JP5013765B2 - Antiseptic disinfectant, cosmetics, pharmaceuticals or foods containing the antiseptic disinfectant - Google Patents

Description

  The present invention relates to an antiseptic disinfectant and a cosmetic, pharmaceutical product or food containing the antiseptic disinfectant.

  Parabens, benzoic acids, salicylic acids and the like are used as antiseptic fungicides in cosmetics (including quasi-drugs), pharmaceuticals and foods. However, the above-mentioned conventional antiseptic disinfectant has a drawback that the concentration range in use is easily limited because of low safety such as high skin irritation. For example, the use restriction concentration of paraben and benzoate is 1%, and the use restriction concentration of benzoic acid and salicylic acid is 0.2%. In addition, since these antiseptic fungicides are easily influenced by pH, the antiseptic antibacterial effect is poor in stability, and the antibacterial antibacterial effect may be significantly reduced by the combined use with other compounding components such as a surfactant. He also had problems. In recent years, the number of people who have allergic reactions to these antiseptic disinfectants has increased, so the consumer safety has become more and more important. Demand for reduced cosmetics and pharmaceuticals is increasing.

  As technologies capable of reducing conventional antiseptic fungicides, compositions for external use (see Patent Document 1) containing a combination of 1,2-pentanediol and 2-phenoxyethanol, and antiseptic fungicides comprising 1,2-alkanediol and parabens are used. (See Patent Document 2). However, these are intended to improve the effect of the preservative by using a conventional preservative and 1,2-alkanediol together, and are not intended to completely eliminate the conventional preservative itself. Also, it was not intended to enhance the antibacterial activity of 1,2-alkanediol.

  Moreover, as a technique which can eliminate the conventional antiseptic disinfectant, a preservative disinfectant composed of 1,2-alkanediol (see Patent Document 3) and a moisturizing agent for detergency or non-detergent cosmetics composed of 1,2-octanediol A bacteriostatic agent (see Patent Document 4) and the like are disclosed. However, when 1,2-alkanediol such as 1,2-octanediol is used alone as an antiseptic disinfectant, a high blending amount may be required to obtain sufficient effectiveness. Since 2-alkanediol has a peculiar raw material odor, a technology capable of exhibiting a sufficient antiseptic sterilization effect even at a low blending amount is desired.

  On the other hand, it has been reported that a grapefruit extract, particularly a grapefruit seed extract, has an antibacterial effect (see, for example, Patent Document 5). However, the antibacterial activity of the grapefruit extract itself is not high, and the present condition is that a sufficient antiseptic effect cannot be obtained even when used as an antiseptic disinfectant for cosmetics and the like.

JP-A-10-53510 JP 11-310506 A Japanese Patent Laid-Open No. 11-322591 JP 2001-48720 A JP 2005-232043 A

  The present invention has been made in view of the prior art, and by using together a 1,5-alkanediol having 5 to 10 carbon atoms and a grapefruit extract, synergistically enhancing antibacterial activity, It is an object of the present invention to provide an antiseptic fungicide capable of enhancing the antibacterial activity inherent to 1,2-alkanediol against various bacterial species, and a cosmetic, a pharmaceutical product or a food containing the antiseptic fungicide.

That is, the present invention
[1] and 1,2-octanediol, antiseptic disinfectants comprising the grapefruit seed extract, and (2) said cosmetic obtained by blending the antiseptic disinfectant according to (1), pharmaceuticals or food < concerning.

  The antiseptic disinfectant of the present invention has the effect of enhancing the antibacterial activity inherent to 1,2-alkanediol against various bacterial species by synergistically enhancing the antibacterial activity. Further, a cosmetic, pharmaceutical product or food containing the antiseptic disinfectant according to the present invention can eliminate the necessity of containing a conventional antiseptic disinfectant such as salicylic acid, benzoic acid, paraben, and the antiseptic disinfectant according to the present invention. Has an excellent antibacterial activity, so that the preservative disinfectant itself can be made into a low blend.

  The antiseptic disinfectant according to the present invention contains 1,2-alkanediol and grapefruit extract as active ingredients.

The first component according to the present invention is 1,2-alkanediol. As the 1,2-alkanediol used, the following formula (1):

R—CH (OH) —CH ₂ —OH (1)
(In the formula, R represents an alkyl group having 3 to 8 carbon atoms.)

A 1,2-alkanediol having 5 to 10 carbon atoms represented by: Specific examples include 1,2-pentanediol, 1,2-hexanediol, 1,2-heptanediol, 1,2-octanediol, 1,2-nonanediol, and 1,2-decanediol. Of these, 1,2-hexanediol and 1,2-octanediol are preferably used, and 1,2-octanediol is more preferably used. In addition, in this invention, these 1 type can also be used individually or in combination of 2 or more types.

  The second component according to the present invention is a grapefruit extract. Examples of grapefruit sites that can be used for extraction include roots, stems, leaves, flowers, fruits, seeds (including immature fruit seeds), and the like. Among them, it is preferable to use a seed extract from the viewpoint of synergistically enhancing the antibacterial activity of 1,2-alkanediol and exhibiting excellent antibacterial activity.

  Examples of the solvent used for extraction include water; alcohols such as methanol, ethanol, 1,3-butanediol, propylene glycol, and glycerin; esters such as ethyl acetate and methyl formate; nitriles such as acetonitrile; diethyl ether and tetrahydrofuran Ethers such as; halogenated hydrocarbon compounds such as chloroform and methylene chloride; and ketones such as acetone and methyl ethyl ketone. These may be used alone or in admixture of two or more. Of these extraction solvents, alcohol is preferred from the viewpoint of preventing skin irritation caused by the residual solvent of the extract.

  In addition, a commercially available product can be used as it is for the grapefruit extract. Examples of commercially available products that can be used include grapefruit seed extract, trade name Desfan (manufactured by Matsuo Pharmaceutical Co., Ltd.), and the like.

  In the antiseptic disinfectant according to the present invention, the content of the first component and the second component described above is not particularly limited, but is 0.1: 1 to 10: 1 by weight, preferably 0.2. : It mix | blends so that it may become 1-5: 1. When the 1,2-alkanediol, which is the first component, is added in an amount exceeding 10 times the content of the second component, and if the amount is less than 0.1 times the antibacterial activity cannot be expected. It is not preferable.

  Since the antiseptic disinfectant according to the present invention contains 1,2-alkanediol as the first component and grapefruit extract as the second component, as shown in the examples described later, Due to the synergistic effect of this component and the second component, an enhancing action with excellent antibacterial activity is exhibited. Therefore, it is not necessary to blend or blend conventionally used antiseptics such as parabens, benzoic acids, and salicylic acids, and an extremely safe antiseptic can be obtained.

  The antiseptic disinfectant of the present invention can be used in cosmetics, pharmaceuticals, foods 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. Cosmetics for specific hair use such as hair cosmetics, stains and freckles (quasi-drugs), acne medicines, gargles, lozenges, and other foods such as chewing gum, candy, and drinking water Can be used.

  When preparing cosmetics, pharmaceuticals or foods using the antiseptic disinfectant of the present invention, in addition to the above-described components, components usually used for cosmetics, pharmaceuticals or foods as long as the effects of the present invention are not impaired. Can be blended as appropriate. For example, in the case of cosmetics (including quasi-drugs) and pharmaceuticals, fats and oils, waxes, higher fatty acids, lower alcohols, higher alcohols, sterols, fatty acid esters, humectants, surfactants, polymer compounds, inorganic pigments , Pigments, antioxidants, ultraviolet absorbers, vitamins, astringents, whitening agents, animal and plant extracts, sequestering agents, purified water, and the like. In the case of food, animal and vegetable oils, polysaccharides, sweeteners, colorants, gum bases and the like can be exemplified.

  When the antiseptic disinfectant of the present invention is blended in cosmetics, pharmaceuticals or foods, the blending amount is not particularly limited, but is 0.01 to 20% by weight, preferably 0.05 to 5% by weight in the composition. This is because when the amount is less than 0.01% by weight, the antibacterial effect is inferior, and even if the amount exceeds 20% by weight, no further effect can be expected.

Example 1
(Test bacteria)
As test bacteria, Escherichia coli IFO3972 (Escherichia coli), which is a gram-negative bacterium, and Staphylococcus aureus IFO13276 (staphylococcus aureus), which is a gram-positive bacterium, were used.

(Preparation of bacterial solution for inoculation)
As a bacterial solution for inoculation, after culturing at 35 ° C. on an agar medium, it was further 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.

(Preparation of dilution series of test substance)
5, 4-, 3, 2.5, 2.25, 2, 1.75, 1.5, 1.25, 1 w / v% 1,2-octane using 20 w / w% ethyl cellosolve as a diluent solvent A diol solution was prepared. For grapefruit seed extract (trade name Desfan, manufactured by Matsuo Pharmaceutical Co., Ltd.) and an equivalent mixture of 1,2-octanediol and grapefruit seed extract, double the 5 w / v% solution. A dilution series was prepared.

(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. The culture was performed at 35 ° C., and the presence or absence of growth of the bacteria after 2 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.

(Dual minimum inhibitory concentration)
The MICs of the obtained 1,2-octanediol, grapefruit seed extract, and the mixture of 1,2-octanediol and grapefruit seed extract were determined based on the blending amount of 1,2-octanediol and grapefruit seed extract. And a binary minimum inhibitory concentration diagram was obtained.

  In addition, the effect at the time of mix | blending two types of substances which have antimicrobial property can be determined with a binary minimum growth inhibitory density | concentration. Specifically, when two types of substances having antibacterial properties are blended, the action caused by the substances is roughly classified into a synergistic action, an additive action, and an antagonistic action. 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 another drug. Then, the method based on the binary minimum growth inhibition concentration diagram is a method of determining from the graph by measuring the MIC for each of the A substance and B substance while changing their ratios, as shown in FIG. According to this, when MIC (point A) in only substance A and MIC (point B) only in substance B are connected, the MIC when both substances are used is on the inner side of this line (point C) is a synergistic effect in which the antibacterial activity is enhanced by the combined use, if it is on the line (point D), if it is an additive action, if it is outside the line (point E), either or both It can be determined that the antagonistic action counteracts the antibacterial activity and decreases the antibacterial activity.

  FIG. 2 shows a binary minimum inhibitory concentration diagram for 1,2-octanediol and grapefruit seed extract.

(Evaluation of antibacterial effect)
From the results of FIG. 2, the combination of 1,2-alkanediol and grapefruit extract synergistically enhances the antibacterial activity inherent to 1,2-alkanediol against gram-negative and gram-positive bacteria. It was recognized that

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
1,2-octanediol 0.25
Grapefruit seed extract 0.1
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
1,2-octanediol 0.5
Grapefruit seed extract 0.2
Purified water residue
Total 100.0

  The antiseptic disinfectant of the present invention enhances the antibacterial activity inherent to 1,2-alkanediol and has an excellent antibacterial activity, as well as high safety. Therefore, the antiseptic of cosmetics, pharmaceuticals, foods, etc. It can be suitably used as a disinfectant.

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. 2 is a binary minimum growth inhibition concentration diagram regarding Example 1. FIG.

Claims (2)

An antiseptic fungicide comprising 1,2-octanediol and a grapefruit seed extract. A cosmetic, pharmaceutical product or food comprising the antiseptic disinfectant according to claim 1.