JPH11310506A - Antiseptic microbicide and cosmetic composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain an antiseptic microbicide which can reduce the amount of paraben used by increasing the antimicrobial potency of paraben, and possesses high safety by using at least one kind of specific three kinds of 1,2- alkanediols and paraben in combination. SOLUTION: This antiseptic microbicide is composed of the combination of (A) at least one kind of parabens of the formula (R is a 1-4C alkyl) and (B) at least one kind selected from 1,2-pentanediol, 1,2-hexanediol or 1,2- octanediol. When this antiseptic microbicide is blended as an antiseptic microbicide for cosmetics for skin and hair, e.g. toilet water, milky lotion, cream and the like, the cosmetic composition having high safety and efficient antimicrobial activity can be obtained. In this case, it is favorable that the combination amount of methyl paraben in the composition is less than 0.2 wt.%. Further, the component B is preferably blended in a proportion of 0.05-20 wt.% in this composition. As a result, a cosmetic having reduced irritation to skin can be provided.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an antiseptic disinfectant and a cosmetic composition, and an object of the present invention is to reduce the amount of paraben used by increasing the antibacterial activity of paraben which has been conventionally used as an antiseptic disinfectant. Another object of the present invention is to provide an antiseptic disinfectant exhibiting excellent antibacterial activity and a highly safe cosmetic composition containing a small amount of paraben. still,
In the present specification, the cosmetic composition refers to cosmetics, pharmaceuticals, and quasi-drugs that are applied directly to human skin.

[0002]

2. Description of the Prior Art Conventionally, parabens such as methylparaben, ethylparaben and propylparaben, benzoic acid and salts thereof, salicylic acid and salts thereof have been used as preservatives and disinfectants in cosmetics, pharmaceuticals and quasi-drugs. In particular, parabens are frequently used.

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

[0004] 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, and glycerin has been proposed.
This is because, in a cosmetic composition, parabens are affected by the amount present in the aqueous phase, and therefore, by adding a polyhydric alcohol such as 1,3-butylene glycol, dipropylene glycol, or glycerin, This is a method of increasing the distribution of parabens into the water phase and increasing its effectiveness.

[0005]

SUMMARY OF THE INVENTION However, 1,3
-The effect of increasing the antibacterial activity of paraben by using a polyhydric alcohol such as butylene glycol, dipropylene glycol or glycerin in combination with paraben is not remarkable, and the amount of paraben used has not been reduced. Also,
Plant extracts and the like have been proposed as antiseptic fungicides that can be used in place of parabens, but none of them has a remarkable antiseptic action compared to parabens. In addition, many of them are oil-soluble and have problems in terms of skin sensitization, so they are not useful, such as the formulation amount is limited in the actual formulation design. Not in.

[0006] Therefore, by increasing the preservative power of paraben and reducing the amount of paraben used, an efficient antiseptic and fungicide capable of providing a cosmetic composition having high safety and excellent antibacterial properties. The creation of is desired. The present inventors have conducted intensive research on preservatives and fungicides,
1,2-Pentanediol originally used as a humectant, and 1,2-hexanediol and 1,2-octanediol, which are also 1,2-alkanediols like 1,2-pentanediol, were added. Three kinds of 1,
The present invention has found that by using one or more of 2-alkanediols as a preservative and disinfectant in combination with paraben, the antibacterial activity of paraben can be increased and the amount of paraben used can be greatly reduced. Was completed.

[0007]

That is, the invention according to claim 1 is an invention which relates to at least one of paraben and 1,2-pentanediol, 1,2-hexanediol, 1,2-hexane.
The present invention relates to an antiseptic disinfectant characterized by being combined with one or more octanediols. The invention according to claim 2 relates to a cosmetic composition comprising the preservative disinfectant according to claim 1 as an antiseptic disinfectant, and the invention according to claim 3 relates to a composition in which the amount of methylparaben compounded is a composition. The cosmetic composition according to claim 2, wherein the content is less than 0.2% by weight.

[0008]

DETAILED DESCRIPTION OF THE INVENTION As described above, the present inventors have used paraben and one or more of 1,2-pentanediol, 1,2-hexanediol, and 1,2-octanediol in combination. By raising the antibacterial power of paraben,
They have found that the amount of paraben used can be significantly reduced, and have completed the present invention.

The paraben used in the present invention is represented by the following formula (5), and four types of methylparaben, ethylparaben, propylparaben and butylparaben have been widely used as a preservative and disinfectant for cosmetic compositions. (In the formula 5, R represents an alkyl group having 1 to 4 carbon atoms).
In the present invention, one or more of the above four types of parabens are used.

Embedded image

Also, 1,2-pentanediol, 1,2
-Hexanediol and 1,2-octanediol are one kind of polyhydric alcohols and are represented by the following formulas (6) and (7), respectively.
(Formula 7) and is shown by the following formula 8 (Formula 8). Of these three polyhydric alcohols, 1,2-pentanediol is
Conventionally, it has been widely used as a base of cosmetics, and has high safety and is easily soluble in water, and thus has been used as a humectant, a stabilizer, a dispersant, a solvent, and the like. Therefore, 1,2-
By using pentanediol, the moisturizing power can be enhanced, so that a cosmetic composition having an excellent moist feeling can be obtained. Further, as is clear from the test examples described later, a cosmetic composition excellent in moist feeling can be similarly obtained when 1,2-hexanediol or 1,2-octanediol is used.

Embedded image

Embedded image

Embedded image

In the present invention, at least one of the above-mentioned parabens and 1,2-pentanediol, 1,1
One or more of 2-hexanediol and 1,2-octanediol are combined to form an antiseptic disinfectant.
When both are used together, the antibacterial activity of each of them is enhanced by a synergistic effect, and when both are used alone, an antiseptic effect is exhibited even against a bacterium having no antiseptic effect.

For example, as apparent from the test examples described below,
In the emulsified formulation system, 1,2-pentanediol is
Although it exhibits an excellent preservative effect on general bacteria, it hardly exerts an antiseptic effect on fungi such as yeasts and molds, and parabens on all general bacteria, yeasts and molds. Although they have almost no antiseptic effect, they can exert an excellent antiseptic effect on all common bacteria, yeasts and molds by using both of them. Also, 1,
2-hexanediol and 1,2-octanediol are
Even when used alone, it exhibits a certain antiseptic effect against general bacteria, yeasts and molds, but when used in combination with parabens, the antiseptic and sterilizing power can be further enhanced.

Therefore, by using at least one of paraben and at least one of 1,2-pentanediol, 1,2-hexanediol and 1,2-octanediol in combination, the amount of paraben used can be reduced. Since the composition can be greatly reduced, a cosmetic composition having high safety and sufficiently imparted antibacterial properties can be obtained by blending the antiseptic disinfectant according to the present invention.

[0014] The cosmetic composition according to the present invention comprises at least one of paraben and 1,2-pentanediol,
The composition is obtained by blending at least one of 1,2-hexanediol and 1,2-octanediol as a preservative and disinfectant. For example, skin and hair cosmetics such as lotions, emulsions, creams, shampoos, and hair treatments; medicated cosmetics (quasi-drugs) with specific uses such as prevention of spots and freckles; and acne treatment The above preservative and bactericide can be blended with the prepared pharmaceutical to obtain the cosmetic composition according to the present invention.

The amount of paraben in the cosmetic composition is not particularly limited, and may be lower than the use limit concentration. However, when the amount of methylparaben is 0.2% by weight or more in the composition, irritation to the skin becomes strong and the feeling of use is deteriorated.
It is preferred to be less than wt%. Even when the amount of methylparaben is less than 0.2% by weight, each of them can be used in combination with at least one of 1,2-pentanediol, 1,2-hexanediol, and 1,2-octanediol. Since the antiseptic power is enhanced, a sufficiently excellent antiseptic and sterilizing effect can be exhibited.

Also, 1,2-pentanediol, 1,2-
Hexanediol and 1,2-octanediol have extremely high safety, as is clear from the results of the safety test described later, and thus can be incorporated in the cosmetic composition up to 20% by weight. However, if the amount is less than 0.05% by weight, the effect of the compounding is not sufficiently exerted. Therefore, the compounding ratio in the composition is 0.05 to 20% by weight, and particularly when 1,2-pentanediol is used, 1%. It is desirable that the content be 10 to 10% by weight.

Hereinafter, 1,2-pentanediol, 1,2
The safety of -hexanediol and 1,2-octanediol will be described based on test results. (Toxicity test) Using rats, mice and rabbits,
The 50% lethal dose (LD ₅₀ ) of 2-pentanediol was determined. The results are shown in Table 1 together with the LD ₅₀ of the four parabens.

[Table 1]

(Irritation test) As an irritation test for 1,2-pentanediol, 1,2-hexanediol and 1,2-octanediol, acute dermal irritation was performed using a total of six rabbits, three males and three females. Perform an irritation test,
An acute eye irritation test was also performed using six male rabbits and three female rabbits. As a result, there was almost no irritation to the skin and eyes. Also, in a skin sensitization test using a total of 20 guinea pigs, 10 males and 10 females, there was almost no irritation to the skin.

Further, 1,2-pentanediol, 1,2
The results of human skin compatibility test, mutagenicity test and patch test for -hexanediol and 1,2-octanediol were all negative. From the results of the above safety test, 1,2-pentanediol, 1,2-
Hexanediol and 1,2-octanediol can be said to be extremely safe substances.

[0020]

Test Examples Hereinafter, the present invention will be described in detail based on test examples. [Test Example 1: Evaluation of preservative power] The creams of Examples 1 to 5 were formulated according to the formulation shown in Table 2, and Comparative Examples 1 to 5 were formulated according to the formulation shown in Table 3.
No. 6 cream was prepared and the preservative power was evaluated by the challenge test.

[Table 2]

[Table 3]

The test bacteria include Escherichia as general bacteria.
coli IFO3972 (Escherichia coli), Staphylococcus aureus IFO1
3276 (Staphylococcus aureus), Bacillus subtilis IFO122
A mixed bacterial solution of 10 (Bacillus subtilis) was used. Also, as yeast
ccharomyces cerevisiae IFO0234, Asperg as a fungus
illus niger (black mold) was used. A culture solution in which these bacteria were pre-cultured in advance was mixed with general bacteria at about 10 ⁸ cells / m
l, S. cerevisiae about 10 ⁷ cells / ml, A. niger about
The suspension diluted to 10 ⁶ cells / ml was used as a bacterial suspension. The number of bacteria was confirmed by the colony counting method.

In a dry-heat sterilized glass container,
5 or 20 g of the creams of Comparative Examples 1 to 6 were added, and 0.2 ml of the above bacterial suspension was inoculated.
revisiae and A. niger were cultured at 25 ° C. For mixed bacteria, S. cerevisiae, A.ni
As for ger, after 7, 14, and 21 days, 1 g of each sample was withdrawn, diluted with physiological saline, mixed with an agar medium and cultured for 48 hours, and the number of residual bacteria in the sample was calculated.
The measurement of A.niger after confirming that it had completely died was omitted.

The results are shown in Table 4 and FIGS. In addition, about Comparative Example 6, since the polyhydric alcohol was not mix | blended, the component was not disperse | distributed and the result was not able to be obtained, and the result about Examples 1-5 and Comparative Examples 1-5 is shown.

[Table 4] In Table 4, * indicates that the measurement was omitted. FIG. 1 is a diagram showing the change in the viable cell count of the mixed bacteria in the example, FIG. 2 is a diagram showing the change in the viable cell count of S. cerevisiae in the example, and FIG. 3 is the viable cell count of A. niger in the example. In the figure, the broken line indicated by a circle indicates the result of Example 1, the broken line indicated by a square indicates the result of Example 2, the broken line indicated by a triangle indicates the result of Example 3,
The broken line of the mark is the result of Example 4, and the broken line of the mark is the result of Example 5.
Is the result of FIG. 4 shows the change in the viable cell count of the mixed bacteria in the comparative example, and FIG. 5 shows S. cerevisiae in the comparative example.
FIG. 6 shows the change in the viable cell count of A. nige in Comparative Example.
r is a graph showing the change in the number of viable bacteria. In the figure, a broken line indicated by a triangle indicates the result of Comparative Example 1, a broken line indicated by a circle indicates the result of Comparative Example 2, a broken line indicated by a circle indicates the result of Comparative Example 3, and The polygonal line is the result of Comparative Example 4, and the polygonal line with a triangle is the result of Comparative Example 5.

From the results shown in Table 4 and FIGS. 1 to 6, Comparative Example 1
When paraben and glycerin, which is one of polyhydric alcohols, are used in combination as in
Even if it is blended by weight, it shows only a very little preservative effect on general bacteria, but as in Examples 1, 4 and 5, paraben and
When used in combination with 1,2-pentanediol, the antiseptic power of each is improved, so that even if the amount of paraben is reduced, a sufficient antiseptic effect is exhibited against general bacteria, and also against yeast and mold. It can be seen that they exhibit the same or higher antiseptic power. Further, when paraben is used in combination with 1,2-hexanediol or 1,2-octanediol as in Examples 2 and 3, the antiseptic power of each is also improved, so that the amount of paraben used can be reduced. It can also be seen that the antiseptic effect is remarkably superior to the case where each of them is used alone, and exhibits an excellent antiseptic effect against all kinds of bacteria, such as general bacteria, yeast and mold.

From the results of Test Example 1, at least one of parabens and 1,2-pentanediol, 1,2
By using in combination with one or more of -hexanediol and 1,2-octanediol, even when the amount of paraben used is reduced, a sufficiently excellent antiseptic and bactericidal effect can be exhibited, and safety can be improved. It can be said that a high cosmetic composition can be obtained.

Test Example 2 Evaluation of Feeling of Use Next, the feeling of use was evaluated using a hair styling cream and a massage cream. (Moist feeling) According to the following formula, a hair styling cream containing 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol or glycerin as a polyhydric alcohol was prepared by a conventional method. Prepared. Hairdressing cream (% by weight) 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 Appropriate amount of purified water Remainder total 100.00

According to the following formula, a massage cream containing 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol or glycerin as a polyhydric alcohol is prepared by a conventional method. did. 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 Methyl paraben 0.15 Propyl paraben 0.05 Perfume 0.10 Purified water Remainder total 100.00

Each of the hairdressing cream and the massage cream prepared according to the above-mentioned formula was used by 10 women, and the feeling of use was evaluated organoleptically from the viewpoint of moist feeling. Based on the results of the sensory evaluation, the determination was made according to the following criteria. ◎: 8 or more of 10 persons judged moist feeling ○: 5 to 7 of 10 persons judged moist feeling ×: 4 or less of 10 persons judged moist feeling

The results are shown in Table 5.

[Table 5]

(Irritation) According to the formulation in Table 6, massage creams of Examples 6 to 10 and Comparative Examples 7 to 8 were prepared by a conventional method.

[Table 6] Each of the above seven types of massage cream was used by 10 women, and the feeling of use was evaluated organoleptically from the viewpoint of irritation. Based on the results of the sensory evaluation, the determination was made according to the following criteria. ◎: No one among 10 felt the stimulus ○: 1 to 3 out of 10 judged to feel the stimulus ×: Judged that 4 or more out of 10 felt the stimulus

The results are shown in Table 7.

[Table 7] From the results shown in Tables 5 and 7, paraben and 1,2-pentanediol, 1,2-hexanediol or 1,2-hexanediol were used.
It can be seen that the cream blended with octanediol is excellent in moisturizing power and extremely low in irritation.

[0032]

Formulation Examples Hereinafter, formulation examples of the cosmetic composition according to the present invention will be described.

[0033]

[0034]

[0035]

As described in detail above, the invention according to claim 1 comprises at least one of paraben and 1,2-pentanediol, 1,2-hexanediol and 1,2-octanediol. Since the present invention relates to an antiseptic disinfectant characterized by being combined with at least one of the following, it has the following effects.

That is, 1,2-pentanediol, 1,2
Since one or more of -hexanediol and 1,2-octanediol and paraben are used as a preservative and disinfectant, their antibacterial activity is enhanced by a synergistic effect, and even if the amount of paraben is reduced. In addition, it exerts extremely excellent antibacterial activity against all microorganisms. Therefore, the amount of paraben conventionally used as an antiseptic can be significantly reduced, and a highly safe cosmetic composition can be obtained.

The invention according to claim 2 relates to a cosmetic composition characterized by containing the antiseptic disinfectant according to claim 1 as an antiseptic disinfectant, so that it has high antiseptic disinfection properties and is safe. The cosmetic composition according to claim 2, wherein the composition according to the third aspect has an effect of being excellent in the properties and feeling of use, and the compounding amount of methyl paraben is less than 0.2% by weight in the composition. Since it is related to an object, there is an effect that there is no irritation to the skin and the feeling of use is extremely good.

[Brief description of the drawings]

FIG. 1 is a diagram showing a change in the number of mixed viable bacteria in Examples in Test Example 1.

FIG. 2 is a diagram showing changes in the number of viable S. cerevisiae bacteria in Examples in Test Example 1.

FIG. 3 is a diagram showing a change in the number of viable A. niger bacteria in Examples in Test Example 1.

FIG. 4 is a diagram showing a change in the number of live mixed bacteria in Comparative Example in Test Example 1.

FIG. 5 is a diagram showing changes in the number of viable S. cerevisiae bacteria in Comparative Example in Test Example 1.

FIG. 6 is a diagram showing changes in the number of viable A. niger bacteria in Comparative Example in Test Example 1.

 ──────────────────────────────────────────────────続 き Continuing from the front page (72) Inventor Nobunori Fujiwara 5-12, 12-kencho, Chuo-ku, Osaka-shi Inside Mandom Central Research Institute Co., Ltd. No. 12 Mandom Central Research Laboratory Co., Ltd.

Claims (3)

[Claims] 1. A method according to claim 1, wherein at least one of the parabens represented by the following formula (1) and 1,2 represented by the following formula (2):
-Pentanediol, 1,2 represented by the following formula 3
-Hexanediol, 1,2 represented by the following formula 4
-An antiseptic disinfectant characterized by being combined with one or more of octanediols (however, R in the formula 1 represents an alkyl group having 1 to 4 carbon atoms). Embedded image Embedded image Embedded image Embedded image 2. A cosmetic composition comprising the antiseptic disinfectant according to claim 1 as an antiseptic disinfectant. 3. The composition according to claim 1, wherein the amount of methylparaben is 0.1% in the composition.
3. The cosmetic composition according to claim 2, wherein the amount is less than 2% by weight.