WO2016153144A1 - Oral composition effective in inhibiting calculus formation - Google Patents

Abstract

The present invention relates to an oral composition for inhibiting calculus formation, containing an anionic sequestering agent and a cationic polymer and, more specifically, to an oral composition in which a phosphate-based anionic sequestering agent and a polyquaternium-based cationic polymer form a coacervate during teeth brushing such that the coacervate adheres to the surface of the teeth, thereby allowing the anionic sequestering agent, which is an ingredient inhibiting calculus formation, to remain in the mouth for a long time even after rinsing. The oral composition for inhibiting calculus formation, of the present invention, can effectively prevent calculus formation on the surface of teeth and can simultaneously improve foaming power while maintaining the flavor of a toothpaste.

Description

Oral composition effective for inhibiting tartar formation

The present invention relates to an oral composition for inhibiting tartar formation containing an anionic metal ion sequestrant and a cationic polymer. More specifically, the phosphate anionic metal ion sequestrant and a polyquaternium cationic polymer are used to treat coacetate. The present invention relates to a composition for oral cavity which is adhered to the tooth surface to form an anionic metal ion sequestrant that inhibits tartar formation and remains in the oral cavity even after rinsing.

In general, oral diseases are caused by various bacteria living in the oral cavity, and harmful oral bacteria eat and remnant such as food from the obtained film to proliferate to form plaques, and plaques are metal ions such as calcium and magnesium in saliva or blood. In combination with calcified calculus. Such plaque and tartar cause gum diseases such as gingivitis and periodontitis, and further damage the teeth. Regular brushing helps prevent the rapid formation of these deposits, but even regular brushing is not enough to remove all the stone deposits attached to the teeth. Therefore, in order to suppress plaque and tartar formation, an abrasive is physically used, and an antibacterial agent and a metal ion blocking agent are used chemically.

Abrasives used in oral products include polymer materials such as calcium carbonate, silica, aluminum hydroxide, calcium phosphate, baking soda, polyethylene and polyvinyl chloride, and antibacterial agents used in oral products include cetylpyridinium chloride and hexahalonium chloride. , Benzalkonium chloride, decarinium chloride, chlorohexidine, triclosan, thymol, isopropylmethylphenol and alkyldiaminoethylglycolic acid, and metal ion sequestrants include pyrophosphate, polyphosphate and polyphosphate. Phosphates and the like.

As described above, metal ion sequestrants have been mainly used to suppress tartar formation, but when the metal ion sequestrants are used alone, they do not remain in the oral cavity when brushing and rinsing. In addition, when an excessive amount of the metal ion blocking agent is added to increase the removal efficiency of tartar, irritation may occur, and the usability may be deteriorated due to inferior taste.

Accordingly, the present inventors have made diligent efforts to find a method for retaining the metal ion sequestrant in the oral cavity even after rinsing the toothpaste, resulting in the composition of the oral composition containing a cationic polymer together with the existing anionic metal ion sequestrant. In this case, the coacervate is formed by the precipitation reaction of the anion and the cation to confirm that it is effective in inhibiting tartar formation by leaving a larger amount of anionic metal ion blocker in the teeth, to complete the present invention.

SUMMARY OF THE INVENTION An object of the present invention is to provide an oral composition which contains an anionic metal ion sequestrant and a cationic polymer to induce coacervation thereof, thereby inhibiting tartar formation by remaining an anionic metal ion sequestrant on the tooth surface. There is.

In order to achieve the above object, the present invention provides an oral composition for inhibiting tartar formation containing an anionic metal ion sequestrant and a cationic polymer as an active ingredient.

Oral composition for inhibiting tartar formation of the present invention can effectively prevent tartar formation on the surface of the tooth, and at the same time maintain the flavor of the toothpaste and improve the foaming force.

Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs. In general, the nomenclature used herein is well known and commonly used in the art.

In the test example of the present invention, as a result of treating the oral composition containing the anionic metal ion sequestrant and the cationic polymer to the tooth simulation material, the anionic metal ion sequestrant and the cationic polymer remained on the tooth surface in the form of coacetate. As a result, it was confirmed that the remaining anionic metal ion blocking agent exhibits an effect of suppressing tartar formation.

Accordingly, the present invention relates to an oral composition for inhibiting tartar formation containing an anionic metal ion sequestrant and a cationic polymer as an active ingredient, and the anionic metal ion sequestrant and the cationic polymer react with each other. It can be characterized in that to form coacervate on the tooth surface.

In the present invention, the composition may be characterized in that it further contains a surfactant.

"Coacervation" refers to a phenomenon in which a colloidal sol concentrated in a dispersion medium is separated from a hydrophilic colloidal solution by a decrease in hydration of the colloidal particles and an electrostatic factor. The colloid concentration is high and the other liquid phase is lower in the colloid concentration. "Coacervate" refers to a colloidal material formed due to coacervation phenomena when anionic polymer electrolyte and cationic polymer electrolyte are mixed under certain conditions.

The anionic metal ion sequestrant contained in the composition for oral cavity of the present invention forms coacervates by ionic bonding with the cationic polymer to precipitate, and the formed coacervates may have a metal ion sequestrant having an effect of inhibiting tartar formation on the tooth surface for a long time. Make sure

In the present invention, the anionic metal ion blocking agent may be characterized in that the phosphate compound. Anionic metal ion sequestrant is a substance that inhibits tartar formation by chelating metal ions which have an important effect on tartar formation. Phosphoric acid-based compounds are preferred, and hexametaphosphate and pyrophosphate. ), Polyphosphate, and salts thereof may be one or more selected from the group consisting of. The salt may be in the form of a combination of 1 to 4 alkali metal cations and an anionic phosphate-based compound, and specific examples thereof include sodium phosphate, monosodium phosphate, disodium phosphate, and tree. Sodium phosphate, Sodium tripolyphosphate, Sodium hexametaphosphate, Tetrasodium pyrophosphate, Sodium acid pyrophosphate, but not necessarily It is not limited.

In addition, in the present invention, the cationic polymer may be a polyquaternium-based compound. The polyquaternium-based compound refers to a polymer compound (polymer) in which quaternary ammonium ions are present at the center, and preferably one selected from the group consisting of polyquaternium-10, polyquaternium-6, and polyquaternium-11 It may be more than, but is not necessarily limited thereto.

In addition, in the present invention, the composition for oral cavity may further comprise a surfactant, in addition to the anionic metal ion blocking agent and the cationic polymer. Specific examples of the surfactant include anionic surfactants such as glycinate, sulfate, sulfosuccinate, sacosinate, phosphate, isethionate, glutamate, and taurate, and betaine. Amphoteric surfactants such as, steine, ampoacetate, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene (cured) castor oil, glycerin fatty acid ester, sorbitan fatty acid ester, sucrose fatty acid ester, alkylolamide, alkylglucose Nonionic surfactants such as seeds, cationic surfactants such as N-alkyldiamino ethylglycine, and the like, preferably sodium lauryl sulfate and sodium methyl cocoyl taurate , And disodium lauryl sulfosuccinate, but may be one or more selected from the group consisting of It is not limited to this.

In addition, in the present invention, the anionic metal ion sequestrant may be contained in 0.1 to 10.0% by weight relative to the total weight of the composition, preferably 1.0 to 7.0% by weight, more preferably 3.0 to 5.0% by weight It may be contained. If the content of the anionic metal ion blocker is less than 0.1% by weight, no coacervate is formed. If the content of the anionic metal ion blocker is greater than 10.0% by weight, the flavor and foaming power may be lowered and the irritation may be increased. have.

In addition, the cationic polymer may be contained in an amount of 0.01 to 0.50% by weight based on the total weight of the composition, preferably 0.05 to 0.50% by weight, more preferably 0.10 to 0.50% by weight. If the content of the cationic polymer is less than 0.01% by weight coacetate is not formed, if the content exceeds 0.50% by weight it may be inconvenient to use the high viscosity in the toothpaste.

In addition, in the present invention, the anionic metal ion blocking agent and the cationic polymer may be mixed and contained in a weight ratio of 0.2: 1 to 1000: 1, preferably 10: 1 to 100: 1, more preferably May be mixed in a weight ratio of 30: 1 to 50: 1. Since the molecular weight of the anionic metal ion blocking agent is relatively small, it is preferable to mix at a higher ratio than the cationic polymer. If the mixing ratio of the anionic metal ion blocking agent and the cationic polymer is less than 0.2: 1 or more than 1000: 1, coacervate may be difficult to form.

The composition for oral cavity of this invention is not specifically limited in the formulation, For example, Toothpaste, Oral detergent, Oral detergent, Chewing gum, Candy, Oral spray, Oral toothpaste, A tooth whitening agent, etc. can be provided. .

The composition for oral cavity of the present invention may contain abrasives, wetting agents, auxiliary foaming agents, binders, sweeteners, pH adjusting agents, preservatives, active ingredients, fragrances, brighteners, pigments, solvents and the like which are commonly used according to the formulation and purpose of use. .

As the abrasive, precipitated silica, silica gel, zirconium silicate, calcium monohydrogen phosphate, calcium monohydrogen phosphate, hydrous alumina, hard calcium carbonate, heavy calcium carbonate, calcium pyrophosphate, insoluble methphosphate, aluminum silicate and the like can be used.

As the wetting agent, concentrated glycerin, glycerin, aqueous sorbitol solution, amorphous sorbitol aqueous solution, polyethylene glycols, propylene glycol and the like can be used.

As the auxiliary foaming agent, anionic and nonionic surfactants such as sodium alkyl sulfate, sodium lauryl sulfate, sucrose fatty acid ester, and sorbitan fatty acid ester may be used.

The binder is sodium carboxymethyl cellulose, carrageenan, xanthan gum, hydroxyethyl cellulose, hydroxypropylmethylcellulose, hydroxypropyl cellulose, guar gum, gellan gum, carbomer, pectin, polyvinylpyrrolidone, carboxyvinyl polymer Sodium alginate, laponite, sodium carboxymethylcellulose, xanthan gum and the like can be used.

Examples of the sweetener include saccharin sodium, sucralose, maltitol, aspartame, erythritol, xylitol, licorice acid, saccharin, and the like. The preservatives include benzoic acid, methylparaben, propylparaben, sodium benzoate, paraoxybenzoic acid ester, and the like. Can be used. In addition, the fragrance may be used alone or mixed with peppermint oil, spearmint oil, menthol, etc., the pH adjuster may be used sodium phosphate, disodium phosphate, citric acid, triethanolamine and the like.

Hereinafter, the present invention will be described in more detail with reference to Examples. These examples are only for illustrating the present invention, and it will be apparent to those skilled in the art that the scope of the present invention is not to be construed as being limited by these examples. Thus, the substantial scope of the present invention will be defined by the appended claims and their equivalents.

[Manufacture of Examples 1-9 and Comparative Examples 1-3]

In order to test the degree of coacervate formation and residual degree of the oral composition of the present invention, purified water, anionic metal ion blocker (sodium hexametaphosphate, tetrasodium pyrophosphate, sodium tripolyphosphate), cationic polymer (polyquaternium -10, polyquaternium-6, polyquaternium-11), surfactant (sodium lauryl sulfate, sodium methyl cocoyl taurate, dissonium lauryl sulfosuccinate) as the main components, Examples 1 to 9, and Comparative Examples 1 to 3, respectively, were prepared to have a total weight of 100 g as in the configuration.

(Unit: weight%)

	Comparative Example 1	Comparative Example 2	Comparative Example 3	Example 1	Example 2	Example 3	Example 4	Example 5	Example 6	Example 7	Example 8	Example 9
Purified water	To 100	To 100	To 100	To100	To100	To100	To100	To 100	To100	To100	To100	To100
Sodium hexametaphosphate	3	0.5	7	3	3	-	-	3	3	3	3	5
Tetrasodium pyrophosphate	-	-	-	-	-	3	-	-	-	-	-	-
Sodium tripolyphosphate	-	-	-	-	-	-	3	-	-	-	-	-
Polyquaternium-10	-	0.1	0.1	0.1	0.1	0.1	0.1	-	-	0.1	0.1	0.1
Polyquaternium-6	-	-	-	-	-	-	-	0.1	-	-	-	-
Polyquaternium-11	-	-	-	-	-	-	-	-	0.1	-	-	-
Sodium lauryl sulfate	2	2	2	-	2	2	2	2	2	-	-	2
Sodium methyl cocoyl taurate	-	-	-	-	-	-	-	-	-	2	-	-
Disodium laurylsulfosuccinate	-	-	-	-	-	-	-	-	-	-	2	-

Test Example 1 Coacervate Formation Measurement

Take samples of Examples 1 to 9 and Comparative Examples 1 to 3, and gradually increase the ratio of purified water added to each, and gradually decrease the ratio of the sample, and adjust the dilution ratio as shown in Table 2 below, but the total weight is 3 g. To maintain. After measuring the transparency (%) of each diluted sample using UV spectroscopy, the results are shown in Table 2. The lower the transparency, the more coacervates were determined.

	2-fold dilution	5x	10 times	20 times	40x
Amount of sample (g)	1.5	0.6	0.3	0.15	0.08
Amount of purified water (g)	1.5	2.4	2.7	2.85	2.93
transparency(%)
Comparative Example 1	100%	100%	100%	100%	100%
Comparative Example 2	99%	95%	90%	95%	99%
Comparative Example 3	99%	90%	85%	88%	99%
Example 1	100%	99%	76%	84%	92%
Example 2	95%	30%	54%	84%	98%
Example 3	99%	80%	85%	96%	99%
Example 4	96%	35%	58%	88%	98%
Example 5	92%	11%	36%	61%	75%
Example 6	99%	98%	77%	83%	94%
Example 7	90%	20%	44%	74%	88%
Example 8	92%	24%	43%	77%	90%
Example 9	92%	25%	40%	64%	90%

As shown in Table 2, in Comparative Example 1 containing no cationic polymer, coacetate was not formed, and Example 1 containing a cationic polymer together with an anionic metal ion sequestrant, but no surfactant. In the case of the dilution conditions showed a difference in the degree of coacervate production. In addition, as the solution containing the anionic metal ion sequestrant, the cationic polymer, and the surfactant was diluted, more coacetate was formed, and it was confirmed that coacervate was not formed again after a certain point. From this, it could be confirmed that the proper dilution ratio is important for coacervate formation.

In addition, in addition to the anionic metal ion blocking agent and the cationic polymer, when a surfactant for foam formation, which is an essential element in the toothpaste formulation, is added, the type of cationic polymer (compare Examples 2, 5, 6), anionic It was confirmed that there was a difference in the degree of coacervate production depending on the type of the metal ion blocking agent (compare Examples 2, 3, 4) or the type of the surfactant (compare Examples 2, 7, 8), and anionic metal ion According to the content of the blocking agent (compare Examples 2, 9) it was confirmed that the difference in the degree of coacetate production.

In addition, compared to Examples 1 to 9, the mixing ratio (weight ratio) of the anionic metal ion sequestering agent and the cationic polymer is 30: 1 in Comparative Example 2 lower than 30: 1, or in Comparative Example 3 higher than 50: 1, It was found that coacervates were not produced well compared to Examples 1 to 9 in the range of ˜50: 1.

Test Example 2 Measurement of Residual Amount of Metal Ion Blocker on Teeth Surface

In Example 1, after confirming that coacervate is formed in a solution containing an anionic metal ion sequestrant, a cationic polymer, and a surfactant, an in vitro test is performed to determine how much coacervate formed remains on the tooth surface. Measured through.

After diluting 10 times the solution of Examples 2, 7, 9 and Comparative Example 1 prepared as shown in Table 1, V-8 cross brushing machine which is an automatic brushing machine on hydroxyapatite disk (Clarkson Chromatography Products) Brushing was performed using (V-8 Cross Brushing Machine®, Sabri, USA). Four disks were used to reduce the error between the hydroxyapatite disks, and the diluted solution was brushed with a brushing machine for 5 minutes, and then washed five times. After repeating this ten times, the coacervate attached to the hydroxyapatite was dissolved in sodium hydroxide solution (0.3M), and the amount of the anionic metal ion sequestrant remaining in the coacervate using ion chromatography (Meon chromatography, Metrohm). The results of the measurement are shown in Table 3.

(Unit: ppm)

	Disc 1	Disc 2	Disc 3	Disc 4	Average (ppm)
Comparative Example 1	2.60	4.30	2.23	2.2	2.83
Example 2	18.13	29.42	12.30	14.05	18.48
Example 7	16.61	25.10	22.40	20.50	21.15
Example 9	35.12	30.22	33.35	36.36	33.76

As shown in Table 3, when there is a cationic polymer (Examples 2, 7, 9) than when there is no cationic polymer (Comparative Example 1), it was found that the residual amount of the anionic metal ion sequestrant was significantly higher. , The difference between the surfactants was slightly but not large (compare Examples 2 and 7), and when the amount of the anionic metal ion sequestrant increased, the residual amount of the anionic metal ion sequestrant increased significantly (Example 2, 9 comparison) could be confirmed.

[Manufacture of Examples 10-11 and Comparative Example 4]

Examples 10 to 11 and Comparative Example 4 in which a coacervate solution containing an anionic metal ion blocking agent and a cationic polymer were included in a paste formulation in the form of a toothpaste were prepared as shown in Table 4 below.

(Unit: weight%)

division	Ingredient Name	Comparative Example 4	Example 10	Example 11
solvent	Purified water	To 100	To 100	To 100
Metal Ion Blocker	Sodium hexametaphosphate	3	3	5
Cationic polymer	Polyquaternium-10	-	0.1	0.1
Active ingredient	Sodium monofluorophosphate	0.76	0.76	0.76
Humectant	Sorbitol Liquid (70%)	50	50	50
Sweetener	Sodium saccharin	0.4	0.4	0.4
abrasive	Silica	10	10	10
Thickener	Hydroxymethylcellulose	1.5	1.5	1.5
Spices	Combination spices	One	One	One
Foam	Sodium lauryl sulfate	2	2	2

[Test Example 3] Measurement of plaque formation inhibitory effect

Based on the results of Test Example 1 and Test Example 2, it was determined whether the composition for oral cavity of the present invention containing an anionic metal ion blocking agent and a cationic polymer has an effect of inhibiting tartar formation.

First, the sanded glass rod was immersed in a solution added with saliva and sugar obtained from the panel, and then aged at 35 degrees for 2 days. After forming plaque on the surface of the glass rod, the glass rod was immersed in a crystallization solution consisting of 25% toothpaste slurry solution (Comparative Examples 4, 10 and 11) and calcium chloride (1.5 mM) and stored overnight for 5 seconds. After washing the glass rod, it was stored again in the toothpaste slurry solution and crystallization solution. The tartar formed by repeating this for two weeks was dissolved in strong acid (1M HCl) and strong base (1M KOH) and analyzed by calcium content using ion chromatography (Ion chromatography, Metrohm). The results are shown in Table 5 below. It was judged that the lower the calcium content, the better the ability to inhibit tartar formation.

	Comparative Example 4	Example 10	Example 11
Average content of calcium extracted from 4 glass rods (μg)	857	608	532

As a result of the calcium content analysis, as shown in Table 5, the content of anionic metal ion blocking agent is lower than that of the case of containing a cationic polymer (Examples 10 and 11), and of the case of not containing (Comparative Example 4). Increasing the (Comparative Example 10, 11) was confirmed that the calcium content is lowered.

[Test Example 4] toothpaste feeling evaluation

Based on the measurement results of calculus formation inhibitory power of Test Example 3, the feeling of use of the toothpaste was evaluated. Each of Example 10, Example 11, and Comparative Example 4 were used by 20 people, and after two weeks of use, a survey was conducted to evaluate flavor, foaming power, stimulus, and overall satisfaction, and the results are shown in Table 6 below. Indicated.

division	Comparative Example 4	Example 10	Example 11
Flavor	3.5	3.3	3.6
Bubble	3.7	4.2	4.0
Irritation	4.0	3.9	3.9
Total satisfaction	3.5	3.7	3.6

(1 point: very dissatisfied / 2 points: dissatisfied / 3 points: normal / 4 points: satisfactory / 5 points: very satisfied)

As shown in Table 6, it was confirmed that the composition containing the cationic polymer (Examples 10 and 11) did not significantly affect the flavor and irritation of the toothpaste, and rather helped in foaming power.

The specific parts of the present invention have been described in detail above, and it is apparent to those skilled in the art that such specific descriptions are merely preferred embodiments, and thus the scope of the present invention is not limited thereto. something to do. Thus, the substantial scope of the present invention will be defined by the appended claims and their equivalents.

Claims (11)

1. Oral composition for inhibiting tartar formation containing an anionic metal ion blocking agent and a cationic polymer as an active ingredient.
2. The oral composition of claim 1, wherein the anionic metal ion sequestrant and the cationic polymer react with each other to form coacervate on the tooth surface.
3. The oral composition according to claim 1, wherein the oral composition further contains a surfactant.
4. The oral composition of claim 1, wherein the anionic metal ion sequestrant is a phosphate compound.
5. The composition for oral cavity of claim 1, wherein the cationic polymer is a polyquaternium-based compound.
6. The group of claim 3, wherein the surfactant is composed of sodium lauryl sulfate, sodium methyl cocoyl taurate, and disodium lauryl sulfosuccinate. Oral composition, characterized in that at least one selected from.
7. The composition for oral cavity according to claim 4, wherein the phosphate-based compound is any one or more selected from the group consisting of hexametaphosphate, pyrophosphate, polyphosphate, and salts thereof.
8. The composition for oral cavity of claim 5, wherein the polyquaternium-based compound is any one or more selected from the group consisting of polyquaternium-10, polyquaternium-6, and polyquaternium-11. .
9. The composition for oral cavity of claim 1, wherein the anionic metal ion sequestrant is contained in an amount of 0.1 to 10.0 wt% based on the total weight of the composition.
10. The composition for oral cavity according to claim 1, wherein the cationic polymer is contained in an amount of 0.01 to 0.50% by weight based on the total weight of the composition.
11. The composition for oral cavity of claim 1, wherein the anionic metal ion sequestrant and the cationic polymer are mixed in a weight ratio of 0.2: 1 to 1000: 1.