JPH10167939A - Composition for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a composition for oral cavity, excellent in (dental) caries preventing effect and stability by incorporating a mixture comprising triclosan, sodium bicarbonate and sodium fluoride with a potassium ion source. SOLUTION: This composition for oral cavity is obtained by incorporating a mixture comprising (A) 0.01 to 1wt.% of triclosan, (B) 1 to 50wt.% of sodium bicarbonate and (C) 0.01 to 1wt.% of sodium fluoride with (D) 0.001 to 20wt.% of a potassium ion source and, as required, one or more other known ingredients, and by forming the above mixture into e.g. a dentifrice (e.g. toothpaste and tooth wash), gargle, mouthwash and paste for the oral cavity, where all of the above percentages being based on the composition. For example, when the composition is to be used for toothpaste or the like, it is compounded with the ingredients A to D, and one or more other ingredients, e.g. an abrasive, binder, viscolizer, surfactant, sweetener, perfume and colorant.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a composition for oral cavity which has a bactericidal effect by triclosan, an acid neutralizing effect by sodium bicarbonate, and a tooth-causing effect by sodium fluoride, which is highly effective in preventing dental caries and has a stabilizing effect. The present invention relates to an oral composition having a high caries prevention effect and excellent stability, using a potassium ion source in combination.

[0002]

BACKGROUND OF THE INVENTION Dental caries is an oral disease caused by caries pathogenic bacteria such as Streptococcus mutans producing acids and demineralizing human teeth. Therefore, in order to enhance the caries prevention effect, it is important to sterilize the causative bacteria of the caries, neutralize the acid produced by the bacteria, and strengthen the tooth structure.

Hitherto, it has been proposed to use a bactericide to kill bacteria in the oral cavity (Japanese Patent Application Laid-Open No. 60-1985).
239409, JP-A-59-101417).
However, since the amount of the fungicide alone is also limited,
A sufficient caries prevention effect cannot be obtained. Further, in the composition for the oral cavity, particularly in the dentifrice composition, there is a problem that the cationic bactericide is inactivated because the anionic activator is indispensable from the viewpoint of feeling of use such as foaming, and a sufficient effect cannot be obtained. .

It is known that sodium bicarbonate is added as an acid neutralizing agent to tooth dentifrices for preventing dental caries (JP-A-56-59703 and JP-A-59-51210). However, there is a problem that a sufficient effect cannot be obtained with an acid neutralizing agent alone due to an acid produced from a bacterium over time.

On the other hand, a fluorine compound is known as an active ingredient for strengthening the tooth structure. However, since the compounding amount of the fluorine compound alone is limited, a sufficient caries prevention effect cannot be obtained.

[0006] Therefore, these oral compositions are not yet satisfactory in terms of caries prevention effects.

The present invention has solved the above problems,
An object of the present invention is to provide an oral composition having a high anticorrosion effect and excellent stability.

[0008]

Means for Solving the Problems and Embodiments of the Invention The present inventors have conducted intensive studies in order to achieve the above-mentioned object, and as a result, by using triclosan, sodium fluoride, and sodium hydrogencarbonate together, That the effect of preventing dental caries is synergistically enhanced, and in this case, by additionally using a potassium ion source in combination with the combined system, it is possible to obtain a highly oral dental composition having a stable effect of preventing dental caries over time. I learned.

That is, a synergistic effect of preventing caries even when a phenolic compound other than triclosan, such as biosol, hinokitiol, carbalkrol, chlorxylenol, trichlorocarbanilide, or chlorthymol, is used in combination with sodium fluoride and sodium hydrogencarbonate. No synergistic effect on caries prevention was observed when stannous fluoride or sodium monofluorophosphate other than sodium fluoride was used in combination with triclosan or sodium bicarbonate. Nevertheless, when triclosan, sodium fluoride and sodium bicarbonate are used in combination, a synergistic effect of caries prevention is produced, and a marked caries prevention effect is produced. Although the effect is reduced, the addition of a potassium ion source It found to exhibit a sufficient caries preventive effect even after exist, in which the present invention has been accomplished.

Hereinafter, the present invention will be described in more detail. The oral composition of the present invention comprises triclosan, sodium fluoride, sodium hydrogen carbonate and a potassium ion source.

Here, the compounding amount of triclosan is as follows:
It is preferably 0.01 to 1% (wt%, hereinafter the same) of the total amount of the composition, more preferably 0.02 to 0.5%.
%. If the amount is less than 0.01%, the plaque formation inhibitory effect is not sufficient, and if it exceeds 1%, the taste of the composition may be significantly reduced.

The compounding amount of sodium fluoride is 0.0
1 to 1% is preferable, and 0.1 to 0.5% is more preferable.
It is. If the amount is less than 0.01%, a sufficient effect cannot be expected, and if it exceeds 1%, the possibility of fluorosis occurs.

The amount of sodium hydrogencarbonate is preferably 1 to 50%, more preferably 5 to 50% of the total amount of the composition.
-40%, more preferably 10-30%.
If the amount is less than 1%, a sufficient effect cannot be expected.
If it exceeds 300, the taste of the composition tends to decrease.

Potassium ion sources include potassium hydroxide, potassium chloride, dipotassium glycyrrhizinate, potassium hydrogen tartrate, potassium carbonate, potassium bicarbonate, potassium citrate, potassium pyrophosphate, potassium metaphosphate, tripotassium phosphate, and phosphoric acid. Potassium dihydrogen or the like is used, and preferably, potassium hydroxide, potassium chloride, and potassium carbonate are used.

The amount of the potassium ion source is 0.001 to
It is preferably 20%, more preferably 0.01 to 10%. If the amount is less than 0.001%, a sufficient effect cannot be expected. If the amount exceeds 20%, the taste of the composition is significantly reduced.

The oral composition of the present invention includes dentifrices such as toothpaste, lubricating toothpaste, liquid dentifrice, mouthwash, mouthwash,
It is prepared as an oral pasta or the like, and in this case, known components according to the type, form, and the like of these compositions can be blended at a normal dose.

Taking dentifrice as an example, an abrasive, a binder, a thickener, a surfactant, a sweetener, a flavor, a coloring agent and the like can be added. Examples of the abrasive include dibasic calcium phosphate, calcium carbonate, calcium pyrophosphate, insoluble sodium metaphosphate, silica-based abrasives (amorphous silicic anhydride, crystalline silicic anhydride, aluminosilicate, zirconosilicate, etc.), aluminum oxide, Aluminum hydroxide, resin and the like can be blended. As a binder, sodium carboxymethylcellulose, hydroxyethylcellulose, alginate, carrageenan, gum arabic,
Polyvinyl alcohol, thickening silicate and the like, as a thickener, polyethylene glycol, sorbitol, glycerin, propylene glycol and the like can be blended,
As the surfactant, sodium lauryl sulfate, sodium dodecylbenzenesulfonate, sodium lauryl sulfoacetate, sodium sodium lauroyl sarcosine and the like, which are anionic surfactants, can be blended.

Saccharin sodium, stevioside and the like are used as sweeteners, and parabens and the like are used as preservatives. Further, as a flavor, 1-menthol, carvone, eugenol, anethole, spearmint oil,
Peppermint oil and the like may be blended. In each case, the components conventionally used can be used in a usual dose.

Taking mouthwash as an example, a thickener,
Sweeteners, pH adjusters, preservatives, solvents, etc. are used. As thickeners, sorbitol, glycerin, propylene glycol, 1,3-butylene glycol, polyoxyethylene glycol, xylitol, maltitol, lactit, etc. are compounded. obtain. Examples of sweeteners include stevioside, stevia extract, rebaudioside, neohesperidyl dihydrochalcone, acesulfame, thaumatin, glycyrrhizin, glycyrrhizin monoglucoside, hernanzurutin, perillartin, saccharin, saccharin sodium, and the like. Organic acids and salts such as acids and salts thereof, phosphoric acids and salts thereof, malic acid and salts thereof, acetic acid and salts thereof, organic acids and salts thereof, preservatives such as methylparaben, solvents such as ethanol and water, and other components are mixed and mixed. Can be manufactured.

In addition, in the case of other oral compositions such as chewing gum and troche, the conventionally used components can be produced in a usual amount and in a usual manner.

In the present invention, the active ingredient such as dextranase, mutanase, lysozyme, amylase, protease, lytic enzyme, superoxide dismutase or other enzyme is used as long as the effect of the present invention is not impaired. One or more kinds may be blended.

[0022]

The oral composition of the present invention has a high caries-inhibiting effect and a high stability over time.

[0023]

EXAMPLES The present invention will be specifically described below with reference to experimental examples and examples, but the present invention is not limited to the following examples. In addition, all% in each example are weight%.

[Experimental Example 1] Synergistic effect confirmation experiment (implemented in a caries preventive animal experiment) (Experimental method) The following animal experiments were performed to examine the caries inhibitory effect of a drug.

Using a golden hamster which is a caries model system, dentifrices containing the components shown in Tables 1 and 2 were prepared, and the caries inhibiting ability was examined.

Three-week-old (male) hamsters, each consisting of 10 rats, were infected with the streptomycin-resistant cariogenic bacterium Streptococcus mutans 10449 strain. Infection was carried out by inoculating one platinum loop of the above strain into 4 ml of BHI medium (manufactured by BBL), culturing at 36 ° C. for 20 hours under anaerobic conditions, and then dropping 0.1 ml of this bacterial solution into the mouth for 3 days. went.

The colonization of the bacteria in each hamster was confirmed using an MS agar medium (manufactured by Difco) containing 0.1% streptomycin.

The administration of the drug should be continued for 5 minutes after confirmation of bacterial colonization.
Went for a week. The drug used was prepared by extracting the above dentifrice that had been used for business with three times the amount of water.

[0029] The administration method was to instill 0.3 ml of 0.1 ml each in the mouth and left and right cheek pouches twice a day.
In the control group, filtered ion-exchanged water was administered dropwise in the same manner as described above.

As a feed during the experiment, a caries-inducing powder sample Diet2000 (manufactured by CLEA Japan) was used. Drinking water used was ion-exchanged water filtered through a membrane filter having a pore size of 0.2 μm. The evaluation of caries was carried out according to the method of KYESE (J. Dent. Res. 23, 1944).

The caries inhibition rate was calculated by the following equation.

[0032]

(Equation 1)

[0033]

[Table 1]

[0034]

[Table 2]

From the results shown in Tables 1 and 2, it can be seen that the composition using triclosan, sodium fluoride and sodium bicarbonate together has a stronger caries-preventing effect than the composition using two kinds in combination. In addition, a synergistic caries preventive effect was not observed with fluorine compounds other than sodium fluoride and phenolic fungicides other than triclosan. That is, triclosan has a caries prevention synergistic effect with sodium fluoride and sodium bicarbonate, and is preferably 0.1%.
It can be seen that a blending amount of 01% or more, more preferably 0.02% or more is good. Sodium fluoride has a caries prevention synergistic effect with triclosan and sodium bicarbonate,
It is understood that the amount is preferably 0.01% or more, more preferably 0.1% or more. Sodium bicarbonate has a caries prevention synergistic effect with triclosan and sodium fluoride, preferably 1% or more, more preferably 5%.
As described above, it is found that the blending amount is more preferably 10% or more.

Experimental Example 2 A dentifrice containing the components shown in Table 3 was prepared and stored at 60 ° C. for one month, and its caries-preventing effect was evaluated using the same method as in Experimental Example 1.

[0037]

[Table 3]

According to the results shown in Table 3, the potassium ion source is preferably added in an amount of 0.001% or more, more preferably 0.01% or more, whereby the synergy of caries suppression in the combined use of triclosan, sodium fluoride and sodium hydrogen carbonate is obtained. It can be seen that the stability over time of the effect increases. Further, it is understood that potassium hydroxide, potassium chloride, and potassium carbonate are preferable as the potassium ion source.

Example 1 Toothpaste Silica anhydride 20.0% Glycerin (85%) 35.0 Propylene glycol 5.0 Sodium lauryl sulfate 1.2 Carboxymethylcellulose sodium 0.6 Carrageenan 0.5 Saccharin sodium 0.1 Fragrance 1.3 Triclosan 0.1 Sodium fluoride 0.2 Sodium bicarbonate 20.0 Potassium hydroxide 0.5 Water Balance 100.0%

Example 2 Toothpaste Dibasic calcium phosphate dihydrate 35.0% Sorbit (70%) 20.0 Propylene glycol 4.0 Sodium lauryl sulfate 1.4 Sodium carboxymethylcellulose 0.8 Carrageenan 2 Saccharin sodium 0.1 Fragrance 1.2 Triclosan 0.2 Sodium fluoride 0.3 Sodium bicarbonate 15.0 Potassium chloride 1.0 Water Balance 100.0%

Example 3 Toothpaste Aluminum Hydroxide 35.0% Sorbit (70%) 25.0 Propylene Glycol 3.0 Sodium Lauryl Sulfate 1.5 Sodium Alginate 0.6 Xanthan Gum 0.5 Gelatin 0.2 Saccharin Sodium 0.1 Perfume 1.0 Triclosan 0.3 Sodium fluoride 0.22 Sodium bicarbonate 10.0 Potassium carbonate 1.0 Dextranase 3000u / g Toothpaste Lauroyl sarcosine sodium 0.5 Water Balance 100.0%

Example 4 Toothpaste Calcium Carbonate 35.0% Glycerin (85%) 25.0 Propylene Glycol 5.0 Sodium Lauryl Sulfate 1.8 Sodium Alginate 0.3 Xanthan Gum 0.1 Saccharin Sodium 0.1 Fragrance 1 .6 Triclosan 0.1 Sodium fluoride 0.1 Sodium bicarbonate 10.0 Potassium bicarbonate 10.0 Water balance 100.0%

Example 5 Toothpaste Silicic anhydride 20.0% Sorbit (70%) 30.0 Propylene glycol 4.0 Sodium lauryl sulfate 1.0 Carboxymethylcellulose sodium 0.7 Carrageenan 0.6 Saccharin sodium 0.1 Perfume 0.8 Triclosan 0.1 Sodium fluoride 0.5 Sodium bicarbonate 15.0 Potassium carbonate 15.0 Water Balance 100.0%

Example 6 Toothpaste Aluminum hydroxide 35.0% Glycerin (85%) 20.0 Propylene glycol 3.0 Sodium lauryl sulfate 1.1 Carboxymethylcellulose sodium 0.4 Carrageenan 0.5 Saccharin sodium 0.1 potassium perfume 1.5 triclosan 0.2 sodium fluoride 0.1 sodium bicarbonate 25.0 metaphosphate 5.0 dextranase 3000 u / g dentifrice lauroylsarcosine sodium 0.5 mutanase 100u / g dentifrice water balance total 100. 0%

Example 7 Liquid Toothpaste 15.0% Silicic Anhydride 1% Glycerin (85%) 10.0 Sorbite (70%) 30.0 Propylene Glycol 1.0 Sodium Lauryl Sulfate 2.0 Decaglyceryl Laurate 0. 5 Sodium sulfate (anhydrous) 0.3 Sodium carboxymethylcellulose 0.3 Sodium saccharin 0.1 Fragrance 1.4 Triclosan 0.05 Sodium fluoride 0.22 Sodium bicarbonate 5.0 Potassium pyrophosphate 1.0 Water Balance 100. 0%

Example 8 Mouthwash Sodium Citrate 0.2% Ethanol 1.0 Glycerin (85%) 10.0 Sodium Saccharin 0.1 Sodium Benzoate 0.3 Methyl Parahydroxybenzoate 0.1 Perfume 0.5 Sodium bicarbonate 5.0 Potassium hydroxide 0.05 Triclosan 0.1 Mutanase 30u / g Toothpaste Sodium fluoride 0.22 Water Balance 100.0%

All of the oral compositions of the above examples exhibited high caries prevention effects.

 ──────────────────────────────────────────────────続 き Continuing from the front page (72) Inventor Satoshi Fukasawa Lyon Co., Ltd. 1-3-7, Honjo, Sumida-ku, Tokyo

Claims (1)

[Claims] 1. An oral composition comprising an oral composition using triclosan, sodium hydrogen carbonate and sodium fluoride in combination with a potassium ion source.