JP2005289953A - ANTIBACTERIAL AGENT COMPRISING METHYL p-HYDROXYBENZOATE AS ACTIVE INGREDIENT AND EXTERNAL COMPOSITION COMPRISING THE SAME - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To obtain an antibacterial agent having excellent antibacterial actions on bacteria of Corynebacterium sp. considered as a cause of a body odor (osmidrosis axillae) and to obtain an external composition comprising the antibacterial agent. <P>SOLUTION: The antibacterial agent against the bacteria of the Corynebacterium sp. comprises methyl p-hydroxybenzoate as an active ingredient. The external composition comprises the antibacterial agent. <P>COPYRIGHT: (C)2006,JPO&NCIPI

Description

  The present invention relates to an antibacterial agent containing methyl paraoxybenzoate as an active ingredient and a composition for external use containing the antibacterial agent.

  The unpleasant odor associated with sweating is known to be caused by the decomposition of the odorless and sterile sweat by microorganisms on the skin surface. When ammonia in the skin surface or sweat is added to this, a more specific odor is generated. It becomes. In particular, the vomiting odor, which is a peculiar odor of body odor, has a certain balance between corynebacterium sp. And epidermis staphylococci that have apocrine sweat secreted from the apocrine sweat glands in the axilla. A group of bacteria that are kept and fixed on the skin is referred to as skin flora) (see, for example, Non-Patent Document 1) Among these skin flora, It is known to be a genus Corynebacterium.

  Conventionally, antiperspirants, antiperspirant astringents, antibiotics or antibacterial agents have been used to suppress the generation of body odor. However, antiperspirants and antiperspirant astringents are not very effective for people with a high amount of sweat, especially antiperspirant astringents made of aluminum salts such as hydroxyaluminum chloride (aluminum chloride hydrate). There is a problem that it is highly irritating to the skin due to its degenerative action. In addition, although antibacterial agents and antibiotics such as benzethonium chloride and benzalkonium chloride are highly effective, not only microorganisms that cause body odor but also microorganisms that form skin flora will be sterilized or bacteriostatic, There is a risk that the skin's original self-cleaning action is impaired due to the formation of healthy skin flora.

Therefore, in order to develop a method for preventing an unpleasant body odor, it is necessary to find an antibacterial agent having a bactericidal action selective to the bacteria that cause the unpleasant odor.
Hurley, H.C. J. et al. Jr. : Diseases of apocrinesweats grands. Dermatology in General Medine. p. 386, McGraw-Hill, New York (1971)

  The main object of the present invention is to provide an antibacterial agent having an excellent antibacterial action against Corynebacterium which is a cause of a bad odor, and an external composition containing the antibacterial agent.

  The present inventors have found that among paraoxybenzoic acids conventionally used as preservatives, methyl paraoxybenzoate has an excellent antibacterial action against Corynebacterium, and the present invention It came to be completed.

The present invention provides the following antibacterial agents and compositions for external use.
Item 1. An antibacterial agent against Corynebacterium which contains methyl paraoxybenzoate as an active ingredient.
Item 2. Item 2. The antibacterial agent according to item 1, wherein the Corynebacterium is Corynebacterium xerosis, Corynebacterium minutishima or Corynebacterium tenuis.
Item 3. Item 3. The antibacterial agent according to any one of Items 1 and 2, which contains 0.2% by weight or more of methyl paraoxybenzoate.
Item 4. Item 4. The antibacterial agent according to any one of Items 1 to 3, further comprising a skin retention agent.
Item 5. Item 5. The antibacterial agent according to Item 4, wherein the skin retention agent is propylene glycol.
Item 6. Item 6. An external composition containing the antibacterial agent according to any one of Items 1 to 5.
Item 7. Item 7. The composition for external use according to Item 6, which is used for preventing odor.

  As the methyl paraoxybenzoate which is an active ingredient of the antibacterial agent of the present invention, those used in the fields of pharmaceuticals, quasi drugs, cosmetics and foods can be widely used. The methyl paraoxybenzoate may be in the form of a salt, and examples of such a salt include alkali metal salts such as methyl sodium paraoxybenzoate. Methyl paraoxybenzoate or a salt thereof can be used alone or in any combination of two or more.

  As shown in the Examples, the antibacterial agent of the present invention is characterized by having an excellent antibacterial effect against Corynebacterium sp. Here, Corynebacterium sp. Is not particularly limited as long as it is a gram-positive gonococcus in the category of this genus, but is preferably a bacterium that causes generation of odor (hereinafter referred to as odor bacterium in the present invention). Examples of such malodorous bacteria include Corynebacterium minutisium, Corynebacterium xerosis, Corynebacterium tenuis, and the like.

  When an antibacterial agent containing methyl paraoxybenzoate as an active ingredient is prepared, the bactericidal action against the genus Corynebacterium is an amount exceeding about 0.1% by weight, preferably 0.15, as an effective amount of methyl paraoxybenzoate. It is about wt% or more, more preferably about 0.2 wt% or more.

  A low volatility and low skin permeability skin retention agent such as propylene glycol, dipropylene glycol, 1,3-butylene glycol can be blended with the antibacterial agent containing methyl paraoxybenzoate as an active ingredient. When used in combination with the antibacterial agent of the present invention, propylene glycol is particularly preferable as the skin retention agent. By using these skin retention agents in combination, the antibacterial agent of the present invention can be retained on the skin, and an antibacterial effect can be obtained for a long time.

  The blending amount of the skin retention agent in the antibacterial agent is not particularly limited as long as it can be retained for a time sufficient to exert an antibacterial action and does not interfere with the effects of the present invention. About 50% by weight, preferably about 5-40% by weight, more preferably about 10-30% by weight.

  Furthermore, the antibacterial agent of the present invention can contain other antibacterial components as components other than methyl paraoxybenzoate as long as the effects of the present invention are not hindered. Specific examples of such antibacterial components include triclosan, trichlorocarbanilide, benzalkonium chloride, benzethonium chloride, halocarban, chlorhexidine hydrochloride, dihydrofarnesol, isopropylmethylphenol, thymol, hinokitiol, cetylpyridinium chloride, ethanol, isopropanol, etc. Can be illustrated. When these antibacterial components are contained in the antibacterial agent of the present invention, methyl paraoxybenzoate can be expected to exhibit an antibacterial action in an amount smaller than the above-mentioned effective amount. Therefore, the effective amount of methyl paraoxybenzoate in the antibacterial agent of the present invention is not limited to the above-described range (amount exceeding 0.1% by weight).

  Since the antibacterial agent of the present invention has an antibacterial action against Corynebacterium sp. Existing in the skin, it can be used as an antibacterial component in an external composition. In particular, the antibacterial agent of the present invention can be used as an antibacterial component of a composition for external use for preventing a bad smell because it exhibits an excellent bactericidal action against bad smell bacteria. In this case, the proportion of the antibacterial agent of the present invention to the composition for external use may be an amount in which the active ingredient methyl paraoxybenzoate exhibits an antibacterial effect against Corynebacterium, and in this range Although not particularly limited, specifically, the amount of methyl paraoxybenzoate in the external composition exceeds about 0.1% by weight, preferably about 0.15% by weight or more, more preferably 0.2% by weight. It is desirable that it be included within a range of more than about.

  The present invention also provides a composition for external use thus prepared. The composition for external use can be widely used in the fields of pharmaceuticals, quasi-drugs, and cosmetics (cosmetics) for the purpose of preventing odor. The form is not particularly limited, and cream, ointment, lotion, spray, aerosol, emulsion, foam, cleaning agent, soap, bath preparation, skin conditioner, lotion, pack agent, foundation and the above antibacterial agent are formed into a sheet-like base material. According to usage forms such as a sheet agent, a patch or a poultice, a roll-on agent, etc. impregnated into a liquid, it is appropriately prepared in a liquid, semi-solid, bubble and solid form.

  In addition to the above-mentioned antibacterial agent containing methyl paraoxybenzoate as an active ingredient, the composition for external use generally comprises a carrier generally incorporated in the composition for external use according to various forms; an antiseptic, a preservative, a stabilizer, a precipitate Contains various additives such as inhibitors, pH adjusters, fragrances, surfactants (anionic, cationic, nonionic, amphoteric surfactants), colorants, refining agents, viscosity modifiers, bactericidal antibacterial agents, and essential oils. can do. Such carriers and additives are preferably those that are safe for the human body, and more preferably those that are not irritating to the skin or the like.

  Examples of the carrier include water (for example, ion-exchanged water), alcohol (for example, ethanol), and a water-soluble solvent (for example, propylene glycol and glycerin) in the case of a liquid form, and various gellings in the case of a solid form. Agents (for example, seaweed polysaccharides such as carrageenan and sodium alginate; seed polysaccharides such as guar gum and tamarind seed gum; plant sap polysaccharides such as gum arabic and tragacanth gum; fermentation polysaccharides such as xanthan gum and gellan gum; proteins such as gelatin; And cellulose derivatives such as carboxymethyl cellulose); inorganic materials such as talc and silica; and polyacrylic acids such as sodium polyacrylate.

  Examples of preservatives include benzoic acid, sorbic acid, propionic acid, dehydroacetic acid, salicylic acid, edetic acid and their salts; inorganic salts such as sodium sulfite, sodium hyposulfite and sodium pyrosulfite; plant-derived components such as pectin extract It can be illustrated.

  Examples of suspending agents include fine particle powders such as silicon dioxide and magnesium stearate, surfactants such as polyoxyethylene hydrogenated castor oil and polyoxyethylene sorbitan monostearate, and gelling agents such as xanthan gum and polyethylene glycol. can do.

  Examples of the pH adjuster include citric acid, fumaric acid, DL-malic acid and salts thereof; carbonates such as sodium hydrogen carbonate and potassium carbonate; phosphates such as phosphoric acid and sodium dihydrogen phosphate; it can.

  The various components described above are merely examples, and the present invention is not limited to these components. That is, in the external preparation for skin of the present invention, various components that are usually used as components for external preparations can be used, including other additive components.

  The composition for external use of the present invention, especially the composition for external use for preventing odor, is an effect of preventing the generation of odor and sweat odor based on the bactericidal action against Corynebacterium, particularly the odor bacterium causing the generation of odor. Is excellent. Therefore, the composition for external use can be positioned as a deodorant (anti-body odorant) used for suppressing the generation of a foul odor or sweat odor from another viewpoint, particularly as a deodorant.

  Furthermore, the composition for external use of the present invention is prepared in a form such as a spray or aerosol, a laundry finish or a coating agent in addition to a use form directly applied to the skin (skin surface) where Corynebacterium is present. Thus, it can be used in a use mode in which spraying, dipping or coating is applied to clothing such as underwear or shirt to which Corynebacterium is attached (or possibly attached).

  In addition to the above-mentioned other antibacterial components, the deodorant of the present invention (anti-body deodorant, anti-deodorant) is blended in clothing sprays, aerosols, etc. in addition to the above antibacterial components. Known preservatives, preservatives, stabilizers, precipitation inhibitors, pH adjusters, fragrances, surfactants (anionic, cationic, nonionic, amphoteric surfactants), clarifiers, viscosity modifiers, bactericides Various additives such as antibacterial agents can be blended. Such carriers and additives are preferably those that are safe for the human body, and more preferably those that are not irritating to the skin or the like.

  According to the present invention, it is possible to provide an antibacterial agent having an excellent antibacterial action against Corynebacterium, and an external composition containing the antibacterial agent. Furthermore, by containing propylene glycol having low volatility and low skin permeability in the antibacterial agent, the antibacterial agent capable of exerting an antibacterial effect for a long time by containing on the skin for a long time and the antibacterial agent are contained. An external composition can be provided.

  EXAMPLES Hereinafter, although an Example and a formulation example are given and this invention is demonstrated concretely, this invention is not limited to these Examples at all.

Test method Antibacterial activity was evaluated by measuring the inhibition circle diameter by the paper disk method.

  Corynebacterium minutishimam was applied to trypticase soy agar medium, and the cells were enriched at 35 ° C. for 24 hours, and then suspended in sterilized physiological saline to have Macfarand 0.5.

  Apply 50 μL of this suspension uniformly on a trypticase soy agar medium in a petri dish with a conical rod, and place a paper disk (diameter 8 mm) on the sample (methyl paraoxybenzoate, ethyl paraoxybenzoate or 50 μL of propyl paraoxybenzoate) was impregnated. After incubation at 35 ° C. for 24 hours, the presence or absence of a blocking circle and its diameter were measured.

Test results In 0.2% by weight of methyl paraoxybenzoate, inhibition circle formation was observed, but no inhibition circle formation was observed at other concentrations. Further, in the case of ethyl paraoxybenzoate and propyl paraoxybenzoate, no inhibition circle formation was observed at any concentration of 0.01% by weight, 0.1% by weight or 0.2% by weight.

  Therefore, it was found that 0.2% by weight of methyl paraoxybenzoate has an antibacterial action against Corynebacterium minutisimam.

  When 0.01%, 0.1%, or 0.2% by weight of methyl paraoxybenzoate, ethyl paraoxybenzoate, or propyl paraoxybenzoate is used, and 5% by weight, 10% by weight, or 20% by weight of propylene glycol Table 1 shows the results of measurement by the paper disk method when% is used.

表２は、パラオキシ安息香酸メチルとプロピレングリコールを併用した場合のペーパーディスク法による測定結果を示す。

Table 2 shows the measurement results by the paper disk method when methyl paraoxybenzoate and propylene glycol are used in combination.

表３は、パラオキシ安息香酸エチルとプロピレングリコールを併用した場合のペーパーディスク法による測定結果を示す。

Table 3 shows the measurement results by the paper disk method when ethyl paraoxybenzoate and propylene glycol are used in combination.

表４は、パラオキシ安息香酸プロピルとプロピレングリコールを併用した場合のペーパーディスク法による測定結果を示す。

Table 4 shows the measurement results by the paper disk method when propyl paraoxybenzoate and propylene glycol are used in combination.

  Hereinafter, although the formulation example of the formulation using methyl paraoxybenzoate is shown, this invention is not limited to this.

[Prescription Example 1]
[G]
Ointment Methyl paraoxybenzoate 0.2
Dipotassium glycyrrhizinate 0.5
Bentonite 25
Kaolin 25
Glycerin 15
Propylene glycol 10
Purified water 24.3
Total 100

[Prescription Example 2]
Liquid [g]
Polyoxyethylene oleyl ether 1
Ethanol 10
Methyl paraoxybenzoate 0.2
Purified water 88.8
Total 100

[Prescription Example 3]
Aerosol [g]
Propylene glycol 20
Methyl paraoxybenzoate 0.2
Isopropyl methylphenol 0.1
Purified water 24.9
Liquefied petroleum gas 50
Total 100

Claims (7)

  Antibacterial agent against Corynebacterium spp. Containing methyl paraoxybenzoate as an active ingredient.   The antibacterial agent according to claim 1, wherein the Corynebacterium is Corynebacterium xerosis, Corynebacterium minutishima or Corynebacterium tenuis.   The antibacterial agent in any one of Claim 1 or 2 containing 0.2 weight% or more of methyl paraoxybenzoates.   Furthermore, the antibacterial agent in any one of Claims 1-3 containing a skin retention agent.   The antibacterial agent according to claim 4, wherein the skin retention agent is propylene glycol.   The composition for external use containing the antibacterial agent in any one of Claims 1-5.   The composition for external use according to claim 6, which is used for preventing odor.