JPH0639375B2 - Anti-caries agent - Google Patents

Description

Description: TECHNICAL FIELD The present invention relates to an anti-caries agent, that is, an oral cavity agent for preventing caries or inhibiting the progress thereof.

[Conventional technology]

In recent years, the prevalence of dental caries, that is, caries has significantly increased, and has become a major social problem. On the other hand, along with this, research on the cause of caries is also progressing, and the current theory is that the cause of caries is that sucrose in food is changed by the action of cariogenic bacteria to produce insoluble and adhesive glucan. Has been done. The glucan thus produced causes dental caries-causing bacteria to adhere to the tooth surface and proliferate to form plaque. Then, based on this dental plaque, bacteria therein generate acid by sugar fermentation, and the acid causes caries to progress. To prevent dental caries, a method to increase tooth resistance, eliminate sucrose, use a sweetener instead of sucrose, decompose insoluble glucan produced from sucrose, or prevent glucan production or caries. Possible methods include eradication of the causative bacteria. Although each of the above methods has its merits and demerits, since the essence of caries is an infection caused by the caries-causing bacterium, it is considered that the elimination of the caries-causing bacterium that causes this is the most effective in preventing caries. . The above-mentioned bacteria include Streptococcus miutans.
Mutans) and Streptococcus sanguis (Sreptococc)
us Sanguis).

[Problems to be Solved by the Invention]

In order to prevent dental caries, many attempts have been made to eliminate such caries-causing bacteria. For example, the use of antibiotics such as penicillin and erythromycin, cell wall lytic enzymes that dissolve the cell wall of caries-causing bacteria, and bactericides such as cyclohexidine have been tried. However, these have a problem that the natural bacterial balance is destroyed by stirring the oral and intestinal bacterial flora, and side effects are caused. It has not been widely used because the problem of such side effects has not been solved. Therefore, the reality is that there is no decisive method to prevent caries, and there is no established preventive method that is superior to the physical method of cleaning after eating with a dipper. Is the current situation.

The present invention has been made in view of such circumstances, and an object thereof is to provide an anti-caries agent having no side effects and extremely high safety.

[Means for Solving the Problems]

In order to achieve the above object, the anti-caries agent of the present invention has a constitution in which at least the component (A) of the following components (A) and (B) is used as an active ingredient.

(A) At least three carboxylic acids selected from the group consisting of enanthic acid, capric acid, lauric acid, myristic acid, valmitic acid and vanillic acid.

(B) d-decalactone, d-dodecalactone, d-
At least 3 selected from the group consisting of undecalactone, d-tridecalactone and d-tetradecalactone
Seed lactone.

[Action]

In order to achieve the above-mentioned object, the present inventors have conducted a series of studies and, based on the hint that a certain fragrance has an antibacterial action, focus on the fragrance component, particularly the acid component and the lactone component, A series of studies were repeated. As a result, if three or more kinds of specific carboxylic acids are combined, or if this is used in combination with three or more kinds of specific lactone,
The inventors have found that the antibacterial action is remarkably improved as compared with the case where carboxylic acids and lactones are used alone, and arrived at the present invention.

Next, the present invention will be described in detail.

Heretofore, there have been reports that some of natural essential oils and active ingredients of natural essential oils have an antibacterial action against Escherichia coli, Shigella, etc. However, few reports have been found on the antibacterial properties of flavoring agents such as carboxylic acids. Therefore, the present inventors first measured the antibacterial activity against Mycobacterium bacillus, which is a relatively widely used carboxylic acid as the first step. The antibacterial activity was determined by using carboxylic acid as a 5% alcohol solution (this is the test component) and adding it to a heart infusion medium containing 5% sucrose at a ratio of 1/100 to 1/1000 (5%). % Alcohol solution ((test component)) concentration is 1/100 to 1/10
00) to solidify the medium, and then add the strain Myutans (Streptococcus migutans RIMD).
3125001) was punctured and inoculated and cultured at 37 ° C. for 72 hours or more, and the growth of bacteria in the medium and on the medium surface was observed and measured. Those having anti-myutans activity are shown in Table 1 below. The fact that it has anti-Myutans bacteria activity means that growth of Myutans bacteria is not observed when the test components are added at a ratio of 1/1000 and cultured at 37 ° C. for 72 hours or longer. Then, by diluting the concentration of the test component steadily, the reciprocal of the minimum concentration (effective growth inhibitory concentration) at which the anti-Myutans activity is recognized, for example, when the concentration of the test component is 1/1000, the reciprocal of 1000 It was shown as the anti-Myutans activity value. Table 1 shows the results of the same experiment using erythromycin, which is an antibiotic having a bactericidal action against magnolol, which is an active ingredient of the magnolia bark extract, and Myutans bacteria. The carboxylic acids listed in Table 1 show excellent anti-Myutans fungal activity equal to or higher than that of the magnolia bark extract known as an anti-caries agent (see JP-A-57-85319).

Thus, since carboxylic acids are extremely rich in anti-Myutans fungal activity, the search range was expanded to the field of lactones, which are also used as flavoring agents like carboxylic acids, and substances with anti-Myutans fungi activity were investigated. The results are shown in Table 2 below, and the lactones listed in the table had extremely high anti-Myutans activity.

Next, the perfume ingredients shown in Tables 1 and 2 were mixed and the anti-Myutans activity thereof was examined. The results are shown in Table 3 below, and anti-Myutans activity values higher than the arithmetic average of the anti-Myutans activity values of the perfume ingredients in Tables 1 and 2 were obtained. This indicates that a large synergistic effect can be obtained by using at least three kinds of the fragrance components shown in Tables 1 and 2. That is, in general, perfume components such as carboxylic acids and lactones are rarely used alone, and various components are mixed to form a desired scent,
Using this is done. Therefore, the first
It is extremely effective in practice that a large synergistic effect as shown in Table 3 can be obtained by using three or more kinds of the fragrance components shown in Tables and Table 2 together.

As described above, the anti-caries agent of the present invention is widely used in the food industry and the like, and is composed of a highly safe fragrance component that is actually used, so that no side effects occur. That is, although the anti-caries agent of the present invention has a slightly lower anti-caries effect as compared with the antibiotic erythromycin, the anti-caries agent of the present invention is not an antibiotic and thus causes side effects (internal microbiota). No agitation, appearance of resistant bacteria) and no problem at all even if used for a long period of time. Moreover, since the anti-caries agent of the present invention comprises a wide range of perfume ingredients such as carboxylic acids and lactones, it is possible to add an appropriate desirable flavor to the product to which the anti-caries agent is added by combining appropriate perfume ingredients. Like This effect is clinically effective considering that administration of an anti-caries agent is continued for a certain period of time, and especially for the prevention of dental caries, administration in infants around 1 year old when tooth eruption begins is desirable. , Is extremely useful.

Furthermore, since the anti-caries agent of the present invention can inhibit the growth of Myutans bacteria at an extremely low concentration, a large anti-caries effect can be obtained with a small amount of use.

〔The invention's effect〕

As described above, the anti-caries agent of the present invention has a great improvement in the anti-caries effect as compared with the case where they are used alone by combining three kinds of the specific acid component and the specific lactone used as the perfume ingredients. Can be realized.
Therefore, even if it is used in a small amount, it is effective, and since the acid component lactone component is used as a perfume component, side effects unlike conventional antibiotics do not occur at all. Can withstand long-term continuous use. The anti-caries agent of the present invention can be incorporated into mouthwashes, troches, toothpastes, chewing gum and the like.

Then, the anti-caries agent of the present invention is effective only by adding a predetermined amount as it is to the above-mentioned mouthwash, troche, brush and the like and mixing. For example, in the case of a mouthwash, the anti-caries agent is a 5% alcohol solution, and this is added to a 10% sucrose solution to a concentration of 1/3000 to 1/5000 (the same as the test component concentration hereinafter). So that it may be added.

Next, examples will be described.

[Example 1] The mixture of No. 1 shown in Table 3 was used as a target, and the activity of Myutans bacteria was determined. As a result, the effective growth inhibitory concentration against Myotans was 1/4000 (anti-Myutans activity 4000). Atsuta 5% of this No. 1 mixture
1/4000 of alcohol solution to 10% sucrose solution
No discomfort or irritation was felt even when added to the mouth to give a concentration of.

[Example 2] The mixture of No. 2 in Table 3 was examined, and the effective growth inhibitory concentration of this mixture against Mycobacterium was examined. As a result, the effective growth inhibitory concentration was 1/4000 (anti-Myutans activity 4
000). A 5% alcohol solution of this mixture was added to a 10% sucrose solution at a concentration of 1/4000 and contained in the mouth without causing any discomfort or irritation.

[Example 3] The mixture of No. 3 in Table 3 was examined, and the effective growth inhibitory concentration of this mixture against Myutans was examined. As a result, the effective inhibitory concentration was 1/4000 (anti-Myutans activity 4
000). A 5% alcohol solution of this mixture was added to a 10% sucrose solution at a concentration of 1/4000 and contained in the mouth without causing any discomfort or irritation.

Claims (1)

[Claims] 1. An anti-caries composition comprising at least the component (A) of the following components (A) and (B) as an active ingredient. (A) At least three carboxylic acids selected from the group consisting of enanthic acid, capric acid, lauric acid, myristic acid, palmitic acid and vanillic acid. (B) d-decalactone, d-dodecalactone, d-
At least 3 selected from the group consisting of undecalactone, d-tridecalactone and d-tetradecalactone
Seed lactone.