JP2020158493A - Water-in-oil type (w/o type) cream containing panthenol - Google Patents

Abstract

To obtain skin tissue restoration action, anti-inflammatory effect and moisture retaining action of panthenol by application in a shorter time than conventional one.SOLUTION: A composition obtained by incorporating panthenol into a water-in-oil type emulsion composition exhibits excellent moisture retaining effect by applying the composition on the skin. Further, when formed into a water-in-oil type emulsion composition, panthenol exhibits excellent moisture retaining effect when used together with a heparin analog used for the purpose of moisture retention or improvement in skin roughness and vitamin E.SELECTED DRAWING: None

Description

The present invention relates to an external application for skin containing panthenol, and more particularly to an external application for skin used for improving dry skin and rough skin.

Panthenol is a water-soluble provitamin, also called provitamin B5, which is converted to vitamin B5 (pantothenic acid) in the body, and is said to have skin tissue repairing, anti-inflammatory, and moisturizing effects. It is added to cosmetics such as milky lotion and cream for the purpose of improving rough skin caused by.

Panthenol is considered to be a highly safe ingredient with few reports of skin irritation or toxicity. Therefore, it has been blended in various ointments and creams (Patent Document 1 and Patent Document 2). However, its action was mild and had no immediate effect, and it was necessary to continue applying it daily for a long period of time to obtain the effect.

JP 2006-335676 JP 2011-231128

An object of the present invention is to obtain the skin tissue repairing effect, anti-inflammatory effect, and moisturizing effect of panthenol by application in a shorter period of time than before.

It has been found that panthenol is contained in a water-in-oil emulsified composition and applied to the skin to exhibit an excellent moisturizing effect in a short time.

Furthermore, it was found that panthenol exerts an excellent moisturizing effect when used in combination with a heparinoid and vitamin E used for moisturizing and improving rough skin when used as a water-in-oil emulsified composition. It was.

More specifically, the present application provides the following aspects in order to solve the above-mentioned problems:
[1]: Water-in-oil (W / O type) emulsified composition containing panthenol or a panthenol-related substance;
[2]: The water-in-oil (W / O type) emulsified composition according to [1], wherein the content of panthenol or a panthenol-related substance is 0.5 to 5.0% by mass;
[3]: The water in oil according to [1] or [2], wherein the panthenol-related substance is selected from the group consisting of pantothenyl ethyl ether, calcium pantothenate, sodium pantothenate, and acetyl panthenyl ethyl ether. Type (W / O type) emulsified composition;
[4]: The water-in-oil (W / O type) emulsified composition according to any one of [1] to [3], which contains a glycerin fatty acid ester as a lipophilic emulsifier;
[5]: The water-in-oil type (W / O type) according to any one of [1] to [4], which further contains heparinoids, vitamin Es, or heparinoids and vitamin Es. Emulsified composition;
[6]: Water-in-oil (W / O type) emulsification according to [5], wherein the content of heparinoids is 0.1 to 0.5% by mass, or the content of vitamin Es is 0.5 to 2.0% by mass. Composition;
[7]: The water-in-oil (W / O type) emulsified composition according to any one of [1] to [6] used for external application to the skin;
[8]: A coating agent for external use on the skin, which is a water-in-oil (W / O type) emulsifying composition according to any one of [1] to [6].

By incorporating panthenol in a water-in-oil emulsified composition and applying it to the skin, an excellent moisturizing effect can be exhibited in a short time. Furthermore, when a water-in-oil emulsified composition is used, panthenol can exert an excellent moisturizing effect even when used in combination with a heparinoid and vitamin E used for the purpose of moisturizing and improving rough skin. ..

FIG. 1 is a diagram showing that the moisturizing effect of panthenol can be effectively obtained by containing panthenol in a water-in-oil (W / O type) emulsified composition (cream). FIG. 2 shows that the moisturizing effect of panthenol can be effectively obtained by containing 0.5 to 4.0% by mass of panthenol in the water-in-oil (W / O type) emulsified composition (cream). It is a figure. Figure 3 shows the moisturizing effect of panthenol even when panthenol is contained in a water-in-oil (W / O type) emulsified composition (cream) in combination with polysulfated chondroitin sulfate and tocopherol acetate. It is a figure which shows that it can be obtained effectively.

The present inventors added panthenol (D-panthenol alcohol) or a panthenol-related substance to a water-in-oil (W / O type) emulsifying composition, and when applied to the skin, in a short time. The present invention has been completed by finding that it exhibits an excellent moisturizing effect.

Based on this finding, the present invention provides a water-in-oil (W / O type) emulsified composition containing panthenol or a panthenol-related substance as an active ingredient.

Panthenol is a water-soluble provitamin also called provitamin B5 that is converted to vitamin B5 (pantothenic acid) in the body, and is known to have a moisturizing effect, a tissue repair promoting effect, and an anti-inflammatory effect.

Panthenol-related substances are a group of derivative substances of panthenol having the same activity as panthenol in vivo, and include pantothenyl ethyl ether, calcium pantothenate, sodium pantothenate, acetyl panthenyl ethyl ether, and the like. Not limited to these.

The present invention is characterized in that panthenol or a panthenol-related substance is used as a water-in-oil (W / O type) emulsified composition. More specifically, the water-in-oil (W / O type) emulsified composition of the present invention is obtained by dispersing droplets of an aqueous component in which panthenol or a panthenol-related substance is dissolved in an oil component. Is.

In the present invention, in order to disperse pantenol or a pantenol-related substance in a hydrophilic (W / O type) emulsifying composition, it is necessary to disperse an aqueous component in an oil component. For this purpose, a surfactant having an HLB value (Hydrophilic-Lipophilic Balance) of about 3 to 8, more preferably about 3 to 6, is used as a lipophilic emulsifier. Examples of such lipophilic emulsifiers (lipophilic nonionic surfactants) include glycerin fatty acid esters, sorbitan monooleate, sorbitan sesquioleate, polyoxyethylene hydrogenated castor oil and the like. Examples of glycerin fatty acid esters include polyglyceryl monooleate, polyglyceryl monostearate, polyglyceryl monoisostearate, polyglyceryl pentaisostearate, polyglyceryl pentaoleate and the like. A method for producing a water-in-oil cream is well known in the art, for example, a method of adding water while stirring the oil phase is known, but other methods well known in the art ( For example, it may be manufactured according to the method described in the "New Cosmetics Handbook").

The content of panthenol or a panthenol-related substance in the water-in-oil (W / O type) emulsified composition of the present invention is 0.1 to 8.0% by mass, more preferably 0.5 to 5.0% by mass, further preferably. Is 1.0 to 3.0% by mass.

Since the water-in-oil (W / O type) emulsifying composition of the present invention is intended to exert a moisturizing action, a tissue repair promoting action, and an anti-inflammatory action, it has a moisturizing action and a tissue repair promoting action in addition to panthenol. It may further contain an active ingredient having an action and an anti-inflammatory action. As a further active ingredient that can be contained in the water-in-oil (W / O type) emulsified composition of the present invention, for example, one or a plurality of ingredients selected from heparinoids, vitamin Es, and the like. Can be used.

In this aspect of the present invention, the term heparinoid refers to a substance having a structure or an action similar to that of "heparin" having a blood coagulation inhibitory action, and is a substance physically called polysulfated chondroitin sulfate. .. In the present invention, in particular, a mucopolysaccharide polysulfate ester conforming to the "heparin-like substance" listed in the Japanese Pharmacopoeia Non-Pharmaceutical Standards can be used. The content of the heparinoid in the water-in-oil (W / O type) emulsified composition of the present invention is, for example, 0.01 to 5.0% by mass, preferably 0.05 to 1.0% by mass, and more preferably 0.1 to 0.1 to the total content. It can be 0.5% by mass.

When referring to vitamin Es in this aspect of the present invention, tocopherol and its derivatives (for example, tocopherol acetate, calcium tocopherol succinate, etc.) can be used.

The content of vitamin E in the water-in-oil (W / O type) emulsified composition of the present invention is, for example, 0.001 to 5.0% by mass, preferably 0.05 to 3.0% by mass, and more preferably 0.5 to 2.0% by mass. Can be%. For example, as a prescription example, a case where vitamin Es are blended as tocopherol acetate in 0.5% can be considered.

The water-in-oil (W / O type) emulsified composition of the present invention can be used in an external application route for skin. Therefore, the present invention also provides a skin external coating agent composed of a water-in-oil (W / O type) emulsified composition containing panthenol or a panthenol-related substance as an active ingredient.

Since the external coating agent for skin of the present invention is a water-in-oil (W / O type) emulsified composition, it is provided as a cream or an emulsion. Such creams or emulsions can be prepared according to preparation methods generally known in the art. The preparation method is not particularly limited, and for example, appropriate components such as known excipients necessary for preparing preparations of various dosage forms are blended together with the above essential components and optional components to prepare each preparation. It can be prepared by the conventional method of.

The external coating agent for skin of the present invention includes panthenol or a panthenol-related substance, a heparinoid substance (for example, polysulfated chondroitin sulfate) which may be added as an additional component, and vitamin Es (for example, tocopherol acetate). ), And if necessary, various active ingredients used in pharmaceuticals, quasi-drugs, cosmetics, etc. may be blended as long as the effects of the present invention are not impaired. Such additional active ingredients include, for example, anti-inflammatory agents, antihistamines, herbal ingredients, antipruritic agents, wound healing agents, local anesthetics, vitamins, refreshing agents, moisturizers, fungicides, vasoconstrictors and Amino acids and the like can be contained.

Hereinafter, the present invention will be specifically described with reference to Examples and Comparative Examples, but the present invention is not limited to the following Examples.

Example 1: Water-in-oil cream containing panthenol In this example, what is the water content of the skin depending on whether the panthenol is a water-in-oil cream or an oil-in-water cream. An experiment was conducted with the aim of clarifying whether it changes to.

In this example, the case where panthenol is used as a water-in-oil cream (Production Example 1) and the case where panthenol is used as an oil-in-water cream (Comparative Example 2) are compared with a water-in-oil cream containing no panthenol (comparison). It was compared with Example 1) and oil-in-water cream (Comparative Example 3). The specific components of the A component (oil phase component) and the B component (aqueous phase component) of each formulation example are as shown in Table 1 below.

In each of the production examples and comparative examples, the components A and B were respectively heated and dissolved at 70 to 80 ° C. Then, component B was gradually added to component A while stirring to emulsify, and then cooled while stirring to obtain a cream.

Next, the skin on the medial forearm of human subjects (male and female, ages ranging from 26 to 35 years) was wiped with gauze soaked in ethanol for disinfection, dried, and the medial forearm was 2 cm in diameter. A circular mark was added to mark the measurement site.

The water content of the stratum corneum at the measurement site was measured with the epidermal stratum corneum water content measuring device SKICON-200EX (manufactured by I.B.S Co., Ltd.). Before applying the cream agent and 1 hour after applying the cream agent, the water content of the stratum corneum at the measurement site was measured by this device.

From the measured value before applying the cream and the measured value 1 hour after applying the cream, the rate of change (%) in the water content of the stratum corneum was calculated according to the following formula:
Rate of change in water content in the stratum corneum (%) = (measured value after 1 hour) / (measured value before application) x 100.

The results are shown in Figure 1. The untreated group to which no cream was applied was designated as "control". The values in the graph are the average values of the 6 cases in each group, and the error bars indicate the standard error.

As shown in Production Example 1, by applying the water-in-oil cream containing panthenol, the stratum corneum moisture was compared with the control (untreated group) and Comparative Example 1 (water-in-oil cream not containing panthenol). The amount increased significantly and the difference was clear.

On the other hand, as shown in Comparative Example 2 and Comparative Example 3, in the oil-in-water cream, no significant difference was observed in the change in the water content of the stratum corneum depending on the presence or absence of panthenol.

Example 2: Effect of panthenol content in water-in-oil cream In this example, what is the water content of the skin when water-in-oil cream containing various amounts of panthenol is prepared? An experiment was conducted with the aim of clarifying whether it changes to.

In this example, the case where 0.5% to 4% of panthenol was used as the water-in-oil cream (Production Examples 3 to 6) was compared with the water-in-oil cream containing no panthenol (Comparative Example 1). .. The specific components of the A component (oil phase component) and B component (aqueous phase component) of each formulation example are as shown in Table 2 below.

In each of the production examples and comparative examples, the components A and B were respectively heated and dissolved at 70 to 80 ° C. Then, component B was gradually added to component A while stirring to emulsify, and then cooled while stirring to obtain a cream.

Data were obtained from 8 human subjects in each group by the same procedure as in Example 1, and the results on the rate of change in stratum corneum water were obtained by the same procedure as in Example 1. The result is shown in figure 2. Also in FIG. 2, the untreated group to which the cream agent was not applied was designated as the “control”. The values in the graph are the average values of the eight cases in each group, and the error bars indicate the standard error.

As shown in Production Examples 3 to 6, by applying the water-in-oil cream containing panthenol, control (untreated group) and Comparative Example 1 (bread) regardless of the amount of panthenol added from 0.5% to 4%. The water content of the stratum corneum was significantly increased as compared with the water-in-oil cream containing no tenor, and the difference was clear.

Example 3: Water-in-oil cream containing panthenol and additional ingredients In this example, how the water content of the skin is when panthenol is made into a water-in-oil cream with additional ingredients. Experiments were conducted with the aim of clarifying whether it would change.

In this example, in the case of a water-in-oil cream containing pantenol together with polysulfated chondroitin sulfate and tocopherol acetate as additional components (Production Example 2), pantenol is not included but is sulfated. Comparison was made with those containing chondroitin sulfate (Comparative Example 4), those containing tocopherol acetate (Comparative Example 5), or those containing both sulfated chondroitin sulfate and tocopherol acetate (Comparative Example 6). The specific components of the A component (oil phase component) and the B component (aqueous phase component) of each formulation example are as shown in Table 3 below.

In each of the production examples and comparative examples, the components A and B were respectively heated and dissolved at 70 to 80 ° C. Then, component B was gradually added to component A while stirring to emulsify, and then cooled while stirring to obtain a cream.

As the polysulfated chondroitin sulfate, a substance conforming to the Japanese Pharmacopoeia non-Japanese drug standard "heparinoid" was used.

Data were obtained from 6 human subjects in each group by the same procedure as in Example 1, and the results on the rate of change in stratum corneum water were obtained by the same procedure as in Example 1. The results are shown in FIGS. 3 (A) and 3 (B). In both FIGS. 3 (A) and 3 (B), the untreated group to which no cream was applied was designated as the "control". The values in the graph are the average values of the 6 cases in each group, and the error bars indicate the standard error.

As shown in Production Example 2, panthenol also exhibited an excellent moisturizing effect in the case of a water-in-oil cream in which panthenol was used in combination with polysulfated chondroitin sulfate and tocopherol acetate. The effects of this combination include the moisturizing effect of a water-in-oil cream containing polysulfated chondroitin sulfate but not panthenol or tocopherol acetate (Comparative Example 4), or the effect of panthenol or polyus containing tocopherol acetate Moisturizing effect of water-in-oil cream containing sulfated chondroitin sulfate (Comparative Example 5), water-in-oil cream containing polysulfated chondroitin sulfate and tocopherol acetate but not panthenol (Comparative Example 6) A higher effect than the moisturizing effect was obtained.

When panthenol was contained in a water-in-oil (W / O type) emulsified composition, when it was applied to the skin, the excellent moisturizing effect of panthenol could be exhibited in a short time. Furthermore, by using a water-in-oil emulsified composition, panthenol can exert an excellent moisturizing effect even when used in combination with heparinoids and vitamin E used for the purpose of moisturizing and improving rough skin. did it.

Claims (8)

A water-in-oil (W / O type) emulsified composition containing panthenol or a panthenol-related substance. The water-in-oil (W / O type) emulsified composition according to claim 1, wherein the content of panthenol or a panthenol-related substance is 0.5 to 5.0% by mass. The water-in-oil type (W / O type) according to claim 1 or 2, wherein the panthenol-related substance is selected from the group consisting of pantothenyl ethyl ether, calcium pantothenate, sodium pantothenate, and acetyl panthenyl ethyl ether. ) Emulsifying composition. The water-in-oil (W / O type) emulsified composition according to any one of claims 1 to 3, which contains a glycerin fatty acid ester as a lipophilic emulsifier. The water-in-oil (W / O type) emulsified composition according to any one of claims 1 to 4, further containing a heparinoid, vitamin E, or a heparinoid and vitamin E. The water-in-oil (W / O type) emulsified composition according to claim 5, wherein the content of heparinoids is 0.1 to 0.5% by mass, or the content of vitamin Es is 0.5 to 2.0% by mass. The water-in-oil (W / O type) emulsified composition according to any one of claims 1 to 6, which is used for external application to the skin. An external coating agent for skin, which is the water-in-oil (W / O type) emulsifying composition according to any one of claims 1 to 6.

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