JP7641466B2 - Composition for topical skin preparation - Google Patents

Description

The present invention relates to a composition for external skin preparation.

In recent years, one of the main functions required for skin care products is "anti-aging," and various drugs that exert anti-aging effects have been proposed. Among these drugs, nicotinamide and retinol palmitate have attracted attention as ingredients with excellent anti-aging effects, and the number of products that use both ingredients in combination is increasing.

However, when nicotinamide and retinol palmitate are used in combination in a large amount in a formulation, it is possible to exert a significantly excellent anti-aging effect, but on the other hand, there are problems such as precipitation due to nicotinamide and odor easily caused by retinol palmitate. Therefore, it is not possible to incorporate a large amount of both components, nicotinamide and retinol palmitate, in the formulation, and there is a problem that the desired anti-aging effect cannot be fully exerted.

To solve such problems, a skin topical composition has been proposed that combines a specific skin-forming polymer having a silicone structure with a specific amount of a wrinkle-improving component such as retinol or nicotinic acid amide (see, for example, Patent Document 1). However, such a skin topical composition using a skin-forming polymer having a silicone structure has the drawbacks of feeling heavy when applied and being more sticky due to poor spreadability on the skin.

On the other hand, a skin external preparation that combines specific amounts of nicotinamide, a salt-resistant water-soluble polymer, retinol or a derivative thereof, and a polyhydric alcohol has also been proposed (see, for example, Patent Document 2). Although this attempt can suppress the precipitation of nicotinamide and the foul odor of retinol palmitate, it has drawbacks such as poor spreadability on the skin, stickiness, and difficulty in obtaining a satisfactory feeling of use.

JP 2022-067065 A JP 2021-098655 A

Therefore, the present invention has been made in consideration of the above-mentioned technology, and an object of the present invention is to provide a composition for external skin preparations which not only suppresses the precipitation of nicotinamide and the like and the odor of retinol palmitate and the like, but also provides a good feel during and after application and exhibits a significantly superior moisturizing effect.

That is, the present invention provides a composition for external skin preparation comprising the following components A, B, C, and D:
Component A: Nicotinic acid and/or its derivatives Component B: Retinol and/or its derivatives Component C: Nonionic surfactant Component D: Ester oil of branched fatty acid and branched alcohol

It is preferable that the above component D is isostearyl isostearate.

It is further preferable that the composition contains the following component E.
Component E: Ester oil of fatty acid and polyhydric alcohol and/or hydrocarbon oil

It is also preferable that the composition further contains Component F below.
Component F: Carbomer and/or (acrylates/alkyl acrylate (C10-30)) crosspolymer

By satisfying the above-mentioned constituent requirements, the composition for topical skin preparation of the present invention has the effect of suppressing both the precipitation caused by component A and the odor caused by component B, thereby exhibiting significantly excellent storage stability of the preparation.

In addition, the composition for topical skin preparations of the present invention has good skin compatibility and spreadability when applied, and has the effect of imparting a smooth, non-sticky feel to the skin while providing an excellent moisturizing effect to the skin after application.

The composition for external skin preparation of the present invention contains the following component A, component B, component C, and component D.
Component A: Nicotinic acid and/or its derivatives Component B: Retinol and/or its derivatives Component C: Nonionic surfactant Component D: Ester oil of branched fatty acid and branched alcohol

Hereinafter, each component used in the composition for external skin preparation of the present invention will be described in detail.

[Component A]
The component A is nicotinic acid and/or a derivative thereof. That is, the component A is one or both of nicotinic acid and a nicotinic acid derivative. In the present invention, by using the component A, it is possible to exert an excellent anti-aging effect.

Specific examples of component A include nicotinic acid, nicotinamide, tocopherol nicotinate, methyl nicotinate, ethyl nicotinate, etc. These components A may be used alone or in appropriate combination of two or more.

Of the above-mentioned component A, from the viewpoint of exerting a better anti-aging effect, it is preferable to use at least one selected from nicotinic acid, nicotinamide, and tocopherol nicotinate, it is more preferable to use nicotinic acid and/or nicotinamide, and it is most preferable to use nicotinamide.

In the present invention, a commercially available product may be used as the above-mentioned component A. The commercially available product of the above-mentioned component A may be a single raw material or a mixed raw material with other components, and is not particularly limited as long as the desired effect is exhibited.

The content of the above-mentioned component A in the composition for external skin preparation of the present invention is not particularly limited as long as the desired effect can be exhibited, but from the viewpoint of exhibiting a good anti-aging effect, it is preferably 1% by mass to 10% by mass, and more preferably 3% by mass to 7% by mass, based on 100% by mass of the composition. Note that the content of the above-mentioned component A is the amount converted into a pure content.

[Component B]
The component B is retinol and/or a derivative thereof. That is, the component B is one or both of retinol and a retinoic acid derivative. In the present invention, by using the component B, it is possible to exert an excellent anti-aging effect.

Specific examples of component B include retinol, retinol palmitate, hydrogenated retinol, retinol acetate, retinol propionate, and retinol linoleate. These components B may be used alone or in appropriate combination of two or more.

Of the above-mentioned component B, from the viewpoint of exerting a better anti-aging effect, it is preferable to use at least one selected from retinol, retinol palmitate, and hydrogenated retinol, it is more preferable to use retinol and/or retinol palmitate, and it is most preferable to use retinol palmitate.

In the present invention, a commercially available product may be used as the component B. The commercially available product of the component B may be a single raw material or a mixed raw material with other components, and is not particularly limited as long as the desired effect is exhibited.

The content of the above-mentioned component B in the composition for external skin preparation of the present invention is not particularly limited as long as the desired effect can be exhibited, but from the viewpoint of exhibiting a good anti-aging effect, it is preferably 0.001% by mass to 1% by mass, and more preferably 0.01% by mass to 0.5% by mass, based on 100% by mass of the composition. Note that the content of the above-mentioned component B is the amount converted into a pure content.

[Component C]
The component C is a nonionic surfactant. In the present invention, by using the component C, the components A and B can be stably blended in the composition.

Examples of the component C include glycerin fatty acid esters, polyoxyethylene glycerin fatty acid esters, polyglycerin fatty acid esters, sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene fatty acids, polyoxyethylene alkyl ethers, polyoxyethylene polyoxypropylene alkyl ethers, etc. One type of these components C may be used alone, or two or more types may be used in appropriate combination.

Of the above component C, from the viewpoint of blending the above components A and B more stably, it is preferable to use at least one selected from glycerin fatty acid esters, polyoxyethylene glycerin fatty acid esters, sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters, and polyglycerin fatty acid esters, and it is more preferable to use at least one selected from glycerin fatty acid esters, sorbitan fatty acid esters, and polyoxyethylene sorbitan fatty acid esters.

In the present invention, a commercially available product may be used as the component C. The commercially available product of the component C may be a single raw material or a mixed raw material with other components, and is not particularly limited as long as the desired effect is exhibited.

The content of the above-mentioned component C in the composition for external skin preparation of the present invention is not particularly limited as long as the desired effect can be exhibited, but from the viewpoint of more stably blending the above-mentioned components A and B, it is preferably 0.5% by mass to 5% by mass, and more preferably 1% by mass to 3% by mass, based on 100% by mass of the composition. Note that the content of the above-mentioned component C is the amount converted into a pure content.

[Component D]
The component D is an ester oil of a branched fatty acid and a branched alcohol. In the present invention, by using the component D, it is possible to improve the storage stability of the preparation by suppressing the precipitation caused by the component A and the odor caused by the component B, and also to improve the skin compatibility and spreadability when applied, and to impart a smooth and non-sticky feel to the skin after application.

Specific examples of component D include octyldodecyl neopentanoate, isocetyl octanoate, isostearyl octanoate, octyl isononanoate, hexyldecyl neodecanoate, octyldodecyl neodecanoate, 2-ethylhexyl isopalmitate, isocetyl isostearate, isostearyl isostearate, octyldodecyl isostearate, etc. One type of component D may be used alone, or two or more types may be used in appropriate combination.

Among the above-mentioned component D, from the viewpoint of further enhancing the storage stability of the formulation by suppressing precipitation caused by the above-mentioned component A and odor change caused by the above-mentioned component B, as well as from the viewpoint of improving skin compatibility and spreadability at the time of application and enhancing a smooth and non-sticky feel on the skin after application, it is preferable to use at least one selected from octyldodecyl neopentanoate, isostearyl isostearate, and octyldodecyl isostearate, it is more preferable to use at least one selected from isostearyl isostearate and octyldodecyl isostearate, and it is most preferable to use isostearyl isostearate.

In the present invention, a commercially available product may be used as the component D. The commercially available product of the component D may be a single raw material or a mixed raw material with other components, and is not particularly limited as long as the desired effect is exhibited.

The content of the above-mentioned component D in the composition for external skin preparation of the present invention is not particularly limited as long as the desired effect can be exhibited, but from the viewpoint of enhancing the storage stability of the preparation by suppressing precipitation caused by the above-mentioned component A and odor change caused by the above-mentioned component B, and from the viewpoint of improving skin compatibility and spreadability at the time of application and imparting a smooth, non-sticky feel to the skin after application, the content is preferably 1% by mass to 8% by mass, and more preferably 2% by mass to 6% by mass, based on 100% by mass of the composition. The content of the above-mentioned component D is the amount converted into a pure content.

In the present invention, from the viewpoint of further enhancing the storage stability of the preparation by suppressing precipitation caused by the above component A and odor change caused by the above component B, as well as from the viewpoint of improving skin compatibility and spreadability at the time of application and enhancing a smooth, non-sticky feel on the skin after application, the content ratio of the sum of the above components A and B to the above component D, "(component A+component B)/component D", is preferably prepared so as to satisfy the range of 0.5 to 2, and more preferably prepared so as to satisfy the range of 0.8 to 1.5.

[Component E]
The composition for external skin preparation of the present invention preferably further contains an ester oil of a fatty acid and a polyhydric alcohol and/or a hydrocarbon oil as component E. In the present invention, by using the above-mentioned component E, not only can the moisturizing effect be enhanced, but also the storage stability of the preparation can be further improved by suppressing the precipitation caused by the above-mentioned component A and the odor caused by the above-mentioned component B. In this specification, the above-mentioned ester oil of a fatty acid and a polyhydric alcohol may be referred to as "component E1", and the above-mentioned hydrocarbon oil may be referred to as "component E2".

Specific examples of component E1 include ethylene glycol dioleate, propylene glycol dicaprylate, propylene glycol di(capryl-capric acid), propylene glycol dicaprate, propylene glycol dioleate, neopentyl glycol dicaprate, neopentyl glycol dioctanoate, glyceryl tricaprylate, glyceryl tri-2-ethylhexanoate, glyceryl tri(capryl-capric acid), glyceryl triundecylate, glyceryl triisopalmitate, glyceryl triisostearate, trimethylolpropane tri-2-ethylhexanoate, trimethylolpropane triisostearate, pentaerythritol tetra-2-ethylhexanoate, pentaerythritol tetramyristate, pentaerythritol tetraisostearate, etc. These components E1 may be used alone or in appropriate combination of two or more.

Specific examples of component E2 include α-olefin oligomer, light isoparaffin, light liquid isoparaffin, synthetic squalane, vegetable squalane, squalane, ceresin, paraffin, polyethylene powder, polybutene, microcrystalline wax, liquid isoparaffin, liquid paraffin, petrolatum, etc. These components E2 may be used alone or in appropriate combination of two or more.

In the present invention, from the viewpoint of suppressing precipitation caused by the component A and odor caused by the component B and further improving the storage stability of the formulation, it is preferable to use the components E1 and E2 in combination, and more specifically, it is most preferable to use glyceryl tri-2-ethylhexanoate and squalane in combination.

In the present invention, a commercially available product may be used as the above-mentioned component E. The commercially available product of the above-mentioned component E may be a single raw material or a mixed raw material with other components, and is not particularly limited as long as the desired effect is exhibited.

The content of the component E in the composition for external skin preparations of the present invention is not particularly limited as long as the desired effect can be exhibited, but from the viewpoint of enhancing the moisturizing effect and enhancing the storage stability of the preparation by suppressing precipitation caused by the component A and odor change caused by the component B, the content is preferably 1% by mass to 10% by mass, and more preferably 3% by mass to 8% by mass, based on 100% by mass of the composition. The content of the component E is the amount converted into a pure content.

In the present invention, from the viewpoint of suppressing precipitation caused by the component A and odor change caused by the component B and further enhancing the storage stability of the preparation, the content ratio of the component E to the component D, "component E/component D," is preferably prepared so as to satisfy the range of 0.5 to 2, and more preferably so as to satisfy the range of 1 to 1.8.

[Component F]
It is preferable that the composition for external skin preparations of the present invention further contains a carboxyvinyl polymer and/or an (acrylates/alkyl acrylate (C10-30)) crosspolymer as component F. In the present invention, by using the above-mentioned component F, it is possible to further improve skin compatibility and spreadability upon application.

The above-mentioned component F is usually neutralized with a basic substance before use. Examples of the basic substance include alkanolamines such as triethanolamine and monoethanolamine; inorganic bases such as ammonia, sodium hydroxide and potassium hydroxide; and basic amino acids such as arginine. The amount of the basic substance added is an amount sufficient to neutralize the above-mentioned component F, and may be appropriately blended depending on the type and amount of these components used.

In the present invention, a commercially available product may be used as the above-mentioned component F. The commercially available product of the above-mentioned component F may be a single raw material or a mixed raw material with other components, and is not particularly limited as long as the desired effect is exhibited.

The content of the above-mentioned component F in the composition for external skin preparations of the present invention is not particularly limited as long as the desired effect can be exhibited, but from the viewpoint of further improving skin compatibility and spreadability upon application, it is preferably 0.01% by mass to 1% by mass, and more preferably 0.1% by mass to 0.8% by mass, based on 100% by mass of the composition. The content of the above-mentioned component F is the amount converted into a pure content.

[Other ingredients]
In addition to the above-mentioned components, the composition for external skin preparation of the present invention may contain, as appropriate depending on the purpose, active ingredients other than the above-mentioned components A and B, surfactants other than the above-mentioned component C, oils other than the above-mentioned components D and E, thickeners other than the above-mentioned component F, polyhydric alcohols, ultraviolet absorbers, fragrances, pH adjusters, film-forming agents, chelating agents, lower alcohols, astringents, antioxidants, preservatives, colorants, plant extracts, plant fermentation extracts, purified water, and the like.

The dosage form of the composition for external skin preparation of the present invention is not particularly limited as long as it can exert the desired effect, and it can be prepared into various dosage forms such as liquid, gel, emulsion, cream, etc. In the present invention, from the viewpoint of exerting a significantly excellent storage stability of the preparation and from the viewpoint of usability, it is preferable to prepare it into a gel, emulsion, or cream, and among them, it is more preferable to prepare it into an emulsion form such as an emulsion or cream.

The method for producing the composition for external skin preparation of the present invention is not particularly limited, but may be, for example, a known method.Specifically, for example, the above-mentioned components are mixed and stirred using a disper mixer, homomixer, disper mill, etc., but the present invention is not limited to these methods.

The area to which the composition for external skin preparation according to one embodiment of the present invention is applied is not particularly limited, but examples include the face (forehead, eyes, corners of the eyes, cheeks, mouth, etc.), arms, elbows, backs of the hands, fingertips, feet, knees, heels, neck, décolleté, armpits, and back.

The present invention will be described in more detail below with reference to examples, but the present invention is not limited to these examples. The blend amounts are expressed in "mass %" unless otherwise specified.

(Sample Preparation 1)
According to the formulations shown in Tables 1 and 2, the compositions for external skin preparations of Examples 1 to 5 and Comparative Examples 1 to 4 were prepared into cream formulations in a conventional manner and subjected to the following evaluations. The results are shown in Tables 1 and 2. The amounts of ingredients in the tables are all values converted to pure contents.

(Test Example 1: Storage stability of preparation)
Each sample obtained in the Examples and Comparative Examples was filled into a 50 mL glass mayonnaise bottle, which was then stored in a thermostatic chamber at 40° C. for 4 weeks, after which the presence or absence of "precipitation" or "unpleasant odor" was confirmed.

The presence or absence of precipitation was evaluated by preparing a pair of transparent glass slides, dispensing 0.02 g of each sample onto one of the slides, sandwiching it with the remaining slide, and rubbing the two slides together to spread the sample. The presence of precipitates in the sample was visually confirmed and evaluated according to the following criteria.

<Evaluation criteria for the presence or absence of precipitation>
○ (Good): No precipitates were observed. △ (Insufficient): Slight precipitates were observed. × (Poor): Obvious precipitates were observed.

The presence or absence of an unpleasant odor was evaluated by smelling each sample directly from the mouth of the mayonnaise bottle to confirm whether or not there was an odor of rancidity, and the odor was evaluated according to the following criteria.

<Evaluation criteria for the presence or absence of strange odor>
○ (Good): No strange odor is detected. △ (Poor): A slight rancid odor is detected. × (Bad): A clearly rancid odor is detected.

(Test Example 2: Evaluation upon application)
A use test was carried out by applying 0.1 g of each sample obtained in the Examples and Comparative Examples to the back of the hand, and a sensory evaluation was carried out on the "skin compatibility" and "spreadability" at the time of application, as well as the "moisturizing feeling" and "non-sticky feeling" of the skin 10 minutes after application, and the results were scored according to the following evaluation points of 1 to 5. Each evaluation was carried out by five expert evaluators, and the average score was calculated from the evaluation results of each evaluator and determined according to the following criteria.

In addition, in the evaluation of "skin compatibility," a product that felt like it was penetrating into the skin was given a high score. In the evaluation of "spreadability," a product that spreads softly and smoothly was given a high score. In the evaluation of "moisturizing feel," a product that felt like it moisturized the skin was given a high score. In the evaluation of "non-sticky feel," a product that felt smooth and not sticky was given a high score.

<Evaluation criteria>
5 points: Very good 4 points: Good 3 points: Average 2 points: Poor 1 point: Very poor

<Criteria>
◎: Average of 4.0 points or more ○: Average of 3.0 points or more and less than 4.0 points △: Average of 2.0 points or more and less than 3.0 points ×: Average of less than 2.0 points

From the results shown in Tables 1 and 2, it can be seen that the compositions for external preparations for skin of the present invention obtained in each Example, compared with those obtained in each Comparative Example, do not show either precipitation due to the above-mentioned component A or odor caused by the above-mentioned component B, and have good storage stability of the preparation. It can also be seen that the compositions have good skin compatibility and spreadability when applied, and can provide excellent moisturizing effect to the skin after application, but have a smooth feel without stickiness. In other words, it can be said that the composition for external preparations for skin of the present invention can fully exert a remarkably excellent effect by satisfying the above-mentioned constituent requirements.

Claims (4)

Component A: 1 to 10% by mass of nicotinamide;
Component B: 0.001 to 1% by mass of retinol and /or its derivative,
Component C: 0.5 to 5% by mass of a nonionic surfactant;
Component D: 1 to 8% by mass of ester oil of branched fatty acid and branched alcohol
The composition comprises
As the retinol and/or its derivative, at least one component selected from the group consisting of retinol palmitate, retinol acetate, retinol propionate, and retinol linoleate is used,
At least one component selected from the group consisting of glycerin fatty acid esters, sorbitan fatty acid esters, and polyoxyethylene sorbitan fatty acid esters is used as the nonionic surfactant,
As the ester oil of the branched fatty acid and the branched alcohol, at least one component selected from the group consisting of octyldodecyl neopentanoate, isocetyl octanoate, isostearyl octanoate, octyl isononanoate, hexyldecyl neodecanoate, octyldodecyl neodecanoate, 2-ethylhexyl isopalmitate, isocetyl isostearate, isostearyl isostearate, and octyldodecyl isostearate is used;
A composition for external skin preparation, wherein the content ratio of the sum of the components A and B to the component D [(component A+component B)/component D] is in the range of 0.5 to 2. The composition for external skin preparation according to claim 1 , wherein said component D is isostearyl isostearate. Component E: Ester oil of fatty acid and polyhydric alcohol and/or hydrocarbon oil
The composition for external skin preparations according to claim 1 or 2, further comprising at least one component selected from the group consisting of ethylene glycol dioleate, propylene glycol dicaprylate, propylene glycol di(capryl-caprate), propylene glycol dicaprate, propylene glycol dioleate, neopentyl glycol dicaprate, neopentyl glycol dioctanoate, glyceryl tricaprylate, glyceryl tri-2-ethylhexanoate, glyceryl tri(capryl-caprate), glyceryl triundecylate, glyceryl triisopalmitate, glyceryl triisostearate, trimethylolpropane tri-2-ethylhexanoate, trimethylolpropane triisostearate, pentaerythritol tetra-2-ethylhexanoate, pentaerythritol tetramyristate, and pentaerythritol tetraisostearate, as the ester oil of the fatty acid and the polyhydric alcohol. Component F : Carboxyvinyl polymer and/or (acrylates/alkyl acrylate (C10-30)) crosspolymer
The composition for external skin preparation according to claim 1 or 2, further comprising :