JPH049330A - Anti-trichophyte agent - Google Patents

Abstract

PURPOSE:To obtain a powerful remedy for athlete's foot, containing a benzoquinone derivative as an active ingredient and having powerful anti- trichophyte action and further excellent permeating action on the skin. CONSTITUTION:A remedy for athlete's foot, containing a benzoquinone derivative such as methylbenzoquinone, methoxybenzoquinone, hydroxybenzoquinone and 2,3-dimethoxy-5-methyl-p-benzoquinone as an active ingredient, having growth inhibitory action on trichophytes causing the athlete's foot and capable of exhibiting powerful treating effects by application thereof to affected parts.

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to an anti-white fungus agent that exhibits a growth inhibiting effect on white fungus that causes athlete's foot.

[Conventional technology]

Conventionally, various antibacterial agents have been used to inhibit the growth of the white fungus that causes athlete's foot. (Japanese Patent Application Laid-Open No. 54-143514)
, oligoglycosides (JP-A-56-83500), propargyl alcohol (JP-A-56-116013), sweet potato juice (JP-A-56-166120), trihaloallyl derivatives, JP-A-57 -11602
6), Ostol (JP-A-58-167512), benzisothiazoline derivatives (JP-A-58-1)
77982), antibiotic 5I-4228 (JP 62-294619), Warburganal and Polygodial (JP 63-156718), trinaftate (JP 63-208517), etc. be.

[Problem to be solved by the invention]

However, as a treatment for athlete's foot, it is necessary to have an action that penetrates into the skin in addition to an anti-white fungus effect, and conventional technology has not yet been able to completely inhibit the growth of white skin fungus in the skin. has not yet been reached.

[Means to solve the problem]

As a result of extensive research aimed at resolving the drawbacks of these conventional therapeutic agents for athlete's foot, the present inventors discovered that a benzoquinone derivative, which had never been used as an anti-fungal agent, was found to be highly effective. They discovered that it not only has a strong anti-whitening effect but also has an excellent skin penetration effect, leading to the completion of the present invention.

Specifically, the present invention relates to an anti-white leprosy agent containing a benzoquinone derivative as an active ingredient, and provides a powerful therapeutic agent for athlete's foot.

The present invention will be explained in more detail below.

The benzoquinone derivatives used in the present invention include 1,2- or l,4-benzoquinone derivatives such as ubiquinone, plastoquinone, embelin, labanone, and mesaquinone, and among them, methyl groups, methoxy groups, hydroxyl groups, etc. are included in the molecule. Methylbenzoquinone, methoxybenzoquinone, hydroxybenzoquinone, and 2,3-dimethoxy-5-methylbarabenzoquinone have particularly excellent anti-whitening action and skin penetration action.

In the present invention, either synthetic or natural benzoquinone can be used as the benzoquinone that is a raw material for the benzoquinone derivative.

In the case of natural benzoquinone, natural raw materials such as actinomycetes, koji, bamboo, and wheat are ground using a ball mill, etc., and then extracted with a solvent such as ethanol, ether, or acetone, and the solvent is evaporated to produce a benzoquinone-containing extract. get. In this case, if necessary, a highly concentrated benzoquinone-containing extract can be obtained by further purification by chromatography using a reversed-phase packing material such as octadecyl chemically bonded silica gel.

The antifungal agent of the present invention contains other antibacterial agents as a synergist, such as alcohol, spices, organic acids, known antibiotics, etc., in an amount of 0.00 parts by weight per 100 parts by weight of the benzoquinone derivative.
It can be added in an amount of 1 to 1000 parts by weight.

Furthermore, in order to improve the permeation effect of the anti-white germ agent of the present invention into the skin, 0.1 to 100% of polyhydric alcohol fatty acid ester such as fatty acid monoglyceride or sorbitan fatty acid ester is added to 100 parts by weight of the benzoquinone derivative. 100
It may be added within the range of 0 parts by weight.

When using the antifungal agent of the present invention, mix it with a suitable base such as ethanol and apply it to the affected area.
The fungus that causes athlete's foot is Trichophyton I.
terdigitale), [Microsporium gypseum J
um) can be prevented from growing. At this time, the concentration of the benzoquinone derivative with respect to the base is 10 to
It is preferable that it is 20000 ppm, and the concentration is 10 p.
If the amount is less than pm, the growth inhibiting effect on the white fungus cannot be obtained, and even if it exceeds 20,000 ppm, the growth inhibiting effect will not be so high.

〔Effect of the invention〕

The antifungal agent of the present invention has a growth inhibiting effect on the fungus that causes athlete's foot, and by applying it to the affected area, a strong therapeutic effect can be expected.

[Examples, comparative examples, usage examples]

Hereinafter, the present invention will be explained in more detail with reference to Examples, Comparative Examples, and Usage Examples.

Example 5, 10, and 25.50 ppm of the benzoquinone derivatives shown in Table 1 (manufactured by Tokyo Chemical Industry Co., Ltd.) were added to a Sabouraud agar medium (Eiken Chemical Co., Ltd. M) and sterilized.

Next, the sterilized medium was placed in a sterile petri dish at 10 mΩ.
The mixture was poured one by one and allowed to cool and solidify. Separately, white fatigue bacteria [Trichophyton interdigital KF-62J] cultured in ordinary broth (manufactured by Eiken Kagaku Co., Ltd.) for 24 hours were used.
and Microsporum gypseum KF-64J suspensions of 5 μΩ were inoculated onto a sterilized medium that had been left to solidify.

After inoculation, the cells were cultured at 30° C. for 48 hours, and the minimum concentration of benzoquinone derivatives required to inhibit the growth of the two types of white fungi was determined for each petri dish. The results are shown in Table 1.

Comparative Example The comparative antibacterial agents shown in Tables 2 and 2 were used to control the growth of white fungus in accordance with the example except that the amount of the comparative antibacterial agent used to sterilize the Sabouraud agar medium was 100, 200, 400, and 11000 pp. The minimum concentration of comparator antimicrobial agent required to achieve inhibition was determined. The results are shown in Table 2.

Example of Use Sample numbers 1 and 2.3 of the benzoquinone derivative of the present invention shown in Table 1 and sample numbers 3 and 5.8 of the comparative antibacterial agent shown in Table 2 were used as active ingredients, and the synergistic effects shown in Table 3 were used as active ingredients. Using the formulations shown in Table 3, formulations 1 to 3 of the products of the present invention and formulations 4 to 6 of comparative products were obtained using the formulations shown in Table 3.

The obtained formulations 1 to 6 were each applied to 20 people infected with athlete's foot three times a day (Ig per application) for one month, and the number of cured patients was determined.

The results are shown in Table 3.

From the results of the above Examples, Comparative Examples, and Usage Examples, it is clear that the anti-white leprosy agent of the present invention has a strong anti-white leprosy effect and exhibits an excellent therapeutic effect against athlete's foot.

Special permission Out wish Man teenager Reason Man Nippon Oil & Fats Co., Ltd.

Claims (1)

[Claims] An antifungal agent containing a benzoquinone derivative as an active ingredient.