JP2021042241A - Composition for external use - Google Patents

Abstract

To provide a novel composition for external use that has excellent affinity for sebum.SOLUTION: In the present invention, a solubilized composition for external use is prepared by using (A) a surfactant that has a single hydrophobic moiety which is a linear structure and that has an HLB value of 15 or greater, and (B) at least one selected from the group consisting of lower alcohols and monoterpenes. The total amount of component (B) is 35 wt.% or less with respect to the entire composition, and the mixed IOB value of component (A) and component (B) is 0.65 or less.SELECTED DRAWING: Figure 1

Description

The present invention relates to an external composition. More specifically, it relates to an external composition having an enhanced affinity for sebum.

Sebum is a type of lipid mainly secreted from the sebaceous glands, and contains glyceride, fatty acids, wax esters, squalene, cholesterol and the like as constituents. Sebum covers the surface of the skin and hair, prevents foreign substances from entering from the outside, and plays an important role in preventing the evaporation of water from the skin surface and exerting a moisturizing effect. The distribution of sebaceous glands that secrete such sebum varies depending on the part of the body, and it is known that sebaceous glands are particularly developed in the scalp, which requires a large amount of sebum to protect hair. It is also known that sebum secretion becomes active under the influence of hormones that increase during the growth period. Especially in young men, the amount of sebum secretion is large, and various troubles such as acne, shine, and stickiness occur. Is the cause of.

Further, in the external composition intended to be applied to the skin and hair, various functional ingredients are blended in anticipation of various effects. However, even if such an external composition is applied to the skin or hair in which excess sebum is secreted, the sebum becomes an obstacle and the water-soluble component becomes difficult to reach the skin or hair. Especially in hair growth agents and hair nourishing agents, it is important for the functional component to reach the deep part of the hair follicle, but there is a concern that the sebum secreted and clogged in the hair follicle hinders the arrival of the component.

Therefore, a means for evaluating the sebum transferability of the test object and simply and accurately determining whether or not the component to be used in the scalp or hair reaches the point of action has been developed (Patent Document 1). ). Furthermore, in a study of skin permeability of a hair restorer, it has been reported that the amount of sebum transferred from a model drug is increased by about 2 times by adding isostearyl alcohol that is compatible with ethanol and sebum (Non-Patent Document 1). ).

Japanese Unexamined Patent Publication No. 2001-174392

Eriko Takeoka, FRAGRANCE JOURNAL, No.329,17-21,2007

An object of the present invention is to provide a useful novel external composition showing high sebum affinity in view of the above-mentioned prior art.

As a result of diligent studies to solve the above problems, the present inventors used a lower alcohol and / or monoterpene in a specific amount together with a specific surfactant, and mixed IOB of these components in the composition. By adjusting the value, it has been found that a solubilized external composition having excellent sebum affinity can be obtained, and the present invention has been completed.

Therefore, the present invention provides the following solubilized external compositions.

(A) A surfactant having a single hydrophobic moiety having a linear structure and an HLB value of 15 or more, and (B) at least one selected from the group consisting of lower alcohols and monoterpenes.
A solubilized external composition containing
A solubilized external composition in which the total amount of the component (B) is 35% by weight or less with respect to the entire composition, and the mixed IOB value of the component (A) and the component (B) is 0.65 or less.

The content of the component (A) can be 0.001 to 10% by weight based on the entire composition.

The content of the component (B) can be 0.0001 to 35% by weight based on the entire composition.

The component (A) is composed of a group consisting of polyoxyethylene alkyl ether, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene polyoxypropylene alkyl ether, polyglycerin fatty acid ester, polyoxyethylene sorbit fatty acid ester, and polyethylene glycol fatty acid ester. It can be at least one selected.

The component (B) is ethanol, isopropanol, propylene glycol, dipropylene glycol, butylene glycol, glycerin, diglycerin, ethoxydiglycol, 1,2-pentanediol, ethylhexanediol, hexylene glycol, menthol, camphor, and eugenol. , Geraniol, Borneol, and Hinokithiol can be at least one selected from the group.

The solubilized external composition may be a solubilized external composition for use on the scalp.

The solubilized external composition may contain a water-soluble hair-growth component and / or a hair-growth component.

The water-soluble hair-growth component and / or hair-growth component includes dipotassium glycyrrhizinate, allantin, pantothenyl ethyl ether, pantenol, pantothenic acid, biotin, nicotinic acid and its derivatives, pyridoxin hydrochloride, carrot extract, senburi extract, and crackle extract. , Shokyo tincture, Hiogi extract, Ogon extract, Tounin extract, Sansha extract, Biwa leaf extract, Confrey extract, Chamomile extract, Zenia oyster extract, Bukuryo extract, Togarashi tincture, Ousei extract, Kagikazura extract, Oazami extract, Henna extract, Kanzo extract, Kashu Extract, Chixetsu carrot extract, Senburi extract, Perilla extract, Hikiokoshi extract, Button extract, Shinano extract, Epine extract, Clara extract, Kujin extract, Shokyo extract, Quachalarate extract, Sophora extract, Amacha extract, Placenta extract, Wine yeast extract, It can be at least one selected from the group consisting of caffeine and its hydrate, and fucoidan.

The present invention is also selected from the group consisting of (A) a surfactant having a single hydrophobic moiety having a linear structure and an HLB value of 15 or more, and (B) a lower alcohol and a monoterpene. At least one of them is used so that the total amount of the component (B) is 35% by weight or less with respect to the entire composition, and the mixed IOB value of the components (A) and (B) is 0.65 or less. As described above, the present invention relates to a method for improving the sebaceous affinity of the external composition, which comprises preparing a solubilized external composition.

INDUSTRIAL APPLICABILITY According to the present invention, it is possible to provide a novel and useful external composition showing high sebum affinity.

It is a figure which shows the result of having evaluated the hair follicle permeability of uranin in Test Example 3. It is a figure which shows the result of having evaluated the hair follicle permeability of dipotassium glycyrrhizinate in Test Example 4. It is a figure which shows the result of having evaluated the hair follicle permeability of pantothenyl ethyl ether in Test Example 5. It is a figure which shows the result of having evaluated the hair follicle permeability of dipotassium glycyrrhizinate in Test Example 6. It is a figure which shows the result of having evaluated the hair follicle permeability of pantothenyl ethyl ether in Test Example 6.

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

(1. External composition)
The external composition of the present invention comprises (A) a surfactant having a single hydrophobic moiety having a linear structure and an HLB value of 15 or more, and (B) a group consisting of a lower alcohol and a monoterpene. Containing at least one selected, the total amount of the component (B) is 35% by weight or less with respect to the entire composition, and the mixed IOB value of the components (A) and (B) is 0.65 or less. A solubilized external composition. Such an external composition of the present invention has a high affinity for sebum and can be useful for improving the transferability of functional components to the skin and hair.

(A) Ingredient:
The component (A) used in the present invention is a surfactant having a single hydrophobic portion having a linear structure and having an HLB value of 15 or more.

Surfactants generally have a hydrophilic portion that is easily compatible with water and a hydrophobic portion that is easily compatible with oil, and have an action of uniformly mixing polar substances and non-polar substances through the formation of a micellar structure or the like. The hydrophobic portion is a portion having a structure exhibiting non-polar properties, and is typically composed of a hydrocarbon group, a fatty acid residue, or the like. Surfactants having various structures have been known so far. For example, in the entire structure of a surfactant, one having only one hydrophobic portion, one having a plurality of hydrophobic portions, or a hydrophobic portion having a linear structure. There are many known ones that have a branched structure and those that have a branched structure.

In the present invention, among the above-mentioned surfactants, those having only one hydrophobic portion, for example, a hydrocarbon group or a fatty acid residue in one molecule, and the hydrophobic portion having a linear structure. Is used. As shown in the results of the test examples described later, it is difficult to obtain the effect of the present invention if the surfactant contains a plurality of hydrophobic portions, and the surfactant having a branched structure in the hydrophobic portion is also described in the present invention. It is not preferable because it is difficult to obtain the effect.

The surfactant having a single hydrophobic moiety, that is, the surfactant having only one hydrophobic moiety is not particularly limited, and is, for example, polyoxyethylene alkyl ether, polyoxyethylene polyoxypropylene alkyl ether, propylene. Glycol fatty acid ester, polyoxyethylene glycerin fatty acid ester; polyoxyethylene sorbitan fatty acid ester, sorbitan fatty acid ester, polyethylene glycol fatty acid ester, glycerin fatty acid ester, polyglycerin fatty acid ester, hydrogenated lecithin, hydroxide lecithin, hydrophobized lysolecithin, polyoxy Examples thereof include surfactants such as ethylene sorbit fatty acid ester having one hydrophobic portion. From the viewpoint that the effects of the present invention can be more reliably exhibited, preferably, polyoxyethylene alkyl ether, polyoxyethylene polyoxypropylene alkyl ether, polyoxyethylene sorbitan fatty acid ester, polyglycerin fatty acid ester, polyoxyethylene sorbit fatty acid. Esters, polyethylene glycol fatty acid esters, more preferably polyoxyethylene alkyl ethers, polyoxyethylene sorbitan fatty acid esters, and even more preferably polyoxyethylene alkyl ethers are used.

Further, the surfactant that can be used as the component (A) in the present invention has a hydrophobic portion having a linear structure. The hydrophobic portion of the linear structure is not particularly limited, and examples thereof include a linear hydrocarbon group and / or a fatty acid residue. The linear hydrocarbon group and fatty acid residue may be saturated or unsaturated as long as they are linear. The carbon number of the linear hydrocarbon group and the fatty acid residue is not particularly limited as long as the effects of the present invention can be obtained, but as an example, the number of carbon atoms is 6 or more, preferably 6 to 30, and more preferably 8. ~ 24, more preferably 10 to 22, and particularly preferably about 12 to 18 are used. Specifically, examples of the linear hydrocarbon group or fatty acid residue include a hexyl group, a heptyl group, an octyl group, a nonyl group, a decyl group, a lauryl group, a myristyl group, a cetyl (palmityl) group, a stearyl group and a behenyl group. Saturated hydrocarbon groups such as groups; unsaturated hydrocarbon groups such as oleyl group, linoleyl group, linoleyl group, lysinorail group; caproic acid, capric acid, capric acid, lauric acid, myristic acid, palmitic acid, stearic acid, behenic acid Saturated fatty acid residues such as; Unsaturated fatty acid residues such as oleic acid, linoleic acid, linolenic acid, and ricinolenic acid can be mentioned, but are not limited thereto. Further, the linear fatty acid residue may be a naturally occurring mixed fatty acid residue containing a plurality of linear fatty acid residues, and examples of such a mixed fatty acid residue include coconut oil fatty acid residue. Examples include, but are not limited to, palm oil fatty acid residues, palm kernel oil fatty acid residues, olive oil fatty acid residues, and the like.

In the present invention, preferred examples of the polyoxyethylene alkyl ether are polyoxyethylene oleyl ether, polyoxyethylene lauryl ether, polyoxyethylene cetyl ether, polyoxyethylene stearyl ether, polyoxyethylene myristyl ether, and polyoxyethylene behenyl. It includes, but is not limited to, ether and the like. In addition, salts of polyoxyethylene alkyl ethers can also be used, and examples of such salts include phosphates, carboxylates, sulfates or acetates.

In the present invention, examples of the polyoxyethylene polyoxypropylene alkyl ether include, but are not limited to, polyoxyethylene polyoxypropylene lauryl ether and polyoxyethylene polyoxypropylene cetyl ether.

Examples of polyoxyethylene sorbitan fatty acid esters include polyoxyethylene coconut oil fatty acid sorbitan, polyoxyethylene sorbitan monolaurate, polyoxyethylene sorbitan monopalmitate, polyoxyethylene sorbitan monostearate, and polyoxyethylene sorbitan monooleate. However, there is no limitation.

Examples of polyglycerin fatty acid esters include, but are not limited to, polyglyceryl monolaurate, tetraglycerin stearate, decaglycerin laurate, decaglycerin stearate, decaglycerin olate, and the like.

Examples of the polyoxyethylene sorbit fatty acid ester include, but are not limited to, sodium lauryl sulfate 6.

Examples of polyethylene glycol fatty acid esters include, but are not limited to, polyethylene glycol monostearate.

Further, the surfactant that can be used as the component (A) in the present invention preferably has an HLB value of 15 or more. The HLB value is a value generally used in the art for evaluating the properties of a surfactant, and is also called a hydrophilic-lipophilic balance (Hydrophile-Lipophile Balance). The HLB value is generally determined as the ratio of the strength of the hydrophilic portion to the whole molecule, and those having a small HLB value tend to have high lipophilicity, and those having a high HLB value tend to have high hydrophilicity. Specifically, in the present invention, the HLB value refers to the measured value by the emulsification method described in "Handbook-Cosmetics / Pharmaceutical Ingredients-", Nikko Chemicals Co., Ltd. (issued on February 1, 1977). .. Specifically, the measured value of HLB by the emulsification method is obtained by the following procedure. First, sorbitan monostearate (NIKKOL SS-10) and polyoxyethylene sorbitan monostearate (NIKKOL TS-10) are used in combination as a standard substance for a surfactant, and liquid paraffin is used as an emulsion. The liquid paraffin is emulsified with the above-mentioned two types of surfactants to calculate the optimum ratio of the surfactants, and the required HLB value of the liquid paraffins is obtained according to the following formula A.
[Formula A] HLB value of liquid paraffin = {(HLB value of TS-10 (14.9) x% used) + (HLB value of SS-10 (4.7) x% used)} / 100
Usually, the required HLB value of liquid paraffin is about 10.1 to 10.3. The unknown surfactant is then measured using liquid paraffin for which the HLB value has been determined. If the unknown surfactant is hydrophilic, combine it with SS-10, and if it is lipophilic, combine it with TS-10 to emulsify liquid paraffin and find the optimum ratio of stable parts. Calculated by applying the HLB value of the activator to the above formula A as x. Here, the emulsification formulation is carried out with 40% of liquid paraffin, 4% of the surfactant used (total amount of the two surfactants used), and 56% of water. The total amount of the surfactant is kept constant, and only the ratio is changed to emulsify until it can be emulsified. The ratio of the surfactant is changed by 0.1%. Cover the resulting emulsion so that water does not evaporate, and after all emulsification work is completed, dilute each of the obtained emulsions to 1%, collect approximately the same amount in a test tube with a stopper, and leave it for a whole day and night. However, judging from the amount of creaming, the degree of white turbidity, the separation of water in the lower layer, etc., the one with the best stability is set as the optimum ratio.

Unexpectedly in the present invention, by using a surfactant having a high HLB value that increases hydrophilicity, an external composition exhibiting high sebum affinity can be obtained. The HLB value of the surfactant used as the component (A) in the present invention is not particularly limited as long as it is 15 or more, but from the viewpoint of more reliably exhibiting a high effect, it is preferably HLB 15 to 20, more preferably HLB 16. ~ 19.5, more preferably HLB 16.5-19.

The HLB value of the surfactant used as the component (A) in the present invention is 15 or more, preferably 16 or more, and more preferably 16.5 or more. The HLB value of the surfactant used as the component (A) in the present invention is preferably 20 or less, more preferably 19.5 or less, still more preferably 19 or less.

Specifically, it is used pharmaceutically or physiologically as a surfactant having a single hydrophobic moiety having a linear structure and having an HLB value of 15 or more, which can be used as the component (A) in the present invention. It is not particularly limited as long as it can be used, but for example, polyoxyethylene (20) oleyl ether, polyoxyethylene (15) oleyl ether, polyoxyethylene (50) oleyl ether, polyoxyethylene (21). Lauryl ether, polyoxyethylene (25) lauryl ether, polyoxyethylene (15) cetyl ether, polyoxyethylene (20) cetyl ether, polyoxyethylene (23) cetyl ether, polyoxyethylene (25) cetyl ether, polyoxy Ethylene (30) cetyl ether, polyoxyethylene (20) stearyl ether, polyoxyethylene (20) behenyl ether, polyoxyethylene (30) behenyl ether, polyoxyethylene (20) polyoxypropylene (4) cetyl ether, poly Oxyethylene (20) Palm oil fatty acid sorbitan, polyoxyethylene monopalmitate (20) sorbitane, polyoxyethylene monooleate (20) sorbitan, sorbeth-6 laurate, polyglyceryl monolaurate-10, polyethylene glycol monostearate ( 25), polyethylene glycol monostearate (40), polyethylene glycol monostearate (45), polyethylene glycol monostearate (55) and the like can be mentioned. From the viewpoint that it can be expected that a higher effect can be exhibited more reliably, preferably, polyoxyethylene (20) oleyl ether, polyoxyethylene (15) oleyl ether, polyoxyethylene (50) oleyl ether, and polyoxyethylene (20). ) Palm oil fatty acid sorbitane, polyoxyethylene monopalmitate (20) sorbitan, polyoxyethylene monooleate (20) sorbitane, polyoxyethylene (20) polyoxypropylene (4) cetyl ether, or polyglyceryl-10 monolaurate It is used, and more preferably, polyoxyethylene (20) oleyl ether or polyoxyethylene (20) coconut oil fatty acid sorbitan is used. Particularly preferred is polyoxyethylene (20) oleyl ether.

In the present invention, the above-mentioned component (A) may be used alone or in any combination of two or more.

The content of the component (A) in the external composition of the present invention is not particularly limited as long as the effects of the present invention can be exhibited, but is preferably 0.001 to 10% by weight based on the entire composition. Is 0.01 to 5% by weight, more preferably 0.1 to 5% by weight. According to the present invention, even if the content of the surfactant as the component (A) is as small as shown above, high sebum affinity can be exhibited.

The content of the component (A) in the external composition of the present invention is preferably 0.001% by weight or more, more preferably 0.01% by weight or more, still more preferably 0.1% by weight, based on the entire composition. % Or more. The content of the component (A) in the external composition of the present invention is preferably 10% by weight or less, more preferably 5% by weight or less, based on the entire composition.

(B) Ingredient:
The external composition of the present invention further contains at least one selected from the group consisting of lower alcohols and monoterpenes. The external composition of the present invention may contain only one of the lower alcohol and the monoterpene as the component (B), or may contain both the lower alcohol and the monoterpene. Although not particularly limited, it is more preferable that the component (B) contains monoterpenes (containing only monoterpenes or containing monoterpenes together with lower alcohols).

In the present specification, the lower alcohol refers to any alcohol having about 1 to 8 carbon atoms, and is not particularly limited as long as it can be used pharmaceutically or physiologically. The lower alcohol used in the present invention may be monohydric or polyhydric, but is preferably a lower alcohol having 1 to 4 hydroxyl groups in the molecule, and more preferably in the molecule. It is a lower alcohol having 1 to 3 hydroxyl groups, and more preferably a lower alcohol having 1 to 2 hydroxyl groups in the molecule.

Specifically, as lower alcohols, monohydric lower alcohols such as ethanol, propanol, isopropanol, n-butyl alcohol, s-butyl alcohol, t-butyl alcohol, isobutyl alcohol, pentyl alcohol, hexyl alcohol, and ethoxydiglycol; Divalent lower alcohols such as propylene glycol, dipropylene glycol, butylene glycol, 1,2-pentanediol, ethylhexanediol, hexylene glycol; trihydric lower alcohols such as glycerin; tetrahydric lower alcohols such as diglycerin ;, Etc., but are not limited to these. Among them, from the viewpoint of more reliably exerting a high effect, preferably ethanol, isopropanol, propylene glycol, dipropylene glycol, butylene glycol, glycerin, diglycerin, ethoxydiglycol, 1,2-pentanediol, ethylhexane. Diol, hexylene glycol, more preferably ethanol, propylene glycol, dipropylene glycol, butylene glycol are used. One of these lower alcohols may be used alone, or two or more thereof may be used in any combination.

The lower alcohol used as the component (B) in the present invention preferably has an IOB value of about 0.1 to 5.0 from the viewpoint that it is easy to adjust to the mixed IOB value described later and a higher effect can be easily obtained. A lower alcohol of about 0.4 to 5.0, more preferably 1.0 to 5.0 is preferable.

The monoterpene that can be used in the present invention is a compound that has a structure composed of two isoprene units and is known as a refreshing agent or the like. Any monoterpene that is pharmaceutically or physiologically acceptable can be used in the present invention. The monoterpene may be d-form, l-form, or dl-form.

Specifically, as monoterpenes, acyclic monoterpenes such as geraniol, nerol, milsenol, linalool, linalool acetate, lavandulol; monocyclic monoterpenes such as menthol, limonene, anator, eugenol, hinokithiol; Bicyclic monoterpenes such as camphor, borneol, isobornol, cineol, pinene; and the like, but are not limited thereto. Among them, monoterpene and bicyclic monoterpenes are preferable, and menthol, camphor, eugenol, geraniol, borneol, and hinokithiol are preferable from the viewpoint of more surely exerting a high effect. More preferably, it is menthol or camphor, and even more preferably, it is menthol. One of these monoterpenes may be used alone, or two or more thereof may be used in any combination.

Further, as the monoterpene, an essential oil containing the monoterpene may be used. Examples of such essential oils include cool mint oil, peppermint oil, peppermint oil, eucalyptus oil, bergamot oil, spare mint oil, rose oil, and cypress oil. For example, essential oils containing menthol and camphor include cool mint oil, peppermint oil, peppermint oil, camphor oil and the like. These essential oils can be collected from plants by known methods. As such known essential oil extraction methods, a steam distillation method, an oil / fat adsorption method in which a plant is added to deodorized animal oil / fat to adsorb the essential oil and then the essential oil is extracted with ethanol, and the plant is organic such as hexane or benzene. Examples thereof include a solvent extraction method and a pressing method in which extraction is performed with a solvent or a supercritical fluid, the extraction solvent is dissolved in ethanol, and then ethanol is evaporated to collect the residue. Monoterpenes can also be recovered from essential oils by various chromatographies.

The monoterpene used as the component (B) in the present invention preferably has an IOB value of about 0.1 to 5.0 from the viewpoint that it is easy to adjust to the mixed IOB value described later and a higher effect can be easily obtained. A monoterpene of about 0.2 to 3.0, more preferably about 0.4 to 2.0 is preferable.

The content of (B) lower alcohol and / or monoterpene in the external composition of the present invention shall be 35% by weight or less based on the entire composition. Of course, since the external composition of the present invention contains the component (B) as an essential component, the composition does not contain the component (B) at all. By setting the content of the component (B) to 35% by weight or more and more than 0% by weight in this way, it is possible to exhibit high sebum affinity. Preferably, the total amount of the component (B) is 0.0001 to 35% by weight, more preferably 0.001 to 33% by weight, still more preferably 0.01, based on the whole composition. ~ 31% by weight, more preferably 0.1 to 31% by weight. More specifically, the content of each component (B) may be in the following range:
When lower alcohol is contained as the component (B): these are in total amounts, preferably 0.01 to 35% by weight, more preferably 0.1 to 33% by weight, still more preferably 1 to 30% based on the entire composition. By weight%. When the lower alcohol is contained as the component (B), the total amount of the lower alcohol may be, for example, about 5 to 30% by weight based on the entire composition.
(B) When monoterpenes are contained as components: these are in total amounts, preferably 0.001 to 10% by weight, more preferably 0.001 to 5% by weight, still more preferably 0.01, based on the entire composition. ~ 1% by weight. When monoterpenes are contained as the component (B), the total amount thereof may be, for example, about 0.1 to 0.5% by weight with respect to the entire composition.

In the external composition of the present invention, the total amount of the component (B) is 0.0001% by weight or more, more preferably 0.001% or more, still more preferably 0.01% by weight or more, more preferably 0.01% by weight or more, based on the entire composition. It is 0.1% by weight or more, 35% by weight or less, more preferably 33% by weight or less, still more preferably 31% by weight or less.

When an essential oil containing a monoterpene is used as the monoterpene, the content of the monoterpene in the essential oil to be blended is set so as to satisfy the above blending amount.

The ratio of the content of the component (B) to the content of the component (A) in the external composition of the present invention is not particularly limited as long as the effect of the present application can be obtained, but from the viewpoint that a higher effect can be more reliably exhibited. Preferably, the total amount of the component (A) is 1 part by weight, and the total amount of the component (B) is 0.00001 to 35,000 parts by weight, more preferably 0.001 to 3300 parts by weight, still more preferably 0.01 to 0.01 to parts by weight. It is 300 parts by weight. Further, for example, the total amount of the component (B) may be 0.1 to 50 parts by weight with respect to 1 part by weight of the total amount of the component (A). More specifically, there is a ratio in which the total amount of each component (B) is in the following range with respect to 1 part by weight of the total amount of component (A):
(B) When lower alcohol is contained as a component: These are usually 0.00001 to 35,000 parts by weight, preferably 0.001 to 3300 parts by weight, and more preferably 0.01 to 300 parts by weight. For example, the total amount of the component (A) may be 1 part by weight, and the amount of lower alcohol may be 1 to 50 parts by weight.
(B) When monoterpenes are contained as components: these are usually 0.0001 to 10000 parts by weight, preferably 0.001 to 500 parts by weight, and more preferably 0.01 to 10 parts by weight in total. For example, the total amount of the component (A) may be 1 part by weight, and the amount of monoterpene may be 0.1 to 5 parts by weight.
When an essential oil containing a monoterpene is used as the monoterpene, the content of the monoterpene in the essential oil to be blended is set so as to satisfy the above blending ratio.

In the present invention, it is important to adjust the mixed IOB value calculated from the IOB value and the content of each of the components (A) and (B) to be blended in the external composition to 0.65 or less. .. As shown in the results of the test examples described later, when the mixed IOB value of the components (A) and (B) is higher than 0.65, the sebum affinity decreases, which is not preferable.

The IOB value (also called the Inorganic Organic Balance value) is an organic conceptual diagram (Akira Fujita, Prediction of Organic Compounds and Organic Conceptual Diagram, Area of Chemistry Vol.11, No.10 (1957). The organic value (OV) and the inorganic value (IV) of the target compound are calculated based on 719-725), and the values are known as those calculated by the ratio (IV / OV) of them. (For details on organic conceptual diagrams, see "New Edition Organic Conceptual Diagrams-Basics and Applications-", by Yoshio Koda et al., Sankyo Publishing, 2008). Specifically, to exemplify the IOB values of some components, polyoxyethylene (20) oleyl ether [IOB value: 1.33], polyoxyethylene (15) oleyl ether [IOB value: 1.22], poly Oxyethylene (50) oleyl ether [IOB value: 1.61], polyoxyethylene (20) coconut oil fatty acid sorbitan [IOB value: 1.53], polyoxyethylene monopalmitate (20) sorbitan [IOB value: 1] .44], polyoxyethylene monooleate (20) sorbitan [IOB value: 1.39], polyoxyethylene (20) polyoxypropylene (4) cetyl ether [IOB value: 1.19], polyglyceryl monolaurate- 10 [IOB value: 1.60], ethanol [IOB value: 2.50], isopropanol [IOB value: 2.00], propylene glycol [IOB value: 3.33], dipropylene glycol [IOB value: 1. 83], butylene glycol [IOB value: 2.50], glycerin [IOB value: 5.00], diglycerin [IOB value: 3.50], ethoxydiglycol [IOB value: 1.63], 1, 2 -Pentanediol [IOB value: 2.00], ethylhexanediol [IOB value: 1.33], hexylene glycol [IOB value: 1.82], hinokithiol [IOB value: 0.95], menthol [IOB value] : 0.58], DL camphor [IOB value: 0.47], Eugenol [IOB value: 0.69], Geraniol [IOB value: 0.58], DL Borneol [IOB value: 0.65] are known. ing.

In the present specification, the mixed IOB value of the component (A) and the component (B) is the weight of each component when the entire composition is 1 part by weight based on the IOB value of each component (A) and (B). The sum of the products multiplied by the values of the parts. For example, take the case of an external composition containing 1% by weight of polyoxyethylene (20) oleyl ether as the component (A), 20% by weight of ethanol and 0.2% by weight of menthol as the component (B). , The mixed IOB value of the component (A) and the component (B) is (1.33 × 0.01) + (2.5 × 0.2) + (0.58 × 0.002) = 0.51446. Calculated. Even if the type and content of each component (A) and component (B) change, the same calculation may be performed.

The mixed IOB value of the component (A) and the component (B) in the external composition of the present invention is not particularly limited as long as it is adjusted to be 0.65 or less, but the lower limit is usually 0.001 or more, preferably 0.001 or more. Is preferably 0.005 or more, more preferably 0.01 or more.

Further, the external composition of the present invention preferably further contains a functional component capable of exerting a useful action on the skin and hair. Since the external composition of the present invention has an excellent affinity for sebum, the site where these functional components are expected to exert their action through the sebum covering the skin and hair (for example, hair in the case of a hair restorer). It becomes easier to reach the deep part of the hair follicle, and it becomes easier to obtain the intended effect. In particular, water-soluble functional components generally do not easily pass through sebum, but according to the present invention, even such water-soluble functional components satisfactorily pass through sebum and act on the skin, hair, etc. It becomes easier to reach.

Specifically, the functional component that can be blended in the external composition of the present invention is not particularly limited as long as it is pharmaceutically or physiologically acceptable, and for example, a hair growth component, a hair nourishing component, and an antiaging component. , UV scattering component, UV absorbing component, component having DNA damage prevention and / or repair action, whitening component, cell activating component, astringent component, antioxidant component, antibacterial component, moisturizing component, minerals, etc. it can. Preferably, as the functional component, a hair-growth component and a hair-nourishing component that are expected to reach the deep part of the hair follicle are blended.

As the hair-growth component and the hair-growth component, any component known to exert a hair-growth effect and / or a hair-growth effect when applied to the scalp can be used. For example, as a hair-growth component and a hair-growth component, carrot extract, senburi extract, crackle extract, ginger extract, ginger extract, ginger extract, tounin extract, sansha extract, biwa leaf extract, comfrey extract, chamomile extract, zegnaoi extract, bukuryo extract. , Togarashi tinki, Osei extract, Kagikazura extract, Oazami extract, Henna extract, Kanzo extract, Kashu extract, Chikusetsu carrot extract, Senburi extract, Shiso extract, Hikiokoshi extract, Button extract, Shinano extract, Epine extract, Clara extract, Kujin extract, Shokyo extract, Biological extracts such as quacharalate extract, sophora extract, amacha extract, placenta extract, wine yeast extract; pantothenyl ethyl ether, pantenol, pantothenic acid, biotin, nicotinic acid and derivatives thereof (eg, nicotinic acid amide, etc.), Vitamins such as pyridoxin hydrochloride, vitamin E and derivatives thereof (for example, tocopherol esters such as tocopherol acetate); anti-inflammatory components such as dipotassium glycyrrhizinate, stearyl glycyrrhetinate, glycyrrhetinic acid, allantin, sodium salicylate, salicylic acid; Thermolysin degradation products, minoxydil and its relatives and their derivatives, fucoidan, photosensitizer, caffeine and its hydrate, mononitroguaiacol, carpronium chloride or its hydrate, cepharanthin, estradiol, ethynyl estradiol, langic acid, 5α Reductase inhibitors (eg finasteride), 12-tetradecanoylforbol-13-acetate, estradiol benzoate, diphenhydramine, resorcin, selenium disulfide, zincpyrythion, pyrocton olamine, sulfur, dialkylmonoamine derivatives, dialkylmono derivatives , Myconazole nitrate, benzoic acid, phytosterol, tacanal, ethynyl estradiol, isopropylmethylphenol, cepharanthin, 6-benzylaminopurine, pentadecanoic acid glyceride, t-flabanone, adenosine, and the like, but not limited to these. Here, the biological extract is an arbitrary extraction solvent (for example, water or an organic solvent (for example, ethanol, methanol, propanol, etc.) from a biological raw material (for example, plants, animals, fungi) by a method well known to those skilled in the art. It can be an extract obtained by extracting by a conventional method using a hydrophilic organic solvent) or a mixed solution of water and an organic solvent (for example, hydrous ethanol). As the hair-growth component and the hair-growth component, one of the above may be used alone, or two or more of them may be used in any combination.

Among the above-mentioned hair-growth components and hair-growth components, water-soluble hair-growth components and hair-growth components are preferably used, and more preferably water-soluble, from the viewpoint that the advantages of obtaining the effects of the present invention are great. Sexual biological extracts, water-soluble vitamins, water-soluble anti-inflammatory components and the like are used. Specific examples of such preferable water-soluble hair-growth and hair-growth components include carrot extract, senburi extract, crackle extract, ginger extract, ginger extract, ginger extract, tounin extract, sansha extract, and biwa leaf extract. Comfrey extract, chamomile extract, zegna oyster extract, bukuryo extract, capsicum tincture, pearl oyster extract, key kazura extract, oyster extract, henna extract, kanzoue BR> L su, kashu extract, chikusetsu carrot extract, senburi extract, perilla extract Extract, Shinano extract, Epine extract, Clara extract, Kujin extract, Shokyo extract, Quachalarate extract, Sophora extract, Amacha extract, Placenta extract, Wine yeast extract, Pantothenyl ethyl ether, Pantenol, Pantothenic acid, Biotin, Nicotinic acid and Examples thereof include, but are not limited to, pyridoxin hydrochloride, dipotassium glycyrrhizinate, allantin, caffeine and its hydrate, fucoidan and the like. Of these, carrot extract, senburi extract, crackle extract, ginger extract, ginger extract, ginger extract, tounin extract, sansha extract, biwa leaf extract, comfrey extract, chamomile extract, zegna oyster extract, bukuryo extract, pantothenyl ethyl ether , Dipotassium glycyrrhizinate, caffeine and its hydrate.

The content of the functional component in the external composition of the present invention may be appropriately varied depending on the degree of desired effect, the age, sex, condition, application site, etc. of the subject to be applied, and is, for example, 0.00001 to 0.00001. It is preferably about 50% by weight, preferably 0.0001 to 30% by weight, and more preferably about 0.001 to 10% by weight.

The content of the functional component in the external composition of the present invention is, for example, 0.00001% by weight or more, preferably 0.0001% by weight or more, more preferably 0.001% by weight or more, and preferably 50. It is preferably 7% by weight or less, more preferably 30% by weight or less, and more preferably 10% by weight or less.

In addition to the above-mentioned components, the external composition of the present invention may appropriately contain components that can be usually used in the fields of pharmaceuticals, quasi-drugs, cosmetics, etc., depending on the intended use or dosage form. The components that can be blended are not particularly limited, but are, for example, bases or carriers, surfactants other than component (A), viscosity regulators (for example, hyaluronic acid and salts thereof, xanthan gum, carrageenan, carboxyvinyl polymers, etc.). Additives such as antioxidants, preservatives, pH adjusters, chelating agents, stabilizers, irritation reducing agents, preservatives, colorants, dispersants, and fragrances can be blended. In addition, these components can be blended alone or in any combination of two or more.

As the base or carrier, aqueous bases such as water; hydrocarbons such as liquid paraffin, squalane, vaseline, gelled hydrocarbons (such as plastibase), ozokelite, α-olefin oligomers, and light liquid paraffins; cetanol, cetostearyl. Higher alcohols such as alcohols, stearyl alcohols, behenyl alcohols; cellulose derivatives such as ethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose; polyvinylpyrrolidone; carrageenan; polyvinylbutyrate; polyethylene glycol; dioxane; polyester butylene glycol adipate; isopropyl myristate , Octyldodecyl myristate, isopropyl palmitate, cetyl palmitate, isononyl isononanoate, pentaerythritate tetra2-ethylhexanoate, esters such as jojoba oil; polysaccharides such as dextrin, maltodextrin; etc. However, it is not limited to these. The external composition of the present invention usually contains at least one aqueous base material, preferably water. When the external composition of the present invention contains water, the content thereof can be appropriately selected, but as an example, 30 to 99% by weight, preferably 40 to 99% by weight, and more preferably 50 to 50% by weight based on the entire composition. It is 95% by weight.

Although the external composition of the present invention is a solubilized external composition using water as a main base, it can exhibit high sebum affinity. Here, the solubilized system refers to a state of a one-phase system in which water and oil do not undergo phase separation and exhibit a uniform and transparent appearance and are thermodynamically stable. That is, the solubilization system is a state excluding the so-called emulsification system. The dosage form of the external composition of the present invention is not particularly limited as long as it is solubilized, and for example, any form such as liquid, lotion, gel, sheet (supporting a base material), aerosol, and spray can be used. Can be. It is preferably liquid.

In addition, the solubilized external composition of the present invention can be prepared in any various product forms, and can be any product form that can be used as, for example, pharmaceuticals, quasi-drugs, cosmetics, and the like. Specifically, hair growth products, hair growth products, scalp hair products (for example, scalp lotions, hair tonics), skin care products (for example, lotions, lotions, facial masks), body care products (for example, for example). Whole body lotion, bath salt), but not limited to these. Preferably, it is beneficial to use in products applied to the scalp with developed sebaceous glands. Furthermore, it is beneficial to prepare as a hair-growth product and / or a hair-growth product, which is hindered by sebum clogged in the hair follicle and whose functional components are generally difficult to reach.

The solubilized external composition of the present invention usually has a liquid property of pH 2.0 to 10.0, but is preferably pH 3.0 from the viewpoint of low irritation to the skin and good usability. It is desirable that the pH is ~ 9.5, more preferably pH 3.0 to 9.0, and particularly preferably about pH 3.5 to 8.5.

The external composition of the present invention is used for skin and hair according to a conventional method. For example, when used as a hair-growth product and / or a hair-growth product, a place where the hair-growth or hair-growth effect is desired (for example, hair, eyebrows, eyebrows, mustache, pubic hair, chest hair, back hair, axillary hair). , Pubic hair, hand and arm hair, shin hair, etc.), especially on the scalp where hair growth or hair growth effect is desired to be exerted on the hair, directly applied, sprayed or immersed It can be applied by doing the above. The usage and dosage for application can be appropriately set according to the form and the degree of desired effect, and for example, when used with the expectation of hair growth or hair nourishing effect on the scalp, an appropriate amount. It may be applied, sprayed or soaked once to several times a day so that (for example, about 0.1 to 10 g) spreads over the entire scalp.

The external composition of the present invention can be used for all people, but it is generally known that men secrete more sebum than women, and the present invention has excellent affinity for sebum. The external composition can be suitably used for such men with a large amount of sebum secretion. Further, since it is known that the amount of sebum secreted is higher in younger people, the external composition of the present invention is preferably used for such young people. One of the situations in which the external composition of the present invention is preferably used is, but is not limited to, application to a person suffering from juvenile alopecia. Juvenile alopecia is a type of alopecia that is known to develop from teens at the earliest, but the amount of sebum secreted in the scalp of such a relatively young age group (generally in the teens to 30s) is high. Many hair follicles often have sebum. According to the present invention, it becomes easy for the active ingredient to reach the site of action even for such juvenile alopecia, so that it is possible to easily exert the intended effect.

(2. Method for improving sebum affinity of external composition)
As described above, the component (A) and the component (B) are used to set the content of the component (B) within a specific range and adjust the mixed IOB value of the component (A) and the component (B). Therefore, it has been confirmed that a solubilized external composition having excellent sebum affinity can be prepared.
Therefore, from yet another point of view, the present invention comprises (A) a surfactant having a single hydrophobic moiety having a linear structure and an HLB value of 15 or more, and (B) lower alcohols and monoterpenes. At least one selected from the above group is used so that the total amount of the component (B) is 35% by weight or less with respect to the entire composition, and the mixed IOB value of the components (A) and (B) is set. Also provided is a method for improving the sebaceous affinity of an external composition, which comprises preparing a solubilized external composition so as to be 0.65 or less.
The types of the components (A) and (B) and their blending ratios in the above method, the types of other components that can be blended and their blending ratios, the uses of the external composition, etc. are described in the above "(1. External composition)". It is the same as that described in.

The following external compositions are disclosed in the present invention.

(A) A surfactant having a single hydrophobic moiety having a linear structure and an HLB value of 15 or more, and (B) at least one selected from the group consisting of lower alcohols and monoterpenes.
A solubilized external composition containing
A solubilized external composition in which the total amount of the component (B) is 35% by weight or less with respect to the entire composition, and the mixed IOB value of the component (A) and the component (B) is 0.65 or less.

The content of the component (A) can be 0.001 to 10% by weight based on the entire composition.

The content of the component (B) can be 0.0001 to 35% by weight based on the total composition.

The component (A) is composed of a group consisting of polyoxyethylene alkyl ether, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene polyoxypropylene alkyl ether, polyglycerin fatty acid ester, polyoxyethylene sorbit fatty acid ester, and polyethylene glycol fatty acid ester. It can be at least one selected.

The component (B) is ethanol, isopropanol, propylene glycol, dipropylene glycol, butylene glycol, glycerin, diglycerin, ethoxydiglycol, 1,2-pentanediol, ethylhexanediol, hexylene glycol, menthol, camphor, and eugenol. , Geraniol, Borneol, and Hinokithiol can be at least one selected from the group.

In the solubilized external composition of the present invention, the total amount of the component (B) is 35% by weight or less with respect to the entire composition, and the mixed IOB value of the components (A) and (B) is 0.65. The following compositions are exemplified, for example:
Composition containing ethanol, l-menthol, polyoxyethylene oleyl ether (20EO) and water;
Composition containing absolute ethanol, l-menthol, polyoxyethylene oleyl ether (20EO) and water;
Composition containing 1,3-butylene glycol, l-menthol, polyoxyethylene oleyl ether (20EO) and water;
Composition containing ethanol, 1,3-butylene glycol, l-menthol, polyoxyethylene oleyl ether (20EO) and water;
Composition containing dipropylene glycol, l-menthol, polyoxyethylene oleyl ether (20EO) and water;
Composition containing propylene glycol, l-menthol, polyoxyethylene oleyl ether (20EO), and water;
Composition containing l-menthol, polyoxyethylene oleyl ether (20EO) and water;
Composition containing ethanol, dipropylene glycol, glycerin, l-menthol, polyoxyethylene oleyl ether (20EO) and water;
Compositions containing ethanol, 1,3-butylene glycol, dipropylene glycol, glycerin, l-menthol, polyoxyethylene oleyl ether (20EO) and water;
Composition containing ethanol, l-menthol, polyoxyethylene coconut oil fatty acid sorbitan (20EO) and water;
Composition containing absolute ethanol, l-menthol, polyoxyethylene coconut oil fatty acid sorbitan (20EO) and water;
Composition containing 1,3-butylene glycol, l-menthol, polyoxyethylene coconut oil fatty acid sorbitan (20EO) and water;
Composition containing ethanol, 1,3-butylene glycol, l-menthol, polyoxyethylene coconut oil fatty acid sorbitan (20EO) and water;
Composition containing dipropylene glycol, l-menthol, polyoxyethylene coconut oil fatty acid sorbitan (20EO) and water;
Composition containing propylene glycol, l-menthol, polyoxyethylene coconut oil fatty acid sorbitan (20EO), and water;
Composition containing l-menthol, polyoxyethylene coconut oil fatty acid sorbitan (20EO) and water;
Composition containing ethanol, dipropylene glycol, glycerin, l-menthol, polyoxyethylene coconut oil fatty acid sorbitan (20EO) and water;
Composition containing ethanol, 1,3-butylene glycol, dipropylene glycol, glycerin, l-menthol, polyoxyethylene coconut oil fatty acid sorbitan (20EO) and water;
Composition containing ethanol, dl-camphor, polyoxyethylene oleyl ether (20EO) and water;
Composition containing absolute ethanol, dl-camphor, polyoxyethylene oleyl ether (20EO) and water;
Composition containing 1,3-butylene glycol, dl-camphor, polyoxyethylene oleyl ether (20EO) and water;
Composition containing ethanol, 1,3-butylene glycol, dl-camphor, polyoxyethylene oleyl ether (20EO) and water;
Composition containing dipropylene glycol, dl-camphor, polyoxyethylene oleyl ether (20EO) and water;
Composition containing propylene glycol, dl-camphor, polyoxyethylene oleyl ether (20EO), and water;
Composition containing dl-camphor, polyoxyethylene oleyl ether (20EO) and water;
Composition containing ethanol, dipropylene glycol, glycerin, dl-camphor, polyoxyethylene oleyl ether (20EO) and water;
Composition containing ethanol, 1,3-butylene glycol, dipropylene glycol, glycerin, dl-camphor, polyoxyethylene oleyl ether (20EO) and water;
Composition containing ethanol, dl-camphor, polyoxyethylene palm oil fatty acid sorbitan (20EO) and water;
Composition containing absolute ethanol, dl-camphor, polyoxyethylene palm oil fatty acid sorbitan (20EO) and water;
Composition containing 1,3-butylene glycol, dl-camphor, polyoxyethylene palm oil fatty acid sorbitan (20EO) and water;
Composition containing ethanol, 1,3-butylene glycol, dl-camphor, polyoxyethylene palm oil fatty acid sorbitan (20EO) and water;
Composition containing dipropylene glycol, dl-camphor, polyoxyethylene palm oil fatty acid sorbitan (20EO) and water;
Composition containing propylene glycol, dl-camphor, polyoxyethylene palm oil fatty acid sorbitan (20EO), and water;
Composition containing dl-camphor, polyoxyethylene palm oil fatty acid sorbitan (20EO) and water;
Composition containing ethanol, dipropylene glycol, glycerin, dl-camphor, polyoxyethylene palm oil fatty acid sorbitan (20EO) and water;
Composition containing ethanol, 1,3-butylene glycol, dipropylene glycol, glycerin, dl-camphor, polyoxyethylene palm oil fatty acid sorbitan (20EO) and water;
Composition containing ethanol, l-menthol, dl-camphor, polyoxyethylene oleyl ether (20EO) and water;
Composition containing absolute ethanol, l-menthol, dl-camphor, polyoxyethylene oleyl ether (20EO) and water;
Composition containing 1,3-butylene glycol, l-menthol, dl-camphor, polyoxyethylene oleyl ether (20EO) and water;
Composition containing ethanol, 1,3-butylene glycol, l-menthol, dl-camphor, polyoxyethylene oleyl ether (20EO) and water;
Composition containing dipropylene glycol, l-menthol, dl-camphor, polyoxyethylene oleyl ether (20EO) and water;
Compositions containing propylene glycol, l-menthol, dl-camphor, polyoxyethylene oleyl ether (20EO), and water;
Composition containing l-menthol, dl-camphor, polyoxyethylene oleyl ether (20EO) and water;
Composition containing ethanol, dipropylene glycol, glycerin, l-menthol, dl-camphor, polyoxyethylene oleyl ether (20EO) and water;
Compositions containing ethanol, 1,3-butylene glycol, dipropylene glycol, glycerin, l-menthol, dl-camphor, polyoxyethylene oleyl ether (20EO) and water;
Composition containing ethanol, l-menthol, dl-camphor, polyoxyethylene palm oil fatty acid sorbitan (20EO) and water;
Composition containing absolute ethanol, l-menthol, dl-camphor, polyoxyethylene palm oil fatty acid sorbitan (20EO) and water;
Composition containing 1,3-butylene glycol, l-menthol, dl-camphor, polyoxyethylene palm oil fatty acid sorbitan (20EO) and water;
Composition containing ethanol, 1,3-butylene glycol, l-menthol, dl-camphor, polyoxyethylene palm oil fatty acid sorbitan (20EO) and water;
Composition containing dipropylene glycol, l-menthol, dl-camphor, polyoxyethylene palm oil fatty acid sorbitan (20EO) and water;
Composition containing propylene glycol, l-menthol, dl-camphor, polyoxyethylene palm oil fatty acid sorbitan (20EO), and water;
Composition containing l-menthol, dl-camphor, polyoxyethylene palm oil fatty acid sorbitan (20EO) and water;
Compositions containing ethanol, dipropylene glycol, glycerin, l-menthol, dl-camphor, polyoxyethylene palm oil fatty acid sorbitan (20EO) and water; or ethanol, 1,3-butylene glycol, dipropylene glycol , Glycerin, l-menthol, dl-camphor, polyoxyethylene palm oil fatty acid sorbitan (20EO) and water.

The solubilized topical composition is preferably used for the scalp. Alternatively, it is used for hair growth or hair growth. The solubilized external composition is preferably used, for example, for the treatment and / or prevention of juvenile alopecia.

The solubilized external composition of the present invention preferably further contains a water-soluble hair-growth component and / or hair-growth component. Such water-soluble hair-growth and / or hair-growth components can be 0.00001 to 50% by weight based on the total composition.

The water-soluble hair-growth component and / or hair-nourishing component includes dipotassium glycyrrhizinate, allantin, pantothenyl ethyl ether, pantenol, pantothenic acid, biotin, nicotinic acid and its derivatives, pyridoxin hydrochloride, carrot extract, senburi extract, and crackle extract. , Shokyo tincture, Hiogi extract, Ogon extract, Tounin extract, Sansha extract, Biwa leaf extract, Confrey extract, Chamomile extract, Zenia oyster extract, Bukuryo extract, Togarashi tincture, Ousei extract, Kagikazura extract, Oazami extract, Henna extract, Kanzo extract, Kashu Extract, Chixetsu carrot extract, Senburi extract, Perilla extract, Hikiokoshi extract, Button extract, Shinano extract, Epine extract, Clara extract, Kujin extract, Shokyo extract, Quachalarate extract, Sophora extract, Amacha extract, Placenta extract, Wine yeast extract, It can be at least one selected from the group consisting of caffeine and its hydrate, and fucoidan.

The present invention is also selected from the group consisting of (A) a surfactant having a single hydrophobic moiety having a linear structure and an HLB value of 15 or more, and (B) a lower alcohol and a monoterpene. At least one of them is used so that the total amount of the component (B) is 35% by weight or less with respect to the entire composition, and the mixed IOB value of the components (A) and (B) is 0.65 or less. As described above, a method for improving the sebaceous affinity of the external composition, which comprises preparing a solubilized external composition, is disclosed.

In the method for improving the sebaceous affinity of the external composition, the component (A) is a polyoxyethylene alkyl ether, a polyoxyethylene sorbitan fatty acid ester, a polyoxyethylene polyoxypropylene alkyl ether, a polyglycerin fatty acid ester, or a polyoxy. It may be at least one selected from the group consisting of ethylene sorbit fatty acid ester and polyethylene glycol fatty acid ester.

In the method for improving the sebaceous affinity of the external composition, the component (B) is ethanol, isopropanol, propylene glycol, dipropylene glycol, butylene glycol, glycerin, diglycerin, ethoxydiglycol, 1,2-pentanediol. , Ethylhexanediol, hexylene glycol, menthol, camphor, eugenol, geraniol, borneol, and hinokithiol.

In the method for improving the sebum affinity of the external composition, the solubilized external composition is preferably used for the scalp. Alternatively, it is used for hair growth or hair growth. The solubilized external composition is preferably used, for example, for the treatment and / or prevention of juvenile alopecia.

In the method for improving the sebum affinity of the external composition, the solubilized external composition preferably further contains a water-soluble hair-growth component and / or hair-growth component.

In the method for improving the sebaceous affinity of the external composition, the water-soluble hair-growth component and / or hair-growth component includes dipotassium glycyrrhizinate, allantin, pantothenyl ethyl ether, pantenol, pantothenic acid, biotin, nicotinic acid and Its derivatives, pyridoxin hydrochloride, carrot extract, senburi extract, crackle extract, ginger extract, ginger extract, tounin extract, sansha extract, biwa leaf extract, comfrey extract, chamomile extract, zegna oyster extract, bukuryo extract, togarashi tincture, Osei extract, Kagikazura extract, Oazami extract, Henna extract, Kanzo extract, Kashu extract, Chikusetsu carrot extract, Senburi extract, Shiso extract, Hikiokoshi extract, Button extract, Shinano extract, Epine extract, Clara extract, Kujin extract, Shokyo extract, Kuachararate extract , Sophora extract, Amacha extract, placenta extract, wine yeast extract, caffeine and its hydrate, and at least one selected from the group consisting of fucoidan.

The present invention also discloses the use of the following external compositions for the production of compositions having excellent sebum affinity. The present invention also discloses the use of the following external compositions for the production of compositions for application to skin and / or hair with high sebum secretion. The present invention further discloses the use of the following external compositions for the production of hair growth agents or hair growth agents. Alternatively, the present invention discloses the use of the following external compositions for the production of scalp preparations. Alternatively, the present invention discloses the use of the following topical compositions for the manufacture of therapeutic and / or prophylactic agents for juvenile alopecia.

That is, the external composition for the above use is
(A) A surfactant having a single hydrophobic moiety having a linear structure and an HLB value of 15 or more, and (B) at least one selected from the group consisting of lower alcohols and monoterpenes.
A solubilized external composition containing
A solubilized external composition in which the total amount of the component (B) is 35% by weight or less with respect to the entire composition, and the mixed IOB value of the component (A) and the component (B) is 0.65 or less. is there.

The component (A) is composed of a group consisting of polyoxyethylene alkyl ether, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene polyoxypropylene alkyl ether, polyglycerin fatty acid ester, polyoxyethylene sorbit fatty acid ester, and polyethylene glycol fatty acid ester. It can be at least one selected.

The component (B) is ethanol, isopropanol, propylene glycol, dipropylene glycol, butylene glycol, glycerin, diglycerin, ethoxydiglycol, 1,2-pentanediol, ethylhexanediol, hexylene glycol, menthol, camphor, and eugenol. , Geraniol, Borneol, and Hinokithiol can be at least one selected from the group.

The external composition for the above use preferably further contains a water-soluble hair-growth component and / or a hair-growth component.

The water-soluble hair-growth component and / or hair-growth component includes dipotassium glycyrrhizinate, allantin, pantothenyl ethyl ether, pantenol, pantothenic acid, biotin, nicotinic acid and its derivatives, pyridoxin hydrochloride, carrot extract, senburi extract, and crackle extract. , Shokyo tincture, Hiogi extract, Ogon extract, Tounin extract, Sansha extract, Biwa leaf extract, Confrey extract, Chamomile extract, Zenia oyster extract, Bukuryo extract, Togarashi tincture, Ousei extract, Kagikazura extract, Oazami extract, Henna extract, Kanzo extract, Kashu Extract, Chixetsu carrot extract, Senburi extract, Perilla extract, Hikiokoshi extract, Button extract, Shinano extract, Epine extract, Clara extract, Kujin extract, Shokyo extract, Quachalarate extract, Sophora extract, Amacha extract, Placenta extract, Wine yeast extract, It can be at least one selected from the group consisting of caffeine and its hydrate, and fucoidan.

Hereinafter, the present invention will be described in detail based on examples, but the present invention is not limited to these examples.

<Test Example 1: Evaluation of sebum affinity>
In this test example, the affinity with artificial sebum was evaluated.
First, solubilized external compositions (Examples 1 to 11 and Comparative Examples 1 to 14) shown in Tables 2 to 5 below were prepared. Specifically, purified water was placed in a beaker, and other components were added and dissolved while stirring with a stirrer. Separately, artificial sebum colored with a pigment (Zudan Black B) was prepared at the blending ratios shown in Table 1 below. To extract this artificial sebum with hexane, prepare an artificial sebum hexane solution with a concentration of 500 mg / ml, add 150 μL of the solution to a 24-well well plate (Corning Incorporated), and then allow it to stand at 50 ° C. for 15 minutes. Hexane was evaporated by allowing it to stand and allowing it to stand at room temperature for 15 minutes to return to room temperature. Then, 2 ml of each sample was added to each well containing the colored artificial sebum after hexane extraction, and the mixture was shaken at 300 rpm for 1.5 hours using a shaker (Shaking Incubator SI-300, AS ONE Corporation). Then, the supernatant was removed while washing with distilled water. The colored artificial sebum remaining after removing the supernatant is extracted again with 5 ml of hexane, 200 μL of the extraction solvent is added to a 96-well well plate (IWAKI), and then a microplate reader (VersaMax ^TM , Molecular Device) is used. , The absorbance at 565 nm, where Zudan Black shows the absorbance, was measured. Separately, the absorbance of the colored artificial sebum that had been subjected to the same treatment as above without adding the test substance (solubilized external composition) was also measured at 565 nm and used as a control. From the absorbances measured for each, the ratio of the amount of sebum removed by adding the test subject to the control was calculated based on the following formula (I), and this was defined as the sebum affinity rate (%).
-Sebum affinity (%) = {(absorbance of control sebum-absorbance of sebum treated with each subject) / absorbance of control sebum} x 100 ... Formula (I)

The results are also shown in the bottom column of Tables 2-5 below. For reference, Tables 2 to 5 also show the mixed IOB values calculated from the respective IOB values and blending amounts of the surfactant, lower alcohol and monoterpene in each external composition.

Here, the PEG-50 glyceryl isostearate used in Comparative Examples 1 to 3 is a known surfactant having a single hydrophobic portion but a branched structure rather than a linear structure and an HLB value of 16. is there. The polyoxyethylene hydrogenated castor oil 100 used in Comparative Examples 4 to 6 is a known surfactant having a linear structure but having a plurality of hydrophobic portions instead of a single one and having an HLB value of 16.5. .. The polyoxyethylene cetyl ethers (6EO) used in Comparative Examples 11 to 13 are known surfactants having a single hydrophobic moiety having a linear structure but having an HLB value of 10.5. is there. In Comparative Examples 7 to 10 and 14, a surfactant having a single hydrophobic portion having a linear structure and having an HLB value of 15 or more (polyoxyethylene oleyl ether (20EO): HLB17). , And polyoxyethylene palm oil fatty acid sorbitan (20EO): HLB16.9), but the mixed IOB value specified by the type and amount of surfactant, lower alcohol and / or monoterpene is 0.65. A higher external composition.

As is clear from the results shown in each of the above tables, a surfactant having a branched structure in the hydrophobic portion (Comparative Examples 1 to 3), a surfactant having a plurality of hydrophobic portions (Comparative Examples 4 to 6), or When a surfactant having an HLB value of less than 15 (Comparative Examples 11 to 13) is used, even if the mixed IOB value calculated from the surfactant, the lower alcohol and the monoterpene is adjusted, the sebum affinity It turns out that does not improve. Further, even when a surfactant having a single hydrophobic portion having a linear structure and an HLB value of 15 or more is used, if the mixed IOB value exceeds 0.65, sebum It was found that the affinity did not improve (Comparative Examples 7-10 and 14).

On the other hand, quite unexpectedly, a polyoxyethylene alkyl ether-based surfactant having a single hydrophobic moiety having a linear structure and an HLB value of 15 or more is used, and the mixed IOB value is It was revealed that when the composition for external use adjusted to be 0.65 or less was used, it showed a very high sebum affinity (Examples 1 to 10). Similarly, a polyoxyethylene sorbitan fatty acid ester-based surfactant having a single hydrophobic portion having a linear structure and an HLB value of 15 or more is used, and the mixed IOB value is set to 0.65 or less. A high sebum affinity rate was confirmed even when adjusted (Example 11). Therefore, it can be seen that the same effect can be obtained by adjusting the mixed IOB value using a surfactant having a single hydrophobic portion having a linear structure and an HLB of 15 or more. That is, from the results of this test example, in order to enhance the sebum affinity, the structure and HLB value of the surfactant to be used are selected, and the mixed IOB calculated from the surfactant, lower alcohol and / or monoterpene is selected. It was recognized that it was important to adjust the values.

<Test Example 2: Evaluation of sebum affinity>
The external compositions of each solubilization system (Examples 12 to 18) shown in Table 6 below were also evaluated for sebum affinity in the same manner as in the method described in Test Example 1 above.

The results of this test are also shown in the bottom column of Table 6 above. In addition, the mixed IOB value calculated from each of the surfactant, lower alcohol and monoterpene in each of the above external composition is also shown in the same table as a reference value. The polyoxyethylene oleyl ether (20EO) used in this test example has a single hydrophobic moiety having a linear structure and is a surfactant of HLB17. As is clear from the above results, similar to the results of Test Example 1, according to the present invention, (A) with a surfactant having a specific structure and HLB value, and (B) a lower alcohol and / or monoterpene. At least one is blended so that the total amount is 35% by weight or less, and the mixed IOB value calculated from each IOB value and content of the components (A) and (B) is 0.65 or less. It was confirmed that by adjusting, a high sebum affinity effect can be exhibited.

<Test Example 3: Hair follicle permeability evaluation>
In order to confirm whether or not the external composition of the present invention showing high sebum affinity in Test Examples 1 and 2 has excellent permeability to hair follicles containing sebum, Table 7 below shows. The external composition of the solubilization system shown (Example 19 and Comparative Examples 15 to 18) was tested in an evaluation system using a hair follicle as a model.

Specifically, as a hair follicle permeability evaluation, a permeability test using Franzcel was performed with reference to the method described in FRAGRANCE JOURNAL, No.329,17-21,2007. First, inject 5 mL of PBS solution into Franzcel (PermeGear, stationary jacket-flat jacket-clear-9 mm, 5 mL, permeation area 0.64 cm2) and silicon between Franzcel and the glass donor with rub. A film (thickness 75 μm) was sandwiched and fixed with a clip. An artificial sebum colored with a pigment (Zudan Black B) having the same composition as that prepared in Test Example 1 was prepared, and an artificial sebum hexane solution having a concentration of 500 mg / mL was prepared. After adding 150 μL of the prepared sebum solution to the glass donor, the mixture was allowed to stand at 50 ° C. for 15 minutes and then allowed to stand at room temperature for 15 minutes to return to room temperature to evaporate hexane. Each of the non-test test compositions shown in Table 7 above, prepared to contain uranin as a model of a functional component intended to act on hair follicles on colored artificial sebum after hexane extraction (Example 19 and comparison). Examples 15 to 18) were added in an amount of 500 μL each, and the mixture was shaken at 300 rpm for 24 hours using a shaker (Shaking Incubator SI-300, AS ONE Corporation). 200 μL of the sample 20 hours and 24 hours after the start of shaking was collected, added to a 96-well well plate (IWAKI), and excited using a fluorescent microplate reader Fluoroskan Ascent, Thermo Fisher Scientific). The wavelength of 485 nm and the fluorescence wavelength of 538 nm were measured, and the amount of uranin permeated through the artificial sebum and reached the PBS solution was calculated. The significant difference test was a Student's t-test.

The test results are shown in FIG. As is clear from the results shown in FIG. 1, when the test composition (Comparative Example 15) containing no surfactant is added, uranin hardly permeates the artificial sebum and does not reach the PBS solution. Further, although the HLB value is 16.5, even when a surfactant (polyoxyethylene cured castor oil 100) having a plurality of hydrophobic portions is used, sebum permeation is similar to the result of Test Example 1 above. The amount was found to be low (Comparative Examples 17, 18). Further, even if a surfactant having a single hydrophobic moiety having a linear structure and an HLB of 15 or more is blended, a mixture calculated based on the surfactant, lower alcohol and / or monoterpene. When the IOB value exceeded 0.65, the sebum permeation amount was found to be inferior (Comparative Example 16). On the other hand, as expected from the results of Test Example 1 and Test Example 2, a surfactant having a specific structure and HLB value specified in the present invention was used, and the mixed IOB value was adjusted to 0.65 or less. The external composition of the present invention showed a very high sebum permeation amount (Example 19). The sebum permeation amount shown in Example 19 was statistically significantly higher than that of Comparative Example 18. Therefore, it has been clarified that the present invention can provide an external composition having an excellent sebum affinity.

<Test Example 4: Hair follicle permeability evaluation>
Similar to Test Example 3 above, a permeability test using a hair follicle using Franzcel was performed, and the permeability of dipotassium glycyrrhizinate as a representative example of a water-soluble hair-growth component and a hair-growth component was evaluated.

First, external compositions (Example 20 and Comparative Examples 19 to 22) of each solubilization system shown in Table 8 above were prepared in the same manner as in Example 1. Next, 5 mL of ultrapure water was injected into a reservoir of Franzcel (PermeGear, static type with jacket-flat jacket-clear-9 mm, 5 mL, permeation area 0.64 square cm), and Franzcel and a glass donor with a rub were used. A silicon film (thickness 75 μm) was sandwiched between them and fixed with a clip. An artificial sebum colored with a pigment (Zudan Black B) having the same composition as that prepared in Test Example 1 was prepared, and an artificial sebum hexane solution having a concentration of 500 mg / mL was prepared. After adding 150 μL of the prepared sebum solution to the glass donor, the mixture was allowed to stand at 50 ° C. for 15 minutes and then allowed to stand at room temperature for 15 minutes to return to room temperature to evaporate hexane. On the colored artificial sebum after hexane extraction, 500 μL of each of the non-test test compositions of Example 20 or Comparative Examples 19 to 22 containing 0.5% by weight of dipotassium glycyrrhizinate was added, and a shaker (Shaking Incubator SI-) was added. It was shaken at 300 rpm for 24 hours using 300, AS ONE Corporation). Twenty-four hours after the start of shaking, 200 μL of the reservoir sample was collected in a glass vial and analyzed by a high performance liquid chromatograph mass spectrometer (LCMS) to permeate the artificial sebum and reach the ultrapure water in the reservoir. The amount of dipotassium glycyrrhizinate was calculated. The measurement conditions for LCMS are as follows.
(LCMS measurement conditions)
・ Equipment used: AB SIX QTRAP (registered trademark)
-Measurement ionization method: Electrospray method (ESI)
-Column used: Inertsil ODS3 5um, 2.1 x 50 mm
・ Analysis time: 30min
-Solvent: 0.05% TFA MeCN and 0.05% TFA MiliQ water
・ Dissolution condition: 65% MeCN (15min) → 100% MeCN (5min) → 65% MeCN (10min)

The result is shown in FIG. As is clear from the results shown in FIG. 2, a surfactant having a single hydrophobic portion having a linear structure and an HLB value of 15 or more was used, and the mixed IOB value was adjusted to 0.65 or less. It was confirmed that the external composition of the present invention exhibited a very high sebum permeability as compared with the external composition of the comparative example. From the above results, by preparing dipotassium glycyrrhizinate, which is well known as a water-soluble hair-growth component and a hair-growth component, as an external composition according to the present invention, it can effectively penetrate into hair follicles filled with sebum. It can be seen that it can reach the deep part of the hair follicle.

<Test Example 5: Evaluation of hair follicle permeability>
By the method using LCMS which is substantially the same as that of Test Example 4, the sebum permeability of pantothenyl ethyl ether as a representative example of the water-soluble hair-growth component and hair-growth component was also obtained from the solubilization system shown in Table 9 below. External compositions (Example 21 and Comparative Examples 23 to 26) were prepared and evaluated.

The measurement conditions of the high performance liquid chromatograph mass spectrometer (LCMS) of pantothenyl ethyl ether used in this test example are as follows.
(LCMS measurement conditions)
・ Equipment used: AB SIX QTRAP (registered trademark)
-Measurement ionization method: Electrospray method (ESI)
-Column used: Inertsil ODS3 5um, 2.1 x 50 mm
・ Analysis time: 30min
-Solvent: 0.05% TFA MeCN and 0.05% TFA MiliQ water
・ Elution conditions: 90% MeCN (0min) → 80% MeCN (15min) → 100% MeCN (20min) → 100% Water (30min)

The result of the transparency evaluation is shown in FIG. As is clear from the results shown in FIG. 3, even when pantothenyl ethyl ether is used as one of the water-soluble hair-growth components and hair-growth components that are desired to allow sebum to permeate, the specification specified in the present invention is specified. The external composition of Example 21 using a surfactant having the above structure and HLB value and having a mixed IOB value adjusted to 0.65 or less can exhibit high sebum permeability and is a hair follicle clogged with sebum. It was confirmed that it could allow the pantothenyl ethyl ether to reach deep into the area.

<Test Example 6: Hair follicle permeability evaluation>
By the same method using LCMS as in Test Examples 4 and 5, the solubilized external compositions shown in Table 10 below were used to determine the permeability of dipotassium glycyrrhizinate and pantothenyl ethyl ether (Examples 22 to 23). And Comparative Examples 27 to 28) were prepared and further evaluated. The measurement conditions of LCMS used in this test example were the same measurement conditions as in Test Example 4 for dipotassium glycyrrhizinate and the same measurement conditions as in Test Example 5 for pantothenyl ethyl ether.

The results are shown in FIG. 4 (dipotassium glycyrrhizinate) and FIG. 5 (pantothenyl ethyl ether). As is clear from the results shown in FIGS. 4 and 5, an interface having a specific structure and HLB value specified in the present invention even when the content of dipotassium glycyrrhizinate or pantothenyl ethyl ether is low. It was confirmed that the external composition (Examples 22 and 23) using the activator and having the mixed IOB value adjusted to 0.65 or less showed higher sebum permeability than the comparative example.

An example of the formulation of the present invention is shown below. Formulation Examples 1 to 4 are hair growth agents, and Formulation Examples 5 to 6 are examples of lotion. These are prepared according to conventional methods.

Claims (7)

(A) A surfactant having a single hydrophobic moiety having a linear structure and an HLB value of 15 or more; and (B) containing at least one selected from the group consisting of lower alcohols and monoterpenes. And
(B) A solubilized external composition having a component content of 0.0001 to 35% by weight.
The mixed IOB value of the component (A) and the component (B) is 0.65 or less.
(B) Contains at least ethanol as a component
A solubilized external composition for use on the scalp, which comprises at least polyoxyethylene oleyl ether as (A). The solubilized external composition according to claim 1, wherein the content of the component (A) is 0.01 to 5% by weight. (A) A surfactant having a single hydrophobic moiety having a linear structure and an HLB value of 15 or more; and (B) containing at least one selected from the group consisting of lower alcohols and monoterpenes. And
(B) A solubilized external composition having a component content of 0.0001 to 12.7% by weight.
The mixed IOB value of the component (A) and the component (B) is 0.65 or less.
(B) Containing at least 0.0001 or more and less than 5% by mass of ethanol as a component,
As the (A), at least polyoxyethylene oleyl ether is contained.
A solubilized external composition. The solubilized external composition according to claims 1 to 3, further containing at least one selected from the group consisting of 1,3-butylene glycol, propylene glycol, and dipropylene glycol as the lower alcohol. .. Further, as a water-soluble hair-growth component and / or hair-growth component, dipotassium glycyrrhizinate, allantin, pantothenyl ethyl ether, pantenol, pantothenic acid, biotin, nicotinic acid and its derivatives, pyridoxin hydrochloride, carrot extract, senburi extract, crackle Extract, ginger extract, ginger extract, ginger extract, tounin extract, sansha extract, biwa leaf extract, comfrey extract, chamomile extract, zegna oyster extract, bukuryo extract, ginger tincture, pearl oyster extract, sardine extract, citrus extract, Kashu extract, Chikusetsu carrot extract, Senburi extract, Perilla extract, Hikiokoshi extract, Button extract, Shinano extract, Epine extract, Clara extract, Kujin extract, Shokyo extract, Quachalarate extract, Sophora extract, Amacha extract, Placenta extract, Wine yeast extract The solubilizing system external composition according to claims 1 to 4, which contains at least one selected from the group consisting of, caffeine and its hydrate, and fucoidan. (A) A surfactant having a single hydrophobic moiety having a linear structure and an HLB value of 15 or more, which is a polyoxyethylene alkyl ether, a polyoxyethylene sorbitan fatty acid ester, or a polyoxyethylene polyoxy. At least one surfactant selected from the group consisting of propylene alkyl ethers, polyglycerin fatty acid esters, and polyoxyethylene sorbitol fatty acid esters; and (B) at least one selected from the group consisting of lower alcohols and monoterpenes. A solubilized external composition containing,
The total amount of the component (B) is 0.0001 to 35% by weight based on the whole composition, and the mixed IOB value of the component (A) and the component (B) is 0.65 or less.
A method for promoting hair follicle permeability in the scalp of a water-soluble functional component coexisting with the external composition. (A) A surfactant having a single hydrophobic moiety having a linear structure and an HLB value of 15 or more, which is a polyoxyethylene alkyl ether, polyoxyethylene sorbitan fatty acid ester, or polyoxyethylene polyoxy. External composition of solubilization system containing at least one surfactant selected from the group consisting of propylene alkyl ether, polyglycerin fatty acid ester, and polyoxyethylene sorbit fatty acid ester; and (B) lower alcohol and monoterpene. It ’s a thing,
The content of the component (A) is 0.01 to 5% by weight based on the entire composition.
The external composition is obtained by setting the total amount of the component (B) to 0.0001 to 35% by weight based on the entire composition and setting the mixed IOB value of the component (A) and the component (B) to 0.65 or less. A method of promoting skin permeability of a water-soluble functional ingredient that coexists with an object.

Images