KR102664431B1 - Oral composition for preventing dental caries - Google Patents

Abstract

The present invention relates to an oral composition that is effective against cavities that may be caused by acids such as orange juice or electrolyte beverages. More specifically, it relates to an oral composition that uses polyacrylate-based polymers and sodium fluoride to alleviate the roughness of the tooth surface caused by acids. It relates to an oral composition that is effective in preventing cavities and inhibiting the progression of early cavities.

Description

Oral composition for preventing dental caries}

The present invention relates to an oral composition that is effective against cavities that may be caused by acids such as orange juice or electrolyte beverages. More specifically, it relates to an oral composition that uses polyacrylate-based polymers and sodium fluoride to alleviate the roughness of the tooth surface caused by acids. It relates to an oral composition that is effective in preventing cavities and inhibiting the progression of early cavities.

Teeth are a mineral made of calcium phosphate, and the major diseases are cavities and periodontal disease. Among these, cavities account for the largest proportion of dental diseases from children to adults, and the frequency of occurrence is increasing. According to a report by the Korean Dental Association, more than 90% of children experience dental caries, and more than 80% of adults have gum disease. The main cause of this disease is infection by microorganisms in the oral cavity, which is caused by the interaction of bacteria, food, and saliva. In other words, the nutrients and moisture necessary for the development of oral bacteria are continuously supplied through food, saliva, and oral fluid, and the oral environment has a temperature (37°C) and pH (near neutral) suitable for the development of microorganisms.

Representative microorganisms that cause periodontal disease include Streptococcus mutans and Prevotella intermedia. These microorganisms cause microbial metabolism that converts sucrose present in food into glucose and fructose, forming insoluble glucan, a polymer of glucose, on the tooth surface. In this process, glucan attaches to other microorganisms in the oral cavity and to the tooth surface, forming a dental plaque. Lactic acid accumulated by lactic acid bacteria, including Streptococcus mutans, inside the formed plaque dissolves the enamel on the tooth surface, making the tooth surface rough, increasing the bacterial attachment rate and causing cavities. Additionally, the alveolar bone is dissolved by products resulting from the proliferation of various bacteria, resulting in periodontal disease.

In order to suppress the above-mentioned cavities and periodontal disease, antibacterial substances such as sodium bicarbonate (NaHCO ₃ ), triclosan (C ₁₂ H ₇ Cl ₃ O ₂ ), polyphosphate, sodium fluoride (NaF), and vancomycin (Vancomycin) are used. , antibiotics such as Chlorhexidine and Spiramycin, or organic/inorganic fluorine have been used. However, although the above methods are effective in preventing cavities, their use is limited due to the disadvantages of vomiting, diarrhea, and antibiotic resistance.

Among these, in particular, to prevent cavities, fluorine compounds such as sodium fluoride, sodium monofluorophosphate, etc. have been used. However, the number of patients with cavities is continuously increasing, and the effect of fluoride in preventing cavities tends to decrease due to polyol ingredients, especially sorbitol, which are essential in oral compositions such as toothpaste, and excessive use of fluoride causes hardening of cartilage and abdominal pain. There was a side effect of causing , so there was a limit to the effectiveness of using fluorine compounds. In addition, there is the problem that the consumption of acidic drinks such as orange juice and electrolyte drinks has recently increased, creating an environment in which cavities can easily occur.

Accordingly, there is a greater need for an oral composition that does not have the above disadvantages and can effectively prevent cavities.

In order to solve the above problems, the present inventor attempted to implement a composition that can improve the tooth surface roughness and/or increase the caries prevention effect by allowing fluorine to remain on the tooth surface longer, and thus general Although the efficacy of fluorine is affected by the polyol component included in the composition, polyol is essential in the formulation of oral compositions, so we wanted to find an component that could help improve surface roughness, and polyacrylate-based After discovering that polymers exhibit this effect, the present invention was completed.

Therefore, the purpose of the present invention is to provide an oral composition that improves the tooth surface roughness and/or prevents tooth decay by fluorine and inhibits the progression of early cavities by containing a combination of fluorine and a specific polymer material.

In order to achieve the above object, the present invention includes a fluorine compound as an active ingredient; Polyacrylate-based polymer; and polyvinylmethylether maleic anhydride copolymer.

When used, the oral composition of the present invention significantly improves the adhesion of the fluorine compound to the tooth surface compared to the conventional oral composition, allowing it to stay on the tooth for a longer period of time, thereby increasing the contact time between the active ingredient and the tooth. By including it in combination with a late-based polymer and polyvinyl methyl ether maleic anhydride copolymer, the effect of improving tooth surface roughness and/or preventing tooth decay caused by fluoride is significantly increased, and can be particularly effective in preventing tooth decay and suppressing the progression of early decay. there is.

Figure 1 is a confocal laser scanning micrograph showing the results when the surface of a toothpaste specimen treated with citric acid was treated with only a fluorine compound.
Figure 2 is a confocal laser scanning micrograph showing the results when the surface of a toothpaste specimen treated with citric acid was treated with a combination of a fluorine compound and a polyacrylate-based polymer.
Figure 3 is a confocal laser scanning micrograph showing the results when the surface of a toothpaste specimen treated with citric acid was treated with a combination of fluorine compound, sodium polyacrylate, and polyvinylmethyl ether maleic anhydride copolymer.

The present invention includes a fluorine compound as an active ingredient; Polyacrylate-based polymer; and oral compositions containing polyvinylmethylether maleic anhydride copolymer.

The fluorine compound used in the present invention is not particularly limited as long as it is generally included in oral compositions. Usable fluorine compounds include, but are not limited to, sodium fluoride, sodium monofluorophosphate, and stannous fluoride. In particular, it is preferable to use sodium fluoride in the present invention.

The polyacrylate-based polymer used in the present invention is not particularly limited as long as it can be used for oral use, but sodium polyacrylate is preferably used.

Additionally, the composition of the present invention contains polyvinylmethylether maleic anhydride copolymer (hereinafter referred to as 'PVM/MA copolymer'). PVM/MA copolymer has the characteristic of remaining on the tooth surface in a certain amount even after rinsing with water, which helps ensure that sodium fluoride and polyacrylate-based polymers remain on the teeth for a longer period of time.

The oral composition of the present invention preferably contains a fluorine compound in an amount of 500 ppm to 1500 ppm based on the total weight of the composition (corresponding to 0.11 to 0.33% by weight based on the total weight of the composition). When used at less than 500ppm, the effect of strengthening teeth is small, and when used at more than 1500ppm, it exceeds the fluorine concentration level set by the Pharmaceutical Affairs Act, and thus does not meet the requirements for approval as a quasi-drug.

The oral composition of the present invention contains polyacrylate-based polymer in an amount of 0.3 to 3.7% by weight, preferably 0.5 to 3.6% by weight, and more preferably 1 to 3.5% by weight, based on the total weight of the composition. If it is less than 0.2% by weight, it is not enough to achieve the desired effect, and if it is more than 3.8% by weight, formulation is difficult.

The oral composition of the present invention contains the PVM/MA copolymer in an amount of 0.3 to 3.7% by weight, preferably 0.4 to 3% by weight, and more preferably 0.5 to 2.5% by weight, based on the total weight of the composition. If it is less than 0.3% by weight, it is not enough to achieve the desired effect, and if it is more than 3.7% by weight, formulation is difficult.

In addition, when the oral composition of the present invention includes both a polyacrylate-based polymer and a PVM/MA copolymer, it is preferable that the combined content thereof is more than 0% by weight and not more than 4% by weight. If it exceeds 4% by weight, the unit cost due to manufacturing increases and the viscosity increases, making formulation difficult.

In particular, if the polyacrylate-based polymer and PVM/MA copolymer are used in the above content range in the composition of the present invention, the combination ratio is not particularly limited, but is preferably 15:1 to 1:15, more preferably 15:1 to 1:15. It is used in combination at a weight ratio of 10:1 to 1:5, more preferably 8:1 to 1:3, and even more preferably 7:1 to 1:2.

The oral composition according to the present invention can reduce the degree of change in tooth surface roughness caused by the oral environment, especially oral acid, and has excellent adhesion to the tooth surface, increasing the contact time between the active ingredient and the tooth. It can effectively prevent cavities, and can also inhibit the further progression of early cavities, which are shallow cavities that occur on the surface of the teeth, that is, in the enamel of the teeth.

Because tooth decay is a progressive disease, it is generally divided into three stages: early, middle, and late. The term “early cavities” used in the present invention refers to the stage where black stained areas, black dots, and black lines along the texture are visible when the teeth are viewed with the naked eye. Cavities occur only in the outer enamel of the teeth and are not accompanied by pain. It refers to the state of tooth decay. In other words, early cavities are caused by acid generated when bacteria present in the oral cavity decompose food residues, and the acid produced in this way causes damage to tooth enamel.

The composition of the present invention is not particularly limited in its formulation, and specifically, it may be in the formulation of toothpaste, mouthwash, or mouthwash, or in the form of a liquid, gel, paste, etc., and may be used as a tool selected from brushes, cotton swabs, etc. It can be used by applying it directly to the surface of the teeth, or it can be used by putting the composition in a dental tray and attaching it to the teeth.

In particular, when the formulation of the oral composition provided by the present invention is toothpaste, in addition to the above-mentioned active ingredients, ingredients such as wetting agents, abrasives, surfactants, thickeners, etc. are required, as well as sweeteners, pH adjusters, preservatives, medicinal ingredients, and flavoring agents. , can be manufactured by adding brighteners, pigments, solvents, etc.

In the case of humectants, they prevent toothpaste from hardening. Representative ingredients include polyols, especially glycerin, sorbitol, polyethylene glycol, and propylene glycol, and these can be used alone or in combination of two or more in an amount of 10 to 60% by weight based on the total weight of the composition. , preferably 20 to 50% by weight, more preferably 25 to 35% by weight.

Abrasives are used to clean teeth by removing plaque and foreign substances, and include calcium carbonate, precipitated silica, aluminum hydroxide, calcium monohydrogen phosphate, and insoluble sodium metaphosphate. Commonly used are silica and calcium carbonate. It is mainly used, and can be used alone or in combination of two or more types in an amount of 1 to 60% by weight, preferably 10 to 50% by weight, based on the total weight of the composition.

Surfactants provide convenience by generating bubbles during oral cleaning and use. Representative ingredients include anionic and nonionic surfactants, especially sodium lauryl sulfate, sodium lauryl sarcosinate, sucrose fatty acid ester, and polyoxyethylene curing. Castor oil, polyoxyethylene polyoxypropylene copolymer, etc. can be used alone or in a mixture of two or more types in an amount of 0.5 to 5% by weight, preferably 0.5 to 3% by weight, based on the total weight of the composition.

In the case of thickeners, they are necessary for the retention of toothpaste on a toothbrush, and representative ingredients include sodium carboxylmethylcellulose, hydroxymethylcellulose, carrageenan, xanthan gum, and sodium alginate, either alone or in a mixture of two or more. It can be mixed and used in an amount of 0.1 to 5% by weight, preferably 0.1 to 2% by weight, based on the total weight of the composition.

In the case of sweeteners, it is preferable to use sodium saccharin, aspartame, stevioside, xylitol, licorice acid, etc. individually or in combination of two or more in an amount of 0.05 to 5% by weight based on the total weight of the composition.

In the case of pH adjusters, sodium phosphate, disodium phosphate, trisodium phosphate, sodium pyrophosphate, citric acid, sodium citrate, tartaric acid, etc. can be used alone or in a mixture of two or more.

In the case of preservatives, methyl paraoxybenzoate, propyl paraoxybenzoate, sodium benzoate, etc. can be used alone or in a mixture of two or more types.

Medicinal ingredients include chlorhexidine, allantoin chlorohydroxyaluminate, aminocaproic acid, tranexamic acid, triclosan, cetylpyridium chloride, zinc chloride, pyridoxine hydrochloride, and tocopherol acetate, which can be used alone or in combination of two or more. You can.

As a fragrance, peppermint oil, spearmint oil, menthol, anethole, etc. can be mixed in an appropriate amount.

Titanium oxides can be used as a brightening agent, food coloring can be used as a coloring agent, and purified water and ethanol can be used as a solvent.

It can be manufactured using a conventional toothpaste manufacturing method by adding the above additives in different compositions and amounts depending on the purpose and conditions.

Hereinafter, the configuration and effects of the present invention will be described in more detail through examples and test examples. However, these examples and test examples are provided only for illustrative purposes to aid understanding of the present invention, and the scope and scope of the present invention are not limited by the following examples and test examples.

[Reference Example 1] Preparation of oral composition formulation

Toothpaste samples #1-1 to #1-3 were prepared with the compositions shown in Table 1 below.

(Content: weight%) #1-1 #1-2 #1-3 Purified water To 100 To 100 To 100 sodium fluoride - 0.22 - Sodium monofluorophosphate - - 0.76

[Test Example 1] Evaluation of tooth surface roughness change rate according to the type of fluorine compound

When teeth are attacked by acids, the surface becomes rough, and from this, the degree of initial decay can be inferred.

The initial cavity prevention effect according to the type of fluorine compound was evaluated by measuring the rate of change in surface roughness by adding acid to tooth specimens treated with samples containing different fluorine compounds.

Specifically, to measure surface roughness, tooth specimens were processed as follows:

1) Tooth specimen: Using hydroxyapatite disk (HAP disk) (3D Biotek LLC, New Jersey, USA)

2) Toothpaste sample processing: After preparing toothpaste slurry (toothpaste: ion water = 1:3), treat on HAP disk at 150rpm for 10 minutes. The toothpaste used at this time was #1-1 to #1-3 described in Reference Example 1 above.

3) Rinse: Wash with tap water for 1 minute (nothing remains on the tooth surface when observed with the naked eye)

4) Decalcification: Soak the rinsed HAP disk in 1% citric acid solution and process at 100rpm for 10 minutes.

5) Rinse: Wash with tap water for 1 minute

6) Drying: Naturally dry for at least 2 hours

7) Evaluation: Measurement of the surface roughness of the HAP disc using a confocal laser scanning microscope (LEXT OLS4500, Olympus). At this time, an objective lens of

The surface roughness of the HAP disk was measured before and after treatment with the toothpaste sample, and the surface roughness change rate was calculated according to Equation 1 below.

The measured surface roughness and surface roughness change rate of the teeth are shown in Table 2 and Figure 1 below.

Unit (nm) Before sample processing After sample processing Rate of change (%) Measurement #1 Measurement #2 Measurement #3 average Measurement #1 Measurement #2 Measurement #3 average #1-1 147 197 131 158 498 542 547 529 234 #1-2 204 182 203 196 282 368 271 307 56 #1-3 153 205 240 199 455 445 402 434 118

Looking at Table 2 and Figure 1, when only citric acid was treated and the sample containing the fluorine compound was not treated, the tooth surface roughness was significantly increased (treated #1-1), whereas when the sample containing the fluorine compound was treated, the tooth surface roughness was significantly increased. It can be seen that the degree of surface roughness is significantly reduced (processing #1-2 and #1-3).

In particular, when the sample containing sodium fluoride in Sample #1-2 was treated, the rate of change in surface roughness was significantly smaller than when the sample containing sodium monofluorophosphate in Sample #1-3 was treated. Sodium has a better effect than sodium monofluorophosphate in protecting against surface roughness caused by acids, so it can be considered to be more effective in preventing early cavities.

[Reference Example 2]

Toothpaste samples #2-1 to #2-9 were prepared with the compositions shown in Table 3 below.

(Content: weight%) #2-1 #
2-2 #
2-3 #
2-4 #
2-5 #
2-6 #
2-7 #
2-8 #
2-9 Purified water To 100 To 100 To 100 To 100 To 100 To 100 To 100 To 100 To 100 Dissension
salt 0.22 0.22 0.22 0.22 0.22 0.22 0.22 0.22 0.22 Sorbitol - 35 - - - - - - - glycerin - - 35 - - - - - - For polishing
silica - - - 10 - - - - - For incremental use
silica - - - - 10 - - - - reshuffle
carbonated
calcium - - - - - 10 - - - medium
carbonated
calcium - - - - - - 10 - - sodium
lauryl
sulfate - - - - - - - 2 - sodium carboxyl
methyl
cellulose - - - - - - - - One

[Test Example 2] Evaluation of the rate of change in tooth surface roughness according to the types of common ingredients included in oral compositions

Since various ingredients are included in the formulation of a general toothpaste, the rate of change in surface roughness according to the mixed use of the ingredients required for toothpaste formulation and fluorine compound was evaluated.

The surface roughness of the tooth was measured according to the method described in Test Example 1, except that #2-1 to #2-9 described in Reference Example 2 were used as samples treated with tooth specimens, and from this, the surface roughness change rate was calculated. The results are shown in Table 4 below.

Sample name Surface roughness
Rate of change (%) #2-1 sodium fluoride 56 #2-2 Sodium fluoride + Sorbitol 35% 167 #2-3 Sodium fluoride + glycerin 35% 94 #2-4 Sodium fluoride + 10% polishing silica 56 #2-5 Sodium fluoride + 10% silica for thickening 61 #2-6 Sodium fluoride + light calcium carbonate 10% 51 #2-7 Sodium fluoride + ground calcium carbonate 10% 100 #2-8 Sodium fluoride + sodium lauryl sulfate 2% 38 #2-9 Sodium fluoride + sodium carboxymethylcellulose 1% 67

Looking at Table 4 above, there are limits to the effectiveness of fluorine compounds due to interference by various components present in the toothpaste formulation. In particular, polyols such as sorbitol and glycerin greatly affect the effect of sodium fluoride, and heavy carbonate, a type of abrasive, significantly affects the effect of sodium fluoride. It can be seen that calcium also has an effect.

However, in order to implement a toothpaste formulation, polyol is generally an essential ingredient, so the above data suggests that other ingredients that can reduce the rate of change in tooth surface roughness are needed even under conditions where polyol is used.

[Reference Example 3]

Toothpaste samples #3-1 to #3-8 were prepared with the compositions shown in Table 5 below.

(Content: weight%) #
3-1 #
3-2 #
3-3 #
3-4 #
3-5 #
3-6 #
3-7 #
3-8 Purified water To 100 To 100 To 100 To 100 To 100 To 100 To 100 To 100 Dissension
salt 0.22 0.22 0.22 0.22 0.22 0.22 0.22 0.22 Sodium Carboxylmethylcellulose - One - - - - - - xanthan gum - - One - - - - - sodium
alginate - - - One - - - - Acrylate/Steareth-20 Methacrylate Copolymer - - - - One - - - sodium polyacrylate - - - - - One - - PVM/MA copolymer - - - - - - One - Polyquaternium-10 - - - - - - - One

[Test Example 3] Evaluation of tooth surface roughness change rate according to the type of polymer

In order to reduce the surface roughness change rate, various polymer materials were used together with fluorine compounds and the resulting surface roughness change rate was evaluated. At this time, anionic and cationic polymers that can be used in representative toothpastes were used as polymers.

The surface roughness of the tooth was measured according to the method described in Test Example 1, except that #3-1 to #3-8 described in Reference Example 3 were used as samples treated with tooth specimens, and from this, the surface roughness change rate was calculated. The results are shown in Table 6 and Figure 2 below.

Sample name Surface roughness
Rate of change (%) #3-1 sodium fluoride 56 #3-2 Sodium fluoride + sodium carboxymethylcellulose 1% 67 #3-3 Sodium fluoride + xanthan gum 1% 93 #3-4 Sodium fluoride + sodium alginate 1% 151 #3-5 Sodium fluoride + acrylate/steareth-20 methacrylate copolymer 1% 184 #3-6 Sodium fluoride + sodium polyacrylate 1% 38 #3-7 Sodium fluoride + PVM/MA copolymer 1% 93 #3-8 Sodium fluoride + polyquaternium-10 1% 63

Looking at Table 6 and Figure 2, it can be seen that the surface roughness change rate was lowest when sodium polyacrylate was used together.

Meanwhile, in the case of PVM/MA copolymer, the rate of change in surface roughness could not be lowered as much as sodium polyacrylate, but it was observed to remain on the tooth surface longer than other polymer materials, suggesting its applicability as an additional ingredient.

[Reference Example 4]

A toothpaste formulation was prepared according to a conventional toothpaste manufacturing method with the composition shown in Table 7 below.

(Content: weight%) Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Comparative Example 5 Comparative Example 6 Comparative Example 7 Example 1 Example 2 Example 3 Example 4 Example 5 ionized water To 100 To 100 To 100 To 100 To 100 To 100 To 100 To 100 To 100 To 100 To 100 To 100 Sodium monofluorophosphate - 0.76 - - - - - - - - - - sodium fluoride - - 0.22 0.22 0.22 0.22 0.22 0.22 0.22 0.22 0.22 0.22 Saccharin Sodium 0.3 0.3 0.3 0.3 0.3 0.3 0.3 0.3 0.3 0.3 0.3 0.3 glycerin 35 35 35 35 35 35 35 35 35 35 35 35 silica 13 13 13 13 13 13 13 13 13 13 13 13 Sodium Carboxylmethylcellulose One One One - - - - - - - - - sodium polyacrylate - - - 0.5 One - - 0.5 One 0.5 1.5 3.5 PVM/MA copolymer - - - - - 0.5 One 0.5 0.5 One 2.5 0.5 incense One One One One One One One One One One One One Sodium Lauryl Sulfate 2 2 2 2 2 2 2 2 2 2 2 2

[Test Example 4] Evaluation of the rate of change in tooth surface roughness according to the combination of polyacrylate-based polymer and PVM/MA copolymer

In addition to fluorine compounds and polyacrylate-based polymers, the effect on surface roughness changes caused by the use of PVM/MA copolymer was evaluated.

Except that the tooth specimen treated as described in Reference Example 4 was used, the surface roughness of the tooth was measured according to the method described in Test Example 1, and the surface roughness change rate was calculated from this. The results are shown in Table 8 and Figure 3 below.

Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Comparative Example 5 Comparative Example 6 Comparative Example 7 Example 1 Example 2 Example 3 Example 4 Example 5 Surface roughness
Rate of change (%) 303 232 148 158 113 165 160 89 80 85 60 55

Looking at Table 8 above, it can be seen that when sodium polyacrylate and PVM/MA copolymer are used simultaneously with a fluorine compound, the effect is significantly increased compared to when they are used individually.

In particular, in the case of containing only fluorine compounds and sodium polyacrylate, the desired degree of surface roughness reduction effect could not be obtained even if sodium polyacrylate was used in an amount of 1.0% by weight, and only fluorine compounds and PVM/MA copolymer were found. In this case, even if PVM/MA copolymer is used in an amount of 1.0% by weight, the surface roughness becomes worse, but if both fluorine compounds, sodium polyacrylate, and PVM/MA copolymer are included, sodium polyacrylate and PVM It can be seen that even when the /MA copolymer is used in an amount of 0.5% by weight, a significant reduction in tooth surface roughness can be obtained (Figure 3).

Claims (10)

Fluorine compounds as active ingredients; Polyacrylate-based polymer; and polyvinylmethylether maleic anhydride copolymer,
The content of the polyacrylate-based polymer is 0.3 to 3.7% by weight based on the total weight of the composition,
The content of the polyvinylmethyl ether maleic anhydride copolymer is 0.3 to 3.7% by weight based on the total weight of the composition,
An oral composition wherein the total content of the polyacrylate-based polymer and polyvinylmethyl ether maleic anhydride copolymer is 4% by weight or less based on the total weight of the composition. The oral composition according to claim 1, wherein the fluorine compound is at least one selected from the group consisting of sodium fluoride, sodium monofluorophosphate, and stannous fluoride. The oral composition according to claim 1, wherein the content of the fluorine compound is 500ppm to 1500ppm based on the total weight of the composition. The oral composition according to claim 1, wherein the polyacrylate-based polymer is sodium polyacrylate. delete delete delete The oral composition according to claim 1, wherein the composition is used to reduce tooth surface roughness. The oral composition according to claim 1, wherein the composition is used to prevent cavities. The oral composition according to claim 9, wherein the cavity is caused by tooth damage caused by acid.