JPH07258053A - Composition for oral cavity - Google Patents

Abstract

PURPOSE:To obtain a composition for oral cavity having an excellent suppression effect of pH reduction of a bacterial plaque, constituted by containing arginine, canavanine or their salts, and a carbon dioxide producing agent or carbon dioxide. CONSTITUTION:Arginine, canavanine which is an arginine analog, and their salts of 0.05-20wt.%, and a carbon dioxide producing agent or carbon dioxide of 0.5-20wt.% are contained in this composition. Further, a calcium ion capturing agent of 0.05-50wt.% is contained in it as indispensable component, and the other optional components which are added in an usual composition for oral cavity, are added to adjust pH of 5-10, when it is dissolved in water of 10 fold amount. By combining arginine, canavanie or their salts having a high safety and the carbon dioxide producing agent or carbon dioxide, with a manifestation of suppressing effect of lactic acid production, together with promoting effect of its decomposition, a reduction of pH of a bacterial plaque is suppressed. Since, even taking a food containing sucrose at the same time, the pH lowering is suppressed, a cariogenicity is reduced, and it is useful in fields of quasi-drug, a cosmetic and a food, and capable of changing a bacterial flora in the oral cavity to a flora rich with a goody bacteria.

Description

Detailed Description of the Invention

[0001]

The present invention relates to quasi drugs, cosmetics,
Regarding the oral composition in the field of food, suppressing the generation of acid that is the cause of caries, promoting the decomposition of the generated acid, suppressing the pH decrease of plaque, to prevent dental caries .

[0002]

2. Description of the Related Art Dental caries is a Streptococcus mutans contained in dental plaque.
It occurs when the pH is lowered by the acid production of bacteria such as s) and the teeth are decalcified. Therefore, conventionally, a composition for oral cavity has been proposed in which a bactericidal agent or a tooth strengthening agent is blended for the purpose of preventing dental caries. Examples of fungicides include chlorhexidines and triclosan, and examples of tooth strengthening agents include fluorides, but these have safety concerns, so they can only be used at low concentrations as active ingredients in medicated dentifrices. is the current situation. As a matter of course, there is a problem that effects cannot be expected because they cannot be used in oral refreshing agents and foods, and although medicinal dentifrices can be expected to some extent, they are not as safe as foods. There is.

Further, as a method for preventing the pH of dental plaque from decreasing, 1) do not ingest saccharides such as sucrose having high cariogenicity, 2) suppress acid production, and 3) remove or decompose acid. 4) to neutralize the acid, etc., and among them, compositions having higher safety than oral compositions containing the above-mentioned bactericide and tooth strengthening agent have been proposed. In particular,
For example, for 1), palatinose, xylitol,
Maltitol is considered as an alternative sugar, but it is practically impossible to substitute all of them for sucrose.
Regarding 2), although one kind of sialin, which is an oligomeric peptide in saliva, has a pH increasing effect, it promotes the production of lactic acid and is industrially difficult to obtain (JP-A-53-263331). , Microbial Asp
ect of Dental Carriers p. 43
3, Information Retrieval
Inc. , 1976. ). In addition, it has been reported that arginine alone suppresses lactic acid production in human whole saliva, and arginine alone does not suppress lactic acid production in human whole saliva (dentistry 69 , 824, 1982.). There are examples (dentistry 73 , 344, 198)
5. ) Etc. are known, but a substance having an excellent suppressing effect has not yet been found. Regarding 3) and 4), only a cleaning agent or a pH adjusting agent has been proposed, and a solution for suppressing an essential pH decrease has not been reached.

[0004]

Therefore, an object of the present invention is to provide an oral composition which is excellent in the effect of suppressing the pH decrease of dental plaque and which is more safe than the composition containing a bactericide or a tooth strengthening agent. To do.

[0005]

In view of the above circumstances, the present inventors have conducted intensive studies to improve the effect of suppressing the pH decrease of dental plaque, and as a result, said arginine, canavanine which is an arginine-related compound or a salt thereof. , A composition for oral cavity in which a carbon dioxide generator or carbon dioxide is combined, fixes the expression of the previously reported effect of suppressing acid production in saliva of arginine or canavanine, and is also excellent in the effect of suppressing pH decrease. The present invention has been completed by finding out that it is remarkable.

That is, the present invention provides an oral composition containing 0.05 to 20% by weight of arginine, canavanine or a salt thereof, and a carbon dioxide generator or carbon dioxide.

The present invention also provides an oral composition which further contains 0.05 to 50% by weight of a calcium ion scavenger in the above composition.

Arginine used in the present invention is one of the amino acids found in bean sprouts, and canavanine is one of the amino acids found in jack beans, both of which naturally exist as L-form. In the present invention, L-arginine, which has high safety and is easily available industrially, is preferable. Examples of these salts include hydrochloride, citrate, glutamate and the like.

[0009] Arginine, canavanine or a salt thereof is generally used in the oral composition of the present invention in an amount of 0.05 to 20% by weight, preferably 0.1 to 10% by weight. 0.0
If it is less than 5% by weight, a sufficient effect cannot be obtained, and if it exceeds 20% by weight, bitterness becomes strong, which is not preferable.

Of the carbon dioxide generators or carbon dioxide used in the present invention, when a carbon dioxide generator is used,
It is not particularly limited as long as it generates carbon dioxide when used, but a combination of a component that decomposes to generate carbon dioxide and a decomposing agent of this component is preferable, for example, a combination of a carbonate and an organic acid. It can be used together. here,
Representative carbonates include sodium hydrogen carbonate, potassium hydrogen carbonate, and the like, and malic acid as the organic acid,
Examples thereof include citric acid, tartaric acid, ascorbic acid, succinic acid and fumaric acid. These carbonates and organic acids may be used alone or as a mixture of two or more.

When a carbonate and an organic acid are used in combination,
By reacting the carbonate with the organic acid, the hydrogen atom of the organic acid reduces the carbonate, and as a result, an organic acid salt is generated, and the carbonate releases water and carbon dioxide. In an environment where water is present, such as in the oral cavity, this reaction is accelerated and the carbon dioxide released causes foaming.

In the present invention, the carbon dioxide generator is 0.5 to 40% by weight, preferably 2.5 to 2% by weight based on the total amount of the composition.
5% by weight is blended. The amount of carbon dioxide generating agent is 0.
If it is less than 5% by weight, a sufficient effect cannot be obtained, and if it exceeds 40% by weight, irritation becomes strong and taste is impaired. When a combination of a carbonate and an organic acid is used as the carbon dioxide generator, the carbonate is preferably added in an amount of 0.2 to 16% by weight, particularly 1 to 10% by weight, based on the total amount of the composition. It is preferable to add 0.3 to 24% by weight, and especially 1.5 to 15% by weight in the total amount of the product.

When carbon dioxide is used, 10% by volume of carbon dioxide is added after the oral composition is placed in a closed container.
It is possible to melt under pressure by filling the gas contained above at a pressure of 1 to 20 kg / cm ² . Here, the closed container is preferably an aerosol type, and since carbon dioxide is a gas at room temperature, it can also function as a propellant. As a propellant other than carbon dioxide, known propellants such as oxygen, nitrogen, helium, liquefied propane gas (LPG), chlorofluorocarbon and liquefied natural gas (LNG) may be used in consideration of safety on the human body. It can also be used as a mixture with.

The oral composition of the present invention is preferably adjusted to have a pH of 5 to 10, particularly 6 to 8 when dissolved in 10 times the amount of water. If the pH is less than 5, the hydroxyapatite, which is the main component of the tooth, dissolves on the acidic side of about pH 5.5, so there is a risk of decalcifying the tooth.
If it exceeds, bitterness is strong, which is not preferable.

As such a pH adjuster, those commonly used can be used. Specifically, in addition to arginine and canavanine which are essential components as a basic substance, sodium hydroxide, potassium hydroxide and triethanol can be used. Amine, ammonia, lysine, sodium hydrogencarbonate, etc. are mentioned, and as an acidic substance, in addition to carbon dioxide which is an essential component, acetic acid,
Examples thereof include hydrochloric acid, sulfuric acid, phosphoric acid, citric acid, tartaric acid and malic acid.

In addition, Streptococcus mutans in dental plaque
Since s) is promoted to grow by calcium ion, the oral composition of the present invention contains a calcium ion scavenger in an amount of 0.05 to 50% by weight, particularly 0.1 to 10% by weight based on the total amount of the composition. Is preferred.

As such a calcium ion scavenger,
Specific examples include 4A type zeolite, albumin, globulin, casein phosphopeptide, disodium citrate, trisodium citrate, pyrophosphate, polyphosphate and the like. Further, examples of the calcium ion scavenger include EDTAs, but these are not preferable because they risk decalcifying teeth.

In addition to the above-mentioned essential components, the oral composition of the present invention may contain conventional medicated components in a mouth-cooling agent, medicated toothpaste and medicated mouthwash. Specifically, vitamins such as ascorbic acid, tocopherol, riboflavin; chlorhexidine hydrochloride, benzalkonium chloride,
Fungicides such as benzethonium chloride, cetylpyridinium chloride, isopropylmethylphenol and triclosan; enzymes such as dextranase, protease and lysozyme; plant components such as glycyrrhizinates and chlorophylls; herbal medicines such as acacia yam and ginger; fluoride Fluorine agents such as sodium and sodium monofluorophosphate may be used. These medicinal components can be used alone or in combination of two or more, and can be used in an amount within the pharmaceutically acceptable range.

Further, the oral composition of the present invention may contain a sweetening agent or a sugar or sugar alcohol which also serves as a sweetening agent and a wetting agent. Such sweeteners include, for example, saccharin, saccharin sodium, aspartame, stevia extract and the like, and sugars or sugar alcohols include, for example, palatinose, panose, xylitol, mannitol, maltitol, sorbitol, lactose, lactitol, fructooligosaccharides and the like. Those having cariogenic properties such as sucrose, glucose and fructose are not preferred.

Furthermore, the oral composition of the present invention contains an optional ingredient such as starch, which is added to a usual oral composition.
Dextran, dextrin, reduced starch degradation product, crystalline cellulose, sodium carboxymethyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, gum arabic,
Caking agents such as carrageenan, pectin, sodium alginate, sodium chondroitin sulfate, sodium caseinate, etc., which are usually used in formulation; solvents such as ethanol, propylene glycol, polyethylene glycol; sodium alkylsulfate, alkylphosphoric acid, polyoxyethylene curing Surfactants such as castor oil, sucrose fatty acid ester, glycerin fatty acid ester; abrasives such as calcium hydrogen phosphate, aluminum hydroxide, silicic acid anhydride, calcium carbonate; taste masking such as zinc chloride, powdered green tea, ginger tincture, etc. Agents; preservatives such as paraben, sodium salicylate, sodium benzoate, etc., and fragrances can also be appropriately added.

The oral composition of the present invention is manufactured by a conventional method and used in the fields of quasi drugs, cosmetics and foods.
In addition, its aspect can also be a mouthwash, mouthwash, powder / dentifrice, confectionery, etc., and its dosage form is liquid,
Various dosage forms such as lozenges, tablets, granules, powders, propellants, pills, etc. can be selected.

When a carbon dioxide generator is added to the oral composition of the present invention, it is necessary to devise it so that carbon dioxide is generated during use. For example, a preparation containing no water or a reaction component was separated. Formulations are possible. Specifically, lozenges and tablets can be produced with a tableting machine having a compression molding function, and the ingredients can be formed into multiple layers according to the purpose.

When a combination of a carbonate and an organic acid is used as a carbon dioxide generator, these are made into separate layers, and at least one of these layers has arginine,
Canavanine or a salt thereof can be contained.
In a further preferred embodiment, a multilayer structure of three layers is formed between the carbonate layer and the organic acid layer via a layer that does not react with these layers, and at least one of these layers contains arginine, canavanine or a salt thereof. is there. Further, the carbonate and / or the organic acid may be coated and used. Examples of the coating agent used here include polyethylene glycol, sodium polyacrylate,
Examples thereof include water-soluble polymers such as hydroxyethyl cellulose, hydroxypropyl cellulose and sodium carboxymethyl cellulose. The coating method can be carried out by a conventional method such as melting and spraying the above-mentioned polymer, or spraying the above-mentioned polymer aqueous solution and then drying. The coating amount of these coating agents is usually 2 to the organic acid or carbonate.
About 30% by weight is preferable.

Further, since the carbonate and / or organic acid gradually reacts even with moisture in the air, the carbonate and / or the organic acid should be coated with the above-mentioned hydrophobic coating or immediately after production, a non-moisture permeable package such as an aluminum pillow sheet. It is preferable to seal with a material.

The oral composition of the present invention can be used at any time, but for the purpose of suppressing the generation of acid and promoting the decomposition of the generated acid to prevent dental caries, it can be used for foods containing sucrose. It is preferably used before, during, or after ingestion, and further effects can be expected when used as a mouth-cooling agent in the form of a formulation that easily remains in the oral cavity before meals and snacks.

[0026]

[Function] In the case of bacteria in the oral cavity, it is difficult to clearly distinguish between good bacteria and bad bacteria, but Streptococcus mutans (S) that produces lactic acid, which is the cause of pH decrease in dental plaque
Cariogenic bacteria such as Treptococcus mutans are obviously bad bacteria, and Streptococcus sanguis (Streptococcus s) that competes with these bacteria
bayionella (Veil) that decomposes anguis) and lactic acid
Streptococcus salivarius (Streptococcus) resident in bacteria of the genus Lonella and saliva
salivarus) is considered to be a good bacterium. Here, arginine or canavanine is Streptococcus
Mutants (Streptococcus muta)
lactic acid production of Streptococcus sanguis (Streptococcus sangu)
is) promotes the growth of. Furthermore, in the presence of a carbon dioxide generator or carbon dioxide, Bayillonella (Veillonell)
a) The decomposition of lactic acid by a genus bacterium is promoted. Bacteria belonging to the genus Baylonella decompose lactic acid into acetic acid and propionic acid, but since these are weaker acids than lactic acid, they will increase the pH of plaque. Further, the pH buffering ability of carbonate ions and bicarbonate ions derived from carbon dioxide is also considered to contribute to the suppression of plaque pH decrease. Conventionally, these components alone could not suppress the decrease in plaque pH so much, but the oral composition of the present invention is a combination of arginine or canavanine and a carbon dioxide generator or carbon dioxide, and the pH of plaque. It was found that a remarkable synergistic effect of suppressing the decrease is exhibited.

[0027]

EFFECT OF THE INVENTION The oral composition of the present invention improves the decomposition promoting effect as well as the decomposition promoting effect by adding highly safe arginine, canavanine or a salt thereof and a carbon dioxide generator or carbon dioxide. To prevent the plaque from lowering its pH. Therefore, the oral composition of the present invention suppresses the pH decrease even when ingesting a food containing sucrose at the same time, the cariogenicity is decreased, and it is useful in the fields of quasi drugs, cosmetics, and foods. Is. It can also be expected to change the oral flora to a flora containing many beneficial bacteria by long-term use.

[0028]

EXAMPLES Next, the present invention will be further described with reference to examples, but the present invention is not limited thereto.

Example 1 Oral troche (mouth cooling agent): After stirring and mixing the components shown in Table 1, a tablet having a diameter of 10φ and 0.5 g was compression-molded with a tableting machine (manufactured by Elwecka). Oral troche (pH of 7 when dissolved in 10 times amount of water)
(Adjusted to 5) was obtained. Next, as a pH decrease inhibition test, about 10 mg of plaque collected from an adult male was suspended in 5 ml of a test solution for pH determination (containing a 10 ml glass bottle), and then the above troche for oral cavity was put therein and tightly stoppered. , 37
It was kept at 1 ° C for 1 hour. Here, the test liquid is sucrose 20.
%, Tryptose 2%, a pH indicator, etc. were used (Pediatric dentistry magazine 21 , 107, 1983.), and the pH was also measured with a pH meter.

[0030]

[Table 1]

Results From Table 1, it was found that the products 1 to 3 of the present invention suppress the pH lowering than those of the comparative products 1 to 3, and the troche for oral cavity of the present invention has a remarkable pH lowering suppressing effect.

Example 2 Aerosol mouthwash: After stirring and mixing the components shown in Table 2, the mixture was placed in an aerosol can and filled with the filling gas shown in Table 2, and then a trace amount of hydrochloric acid or water was added so that the pH became 7.5. After adding sodium oxide, each gas was filled at a pressure of 5 kg / cm ² to obtain an aerosol type mouth rinse. Thereafter, 0.5 ml of these mouthwashes were taken out and immediately subjected to a pH reduction inhibition test in the same manner as in Example 1.

[0033]

[Table 2]

Results From Table 2, it was found that the products of the present invention 4 to 6 suppressed the pH lowering than the comparative products 4 to 5, and the aerosol type mouth rinse of the present invention had a remarkable pH lowering suppressing effect.

Example 3 Pills (cooling agent in mouth): Using a centrifugal fluidized granulator (CF granulator, manufactured by Freund), with crystalline sorbitol (20 mesh) as a core, the following one-component and two-layer components A small amount of water was sprayed in this order on the components and the three-layer component to coat them while drying, and granulated to a diameter of about 5 mm. Then, water was removed with a dry heat dryer to prepare pills that were chewed and used when applied in the oral cavity.

[0036]

[Table 3] Ingredients (%) (Nuclear ingredient) Sorbitol (20 mesh) 10.9 (One-layer ingredient) Sorbitol (fine powder) 14.0 Sodium hydrogen carbonate (fine powder) 5.0 l-Arginine (fine powder) 10 0.0 (two-layer component) xylitol (fine powder) 26.0 aspartame 0.1 porous dextrin 3.5 l-menthol 0.5 fragrance 0.5 (three-layer component) sorbitol (fine powder) 14.0 citric acid Powder 10.0 Tartaric acid powder 5.0 l-Ascorbic acid powder 0.5 Total 100.0

Example 4 Powder Dentifrice: The following ingredients were mixed to obtain a powder dentifrice.

[0038]

[Table 4] Components (%) Sorbitol (50 mesh) 51.74 Aluminum hydroxide 20.0 4A type zeolite 2.0 Myristyl phosphate 1.0 Polyethylene glycol-treated citric acid ^{* 1} Polyethylene glycol 2.0 Citric acid 9. 0 sodium hydrogen carbonate 7.0 l-arginine 4.0 sodium fluoride 0.20 sodium saccharin 0.05 dipotassium glycyrrhizinate 0.01 adsorbed dextrin ^{* 2} porous dextrin 1.2 α-cyclodextrin 1.0 l-menthol 0 .4 Peppermint oil 0.4 Total 100.0 * 1: Citric acid with polyethylene glycol stirred and adsorbed with a Henschel mixer (coating treatment). * 2: 1-Menthol was dissolved in peppermint oil, then stirred with a Henschel mixer together with porous dextrin and α-cyclodextrin, and the particle size was adjusted while adsorbing.

Claims (9)

[Claims] 1. An oral composition comprising 0.05 to 20% by weight of arginine, canavanine or a salt thereof, and a carbon dioxide generator or carbon dioxide. 2. The oral composition according to claim 1, wherein the amount of carbon dioxide generator is 0.5 to 40% by weight. 3. The oral composition according to claim 2, wherein the carbon dioxide generator is a combination of a carbonate and an organic acid. 4. The oral composition according to claim 3, wherein the carbonate and the organic acid are provided in separate layers, and at least one of these layers contains arginine, canavanine or a salt thereof. 5. The carbonate layer and the organic acid layer are overlaid via a layer which does not react with these layers, and at least one layer of these layers contains arginine, canavanine or a salt thereof. Oral composition. 6. The oral composition according to claim 3, wherein the carbonate and / or the organic acid is coated with a hydrophobic coating. 7. A gas containing 10% by volume or more of carbon dioxide.
1 to 20 kg / cm ²Melted under pressure with pressure
The oral cavity according to claim 1, which is filled in a closed container.
Composition. 8. A pH of 5 to 1 when dissolved in 10 times the amount of water.
The composition for oral cavity according to claim 1, wherein the composition is 0. 9. A calcium ion scavenger 0.05
% To 50% by weight.
The composition for oral cavity according to any one of 1.