JP2004238375A - Bactericidal oral composition - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To obtain a bactericidal composition used for oral cavity, having a bactericidal effect on Actinobacillus actinomycetemcomitans. <P>SOLUTION: This bactericidal composition used for oral cavity contains anise oil as an active ingredient and is characterized by having the bactericidal effect on the Actinobacillus actinomycetemcomitans. <P>COPYRIGHT: (C)2004,JPO&NCIPI

Description

【００２５】
試験２
表２記載の供試製剤を用いて、試験１と同様の試験を行った。試験は５回反復して行い、その結果を表２に併記した。
実施例３〜５のとおり、メントール及び／又はチモールを併用することにより殺菌効果の増強が確認された。
【００２６】
【表２】

【００２７】
試験３
表２記載の実施例２〜５及び比較例３に塩化セチルピリジニウム０．０５ｇを加えた供試製剤（実施例６〜９、比較例５）を用いて、試験１と同様の試験を行った。ここでは対象細菌として、アクチノバチラス・アクチノミセテムコミタンス（Ａ．ａｃｔｉｎｏｍｙｃｅｔｅｍｃｏｍｉｔａｎｓ）カンジダ・アルビカンス（Ｃ．ａｌｂｉｃａｎｓ）、ポルフィロモナス・ジンジバリス（Ｐ．ｇｉｎｇｉｂａｒｉｓｅ）、ストレプトコッカス・ミュータンス（Ｓ．ｍｕｔａｎｓ）について評価した。試験は５回反復して行い、その結果を表３に示した。
実施例６〜９のとおり、アニス油、アニス油とメントール及び／又はチモールを併用することで、比較例５の塩化セチルピリジニウム単独と比べて殺菌効果の増強が確認され、殺菌スペクトラムも広いものとなった。
【００２８】
【表３】

【００２９】
試験４
製剤例２記載のマウスウォッシュを用いて刺激、香味の観点から、モニター１０名（男女各５名）により使用感を評価した。比較として、チモール、メントール、ユーカリプトール、サリチル酸メチルを有効成分とした殺菌性マウスウォッシュ（市販品）を用いた。試験は各マウスウォッシュ２０ｍｌを口に含み、３０秒間洗口した後、吐き出した。その結果は表４に示したとおり、刺激がなく、香味もよく、使用感に優れたものであった。
【００３０】
【表４】

【００３１】
【発明の効果】
本発明によって、若年性歯周炎の原因菌と考えられているアクチノバチラス・アクチノミセテムコミタンスに対して殺菌作用を有する、使用感に優れた殺菌性口腔用組成物を提供することができる。[0001]
TECHNICAL FIELD OF THE INVENTION
The present invention relates to a bactericidal oral composition having a bactericidal effect on Actinobacillus actinomycetemcomitans and having an excellent feeling in use.
[0002]
[Prior art]
In recent years, research on periodontal disease has been advanced, and it has been found that specific bacteria cause specific periodontal disease. Usually, in order to kill bacteria causing such periodontal diseases, cationic germicides such as cetylpyridinium chloride and benzethonium chloride are often used. However, when these cationic germicides are used at a high concentration, brown coloring may be observed on the teeth or the emergence of resistant bacteria may be promoted (for example, see Non-Patent Document 1). Further, these cationic bactericides tend to have a weak bactericidal effect against Actinobacillus actinomycetemcomitans, which is considered to be the causative bacterium of juvenile periodontitis.
[0003]
On the other hand, bactericidal mouthwashes containing thymol, menthol, eucalyptol, and methyl salicylate as active ingredients have been developed to solve the above-mentioned inconvenience, but they are used because of their unique irritation and flavor that affect taste. It was difficult.
[0004]
[Non-patent document 1]
Kiichi Iizuka et al., "Science of Dentifrice", Gakken Shoin, July 6, 1994, p. 80-85
[0005]
[Problems to be solved by the invention]
The present invention has been made in view of the above circumstances, and an object of the present invention is to have a bactericidal effect on Actinobacillus actinomycetemcomitans, a bactericidal oral composition having excellent feeling in use. It is to provide things.
[0006]
[Means for Solving the Problems]
The present inventors have conducted intensive studies in order to solve the above problems, and found that anise oil exerts an excellent bactericidal effect on Actinobacillus actinomycetemcomitans, and relates to a bactericidal oral composition. The present invention has been completed. That is, the present invention is achieved by the following configurations.
(1) A bactericidal oral composition comprising anise oil as an active ingredient and having a bactericidal effect on Actinobacillus actinomycetemcomitans.
(2) The bactericidal composition for oral cavity according to (1), wherein menthol and / or thymol are used in combination as an active ingredient.
(3) The bactericidal oral composition according to (1) or (2), which is a mouthwash.
[0007]
BEST MODE FOR CARRYING OUT THE INVENTION
As the anise oil which is an active ingredient of the present invention, essential oils obtained from anise of the family Apiaceae (Pimpinella anisum Linne) and a star anise of the magnolia family (Illicium verum Hooker fiilis) can be used. For example, ripe fruits of the aforementioned anise An essential oil obtained by steam distillation of the oil can be used.
[0008]
Anise oil may be contained in an amount of 0.01 to 5% by weight, preferably 0.02 to 1% by weight, based on the total amount of the bactericidal oral composition.
[0009]
Further, it is preferable to use menthol and / or thymol in combination as an active ingredient because the bactericidal effect on Actinobacillus actinomycetemcomitans is enhanced. Anise oil and menthol and / or thymol may be contained in a weight ratio of 10: 1 to 1:20, preferably 1: 1 to 1:10. As menthol, L-menthol is preferable from the viewpoint of the bactericidal effect, and essential oils such as menthol, mint oil containing thymol, herbal oil, citronella oil, and thyme oil may be used as long as the effects of the present invention are exhibited.
[0010]
The bactericidal composition for the oral cavity of the present invention can be a known preparation such as a dentifrice or a mouthwash, and is suitably used as a mouthwash which only requires washing the mouth.
Mouthwash may be prepared by a conventional method using water (purified water, ionized water, etc.), ethanol or the like as a solvent, and the pH is adjusted to 5 to 10, preferably 5.5 to 9 using a buffer. The feeling of use is improved. When the amount of ethanol used is 25% by weight or less, preferably 5 to 20% by weight based on the total amount of the mouthwash, the stimulation in the oral cavity may be reduced. In addition, as ethanol, besides ordinary ethanol, ethanol-based denatured alcohol denatured with various denaturants such as brucine, geraniol, and fragrance may be used.
[0011]
In addition, in order to smoothly dissolve, disperse, and solubilize the various components to be added, it is preferable to use a nonionic surfactant, such as glycerin fatty acid ester, sorbitan fatty acid ester, sucrose fatty acid ester, polyoxyethylene alkyl ether, or polyoxyethylene alkyl ether. Oxyethylene alkyl phenyl ether, polyoxyethylene polyoxypropylene glycol, polyethylene glycol fatty acid ester, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene hydrogenated castor oil, and the like.
[0012]
In the bactericidal oral composition of the present invention, various components used in this field can be used, if necessary, as long as the effects of the present invention are exhibited.
[0013]
These components include fluorides such as sodium fluoride and sodium monofluorophosphate; azulene, azulene sulfonate, β-glycyrrhetinic acid, glycyrrhizic acid and salts, dihydrocholesterol, epidihydrocholesterin, ouba extract, and touki extract Anti-inflammatory agents such as dl-α-tocopherol acetate, ε-aminocaproic acid, tranexamic acid; bactericides such as cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, chlorhexidine salts, triclosan, isopropylmethylphenol, alkyldiaminoethylglycine hydrochloride; Anticalculus agents such as gantrezic acid, zinc chloride, and organic acid zinc; hinokitiol, allantoin, allantoinchlorohydroxyaluminum, allantoindihydroxyaluminum, natochloride Astringents such as sodium; humectants such as glycerin, sorbitol, and polyethylene glycol; foaming agents such as sodium lauryl sulfate; α-pinene, peppermint oil, cinnamon oil, glove oil, eugenol, lemon oil, vanillin, cineol, eucalyptus oil, etc. Sweeteners such as saccharin, saccharin sodium, xylitol, erythitol, sorbitol, stevia, dipotassium glycyrrhizinate; blue No. 1, yellow 4, yellow 202 (1), green 3, yellow 201, red 102 And a preservative such as parabens and sodium benzoate; and a buffering agent such as monosodium dihydrogen phosphate and disodium monohydrogen phosphate.
[0014]
Other examples include aluminum lactate, potassium nitrate, shellac, beeswax, hydroxyapatite, sodium copper chlorophyllin, vitamins, calcium phosphates, essential oil components, plant extracts, and aroma components. The use of these components is not limited to the above.
[0015]
Examples of preferred formulations of the bactericidal oral composition are shown below, but the present invention is not limited thereto.
[0016]
(Formulation Example 1)
Anise oil 0.05g
Ethanol 20.00ml
9.00 g of concentrated glycerin
0.40 g of polyoxyethylene hydrogenated castor oil
Monosodium dihydrogen phosphate 0.07g
Disodium hydrogen phosphate 0.02g
Paraoxybenzoate 0.04g
Mint spice 0.10g
Purified water appropriate amount total 100.00ml
Was prepared.
[0017]
(Formulation Example 2)
Anise oil 0.02g
L-menthol 0.02g
Thymol 0.02g
Ethanol 20.00ml
9.00 g of concentrated glycerin
Polyoxyethylene hydrogenated castor oil 0.50g
Monosodium dihydrogen phosphate 0.12g
Disodium hydrogen phosphate 0.03g
Paraoxybenzoic acid ester 0.03 g
Xylitol 0.80g
Mint spice 0.10g
Purified water appropriate amount total 100.00ml
Was prepared.
[0018]
(Formulation Example 3)
Anise oil 0.02g
Cetylpyridinium chloride 0.05g
Ethanol 10.00ml
Sorbitol solution 15.00g
Polyoxyethylene hydrogenated castor oil 0.60g
Monosodium dihydrogen phosphate 0.08g
Disodium hydrogen phosphate 0.04g
Paraoxybenzoate 0.04g
Mint spice 0.10g
Purified water appropriate amount total 100.00ml
Was prepared.
[0019]
(Formulation Example 4)
Anise oil 0.02g
L-menthol 0.02g
Cetylpyridinium chloride 0.05g
Ethanol 10.00ml
Sorbitol solution 15.00g
Polyoxyethylene hydrogenated castor oil 0.60g
Monosodium dihydrogen phosphate 0.08g
Disodium hydrogen phosphate 0.04g
Paraoxybenzoate 0.04g
Mint spice 0.10g
Purified water appropriate amount total 100.00ml
Was prepared.
[0020]
(Formulation Example 5)
Anise oil 0.02g
L-menthol 0.02g
Thymol 0.02g
Cetylpyridinium chloride 0.05g
Dipotassium glycyrrhizinate 0.02g
Ethanol 20.00ml
9.00 g of concentrated glycerin
Polyoxyethylene hydrogenated castor oil 0.50g
Monosodium dihydrogen phosphate 0.12g
Disodium hydrogen phosphate 0.03g
Paraoxybenzoic acid ester 0.03 g
Xylitol 0.80g
Mint spice 0.10g
Purified water appropriate amount total 100.00ml
Was prepared.
[0021]
(Formulation Example 6)
L-menthol 0.02g
Thymol 0.02g
Anise oil 0.02g
Zinc chloride 0.10g
Ethanol 10.00ml
Concentrated glycerin 10.00g
Polyoxyethylene hydrogenated castor oil 0.60g
0.035 g of citric acid
0.125 g of sodium citrate
Paraoxybenzoate 0.01 g
Xylitol 0.02g
Blue No. 1 trace mint spice 0.18g
Purified water appropriate amount total 100.00ml
Was prepared.
[0022]
【Example】
Hereinafter, the present invention will be described in more detail by way of examples, but the present invention is not limited thereto.
[0023]
Test 1
0.1 ml of an inoculum (10 ⁶ to 10 ⁸ CFU / ml) of Actinobacillus actinomycetemcomitans cultured in a BHI medium was added to 0.4 ml of the test preparation described in Table 1, and mixed and stirred for 30 seconds. And sterilized. Among added and mixed SCDLP medium 10ml to 0.1ml, was further diluted 1 to 10 ^4, was further inoculated Among 0.1ml to TS blood agar. Then, the cells were cultured under anaerobic conditions at 37 ° C. for 2 days, the number of surviving bacteria (the number of colonies where proliferation of the bacteria was recognized) was counted, and the logarithm of the number of surviving bacteria was calculated and evaluated. The test was repeated five times, and the results are shown in Table 1.
In Example 1, the number of surviving bacteria (Log) reached a detection limit of 3.00, and a strong bactericidal effect was confirmed.
[0024]
[Table 1]

[0025]
Test 2
A test similar to Test 1 was performed using the test preparations shown in Table 2. The test was repeated five times, and the results are shown in Table 2.
As in Examples 3 to 5, it was confirmed that the bactericidal effect was enhanced by using menthol and / or thymol in combination.
[0026]
[Table 2]

[0027]
Test 3
A test similar to Test 1 was performed using test preparations (Examples 6 to 9 and Comparative Example 5) obtained by adding 0.05 g of cetylpyridinium chloride to Examples 2 to 5 and Comparative Example 3 described in Table 2. . Here, as target bacteria, Actinobacillus actinomycetemcomitans (A. actinomycetemcomitans) Candida albicans (C. albicans), Porphyromonas gingivalis (P. gingivalis), Streptococcus mutans (S.m. did. The test was repeated five times, and the results are shown in Table 3.
As in Examples 6 to 9, by using anise oil, anise oil and menthol and / or thymol in combination, it was confirmed that the bactericidal effect was enhanced as compared with cetylpyridinium chloride alone of Comparative Example 5, and the bactericidal spectrum was wide. became.
[0028]
[Table 3]

[0029]
Test 4
Using the mouthwash described in Formulation Example 2, the feeling of use was evaluated by 10 monitors (five men and women) from the viewpoint of irritation and flavor. For comparison, a bactericidal mouthwash (commercially available) containing thymol, menthol, eucalyptol, and methyl salicylate as active ingredients was used. The test contained 20 ml of each mouthwash in the mouth, rinsed for 30 seconds, and then exhaled. As shown in Table 4, the results were not irritating, had a good flavor, and were excellent in use feeling.
[0030]
[Table 4]

[0031]
【The invention's effect】
According to the present invention, it is possible to provide a bactericidal oral composition having a bactericidal effect on Actinobacillus actinomycetemcomitans, which is considered to be the causative bacterium of juvenile periodontitis, and having an excellent feeling in use. .

Claims (3)

A bactericidal oral composition comprising anise oil as an active ingredient and having a bactericidal effect on Actinobacillus actinomycetemcomitans. The bactericidal oral composition according to claim 1, wherein menthol and / or thymol are used in combination as an active ingredient. 3. The bactericidal oral composition according to claim 1, wherein the composition is a mouthwash.