JP3774219B2 - Antiseptic disinfectant and cosmetics, pharmaceuticals and foods containing the antiseptic disinfectant - Google Patents

Description

The present invention is a cosmetic containing a combination of antiseptic disinfectant and anti-corrosion fungicides, and medicines and foods.
The object of the present invention is to increase the antibacterial activity of the antibacterial activity originally enhanced by the 1,5-alkanediol having 5 to 10 carbon atoms and the inherent antimicrobial activity of the 1,2-alkanediol having 6 to 10 carbon atoms. The object is to provide cosmetics, pharmaceuticals and foods containing a preservative fungicide .

Parabens, benzoic acids, salicylic acids, and the like are used as antiseptic fungicides in cosmetics (including quasi drugs), pharmaceuticals, and foods. However, the antiseptic disinfectant described above has a drawback that the concentration range of use is limited because it is highly skin irritating and low in safety. For example, the use concentration of paraben or benzoate is limited to 1%, and the use concentration of benzoic acid or salicylic acid is limited to 0.2%.
Moreover, since the above-mentioned antiseptic disinfectant is easily influenced by pH, the antiseptic disinfecting effect is poor in stability, and the antibacterial and antibacterial activity is remarkably reduced by the combined use with other components such as surfactants. There was also a problem that there was a case.

  In recent years, there has been a tendency to increase the number of people who cause allergic reactions to the above-mentioned antiseptic disinfectants. There is an increasing demand for cosmetics, pharmaceuticals and foods with reduced amounts.

In recent years, 1,2-alkanediol has attracted attention as a compound that can replace the above-mentioned conventional antiseptic fungicides. For example, Patent Document 1 discloses a preservative disinfectant composed of 1,2-alkanediol, and Patent Document 2 discloses a detergency or non-detergent cosmetic moisturizing bacteriostatic agent composed of 1,2-octanediol. Has been.
Patent Document 3 discloses an external composition containing a combination of 1,2-pentanediol and 2-phenoxyethanol, and Patent Document 4 discloses an antiseptic disinfectant composed of 1,2-alkanediol and paraben. .
Patent Document 5 includes an ultraviolet absorber, seaweed extract, plant extract, deodorant component, whitening component, melanin production inhibitor component, keratin remover, moisturizer, rough skin improver, anti-inflammatory agent, antioxidant, wrinkle An external preparation composition containing, as an active ingredient, one or more selected from an improving agent, a blood circulation promoter, an acne prevention agent, and a sebum control agent, and 1,2-alkanediol is disclosed.

Japanese Patent Laid-Open No. 11-322591 JP 2001-48720 A JP-A-10-53510 JP 11-310506 A JP 2003-81736 A

  However, as in the inventions described in Patent Document 1 and Patent Document 2, when 1,2-alkanediol such as 1,2-octanediol is used alone as an antiseptic disinfectant, sufficient effects are obtained. Sometimes required high loadings. In addition, since 1,2-alkanediol has a unique raw material odor, when 1,2-alkanediol is used in a high blending amount, it has a problem that odor is generated when blended into cosmetics and the like. .

  On the other hand, in the inventions described in Patent Document 3 and Patent Document 4, the antiseptic sterilization effect of 1,2-alkanediol is enhanced to obtain a sufficient antiseptic sterilization effect even when the 1,2-alkanediol is contained in a low amount. Has been tried. However, the inventions described in Patent Document 3 and Patent Document 4 aim to improve the antiseptic sterilization effect by using 1,2-alkanediol in combination with a conventional antiseptic disinfectant. It was not intended to reduce the blending amount of the agent itself or to completely eliminate the blending of the conventional antiseptic disinfectant itself.

  In the invention described in Patent Document 5, in addition to 1,2-alkanediol, components that are blended in ordinary cosmetics such as ultraviolet absorbers, seaweed extracts, plant extracts, and deodorant components are used in combination. . However, the present invention merely confirms that the antiseptic and bactericidal effect of 1,2-alkanediol is exhibited even in the presence of components blended in ordinary cosmetics. It was not an invention that attempted to enhance the antiseptic effect.

The present invention synergistically enhances the antibacterial activity inherently possessed by 1,5-alkanediol having 5 to 10 carbon atoms and the antibacterial activity inherently possessed by 1,2-alkanediol having 6 to 10 carbon atoms It is an object of the present invention to provide cosmetics, pharmaceuticals and foods containing the prepared antiseptic disinfectant .

The present invention has been made in order to solve the above-mentioned problems, and the invention according to claim 1 includes a 1,2-alkanediol having 5 to 10 carbon atoms, terpinen-4-ol and / or linalool. The present invention relates to an antiseptic disinfectant characterized by containing.
The invention according to claim 2 relates to the antiseptic fungicide according to claim 1, wherein the 1,2-alkanediol is 1,2-hexanediol and / or 1,2-octanediol.
The invention according to claim 3 relates to the antiseptic fungicide according to claim 1, wherein the 1,2-alkanediol is 1,2-octanediol.
The invention according to claim 4 is a cosmetic characterized in that it contains a preservative fungicide containing 1,2-alkanediol having 6 to 10 carbon atoms and terpinen-4-ol and / or linalool , It relates to medicines or foods.

  Since the antiseptic disinfectant according to the present invention contains 1,2-alkanediol and terpinen-4-ol and / or linalool as active ingredients, the antibacterial activity inherent in 1,2-alkanediol is synergistic. Can be enhanced.

  When 1,2-hexanediol or 1,2-octanediol is used as the 1,2-alkanediol, an antiseptic disinfectant with higher antibacterial activity can be obtained.

  Since the cosmetics, pharmaceuticals and foods according to the present invention contain 1,2-alkanediol and terpinen-4-ol and / or linalool as antiseptic fungicides, conventional antiseptics such as salicylic acid, benzoic acid and parabens are used. Can be made into a low blending amount or substantially no blending amount, and extremely high safety can be obtained.

  Hereinafter, the antiseptic fungicide according to the present invention will be described in detail. The antiseptic disinfectant according to the present invention contains 1,2-alkanediol, terpinen-4-ol and / or linalool as active ingredients.

  The first component of the antiseptic fungicide according to the present invention is a 1,2-alkanediol having 5 to 10 carbon atoms represented by the following formula 1 (Chemical formula 1), specifically, 1,2-pentanediol. 1,2-hexanediol, 1,2-heptanediol, 1,2-octanediol, 1,2-nonanediol, 1,2-decanediol.

（但し、式中、ｎは２〜７の整数を示す。）

(In the formula, n represents an integer of 2 to 7.)

In the present invention, one of the above-mentioned 1,5-alkanediols having 5 to 10 carbon atoms can be used alone, or two or more kinds can be mixed and used.
1,2-alkanediol itself has excellent antibacterial activity, and has the effect of enhancing the antibacterial activity of the antiseptic disinfectant according to the present invention. In particular, in the present invention, since it exhibits an excellent antibacterial action against Pseudomonas aeruginosa and the like, among 1,2-alkanediols having 5 to 10 carbon atoms, 1,2-hexanediol and 1,2-octanediol are It is preferable to use 1,2-octanediol, and more preferable to use.

The second component of the antiseptic disinfectant according to the present invention is terpinen-4-ol and / or linalool.
Terpinen-4-ol is a kind of perfume ingredient, and is a kind of monoterpene alcohol that is found naturally in apricots, citrus fruits, berries, grapes and the like. There are d-form and l-form optical isomers. In the present invention, any of d-form, l-form, and dl-form can be used preferably.

Linalool is a kind of perfume ingredient, and is a kind of monoterpene alcohol contained in essential oils such as clary sage, coriander, marjoram, oregano, rosewood, spearmint, and ylang ylang. Two types, terpinolene type and limonene type, are known. In the present invention, either terpinolene type or limonene type can be preferably used. Most of the linalool that exists in nature is of the terpinolene type.
In addition, d-form and l-form optical isomers exist in linalool. In the present invention, any of d-form, l-form, or dl-form can be preferably used.

  By using terpinen-4-ol and / or linalool together with a 1,2-alkanediol having 5 to 10 carbon atoms, the antibacterial action of the 1,2-alkanediol having 5 to 10 carbon atoms can be synergistically increased. it can.

  In the antiseptic disinfectant according to the present invention, the contents of the first component 1,2-alkanediol having 5 to 10 carbon atoms and the second component terpinen-4-ol and / or linalool are not particularly limited. However, it mix | blends so that it may become 1: 100-100: 1 by weight ratio, Preferably it is 1: 10-10: 1. When 1,2-alkanediol is blended in an amount exceeding 100 times the blending amount of terpinen-4-ol and / or linalool, terpinen-4-ol and / or linalool is blended in the blending amount of 1,2-alkanediol. It is not preferable to add more than 100 times by weight because the antibacterial activity enhancing effect cannot be expected.

  Since the antiseptic fungicide according to the present invention contains 1,2-alkanediol as the first component and terpinen-4-ol and / or linalool as the second component, it is shown in the test examples described later. As described above, an excellent antiseptic sterilization effect can be exhibited by the synergistic effect of the first component and the second component. Therefore, it is not necessary to blend or blend a preservative disinfectant that has been used in the past, such as paraben, benzoic acid, and salicylic acid, and extremely high safety can be obtained.

The antiseptic disinfectant according to the present invention described above can be used in cosmetics, pharmaceuticals, foods and the like.
Specifically, cosmetics for skin such as face wash, lotion, milky lotion, cream, foundation, mascara, nail enamel, lipstick, shampoo, hair treatment, hair nourishing and hair restorer, hair cream, hair lotion, hair foam, Hair cosmetics such as permanent wave agents, medicinal cosmetics (quasi-drugs) with specific uses such as stains and freckles, acne medicines, gargles, lozenges, chewing gum, candy, It can use suitably for foodstuffs, such as a drink and confectionery.

In the case of preparing cosmetics, pharmaceuticals or foods using the antiseptic disinfectant according to the present invention, components usually used in cosmetics, pharmaceuticals or foods can be arbitrarily arbitrarily blended within the range where the effects of the present invention are not impaired. .
Ingredients commonly used in cosmetics and pharmaceuticals (including quasi-drugs) include olive oil, wheat germ oil, turtle oil, camellia oil, castor oil, egg yolk oil, owl, coconut oil, hardened oil and fats; carnauba wax, Waxes such as candelilla wax, montan wax, beeswax, lanolin; hydrocarbons such as liquid paraffin, petrolatum, paraffin, squalane; higher fatty acids such as lauric acid, myristic acid, palmitic acid, stearic acid, oleic acid, lanolin fatty acid; lauryl Alcohol, cetyl alcohol, oleyl alcohol, lanolin alcohol, hydrogenated lanolin alcohol, higher alcohols such as isostearyl alcohol; sterols such as cholesterol, dihydrocholesterol, phytosterol; alkyl linoleate, myristate alcohol Fatty acid esters such as kill, alkyl lanolin fatty acid, hexyl laurate, alkyl oleate; humectants such as glycerin, propylene glycol, 1,3-butylene glycol, polyethylene glycol, sorbitol; nonionic surfactants, cationic interfaces Surfactants such as active agents, anionic surfactants, amphoteric surfactants; guar gum, locust bean gum, karaya gum, gelatin, methylcellulose, sodium alginate, hydroxypropylcellulose, polyvinylpyrrolidone, sodium polyacrylate, carboxyvinyl polymer , Polymer compounds such as polyvinyl methyl cellulose; other inorganic pigments, dyes, fragrances, antioxidants, ultraviolet absorbers, vitamins, astringents, whitening agents, animal and plant extracts, sequestering agents, lower Alcohol, and the like purified water can be exemplified.

  Ingredients usually used in food include animal and vegetable oils such as beef tallow, pork tallow, corn oil, soybean oil, fats such as shortening, margarine, butter, starch, polysaccharides such as sodium carboxymethylcellulose, xanthan gum, agar, cyclodextrin, Examples include sweeteners such as sucrose, glucose, fructose, and xylose, seasonings, spices, coloring agents, and gum base.

  When preparing cosmetics, pharmaceuticals or foods, the compounding amount of the antiseptic disinfectant according to the present invention is not particularly limited, but is 0.01 to 20% by weight, preferably 0.05 to 5% by weight in the composition. Even if it exceeds 20% by weight, no further effect can be expected. If it is less than 0.01% by weight, the antibacterial effect is inferior, which is not preferable.

[Test example: Evaluation of antibacterial effect]
1. Preparation of bacterial solution for inoculation
Pseudomonas aeruginosa IFO13275 (Pseudomonas aeruginosa) was cultured in an agar medium at 35 ° C., then transferred 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.

2. Preparation of dilution series of test substance 5%, 4, 3, 2.5, 2.25, 2, 1.75, 1.5, 1.25, 1 w / w A v% 1,2-octanediol solution was prepared.
Moreover, about terpinen-4-ol and an equal weight mixture of 1,2-octanediol and terpinen-4-ol, a dilution series was prepared by diluting a 5 w / v% solution twice.

3. Measurement of Minimum Growth Inhibitory Concentration (MIC) Each agar medium to which a dilution series containing the test substance was added was placed in a petri dish, and the inoculum was streaked to a length of about 1 cm.
Cultivation was performed at 35 ° C., and the presence or absence of bacterial growth after 2 days was determined. At this time, the minimum concentration at which no growth was observed was determined as MIC.
As a result, 1,2-octanediol was 2250 μg / ml, terpinen-4-ol was 2500 μg / ml, and an equal weight mixture of 1,2-octanediol and terpinen-4-ol was 1250 μg / ml.
The antibacterial activity can be evaluated by the minimum inhibitory concentration (MIC). There is no effect on microorganisms when the concentration of the test substance is low, but growth suppression occurs when the concentration is increased. This degree of growth proceeds depending on the concentration, and finally the growth stops. The concentration at that time is expressed as MIC. Therefore, when the concentration is higher than MIC, the microorganisms are killed.

4). Binary minimum inhibitory concentration Each MIC of the resulting 1,2-octanediol, terpinen-4-ol, and an equal weight mixture of 1,2-octanediol and terpinen-4-ol was converted to 1,2-octanediol and Plotting with respect to the amount of terpinen-4-ol, a binary minimum inhibitory concentration diagram was obtained. The results are shown in FIG.

A binary minimum inhibitory concentration diagram was determined in the same manner as the above method except that linalool was used instead of terpinen-4-ol. The results are shown in FIG.
The MIC of 1,2-octanediol was 2250 μg / ml, the MIC of linalool was 2500 μg / ml, and the MIC of an equal weight mixture of 1,2-octanediol and linalool was 1250 μg / ml.

5. Evaluation of antibacterial effect The action and effect when two kinds of substances having antibacterial properties are blended can be determined by the binary minimum growth inhibitory concentration. Specifically, when two types of substances having antibacterial properties are blended, the resulting action is roughly classified into synergistic action, additive action, and antagonism. The synergistic action is an action in which two drugs act synergistically to further enhance the inherent antibacterial power. The additive action is an action in which the antibacterial powers of the respective drugs are combined. Antagonism is an action when one drug counteracts the antibacterial activity of the other drug. And the determination method of the effect by the binary minimum growth inhibitory density | concentration is a method of measuring MIC by changing each ratio about substance A and substance B, for example, as shown in FIG. 3, and judging from a graph. According to this, when MIC (point A) only for substance A and MIC (point B) only for substance B are connected, the MIC when both substances are used is inside this line (point C) is a synergistic effect in which antibacterial activity is enhanced by the combined use, when it is on the line (point D), when it is an additive action, when it is outside the line (point E), one or both It can be determined that the antibacterial activity is an antagonism that counteracts the antibacterial activity and decreases the antibacterial activity.

6). Results The antibacterial effect when 1,2-octanediol and terpinen-4-ol were mixed was determined from the binary minimum growth inhibitory concentration diagram of FIG.
The antibacterial effect when 1,2-octanediol and linalool were mixed was determined from the binary minimum growth inhibitory concentration diagram of FIG.
As a result, the action when 1,2-alkanediol and terpinen-4-ol were used in combination was a synergistic action in which antibacterial activity was enhanced by the combination.
The action when 1,2-alkanediol and linalool were used in combination was a synergistic action in which antibacterial activity was enhanced by the combined use.
Therefore, it was confirmed that the antibacterial activity inherent to 1,2-alkanediol can be synergistically enhanced by using 1,2-alkanediol in combination with terpinen-4-ol or linalool.

Hereinafter, formulation examples of cosmetics, pharmaceuticals and foods containing the antiseptic disinfectant according to the present invention will be shown.
<Formulation Example 1: Moisturizing cream>
Decaglyceryl monolaurate 1.0
Monostearic acid POE (15) glyceryl 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
1,2-octanediol 0.25
Terpinen-4-ol 0.10
Purified water
Total 100.0% by weight

<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
1,2-hexanediol 0.5
Terpinen-4-ol 0.2
Purified water
Total 100.0% by weight

<Prescription Example 3: Beverage>
Glucose liquid sugar 33.0
Grapefruit juice 64.0
1,2-pentanediol 0.5
Linalool 0.01
Fragrance 0.5
Acidulant appropriate amount
Total 100.0% by weight

The antiseptic disinfectant according to the present invention is an antiseptic disinfectant originally possessed by 1,2-alkanediol by using together 1,2-alkanediol having 5 to 10 carbon atoms and terpinen-4-ol and / or linalool. Can be synergistically enhanced, and is useful as an antiseptic disinfectant for cosmetics, pharmaceuticals, foods and the like.
The cosmetics, pharmaceuticals or foods according to the present invention contain 1,2-alkanediol having 6 to 10 carbon atoms and terpinen-4-ol and / or linalool as antiseptic fungicides. The blending amount of the bactericidal agent can be low or substantially non-blending, and it is useful as a cosmetic, pharmaceutical or food product having high safety.

It is a binary minimum inhibitory concentration diagram of 1,2-octanediol and terpinen-4-ol. It is a binary minimum growth inhibitory concentration diagram of 1,2-octanediol and linalool. It is a figure which shows an example of the method of judging the effect produced by the case where 2 types of substances which have antimicrobial property are mix | blended from binary minimum growth inhibitory density | concentration.

Claims (4)

An antiseptic disinfectant comprising a 1,2-alkanediol having 5 to 10 carbon atoms and terpinen-4-ol and / or linalool. The antiseptic disinfectant according to claim 1, wherein the 1,2-alkanediol is 1,2-hexanediol and / or 1,2-octanediol. The antiseptic disinfectant according to claim 1, wherein the 1,2-alkanediol is 1,2-octanediol. A cosmetic, pharmaceutical or food product comprising a preservative bactericidal agent containing 1,2-alkanediol having 6 to 10 carbon atoms and terpinen-4-ol and / or linalool .

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