EA041473B1 - ORAL CARE COMPOSITIONS - Google Patents

Description

The present invention relates to oral care compositions that improve the whiteness of teeth.

Compositions containing pigments that whiten teeth are described in WO 16099544 and WO 150975709.

Document No. EP 1935395 describes a whitening composition containing a pigment having a hue angle, h, in the CIELAB system of 220 to 320°, and a soluble pigment deposition additive.

It is an object of the present invention to provide an improved whitening effect on teeth.

Brief description of the invention

In a first aspect, the present invention relates to an oral care composition comprising an alkoxylated alcohol nonionic surfactant, a pigment having a CIELAB hue angle, h, of 220 to 320°, and a water-soluble polymer deposition aid. a pigment containing copolymers of maleic anhydride and methyl vinyl ether with a molecular weight of 200,000 or more, in which the anhydride fragment may be in a partially or completely hydrolyzed or alcoholized form.

In a second aspect, the present invention relates to the use of the composition described above for improving tooth whitening.

Detailed description of the invention

Compositions according to the present invention contain a pigment which should have a hue angle, h, in the CIELAB system from 220 to 320°, most preferably from 250 to 290°. A detailed description of the hue angle can be found on page 57 of the 3rd edition of Color Chemistry by H. Zollinger, published by Wiley-VCH.

Pigment is generally understood to mean an opaque/material which is insoluble in the respective medium at the respective temperature. In this it differs from dyes, which are soluble. In the context of the present invention, the appropriate medium is human saliva, the liquid medium in which the composition is applied, at the temperature of the oral cavity during brushing, i.e. up to 37°C. As a reasonable approximation, water can be considered the appropriate medium and 25°C can be considered the corresponding temperature.

Preferably, the pigment is capable of reflecting enough light to make the treated tooth noticeably whiter than its original color. Preferably the pigment is dyed such that its natural color is in the range of violet-red to green-blue, preferably violet to blue.

Preferably the pigment is violet or blue, more preferably one of the pigments listed in the Color Index International. These pigments are listed as Pigment Violet 1 to Pigment Violet 56 and Pigment Blue 1 to 83.

Preferred Pigment Violets are Pigment Violet 1, 1:1, 1:2, 2, 3, 5:1, 13, 19, 23, 25, 27, 31, 32, 37, 39, 42, 44, and 50.

Preferred Pigment Blues are Pigment Blues 1, 2, 9, 10, 14, 15, 15:1, 15:2, 15:3, 15:4, 15:6, 16, 18, 19, 24:1, 25, 56, 60, 61, 62 and 66.

Other suitable pigments are Pigment Ultramarine Blue and Ultramarine Violet.

Preferably the pigment is Pigment Blue 15, more preferably Pigment Blue 15:1, 15:2, 15:3, 15:4, 15:5 or 15:6, most preferably 15:1.

Blue Covarine is particularly preferred.

The amount of pigment in the composition is preferably 0.001 to 0.3% by weight, more preferably 0.005 to 0.1% by weight, and most preferably 0.01 to 0.08% by weight. Weight percent refers to the total amount of active substance present and excludes any carriers that may be present. The pigment may be evenly distributed throughout the composition, or it may be dispersed in a second phase such as a strip or other co-extruded second phase.

The compositions of the present invention contain a water-soluble polymeric deposition aid. In the context of the present invention, a water-soluble polymeric deposition aid is a material that is water-soluble, typically having a solubility of 0.5 wt% or more, and more typically 5 wt% or more at 25°C. In addition, such a material remains soluble after drying, i. it can be redissolved after drying. Such materials are polymers, but not film-forming polymers. Water solubility is required to avoid buildup of the deposition aid on the teeth, which can also be a significant problem for film-forming polymers.

The soluble polymeric deposition enhancer enhances the deposition of the pigment on the teeth and thus enhances the discoloration caused by the pigment. More specifically, the deposition enhancing agent of the present invention is capable of enhancing the deposition of a pigment such as

- 1 041473 as Blue Covarine, when included in the composition in an amount of 0.02 wt.%, especially when the content of the deposition improver itself is in the amount of 1 wt.%.

The settling aid is preferably incorporated into the composition in an amount of 0.01 to 10% by weight, more preferably 0.05 to 5% by weight, and most preferably 0.1 to 1% by weight.

Settling improvers for use in the present invention are typically high molecular weight polymers, i.e. polymers with a molecular weight of 200,000 or more. Preferred deposition aids are Gantrez® type polymers and high molecular weight PEGs. Particularly preferred deposition aids are Gantrez® type polymers and high molecular weight PEGs. Particularly preferred settling aids are polymers of the Gantrez® type.

Gantrez® type polymers are copolymers of maleic anhydride and methyl vinyl ether in which the anhydride moiety may be in a partially or fully hydrolyzed or alcoholized form. The Gantrez® polymers themselves are available from ISP Inc. Suitable Gantrez® polymers are Gantrez S-95: molecular weight 216,000; free acid; Gantrez S-96: molecular weight 700,000; free acid; Gantrez S-97: molecular weight 1500000; free acid and Gantrez MS-955: molecular weight 1060000; calcium/sodium salt.

Gantrez® type polymers in which the anhydride moiety is fully hydrolyzed are preferred. They can be considered as copolymers of maleic acid and methyl vinyl ether. Especially preferred copolymers of maleic acid and methyl vinyl ether have a molecular weight of 1,000,000 or more, and a particularly preferred material is Gantrez S-97.

High molecular weight PEGs are ethylene glycol polymers with a molecular weight of 1,000,000 or more, preferably 2,000,000 or more. A preferred high molecular weight PEG is Polyox 60K, a polymer of about 2,000,000 molecular weight.

The oral care composition contains a non-ionic alkoxylated alcohol surfactant, preferably in an amount of 0.2 to 10% by weight, based on the total weight of the composition. Ethers of polyethylene glycol and fatty alcohols are preferred, in particular polyethylene glycol ethers containing from 20 to 40 ethylene oxide groups per unit. An example of such a nonionic surfactant includes a group of surfactants known as stearetes, such as stearet 30. More preferably, the content of nonionic surfactant is from 0.5 to 7 wt.% of the total composition, most preferably from 1 to 5 wt. .% of the total composition.

Preferably, the weight ratio of nonionic surfactant to polymeric deposition aid is 5:1 to 40:1, more preferably 10:1 to 30:1.

If other surfactants are present, it is preferred that the alkoxylated alcohol based nonionic surfactant makes up at least 75% by weight of the total surfactants in the composition. Preferably, the ratio of nonionic alkoxylated alcohol surfactant to other type of surfactant is greater than 2:1, more preferably greater than 3:1, most preferably greater than 5:1. Although other surfactants, such as anionic and amphoteric surfactants, may be present, it is preferred that their contents are less than 0.5% by weight of the total composition, preferably less than 0.1% by weight of the total composition. This is especially true for anionic surfactants.

Preferably, the oral composition contains water, a thickener, and an abrasive. Suitable thickeners include silica and calcium carbonate. The preferred thickener is silicon oxides.

Preferred abrasives include silicas, aluminas, calcium carbonates, dicalcium phosphates, calcium pyrophosphates, hydroxyapatites, trimetaphosphates, insoluble hexametaphosphates, etc., including agglomerated particulate abrasives, typically in an amount of 3 to 60% by weight of the composition for oral care. The most preferred abrasive agents are calcium carbonate and silica, especially silica.

The oral care compositions of the present invention may further contain ingredients that are conventional in the art, such as:

antimicrobial agents, for example triclosan, chlorhexidine, copper, zinc and tin salts such as zinc citrate, zinc sulfate, zinc glycinate, sodium zinc citrate and tin pyrophosphate, sanguinarine extract, metronidazole, quaternary ammonium compounds such as cetylpyridinium chloride; bisbiguanides such as chlorhexidine digluconate, hexetidine, octenidine, alexidine; and halogenated bisphenolic compounds such as 2,2'-methylene-bis-(4-chloro-6-bromophenol);

anti-inflammatory agents such as ibuprofen, flurbiprofen, aspirin, indomethacin, etc.;

anti-caries agents such as sodium and tin fluorides, amine fluorides, monofluorophosphate on

- 2 041473 triium, sodium trimetaphosphate and casein;

antiplaque agents such as urea, calcium lactate, calcium glycerophosphate and strontium polyacrylates;

vitamins such as vitamins A, C and E;

plant extracts;

desensitizers, for example potassium citrate, potassium chloride, potassium tartrate, potassium bicarbonate, potassium oxalate, potassium nitrate and strontium salts;

antitartar agents such as alkali metal pyrophosphates, polymers containing pyrophosphites, organic phosphonates and phosphocitrates, etc.;

biomolecules such as bacteriocins, antibodies, enzymes, etc.;

flavorings such as peppermint and spearmint oils;

protein materials such as collagen;

preservatives;

opacifiers;

dyes;

pH regulators;

sweeteners;

pharmaceutically acceptable carriers such as starch, sucrose, water or water/alcohol systems, etc.;

humectants such as glycerin, sorbitol, propylene glycol, xylitol, lactitol, etc.;

binders and thickeners such as sodium carboxymethylcellulose, xanthan gum, gum arabic, etc., as well as synthetic polymers such as polyacrylates and carboxyvinyl polymers such as Carbopol®;

buffers and salts for buffering the pH and ionic strength of the oral composition;

other optional ingredients that may be present, such as bleaching agents such as peroxy compounds, such as potassium peroxydiphosphate, foaming systems such as sodium bicarbonate and citric acid systems, color change systems, etc.

Liposomes can also be used to improve the delivery or stability of the active ingredients.

The oral care compositions may be in any form standard in the art, such as toothpaste, gel, mousse, aerosol, chewing gum, lozenge, powder, cream, and may also be formulated as systems for use in dispensers of two-chamber type. Preferred forms are toothpastes.

In the following non-limiting examples, amounts are weight percent unless otherwise indicated.

The above formulations were used to whiten teeth as follows. Extracted human incisors and premolars were cleaned with white toothpaste and placed in sterile saliva for 2 hours. After washing with water, the initial color of the teeth was measured using a colorimeter. Then the tooth samples were cleaned with a suspension of water:toothpaste (2:1) with the tested toothpastes for 60 s using

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Claims (11)

cabbage soup of a toothbrush, washed with water and re-measured their color. Tooth color changes were calculated using the WIO tooth whiteness index. The results of bleaching are shown in table. 2. table 2 Example WIO change A 0.4 1 5.6 Formulations with alternative surfactants. Table 3 Ingredient Etc. 2 Etc. IN Etc. WITH Etc. D Ex.E Sorbitol 69.5 69.5 69.5 69.5 69.5 PEG-32 2 2 2 2 2 Trisodium phosphate 0.11 0.11 0.11 0.11 0.11 Blue Covarine 0.19 0.19 0.19 0.19 0.19 Gantrez S97 1 1 1 1 1 Zeodent165 4.5 4.5 4.5 4.5 4.5 Sorbosil AC77 8 8 8 8 8 Sorbosil AC33 1.7 1.7 1.7 1.7 1.7 Cellulose gum 9H 0.5 0.5 0.5 0.5 0.5 flavoring 1.3 1.3 1.3 1.3 1.3 Steareth 30 1.8 0 0 0 0 sodium cocosulfate 0 1.8 0 0 0 Sodium methyl cocoyl taurate 0 0 1.8 0 0 Alpha olefin sulfonate 0 0 0 1.8 0 Sodium cocoyl isethionate 0 0 0 0 1.8 Water and other ingredients Up to 100 Up to 100 Up to 100 Up to 100 Up to 100 The examples were evaluated for teeth whitening as described previously. The results of bleaching are shown in table. 4. Table 4 Example WIO change 2 7.7 IN 3.6 WITH 2.6 D 1.0 E 1.3 CLAIM 1. An oral care composition containing a non-ionic alkoxylated alcohol surfactant, which is a polyethylene glycol and fatty alcohol ether, a pigment having a hue angle, h, in the CIELAB system from 220 to 320°, and a water-soluble a polymer additive that improves the deposition of the pigment, containing copolymers of maleic anhydride and methyl vinyl ether with a molecular weight of 200,000 or more, in which the anhydride fragment may be in a partially or completely hydrolyzed or alcoholized form. 2. An oral care composition according to claim 1, characterized in that the pigment has a hue angle, h, in the CIELAB system from 250° to 290°. 3. An oral care composition according to any one of the preceding claims, wherein the pigment comprises Blue Covarine. 4. An oral care composition according to any one of the preceding claims, wherein the pigment is present in an amount of 0.01 to 0.3% by weight of the total composition. 5. An oral care composition according to any one of the preceding claims, wherein the nonionic surfactant is a polyethylene glycol fatty alcohol ether containing 20 to 40 ethylene oxide groups per unit. 6. The oral care composition of any one of the preceding claims, wherein the nonionic surfactant is steareth 30. 7. An oral care composition according to any one of the preceding claims, wherein the weight ratio of nonionic surfactant to polymeric deposition aid is from 10:1 to 30:1. 8. An oral care composition according to any one of the preceding claims, wherein the alkoxylated alcohol based nonionic surfactant makes up at least 75% by weight of the total weight of surfactants in the composition. 9. An oral care composition according to any of the preceding claims, further comprising water, a thickening agent, and an abrasive agent. 10. An oral care composition according to claim 9, characterized in that the thickener comprises di- - 4 041473 silicon oxide. 11. The use of an oral composition according to any one of claims 1 to 10 in a method for improving tooth whitening. Eurasian Patent Organization, EAPO Russia, 109012, Moscow, Maly Cherkassky per., 2