JP5072930B2 - Antiseptic disinfectant and cosmetic composition - Google Patents

Description

  The present invention relates to an antiseptic disinfectant and a cosmetic composition, the purpose of which is to increase the antibacterial activity of parabens that have been used as an antiseptic disinfectant so far. An object of the present invention is to provide an antiseptic disinfectant to be exhibited and a highly safe cosmetic composition with a small amount of paraben. In the present specification, the cosmetic composition refers to cosmetics, pharmaceuticals, and quasi drugs that are applied directly to the human skin.

  Conventionally, parabens such as methylparaben, ethylparaben, and propylparaben, benzoic acid and salts thereof, salicylic acid and salts thereof, and the like have been used as antiseptic fungicides in cosmetics, pharmaceuticals, and quasi drugs. Is frequently used.

  However, in recent years, the skin irritation of parabens has become a problem, and from the viewpoint of safety, reduction of the blending amount is desired. On the other hand, recently, since cosmetic formulations have become diversified and complicated, parabens are often inactivated by other ingredients such as surfactants. In particular, in an emulsified formulation system, it is extremely difficult to obtain antiseptic power by blending parabens.

  Thus, various attempts have been made to increase the efficacy of parabens and reduce the amount of parabens used in combination with other substances. For example, a method of adding a polyhydric alcohol such as 1,3-butylene glycol, dipropylene glycol, or glycerin has been devised. This is because in cosmetic compositions, parabens are affected by the amount present in the aqueous phase, so by adding a polyhydric alcohol such as 1,3-butylene glycol, dipropylene glycol or glycerin, It is a way to increase the distribution of parabens into the water phase and increase its efficacy.

  However, the effect of increasing the antibacterial activity of parabens by using polyalcohols such as 1,3-butylene glycol, dipropylene glycol and glycerin together with parabens is not remarkable, and the amount of parabens used has not been reduced. Moreover, although plant extracts etc. are proposed as what can be used as a preservative disinfectant instead of a paraben, the antiseptic disinfection action is not remarkable compared with a paraben. In addition, many oil-soluble ones are problematic in terms of skin sensitization, so it is not useful, for example, the amount of blending is limited in the actual formulation design, and it also leads to reducing the amount of paraben used. Not in.

  Therefore, by increasing the antiseptic power of parabens and reducing the amount of parabens used, the creation of an efficient antiseptic disinfectant that can provide a cosmetic composition with high safety and excellent antibacterial properties is achieved. It is desired. As a result of intensive research on antiseptic fungicides, the present inventors have found that 1,2-pentanediol, which is originally used as a moisturizing agent, and also 1,2-alkanediol as well as 1,2-pentanediol. By using one or more of three 1,2-alkanediols added with 1,2-hexanediol and 1,2-octanediol in combination with parabens as antiseptic fungicides, The inventors have found that the amount of paraben used can be greatly reduced by increasing the power, and the present invention has been completed.

That is, the invention according to claim 1, and at least one of parabens, preservatives disinfectant, characterized by comprising in combination with 1,2-pentanediol (provided that 1,2-pentanediol 3. 0% by weight, 0.2% by weight of methyl paraben and 2.0% by weight of ethyl alcohol, and a case of containing an aqueous dispersion of film-forming polymer particles) . The invention according to claim 2 is a cosmetic composition comprising the antiseptic disinfectant according to claim 1 as an antiseptic disinfectant (however, in the water phase, a perfume hardly soluble in water and 1, The invention according to claim 3 relates to 2-pentanediol and excludes a fragrance solubilized composition obtained by solubilizing this fragrance in an aqueous phase without using a surfactant . 3. The cosmetic composition according to claim 2, wherein the compounding amount of methylparaben is less than 0.2% by weight in the composition.

According to claim 1 invention comprises at least one of parabens, since it relates to antiseptic disinfectant, characterized by comprising in combination with 1,2-pentanediol, the following effects .

That is, 1,2-pentanediol and paraben are combined to form an antiseptic disinfectant, so that each antibacterial activity is enhanced by a synergistic effect, and even if the amount of paraben is reduced, it is extremely excellent against all microorganisms. The antibacterial activity will be demonstrated. Therefore, the amount of paraben used as an antiseptic disinfectant can be greatly reduced, and a highly safe cosmetic composition can be obtained.

  The invention according to claim 2 relates to a cosmetic composition characterized in that the antiseptic disinfectant according to claim 1 is blended as an antiseptic disinfectant. The invention according to claim 3 relates to the cosmetic composition according to claim 2, characterized in that the blending amount of methylparaben is less than 0.2% by weight in the composition. Therefore, there is an effect that there is no irritation to the skin and the feeling of use is very good.

It is a figure showing the change of the number of living mixed bacteria of an Example and a reference example in Test Example 1. It is a figure showing the change of the S. cerevisiae viable cell count of an Example and a reference example in Test Example 1. It is a figure showing the change of the A.niger viable count of an Example and a reference example in Test Example 1. It is a figure showing the change of the mixed microbe count of a comparative example in the test example 1. It is a figure showing the change of the S. cerevisiae viable count of the comparative example in Test Example 1. It is a figure showing the change of A.niger viable cell count of the comparative example in the test example 1. FIG.

  As described above, the present inventors have improved the antibacterial activity of paraben by using paraben in combination with one or more of 1,2-pentanediol, 1,2-hexanediol, and 1,2-octanediol. As a result, it was found that the amount of paraben used can be greatly reduced, and the present invention has been completed.

（但し、式１中Ｒは炭素数１〜４のアルキル基を示す） The paraben used in the present invention is represented by the following formula 1 (chemical formula 1), and four kinds of methyl paraben, ethyl paraben, propyl paraben, and butyl paraben have been widely used as antiseptics and fungicides for cosmetic compositions. . Also in the present invention, one or more of the above four types of parabens are used.

(In the formula 1, R represents an alkyl group having 1 to 4 carbon atoms)

Further, 1,2-pentanediol in one polyhydric alcohol, represented by the following formula 2 (of 2). 1, 2-pentanediol is widely used as a cosmetic base conventionally, since it is easily soluble in high water safety, humectants, stabilizing agents are used dispersing agent, as such a solvent . Accordingly, the use of 1,2-pentanediol also enhances the moisturizing power, so that it can be made into a cosmetic composition having a moist feeling .

In the present invention, at least one 1,2-pentanediol of the parabens as described above are combined into an antiseptic disinfectant. When both are used in combination, the antibacterial activity is enhanced by a synergistic effect, and the antiseptic effect is also exerted against bacteria that do not exhibit any antiseptic effect when they are blended alone.

For example, as will be apparent from the test examples described later, in the emulsion formulation system, 1,2-pentanediol exhibits an excellent antiseptic effect against general bacteria, but it is antiseptic against fungi such as yeast and mold. It has almost no effect, and parabens have little antiseptic effect on all of general bacteria, yeast and mold, but by using both together, it can be used against all of general bacteria, yeast and mold. And exhibit an excellent antiseptic effect .

Therefore, the combined use of at least one 1,2-pentanediol of parabens, it is possible to greatly reduce the amount of paraben, by incorporating an antiseptic disinfectant of the present invention, safety It is possible to obtain a cosmetic composition having high properties and sufficient antibacterial properties.

Cosmetic composition according to the present invention includes at least one of paraben, a composition and 1,2-pentanediol, which are formulated as an antiseptic disinfectant. For example, skin and hair cosmetics such as lotions, emulsions, creams, shampoos, hair treatments, medicinal cosmetics (quasi-drugs) with specific purposes such as prevention of stains and freckles, and acne treatment The above-mentioned antiseptic disinfectant can be blended with the above-mentioned pharmaceutical product to obtain a cosmetic composition according to the present invention.

The blending amount of paraben in the cosmetic composition is not particularly limited, and may be set to a use limit concentration or less. However, when the amount of methyl paraben is 0.2% by weight or more in the composition, the irritation to the skin becomes strong and the feeling of use deteriorates, so the amount of methyl paraben is particularly less than 0.2% by weight in the composition. It is preferable to do this. In addition, even if the blending amount of methylparaben is less than 0.2% by weight , the combined use with 1,2-pentanediol enhances the antiseptic power of each, so that it exhibits a sufficiently excellent antiseptic sterilizing effect. Can do.

Moreover, 1,2-pentanediol is extremely high in safety as will be apparent from the results of the safety test described later, so that it can be blended up to 20% by weight in the cosmetic composition. However, if the amount is less than 0.05% by weight, the effect of blending is not sufficiently exhibited. Therefore, the blending ratio in the composition is 0.05 to 20% by weight, and preferably 1 to 10% by weight.

Hereinafter, the safety of 1,2-pentanediol will be described based on test results.

(Toxicity test)
Rats, mice, and rabbits were used to examine the 50% lethal dose (LD ₅₀ ) of 1,2-pentanediol. The results are shown in Table 1 together with the LD ₅₀ of the four parabens.

(Irritation test)
As irritation test about the 1,2-pentanediol, by 3 animals per sex, using a total of six rabbits, performed acute skin irritation test, also of 6 male rabbits and 3 female rabbits Was used to conduct an acute eye irritation test. As a result, there was almost no irritation to the skin and eyes. Further, in the skin sensitization test with 10 males and 10 females, a total of 20 guinea pigs, there was almost no irritation to the skin.

Furthermore, regarding the 1,2-pentanediol, skin compatibility test with human, mutagenicity test, the results of the patch test were all negative. From the results of the above safety test, it can be said that 1,2-pentanediol is an extremely safe substance.

Hereinafter, the present invention will be described in detail based on test examples.
[Test Example 1: Preservative strength evaluation]
The creams of Examples 1 to 3 and Reference Examples 1 to 2 were prepared according to the formulation shown in Table 2 , the creams of Comparative Examples 1 to 6 were prepared according to the formulation shown in Table 3, and the antiseptic power was evaluated by a challenge test.

As a test bacterium, a mixed bacterial solution of Escherichia coli IFO3972 (E. coli), Staphylococcus aureus IFO13276 (Staphylococcus aureus) and Bacillus subtilis IFO12210 (Bacillus subtilis) was used as a general bacterium. Moreover, Saccharomyces cerevisiae IFO0234 was used as yeast, and Aspergillus niger (black mold) was used as a fungus. The culture solution in which these bacteria were pre-cultured was diluted to about 10 ⁸ cells / ml for mixed bacteria of general bacteria, about 10 ⁷ cells / ml for S. cerevisiae, and about 10 ⁶ cells / ml for A. niger. This was used as a bacterial suspension. The number of bacteria was confirmed by the colony count method.

20 g of the cream of Examples 1 to 3 , Reference Examples 1 to 2 or Comparative Examples 1 to 6 is put into a glass container that has been sterilized by dry heat, 0.2 ml of the above bacterial suspension is inoculated, and the mixed bacteria is 35 ° C. S. cerevisiae and A. niger were cultured at 25 ° C. 1 and 7 days after inoculation for mixed bacteria and S. cerevisiae, and 7, 14, and 21 days for A. niger, 1 g of each sample was taken out and diluted with physiological saline into the agar medium. For 48 hours, and the number of remaining bacteria in the sample was calculated. As for A.niger, measurement after confirming complete death was omitted.

The results are shown in Table 4 and FIGS. In addition, since the polyhydric alcohol was not mix | blended about the comparative example 6, since a component did not disperse | distribute and a result was not able to be obtained, Examples 1-3 , Reference Examples 1-2, and Comparative Examples 1-5 The result about is shown.

In Table 4, * indicates that measurement was omitted. FIG. 1 is a graph showing changes in the number of viable mixed bacteria in Examples, FIG. 2 is a graph showing changes in the number of viable S. cerevisiae in Examples, and FIG. 3 is the number of live A. niger cells in Examples. In the figure, the broken line marked with ○ is the result of Example 1, the broken line marked with △ is the result of Reference Example 2 , the broken line marked with ● is the result of Example 2 , and the broken line marked with ■ is Example 3. As a result, the polygonal line of □ is the result of Reference Example 1. 4 is a graph showing changes in the number of viable mixed bacteria in the comparative example, FIG. 5 is a diagram showing changes in the number of viable S. cerevisiae in the comparative example, and FIG. 6 is a live cell of A. niger in the comparative example. In the figure, the broken line with ■ is the result of Comparative Example 1, the broken line with ● is the result of Comparative Example 2, the broken line with ○ is the result of Comparative Example 3, and the broken line with □ is a Comparative Example As a result of 4, the broken line indicated by Δ is the result of Comparative Example 5.

Table 4 and the results of Figures 1-6, as in Comparative Example 1 and 2, when used in combination with the glycerol, which is a type of parabens and polyhydric alcohols, compounded paraben 0.3 wt% However, as shown in Examples 1, 2 and 3 , when paraben and 1,2-pentanediol are used in combination, the respective antiseptic power is improved. It can be seen that, even if the amount of use is reduced, a sufficient antiseptic effect is exhibited against general bacteria, and the antiseptic ability of the same degree or more is exhibited against yeast and mold. Also, as in Reference Example 2, when paraben and 1,2-octanediol are used in combination, the antiseptic power of each is also improved, so even if the amount of paraben used is reduced, it is more than when each is used alone. It can be seen that the antiseptic power is remarkably superior and exhibits excellent antiseptic effects against all bacterial species such as general bacteria, yeast and mold.

From the results of Test Example 1 above , by using at least one of the parabens and 1,2-pentanediol in combination, even if the amount of paraben used is reduced, a sufficiently excellent antiseptic sterilizing effect is exhibited. It can be said that a highly safe cosmetic composition can be obtained.

[Test Example 2: Usability evaluation]
Next, the feeling of use was evaluated using a hair styling cream and a massage cream.
(About moist feeling)
According to the following formulation, as the polyhydric alcohol, some have 1,2-pentanediol a hairstyling cream glycerin is blended, were prepared by a conventional method.

Hairdressing cream (wt%)
Methylpolysiloxane 5.00
Paraffin 10.00
POE sorbitan monostearate 3.30
Carboxyvinyl polymer 0.22
Triethanolamine 0.20
Polyhydric alcohol 5.00
Methylparaben 0.15
Fragrance 0.10
UV absorber
Purified water balance
Total 100.00

Further, according to the following formulation, as the polyhydric alcohol, some have 1,2-pentanediol massage cream glycerin is blended, were prepared by a conventional method.

Massage cream (wt%)
Beeswax 15.00
Liquid paraffin 35.00
POE sorbitan monostearate 3.30
Sorbitan monostearate 3.30
Carboxyvinyl polymer 0.02
Triethanolamine 0.15
Polyhydric alcohol 3.00
Liquid isoparaffin 17.00
Methylparaben 0.15
Propylparaben 0.05
Fragrance 0.10
Purified water balance
Total 100.00

  Each of 10 female hairdressing creams and massage creams prepared according to the above prescriptions was used, and the usability was sensorially evaluated from the viewpoint of moist feeling. Based on the results of sensory evaluation, the determination was made according to the following criteria.

◎: Eight or more out of 10 people judged to have moist feeling ○; 5 out of 10 people judged to have moist feeling ×; 4 or less of 10 people judged to have moist feeling

The results are shown in Table 5.

(Irritating feeling)
According to the formulation of Table 6, massage creams of Examples 4 to 6 , Reference Examples 3 to 4 and Comparative Examples 7 to 8 were prepared by a conventional method.

  Each of the seven types of massage creams was used by 10 women, and the sensory evaluation was performed on the feeling of use from the viewpoint of irritation. Based on the results of sensory evaluation, the determination was made according to the following criteria.

◎: No one in 10 feels a stimulus ○: 1-3 out of 10 are judged to be stimulated x; More than 4 out of 10 are judged to be a stimulus

The results are shown in Table 7.

From the results in Table 5 and Table 7, the parabens, 1,2-pentanediol and is blended cream is excellent in moisturizing power, yet it can be seen that very low irritation.

Hereinafter, formulation examples of the cosmetic composition according to the present invention will be shown.
(Reference Formulation Example 1 )
Lotion (wt%)
Polyethylene glycol 1500 2.00
1,2-hexanediol 2.00
Polyoxyethylene oleyl ether (25E.O.) 1.50
Methylparaben 0.10
Perfume appropriate amount UV absorber appropriate amount
Purified water balance
Total 100.00

(Prescription Example 1)
Shampoo (% by weight)
Lauryl polyoxyethylene sulfate sodium salt (30% aqueous solution) 30.00
Lauryl sulfate
Sodium salt (30% aqueous solution) 10.00
Palm oil fatty acid diethanolamide 4.00
1,2-pentanediol 3.00
Methylparaben 0.10
Propylparaben 0.05
Perfume Appropriate amount Dye Appropriate amount Chelating agent Appropriate amount
Purified water balance
Total 100.00

( Reference formulation example 2)
Acne prevention cream Stearyl alcohol 8.00
Stearic acid 3.00
Purified lanolin 6.00
1,2-octanediol 1.00
Glycerin 3.00
Glycerol monostearate 2.00
Polyoxyethylene cetyl alcohol ether 3.00
Isopropylmethylphenol 1.00
Methylparaben 0.15
Perfume Appropriate amount Antioxidant Appropriate amount
Purified water balance
Total 100.00

Claims (3)

Following formula 1 (Formula 1) at least one of paraben represented by the following formula 2 (of 2), characterized by comprising in combination with 1,2-pentanediol is represented by an antiseptic disinfectant ( (However, the case where it contains 3.0% by weight of 1,2-pentanediol, 0.2% by weight of methyl paraben and 2.0% by weight of ethyl alcohol, and the case where it contains an aqueous dispersion of film-forming polymer particles) .

(In the formula 1, R represents an alkyl group having 1 to 4 carbon atoms)

A cosmetic composition comprising the antiseptic disinfectant according to claim 1 as an antiseptic disinfectant (however, in the aqueous phase, a water-insoluble fragrance and 1,2-pentanediol are associated with each other). , Except those containing a fragrance solubilized composition obtained by solubilizing this fragrance in an aqueous phase without using a surfactant).   The cosmetic composition according to claim 2, wherein the amount of methyl paraben is less than 0.2% by weight in the composition.

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