a carbomer. In some embodiments the carbomer is Carbopol.
• the Carbopol is Carbopol 940 NF, Carbopol Ultrez 10NF and combinations thereof
• the Carbopo! 940 NF comprises about 0.98% of the composition by weight.
• the Carbopol ' Ultrez: IONF comprises about 0.23% of the composition by weight.
• the composition comprises propylene glycol, Carbopol 940 NF, and Carbopol Ultrez IONF.
• the Carbopol 940 NF comprises about 0.98% of the composition by weight.
• the Carbopol Ultrez IONF comprises about 0.23% of the composition by weight.
• the propylene glycol comprises about 1.10% of the composition by weight.
• the composition further comprises a base.
• the base is selected .from potassium hydroxide.
• the potassium hydroxide comprises about 0.26% of the composition by weight.
• the composition further comprises a pH adjusting agent, in some embodiments, the pH adjusting agent is selected from sodium hydroxide, potassium hydroxide, ammonium hydroxide, sodium carbonate, potassium carbonate, TRIS, triethanolamine, or any other salt of an alkaline base which is safely used in die mouth.
• the pH adjusting agent is triethanolamine. in some embodiments, the triethanolamine comprises about 0.49% of the composition by weight.
• the met anolamine may also act as a thickening agent.
• the composition further comprises methyiparaben, propylparaben or a combination thereof In some embodiments, the methyiparaben comprises about 0.02% of the composition by weight. In some embodiments, the propylparaben comprises about 0.01% of the composition by weight. In some embodiments, the composition further comprises methyiparaben and propylparaben, in some embodiments, the methyiparaben comprises about 0,02% of the composition by weight. In some embodiments, the propylparaben comprises about 0,01 % of the composition by weight.
• die composition further comprises glycerin, in some embodiments, the glycerin comprises about 25.24% of the composition by weight.
• the composition further comprises ethanoL
• cthanol comprises about 1.8,78% of the composition by weight.
• the composition further comprises peppermint essential oil.
• the peppermint essential oil comprises about 0.49% of the composition by weight,
• the composition further comprises water, in some embodiments, the water comprises about 4.28% of the composition by we ight.
• the composition comprises carbamide peroxide, eosin Y and fluorescein.
• the carbamide peroxide comprises about 22% or less of the composition by weight.
• the eosin Y comprises between about 0.001 % to about 1% of the composition by weight
• die fluorescein comprises between about 0.001% to about 1% of the composition by weight
• the carbamide peroxide comprises about 17.97% of the composition by weight
• die eosin Y comprises about 0.02% of the composition by weight.
• fluorescein comprises about 0.01% of the composition by weight, in some embodinienis, the eostn Y comprises about 0.016% of the composition by weight. In some embodiments, fluorescein comprises about 0.005% of the composition by weight. In some embodiments, the composition further comprises sodium EDTA. propylene glycol, Carbopoi 940 NF « Carbopo! Uifrez 10NF, potassium hydroxide, triefhanoiamine, methylparaben, propylparaben, glycerin, ethanol. peppermint essential oil, and water.
• the composition comprises carbamide peroxide, eosin Y and fluorescein.
• the carbamide peroxide comprises about 17.97% of the composition by weight.
• the eosin Y comprises about 0,01% of die composition by weight, hi some embodiments, the fluorescein comprises about 0.02% of the composition by weight.
• the eosin Y comprises about 0.016% of the composition by weight In. some embodiments, fluorescein comprises about 0,005% of the composition by weight.
• the composition further comprises sodium EDTA, propylene glycol, Carbopoi 940 NF, Carbopoi UStrez l NF, potassium hydroxide, rrieihanoiamine, methylparabcn, propylparaben, glycerin, ethanoi, peppermint essential oil, and water.
• the composition comprises carbamide peroxide, eosin Y, fluorescein, sodium: EDTA, propylene glycol Carbopoi 940 NF, Carbopoi Uitrez 1 GNF, potassium hydroxide, triethaiiolaminc, methyiparabeii, propylparaben, glycerin, ethanoi, peppermint essential oil, and water.
• the carbamide peroxide comprises about 22% or less of the composition by weight, hi some embodiments, the carbamide peroxide comprises about 17.97% of the composition by weight.
• the eosin Y comprises between about 0.001% to abou t 1% of the composition by weight. In some embodiments, fluorescein comprises between about 0.001% to about i% of the composition by weight, in some embodiments, the eosin Y comprises about 0.02% of the compositioii by weight. In some embodiments, fluorescein comprises about 0.01 % of the composition by weight In some embodiments, the eosin Y comprises about 0.016% of the composition by weight. In some embodiments, fluorescein comprises about 0.005% of the composition by weight.
• die sodium EDTA comprises about 0.13% of die composition by weight in some embodiments, the propylene glycol comprises about 31.10% of the composition by weight, in some embodiments, the Carbopoi 940 NF comprises about 0,98% of the composition by weight. In some embodiments, the composition the Carbopoi Ulteez iONF comprises about 0.23% of the composition by weight. In some embodiments, the potassium hydroxide comprises about 0.26% of the composition by weight. In some embodiments, the trietlHuiolamirse comprises about 0.49% of the composition by weight. In some embodiments, the methylparaben comprises about 0.02% of the composition by weight.
• the propylparaben comprises about 0.01% of the composition by weight.
• the glycerin comprises about 25.24% of the compositioii by weight.
• the ethanoi comprises about 18.78% of the composition by weight.
• the peppermint essential oil comprises about 0.49% of the composition by weighi.
• the water comprises about 4.28% of the composition by weight.
• the composition comprises carbamide peroxide, eosin Y, fluorescein, sodium EDTA, propylene glycol Carbopoi 940 NF, Carbopoi Uitrez 10 F, potassium hydroxide, tnetbaiiokmme, methylparaben, propylparaben, glycerin, ethanoi, peppermint esseotia! oil, and water.
• the carbamide peroxide comprises about 1.7.97% of the composition by weight
• the eosin Y comprises about 0,02% of the composition by weight
• fluorescein comprises about 0.01% of the composition by weight.
• the eosin Y comprises about 0.016% of the composition by weight.
• fluorescein comprises about 0.005% of the composition by weight
• the sodium EDTA comprises about 0.13% of the composition by weight.
• the propylene glycol comprises about 31.1 % of the composition by weight.
• the Carbopo! 940 NF comprises about 0.98% of the composition by weight.
• the composition the Carbopo! U!trez 1 NF comprises about 0.23% of the composition by weight.
• the potassium hydroxide comprises about 0.26% of the composition by weight.
• the triethanoiamine comprises about 0.49% of the composition by weight.
• the methylparaben comprises about 0.02% of the composition by weight la some embodiments, the propylparaben comprises about 0.01% of the composition by weight, in some embodiments, the glycerin comprises about 25.24% of the composition by weight, in some embodiments, ethane! comprises about 18.78% of the composition by weight. In some embodiment, the peppermint essential oil comprises about 0.49% of the composition by weight. In some embodiments, the water comprises about 4.28% of the composition by weight.
• Embodiments herein are directed to compositions that when combined may be used for teeth whitening.
• at least two compositions are combined for use in teeth whitening.
• a first composition (oxidizing pre-mix) and a second composition (chromophore gel pre-mix are combined to form a third composition.
• the third composition is suitable for use in teeth whitening.
• the first composition comprises aa oxidizing agent.
• the oxidizing agent is selected from hydrogen peroxide, carbamide peroxide, or a combination thereof.
• the oxidizing agent is carbamide peroxide, In some embodiments, the carbamide peroxide comprises about 22% or less of the first composition by weight.
• the first composition further comprises propylene glycol, Carbopol 940 NF , ethanol, glycerin, peppermint essential oil, and triethanolamine or any combination thereof, in some embodiments, propylene glycol comprises about 34.6% of the first composition by weight ' hi. some embodiments, Carbopol 940 NF comprises about 12% of the first composition by weight. In some embodiments, ethanol comprises about 23% of the first composition by weight. In some embodiments, glycerin comprises about 18% of the first composition by weight. In some embodiments, peppermint essential oil comprises about 0,6% of the first composition. In some embodiments, triethanolamine comprises about 0.6% of die first composition by weight.
• the second composition (ehromophore gel pre- mix) comprises at least one chromophore.
• the chromophore is selected from eosin Y, fluorescein and a combination thereof.
• the second composition comprises eosin Y and fluorescein.
• the eosin Y comprises between about 0.001 % to about 1% of the composition by weight.
• fluorescein comprises between about 0.001% to about 1% of the composition by weight
• the eosin Y comprises about 0.088% of the composition by weight.
• fluorescein comprises about 0.029% of the composition by weight.
• the second composition further comprises sodium EDTA, propylene glycol Carbopol CJltrez 10NF, potassium hydroxide, methylparaben, propylparaben, glycerin, and water, in some embodiments sodium EDTA comprises about 7% of the second composition by weight, m some embodiments, propylene glycol comprises about .15.525% of the second composition by weight. In some embodiments, Carbopol Ultrez 10NP comprises about 1.250% of the second composition by weight. In some embodiments. potassium hydroxide comprises about 1.42% of the second composition by weight.
• methylparaben comprises about 0.1 63% of the second composition by weight
• propylparaben comprises about 0,0563% of the second composition by weight
• glycerin comprises about 57.5% of the second composition by weight
• water comprises about 23.33% of the second composition b weight
• the third composition comprises the components of the first and second compositions. In some embodiments, the third composition is any one of the compositions described herein,
• Embodiments herein are directed to methods for teeth whitening. ⁇ « some embodiments, the compositions described herein are used in methods for teeth whitening.
• Some embodiments are directed to methods for whitening teeth comprising providing a composition described herein; applying the composition to at least one tooth; and exposing the composition on the at least one tooth to actinic light,
• Some embodiments further comprise combining a firs composition (Oxidizing pre-mix) with a second composition (Chromophobe gei. pre-mix.) to form the compositions described herein.
• a firs composition Oxidizing pre-mix
• a second composition Chromophobe gei. pre-mix.
• the first composition (Oxidizing pre- mix) and the second composition Chromophore gel pre-mix) are those described herein.
• the first and second compositions are combined prior to application to at least one tooth
• each tooth is exposed to the actinic light for about 1 -30 seconds. In some embodiments, each tooth is exposed to the actinic light for about 3- 10 seconds, in some embodiments, each tooth is exposed to the actinic light for about 5- 10 seconds.
• kits for preparing and/or applying any of the compositions of the present disclosure comprises the first, composition (oxidizing pre-raix) nd the second composition (chromophore pre-mix) described herein, in some embodiments, the kits may include containers comprising tlie compositions of the present disclosure. In some embodiments, the kits may also include directions for application. Additionally or alternatively, the kit can include apparatus for application (e.g., brushes or trays or both). In some embodiments, the kits can also include charts or other information helpful in assessing the whitening effect desired and/or achieved by the methods and compositions of the disclosure.
• kits may also include a source of actinic light. In some embodiments, the kits may also include a retractor for the lips, month, cheeks in order to expose the teeth for the treatment. In some embodiments, the kits of the disclosure may also include an applicator or a dispenser containing a tooth brightening composition.
• Some embodiments are a composition comprising; an oxidizing agent; and Eosin Y and Fluorescein. Some embodiments are a composition comprising: an oxidizing agent; and Eosin Y, Fluorescein and Rose Bengal. So ic embodiments are composition comprising: an oxidizing agent: and Eosin Y and Rose .Bengal- Some embodiments are a composition comprising: an oxidizing agent; and Fluorescein and Rose Bengal. Some embodiments are a composition comprising: an oxidizing agent; and Eosin Y, Fluorescein and Eryfhrosme.
• An of the forgoing embodiments ma further comprise erythrosine.
• the oxidizing agent comprises hydrogen peroxide.
• the hydrogen peroxide content is less than or equal to 6% by weight of hydrogen peroxide i the composition
• the oxidizing agent comprises carbamide peroxide.
• the carbamide peroxide content is less than or equal to 22% by of the composition.
• the carbamide peroxide contents is greater than 0% by weight but less than or equal to 22% by weight of the compositions.
• the total content of the oxidizing agent is equivalent to about 6% by weight of hydrogen peroxide content.
• Any of the forgoing embodiments may farther comprise a stabilizing agent.
• Any of the forgoing embodiments may further comprise a thickening agent.
• the thickening agent is silicon dioxide and/or fumed silica having a particle size less than one micron.
• any of the forgoing embodiments may further comprise a hydrophih ' c gelling agent, in any of die forgoing embodiments, the hydrophilie gelling agent comprises polypropylene glycol, -polyethylene glycol, propylene glycol, glycerol, or a large molecular weight polyol, or any combination thereof
• a ny of the forgoing embodi ments may further comprise a base.
• the base is potasium hydroxide.
• the pH of the composition is between 2 and 1 , In any of the forgoing embodiments, the pH of the composition i s between 4 and 8, preferably between 6 and 7, more preferably 6.5.
• Eosin Y is present in an amount of 0.001 % to I % weight per weight of the composition.
• Fluorescein is present in an amount of 0.001 % to 1 % weight per weight of the composition.
• Rose Bengal is present in an amount of 0.001 % to 1 % weight per weight of the composition, in any of the forgoing embodiments, Erythrosin is present in an amount of 0.001 % to I % weight per weight of the composition.
• kits comprising: a first component comprising an oxidizing agent; a d a second component comprising Eosin Y and Fluorescein, Some embodiments arc a kit comprising: a first component comprising an oxidizing agent; and a second component comprising Eosin Y, Fluorescein and Rose Bengal. Some embodiments are a kit comprising: a. first component comprising an oxidizing agent, and a second component comprising Eosin Y and Rose Bengal.
• kits comprising: a first component comprising an oxidizing agent; and a second component comprising Fluorescein and Rose Bengal, Some embodiments are a kit comprising: a first component comprising an oxidizing agent; and a second component comprising Eosin Y, Fluorescein and Erythresine,
• the second component further comprises erythrosme.
• the oxidizing agent comprises hydrogen peroxide or carbamide peroxide, in any of the forgoing embodiments, the oxidizing agent is carbamide peroxide.
• one or both of the first: and second components further comprises a thickening agent.
• the thickening agent is silicon dioxide and/or fumed silica having a particle size less than one micron.
• one or both of the first and second components further comprises a hydrophilic gelling agent.
• An of the forgoing embodiments may further comprise an applicator containing a tooth brightening composition.
• the brightening composition comprises an oxidizing agent, in any of the forgoing embodiments, the oxidizing agent comprises hydrogen peroxide or carbamide peroxide.
• Any of the .forgoing embodiments may further comprise a gingival barrier composition. Any of the forgoing embodiments may further comprise instructions for using the kit, apparatus for mixing together the first and second components, a light source, or information for assessing the efficacy of the composition.
• Some embodiments arc- directed to the use of any of the forgoing compositions for whitening teeth. Some embodiments are directed to the use of any of the forgoing kits tor whitening teeth.
• Some embodiments are a method tor whitening teeth comprising: providing a composition according to any one of forgoing embodiments; applying the composition to at least one tooth; and exposing die composition on the at least one tooth to actinic light,
• each tooth is exposed to the actinic light for about 1 -30 seconds. In any of the forgoing embodiments, each tooth is exposed to the actinic light for about 3- 10 seconds. In. any of the forgoing embodiments, each tooth is exposed to the actinic light for about 5-10 seconds,
• the teeth whitening composition of Example 1 was applied to the upper and lower teeth of eight patients, covering the central incisors, lateral incisors, canines and pre-molars.
• a gingival barrier was applied to the gums.
• the teeth were then exposed for approximately three to five minutes (5-10 seconds per tooth) with a blue light (dental curing light) to activate the composition on the teeth.
• the activated composition was then removed.
• Four (4) successive applications of the composition and light exposure were performed on cadi patient.
• the shades of the treated teeth were then evaluated using Vita Shade assessment; before and immediately after the procedure. The results are summarized in Table 3. Whitening of the teeth by at ieast 6 shades was observed in all of the patients. None of the patients noticed gum or teeth sensitivity during or after the procedure.
• Example 1 The whitening effect of the composition of Example 1 was evaluated on 6 patients having discoloured teeth due to tetracycline antibiotics. One patient had severe tetracycline staining, 3 had moderate staining and 2 had mild staining.
• the composition of Example 1 was applied to the teeth of each patient. The teeth were then exposed to blue dental light for approximately 5- ⁇ 0 seconds per tooth. The activated composition was removed, and new composition applied to the teeth. This was repeated for a total of 4 cycles of composition application and light exposure.
• the shades of the treated teeth were then evaluated using Vita Shade®- 1 assessment, before and immediately after the procedure. Whitening of the teeth by at least 6 shades was observed in all of the patients. None of the patients noticed gum or teeth sensitivity during or after the procedure.
• Example .1 The continuation of the whitening effect of the composition of Example .1 on 6 patients was evaluated 14 days, .1 month and 2 months post-treatment.
• the whitening composition was applied as in Examples I and 3. No change in the shade of the teeth was observed according to Vita Shade® evaluation.
• a flexstation 384 11 spectrometer was used with the following parameters: mode fluorescence, excitation 460 am, emission spectra 465-750 mn
• the absorption and emission spectra are shown in Figures 6a and 6b, which shows an unexpected synergy between the Eosin Y and Fluorescein components, in the absence of an oxidizing agent.

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