JP2002104983A - Anticariogenic agent - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide an anticariogenic agent containing a material which is available at a low cost and safe for the human body as an active ingredient, and to provide an oral cavity composition containing as an active ingredient such a material that can be added safely not only to the oral cavity composition, e.g. a mouthwash, but also to food and drink as a food additive. SOLUTION: This anticariogenic agent contains at least one kind of extract selected from an extract of Sanguisorba officinalis, an extract of Betula platyphylla var. japonica, and an extract of Tilia japonica as an active ingredient. The oral cavity composition contains the anticariogenic agent.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an anti-carious agent. More specifically, the present invention relates to an anti-cariogenic agent containing a specific plant extract as an active ingredient.

[0002]

2. Description of the Related Art Caries are generally called caries, and the causes thereof are considered as follows. Naturally, certain kinds of bacteria are adsorbed on teeth due to the interaction between the glycoprotein, which is a component in saliva, and the cell surface substance of bacteria resident in the oral cavity. This bacterium is a glucosyltransferase (hereinafter referred to as "G"), which is an enzyme secreted outside the cells.
Tase ”. ), Food-derived sucrose is denatured into a sticky polysaccharide, and adheres more firmly to the tooth surface. This is generally called plaque, and the attached bacteria metabolize sugars in the plaque and generate an acid as a metabolite thereof.
The acid demineralizes the enamel surface of the tooth and promotes dental caries. It is said that plaque causes not only caries, but also bad breath, and depending on its progress, periodontal disease, gingivitis, and even alveolar pyorrhea.

[0003]

An object of the present invention is to provide an anti-cariogenic agent which is available at a low cost and contains a substance which is safe for the human body as an active ingredient. Further, a second object of the present invention is to provide an anti-cariogenic agent comprising, as an active ingredient, a substance which can be safely compounded in oral compositions such as mouthwashes and dentifrices, and which can also be compounded in foods and drinks. It is to be.
A third object of the present invention is to provide an anti-cariogenic agent which is useful for preventing oral diseases such as bad breath, periodontal disease, gingivitis and alveolar pyorrhea by suppressing the formation of plaque. It is.

[0004]

SUMMARY OF THE INVENTION In view of the above circumstances, the present inventor has conducted intensive studies day and night in search of an anti-cariogenic agent which is suitable for prevention of dental caries and periodontal disease and which is safe for the human body. However, it has been found that extracts of specific plants such as Warmoko , birch and linden have a significant effect of preventing S. mutans and S. sobrinus from adhering to teeth. It was confirmed that it was effective as an agent. The present invention has been completed based on such findings.

[0005] That is, the present invention relates to at least one selected from the group consisting of Warmoko, Birch and Linden.
It is an anti-cariogenic agent containing an extract of a plant of the species as an active ingredient.

The present invention is also an oral composition (including food and drink) containing the above-mentioned anti-carious agent.

[0007]

BEST MODE FOR CARRYING OUT THE INVENTION In the present invention, as an active ingredient having an anti-cariogenic effect, a whole plant or a part thereof (e.g., root, rhizome,
Solvent extracts of stems, leaves, fruits (seed), flower buds, bark, bugs, xylem, heartwood, etc.) are used. The plant part used for extraction is not particularly limited as long as it is the whole plant or a part thereof. The whole plant of the plant or a part thereof may be subjected to an extraction operation as it is or as a crushed product, and after drying,
If necessary, it may be subjected to an extraction operation as a pulverized powder.

[0008] In the present invention, Warmoko used as a raw material plant of the extract is a plant belonging to the genus Rosaceae (Rosaceae), belonging to the genus Sanguisorba L., and specific examples include the scientific name: Sanguisorba officinalis Linne. . Similarly, as a plant belonging to the genus Waremoko, a long-spotted moth ( Sanguisorba tenuifolia Fisc
h. var. alba Trautv. et Mey), callite ( Sangu )
isorba hakusanensis Makino).
The root of the plant has been conventionally used as a Chinese medicine to stop hemoptysis and hemoptysis.

[0009] Birch is a plant belonging to the birch family (Betulaceae), birch genus ( Betula L.). Specifically, birch ( Betula alba L. or Betula platyphyl)
la Sukatchev var. japonica Hara). Similarly, birch birch ( Betula ernmani Cham.) And Udai birch ( Betu
la maximowicziana Regel), Betula ( Betula c)
orylifolia Regel etMaxim.) and Betula grossa Sieb. et Zucc.

The linden is a plant belonging to the genus Tiliaceae ( Tilia L.), and specifically, linden ( Tilia cordata Mill. Or Tilia japonica Si).
mk.). Similarly, as a plant belonging to the genus linden, bollige ( Tilia miqueliana Maxi
m.), Hera ( Tilia kiusiana Makino et Shirasaw
a), Psyllium japonicus ( Tilia maximowicziana Shirasa
wa).

The solvent used in the above extraction is not particularly limited, and lower alcohols, polyhydric alcohols, non-polar solvents and polar solvents can be widely used. More specifically, lower alcohols include alcohols having 1 to 4 carbon atoms such as methanol, ethanol, propanol and isopropyl alcohol, butanol; polyhydric alcohols such as glycerin and polyethylene glycol; non-polar solvents such as pentane; Saturated hydrocarbons such as hexane, heptane, octane, nonane and decane and unsaturated hydrocarbons such as hexene and heptene; water, acetone, ethyl acetate, methyl acetate and the like are used as polar solvents. These solvents may be used alone or in combination of two or more. For example, in the case of a raw material having a high fat content, after a defatting extraction treatment with a non-polar solvent, an extraction treatment may be carried out with various arbitrary solvents, or an extraction treatment using a water-containing organic solvent may be carried out.

As an extraction method, a generally used method can be adopted. Although there is no limitation, for example, a method of immersing whole or part of the plant (as is or coarse powder, finely chopped material) or dried and crushed material (powder, etc.) in a solvent by cold immersion, hot immersion, etc., heating and stirring Extraction and filtration are performed to obtain an extract, or percolation.

The obtained extract is subjected to filtration or centrifugation, if necessary, to remove solids, and then, depending on the mode of use, may be used as it is or may be partially concentrated or dried by distilling off the solvent. May be used. After concentration or drying, the concentrated or dried product may be washed with an insoluble solvent and purified for use, or it may be further dissolved or suspended in a suitable solvent for use. In addition, the extract can be used by obtaining and purifying a fraction having an antioxidant activity and an active oxygen scavenging activity using a conventional purification method, for example, a countercurrent distribution method or liquid chromatography. It is. Furthermore, in the present invention, for example, the solvent extract obtained as described above can be used as a dried plant extract by ordinary means such as drying under reduced pressure and freeze drying.

The anti-caries agent of the present invention contains the above-mentioned plant extract as an active ingredient, and is formulated as an ingredient of various oral compositions such as foods, quasi-drugs, and pharmaceuticals. It prevents plaque formation in the oral cavity and can be effectively used as an anti-carious agent. The blending amount of the plant extract contained in the anti-carious agent can be appropriately changed according to its use and application target, and is not particularly limited. Further, the plant extract itself can be used as it is as an anti-carious agent.

The oral composition includes both those which are taken orally, such as food and drink, and those used in the mouth, such as toothpaste and mouthwash.

Specific examples of the oral composition include various foods such as troches, chewing gums, candy, gummy candy, chocolate, juice, etc .; dentifrice (paste, liquid, powder solid), mouth spray such as mouse spray, etc. Pharmaceutical or quasi-drugs such as fresheners, chewing agents, lozenges, oral pasta, gargles, syrups; dentifrices
Oral cosmetics such as mouthwash and mouth rinse can be mentioned. Preferably, foods such as troches, chewing gums and candy, and mouthwashes such as dentifrices, mouthwashes and mouth rinses can be mentioned.

These forms and dosage forms are not particularly limited, and can be arbitrarily determined according to the type.

The concentration of the anti-caries agent of the present invention depends on the type of the oral composition, the ratio of the active ingredient contained in the plant extract,
It can be appropriately selected and determined in consideration of various factors such as dilution in the mouth. Although not particularly limited, the specific compounding ratio of the anti-cariogenic agent mixed per 100% by weight of the oral composition is as follows:
/ Ml), which is usually 0.0
1 to 10% by weight, preferably 0.05 to 5% by weight or more; for birch, usually 0.01 to 10% by weight, preferably 0.05 to 5% by weight or more; Is usually 0.01 to 10% by weight, preferably 0.1 to 10% by weight.
It is at least 0.5 to 5% by weight.

The anti-caries agent of the present invention may contain the above-mentioned plant extract alone as an active ingredient, or may contain both of them.

The anti-cariogenic agent of the present invention is, as long as it does not interfere with the effects of the present invention, known or may be known in the future as an antibacterial agent against S. mutans or S. sobrinus , and the teeth of these bacteria. Anti-adhesive agent or GTase on the surface
An anti-caries agent such as an inhibitor, or a component such as an anti-inflammatory agent may be used in combination.

The anti-caries agent of the present invention can be used in combination with a component usually blended in the oral composition, depending on the type of the oral composition to be applied.

For example, in the case of toothpaste, an abrasive such as dibasic calcium phosphate, calcium carbonate, insoluble sodium metaphosphate, amorphous silica, aluminum oxide, etc .; carboxymethylcellulose, hydroxyethylcellulose, alginate, carrageenan, gum arabic, polyvinyl alcohol, etc. Binders such as polyethylene glycol, sorbitol, glycerin, propylene glycol;
Sodium lauryl sulfate, sodium dodecylbenzene sulfonate, hydrogenated coconut fatty acid sodium monoglyceride monosulfate, sodium lauryl sulfoacetate,
Foaming agents such as sodium N-lauroyl sarcosinate, N-acyl glutamate, sucrose fatty acid esters and the like can be mentioned. Further, flavoring agents such as menthol and flavoring or sweetening agents, preservatives and the like which are usually used therefor can be used. Can be blended. In the case of mouthwashes such as mouthwashes and foods such as chewing gum, conventional ingredients can be used in combination. In addition, as a sweetener combined and used, those with low or no caries are preferable, and for example, D-xylose, xylitol, saccharin sodium, aspartame, trehalose and the like can be suitably mentioned.

Further, the anti-caries agent of the present invention includes lysozyme chloride, lytic enzyme, dextranase, mutanase, chlorhexidine, sorbic acid, alexidine, hinokitiol, cetylpyridinium, alkylglycine, alkyldiaminoethylglycine salt, monofluorophosphate Sodium, sodium fluoride, stannous fluoride, water-soluble primary or secondary phosphate, quaternary ammonium compound,
It can be used in combination with components such as sodium chloride.

[0024]

EXAMPLES Hereinafter, the present invention will be described in more detail with reference to Production Examples, Test Examples and Examples, but the present invention is not limited to these Examples. <Production Example> Production Example 1 100 L of 90 vol% ethanol was added to 10 kg of roots and rhizomes of Warm Mob ( Sanguisorba officinalis Linne), and 5
After heat extraction for a period of time, the mixture is filtered. The filtration residue is further extracted in the same manner using 90 vol% ethanol (twice), and all the extracts are combined and concentrated under reduced pressure to about 1/10 volume. After leaving this to stand in a cool place for 7 days, it is filtered, and ethanol and purified water are added to the obtained filtrate to obtain an extract (50 kg) having an ethanol concentration of 50%. Hereinafter, this will be referred to as "Walmoko extract".

Production Example 2 90 vol. Per 10 kg of bark of birch ( Betula alba L.)
% Ethanol and immersed at room temperature for 7 days,
Filter. The filtration residue is further extracted using 90 vol% ethanol in the same manner, and all the extracts are combined and concentrated under reduced pressure at 50 ° C. Ethanol and purified water are added thereto, and an extract (50 L) having an ethanol concentration of 50% is added. obtain. Hereinafter, this is referred to as birch extract.

Production Example 3 10 kg of leaves and flowers of linden ( Tilia cordata Mill.)
Then, 50 L of 90 vol% ethanol is added thereto, immersed at room temperature for 7 days, and then filtered. The filtration residue is further subjected to 90 vo
Extract with 1% ethanol and combine all extracts to 5
The mixture was concentrated under reduced pressure at 0 ° C., and ethanol and purified water were added thereto to obtain an extract (50 L) having an ethanol concentration of 50%.
Hereinafter, this is referred to as linden extract.

<Test Example> Plaque (bacteria) adhesion inhibition test was carried out for the extract of Waremokou, birch extract and linden extract prepared in the above production example, and the respective plaque (fungus) adhesion inhibition effects were examined. did.

[0028] Test Example 1 Anti-caries effect of burnet extract burnet extract, plaque (bacteria) suppressing adhesion test described below (Streptococcus mutans bacteria and Str
Inhibitory effect of plaque (fungus) on eptococcus sobrinus bacteria Streptococcus mutans and Streptococcus sobrinu
was assessed by plaque (bacteria) adhering inhibition test) for the s-bacteria. The plaque (bacteria) adhesion test was performed using a glass test tube instead of the tooth surface.

First, MT8 of Streptococcus mutans
148 strains (serotype c ) or Streptococcus sobrinus
Overnight culture 3 of brain heart infusion liquid medium (BHI medium) containing strain 6715 (serotype g )
0 μl was added to 3 ml of BHI medium containing 1% sucrose (sterilized test tube with a lid), into which the extract of Waremokou (0.2 g / m in terms of dryness of Waremokou plant (root, rhizome) on a dry basis) was added.
The mixture was mixed at various concentrations (0-200 μl / 3 ml), and the test tube was inclined at 30 ° and incubated at 37 ° C. for 18 hours.

After culturing for 18 hours, the test tube was slowly rotated three times while keeping the angle of 30 °, and the culture solution was slowly decanted into an empty test tube (sample 1). Place the above 1 in an empty test tube with the plaque (fungus) attached to the inner surface of the test tube
3 ml of BHI medium containing 3% sucrose was added, and the mixture was stirred with a vortex mixer to wash and elute a part of the plaque (bacteria) deposit on the inner surface of the test tube. Was decanted into a test tube (sample 2). Then, 3 ml of 1% sucrose-containing BHI medium was again added to the obtained plaque (bacteria) attached test tube, the plaque (bacteria) firmly adhered to the inner surface of the test tube was scraped off with a spatula, and the solution was sampled. It was set to 3. Note that, of the above operations, the vortex stirring operation is based on the assumption that the mouth is rinsed. That is, Sample 2 reflects the amount of plaque (bacterium) that can be obtained by rinsing the mouth, and Sample 3 reflects the amount of plaque (bacterium) that cannot be obtained by rinsing the mouth.

Further, the amount of plaque (bacteria) contained in each sample solution was determined by measuring the turbidity (OD: absorbance 550 nm) of the solution. Next, the plaque (bacteria) adhesion rate was determined from the turbidity of the solution by the following formula, and the plaque (bacterium) adhesion-suppressing action of the Waremokou extract was evaluated based on the adhesion rate (%).

[0032]

(Equation 1)

The results are shown in Table 1.

[0034]

[Table 1]

From the above results, it was found that the extract of Waremokou had a significantly excellent plaque (bacteria) adhesion inhibitory action and was an effective anti-carious agent.

Test Example 2 Birch extract The anti-cariogenic effect of the birch extract was evaluated by performing a plaque (bacteria) adhesion inhibition test in the same manner as in Test Example 1 described above. In addition, 1 ml of the used birch extract was equivalent to 0.2 g of the bark (dry matter) of the original plant.

Table 2 shows the results showing the plaque (fungus) adhesion inhibitory effect on Streptococcus mutans bacteria and the plaque (fungus) adhesion inhibitory effect on Streptococcus sobrinus bacteria, respectively.

[0038]

[Table 2]

From the above results, it was found that the birch extract has an effect of inhibiting plaque (bacteria) adhesion and is an effective anti-carious agent.

Test Example 3 Lindwood extract The anti-cariogenic effect of the Lindwood extract was evaluated by performing a plaque (bacteria) adhesion inhibition test in the same manner as in Test Example 1. In addition, 1 ml of the used linden extract was used for the leaves of the original plant.
It was equivalent to 0.2 g of flower (dried product).

Table 3 shows the results showing the plaque (fungus) adhesion inhibitory effect on Streptococcus mutans bacteria and the plaque (fungus) adhesion inhibitory effect on Streptococcus sobrinus bacteria, respectively.

[0042]

[Table 3]

From the above results, it was found that the linden extract has a plaque (bacterium) adhesion inhibitory action and is an effective anti-carious agent.

<Examples> Examples of application of the anti-caries agent of the present invention will be described below as examples. The unit of each prescription means part by weight unless otherwise specified.

[0045]

Example 3 Sugar-Coated Tablet A mouthwash was prepared by coating 200 parts by weight of a tablet portion with 130 parts by weight of a sugar-coated portion.

[0047]

[0048]

[0049]

[0050]

[0051]

[0052]

[0053]

Example 10 Oral Pasta Liquid Paraffin 13.00 Cetanol 10.00 Glycerin 25.00 Sorbitan Monopalmitate 0.60 Polyoxyethylene Sorbitan Monostearate 5.00 Sodium Lauryl Sulfate 0.10 Benzotonium Chloride 0.10 Methyl Salicylate 0.10 Saccharin 0.20 Flavor 0.25 Waremokou Extract (Concentration 20) %) 1.00 water The remaining balance is 100.00.

In the above Examples 1 to 10, birch extract (concentration 20%) was used instead of Waremokou extract (concentration 20%).
Alternatively, each formulation was similarly prepared using linden extract (20% concentration).

[0056]

[0057]

[0058]

──────────────────────────────────────────────────の Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (reference) // A23G 3/00 101 A23G 3/00 101 109 109 3/30 3/30 F term (reference) 4B014 GB08 GB13 GG18 GK12 4B018 MD61 ME09 MF01 4C083 AA111 AA112 AA122 AB222 AB282 AC102 AC122 AC132 AC302 AC312 AC432 AC482 AC782 AC862 AD272 AD302 AD352 AD412 CC41 DD22 DD23 DD27 EE32 4C088 AB12 AB25 AB51 AC01 BA08 CA03 MA52 NA14 ZA

Claims (2)

[Claims] 1. An anti-carious agent comprising as an active ingredient an extract of at least one plant selected from the group consisting of Warmoko, Birch and Linden. 2. An oral composition comprising the anti-cariogenic agent according to claim 1.