JP7485386B2 - Skin preparations - Google Patents

Description

The present invention relates to a skin preparation for external use that contains a heparinoid. In particular, the present invention relates to an oil-in-water emulsified skin preparation for external use that contains a heparinoid.

In recent years, various topical preparations using heparinoids have been proposed. Heparinoids have been widely used as active ingredients in topical preparations because they have excellent moisturizing, anti-inflammatory, and blood circulation promoting effects (Patent Document 1). However, cosmetics containing heparinoids have problems in that they do not blend well with the skin and are difficult to penetrate and moisturize. In addition, because of their high medicinal properties, there is a demand for heparinoids to be used in a variety of cosmetics, not just basic cosmetics such as various creams and lotions, but the development of such products has been insufficient.

Japanese Patent Publication No. 62-004362

The inventors therefore conducted various studies with the goal of providing a skin preparation that enhances the effects of heparinoids and has an excellent feel when used.

As a result, the inventors succeeded in developing a topical skin preparation that combines moisturizing properties and a pleasant feel by combining a heparinoid with an ultraviolet scattering agent and a specific powder, thus completing the present invention.

That is, the present invention is as follows.
<1> A skin topical preparation comprising the following (a) to (c):
(a) a heparinoid; (b) an ultraviolet scattering agent; and (c) a powder having an average particle size of 1 to 100 μm. <2> The topical skin preparation according to <1>, further comprising (d) an oil.
<3> The topical skin preparation according to either <1> or <2>, which is an oil-in-water emulsion.
<4> The topical skin preparation according to any one of <1> to <3>, characterized in that the viscosity is 3,000 mPa·s or more.
<5> The external skin preparation according to any one of <1> to <4>, wherein the average particle size of the ultraviolet scattering agent (b) is 5 to 500 nm.
<6> The topical skin preparation according to any one of <1> to <5>, characterized in that the content of the heparinoid (a) in the composition is 0.0001% by mass or more and 0.5% by mass or less.
<7> The external skin preparation according to any one of <1> to <6>, which is used for sunscreen.

According to the present invention, by containing a heparinoid, an ultraviolet light scattering agent, and a specific powder, it is possible to obtain a skin preparation that has high moisturizing effects, wrinkle concealing effects, and an excellent feel when used.

The topical skin preparation of the present invention will be described in detail below. Note that the present invention is not limited to the embodiments shown below, and can be modified within the scope of what a person skilled in the art can imagine, including other embodiments, additions, modifications, deletions, etc., and any embodiment is within the scope of the present invention as long as it achieves the action and effect of the present invention.

(a) Heparinoids
The skin topical preparation of the present invention is characterized by containing a heparinoid, which is a polysulfated mucopolysaccharide such as chondroitin polysulfate obtained by polysulfating a polysaccharide having a repeating unit of a disaccharide consisting of D-glucuronic acid and N-acetyl-D-galactosamine, and is known to have moisturizing, anti-inflammatory, blood circulation promoting, and other effects.

The content of the heparinoid (a) in the topical skin preparation of the present invention is not particularly limited, and is, for example, preferably 0.00001 mass% or more, more preferably 0.00005 mass% or more, and particularly preferably 0.0001 mass% or more from the viewpoint of obtaining a topical skin preparation with high moisturizing effect, wrinkle concealing effect, and excellent usability. Also, 5 mass% or less is preferable, 1 mass% or less is more preferable, and 0.5 mass% or less is particularly preferable from the viewpoint of obtaining a topical skin preparation with high moisturizing effect, wrinkle concealing effect, and excellent usability.

<(b) Ultraviolet Scattering Agent>
The skin external preparation of the present invention contains an ultraviolet scattering agent.The ultraviolet scattering agent that can be used in the present invention is not particularly limited as long as it is one that is usually used in skin external preparations, but from the viewpoint of high ultraviolet scattering effect, inorganic compounds are preferred, and metal oxides are more preferred.Specifically, one or more selected from titanium oxide, zinc oxide, iron oxide, zirconium oxide, and cerium oxide can be mentioned.Among these, titanium oxide and zinc oxide are preferred.

The UV scattering agent used in the present invention is preferably one that has been subjected to a hydrophobic treatment. By hydrophobizing the surface, it is possible to improve dispersibility in oil and water resistance. The UV scattering agent may be hydrophobized using a known surface treatment agent that provides hydrophobicity, and examples of such treatment include silicone treatment such as methylhydrogenpolysiloxane, methylpolysiloxane, etc.; alkylsilane treatment; fluorine treatment using perfluoroalkyl phosphate ester, perfluoroalcohol, etc.; amino acid treatment using N-acylglutamic acid, etc.; lecithin treatment; metal soap treatment; fatty acid treatment; alkyl phosphate ester treatment, etc.

The UV scattering agent used in the present invention preferably has an average particle size 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 topical agent with high moisturizing effect, wrinkle concealing effect, and excellent usability. The average particle size of the UV scattering agent used in the present invention is measured by dynamic light scattering.

The content of the ultraviolet scattering agent (b) in the topical skin preparation of the present invention is not particularly limited, and is preferably 1 mass% or more, more preferably 3 mass% or more, and from the viewpoint of obtaining a topical skin preparation with high moisturizing effect, wrinkle concealing effect, and excellent usability, it is particularly preferably 5 mass% or more. Also, it is preferably 50 mass% or less, more preferably 40 mass% or less, and from the viewpoint of obtaining a topical skin preparation with high moisturizing effect, wrinkle concealing effect, and excellent usability, it is particularly preferably 30 mass% or less.

<(c) Powder having an average particle size of 1 to 100 μm>
The external skin preparation of the present invention contains a powder having an average particle size of 1 to 100 μm.

Examples of powders that can be used in the present invention include mica, talc, kaolin, sericite, montmorillonite, kaolinite, mica, muscovite, phlogopite, synthetic mica, red mica, black mica, permiculite, magnesium carbonate, calcium carbonate, aluminum silicate, barium silicate, calcium silicate, magnesium silicate, strontium silicate, tungstate metal salts, magnesium, zeolite, barium sulfate, calcined calcium sulfate, calcium phosphate, fluorapatite, hydroxyapatite, ceramic powder, bentonite, smectite, clay, mud, metal soap (e.g., zinc myristate, calcium palmitate, aluminum stearate), calcium carbonate, red ocher, yellow iron oxide, black iron oxide, ultramarine, Prussian blue, carbon black, titanium oxide, zinc oxide, alumina, silica, fumed silica (ultrafine silica anhydrous). , titanium mica, fish scale foil, boron nitride, photochromic pigments, synthetic fluorine-containing mica, fine particle composite powder, gold, aluminum, and other inorganic powders, and powders which have been hydrophobized or hydrophilized by treating these with various surface treatment agents such as silicones such as hydrogen silicone and cyclic hydrogen silicone, other silanes, or titanium coupling agents; organic powders and surface-treated powders such as starch, cellulose, nylon powder, polyethylene powder, polymethyl methacrylate powder, polystyrene powder, styrene and acrylic acid copolymer resin powder, polyester powder, benzoguanamine resin powder, polyethylene terephthalate-polymethyl methacrylate laminate powder, polyethylene terephthalate-aluminum-epoxy laminate powder, urethane powder, silicone powder, Teflon (registered trademark) powder, and other organic-inorganic composite powders.

The average particle size of the powder used in the topical skin preparation of the present invention is 1 to 100 μm, preferably 1 to 50 μm, and particularly preferably 1 to 30 μm from the viewpoint of obtaining a topical skin preparation with high moisturizing effect, wrinkle concealing effect, and excellent usability. The average particle size of the powder in the present invention is measured by a laser diffraction/scattering method.

The content of (c) powder having an average particle size of 1 to 100 μm in the topical skin preparation of the present invention is not particularly limited, and is, for example, preferably 0.01% by mass or more, more preferably 0.05% by mass or more, and particularly preferably 0.1% by mass or more from the viewpoint of obtaining a topical skin preparation with high moisturizing effect, wrinkle concealing effect, and excellent usability. Also, 20% by mass or less is preferable, 15% by mass or less is more preferable, and 10% by mass or less is particularly preferable from the viewpoint of obtaining a topical skin preparation with high moisturizing effect, wrinkle concealing effect, and excellent usability.

<(d) Oil Agent>
The skin external preparation of the present invention preferably contains an oily agent. The oily agent that can be used in the present invention is not particularly limited as long as it is one that is usually used in skin external preparations, but an oily agent that is liquid at 25° C. is preferable, and a non-volatile oily agent is particularly preferable. Specific examples of such oils include liquid paraffin, squalane, squalene, and other hydrocarbon oils; isostearic acid, oleic acid, polyhydroxystearic acid, and other fatty acids; octyldodecanol, tetradecyldecanol, and other higher alcohols; 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, diisostearyl malate, neopentyl glycol dioctanoate, propylene glycol dicaprate, propylene glycol dicaprylate, glyceryl tri-2-ethylhexanoate, monoisopropyl glyceryl tristearate, glyceryl mono ... Examples of the oils include ester oils such as polyglyceryl isostearate, 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), and N-lauroyl-sarcosine-isopropyl; and silicone oils such as dimethylpolysiloxane, cyclopentasiloxane, and alkoxy-modified polysiloxane. One or more of these oils may be used.

When an oil (d) is blended into the topical skin preparation of the present invention, its content is not particularly limited, but is preferably 1 mass% or more, more preferably 3 mass% or more, and from the viewpoint of obtaining a topical skin preparation with high moisturizing effect, wrinkle concealing effect, and excellent usability, it is particularly preferably 5 mass% or more. Also, it is preferably 50 mass% or less, more preferably 40 mass% or less, and from the viewpoint of obtaining a topical skin preparation with high moisturizing effect, wrinkle concealing effect, and excellent usability, it is particularly preferably 30 mass% or less.

<Other ingredients>
In addition to the above-mentioned components, the skin external preparation of the present invention may contain other components as necessary. Examples of other components include water, thickeners, gelling agents, moisturizing agents, dispersants, plasticizers, spreading agents, preservatives, fragrances, surfactants such as anionic surfactants, amphoteric surfactants, and nonionic surfactants, film-forming agents, pH adjusters, deodorants, chelating agents, antioxidants, antibacterial agents, antibacterial and antifungal agents, anti-inflammatory agents, and skin-whitening agents, as well as cosmetic and medicinal components such as animal and plant extracts, and one or more components that are usually used in skin external preparations.

<External skin preparations>
The skin topical agent of the present invention is a composition that is applied to the skin and used. The skin topical agent of the present invention is preferably an emulsion, and particularly preferably an oil-in-water emulsion. By making it an oil-in-water emulsion, it is possible to achieve both high moisturizing effect and wrinkle concealing effect when applied to the skin, as well as good usability. The skin topical agent of the present invention is preferably one that has a high viscosity, preferably 3,000 mPa·s or more, more preferably 3,500 mPa·s or more, and particularly preferably 4,000 mPa·s or more. In addition, it is preferably 500,000 mPa·s or less, more preferably 300,000 mPa·s or less, and particularly preferably 200,000 mPa·s or less.

The topical skin preparation of the present invention is preferably an emulsion. The emulsion form may be any of oil-in-water, water-in-oil, water-in-oil-in-water, and oil-in-water-in-oil, but an oil-in-water emulsion is preferred because it has a high moisturizing effect, wrinkle concealing effect, and excellent usability.

The topical skin preparation of the present invention can be used in medicines, quasi-drugs, and cosmetics. For example, it can be used in various forms of products, such as medicines such as topical skin preparations containing drugs; quasi-drugs such as medicated cosmetics; skin care cosmetics such as gel-type lotions, milky lotions, creams, beauty serums, sunscreens, and daytime moisturizers; and makeup cosmetics such as foundations and makeup bases. Of these, the topical skin preparation of the present invention is preferably a sunscreen or makeup base, with sunscreens being particularly preferred.

The topical skin preparation of the present invention can be manufactured according to a conventional method. That is, the aqueous phase component and the oil phase component are each prepared at a predetermined temperature of about 25°C, heated to 80°C for emulsification, and then cooled to room temperature while stirring to obtain the topical skin preparation of the present invention.

The present invention will now be described with reference to examples.

<Evaluation of topical skin preparations>
According to the compositions shown in Table 1 below, topical skin preparations (Examples 1 to 8, Comparative Examples 1 and 2) that are oil-in-water emulsions were produced. Specifically, 1,3-butylene glycol, (a), and phenoxyethanol were added to water and mixed to prepare an aqueous phase component, and (b), (c), and sodium acrylate-sodium acryloyldimethyltaurate copolymer were added to the oil agent (d) and mixed to prepare an oil phase component. The aqueous phase component was heated to 80° C. to emulsify, and then cooled to about room temperature while stirring. The obtained topical skin preparations were evaluated for the following items. The results are shown in Table 1.
Viscosity measurements
The viscosity of the obtained skin preparation was measured using a viscometer (Model RVT, manufactured by Brookfield).
Evaluation of usability
Five subjects in their 20s to 30s were randomly selected as subjects. The skin topical preparation was applied to the face of each subject, and the subject was asked to evaluate the feel of the product (spreadability upon application, smoothness, non-stickiness after application, non-squeakiness, and moderate moisturizing sensation) comprehensively, and a questionnaire was administered based on a five-point scale. The average value of the questionnaire was calculated and evaluated.
・5: Very good ・4: Good ・3: Neither good nor bad ・2: Bad ・1: Very bad
Evaluation of wrinkle hiding effect
Five subjects in their 20s to 30s were randomly selected as subjects. The subjects used the skin topical agent on their faces, and were asked to rate the extent to which wrinkles had become less noticeable after use, based on a five-point scale. The average value of the questionnaire was calculated and evaluated.
・5: Very good (wrinkles are less noticeable than before use)
・4: Good ・3: No change before and after use ・2: Bad ・1: Very bad (wrinkles are more noticeable than before use)
Assessment of stratum corneum moisture content
Five subjects in their 20s to 30s were randomly selected as subjects. The moisture content of the stratum corneum was measured in a 4 cm x 4 cm measurement area on the inside of the forearm where the topical skin preparation was to be applied, using a skin epidermal moisture content measuring device SKICON-200EX (manufactured by IBS Co., Ltd.) by the following method. This skin epidermal moisture content measuring device evaluates the moisture content of the stratum corneum as the skin conductance (electrical conductivity, unit: μS). Next, the topical skin preparation was applied to the measurement site, and the moisture content of the stratum corneum was measured when the topical skin preparation was used.

As shown in Table 1, the compositions of the present invention, Examples 1 to 8, showed a high viscosity of 4,800 mPa·s or more. As is clear from Table 1, the skin topical preparations of Examples 1 to 8 have a high moisturizing effect due to the high moisture content of the stratum corneum during use, excellent wrinkle concealing effect, and further have a good feel when used, such as good spreadability when applied, good slipperiness, no stickiness after application, no squeaking, and a moderate moist feeling. In contrast, the skin topical preparation of Comparative Example 1 has a low wrinkle concealing effect and a poor feel when used, and the skin topical preparation of Comparative Example 2 not only has a low wrinkle concealing effect and a poor feel when used, but also has a low moisture content in the stratum corneum and a low moisturizing effect. From the above results, it is clear that the skin topical preparations of the present invention have a high moisturizing effect, excellent wrinkle concealing effect, and excellent feel when used.

<Production Examples 1 to 10>
According to the composition shown in Table 2 below, a skin topical preparation that is an oil-in-water emulsion was produced in the same manner as in Example 1. The skin topical preparation obtained in the following production example has a viscosity of 3,000 mPa·s or more, and is excellent in terms of moisturizing effect, wrinkle concealing effect, and usability.

The topical skin preparation of the present invention contains a heparinoid, an ultraviolet light scattering agent, and a specific powder, and thus provides a topical skin preparation that has high moisturizing effects, wrinkle concealing effects, and an excellent feel when used, and has high industrial applicability.

Claims (2)

A sunscreen skin preparation for external use, which contains the following (a) to (d), and is an oil-in-water emulsion (excluding sunscreen creams containing heparin, dipotassium glycyrrhizinate, potassium hydroxide, water, butylene glycol, phenoxyethanol, silica, isostearic acid, ethylhexyl methoxycinnamate, (acrylates/C10-30 alkyl acrylate) crosspolymer, 1,2-pentanediol, polyglyceryl-10 myristate, diethylamino hydroxybenzoylhexyl benzoate, and bis-ethylhexyloxyphenol methoxyphenyl triazine) :
(a) a heparinoid; (b) at least one type of ultraviolet scattering agent other than a powder selected from silica and pigment-grade titanium oxide;
(c) at least one powder selected from silica or pigment-grade titanium oxide; (d) at least one oil selected from ethylhexyl palmitate, isostearic acid, or polyhydroxystearic acid. 2. The skin topical preparation according to claim 1 , having a viscosity of 3,000 mPa·s or more.