Topical skin preparation

Abstract

To provide a topical skin preparation which contains niacinamide and an ultraviolet protection agent while exhibiting superior usability.SOLUTION: A topical skin preparation comprises: (A) niacinamide, (B) tranexamic acid, (C) D-panthenyl alcohol, and (D) an ultraviolet protection agent.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] Ultraviolet rays are known to cause various phenomena such as skin inflammation and aging. Sunscreen cosmetics are used to relieve skin inflammation. In addition, various active ingredients can be formulated in topical skin preparations. For example, niacinamide is known to be highly safe and have an anti-skin-aging effect (Patent Document 1). However, niacinamide tends to cause stickiness after application to the skin, and there is a problem that the feeling of use is poor. In addition, sunscreen cosmetics contain components having an ultraviolet ray protection effect, such as an ultraviolet ray scattering agent and an ultraviolet ray absorber. For example, the ultraviolet ray scattering agent has a problem that it has poor extensibility during application and is likely to generate a crunching sound after application (Patent Document 2).

Prior Art Documents

Patent Documents

[0003]

Patent Document 1

Patent Document 2

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 and an ultraviolet ray protection agent.

Means for Solving the Problems

[0005] As a result, the inventors have succeeded in developing a topical skin preparation with excellent usability by using a topical skin preparation containing niacinamide, a UV protectant, tranexamic acid, and D-pantothenyl alcohol, and have completed the present invention.

[0006] That is, the present invention is as follows. <1> A topical skin preparation characterized by containing (A) niacinamide, (B) tranexamic acid, (C) D-pantothenyl alcohol, and (D) a UV protectant <2> The topical skin preparation according to <1>, further characterized by containing (E) a bactericide. <3> The topical skin preparation according to <2>, wherein (E) is at least one selected from salicylic acid or its salt and isopropylmethylphenol. <4> The topical skin preparation according to <1>, wherein (A) niacinamide is 3% by mass or more. <5> The topical skin preparation according to <1>, wherein (B) tranexamic acid is 0.1% by mass or more. <6> The topical skin preparation according to <1>, wherein (C) D-pantothenyl alcohol is 0.01% by mass or more. <7> The topical skin preparation according to <2>, wherein (E) the bactericide is 0.01% by mass or more. <8> The topical skin preparation according to <1>, further characterized by containing at least one selected from (F) a polyhydric alcohol, (G) a thickener, and (H) an oil agent. <9> The topical skin preparation according to <1>, which is an oil-in-water emulsion.

[0007] According to the present invention, by containing niacinamide, an ultraviolet ray protecting agent, tranexamic acid, and D-panthenyl alcohol, a topical skin preparation excellent in usability can be provided. Further, by containing at least one selected from polyhydric alcohols, thickeners, and oils, and a bactericide together with niacinamide, tranexamic acid, D-panthenyl alcohol, and an ultraviolet ray protecting agent, a topical skin preparation excellent in usability and rubbing resistance can be provided.

Mode for Carrying Out the Invention

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

[0009] <(A) Niacinamide> The topical skin 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 vitamin B group and a water-soluble vitamin. In the present invention, as niacinamide, those 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 topical skin preparation of the present invention, the content of niacinamide is not particularly limited. For example, 0.1% by mass or more is preferable, 1% by mass or more is more preferable, and from the viewpoint of excellent usability and enjoying the effects of niacinamide, 3% by mass or more is particularly preferable, and especially 5% by mass or more is preferable. Also, the upper limit is not particularly limited, but 30% by mass or less is preferable, more preferably 20% by mass or less, and particularly preferably 10% by mass or less from the viewpoint of obtaining a topical skin preparation with excellent usability and enjoying the effects of niacinamide. The content of niacinamide in the topical skin preparation of the present invention can be analyzed, for example, by high performance liquid chromatography.

[0011] <(B) Tranexamic acid> The topical skin 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 enjoying 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, for example, according to the quantification method of tranexamic acid described in the 18th revised Japanese Pharmacopoeia.

[0013] <(C) D-Panthenyl alcohol> The external preparation for skin of the present invention is characterized by containing D-panthenyl alcohol. D-panthenyl alcohol, also called panthenol, is a derivative of vitamin B5 (pantothenic acid), which 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, commercially available products such as those extracted from natural products, those purified therefrom, and those synthesized by known methods can also be used.

[0014] In the external preparation for skin 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 enjoying 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 external preparation for skin of the present invention can be analyzed by, for example, high performance liquid chromatography, and the conditions can be, for example, quantified according to the quantification method of D-panthenyl alcohol described in the Quasi-drug Raw Material Standard 2021.

[0015] <(D) UV protectant> The external preparation for skin of the present invention is characterized by containing a UV protectant. The UV protectant 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, a UV scattering agent and a UV absorber can be used.

[0016] As the UV scattering agent, an inorganic compound is preferable and a metal oxide is more preferable from the viewpoint of high UV scattering effect. Specifically, one or more selected from titanium oxide, zinc oxide, iron oxide, zirconium oxide, and cerium oxide can be mentioned. Among these, it is preferable to use one or more selected from titanium oxide and zinc oxide.

[0017] In addition, the ultraviolet light scattering agent used in the present invention preferably undergoes a hydrophobization treatment. By hydrophobizing the surface, the dispersibility in oil and water resistance can be improved. The hydrophobization treatment of the ultraviolet light scattering agent may be carried out using a known surface treatment agent to be hydrophobized. For example, silicone treatment such as methylhydrogenpolysiloxane and methylpolysiloxane; alkylsilane treatment; fluorine treatment with perfluoroalkyl phosphate ester, perfluoroalcohol, etc.; amino acid treatment with N-acylglutamic acid, etc.; other treatments such as lecithin treatment; metal soap treatment; fatty acid treatment; alkyl phosphate ester treatment, etc. can be mentioned.

[0018] The ultraviolet light scattering agent used in the present invention preferably has an average particle diameter of 1 to 1000 nm, more preferably 5 to 500 nm, and particularly preferably 10 to 300 nm from the viewpoint of obtaining a skin external preparation excellent in usability and sunscreen effect. The average particle diameter of the ultraviolet light scattering agent used in the present invention is measured by the dynamic light scattering method.

[0019] In addition, examples of the ultraviolet absorber include ethylhexyl methoxycinnamate, octocrylene, dimethyldiethylbenzalmalonate, polysilicone-15, t-butylmethoxydibenzoylmethane, ethylhexyl triazone, diethylamino hydroxybenzoyl hexyl benzoate, bis-ethylhexyloxyphenol methoxyphenyl triazine, oxybenzone-3, methylene bisbenzotriazolyl tetramethylbutylphenol, phenylbenzimidazole sulfonic acid, homosalate, ethylhexyl salicylate, etc. Among these, it is preferable to use one or more selected from ethylhexyl methoxycinnamate, diethylamino hydroxybenzoyl hexyl benzoate, and bis-ethylhexyloxyphenol methoxyphenyl triazine.

[0020] The content of the ultraviolet ray protector in the external preparation for skin of the present invention is not particularly limited, preferably 1% by mass or more, more preferably 3% by mass or more, and particularly preferably 5% by mass or more from the viewpoint of obtaining an external preparation for skin excellent in usability and sunburn prevention effect. Also, it is preferably 50% by mass or less, more preferably 40% by mass or less, and particularly preferably 30% by mass or less. When two or more kinds of ultraviolet ray protectors are used, it is the total amount thereof.

[0021] In addition, the content of the ultraviolet ray scattering agent in the external preparation for skin of the present invention is not particularly limited, preferably 1% by mass or more, more preferably 3% by mass or more, and particularly preferably 5% by mass or more from the viewpoint of obtaining an external preparation for skin excellent in usability and sunburn prevention effect. Also, it is preferably 40% by mass or less, more preferably 30% by mass or less, and particularly preferably 25% by mass or less. When two or more kinds of ultraviolet ray scattering agents are used, it is the total amount thereof.

[0022] <(E)Bactericide> In addition to (A) to (D), it is preferable to incorporate a bactericide in the external preparation for skin of the present invention. 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. may be mentioned, and one kind or two or more kinds can be used from these. Among these, isopropylmethylphenol, benzalkonium chloride, benzethonium chloride, triclosan, piroctone olamine, salicylic acid or its salts are preferable, and isopropylmethylphenol, salicylic acid or its salts are more preferable.

[0023] When a bactericide is formulated 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. In the case of formulating two or more bactericides, it is the total amount thereof.

[0024] <(F) Polyhydric alcohol> In addition to (A) to (D), the external preparation for skin of the present invention preferably contains at least one selected from polyhydric alcohols, thickeners, and oils. Examples of 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 a dihydric to trihydric polyhydric alcohol 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.

[0025] When a polyhydric alcohol is formulated in the external preparation for skin of the present invention, its content is not particularly limited. For example, 0.01% by mass or more is preferable, 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, 50% by mass or less is preferable, more preferably 40% by mass or less, and particularly preferably 35% by mass or less. In the case of formulating two or more polyhydric alcohols, it is the total amount thereof.

[0026] <(G) Thickener> In addition to (A) to (D), the topical skin preparation of the present invention preferably contains at least one selected from polyhydric alcohols, thickeners, and oils. The thickeners that can be used in the topical skin preparation of the present invention are not particularly limited as long as they are water-soluble components that can be used in cosmetics, topical pharmaceuticals, quasi-drugs, etc., and synthetic polymers, semi-synthetic polymers, natural polymers, viscous minerals, etc. can be used.

[0027] Examples of synthetic polymers include hydrophilic synthetic polymers such as carboxyvinyl polymer, polyvinyl alcohol, acrylic acid / methacrylic acid alkyl copolymer, acrylates / acrylic acid alkyl crosspolymer, polyacrylic acid, polyacrylamide, polyalkylacrylamide / polyacrylamide copolymer, carboxymethyl cellulose, and cationized cellulose.

[0028] Examples of semi-synthetic polymers as cellulose derivatives include 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.

[0029] 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.

[0030] Examples of the clay mineral include laponite, bentonite, smectite, kaolinite, montmorillonite and the like.

[0031] 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 kinds of thickeners are blended, it is the total amount thereof.

[0032] <(H) Oil agent> In addition to (A) to (D), the skin external preparation of the present invention preferably contains 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 skin external preparations, 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.

[0033] When formulating an oily agent in the external preparation for skin of the present invention, its content is not particularly limited. For example, it is preferably 0.1% by mass or more, 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, it is preferably 30% by mass or less, 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.

[0034] <Other components> In addition to the above components, other components can be formulated in 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 ingredients and medicinal ingredients such as vitamins other than niacinamide and D-pantothenyl alcohol, and one or more of the components usually used in external preparations for skin.

[0035] <External preparation for skin> The external preparation for skin of the present invention is a composition to be applied to the skin and used. 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).

[0036] 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.

[0037] 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 lotions, creams, gels, beauty essences, makeup bases, sunscreens, and foundations. Among these, makeup bases and sunscreens are preferred, and sunscreens are particularly preferred.

[0038] 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 oil phase in which a sunscreen agent (D) is uniformly dispersed in an oil agent is added to an aqueous phase in which niacinamide (A), tranexamic acid (B), pantothenyl alcohol (C), and optionally a humectant, a thickener, and an emulsifier are uniformly dissolved in water, and uniformly emulsified with a homomixer or the like, and the pH is adjusted as necessary to obtain the external preparation for skin of the present invention.

Examples

[0039] 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.

[0040] <Preparation of External Preparation for Skin> According to Table 1, oil-in-water type external preparations for skin of Examples and Comparative Examples were prepared by the following method. Specifically, an aqueous phase in which (A), (B), (C), (F), (G), phenoxyethanol, polysorbate 60, and sorbitan stearate were uniformly dispersed in water was prepared. An oil phase in which (D) was uniformly dispersed in (H) was added to the aqueous phase, and uniform emulsification was performed using a homomixer. Thereafter, the pH was adjusted using sodium hydroxide to obtain an oil-in-water type external preparation for skin. When (E) was blended, an oil-in-water type 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 (C) and the like.

[0041]

Table 1

[0042] <Measurement of Physical Properties of External Preparation for Skin> (1) Viscosity Measurement The viscosity of the obtained topical skin preparation 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.

[0043] <Evaluation of Topical Skin Preparation> (1) Evaluation of usability The usability of the obtained topical skin preparation was evaluated. Five subjects aged in their 20s to 40s with experience using sunscreen cosmetics were randomly selected. The subjects applied the topical skin preparations obtained in the above Examples and Comparative Examples to their forearms, and comprehensively judged the usability (good elongation during application) as an evaluation item, and conducted a questionnaire based on a five-point evaluation criterion. The average value of each item of the questionnaire was calculated and used as the evaluation result. Samples were evaluated using each sample after production (day 0 from the production date) and after storage at 40 °C for 1 month after production. The results are shown in Table 2. (Good elongation during application) ·5: Very good (smooth and stretches well) ·4: Good (stretches well) ·3: Neither (elongation that is not noticeable during use) ·2: Bad (poor elongation and noticeable during use) ·1: Very bad (very poor elongation and unsuitable for use)

[0044] (2) Evaluation of abrasion resistance The abrasion resistance of the obtained topical skin preparation was evaluated. Abrasion resistance is an evaluation indicating resistance to friction, such as wiping off with a towel or makeup smudging due to rubbing between the skin and a mask. A 2 mg / cm 2 sample was uniformly applied to a PMMA plate, and the SPF was measured using SPF MASTER (manufactured by Shiseido Co., Ltd.). After the measurement, the surface of the plate was wiped with a 300 g load for 10 seconds, and then the SPF was measured again. The difference between the SPF value before wiping and the SPF value after wiping was calculated, and the change in SPF due to wiping was calculated. A smaller change value indicates better abrasion resistance. Samples were evaluated using each sample after production (day 0 from the production date). The results are shown in Table 2.

[0045]

Table 2

[0046] All the compositions of the present invention had a viscosity of 1500 mPa·s or more. Further, Examples 1 to 7 which are the compositions of the present invention had good elongation during application and excellent usability compared to Comparative Examples 1 to 7 both after production (day 0) and after storage at 40°C for 1 month. Furthermore, from the evaluation of abrasion resistance, it can be seen that Examples 1 to 7 which are the compositions of the present invention are more resistant to friction and less likely to cause makeup smudging compared to Comparative Examples 1 to 5.

[0047] From the above results, it can be seen that the composition of the present invention can obtain a skin external preparation excellent in usability and abrasion resistance by containing tranexamic acid and D-pantothenyl alcohol together with niacinamide and an ultraviolet protector. In particular, it can be seen that by containing a polyhydric alcohol, a thickener, an oil agent, and a bactericide together with niacinamide, tranexamic acid, D-pantothenyl alcohol, and an ultraviolet protector, a skin external preparation more excellent in usability and abrasion resistance can be obtained.

[0048] <Preparation of Skin External Preparation> The oil-in-water type skin external preparations described in Tables 3 to 5 were prepared in the same manner as in the examples. All of the obtained skin external preparations had a viscosity of 5,000 mPa·s or more and were excellent in ease of application and abrasion resistance during use.

[0049]

Table 3

[0050]

Table 4

[0051]

Table 5

Industrial Applicability

[0052] The external preparation for skin of the present invention contains tranexamic acid and D-panthenyl alcohol together with niacinamide and an ultraviolet protector, and thus can provide an external preparation for skin excellent in usability and rub resistance, and has high industrial applicability.

Claims

1. (A)Niacinamide, (B)Tranexamic acid, (C)D-Pantothenyl alcohol, and (D)An ultraviolet protecting agent A topical skin preparation characterized by containing the same.

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

3. The topical skin preparation according to Claim 2, wherein (E) 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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