JP2005232056A - Antibacterial and antifungal agent - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide an antibacterial and antifungal agent having high antibacterial and antifungal activities and high in safety. <P>SOLUTION: The antibacterial/antifungal agent consists of benzyl oxyethanol. The antiseptic consists of benzyl oxyethanol and a paraben. <P>COPYRIGHT: (C)2005,JPO&NCIPI

Description

  The present invention relates to an antibacterial and antifungal agent and an antiseptic that can be used in medicines, miscellaneous goods and the like.

  Conventionally, in order to prevent alteration due to contamination of microorganisms such as bacteria and fungi at the time of manufacture and use, or to suppress the growth of bacteria, pharmaceuticals and the like have paraoxybenzoic acid according to the characteristics of the product. Preservatives and antibacterial antifungal agents such as esters and salts thereof, sodium benzoate and salts thereof, dehydroacetic acid and salts thereof, benzalkonium chloride, methylchloroisothiazolion (Caisson CG), and triclosan are blended.

  However, such antiseptics and antibacterial and antifungal agents have been reported to be irritating, sensitizing, etc., and their amount is often regulated from the viewpoint of safety. Often cannot be formulated. Therefore, an antibacterial agent having superior antibacterial activity and high safety is required.

On the other hand, benzyloxyethanol has an effect of increasing the penetration rate of hair treatment components into hair, and is blended in hair treatment agents and hair dyes as penetration enhancers (see, for example, Patent Documents 1 and 2). However, it is not known at all that benzyloxyethanol has antibacterial and antifungal activity.
Japanese Patent No. 1952826 Japanese Patent No. 1991404

  An object of the present invention is to provide an antibacterial and antifungal agent having a superior antibacterial and antifungal activity and high safety, and a preservative.

  The present inventors searched for a highly safe substance having antibacterial and antifungal activity, and as a result, benzyloxyethanol has an excellent antibacterial and antifungal activity. Further, when benzyloxyethanol and parabens are combined, the antibacterial activity is increased. Has been found to improve synergistically.

  That is, the present invention provides an antibacterial and antifungal agent or preservative comprising benzyloxyethanol.

  The present invention also provides a preservative comprising benzyloxyethanol and parabens.

  The present invention also provides an antibacterial and antifungal agent or preservative containing benzyloxyethanol as an active ingredient.

  The present invention also provides an antibacterial and antifungal agent comprising benzyloxyethanol and parabens as active ingredients.

  The antibacterial and antifungal agent or preservative of the present invention has an excellent antibacterial and antifungal or antiseptic effect.

  Benzyloxyethanol is a known substance, can be produced using a known method, and a commercially available product can also be used. For example, trade name: benzyl glycol (BzG) (manufactured by Nippon Emulsifier Co., Ltd.) can be used.

  As is apparent from the examples below, benzyloxyethanol alone exhibits excellent antibacterial activity against bacteria, fungi, and the like, and when combined with parabens that are used as antibacterial and antifungal agents, Its antibacterial power is dramatically improved. Therefore, benzyloxyethanol, or benzyloxyethanol and parabens, can be used as they are as antibacterial and antifungal agents or preservatives, and are usually added to pharmaceuticals, quasi drugs and household antibacterial products. For the purpose of preventing microbial alteration of products such as pharmaceuticals, quasi-drugs, household products, etc., or pharmaceuticals, quasi-drugs, household products, sundries, etc. It can be used in products.

In particular, a combination of benzyloxyethanol and parabens is useful as a preservative that exhibits superior antibacterial activity. Here, examples of the parabens include paraoxybenzoic acid esters and salts thereof, and specific examples include methyl paraben, ethyl paraben, propyl paraben, butyl paraben, and salts thereof.
The blending ratio of benzyloxyethanol and parabens is preferably 0.01-10% by mass of parabens per 1 mass of benzyloxyethanol.

  The drug or quasi drug containing benzyloxyethanol or benzyloxyethanol and parabens of the present invention is benzyloxyethanol or benzyloxyethanol and parabens, alcohol such as water, ethyl alcohol, isopropyl alcohol, glycerin, etc. Can be produced by appropriately blending solvent, oil, higher fatty acids, alcohols, silicones, surfactants, water-soluble polymers, chelating agents, pH adjusters, thickeners, powder components, pigments, fragrances, and the like. it can.

  Examples of the dosage form of such a preparation include an aqueous solution system, a solubilization system, an emulsification system, a water-oil two-layer system, and a water-oil-powder three-layer system. Specific examples include ointments, creams, emulsions, The form of a liquid agent etc. is mentioned.

  The above-mentioned preparations containing benzyloxyethanol usually contain preservatives (eg, parabens, 2-phenoxyethanol, benzoic acid and salts thereof, salicylic acid and salts thereof, sorbic acid and salts thereof, dehydroacetic acid and salts thereof). Salts, p-toluenesulfonic acid and its salts, alcohols such as ethanol and isopropanol, quaternary ammonium salts such as benzalkonium chloride, etc.) and antiseptic raw materials (polyhydric alcohols, medium chain fatty acids and esters thereof) , And EDTA and other chelating agents) can be used in combination, but in that case, the combined use provides a synergistic effect, and the amount of the preservative and specific raw material used can be reduced. . In particular, when benzyloxyethanol and parabens are used in combination, the preservative power is much better than when benzyloxyethanol or parabens are used alone, so benzyloxyethanol and parabens are combined. When the preservative is used, the amount of the parabens and the preservative added at the same time can be considerably reduced, and it can be used very safely even for a person sensitive to the preservative.

  The blending amount of benzyloxyethanol in the preparation of the above-mentioned pharmaceutical and quasi-drug varies depending on the purpose of use, dosage form, etc., but in the preparation, 0.01 to 30% by mass, preferably 0.05 to 5% by mass, More preferably, it is 0.1-2 mass%, More preferably, it is preferable to set it as the range of 0.1-1 mass%.

  Benzyloxyethanol of the present invention, or household products containing benzyloxyethanol and parabens, miscellaneous goods, etc., as antibacterial and antifungal agents, liquid type antibacterial finishing agents for clothing, antibacterial detergents for clothing, antibacterial softeners for clothing, Antibacterial products such as antibacterial bleaching agent for clothing, antibacterial detergent for residential use, antibacterial detergent for drainage, antibacterial detergent for bathroom, antibacterial detergent for washing machine, antibacterial detergent for kitchen, antibacterial detergent for dish And miscellaneous goods. Such products can be in the form of liquid, gel, solid, etc. by holding benzyloxyethanol or benzyloxyethanol and parabens on a carrier.

  Examples of liquid carriers include water; various alcohols such as ethanol and isopropyl alcohol; glycols such as propylene glycol, dipropylene glycol and polyethylene glycol; esters such as phthalic acid esters and adipic acid esters; liquid paraffin, isoparaffin and squalane. Hydrocarbon oils such as silicone oils such as methylpolysiloxane can be used, and benzyloxyethanol is dissolved or dispersed in these liquids. At this time, various auxiliary components can be added and dissolved as necessary. Examples of auxiliary components include nonionic, anionic or cationic surfactants, colorants, viscosity modifiers, antioxidants, pH adjusters and the like.

  Examples of the gel-like carrier include agar, carrageenan, gelatin, carboxymethylcellulose, glue, alginic acid, polyvinyl alcohol, dextrin, metal soap gel, and the like. As a method for retaining benzyloxyethanol on a gel-like carrier, in addition to a method in which benzyloxyethanol is mixed and dispersed in a previously produced gel-like substance, it can be used as a raw material for producing a gel-like substance, particularly when producing a gel-like substance. There is a method of adding benzyloxyethanol.

  As the solid carrier, inorganic or organic porous materials can be used. Examples of such inorganic porous materials include diatomaceous earth, ocher, clay, clay, talc, scumite, montmorillonite, calcium carbonate, zeolite, attapulgite. , Sepiolite, silica, silica gel, alumina, magnesia, silica alumina, silica magnesia, synthetic aluminosilicate and the like. Examples of the organic porous material include activated carbon, paper such as filter paper, processed cellulose products, processed wood products, potpourri (dried plants and flowers, etc.), non-woven fabrics, woven fabrics, dextrins and the like. As these porous materials, those having various shapes such as powder, beads, pellets, spheres, columns, and cylinders can be used. Further, as other solid carriers, they can be held by impregnation or kneading into various synthetic resin sheets, fibers, and building materials. In that case, what was hold | maintained to the porous substance as an active ingredient, and the thing enclosed with the microcapsule can also be used.

In order to enhance the antibacterial and antifungal effects in the above products, other antibacterial and antifungal agents, specifically antifungal agents such as imidazole compounds, antibacterial agents such as parabens, and natural antibacterial and antifungal agents such as Soso bamboo extract It is also possible to enhance the effect by combining antibacterial and antifungal agents mainly having a bleaching action such as hypochlorous acid and hydrogen peroxide. Even in this case, it is preferable to combine parabens because they exhibit superior antibacterial activity.
Moreover, a general fragrance | flavor substance can also be used together for the improvement of a usability | use_condition, and masking of a bacterial odor and a mold odor.

  The above products, when held on a liquid carrier, trigger spray products, squeeze (extruded) products with holes, bottle products with measuring caps, aerosol spray products, mechanical spray products, capsules The product can be made into a gel-like mold by adjusting the mold or viscosity.

  The blending amount of benzyloxyethanol in the products such as household goods and sundries is generally in the range of 0.01 to 30% by mass in the composition, preferably 0.1 to 5% by mass, more preferably 0.1. It is good that it is in the range of ˜2% by mass, more preferably 0.1˜1% by mass.

Example 1 Antibacterial activity of benzyloxyethanol The results of examining the minimum inhibitory concentration (MIC) of benzyloxyethanol against bacteria and fungi using the agar plate dilution method are shown.
The bacterial strains used here are Staphylococcus aureus IFO13276, Escherichia coli IFO3972, Pseudomonas aeruginosa IFO13275, Algenigenes faecalis IFO111, Alcaligenes faecalis IFO111, Penicillium citrinum IFO6352) Cladosporium cladosporoides IFO 6348). The medium was SCD agar medium (Wako Pure Chemical Industries) for bacteria and GP agar medium (Wako Pure Chemical Industries) was added to benzyl alcohol for fungi.

Test Example 1 Sensitization test of benzyloxyethanol A maximization test using guinea pigs was performed. That is, after inducing sensitization with 0.3% intradermal sensitization and 30% contact sensitization using 10 guinea pigs per group, application induction was performed at a concentration that did not cause an irritant reaction. A case in which erythema was observed was judged as positive. As a result, the positive rate was 0%.

Example 2 Synergistic effect of antiseptic power by the combination of benzyloxyethanol (BOE) and methylparaben A 50 g sample having the composition shown in Table 2 below was used to conduct a storage efficacy test at 30 ° C. using bacteria, and the change in the number of bacteria over time The antiseptic power was judged by.
The strains used here are Staphylococcus aureus IFO13276, Escherichia coli IFO3972, and Pseudomonas aeruginosa IFO13275. The results are shown in Table 2.

  By using BOE and methylparaben in combination, the use amounts of BOE and methylparaben were reduced to 60% and 25%, respectively, and a synergistic effect was confirmed.

Claims (6)

  Antibacterial and antifungal agent consisting of benzyloxyethanol.   Preservative made of benzyloxyethanol.   An antiseptic comprising benzyloxyethanol and parabens.   Antibacterial and antifungal agent containing benzyloxyethanol as an active ingredient.   A preservative containing benzyloxyethanol as an active ingredient.   Antibacterial and antifungal agent containing benzyloxyethanol and parabens as active ingredients.