JPH0432047B2 - - Google Patents

Description

[Detailed description of the invention]

[Industrial Application Field] This invention relates to an anti-caries composition, that is, a composition used to prevent caries or inhibit its progression. [Prior Art] In recent years, the prevalence of caries, that is, dental caries, has increased significantly and has developed into a major social problem. At the same time, research into the causes of caries is progressing, and the current theory is that the sucrose in food undergoes changes due to the action of caries-causing bacteria, producing insoluble and sticky glucans. It is said that Due to the glucan thus produced, caries-causing bacteria adhere to the tooth surface and multiply to form dental plaque. Using this plaque as a base, bacteria within it generate acid through sugar fermentation, and this acid causes dental caries to progress. To prevent caries, there are ways to increase tooth resistance, eliminate sucrose or use sweeteners instead of sucrose, break down the insoluble glucan produced by sucrose or prevent the production of glucan, or caries. Possible methods include eradicating the causative bacteria. Each of the above methods has advantages and disadvantages, but since caries is essentially an infection caused by caries-causing bacteria, eradicating the caries-causing bacteria is considered to be the most effective way to prevent caries. . The above bacteria include Streptococcus Mutans
and Streptococcus Sanguis. Many attempts have been made to eliminate such caries-causing bacteria in order to prevent caries. For example, attempts have been made to use antibiotics such as penicillin and erythromycin, cell wall lytic enzymes that dissolve the cell walls of caries-causing bacteria, and bactericidal agents such as cyclohexidine. [Problems to be Solved by the Invention] However, this method has the problem of disrupting the natural bacterial balance by disturbing the oral and intestinal flora, and causing side effects. Since the problem of such side effects has not been solved, it has not been widely used. In addition, attempts have been made to kill the caries-causing bacteria using hinokitiol, a component of the natural essential oil cypress oil, but the anti-caries properties of hinokitiol are also limited, and when used alone, loses its anti-caries properties relatively quickly. Therefore, even if it is added to something that is chewed for a relatively long time, such as chewing gum, a sufficient caries prevention effect cannot be expected. Therefore, the reality is that there is currently no definitive method for preventing dental caries.
Currently, no preventive method has been established that is superior to the physical method of cleaning with a toothbrush. The present invention was made in view of the above circumstances, and an object of the present invention is to provide an anti-caries composition that has no side effects, is highly safe, can be used repeatedly, and has an excellent caries preventive effect. [Means for Solving the Problem] In order to achieve the above object, the anti-caries composition of the present invention contains the following (A) component and (B) as active ingredients.
At least one of component (C) and component (D) is contained together with the components, and the content of component (A) is set to 0.01% by weight or more based on the total weight. (A) Hinokitiol. (B) At least one synthetic fragrance selected from the group consisting of cresyl acetate, cyclamenaldehyde, isoeugenol, heliotropin, ethyl salicylate, n-decanal, p-methylacetophenone, and methyleugenol. (C) _C3 to _C18 carboxylic acid. (D) _C9 - _C14 lactones. [Effect] Specifically, the present inventors focused on the excellent anti-caries properties of hinokitiol itself, and conducted a series of studies focusing on improving its caries-preventing effect. As a result, it was found that when hinokitiol is not used alone but in combination with various other compounds, the caries prevention effect increases depending on the combination of compounds. As a result of further research, it was found that among the various compounds mentioned above, a specific carboxylic acid and a specific lactone are the most effective in terms of effectiveness, and when they are combined with a specific synthetic fragrance, the effect is further increased. This invention was achieved by discovering the following. As described above, the greatest feature of this invention is that hinokitiol, which has no side effects and is extremely safe, carboxylic acid, lactone, and synthetic fragrance are used as the active ingredients of the anti-caries composition. Next, this invention will be explained in detail. There are reports that natural essential oils, natural substances, fragrance compounds, or certain of their active ingredients have antibacterial effects. However, there are no reports regarding antibacterial activity against Myutans bacteria, which has the strongest cariogenic effect. Therefore, prior to confirming the antibacterial effect of hinokitiol, the present inventors first measured the antibacterial activity against B. mutans using natural essential oils that have been reported to have any antibacterial effect or are relatively widely used. The antibacterial activity of each of the above natural essential oils is
% alcohol solution (this is used as the test component), and this is added to a heart infusion medium containing 5% moss etc., so that the ratio of natural essential oil to the entire medium is 1/100 to 1/1000 (5%). % alcohol solution so that the concentration of natural essential oil is 1/100 to 1/1000), and after the medium has solidified, add Streptococcus miutans.
RIMD3125001) was inoculated by puncture and cultured at 37°C for 72 hours or more, and the growth of the bacteria in the medium and on the surface of the medium was observed and measured. Those having anti-myutans activity are shown in Table 1 below. Anti-myutans activity means that natural essential oil is added to the culture medium at a ratio of 1/1000 and incubated at 37°C.
This means that no growth of M. myutans was observed when cultured for 72 hours or more. Then, the concentration of natural essential oil in the test component is gradually diluted, and the reciprocal of the minimum concentration (effective growth inhibitory concentration) at which antimyutans activity is observed, for example, when the concentration of natural essential oil is 1/1000, reciprocal
1000 was shown as the antimyutans activity value. Similar experiments were conducted using Atsuboku extract, Magnolol, which is an active ingredient of Atsubaku extract, and erythromycin, an antibiotic that has a bactericidal effect on B. myutans, and are shown in Table 1.
The natural essential oils listed in Table 1 are Koboku extract (see Japanese Patent Application Laid-Open No. 57-85319), which is known as an anti-caries agent.
shows superior antimyutans activity. In this way, since the active ingredients of natural essential oils are extremely rich in anti-myutans activity, we have expanded the scope of our search to the field of synthetic fragrances and flavoring agents such as carboxylic acids and lactones to find substances with anti-myutans activity. Examined. The results are shown in Table 2 below. The synthetic fragrances, carboxylic acids, and lactones listed in Table 2 had extremely high antimyutans activity. Next, hinokitiol was used as an essential component, and the components shown in Tables 1 and 2 above were mixed therewith to examine its antimyutans activity. The results are shown in Table 3 below.

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〔Effect of the invention〕

As described above, the anti-caries composition of the present invention contains hinokitiol, a specific synthetic fragrance, and one or both of a specific carboxylic acid and a specific lactone as active ingredients, and the above-mentioned hinokitiol is contained in a total amount of By setting it at 0.01% by weight or more and combining it with the above-mentioned components, an excellent anti-caries effect can be obtained, making it ideal for gargles, troches, toothpastes, chewing gums, etc. Moreover, its use does not cause any side effects unlike those of conventional antibiotics, and it is highly practical as it can withstand long-term use. Next, the present invention will be explained based on examples and in comparison with comparative examples. However, in the following examples, excellent synergistic effects were obtained by mixing hinokitiol with other ingredients, and the mixtures shown in Table 3 were used. Comparative Example 1 Targeting the No. 1 mixture listed in Table 3,
When the activity of B. myutans was determined, the effective growth-inhibiting concentration against B. myutans was 1/
10,000 (antimyutans activity 10,000). Comparative Example 2 The effective growth-inhibiting concentration against B. myutans was investigated using the mixture No. 2 in Table 3, and the effective growth-inhibiting concentration was found to be 1/8000 (anti-Myutans activity: 8000). Comparative Example 3 Using the mixture No. 3 in Table 3, its effective growth-inhibiting concentration against P. myutans was determined. The effective growth-inhibiting concentration of this product was 1/8000 (anti-Myutans activity 8000). Comparative Example 4 Targeting the mixture No. 4 in Table 3, the effective growth-inhibiting concentration of this mixture against B. myutans was determined. As a result, the effective growth inhibitory concentration was 1/6000
(Anti-myutans activity 6000). Example 1 Targeting the mixture No. 5 in Table 3, the effective growth-inhibiting concentration corresponding to P. myutans was determined. The effective growth-inhibiting concentration of this product was 1/10,000 (anti-myutans activity 10,000). This mixture has a spicy floral flavor, and even if you add a 5% alcohol solution of this mixture to a 10% sucrose solution at a ratio of 1/10,000 and put it in your mouth, you will not feel any discomfort or irritation at all. Ta. Comparative Example 5 Using the mixture No. 6 in Table 3, its effective growth-inhibiting concentration against P. myutans was determined. The effective growth-inhibiting concentration of this product was 1/8000 (anti-Myutans activity 8000). Example 2 Targeting the mixture No. 7 in Table 3, the effective growth-inhibiting concentration against B. myutans was determined.
The effective growth-inhibiting concentration of this product was 1/9000 (anti-Myutans activity 9000). This mixture is
The spicy flavor with a strong fatty acid odor of No. 3 becomes milder and has a refreshing aftertaste.A 5% alcohol solution of No. 3 is added to a 10% sucrose solution at a ratio of 1/10,000 and tasted. Even when containing hinokitiol, no discomfort or irritation caused by hinokitiol or the like was felt at all. Example 3 Targeting the mixture No. 8 in Table 3, the effective growth-inhibiting concentration against B. myutans was determined.
The effective growth-inhibiting concentration of this product was 1/7000 (anti-myutans activity 7000). This mixture is
The spicy fruit flavor of No. 4 becomes milder and has a refreshing lingering aroma.
Even when it was added at a ratio of 10,000% and taken into the mouth, no discomfort or irritation caused by hinokitiol or the like was felt at all.

Claims (1)

[Claims] 1. At least one of the following components (A) and (B) as well as components (C) and (D) is contained as active ingredients, and the content of the above (A) component is for the whole
An anti-caries composition characterized by having a caries content of 0.01% by weight or more. (A) Hinokitiol. (B) At least one synthetic fragrance selected from the group consisting of cresyl acetate, cyclamenaldehyde, isoeugenol, heliotropin, ethyl salicylate, n-decanal, p-methylacetophenone, and methyleugenol. (C) _C3 to _C18 carboxylic acid. (D) _C9 - _C14 lactones.