JP5989271B1 - Scalp composition for external use - Google Patents

Abstract

A scalp and an external composition for scalp with improved delivery efficiency to the deep part of the hair follicle are provided. An external composition for scalp, which is contained in a container having a coating portion that includes a lower alcohol and is formed of a soft porous material. [Selection] Figure 1

Description

  The present invention relates to an external composition for scalp. More specifically, the present invention relates to an external composition for scalp that is housed in a container having an application part formed of a soft porous material.

  The skin of mammals including humans is composed of epidermis, dermis and subcutaneous tissue, and has a structure in which skin appendages such as hair follicles, sweat glands and sebaceous glands are present.

There are many hair follicles in human skin, but the density and depth of hair follicles vary greatly depending on the site (Non-patent Document 1). It is known that the hair follicles of the abdomen, arms and lower thighs that occupy most of human skin have a low hair follicle density of 60 to 80 pieces / cm ² and tend to be shallow. On the other hand, the hair follicle of the human scalp has a very high hair follicle density of 350 to 500 / cm ² and a deep depth. In addition, hair follicles such as the abdomen have a structure that is slightly inclined with respect to the surface, whereas hair follicles on the scalp have a structure that is relatively long and straight from the surface of the skin downward. It has been known.

  When an active ingredient such as a drug is transdermally administered / applied, the permeation route of the active ingredient through the skin includes a route through the stratum corneum of the epidermis and a route through a skin appendage such as a hair follicle. Are known. Since the stratum corneum occupies most of the skin surface area, the application site is wide, but there is a problem that large components are not easily transmitted. On the other hand, skin appendages such as hair follicles have a merit that the permeation resistance is often lower than that of the stratum corneum route, although the proportion of the skin surface area itself is low.

  As an external composition applied to the scalp, there are a therapeutic agent and an improving agent for scalp eczema causing symptoms such as itching in the scalp, a hair nourishing agent, and a hair restoring agent. As one of the causes of scalp eczema, it is pointed out that excessive growth of Malassezia fungi (Malassezia) in the hair follicles of the scalp is pointed out. Hair growth agents and hair nourishing agents are preparations that are desired to deliver a sufficient amount of the active ingredient to the hair flow in the hair follicle deep in the hair follicle and to the blood flow of the capillaries of the dermis and subcutaneous tissue passing thereunder. In addition, drying of the scalp and lowering of the barrier function worsen the scalp environment and cause dandruff, itching, thinning hair, and the like, and thus it is desired to prevent or improve at an early stage. Any such topical composition is expected to benefit the delivery of the active ingredient to the scalp and deep into the hair follicle.

  However, when an external composition is applied to the scalp, there is a concern that the hair may interfere and it becomes difficult to deliver a sufficient amount of the external composition to the scalp and its deep follicles. Therefore, in order to avoid the hair and apply the external composition to the scalp, a spray type container that discharges the external composition in a spray form is adopted, and the external composition is pinpointed to the site where the opening is pressed. Employing a discharge type container (a so-called narrow-mouthed container for liquid, see FIG. 4) has become the mainstream.

Illustrative histology centered on function, 4th edition, Hidetomo Yamada, et al., School of Medicine, July 2001

  An object of the present invention is to provide an external composition for scalp having improved delivery efficiency to the scalp and its deep follicle.

  The present inventors, as a container for containing an external composition containing a lower alcohol, press an application part formed of a soft porous material or spread it while pressing and discharge the external composition in a planar shape. Surprisingly, it was found that the delivery efficiency of the composition for external use to the deep follicle of the scalp is improved by adopting a container of this type. The present invention is based on this novel finding.

The present invention relates to the following inventions, for example.
[1] An external composition for scalp, which contains a lower alcohol and is housed in a container having a coating portion formed of a soft porous material.
[2] The external composition for scalp according to [1], which is used for a hair growth site.
[3] The external composition for scalp according to [1] or [2], wherein the content of the lower alcohol is 5 to 70 w / w% based on the total amount of the external composition.
[4] For prevention, treatment and / or improvement of at least one symptom selected from the group consisting of eczema, dermatitis, hair loss, thinning hair, dandruff, itching, dryness and reduced barrier function in the scalp. [1] The external composition for scalp in any one of-[3].
[5] The external composition for scalp according to any one of [1] to [4], wherein the lower alcohol is ethanol.
[6] The scalp external composition according to any one of [1] to [5], which is a solubilized composition.
[7] The external composition for scalp according to any one of [1] to [6], further comprising at least one selected from the group consisting of steroids, monoterpenes, and antihistamine components.
[8] The scalp external composition according to any one of [1] to [7], further comprising a thickener.
[9] An external composition for scalp containing a container, wherein the external composition for scalp containing a lower alcohol is contained in a container having an application part formed of a soft porous material.

  According to the present invention, since a container having an application part formed of a soft porous material is used as a container for storing an external composition containing a lower alcohol, the external composition to the deep part of the hair follicle of the scalp is adopted. The delivery efficiency of the object is improved. Since the container is a container of a type in which the application part is pressed against the application site or is spread while being pressed and the external composition in the container is discharged in a planar shape, the composition for external application directly on the scalp avoiding hair It was difficult to apply the product, and it was thought that it was not suitable as a container for storing the external composition for scalp. That is, the effect by this invention that the delivery efficiency of the composition for external use to the hair follicle deep part of a scalp improves is completely surprising.

It is a perspective view which shows one Embodiment of a container provided with the application part formed with the soft porous material. It is explanatory drawing of the measuring method of the osmosis | permeation amount using a scalp model with a hair follicle. (A) No hair, (b) Hair. 6 is a graph showing the results of Test Example 1. It is a perspective view which shows an example of the narrow mouth container for liquids.

  Hereinafter, embodiments for carrying out the present invention will be described in detail. However, the present invention is not limited to the following embodiments.

  The scalp external composition of the present invention contains a lower alcohol. Moreover, the external composition for scalp of this invention is accommodated in the container provided with the application part formed with the soft porous material.

〔container〕
FIG. 1 is a perspective view showing a container according to an embodiment. The container is called a liquid application plug-type container provided with a soft porous application part. A liquid application stopper-type container 100 having a soft porous application part shown in FIG. 1 includes a container body 10 for storing an external composition 20 and a cap 30 that is detachably screwed into the container body 10. The cap 30 has a substantially inverted U-shaped cross section, and a screw is formed on the inner peripheral surface. This screw is screwed with the screw 40 of the container body 10. The container body 10 is formed with an application part 50 for discharging the external composition 20. The application unit 50 may be formed integrally with the container body 10 or may be configured to be detachable.

  The application part 50 is formed of a soft porous material. In the present specification, “formed of a soft porous material” means at least a part of an application portion (preferably about 70% or more, more preferably about 80% or more, further preferably about 90% or more, Preferably, the whole is composed of a soft porous material. The soft porous material is a porous material having a softness suitable for application to the skin and having a large number of pores, and the composition for external use inside the container is discharged to the outside of the container. That's fine. The structure of the soft porous material may be any of a sponge structure, a balloon structure, a honeycomb structure, and the like. From the viewpoint that the composition for external use can be more efficiently applied, the pore diameter is preferably 1 mm or less, more preferably 0.7 mm or less, and further preferably 0.5 mm or less. Preferably, it is still more preferable that it is 0.3 mm or less. Further, the pore diameter is preferably 0.01 μm or more, more preferably 0.1 μm or more, and further preferably 1 μm or more.

  Specific examples of the soft porous material include a resin foam having an open cell structure. The resin foam may include a closed cell structure. Specific examples of the resin foam include natural rubber foam; synthetic rubber foam such as polyurethane foam, polystyrene foam, polypropylene foam, and polyethylene foam; melamine resin foam. As the resin foam, natural rubber foam and synthetic rubber foam are preferable, natural rubber foam and polyurethane foam (for example, soft urethane) are more preferable, since natural effects of the present invention are more remarkably exhibited. A rubber foam is more preferred. The application part 50 may be formed using these soft porous materials individually by 1 type, and may be formed using combining 2 or more types.

  Examples of materials for forming the container body 10 and the cap 30 include metals such as polyethylene terephthalate (PET), polypropylene (PP), polyethylene (high density polyethylene: HDPE, low density polyethylene: LDPE), polystyrene, glass, and aluminum. Can be mentioned. These may be used alone or in combination of two or more. Moreover, the container main body 10 and the cap 30 may be formed with the same material, and may be formed with a different material.

  The shape of the container main body 10 is not limited to the shape shown in FIG. 1 as long as it has an application part formed of a soft porous material. For example, the application part is sideways, downward, slightly upward or downward. You may have the shape bent so that it might become the direction inclined to. The cap 30 is not limited to the screw fitting structure as long as it is detachable from the container body 10, and may have any fitting structure such as one-touch lock fitting or external fitting.

〔Composition〕
The scalp external composition according to the present embodiment contains a lower alcohol. In the present specification, the lower alcohol means a monovalent alcohol having 1 to 6 carbon atoms.

  The lower alcohol is not particularly limited as long as it is physiologically or pharmaceutically acceptable. Specific examples of the lower alcohol include ethanol, propanol, isopropanol, n-butyl alcohol, s-butyl alcohol, t-butyl alcohol, isobutyl alcohol, pentyl alcohol and hexyl alcohol. From the viewpoint that the effects of the present invention are more remarkably exhibited, the lower alcohol is preferably ethanol, propanol, isopropanol, n-butyl alcohol, s-butyl alcohol, t-butyl alcohol and isobutyl alcohol, and ethanol and isopropanol. More preferably, it is more preferable that it is ethanol. A lower alcohol may be used individually by 1 type, and may be used in combination of 2 or more type.

  The content of the lower alcohol in the scalp external composition is more preferably 5 to 70 w / w% based on the total amount of the external composition, since the effects of the present invention are more remarkably achieved. More preferably, it is w%, 10-50 w / w% is still more preferable, and it is still more preferable that it is 30-50 w / w%.

  The external composition for scalp which concerns on this embodiment may further contain the active ingredient or functional ingredient used for a pharmaceutical, a quasi-drug, or cosmetics. Specific examples of active ingredients or functional ingredients include, for example, steroids, moisturizing ingredients, anti-inflammatory ingredients, antihistamine ingredients, antibacterial ingredients, vitamins, antipruritic ingredients, local anesthetic ingredients, local stimulating ingredients, hair nourishing / hair restoring ingredients, Monoterpene, peptide or derivative thereof, amino acid or derivative thereof, cell activation component, anti-aging component, blood circulation promoting component, keratin softening component, whitening component, astringent component, UV protection component (UV absorption component, UV scattering component) It is done. By containing these, application development according to the active ingredient or functional ingredient becomes possible. These active ingredients or functional ingredients may be used alone or in combination of two or more.

  The scalp external composition according to the present embodiment is selected from the group consisting of eczema, dermatitis, hair loss, thin hair, dandruff, itching, dryness, and reduced barrier function in the scalp, depending on the active ingredient or functional ingredient. It is suitably used for the prevention, treatment and / or amelioration of at least one symptom. Since the composition for external use for scalp of this invention improves the delivery efficiency of an active ingredient or a functional ingredient to the hair follicle deep part of a scalp, it can fully exhibit the effect of these components.

  The scalp external composition according to this embodiment may further contain at least one selected from the group consisting of steroids, monoterpenes, and antihistamine components. When the composition for external use for scalp contains a steroid, a monoterpene, or an antihistamine component, the delivery efficiency to the scalp and its deep hair follicle is further improved. Moreover, the use development according to the effect | action by a steroid, a monoterpene, or an antihistamine component is attained.

  Steroids are steroid hormones having a steroid nucleus and derivatives thereof, and salts thereof, and have anti-inflammatory action, immunosuppressive action, anti-allergic action, and the like. Steroids are also referred to as steroidal anti-inflammatory drugs. A commercially available steroid can also be used.

  Steroid hormone derivatives include those obtained by chemically modifying a part of the functional group of the steroid hormone, those obtained by adding a protecting group to a part of the functional group, and including isomers. For example, one or more hydrogen atoms of the steroid nucleus are hydroxyl group, amino group, chloro group, bromo group, iodo group, fluoro group, trifluoro group, nitro group, cyano group, carboxyl group, carbon number 1 to An alkyl group having 6 carbon atoms, an acetyl group having 2 to 6 carbon atoms, an aryl group having 6 to 10 carbon atoms, an alkynyl group having 2 to 6 carbon atoms, an alkenyl group having 2 to 6 carbon atoms, an alkoxyl group having 1 to 6 carbon atoms, One substituted with an alkylamino group having 1 to 6 carbon atoms, one esterified with an organic acid (for example, valeric acid, acetic acid, butyric acid, propionic acid, furancarboxylic acid, etc.), or a steroid by removing the protecting group And precursors modified to have activity as systemic anti-inflammatory agents.

  The salt of the steroid hormone and its derivative is not particularly limited as long as it is physiologically or pharmaceutically acceptable. Specific examples include salts with alkali metal salts, alkaline earth metal salts, organic bases, and the like, and salts with sodium, potassium, calcium, magnesium, ammonium, diethanolamine, ethylenediamine, and the like. Furthermore, ammonia, methylamine, dimethylamine, trimethylamine, dicyclohexylamine, tris (hydroxymethyl) aminomethane, N, N-bis (hydroxyethyl) piperazine, 2-amino-2-methyl-1-propanol, ethanolamine, Examples thereof include salts with amines such as N-methylglucamine and L-glucamine; salts with basic amino acids such as lysine, δ-hydroxylysine and arginine. Also, for example, salts with mineral acids such as hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid; methanesulfonic acid, benzenesulfonic acid, paratoluenesulfonic acid, acetic acid, propionic acid, tartaric acid, fumaric acid, maleic acid , Salts with organic acids such as malic acid, oxalic acid, succinic acid, valeric acid, citric acid, benzoic acid, mandelic acid, cinnamic acid, lactic acid, glycolic acid, glucuronic acid, ascorbic acid, nicotinic acid, salicylic acid; asparagine Also included are salts with acidic amino acids such as acid and glutamic acid. The salts of steroid hormones and derivatives thereof may be solvates or hydrates.

  Specific examples of steroids include, for example, prednisolone, hydrocortisone, cortisone, dexamethasone, betamethasone, triamcinolone, triamcinolone acetonide, diflupredado, mometasone, diflucortron, fluoniside, bechrometazone, deprodon, clobetasone, alclomethasone and their derivatives. More specifically, clobetasol propionate, halobetasol propionate, diflorazone acetate, betamethasone dipropionate, diflucortron divalerate, mometasone furanate, betamethasone dipropionate, amsinonide, propione Dexamethasone acid, difluprednate, fluoniside, hydrocortisone butyrate propionate, predicate valerate acetate Zolone (prednisolone valerate acetate), betamethasone dipropionate, prednisolone, beclomethasone dipropionate, beclomethasone propionate, dexamethasone valerate, betamethasone valerate, fluocinolone acetonide, triamcinolone acetonide, hydrocortisone butyrate, hydrocortisone acetate Examples include clobetasone acetate, alclomethasone propionate, dexamethasone, hydrocortisone, betamethasone, dexamethasone acetate, hydrocortisone, cortisone acetate, and prednisolone acetate.

  As the steroid, prednisolone acetate valerate, hydrocortisone butyrate, hydrocortisone butyrate propionate, diflupredonate and beclomethasone propionate are preferable, and prednisolone valerate acetate is more preferable because the effects of the present invention are more remarkably exhibited.

  A steroid may be used individually by 1 type and may be used in combination of 2 or more type.

  The content of steroid in the external composition for scalp according to the present embodiment is not particularly limited, and is appropriately set according to the type of steroid, the type and content of other compounding components, the use and formulation form of the external composition. The The content of steroid is preferably from 0.01 to 2 w / w% based on the total amount of the composition for external use, for example, from the viewpoint of more prominently achieving the effects of the present invention. 0.02 to 1 w / w% is more preferable, 0.025 to 0.5 w / w% is further preferable, and 0.05 to 0.25 w / w% is particularly preferable.

  In the external composition for scalp according to this embodiment, the content ratio of the steroid to the lower alcohol is not particularly limited, the type of the lower alcohol and the steroid, the type and content of other compounding ingredients, the use of the external composition and the preparation form It sets suitably according to etc. The content ratio of the steroid to the lower alcohol is, for example, from the viewpoint of further enhancing the effect of the present invention, for example, with respect to 1 part by weight of the total content of the lower alcohol contained in the external composition for scalp according to this embodiment. The total content of is preferably 0.0001 to 0.05 parts by weight, more preferably 0.0002 to 0.03 parts by weight, and 0.0003 to 0.02 parts by weight. More preferred is 0.0005 to 0.01 part by weight.

  When the external composition for scalp according to the present embodiment contains a steroid, for example, prevention, treatment, and / or at least one symptom selected from the group consisting of eczema, dermatitis, dandruff, itching, and dryness on the scalp. Or it is used suitably for improvement.

  Monoterpene has a structure composed of two isoprene units and is a known compound as a cooling agent. The monoterpene is not particularly limited as long as it is physiologically or pharmaceutically acceptable. The monoterpene may be any of d-form, l-form, or dl-form.

  Specific examples of monoterpenes include, for example, monocyclic monoterpenes such as menthol, eugenol, thymol, limonene, anethole, cymene and terpineol, bicyclic rings such as camphor, borneol, cineol, pinene, camphene, isoborneol and fenchen. And monocyclic terpenes such as geraniol, nerol, myrcene, myrsenol, linalool, linalool acetate and lavandulol.

  As monoterpenes, since the effects of the present invention are more remarkably exhibited, monocyclic monoterpenes such as menthol, eugenol, thymol, limonene, anethole, cymene and terpineol, camphor, borneol, cineol, pinene, camphene, isoform Bicyclic monoterpenes such as borneol and fenchen are preferred, menthol, camphor and borneol are more preferred, and menthol is even more preferred.

  A monoterpene may be used individually by 1 type and may be used in combination of 2 or more type.

  As the monoterpene, an essential oil containing monoterpene may be used. Examples of such essential oils include cool mint oil, peppermint oil, mint oil, eucalyptus oil, bergamot oil, spearmint oil, rose oil and camphor oil. Examples of essential oils including menthol and camphor include cool mint oil, peppermint oil, mint oil and camphor oil.

  The monoterpene content in the scalp external composition according to the present embodiment is not particularly limited, and is appropriately determined according to the type of monoterpene, the type and content of other compounding components, the use and formulation form of the external composition, and the like. Is set. The monoterpene content is, for example, from the viewpoint of achieving the effect of the present invention more remarkably, for example, based on the total amount of the composition for external use, the total monoterpene content is 0.01 to 5.0 w / w%. Preferably, it is 0.05 to 4.0 w / w%, more preferably 0.1 to 3.5 w / w%, and 0.5 to 3.5 w / w%. Even more preferably, it is particularly preferably 1.0 to 3.5 w / w%. When the external composition for scalp which concerns on this embodiment contains an essential oil as a monoterpene, it is preferable to set so that the monoterpene content in an essential oil may exist in the said range.

  In the external composition for scalp according to this embodiment, the content ratio of monoterpene to the lower alcohol is not particularly limited, the type of lower alcohol and monoterpene, the type and content of other compounding components, the use of the external composition and It is appropriately set according to the formulation form. As the content ratio of monoterpene to the lower alcohol, from the viewpoint of further enhancing the effect of the present invention, for example, with respect to 1 part by weight of the total content of the lower alcohol contained in the scalp external composition according to the present embodiment, The total monoterpene content is preferably 0.0001 to 1 part by weight, more preferably 0.0005 to 0.8 part by weight, and 0.001 to 0.7 part by weight. More preferably, it is still more preferably 0.005 to 0.5 part by weight, and particularly preferably 0.01 to 0.1 part by weight. When the external composition for scalp which concerns on this embodiment contains an essential oil as a monoterpene, it is preferable to set so that the ratio of the monoterpene content in an essential oil may be in the said range.

  When the scalp external composition according to the present embodiment contains a monoterpene, for example, prevention, treatment, and / or at least one symptom selected from the group consisting of eczema, dermatitis, dandruff, and itching in the scalp. It is preferably used for improvement.

  The antihistamine component is not particularly limited as long as it is physiologically or pharmaceutically acceptable. Antihistamine components include, for example, diphenhydramine, chlorpheniramine, isothipentyl, ketotifen, bepotastine, dimenhydrinate, cyproheptadine, diphenylpyralin, promethazine, iproheptin, emedastine, clemastine, azelastine, levocabastine, hydroxyzine, methafazine Phenazine, cetirizine, oxatomide, terphenazine, epinastine, astemizole, ebastine, and salts of these compounds. The salt of the above compound is not particularly limited as long as it is physiologically or pharmaceutically acceptable, and examples thereof include various salts as exemplified above for the salts of steroid hormones and derivatives thereof. The salt of the antihistamine component may be a solvate or a hydrate.

  Specific examples of the antihistamine component include ethanolamine compounds such as diphenhydramine hydrochloride, diphenhydramine and dimenhydrinate; propylamine compounds such as chlorpheniramine maleate and chlorpheniramine; phenothiazine compounds such as promethazine hydrochloride and istipendil hydrochloride Piperazine compounds such as hydroxyzine; piperidine compounds such as cyproheptadine hydrochloride; epinastine hydrochloride, loratadine, and fexofenadine hydrochloride.

  As the antihistamine component, ethanolamine compounds, propylamine compounds, and phenothiazine compounds are preferred because the effects of the present invention are more prominent.Diphenhydramine hydrochloride, diphenhydramine, chlorpheniramine maleate, chlorpheniramine, Isotipendyl hydrochloride is more preferred, and diphenhydramine hydrochloride and diphenhydramine are still more preferred.

  An antihistamine component may be used individually by 1 type, and may be used in combination of 2 or more type.

  The content of the antihistamine component in the scalp external composition according to the present embodiment is not particularly limited, depending on the type of antihistamine component, the type and content of other compounding components, the use and formulation form of the external composition, etc. Is set as appropriate. The content of the antihistamine component is, for example, a total content of the antihistamine component of 0.1 to 5.0 w / w, based on the total amount of the composition for external use, from the viewpoint of exhibiting the effects of the present invention more remarkably. %, More preferably 0.15 to 4.5 w / w%, still more preferably 0.2 to 4.0 w / w%, and 0.3 to 3.0 w / w. % Is particularly preferred.

  In the external composition for scalp according to the present embodiment, the content ratio of the antihistamine component to the lower alcohol is not particularly limited, the types of the lower alcohol and the antihistamine component, the types and contents of other compounding components, the composition of the external composition It is set as appropriate according to the use and formulation form. The content ratio of the antihistamine component to the lower alcohol is, for example, from the viewpoint of further enhancing the effect of the present invention, for example, relative to 1 part by weight of the total content of the lower alcohol contained in the scalp external composition according to the present embodiment. The total content of the antihistamine component is preferably 0.001 to 1 part by weight, more preferably 0.002 to 0.9 part by weight, and 0.003 to 0.8 part by weight. More preferably, the amount is 0.004 to 0.6 parts by weight.

  When the external composition for scalp according to this embodiment contains an antihistamine component, for example, prevention, treatment, and / or at least one symptom selected from the group consisting of eczema, dermatitis, dandruff, and itching in the scalp Or it is used suitably for improvement.

  Specific examples of other active ingredients or functional ingredients that can be included in the external composition for scalp according to this embodiment include antipruritic ingredients such as crotamiton; glycyrrhizic acid and its derivatives, and salts thereof (for example, dipotassium glycyrrhizinate) Glycyrrhetinic acid monoammonium), glycyrrhetinic acid and its derivatives (eg stearyl glycyrrhetinic acid) and their salts, salicylic acid and its derivatives (eg glycolic salicylate, methyl salicylate) and their salts, anti-inflammatory components such as allantoin; isopropyl Antibacterial components such as methylphenol, benzalkonium chloride, and benzethonium chloride; astringent components such as zinc oxide and calamine; ethyl aminobenzoate, oxypolyethoxydodecane, dibucaine, dibucaine hydrochloride, lidocaine, lidide hydrochloride Local anesthetic ingredients such as indium; Local stimulating ingredients such as aqueous ammonia; Vitamins such as tocopherol acetate, tocopherol, panthenol, vitamin A oil, retinol palmitate; piroctone olamine, carrot extract, assembly extract, pantothenylethyl Ether, D-pantothenyl alcohol, seaweed extract, minoxidil, finasteride, carpronium chloride, hinokitiol, estradiol benzoate, pyridoxine hydrochloride, potassium pantothenate, resorcin, chixetnin ginseng, cashew tincture, arnica tincture, dl-α -Tocopherol, 2-L-ascorbic acid phosphoric acid diester potassium salt, hair-restoring / hair-growing components such as 6-benzylaminopurine, and the like can be mentioned, but are not limited thereto.

  The scalp external composition according to this embodiment contains, in addition to the above components, a base or carrier other than the lower alcohol usually used in pharmaceuticals, quasi drugs, and cosmetics, as long as the effects of the present invention are not impaired. It may be. Moreover, the external composition for scalp which concerns on this embodiment may contain the additive normally used for a pharmaceutical, a quasi-drug, or cosmetics in the range which does not impair the effect of this invention.

  When the external composition for scalp which concerns on this embodiment contains a thickener as an additive, even if it applies an external composition to a scalp by the thickening effect, the delivery efficiency of an active ingredient or a functional ingredient to a hair follicle is There is concern about the tendency to be suppressed. However, according to the present invention, since the composition for external use is housed and used in a container having an application part formed of a soft porous material, the scalp and its hair follicles are included even when a thickener is included. The delivery efficiency of the active ingredient or functional ingredient to is increased.

  Examples of the thickener include cellulose thickeners such as cellulose, methylcellulose, ethylcellulose, hydroxyethylcellulose, hydroxymethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, hydrophobized hydroxypropylmethylcellulose, carboxymethylcellulose, carboxyethylcellulose; polyvinyl alcohol, Vinyl thickeners such as polyvinylpyrrolidone and carboxyvinyl polymer; hyaluronic acid, acetylated hyaluronic acid, oligohyaluronic acid, hydrolyzed hyaluronic acid, chondroitin sulfate, alginic acid, and salts thereof (for example, sodium hyaluronate, acetyl hyaluronic acid) Mucopolysaccharide thickeners such as sodium, sodium chondroitin sulfate, sodium alginate) Guar gum, cationic guar gum, locust bean gum, carrageenan, xanthan gum, alkyl methacrylate copolymer acrylate acid, polyethylene glycol, bentonite, macrogol, quince seed, dextran, gellan gum.

  As the thickener, cellulose-based thickeners, vinyl-based thickeners, mucopolysaccharide-based thickeners are preferred from the viewpoint that the effects of the present invention can be more significantly obtained, and methylcellulose, ethylcellulose, hydroxyethylcellulose, Hydroxymethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, hydrophobized hydroxypropylmethylcellulose, carboxymethylcellulose, carboxyethylcellulose, polyvinyl alcohol, polyvinylpyrrolidone, carboxyvinyl polymer, hyaluronic acid, acetylated hyaluronic acid, oligohyaluronic acid, hydrolyzed hyaluronic acid, Chondroitin sulfate, alginic acid, sodium hyaluronate, sodium acetyl hyaluronate, sodium chondroitin sulfate, al More preferably sodium phosphate is methyl cellulose, ethyl cellulose, hydroxyethyl cellulose, hydroxymethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, hydrophobic hydroxypropyl methyl cellulose, carboxymethyl cellulose, carboxyethyl cellulose is more preferable.

  A thickener may be used individually by 1 type and may be used in combination of 2 or more type.

  The content of the thickener in the scalp external composition according to the present embodiment is not particularly limited, depending on the type of thickener, the type and content of other compounding ingredients, the use and formulation form of the external composition, etc. Is set as appropriate. The content of the thickener is, for example, from the viewpoint of more prominently achieving the effects of the present invention, for example, based on the total amount of the composition for external use, the total content of the thickener is 0.01 to 3.0 w / w. %, More preferably 0.05-2.5 w / w%, still more preferably 0.05-2.0 w / w%, 0.1-1.5 w / w % Is particularly preferred.

  In the external composition for scalp according to the present embodiment, the content ratio of the thickener to the lower alcohol is not particularly limited, the type of the lower alcohol and the thickener, the type and content of other compounding components, the composition of the external composition It is set as appropriate according to the use and formulation form. The content ratio of the thickener to the lower alcohol is, for example, from the viewpoint of further enhancing the effect of the present invention, for example, with respect to 1 part by weight of the total content of the lower alcohol contained in the scalp external composition according to the present embodiment. The total content of the thickener is preferably 0.0001 to 0.6 parts by weight, more preferably 0.0005 to 0.5 parts by weight, and 0.0008 to 0.4 parts by weight. More preferably, it is 0.001-0.3 weight part.

  Examples of the base or carrier include hydrocarbons such as liquid paraffin, squalane, petrolatum, gelled hydrocarbon (plasty base, etc.), ozokerite, α-olefin oligomer, and light liquid paraffin; methyl polysiloxane, cross-linked methyl polysiloxane , Highly polymerized methylpolysiloxane, cyclic silicone, alkyl-modified silicone, cross-linked alkyl-modified silicone, amino-modified silicone, polyether-modified silicone, polyglycerin-modified silicone, cross-linked polyether-modified silicone, cross-linked alkyl polyether-modified silicone, silicone・ Alkyl chain co-modified polyether-modified silicone, silicone ・ alkyl chain co-modified polyglycerin-modified silicone, polyether-modified branched silicone, polyglycerin-modified branched silicone, Silicone oils such as silyl silicone, phenyl-modified silicone, and silicone resin; higher alcohols such as cetanol, cetostearyl alcohol, stearyl alcohol, and behenyl alcohol; sterols such as cholesterol, phytosterol, and phytosteryl hydroxystearate; jojoba oil, meadow foam oil, sunflower Vegetable oils such as oil, grape seed oil, coconut oil, squalane, shea butter, rice germ oil; animal oils such as lanolin, orange raffie oil, squalane, horse oil; polyvinyl butyrate; polyethylene glycol; dioxane; butylene glycol adipic acid polyester; myristin Isopropyl acid, octyldodecyl myristate, isopropyl palmitate, cetyl palmitate, isononyl isononanoate, tetra-2-ethyl Esters such as pentaerythritol xanthate, jojoba oil, tri (caprylic acid / capric acid) glyceryl; polysaccharides such as dextrin and maltodextrin; polyhydric alcohols having 2 to 6 carbon atoms and 2 to 4 hydroxyl groups; succinic acid Organic acids such as glycolic acid, gluconic acid and citric acid; and aqueous bases such as water.

  A base or a carrier may be used alone or in combination of two or more.

  Examples of the additive include an antioxidant, a surfactant, an antiseptic, a preservative, a pH adjuster, a stabilizer, an irritation reducing agent, a colorant, a fragrance, and a pearl luster imparting agent.

  Examples of the antioxidant include dibutylhydroxytoluene, butylhydroxyanisole, sorbic acid, sodium sulfite, sodium pyrosulfite, ascorbic acid, ascorbic acid derivative, tocopherol, tocopherol derivative, erythorbic acid, and L-cysteine hydrochloride.

  Examples of the surfactant include sorbitan monoisostearate, sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, diglycerol sorbitan penta-2-ethylhexylate, and diglycerol sorbitan tetra-2-ethylhexylate. Sorbitan fatty acid esters of propylene glycol such as propylene glycol monostearate; polyoxyethylene hydrogenated castor oil 40 (HCO-40), polyoxyethylene hydrogenated castor oil 50 (HCO-50), polyoxyethylene hydrogenated castor Hardened castor oil derivatives such as oil 60 (HCO-60) and polyoxyethylene hardened castor oil 80; polyoxyethylene (20) sorbitan monolaurate (polysorbate 20), monostearic acid Polyoxyethylene sorbitan fatty acid esters such as reoxyethylene (20) sorbitan (polysorbate 60), polyoxyethylene monooleate (20) sorbitan (polysorbate 80), polyoxyethylene (20) sorbitan isostearate; polyoxyethylene mono Palm oil fatty acid glyceryl; glycerin alkyl ether; alkyl glucoside such as cetostearyl glucoside; polyoxyalkylene alkyl ether such as polyoxyethylene cetyl ether and polyoxyethylene behenyl ether; amines such as stearylamine and oleylamine; polyoxyethylene methyl Polysiloxane copolymer, lauryl PEG-9 polydimethylsiloxyethyl dimethicone, PEG-9 polydimethylsiloxyethyl dimethicone Silicone surfactants; natural surfactants such as phospholipids, surfactins, and saponins; fatty acid amide amines such as diethylaminoethylamide stearate and diethylaminopropyl stearate; trilaurylamine, dimethylstearylamine, di-2- Examples thereof include alkylamines such as ethylhexylamine; betaine amphoteric surfactants such as dimethylaminopropylamide stearate and laurylhydroxysulfobetaine.

  Examples of preservatives or preservatives include benzoic acid, sodium benzoate, dehydroacetic acid, sodium dehydroacetate, isobutyl paraoxybenzoate, isopropyl paraoxybenzoate, butyl paraoxybenzoate, ethyl paraoxybenzoate, propyl paraoxybenzoate, paraoxybenzoate Examples include benzyl benzoate, methyl paraoxybenzoate, phenoxyethanol, benzyl alcohol, chlorobutanol, sorbic acid and its salts, chlorhexidine gluconate, alkanediol, and glycerin fatty acid ester.

  Examples of pH adjusters include inorganic acids (hydrochloric acid, sulfuric acid, etc.), organic acids (lactic acid, sodium lactate, citric acid, sodium citrate, succinic acid, sodium succinate, etc.), inorganic bases (potassium hydroxide, hydroxide) Sodium) and organic bases (triethanolamine, diisopropanolamine, triisopropanolamine, etc.).

  Examples of the stabilizer include sodium polyacrylate, dibutylhydroxytoluene, and butylhydroxyanisole.

  Examples of the irritation reducing agent include licorice extract, sodium alginate, and 2-methacryloyloxyethyl phosphorylcholine.

  Examples of the colorant include inorganic pigments and natural pigments.

  Examples of the pearl luster imparting agent include ethylene glycol distearate, ethylene glycol monostearate, and triethylene glycol distearate.

  An additive may be used individually by 1 type and may be used in combination of 2 or more type.

  The pH of the scalp external composition according to this embodiment is not particularly limited as long as it is within a physiologically or pharmaceutically acceptable range, but may be, for example, 3-9, and 3.5-8.5. Preferably, it is preferably 4-8, more preferably 4-7.

  The external composition for scalp which concerns on this embodiment may be a composition of a solubilization system, an emulsion system, or a powder dispersion system, for example. From the viewpoint of more prominently achieving the effects of the present invention, the scalp external composition is preferably a solubilized composition. In the present specification, the solubilization system refers to a one-phase system state in which water and oil do not undergo phase separation and exhibit a uniform and transparent appearance and are also thermodynamically stable. That is, the solubilization system is a state excluding an emulsification system or a powder dispersion system.

  The dosage form of the external composition for scalp according to the present embodiment can be arbitrarily selected according to the use of the external composition for scalp, for example, an external solution, a liniment, a lotion, an ointment, a cream. , Gel agents and the like. These dosage forms can be formulated according to known methods. The dosage form of the scalp external composition according to the present embodiment is preferably an external liquid, lotion, or gel, and more preferably an external liquid or lotion.

  The scalp external composition according to the present embodiment can be applied to the scalp by pressing an application part formed of a soft porous material onto the hair or directly against the scalp or spreading while pressing. it can. Thereby, regardless of whether it is a hair growth site | part, the delivery of an active ingredient or a functional ingredient to a hair follicle deep part becomes possible efficiently. The effective dose of the external composition for scalp according to this embodiment can be appropriately set according to the type and content of the compounding ingredients, the use and dosage form, the symptoms, and the like.

The scalp external composition according to the present embodiment can be used by, for example, applying an appropriate amount to the scalp several times a day or when symptoms (itchiness, etc.) appear. When applying regularly, it is preferable to apply to scalp after scalp washing and hair washing. Although it does not specifically limit as an appropriate amount, For example, it can be about 20-60 mg / cm < ² > once per unit area.

  EXAMPLES Hereinafter, although this invention is demonstrated concretely based on an Example etc., this invention is not limited to these.

〔Test method〕
(Scalp model with hair follicle)
A silicon sheet (as one, silicon rubber sheet 5t300 square) having a thickness of 5 mm (corresponding to the hair depth in a human scalp hair follicle) is formed into a circular shape of 4.15 cm ² (1.1 cm × 1.1 cm × 3.14). Die cut. Using a 1 mm biopsy punch (Kai Medical BP-10F, biopsy trepan), 25 through holes were formed in the thickness direction of the punched sheet. This was used as a scalp model with hair follicles.

(Discharge rate adjustment)
In order to arrange the discharge amount in the penetration test, the discharge amount was measured in advance for each test preparation. In the test preparation, the composition (prescription) described in each table is contained in a liquid narrow mouth container (see FIG. 4) or a liquid application stopper type container (see FIG. 1) having a soft porous coating part. is there. First, the amount of the composition discharged from the container was measured from the change in the weight of the Kim towel before and after the application part of the container was pressed against the Kim towel five times, and this was repeated five times to obtain the average value of the measured values. This average value was defined as one discharge amount. The number of pressings was adjusted so that the discharge amount was the same (0.4 g) between the test preparations to be compared from the single discharge amount thus obtained.

(Penetration test-no hair)
This will be described with reference to FIG. First, a silicon sheet 120 (a scalp model with a hair follicle) having a through hole 110 is placed on the Kim towel 130, and a test preparation (in FIG. 2 (a), from the surface opposite to the Kim towel 130 of the scalp model with a hair follicle, The stopper-type container 100 for liquid application provided with a soft porous application part was pressed evenly. The number of pressings was adjusted so that the discharge amount of each test preparation was 0.4 g. After the pressing, the permeated liquid 140 that permeated through the through hole 110 was absorbed by the Kim towel 130. From the change in the weight of the Kim towel before and after pressing, the amount of the composition that penetrated the Kim towel was measured. This measured value was defined as the amount of penetration into the hair follicle (without hair).

(Penetration test-with hair)
This will be described with reference to FIG. First, a silicon sheet 120 (a scalp model with a hair follicle) having a through hole 110 is placed on the Kim towel 130, and a hair sample 150 (Buelux, BM-B15) is placed on the surface opposite to the Kim towel 130 of the scalp model with a hair follicle. ) Was placed. From the surface on which the hair sample 150 is placed, the test preparation (in FIG. 2 (b), the stopper-type container 100 for liquid application provided with a soft porous application part) was pressed evenly. The number of pressings was adjusted so that the discharge amount of each test preparation was 0.4 g. After the pressing, the permeated liquid 140 that permeated through the through hole 110 was absorbed by the Kim towel 130. From the change in the weight of the Kim towel before and after pressing, the amount of the composition that penetrated the Kim towel was measured. This measured value was defined as the amount of penetration into the hair follicle (with hair).

[Test Example 1: Comparison of containers (1)]
Each formulation shown in Table 1 was prepared and stored in a liquid-coated stopper-type container provided with a soft porous coating part formed of a soft porous natural rubber foam or a liquid narrow-mouthed container to obtain a test preparation. . Blue No. 1 is added to increase the visibility of the prescription.

The penetration amount (without hair) and penetration amount (with hair) of each test preparation were measured by the method described in [Test method]. The results are shown in Table 2 and FIG. FIG. 3A is a graph plotting the amount of penetration (without hair) against the ethanol concentration. FIG. 3B is a graph in which the amount of penetration (with hair) is plotted against the ethanol concentration.

  Surprisingly, as shown in Table 2 and FIG. 3, the liquid-sealed stopper-type container provided with a soft porous coating portion at least in the ethanol concentration range of 5 to 70 w / w% regardless of the presence or absence of hair. However, there was more penetration into the hair follicles of the scalp. In particular, in the case of the presence of hair, the stopper-type container for liquid application provided with a soft porous application part has a significant amount of penetration into the hair follicle of the scalp when the ethanol concentration is in the range of 5 to 50 w / w%.

[Test Example 2: Comparison of prescriptions (1)]
Each formulation shown in Table 3 was prepared and stored in a liquid application stopper-type container provided with a soft porous coating part formed of a soft porous natural rubber foam, or a liquid narrow mouth container to obtain a test preparation. . Blue No. 1 is added to increase the visibility of the prescription.

The penetration amount (with hair) of each test preparation was measured by the method described in [Test Method]. Formula 4 and Formula 6, which were the same formulations as Formula 7 and Formula 8, except that prednisolone valerate acetate (PVA) was not included were also measured in the same manner. The results are also shown in Table 4.

  As shown in Table 4, when the composition contained in the container contained PVA in addition to ethanol, the amount of penetration of the scalp into the hair follicle (with hair) increased significantly. This effect was more remarkable in the case of a liquid application stopper-type container provided with a soft porous application part.

[Test Example 3: Prescription comparison (2)]
Each formulation shown in Table 5 was prepared and stored in a liquid-coated stopper-type container provided with a soft porous coating portion formed of a soft porous natural rubber foam or a liquid narrow-mouthed container to obtain a test formulation. . Blue No. 1 is added to increase the visibility of the prescription.

The penetration amount (with hair) of each test preparation was measured by the method described in [Test Method]. Formulas 6 and 5 which were the same formulas as Formula 9 (or Formula 10) and Formula 11 except that 1-menthol was not included were also measured in the same manner. The results are shown in Tables 6 and 7.

  As shown in Tables 6 and 7, when the composition contained in the container contained menthol in addition to ethanol, the amount of penetration of the scalp into the hair follicle (with hair) increased significantly. This effect was more remarkable in the case of a liquid application stopper-type container provided with a soft porous application part.

[Test Example 4: Comparison of prescriptions (3)]
Formulations shown in Table 8 were prepared and stored in a liquid application stopper-type container provided with a soft porous coating portion formed of a soft porous natural rubber foam or a liquid narrow mouth container to obtain a test preparation. Blue No. 1 is added to increase the visibility of the prescription.

The penetration amount (with hair) of the formulation 12 was measured by the method described in [Test method]. Formulation 6, which was the same formulation as formulation 12, except that diphenhydramine hydrochloride was not included, was measured in the same manner. The results are shown in Table 9.

  As shown in Table 9, when the composition contained in the container contained diphenhydramine hydrochloride in addition to ethanol, the amount of penetration into the hair follicle of the scalp (with hair) increased significantly. This effect was more remarkable in the case of a liquid application stopper-type container provided with a soft porous application part.

[Test Example 5: Comparison of containers (2)]
Each formulation shown in Table 10 was prepared and stored in a liquid-coated stopper-type container provided with a soft porous coating portion formed of a soft porous natural rubber foam, or a liquid narrow mouth container to obtain a test formulation. . Blue No. 1 is added to increase the visibility of the prescription.

The penetration amount (with hair) of each test preparation was measured by the method described in [Test Method]. The results are also shown in Table 11.

  The composition for external use containing a thickener (hydrophobized hydroxypropylmethylcellulose) has a slightly increased viscosity, and therefore tends to hardly penetrate into hair follicles with small scalp. However, as shown in Table 11, even when the composition for external use is blended with a thickener, the amount of penetration into the hair follicle of the scalp is obtained by using a liquid-applicable plug-type container having a soft porous coating part. (With hair) increased significantly.

[Test Example 6: Comparison of containers (3)]
Formulation 4 shown in Table 1 is stored in a liquid-coated stopper-type container having a soft porous coating portion formed of a soft porous polyurethane foam (soft urethane), or a liquid narrow mouth container, and a test formulation It was. The penetration amount (with hair) of each test preparation was measured by the method described in [Test Method]. The results are also shown in Table 12.

  As shown in Table 12, the amount of penetration into the hair follicle is also increased when using a liquid application stopper type container having a soft porous coating portion formed of a soft porous polyurethane foam (soft urethane). It was.

  Separately, the same amount (0.4 g) of prescription 4 as that contained in a container is dropped on the hair sample 150 shown in FIG. Evaluation was also made when the coating was carried out without using. As a result, it was confirmed that even when trying to spread with a finger, the test preparation of Formula 4 was repelled by the hair and very difficult to penetrate, and the amount of penetration tends to be inferior to the case of using a narrow mouth container for liquid.

[Formulation formulation example]
Below, the formulation example of a formulation of this invention is shown. When applied to the scalp, these lotions can not only be applied over a wide range, they are difficult to drip, and even if there is hair, there is a sense that the liquid has reached the scalp and is excellent in effectiveness.

<Prescription Formulation Example 1: Lotion>
(1) Ion exchange water Residue (2) Prednisolone valerate acetate 0.15% by weight
(3) l-Menthol 3.5% by weight
(4) 1,3-butylene glycol 5% by weight
(5) Paraben 0.1% by weight
(6) Disodium edetate 0.05% by weight
(7) Hydrophobized hydroxypropyl methylcellulose 0.1% by weight
(8) 45% by weight absolute ethanol
According to a conventional method, a prescription containing the above components is prepared. The lotion preparation of this embodiment can be produced by filling the prepared formulation into a container having an application part formed of a soft porous material (natural rubber foam).

<Prescription Formulation Example 2: Lotion>
(1) Ion exchange water Residual (2) Diphenhydramine hydrochloride 1.0% by weight
(3) l-Menthol 3.5% by weight
(4) 1,3-butylene glycol 10% by weight
(5) Paraben 0.1% by weight
(6) Disodium edetate 0.05% by weight
(7) Hydrophobized hydroxypropyl methylcellulose 0.2% by weight
(8) 50% by weight absolute ethanol
According to a conventional method, a prescription containing the above components is prepared. The lotion preparation of this embodiment can be produced by filling the prepared formulation into a container having an application part formed of a soft porous material (natural rubber foam).

<Prescription Formulation Example 3: Lotion>
(1) Ion exchange water Residual (2) Dipotassium glycyrrhizinate 0.1% by weight
(3) Tocopherol acetate 0.05% by weight
(4) 1,3-butylene glycol 5% by weight
(5) Paraben 0.1% by weight
(6) Disodium edetate 0.05% by weight
(7) Carboxyvinyl polymer 0.15% by weight
(8) Potassium hydroxide 0.05% by weight
(9) Absolute ethanol 10% by weight
According to a conventional method, a prescription containing the above components is prepared. The lotion preparation of this embodiment can be produced by filling the prepared formulation into a container having an application part formed of a soft porous material (polyurethane foam).

<Prescription Formulation Example 4: Emulsion Lotion>
(1) Ion exchange water Residue (2) Prednisolone valerate acetate 0.15% by weight
(3) Allantoin 0.2% by weight
(4) Dipropylene glycol 3% by weight
(5) Diglycerin 1% by weight
(6) Light liquid paraffin 1.5% by weight
(7) Isopropyl palmitate 0.5 wt%
(8) Sorbitan monostearate 0.5% by weight
(9) Polysorbate 60 1.5% by weight
(10) Paraben 0.2% by weight
(11) Edetate disodium 0.05 wt%
(12) Carboxyvinyl polymer 0.2% by weight
(13) Triethanolamine 0.3% by weight
(14) Absolute ethanol 5% by weight
According to a conventional method, a prescription containing the above components is prepared. By filling the prepared formulation into a container having an application part formed of a soft porous material (natural rubber foam), the emulsification lotion of this embodiment can be produced.

  DESCRIPTION OF SYMBOLS 10,11 ... Container body, 20, 21 ... Composition for external use, 30, 31 ... Cap, 40, 41 ... Screw, 50 ... Application part, 51 ... Opening part (application part), 100 ... Soft porous application part A liquid-coated stopper-type container, 110 through-hole, 120 silicon sheet, 130 Kim towel, 140 penetrating liquid, 150 hair sample, 200 fine-mouth container for liquid.

Claims (7)

Lower alcohol ,
An external composition for scalp containing at least one selected from the group consisting of steroids, monoterpenes, and antihistamine components and housed in a container having an application part formed of a soft porous material.   The composition for external use for scalp of Claim 1 used with respect to a hair growth site | part.   The external composition for scalp according to claim 1 or 2, wherein the content of the lower alcohol is 5 to 70 w / w% based on the total amount of the external composition.   It is for prevention, treatment, and / or amelioration of at least one symptom selected from the group consisting of eczema, dermatitis, hair loss, thinning hair, dandruff, itching, dryness and reduced barrier function in the scalp. The external composition for scalp as described in any one of Claims.   The scalp external composition according to any one of claims 1 to 4, wherein the lower alcohol is ethanol.   The external composition for scalp according to any one of claims 1 to 5, which is a solubilized composition. The external composition for scalp as described in any one of Claims 1-6 which further contains a thickener.

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