JP4344844B2 - Oral composition - Google Patents

Description

  The present invention relates to a composition for oral cavity, and more specifically, by using it in contact with the gums, preventing changes in the color of the gums due to smoking, dental restorations, and periodontal diseases, making the gums more natural and healthy The composition for oral cavity which has the effect | action which improves to a favorable color tone, and is highly safe.

In the gums, pigment cells are present just like skin. It is known that the production of melanin pigment from pigment cells is increased by factors such as smoking, metal eluted from dental restorations, inflammation, and dryness in the oral cavity, leading to pigmentation of gums. Another factor is considered to be the adhesion of spears to the gums and deterioration of blood circulation due to smoking.
In the oral mucosa, gums are frequently pigmented and easy to see. With the recent increase in awareness regarding dental esthetics, teeth are required to be beautiful and white, and whitening has become common. At the same time, a natural and healthy pink color tone is required for gums.

The coloration of gums is often due to melanin as well as the skin pigmentation by ultraviolet rays. Conventionally, various studies have been carried out to suppress skin pigmentation. These include a method of directly acting on pigment cells that produce melanin pigment, a method of inhibiting tyrosinase, which is a rate-limiting enzyme that produces melanin, and suppression of pigment cell growth factor produced by ultraviolet rays.
On the other hand, an oral composition containing a hydroxy-2-pyrrolidone derivative has been proposed as an anti-discoloration agent for oral mucosa (see, for example, Patent Document 1).
However, many of the conventionally used substances have problems in stability and safety, and the effect of preventing pigment deposition is not yet satisfactory, and development of better drugs is expected.

JP 2000-38312 A

  An object of the present invention is to provide an oral composition that has an action of improving gums to a more natural and healthy color tone and is highly safe.

As a result of intensive studies in view of the above circumstances, the present inventors have noted that α-arbutin has an excellent melanin production inhibitory effect, and can exhibit an effect of improving gums to a natural and healthy color tone. That is, α-arbutin was found to be effective as a so-called whitening component for gums, and the present invention was completed.
Accordingly, the present invention is an oral composition containing α-arbutin. In the embodiment of the present invention, it is appropriate to contain 0.001 to 10% by mass of α-arbutin in the composition for oral cavity.

  The composition for oral cavity containing α-arbutin of the present invention can exhibit an excellent inhibitory action on melanin production, exhibits a high inhibitory effect on the pigmentation of gums, and a natural and healthy color tone of gums. It is effective for improvement.

The oral composition as used in the present invention is not particularly limited as long as it can be in contact with the gums at the time of use, and includes various dosage forms such as a dentifrice, a mouthwash, and a massaging gum. can do. Specific forms of the oral composition include, for example, toothpastes, toothpastes, liquid dentifrices, moisturized dentifrices, liquid dentifrices, and other mouthwashes, mouthwashes, mouthwashes, mouth fresheners, and gargles. Tablet, ointment preparation, cream preparation, chewing gum and the like.
In the present specification, α-arbutin means hydroquinone-α-D-glucopyranoside, and its structure is as follows.

α-Arbutin is obtained, for example, by glycosylation of hydroquinone with an enzyme derived from bacteria. This enzyme is α-amylase, and this α-amylase is, for example, amylase X-23 disclosed in Japanese Patent No. 2666667. It may be. α-amylase is also commercially available and can be obtained on the market, and a commercially available product can be used in the present invention.
The content of α-arbutin in the oral composition of the present invention is suitably 0.001 to 10% by mass based on the total mass of the oral composition from the viewpoint of cost and the effects intended by the present invention. Preferably, it is 0.01-5 mass%, More preferably, it is 0.1-5 mass%.

The oral composition of the present invention can be prepared according to a conventional method by blending appropriate bases and additives conventionally used according to various forms of the oral composition.
For example, the following bases and additives can be blended in a dentifrice such as a toothpaste.
Abrasive: Silica-based abrasive such as crystalline silica, amorphous silica, other silicic anhydride, hydrous silicic acid, aluminosilicate, aluminum oxide, aluminum hydroxide, insoluble sodium metaphosphate, insoluble potassium metaphosphate, titanium oxide, Dibasic calcium phosphate dihydrate, dibasic calcium phosphate anhydrate, heavy calcium carbonate, light calcium carbonate, calcium pyrophosphate, etc. (usually 3 to 99% by mass).

Binder: Carrageenan, carboxymethylcellulose, sodium carboxymethylcellulose, cellulose derivatives such as methylcellulose, hydroxymethylcellulose, sodium carboxymethylhydroxymethylcellulose, alkali metal alginates such as sodium alginate, propylene glycol alginate, xanthan gum, tragacanth gum, caraya gum, gum arabic, etc. Synthetic binders such as gums, polyvinyl alcohol, sodium polyacrylate, carboxyvinyl polymer, polyvinylpyrrolidone, and inorganic binders such as gelling silica, gelling aluminum silica, vegant, and laponite (normal blending amount 0) .5 to 10% by mass).
Wetting agent: sorbit, glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, polyethylene glycol, polypropylene glycol, xylit, maltite, lactit, etc. (usually 1 to 50% by mass).

  Surfactant: sodium lauryl sulfate, sodium α-olefin sulfonate, sodium dodecylbenzene sulfonate, sodium lauryl sulfoacetate, sodium N-lauroyl sarcosine, N-acyl glutamate, sucrose fatty acid ester, polyoxyethylene hydrogenated castor Oils, polyoxyethylene polyoxypropylene block copolymers, alkylglycosides, sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters, alkyldimethylamine oxide, and the like (the amount is usually 0 to 5% by mass).

Further, as optional components, for example, sweeteners such as saccharin sodium, stevioside, glycyrrhizin, perilartin, thaumatin, aspartylphenylalanine methyl ester, p-methoxycinamic aldehyde, sucrose, fructose, sodium cyclamate; spearmint oil, peppermint oil, winter green Perfume such as oil, sassafras oil, clove oil, eucalyptus oil, sage oil, mayonnaise oil, thyme oil, lemon oil, orange oil, l-menthol, carvone, anethole, eugenol, thymol, methyl salicylate; benzoic acid, sodium benzoate , P-hydroxypropyl benzoic acid, p-hydroxybutyl benzoic acid, lower fatty acid monoglycerides, parabens and other preservatives; quaternary ammonium salts, tri Bactericides such as Losan, alkyldiaminoethylglycine hydrochloride, cetylpyridinium chloride, decalinium chloride, benzethonium chloride; enzymes such as ε-aminocaproic acid, dextranase, amylase, protease, mutanase, lytic enzyme, lysozyme; monofluorophosphoric acid Fluorides such as sodium, potassium monofluorophosphate, sodium fluoride, ammonium fluoride, stannous fluoride; chlorhexidine salts, dihydrocholesterol, glycyrrhetin salts, glycyrrhetinic acid, chlorophyll, caropeptide, tocopherol acetate, azulene, lysozyme chloride, Anticalculus agents such as zeolite and polyphosphoric acid, anti-plaque agents, potassium nitrate, aluminum lactate and the like can be added.
In addition, the addition amount of these arbitrary components can be made into a normal amount in the range which cannot prevent the effect of this invention.

Test examples are shown below. In addition, description of only% means the mass%.
[Test of melanin production inhibitory effect]
α-Arbutin was tested for melanin production inhibitory action.
[Test method and evaluation method]
Mouse-derived B16 melanoma cells were seeded in a 25 cm ² culture flask and cultured under conditions of carbon dioxide concentration 5% and 37 ° C. using Eagle's MEM medium containing 10% FBS. After 24 hours of culture, the medium was replaced with Eagle's MEM medium containing 10% FBS and theophylline (0.08 mg / ml), and α-arbutin was added to a final concentration of 10, 100 μg / ml and mixed. After further culturing for 2 days, the medium was removed, washed with a phosphate buffer, cells were detached from the flask using trypsin and EDTA-containing medium, and the cells were recovered from the cell suspension by centrifugation. The obtained cells were added with 1N NaOH containing 10% DMSO, heated and dissolved at 80 ° C. for 60 minutes, the absorbance at 405 nm was measured, and the inhibition rate of melanin production was determined by the following formula.
The amount of melanin was determined as the amount per cell. For comparison, β-arbutin was similarly tested.
Melanin production inhibition rate (%) = {(control melanin amount−sample melanin amount) / control melanin amount} × 100
The results are shown in Table 1.

表１の結果から、β−アルブチンと比較してα−アルブチンが強いメラニン生成抑制効果を有していることが認められた。従ってα−アルブチンを歯ぐきに適用することにより優れたメラニン生成抑制作用を発揮して、歯ぐきの色素沈着をより効果的に抑制することが期待できる。

From the results of Table 1, it was confirmed that α-arbutin has a stronger melanin production inhibitory effect than β-arbutin. Therefore, by applying α-arbutin to the gums, it is possible to exhibit an excellent inhibitory effect on melanin production and to more effectively suppress gum pigmentation.

A toothpaste was prepared by a conventional method with the composition (unit: mass%) shown in Table 2 below, and the gum whitening effect when α-arbutin was blended was examined. For comparison, a toothpaste containing no α-arbutin was prepared.
The test method was 10 males for each dentifrice, and was used to massage the gums on a toothbrush twice daily in the morning and evening. The test was conducted for 40 days. As a whitening effect, returning to the original gum color was evaluated according to the following criteria, and the scores of 10 people were totaled. The results are shown in Table 2.
Score 3 Excellent score 2 Effective score 1 Slightly effective score 0 Invalid

表２の結果に示されたように，α−アルブチンを配合した本発明の練歯磨剤を歯ぐきに適用することにより、健康的な歯ぐきの色調へと改善されることが明らかとなった。

As shown in the results of Table 2, it was clarified that the toothpaste of the present invention containing α-arbutin was improved to a healthy gum color by applying it to the gums.

Preparation of toothpaste A toothpaste was prepared according to a conventional method with the following formulation (unit: mass%).
Calcium hydrogen phosphate anhydrate 20.0
Calcium hydrogen phosphate dihydrate 20.0
Silicic anhydride 5.0
Color Guinan 0.7
Sodium carboxymethylcellulose 0.3
Glycerin 20.0
70% sorbite solution 10.0
Methyl paraoxybenzoate 0.1
Triclosan 0.1
Saccharin sodium 0.1
Sodium lauryl sulfate 1.5
DL-α-tocopherol 0.1
Polyethylene glycol 1.0
α-Arbutin 0.1
Fragrance 1.0
Purified water remaining
100.0%

Preparation of toothpaste A toothpaste was prepared according to a conventional method with the following formulation (unit: mass%).
Silica anhydride 20.0
Titanium dioxide 0.5
Color Guinan 1.0
Propylene glycol 3.0
70% sorbite solution 20.0
Glycerin 20.0
Methyl paraoxybenzoate 0.1
Sodium monofluorophosphate 0.05
Cetylpyridinium chloride 0.1
Sodium lauryl sulfate 1.7
Lauroyl sarcosine sodium 0.3
Copper chlorophyllin sodium 0.05
DL-α-tocopherol 0.1
Polyethylene glycol 1.0
α-Arbutin 0.1
Fragrance 1.0
Purified water remaining
100.0%

Preparation of toothpaste A toothpaste was prepared according to a conventional method with the following formulation (unit: mass%).
Aluminum hydroxide 30.0
Silicic anhydride 5.0
Sodium chloride 10.0
Sodium carboxymethylcellulose 1.0
Glycerin 20.0
Sodium lauryl sulfate 1.8
Isopropylmethylphenol 0.02
Tocopherol acetate 0.1
Polyoxyethylene hydrogenated castor oil 3.0
Ethyl paraoxybenzoate 0.1
DL-α-tocopherol 0.1
Polyethylene glycol 1.0
α-Arbutin 0.1
Fragrance 1.0
Purified water remaining
100.0%

Preparation of toothpaste A toothpaste was prepared according to a conventional method with the following formulation (unit: mass%).
Calcium pyrophosphate 32.0
Silica anhydride 6.0
Sodium carboxymethylcellulose 1.0
Glycerin 25.0
Glycyrrhetinic acid 0.2
Cetylpyridinium chloride 0.05
Epsilon aminocaproic acid 0.1
DL-α-tocopherol 0.1
Polyethylene glycol 1.0
α-Arbutin 0.1
Fragrance 0.1
Purified water remaining
100.0%

Preparation of liquid dentifrice A liquid dentifrice was prepared according to a conventional method with the following formulation (unit: mass%).
Silicic acid 10.0
Xanthan gum 1.0
Glycerin 10.0
70% sorbite solution 30.0
Xylitol 1.0
Ethyl paraoxybenzoate 0.1
Butyl paraoxybenzoate 0.05
Sodium dihydrogen phosphate dihydrate 0.3
Sodium hydroxide 0.05
DL-α-tocopherol 0.1
Polyethylene glycol 1.0
α-Arbutin 0.1
Fragrance 0.5
Purified water remaining
100.0%

Preparation of mouthwash A mouthwash was prepared according to a conventional method with the following formulation (unit: mass%).
Ethanol 5.0
Polyoxyethylene hydrogenated castor oil 0.5
Glycerin 5.0
Xylitol 25.0
Cetylpyridinium chloride 0.05
Dipotassium glycyrrhizinate 0.05
Ethyl paraoxybenzoate 0.05
Propyl paraoxybenzoate 0.05
Citric acid 0.03
Sodium citrate 0.12
Yellow No. 0.0002
Green No. 3 0.0002
DL-α-tocopherol 0.1
Polyethylene glycol 1.0
α-Arbutin 0.1
Purified water remaining
100.0%

Preparation of chewing gum Chewing gum was prepared according to a conventional method with the following formulation (unit: mass%).
Gum base 40.0
Calcium carbonate 2.0
Water candy 15.0
Sugar 30.0
Magnesium citrate 2.55
Sorbic acid 0.2
DL-α-tocopherol 0.1
Polyethylene glycol 1.0
α-Arbutin 0.1
Purified water remaining
100.0%

Preparation of Ointment An ointment was prepared according to a conventional method with the following formulation (unit: mass%).
Cetanol 20.0
Squalane 5.0
Sorbitan monooleate 1.0
Saccharin sodium 0.1
Fragrance 0.3
α-Arbutin 0.1
Purified water remaining
100.0%

Preparation of ointment White petrolatum prepared according to a conventional method with the following formulation (unit:% by weight) 10.0
Propylene glycol 5.0
Stearyl alcohol 10.0
Hydroxypropylcellulose 2.0
Polyethylene glycol 400 60.0
Saccharin sodium 0.1
Fragrance 0.3
α-Arbutin 0.1
Purified water remaining
100.0%

Preparation of Ointment An ointment was prepared according to a conventional method with the following formulation (unit: mass%).
Concentrated glycerin 30.0
Sodium carboxymethylcellulose 2.0
Saccharin sodium 0.1
Fragrance 0.3
α-Arbutin 0.1
Purified water remaining
100.0%

Preparation of Ointment An ointment was prepared according to a conventional method with the following formulation (unit: mass%).
Concentrated glycerin 30.0
Agar 2.0
Saccharin sodium 0.1
Fragrance 0.3
α-Arbutin 0.1
Purified water remaining
100.0%

Preparation of Ointment An ointment was prepared according to a conventional method with the following formulation (unit: wt%).
Ethanol 1.0
Saccharin sodium 0.1
Fragrance 0.3
α-Arbutin 0.1
Gelled hydrocarbon remaining
100.0%

Claims (4)

A dentifrice composition comprising α-arbutin. The dentifrice composition according to claim 1, which is selected from powder dentifrices, toothpastes, liquid dentifrices, moisturizing dentifrices and liquid dentifrices. The dentifrice composition according to claim 1 or 2, comprising 0.001 to 10% by mass of α-arbutin. The dentifrice composition of Claim 3 containing 0.1-1.0 mass% of alpha-arbutin.