WO2008038807A1

WO2008038807A1 - External composition for skin

Info

Publication number: WO2008038807A1
Application number: PCT/JP2007/069111
Authority: WO
Inventors: Shigeki Sawamura
Original assignee: Kobayashi Pharmaceutical Co., Ltd.
Priority date: 2006-09-29
Filing date: 2007-09-28
Publication date: 2008-04-03
Also published as: JP5063072B2; JP2008088100A

Abstract

It is intended to provide an external composition for skin capable of imparting a physical feeling of stimulation to the skin, replacing pruritus such as particularly insect bites or hypersensitive skin with a feeling of stimulation, and effectively suppressing pruritus. The external composition for skin is characterized by containing butylhydroxytoluene in a solid state.

Description

Specification

Skin external composition

Technical field

[0001] The present invention relates to a composition for external use on skin having an itching suppression effect, a massage effect and the like.

Background art

[0002] Physically stimulating the skin is known to have effects such as blood circulation promotion, massage, and itching suppression (antipruritus).

[0003] For example, the power of performing massage or the like to obtain a beauty or relaxation effect. At that time, water-insoluble particles are blended as a scrub agent in order to exert a massage effect by physical stimulation. As scrubbing agents, hard scrubbing agents such as polyethylene beads, talmi shell grains, and crystalline cellulose are widely used. Although hard scrubs are excellent in removing dirt on the skin and in massaging the skin, there are cases in which unpleasant skin irritation or foreign body sensation is felt during use.

[0004] In addition, “itch” is defined as “a sensation that causes the skin to break! /, And! /”, And is generally an unpleasant sensation. Symptoms associated with “itch” include various forms such as atopic dermatitis, urticaria, insect bites, dry skin, and hypersensitive skin. Depending on the condition, antihistamines, local anesthetics, moisturizing Agents are used. However, since they penetrate into the inner surface of the skin and involve a scientific approach, it takes time to take effect.

[0005] Against this background, there has been a demand for an external composition for skin that can effectively suppress itching in a short time. Many external preparations for skin used for the purpose of suppressing itching have been known. For example, Patent Document 1 discloses an external preparation for skin containing natural oils and fats and antioxidants. In such external preparations for skin, butylhydroxytoluene is generally added in an amount of about 0.0 ;! to 1% as a preservative, stabilizer, antioxidant and the like. However, these external preparations have also been unable to effectively suppress the skin rather than those intended to irritate the skin.

Patent Document 1: JP 2000-159678 Disclosure of the invention

Problems to be solved by the invention

[0006] The main object of the present invention is to provide an external preparation for skin that gives skin irritation by application and exhibits a comfortable massage effect. Another object of the present invention is to provide an external composition for skin, which can replace itching caused by insects and hypersensitivity skin with irritation, and can effectively suppress itching. Is.

Means for solving the problem

[0007] As a result of intensive studies to solve the above-mentioned problems, the present inventor formulated ptylhydroxytonolene (hereinafter sometimes abbreviated as BHT) into an external preparation in a solid state, and this was applied to the skin. It has been found that a massage effect can be obtained by applying it. BHT is a component that is widely used in external preparations such as cosmetics, but it is a component that is formulated exclusively for anti-oxidation, stabilization, etc., and it has never been recalled for use for purposes such as massage or wrinkles. Power, ivy. The present invention has been completed as a result of further research based on such knowledge.

[0008] The present invention provides the following external composition for skin.

Item 1. A composition for external use on skin, characterized by containing solid-state butylhydroxytoluene (hereinafter referred to as BHT).

Item 2. The external composition for skin according to Item 1, wherein the particle size of BHT is 1000 m or less.

Item 3. A BHT having a particle size of less than 350, a BHT having a particle size of 350 to 500, a particle size of 50;! To 1 000 m, or a combination of two or more BHTs. The composition for external application to skin.

Item 4. The composition for external application to skin according to any one of Items 1 to 3, wherein the BHT content is 10 to 40% by weight.

Item 5. The external composition for skin according to any one of Items 1 to 4, further comprising a water-soluble polymer.

The invention's effect [0009] The external composition for skin according to the present invention is applied directly to the skin, and the BHT in a solid state physically stimulates the skin, so that an appropriate massage stimulus can be given to the skin. In addition, when the composition for external use of the skin of the present invention is applied to an affected area having itching, it can be replaced with a feeling of irritation in a short time by physical stimulation of BHT in a solid state, and the itching is effectively suppressed. can do.

BEST MODE FOR CARRYING OUT THE INVENTION

[0010] The composition for external use of the skin of the present invention is characterized mainly by containing BHT in a solid state. Hereinafter, each component, manufacturing method, application, etc. of the composition for external use of the present invention will be described.

* The antipruritic agent of this invention contains BHT as an essential component. Ptylhydroxytoluene is a compound having a white crystal shape, and both 1S, also called dibutylhydroxytoluene, refer to the same compound ([(CH 3) C] C H (CH 2) OH). BHT, traditionally makeup

3 3 2 6 2 3

It is blended for uses such as antioxidants and stabilizers for foods, pharmaceuticals, foods and the like.

[0011] As BHT, commercially available ones can be used. For example, butyl hydroxytoluene (Sanei Chemical Co., Ltd.), dibutylhydroxytoluene (Eastman Chemica Norre Japan Co., Ltd., Ueno Pharmaceutical Co., Ltd.) API Corporation, Sumitomo Chemical Co., Ltd., Nagase Sangyo Co., Ltd., JGC Universal Co., Ltd., Mitsubishi Wel Pharma Co., Ltd.).

[0012] The particle size of BHT used in the present invention is about lOOOO ^ m or less, preferably about 1000 to 50 to 111, more preferably about 1000 to; about 100 to m, more preferably about 1000 to; About 180 in. Here, BHT having each particle diameter can be obtained by pulverizing BHT with a mortar or the like and then applying it to a sieve having each diameter.

[0013] Further, in the present invention, by using a combination of BHTs having different particle sizes, a more excellent effect can be obtained. Therefore, it is possible to combine BHTs having two or more types of particle sizes in combination. Desirably, for example, BHT having a particle size of less than 350 111, particle size of 350-500 ^ HK BHT, particle size of 50;! Preferred combinations include, for example, (a) 501-; about 1000 m A combination of BHT with a particle size of and ΒΗΤ having a particle size of about 350 to 500 μm; (b) BHT with a particle size of less than 350 [Im and a particle size of about 350 to 500 μm A combination of BHT having

[0014] When two or more types of BHT having a particle size are used in combination, the blending ratio of BHT having each particle size is appropriately set as long as the substitution effect on the irritating feeling of itchiness can be exhibited. For example, in the case of the combination (a) above, when 1 part by weight of BHT having a particle size of about 350 to 500 111 is used, BHT having a particle size of about 501 to 1000 m is set to 0. About 10 to 10 parts by weight, preferably about 0.25 to 7-5 parts by weight, more preferably about 0.5 to 5 parts by weight; with the combination (b) above, about 350 to 500 111 grains In the case of 1 part by weight of BHT having a child diameter, BHT having a particle diameter of less than 350 m is about 0.;! To about 10 parts by weight, preferably about 0.25-7. 5 parts by weight, more preferably 0. Used in combination at a ratio of about 5 to 5 parts by weight.

[0015] Although a limited interpretation of the present invention is not desired, the effects of the present invention can be more remarkably achieved by blending BHT having a non-uniform particle size.

[0016] The amount of BHT in the external composition for skin of the present invention is about 10 to 40% by weight, preferably about 15 to 35% by weight, more preferably about 20 to 30% by weight. With such a blending amount, the massage effect and the antipruritic effect due to skin irritation can be exhibited more significantly while maintaining the stability as a preparation.

[0017] (2) Other ingredients

The composition for external use of the present invention preferably contains alcohol in addition to the BHT. By blending alcohol, solid-state BHT can be dispersed favorably, and the skin can be uniformly and moderately stimulated. The alcohol used in the present invention is not particularly limited as long as it is commonly used in the fields of cosmetics and pharmaceuticals. For example, methanol, ethanol, propanol, isopropanol, butanol, isobutanol and the like are used. Lower alcohol having 1 to 6 carbon atoms, preferably 1 to 3 carbon atoms; propylene glycol, dipropylene glycol, glycerin, 1,3-butylene glycol, butylene glycol, concentrated glycerin, polyethylene glycol, maltitol, mannitol, sorbitol, etc. Examples include polyhydric alcohols. these May be used alone or in combination of two or more. The lower alcohol may be anhydrous or hydrated. In the present invention, it is preferable to use (hydrous) ethanol, absolute ethanol, or isopropanol!

[0018] The blending amount of alcohol in the composition for external use of the present invention is about 0 to 45% by weight, preferably about 4 to 40% by weight, more preferably about 4 to 35% by weight.

The blending ratio of BHT and alcohol in the external composition for skin of the present invention is such that when BHT is 1 part by weight, alcohol is about 3 parts by weight or less, preferably about 2 parts by weight or less, and more preferably about 1 part by weight or less. With such a blending ratio, the solid state of BHT can be maintained and an appropriate stimulus can be given to the skin.

[0020] The external composition for skin of the present invention may contain water, a water-soluble polymer, or the like, if necessary. Conventionally known water-soluble polymers can be used, for example, carboxyvininole polymer, polyvinyl alcohol, polyvinyl methyl ether, polyvinylinoxychetyl cellulose, pullulan, agar, gelatin, alginic acid and its salts, carrageen Examples include naan and gums. These may be used alone or in combination of two or more.

[0021] The amount of water in the external composition for skin of the present invention is about 25 to 89.5% by weight, preferably about 27 to 80.2% by weight, more preferably about 28 to 75% by weight; The amount of the conductive polymer to be combined is about 0.5 to 5% by weight, preferably about 0.8 to 4% by weight, and more preferably about 1 to 3% by weight.

[0022] Typical formulation examples of the present invention, 10 to 40 weight BHT ^_0/0, the Anorekonore 0-45 wt%, a water-soluble polymer 0.5 to 5% by weight, water 25-89. A composition for external use containing 5% by weight is exemplified.

[0023] In addition to the above, the composition for external use of the skin of the present invention includes various components generally used in cosmetics, quasi-drugs, pharmaceuticals, aqueous components, oil-based components, moisturizing components, moisturizing components, and so on. Forms, thickeners, preservatives, antioxidants, pH adjusters, carriers, fragrances, colorants, drugs and the like can be prepared in various dosage forms alone or in combination of two or more. In addition, the composition for external use of the skin of the present invention includes a known local anesthetic and antibacterial agent within the range not impairing the effects of the present invention. For example, local anesthetics such as lidocaine, dibu force in, dibu force in hydrochloride, diphenhydramine, ethyl aminobenzoate, desitthecin; chlorpheniramine maleate, diphenhydramine, diphenhydramine hydrochloride, glycyrrhetinic acid, glycyrrhizin Anti-inflammatory agents such as dipotassium phosphate, monoammonium glycyrrhizinate, allantoin, methyl salicylate; 1-menthol nole, dl-menthol nole, camphor, dl-strengthen, lactic acid menthylate, etc .; Moisturizers such as urea, salicylic acid, sodium hyaluronate Bactericides such as isopropylmethyl phenol, quaternary ammonium salts (benzalkonium chloride, benzethonium chloride, etc.), chlorhexidine hydrochloride, sulfadiazine, etc .; oxyconazole nitrate, butenaf hydrochloride Emissions, hydrochloric Amororufuin, hydrochloric Terubinafuin, antifungal agents such as lanoconazole; capsicum tincture, and the like thermal components such Kabusaishin.

[0024] Examples of the dosage form of the external composition for skin of the present invention include force S that can be prepared into a conventionally known dosage form according to the method of use and application, such as an ointment, lotion, gel, aerosol, and the like. It is done.

[0025] The external composition for skin of the present invention contains an appropriate amount of a base for obtaining a desired dosage form. For example, but not limited to, paraffin, petrolatum, squalane, norafin, white wax, plastibase, polyethylene glycolenore, macrogonole, lauromacronore, silicone oil, silicone, polysorbate, polyoxyethylene hydrogenated castor oil, Oil bases such as olive oil, cottonseed oil, soybean oil, coconut oil; higher alcohols such as cetanol and stearyl alcohol; fatty acid esters (such as isopropyl myristate and sorbitan fatty acid ester), higher fatty acid salt emulsifiers, highly refined egg yolk lecithin , Soybean lecithin, refined soybean lecithin, white beeswax, propylene carbonate, egg yolk phospholipid, egg yolk oil, coconut oil fatty acid, sodium lauryl sulfate, other ionic and nonionic surfactants, etc .; phosphoric acid, acetic acid, salt PH adjusting agents such as acid and sodium hydroxide; propellants such as liquefied petroleum gas and dimethylol ether.

[0026] The composition for external use of the present invention can be prepared by mixing and preparing the above components according to a conventionally known method. Conditions such as temperature in preparation, order of addition of each component, mixing time, etc. should be set as appropriate based on the common general technical knowledge according to the physical or scientific properties of each component, concentration, instrument stress, etc. Is not particularly limited. The external preparation for skin of the present invention comprises For example, it can be prepared by dissolving components soluble in water and alcohol, mixing them and stirring them uniformly, and finally adding BHT.

[0027] The composition for external use of the skin of the present invention can be applied as an antipruritic agent, athlete's foot drug or the like to a place where itching occurs. The application target is not particularly limited as long as it is used for this purpose, but for example, when used as an antipruritic agent, it can be applied to symptom accompanied by itching, insect bite, dry skin, hypersensitive skin, etc. .

[0028] In the present invention, "itch" refers to "a feeling that causes the idea of wanting to break through the skin" as described above.

[0029] When the external composition for skin of the present invention is used for the purpose of reducing the itching, an appropriate amount of the external composition for skin of the present invention may be spread over the itchy part of the skin. By spreading the coating, the solid BHT can physically irritate the itchy part of the skin, replace the itching with a feeling of irritation, and suppress the itching without further rebating. Here, “replacing itching with a sense of irritation” refers to making the skin sensation in a short-term (instantaneous) state of feeling an irritation (feeling itchy) other than “itching”.

[0030] Further, the skin irritation by the external preparation for skin of the present invention is an appropriate stimulation without damaging the skin, and thus can be used for promoting blood circulation at the application site. Therefore, the external preparation for skin of the present invention can also be used as a massage agent, an external anti-inflammatory analgesic or the like.

Example

[0031] Hereinafter, the present invention will be described in more detail with reference to Examples and the like, but the present invention is not limited thereto.

[0032] Based on the formulation shown in Table 1 below, various components were blended to obtain an external composition for skin.

A portion of the amount of water specified in Table 1 was sampled, and the carboxybule polymer was gradually added thereto with stirring. Separately, components other than BHT (Ptylhydroxytoluene: Sanei Chemical Co., Ltd.) and a pH adjuster (triethanolamine) were added to a part of the amount of alcohol specified in Table 1 and mixed with stirring. This solution was gradually added to the aqueous solution mixed with the carboxybutyl polymer while stirring. When adding a pH adjuster (triethanolamine), a mixture of the pH adjuster and the remaining water was further added. Obtained The resulting solution was stirred for a certain time, and finally BHT was added and further stirred to prepare a composition for external use on the skin. Here, BHT used was crushed in a mortar and classified by a sieve having each diameter.

[0033] The obtained external composition for skin was stored at room temperature (about 25 ° C) for 1 week, and its properties were visually confirmed to evaluate the stability. Specifically, dispersibility (presence / absence of particle settling and agglomeration (aggregation of particles)), shape retention (presence / absence of obvious changes compared to initial properties such as viscosity reduction), and particles are solid It was confirmed whether the properties were maintained (softening / dissolution). When there was no change in any of these properties, it was marked as ◯, and when any one of the changes was confirmed, it was marked as X.

[0034] In addition, the composition for external use with a stability evaluation result of “◯” was applied to the affected area of 10 subjects complaining of itching caused by insect bites, etc., and it was easy to apply (one point when it was difficult to apply) 5 points when easy to apply), replacement of itching with irritation (1 point when not replaced with irritation, 5 points when replaced with irritation) and anti-itching effect (when itching does not stop) 1 point and 5 points when itching stops) were evaluated in 5 stages each.

[0035] Furthermore, the obtained composition for external application on skin was applied to the skin of 10 healthy subjects, and with regard to comfortable physical irritation (1 point when not felt, 5 points when felt) Evaluation was performed.

[0036] The scores by each subject were totaled, and the total score was 45-50 points: ◎, 35-45 points: ◯, 25-35 points; Δ, less than 25 points: X.

[0037] Table 1 shows the evaluation results. In the table, CVP represents carboxybulle polymer and PG represents propylene glycol.

[0038] [Table 1]

[0039] In addition, the composition for external use with skin containing particles other than BHT (Comparative Examples;! -32) was also evaluated in the same manner. The results are shown in Table 2-1 and Table 2-2 below.

[0040] In the table, CVP represents a carboxybule polymer, and PG represents propylene glycol.

[0041] [Table 2-1]

[0042] [Table 2-2]

[0043] In the table, Comparative Examples;! To 8, 14, 15, 17-24, 30 and 31 could not be evaluated due to poor stability of the compositions.

[0044] Comparative Examples 9 to 13, 16, 25 to 29, and 32 are compositions for external use in skin that contain conventionally known particles. These external preparations for skin were relatively stable and good, but all of them had a replacement effect on the irritating feeling of itchiness and a pleasant stimulating action. In the preparations in which BHT was dissolved, it was not possible to obtain a sensation of itchiness or a pleasant irritation (data not shown).

[0045] On the other hand, it was shown that all of the compositions for external use of skin in Examples;! To 19 were excellent in stability and softness to application to the skin. In addition, because it contains BHT in a solid state, it can provide a comfortable irritation feeling when applied to the skin, and it also has an anti-itching effect and an action to replace itching with irritation. It was shown that. In particular, it was shown that the combination of BHT with different particle sizes exerted a more comfortable and comfortable irritation, anti-itching effect, and the action of replacing itching with irritation.

[0046] Itching is known that itching is enhanced when a physical stimulus is applied. However, it was shown that the composition for external use of the skin of the present invention has an excellent anti-itching effect as well as a temporary anti-itching effect of replacing itching with a stimulating feeling. That is, the external composition for skin of the present invention has an immediate and long-lasting itch suppression effect.

[0047] Formulation examples are shown below. In the table, CVP represents carboxybutyl polymer, PG represents propylene glycol, HPC represents hydroxypropyl cellulose, DPG represents dipropylene glycol, and 1,3-BG represents 1,3-butylene glycol.

[0048] [Table 3-1] [] D¾¾00934I

Claims

The scope of the claims

[1] A composition for external use on skin, characterized by containing solid-state butyl hydroxytoluene (hereinafter referred to as BHT).

[2] The external composition for skin according to claim 1, wherein the particle size of BHT is 1000 m or less.

[3] BH D with a particle size of less than 350 111, BH D with a particle size of 350-500 m, Particle size 501-;

The external composition for skin according to claim 1 or 2, wherein 0 m of BHT is used alone or in combination of two or more.

[4] The external composition for skin according to any one of claims 1 to 3, wherein the BHT content is 10 to 40% by weight.

[5] The external composition for skin according to any one of claims 1 to 4, further comprising a water-soluble polymer.