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GB2409976A - Tooth whitening composition - Google Patents

Tooth whitening composition Download PDF

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Publication number
GB2409976A
GB2409976A GB0401115A GB0401115A GB2409976A GB 2409976 A GB2409976 A GB 2409976A GB 0401115 A GB0401115 A GB 0401115A GB 0401115 A GB0401115 A GB 0401115A GB 2409976 A GB2409976 A GB 2409976A
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Patent type
Prior art keywords
composition
whitening
teeth
peroxide
agents
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Application number
GB0401115A
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GB0401115D0 (en )
Inventor
Andrew Hunt
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Glaxo Group Ltd
Original Assignee
Glaxo Group Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K8/00Cosmetics or similar toilet preparations
    • A61K8/18Cosmetics or similar toilet preparations characterised by the composition
    • A61K8/19Cosmetics or similar toilet preparations characterised by the composition containing inorganic ingredients
    • A61K8/22Peroxides; Oxygen; Ozone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K8/00Cosmetics or similar toilet preparations
    • A61K8/18Cosmetics or similar toilet preparations characterised by the composition
    • A61K8/30Cosmetics or similar toilet preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toilet preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/345Alcohols containing more than one hydroxy group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K8/00Cosmetics or similar toilet preparations
    • A61K8/18Cosmetics or similar toilet preparations characterised by the composition
    • A61K8/72Cosmetics or similar toilet preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/81Cosmetics or similar toilet preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
    • A61K8/8141Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by only one carboxyl radical, or of salts, anhydrides, esters, amides, imides or nitriles thereof; Compositions of derivatives of such polymers
    • A61K8/8152Homopolymers or copolymers of esters, e.g. (meth)acrylic acid esters; Compositions of derivatives of such polymers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILET PREPARATIONS
    • A61Q11/00Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

Abstract

An aqueous tooth whitening composition comprising a peroxide containing compound dispersed in an orally acceptable carrier, wherein the carrier comprises a humectant and a combination of bioadhesive agents consisting essentially of a partially neutralised carbomer and a carbomer copolymer. The humectant is preferably glycerin.

Description

TOOTH WHITENING COMPOSITION

The present invention relates to a tooth whitening composition for bleaching tooth enamel. Specifically the present invention relates to a stable aqueous tooth whitening composition comprising a peroxide containing compound.

White teeth have long been considered cosmetically desirable. Unfortunately, teeth almost invariably become discoloured in the absence of intervention. The tooth structure which is generally responsible for presenting a stained appearance is the enamel layer. Several factors contribute to enamel discoloration, but the three main factors are believed to be: (i) formation of plaque and tartar matrices on the tooth surface which then entraps stains; (ii) ingestion of certain drugs during gestational tooth formation; and (iii) discoloration due to oral cavity traumatization following which blood break-down products seep into the mineralized area of the teeth during enamel formation. This invention is primarily concerned with the first factor of tooth discoloration, that is, the natural stain which accumulates on teeth.

Over-the-counter teeth whitening preparations have been developed to address the cosmetic preference of many to restore luster to tooth enamel discolored by surface entrapped materials. While all dentifrices and mouthwashes contain some cleaning and polishing agents, some enamel deposits become intractable to being fully removed by these agents under normal use conditions. For example, smokers often develop discolored enamel because the tars and particulate in exhaled cigarette smoke collect on the teeth. Further, a number of comestibles, such as tea, or some medicinal agents, can stain or discolor tooth enamel.

There are various approaches to enamel whitening currently in general use. One approach is a physical abrading of the stain to effect stain removal. Harsher abrasives, also known as polishing agents, than those used in typical non-whitening toothpaste preparations, are employed in this approach. Most, if not all of these preparations are toothpastes, gels or powder dentifrices. The mechanical process may be supplemented or even replaced by a chemical process which may involve an oxidative or enzymatic step to effect stain removal.

The chemical process generally utilizes a tooth whitening or bleaching formulation applied to a stained tooth surface for a specified period, after which the formulation is removed. Oxidizing agents represent one of the most widely distributed and utilized active agents in commercially available tooth whitening or bleaching products. Peroxide-containing agents such as carbamide peroxide, hydrogen peroxide and calcium peroxide are the most commonly used oxidizing agents, and are typically formulated into a liquid, solution, gel or paste. However it is known that products containing such agents may lose their whitening efficacy with time. In addition aqueous peroxide formulations may have only a brief period of efficacy when applied to teeth in the oral cavity because of rapid decomposition of peroxide on exposure to the enzyme, catalase, present in high concentrations in saliva.

Moreover low viscosities of aqueous peroxide solutions do not allow the peroxide whitening agent to remain in contact with teeth for the necessary time period to effect substantive whitening because of constant flushing effects of salivary secretions. WO 03/099246 (Colgate-Palmolive) aims to address these problems with the provision of an aqueous tooth whitening liquid composition comprising an orally acceptable vehicle comprising water and monohydric alcohol having dispersed therein a film forming combination of a poly(ethylene oxide) and a carbomer.

However there remains a need for alternatives that do not suffer drawbacks encountered with known formulations. Moreover it would be desirable to provide simple formulations that do not require extensive stabilization, that are easy to manufacture and are sufficiently substantive and robust to enable once-a-day application.

It is an object of the present invention to provide a composition that meets these requirements. This object is met according to the invention by the provision of an aqueous tooth whitening composition comprising a peroxide containing compound dispersed in an orally acceptable carrier, wherein the carrier comprises a humectant - 2 and a combination of bioadhesive agents consisting essentially of a partially neutralised carbomer and a carbomer copolymer.

Although the composition of the present invention is termed "aqueous" the amount of water required is low. Suitably only amounts in the range 1-20% w/w maybe used in the composition and preferably 5-15%w/w.

The composition of the invention is suitably in the form of a gel that may conveniently be painted onto teeth. On application to teeth, the composition forms a protective barrier which adheres firmly to the teeth and retains the components of the formulation in a matrix-type environment.

The composition adheres sufficiently to remain on the teeth for a period of time e.g. up to a few hours. Suitably the composition is applied at night time, allowing peroxide activity to take place during sleep periods. During use, the peroxide is released slowly from the gel, in an amount and at such a rate as required to effect stain removal. The gel may be removed from the user's teeth by any co nvenient means e.g. brushing and/or by rinsing with a mouthwash.

The term "painted onto the teeth" above is intended to encompass all manner of applying the whitening composition to the teeth and includes sponging, coating, daubing, spraying, wiping and rubbing. Preferably the composition is applied to the teeth with a soft applicator brush. Suitably the composition is housed in a container such as a bottle or tube, and the composition is applied with a soft applicator brush.

If the composition is to be supplied in a bottle and brush this may be provided in a kit form e.g. as may be used with a conventional nail varnish kit. Alternatively the composition may be housed in a dispensing device such as a pen with an applicator brush attached thereto e.g. generally of the type used with the Brite Smile To Go_ Whitening pen.

Peroxide containing compounds used as whitening agents in the present invention include the following compounds and mixtures thereof: hydrogen peroxide e.g. as a - 3 30%w/w aqueous solution, carbamide peroxide, calcium peroxide and percarbonates.

Suitably the total amount of peroxide present in the liquid whitening composition of the invention is in the range of 1 to 30% w/w, preferably in the range 2 to 20%w/w, more preferably in the range 3 to 10%w/w.

A humectant is a key component of a composition of the invention. Suitable humectants include the following and mixtures thereof: glycerin, sorbitol, propylene glycol, sugars, such as glucose or sucrose, and low molecular weight polyethylene glycols (PEGs) i.e. in the range 200-600 e. g. PEG 200, 300, 400, and 600, available from Dow Chemicals USA, PO Box 1206, Midland MI48642. Preferred humectants include glycerin and PEGs.

Suitably the humectant is present in an amount ranging from 30 to 95%w/w, preferably in the range 50 to 85%w/w.

A combination of bioadhesive agents are included in a composition of the invention.

A bioadhesive agent will enhance the substantivity of the composition to teeth.

Suitably the bioadhesive agents of the invention exhibit mucoadhesive behaviour i.e. it has an affinity for biological surfaces such as teeth.

The combination will include a partially neutralized carbomer and a carbomer copolymer. Carbomers are synthetic high molecular weight polymers of acrylic acid that are crosslinked with either allylsucrose or allylethers of pentaerythritol.

Carbomers can be either partially or fully neutralised. Carbomers sold under the trade name "PNC 400", is a partially neutralised carbomer and is available from 3V Sigma, PO Box 219, Via Torquato Tasso, 58, 24100 Bergamo, Italy. Other suitable carbomers include the copolymers under the Pemulen_ name and polymers Ultrez_ and Carbopol(D, available from Noveon Inc. 9911 Brecksville Road, Cleveland, Ohio 44141-3247. Examples of which include Pemulen TR1, Pemulen TR2 and Ultrez 10.

Preferably the bioadhesive agents are a mixture of a partially neutralised carbomer e.g. PNC 400 and a carbomer copolymer e.g. Pemulen TR2.

Suitably the total amount of bioadhesive agents present are in an amount ranging from 0.5 to 30% w/w, preferably from 1 to 20%w/w, more pfereably 2 to 10%w/w.

Additionally, compositions of the present invention will suitably contain acceptable additives or excipients conventional in the field of oral care products including for example chelating agents such as ethylenediaminetetraacetic acid and/or citric acid, antisensitivity agents such as potassium and strontium salts, colouring agents, a fluoride source such as sodium fluoride or sodium monoflurophosphate, flavouring agents and sweetening agents. The additives or excipients used in any given composition will be compatible both with each other and with the essential ingredients of the composition such that there is no interaction which would impair the performance of the active ingredients. All additives or excipients must of course be non-toxic and of sufficient purity to render them suitable for human use.

The pH of the whitening compositions prior to use is approximately 4.5-6. During use the formulation rapidly takes up moisture from the teeth surface, allowing for the wetting and swelling of the polymer. This is turn solubilises the partially neutralized carbomer raising the pH to above this value, e.g approximately 6.5. This in itself thickens the gel by increasing its bioadhesive properties. The rise in pH observed is beneficial to the breakdown reaction of the peroxide and so increasing the bleaching efficiency of the formulation.

The whitening compositions of the present invention are prepared by adding and mixing the ingredients of the composition in a suitable vessel such as a stainless steel tank provided with a mixer. In the preparation of the composition the ingredients are suitably added to the mixer in the following order: humectant, chelating agents (if used), peroxide, bioadhesive agents and water, as appropriate to the raw material suppliers recommendation of manufacture. The fmal whitening product prepared is then suitably packaged and stored as required.

Advantageously the composition of the invention is suitably prepared as a single or one component system i.e. it does not require segregation and then mixing of ingredients just prior to use. In a second aspect of the invention there is provided a kit of parts comprising an anhydrous liquid tooth whitening composition as hereinbefore described, a container for housing the composition and an applicator for applying the composition to teeth to be whitened.

In an alternative aspect there is provided a method of whitening teeth comprising: a. preparing a tooth whitening composition as hereinbefore described; b. painting the composition onto teeth to be whitened, suitably at night-time c. maintaining the composition in contact with the teeth for a plurality of hours per day e.g. up to twelve hours per day, d. repeating steps b and c for multiple days e.g. up to fourteen days, to thereby whiten the teeth.

The present invention is illustrated by the following examples but is not limited thereby.

Examples

1. A whitening composition was prepared having the following ingredients: Ingredient %w/w Glycerin 67.80 PNC 400 2.00 Pemulen TR2 2.00 Deionised water 10.00 Carbamide peroxide 18.00 Stabilisers 0.20 Total 100.00 - 6 2. A whitening composition was prepared having the following ingredients: Ingredient %w/w Glycerin 67.80 PNC 400 1.00 Ultrez 10 3 00 Deionised water 10.00 Carbamide peroxide 18.00 Stabilisers 0.20 Total 100.00 Determination of bleaching effects using Bovine Enamel Whitening Model.

The bleaching effects of the composition disclosed in Example 1 above was determined and compared to the bleaching effects observed with a commercially available preparation.

Method Bovine teeth were used and L* (from CIE 1976 L*a*b* colour space scale) was measured at the start of the experiment using a spectrocolorimeter. Example I was applied to the teeth and these were placed into a container such that a liquid substantivity challenge was applied to the treated teeth. At the end of the treatment time the teeth were rinsed and dried and L* was remeasured using a spectrocolorimeter. This method was repeated for a number of days to mimic in-vivo night time use of the product. At the end of the experiment the overall change in L* (i.c AL) was calculated. - 7

Results Sample AL after 12 hrs treatment

Example 1 7.24

Crest Night Effects 5.67 Deionised water 1.24

Conclusion

The results indicate that the change in L (AL)after 12 hours treatment was higher than a commercially available night time product. The results are illustrated graphically in Fig 1 below. - 8

Claims (6)

  1. Claims 1. An aqueous liquid tooth whitening composition comprising a
    peroxide contaning compound dispersed in an orally acceptable carrier, wherein the carrier comprises a humectant and a combination of bioadhesive agents consisting essentially of a partially neutralised carbomer and a carbomer copolymer.
  2. 2. An aqueous liquid tooth whitening composition according to claim I wherein the peroxide is selected from carbamide peroxide, and mixtures of carbamide peroxide with hydrogen peroxide
  3. 3. An aqueous liquid tooth whitening composition according to claim 1 or claim 2 wherein the humectant is glycerin.
  4. 4. An aqueous liquid tooth whitening composition according to any one of claims 1 to 3 wherein the bioadhesive agents are selected from a partially neutralised carbomer and a carbomer copolymer.
  5. S. A kit of parts comprising an anhydrous liquid tooth whitening composition according to any one of claims 1 to 4, a container for housing the composition and an applicator for applying the composition to teeth to be whitened.
  6. 6. A method of whitening teeth comprising: a. preparing a tooth whitening composition according to any one of claims 1 to 4; b. painting the composition onto teeth to be whitened; c. maintaining the composition in contact with the teeth for a plurality of hours per day; and then d. repeating steps b and c for multiple days to thereby whiten the teeth.
GB0401115A 2004-01-19 2004-01-19 Tooth whitening composition Withdrawn GB0401115D0 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
GB0401115A GB0401115D0 (en) 2004-01-19 2004-01-19 Tooth whitening composition

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Application Number Priority Date Filing Date Title
GB0401115A GB0401115D0 (en) 2004-01-19 2004-01-19 Tooth whitening composition

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GB2409976A true true GB2409976A (en) 2005-07-20

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Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5208010A (en) * 1991-06-17 1993-05-04 Dental Concepts Inc. Tooth whitening dentifrice
US5302374A (en) * 1993-04-21 1994-04-12 Dental Concepts Inc. Oral hygiene system
WO2000028953A1 (en) * 1998-11-12 2000-05-25 Ultradent Products, Inc. Compositions and methods for whitening teeth
US20030219390A1 (en) * 2002-05-24 2003-11-27 Santarpia R. Peter Liquid tooth whitening composition
US6669930B1 (en) * 2003-01-15 2003-12-30 Colgate Palmolive Company Liquid tooth whitening gel

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5208010A (en) * 1991-06-17 1993-05-04 Dental Concepts Inc. Tooth whitening dentifrice
US5302374A (en) * 1993-04-21 1994-04-12 Dental Concepts Inc. Oral hygiene system
WO2000028953A1 (en) * 1998-11-12 2000-05-25 Ultradent Products, Inc. Compositions and methods for whitening teeth
US20030219390A1 (en) * 2002-05-24 2003-11-27 Santarpia R. Peter Liquid tooth whitening composition
US6669930B1 (en) * 2003-01-15 2003-12-30 Colgate Palmolive Company Liquid tooth whitening gel

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Publication number Publication date Type
GB0401115D0 (en) 2004-02-18 grant

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