JP2001089344A - 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 the human bodies as active ingredients and further provide an anti-dental caries 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, an extract from guarana (Paullinia cupana) or Karin (Chaenomeles sinensis Koehne), particularly the extract from the fruits or the seeds is used as the active ingredient.

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 an extract extracted from plant fruits and seeds 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-cariogenic agent which is suitable for prevention of dental caries and periodontal disease and which is safe for the human body. However, extracts of guarana and karin, which are a kind of food additive, and especially extracts of their fruits or seeds, contain S. mut.
found that ans bacteria and S.sobrinus bacteria has the effect of significantly prevented from adhering to the teeth, was confirmed to be effective as an anti-caries agent. The present invention has been completed based on such findings.

[0005] That is, the present invention is an anti-cariogenic agent containing an extract of guarana or karin, particularly an extract of fruit or seed, 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 guarana ( Paullinia cupania ) used for the anti-cariogenic agent of the present invention is an evergreen broad-leaved tree belonging to the genus Guarana of the family Scrophulariaceae , and the quince ( Chaenomeles sinens).
is Koehne) is a deciduous tree of the genus Karin in the family Rosaceae, and a solvent extract thereof, preferably a fruit or seed solvent extract, is used as the active ingredient of the present invention. Note that these fruits may be fruits at any time regardless of whether they are mature fruits or immature fruits.

The fruit or seed 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. There is no limitation, for example, a method of immersing a fruit or seed (as is or coarse powder, finely chopped) or a dried and crushed product thereof (powder, etc.) in a solvent by cold immersion, digestion, etc., while heating and stirring. Extraction and filtration are performed to obtain an extract, or 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,
It can also be used as a dried plant extract by ordinary means such as drying under reduced pressure and freeze drying.

[0011] Guarana fruit / seed extract is defined as a raw material for pharmaceuticals, such as guarana stream extract, and both guarana fruit / seed extract and karin fruit / seed extract are commercially available as food additives. It is what is being sold. Therefore, in the present invention, they can be used simply.

The anti-cariogenic agent of the present invention contains the above-mentioned extract of guarana or karin fruit or seed as an active ingredient, and is a component of various oral compositions such as foods, quasi-drugs or pharmaceuticals. By being formulated as
It can be effectively used to prevent the formation of plaque 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 gum, candy, gummy candy, chocolate, juice, etc .; dentifrice (paste, liquid, powdered solid), mouth spray, etc. Pharmaceutical or quasi-drugs such as refreshing agents, chewing agents, troches, oral pasta agents, gargles, syrups; dentifrices; and oral cosmetics such as mouthwashes and mouth rinses. 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-caries agent of the present invention is determined by the type of oral composition, the effective concentration of guarana or karin extract,
It can be appropriately selected and determined in consideration of factors such as dilution in the mouth. As a suitable concentration, in the case of guarana fruit / seed extract (1 g / ml in terms of guarana dry matter), 0.5 to 10% by weight, especially 1% by weight per 100% by weight of the oral composition
-5% by weight. In the case of a karin fruit / seed extract (1 g / ml in terms of dry kalin), the range is 0.1 to 10% by weight, particularly 0.5 to 5% by weight.

The anti-cariogenic agent of the present invention is an antibacterial agent against S. mutans or S. sobrinus, or a tooth of such a bacterium, as another component, as long as the effect of the present invention is not impaired. Anti-adhesion agent to surface or anti-GT
An anti-caries agent such as an ase agent, or a component such as an anti-inflammatory agent may be combined and compounded.

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 gums, 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 (Bacteria) Adhesion Inhibition Test (a) Guarana Fruit / Seed Extract The anti-cariogenic effect of the guarana fruit / seed extract was evaluated by the plaque (fungus) adhesion suppression test described below. The plaque (bacteria) 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 is added to 3 ml of BHI medium containing 1% sucrose (sterilized test tube with a lid), and an extract of guarana seeds (containing 1 g / ml in terms of dryness of guarana component) is contained therein (hereinafter referred to as "Garana extract"). "
) Were mixed at various concentration ratios, and the test tube was incubated at 37 ° C. for 18 hours at an angle of 30 °.

The guarana extract was prepared in the following manner according to the Japanese Pharmacopoeia General Rules for Preparations and the method for producing a liquid extract. That is, Guarana seed ( Paullinia cupana Humbo
ldt seeds) 300 g was ground and cold-soaked in 500 ml of ethanol diluted twice with water for 2 days to remove leachate,
Then, 300 ml of ethanol diluted twice with water.
Was added, and the mixture was cooled for 1 day and filtered. Both leachates obtained by such an operation were concentrated under reduced pressure until the total amount reached 300 ml. 1 ml of the obtained extract was equivalent to 1 g of original guarana seed (dried product).

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 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 according to the following formula, and the plaque (bacterium) adhesion suppression effect of the guarana extract was evaluated based on the adhesion rate (%).

[0025]

(Equation 1)

The results are shown in Table 1.

As a control, guarana extract was not added to the test tube (guarana extract concentration: 0 μl / 3 ml).
Plaque (bacteria) deposition rate when subjected to the same experiment as described above, and in place of the Guarana extract as a comparative example, Toshishi (Cusc
Table 1 also shows the plaque (bacteria) adhesion rate when an experiment was performed using seeds of uta Chineniss. Lam and Cuscuta. japonica Chois) similarly extracted.

[0028]

[Table 1]

(Ii) Inhibitory effect on plaque (bacteria) adhesion to Streptococcus sobrinus bacteria The plaque (bacterium) adhesion suppression test was also performed on Streptococcus sobrinus strain 6715 (serotype g) in the same manner as in the above (i) to extract guarana. 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 guarana fruit / seed extract has a plaque (fungus) adhesion inhibitory effect and is an effective anti-carious agent.

(B) Karin fruit / seed extract
In the same manner as (i) and (ii), evaluation was performed by performing a plaque (bacteria) adhesion suppression test.

Incidentally, the karin fruit / seed extract was prepared as follows using mature karin fruits. That is, 50 L of 30 v / v% ethanol was added to 10 kg of the dried product of the matured karin fruit, mixed well, and allowed to stand at room temperature for 3 days. After natural filtration, 40 L of 30 v / v% ethanol was further added to the residue. For 2 days and filtered naturally. After the filtrates obtained by the above operations were combined and concentrated under reduced pressure at 60 ° C. or lower, ethanol was added thereto to adjust the total volume to about 10 L.
After standing at room temperature for days, diatomaceous earth filtration was performed. 1 ml of the obtained extract was equivalent to 1 g of the original Karin fruit (dried product).

[0034] (i) Streptococcus plaque against mutans bacteria (bacteria) as defined above as an adhesion inhibiting action Streptococcus mutans bacteria MT8148
Using the strain (serotype c), the plaque (bacteria) adhesion inhibitory effect of the kalin extract was evaluated in the same manner as in (a) (i) above. As a control, the experiment was carried out in the same manner as described above without adding the karin extract to the test tube (concentration of the karin extract: 0 μl / 3 ml). The experiment was performed using
Table 3 also shows the results.

[0035]

[Table 3]

(Ii) Inhibitory effect of plaque (bacteria) adhesion on Streptococcus sobrinus bacteria The plaque (fungus) adhesion suppression test was also performed on Streptococcus sobrinus strain 6715 (serotype g) in the same manner as in (i) above. -The plaque (bacteria) adhesion inhibitory effect of the seed extract was evaluated. Table 4 shows the results.

[0037]

[Table 4]

From the above results, it was found that the karin fruit extract had an effect of inhibiting plaque (fungus) adhesion similarly to the guarana fruit / seed extract, and was 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 is unless otherwise specified.
It means parts by weight.

[0039]

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.

[0041]

[0042]

[0043]

[0044]

[0045]

[0046]

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 Guarana Extract 1.00 Water Residue Total 100.00

Continuing from the front page (72) Inventor, Noriko Yoshii 3-13-35, Mitsujinaminami, Yodogawa-ku, Osaka-shi, Osaka F-term (reference) 4C083 AA072 AA111 AA112 AA122 AB222 AB292 AB322 AB472 AC012 AC022 AC072 AC102 AC122 AC132 AC302 AC312 AC432 AC442 AC472 AC582 AC642 AC692 AC782 AC862 AD092 AD212 AD222 AD272 AD302 AD352 AD392 AD432 CC41 DD12 DD15 DD21 DD22 DD23 EE32 4C088 AB12 AB53 AC04 BA09 CA03 MA57 ZA33

Claims (3)

[Claims] 1. An anti-cariogenic agent comprising an extract of guarana or karin as an active ingredient. 2. An anti-cariogenic agent comprising an extract of guarana or karin fruit or seed as an active ingredient. 3. An oral composition comprising the anti-caries agent according to claim 1 or 2.