JP2016190816A - External composition - Google Patents

Abstract

Disclosed is a composition for external use that is uniform and highly stable despite containing a high concentration of ceramides.
The present invention relates to an external use comprising (A) ceramides 2.5 to 6% by weight, (B) phytosterol derivatives 15 to 30% by weight, (C) fatty oil, and (D) dextrin fatty acid ester. Relates to the composition. Furthermore, it is preferable to contain (E) a higher alcohol.
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Description

The present invention relates to an external composition containing ceramides at a high concentration, and particularly to a liquid or semi-solid external composition.

Ceramides are intercellular lipids present in human skin (stratum corneum), and it is known that ceramide in the stratum corneum decreases with aging and the like. Along with this, the skin is dried to cause wrinkles and the like, and due to the lowered barrier function, allergens and the like are invaded, causing inflammation and itching. For such a symptom, it is effective to apply ceramides externally, and in that case, penetration into the target site can be achieved by bringing the ceramides into a dissolved state. Moreover, since it has concentration dependency, it is preferably contained at a concentration as high as possible, and from the viewpoint of osmotic power, the properties of the preparation are preferably liquid to semi-solid.

However, ceramides are components that are difficult to dissolve in water and oil, and are difficult to be dissolved even at low concentrations. Various techniques have been proposed as methods for improving the solubility of ceramides, but there are problems such as lack of safety, and further improvements are desired. In addition, when ceramides are blended at a high concentration, the formulation tends to solidify and precipitate, and it is very difficult to keep it in a liquid to semi-solid state, transparent and endurable to use. Met. Moreover, even if it could be dissolved at a high concentration temporarily, ceramides may precipitate over time or solidify, and the stability was poor.

For example, Patent Document 1 proposes a composition containing a fatty acid triglyceride and a phytosterol derivative, and Patent Document 2 proposes a composition containing a polyglycerol fatty acid ester and a fatty acid monoglyceride. However, in the compositions specifically disclosed in these documents, the concentration of ceramides was low.

JP 2008-297301 A JP 2011-73992 A

An object of the present invention is to provide a uniform and highly stable composition for external use despite containing a high concentration of ceramides.

The inventors of the present invention have made extensive studies on increasing the concentration of ceramides, and, despite containing (A) ceramides at a high concentration of 2.5 to 6% by weight, (B) phytosterol derivatives 15 to 15%. It has been found that by blending 30% by weight, (C) fatty oil and (D) dextrin fatty acid ester, the external composition can be made into a liquid to semi-solid external composition without becoming solid. Furthermore, it has also been found that when (E) a higher alcohol is blended, it becomes a transparent composition excellent in stability without causing precipitation, separation, solidification, etc., and the present invention has been completed.

That is, the present invention provides an external composition comprising (A) ceramides 2.5 to 6% by weight, (B) phytosterol derivative 15 to 30% by weight, (C) fatty oil, and (D) dextrin fatty acid ester. About.

(B) phytosterol derivatives are dimer linoleic acid (phytosteryl / isostearyl / cetyl / stearyl / behenyl), dimer linoleic acid di (isostearyl / phytosteryl), lauroyl glutamate (octyldodecyl / phytosteryl / behenyl), and One or more selected from the group consisting of dilauroyl glutamate (phytosteryl / octyldodecyl) is preferable.

Furthermore, it is preferable to contain (E) a higher alcohol.

(C) It is preferable to contain 58 to 79.9% by weight of fatty oil, (D) 0.1 to 1% by weight of dextrin fatty acid ester, and (E) 2.5 to 6% by weight of higher alcohol.

The external composition is preferably liquid or semi-solid.

According to the present invention, since (B) a phytosterol derivative, (C) fatty oil, and (D) a dextrin fatty acid ester are contained, (A) ceramides can be contained at a high concentration. In spite of being contained in, it can provide a uniform and highly stable composition for external use.

The composition for external use of the present invention contains (A) ceramides 2.5 to 6% by weight, (B) phytosterol derivatives 15 to 30% by weight, (C) fatty oil, and (D) dextrin fatty acid ester. It is characterized by.

(A) Ceramides are compounds that have a sphingosine or similar base of sphingosine such as phytosphingosine as a central skeleton, and are bonded to a fatty acid, α-hydroxy fatty acid or ω-hydroxy fatty acid having no OH by an amide bond It is. It is a component that constitutes intercellular lipid present in human skin (keratin), and is used externally for improving moisture retention and improving barrier function.

(A) The ceramides may be derived from synthetic or natural types, but natural or natural ceramides are preferred. Examples thereof include ceramide 1 (ceramide I), ceramide 2 (ceramide II), ceramide 3 (ceramide III), ceramide 4 (ceramide IV), ceramide 5 (ceramide V), and ceramide 6 (ceramide VI). Among these, ceramide 1, ceramide 2 and ceramide 3 are preferable in terms of effectiveness such as an anti-wrinkle effect and moisture retention. These ceramides can be used alone or in combination of two or more.

(A) Although content of ceramides is 2.5 to 6 weight% in an external composition, 2.5 to 5 weight% is preferable. If the amount is less than 2.5% by weight, the user's satisfaction tends to be insufficient. If the amount exceeds 6% by weight, the composition may not be liquid or semi-solid.

(B) A phytosterol derivative is a biologically similar component and has an effect of improving skin roughness. For example, dimer dilinoleic acid (phytosteryl / isostearyl / cetyl / stearyl / behenyl), dimer dilinoleic acid di (isostearyl / phytosteryl), lauroyl glutamate di (octyldodecyl / phytosteryl / behenyl), lauroyl glutamate di (phytosteryl / octyl) Dodecyl) and the like. These derivatives can be used alone or in combination of two or more.

(B) Although content of a phytosterol derivative is 15-30 weight% in a composition for external use, 15-20 weight% is preferable. If it is less than 15% by weight, it tends to be a composition lacking in property stability, and if it exceeds 30% by weight, it may not be a liquid or semi-solid composition.

Further, the ratio of (B) phytosterol derivative to (A) ceramides may be within a range that can satisfy the range of the content of (A) ceramides and (B) phytosterol derivatives described above, Specifically, (B) phytosterol derivative is 2.5 to 12 parts by weight, more preferably 3 to 12 parts by weight, per 1 part by weight of (A) ceramides.

(C) Fat oil is oil that is liquid at room temperature among fats and oils. Examples include vegetable oils such as olive oil, macadamia nut oil, mountain tea flower oil, coconut oil, corn oil, sesame oil, jojoba oil, safflower oil, sunflower seed oil, hazelnut oil, yucha oil and the like. Of these, olive oil, macadamia nut oil, sunflower seed oil, hazelnut oil, yucha oil and the like are preferable from the viewpoint of the properties and feeling of use of the composition. These fatty oils can be used singly or in combination of two or more.

(C) 58-79.9 weight% is preferable in an external composition, and, as for content of a fatty oil, 63-79.9 weight% is more preferable. If it is less than 58% by weight, it may not be a liquid or semi-solid composition, and if it exceeds 79.9% by weight, it tends to be a composition lacking in property stability.

In addition, the ratio of (C) fatty oil to (A) ceramides may be within a range that can satisfy the range of the content of (A) ceramides and (C) fatty oil described above. Specifically, (C) fatty oil is 9 to 32 parts by weight, more preferably 11 to 32 parts by weight per part by weight of (A) ceramides.

(D) Dextrin fatty acid ester is an ester of dextrin and higher fatty acid, and its use as an emulsifier is known and has a function of imparting viscosity to liquid oil. Examples of (D) dextrin fatty acid ester include myristic dextrin, palmitic dextrin, (palmitic acid / ethylhexanoic acid) dextrin, and octanoic acid dextrin. Of these, dextrin myristate is preferable from the viewpoint of property stability. These dextrin fatty acid esters can be used alone or in combination of two or more.

In addition, the ratio of (D) dextrin fatty acid ester to (A) ceramide may be within a range that can satisfy the above-described content ranges of (A) ceramide and (D) dextrin fatty acid ester. However, specifically, (D) dextrin fatty acid ester is 0.01 to 0.4 part by weight, more preferably 0.08 to 0.2 part by weight per part by weight of (A) ceramide.

The content of (D) dextrin fatty acid ester is preferably 0.1 to 1% by weight, more preferably 0.1 to 0.5% by weight in the composition for external use. If the amount is less than 0.1% by weight, the composition is subjected to property stability. If the amount exceeds 1% by weight, the composition may not be liquid or semi-solid.

(E) The higher alcohol is generally an alcohol having 6 or more carbon atoms, and a transparent composition excellent in stability can be obtained by blending into the external composition of the present invention. What is a liquid property at normal temperature is desirable. Specific examples include isostearyl alcohol, oleyl alcohol, octyldodecanol, hexyldecanol, decyltetradecanol and the like. Among these, isostearyl alcohol is preferable from the viewpoint of the stability of the composition. These higher alcohols can be used alone or in combination of two or more.

(E) The content of the higher alcohol is preferably 2.5 to 6% by weight, more preferably 2.5 to 5% by weight in the composition for external use. If it is less than 2.5% by weight, the composition lacks property stability, and if it exceeds 6% by weight, the feeling of use tends to be lowered.

In addition, the ratio of (E) higher alcohol to (A) ceramides may be within a range that can satisfy the above-described content range of (A) ceramides and (E) higher alcohol. Specifically, (A) higher alcohol is 0.4 to 2.4 parts by weight, more preferably 0.5 to 2 parts by weight per part by weight of (A) ceramides.

The composition for external use of the present invention is preferably liquid or semi-solid in terms of penetrating power and ease of application. Examples of the liquid or semisolid external composition include gels and creams. In addition, since the composition for external use of the present invention has a high moisturizing effect, it should be applied to applications such as cosmetic liquids, anti-wrinkle liquids, moisturizers, skin oils, baby oils, tanning oils, packs, and nail oils. Can do.

The composition for external use of this invention may contain the component normally used in the said technical field in the range which does not impair the effect of this invention other than the component mentioned above. Examples of such components include antiseptics, bactericides, antibacterial agents, anti-inflammatory agents, wetting agents, excipients, fragrances, cooling agents, dyes, surfactants, pH adjusters, and the like.

Moreover, in the composition for external use of this invention, physiologically active components and pharmacologically active components other than ceramide can also be mix | blended with the external composition of this invention as needed in the range which does not impair the effect of this invention. Examples of such components include vitamins, amino acids and their polymers (peptides, proteins), polyphenols, plant extracts, royal jelly, proteins, carnitine, lactic acid bacteria, elastin, collagen, hyaluronic acid, and the like.

The composition for external use of the present invention is prepared by mixing the above-described components, and may be heated to, for example, 80 to 150 ° C. when mixing.

The present invention will be specifically described based on examples, but the present invention is not limited to these examples.

Examples 1-10 and Comparative Examples 1-8
Each component having a content shown in Table 1 was heated to about 100 ° C. to 120 ° C., and stirred, mixed, and cooled to prepare an external composition. About the obtained composition, the property of a formulation was evaluated on the basis of the following. Further, the sample was allowed to stand at 25 ° C. for 1 week, and the stability was evaluated based on the following criteria based on the occurrence of separation, precipitation (transparency) and solidification. The evaluation results for each item are shown in Table 1. The unit in Table 1 is “% by weight”. For ceramides 2 and 3 in Table 1, the following raw materials were used.
Ceramide 2: N-stearoyl dihydrosphingosine (trade name: CERAMIDE TIC-001 (manufactured by Takasago International Corporation))
Ceramide 3: N-stearoyl phytosphingosine (CERAMIDE III (Evonik Japan Co., Ltd.))

<Properties of formulation>
○: Liquid △: Semi-solid ×: Solid

<Stability>
○: No separation / precipitation / solidification ×: One or more of separation / precipitation / solidification occurred

As is apparent from Table 1, in the preparations for external use of Examples 1 to 10 containing 2.5 to 6% by weight of ceramides, 15 to 30% by weight of phytosterol derivatives, fatty oil and dextrin fatty acid ester in the preparation. When the composition became liquid or semi-solid and further contained higher alcohol, precipitation of ceramide, separation and solidification of the preparation could be prevented, and the properties and transparency could be maintained. In particular, when the content of the dextrin fatty acid ester was 0.1 to 0.5% by weight, a liquid composition was obtained (Examples 1, 4, 5, 7 to 10).

On the other hand, when ceramide is contained in the preparation in an amount of 2.5% by weight or more, the composition for external use of Comparative Examples 1 to 3 and 6 to 8 in which the phytosterol derivative is less than 15% by weight in the preparation and does not contain dextrin fatty acid ester In the composition for external use of Comparative Examples 4 and 5 containing a fatty acid ester having a similar function and use instead of the product or dextrin fatty acid ester, it does not become a liquid or semi-solid composition. Precipitation, separation of the formulation and solidification occurred.

Formulation Examples 1-3
Table 2 shows formulation examples of the composition for external use of the present invention. The unit in Table 2 is “% by weight”. The following raw materials were used for ceramide 1 in Table 2, and the same raw materials as in Table 1 were used for ceramides 2 and 3, respectively.
Ceramide 1: N- (27-stearoyloxyheptacosanoyl) phytosphingosine (trade name: CERAMIDE I (Evonik Japan Co., Ltd.))

The compositions for external use shown in these formulation examples also showed good stability.

The composition for external use of the present invention is liquid or semi-solid despite containing a high concentration of ceramides, so it has excellent permeability and good usability, and is a cosmetic liquid, anti-wrinkle liquid, It can be applied to various uses such as moisturizer, skin oil, baby oil, suntan oil, pack agent, nail oil.

Claims (5)

(A) Ceramides 2.5 to 6% by weight,
(B) 15-30% by weight of phytosterol derivative,
(C) fatty oil, and
(D) An external composition containing a dextrin fatty acid ester. (B) a phytosterol derivative is dimer linoleic acid (phytosteryl / isostearyl / cetyl / stearyl / behenyl), dimer linoleic acid di (isostearyl / phytosteryl), lauroyl glutamate di (octyldodecyl / phytosteryl / behenyl), and The composition for external use according to claim 1, wherein the composition is one or more selected from the group consisting of dilauroyl glutamate (phytosteryl / octyldodecyl). The composition for external use according to claim 1 or 2, further comprising (E) a higher alcohol. (C) 58-79.9 weight% of fatty oil, (D) 0.1-1 weight% of dextrin fatty acid ester, (E) 2.5-6 weight% of higher alcohol is contained. Composition for external use. The composition for external use according to any one of claims 1 to 4, which is liquid or semi-solid.