JP7587933B2 - External Composition - Google Patents

Description

The present invention relates to a composition for external use used to improve skin inflammation after shaving.

With the growing awareness of beauty in recent years, body hair removal is being practiced by a wide range of people. Methods for removing body hair are usually epilation, shaving, and depilation, and epilation is widely practiced by specialized institutions (medical institutions and beauty salons) using specialized equipment.

On the other hand, self-care shaving is still the most common method of hair removal. Although self-care may involve the use of home appliances, tweezers, or hair removal cosmetics, the ease of shaving far surpasses other methods. Furthermore, the reality is that shaving is essentially the only method available for self-care of sensitive areas (lower abdomen, vulva, and anal area).

During shaving, the skin is subject to contact stimuli such as contact with the blade of the shaving tool and friction from protective equipment such as blade guards, making it prone to inflammation after shaving. Furthermore, the tips of shaved body hair have sharp edges, and they grow quickly, making the surrounding skin more susceptible to injury, which also causes inflammation. In general, skin inflammation due to shaving is relatively low in the skin of the arms and legs (Non-Patent Document 1), but the skin of the pubic area in particular is thinner and more sensitive than the skin of other parts of the body, has thicker body hair than other parts of the body, makes it difficult to handle the shaving tool and is more likely to cause irritation, and is constantly exposed to a harsh, humid environment due to pressure from underwear after shaving, so the risk of inflammation due to shaving is extremely high. For this reason, there is no end to problems caused by shaving when shaving yourself.

J. Soc. Cosmet. Chem. Jpn. 44 (4) 298-303 (2010)

The present invention aims to provide a composition for external use that can be used to improve skin inflammation after shaving.

After extensive research, the inventors discovered that a topical composition containing ufenamate and lidocaines is highly effective in improving skin inflammation after shaving. The present invention was completed based on this finding and through further research.

That is, the present invention provides the following aspects.
Item 1. A composition for external use comprising (A) ufenamate and (B) lidocaine and/or a salt thereof, which is used to improve inflammation of the skin after shaving.
Item 2. The composition for external use according to Item 1, which is applied to inflammation of the skin in the lower abdomen, vulva, and/or anal area.
Item 3. The composition for external use according to Item 1 or 2, which is applied to inflammation not accompanied by itching.
Item 4. The composition for external use according to any one of Items 1 to 3, further comprising (C) glycyrrhetinic acid, a derivative of glycyrrhetinic acid, and/or a salt thereof, (D) diphenhydramine and/or a salt thereof, (E) tocopherol and/or a derivative thereof, and/or (F) an antibacterial or bactericidal agent.

The present invention provides a composition for external use that is used to improve skin inflammation after shaving.

The topical composition of the present invention contains (A) ufenamate (hereinafter also referred to as "component (A)") and (B) lidocaine and/or a salt thereof (hereinafter also referred to as "component (B)" or "lidocaines"), and is characterized in that it is used to improve inflammation of the skin after shaving. The topical composition of the present invention may further contain (C) glycyrrhetinic acid, a derivative of glycyrrhetinic acid, and/or a salt thereof (hereinafter also referred to as "component (C)" or "glycyrrhetinic acids"), (D) diphenhydramine and/or a salt thereof (hereinafter also referred to as "component (D)" or "diphenhydramines"), (E) tocopherol and/or a derivative thereof (hereinafter also referred to as "component (E)" or "tocopherols"), and/or (F) a quaternary ammonium antibacterial agent (hereinafter also referred to as "component (F)"). From the viewpoint of further improving the effect of improving skin inflammation after shaving, the topical composition of the present invention preferably contains components (A), (B), (C), (D), (E), and (F). The topical composition of the present invention will be described in detail below.

(A) Ufenamate The topical composition of the present invention contains ufenamate as component (A). Ufenamate is also called butyl flufenamate and is a known drug as a fat-soluble nonsteroidal anti-inflammatory drug. Component (A) alone does not have much effect on improving skin inflammation after shaving, but the topical composition of the present invention can exhibit an excellent effect on improving skin inflammation after shaving.

In the topical composition of the present invention, the content of component (A) is appropriately set depending on the medicinal effect to be exerted, and may be, for example, 1 to 20% by weight. From the viewpoint of further improving the effect of improving skin inflammation after shaving, the content of component (A) in the topical composition of the present invention is preferably 3 to 6% by weight, and more preferably 4.5 to 5.5% by weight.

(B) Lidocaine The topical composition of the present invention contains lidocaine and/or its salt as component (B). Lidocaine is also called xylocaine and is a known drug known to have a local anesthetic effect. Component (B) is a local anesthetic and does not improve inflammation by itself, but when combined with component (A), it dramatically improves the improving effect on skin inflammation after shaving.

There are no particular limitations on the salt of lidocaine as long as it is pharma- ceutical acceptable, but specific examples include inorganic acid salts such as hydrochloride.

In the topical composition of the present invention, one of lidocaine and its salts may be selected and used alone, or two or more of them may be used in combination. Among lidocaine and its salts, lidocaine is preferred from the viewpoint of further improving the effect of improving skin inflammation after shaving.

The content of component (B) in the topical composition of the present invention may be appropriately set depending on the medicinal effect to be imparted, and may be, for example, 0.1 to 5% by weight, preferably 0.2 to 2% by weight, and more preferably 0.5 to 1.5% by weight, of the total amount of component (B).

In the topical composition of the present invention, the ratio of component (B) to component (A) is determined according to the respective contents of components (A) and (B), but for example, the total amount of component (B) per 1 part by weight of component (A) is, for example, 0.01 to 1.5 parts by weight, preferably 0.05 to 1 part by weight, and more preferably 0.1 to 0.5 parts by weight.

(C) Glycyrrhetinic Acids The topical composition of the present invention may contain glycyrrhetinic acid, its derivatives, and/or salts thereof as component (C) in order to further improve the effect of improving skin inflammation after shaving.

Glycyrrhetinic acid is a known drug that is known to have anti-inflammatory and anti-allergic effects.

The derivatives of glycyrrhetinic acid are not particularly limited as long as they are pharma- ceutical acceptable, but specific examples include pyridoxine glycyrrhetinate, stearyl glycyrrhetinate, glyceryl glycyrrhetinate, and monoglucuronide glycyrrhetinate. These derivatives of glycyrrhetinic acid may be used alone or in combination of two or more.

The salts of glycyrrhetinic acid and/or its derivatives are not particularly limited as long as they are pharma- ceutically acceptable, but specific examples include alkali metal salts such as sodium salts and potassium salts; ammonium salts, etc. These salts may be used alone or in combination of two or more.

The topical composition of the present invention may use one or a combination of two or more of glycyrrhetinic acid, salts of glycyrrhetinic acid, derivatives of glycyrrhetinic acid, and salts of derivatives of glycyrrhetinic acid as component (C).

Among these (C) components, glycyrrhetinic acid is preferred from the viewpoint of further improving the effect of improving skin inflammation after shaving.

In the topical composition of the present invention, the content of component (C) is not particularly limited and may be set appropriately depending on the medicinal effect to be imparted, but for example, the total amount of component (C) is 0.05 to 5% by weight, and from the viewpoint of further improving the effect of improving skin inflammation after shaving, the content is preferably 0.1 to 1% by weight, and more preferably 0.2 to 0.5% by weight.

In the topical composition of the present invention, the ratio of component (C) to component (A) is determined according to the respective contents of components (A) and (C), but for example, the total amount of component (C) is 0.01 to 0.9 parts by weight per part by weight of component (A). From the viewpoint of further improving the effect of improving skin inflammation after shaving, the total amount of component (C) is preferably 0.03 to 0.5 parts by weight, more preferably 0.05 to 0.1 parts by weight, per part by weight of component (A).

(D) Diphenhydramines The topical composition of the present invention may contain diphenhydramine and/or a salt thereof as component (D) in order to further improve the effect of improving skin inflammation after shaving. Diphenhydramine is a known drug known to have an antihistamine effect. Component (D) alone has almost no effect of improving skin inflammation after shaving, but when combined with components (A) and (B), it is possible to significantly improve the effect of improving skin inflammation after shaving.

There are no particular limitations on the salts of diphenhydramine as long as they are pharma- ceutically acceptable, but specific examples include acid addition salts such as hydrochloride, citrate, succinate, tartrate, fumarate, maleate, salicylate, diphenyl disulfonate, tannate, lauryl sulfate, and sulfate. These salts may be used alone or in combination of two or more.

The topical composition of the present invention may use one or more of diphenhydramine and its salts as component (D).

Among these (D) components, diphenhydramine is preferred from the viewpoint of further improving the effect of improving skin inflammation after shaving.

In the topical composition of the present invention, the content of component (D) is not particularly limited, but may be, for example, 0.1 to 5% by weight in total of component (D). From the viewpoint of further improving the effect of improving skin inflammation after shaving, the content of component (D) in the topical composition of the present invention is preferably 0.3 to 2% by weight, more preferably 0.5 to 1.5% by weight.

In the topical composition of the present invention, the ratio of component (D) to component (A) is determined according to the respective contents of components (A) and (D), but for example, the total amount of component (D) is 0.01 to 1.2 parts by weight per part by weight of component (A). From the viewpoint of further improving the effect of improving skin inflammation after shaving, the total amount of component (D) is preferably 0.05 to 0.8 parts by weight, more preferably 0.1 to 0.5 parts by weight, per part by weight of component (A).

(E) Tocopherols The topical composition of the present invention may further contain tocopherol and/or a derivative thereof as component (E) from the viewpoint of further improving the effect of improving skin inflammation after shaving.

Tocopherol is a known compound known as vitamin E. Tocopherol may be in the d-, l-, or dl-form, with the dl-form being preferred. Tocopherol may be in the α-, β-, γ-, or δ-form, with the α-form being preferred.

Tocopherol derivatives are not particularly limited as long as they are pharma- ceutically acceptable, but examples include esters with carboxylic acids such as acetic acid, nicotinic acid, and succinic acid, and diesters with phosphoric acid. Among these tocopherol derivatives, esters with carboxylic acids are preferred, and tocopherol acetate is even more preferred, from the viewpoint of further improving the effect of improving skin inflammation after shaving.

The tocopherol derivative may be any of the d-, l-, or dl-forms, with the dl-form being preferred. The tocopherol derivative may be any of the α-, β-, γ-, or δ-forms, with the α-form being preferred.

In the topical composition of the present invention, one of tocopherol and its derivatives may be selected as component (E) and used alone, or two or more of them may be used in combination. Among the components (E), from the viewpoint of further improving the effect of improving skin inflammation after shaving, preferred are tocopherol derivatives, more preferred are tocopherol esters with carboxylic acids, even more preferred are tocopherol acetate, and particularly preferred are d-α-tocopherol acetate, l-α-tocopherol acetate, and dl-α-tocopherol acetate.

When the topical composition of the present invention contains component (E), the content of component (E) is not particularly limited, but from the viewpoint of further improving the effect of improving skin inflammation after shaving, the total amount of component (E) is, for example, 0.05 to 2% by weight, preferably 0.1 to 1.3% by weight, and more preferably 0.3 to 0.8% by weight.

When the topical composition of the present invention contains component (E), the ratio of component (E) to component (A) is determined based on the range of the content of each component, but from the viewpoint of further improving the effect of improving skin inflammation after shaving, the total amount of component (E) is 0.01 to 1 part by weight, preferably 0.03 to 0.5 parts by weight, and more preferably 0.05 to 0.3 parts by weight per part by weight of component (A).

(F) Antibacterial or Bactericidal Agent From the viewpoint of further improving the effect of improving skin inflammation after shaving, the topical composition of the present invention may further contain an antibacterial or bactericidal agent as component (F).

Antibacterial or bactericidal agents are not particularly limited, provided that they are pharma- ceutically or cosmetically acceptable. Examples include quaternary ammonium antibacterial agents, isopropylmethylphenol, hinokitiol, chlorhexidine hydrochloride, chlorhexidine gluconate, triclosan, lysozyme chloride, sulfazine, etc. Specific examples of quaternary ammonium antibacterial agents include cetylpyridinium chloride, benzethonium chloride, benzalkonium chloride, dequalinium chloride, alkyldimethylammonium chloride, alkyltrimethylammonium chloride, methylbenzethonium chloride, lauroylcollaminoformylmethylpyridinium chloride, etc.

These antibacterial or bactericidal agents may be used alone or in combination of two or more.

Among these antibacterial or bactericidal agents, isopropyl methylphenol is preferred from the viewpoint of further improving the effect of improving skin inflammation after shaving.

When the topical composition of the present invention contains component (F), the content of component (F) may be appropriately set depending on the type of antibacterial or bactericidal agent used, and may be, for example, 0.01 to 1% by weight. From the viewpoint of further improving the effect of improving skin inflammation after shaving, the content of component (C) is preferably 0.03 to 0.5% by weight, and more preferably 0.05 to 0.3% by weight.

When the topical composition of the present invention contains component (F), the ratio of component (A) to component (F) is determined according to the respective contents of these two components described above, but for example, the ratio of component (F) is 0.001 to 0.5 parts by weight, preferably 0.005 to 0.1 parts by weight, and more preferably 0.01 to 0.05 parts by weight per part by weight of component (A).

Other components The topical composition of the present invention may contain other pharmacological components, if necessary, in addition to the above-mentioned components. Such pharmacological components include, for example, antihistamines (chlorpheniramine maleate, etc.), local anesthetics (dibucaine, procaine, tetracaine, bupivacaine, mepivacaine, chloroprocaine, proparacaine, meprylcaine, or salts thereof), alkyl benzoates (e.g., ethyl aminobenzoate, diethylaminoethyl p-butylaminobenzoate hydrochloride), orthocaine, oxethazaine, oxypolyethyleneoxydecane, Scopolia extract, percaminpase, tesitdesitin, etc.), anti-inflammatory agents (allantoin , salicylic acid, glycol salicylate, methyl salicylate, indomethacin, felbinac, diclofenac sodium, loxoprofen sodium, etc.), antipruritic agents (crotamiton, thianthol, etc.), skin protective agents (collodion, castor oil, etc.), blood circulation promoting ingredients (vanillyl nonyl amide, nicotinic acid benzyl ester, capsaicin, chili pepper extract, etc.), refreshing agents (menthol, camphor, etc.), vitamins (vitamins A, B, C, D, etc.), mucopolysaccharides (sodium chondroitin sulfate, hyaluronic acid, etc.), etc.

In addition to the above-mentioned components, other bases and additives commonly used in skin topicals and the like may be included as necessary. Such bases and additives are not particularly limited as long as they are pharma- ceutically acceptable, but examples of such bases and additives include aqueous bases such as water, lower alcohols (e.g., isopropanol), and polyhydric alcohols (glycerin, propylene glycol, dipropylene glycol, 1,3-butylene glycol, etc.); oils (olive oil, safflower oil, soybean oil, camellia oil, corn oil, rapeseed oil, sunflower oil, cottonseed oil, peanut oil, lard, squalane, fish oil, etc.), mineral oils (liquid paraffin, paraffin, gelling hydrocarbons, petrolatum, etc.), waxes and waxes (beeswax, kaolin, etc.), and the like. Lunauba wax, candelilla wax, ceresin, rice wax, microcrystalline wax, etc.), ester oils (isopropyl myristate, isopropyl adipate, diethyl sebacate, isopropyl sebacate, isopropyl palmitate, cetyl palmitate, ethyl oleate, etc.), fatty acid alkyl esters, fatty acids (stearic acid, oleic acid, palmitic acid, behenic acid, linoleic acid, lanolin, etc.), fatty acid esters (cetyl palmitate, isopropyl palmitate, isopropyl myristate, ethyl linoleate, etc.), high-grade alcohols oily bases such as glyceryl tri-2-ethylhexanoate, cetyl 2-ethylhexanoate, and silicone oils (dimethylpolysiloxane, cyclic silicone, and the like); POE (10-50 mol) phytosterol ether, POE (10-50 mol) dihydrocholesterol ether, POE (10-50 mol) 2-octyldodecyl ether, and POE (10-50 mol) decyl ether; polyoxyethylene alkyl ethers such as tetradecyl ether, POE (10-50 mol) oleyl ether, POE (2-50 mol) cetyl ether (e.g., cetomacrogol 1000), POE (5-50 mol) behenyl ether, POE (5-30 mol) polyoxypropylene (5-30 mol) 2-decyltetradecyl ether, POE (10-50 mol) polyoxypropylene (2-30 mol) cetyl ether, phosphoric acids and phosphates thereof (e.g., sodium POE cetyl ether phosphate), POE (20-60 mol) sorbitan monooleate, P OE (10-60 mol) sorbitan monoisostearate, POE (10-80 mol) glyceryl monoisostearate, POE (10-30 mol) glyceryl monostearate, POE (20-100 mol) polyoxypropylene modified silicone, POE-alkyl modified silicone, polyethylene glycol monolaurate, polyethylene glycol monopalmitate, polyethylene glycol monostearate, polyethylene glycol dilaurate, polyethylene glycol dipalmitate, polyethylene glycol distearate, dioleate surfactants such as polyethylene glycol diricinoleate, polyethylene glycol diricinoleate, polyoxyethylene hydrogenated castor oil (5-100), polysorbate (20-85), glycerin fatty acid esters (glycerin monostearate, etc.), hydrogenated soybean phospholipids, and hydrogenated lanolin alcohol; freshening agents (menthol, camphor, borneol, peppermint water, peppermint oil, etc.), preservatives (methylparaben, propylparaben, benzoic acid, sodium benzoate, sorbic acid, etc.), flavoring agents (citral, 1,8-sional, citronellal, farnesol) etc.), coloring agents (tar dyes (Brown No. 201, Blue No. 201, Yellow No. 4, Yellow No. 403, etc.), cacao dyes, chlorophyll, aluminum oxide, etc.), thickening agents (carboxyvinyl polymer, hypromellose, polyvinylpyrrolidone, sodium alginate, ethyl cellulose, hydroxyethyl cellulose, sodium carboxymethyl cellulose, xanthan gum, carrageenan, etc.), pH adjusters (phosphoric acid, hydrochloric acid, citric acid, sodium citrate, succinic acid, tartaric acid, sodium hydroxide, potassium hydroxide, triethanolamine, triisopropanol amine, etc.), wetting agents (sodium dl-pyrrolidone carboxylate solution, D-sorbitol solution, macrogol, etc.), stabilizers (dibutylhydroxytoluene, butylhydroxyanisole, sodium edetate, sodium metaphosphate, L-arginine, L-aspartic acid, DL-alanine, glycine, sodium erythorbate, propyl gallate, sodium sulfite, sulfur dioxide, chlorogenic acid, catechin, rosemary extract, etc.), antioxidants, UV absorbers, chelating agents, adhesives, buffers, dissolution aids, solubilizers, preservatives, and other additives.

Properties, Formulations, etc. The properties of the topical composition of the present invention are not particularly limited, and include aqueous liquid compositions, aqueous gel compositions, oily gel compositions, emulsion compositions, etc. Among these, from the viewpoint of further improving the effect of improving skin inflammation after shaving, preferably emulsion compositions are used. The emulsion state of the emulsion composition may be either oil-in-water type or water-in-oil type, but from the viewpoint of further improving the effect of improving skin inflammation after shaving, preferably oil-in-water type is used.

The formulation of the topical composition of the present invention is not particularly limited, and examples thereof include lotions, emulsions, ointments, creams, and the like. Among these, from the viewpoint of further improving the effect of improving skin inflammation after shaving and from the viewpoint of ease of application, emulsions and creams are preferred.

Specific examples of the topical composition of the present invention include pharmaceuticals, quasi-drugs, cosmetics, etc. Among these formulations, pharmaceuticals are preferred.

The topical composition of the present invention is used to improve inflammation of the skin after shaving. The site of inflammation to which the composition is applied is not particularly limited as long as the site has been shaved, but the topical composition of the present invention is particularly preferably applied to inflammation of the skin in the so-called delicate zones, namely the lower abdomen (V zone), the vulva (I zone), the buttocks, and/or the anal area (O zone).

The type of skin inflammation is not particularly limited, but may include pain (stinging sensation), rash, red bumps, etc. In addition, the present invention can be preferably applied to inflammation that is not accompanied by itching.

The topical composition of the present invention can be applied to skin suffering from post-shaving dermatitis by applying it 1 to 6 times a day. In order to more effectively improve post-shaving skin inflammation, the topical composition of the present invention is preferably applied for, for example, 5 days or more, preferably 1 week or more.

The present invention will be described in detail below with reference to examples, but the present invention is not limited to these examples.

Test Example: A topical composition having the composition shown in Table 1 was prepared as an oil-in-water emulsion composition (cream). Subjects (N=15) who had razor burn caused by shaving at least once a week and suffered from inflammation of the lower abdomen (V zone) and vulva (I zone) with rash, redness, and stinging sensation (all without itching) were asked to apply the topical composition to the affected area for one week (three times a day). After one week, the satisfaction with the improvement of inflammation was evaluated using a five-level VAS (satisfied, somewhat satisfied, neutral, somewhat dissatisfied, dissatisfied), and the percentage (%) of the 15 subjects who answered "satisfied" was calculated as the "effectiveness rate". First, Comparative Examples 1 and 2 and Example 2 were tested, and then, after the symptoms caused by shaving recurred to the same extent as before the test, Comparative Examples 3 to 5 and Example 2 were tested. The results are shown in Table 1.

As shown in Table 1, only a few subjects were satisfied with the topical composition of Comparative Example 1, which contained only ufenamate as the active ingredient, and even fewer were satisfied with Comparative Example 2, which contained only lidocaine as the active ingredient. However, the topical composition of Example 1, which contained ufenamate and lidocaine, showed a high effect of improving inflammation, with more than half of the subjects responding that they were satisfied. In addition, only a few subjects were satisfied with the topical composition of Comparative Example 3, which contained diphenhydramine, glycyrrhetinic acid, tocopherol acetate, and isopropylmethylphenol, and even less than half of the subjects were satisfied with the topical compositions of Comparative Examples 4 and 5, which contained ufenamate or lidocaine. On the other hand, the topical composition of Example 2, which contained ufenamate and lidocaine together with diphenhydramine, glycyrrhetinic acid, tocopherol acetate, and isopropylmethylphenol, showed an even higher effect of improving inflammation, with most of the subjects responding that they were satisfied.

[Prescription Example]
The topical compositions having the formulations shown in Table 2 were prepared as oil-in-water emulsion compositions (creams). All of the topical compositions showed excellent effects of improving skin inflammation after shaving.

Claims (3)

A composition for external use used to improve inflammation of the skin after shaving, comprising (A) ufenamate , (B) lidocaine and/or a salt thereof, (C) glycyrrhetinic acid, a derivative of glycyrrhetinic acid, and/or a salt thereof, (D) diphenhydramine and/or a salt thereof, (E) tocopherol and/or a derivative thereof, and (F) an antibacterial or bactericidal agent. The topical composition according to claim 1, which is applied to inflammation of the skin in the lower abdomen, vulva, and/or anal area. The external composition according to claim 1 or 2, which is applied to inflammation not accompanied by itching.