Topical skin preparation

Abstract

To provide a topical skin preparation which contains niacinamide while exhibiting superior usability.SOLUTION: A topical skin preparation comprises: (A) 3 mass% or more of niacinamide; (B) tranexamic acid; (C) D-panthenyl alcohol; and at least one selected from (D) polyhydric alcohols, (E) thickening agents, and (F) oil agents.SELECTED DRAWING: None

Description

Technical Field

[0001] The present invention relates to a topical skin preparation containing niacinamide, tranexamic acid, and D-pantothenyl alcohol.

Background Art

[0002] Since niacinamide has effects as whitening, anti-wrinkle, and anti-aging, various topical skin preparations containing niacinamide have been proposed (Patent Document 1). In order to exhibit these effects, it is necessary to formulate a large amount of niacinamide. However, cosmetics containing niacinamide have problems in terms of usability. In addition, although it has also been proposed to formulate tranexamic acid or D-pantothenyl alcohol in a topical skin preparation in expectation of effects on the skin, it is known that the formulation of these components also has problems in terms of usability.

Prior Art Documents

Patent Documents

[0003]

Patent Document 1

Summary of the Invention

Problems to be Solved by the Invention

[0004] Therefore, the present inventors have made various studies with the problem of providing a topical skin preparation having excellent usability while containing niacinamide.

Means for Solving the Problems

[0005] As a result, the present inventors have succeeded in developing a topical skin preparation having excellent usability by using a topical skin preparation containing niacinamide, tranexamic acid, D-pantothenyl alcohol, and at least one selected from polyhydric alcohols, thickeners, and oils, and have completed the present invention.

[0006] That is, the present invention is as follows. <1> (A) 3% by mass or more of niacinamide, (B) tranexamic acid, (C) D-pantothenyl alcohol, and (D) at least one selected from polyhydric alcohols, (E) thickeners, and (F) oily agents A skin external preparation characterized by containing <2> Further, a skin external preparation according to <1>, characterized by containing (G) a bactericide. <3> A skin external preparation according to <1>, characterized in that (B) tranexamic acid is 0.1% by mass or more. <4> A skin external preparation according to <1>, characterized in that D-pantothenyl alcohol is 0.01% by mass or more. <6> A skin external preparation according to <1>, characterized by containing (D) polyhydric alcohol, (E) thickener, and (F) oily agent. <7> A skin external preparation according to <2>, wherein (G) is at least one selected from salicylic acid or its salt, and isopropylmethylphenol. <8> A skin external preparation according to <2>, characterized in that (G) the bactericide is 0.01% by mass or more. <9> A skin external preparation according to any one of <1> or <2>, which is an oil-in-water emulsion.

[0007] According to the present invention, by containing at least one selected from polyhydric alcohols, thickeners, and oily agents together with niacinamide, tranexamic acid, and D-pantothenyl alcohol, a skin external preparation excellent in usability can be provided. Further, by containing at least one selected from polyhydric alcohols, thickeners, and oily agents together with niacinamide, tranexamic acid, and D-pantothenyl alcohol, and a bactericide, a skin external preparation excellent in moisture retention and stability can be provided together with usability.

Mode for Carrying Out the Invention

[0008] Hereinafter, the skin external preparation of the present invention will be described in detail. Note that the present invention is not limited to the embodiments shown below, and can be changed within the scope that those skilled in the art can conceive, such as other embodiments, additions, modifications, deletions, etc. As long as the functions and effects of the present invention are exhibited in any aspect, it is included in the scope of the present invention.

[0009] <(A) Niacinamide> The skin external preparation of the present invention is characterized by containing niacinamide. Niacinamide is an amide of niacin (nicotinic acid / vitamin B 3 ) and is a kind of water-soluble vitamin in the vitamin B group. In the present invention, niacinamide that is usually used in cosmetics, quasi-drugs, etc. can be used. For example, those extracted from natural products, those purified therefrom, those synthesized by known methods, etc., and commercially available products can also be used.

[0010] In the skin external preparation of the present invention, from the viewpoint of exerting its effect, niacinamide is formulated in the skin external preparation at 3% by mass or more. From the viewpoint of enjoying its effect, 4% by mass or more is preferable, and 5% by mass or more is particularly preferable. The upper limit is not particularly limited, but 30% by mass or less is preferable, more preferably 20% by mass or less, and from the viewpoint of obtaining a skin external preparation with excellent usability and enjoying the effect of niacinamide, it is particularly preferably 10% by mass or less. The content of niacinamide in the skin external preparation of the present invention can be analyzed, for example, by high performance liquid chromatography.

[0011] <(B) Tranexamic acid> The skin external preparation of the present invention is characterized by containing tranexamic acid. Tranexamic acid is a kind of synthetic amino acid and is used as a hemostatic agent, anti-inflammatory agent, etc. In the present invention, tranexamic acid that is usually used in cosmetics, quasi-drugs, etc. can be used.

[0012] In the topical skin preparation of the present invention, the content of tranexamic acid is not particularly limited. For example, 0.1% by mass or more is preferable, 0.5% by mass or more is more preferable, and from the viewpoint of excellent usability and the ability to enjoy the effects of tranexamic acid, 1% by mass or more is particularly preferable. The upper limit is not particularly limited, but 20% by mass or less is preferable, more preferably 15% by mass or less, and particularly preferably 10% by mass or less. The content of tranexamic acid in the topical skin preparation of the present invention can be analyzed, for example, by high performance liquid chromatography, and as the conditions, it can be quantified according to, for example, the quantification method of tranexamic acid described in the 18th revised Japanese Pharmacopoeia.

[0013] <(C)D-Panthenyl alcohol> The topical skin preparation of the present invention is characterized by containing D-panthenyl alcohol. D-panthenyl alcohol is also called panthenol, is a derivative of vitamin B5 (pantothenic acid), and is a kind of vitamin B group and a water-soluble vitamin. In the present invention, D-panthenyl alcohol that is usually used in cosmetics, quasi-drugs, etc. can be used. For example, those extracted from natural products, those purified therefrom, those synthesized by known methods, etc., and commercially available products can also be used.

[0014] In the topical skin preparation of the present invention, the content of D-panthenyl alcohol is not particularly limited. For example, 0.01% by mass or more is preferable, 0.05% by mass or more is more preferable, and from the viewpoint of excellent usability and the ability to enjoy the effects of D-panthenyl alcohol, 0.1% by mass or more is particularly preferable. The upper limit is not particularly limited, but 5% by mass or less is preferable, more preferably 3% by mass or less, and particularly preferably 1% by mass or less. The content of D-panthenyl alcohol in the topical skin preparation of the present invention can be analyzed, for example, by high performance liquid chromatography, and as the conditions, it can be quantified according to, for example, the quantification method of D-panthenyl alcohol described in the Quasi-drug Raw Material Standard 2021.

[0015] <(D)Polyhydric alcohol> The external preparation for skin of the present invention is characterized by containing at least one selected from polyhydric alcohols, thickeners, and oils. Examples of the polyhydric alcohols that can be used in the present invention include dihydric to trihydric polyhydric alcohols such as propylene glycol (PG), 1,3-butylene glycol (BG), dipropylene glycol, tripropylene glycol, 1,2-pentanediol (pentylene glycol), 1,5-pentanediol, 1,2-hexanediol, 1,2-octanediol, glycerin, and polyethylene glycol; and sugar alcohols such as sorbitol and xylitol. Among these, in the present invention, it is preferable to use one or more selected from dihydric to trihydric polyhydric alcohols, and it is particularly preferable to use dihydric to trihydric polyhydric alcohols having 3 to 9 carbon atoms such as propylene glycol (PG), 1,3-butylene glycol (BG), dipropylene glycol, tripropylene glycol, 1,2-pentanediol (pentylene glycol), 1,5-pentanediol, 1,2-hexanediol, 1,2-octanediol, and glycerin.

[0016] When a polyhydric alcohol is blended in the external preparation for skin of the present invention, its content is not particularly limited. For example, it is preferably 0.01% by mass or more, more preferably 0.1% by mass or more, and particularly preferably 1% by mass or more from the viewpoint of obtaining an external preparation for skin with excellent usability. Also, it is preferably 50% by mass or less, more preferably 40% by mass or less, and particularly preferably 35% by mass or less. When two or more polyhydric alcohols are blended, it is the total amount thereof.

[0017] <(E) Thickener> The external preparation for skin of the present invention is characterized by containing at least one selected from polyhydric alcohols, thickeners, and oils. The thickeners that can be used in the external preparation for skin of the present invention are not particularly limited as long as they are water-soluble components that can be used in cosmetics, external pharmaceuticals, quasi-drugs, etc., and synthetic polymers, semi-synthetic polymers, natural polymers, viscous minerals, etc. can be used.

[0018] Examples of synthetic polymers include hydrophilic synthetic polymers such as carboxyvinyl polymer, polyvinyl alcohol, acrylic acid / alkyl methacrylate copolymer, acrylates / alkyl acrylate cross-polymer, polyacrylic acid, polyacrylamide, polyalkylacrylamide / polyacrylamide copolymer, carboxymethyl cellulose, and cationized cellulose.

[0019] Examples of semi-synthetic polymers include cellulose derivatives such as carboxymethyl cellulose or its salts, methyl cellulose, ethyl cellulose, propyl cellulose, hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl methyl cellulose, sulfonated cellulose derivatives, etc. Other semi-synthetic polymers include propylene glycol alginate, ethylene glycol alginate, dextrin fatty acid ester, gelatin fatty acid ester, gelatin fatty acid amide, etc.

[0020] Examples of natural polymers include polysaccharides and their derivatives such as xanthan gum, succinoglycan, carrageenan, guar gum, locust bean gum, celluloses, galactan, gum arabic, tragacanth gum, tamarind gum, agar, agarose, mannan, curdlan, alginic acid or its salts, gum arabic, pectin, quince seed, starch, algocolloid, casein, collagen, gelatin, albumin, fibroin, elastin, keratin, sericin and other water-soluble proteins.

[0021] Examples of clay minerals include laponite, bentonite, smectite kaolinite, montmorillonite, etc.

[0022] When a thickener is blended in the external preparation for skin of the present invention, its content is not particularly limited. For example, it is preferably 0.001% by mass or more, more preferably 0.005% by mass or more, and particularly preferably 0.01% by mass or more from the viewpoint of obtaining an external preparation for skin having excellent usability. Also, it is preferably 20% by mass or less, more preferably 15% by mass or less, and particularly preferably 10% by mass or less. When two or more thickeners are blended, it is the total amount thereof.

[0023] <(F) Oil agent> The external preparation for skin of the present invention is characterized by containing at least one selected from polyhydric alcohols, thickeners, and oils. The oils that can be used in the present invention are not particularly limited as long as they are those usually used in external preparations for skin, but oils that are liquid at 25°C are preferred, and those that are non-volatile are particularly preferred. Specifically, for example, hydrocarbon oils such as liquid paraffin, squalane, and squalene; fatty acids such as isostearic acid, oleic acid, and polyhydroxystearic acid; higher alcohols such as octyldodecanol and tetradecyldecanol; isopropyl palmitate, isopropyl myristate, isopropyl stearate, isobutyl stearate, 2-ethylhexyl stearate, isopropyl isostearate, butyl isostearate, decyl isostearate, lauryl isostearate, isodecyl isodecanoate, isodecyl isononanoate, isotridecyl isononanoate, isononyl isononanoate, distearyl malate, neopentyl glycol dioctanoate, propylene glycol dicaprate, propylene glycol dicaprylate, glyceryl tri(2-ethylhexanoate), polyglyceryl monoisostearate, polyglyceryl diisostearate, diglyceryl triisostearate, diglyceryl tetraisostearate, diethyl sebacate, cetyl 2-ethylhexanoate, ethylhexyl palmitate, octyldodecyl myristate, oleyl oleate, ethyl oleate, N-lauroyl-glutamic acid di(phytosteryl / 2-octyldodecyl), N-lauroyl-glutamic acid di(phytosteryl / behenyl / 2-octyldodecyl), N-lauroyl-glutamic acid di(cholesteryl / 2-octyldodecyl), isopropyl N-lauroyl-sarcosinate and other ester oils; silicone oils such as dimethylpolysiloxane, cyclopentasiloxane, and alkoxy-modified polysiloxane; etc. can be mentioned, and one or more of these can be used.

[0024] When formulating an oily agent in the external preparation for skin of the present invention, its content is not particularly limited. For example, 0.1% by mass or more is preferable, more preferably 0.5% by mass or more, and particularly preferably 1% by mass or more from the viewpoint of obtaining an external preparation for skin with excellent usability. Also, 30% by mass or less is preferable, more preferably 25% by mass or less, and particularly preferably 20% by mass or less. When two or more kinds of oily agents are formulated, it is the total amount thereof.

[0025] <(G) Bactericide> In the external preparation for skin of the present invention, in addition to at least one selected from polyhydric alcohols, thickeners, and oily agents together with niacinamide, tranexamic acid, and D-panthenyl alcohol, it is preferable to formulate a bactericide. A bactericide is a component that suppresses the growth of skin resident bacteria that produce substances causing skin troubles such as acne and eruptions. The bactericide that can be used in the present invention is not particularly limited as long as it is usually used in external preparations for skin. For example, isopropylmethylphenol, benzalkonium chloride, benzethonium chloride, chlorhexidine hydrochloride, phenol, trichlorocarbanilide, chlorhexidine gluconate, triclosan, triclocarban, piroctone olamine, zinc pyrithione, salicylic acid or its salts, sorbic acid or its salts, lysozyme chloride, sulfur, etc. can be mentioned, and one kind or two or more kinds thereof can be used. Among these, isopropylmethylphenol, benzalkonium chloride, benzethonium chloride, piroctone olamine, salicylic acid or its salts are preferable, and isopropylmethylphenol, salicylic acid or its salts are more preferable.

[0026] When formulating a bactericide in the external preparation for skin of the present invention, its content is not particularly limited. For example, 0.001% by mass or more is preferable, more preferably 0.005% by mass or more, and particularly preferably 0.01% by mass or more from the viewpoint of obtaining an external preparation for skin with excellent usability. Also, 10% by mass or less is preferable, more preferably 5% by mass or less, and particularly preferably 1% by mass or less. When two or more kinds of bactericides are formulated, it is the total amount thereof.

[0027] <Other components> In addition to the above components, other components can be blended into the external preparation for skin of the present invention as needed. Examples of other components include monohydric alcohols, humectants, dispersants, plasticizers, spreading agents, preservatives, fragrances, surfactants, film-forming agents, pH adjusters, deodorants, chelating agents, antioxidants, antibacterial and antifungal agents, anti-inflammatory agents, whitening agents, and other active ingredients, animal extracts, plant extracts, beauty components and medicinal components such as vitamins other than niacinamide and D-pantothenyl alcohol, and one or more of the components usually used in external preparations for skin.

[0028] <External preparation for skin> The external preparation for skin of the present invention is a composition to be applied to the skin for use. The external preparation for skin of the present invention preferably has a high viscosity, preferably 500 mPa·s or more, more preferably 1,000 mPa·s or more, and particularly preferably 1,500 mPa·s or more from the viewpoint of excellent usability. The viscosity of the external preparation for skin of the present invention can be measured, for example, with a B-type viscometer (Brookfield rotational viscometer, temperature: 25°C, rotation speed: 5 rpm).

[0029] Also, the external preparation for skin of the present invention preferably has a pH of 4 to 8, and more preferably 5 to 7 from the viewpoint of excellent usability. The pH of the external preparation for skin of the present invention can be measured, for example, by the glass electrode method using a pH meter.

[0030] The external preparation for skin of the present invention can be used in pharmaceuticals, quasi-drugs, and cosmetics, and can be used, for example, in skin care cosmetics such as lotions, emulsions, creams, and beauty essences. Among these, the external preparation for skin of the present invention is preferably a lotion or a beauty essence.

[0031] The external preparation for skin of the present invention can be produced according to a conventional method. For example, when obtaining an oil-in-water type composition, an aqueous phase in which (A) niacinamide, (B) tranexamic acid, (C) panthenyl alcohol, and optionally a humectant, a thickener, an emulsifier, etc. are uniformly dispersed in water is prepared, a previously homogenized oil agent is added, and uniform emulsification is carried out using a homomixer or the like. The external preparation for skin of the present invention can be obtained by adjusting the pH as necessary.

Examples

[0032] Hereinafter, the present invention will be described based on examples, but the present invention is not limited to these examples and can take various forms. The amounts of the respective components used in the examples are in mass% unless otherwise specified.

[0033] <Preparation of External Preparation for Skin> According to Table 1, the oil-in-water type gel-like external preparations for skin of the examples and comparative examples were prepared by the following method. Specifically, an aqueous phase in which (A), (B), (C), (D), (E), phenoxyethanol, polysorbate 60, and glyceryl stearate were uniformly dispersed in water was prepared, the homogenized (F) was added, and uniform emulsification was carried out using a homomixer. Then, the pH was adjusted using sodium hydroxide to obtain an oil-in-water type gel-like external preparation for skin. When (G) was blended, an oil-in-water type gel-like external preparation for skin was obtained in the same manner as above except that it was previously dispersed in the aqueous phase together with (A) to (E) and the like.

[0034]

Table 1

[0035] <Measurement of Physical Properties of External Preparation for Skin> (1) Viscosity Measurement The viscosity of the obtained external preparation for skin was measured using a B-type viscometer (RVT type manufactured by Brookfield, temperature: 25°C, rotation speed: 5 rpm). The results are shown in Table 2.

[0036] <Evaluation of External Preparation for Skin> (1) Evaluation of Stability The stability of the obtained topical skin preparation was evaluated in terms of precipitation during storage. Specifically, 10 g of each sample from the examples and comparative examples was weighed into a 30-mL glass container and stored at 5°C for 2 months. After storage, the obtained samples were evaluated for precipitation. The results are shown in Table 2.

[0037] (2) Evaluation of usability The usability of the obtained topical skin preparation was evaluated. Five subjects aged in their 20s to 40s with experience in using topical skin preparations were randomly selected. The topical skin preparations obtained in the above examples and comparative examples were used on the forearms of the subjects, and the usability (good extensibility during application) was comprehensively judged as an evaluation item, and a questionnaire was conducted based on a 5-point evaluation criterion. The average value of each item of the questionnaire was calculated and used as the evaluation result. Samples were used and evaluated immediately after production (day 0 from the production date) and after storage at 5°C for 2 months after production. The results are shown in Table 2. (Good extensibility during application) ·5: Very good (smooth and extensible) ·4: Good (extensible) ·3: Neither (extensibility that does not matter during use) ·2: Bad (poor extensibility and noticeable during use) ·1: Very bad (very poor extensibility and unsuitable for use)

[0038] (3) Evaluation of stratum corneum water content The stratum corneum water content of the obtained topical skin preparation was evaluated. First, the measurement site (5×5 cm) on the inner side of the forearm of the subjects (1 male and 1 female in their 20s) was washed with facial cleanser and allowed to rest for 15 minutes. Next, 2 g of the topical skin preparations obtained in the above examples and comparative examples was applied to the measurement site. After 15 minutes, the stratum corneum water content was measured using a stratum corneum water content measuring device SKICON-200EX (manufactured by IBS Co., Ltd.), and the average value of all the subjects was calculated. The samples were evaluated using the samples on the production day 0, and the subjects remained at rest in the measurement room during the measurement. The results are shown in Table 2.

[0039]

Table 2

[0040] The compositions of the present invention all had a viscosity of 1500 mPa·s or more. In addition, while no precipitation was observed in any of the compositions of the present invention when stored at 5°C, precipitation was observed in Comparative Example 4, which does not contain D to F, which shows that the compositions of the present invention have high storage stability. In addition, the compositions of the present invention, Examples 1 to 7, had better spreadability when applied and a higher stratum corneum moisture content than Comparative Examples 1 to 7, and were therefore compositions with excellent usability and moisturizing properties. Furthermore, they were also excellent in usability even after storage at 5°C for 2 months. In particular, it was found that Examples 1 to 3, which contain niacinamide, tranexamic acid, D-pantothenyl alcohol, as well as polyhydric alcohol, thickener, oil, and bactericide, have particularly high usability and moisturizing properties.

[0041] From the above results, it is understood that the composition of the present invention contains one or more selected from polyhydric alcohols, thickeners, and oils in addition to niacinamide, tranexamic acid, and D-pantothenyl alcohol, thereby making it possible to obtain an external skin preparation that is highly stable and has excellent usability and moisturizing properties. In particular, it is understood that the composition of the present invention contains a polyhydric alcohol, thickener, oil, and bactericide in addition to niacinamide, tranexamic acid, and D-pantothenyl alcohol, thereby making it possible to obtain an external skin preparation that has even better usability and moisturizing properties.

[0042] <Preparation of topical skin preparation> The oil-in-water type gel-type topical skin preparations shown in Tables 3 and 6 were prepared in the same manner as in the Examples. All of the obtained topical skin preparations had a viscosity of 5,000 mPa s or more, and were easy to apply and had a good moisturizing feel after use.

[0043] [Table 3]

[0044] [Table 4]

[0045]

Table 5

[0046]

Table 6

Industrial Applicability

[0047] The external preparation for skin of the present invention contains at least one selected from polyhydric alcohols, thickeners, and oils together with niacinamide, tranexamic acid, and D-panthenyl alcohol, whereby it is possible to provide an external preparation for skin having high stability, excellent usability and moisturizing property, and having high industrial applicability.

Claims

1. (A) 3% by mass or more of niacinamide, (B) tranexamic acid, (C) D-pantothenyl alcohol, and (D) at least one selected from polyhydric alcohols, (E) thickeners, and (F) oily agents A topical skin preparation characterized by containing the same.

2. The topical skin preparation according to Claim 1, further characterized by containing (G) a bactericide.

3. The topical skin preparation according to Claim 2, wherein (G) is at least one selected from salicylic acid or its salt and isopropylmethylphenol.

4. The topical skin preparation according to any one of Claims 1 or 2, which is an oil-in-water emulsion.

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