JP2001089385A - Anti-dental caries agent - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide an anti-dental caries agent that is inexpensively available and includes the substances safe to human bodies as active ingredients and further provide an anti-teeth-decaying agent that permits not only oral compositions, for example, a mouth-washing solution, to be formulated, but also can be formulated to foods and beverages as an food additive. SOLUTION: The objective anti-dental caries agent comprises, as an active ingredient, the extracts from the dried bark of a cinnamon tree (Cinnamomum cassia Blume), or from cherry tree bark (Prunus jamasakura Siebold). An composition for oral cavity that includes the anti-dental caries agent is provided.

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-carious agent containing an extract extracted from the bark of a plant 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. 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 blended into an oral composition such as a mouthwash or a dentifrice, and which can be blended into food or drink as a food additive. It is to provide. 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-caries agent which is suitable for prevention of caries and periodontal disease and which is safe for the human body. However, it has been found that extracts of cauliflower and spruce , which are a kind of food additive, have an effect of significantly preventing S. mutans and S. sobrinus from adhering to teeth, and are effective as an anti-cariogenic agent. Confirmed that there is. The present invention has been completed based on such findings.

That is, the present invention is an anti-cariogenic agent containing an extract of plant bark such as cinnamon or spruce 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 The cinnamon (cinnamon bark) used as an active ingredient of the anti-cariogenic agent of the present invention is a member of the camphor family, Camphor Tree
Cinnamomum ccassia Blume, a bark peeled off from a branch of a closely related plant, and spruce (cherry bark) is a bark of Prunus jamasakura Siebold of the genus Rosaceae, or a closely related plant (Rosaceae). In the present invention, these solvent extracts are suitably used.

The bark may be subjected to an extraction operation as it is or as a crushed product, or after drying, may be subjected to an extraction operation as a pulverized powder if necessary.

Examples of the extraction solvent include water, lower alcohols having 1 to 4 carbon atoms such as methanol, ethanol, propanol and butanol; lower alkyl esters such as ethyl acetate; ethylene glycol, butylene glycol, propylene glycol, glycerin and the like. Other known organic solvents such as glycols; other polar solvents such as ethyl ether, acetone and acetic acid; hydrocarbons such as benzene and hexane; and nonpolar solvents such as ethers such as ether and petroleum ether. 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, an appropriate amount of water can be added to an organic solvent as needed to be used as a water-containing organic solvent. In the present invention, preferably,
Alcohols such as ethanol or aqueous alcohol solutions such as 20 to 40% by weight aqueous ethanol solution can be used.

As an extraction method, a generally used method can be adopted. Although there is no limitation, for example, a method of immersing bark (as is or coarse powder, finely chopped material) or a dried and crushed product thereof (powder, etc.) in a solvent by cold immersion, digestion, etc. And a method of obtaining an extract by filtration and percolation. The obtained extract may be used after removal of solids by filtration or centrifugation as necessary, depending on the mode of use, or may be used as it is, or may be partially concentrated or dried by evaporating the solvent. . 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, a fraction having glucosyltransferase inhibitory activity can be obtained and purified from the extract using a conventional purification method, for example, a countercurrent distribution method or liquid chromatography, and used. Further, in the present invention, for example,
The solvent extract obtained as described above can also be used as a dried plant extract by ordinary means such as drying under reduced pressure and freeze drying.

[0011] Both cinnamon and spruce extracts are used as pharmaceutical raw materials such as extracts and liquid extracts.
It is also commercially sold as a food additive. Therefore, in the present invention, they can be used simply.

The anti-caries agent of the present invention contains the above extract of calyx or spruce as an active ingredient,
By being blended as a component of various oral compositions such as foods, quasi-drugs, and pharmaceuticals, it can be effectively used to prevent plaque formation in the oral cavity. Here, the oral composition includes both those that are taken orally, such as food and drink, and those that are used in the oral cavity, 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.

[0014] These forms and dosage forms are not particularly limited, and can be arbitrarily determined according to the type.

The application concentration of the anti-carious agent of the present invention depends on the type of the oral composition, the effective concentration of the extract of cinnamon or spruce,
It can be appropriately selected and determined in consideration of factors such as dilution in the mouth. As a preferable concentration, in the case of a cinnamon extract (1 g / ml in terms of dried cinnamon), the oral composition 10
The range is 0.3 to 10% by weight, particularly 0.5 to 5% by weight per 0% by weight. In the case of spruce extract (1 g / ml in terms of dried spruce), 0.5 to 10
% By weight, in particular from 1 to 5% by weight.

The anti-cariogenic agent of the present invention is known or may be known in the future as an antibacterial agent against S. mutans or S. sobrinus , as long as the effects of the present invention are not impaired. Anti-adhesion agent to surface or anti-GTas
It can also be compounded in combination with components such as anti-caries agents such as e-agents or anti-inflammatory agents.

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, abrasives such as dibasic calcium phosphate, calcium carbonate, insoluble sodium metaphosphate, amorphous silica and aluminum oxide; 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.

[0020]

The present invention will be described in more detail with reference to the following Test Examples and Examples, which should not be construed as limiting the present invention. Test Example (1) Plaque (Bacterial) Adhesion Inhibition Test (a) Caulis Extract The anti-cariogenic effect of the caulis extract was evaluated by the plaque (fungus) adhesion inhibition test described below. In addition, plaque (fungus)
The adhesion test was performed using a glass test tube instead of the tooth surface.

[0021] The (i) Streptococcus mutans plaque against bacteria (bacteria) adhesion prevention effect First, overnight cultures 30μl of Streptococcus mutans bacteria MT8148 strain brain heart infusion liquid medium containing (serotype c) (BHI medium) It was added to 3 ml of BHI medium containing 1% sucrose (sterilized test tube with a lid), and the bark extract of cinnamon bark (containing 1 g / ml in terms of cinnamon component dry matter) was added thereto. "
) Were mixed at various concentration ratios, and the test tube was incubated at 37 ° C. for 18 hours at an angle of 30 °.

The extract of caffeine extract was prepared according to the method of Japanese Pharmacopoeia, General Rules for Pharmaceutical Preparations and General Extract, using 10 kg of finely cut pieces of Caffeine of the Japanese Pharmacopoeia as raw materials and a 30% aqueous ethanol solution as a leaching agent. It was prepared as follows. That is, 10 kg of fine pieces of Japanese Pharmacopoeia "Keihi" were
(0% ethanol aqueous solution), and allowed to stand at room temperature for 2 days in a sealed state. This is densely packed in a leaching device, and after opening the lower opening of the leaching device, a second leaching agent (30% aqueous ethanol solution) is gradually added from the top until the cabbage is covered.
When the leachate began to drip, the lower mouth was closed and sealed, allowed to stand at room temperature for 2 to 3 days, and the leachate was allowed to flow out at a rate of 0.5 to 1 mL per minute. The first obtained 8.5 L was separately stored as a first leachate, and a second leachate was further added to the leachate to continue the outflow to obtain a second leachate. The second leachate is then concentrated and combined with the first leachate, and the second leachate is added to
After standing for 2 days as L, the supernatant was taken. 1 ml of the obtained extract corresponded to 1 g of original cinnamon (dry matter).

Next, 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). 3 ml of the above-mentioned 1% sucrose-containing BHI medium is placed in an empty test tube having plaque (fungi) adhered to the inside surface of the test tube, and the mixture is stirred with a vortex mixer to attach plaque (fungus) on the inside surface of the test tube. A part of the kimono was washed and eluted, and the culture solution containing the plaque (bacteria) eluate was decanted into an empty 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 plaque (fungi) that can be taken with a mouth rinse, and sample 3 reflects plaque (fungi) that cannot be taken with a mouth rinse.

Further, the amount of cells 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 according to the following equation, and the plaque (bacterium) adhesion suppression effect of the caffeine extract was evaluated based on the adhesion rate (%).

[0025]

(Equation 1)

The results are shown in Table 1.

As a control, do not add the caffeine extract to the test tube (concentration of caffeine extract: 0 μl / 3 ml).
The plaque (bacteria) adhesion rate when the experiment was performed in the same manner as above, and as a comparative example, Eucalyptus ( Eu
Table 1 also shows the plaque (bacteria) adhesion rate when the same experiment was performed using the bark of cammia ulmoides Oliver).

[0028]

[Table 1]

(Ii) Inhibitory effect on plaque (bacteria) adhesion to Streptococcus sobrinus bacteria The plaque (bacteria) adhesion inhibition test was also performed on Streptococcus sobrinus strain 6715 (serotype g) in the same manner as in (i) above, and Cahi extract was extracted. The plaque (bacteria) adhesion inhibitory action of the product was evaluated. Table 2 shows the results.

[0030]

[Table 2]

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

(B) Spruce extract The anticariogenic effect of the spruce extract was determined by the above (a) (i) and (ii)
In the same manner as described above, evaluation was performed by performing a plaque (fungus) adhesion suppression test. The spruce extract was prepared as follows using cherry bark. That is, the crude powder of spruce (Rosaceae plant, Prunus jamasakura siebold., Peeled and dried) was mixed with ordinary water, soaked in water for 3 days with occasional stirring, and filtered, and the resulting filtrate was carbonated lime. (1%) was added, and the mixture was left for 3 days while stirring well. Ethanol was added to the filtrate obtained by filtering this to adjust the alcohol concentration of the final preparation to 25% to prepare a spruce extract. 1 ml of the obtained extract corresponded to 1 g of raw spruce (dry matter).

(I) an inhibitory effect on plaque (fungus) adhesion to Streptococcus mutans bacteria, and (ii) a Streptococcus sobri.
Tables 3 and 4 show the results showing the plaque (bacteria) adhesion inhibitory effect on the Nus bacteria, respectively.

[0034]

[Table 3]

[0035]

[Table 4]

From the above results, it was found that the spruce extract has an effect of inhibiting plaque (bacteria) adhesion and is an effective anti-carious agent. Examples Hereinafter, application examples of the anti-caries agent of the present invention will be described as examples. The unit of each prescription means part by weight unless otherwise specified.

[0037]

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.

[0039]

[0040]

[0041]

[0042]

[0043]

[0044]

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 Fragrance 0.25 Caffeine Extract 0.50 Water Residue Total 100.00

Continuation of the front page (72) Inventor Noriyoshi Yoshii 3-13-35, Mitsujinaminami, Yodogawa-ku, Osaka-shi, Osaka F-term (reference) 4C083 AA072 AA111 AA112 AA122 AB222 AB282 AB292 AB322 AB472 AC012 AC022 AC072 AC102 AC122 AC132 AC242 AC302 AC312 AC402 AC432 AC442 AC482 AC542 AC582 AC692 AC782 AC862 AD212 AD222 AD272 AD302 AD352 AD412 CC41 DD12 DD15 DD22 DD23 DD27 EE32 4C088 AB33 AB52 AC06 BA08 BA09 BA10 NA14 ZA67

Claims (2)

[Claims] 1. An anti-cariogenic agent comprising an extract of cinnamon or spruce as an active ingredient. 2. An oral composition comprising the anti-cariogenic agent according to claim 1.