JPH0826952A - Composition for oral cavity - Google Patents

Abstract

PURPOSE:To obtain a composition for oral cavity sufficiently presenting the activity of the cationic polysaccharide therein, having no offensive taste, good in usability, and excellent in preservability. CONSTITUTION:This composition for oral cavity is obtained by formulating a composition for oral cavity containing a cationic polysaccharide but free from both anionic and nonionic surfactants with a cyclodextrin and/or a water- soluble perfume obtained by extracting an oil-soluble perfume with a hydrous ethanol solution.

Description

Detailed Description of the Invention

[0001]

INDUSTRIAL APPLICABILITY The present invention sufficiently exhibits the active effect of cationic polysaccharides such as chitin and chitosan.
The present invention relates to a composition for oral cavity which has no off-taste and is easy to use and has excellent storage stability.

[0002]

2. Description of the Related Art Conventionally, the problems to be solved by the invention
It is known to mix chitin and chitosans as an active ingredient for caries prevention, alveolar pyorrhea prevention, and halitosis prevention (JP-A-59-101416, etc.). These chitins and chitosans are known to suppress the production of water-insoluble extracellular glucan by Streptococcus mutans, and are known to have the effect of firmly adhering to the tooth surface (Japanese Patent Laid-Open No. 61-216648). ), And is known to have an antibacterial action, therefore, it is effective to incorporate a cationic polysaccharide such as chitin or chitosan into an oral composition.

By the way, an oral composition generally contains a fragrance for masking the off-taste derived from a base or a compounding agent and for enhancing the feeling of use. In particular, when a component having a strong off taste such as bitterness such as a cationic polysaccharide is blended, an oil-soluble flavor is used in terms of potency.

However, when an oil-soluble flavoring agent is added to a formulation system, an anionic or nonionic surfactant is generally added as a solubilizing agent, but a cationic polysaccharide is used in combination with the above-mentioned surfactant. Has the drawback of being deactivated. Further, for example, the above problem can be avoided by blending an excessive amount of a cationic polysaccharide, but in this case, problems may occur in terms of harmfulness, preservation stability, masking of bitterness, and anionic type. Alternatively, the nonionic surfactant itself also causes oral mucous membrane delamination, oral irritation and off-taste, which causes adverse effects such as changes in food taste and reduced usability. As described above, when a cationic polysaccharide is added to the oral composition, any one of storage stability, masking of an unpleasant taste, and an optimum amount of compound must be sacrificed.

Japanese Patent Laid-Open No. 54-70443 proposes an attempt to use an oil-soluble fragrance as an essence in order to mask an unpleasant taste and improve usability in a dentifrice composition. It cannot be used without the presence of the above surfactants which reduce the activity of the polysaccharide. Further, regarding the cationic bactericidal agent, see Japanese Patent Application Laid-Open No.
No. 931 discloses a taste improving method using a quaternary ammonium salt in a cationic bactericide in a limited manner.
However, this method is effective only within a limited range of cationic bactericides, which limits the range of applications.

Therefore, in the oral composition containing a cationic polysaccharide, it is desired that the cationic polysaccharide has a high activity effect in a wide range, an improvement in taste, an improvement in usability and a preservation stability.

The present invention has been made in view of the above circumstances,
It is an object of the present invention to provide an oral composition that exhibits the active effect of a cationic polysaccharide sufficiently, exhibits no off-taste, has good usability, and has excellent storage stability.

[0008]

Means and Actions for Solving the Problems As a result of extensive studies conducted by the present inventor to achieve the above object, the composition for oral cavity containing a cationic polysaccharide was extracted with an oil-soluble perfume by a hydrous ethanol solution. When one or both of the water-soluble fragrance and the cyclodextrin obtained by blending, it is not necessary to blend the anionic and nonionic surfactants, especially when using cyclodextrin, oil-soluble fragrance Is solubilized even if used as it is, the high bactericidal activity of the cationic polysaccharide is sufficiently exerted, and the taste derived from the cationic polysaccharide is masked so that the taste is not exhibited and the usability is good, and storage is also possible. The present invention has been accomplished by finding that an oral composition that is excellent in stability and can be widely used is obtained.

Therefore, the present invention is a water-soluble composition obtained by extracting an oil-soluble fragrance with a hydrous ethanol solution to an oral composition containing a cationic polysaccharide and containing no anionic or nonionic surfactant. There is provided a composition for oral cavity, which comprises blending either one or both of a fragrance and a cyclodextrin.

The present invention will be described in more detail below. The oral composition of the present invention comprises a liquid mouth freshener such as mouthwash, mouthwash, dental rinse and mouth spray, a mouthwash, and a solid mouth like troche. It is prepared as a refreshing agent, toothpaste, moisturized toothpaste, powdered toothpaste, toothpaste such as liquid toothpaste, chewing gum, oral pasta, etc., containing a cationic polysaccharide as an active ingredient and containing an oil-soluble fragrance. It contains either or both of a water-soluble flavor and a cyclodextrin obtained by extraction with a hydrous ethanol solution.

Here, as the cationic polysaccharide, chitin and chitosan obtained from crab, shrimp, squid, etc.,
Natural glycols such as ethylene glycolated chitin, ethylene glycolated chitosan, sulfated chitin, phosphorylated chitin, phosphorylated chitosan, deacetylated 50% chitin, enzyme, acid-decomposed low molecular weight chitin, chitosan and polygalactosamine. Examples include saccharides, and these can be used alone or in combination of two or more.

The amount of the cationic polysaccharide is 0.05 to 5% (% by weight, the same applies hereinafter) of the total composition, especially 0.1 to 1.
It can be%. If it is less than 0.05%, sufficient activity may not be obtained, and if it exceeds 5%, it may cause irritation in the oral cavity and may cause off-taste or off-flavor.

Next, as the oil-soluble fragrance extracted with a water-containing ethanol solution, one kind selected from fragrance components such as limonene, cineol, menthol, linalool, anethole, eugenol, menthone, carvone, methyl salicylate, cinnamic aldehyde, etc. Alternatively, two or more kinds are preferably used. It is also possible to use an essential oil containing these fragrance components.

The water-soluble flavor added to the composition of the present invention can be obtained by adding and mixing the above oil-soluble flavor to a water-containing ethanol solution, extracting the mixture, and collecting the lower layer. In this case, the mixing ratio of the water-containing ethanol and the oil-soluble flavor is 0.1 to 10 parts, particularly 0.2 to 3 parts, of the oil-soluble flavor to 1 part of water-containing ethanol (part by weight, the same applies hereinafter). If the amount is less than 0.1 part, the two may not separate well, or even if the separated lower layer is blended in the composition, unpleasant masking may not be achieved, and if it exceeds 10 parts, the lower layer obtained. Even if it is added to the composition, it may cause insoluble matter or liquid separation.

Further, in the hydrous ethanol, the weight ratio of ethanol to water is preferably 8: 2 to 2: 8, particularly 6: 4 to 4: 6, and the ethanol concentration is high. When the soluble fragrance is mixed, it does not separate into two layers, and if it is blended, the storage stability may be poor or masking of off taste may not be achieved. Also, if the ethanol concentration is low and it is out of the above range, storage Although the stability is good, it may not be possible to improve the off taste.

The amount of the above-mentioned water-soluble fragrance is preferably 0.01 to 2%, especially 0.1 to 1% of the total composition, and when the amount is less than 0.01%, it becomes a cationic polysaccharide. The resulting off-taste may not be improved, and if it exceeds 2%, it may be difficult to ensure storage stability.

On the other hand, as cyclodextrin, α-
Cyclodextrin, β, γ-branched type, chemically modified type and the like can be used.

The amount of cyclodextrin blended is preferably 0.002 to 10%, particularly 0.01 to 5% of the total composition. If it is less than 0.002%, storage stability may not be improved. If it exceeds 10%, there may be a problem in terms of product cost.

In addition to the above-mentioned water-soluble fragrances, oil-soluble fragrances which are usually used can be added to the composition of the present invention within a range that does not impair the effects of the present invention. Particularly when cyclodextrin is used, the oil-soluble fragrance is used. Since it solubilizes, a conventional amount can be used.

In addition to the above-mentioned essential components, the oral composition of the present invention contains, as active ingredients, organic acids or organic acid salts such as tranexamic acid and glycyrrhizin salts, dextranase,
Amylase, protease, mutanase, lysozyme,
Enzymes such as retechenzyme, alkyl metal monofluorophosphates such as sodium monofluorophosphate, sodium fluoride, fluorides and stannous compounds such as stannous fluoride, epsilon aminocaproic acid, aluminum chlorohydroxy allantoin, dihydrocholesterol, One or more kinds of water-soluble phosphate compounds such as sodium chloride, potassium orthophosphoric acid salt and sodium salt, azulene, vitamins and the like can be blended. The compounding amount of the above-mentioned active ingredient can be a usual amount as long as the effect of the present invention is not impaired. Furthermore, the composition of the present invention can be prepared by adding a proper component depending on the dosage form as other optional component and by a usual method. For example, when preparing a mouthwash, a viscous agent, a sweetening agent, a pH adjusting agent, a preservative, a solvent, etc. are used, and as the viscous agent, sorbit, glycerin, propylene glycol, 1,3-butylene glycol, One kind or two or more kinds of polyoxyethylene glycol, xylit, maltite, lactit and the like may be blended. As the sweetener, one or more of stevioside, stevia extract, rebaudioside, neohesperidyl dihydrochalcone, acesulfame, thaumatin, glycyrrhizin, glycyrrhizin monogluconide, hernandultin, perillartin, saccharin, saccharin sodium, etc., pH
As the regulator, one or more kinds of organic acids and salts thereof such as citric acid and salts thereof, phosphoric acid and salts thereof, malic acid and salts thereof, acetic acid and salts thereof, preservatives such as methylparaben, ethanol and the like. It can be produced by mixing a solvent such as water and other components and mixing them.

Further, other oral compositions can be produced by using the components depending on the kind thereof. The composition thus obtained is put into a predetermined container such as a laminated tube or a plastic tube obtained by laminating both surfaces of an aluminum foil with plastic or the like, or an aluminum tube, a bottle-shaped container, an aerosol container, etc., and used. be able to.

[0022]

EFFECTS OF THE INVENTION The oral composition of the present invention exhibits good activity of the cationic polysaccharide, and has good usability without masking the off-taste derived from the cationic polysaccharide. Moreover, it has excellent storage stability and can be widely used.

[0023]

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. All percentages are by weight.

[Experimental Example 1] The influence of the activity of the cationic polysaccharide by blending the anionic and nonionic surfactants was measured by the following method.

Measurement method A predetermined THB medium (TODD HE containing a test drug)
WITT BROTH medium: manufactured by DIFCO) A. v bacteria (Actinomyces viscosus
Add 40 μl of T14V strain and anaerobically (10% C
_{O 2, 10% H 2,} 80% N 2) in cultured at 37 ° C., to determine the degree of growth of the bacteria in turbidity by visual, determining the minimum inhibitory concentration by the dilution factor (MIC).

A water-soluble salt of a cationic polysaccharide (chitosan) was used as a standard, and the antibacterial activity of each of the following solution formulations was evaluated.

Solution formulation Cationic polysaccharide (chitosan) 0.01% Surfactant shown in Table 1 1.0 Water balance 100.0%

[0028]

[Table 1]

From the results shown in Table 1, it can be seen that when anionic and nonionic surfactants having a soluble property which are usually used in oral compositions are blended, the activity of the cationic polysaccharide is significantly reduced. Therefore, it is difficult to achieve the purpose even if a large amount of a cationic polysaccharide is blended in order to secure the same activity as when no active agent is added, or if a small amount of an active agent that does not easily reduce the activity is used. Causes oral mucous membrane detachment and irritation in the oral cavity, and in the latter case the activity is also reduced, and the taste of the active agent itself and the taste caused by the base or cationic polysaccharide cannot be masked, resulting in poor usability. Therefore, it is very difficult to achieve both storage stability and masking of a strange taste.

[Experimental Example 2] A liquid mouth freshener having the formulation shown in Table 2 was prepared, and the antibacterial activity, masking of off taste and storage stability were observed when the cationic polysaccharide and the water-soluble flavor shown in Table 3 were used in combination. Evaluation was made according to the criteria shown in Table 4. Table 2 shows the results.

[0031]

[Table 2] * Water-soluble fragrance (lower layer of oil-soluble fragrance extracted with hydrous ethanol solution in the table below)

[0032]

[Table 3]

[0033]

[Table 4] * Weighed average is calculated by a 5-point evaluation method by 10 professional panels

From the results shown in Table 2, when the water-soluble fragrance obtained by extracting the oil-soluble fragrance with water-containing ethanol was added to the composition for oral cavity containing the cationic polysaccharide, the antibacterial activity effect could be improved and the water-solubility was further improved. It was found that when the fragrance was extracted with a water-containing ethanol solution in which the weight ratio of ethanol and water was 8: 2 to 2: 8, not only antibacterial activity but also masking of foreign taste and improvement of storage stability could be achieved. It was

[Experimental Example 3] A liquid mouth cooling agent having the formulation shown in Table 5 was prepared, and antibacterial activity, masking of off taste, and storage stability when the cationic polysaccharide and α-cyclodextrin were used in combination were shown in Table 4 above. It evaluated by the standard of. The results are shown in Table 5.

[0036]

[Table 5] ** The same formulation as the oil-soluble flavor used for extraction of the water-soluble flavor in Table 3 above was used.

From the results in Table 5, when α-cyclodextrin was added to the oral composition containing a cationic polysaccharide, the oil-soluble flavor was solubilized without adding a surfactant having a soluble property, which was high. It was found that in addition to having antibacterial activity, the taste is masked and the storage stability can be improved.

[Experimental Example 4] An antibacterial effect was obtained when a liquid mouth freshener having the formulation shown in Table 6 was prepared, and a cationic polysaccharide and an oil-soluble flavor were extracted with water-containing ethanol and a water-soluble flavor and α-cyclodextrin were used in combination. The activity, masking of off taste, and storage stability were evaluated according to the criteria shown in Table 4 above. The results are shown in Table 6.

[0039]

[Table 6] *** Water-soluble fragrance (lower layer part where oil-soluble fragrance was extracted with the following hydrous ethanol) ** The same formulation as the oil-soluble flavor used for the water-soluble flavor of Table 3 was used.

From the results shown in Table 6, the antibacterial activity was obtained by adding both the water-soluble fragrance and cyclodextrin to an oral composition containing a cationic polysaccharide and containing no active agent having a solubilizing ability. It was clarified that masking of an unpleasant taste and ensuring of storage stability can be achieved without decreasing the value.

Example 1 Dental phosphorus chitosan lactate 0.5 triclosan 0.005 xylit 15.0 thaumatin 0.05 glycyrrhizin monogluconide 0.003 branched cyclodextrin 0.03 menthol 0.01 fruit flavor 0 0.005 Ethanol 5.0 Purified water Residual 100.0%

[Example 2] Mouthwash Ethylene glycolated chitosan 0.5 Sodium fluoride 0.05 Sorbit (65%) 20.0 Acesulfame 0.005 Methylparaben 0.01 β-Cyclodextrin 0.01 Water-soluble spearmint Oil * 1 0.5 Menthol 0.05 Methyl salicylate 0.005 Water-soluble spice mix oil * 2 0.05 Ethanol 15.0 Purified water Residual 100.0% * 1: Water containing spearmint oil (ethanol and water Lower part extracted with a ratio of 5: 5) * 2: Lower part extracted with hydrous ethanol (with a ratio of ethanol to water of 4: 6) with spice mix oil

Example 3 Mouthwash Phosphorylated chitosan 0.5 Tranexamic acid 0.05 Glycerin (85%) 9.0 Hernandultin 0.05 Citric acid 0.05 Sodium citrate 0.3 Water-soluble peppermint oil * 0.5 Menthol 0.01 Ethanol 15.0 Purified water Residual total 100.0% *: Lower part of peppermint oil extracted in hydrous ethanol (ratio of ethanol to water is 6: 4)

Example 4 Oral Coolant (Liquid) Chitosan Lactate 0.2 Triclosan 0.005 Glycerin (85%) 15.0 Hernandultin 0.05 Perillartine 0.05 Vitamin C 0.003 Modified Cyclo Dextrin 0.03 Menthol 0.20 Water-soluble fruit flavor * 0.5 Anethole 0.003 Ethanol 50.0 Purified water Residual 100.0% *: Water containing fruit flavor oil Ethanol (ratio of ethanol to water is 7: 3). Lower part extracted by Nomono)

[Example 5] troche gum arabic 7.0 glucose 80.0 gelatin 4.0 ethylene glycolated chitosan 0.5 lysozyme chloride 0.05 citric acid 0.05 sodium acetate 5.0 water-soluble strawberry oil * 1 0.0 Purified water Residual 100.0% *: Lower part of strawberry oil extracted with hydrous ethanol (ratio of ethanol and water is 7: 3)

[Example 6] Toothpaste Sulfated esterified chitin 0.05 Triclosan 0.005 Sodium fluoride 0.005 Calcium carbonate 50.0 Carrageenan 0.6 Carboxymethyl cellulose sodium 0.5 Glycerin (85%) 20.0 Vitamin E 0.003 Sodium chloride 0.5 Menthol 0.50 Water-soluble crude oil * 0.50 Anethole 0.1 Pepper flavor 0.001 Spiranthol 0.003 Purified water Residual 100.0% *: Ethanol containing hydrous crude oil Lower layer extracted with (ratio of ethanol and water is 4: 6)

[Example 7] Toothpaste Deacetylation degree 50% Chitin 0.2 Cetylpyridinium bromide 0.05 Stannous fluoride 0.005 Azulene 0.001 Dicalcium phosphate dihydrate 50.0 Carrageenan 0.8 Sodium carboxymethyl cellulose 0.6 Sorbit (60%) 25.0 Propylparaben 0.01 Menthol 0.30 Water-soluble floral flavor * 1 0.50 Water-soluble star anise flavor * 2 0.3 Peppermint oil 0. 02 γ-cyclodextrin 0.02 Purified water Residual total 100.0% * 1: Lower layer part extracted with hydrous ethanol with hydrous ethanol (ratio of ethanol and water is 4: 6) * 2: Star anise flavor Under extraction with hydrous ethanol (ethanol / water ratio of 8: 2) Part

Example 8 Liquid Toothpaste Ethylene glycolated chitosan 0.5 Triclosan 0.05 Dextranase 2000 U / g Silicic anhydride 30.0 Glycerin (85%) 35.0 Propylene glycol 5.0 Menthol 0.50 Water-soluble citrus oil * 0.50 Eucalyptus oil 0.1 Clove oil 0.002 Ethanol 2.5 Dye micro- purified water Residual amount 100.0% *: Citrus oil-containing ethanol (ratio of ethanol to water is 4: 6) Lower part extracted with

 ─────────────────────────────────────────────────── ─── Continuation of the front page (72) Inventor Kazuo Mukasa 5-2-8-405 Chuo, Kasukabe City, Saitama Prefecture (72) Inventor Takao Yokoo 1-7-1 Nadogaya, Kashiwa City, Chiba Dorf Eirakudai A-202

Claims (2)

[Claims] 1. A water-soluble fragrance and cyclodextrin obtained by extracting an oil-soluble fragrance with an aqueous ethanol solution into an oral composition containing a cationic polysaccharide and containing no anionic or nonionic surfactant. An oral composition comprising one or both of 2. The oral composition according to claim 1, wherein the water-containing ethanol solution has a weight ratio of ethanol to water of 8: 2 to 2: 8.