JP2007161654A - Antiseptic microbicide, cosmetic or medicine comprising the same antiseptic microbicide formulated therein and antiseptic microbicidal method - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide an antiseptic microbicide having enhanced antiseptic microbicidal effects of an isothiazolines-based antiseptic agent and maintaining antiseptic mildewproofing stability even when the amount of the isothiazolines antiseptic agent itself formulated is reduced, to provide a cosmetic or a medicine comprising the antiseptic microbicide formulated therein and to provide an antiseptic microbicidal method for the cosmetic or medicine. <P>SOLUTION: The antiseptic microbicide comprises (A) 2-methyl-4-isothiazolin-3-one and/or 5-chloro-2-methyl-4-isothiazolin-3-one and (B) one or more selected from the group consisting of menthol, menthyl glyceryl ether and camphor. The cosmetic or medicine is obtained by formulating the antiseptic microbicide. Furthermore, the antiseptic microbicidal method for the cosmetic or medicine is characterized as including (A) the 2-methyl-4-isothiazolin-3-one and/or 5-chloro-2-methyl-4-isothiazolin-3-one and (B) the one or more selected from the group consisting of the menthol, menthyl glyceryl ether and camphor as an active ingredient of the antiseptic microbicidal effects. <P>COPYRIGHT: (C)2007,JPO&INPIT

Description

  The present invention relates to an antiseptic disinfectant, a cosmetic or pharmaceutical product containing the antiseptic disinfectant, and a method for preserving cosmetics or pharmaceuticals.

  For cosmetics (including quasi-drugs) and pharmaceuticals, paraoxybenzoic acid esters (parabens), benzoic acids, isothiazolines, phenoxyethanol, etc. are usually used to ensure antiseptic / antifungal properties and improve storage stability. Preservatives are used. However, these conventional antiseptics have drawbacks such as low skin safety and low safety. Therefore, there is a demand for a technique capable of maintaining antiseptic and antifungal stability even if the blending amount of the conventional preservative is reduced.

  As a technique for reducing such a conventional preservative, a technique for reducing the amount of parabens, benzoic acids, phenoxyethanol and the like by combining with 1,2-alkanediols has been reported (Patent Document 1). ~ 3).

  However, a technique for reducing isothiazoline-based preservatives has not yet been reported.

JP-A-10-53510 JP 11-310506 A Japanese Patent Laid-Open No. 11-322591

  Therefore, as a result of intensive studies by the present inventors, when a cooling sensation agent such as menthol, menthyl glyceryl ether, or camphor is used together with an isothiazoline-based preservative, even if the preservative content is reduced, The present inventors have found that stability can be maintained and have completed the present invention.

That is, the invention according to claim 1 includes (A) 2-methyl-4-isothiazolin-3-one and / or 5-chloro-2-methyl-4-isothiazolin-3-one, and (B) menthol and menthyl. The present invention relates to an antiseptic fungicide containing at least one selected from the group consisting of glyceryl ether and camphor.
The invention according to claim 2 relates to a cosmetic or pharmaceutical product comprising the antiseptic disinfectant according to claim 1.
The invention according to claim 3 includes (A) 2-methyl-4-isothiazolin-3-one and / or 5-chloro-2-methyl-4-isothiazolin-3-one, and (B) menthol and menthyl glyceryl ether. And at least one selected from the group consisting of camphor as an active ingredient for antiseptic sterilization effect.

  The antiseptic disinfectant of the present invention has the effect of enhancing the antiseptic disinfecting effect of the isothiazoline-based antiseptic by using a specific cooling sensation agent. In addition, cosmetics or pharmaceuticals containing the antiseptic disinfectant according to the present invention can maintain the antiseptic disinfecting effect even if the amount of the isothiazoline-based antiseptic is reduced, so that the preservative itself is reduced. There is an effect that it can be blended.

  The antiseptic fungicide according to the present invention includes (A) 2-methyl-4-isothiazolin-3-one and / or 5-chloro-2-methyl-4-isothiazolin-3-one, and (B) menthol and menthyl glyceryl. 1 or more types chosen from the group which consists of ether and camphor.

  The component (A) according to the present invention is an isothiazoline-based preservative, and 2-methyl-4-isothiazolin-3-one or 5-chloro-2-methyl-4-isothiazoline- represented by the following formula (1) 3-one. These may be used individually by 1 type and may be used in mixture of 2 types suitably.

  In addition, a commercial item can be used as it is for the aforementioned isothiazoline-based preservatives. Examples of commercially available products that can be used include trade names ZONEN-MT, ZONEN-C (both manufactured by Chemiclear).

  As the component (B) according to the present invention, a cooling sensation agent is used. As the cooling sensate used, menthol, menthyl glyceryl ether, and camphor are used, and one of these can be used alone or two or more can be used in appropriate combination.

  In the antiseptic disinfectant according to the present invention, the content of the component (A) and the component (B) is not particularly limited, but is 1: 0.1 to 1: 100, preferably 1: 0.5 in weight ratio. To 1:50, more preferably 1: 1 to 1: 5. When the preservative of the component (A) exceeds 10 times the weight of the component (B), or the cooling sensation of the component (B) exceeds 100 times the weight of the component (A), the component (A) This is not preferable because it cannot be expected to enhance the antiseptic sterilization effect.

  Although the specific cooling sensation agent itself used in the antiseptic disinfectant according to the present invention does not exhibit an antiseptic disinfecting effect, when combined with the above-mentioned isothiazoline-based antiseptics, The action of enhancing the antiseptic sterilization effect is shown. Therefore, even if the amount of the isothiazoline-based preservative is low, the antiseptic / antifungal effect can be maintained, so that a highly safe antiseptic sterilizer can be obtained.

  The antiseptic disinfectant of the present invention can be used by blending it in cosmetics, pharmaceuticals and the like. Specifically, facial cleanser, lotion, milky lotion, skin cream, foundation, mascara, nail enamel, lipstick and other skin cosmetics, shampoo, hair treatment, hair growth / hair restorer, hair cream, hair foam, permanent wave agent, etc. It can be used for pharmaceuticals such as cosmetics for hair, medicinal cosmetics (quasi-drugs) having a specific purpose of use, such as stains and freckles, and acne remedies.

  When preparing cosmetics or pharmaceuticals using the antiseptic disinfectant of the present invention, within the range that does not impair the effects of the present invention, in addition to the above-described components, components usually used in cosmetics or pharmaceuticals are arbitrarily arbitrarily selected. Can be blended. For example, fats and oils, waxes, higher fatty acids, lower alcohols, higher alcohols, sterols, fatty acid esters, humectants, surfactants, polymer compounds, inorganic pigments, dyes, antioxidants, ultraviolet absorbers, vitamins, astringent Examples include agents, whitening agents, animal and plant extracts, sequestering agents, purified water, and the like.

  When the antiseptic disinfectant of the present invention is blended in cosmetics or pharmaceuticals, the blending amount is not particularly limited, but is preferably 0.001 to 5% by weight, more preferably 0.01 to 1% by weight, even more preferably in the composition. It is 0.1 to 0.5% by weight. This is because when the amount is less than 0.001% by weight, the antibacterial effect is inferior, and even if the amount exceeds 5% by weight, no further effect can be expected.

Example 1
(Test bacteria)
As test bacteria, Escherichia coli IFO3972 (E. coli), Pseudomonas aeruginosa IFO13275 (Pseudomonas aeruginosa), and Aspergillus niger IFO9455 (Black mold) were used.

(Preparation of bacterial solution for inoculation)
As the inoculum, Escherichia coli and Pseudomonas aeruginosa were cultured at 35 ° C. on an agar medium, then transplanted to a bouillon medium and cultured at 35 ° C. A solution obtained by diluting the obtained culture solution to about 10 ⁸ cells / ml with a bouillon medium was used as a bacterial solution for inoculation.
As for Aspergillus niger, after cultured at 25 ° C. Tween 80 (polyoxyethylene (20) sorbitan monooleate) inoculating bacteria those prepared approximately 10 ⁶ cells / ml were suspended spores 2% pressurized saline Liquid.

(Preparation of dilution series of test substance)
Using purified water as a dilution solvent, a 1.25 w / v% solution of 2-methyl-4-isothiazolin-3-one was diluted twice to prepare a dilution series. As for menthol, 20 w / w% ethyl cellosolve was used as a dilution solvent, and a 5 w / v% solution was diluted twice to prepare a dilution series.
In addition, a mixture obtained by mixing 2-methyl-4-isothiazolin-3-one and menthol at a weight ratio of 1: 1 uses 20 w / w% ethyl cellosolve as a diluent solvent and doubles a 5 w / v% solution. Dilution series was prepared by dilution.

(Measurement of minimum inhibitory concentration (MIC))
For each 1 mL of the dilution series containing the test substance, 9 mL of each agar medium was placed in a petri dish, and the inoculum for the inoculum was streaked to a length of about 1 cm. Cultivation was performed at 35 ° C. for Escherichia coli and Pseudomonas aeruginosa, and the presence or absence of bacterial growth after 2 days was determined. Moreover, about black mold, it culture | cultivated at 25 degreeC and the presence or absence of the growth of a microbe after 3 days was determined. At this time, the minimum concentration at which no growth was observed was determined as MIC. The results are shown in Table 1.

  In addition, antibacterial power can be evaluated by MIC. When the test substance concentration is low, there is no effect on microorganisms, but growth increases when the concentration is increased. This degree of growth proceeds depending on the concentration, and finally the growth stops. The concentration at this time is expressed as MIC. Therefore, when the concentration is higher than MIC, the microorganisms are killed.

Example 2
MIC was determined in the same manner as in Example 1 using menthyl glyceryl ether instead of menthol. The results are shown in Table 2.

Example 3
MIC was calculated | required by the operation similar to Example 1 using camphor instead of menthol. The results are shown in Table 3.

  From the results of Tables 1 to 3, although all of menthol, menthyl glyceryl ether, and camphor did not exhibit antibacterial activity even at a high concentration of 5000 μg / mL for all the test bacteria, It can be seen that when used in combination with a preservative, antibacterial activity is exhibited for all test bacteria even at a concentration that is half the minimum growth inhibitory concentration of the isothiazoline-based preservative. Therefore, it was confirmed that when used in combination with menthol, menthyl glyceryl ether, or camphor, the antiseptic sterilizing effect of the isothiazoline-based preservatives was remarkably enhanced.

Hereinafter, formulation examples of cosmetics and pharmaceuticals containing the antiseptic disinfectant of the present invention will be shown. In addition, a compounding quantity is weight%.
(Formulation example 1: moisturizing cream)
Decaglyceryl monolaurate 1.0
Polyoxyethylene (15) glyceryl monostearate 1.0
Hydrogenated soybean phospholipid 1.0
Stearic acid 4.0
Cetanol 2.0
Behenyl alcohol 2.0
Paraffin 3.0
Squalane 12.0
Jojoba oil 4.0
Methylpolysiloxane 0.2
1,3-butylene glycol 3.0
L-Arginine 0.1
Xanthan gum 0.001
2-Methyl-4-isothiazolin-3-one 0.01
Camphor 0.2
Purified water residue
Total 100.0

(Formulation example 2: hydrophilic ointment)
Ascorbic acid 0.5
Polyoxyethylene cetyl ether 2.0
Hydrogenated soybean phospholipid 1.0
Stearic acid 4.0
Glycerol monostearate 10.0
Liquid paraffin 10.0
Vaseline 4.0
Cetanol 5.0
Propylene glycol 5.0
2-Methyl-4-isothiazolin-3-one 0.005
Menthyl glyceryl ether 0.5
Purified water residue
Total 100.0

(Formulation Example 3: Lotion)
Ethanol 5.0
Glycerin 3.0
Dipropylene glycol 3.0
1,3-butylene glycol 3.0
2-Methyl-4-isothiazolin-3-one 0.01
Menthol 0.8
Purified water residue
Total 100.0

(Formulation example 4: medicated shaving gel)
Dipotassium glycyrrhizinate 0.1
Dipropylene glycol 7.0
Polyethylene glycol 1500 8.0
Carboxyvinyl polymer 0.4
Polyoxyethylene (15) oleyl alcohol ether 1.0
Potassium hydroxide 0.1
2-Methyl-4-isothiazolin-3-one 0.003
5-Chloro-2-methyl-4-isothiazolin-3-one 0.003
Menthol 0.05
Camphor 0.01
Perfume appropriate amount
Purified water residue
Total 100.0

(Formulation Example 5: Liquid body deodorant)
Zinc paraphenol sulfonate 2.0
Ethanol 30.0
1,3-butylene glycol 3.0
2-Methyl-4-isothiazolin-3-one 0.01
Menthol 0.1
Polyoxyethylene (50) hydrogenated castor oil 0.5
Perfume appropriate amount
Purified water residue
Total 100.0

The antiseptic disinfectant of the present invention has an excellent antibacterial activity by enhancing the antiseptic disinfecting effect of the isothiazoline-based preservatives, the preservative itself can have a low blending amount, and has high safety. Therefore, it can be suitably used as a preservative disinfectant for cosmetics and pharmaceuticals.

Claims (3)

  (A) selected from the group consisting of 2-methyl-4-isothiazolin-3-one and / or 5-chloro-2-methyl-4-isothiazolin-3-one and (B) menthol, menthyl glyceryl ether and camphor An antiseptic disinfectant comprising at least one kind.   A cosmetic or pharmaceutical product comprising the antiseptic disinfectant according to claim 1. (A) selected from the group consisting of 2-methyl-4-isothiazolin-3-one and / or 5-chloro-2-methyl-4-isothiazolin-3-one and (B) menthol, menthyl glyceryl ether and camphor A method of preserving and sterilizing cosmetics or pharmaceuticals, comprising one or more active ingredients as antiseptic and sterilizing active ingredients.