JPH04164021A - Composition for oral cavity - Google Patents

Abstract

PURPOSE:To obtain a composition for oral cavity for dentifrice having excellent effects on prevention and treatment for caries or periodontosis by blending an oil soluble extract of Glycyrrhiza and plant belonging to the same genus. CONSTITUTION:An oil soluble extract of Glycyrrhiza and plant belonging to the same genus are blended. The extract is obtained from a Glycyrrhiza such as Glycyrrhiza glabra Linne or Glycyrrhiza inflata Batalin and especially preferably extracted from root. One or two or more kind of these effective ingredients are preferably used in a high content, e.g. of >=0.5wt.% based on dried weight of extract. An antimicrobial activity of the extract is raised by further blending l-menthol or l-carvone or both thereof with the above-mentioned composition each at an amount of 0.005-5wt.% based on total amount of composition.

Description

Detailed Description of the Invention [Field of Industrial Application] The present invention provides toothpastes, mouthwashes,
It relates to oral compositions such as pasta.

[Conventional techniques and issues] Caries and periodontal disease are infections caused by certain oral bacteria, and Streptofuccus mutans is a typical bacterial cause of caries. Durham-negative anaerobic bacteria, represented by Bacteroides gingivalis, are candidates for the causative bacteria of the disease. From this perspective, attempts have been made to suppress pathogenic bacteria using antibacterial agents as a means of preventing or treating caries and periodontal disease. Conventionally, synthetic antibacterial agents such as chlorhexidine and cetylpyridinium chloride have been used in tooth brushing It has been added to mouthwash and its effectiveness has been confirmed.

However, when considering long-term use of these agents and application to the mouth, it is considered preferable to use naturally derived antibacterial agents from the standpoint of safety. However, to date, natural antibacterial agents against pathogenic bacteria in the oral cavity have not been sufficiently investigated.

In recent years, as research on licorice extract has progressed, the oil-soluble fraction containing various flavonoids has been shown to have antioxidant effects (
JP-A No. 58-217583), enzyme inhibitory action (JP-A No. 1-149706), antibacterial action (JP-A No. 59-462)
No. 10) has been found to have a useful effect, and its antibacterial effect is also being investigated. However, its antibacterial activity against Gram-negative bacteria is low within the range of bacterial species studied so far (Fragrans, L).
Journal, 6, 122-125.1989), but the effect on oral bacteria has hardly been investigated. In particular, the effect on periodontal pathogenic bacteria, which are Gram-negative bacteria, is completely unknown.

[Means for solving problems].

In view of these circumstances, the present inventors have conducted various studies on the application of the oil-soluble fraction of licorice to the prevention and treatment of periodontal disease. As a result, the oil-soluble extract of licorice (hereinafter referred to as oil-soluble licorice extract) unexpectedly showed very strong antibacterial activity against the periodontal pathogen Bacteroides gintsuvaris, which is a Durum-negative anaerobic bacterium. By adding a small amount of termenthol and/or ρ-carvone to licorice extract, its antibacterial activity is significantly increased, and it is effective against not only Bacteroides gintsuvaris but also Streptococcus mycotans, which is a bacterium that causes caries, and the bacteria that causes gingivitis. It was discovered that a certain Actinomyces hiscosus also exhibits strong antibacterial activity, leading to the completion of the present invention.

That is, the present invention provides an oral composition comprising an oil-soluble licorice extract, preferably an oral composition comprising an oil-soluble licorice extract and Q-menthol and/or ρ-carvone. A composition is provided.

The oral composition of the present invention significantly suppresses bacteria causing caries and periodontal disease, and is extremely useful for preventing and treating these diseases.

The oil-soluble licorice extract used as the antibacterial component in the oral composition of the present invention may be prepared from licorice or its congeners, for example,
Glycyrrhiza g
G lycyrrhiza 1nflata
Batalin), Glychiriza araresis (G.
It is an oil-soluble extract obtained from Iycyrrhiza araleasis, and in particular, one extracted from the root is preferable. These oil-soluble licorice extracts include clavulizine, glabrene, and lycope as active ingredients.

8. It has been found that the oil-soluble licorice extract contains Ricobu J7 Recon B and Ricokumarono. In the present invention, the oil-soluble licorice extract contains one or more of these active ingredients in a high content, for example, by drying the extract. It is preferable to use one containing 0.5% by weight or more based on weight. Also,
As the oil-soluble licorice extract, one or more of these active ingredient isolates or concentrates may be used.

The oil-soluble licorice extract is usually obtained by extracting licorice or its related plants, preferably its roots, with an organic solvent such as methanol, ethanol, acetone, ethyl acetate, chloroform, etc. The raw material for extraction may be either fresh or dried plant matter, or it may be a residue obtained by extracting glycyrrhizin, which is useful as a sweetener, etc., by extracting the plant body with water. For the extraction operation, methods known for extraction using ordinary organic solvents can be employed.

In the present invention, the oil-soluble licorice extract is expressed as an extract dry weight of 00005 to 10
The desired effect can be obtained by blending the components in an amount of 0.005 to 5% by weight.

Furthermore, in the present invention, as described above, it is preferable to incorporate C-menthol and/or Q-carvone, which increases the antibacterial activity of the oil-soluble licorice extract. By blending termenthol and a-carvone in an amount of 0005 to 5% by weight based on the total amount of the oral composition, the desired effect of increasing antibacterial activity is exhibited. Incorporation of too large a quantity is not preferable because it affects the flavor of the oral composition.

The oral composition of the present invention can be made into the form of toothpaste, mouthwash, pasta, chewing gum, candy, etc. according to a conventional method, and the other ingredients are not particularly limited. You can use the one that is mixed into the product.

[Example] Next, the present invention will be explained in more detail by giving Examples and Test Examples.

Example 1 Licorice (G lycyrrhiza glabra)
L 1nne) and licorice (G 1ycyrrhiza
1kfl root of 1nflata Batalin)
Anhydrous ethanol 1012 was added to the solution, and extraction was performed under reflux for 5 hours. The obtained extract was concentrated under reduced pressure, and after drying, 10 ρ of ethyl acetate was added to the residue and extracted for 5 hours. The ethyl acetate extract was concentrated under reduced pressure and dried to obtain about 30 g of extracts A and B, respectively.

The content of typical flavonoids in Extract A and Extract B was determined by HPLC, and the results were as follows.

Extract A Nigellabridin approx. 10%, Glabrene approx. 3% Extract B: Licochalcone A approx. 20%, Licochalcone B approx. 1.5% Example 2 Licorice (G Iycyrrhiza araleasi)
A mixed solvent of hexane:ethanol-2:l (10I2) was added to 2ky roots of s), and extraction was performed under reflux for 2 hours. The extract was concentrated under reduced pressure and dried to obtain about 409 Extract C.

Extract C contains approximately 2 licocumaron as a representative flavonoid.
It contained %.

Example 3 A toothpaste containing oil-soluble licorice extract A and Q-carvone was prepared according to the following formulation.

Aluminum hydroxide 45% carrageenan 0.5 sodium alginate
0.5 gelatin
0.3 Propylene glycol 3.0 Sorbiturate liquid 30 Sodium lauryl sulfate 1.2 Lauric acid diethanolamide 1.5 Sodium saccharin
0.1 oil-soluble licorice extract A O, IQ
-Carvone 0.5 purified water
Total remaining 100.0
% Example 4 A mouthwash containing oil-soluble licorice extract C and Q-menthol was prepared according to the following recipe.

Ethyl alcohol 15.0% sorbitol 1O10 citric acid
0.05 Sodium citrate, rum
02 Sodium benzoate 0,2
Sodium lauryl sulfate 0.2 Saccharin sodium 0.05 Blue No. 1
0.001 Oil-soluble licorice extract C002 g-menthol 0.05 Purified ice
Total remaining t o o, o% Example 5 Chewing gum was prepared according to a conventional method with the composition shown below.

Chewing gum base 20% powdered sugar
51.15 Glucose 10 Starch syrup
18 Oil-soluble licorice extract B O,05ρ-menthol 0,8 total 10
0.0% Example 6 Hard candy was prepared according to a conventional method using the composition shown below.

Granulated sugar 46.8% starch syrup
52.34 Citric acid 0.3 Oil-soluble licorice extract A O,03〃CO,03 g-Carvone 0.5 Total
100.0% Test example! Oil-soluble licorice extracts A and B extracted in Examples 1 and 2,
The minimum inhibitory concentration (MIC) of C, Q-menthol and Q-carvone against three types of oral bacteria was determined in plain form.
It was determined by a liquid medium dilution method using Heart Infection Broth (BHr Broth). Note that cetylpyridinium chloride, an antibacterial agent, was used as a positive control. Approximately 1
08 bacteria/suspension of red bacteria and each test drug prepared at various concentrations were mixed in BHI broth, and incubated at 37°C and 48°C.
Time anaerobic culture (HtlO%, C0,5%, N, 85%)
Afterwards, the presence or absence of bacterial growth was visually determined. The minimum concentration at which no growth was observed was defined as MIC (μ9/ml). The results are shown in Table 1.

Table 1 381゛Minimum inhibitory concentration, μ9/11ρ Oil-soluble licorice extracts A, B, and C all showed antibacterial activity in the range of 313 to 100 μ9/II (l) against the tested bacterial strains. 3.13-6.25μ for Bacteroides gintubalis, a negative anaerobic bacterium.
9/MIC of chu, indicating excellent antibacterial activity. However, its activity was lower than that of cetylpyridinium chloride. On the other hand, no antibacterial activity was observed for Q-menthol and Q-carvone within the concentration range used.

Test Example 2 In the presence of fragrance ingredients such as Q-menthol and ρ-carvone,
The antibacterial activity of oil-soluble licorice extracts A and B against oral bacteria was investigated. 100μg/xQ or 500μg
Licorice extract of various concentrations was added to BHI broth containing /
The presence or absence of growth was determined. The results are shown in Table 2. The results are expressed as the minimum concentration of licorice extract μ9/xQ that exhibits antibacterial activity in the presence of each fragrance component.

Table 2 No additives 50 50 3.13 6.25
Termettol 100μLi/xQ 12.5 12.5 0.7
8 1.56500μti/pass 6.25 6.25
0,39 0.39Q-cal main 100μ9/*Q 25 25 1.56 1
．． 56500μ9/xQ 12.5 12.5 0
,78 0.78 Anis Athlete 500μ9/touge 50 50 3.13 6.2
5 Shinami Fukuarthito 500μ9/ytQ 50 50 3.13
6.25 Isoamyl acetate 500μ9/branch 50 50 3.13 6.2
5.Vanillin 3.13 6.13 Minimum concentration showing antibacterial activity 2μ9/wρ As shown in Table 2, the presence of Q-menthol and C-carvone makes licorice extracts A and B antibacterial. Activity increased significantly.

On the other hand, other fragrance ingredients did not affect the antibacterial activity of licorice extract.

Test Example 3 According to the formulation of Example 4, a mouse water tsunyu (tested world) containing oil-soluble licorice extract C and Q-menthol was prepared.

On the other hand, a mouthwash containing the same concentration of vanillin instead of Q-menthol (Control World 1) and a mouthwash containing no oil-soluble licorice extract C (Control World 2) were created.
The antibacterial activity was compared.

After heat sterilizing the BHI agar medium, cool it to 50°C, add a solution of Actinomyces viscosus Tl4V bacteria cultured in BHI broth in advance to about 10' cells (IRQ), and immediately transfer to a sterile Petri dish with a diameter of 90+no+. The solution was dispensed into 10xQ portions and solidified. On this flat plate, the inner diameter is 8
Erect a cylinder with a f/1 m and a height of 10 nm, fill it with the three types of mouthwashes mentioned above, and after culturing anaerobically at 37°C for 48 hours, measure the diameter of the zone where no bacteria grow (inside the inhibition) to determine antibacterial activity. The results are shown in Table 3.

Table 3 Test product Control field 1 Control field 2 Diameter for inhibition 15 8 0 (mm) As shown in Table 3, control field 2 not containing oil-soluble licorice extract C
No inhibitory effect was observed at all. On the other hand, in Control Area 1, inhibition was observed only in the inner diameter portion of the cylinder, whereas in the test product containing both licorice extract C and Q-menthol, a large inhibition was formed, indicating strong antibacterial activity. .

[Effects of the Invention] According to the present invention, an oral composition containing a naturally-derived antibacterial agent and exhibiting excellent effects in preventing or treating dental caries or periodontal disease can be obtained.

Claims (5)

[Claims] (1) An oral composition characterized by containing an oil-soluble extract of licorice or its congenerous plants. (2) The oral composition according to claim (1), which contains the oil-soluble extract and l-menthol or l-carvone. (3) The oral composition according to claim (1) or (2), wherein the oil-soluble extract is glabridin or glabren. (4) The oral composition according to claim 1 or 2, wherein the oil-soluble extract is licochalcone A or licochalcone B. (5) Claim (1) wherein the oil-soluble extract is licocumaron.
) or the oral composition described in (2).