JPH0640867A - Composition for oral cavity application - Google Patents

Abstract

PURPOSE:To provide a composition for oral cavity application, exhibiting selective antibacterial power exclusively to periodontosis-causative bacteria and free from antibacterial effect on enteric bacteria beneficial to human body. CONSTITUTION:The composition for oral cavity application contains a water-or organic solvent-soluble fraction of one or more kinds of plants selected from ENMEISO (grass of Plectranthus rugosus), KIJITU (young fruit of Citrus auranthium), KOTOUSEIHI (shell of Juglans regia), HACHIGATSUSATSU (fruit of Akebia quinata) and ICHIJIKUYOU (leaf of Ficus carica). Since the above active components are originated from crude drugs, the risk of causing superinfection is low.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an oral composition which is effective in preventing and treating periodontal diseases.

[0002]

BACKGROUND ART Periodontal diseases such as gingivitis and periodontitis are anaerobic bacteria that grow in plaque and gingival sulcus, Prophyromonas (Bacteroides) gingivalis.
eroides) gingivalis] and other infections caused by periodontal disease-causing bacteria, and various fungicides and antibiotics have been conventionally used for the prevention and treatment of such periodontal diseases. As the bactericide used for this purpose, there are synthetic bactericides such as chlorhexidine hydrochloride, and as the antibiotics, there are tetracycline and minocycline. However, since chlorhexidine hydrochloride has a risk of causing allergies, its content in dentifrice and the like is limited to a low concentration, and a sufficient preventive and therapeutic effect cannot be obtained. In addition, since antibiotics such as tetracycline show a wide spectrum of antibacterial spectrum, there is a risk that they may cause bacterial metastasis such as candidiasis, and that they also adversely affect the balance of intestinal microflora useful for the human body. There is. Furthermore, since the periodontal disease-causing bacterium is a resident bacterium, in order to continuously prevent the disease, it is necessary to administer antibiotics at all times, which is a factor that makes the above-mentioned problems such as transmutation more serious. Is not suitable.

In addition to these bactericides, thymol and eugenol, which are antibacterial agents derived from plant flavors, are known as those having safer antibacterial activity for human body.
However, these have a problem that their antibacterial activity against periodontal disease-causing bacteria is weak.

In addition, an oral composition containing an extract obtained from a herbal medicine is also known (for example, Japanese Patent Laid-Open No. Sho 63-63).
-267714, JP-A-3-167132 and JP-A-4-5222). However, the active ingredients contained in these compositions have not only sufficient antibacterial activity against periodontal disease-causing bacteria, but also have low persistence in the oral cavity, and thus have long-lasting drug efficacy. There is also the problem of being small.

[0005]

[Problems to be Solved by the Invention] Various synthetic fungicides, antibiotics and thymol derived from botanical fragrances which have been used for the prevention and treatment of periodontal diseases in the related art, all have the above-mentioned preventive and therapeutic effects and safety. The thing which can satisfy both sides of is not yet found. Furthermore, the above-mentioned JP-A-63-26771.
The prior art described in Japanese Patent Publication No. 4 and the like is not sufficiently satisfactory in terms of the antibacterial activity of the active ingredient itself and the persistence after use (that is, persistence of effect). Therefore, an object of the present invention is to solve the above problems, and to provide an oral composition that has high preventive and therapeutic effects against periodontal disease and high safety.

[0006]

[Means for Solving the Problems] The inventors of the present invention focused on an extract of a herbal medicine plant, which has been used for a long time and whose safety is well known, and extensively studied its antibacterial action. It was found that the extract of No. 1 exerts an antibacterial activity selectively against pathogens of periodontal disease with almost no effect on intestinal bacteria, and has completed the present invention.

That is, the present invention is characterized in that it contains a water-soluble or organic solvent-soluble fraction of one or more kinds of plants selected from Enmeisou, Buri, walnut green peel, August bills and flowerless leaves. An oral composition is provided.

The plants used in the present invention include Enmeisou (Pl
ectranthus rugosus Mak., the herbaceous herbaceous herb),
Agari (Citrus aurantium L., young fruit of Rutaceae), walnut blue peel (Juglans regia L., walnut walnut outer skin), August tag (Akebia quinata Decne., Fruit of Akebidae) or flowerless fruit leaf ( Ficus carica L., fig leaves of the Moraceae family. These may be used alone or in combination of two or more.

The water-soluble or organic solvent-soluble fraction used in the present invention is obtained by extracting the above-mentioned plant with water, an organic solvent or a mixture thereof by an appropriate method.

The organic solvent is not particularly limited,
Examples thereof include alcohols such as methanol, ethanol and isopropanol, acetone, ethyl acetate and ethyl ether. These may be used in combination of two or more. Further, when a mixture of water and an organic solvent is used, the content ratio of water is preferably 50% or less.

The extraction method is not particularly limited,
An extraction method using water, an organic solvent or a mixture thereof, a steam distillation method, a liquid-liquid partition extraction method in which water and an organic solvent or organic solvents are appropriately combined can be applied, and each of these extraction methods is appropriate. Can also be combined with. For example, liquid-liquid distribution by a desired combination of solvents using a separatory funnel, etc., to the extract obtained by immersing the above-mentioned plant into shreds or pulverized as required, in water or an organic solvent. A method can be applied in which extraction is performed once or more to finally obtain the target soluble fraction. These extraction methods are preferably carried out between room temperature and 55 ° C. As a particularly preferred extraction method, a crude extract obtained by extracting the solvent by distilling the solvent by the usual extraction method or steam distillation,
Liquid-liquid partition extraction with ethyl acetate and water, further solvent-distillation of ethyl acetate fraction, further liquid-liquid partition extraction with hexane and 90% methanol aqueous solution, and solvent distillation of methanol fraction can be mentioned. .

The water-soluble or organic solvent-soluble fraction thus obtained can be used as a constituent of the oral composition of the present invention as it is, or if necessary, dried and powdered. The amount of such water or organic solvent soluble fraction to be added to the oral composition of the present invention is not particularly limited as long as it exhibits an antibacterial activity against periodontal disease-causing bacteria, but is 5 in terms of dry weight.
0 ppm or more is preferable.

The oral composition of the present invention contains dextrins such as dextrin, α-cyclodextrin and β-cyclodextrin for the purpose of improving the adsorption of the active ingredient in the oral cavity and maintaining the antibacterial activity. It is preferable. The mixing ratio of these dextrins is preferably 0.1 to 50% by weight based on the total amount of the oral composition. Further, in order to impart foamability to the composition for oral cavity of the present invention, it is preferable to add a phosphoric acid alkyl ester such as lauryl phosphoric acid, myristyl phosphoric acid, cetyl phosphoric acid or salts thereof. The mixing ratio of these phosphoric acid alkyl esters is 0.1 to 2 with respect to the total amount of the composition for oral cavity.
It is preferably in the weight%.

In addition to the above-mentioned components, the oral composition of the present invention may also contain, if necessary, various known components which are mixed in dentifrices, mouthwashes, mouthwashes, chewing gums and the like. it can. These known ingredients include sodium fluoride, sodium monofluorophosphate, allantoin, tranexamic acid, vitamin C, vitamin E, sodium chloride, chlorhexidine salt, cetylpyridinium salt, lysozyme, dextranase, protease, glycyrrhizinate and the like. Active ingredients; Abrasives such as aluminum hydroxide, silica gels, aluminosilicates; Binders such as carrageenan, sodium carboxymethyl cellulose, hydroxyethyl cellulose, sodium polyacrylate, sodium alginate, gum arabic; polyoxyethylene-polyoxypropylene Block copolymer, polyoxyethylene sorbitan fatty acid ester, sorbitan fatty acid ester, sodium acylglutamate, sucrose fatty acid ester, polyoxy May be mentioned a surfactant such as styrene hydrogenated castor oil.

The oral composition of the present invention can be produced by a conventional method by mixing the above-mentioned components, and it is provided for the purpose of preventing periodontal diseases and the like. Dentifrice, mouthwash, mouthwash, oral lozenge. , Chewing gum, candy, etc.

[0016]

EXAMPLES The present invention will be described below with reference to examples, but the present invention is not limited to these examples.

Production Example 500 g of each of Enmeisou, Buri, walnut green peel, August bills and flowerless leaves were immersed in 1 liter of methanol for 1 day at room temperature, and then treated in the same manner in the order of ethanol and water.
Next, the respective extracts were combined, and those solvents were distilled off under reduced pressure by an evaporator to obtain a crude extract (water or an organic solvent-soluble fraction). Then 5 of these crude extracts
About 0 g, 600 ml of ethyl acetate and 200 m of water
Liquid-liquid partition extraction was performed using 1. Next, the ethyl acetate fraction was collected, the ethyl acetate in the fraction was distilled off, and then 600 ml of n-hexane and 600 ml of 90% aqueous methanol solution were added.
Was used for liquid-liquid partition extraction. Then, the methanol fraction was separated and the methanol was distilled off to obtain a methanol-soluble fraction.

Test Example 1 Using the crude extract and the methanol-soluble fraction obtained in Production Example, their antibacterial activity was tested by the following method. First, BHI agar medium (hemin, menadione,
The crude extract and the methanol-soluble fraction were added to 5% by weight sheep blood (manufactured by Difco) and SCD agar medium (manufactured by Nissui) at 25, 50, 100, 200 and 400, respectively.
It was added so as to be ppm. Next, as a test bacterium, Prophyromonas gingival
is) (ATCC33277) (P.g) and Escherichia coli (IFO3972) (E.
c), and suspend them in physiological saline to obtain 10 ⁷ CF.
A U / ml bacterial solution was prepared. After that, P. g Bacteria solution is anaerobic glove box (N ₂ : H ₂ : CO ₂ = 80: 10:
10) in BHI agar medium, E. One drop each of the c-bacterial solution was inoculated on the SCD agar medium in an aerobic environment. next,
They were cultured in each environment at 37 ° C. for 3 days, and the minimum concentration at which no bacterial growth was observed was defined as the minimum inhibitory concentration (MIC). In addition, as a comparative example, the same test was carried out for those to which thymol, eugenol, and latania root extract for which antibacterial activity was reported were added. The results are shown in Table 1.

[0019]

[Table 1]

As is clear from Table 1, each of the fractions obtained in the production examples had P. Although it showed remarkable antibacterial activity against g.
It showed no antibacterial activity against c. On the other hand, in the comparative example, P. g and E. No antibacterial activity was shown against any of c.

Test Example 2 Using the crude extract of each plant and the methanol-soluble fraction obtained in the Production Example, an antibacterial activity sustaining test was conducted. An adult male was rinsed with 10 ml of each sample solution having the composition shown in Table 2 for 30 seconds.
After that, saliva collected after 2 hours while eating and drinking was stopped was put into an anaerobic glove box (N ₂ : H ₂ : CO ₂ = 8).
Diluted with physiological saline within 0:10:10). Next, 0.1 ml of the diluted solution was inoculated into Bacteroides agar medium (manufactured by Nissui). Then, the number of colonies formed by culturing the cells at 37 ° C. for 5 days was measured to determine the number of viable bacteria of the genus Prophylomonas in saliva. Further, as a comparative example, the same test was performed using 10 ml of the sample liquid having the composition shown in Table 2. The results are shown in Table 2.

[0022]

[Table 2]

As is clear from Table 2, the composition of each Example was confirmed to have a sustained antibacterial activity even 2 hours after the mouth washes.

Example 1 Components of the following composition were deaerated and mixed to obtain a paste-like dentifrice.

[0025]

[Table 3] (Components) Blending amount (wt%) Crude fruit crude extract obtained in Production Example 0.1 Enmeiso grass methanol fraction obtained in Production Example 0.1 Dextrin 1.0 Aluminum hydroxide 37.0 Anhydrous Silicic acid 3.0 Glycerin 10.0 70% Sorbitol 15.0 Sodium carboxymethyl cellulose 2.0 Methyl paraben 0.1 Sodium lauryl phosphate 1.5 Cetyl phosphate 0.5 Perfume 0.8 Purified water Qualifying amount 100.0

Example 2 Components of the following composition were deaerated and mixed to obtain a paste-like transparent dentifrice.

[0027]

[Table 4] (Component) Blending amount (% by weight) Starch methanol-soluble fraction obtained in Production Example 0.1 Walnut blue peel methanol-soluble fraction obtained in Production Example 0.1 α-Cyclodextrin 1.0 Silica Acid 25.0 Glycerin 30.0 70% Sorbitol 30.0 Sodium carboxymethyl cellulose 1.8 Carrageenan 0.2 Methylparaben 0.1 Arginine laurylphosphate 1.5 Perfume 0.8 Purified water Qty 100.0

Example 3 The components of the following composition were mixed with stirring to obtain a mouthwash.

[0029]

[Table 5] (Components) Blending amount (wt%) Methanol-soluble fraction of August tag obtained in Production Example 0.1 Methanol-soluble fraction of dried nuts obtained in Production Example 0.1 Dextrin 1.0 Ethanol 4. 0 70% Sorbitol 3.0 Sodium carboxymethylcellulose 1.8 Polyoxyethylene hydrogenated castor oil 0.2 Methylparaben 0.1 Arginine myristylphosphate 0.2 Perfume 0.8 Purified water Qty 100.0

Example 4 Chewing gum was obtained by mixing the respective components of the following composition while heating and dissolving them, and further spreading them into a plate shape and then cooling and solidifying.

[0031]

[Table 6] (Component) Blending amount (% by weight) Crude extract of August paste obtained in Production Example 0.1 Methanol-soluble fraction of flowerless fruit leaf obtained in Production Example 0.1 β-Cyclodextrin 1.0 Gum base 25.0 Palatinose 50.0 Corn syrup 23.6 Perfume 0.2 Total 100.0

Example 5 After mixing the components of the following composition, the mixture was molded into a disk using a tableting machine to obtain an oral troche.

[0033]

[Table 7] (Component) Blending amount (% by weight) Methanol-soluble fraction of Enmeisou obtained in Production Example 0.1 Crude extract of dried nuts obtained in Production Example 0.3 Dextrin 5.0 Citric acid 0.2 Aspartame 0.1 Lysozyme chloride 0.1 Gum arabic 7.0 Fragrance 0.2 Lactose Appropriate amount 100.0

Example 6 The following sugar component dissolved in purified water was boiled down to 145 ° C., cooled to 100 ° C. or lower, and then the following remaining components were added and cooled to room temperature to obtain a candy.

[0035]

[Table 8] (Component) Blending ratio (% by weight) (Sugar component) Sucrose 86.6 Maltose reduced starch syrup 12.0 (Other components) Crude extract of Enmeisou obtained in Example 1 0.1 Example Crude extract of unflowered fruit leaf obtained in 1 0.1 Methanol-soluble fraction of drought obtained in Example 1 0.2 β-Cyclodextrin 0.5 Citric acid 0.2 Sodium citrate 0.1 Vitamin C 0. 1 fragrance 0.1 Total 100.0

[0036]

EFFECT OF THE INVENTION The water-soluble or organic-solvent-soluble fraction of a herbal medicine, which is an active ingredient of the oral composition of the present invention, is a bacterium causing periodontal disease, Prophyromonas gingivalis.
monasgingivalis), but it has a selective antibacterial property that shows almost no antibacterial activity against intestinal bacteria such as Escherichia coli. Moreover, since it is a component derived from a herbal medicine plant, it has a low risk of causing bacterial symptomatosis. Therefore, the oral composition of the present invention has an excellent preventive effect on periodontal disease and the like, and is highly safe. In addition, the composition of the present invention containing dextrin as a constituent component can maintain the antibacterial activity for a longer period of time.

Claims (1)

[Claims] 1. An oral composition characterized by containing a water-soluble or organic solvent-soluble fraction of one or more plants selected from Enmeisou, Fructus kuri, walnut green peel, August bills and flowerless leaves. .