JP2014065704A - Skin external composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a composition which can effectively suppress proliferation of bacteria causing skin trouble such as a razor rash.SOLUTION: A skin external composition is prepared by blending of (A) chlorobutanol, (B) antiinflammatory agent, and (C) terpenoid.

Description

  The present invention relates to an external composition for skin.

  Various troubles are associated with the skin. In recent years, attention has been focused on dealing with skin problems not only for women but also for men because of the increased awareness of beautiful skin.

  One of the skin problems peculiar to such men is razor loss, which tends to occur after daily shaving. Losing a razor is also called acne vulgaris, and is a folliculitis and perifollitis that tends to occur on hard bearded parts such as under the chin and nose. It has been reported that folliculitis and periosteumitis are caused by infection with bacteria such as Staphylococcus aureus (Non-Patent Document 1). In daily shaving activities, when shave the skin with a razor or electric shaver, the stratum corneum is often scraped off and the skin is often damaged, and it is easy for bacteria to be infected. It is a skin problem that is likely to occur even in healthy people.

  Bacteria such as Staphylococcus aureus are also considered to cause acne. And if bacteria grow and acne on the part where the beard grows, the skin will become uneven, so it will be easier to create a wound when applying a razor or electric shaver with a shaving that usually has to be done every day, and a vicious circle Invite.

  Therefore, in order to effectively prevent and improve skin troubles such as razor loss, it is required to fundamentally prevent and treat bacteria by suppressing the growth of bacteria, which is one of the major causes.

  Up to now, after-shave lotion and the like are known as methods for adjusting the feel of the skin after shaving. This is intended to give a moist and moisturizing feeling mainly by applying to the skin after shaving. In addition, after shave lotion is usually a liquid agent, and when applied to damaged skin after shaving, etc., it may feel a biting and stinging pain, making continuous use difficult. It was.

  In order to reduce the pain of biting and stinging, which tends to occur when applied to such damaged skin, to make a preparation with a good feeling of use, it is possible to use a cream rather than a liquid. On the other hand, however, there is a problem that the antibacterial power is likely to be reduced because the cream contains an oil (Non-patent Document 2). Moreover, when it is set as a cream agent, the subject that a formulation viscosity etc. become easily unstable by environmental factors, such as light, is also known.

Hino Haruko, Hichikai Journal: 115 (7), 985-994, 2005 Prevention of microbial contamination and antiseptic design technology in cosmetics and external preparations, published by Technical Information Association, 223-229, 2001

  The present invention has been made in view of the above-described prior art, and can provide an external composition for skin that can effectively suppress the growth of bacteria that cause skin troubles and is excellent in usability. Objective.

  As a result of intensive studies to solve the above-mentioned problems, the present inventors cause skin troubles by combining (A) chlorobutanol with (B) an anti-inflammatory agent and (C) a terpenoid. It has been found that the growth of bacteria can be remarkably suppressed. Furthermore, the present inventors have further studied and found that the viscosity stability against light, which is likely to be a problem when used as a cream, can be improved by combining the three components (A) to (C). . Moreover, the composition for external use of skin containing a combination of the three components (A) to (C) is a preparation excellent in usability even when applied to wound skin where irritation is easily felt after shaving or the like. As a result, the present invention has been completed.

Accordingly, the present invention provides the following external composition for skin.
Item 1. A composition for external use on skin containing (A) chlorobutanol, (B) an anti-inflammatory agent, and (C) a terpenoid.
Item 2. (C) The external composition for skin according to Item 1, wherein the terpenoid content is 0.1 w / w% or more based on the total composition.
Item 3. (B) The external composition for skin according to Item 1 or 2, wherein the anti-inflammatory agent is a non-steroidal anti-inflammatory agent.
Item 4. (B) Anti-inflammatory agent is glycyrrhizic acid, glycyrrhetinic acid, stearyl glycyrrhetinate, allantoin, epsilon aminocaproic acid, salicylic acid, methyl salicylate, glycolic salicylate, indomethacin, felbinac, ibuprofen, ibuprofen piconol, ketoprofen, bufexamac, flufenamic acid, butyl Item 4. The external composition for skin according to any one of Items 1 to 3, which is at least one selected from the group consisting of vendazac, piroxicam, suprofen, ufenamate, heparin-like substances, azulene, guaiazulene, and salts thereof.
Item 5. (C) The external composition for skin according to any one of Items 1 to 4, wherein the terpenoid is a monoterpenoid.
Item 6. (C) at least the terpenoid is selected from the group consisting of menthol, camphor, borneol, limonene, anethole, eugenol, geraniol, nerol, myrsenol, linalool, linalool acetate, lavandolol, isoborneol, cineol, pinene, and terpinolene Item 6. The external composition for skin according to any one of Items 1 to 5, which is one type.
Item 7. Item 7. The external composition for skin according to any one of Items 1 to 6, which is used for skin after wounding.
Item 8. Item 8. The external composition for skin according to any one of Items 1 to 7, which is used for the skin after shaving.
Item 9. Item 10. The external composition for skin according to any one of Items 1 to 8, which is a cream.

  ADVANTAGE OF THE INVENTION By this invention, the composition for external use of skin which can suppress effectively the proliferation of the bacteria which causes a skin trouble is provided. In addition, according to the present invention, a composition for external use having excellent light stability can be provided even when a dosage form such as a cream is apt to be unstable to light. Furthermore, according to the present invention, it is possible to provide a composition for external use on the skin that is excellent in use feeling.

In Test Example 3 (light stability test), it is the figure which showed schematic structure of the single cylindrical rotational viscometer used for the viscosity measurement of a formulation. It is a graph which shows the result of Test Example 4 (use feeling evaluation).

Hereinafter, the present invention will be described in detail.
It should be understood that the terms used in the present specification are used in the meaning normally used in the art unless otherwise specified.

(1. Composition for external use on skin)
The external composition for skin of the present invention contains (A) chlorobutanol, (B) an anti-inflammatory agent, and (C) a terpenoid.

(A) Chlorobutanol The composition for external use of the skin of the present invention contains chlorobutanol (hereinafter sometimes referred to as component (A)).
Chlorobutanol is a known compound also called 1,1,1, -trichloro-2-methyl-2-propanol, and may be synthesized by a known method or obtained as a commercial product.

  In the external composition for skin of the present invention, the content of the component (A) is appropriately set according to the formulation form of the external composition for skin. As an example, for the entire external composition for skin ( A) component is 0.01 to 1.5 w / w%, preferably 0.1 to 1.0 w / w%, more preferably 0.1 to 0.5 w / w%.

(B) Anti-inflammatory agent The composition for external use of the skin of the present invention further contains an anti-inflammatory agent (hereinafter sometimes referred to as the component (B)) in addition to the component (A).

  The anti-inflammatory agent is a known component having an action of suppressing inflammation. Anti-inflammatory agents can be distinguished from steroidal anti-inflammatory agents and non-steroidal anti-inflammatory agents from the difference in their basic skeletal structure. Both of them can be used in the composition for external use of the present invention, but it is preferable to use a non-steroidal anti-inflammatory agent in the present invention from the viewpoint that the effects of the present invention can be more reliably exhibited. .

  Non-steroidal anti-inflammatory agent is not particularly limited, for example, glycyrrhizic acid, glycyrrhetinic acid, stearyl glycyrrhetinate, allantoin, epsilon aminocaproic acid, salicylic acid, methyl salicylate, glycol salicylate, indomethacin, ferbinac, ibuprofen, ibuprofen piconol, Ketoprofen, bufexamac, flufenamic acid butyl, bendazac, piroxicam, suprofen, ufenamate, heparin analogues, azulene, guaiazulene, and salts thereof can be mentioned. The non-steroidal anti-inflammatory agent may be a plant extract such as licorice extract, sage extract or rosemary extract containing an anti-inflammatory component such as glycyrrhizic acid.

  The form of the salt of the anti-inflammatory agent is not particularly limited as long as it is a physiologically acceptable salt. For example, a salt with an inorganic base [for example, ammonium salt; alkali metal (sodium, potassium, etc.), alkali Earth metals (calcium, magnesium, etc.), salts with metals such as aluminum, etc.]; salts with organic bases (eg, organic amines such as methylamine, triethylamine, triethanolamine, morpholine, piperazine, pyrrolidine, tripyridine, picoline) Inorganic salts (eg, hydrochloride, sulfate, nitrate, hydrobromide, phosphate, etc.); organic acid salts [eg, monocarboxylate (acetate, trifluoroacetate, etc.) , Butyrate, palmitate, stearate, etc.), polyvalent carboxylate (fumarate, maleate, succinate, malonate, etc.), oxy Carboxylate (lactate, tartrate, citrate, etc.), organic sulfonates (methanesulfonate, toluenesulfonate, tosylate, etc.), etc.] or the like. Among these salts, preferably a salt with an inorganic base and / or an organic base, more preferably a salt with an inorganic base, more preferably an alkali metal salt and / or an ammonium salt, particularly preferably a potassium salt or sodium. Salts and / or ammonium salts.

  In the external composition for skin of the present invention, only one type of anti-inflammatory agent as described above may be blended, or two or more types may be blended.

  From the standpoint that the effects of the present invention can be further enhanced, the anti-inflammatory agent used in the composition for external use of the present invention is preferably glycyrrhizic acid, glycyrrhetinic acid, stearyl glycyrrhetinate, allantoin, epsilon aminocaproic acid and / or Or a salt thereof, more preferably glycyrrhizic acid, glycyrrhetinic acid, stearyl glycyrrhetinate, allantoin and / or a salt thereof, more preferably glycyrrhizic acid, allantoin and / or a salt thereof, particularly preferably. Glycyrrhizic acid and / or a salt thereof (for example, dipotassium glycyrrhizinate, monoammonium glycyrrhizinate, etc.).

In the external composition for skin of the present invention, the content of the component (B) is appropriately set according to the preparation form of the external composition for skin, the type of the component (B), etc. The total amount of the component (B) is 0.01 to 4 w / w%, preferably 0.1 to 4 w / w%, more preferably 0.1 to 2 w / w% with respect to the entire composition. More specifically, the following ranges are illustrated as content of each (B) component with respect to the whole external composition for skin of this invention.
When the component (B) is glycyrrhizic acid, glycyrrhetinic acid, stearyl glycyrrhetinate and / or a salt thereof: These are total amounts, usually 0.01-2 w / w%, preferably 0.1-2 w / w%, more preferably 0.1-1 w / w%;
When component (B) is allantoin and / or a salt thereof: these are total amounts, usually 0.01-2 w / w%, preferably 0.1-2 w / w%, more preferably 0.1-1 w / w%;
When the component (B) is epsilon aminocaproic acid and / or a salt thereof: These are total amounts, usually 0.01 to 1 w / w%, preferably 0.1 to 1 w / w%, more preferably 0.1 to 0.5 w / w%.

Furthermore, in the composition for external skin of the present invention, the ratio of the content of the component (B) to the content of the component (A) is not particularly limited, but from the viewpoint that the effect of the present invention can be exhibited more effectively. For example, per 100 parts by weight of component (A), the total content of component (B) is 1 to 50000 parts by weight, preferably 10 to 40,000 parts by weight, more preferably 20 to 4000 parts by weight. The ratio is illustrated. More specifically, the following ranges are exemplified as the ratio of the content of each component (B) per 100 parts by weight of the content of component (A).
When the component (B) is glycyrrhizic acid, glycyrrhetinic acid, stearyl glycyrrhetinate and / or a salt thereof: the total amount is usually 1 to 2000 parts by weight, preferably 10 to 2000 parts by weight, more preferably 20 to 2000 parts by weight ;
When component (B) is allantoin and / or a salt thereof: these are total amounts, usually 1 to 2000 parts by weight, preferably 10 to 2000 parts by weight, more preferably 20 to 2000 parts by weight;
When the component (B) is epsilon aminocaproic acid and / or a salt thereof: these are the total amount, usually 1 to 1000 parts by weight, preferably 10 to 1000 parts by weight, more preferably 20 to 1000 parts by weight.

  In addition, when using the plant extract containing anti-inflammatory components, such as glycyrrhizic acid, as an anti-inflammatory agent, it sets so that content of the anti-inflammatory component in the plant extract mix | blended may be in the said range.

(C) Terpenoid The external composition for skin of the present invention further contains a terpenoid (hereinafter sometimes referred to as (C) component) in addition to the components (A) and (B).

  Terpenoids are known compounds having a structure having an isoprene unit as a structural unit, and may be any of d-form, l-form, or dl-form. Terpenoids are distinguished by being called monoterpenoids, sesquiterpenoids, diterpenoids, sesterterpenoids, etc., depending on the number of isoprene units constituting the terpenoid. Any of the terpenoids can be used in the external composition for skin of the present invention, but it is preferable to use a monoterpenoid in the present invention from the viewpoint that the effects of the present invention can be exhibited more reliably.

  Examples of monoterpenoids include, but are not limited to, acyclic monoterpenes such as geraniol, nerol, myrsenol, linalool, linalool acetate, and lavandulol; monocyclic such as menthol, limonene, anethole, eugenol, and terpinolene Monoterpenes; bicyclic monoterpenes such as camphor, borneol, isoborneol, cineol, and pinene. As a monoterpenoid, you may use the essential oil containing it. Such essential oils include, but are not limited to, peppermint oil, eucalyptus oil, peppermint oil, bergamot oil, spearmint oil, rose oil and the like.

  Only one terpenoid as described above may be blended in the composition for external use of the present invention, or two or more terpenoids may be blended in combination.

  From the viewpoint that the effects of the present invention can be further enhanced, the terpenoid used in the external composition for skin of the present invention is preferably a monocyclic monoterpenoid and / or a bicyclic monoterpenoid, more preferably. Is menthol (l-menthol, dl-menthol, etc.), camphor (d-camphor, dl-camphor, etc.), borneol (d-borneol, dl-borneol, etc.), more preferably menthol and / or camphor, Particularly preferred is menthol.

In the external composition for skin of the present invention, the content of the component (C) is appropriately set according to the preparation form of the external composition for skin, the type of the component (C), and the like. However, as shown in the results of test examples described later, it has been found that the content of the component (C) is remarkably high when the content of the component (C) is 0.1 w / w% or more, and the effects of the present invention are exhibited. Therefore, although not particularly limited, the total content of the component (C) with respect to the entire skin external composition is usually 0.01 to 4 w / w%, preferably 0.1 to 4 w / w%, more preferably 0.1 to 2 w / w. %, More preferably 0.1-1 w / w%, particularly preferably 0.1-0.3 w / w%. More specifically, the following ranges are illustrated as content of each (C) component with respect to the whole external composition for skin of this invention.
When component (C) is menthol: These are total amounts, usually 0.01 to 2 w / w%, preferably 0.1 to 2 w / w%, more preferably 0.1 to 1 w / w%, still more preferably 0.1 to 0.3 w / w %;
When component (C) is camphor: These are total amounts, usually 0.01 to 2 w / w%, preferably 0.1 to 2 w / w%, more preferably 0.1 to 1 w / w%, still more preferably 0.1 to 0.3 w / w %;
When component (C) is borneol: These are total amounts, usually 0.01-2 w / w%, preferably 0.1-1 w / w%, more preferably 0.1-0.5 w / w%, still more preferably 0.1-0.3 w / w. w%.

Furthermore, in the composition for external use of the skin of the present invention, the ratio of the content of the component (C) to the content of the component (A) is not particularly limited, but from the viewpoint that the effect of the present invention can be exhibited more effectively. For example, per 100 parts by weight of component (A), the total content of component (C) is 1 to 40,000 parts by weight, preferably 10 to 40,000 parts by weight, more preferably 10 to 20000 parts by weight, The ratio is preferably 20 to 10,000 parts by weight, particularly preferably 20 to 600 parts by weight. More specifically, the following ranges are exemplified as the ratio of the content of each component (C) per 100 parts by weight of the content of component (A).
When the component (C) is menthol: these are the total amount, usually 1 to 2000 parts by weight, preferably 10 to 2000 parts by weight, more preferably 10 to 1000 parts by weight, still more preferably 20 to 300 parts by weight;
When component (C) is camphor: These are the total amount, usually 1 to 2000 parts by weight, preferably 10 to 2000 parts by weight, more preferably 10 to 1000 parts by weight, still more preferably 20 to 300 parts by weight;
When component (C) is borneol: These are total amounts, usually 1 to 1000 parts by weight, preferably 10 to 1000 parts by weight, more preferably 10 to 500 parts by weight, and still more preferably 20 to 300 parts by weight.

  In addition, when using the essential oil containing terpenoid components, such as menthol, as a terpenoid, it sets so that content of the terpenoid component in the essential oil mix | blended may be in the said range.

The external composition for skin of the present invention may further contain a moisturizing agent.
By blending a moisturizing agent, the skin after shaving or the like can be moisturized to improve rough skin, and a moist and good feeling of use can be increased.

  The moisturizing agent that can be blended in the external composition for skin of the present invention is not particularly limited. For example, polyhydric alcohols such as glycerin, 1,3-butylene glycol, propylene glycol, and polyethylene glycol; alanine, serine, leucine, and isoleucine. Amino acids such as threonine, glycine, proline, hydroxyproline, glucosamine, and theanine; peptides such as collagen, collagen peptide, and gelatin; sugar alcohols such as sorbitol, and the like. A polyhydric alcohol is preferable.

  The content of the humectant in the external composition for skin of the present invention is not particularly limited, but the total amount relative to the entire composition is usually about 0.1 to 50 w / w%, preferably about 1 to 30 w / w%. Good.

The external composition for skin of the present invention can further contain an oily base.
Compositions containing oils such as oily bases are generally known to be less likely to exert their antibacterial action even if they contain components that exhibit antibacterial action, compared to compositions such as liquids that contain little of them. Yes. However, according to the present invention, by blending the above components (A) to (C), even when a composition containing such an oil component is obtained, a sufficiently high antibacterial action can be exhibited practically. .

  The oily base that may be blended in the external composition for skin of the present invention is not particularly limited. For example, petrolatum (white petrolatum, yellow petrolatum), paraffin, liquid paraffin, light isoparaffin, liquid isoparaffin, ozokerite, ceresin, Hard fat, microcrystalline wax, squalane (synthetic / vegetable), α-olefin oligomer, polyethylene powder, etc .; stearyl alcohol, cetanol, behenyl alcohol, cetostearyl alcohol, hexyl decanol, isostearyl alcohol, octyldodecanol, oleyl alcohol , Higher alcohols such as decyltetradecanol and myristyl alcohol; isopropyl palmitate, isopropyl myristate, octyldodecyl myristate, palmitic acid Examples include ester oils such as cetyl, glyceryl tri-2-ethylhexyl, and medium chain fatty acid triglycerides; polymerized silicones such as dimethylpolysiloxane and dimethylsiloxane; vegetable oils such as olive oil. Preferably, the oily base is a hydrocarbon, higher alcohol and / or ester oil.

  The content of the oily base in the external composition for skin of the present invention is not particularly limited, but is generally 1 to 95 w / w%, preferably about 1 to 30 w / w% as a total amount with respect to the entire composition. Is good.

Furthermore, it is preferable that the external composition for skin of this invention contains surfactant.
By blending the surfactant, the effect of the present invention can be more easily exhibited, and a composition for external use on the skin having high pharmaceutical stability can be obtained.

  The surfactant is not particularly limited, but a surfactant having a hydrophilic-lipophilic balance (HLB) value of usually about 3 to 16, preferably about 8 to 16 is used. Surfactants are distinguished from nonionic surfactants, cationic surfactants, anionic surfactants, and zwitterionic surfactants depending on the ionization of hydrophilic groups. Any of the surfactants used in the composition for external skin of the present invention may be used, but from the viewpoint that the effects of the present invention can be more reliably and easily exhibited, preferably a nonionic surfactant is used. Used.

  The nonionic surfactant that can be blended in the external composition for skin of the present invention is not particularly limited, and examples thereof include polyoxyethylene hydrogenated castor oil; glyceryl fatty acid esters such as glyceryl monostearate and polyglyceryl monostearate; Sorbitan fatty acid esters such as sorbitan oleate and sorbitan monostearate; polyoxyethylene alkyl ethers such as polyoxyethylene behenyl ether, polyoxyethylene stearyl ether and polyoxyethylene cetyl ether; poly such as polyoxyethylene polyoxypropylene cetyl ether Oxyethylene polyoxypropylene alkyl ether; polyoxyethylene sorbitan fatty acid ester such as polyoxyethylene sorbitan stearate; polyoxy stearate Polyoxyethylene fatty acid esters, such as Le; stearate macrogol; lanolin alcohols; and lecithin. Preferably, the surfactant is polyoxyethylene hydrogenated castor oil and / or glycerin fatty acid ester.

  The content of the surfactant in the external composition for skin of the present invention is not particularly limited, but is generally 0.01 to 10 w / w%, preferably about 0.1 to 5 w / w% as a total amount with respect to the entire composition. Is good.

  Moreover, it is preferable that the external composition for skin of this invention contains water-soluble polymer. By blending a water-soluble polymer, the effect of the present invention can be more easily exhibited, and a composition for external use on the skin having high pharmaceutical stability can be obtained.

  The water-soluble polymer that can be blended in the external composition for skin of the present invention is not particularly limited. For example, carboxyvinyl polymer, polyvinyl alcohol (partially saponified product), polyvinyl pyrrolidone, polyethylene glycol, polyvinyl methyl ether, N-acryloyl. Vinyl polymers such as ammonium dimethyltaurine / vinylpyrrolidone copolymer; celluloses such as methylcellulose, ethylcellulose, carboxymethylcellulose, hydroxyethylcellulose, hydroxyethylmethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, carmellose sodium, stearoxyhydroxypropylmethylcellulose Polymers: gum arabic, gum tragacanth, galactan, guar gum, pectin, color Nan, alginic acid, sodium alginate, plant-based polymers such as propylene glycol alginate; xanthan gum, dextran, microbial polymers such as pullulan. Preferably, the water-soluble polymer is a vinyl polymer.

  The content of the water-soluble polymer in the external composition for skin of the present invention is not particularly limited, but is generally about 0.1 to 20 w / w%, preferably about 0.1 to 10 w / w% as a total amount with respect to the entire composition. It is good.

  The external composition for skin of the present invention further comprises a local anesthetic (such as lidocaine), a tissue repair component (such as tocopherol acetate), an antihistamine (such as diphenhydramine, chlorpheniramine), an antipruritic agent, a keratin softener, an astringent, and a hair growth inhibitor. An active ingredient such as an agent, an ultraviolet absorber, an ultraviolet scattering agent, and / or vitamins may be included. Moreover, the composition for external use of the present invention may further contain other antibacterial components (such as isopropylmethylphenol). Thus, by blending other antibacterial components, it is possible to obtain a higher antibacterial action.

  The content of other active ingredients as described above in the external composition for skin of the present invention is not particularly limited, but is generally 0.01 to 30 w / w%, preferably 0.1 to 25 w / w% as a total amount with respect to the entire composition. It is good to be about.

  Moreover, you may mix | blend the additive generally used in the field | area of a pharmaceutical, a quasi-drug, or cosmetics with the composition for external use of this invention as needed. Such additives include aqueous bases (including water), preservatives, pH adjusters, stabilizers, preservatives, colorants, dispersants, antioxidants, chelating agents and / or fragrances. Can be mentioned.

  The content of other additives as described above in the external composition for skin of the present invention is not particularly limited, but is generally 0.01 to 70 w / w%, preferably 0.1 to 30 w / w% as a total amount with respect to the entire composition. It is good to be about.

  The external composition for skin of the present invention can be prepared in various forms according to a conventional method. Examples of forms suitable for application to the skin include creams, emulsions, ointments, mousses, sheets (substrate support), gels, liquids, aerosols, sprays, and the like. . In an embodiment intended to be applied to skin sensitive to irritation after shaving or the like, a cream is preferably used to suppress irritation.

  In the form of emulsified water phase and oil phase (emulsion composition) such as creams and emulsions, oil-in-water (O / W) type, water-in-oil (W / O) type, water-in-oil-in-water type (W / O / W) type or any emulsified form such as oil-in-oil-in-oil type (O / W / O) type, but from the viewpoint that a better feeling of use can be obtained by suppressing stickiness The oil-in-water (O / W) type is preferable.

  The viscosity (25 ° C.) of the external composition for skin of the present invention is not particularly limited, but when applied to the skin, it is about 2000 to 100000 mPa · s from the viewpoint of being difficult to dripping and easy to spread. Preferably, it is about 5,000 to 100,000 mPa · s, more preferably about 5,000 to 100,000 mPa · s. As shown in the test examples to be described later, it was found that the external composition for skin according to the present invention is very stable and hardly changes in viscosity even when exposed to environmental factors such as light that easily cause a change in viscosity. Yes. Therefore, in the composition for external use of the skin of the present invention, it is practically possible to obtain a preparation having a relatively high viscosity as described above. In addition, the above viscosity (25 degreeC) is measured according to the method as described in the below-mentioned test example.

The pH of the external composition for skin of the present invention is not particularly limited, but is preferably about pH 3 to 10, more preferably from the viewpoint that the effect of the present invention can be exerted higher while suppressing irritation when applied to the skin. Is pH
It should be about 4-9.

  The amount and site of application of the external composition for skin of the present invention to the skin are not particularly limited, and any skin that is desired to exhibit an antibacterial action (particularly, an antiproliferative action against bacteria such as Staphylococcus aureus). An appropriate amount (about 0.1 to 0.5 g) may be applied to the part by applying, rubbing or spraying. Examples of the site where it is desired to exert a growth-inhibiting action against S. aureus include, for example, sites where the bacteria tend to cause razor loss (sites where mustache, chin and mustaches grow), Examples include armpits that tend to cause a stinking odor, and parts such as the face, chest, and back where the bacteria tend to cause acne and pimples. According to the present invention, a high antibacterial effect (especially a high S. aureus growth inhibitory effect) can be exerted at such sites, so that skin inflammatory symptoms (redness, razor loss, acne, pimples, etc. caused by those bacteria can be achieved. , Pain, tingling, eczema, etc.) can be effectively prevented, ameliorated and / or treated.

  As shown in the test examples to be described later, the composition for external use of the skin of the present invention has a keratin layer that is thinly scraped after shaving or the like, or a small incision can be made with a razor or an electric shaver. Even when applied to various skin conditions, it is clear that it is excellent in use feeling. Moreover, the site | part of the skin which received the wound in this way is a site | part especially desired to exhibit an antibacterial action also from the point that it is easy to cause the infection by a microbe. In consideration of such points, the stratum corneum is scraped off with a razor or the like on a daily basis, and the skin external composition of the present invention is preferably used in a bearded region and / or an armpit region that is easily damaged. It is particularly preferably used for the part where the stalk grows.

  The timing for applying the external composition for skin of the present invention to the skin is not particularly limited, but may be periodically applied several times a day (for example, about 2 to 3 times), or a razor or an electric shaver by shaving or the like. You may apply when you feel redness, pain, eczema, or tingling, etc.

(2. Method and mode of use)
As described above, according to the present invention, by using a combination of the three components (A) to (C), a high antibacterial action can be exhibited, viscosity stability against light can be improved, or when applied to the skin. Usability can be improved.

Therefore, the present invention also provides the following method embodiments from another viewpoint.
(A) A method for enhancing the antibacterial action of a composition for external skin, comprising adding a chlorobutanol, (B) an anti-inflammatory agent, and (C) a terpenoid to prepare a composition for external skin.
(A) A method for improving the stability of a skin external composition to light, which comprises adding a chlorobutanol, (B) an anti-inflammatory agent, and (C) a terpenoid to prepare a skin external composition.
(A) A method for improving the feeling of use of the external composition for skin, comprising adding a chlorobutanol, (B) an anti-inflammatory agent, and (C) a terpenoid to prepare an external composition for skin.

The present invention also provides the following modes of use from still another viewpoint.
Use of (A) chlorobutanol, (B) an anti-inflammatory agent, and (C) a terpenoid in the manufacture of a composition for external use having enhanced antibacterial activity.
Use of (A) chlorobutanol, (B) an anti-inflammatory agent, and (C) a terpenoid in the manufacture of a composition for external application to the skin with improved stability to light.
Use of (A) chlorobutanol, (B) an anti-inflammatory agent, and (C) a terpenoid in the manufacture of a composition for external use with improved skin feel.

  The kind, content, dosage form, viscosity, application site, application amount, and the like of each component in the method and use as described above are the same as those for the aforementioned external composition for skin.

EXAMPLES The present invention will be described in detail below based on examples, but the present invention is not limited to these examples.
<Test Example 1: Antibacterial test 1>
Each test preparation shown in Table 1 below was evaluated for the growth inhibitory action against Staphylococcus aureus (ATCC6538).

First, according to a conventional method, creams (O / W type) having the formulations shown in Comparative Examples 1 to 7 and Example 1 were prepared in a sterile state. About each obtained formulation, the antibacterial action was evaluated by the method shown below.
First, Staphylococcus
aureus (ATCC6538) was inoculated on the surface of soy bean casein digest slope medium and cultured at 33 ° C. for 24 hours. The cultured cells were aseptically collected with a platinum loop and suspended in an appropriate amount of sterile physiological saline to prepare a bacterial suspension containing about 1 × 10 ^{6 to 7} CFU / mL viable bacteria. The number of viable bacteria in the suspension was measured by separately culturing. Next, 10 g of each test preparation (Comparative Examples 1 to 7 and Example 1) was filled into a 25 mL conical tube (PP). Staphylococcus so that each test preparation has a viable count (final concentration) of about 10 ^4-5 CFU / mL
Aureus bacterial solution (suspended in physiological saline) was inoculated and stirred well to prepare a sample. Samples were stored for 8 hours at 25 ° C., protected from light. After 8 hours, a sample containing bacteria is prepared with a 1% polysorbate 80 solution to an appropriate concentration for counting, and seeded on SCDLP agar medium (lecithin / polysorbate 80 / soybean / casein / digest / agar medium). After culturing overnight at 0 ° C., the number of viable bacteria was determined by counting the number of colonies observed.

  The results are also shown in Table 1 above. As apparent from the results in Table 1, in the preparations (Comparative Examples 2, 3, and 5) each containing (A) chlorobutanol, (B) dipotassium glycyrrhizinate, and (C) 1-menthol alone, chlorobutanol Or when 1-menthol is included, although an antibacterial effect is exhibited a little, it is not enough. In addition, it is difficult to say that a sufficient antibacterial effect is still exhibited even in the preparations (Comparative Examples 4, 6, and 7) containing the above-mentioned components in combination of two. On the other hand, unexpectedly, in Example 1, which was formulated by combining three components of chlorobutanol, dipotassium glycyrrhizinate and l-menthol, it was recognized that a remarkably high antibacterial effect was exhibited synergistically. It was.

  In general, it is known that a cream containing an oil component is inferior in antibacterial action compared to a liquid agent not containing much oil. According to the present invention, even such a cream agent whose antibacterial action is likely to drop exhibits a significantly high antibacterial action and is extremely useful in practice.

<Test Example 2: Antibacterial test 2>
The antibacterial action was evaluated for each test preparation shown in Table 2 in the same manner as in Test Example 1 except that the storage time after inoculation with S. aureus was changed from 8 hours to 24 hours. The results are also shown in Table 2 below.

  As is apparent from the results in Table 2, also in this test example, in Example 2 where (A) chlorobutanol, (B) dipotassium glycyrrhizinate and (C) 1-menthol were combined, extremely high antibacterial activity Was observed to be demonstrated. In addition, from this test example, it was confirmed that the concentration of the component (C) should be 0.1 w / w% or more.

<Test Example 3: Light Stability Test>
Cream agents (Comparative Examples 15 to 19 and Examples 3 to 4) shown in Table 3 below were prepared and evaluated for viscosity stability when irradiated with light.

First, according to Table 3, each cream (O / W type) was prepared according to a conventional method. Each of the obtained test preparations was filled into a 30 mL glass container in an amount of 20 mL, and the viscosity at 25 ° C. was measured under the viscosity measurement conditions described later to obtain an initial viscosity. Thereafter, light irradiation corresponding to 150,000 kJ / m ² was performed with SUNTEST XLS + (Toyo Seiki Seisakusho). After the light irradiation, the viscosity at 25 ° C. was measured in the same manner as before the light irradiation.

A specific method for measuring the viscosity is as follows.
The measurement is based on the test method of “Single Cylindrical Rotational Viscometer (Brookfield Viscometer)” described in the 16th Revised Japanese Pharmacopoeia General Test Method Viscosity Measurement Method Second Method Rotational Viscometer Method TV-10 TVM (Toki Sangyo) was used.
A single cylindrical rotational viscometer is a viscometer that measures torque when a cylinder in a preparation is rotated at a constant angular velocity. The outline of the apparatus is shown in FIG. By establishing experimentally K _B in advance using a viscometer calibration standard solution, it is possible to calculate the viscosity of the formulation η by the following equation.
η = _{K B} × T / ω
η: Viscosity of liquid (mPa · s)
K _B : Equipment constant (rad / cm ³ )
ω: Angular velocity (rad / s)
T: Torque acting on the cylindrical surface (10 ⁻⁷ N · m)

(Viscosity measurement conditions)
Measurement temperature 25 ℃
Measured value The viscosity after 1 minute was taken as the measured value.
Rotation speed and rotor No.
Viscosity 5000mPa ・ s or more, rotation speed 12rpm, rotor No.M4
Viscosity 5000mPa ・ s or less Rotation speed 30rpm, Rotor No.M3

The viscosity (25 ° C) of the unirradiated preparation and the post-irradiation preparation is measured under the above conditions, the viscosity of the unirradiated preparation is taken as 100, and the viscosity of the preparation after irradiation is expressed as a relative viscosity. The reduction rate (%) was calculated as in the following formula I.
Viscosity reduction rate (%) = 100− {viscosity after irradiation (25 ° C.) / Viscosity of unirradiated preparation (25 ° C.) × 100} (Formula I)

  The viscosity reduction rate after light irradiation calculated for each test preparation is also shown in Table 3 above. As a result, the creams of the examples containing the three components (A) to (C) were stable without significantly decreasing or increasing the viscosity due to light irradiation. In particular, when the concentration of component (C) is 0.1 w / w% or higher, the viscosity reduction rate after light irradiation is only 4.86%, and a high-viscosity preparation of about 40,000 mPa · s (25 ° C) However, it was confirmed that the cream preparation was extremely stable even when exposed to light.

<Test Example 4: Usability Evaluation 1>
For each test preparation shown in Table 4 below, sensory evaluation on the feeling of use was performed.

  First, a male subject was shaved with a razor, and then each test preparation was applied in an appropriate amount to the shaved skin, and immediately after that, each evaluation item (film feeling, smooth skin) Now, for the refreshing feeling, a score was given in a five-step evaluation from 1 (not felt) to 5 (feel). Next, each of the intermediate points is converted to 0 so that 1 point (−2), 2 points (−1), 3 points (0), 4 points (+1), and 5 points (+2) are converted. The sum was calculated from the converted values of the subjects. The evaluation results are shown in FIG.

  It is generally known that creams are superior to liquids in that they are less likely to feel biting and stabbed pain in sensitive skin (for example, after being shaved and sensitive skin). ing. Furthermore, as is clear from the results of this test, the preparation containing the three components (A) to (C) of the present invention has a coating feeling that covers rough skin, smoothness of the skin, and a refreshing feeling. In terms of the point, it was confirmed that the preparation was comprehensively good.

<Test Example 5: Antibacterial test 3>
About the external composition for skin of this invention shown in following Table 5, the antimicrobial activity with respect to Staphylococcus aureus was evaluated. Specifically, a bacterial suspension was prepared according to the same procedure as in Test Example 1 above, and the bacterial solution was inoculated into 10 g of the cream (O / W type) prepared in Example 6 according to the conventional method. (Bacterial concentration: 134500 cfu / mL), well stirred, and stored at 25 ° C. in the dark. A test sample was taken out 4 hours and 8 hours after the start of storage, and the number of viable bacteria contained in the sample was determined in the same procedure as in Test Example 1. The results are also shown in Table 5 below.

  As is apparent from the results in Table 5, a significant decrease in the number of viable bacteria was observed even after 4 hours from the inoculation, and the number of viable bacteria decreased to a level where no viable bacteria could be confirmed after 8 hours. It was. That is, from this test result, even when (B) allantoin is used as an anti-inflammatory agent, a high antibacterial activity is demonstrated against Staphylococcus aureus by combining with (A) chlorobutanol and (C) 1-menthol. I understand that

<Test Example 6: Usability evaluation 2>
Each cream preparation (O / W type) shown in Table 6 below was prepared according to a conventional method, and the usability when used for sensitive skin after shaving was evaluated.

  First, a male subject was shaved with a razor, and then each test preparation was applied in an appropriate amount to the shaved skin, and immediately after that, the presence or absence of tingling was evaluated in a questionnaire format. . Specifically, the score was given by a five-step evaluation of 1 point (not felt) to 5 points (feel). Based on this questionnaire result, the result of calculating the ratio of the number of people who gave an evaluation that they did not feel tingling (namely, rating 1) is shown in Table 6 above. As a composition for external use to be used after the stratum corneum has been shaved off by shaving, it may cause pain and irritation to the user and may make it difficult to continue use. is there. Therefore, it is very important for such an external composition for skin to have a feeling of use that reduces tingling after application.

  In general, it is known that creams are easier to reduce the pain of biting and stinging than liquids, and this point is compared to Comparative Example 23 (control) consisting only of a cream base as shown in the results of Table 6 above. Even when applied, it is clear that about 70% of subjects evaluated that they did not feel tingling after application. And when it sees the case where the cream agent of the comparative examples 24-26 which mix | blended each of (A) chlorobutanol, (B) allantoin, or (C) 1-menthol individually was used for this cream base, In the case of only the cream (Comparative Example 23), or in the case of a cream preparation (Comparative Example 26) containing l-menthol alone, the number of people evaluated as not feeling tingling is significantly less than half. As a result, it can be seen that each of the components (A) to (C) alone does not contribute much to improvement of the tingling feeling. On the other hand, unexpectedly, when the cream of Example 7 containing the three components (A) chlorobutanol, (B) allantoin, and (C) 1-menthol was used, the tingling sensation was not felt. The percentage of people evaluated increased to a level exceeding 85%. From this result, the external composition for skin containing the three components (A) to (C) of the present invention has an excellent usability that is desirable for application to sensitive skin after treatment with a razor such as after shaving. It was recognized that he played.

<Prescription Formulation Example 1>
Below, the formulation example of the external composition for skin of this invention is shown. Formulation Examples 1 to 3 are creams, Formulation Example 4 is an ointment, and Formulation Example 5 is a gel.

<Prescription Formulation Example 2>
Below, the formulation example of the external composition for skin of this invention is shown. Formulation Examples 6 to 8 are lotions, Formulation Example 9 is an emulsion, and Formulation Example 10 is a gel.

Claims (9)

  A composition for external use on skin containing (A) chlorobutanol, (B) an anti-inflammatory agent, and (C) a terpenoid.   (C) Composition for external use of skin of Claim 1 whose content of terpenoid is 0.1 w / w% or more with respect to the whole composition.   (B) The external composition for skin according to claim 1 or 2, wherein the anti-inflammatory agent is a non-steroidal anti-inflammatory agent.   (B) Anti-inflammatory agent is glycyrrhizic acid, glycyrrhetinic acid, stearyl glycyrrhetinate, allantoin, epsilon aminocaproic acid, salicylic acid, methyl salicylate, glycolic salicylate, indomethacin, felbinac, ibuprofen, ibuprofen piconol, ketoprofen, bufexamac, flufenamic acid, butyl The external composition for skin according to any one of claims 1 to 3, which is at least one selected from the group consisting of vendazac, piroxicam, suprofen, ufenamate, heparin-like substance, azulene, guaiazulene and salts thereof.   (C) The external composition for skin according to any one of claims 1 to 4, wherein the terpenoid is a monoterpenoid.   (C) the terpenoid is at least selected from the group consisting of menthol, camphor, borneol, limonene, anethole, eugenol, geraniol, nerol, myrsenol, linalool, linalool acetate, lavandolol, isoborneol, cineol, pinene, and terpinolene The composition for external use of the skin according to any one of claims 1 to 5, which is one type.   The external composition for skin according to any one of claims 1 to 6, which is used for skin after wounding.   The composition for external use of skin according to any one of claims 1 to 7, which is used for skin after shaving.   The external composition for skin according to any one of claims 1 to 8, which is a cream.

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