NL1004386C2 - Oral care product. - Google Patents

Description

Title: Oral care product

The present invention relates to a fluoride-containing oral care agent, wherein the effectiveness of the fluoride contained in the agent is enhanced.

5 Oral care products are those products that are not or hardly swallowed during normal use, but which remain in the oral cavity for some time, whereby the product comes into intensive contact with almost all dental surfaces. Examples of such agents are toothpastes, dental polishes, chewing gum, mouthwashes and mouth powders.

Regular brushing and care of the oral cavity using an appropriate agent such as a toothpaste or mouthwash will help prevent rapid plaque build-up and other conditions from occurring, but even regular brushing is not enough to completely remove plaque and combating dental caries.

It is known that it is possible to combat the caries progression by adding various compounds to oral care products. The most well-known compounds are those which provide fluoride ions, such as NaF, tin fluoride, long chain amine fluoride and sodium monofluorophosphate. The action of such fluoride compounds is based on stimulation of mineral transformations in the tooth enamel.

However, the action of such fluoride compounds is limited in time and effectiveness, especially when using sodium fluoride as a fluoride source. It is therefore an object of the invention to provide an oral care agent which exhibits a markedly enhanced action of fluoride, in particular from sodium fluoride.

Surprisingly, it has been found that the use of a combination of xanthan gum and a carboxylated vinyl polymer in fluoride-containing oral care products 1004386 2 exhibits a particularly good effect on the action of the fluoride. This is especially true when using sodium fluoride as a fluoride source.

The invention therefore relates to a fluoride-containing oral care agent comprising a combination of xanthan gum and a carboxylated vinyl polymer, as well as the usual excipients.

As usual auxiliary substances, the substances commonly used for oral care products can be used. Examples 10 thereof include anti-bacterial agents, polishing agents, carrier, wetting agent, thickener, flavors and fragrances, anti-tartar agents, teeth sensitivity control agents, wound healing agents, as well as activity-enhancing agents such as the 15 various polymers. It may also be useful to include hydrogen peroxide-producing enzyme systems in the agents.

The presence of fluoride-producing agents in the oral care compositions of the invention is important.

Suitable compounds can be completely or slightly water-soluble. Suitable compounds are the inorganic fluoride salts, such as water-soluble alkali and alkaline earth metal salts, for example sodium fluoride, potassium fluoride, barium fluoride, calcium fluoride, ammonium fluoride, copper fluoride or zinc fluoride. Alkali metal and tin fluoride, such as sodium fluoride, are preferred.

The amount of the fluoride-providing compound depends to some extent on the nature of the compounds, the solubility and the nature of the oral care agent. However, it should be a non-toxic, effective amount. In toothpastes, this will generally be between 0.005 to 3.0%, which amount is capable of providing up to about 5000 ppm of fluorine ions. A suitable minimum amount is preferably 300 ppm. In general, it is preferable to use an amount that results in the presence of 300 to about 2000, more particularly 800 to about 1500 ppm, of fluoride ions in the oral care agent. In the case of using alkali metal fluorides and tin fluorides, the fluoride compound is present in an amount of up to about 2% by weight, more in particular from 0.5 to 1% by weight.

According to the invention it is important that a combination of a xanthan gum and an effective amount of carboxylated vinyl polymer is present. This amount depends on the effectiveness of the polymer, which is determined inter alia by the amount of carboxyl groups and the molecular weight. Suitable amounts are between 0.001 and 10% by weight, based on the weight of the agents. The amount of xanthan gum can range from 0.001 to 4% by weight.

Suitable types of carboxylated vinyl polymers are commercially available under the trademark Carbopol® from B.F. Goodrich. More particularly, types 956, 980, 2984, 5984, and 974 are suitable, with the last three types being particularly preferred.

To further improve the action of the oral care agents and to enhance the effectiveness of the fluoride, it may be desirable to add two or twenty trivalent cations. Examples thereof are magnesium, calcium, titanium, tin and / or aluminum ions, generally in the form of their water-soluble salts. Suitable amounts thereof are between 0.1 and 5% by weight calculated on the basis of the metal ion to the weight of the oral care agent.

In order to obtain an antibacterial activity, one can use known antibacterial agents, such as xylitol, a diphenyl ether or a phenol derivative, such as triclosan or bromochlorophene. However, it is also possible to use one of the other antibacterial agents. More specifically, one may consider using a lantibiotic, such as nisin, optionally in combination with triclosan or any of the other components mentioned.

In case the oral care agent is in the form of a toothpaste, it also contains a polishing agent. Common polishing agents are water-insoluble sodium metaphosphate, potassium metaphosphate, tricalcium phosphate, dehydrated 1004386 4 calcium phosphate, anhydrous dicalcium phosphate, calcium pyrophosphate, magnesium orthophosphate, trimagnesium phosphate, aluminum oxide, alumina hydrate, calcium carbonate, calcium carbonate polishes. Other suitable polishing materials include the particulate thermosetting resins such as melamine phenol, and urea formaldehydes, as well as cross-linked polyepoxides and polyesters. Preferred polishing agents include silica having a particle size from 10 to about 7 µm, an average particle size of about 1.1 µm and an area of up to 5 cm 2 / g, silica gel or colloidal silica, as well as complex amorphous alkali metal alumino silicate.

Preferably, if visually clear gels are desired, a colloidal silica polishing agent is used

Syloid 72 and Syloid 74 or Santocel 100 have been used, as have alkali metal aluminosilicate complexes. These materials have refractive indices close to the refractive index of the gel systems used for this.

The polishing agent is generally present in the toothpaste in amounts of 10-99% by weight. Preferably, however, this is 10-75%.

In a toothpaste, the liquid carrier will generally contain water and a humectant in amounts of 10-90% by weight. Glycerine, propylene glycol, sorbitol, polypropylene glycol and / or polyethylene glycol are examples of suitable humectants / carriers. It may also be advantageous to use liquid mixtures of water, glycerine and sorbitol. The clear gels, where the refractive index is an important consideration, preferably use 3-30 wt.% Water, 0-80 wt.% Glycerine and about 20-80 wt.% Sorbitol.

It is known to add phosphate compounds to oral care products. Known inorganic phosphate compounds are trimetaphosphate and calcium phosphate. It is also known to add organic phosphate compounds to oral care products. These substances adhere strongly to the 1004386 5 tooth enamel, reducing the surface tension.

This would reduce the adhesion of plaque to the enamel. Preferably polyphosphates are used, such as linear, tri and / or tetra polyphosphates, most preferably in amounts from 5 to about 15% by weight, based on the weight of the oral care product.

Toothpastes and gels generally contain a natural or synthetic thickener or gelling agent in amounts from about 0.1 to 10, preferably from about 0.5 to about 5, weight percent. A suitable thickening agent is synthetic hectorite, a synthetic colloidal magnesium alkali metal silicate complex clay available, for example, as Laponite (e.g. CP, SP 2002, D) from Laporte Industries Limited.

Other suitable thickeners include Irish moss, tragacanth gum, starch, polyvinylpyrrolidone, hydroxyethyl propyl cellulose, hydroxybutylmethyl cellulose, hydroxypropylmethyl cellulose, hydroxyethyl cellulose (e.g. Natrosol), sodium carboxymethyl cellulose, and colloidal silica.

Suitable flavorings or sweeteners can also be used. Examples of suitable flavor components are the flavor oils such as spearmint, peppermint oil, wintergreen, sassafras, cloves, sage, eucalyptus, marjoram, lemon, orange and methyl salicylate. Suitable sweeteners include sucrose, lactose, maltose, sorbitol, sodium cyclamate, perillartine, aspartame, saccharin and the like. The amount of the combined flavors and sweeteners together is preferably 0.1-5% by weight of the preparation.

Oral care compositions according to the invention may contain components that reduce the sensitivity of teeth, such as specific alkali metal salts (strontium salts and / or potassium nitrate and / or potassium citrate). Wound healing agents may also be present, such as alantoin, chlorophyll, tocopherol and herbal extracts. Activity-enhancing agents, ie agents which extend the residence time of the active components in the oral cavity 1004386 6, are in particular all kinds of polymers such as Gantrez and phosphonates.

In a preferred embodiment, the oral care agents also contain an enzyme system as described in U.S. Patents 4,150,113 and 4,871,532. The hydrogen peroxide-producing enzyme systems described therein also have an beneficial effect on the reduction of bacterial activity in the oral cavity. The most effective enzyme is the oxidoreductase enzyme glucose oxidase. This enzyme can be present in combination with other enzymes such as amyloglucosidase, dextranase and / or mutanase, optionally in combination with zinc ion-providing compounds and / or 8-hydroxyquinoline derivatives.

Other enzymes such as lactoperoxidase, lactoferrin and lysozyme may also be present and provide an oral care agent with attractive additional properties.

Surfactants may also be present in the oral care compositions, more particularly non-ionic surfactants, although anionic surfactants may also be used.

Examples of such surfactants which may be present in amounts between 0.01 and 5% by weight include ethoxylated alcohols and the like.

In case the oral care agent is a mouthwash, water is preferably used as a carrier, optionally in combination with a humectant, such as glycerol.

The manufacture of the oral care preparations according to the invention comprises the usual methods known to the skilled person.

The invention is now illustrated by some non-limiting examples.

EXAMPLE 1 A toothpaste was prepared in a manner usual for toothpastes. The compositions thereof were as follows.

1004386 7 silica 20.00 20 20 20 sodium fluoride 0.32 0.32 0.32 0.32 5 sorbitol 10 42 36 20 glycerol 3 - 3 5

Polyol - 4.5 2.0 PEG 3 2.5 2.5 3 xylitol - 10-- 10 xanthan gum 1.0 0.4 0.6 1.0

Carbopol 0.2 0.2 0.2 0.2 titanium dioxide 0.5 - - 0.5 phosphate buffer 1 111 α-olefin sulfonate 1.5 1.5 1.5 1.5 15 water to 100 100 100 100 1004 386

Claims (10)

A fluoride-containing oral care agent comprising an effective amount of a combination of xanthan gum and a carboxylated vinyl polymer as well as the usual excipients. An oral care agent according to claim 1, wherein the amount of carboxylated vinyl polymer is between 0.001 and 2.0 wt%. Oral care agent according to claim 1 or 2, wherein the amount of xanthan gum is between 0.001 and 4% by weight. Oral care agent according to claim 1, wherein sodium fluoride is used as the fluoride source. Oral care agent according to claims 1-4, comprising mouthwash, toothpaste or gel. Oral care agent according to claim 5, comprising a toothpaste or gel, which also contains an abrasive and a thickening agent, as well as an aqueous carrier. Oral care agent according to claim 5, comprising a mouthwash which also contains an aqueous vehicle and an aroma. 8. Oral care agent according to claims 1-6, in the form of a toothpaste, wherein as auxiliary substances one or more of the components are present from the group consisting of water, antibacterial agents, polishing agents, foaming agents, enzymes, dyes, flavors and moisturizers. Use of an effective amount of a combination of a fluoride, a carboxylated vinyl polymer and xanthan gum, in combination with at least one or more excipients in oral care products. 1004386 Use according to claim 9 for enhancing the effectiveness of the fluoride. 1004 386 COOPERATION TREATY (PCT) REPORT ON NEWNESS RESEARCH OF INTERNATIONAL TYPE OF LOAN IDENTIFICATION OF THE NATIONAL APPLICATION Identification of the applicant to the party | __Nw 9353_ | Neoenanase application no. Submissionscaaim 1004386 30 October 1996 Invited priority oaajm Applicant (Name) 'ji SARA LEE / DE NV j OaAim of just reconciliation for a subject of intemonaonate type By oe Insanae for Intemasonal Research * (ISA) to just reconcile for a research of internaoonaaj type begexene nr SN 29802 NL __ i. CLASSIFICATION OF THE SUBJECT (with Decassmg of various etassitcaoes. Specify all «tassificaoesym boats) j According to the Ina ma aorta ie dassilicaae (IPC) Int.Cl.a 61 K 7/16 _ I II. FIELDS OF TECHNIQUE EXAMINED j _Qnaerzocftte minimum documentation____J Classification system I_Classification scattering __-_ I i | £! f Int.Cl.6: I A 61 K j! I! i i i Onaorzocnte anoere aocjmamaoa at a minimum occumenaoe insofar as agered documents are ceaeaed in a researcher ζλπ j o eyes around and | i j i! j i i __i III. I 1 NO RESEARCH POSSIBLE FOR CERTAIN CONCLUSIONS (remarks including supplemental! IV. LACK OF UNITY OF INVENTION (cpmerKirtgen 00 additionalincsoiafl) = orn PC7; iSAi23tlaiCê ISS *