JP2000053547A - Composition for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To prepare a composition for oral cavity, excellent in safety, capable of effectively inhibiting stain formation without damaging teeth, and improved in taste by including both a specific sulfosuccinic acid-based surfactant and water soluble bivalent metal salt. SOLUTION: This composition is prepared by formulating (A) 0.01-5 wt.% sulfosuccinic acid-based surfactant of formulae I and II [R1 is an 8-22C alkyl or an alkenyl; AO is a 2-3C oxyalkylene; its average addition mol number (n) is 0-20; B is NH, a 2-3C monoalkanolamine residue, or the like; M1 and M2 are each H, an alkali (or alkaline earth) metal, ammonium, or the like], (B) 0.01-2 wt.% water soluble bivalent metal salt and, optionally, (C) 0.1-5 wt.% nonionic surfactant.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

[0001] The present invention relates to a sulfosuccinic acid-based surfactant in an amount of 0.01 to 5% by weight, a water-soluble divalent metal salt in an amount of 0.01 to 2% by weight, and more preferably a nonionic surfactant. The present invention relates to an oral composition having an effect of inhibiting stain formation, which is contained in an amount of 0.1 to 5% by weight.

[0002]

2. Description of the Related Art Stain is a pigmentary deposit on teeth that is thought to be caused by fungicides such as chlorhexidine, tannin-based substances contained in tea, and metals such as iron. It is a problem. As a means for solving this, a method of removing stain and a method of inhibiting the formation of stain can be considered. Abrasives and bleaching agents are generally used to remove stains, but these have the problems of damaging the teeth and of being highly irritating.

[0003] Japanese Unexamined Patent Publication (Kokai) No. 1-125315 discloses that polystyrene sulfonic acid inhibits stains caused by tannin-based substances, and Japanese Unexamined Patent Publication (Kokai) No. 2-56413 discloses non-enzymatic stains. Although methods for inhibiting the progress of the browning reaction and inhibiting the formation of stains have been described, these are intended only for specific stain substances and are not effective for all stains. Further, aminoalkyl silicones disclosed in JP-A-2-200618, JP-A-2-209805, JP-A-2-223512, and
The fluoroalkyl phosphates disclosed in JP-B-38517 and JP-A-5-163126 form a coating on the tooth surface, improve the acid resistance of the tooth, inhibit the formation of plaque, and reduce the stain. It also inhibits formation. However, the effect is not satisfactory enough,
The improvement is desired.

[0004] On the other hand, the use of a sulfosuccinic acid-based surfactant as a stain formation inhibitor in oral compositions is disclosed in JP-A-10-17443. But,
Sulfosuccinic surfactants have strong bitterness and astringency,
In the oral composition containing the surfactant, it is desired to improve the feeling in use.

[0005]

SUMMARY OF THE INVENTION An object of the present invention is to mix a sulfosuccinic surfactant with a sulfosuccinic surfactant in order to provide excellent safety and effectively inhibit stain formation without damaging the teeth. An object of the present invention is to provide a composition for oral cavity in which the bad taste derived from a surfactant is improved.

[0006]

In view of such a situation,
The present inventors have conducted intensive studies and found that a water-soluble divalent metal salt has an effect of suppressing bitterness and astringency derived from a sulfosuccinic acid-based surfactant. The inventors have found that the bitterness of the acid surfactant is also reduced, and have completed the present invention.

That is, in the present invention, 0.01 to 5% by weight of a sulfosuccinic acid-based surfactant, 0.01 to 2% by weight of a water-soluble divalent metal salt, and more preferably 0.1 to 2% by weight of a nonionic surfactant. An object of the present invention is to provide an oral composition for inhibiting stain formation, which is excellent in safety, does not damage teeth, and has no bitterness or astringency by being blended in an amount of 1 to 5% by weight.

[0008]

BEST MODE FOR CARRYING OUT THE INVENTION The sulfosuccinic surfactant used in the present invention has a general formula (1):

Embedded image And (2):

Embedded image [In Formulas 1 and 2, R ₁ is an alkyl group or alkenyl group having 8 to 22 carbon atoms, AO is an oxyalkylene group having 2 to 3 carbon atoms, n is 0 to 20, B is -NH- or 2 carbon atoms. 3 monoalkanolamine residues, M ₁ and M
₂ is the same or different and represents hydrogen, an alkali metal, an alkaline earth metal, ammonium or alkanolamine. The sulfo succinic acid monoester represented by the formula [I] is not particularly limited.

In these sulfosuccinic acid monoesters, R ₁ is either a naturally-derived or synthesized linear or branched alkyl or alkenyl group having 8 to 22 carbon atoms, such as lauryl, cocoyl, myristyl, stearyl, C ₁₂ -C ₁₄ synthetic alkyl, isononyl, isododecyl, octenyl, etc. Dodekeniru can be exemplified.
As the carbon number of R ₁ is longer, the bitterness and irritation are reduced, and as the carbon number is shorter, the effect of inhibiting the formation of stain is increased.
R ₁ preferably has 10 to 16 carbon atoms, more preferably 12 to 14 carbon atoms, and most preferably uses C _{12 to} C ₁₄ synthetic alkyl or a combination of lauryl and myristyl. M1
And M2 are hydrogen, alkali metal, alkaline earth metal,
One kind selected from ammonium and alkanolamine, which may be the same or different. Examples of the alkali metal include sodium and potassium, examples of the alkaline earth metal include magnesium, and examples of the alkanolamine include monoethanolamine, diethanolamine, and triethanolamine. Particularly, sodium and magnesium are preferable. The AO group is preferably an oxyethylene group, and the average number of added moles n is 0.
~ 20 is preferred. As the average number of moles added n is smaller, the effect of inhibiting the formation of stain is higher and the bitterness is reduced,
n is preferably 0 to 7, and most preferably 0 to 2.
Here, the average number of added moles of 0 means a sulfosuccinic acid monoester to which no oxyalkylene is added.

Examples of the sulfosuccinic acid monoester represented by the general formula (1) include polyoxyethylene sulfosuccinate (7 moles) lauryl disodium, polyoxyethylene sulfosuccinate (2 moles) lauryl disodium, and polyoxysulfosuccinate. ethylene (1 mol) lauryl disodium, sodium lauryl sulfosuccinate 2, sulfosuccinic acid polyoxyethylene (7 mol) myristyl disodium, sulfosuccinate, polyoxyethylene (2 mol) alkyl (C ₁₂ -C ₁₄₎ disodium, sulfosuccinate polyoxyethylene (1 mol) alkyl (C ₁₂ -C ₁₄₎ 2 sodium alkyl sulfosuccinate (C ₁₂ -C ₁₄₎ 2 sodium sulfosuccinic acid polyoxyethylene (2 mol) lauryl magnesium, polyoxy sulfosuccinate Styrene (2 moles) alkyl (C ₁₂ ~
C ₁₄ ) magnesium, polyoxyethylene sulfosuccinate (7 mol) myristyl 2-triethanolamine and the like. Examples of the compound represented by the general formula (2) include disodium sulfosuccinate oleic acid amide, disodium polyoxyethylene sulfosuccinate (5 mol), disodium lauroylethanolamide, and disodium polyoxyethylene sulfosuccinate (2 mol) cocoyl isopropanolamide. Can be exemplified.

The most preferred sulfosuccinic acid monoester is that R ₁ is an alkyl group having 12 to 14 carbon atoms, the AO group is an oxyethylene group, and the average number of added moles n is 0.
Particularly preferred are the sodium salts of ~ 2. These are specifically sulfosuccinate, polyoxyethylene (2 mol) alkyl (C ₁₂ -C ₁₄₎ 2 Sodium sulfosuccinic acid polyoxyethylene (1 mol) alkyl (C ₁₂ -C ₁₄₎ 2 sodium alkyl sulfosuccinate (C ₁₂ ~C _14), such as disodium and the like. These may be used alone or in combination of two or more.

The sulfosuccinic acid monoesters of the general formulas (1) and (2) are each represented by the general formula (3):

Embedded image And (4):

Embedded image [In Formulas 3 and 4, R ₁ is an alkyl group or alkenyl group having 8 to 22 carbon atoms, AO is an oxyalkylene group having 2 to 3 carbon atoms, n is 0 to 20, B is -NH- or 2 carbon atoms. ~ 3 monoalkanolamine residues, M ₁ and M ₂
Are the same or different, respectively, hydrogen, alkali metal,
Represents an alkaline earth metal, ammonium or alkanolamine. ], And in the present specification, these structural isomers are represented by the general formulas (1) and (2).

The amount of the sulfosuccinic acid monoester is usually 0.01 to 5% by weight based on the whole composition.
And more preferably 0.1 to 1% by weight. If the amount is less than 0.01% by weight, a sufficient effect of inhibiting the formation of stain cannot be obtained. If the amount exceeds 5% by weight, the bitterness is not improved even when a water-soluble divalent metal salt is added.

The water-soluble divalent metal salt used in the present invention specifically refers to a water-soluble salt of magnesium or calcium. The water-soluble salt may be any of an inorganic salt and an organic acid salt, and is not particularly limited. For example, hydrochloride, nitrate, sulfate, phosphate, carbonate, citrate, malate and the like can be mentioned, among which magnesium chloride and calcium chloride are preferable, and magnesium chloride is particularly preferable in view of the effect of improving the bitter taste.

[0015] These water-soluble divalent metal salts are usually added in an amount of 0.01 to 2% by weight, more preferably 0.1 to 1% by weight, based on the whole composition. 0.01% by weight
If the content is less than 2, the sufficient bitter taste improving effect cannot be obtained, and if it exceeds 2% by weight, on the contrary, the bitterness of the water-soluble divalent metal salt itself is undesirably exhibited.

In the present invention, it is preferable to further add 0.1 to 5% by weight of a nonionic surfactant since the irritation caused by the bitter taste of the sulfosuccinic acid-based surfactant is further reduced. The nonionic surfactant used in the present invention is not particularly limited. Specifically, sucrose fatty acid esters, fatty acid esters of sugars or sugar alcohols such as sorbitan fatty acid esters, polyoxyethylene polyoxypropylene glycol ether, polyoxyethylene Polyoxyethylene sorbitan fatty acid esters such as sorbitan monolaurate and polyoxyethylene sorbitan monostearate, polyoxyethylene hydrogenated castor oil, polyoxyethylene fatty acid esters, fatty acid monoglycerides, polyoxyethylene higher alcohol ethers, polyoxyethylene polyoxypropylene Fatty acid esters and the like. Among them, polyoxyethylene polyoxypropylene glycol ether and polyoxyethylene hydrogenated castor oil are most preferred. In addition, these nonionic surfactants may be used alone or in combination of two or more, but the compounding amount is usually 0.1 to 5% by weight based on the whole composition. If the amount is less than 0.1% by weight, a sufficient effect of alleviating irritation caused by bitterness cannot be obtained, and if it exceeds 5% by weight, the nonionic surfactant itself exhibits bitterness, which is not preferable.

The oral composition for inhibiting the formation of stains according to the present invention may be prepared by a conventional method such as toothpaste, toothpaste, gel, pasta, liquid dentifrice, mouthwash, chewing gum, dental floss, patch, sealant, tablet, etc. Can be shaped,
Dental dentifrices, liquid dentifrices, or mouthwashes are particularly preferred from the viewpoint of usability.

In the oral composition of the present invention, in addition to a sulfosuccinic acid-based surfactant, a water-soluble divalent metal salt, and a nonionic surfactant, an abrasive, a foaming agent, Agents, flavors, sweeteners, binders, pH adjusters, wetting agents, and other base materials, as well as medicinal ingredients, can be blended as long as the effects of the invention are not impaired.

For example, in the case of a dentifrice, a second
Calcium phosphate dihydrate and anhydrate, calcium phosphate, tribasic calcium phosphate, calcium carbonate, calcium pyrophosphate, aluminum hydroxide, alumina,
Silicic anhydride, silica gel, aluminum silicate, precipitated silica, insoluble sodium metaphosphate, tribasic magnesium phosphate, magnesium carbonate, calcium sulfate, polymethyl methacrylate, benite, zirconium silicate,
Hydroxyapatite, synthetic resin and the like can be used. These abrasives may be used alone or in combination of two or more. The compounding amount is usually 5 to 90% by weight, and in the case of toothpaste, 5 to 50% by weight.

Examples of the foaming agent include anionic surfactants (excluding sulfosuccinic surfactants). For example, the alkyl group such as sodium lauryl sulfate and sodium myristyl sulfate has 8 to 18 carbon atoms. Higher alkyl sulfates, N-long chain acyl amino acid salts, α-
Olefin sulfonate salt, higher fatty acid sodium monoglyceride monosulfate, N-methyl-N-palmitoyl tauride salt and the like can be blended. Many of these anionic surfactants have a high stain removal effect by chemical dissolution, and in particular, the addition of sodium lauryl sulfate is preferable because the effect of inhibiting the formation of stain is synergistically enhanced. These anionic surfactants may be used alone or in combination of two or more.
Usually, it is 0.001 to 5% by weight, preferably 0.01 to 2% by weight, based on the whole composition.

In addition to the above-mentioned nonionic surfactants and anionic surfactants, amphoteric surfactants and cationic surfactants usually used in oral compositions may be blended. 0.001 to 5 based on the whole composition
% By weight, preferably 0.01 to 2% by weight.

Examples of the binder include cellulose derivatives such as carboxymethylcellulose, alkali metal alginate such as sodium alginate, propylene glycol alginate, xanthan gum, tragacanth gum, karaya gum, gum arabic, gum such as carrageenan, polyvinyl alcohol, polyacrylic acid. Sodium, a carboxyvinyl polymer, a synthetic binder such as polyvinylpyrrolidone, etc. may be used alone or in combination of two or more, and the compounding amount is usually 0.3 to 5% by weight based on the whole composition. %.

Further, menthol, carvone, anethole, eugenol, methyl salicylate, limonene, ocimene, n-decyl alcohol, citronellol, α-terpineol, methyl acetate, citronellyl acetate, methyl eugenol, lionol, linalool, linalool,
Ethyl linalool, crocodile, thymol, spearmint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, cinnamon oil, pimento oil, diatom oil, perilla oil, winter green oil, clove oil, eucalyptus oil, etc. In particular, a high content of anethole is particularly effective in masking the bitterness derived from the sulfosuccinic acid-based surfactant. These flavoring agents may be used alone or in combination of two or more, and the amount of the flavoring agent is usually 0.05% based on the whole composition.
10 to 10% by weight, preferably 0.1 to 5% by weight.

Also, two or more sweeteners such as saccharin sodium, acesulfame potassium, stevioside, glycyrrhizin, perillartin, thaumatin, aspartylphenylalanine methyl ester, xylitol, palatinose, palatinit, erythritol, maltitol can be used alone. May be used in combination, usually in an amount of 0.01 to 5% by weight based on the whole composition.
It is.

Further, a humectant such as sorbit, glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, polyethylene glycol, polypropylene glycol, xylit, maltitol, or lactit may be used alone or in combination of two or more. Well,
The compounding amount is usually 5 to 70% by weight based on the whole composition.

Also, sodium hydrogen phosphate, citric acid,
PH adjusters such as sodium citrate, bactericides such as chlorhexidine gluconate, cetylpyridinium chloride, and triclosan; enzymes such as dextranase, amylase, protease, mutanase, lysozyme, lytic enzyme (Litek enzyme), monofluoro Sodium phosphate, alkali metal monofluorophosphates such as potassium monofluorophosphate, sodium fluoride, fluorides such as stannous fluoride, tranexamic acid and epsilon aminocaproic acid, aluminum chlorohydroxyl allantoin, dihydrocholesterol, vitamin E derivatives, Active ingredients such as glycyrrhizin salts, glycyrrhetinic acid, glycerophosphate, chlorophyll, sodium chloride, caropeptide, and water-soluble inorganic phosphate compounds can be used alone or in combination. It may be.

[0027]

The present invention will be described below in more detail with reference to examples, but the present invention is not limited to these examples. Unless otherwise specified, [%] indicates [% by weight].

The following components were blended, a toothpaste was prepared according to a conventional method, and used for evaluation. Formulation Ingredients Blending amount (%) Silicic anhydride 20.0 Sorbit 35.0 Sulfosuccinic acid-based surfactant Divalent metal salt shown in Table 1 Nonionic surfactant shown in Table 1 Lauroyl sarcosinate shown in Table 1 0. 1 Carrageenan 1.0 Saccharin sodium 0.2 Flavor 0.9 Paraben 0.2 Water balance 100.0

Evaluation method (Stain formation inhibitory effect) Using a hydroxyapatite disc having a diameter of 1 cm as a tooth model, human whole saliva, 0.2% chlorhexidine gluconate aqueous solution, 4-fold slurry supernatant of the test dentifrice, 0. The immersion of 3% iron ammonium citrate aqueous solution and black tea extract in this order was repeated 10 times, and the color difference from the disc before the experiment was measured (Δ
E). Using the color difference (referred to as ΔE ₀ ) when distilled water was used instead of the test dentifrice as a control, the stain formation inhibition rate was calculated by the following equation. The color difference was measured using a color difference system CR-241 (manufactured by Minolta). Stain formation inhibition rate (%) = (ΔE ₀ −ΔE) × 100
The greater the / ΔE ₀ stain formation inhibition rate, the higher the effect, indicating that 50% or more was effective. Table 1 shows the evaluation results together with the evaluation results of bitterness and irritation when the teeth were brushed with the test dentifrice.

[0030]

[Table 1]

As shown in Table 1, all dentifrices containing a sulfosuccinic acid-based surfactant exhibited a high inhibition rate of stain formation of 50% or more (Examples 1 to 5, Comparative Example 6,
7). On the other hand, when a divalent metal salt was blended, there was no bitterness (Examples 1 to 5, Comparative Example 8), and when a nonionic surfactant was further blended, there was no irritation (Examples 2 to 5, Comparative Example). 8).

Example 6 Toothpaste was prepared according to a conventional method according to the following formulation. Ingredients Blending amount (%) Hydroxyapatite 3.0 Dibasic calcium phosphate dihydrate 20.0 Dibasic calcium phosphate dihydrate 10.0 Silicic anhydride 3.0 Sorbit 30.0 Polyethylene glycol 400 5.0 Carboxymethylcellulose Sodium 1.0 Sodium lauryl sulfate 1.2 Disodium lauryl sulfosuccinate 1.0 Calcium chloride 0.5 Fragrance 1.0 Sodium saccharin 0.2 Water Remainder 100.0 Centrifuge the 4x water diluted slurry of this product, When the stain formation inhibition rate of the obtained supernatant was examined, it was 75%.
There was no bitterness.

Example 7 A toothpaste was prepared according to the following formulation according to a conventional method. Ingredients Amount (%) Silicic anhydride 20.0 Sorbit 40.0 Titanium oxide 0.5 Polyethylene glycol 1.0 Sodium carboxymethyl cellulose 1.0 Sodium lauryl sulfate 1.0 Polyoxyethylene (60) hydrogenated castor oil 1.0 Polyoxyethylene (2 mol) alkyl (12-14) disodium sulfosuccinate 0.6 Magnesium chloride 0.2 Sodium fluoride 0.2 Triclosan 0.1 Fragrance 1.0 Saccharin sodium 0.2 Water Remaining Total 100.0 The 4-fold water-diluted slurry of the product was centrifuged, and the stain formation inhibition rate of the resulting supernatant was determined to be 62%.
There was no bitterness or irritation.

Example 8 A mouthwash was prepared according to a conventional method according to the following formulation. Ingredients Blended amount (%) Glycerin 10.0 Ethanol 8.0 Polyoxyethylene (60) hydrogenated castor oil 0.5 Perfume 0.3 Saccharin sodium 0.1 Polyoxyethylene (2 mol) Myristyl disodium succinate 0.3 Sulfuric acid 0.3 Sulfuric acid Magnesium 0.05 Water Remainder Total 100.0 The product had a stain formation inhibition rate of 90%, and was neither bitter nor irritating.

Example 9 A liquid dentifrice was prepared according to a conventional method according to the following formulation. Ingredients Amount (%) Sorbit 15.0 Propylene glycol 5.0 Polyoxyethylene (200 mol) Polyoxypropylene (70 mol) Glycol 1.5 Polyvinylpyrrolidone 1.0 Fragrance 0.2 Saccharin sodium 0.1 Polyoxyethylene ( 1 mol) Lauryl sulfosuccinate disodium 0.4 Magnesium nitrate 0.1 Water balance Total 100.0 The stain formation inhibition rate of this product was 86%, and there was no bitterness or irritation.

Example 10 An oral pasta was prepared according to the following formulation according to a conventional method. Ingredients Amount (%) Polyoxyethylene (200 mol) Polyoxypropylene (40 mol) Glycol 40.0 Glycerin 10.0 Triclosan 0.1 Polyoxyethylene (7 mol) Alkyl sulfosuccinate (12-14) disodium 0 5.5 Magnesium chloride 0.08 Polyvinylpyrrolidone 1.0 Acesulfame potassium 0.1 Perfume 0.7 Water Remaining Total 100.0 Centrifugation of a 4x water-diluted slurry of this product, and stain formation of the resulting supernatant When the inhibition rate was examined, it was 59%, and there was neither bitterness nor irritation.

Example 11 An oral tablet was prepared according to a conventional method according to the following formulation. Ingredients Amount (%) Lactose 88.0 Xylitol 5.0 Polyvinylpyrrolidone 2.0 Polyoxyethylene (1 mol) Laurylmagnesium sulfosuccinate 1.0 Magnesium chloride 0.2 Polyoxyethylene (60 mol) Monostearate 0. 3 Sodium saccharin 0.2 Fragrance 0.05 Hydroxyethylcellulose Residual 100.0 Centrifuged a slurry of this product diluted 4 times with water and examined the inhibition rate of stain formation of the obtained supernatant. There was no irritation.

[0038]

According to the present invention, it is possible to maintain excellent aesthetic teeth by excelling in safety to the living body and effectively inhibiting the formation of stain, and furthermore, it is excellent in use feeling without bitterness or irritation. Oral compositions can be provided.

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Claims (6)

[Claims] 1. A compound represented by the general formula (1): , And (2): [In Formulas 1 and 2, R ₁ is an alkyl group or alkenyl group having 8 to 22 carbon atoms, an AO group is an oxyalkylene group having 2 to 3 carbon atoms, the average number of added moles n is 0 to 20, and B is -N
H- or a monoalkanolamine residue having 2 to 3 carbon atoms, M ₁ and M ₂ are the same or different, and each represents hydrogen, an alkali metal, an alkaline earth metal, ammonium,
Represents any one of alkanolamines. One or more sulfosuccinic surfactants represented by the formula
0.01 to 5% by weight, and 0.01 to 5% by weight of the water-soluble divalent metal salt.
An oral composition for inhibiting the formation of stain, which is contained in an amount of 2% by weight. 2. The oral composition for inhibiting stain formation according to claim 1, wherein the average number of moles n of the AO group added to the sulfosuccinic acid-based surfactant is from 0 to 7. 3. The oral cavity composition for inhibiting stain formation according to claim 1, wherein the sulfosuccinic acid-based surfactant is an alkyl group or an alkenyl group in which R ₁ has 10 to 14 carbon atoms. 4. The oral composition for inhibiting stain formation according to claim ₁ , wherein M ₁ and M ₂ of the sulfosuccinic acid-based surfactant are sodium. 5. The oral composition for inhibiting stain formation according to claim 1, wherein the water-soluble divalent metal salt is a hydrochloride. 6. The oral composition for inhibiting stain formation according to any one of claims 1 to 5, further comprising 0.1 to 5% by weight of a nonionic surfactant.