JP2001039884A - Periodontosis inhibitor - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject inhibitor, a medicament capable of exhibiting excellent growth inhibitory action on periodontosis-related pathogenic bacteria involved in bacterial plaque production and periodontosis onset by including, as active ingredient, an extract of guava leaves. SOLUTION: This inhibitor contains, as active ingredient, an extract of guava leaves. The guava leaves to be used are pref. dried and ground ones. The extract can easily be obtained, for example, by subjecting guava leaves to extraction treatment with water, a hydrophilic organic solvent or a mixture thereof, and the extract thus obtained contain pref. >=1 wt.%, more pref. >=3 wt.% of total polyphenols. The proportion of this inhibitor to be formulated in an oral cavity composition for inhibiting periodontosis is pref. 0.001-5 wt.% calculated as the above extract. Thereby, onset inhibition for chronic gingivitis and pyrorrhea alveolaris can be expected.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an intraoral region which is greatly involved in the cause of so-called periodontal disease, in which the periodontal tissue consisting of the gingiva, alveolar bone, cementum, and periodontal ligament supporting the teeth is damaged. Bacteria Prevoteira Intel Media (Pre
The present invention relates to an agent for preventing periodontal disease, which has an excellent effect of inhibiting the growth of periodontal disease pathogens represented by botella intermedia and prevents chronic gingivitis and alveolar purulence. More specifically, the present invention relates to an excellent periodontal disease inhibitor containing an extract of guava leaves as an active ingredient.
The periodontal disease preventive agent of the present invention is a periodontal disease preventive agent of natural plant origin, such as dentifrices, troches, mouthwashes,
It can be used by blending it with oral compositions such as chewing gums and oral fresheners.

[0002]

2. Description of the Related Art It is said that tooth decay (caries) and periodontal disease are caused by oral microorganisms, plaque and tartar. Two-thirds, about four-fifths of middle-aged people, nine out of ten over the age of 65
It is said that even humans suffer from this disease.

[0003] Dental plaque is a transparent or yellowish-white glue that sticks to the surface of the tooth, and various bacteria resident in the mouth grow on the plaque. Approximately 80% of the ingredients are Prevoteira Intel Media (Prevo)
It is said to be a bacterium represented by T. intermedia. These bacteria cause gingival inflammation and periodontal disease.

As an agent for preventing the formation of such plaque, persimmon leaves and / or seeds of kaemponashi are used as alcohols such as methanol and ethanol, and glycols such as ethylene glycol. Of plaque that is the cause of dental caries (JP-A-2-78609), consisting of an extract obtained by extraction with a hydrophilic organic solvent such as ketones such as acetone, ketones, etc. -Rong tea,
An oral fungus inhibitor (JP-A-1-190624) having an excellent effect on Streptococcus mutans bacteria, which comprises a hot water extract of tea leaves such as black tea as an active ingredient, Sengkyu, Agetsu, Betel wax and / or Kujin. An oral composition (Japanese Patent Application Laid-Open No. 4-159213), which effectively inhibits the growth of Streptococcus mutans containing a crude drug extract as an active ingredient to effectively prevent tooth decay and periodontal disease. Grapefruit, navel orange, hassaku, unshu mandarin orange, kumquat, iyokan, summer tangerine,
Japanese Patent Application Laid-Open No. 4-346933 discloses an agent for inhibiting the growth of caries and periodontal pathogens, which comprises as an active ingredient an organic solvent of citrus peel or a peel-containing substance selected from daidai or the like, preferably methanol or ethanol. ) Has been proposed.

The applicant of the present application has found that the extract of guava leaf extract has an excellent effect on Streptococcus mutans bacteria, and has previously described an anti-caries agent containing the extract as an active ingredient (Japanese Patent Application Laid-Open No. 8-99893). Official Gazette).

[0006]

As described above, the anti-caries agent is proposed by the present applicant (Japanese Patent Laid-Open No. 8-9989).
No. 3) is effective and satisfactory, but the above-mentioned conventionally proposed periodontal disease inhibitor is not always satisfactory in the effect of inhibiting plaque formation, and is more excellent in inhibiting the growth of periodontal disease pathogens. It has been desired to develop a periodontal disease inhibitor.

[0007]

Means for Solving the Problems Accordingly, the present inventors have developed Prevoteira intermedia (P.
revotella intermedia) JCM7
365 strains, Porphyromonas gingivalis (Porp)
hydromonas gingivalis) ATCC
33277 strains, Prevoteira melaninogenica (Pr
evotella melaninogenica) J
CM6325 strain, Capnocytophaga oracea A
We have been studying growth suppression methods for TCC33596 strain and the like.

As a result, an extract of guava leaves extracted with water and / or a hydrophilic organic solvent, which has not been proposed or even suggested as an agent for preventing periodontal disease, greatly contributes to plaque formation and periodontal disease onset. The present invention was found to have an inhibitory action on the growth of periodontal disease pathogens represented by Prevoteira intermedia, and completed the present invention.

Accordingly, an object of the present invention is to provide an excellent periodontal disease inhibitor characterized by containing an extract of guava leaves as an active ingredient.

[0010]

DETAILED DESCRIPTION OF THE INVENTION Guava (Psidium gua)
Java L. ) Is a shrub native to Central America belonging to the genus Bunjiro belonging to the family Myrtaceae, which is widely grown or cultivated in tropical and subtropical regions such as Southeast Asia, southern China, and Hawaii. It has been used to prevent diabetes and diarrhea. The guava leaves used in the present invention may be semi-dried or dried products in addition to fresh leaves, and dried products are particularly preferred. These raw materials are preferably used after being ground.

The guava leaf extract used in the present invention can be easily obtained by subjecting the above guava leaf to 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 be used, for example, in the form of a hydrated solvent mixed with water at an arbitrary ratio.

The extraction operation and extraction conditions can be variously changed according to the type of extraction solvent used. However, when extraction is performed using the above-mentioned hydrophilic organic solvent or a mixture thereof with water as the extraction solvent. For example, 1.5 to 50 times by weight of a solvent is added to guava leaves, and the mixture is allowed to stand or stirred at room temperature to the boiling point of the used solvent for 5 minutes to 24 hours. After performing the extraction operation in this manner, an extract of guava leaves can be obtained by removing insoluble residues by, for example, centrifugation, filtration, squeezing, or other solid-liquid separation means. If necessary, an extraction solvent can be added to the insoluble solid extraction residue, and the same operation can 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, or it may be obtained by concentrating the extract by removing the solvent. The concentrate, or a dried product obtained by drying it under reduced pressure or freeze-drying, can also 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 performed by adding an appropriate amount of an adsorbent to a solution obtained by dissolving the extracted extract as it is or by concentrating the extracted extract in an appropriate solvent such as water, and performing an adsorption treatment. As the adsorption treatment liquid, a concentrated liquid obtained by condensing it as it is or under reduced pressure, and a dried product obtained by drying it under reduced pressure or freeze-drying, for example, can also be used as an extract.

Furthermore, the above-mentioned extract before or after the decolorizing and deodorizing treatment is dissolved in, for example, an appropriate amount of water to obtain a synthetic adsorbent having a resin matrix of, for example, styrene / divinylbenzene, methacrylic acid ester or the like. The active ingredient is subjected to adsorption treatment using, for example, ethanol, methanol,
Acetone, purified by performing a desorption operation with a hydrophilic organic solvent such as ethyl acetate or a mixed solvent of these and water, and concentrating the active ingredient in the guava leaf extract, may also be used as the extract of the present invention. it can. The adsorption / desorption operation can be performed in a batch system or a column system, and preferably, a column system is employed. The desorbed solution after the operation can be used as it is as the extract of the present invention, or a concentrated solution obtained by concentrating under reduced pressure, and further, a dried product obtained by, for example, drying under reduced pressure or freeze-drying Can also be used as the extract of the present invention.

In the case of extracting guava leaves with water, for example, fresh guava leaves, semi-dried products, dried products or pulverized products are used as raw materials.
Water can be extracted at a temperature of, for example, about 50 to 80 ° C. while stirring for about 1 to 5 hours, for example, by adding water of about 100 times the weight. Subsequently, the extract of the present invention can be obtained by performing centrifugation, filtration, and the like, and preferably concentrating and drying the filtrate under reduced pressure.

The guava leaf extract prepared as described above is effective as a periodontal disease inhibitor if the total polyphenol content of the extract is at least about 1% or more. , But preferably about 3
% Or more is good.

Further, natural or high molecular substances such as starch, dextrin, gum arabic, gelatin and the like are added to the liquid or dried product extract obtained by the various treatments as described above.
It is also possible to add a synthetic polymer substance such as carboxymethylcellulose, silica gel, etc., and use it in a powder form by a commonly used drying means such as spray drying.

The oral composition in which the guava leaf extract according to the present invention can be blended as a periodontal disease inhibitor includes, for example, toothpaste, powdery toothpaste, troche, mouthwash, solid oral freshener, and chewing agent. -Ingums, coatings and the like.

The mixing ratio of the periodontal disease preventing agent comprising the guava leaf extract of the present invention to the above-mentioned periodontal disease preventing oral composition varies depending on the type of the composition and the like. The guava leaf extract is contained in an amount of 0.001% to 5% by weight, particularly preferably 0.0% by weight, based on the oral composition.
It can be blended in the range of 1 to 2% by weight. The guava leaf extract according to the present invention can be blended with other raw materials blended in a usual oral composition without any restrictions.

Hereinafter, several embodiments of the present invention will be described more specifically with reference to examples.

[0022]

EXAMPLE 1 6,400 g of hot water was added to 400 g of crushed guava leaves,
The mixture was stirred at 0 ° C. to 95 ° C. for 2 hours to perform an extraction treatment, followed by centrifugation and filtration to obtain 5,440 g of a filtrate. The filtrate was evaporated to dryness under reduced pressure to obtain 63 g of a dry extract. The polyphenol content of the dried extract was 25.4% (Product 1 of the present invention).

Test Example 1 The product 1 of the present invention obtained in Example 1 (polyphenol content 2
5.4%), commercially available polyphenon 30 (manufactured by Mitsui Norin Co., Ltd .;
GAM agar medium (peptone) to which green tea extract, polyphenol content of 42.3%) and apple phenone (Nikka Whiskey Co .; apple extract, polyphenol content of 40.3%) are added at different polyphenol concentrations. , Soy peptone, proteose peptone, digested serum powder, meat extract, liver extract powder, glucose, potassium dihydrogen phosphate, sodium chloride, soluble starch, L-cysteine hydrochloride, sodium thioglycolate, agar) 2
0 ml to Prevoteira Intel Media (Prev
otella intermedia) JCM7365
Add strain to x10 ⁴ CFU / ml. 37
The cells were cultured under anaerobic conditions at 4 ° C. for 4 days, and the number of bacteria of Prevotilla intermedia JCM7365 strain was measured. Table 1 shows the measurement results of the growth inhibitory effect.

[0024]

[Table 1]

++: Number of bacteria 500 or more +: Number of bacteria 500 or less −: Number of bacteria 0

As is clear from the results shown in Table 1, the product 1 of the present invention has a content of 0.01%, and the polyphenon 30 has a content of 0.04%.
At the above concentration of polyphenol content, the growth inhibitory effect of Prevoteira intermedia was observed, but that of Applephenone was not. In addition, it can be determined that the product 1 of the present invention has a remarkable growth inhibitory effect four times as high as that of polyphenon 30, and from this, the guava leaf extract of the present invention contains polyphenols or other polyphenols not contained in polyphenone 30 or applephenone. It is believed that antimicrobial substances are present.

Test Example 2 Porphyromonas gingivalis was used in place of Prevoteira intermedia of Test Example 1.
nas gingivalis) ATCC 33277
Prevoteira melaninogenica (Prevote)
lla melaninogenica) JCM632
5 strains, Capnosite Ferga Ochracea (Capn
ocytophaga oracea) ATCC33
A similar test was performed using 596 strains.
We got almost the same result as Intel Media.

[0028]

EFFECTS OF THE INVENTION The periodontal disease inhibitor comprising the guava leaf extract of the present invention as an active ingredient exhibits an excellent growth inhibitory effect against periodontal disease pathogens represented by Prevoteira intermedia and plaque. To prevent the onset of periodontal disease.

 ────────────────────────────────────────────────── ─── Continuing on the front page (72) Inventor Hideko Hirai 335 Karijuku, Hasegawa Nakahara-ku, Kawasaki-shi, Kanagawa F-term in the Technical Research Institute Co., Ltd. 4C088 AB57 AC05 BA08 BA10 BA14 NA14 ZA67

Claims (1)

[Claims] 1. A periodontal disease preventive comprising a guava leaf extract as an active ingredient.