JP3222021B2 - Anti-caries agent - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention exhibits an excellent inhibitory effect on the growth of oral microorganisms represented by Streptococcus mutans, which is greatly involved in the formation of dental caries (caries). The present invention relates to an anti-caries agent useful for preventing tooth decay, which can prevent plaque formation involving oral microorganisms. More specifically, the present invention relates to an excellent anti-caries agent containing an extract of guava leaves as an active ingredient. The anti-caries agent of the present invention is an anti-caries agent of natural plant origin, and is formulated in oral compositions such as dentifrices, troches, mouthwashes, chewing gums, and mouth fresheners. Can be used.

[0002]

2. Description of the Related Art Caries (dental caries) are caused by oral microbes and plaque,
It is said that it occurs only when there are three conditions of ingredients in food, especially sugar and tooth substance, and it is said that the use of sugar in recent years is particularly likely to affect worm teeth from childhood.

[0003] Dental plaque is formed on the tooth surface by oral bacteria, food residues and salivary organic substances. One of the oral bacteria, Streptococcus mutans, synthesizes a dextran-like polysaccharide from sucrose. It is known that caries is produced by producing acids from other sugars, retaining them in plaque, and causing demineralization of teeth.

[0004] Agents for preventing the formation of such plaque (hereinafter referred to as anti-caries agents) include persimmon leaves and / or
Alternatively, an extract obtained by extracting the seeds of Kamponashi with a hydrophilic organic solvent such as alcohols such as methanol and ethanol, glycols such as ethylene glycol, and ketones such as acetone. A plaque formation inhibitor causing caries (Japanese Patent Laid-Open No. 2-78609)
Gazette): An oral fungus inhibitor having an excellent effect on Streptococcus mutans bacteria, comprising a hot water extract of tea leaves such as green tea, oolong tea and black tea as an active ingredient (Japanese Patent Laid-Open No. 1-19)
0624 gazette): An oral composition which effectively inhibits the growth of Streptococcus mutans containing a crude drug extract of Senkyu, Agetsu, Betel Nut and / or Kudjin as an active ingredient, and thereby favorably prevents tooth decay and periodontal disease ( JP-A-4-
159213): Also, lemon, grape ful-
An organic solvent, preferably methanol or ethanol extract, of citrus peel or pericarp-containing material selected from tuna, naple orange, hassaku, Satsuma mandarin, kumquat, ikan, summer tangerine, daidai, etc. Inhibitor of dental caries and periodontal pathogens as components (Japanese Patent Laid-Open No. 4-34693)
3 publication) have been proposed.

[0005]

However, the above-mentioned anti-caries agents proposed in the prior art are not always satisfactory in the effect of inhibiting plaque formation, and there is a need for the development of a more excellent anti-caries agent.

[0006]

Accordingly, the present inventors studied a method for inhibiting the growth of Streptococcus mutans, a typical oral bacterium, which is greatly involved in the formation of dental plaque causing caries. I went.

As a result, water and / or a hydrophilic organic solvent for guava leaves which have heretofore not been known to contain a substance having an inhibitory action on caries-forming microorganisms represented by Streptococcus mutans have been known. Has been found to have an excellent inhibitory effect on oral microorganisms typified by Streptococcus mutans, which are greatly involved in caries formation and plaque formation.

Accordingly, an object of the present invention is to provide an excellent anti-caries agent comprising an extract of guava leaves as an active ingredient.

[0009] Guava (Psidium java)
L. ) Is a shrub native to Central America belonging to the genus Bunjiro, which belongs to the family Myrtaceae. It 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 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 be used, for example, in the form of a hydrated solvent mixed with water at an arbitrary ratio.

The extraction operation and the extraction conditions can be variously changed according to the kind of the extraction solvent to be used. However, when the extraction is carried out using the above-mentioned hydrophilic organic solvent or a mixture thereof with water as the extraction solvent. Can be carried out, for example, by adding a solvent of about 1.5 times to about 50 times the weight of guava leaves and allowing the mixture to stand or stir at room temperature to the boiling point of the used solvent for about 5 minutes to about 24 hours. After performing the extraction operation in this manner, for example, centrifugation, filtration, squeezing or other solid-liquid separation means to remove insoluble residues,
A guava leaf extract can be obtained. 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 by the above method from guava leaves may be used as it is as the extract of the present invention,
Alternatively, a concentrate obtained by removing the solvent from the extract to obtain a concentrate, and further a dried product obtained by drying it under reduced pressure 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 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. The adsorption treatment liquid is
A concentrated liquid obtained 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 extract before or after the decolorization and deodorization treatment is dissolved in, for example, an appropriate amount of water, and is effectively used using a synthetic adsorbent having a resin matrix of, for example, styrene / divinylbenzene, methacrylate, or the like. The components are adsorbed and purified, for example, by desorption with a hydrophilic organic solvent such as ethanol, methanol, acetone or ethyl acetate or a mixed solvent of these and water, and 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 method or a column method, and preferably, a column method is employed. The desorbed solution after the operation can be used as it is as the extract of the present invention, but also 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.

[0012] When water is extracted from guava leaves using water, for example, guava, fresh leaves, semi-dried, dried or pulverized materials are used as raw materials, and for example, about 10 to about 100 Double weight water is added, for example, 50-80 ° C
Extraction can be carried out at about the same temperature, for example, while stirring for about 1 to 5 hours. Subsequently, centrifugation, filtration, etc. are performed, and preferably the filtrate is concentrated to dryness under reduced pressure to obtain the extract of the present invention.

The guava leaf extract prepared as described above has a sufficient effect as an anti-caries agent if the total polyphenol content of the extract is at least about 1% or more. Demonstrates, preferably about 3%
Good.

The oral composition in which the above guava leaf extract according to the present invention can be compounded as an anti-caries agent includes, for example, toothpaste, powdery toothpaste, troche, mouthwash, solid oral freshener, chewing gum , A coating agent and the like.

The mixing ratio of the anti-caries agent comprising the guava leaf extract of the present invention to the oral composition for preventing dental cavities as described above varies depending on the type of the composition and the like. 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 in the range of from 01 to about 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 by way of examples.

[0017]

【Example】

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

Example 2 1500 g of water was added to 150 g of crushed guava leaves, and
The mixture was stirred at 0 ° C. for 2 hours, subjected to an extraction treatment, centrifuged, and filtered to obtain 1200 g of a filtrate. The filtrate was concentrated to dryness under reduced pressure to obtain 20 g of a dry extract. The total polyphenol content of this extract was 22%.

Test Example 1 An extract containing the extract obtained in Examples 1 and 2 and a commercially available polyphenone 60 (manufactured by Mitsui Norin; green tea extract, polyphenol content 60%) at predetermined concentrations.
-TGC medium (tryptone, soypeptone, glucose,
20 ml of sodium chloride, sodium thioglycolate, L-cystine, sodium sulfite, agar) was added to Streptococcus mutans (Streptococcus).
mutans) IID973 strain at × 10 ⁴ CFU
/ Ml. The cells were cultured at 37 ° C., and over time these cells were streptococcus mutans I.
The number of ID973 strains was measured. Table 1 shows the measurement results of the growth inhibitory effect.

[0020] As is clear from the results shown in Table 1, the extract of Example 1 and Example 2 showed a remarkable growth inhibitory effect on Streptococcus mutans.

[0021]

EFFECTS OF THE INVENTION The anti-caries agent comprising the guava leaf extract of the present invention as an active ingredient is excellent against oral microbes which are crucially involved in caries formation and plaque formation represented by Streptococcus mutans bacteria. Effect.

──────────────────────────────────────────────────続 き Continuation of the front page (72) Inventor Mika Izawa 335 Kariyuku, Nakahara-ku, Kawasaki-shi, Kanagawa Hasegawa Perfumery Co., Ltd. (56) References Chemical Abstracts, Vol. 124, no. 5, pp. 1068, 124: 54152 (1996, January 29, 58) (58) Fields investigated (Int. Cl. ⁷ , DB name) A61K 35/78 BIOSIS (DIALOG) CA (STN) MEDLINE (STN)

Claims (1)

(57) [Claims] 1. An anti-caries agent comprising a guava leaf extract as an active ingredient.