JPH0899893A - Dental carries-preventing agent - Google Patents

Abstract

PURPOSE: To obtain a dental carries-preventing agent containing an extract of leaf of Psidium java L. as an active ingredient and excellent in preventing effect on proliferation of intraoral microorganisms such as Storeptcoccus mutans which largely participate in formation of dental carries and dental plaque. CONSTITUTION: This dental carries-preventing agent contains about 0.001-5wt.% (especially preferably about 0.01-2%) of an extract obtained by adding a porous organic solvent such as water and/or methanol, acetone, glycerol of about 1.5-50 times based on weight of leaf of Psidium java L. to the leaf of Psidium Java L., allowing the organic solvent to stand or extracting the organic solvent at room temperature to boiling point of the solvent for about 5min to 24hr to carry out extract of the leaf, removing insoluble residue by centrifugal separation, filtration, squeezing, etc., and as necessary, concentrating and drying the extracted solution and having about >=1% (preferably >=3%) total polyphenol content. The preventing agent can be blended with oral cavity composition such as dentifrices, troches, mouse washes, chewing gums and oral refrigerant.

Description

Detailed Description of the Invention

[0001]

FIELD OF THE INVENTION The present invention shows an excellent inhibitory effect on the growth inhibition of oral microorganisms represented by Streptococcus mutans, which are largely involved in the formation of caries (caries). The present invention relates to an anti-cavity agent useful for preventing dental caries, which is capable of preventing the formation of plaque associated with microorganisms in the oral cavity. More specifically, the present invention relates to an excellent anti-cavity agent containing a guava leaf extract as an active ingredient. The anti-cavity agent of the present invention is an anti-cavity agent of natural plant origin, and is incorporated into oral compositions such as dentifrice, troches, mouthwashes, chewing gums, and mouth refreshers. Can be used.

[0002]

2. Description of the Related Art Caries (dental caries) is caused by oral microbes and dental plaque.
It is said that it occurs for the first time with the three conditions of food ingredients, particularly sugar, and dentin, and it is said that the percentage of caries teeth is high from the childhood due to the heavy use of sugar in recent years.

Plaque plaque is formed on the tooth surface by oral bacteria, food residues, salivary organic substances, etc., and one of the oral bacteria, Streptococcus mutans, synthesizes a dextran-like polysaccharide from sucrose. However, it is known that acid is produced from other sugars and retained in dental plaque to cause decalcification of teeth, thereby causing caries.

As a drug for preventing the formation of such plaque (hereinafter referred to as anticaries agent), persimmon leaves and / or
Or an extract obtained by extracting the seeds of kenponashi with a hydrophilic organic solvent such as methanol, alcohols such as ethanol, glycols such as ethylene glycol, and ketones such as acetone An agent for inhibiting the formation of dental plaque, which is the cause of dental caries (JP-A-2-78609).
Gazette): an oral fungus inhibitor which exhibits an excellent effect against Streptococcus mutans bacteria, which comprises a hot water extract of tea leaves such as green tea, oolong tea and black tea as an active ingredient (JP-A 1-19
(0624 gazette): An oral composition which effectively suppresses the growth of Streptococcus mutans and which effectively prevents tooth decay and periodontal disease, which contains a crude drug extract of senkyu, ages, betel nut and / or kujin ( Japanese Patent Laid-Open No. 4-
159213): Also, lemon and grapefruit-
Tung, Naple orange, Hassaku, Satsuma mandarin orange, kumquat, citrus fruit, summer mandarin orange, organic solvent of citrus fruit peel or skin-containing substance selected from daidaidai, etc., preferably extract with methanol, ethanol Tooth decay and periodontopathic bacteria growth inhibitor as a component (Japanese Patent Application Laid-Open No. 4-34693)
3) and the like have been proposed.

[0005]

However, the above-mentioned conventionally proposed anti-cavity agents are not always satisfactory in the effect of inhibiting plaque formation, and there is a demand for the development of even more excellent anti-cavity agents.

[0006]

Therefore, the present inventors have conducted research on a method for inhibiting the growth of Streptococcus mutans, which is a typical oral bacterium that is largely involved in the formation of dental plaque that causes dental caries. I went.

As a result, the water and / or hydrophilic organic solvent of guava leaves, which was not previously known to contain a substance showing an inhibitory effect on the microorganisms involved in caries formation represented by Streptococcus mutans, was found. It has been discovered that the extract obtained by the above method has an excellent inhibitory action against oral microorganisms represented by Streptococcus mutans which are largely involved in caries formation and plaque formation.

Therefore, an object of the present invention is to provide an excellent anti-cavity agent containing the extract of guava leaf as an active ingredient.

Guava (Psidium Java)
L. ) Is a shrub native to Central America that belongs to the genus Vanjirou, belonging to the genus Fusarium, and is widely grown or cultivated widely in tropical and subtropical regions such as Southeast Asia, southern China, and Hawaii, and its fruits, roots, and leaves are private herbs. It is used for diabetes and diarrhea. The guava leaves used in the present invention may be semi-dried or dried products in addition to fresh leaves, but dried products are particularly preferable. These raw materials are preferably crushed before use.

The guava leaf extract used in the present invention can be easily obtained by subjecting the above-mentioned guava leaf to an extraction treatment with water, a hydrophilic organic solvent or a mixture thereof (hereinafter referred to as an extraction solvent). Examples of the hydrophilic organic solvent that can be used in the extraction treatment include solvents such as methanol, ethanol, n-propyl alcohol, acetone, propylene glycol and glycerin. These solvents can also be used, for example, in the form of a water-containing solvent mixed with water at an arbitrary ratio.

The extraction operation and the extraction conditions can be variously changed according to the type of the extraction solvent used, but when the extraction is carried out using the hydrophilic organic solvent as described above or a mixture thereof with water as the extraction solvent. Can be carried out, for example, by adding about 1.5 to about 50 times by weight of the solvent to guava leaves and allowing the mixture to stand or stir at room temperature to the boiling point of the solvent used for about 5 minutes to about 24 hours. After performing the extraction operation in this manner, for example, by removing the insoluble residue by centrifugation, filtration, pressing or other solid-liquid separation means,
A guava leaf extract can be obtained. If necessary, an extraction solvent may be added to the insoluble solid content extraction residue, and the same operation may be repeated to perform extraction. In the present invention, the extract obtained from the guava leaves by the above method may be used as it is as the extract of the present invention,
Alternatively, a concentrate obtained by concentrating by removing the solvent from the extract, and further a dried product obtained by subjecting the concentrate to vacuum drying or freeze drying, can be used as the extract of the present invention. Further, the extract obtained by the above method may be decolorized and deodorized with an adsorbent such as silica gel, activated carbon, activated alumina, bentonite, acid clay and diatomaceous earth. The adsorption operation can be carried out by adding an appropriate amount of an adsorbent to the solution obtained by dissolving the extracted extract as it is or by concentrating the extracted extract in a suitable solvent such as water, and performing an adsorption treatment. The adsorption treatment liquid is
A concentrated liquid obtained by concentrating as it is or under reduced pressure, and a dried product obtained by further drying it, for example, under reduced pressure or freeze-drying can also be used as an extract. Furthermore, the above-mentioned extracted extract before or after decolorization or deodorization is dissolved in, for example, an appropriate amount of water, and is effective by using a synthetic adsorbent having, for example, styrene / divinylbenzene or methacrylic acid ester as a resin matrix. The components are adsorbed, purified by desorption with a hydrophilic organic solvent such as ethanol, methanol, acetone, ethyl acetate or a mixed solvent of these with water, and then purified in a guava leaf extract. The components can be concentrated and used as the extract of the present invention. The adsorption / desorption operation can be performed by a batch system or a column system, and preferably the column system is adopted. The desorbed liquid after the operation can be used as it is as the extract of the present invention, but it is also a concentrated liquid obtained by concentrating under reduced pressure, and a dried product obtained by subjecting it to, for example, vacuum drying or freeze drying. Can also be used as the extract of the present invention.

In the case of extracting from guava leaves with water, for example, guava, raw leaves, semi-dried products, dried products or crushed products are used as raw materials, and the raw materials are, for example, about 10 to about 100. Add double weight of water, for example 50 ~ 80 ℃
Extraction can be performed at a temperature of about 1 to 5 hours with stirring. Then, the extract of the present invention can be obtained by performing centrifugal separation, filtration treatment and the like, and preferably concentrating and drying the filtrate under reduced pressure.

The extract of guava leaves prepared as described above has sufficient effect as an anticaries agent if the content of total polyphenol in the extract is at least about 1%. Demonstrate, but preferably about 3%
The above is good.

Examples of the oral composition in which the guava leaf extract according to the present invention can be incorporated as an anti-cavity agent include, for example, toothpaste, powdered toothpaste, troches, mouthwashes, solid mouth-cooling agents and chewing gum. , Coating agents and the like.

The ratio of the anti-cavity agent comprising the guava leaf extract of the present invention to the oral cavity composition for preventing dental caries as described above varies depending on the kind of the composition and the like, but generally, for example, in the oral composition. On the other hand, the guava leaf extract is contained in an amount of about 0.001% to about 5% by weight, particularly preferably about 0.
It can be blended within the range of 01 to about 2% by weight. The guava leaf extract according to the present invention can be blended with other raw materials to be blended in a usual oral composition without any restriction.

Hereinafter, several embodiments of the present invention will be described more specifically by way of examples.

[0017]

【Example】

Example 1 10% 70% aqueous ethanol solution was added to 150 g of guava ground product.
50 g was added, and the mixture was stirred at 60 ° to 70 ° C. for 2 hours for extraction treatment, centrifuged, and filtered to obtain 900 g of a filtrate. To this filtrate was added 9 g of activated carbon, and the mixture was stirred at room temperature for 20 minutes and filtered with a paper filter to obtain 780 g of a filtrate. The filtrate was concentrated to dryness under reduced pressure to obtain 25 g of a dry extract. To 10 g of this extract was added 500 g of water to dissolve it, and this solution was passed through a column packed with a commercially available SP-207 resin (manufactured by Mitsubishi Kasei) (SV = 2) for adsorption treatment. Next, desorption treatment was sequentially performed with 400 g of 95% ethano-water solution at a speed of SV = 1. The obtained desorption treatment solution was concentrated under reduced pressure and further under reduced pressure (5 to 10 mmHg, 70 ° C., 1
After evaporating to dryness for 6 hours, 6.1 g of a dry extract was obtained. The total polyphenol content of this extract was 59%.

Example 2 1500 g of water was added to 150 g of guava leaf ground product, and 60 to 7 was added.
The mixture was stirred at 0 ° C. for 2 hours, extracted, subjected to centrifugation and filtration to obtain 1200 g of a filtrate. The filtrate was concentrated to dryness under reduced pressure to obtain 20 g of dried extract. The total polyphenol content of this extract was 22%.

Test Example 1 Each of the extracted extracts obtained in Examples 1 and 2 and commercially available polyphenon 60 (manufactured by Mitsui Norin; green tea extract, polyphenol content 60%) was contained at a predetermined concentration.
-TGC medium (tryptone, soypeptone, glucose,
Sodium chloride, sodium thioglycolate, L-cystine, sodium sulfite, agar) 20 ml, Streptococcus mutans (Streptcocc
us mutans) IID973 strain × 10 ⁴ CFU
/ Ml. Culturing at 37 ° C., and Streptococcus mutans I of these were chronologically analyzed.
The number of strains of the ID973 strain was measured. Table 1 shows the measurement results of the growth inhibitory effect.

[0020] As is clear from the results in Table 1, the extract extracts of Example 1 and Example 2 were found to have a remarkable antiproliferative effect on Streptococcus mutans.

[0021]

The anti-cavity agent containing the guava leaf extract according to the present invention as an active ingredient is excellent against oral cavity microorganisms typified by Streptococcus mutans bacteria and having significant involvement in dental caries formation and plaque formation. Show the effect.

 ─────────────────────────────────────────────────── ─── Continuation of the front page (72) Inventor Mika Izawa 335 Kayajuku, Nakahara-ku, Kawasaki City, Kanagawa Prefecture

Claims (1)

[Claims] 1. An anticaries agent comprising a guava leaf extract as an active ingredient.