JP2002193755A - Antidandruff and anti-itching hair cosmetic and hair- shampooing cosmetic - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide an antidandruff and anti-itching hair cosmetic, hair- shampooing cosmetic and hair shampoo for animals (pets) that has high safety to the skin, high stability in the preparation or on the skin, can be reduced in the formulation amount, because it has stronger antimicrobial properties in comparison with the conventional active ingredients with higher immediate effectivity with higher skin-staying properties. SOLUTION: The objective hair cosmetic characteristically includes lanoconazole represented by the following chemical formula (1) as an active ingredient. This lanoconazole is also used as an active ingredient for human hair cosmetic and for hair-washing agent for animals (pets).

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a hair cosmetic, a hair washing cosmetic and a hair cleansing agent for animals (pets). More particularly, the present invention relates to lanconazole as an active ingredient, which is effective for skin safety. Higher stability in the formulation or on the skin, higher antibacterial properties than conventional active ingredients, can be set at a lower amount, has high immediate effect, and protects the skin (scalp), Skin (scalp)
The present invention relates to a hair cosmetic, a hair wash cosmetic, and a hair cleanser for animals (pets) having a high storability and having an excellent dandruff / kayumi prevention / deterrent effect.

[0002]

2. Description of the Related Art As methods for preventing dandruff, keratinization control, microbial control, sebaceous gland control and the like have been known. Trying to achieve the goal using. The main cause of the occurrence of dandruff and Kayumi is microorganisms present on the scalp.
The theory is that it is due to the proliferation of ur). Miconazole nitrate, zinc pyrithione, sulfur, selenium disulfide, and the like have been used as antidandruff and anti-swelling agents based on antibacterial properties.

[0003] However, many of these dandruff and kayumi preventive agents are hardly soluble or insoluble in shampoos, and when such components are used, they are greatly restricted in formulation in order to maintain the dispersion stability of the drugs. However, the shampoo itself had a disadvantage that its performance such as foaming and feeling of shampoo was considerably inferior to that of a general shampoo. For this reason, attempts have been made to incorporate triclosan, triclocarban, trichlorocarbanilide, pyrocton olamine, solubilized sulfur, and the like as a type of dandruff and anti-dandruff agent that is easily dissolved in shampoo. However, when these ingredients are blended with shampoo, the antibacterial properties and immediate effect are significantly reduced,
There is a problem that the compounding amount is suppressed to be low due to irritation and coloring properties, and the effect of preventing dandruff and kayumi cannot be sufficiently exerted.

[0004] In addition, as substances which are not based on antibacterial properties and have an effect of inhibiting dandruff and kayumi, α-tocopherol, vitamin A ester (JP-A-51-73137), pantothenic acid and hydroquinone glycoside ( Japanese Patent Application Laid-Open No. 61-21002) has been proposed, but has the drawback that the effect of preventing dandruff and kayumi is not sufficient, and that it lacks immediate effect and stability when compared with a drug based on antibacterial properties. . As described above, although various hair cosmetics and hair wash cosmetics for preventing dandruff and kayumi have been developed, there are problems with their effects, safety and formulation stability. The development of an excellent material which showed no irritation or coloration and maintained the effect of preventing dandruff and Kayumi was a continuing challenge.

[0005]

SUMMARY OF THE INVENTION Accordingly, an object of the present invention is to provide a composition having a high safety to the skin, a high stability in a preparation or on the skin, a high antibacterial property as compared with the conventional active ingredient, and a low compounding amount. Hair cosmetics, hair wash cosmetics and animals that have an excellent dandruff, scalp prevention and deterrent effect that can be used, have a high immediate effect, protect the skin (scalp), and have a high skin (scalp) retention of components. An object of the present invention is to provide a (pet) hair cleaner.

[0006]

In view of this situation, the present inventor has found that the safety of the skin is high, the stability in the preparation or on the skin is high, and the antibacterial property is stronger than that of the conventional active ingredient. Studies have been conducted to obtain hair cosmetics and shampoo cosmetics that have a small amount of dandruff and have excellent dandruff and Kayumi prevention and deterrent effects. As a result, by blending lanoconazole used as an antifungal agent, the safety to the skin is high, the stability in the formulation or on the skin is high,
Excellent anti-dandruff, strong in antibacterial properties compared to conventional active ingredients, can be set at a lower amount, has high immediate effect, protects skin (scalp), and has high skin (scalp) retention of ingredients.
The present inventors have found that hair cosmetics, hair wash cosmetics and animal (pet) hair cleansing agents having a Kayumi prevention / deterrent effect can be obtained, and have completed the present invention.

That is, according to the present invention, the following chemical formula
The present invention provides a hair cosmetic, a hair wash cosmetic, and a hair cleanser for animals (pets), characterized by containing lanconazole represented by (1) as an active ingredient.

Embedded image Chemical formula (1)

[0008] The hair cosmetic and the hair wash cosmetic of the present invention are:
High skin safety, high stability in the formulation or on the skin, high antibacterial properties compared to conventional active ingredients, can be set at a lower amount, has high immediate effect, and improves skin (scalp) Protect and have high skin (scalp) retention of ingredients,
Has excellent dandruff and Kayumi prevention and deterrent effects. Animal (pet) hair cleaners have the same mechanism of action as hair and hair wash cosmetics, thereby suppressing the growth of microorganisms on the epidermis of animals and preventing the occurrence of dandruff and the occurrence of mites And has the effect of keeping the pet clean.
In addition, the animal is prevented from scratching the epidermis with nails in order to prevent Kayumi, which has the effect of keeping the environment clean.

[0009]

BEST MODE FOR CARRYING OUT THE INVENTION In the hair cosmetics and the hair wash cosmetics of the present invention, lanconazole represented by the above chemical formula has a strong dandruff / kayumi prevention / deterrent effect on the scalp or animal epidermis. Lanoconazole is a known compound that is practically used as a pharmaceutical antifungal agent (repellent for athlete's foot) because of its strong antibacterial activity and high skin retention. The compound is a white crystalline powder and is dissolved in ethanol at about 1%.

The hair cosmetics, hair wash cosmetics and animal (pet) hair cleansers of the present invention include pharmaceuticals, quasi-drugs, and cosmetics. For example, it can be formulated into known forms such as hair shampoo, hair rinse, hair cream, hair tonic, hair treatment, hair liquid, hair spray, hair mousse, aerosol and the like.

The above-mentioned hair cosmetics, hair wash cosmetics, and animal (pet) hair cleansing agents may be used alone in the preparation, or may be used to prevent dandruff and kayumi in order to enhance the effect. Active ingredients can be used in combination. Examples of active ingredients that can be used in combination include dandruff and
Miconazole nitrate, ketoconazole, zinc pyrithione, pyrocton olamine, benzalkonium chloride, triclosan, triclocarban, trichlorocarbanilide, sulfur, selenium disulfide, solubilized sulfur, etc., which are substances usually used as active ingredients for preventing Kayumi, Alternatively, by using benzoate, a substance having antibacterial properties, salicylic acid, sorbic acid, dehydroacetic acid, hinokitiol, resorcinol, alcohols, etc. in combination, it is possible to enhance the anti-dandruff / kayumi effect of the substance of the present invention. it can.

In addition, for example, vitamins such as vitamin A, vitamin E, nicotinic acid, nicotinamide, and biotin; cooling agents such as camphor and menthol; anti-inflammatory agents such as lysozyme chloride, glycyrrhizinate, and allantoin; Cell activators such as assembly extract, carrot extract, rosemary extract, aloe extract, placenta extract, and malt root extract can be appropriately selected and used freely. In addition, various additives such as known humectants, thickeners, preservatives, antioxidants, ultraviolet absorbers, stabilizers, colorants, and the like, as necessary, base components such as surfactants and fats and oils. Can be added.

Examples of the surfactant include lauryl sulfate, coconut oil fatty acid sulfate, palm oil fatty acid sulfate, polyoxyethylene lauryl sulfate, palm oil fatty acid glutamate, lauryl phosphate, laurin. Acid, stearic acid, myristic acid, oleic acid, coconut oil fatty acid, hydrogenated coconut oil fatty acid, tallow fatty acid, lauryl dimethyl acetate betaine, coconut oil dimethyl acetate betaine, palm oil fatty acid dimethyl acetate betaine, coconut oil sucrose ester, glyceride Mono fatty acid esters, polyoxyethylene hydrogenated castor oil and the like can be used.

The fats and oils include, for example, olive oil, camellia oil, castor oil, jojoba oil, rapeseed oil, hardened oil, mink oil and the like.

As the humectant or thickener, for example,
Ceramides, dermatan sulfate, sodium alginate,
Examples thereof include carrageenan, guar gum, chondroitin sulfate, casein, sodium carboxymethylcellulose, crystalline cellulose, cationized dextran, carboxyvinyl polymer, sodium polyacrylate, polyvinyl alcohol, and polyvinylpyrrolidone.

Examples of the preservative include benzoate, salicylic acid, sorbic acid, dehydroacetic acid, paraoxybenzoate, benzalkonium chloride, hinokitiol, resorcinol, alcohols and the like.

Examples of the antioxidant include dibutylhydroxytoluene, butylhydroxyanisole, propyl gallate and the like.

Examples of the ultraviolet absorber include 4-methoxybenzophenone, octyldimethylparaaminobenzoate, ethylhexylparamethoxycinnamate,
Examples include titanium oxide, kaolin, and talc.

Examples of the stabilizer include chelating agents such as ethylenediaminetetraacetic acid, pyrophosphate, hexametaphosphate, citrate, tartaric acid, and gluconic acid, and sodium hydroxide, potassium hydrogen phosphate, and citric acid. pH
Each of the adjusting agents can be exemplified.

The amount of lanoconazole used in the present invention may be appropriately changed depending on the degree of symptoms, dosage form, etc., but is usually about 0.001 to 10% by weight, preferably about 0.01 to 1% by weight. Is incorporated into the formulation.

[0021]

EXAMPLES Next, there will be given prescription examples of the hair cosmetics and the hair wash cosmetics of the present invention and test examples for showing the effects thereof, but these do not limit the present invention at all. In the proportions in the prescription examples, [appropriate amount] means that the entire prescription is 1
It means the ratio to become 00% by weight.

<Formulation Example 1> Hair shampoo Raw material name% by weight A Disodium edetate 0.01 Paraoxybenzoate 0.3 1,3-butylene glycol 7.0 Lananoconazole 0.05 Citric acid 0.5 Purified water Quantity B Coconut oil fatty acid methyl methyl taurine sodium 20.0 O. E. FIG. Sodium lauryl ether sulfate 20.0 amidopropyl betaine laurate 10.0 ethylene glycol distearate 2.0 O. E. FIG. The components belonging to lauryl ether 1.0 A are dissolved by heating. Separately, the components belonging to B are dissolved by heating. B was added to A, stirred, emulsified and then cooled to produce a hair shampoo.

<Formulation Example 2> Hair rinse Raw material name wt% A Cetyl alcohol 5.0 Isopropyl palmitate 5.0 Decamethylcyclopentasiloxane 5.0 Jojoba oil 2.0 Lanoconazole 0.07 Methylpolysiloxane 2.0 Polyoxy Ethylene oleyl ether 1.0 Stearyltrimethylammonium chloride 2.0 B Glycerin 10.0 Cationized cellulose 0.3 Paraoxybenzoate 0.4 Purified water Suitable amount A component belonging to A is heated and dissolved. Separately, the components belonging to B are dissolved by heating. B was added to A, stirred, emulsified, and cooled to produce a hair rinse.

<Formulation Example 3> Hair tonic Raw material name% by weight A Polyoxyethylene hydrogenated castor oil 1.0 Pepper tincture 0.2 Tocopherol acetate 0.05 95% Undenatured ethanol 50.0 Lanoconazole 0.2 B Paraoxybenzoic acid Ester 0.4 95% Undenatured alcohol 5.0 Purified water Amount The components belonging to A are dissolved by heating. Separately, the components belonging to B are dissolved. B was added to A, stirred, mixed, and cooled to produce a hair tonic.

<Formulation Example 4> Hair treatment Raw material name% by weight A Glyceryl tri-2-ethylhexanoate 5.0 Squalane 5.0 Liquid paraffin 10.0 Cetyl alcohol 5.0 Stearyl alcohol 5.0 Highly polymerized methylpolysiloxane 2.0 Polyoxyethylene Cetyl Ether 2.0 Stearyl Trimethylammonium Chloride 2.0 Lanoconazole 0.1 Purified Water Appropriate Amount B Glycerin 10.0 Propylene Glycol 5.0 Xanthan Gum 0.5 Paraoxybenzoate 0.3 A The components are dissolved by heating. Separately, the components belonging to B are dissolved by heating. B was added to A, stirred, emulsified and then cooled to produce a hair treatment.

<Formulation Example 5> Aerosol Raw material name% by weight A Highly polymerized methylpolysiloxane 1.0 Methylpolysiloxane 1.0 Tocopherol acetate 0.05 Cetanol 1.5 Stearyltrimethylammonium chloride 1.0 Propylene glycol 4.0 95 % Undenatured ethanol 10.0 Lanoconazole 0.1 Purified water Appropriate amount B Liquefied petroleum gas (propellant) 7.0 A component belonging to A is uniformly mixed and dissolved, put into an aerosol container, and B is filled into the container by a standard method. To produce an aerosol.

<Formulation Example 6> Hair spray Raw material name% by weight A 95% unmodified ethanol 30.0 Highly polymerized methylpolysiloxane 2.0 Methylpolysiloxane 2.0 2-Ethylhexyl paramethoxycinnamate 3.0 Polyoxyethylene Hardened castor oil 1.0 Polyoxyethylene / methyl polysiloxane copolymer 2.0 Lanoconazole 0.1 Purified water qs Dissolve the ingredients belonging to A by heating, stir, mix, cool, and fill in a spray container. A hair spray was manufactured.

<Test Example 1> The results of human tests on the effect of the shampoo containing 0.05% of lanconazole in Formulation Example 1 on the prevention of dandruff and kayumi are shown. As a comparative example, the results of human tests on the effect of a shampoo containing 0.5% zinc pyrithione in place of lanconazole in Formulation Example 1 for preventing dandruff and kayumi are shown.

1) Test subjects 25 test subjects were male volunteers.

2) Test method In order to eliminate the influence of the commercial shampoo used until the test, 20 male volunteers were given a shampoo (base shampoo) excluding lanconazole from Formulation Example 1 for 3 weeks after the start of the test. The hair was washed at least four times a week. After using the base shampoo, the hair was washed four or more times a week using the shampoo of Formulation Example 1 (shampoo containing 0.05% lanconazole) for 4 weeks. Every week, measurement was performed on a specific day of the week determined for each volunteer, and hair was washed on the day before the measurement. To five male volunteers,
Similarly, the hair was washed with a base shampoo for three weeks after the start of the test. For 4 weeks after using the base shampoo, shampoo containing 0.5% zinc pyrithione instead of lanconazole in Formulation Example 1 (zinc pyrithione 0.5%)
% Shampoo). Every week, measurement was performed on a specific day of the week determined for each volunteer, and hair was washed on the day before the measurement.

3) Method of measuring dandruff The volunteers used a hairbrush to scrape the entire scalp evenly and strongly for exactly 2 minutes, and dropped dandruff on black paper. After removing hair and dust from the collected dandruff, all the dandruff was placed on a medicine wrapper, and the total weight (mg) of the dandruff of each volunteer was measured using an electronic balance.

4) Evaluation method of Kayumi Kayumi on the scalp was examined by self-report of volunteers. In the self-assessment, Kayumi was selected from the following four levels every week and self-reported with a number from 0 to 3. Level 0 (No Kayumi): No Kayumi at all Level 1 (Mild Kayumi): Feel a little Kayumi,
Sometimes lightly scratches the scalp Level 2 (Medium Kayumi): Feels clear and sometimes scratches the scalp Level 3 (Strong Kayumi): Feels strong Kayumi
Frequently scratching the scalp

5) Method for measuring dandruff microorganisms (fungi) All the dandruff collected by each volunteer and used for the weight measurement were put into a sterilized Erlenmeyer flask containing 100 mL of physiological saline, and mixed by shaking 50 times. 1 mL thereof was placed in a petri dish. Approximately 15 mL of a fungal medium (potato dextrose agar medium, Nissui Pharmaceutical) was added to each dish, and the mixture was pulverized and cultured at 25 ° C. for 4 days. Was calculated.

6) Test results The following Tables 1 to 10 show the results. Description of Tables 1 and 2 Table 1 shows the fluctuation of the total amount of dandruff of each volunteer in the shampoo group containing 0.05% lanconazole. Table 2 shows the change in the total amount of dandruff (%) when the sample shampoo was used, assuming that the total amount of dandruff after using the base shampoo for 3 weeks was 100% for each volunteer in the group using the shampoo containing lanconazole 0.05% shown in Table 1. Was. 1 out of 20 volunteers
A clear decrease in dandruff was observed in 8 subjects.

[0035]

[Table 1]

[0036]

[Table 2]

Description of Tables 3 and 4 Table 3 shows changes in the total amount of dandruff of each volunteer in the group using the shampoo containing 0.5% zinc pyrithione. Table 4 shows the change in the total amount of dandruff (%) when the sample shampoo was used, assuming that the total amount of dandruff after using the base shampoo for 3 weeks was 100% for each volunteer in the group using the shampoo containing zinc pyrithione 0.5% shown in Table 3. Was. Decrease in dandruff was observed in 3 out of 5 volunteers, but the decrease was observed from the third or fourth week.

[0038]

[Table 3]

[0039]

[Table 4]

Description of Table 5 Table 5 shows the results of self-report of Kayumi of each volunteer of the group using the shampoo containing 0.05% lanconazole. Thirteen out of twenty volunteers showed a clear decrease in Kayumi, with a total score of lanconazole 0.05%.
There was a clear decrease after using the combination shampoo.

[0041]

[Table 5]

Description of Table 6 Table 6 shows the self-report results of Kayumi of each volunteer of the group using the shampoo containing 0.5% zinc pyrithione. No apparent decrease in Kayumi was observed in 5 volunteers.

[0043]

[Table 6]

Description of Tables 7 and 8 Table 7 shows the change in the number of dandruff microorganisms (fungi) of each volunteer in the group using the shampoo containing 0.05% lanconazole. Base shampoo 3 of each volunteer shown in Table 7
Table 8 shows the change in the number of microorganisms (fungi) (%) when the sample shampoo was used, assuming that the number of microorganisms (fungi) after weekly use was 100%. A clear decrease in the number of microorganisms (fungi) was observed in 19 out of 20 volunteers.

[0045]

[Table 7]

[0046]

[Table 8]

Description of Tables 9 and 10 Table 9 shows the change in the number of dandruff microorganisms (fungi) of each volunteer in the group using the shampoo containing 0.5% zinc pyrithione. Base shampoo 3 of each volunteer shown in Table 9
Table 10 shows the change in the number of microorganisms (fungi) (%) when the sample shampoo was used, assuming that the number of microorganisms (fungi) after weekly use was 100%. A decrease in the number of fungi was observed in two of the five volunteers, but from the third or fourth week.

[0048]

[Table 9]

[0049]

[Table 10]

As described above, the lanconazole of the present invention was superior to zinc pyrithione used in Comparative Examples in terms of its effectiveness against dandruff and Kayumi and in reducing the number of microorganisms, and was excellent in the rapidity and effectiveness of exerting its effects. The same effects as in Formulation Example 1 were observed in Formulation Examples 2 to 6.

[0051]

EFFECTS OF THE INVENTION The hair cosmetics and shampoos containing the lanconazole of the present invention have high safety to the skin, high stability in the preparation or on the skin, and high antibacterial properties as compared with conventional active ingredients. The compounding amount can be reduced and the skin (scalp) is protected, and it has an excellent dandruff and Kayumi prevention / deterrent effect. The animal (pet) hair cleaner containing lanconazole of the present invention has the same safety and action as hair cosmetics and hair wash cosmetics, suppresses microbial growth on the epidermis of animals, and prevents dandruff. At the same time, it has the effect of suppressing the occurrence of mites and keeping pets clean.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (Reference) A61P 17/00 171 A61P 17/00 171 31/04 31/04 F term (Reference) 4C083 AA122 AB052 AC022 AC072 AC102 AC122 AC182 AC302 AC352 AC392 AC432 AC482 AC532 AC712 AC782 AC792 AC812 AC861 AC862 AD132 AD152 AD162 AD352 AD662 CC31 CC33 CC38 CC39 DD08 DD23 DD31 EE12 EE23 4C086 AA01 AA02 BC38 GA04 GA07 MA01 MA04 NA14 ZA92 ZB21 ZC61

Claims (3)

[Claims] A hair cosmetic comprising lanconazole represented by the following chemical formula (1) as an active ingredient. Embedded image Chemical formula (1) 2. A hair wash cosmetic comprising lanconazole represented by the above chemical formula (1) as an active ingredient. 3. A hair cleansing agent for animals (pets), comprising lanconazole represented by the chemical formula (1) as an active ingredient.