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WO1992004006A1 - Composition dentaire desensibilisante - Google Patents

Composition dentaire desensibilisante Download PDF

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Publication number
WO1992004006A1
WO1992004006A1 PCT/EP1991/001616 EP9101616W WO9204006A1 WO 1992004006 A1 WO1992004006 A1 WO 1992004006A1 EP 9101616 W EP9101616 W EP 9101616W WO 9204006 A1 WO9204006 A1 WO 9204006A1
Authority
WO
WIPO (PCT)
Prior art keywords
strontium
calcium
anion
composition
source
Prior art date
Application number
PCT/EP1991/001616
Other languages
English (en)
Inventor
Rudi Dominique Neirinckx
Original Assignee
Rudi Dominique Neirinckx
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.)
Filing date
Publication date
Application filed by Rudi Dominique Neirinckx filed Critical Rudi Dominique Neirinckx
Publication of WO1992004006A1 publication Critical patent/WO1992004006A1/fr

Links

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
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • 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
    • A61K8/20—Halogens; Compounds thereof
    • A61K8/21—Fluorides; Derivatives thereof
    • 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
    • A61K8/24—Phosphorous; Compounds thereof
    • 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
    • A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
    • A61K2800/88—Two- or multipart kits

Definitions

  • This invention relates to a desensitizing dental composition.
  • Hypersensitivity is a common phenomenon among dental patients that often causes the patient to reject dental treatment.
  • the sensitivity may be local or general and very often
  • Treatment of hypersensitivity has resulted in varying degrees of success.
  • the treatment often has relied upon the astringent or coagulating effects of various agents, occulating properties or the ability to render calcium less soluble.
  • agents include formaldehyde, silver nitrate, zinc oxide and strontium chloride.
  • tooth hypersensitivity can be countered by applying one or more specifically formulated compositions to the tooth surface, which compositions contain ionic species which result in the formation of precipitates within the enamel tubules with the formation of precipitated salts or other compounds having a particularly low solubility.
  • in situ mixing of cations and anions, or reaction with oral liquids leads to the formation of low-solubility compounds leading to increased deposition of these compounds on tooth surfaces and in dentinal tubules which can lead to dentinal desensitisation.
  • the present invent ion provides a system allowing the accelerated deposition of calcium and/or strontium salts in or near the dentinal tubules of the tooth in order to alleviate the pain of dental sensitivity.
  • This accelerated deposition may be achieved by in situ formation of low solubility compounds in two ways: (1) The mixing immediately prior to or at the time of
  • a suitable anionic component which upon interaction with oral liquids such as saliva, can decompose to form an anionic species which can lower the solubility of the strontium and/or calcium.
  • NaMFP sodium monofluorophosphate
  • This fluoride and/or phosphate will react with Ca 2+ and/or Sr 2+ and lower the solubility of these
  • composition said system comprising a source of a first cationic species and a source of a second anionic species, both sources being in physiologically acceptable form and said sources being segregated from each other, said first ionic species being selected from calcium and/or strontium ions and said second ionic species being selected from anions which combine with the first ionic species to form a salt whose solubility is less than 10 mg in 100 ml of cold water.
  • a dispensing means arranged to dispense said sources of ions so that a mixture thereof may be formed on, or immediately prior to application (of the composition) to, the teeth.
  • a densensitising composition comprising a physiologically acceptable source of strontium and/or calcium ions and a
  • physiologically acceptable source of a suitable anion the anions being bound in a form such that the sources are unreactive with each other at ambient conditions (e.g. during storage) but upon reaction with oral liquids such as saliva a precipitate of a salt or other compound of the anion and cation is formed.
  • the precipitate it is preferred, but not essential, for the precipitate to have a solubility of less than 10 mg in 100 ml of cold water. It will be understood that with this modified form of the invention, the sources of cation and anion do not have to be kept apart from each other prior to use.
  • densensitising composition which includes a physiologically acceptable source of strontium and/or calcium ions and a physiologically acceptable source of anion as described above, wherein these two sources are maintained separate from each other and are not admixed until application to the teeth is desired.
  • a precipitate may be formed whose action is desensitizing.
  • the package may include compartments, one for housing the calcium and/or strontium ions in the absence of said specified anion, and the other for housing the specified anion, preferably in the absence of calcium and/or strontium ions.
  • the said sources of ions can then be dispensed simultaneously on the teeth surfaces.
  • dentinal desensitizing compositions have been formulated using alkaline earth metals, but always in the form of soluble salts. It was felt that insoluble salts would act only as abrasives and could not provide the cation species necessary for deposition in, or in the proximity of, the dentinal tubule. It has now been found in accordance with this invention however, that in situ formation of low solubility salts in the process of dental
  • desensitization can be effective. It is postulated that in the present invention the desensitizing action occurs due to the formation of particles, e.g. crystals, of insoluble precipitate inside the dentinal tubles, thereby blocking them.
  • the calcium or strontium ion and the anion, respectively are provided in their respective sources in concentrations such that upon mixing small particles can be formed in the tubules in a suitably short time, i.e. before the reagent diffuses out.
  • Physiologically safe reagents should be used as the sources of the ions to form the precipitates.
  • acceptable anions that may be employed to obtain with calcium and/or strontium, precipitates of the required low solubility include fluoride, orthophosphate, pyrophosphate, metaphosphate, carbonate and oxalate; it being understood that not all these anions are suitable with both cations; for example the solubility of
  • strontium fluoride is above 11 mg per 100 ml in cold water.
  • the approximate solubilities of some of the preferred salts in 100 ml of cold water are given below:
  • Strontium fluoride (which may be formed as a precipitate on admixing separate compositions containing stontium ions as the sole cationic species and fluoride ions as the sole anionic species, e.g. as desribed in my previous International Patent Application No
  • W087/2890 has a solubility of around 11 mg/100ml. Accordingly compositions which on use result in the formation of strontium fluoride as the sole low-solubility salt do not form part of Variant (1)-the present invention. The formation of strontim fluoride is however encompassed by Variant (2).
  • the invention further provides a kit for desensitizing the dental area of a patient having hypersensitive teeth which comprises supplies of two separate dentifrice or mouthwash compositions, one of said compositions containing a source of a physiologically acceptable free calcium and/or strontium ion and the other of said compositions containing a physiologically acceptable source of free anion, and optionally instructions for admixing said compositions on or
  • the invention also provides the use of a physiologically acceptable source of strontium and/or calcium cations to produce industrially a kit or system for the treatment of teeth in a combination therapy involving the application of said cations and anions which will combine with the chosen cations to produce a precipitate having a solubility of less than 10 mg in 100 ml of cold water, using separate compositions containing respectively said cations and said anions.
  • the invention further provides the use of a physiologically acceptable source of anions to produce industrially a kit or system for the treatment of teeth in a combination therapy involving the application of said anion and cations selected from calcium and/or strontium ions which will combine with the chosen anion to produce a precipitate having a solubility of less than 10 mg per 100 ml of cold water using separate compositions containing respectively said anions and said cations.
  • any convenient means for effecting separation of the source of calcium and/or strontium ions and the source of the prescribed anion according to the first aspect of the invention can be utilized.
  • a single container may be compartmentalized so that the calcium and/or strontium containing source and the anion containing source are housed in separate compartments and are not admixed until applied to the teeth or immediately before such application.
  • the segregating means may comprise a physiologically acceptable composition located between and separating the two sources in a single compartment and adapted to be dispensed with said segregated ion-containing phases.
  • the calcium and/or strontium containing source is preferably maintained at a pH of between about 3 and about 7 more preferably between about 5 and 7 so that the calcium and/or strontium ions are solubilized within the source at the desired concentration.
  • the preferred sources of strontium and calcium are strontium and calcium chlorides since they are readily dissolved in an aqueous medium.
  • the sources of the strontium and/or calcium ions and the anion are most conveniently each maintained in a viscous aqueous medium such as in the form of a gel or a paste.
  • the preferred concentration ranges for the active ingredients are as follows (most preferred concentrations in brackets).
  • the strontium and/or calcium and the chosen anion be present in either a toothpaste composition suitable for cleaning teeth, in a mouthwash with desensitizing properties, or in a gel composition of the type commonly used by dentists in order to apply treatment compositions to the teeth or gum surface.
  • a toothpaste composition suitable for cleaning teeth in a mouthwash with desensitizing properties
  • a gel composition of the type commonly used by dentists in order to apply treatment compositions to the teeth or gum surface.
  • the compositions of this invention may also contain other excipients.
  • anionic binding agents are preferably avoided
  • the toothpaste formulations may contain abrasive, binding agents, humectants, thickening agents, surfactants, preservative, flavouring agents, sweetening agents, anti-bacterial agents, colouring agents, anti-corrosive agents, pH-adjusters and anti-plaque additives.
  • Mouthwash formulations may contain humectants, alcohol,
  • flavouring agents sweetening agents, preservatives, antibacterial agents, colouring agents, pH-adjusters, anti-plaque additives and surfactants.
  • compositions used in accordance with the invention contain abrasives
  • the abrasive may be synthetic silicas or
  • abrasive is generally present in an amount of 10 to 60% by weight of the composition.
  • composition of the invention may include one or more
  • non-ionic binding agents such as hydroxy ethylcellulose, or xanthan gums. These binding agents may be present in an amount, for example of 0.1% to 5% by weight of the composition.
  • compositions may also include one or more humectants in a total amount, for example of up to 90% by weight of the composition.
  • humectants include glycerin, sorbitol syrup, polyethylene glycols and propylene glycol.
  • composition may include thickening agents in an amount for example of up to 20%, preferably 0.5% to 10% by weight of the
  • thickening agents include pyrogenic silica and natural and synthetic clays, such as hydrated sodium magnesium lithium silicates.
  • compositions may also include one or more preservatives for example benzoic acid, methyl p-hydroxybenzoate or sodium benzoate.
  • the preservatives may be present in an amount, for example up to 5%, preferably 0.05% to 1%, by weight of the composition.
  • Chloroform may alternatively or additionally be included as a preservative in an amount, for example, of up to 5%, preferably 0.1% to 2%, by weight of the composition. Chloroform also acts as a flavouring agent.
  • flavouring agents may be included in an amount, for example of up to 5%, preferably 0.5% to 2%, by weight of the composition.
  • flavouring agents include conventional flavouring oils, such as oils of spearmint, peppermint, wintergreen and cloves.
  • Sweetening agents especially saccharin, may additionally or
  • compositions alternatively be included in an amount, for example of up to 5%, preferably 0.1% to 1% by weight of the composition.
  • compositions may also include anti-bacterial agents in an amount of, for example up to 5%, preferably 0.1% to 1%, by weight of the composition.
  • a particularly suitable anti-bacterial agent is chlorhexidine (1,1'-hexamethylene-bis-[5-(4-chlorophenyl)biguanide]).
  • compositions may also include anti-plaque additives, e.g. sparingly water-soluble zinc salts, especially zinc citrate, in an amount for example of from 0.25% to 10% by weight of the composition.
  • anti-plaque additives e.g. sparingly water-soluble zinc salts, especially zinc citrate, in an amount for example of from 0.25% to 10% by weight of the composition.
  • anti-plaque additives include xylitol and 8-hydroxyquinoline and derivatives thereof, e.g. 4,5-dimethyl and 5-methoxy-4-methyl-8-hydroxyquinoline.
  • additives may include one or more of colouring agents; anti-corrosive agents, e.g. sodium silicate; pH adjusters, e.g. citric acid.
  • colouring agents e.g. sodium silicate
  • pH adjusters e.g. citric acid.
  • Each of these agents may be present in amounts, for example of up to 2%, preferably 0.1% to 1%, by weight of the composition.
  • compositions are usually aqueous compositions and include water in an amount of up to, for example 50%, preferably 10% to 30%, by weight of the composition.
  • an aqueous solution of the ion may be admixed with a pharmaceutically acceptable gelling agent such as sodium
  • thixotropic properties of the resultant gel can be varied by varying the concentration of the gelling agent, with increased concentrations providing increased thixotropic properties as is well known in the art.
  • aqueous solutions of calcium and/or strontium and of the anion may, for example, be enclosed in a two-compartment bottle in accordance with the first spect of the invention from which both solutions can be dispensed simultaneously immediately prior to use as a mouthwash.
  • compositions utilized in the present invention are:
  • the concentration of the calcium and/or strontium compound may be such that in the final composition it comprises between 0.01 and 20 weight per cent of the final composition (exclusive of the prescribed anion-containing composition), preferably between 1 and 10 weight percent.
  • the prescribed anion-containing composition in the aqueous solution may be such that concentration in the final composition is between 0.01 and 5 weight percent (exclusive of the calcium and/or strontium containing phase), more preferably between 0.1 and 3 weight percent.
  • the conventional agents utilized to form a paste or a gel or the like may then be admixed with the aqueous solution to form the final composition.
  • a suitable container (10) useful for housing said first and second sources in accordance with the first aspect of the present invention comprises an outer wall formed of a flexible material such as a polymer which can contain a sheet of flexible metal such as aluminium (12).
  • the container (10) is segmented into two compartments (14) and (16) by means of a wall (18) which is sealed to the interior surface of the outer wall (12).
  • One end (20) of the container is sealed while the opposing end (22) is open so that it can be conveniently opened or closed in a conventional manner such as with a screw cap (not shown).
  • Compartment (14) can house either the cation-containing source or the anion-containing source while the other compartment (16) can house the source not housed within compartment (14).
  • containing source and the anion-containing source can be housed in separate containers from which they can be conveniently dispensed just prior to being topically applied to the dental area of the user.
  • an intermediate layer of toothpaste, gel or the like containing neither cation nor anion can be interposed between the layer of calcium and/or strontium source and the layer of anion source within the same container so that mixture of the ion containing layers does not occur until use.
  • the cation and anion containing sources can be housed together in a container with a single compartment as is used commonly for mouthwashes, gels and toothpaste, because precipitate formation does not occur until the anion is released from its chemically bound form by contact with oral liquids.
  • Aqueous solutions were made of 102 SrCl 2 .6H 2 O, 10%
  • the resulting fine precipitate was allowed to settle overnight and filtered off.
  • a precipitate forms rapidly and is heavy within five minutes. Even in a four-fold diluted solution, the saliva causes a precipitate to form.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cosmetics (AREA)

Abstract

L'invention décrit des compositions servant à soulager l'hypersensibilité dentaire en appliquant une ou plusieurs compositions spécialement formulées à la surface de la dent. Les compositions contiennent des espèces ioniques qui provoquent la formation de précipités à l'intérieur des tubules de l'émail, avec la formation de sels ou autres composés précipités dont le point de dissolution est particulièrement bas, soit en mélange in situ de cations et d'anions, soit en réaction avec les liquides buccaux. La formation de composés peu solubles provoque l'augmentation du dépôt desdits composés sur les surfaces dentaires et les tubules dentinaires, ce qui peut produire une désensibilisation dentinaire.
PCT/EP1991/001616 1990-08-29 1991-08-17 Composition dentaire desensibilisante WO1992004006A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB909018836A GB9018836D0 (en) 1990-08-29 1990-08-29 Desensitising dental composition
GB9018836.8 1990-08-29

Publications (1)

Publication Number Publication Date
WO1992004006A1 true WO1992004006A1 (fr) 1992-03-19

Family

ID=10681328

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1991/001616 WO1992004006A1 (fr) 1990-08-29 1991-08-17 Composition dentaire desensibilisante

Country Status (5)

Country Link
AU (1) AU8406991A (fr)
GB (1) GB9018836D0 (fr)
IE (1) IE913026A1 (fr)
WO (1) WO1992004006A1 (fr)
ZA (1) ZA916570B (fr)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995007685A1 (fr) * 1993-09-13 1995-03-23 American Dental Association Health Foundation Solutes buccaux, dentifrices et gommes a macher contenant un complex calcium et fluorure
US5476647A (en) * 1993-09-13 1995-12-19 American Dental Association Health Foundation Complex calcium and fluoride containing mouth rinses, dentifrices, and chewable tablets
EP0721773A3 (fr) * 1994-12-13 1997-06-18 Sun Medical Co Ltd Composition de soin dentaire pour soulager l'hypersensibilité de la dentine
WO1999003445A3 (fr) * 1997-07-17 1999-04-08 Henkel Kgaa Agents de soin a usage buccal et dentaire pour dents sensibles
WO1999044570A1 (fr) * 1998-03-06 1999-09-10 Italmed S.N.C. Di Galli G. E Pacini G. Composition dentaire desensibilisante
EP1120106A1 (fr) * 2000-01-25 2001-08-01 Rudi Dominique Dr. Neirinckx Procédés pour boucher des tubes dentines par formation in-situ de précipites difficilement solubles
US9180318B2 (en) 2010-03-09 2015-11-10 Conopco, Inc. Stable oral care compositions

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2329292A1 (fr) * 1975-10-31 1977-05-27 Nat Res Dev Compositions remineralisantes pour les surfaces dentaires
US4080440A (en) * 1974-12-13 1978-03-21 The Procter & Gamble Company Method for remineralizing tooth enamel
EP0080293A2 (fr) * 1981-11-25 1983-06-01 Murray L. Schole Dentifrice contenant du fluorure
EP0089136A2 (fr) * 1982-03-10 1983-09-21 The Procter & Gamble Company Produits d'hygiène orale
WO1987002890A1 (fr) * 1985-11-13 1987-05-21 Rudi Dominique Neirinckx Composition dentaire de desensibilisation
EP0263638A2 (fr) * 1986-10-02 1988-04-13 Unilever Plc Composition orale
WO1990010435A2 (fr) * 1989-03-13 1990-09-20 American Dental Association Health Foundation Collutoires, dentifrices, gels et pastilles a macher contenant du fluorure

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4080440A (en) * 1974-12-13 1978-03-21 The Procter & Gamble Company Method for remineralizing tooth enamel
FR2329292A1 (fr) * 1975-10-31 1977-05-27 Nat Res Dev Compositions remineralisantes pour les surfaces dentaires
EP0080293A2 (fr) * 1981-11-25 1983-06-01 Murray L. Schole Dentifrice contenant du fluorure
EP0089136A2 (fr) * 1982-03-10 1983-09-21 The Procter & Gamble Company Produits d'hygiène orale
WO1987002890A1 (fr) * 1985-11-13 1987-05-21 Rudi Dominique Neirinckx Composition dentaire de desensibilisation
EP0263638A2 (fr) * 1986-10-02 1988-04-13 Unilever Plc Composition orale
WO1990010435A2 (fr) * 1989-03-13 1990-09-20 American Dental Association Health Foundation Collutoires, dentifrices, gels et pastilles a macher contenant du fluorure

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995007685A1 (fr) * 1993-09-13 1995-03-23 American Dental Association Health Foundation Solutes buccaux, dentifrices et gommes a macher contenant un complex calcium et fluorure
US5476647A (en) * 1993-09-13 1995-12-19 American Dental Association Health Foundation Complex calcium and fluoride containing mouth rinses, dentifrices, and chewable tablets
EP0721773A3 (fr) * 1994-12-13 1997-06-18 Sun Medical Co Ltd Composition de soin dentaire pour soulager l'hypersensibilité de la dentine
US5766328A (en) * 1994-12-13 1998-06-16 Sun Medical Co., Ltd. Dental composition for relieving dentin hypersensitivity
WO1999003445A3 (fr) * 1997-07-17 1999-04-08 Henkel Kgaa Agents de soin a usage buccal et dentaire pour dents sensibles
WO1999044570A1 (fr) * 1998-03-06 1999-09-10 Italmed S.N.C. Di Galli G. E Pacini G. Composition dentaire desensibilisante
EP1120106A1 (fr) * 2000-01-25 2001-08-01 Rudi Dominique Dr. Neirinckx Procédés pour boucher des tubes dentines par formation in-situ de précipites difficilement solubles
US9180318B2 (en) 2010-03-09 2015-11-10 Conopco, Inc. Stable oral care compositions

Also Published As

Publication number Publication date
GB9018836D0 (en) 1990-10-10
ZA916570B (en) 1992-04-29
IE913026A1 (en) 1992-03-11
AU8406991A (en) 1992-03-30

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