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WO2024241430A1 - Préparation externe pour la peau - Google Patents

Préparation externe pour la peau Download PDF

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Publication number
WO2024241430A1
WO2024241430A1 PCT/JP2023/018955 JP2023018955W WO2024241430A1 WO 2024241430 A1 WO2024241430 A1 WO 2024241430A1 JP 2023018955 W JP2023018955 W JP 2023018955W WO 2024241430 A1 WO2024241430 A1 WO 2024241430A1
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WIPO (PCT)
Prior art keywords
mass
parts
amount
skin
present
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PCT/JP2023/018955
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English (en)
Japanese (ja)
Inventor
明穂 桑畑
健志 吉田
昌明 森山
伸次 小林
Original Assignee
プレミアアンチエイジング株式会社
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Application filed by プレミアアンチエイジング株式会社 filed Critical プレミアアンチエイジング株式会社
Priority to PCT/JP2023/018955 priority Critical patent/WO2024241430A1/fr
Publication of WO2024241430A1 publication Critical patent/WO2024241430A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67—Vitamins

Definitions

  • the present invention relates to a skin preparation for external use.
  • active ingredients have been proposed for topical skin preparations, and cosmetics and pharmaceuticals containing these active ingredients are on the market.
  • active ingredients include cell activating ingredients such as ⁇ -hydroxycarboxylic acids; extracellular matrix ingredients such as collagen, elastin, hyaluronic acid or salts thereof; and moisturizing agents such as urea.
  • cell activating ingredients such as ⁇ -hydroxycarboxylic acids
  • extracellular matrix ingredients such as collagen, elastin, hyaluronic acid or salts thereof
  • moisturizing agents such as urea.
  • antioxidants and moisturizing agents derived from plants have also been proposed.
  • Patent Document 1 describes that an external skin preparation containing niacinamide and an extract of the fruit of Ziziphus jujuba of the Rhamnaceae family as active ingredients can improve the barrier function of the skin, prevent and improve dry skin, and prevent and improve thinning of the skin, and also describes an essence containing niacinamide and ceramide (e.g., Patent Document 1).
  • Patent Document 2 describes an external skin preparation for improving wrinkles, which contains D-pantothenyl alcohol and niacinamide.
  • JP 2022-163643 A Patent Publication No. 2021-063076
  • the present invention aims to provide an external skin preparation which uses niacinamide and has excellent moisturizing effect and feeling of use.
  • a skin topical preparation which is a composition containing the following components (A), (B), (C), (D), (E) and (F) niacinamide, in which (C), (D) and (E) are encapsulated in liposomes containing (F) hydrogenated soybean phospholipid.
  • A Niacinamide.
  • B D-pantothenyl alcohol.
  • C 3-O-ethyl ascorbic acid.
  • D Pine bark extract.
  • E At least one selected from glutathione and ceramides.
  • F Hydrogenated soybean phospholipid.
  • the present invention uses niacinamide to provide a skin care product that has excellent moisturizing effects and a pleasant feel when used.
  • the "feel when used" refers to smoothness when applied and improvement in skin clarity and firmness after use.
  • the moisturizing effect refers to the effect of increasing the moisture content of the stratum corneum.
  • the present invention provides a skin external preparation which is a composition containing the above (A), (B), (C), (D), (E) and (F), and in which (C), (D) and (E) are encapsulated in liposomes containing (F) hydrogenated soybean phospholipid.
  • a liposome is a closed vesicle formed by a lipid bilayer containing a lipid such as lecithin, and has an aqueous phase (internal aqueous phase) in the space of the closed vesicle.
  • the liposome exists in a dispersed state in an aqueous solution (external aqueous phase) outside the closed vesicle.
  • the expression "a given component is encapsulated in a liposome” means that the component is not present only in the external aqueous phase, but that at least a portion of the component is present in the membrane of the liposome or in the internal aqueous phase within the liposome.
  • Niacinamide The skin topical preparation of the present invention contains (A) niacinamide in the presence of (B) to (F), thereby enhancing the moisturizing effect and improving the feeling of use, such as smoothness when applied and firmness of the skin after use.
  • Niacinamide is also known as nicotinamide.
  • Niacinamide may be an extract extracted from natural products such as rice bran, or a synthetic product synthesized by a known manufacturing method, or a commercially available product may be obtained and used. Specifically, nicotinamide listed in the 17th revised Japanese Pharmacopoeia may be used.
  • Niacinamide may be encapsulated in liposomes containing (F) hydrogenated soybean phospholipids, or may be present in the external aqueous phase outside the liposomes.
  • (A) niacinamide is contained in the topical skin preparation of the present invention at 1% by mass or more, and more preferably at 2% by mass or more.
  • (A) niacinamide is contained in the topical skin preparation at 3% by mass or more, particularly preferably at 4% by mass or more, and most preferably at 5% by mass or more.
  • the upper limit of the amount of (A) niacinamide in the topical skin preparation is preferably 15% by mass or less, from the viewpoint of obtaining a topical skin preparation with excellent usability, more preferably 12% by mass or less, and most preferably 10% by mass or less.
  • the skin topical preparation of the present invention contains (B) D-pantothenyl alcohol in the presence of (A), (C) to (F), and thereby has excellent moisturizing effect, smoothness upon application, and excellent skin transparency and firmness after use.
  • D-pantothenyl alcohol a commercially available product can be used, and specifically, D-pantothenyl alcohol listed in the Quasi-Drug Raw Materials Standards 2021 can be used.
  • the amount of (B) D-pantothenyl alcohol is preferably 0.01% by mass or more in the topical skin preparation in order to enhance the effects of the present invention by using (B) D-pantothenyl alcohol.
  • the amount of (B) D-pantothenyl alcohol in the topical skin preparation is even more preferably 0.05% by mass or more, and particularly preferably 0.1% by mass or more.
  • the amount of (B) D-pantothenyl alcohol in the topical skin preparation is preferably 20% by mass or less, even more preferably 10% by mass or less, and particularly preferably 5% by mass or less.
  • D-pantothenyl alcohol may be encapsulated in a liposome containing (F) hydrogenated soybean phospholipid, or may be present in the external aqueous phase outside the liposome.
  • the amount of D-pantothenyl alcohol (B) is preferably 0.1 to 100 parts by mass per 100 parts by mass of niacinamide (A), in order to further improve the effects of the present invention. From this perspective, the amount of D-pantothenyl alcohol (B) is even more preferably 1 part by mass or more, and particularly preferably 5 parts by mass or more, per 100 parts by mass of niacinamide (A). From the perspective of further improving the effects of the present invention, the amount of D-pantothenyl alcohol (B) is even more preferably 80 parts by mass or less, and particularly preferably 50 parts by mass or less, per 100 parts by mass of niacinamide (A).
  • the topical skin preparation of the present invention contains (C) 3-O-ethyl ascorbic acid in the presence of (A), (B), and (D) to (F), which not only enhances the moisturizing effect but also improves the smoothness upon application and the firmness of the skin after use.
  • the 3-O-ethyl ascorbic acid is not particularly limited, so long as it is used as an ingredient in pharmaceuticals, quasi-drugs, or cosmetics for external skin preparations.
  • Synthetic 3-O-ethyl ascorbic acid can be used.
  • One synthesis method is to ethoxylate the hydroxyl group at the 3-position of ascorbic acid, as described, for example, in JP-A-8-134055.
  • Commercially available 3-O-ethyl ascorbic acid can also be used as is.
  • component (C) 3-O-ethyl ascorbic acid is encapsulated in liposomes containing (F) hydrogenated soybean phospholipid.
  • This improves the stability of (C) 3-O-ethyl ascorbic acid in the topical skin preparation of the present invention, thereby enhancing the moisturizing effect as well as the effect of improving smoothness upon application and firmness of the skin after use.
  • component (C) is encapsulated in liposomes containing (F) hydrogenated soybean phospholipid by removing the liposomes from the topical skin preparation and then conducting confirmation tests for each component.
  • the presence of component (C) in the liposomes can be confirmed, for example, by removing the external aqueous phase outside the liposomes by gel filtration chromatography, followed by liquid chromatography or the like.
  • the amount of (C) 3-O-ethyl ascorbic acid is preferably 0.00001% by mass or more in the topical skin preparation in order to enhance the effects of the present invention by using (C) 3-O-ethyl ascorbic acid.
  • the amount of (C) 3-O-ethyl ascorbic acid in the topical skin preparation is even more preferably 0.00005% by mass or more, and particularly preferably 0.0001% by mass or more.
  • the amount of (C) 3-O-ethyl ascorbic acid in the topical skin preparation is preferably 10% by mass or less, even more preferably 5% by mass or less, and particularly preferably 1% by mass or less.
  • the amount of (C) 3-O-ethyl ascorbic acid is preferably 0.0001 to 50 parts by mass per 100 parts by mass of (A) niacinamide, in order to further improve the effects of the present invention. From this perspective, the amount of (C) 3-O-ethyl ascorbic acid is even more preferably 0.001 parts by mass or more, and particularly preferably 0.005 parts by mass or more, per 100 parts by mass of (A) niacinamide.
  • the amount of (C) 3-O-ethyl ascorbic acid is even more preferably 30 parts by mass or less, and particularly preferably 10 parts by mass or less, per 100 parts by mass of (A) niacinamide.
  • the topical skin preparation of the present invention contains (D) pine bark extract in the presence of (A) to (C), (E) and (F), which not only effectively enhances the moisturizing effect but also improves the smoothness upon application and the firmness of the skin after use.
  • pines that can be used as the source of the pine bark extract (D) include, but are not limited to, plants belonging to the order Pinales, such as French maritime pine, larch, black pine, red pine, Pinus sieboldii, Japanese red pine, Chinese red pine, Korean pine, Japanese pine, Ryukyu pine, Japanese white pine, white pine, and Aneda in the Quebec region of Canada.
  • French maritime pine Pierus pinaster
  • a maritime pine that grows on the Atlantic coast of southern France is preferred, as its safety as a skin topical agent has been confirmed and it contains high concentrations of antioxidants such as catechin.
  • Pine bark extract is obtained by extracting pine bark with a solvent.
  • the solvent include water, organic solvents, and aqueous organic solvents (aqueous alcohols such as aqueous ethanol).
  • the organic solvent used for the extraction is usually an organic solvent that is acceptable for extracting natural product components, and examples of the organic solvent include monohydric alcohols such as methanol, ethanol, 1-propanol, 2-propanol, 1-butanol, and 2-butanol, glycols such as propylene glycol, polyhydric alcohols such as glycerin, butane, acetone, hexane, cyclohexane, aqueous ethanol, aqueous propylene glycol, ethyl methyl ketone, methyl acetate, ethyl acetate, diethyl ether, dichloromethane, edible oils and fats, 1,1,1,2-tetrafluoroethane, and 1,1,2-trichloroethene.
  • the temperature during extraction may be appropriately adjusted from room temperature to a temperature below the boiling point of the extraction solvent.
  • at least one selected from water, aqueous ethanol, and aqueous propylene glycol is preferably used.
  • the extraction method is not particularly limited as long as it is a method that is generally acceptable for extracting natural product components, but examples include solid-liquid extraction methods such as heated extraction and supercritical fluid extraction.
  • Heat extraction is, for example, a method in which the test substance is brought into contact with a solvent and treated at a temperature below the boiling point of the solvent to extract the components contained in the test substance into the solvent.
  • Reflux extraction may also be used.
  • Supercritical fluid extraction is, for example, a method in which extraction is performed using a supercritical fluid, which is a fluid in a state that exceeds the gas-liquid critical point (critical temperature, critical pressure) of the substance. Examples of supercritical fluids include carbon dioxide, ethylene, propane, and nitrous oxide (laughing gas).
  • an entrainer addition method may be performed.
  • ethanol, propanol, n-hexane, acetone, toluene, other aliphatic lower alcohols, aliphatic hydrocarbons, aromatic hydrocarbons, and ketones are added to the extraction fluid at about 2 to 20 W/V %, and supercritical fluid extraction is performed using this fluid.
  • extraction from pine bark may be performed by a liquid carbon dioxide batch method, a liquid carbon dioxide reflux method, a supercritical carbon dioxide reflux method, or the like.
  • an extraction step in which the target component is extracted with a supercritical fluid and a separation step in which the target component is separated from the supercritical fluid are performed.
  • the separation step extraction and separation by pressure change, extraction and separation by temperature change, or extraction and separation using an adsorbent or absorbent may be performed.
  • the pine bark extract (D) may be in a liquid form, or may be in a paste or dry powder form. When the pine bark extract is in a paste or dry powder form, it may be produced by itself or may be processed together with an excipient.
  • the pine bark extract obtained by extraction may be purified by ultrafiltration, a column method using an adsorptive carrier (Diaion HP-20, Sephadex-LH20, chitin, etc.), a batch method, or the like.
  • the pine bark extract to be added to the topical skin preparation is preferably in powder form, from the viewpoint of storage and processability, and more preferably in dry powder form.
  • drying method There are no particular limitations on the drying method, and examples of drying methods include heating, sun drying, hot air drying, freeze drying, and reduced pressure drying of the pine bark extract containing a solvent.
  • the solid pine bark extract may be pulverized.
  • the pine bark extract may be commercially available, and examples of commercially available pine bark extract include Flavangenol (registered trademark; Toyo Shinyaku Co., Ltd.).
  • the pine bark extract (D) is encapsulated in liposomes containing hydrogenated soybean phospholipids (F). This improves the stability of the pine bark extract (D) in the topical skin preparation of the present invention, and enhances the moisturizing effect of the topical skin preparation as well as the effects of improving the smoothness upon application and the firmness of the skin after use.
  • the presence of the component (D) in the liposomes can be confirmed by, for example, liquid chromatography to confirm the presence of polyphenols derived from the component (D) after removing the liposomes.
  • the amount of (D) pine bark extract is preferably 0.000001% by mass or more in the topical skin preparation, in order to enhance the effects of the present invention by using (D) pine bark extract.
  • the amount of (D) pine bark extract in the topical skin preparation is even more preferably 0.000005% by mass or more, and particularly preferably 0.00001% by mass or more.
  • the amount of (D) pine bark extract in the topical skin preparation is preferably 10% by mass or less, even more preferably 5% by mass or less, and particularly preferably 1% by mass or less.
  • the amount of the pine bark extract (D) is preferably 0.0001 to 10 parts by mass relative to 100 parts by mass of the niacinamide (A), in order to further improve the effects of the present invention.
  • the amount of the pine bark extract (D) is even more preferably 0.0005 parts by mass or more, and particularly preferably 0.001 parts by mass or more, relative to 100 parts by mass of the niacinamide (A).
  • the amount of the pine bark extract (D) is even more preferably 8 parts by mass or less, and particularly preferably 5 parts by mass or less, relative to 100 parts by mass of the niacinamide (A).
  • the amount of each of the above components (D) may be determined as the amount of solids.
  • the topical skin preparation of the present invention contains (E) at least one selected from glutathione and ceramides, which not only effectively enhances the moisturizing effect but also improves the smoothness upon application and the firmness of the skin after use.
  • Glutathione may be reduced glutathione, oxidized glutathione, or a mixture of these, but reduced glutathione is preferred because it is expected to exert an antioxidant effect.
  • Ceramides that can be used include human ceramides such as ceramide 1, ceramide 2, and ceramide 3, animal-derived ceramides extracted from the brains and spinal cords of cows, horses, pigs, etc., and plant-derived ceramides extracted from wheat, rice, soybeans, spinach, corn, konjac, pineapple, etc.
  • the ceramides used in the present invention may be sugar ceramides, and specific examples include those bound to monosaccharides such as galactosylceramide and glucosylceramide, and those bound to oligosaccharides.
  • At least one selected from glutathione and ceramides is encapsulated in liposomes containing (F) hydrogenated soybean phospholipids.
  • This improves the stability of (E) at least one selected from glutathione and ceramides in the topical skin preparation of the present invention, thereby enhancing the moisturizing effect as well as the effect of improving smoothness upon application and firmness of the skin after use.
  • the presence of component (E) in the liposomes can be confirmed by, for example, IR (infrared spectroscopy) after removing the liposomes from the topical skin preparation.
  • the amount of glutathione in the topical skin preparation is preferably 0.000001% by mass or more in order to enhance the effects of the present invention by using glutathione. From this perspective, the amount of glutathione in the topical skin preparation is even more preferably 0.000005% by mass or more, and especially preferably 0.00001% by mass or more. From the same perspective, the amount of glutathione in the topical skin preparation is preferably 10% by mass or less, even more preferably 5% by mass or less, and especially preferably 1% by mass or less.
  • the amount is preferably 0.01 to 50 parts by mass per 100 parts by mass of (A) niacinamide, in order to further improve the effects of the present invention.
  • the amount of glutathione is even more preferably 0.05 parts by mass or more, and particularly preferably 0.1 parts by mass or more, per 100 parts by mass of (A) niacinamide.
  • the amount of (C) glutathione is even more preferably 30 parts by mass or less, and particularly preferably 10 parts by mass or less, per 100 parts by mass of (A) niacinamide.
  • the amount of ceramides in the topical skin preparation is preferably 0.000001% by mass or more in order to enhance the effects of the present invention achieved by using ceramides. From this viewpoint, the amount of ceramides in the topical skin preparation is even more preferably 0.000005% by mass or more, and particularly preferably 0.00001% by mass or more. From the same viewpoint, the amount of ceramides in the topical skin preparation is preferably 0.01% by mass or less, even more preferably 0.005% by mass or less, and particularly preferably 0.001% by mass or less.
  • the amount is preferably 0.00001 to 1 part by mass per 100 parts by mass of niacinamide (A), in order to further improve the effects of the present invention.
  • the amount of ceramides is even more preferably 0.00005 parts by mass or more, and particularly preferably 0.0001 parts by mass or more, per 100 parts by mass of niacinamide (A).
  • the amount of ceramides is even more preferably 0.1 parts by mass or less, and particularly preferably 0.01 parts by mass or less, per 100 parts by mass of niacinamide (A).
  • the topical skin preparation contains liposomes containing (F) hydrogenated soybean phospholipid as a membrane component, and the liposomes encapsulate at least one selected from (C) 3-O-ethyl ascorbic acid, (D) pine bark extract, and (E) glutathione and ceramides. This effectively enhances the moisturizing effect of the topical skin preparation, and also enhances the effects of improving the smoothness of the skin upon application and the firmness of the skin after use.
  • (F) Liposomes using hydrogenated soybean phospholipids are particularly important for maintaining the emulsification stability of topical skin preparations.
  • the hydrogenated soybean phospholipid used in the present invention may be hydrogenated soybean lecithin, etc., in which the unsaturated carbon chains in soybean phospholipids such as soybean lecithin have been converted to saturated bonds by hydrogenation.
  • Liposomes containing hydrogenated soybean phospholipids as a membrane component preferably have an average particle diameter of 30 nm to 300 nm, which can improve stability over time, improve the encapsulation rate of (C) to (E), and improve the permeability of the liposomes into the skin, etc.
  • the average particle diameter of the liposomes is preferably 40 nm to 250 nm, and more preferably 50 nm to 200 nm.
  • the average particle diameter of the liposomes can be measured by a commercially available particle size distribution analyzer such as a laser diffraction particle size distribution analyzer or a light scattering photometer, but is preferably measured by a dynamic light scattering particle size distribution analyzer.
  • a Zetasizer S manufactured by Malvern Instruments can be used.
  • liposomes encapsulating (C) to (E) can be prepared as follows. First, (F) hydrogenated soybean phospholipids and an organic solvent are mixed to prepare a phospholipid liquid. As the organic solvent, a dihydric alcohol can be preferably used. In order to successfully obtain liposomes encapsulating (C) to (E), the preparation of the phospholipid liquid is preferably carried out at 80 to 90°C, more preferably at 85 to 90°C.
  • the amount of organic solvent used to prepare the phospholipid liquid is preferably 180 to 400 parts by mass, more preferably 200 to 350 parts by mass, per 100 parts by mass of hydrogenated soybean phospholipid (F).
  • the phospholipid liquid before adding the aqueous phase described below contain an oily component such as sterol.
  • the amount of hydrogenated soybean phospholipid (F) per 100 parts by mass of the total amount of (C) to (E) may be the ratio of (C) to (E) and (F) in the topical skin preparation described below, but 80 to 250 parts by mass is particularly preferable, and 100 to 220 parts by mass is even more preferable.
  • the amount of water for preparing the aqueous phase may be appropriately adjusted to an appropriate amount in order to disperse (C), (D) and (E) and encapsulate the phospholipids described below, but may be 1,000 to 5,000,000 parts by mass, or 4,000 to 2,000,000 parts by mass per 100 parts by mass of the total amount of (C), (D) and (E).
  • the preparation of the aqueous phase containing (C), (D) and (E) is preferably carried out at 80 to 90°C, more preferably at 85 to 90°C.
  • the timing of adding (C), (D) and (E) to the water may be one time or may be different times.
  • the phospholipid liquid is mixed with the aqueous phase.
  • this mixing is preferably carried out at 80 to 90°C, and more preferably at 85 to 90°C. This mixing can also be carried out by gentle stirring using a propeller or the like.
  • the component (A) is preferably added to the external skin preparation at a timing after the preparation of the liposomes.
  • component (B) it is preferable to add component (B) to the topical skin preparation at a timing after the preparation of liposomes.
  • the content of (F) hydrogenated soybean phospholipid in the topical skin preparation is preferably 0.001% by mass or more from the viewpoint of successfully obtaining liposomes with an excellent encapsulation rate of the components (C) to (E), more preferably 0.01% by mass or more, and particularly preferably 0.05% by mass or more. Furthermore, the content of (F) hydrogenated soybean phospholipid in the topical skin preparation is preferably 20% by mass or less from the viewpoint of obtaining a topical skin preparation that is smooth to the touch and has excellent skin penetration, more preferably 10% by mass or less, and even more preferably 5% by mass or less.
  • the content of hydrogenated soybean phospholipid (F) in the topical skin preparation is preferably 0.01 parts by mass or more per part by mass of the total amount of (C), (D), and (E) in order to successfully obtain a liposome membrane with an excellent encapsulation rate of the components (C) to (E), more preferably 0.05 parts by mass or more, and particularly preferably 0.1 parts by mass or more.
  • the content of hydrogenated soybean phospholipid (F) in the topical skin preparation is preferably 20 parts by mass or less per part by mass of the total amount of (C), (D), and (E) in order to obtain a topical skin preparation that is smooth to use and has excellent skin penetration, more preferably 15 parts by mass or less, and even more preferably 10 parts by mass or less.
  • the topical skin preparation of the present invention preferably further contains at least one component selected from (G1) antioxidants, (G2) moisturizing agents, (G3) anti-inflammatory agents, (G4) whitening agents, (G5) vitamins, and (G6) peeling agents as a component different from the components (A) to (F), as this enhances the moisturizing effect and effectively improves the smoothness upon application and the transparency and firmness of the skin after use.
  • a peeling agent is an agent used to increase the flexibility of keratin and remove it.
  • Antioxidants include ubiquinone and astaxanthin, with astaxanthin being particularly preferred from the standpoint of improving moisturizing effects and usability. Astaxanthin is known to be contained in Haematococcus algae, crustaceans such as shrimp and crab, and salmon. There are no particular limitations on the astaxanthin that can be used in the present invention, but astaxanthin derived from Haematococcus algae is preferred from the standpoint of ease of use. Haematococcus (Haematococcus pluvialis) is a type of microalgae.
  • the amount of the antioxidant is preferably 0.000001% by mass or more in the topical skin preparation, in order to enhance the effects of the present invention achieved by using the antioxidant (G1).
  • the amount of the antioxidant (G1) in the topical skin preparation is even more preferably 0.000005% by mass or more, and particularly preferably 0.00001% by mass or more.
  • the amount of the antioxidant (G1) in the topical skin preparation is preferably 1% by mass or less, even more preferably 0.5% by mass or less, and particularly preferably 0.1% by mass or less.
  • the amount of the antioxidant (G1) is preferably 0.00005 to 0.2 parts by mass per 100 parts by mass of niacinamide (A) in order to improve the moisturizing effect and the improvement of the feeling of use using the antioxidant (G1).
  • the amount of the antioxidant (G1) is even more preferably 0.0002 parts by mass or more, and particularly preferably 0.0005 parts by mass or more, per 100 parts by mass of niacinamide (A).
  • the amount of the antioxidant (G1) is even more preferably 0.08 parts by mass or less, and particularly preferably 0.05 parts by mass or less, per 100 parts by mass of niacinamide (A).
  • the antioxidant (G1) may be encapsulated in a liposome containing hydrogenated soybean phospholipid (F) as a membrane component, or may be present in the external aqueous phase outside the liposome, but is preferably present in the external aqueous phase.
  • moisturizing agents examples include bilberry leaf extract; Phellodendron bark extract; hydrolyzed hyaluronic acid, acetylated hyaluronic acid, sodium hyaluronate; 2-methacryloyloxyethyl phosphorylcholine/butyl methacrylate copolymer; heparinoids; isomerized sugar; proteoglycan; aminobutyric acid, and the like.
  • bilberry leaf extract is particularly preferred from the viewpoint of improving moisturizing effect and usability.
  • “Bilberry” also known as Vaccinium myrtillus L.
  • Vaccinium myrtillus L. may be used as the leaf of a plant of the Ericaceae family and the Vaccinium genus, but the leaf of the same genus plant Vaccinium myrtillus (V.smallii A.Gray var glabrum Koidz.) may also be used.
  • the part to be extracted may contain other parts such as stems and flowers as long as it contains leaves.
  • the bilberry leaf extract may be an extract containing the leaves of a plant body, either as is or after crushing, and squeezed out, or it may be extracted with a solvent, either as is or after crushing.
  • the extraction solvent may be water, a hydrophilic organic solvent, or a water-containing hydrophilic organic solvent.
  • hydrophilic organic solvents include lower aliphatic alcohols with 1 to 3 carbon atoms, such as methanol, ethanol, propanol, and isopropanol, and polyhydric alcohols with 2 to 4 carbon atoms, such as 1,3-butylene glycol, propylene glycol, and glycerin.
  • the amount of the moisturizing agent is preferably 0.000001% by mass or more in the topical skin preparation in order to ensure excellent antioxidant and other effects due to the use of the moisturizing agent (G2).
  • the amount of the moisturizing agent (G2) in the topical skin preparation is even more preferably 0.000005% by mass or more, and especially preferably 0.00001% by mass or more.
  • the amount of the moisturizing agent (G2) in the topical skin preparation is preferably 1% by mass or less, even more preferably 0.5% by mass or less, and especially preferably 0.1% by mass or less.
  • the amount of the moisturizing agent (G2) is preferably 0.0001 to 0.2 parts by mass relative to 100 parts by mass of niacinamide (A), in order to further improve the effects of the present invention.
  • the amount of the moisturizing agent (G2) is more preferably 0.0005 parts by mass or more relative to 100 parts by mass of niacinamide (A), and particularly preferably 0.001 parts by mass or more.
  • the amount of the moisturizing agent (G2) is more preferably 0.1 parts by mass or less relative to 100 parts by mass of niacinamide (A), and particularly preferably 0.02 parts by mass or less.
  • the amount of each of the above (G2) can be the amount of solid content.
  • the moisturizing agent (G2) may be encapsulated in liposomes containing (F) hydrogenated soybean phospholipid as a membrane component, or may be present in the external aqueous phase outside the liposome, but is preferably present in the external aqueous phase.
  • Centella Asiatica leaf extract is an extract of Centella Asiatica leaves. Centella Asiatica leaf extract may be one that uses other parts of Centella Asiatica such as flowers and stems in addition to the leaves. Centella Asiatica leaf extract can be obtained by extracting Centella Asiatica leaves as is, or by drying, crushing, or crushing and squeezing the leaves and extracting them with an extraction solvent.
  • the extraction solvent water (including hot water), alcohols such as methanol, ethanol, isopropanol, ethylene glycol, propylene glycol, butylene glycol, and glycerin, esters such as ethyl acetate, ketones such as acetone and methyl ethyl ketone, nitriles such as acetonitrile, ethers such as diethyl ether and tetrahydrofuran, saturated hydrocarbons such as pentane, hexane, cyclopentane, and cyclohexane, aromatic hydrocarbons such as toluene, halogenated hydrocarbons such as dichloromethane and chloroform, and other organic solvents such as dimethylformamide and dimethyl sulfoxide (which may all contain water), can be appropriately used, and a mixture of one or two of them may also be used.
  • alcohols are preferable, and ethanol, propylene glycol, and butylene
  • the amount of the anti-inflammatory agent is preferably 0.000001% by mass or more in the topical skin preparation in order to ensure excellent antioxidant and other effects due to the use of the anti-inflammatory agent (G3).
  • the amount of the anti-inflammatory agent (G3) in the topical skin preparation is even more preferably 0.000005% by mass or more, and especially preferably 0.00001% by mass or more.
  • the amount of the anti-inflammatory agent (G3) in the topical skin preparation is preferably 1% by mass or less, even more preferably 0.5% by mass or less, and especially preferably 0.3% by mass or less.
  • the amount is preferably 0.1 to 25 parts by mass relative to 100 parts by mass of niacinamide (A) in terms of improving moisturizing effect and usability.
  • the amount of the anti-inflammatory agent (G3) is more preferably 0.2 parts by mass or more relative to 100 parts by mass of niacinamide (A), and particularly preferably 0.5 parts by mass or more.
  • the amount of the anti-inflammatory agent (G3) is more preferably 20 parts by mass or less relative to 100 parts by mass of niacinamide (A), and particularly preferably 10 parts by mass or less.
  • the amount of each of the above components (G3) may be the amount of solid content.
  • the (G3) anti-inflammatory agent may be encapsulated in a liposome containing (F) hydrogenated soybean phospholipid as a membrane component, or may be present in the external aqueous phase outside the liposome, but is preferably present in the external aqueous phase.
  • Examples of skin whitening agents include ascorbic acid, 3-laurylglyceryl ascorbic acid, myristyl 3-glyceryl ascorbic acid, bisglyceryl ascorbic acid, 3-glyceryl ascorbic acid, trisodium ascorbyl palmitate phosphate, ascorbyl tetrahexyldecanoate, L-ascorbic acid 2-glucoside, magnesium ascorbyl phosphate, sodium ascorbyl phosphate, and other ascorbic acid derivatives; tranexamic acid, hydroquinone, arbutin, placenta extract, kojic acid, and the like.
  • ascorbic acid derivatives are preferred, and bisglyceryl ascorbic acid is particularly preferred from the standpoint of enhancing the moisturizing effect and usability.
  • the amount of the whitening agent is preferably 0.000001 mass% or more in terms of solid content in the topical skin preparation, in order to ensure excellent effects such as improved transparency achieved by using the whitening agent (G4).
  • the amount of Centella asiatica leaf extract in the topical skin preparation is even more preferably 0.000005 mass% or more, and particularly preferably 0.00001 mass% or more.
  • the amount of the whitening agent (G4) in the topical skin preparation is preferably 1 mass% or less, even more preferably 0.5 mass% or less, and particularly preferably 0.1 mass% or less.
  • the amount of the whitening agent (G4) is preferably 0.1 to 25 parts by mass, in terms of solid content, per 100 parts by mass of niacinamide (A), in order to improve the moisturizing effect and the effect of improving the feeling of use.
  • the amount of the whitening agent (G4) is even more preferably 0.2 parts by mass or more, and particularly preferably 0.5 parts by mass or more, per 100 parts by mass of niacinamide (A).
  • the amount of the whitening agent (G4) is even more preferably 20 parts by mass or less, and particularly preferably 10 parts by mass or less, per 100 parts by mass of niacinamide (A).
  • the (G4) skin whitening agent may be encapsulated in liposomes containing (F) hydrogenated soybean phospholipid as a membrane component, or may be present in the external aqueous phase outside the liposome, but is preferably present in the external aqueous phase.
  • Vitamins include salts and derivatives of vitamins A, B, E, and P, such as biotin, calcium pantothenate, tocopherol, tocopherol acetate, sodium tocopheryl phosphate, retinol, retinol palmitate, retinol acetate, retinol propionate, retinol linoleate, hydrogenated retinol, cyanocobalamin, folic acid, glucosyl hesperingin, and pyridoxine hydrochloride.
  • tocopherol is preferred in terms of moisturizing effect and usability.
  • Tocopherol may be any of ⁇ , ⁇ , ⁇ , and ⁇ tocopherol.
  • the amount of the vitamins is preferably 0.000001 mass% or more in terms of solid content in the topical skin preparation, in order to ensure excellent antioxidant and other effects due to the use of the (G5) vitamins. From this perspective, the amount of the (G5) vitamins in the topical skin preparation is even more preferably 0.000005 mass% or more, and particularly preferably 0.00001 mass% or more. From the same perspective, the amount of the (G5) vitamins in the topical skin preparation is preferably 1 mass% or less, even more preferably 0.5 mass% or less, and particularly preferably 0.2 mass% or less.
  • the amount of (G5) vitamins is preferably 0.1 to 25 parts by mass per 100 parts by mass of (A) niacinamide in order to improve the moisturizing effect and the effect of improving the feeling of use.
  • the amount of (G5) vitamins is even more preferably 0.2 parts by mass or more, and particularly preferably 0.5 parts by mass or more, per 100 parts by mass of (A) niacinamide.
  • the amount of (G5) vitamins is even more preferably 20 parts by mass or less, and particularly preferably 10 parts by mass or less, per 100 parts by mass of (A) niacinamide.
  • the vitamins (G5) may be encapsulated in liposomes containing (F) hydrogenated soybean phospholipid as a membrane component, or may be present in the external aqueous phase outside the liposome, but are preferably present in the external aqueous phase.
  • organic acids are suitable, such as lactic acid, salicylic acid, glycolic acid, malic acid, mandelic acid, and lactobionic acid, with lactic acid being particularly preferred in terms of its moisturizing effect and usability.
  • the amount of the peeling agent in the topical skin preparation is preferably 0.000001% by mass or more in order to ensure excellent peeling and other effects achieved by using the peeling agent. From this perspective, the amount of the peeling agent (G6) in the topical skin preparation is even more preferably 0.000005% by mass or more, and particularly preferably 0.00001% by mass or more. From the same perspective, the amount of the peeling agent (G6) in the topical skin preparation is preferably 1% by mass or less, even more preferably 0.5% by mass or less, and particularly preferably 0.2% by mass or less.
  • the amount of the peeling agent is preferably 0.1 to 25 parts by mass per 100 parts by mass of niacinamide (A) in order to improve the moisturizing effect and the effect of improving the feeling of use.
  • the amount of the peeling agent (G6) is even more preferably 0.2 parts by mass or more, and particularly preferably 0.5 parts by mass or more, per 100 parts by mass of niacinamide (A).
  • the amount of the peeling agent (G6) is even more preferably 20 parts by mass or less, and particularly preferably 10 parts by mass or less, per 100 parts by mass of niacinamide (A).
  • the peeling agent (G6) may be encapsulated in liposomes containing (F) hydrogenated soybean phospholipid as a membrane component, or may be present in the external aqueous phase outside the liposome, but is preferably present in the external aqueous phase.
  • At least one selected from (G) antioxidants, (G2) moisturizers, (G3) anti-inflammatory agents, (G4) whitening agents, (G5) vitamins, and (G6) peeling agents it is preferable to use one or more selected from (g1) astaxanthin, (g2) bilberry leaf extract, (g3) Centella asiatica leaf extract, (g4) bisglyceryl ascorbic acid, (g5) tocopherol, and (g6) lactic acid, and in particular, it is preferable to contain bilberry leaf extract in order to increase the moisture content of the stratum corneum.
  • the skin topical preparation may contain (H) other components, such as organic solvents, sterols, oils other than sterols, thickeners, chelating agents, pH adjusters, fragrances, surfactants, and preservatives, which are generally used in skin topical preparations.
  • H other components, such as organic solvents, sterols, oils other than sterols, thickeners, chelating agents, pH adjusters, fragrances, surfactants, and preservatives, which are generally used in skin topical preparations.
  • the organic solvent may be any of the organic solvents used to prepare the phospholipid liquid listed above, or in addition to the organic solvents, monohydric alcohols having 4 or less carbon atoms, such as ethanol, 2-propanol (isopropyl alcohol), butanol, and isobutyl alcohol; dihydric alcohols having 5 to 12 carbon atoms, such as propylene glycol, 1,3-butylene glycol, pentylene glycol, isopentyl diol, diethylene glycol, dipropylene glycol, ethylhexylglycerin, 1,3-propanediol, 1,5-pentanediol, 1,2-hexanediol, 1,2-octanediol, and 1,2-decanediol; diethylene glycol monoethyl ether;
  • the glycol ethers include glycol ethers such as ethylene glycol monoethyl ether (ethoxydiglycol), ethylene
  • a dihydric alcohol having 5 to 12 carbon atoms in terms of moisturizing properties, feeling in use, and bacteriostasis, and it is particularly preferable to use 1,3-butylene glycol and/or pentylene glycol.
  • the amount of organic solvent in the topical skin preparation is preferably 1 to 35% by mass, and more preferably 3 to 25% by mass.
  • the amount of pentylene glycol is preferably 10 to 50 parts by mass per 100 parts by mass of 1,3-butylene glycol.
  • the sterol may be one contained as a component of the membrane containing (F) hydrogenated soybean phospholipid.
  • the liposome may contain a sterol in addition to (F) hydrogenated soybean phospholipid as a membrane component.
  • the liposome membrane is stabilized, which makes it easier to further improve the moisturizing effect, smoothness upon application, transparency after use, and firmness effect achieved by the combination of (C), (D), and (E) described above.
  • sterols include cholesterol and phytosterol, with phytosterol being preferred in terms of the feel when used and the stability of the liposome.
  • Phytosterol is a general term for sterols contained in plants, and the main components known to be ⁇ -sitosterol, stigmasterol, campesterol, brassicasterol, etc.
  • the sterol may be a mixture of multiple sterols.
  • the content of sterol in the skin topical preparation is preferably 0.01% by mass or more from the viewpoint of more successfully obtaining a liposome membrane having an excellent encapsulation rate of the components (C) to (E), more preferably 0.04% by mass or more, and particularly preferably 0.08% by mass or more.
  • the content of sterol in the skin topical preparation is preferably 10% by mass or less from the viewpoint of easily obtaining a skin topical preparation having a smooth feel and excellent skin permeability and from the viewpoint of good stability of the liposome, more preferably 5% by mass or less, and even more preferably 3% by mass or less.
  • sterol When sterol is added in the above-mentioned liposome production process, it is preferable from the viewpoint of usability and liposome stability to add the sterol to the phospholipid liquid for preparing the liposomes or to add the sterol at the timing of mixing the hydrogenated soybean phospholipid and the encapsulated component.
  • Oils include vegetable oils such as safflower oil, soybean oil, evening primrose oil, grape seed oil, rosehip oil, kukui nut oil, almond oil, sesame oil, wheat germ oil, corn oil, cottonseed oil, avocado oil, olive oil, camellia oil, persic oil, castor oil, peanut oil, hazelnut oil, macadamia nut oil, and medfoam oil; animal oils such as squalane; hydrocarbon oils such as liquid paraffin, liquid isoparaffin, and petrolatum; ethyl oleate, ethyl linoleate, and myristic acid.
  • vegetable oils such as safflower oil, soybean oil, evening primrose oil, grape seed oil, rosehip oil, kukui nut oil, almond oil, sesame oil, wheat germ oil, corn oil, cottonseed oil, avocado oil, olive oil, camellia oil, persic oil, castor oil, peanut oil, hazelnut oil, macadamia nut oil,
  • the oil include diisostearyl malate, dioctyl succinate, glyceryl tricaprylate, glyceryl tri-2-ethylhexanoate (triethyl
  • ester oil glyceryl tri-2-ethylhexanoate is preferred, and as the silicone oil, dimethicone is preferred.
  • the skin topical preparation contains the oil
  • its content is preferably 0.5% to 30% by mass in terms of usability, and more preferably 1% to 20% by mass.
  • the preferred mass ratio of the two is 100 parts by mass of ester oil to 0.1 to 60 parts by mass of silicone oil.
  • thickeners include various types that can be used in the fields of cosmetics and pharmaceuticals.
  • natural polysaccharides cellulose-based polymers, synthetic polymers, clay minerals, etc. can be used.
  • Natural polysaccharides include polysaccharides derived from plants or animals or from microbial fermentation. Specific examples include xanthan gum, succinoglycan, carrageenan, guar gum, locust bean gum, galactan, gum arabic, tragacanth gum, tamarind gum, agar, agarose, mannan, curdlan, alginic acid or its salts, gum arabic, pectin, quince seed, starch, algae colloid, chondroitin sulfate or its salts, chitosan and its derivatives, nucleic acid or its salts, ribonucleic acid or its salts, casein, collagen, gelatin, albumin, fibroin, elastin, keratin, sericin and other water-soluble proteins, hyaluronic acid or its salts, chondroitin sulfate and other mucopolysaccharides. Among these, xanthan gum is preferred from the viewpoint of usability.
  • Cellulosic polymers are polymers that are composed of units of cellulose or its derivatives. Specific examples include carboxymethylcellulose or its salts, methylcellulose, ethylcellulose, propylcellulose, hydroxymethylcellulose, hydroxyethylcellulose, hydroxypropylmethylcellulose, and sulfonated cellulose derivatives.
  • Synthetic polymers are polymers artificially synthesized using monomers as building blocks.
  • Specific examples include vinyl polymers such as carboxyvinyl polymers and polyvinyl alcohol, acrylic acid-alkyl methacrylate copolymers, acrylates/alkyl acrylate crosspolymers, acrylic acid polymers such as polyacrylic acid, acrylamide polymers such as polyalkylacrylamide/polyacrylamide copolymers, and (PEG-240/decyltetradeceth-20/HDI) copolymers.
  • carboxyvinyl polymers and acrylic acid-alkyl methacrylate copolymers are preferred from the viewpoint of usability.
  • Clay minerals refer to substances commonly known as the main component minerals that make up clay. Specific examples include laponite, bentonite, smectite kaolinite, and montmorillonite.
  • the amount of thickener in the topical skin preparation is preferably 0.1 to 3% by mass, and when natural polysaccharides and synthetic polymers are combined, the mass ratio of the two is preferably 100 parts by mass of natural polysaccharide to 50 to 350 parts by mass of synthetic polymer.
  • Antibacterial and preservative agents include parabens (hydroxybenzoic acid esters) such as methylparaben, ethylparaben, propylparaben, and butylparaben; phenoxyethanol; alkyl glyceryl ethers such as 2-ethylhexylglyceryl ether (ethylhexylglycerin); salicylic acid; lanolin fatty acids and their salts; sodium benzoate; isothiazolinone derivatives such as methylchloroisothiazolinone and methylisothiazolinone; imidazolinium urea; dehydroacetic acid and its salts; phenols; and halides such as triclosan.
  • parabens hydroxybenzoic acid esters
  • methylparaben such as methylparaben, ethylparaben, propylparaben, and butylparaben
  • phenoxyethanol alkyl gly
  • 1,2-alkanediols examples include halogenated bisphenols, acid amides, and quaternary ammonium salts; trichlorocarbanide, zinc pyrithione, benzalkonium chloride, benzethonium chloride, sorbic acid, chlorhexidine, chlorhexidine gluconate, halocarban, hexachlorophene, and hinokitiol; other phenols such as phenol, isopropylphenol, cresol, thymol, parachlorophenol, phenylphenol, and sodium phenylphenol; phenylethyl alcohol, photosensitizers, antibacterial zeolites, and silver ions.
  • trichlorocarbanide zinc pyrithione
  • benzalkonium chloride benzethonium chloride
  • sorbic acid chlorhexidine, chlorhexidine gluconate
  • halocarban hexachlorophene
  • 1,2-alkanediols such as pentylene glycol can also be used as antibacterial and preservative agents.
  • the amount of the 1,2-alkanediols is included in the amount of the organic solvent, and is not included in the amount of the antibacterial and preservative described below.
  • the amount of antibacterial/antiseptic agent in the topical skin preparation is preferably 0.01 to 1% by mass, and more preferably 0.05 to 0.5% by mass.
  • Chelating agents include edetates (ethylenediaminetetraacetates) such as EDTA, EDTA2Na, EDTA3Na, EDTA4Na; hydroxyethylethylenediaminetriacetates such as HEDTA3Na; pentetates (diethylenetriaminepentaacetate); phytic acid; phosphonic acids such as etidronic acid and their sodium salts; sodium oxalate; polypolyamino acids such as polyaspartic acid and polyglutamic acid; sodium polyphosphate, sodium metaphosphate, phosphoric acid; sodium citrate, and citric acid.
  • edetates ethylenediaminetetraacetates
  • HEDTA3Na EDTA4Na
  • hydroxyethylethylenediaminetriacetates such as HEDTA3Na
  • pentetates diethylenetriaminepentaacetate
  • phytic acid phosphonic acids such as eti
  • the amount of chelating agent in the topical skin preparation is preferably 0.008 to 1 mass %, and more preferably 0.01 to 0.5 mass %.
  • pH adjusters, acids, and alkalis include acetic acid, sodium acetate, hydrochloric acid, sulfuric acid, monoethanolamine, diethanolamine, triethanolamine, isopropanolamine, triisopropanolamine, 2-amino-2-methyl-1,3-propanediol, 2-amino-2-hydroxymethyl-1,3-propanediol, arginine, sodium hydroxide, potassium hydroxide, aqueous ammonia, guanidine carbonate, and ammonium carbonate.
  • the amount of water in the topical skin preparation is preferably 40 to 90% by weight, for example.
  • Types of topical skin preparations of the present invention include hair cosmetics, skin cosmetics, makeup cosmetics, fragrance cosmetics, body cosmetics, etc.
  • the topical skin preparations of the present invention can be manufactured according to conventional methods.
  • preferred hair cosmetics include shampoos such as oil shampoo, cream shampoo, conditioning shampoo, anti-dandruff shampoo, hair color shampoo, and rinse-combined shampoo; hair care products such as rinse, conditioner, treatment, hair pack, hair mist, and hair oil; hair styling products such as hair foam, hair mousse, hair spray, hair wax, hair gel, hair cream, water grease, setting lotion, pomade, and hair styling products; hair dye products such as color lotion, hair color treatment, hair manicure, and oxidation hair dye; hair tonic, hair liquid, hair blow, split end coat, permanent wave agent, straight perm agent, hair bleach, hair color pre-treatment, hair color after-treatment, perm pre-treatment, perm after-treatment, and hair growth agent.
  • hair care products such as rinse, conditioner, treatment, hair pack, hair mist, and hair oil
  • hair styling products such as hair foam, hair mousse, hair spray, hair wax, hair gel, hair cream, water grease, setting lotion, pomade, and hair styling products
  • hair dye products such as color lotion, hair color treatment, hair manicure, and
  • Skin cosmetics include lotions such as softening lotion, astringent lotion, cleansing lotion, multi-layered lotion, and liposome lotion; emulsions such as emollient lotion, moisture lotion, milky lotion, nourishing lotion, nourishing milk, skin moisture, moisturizing emulsion, massage lotion, exfoliating smoother, elbow lotion, hand lotion, and body lotion; emollient cream, nourishing cream, nourishing cream, vanishing cream, moisture cream, night cream, massage cream, cleansing cream, makeup cream, base cream, pre-makeup cream, sunscreen cream, suntan cream, hair removal cream, deodorant cream, shaving cream, etc.
  • lotions such as softening lotion, astringent lotion, cleansing lotion, multi-layered lotion, and liposome lotion
  • emulsions such as emollient lotion, moisture lotion, milky lotion, nourishing lotion, nourishing milk, skin moisture, moisturizing emulsion, massage lotion, exfoliating smoother, elbow lotion, hand lotion, and body lotion
  • creams such as moisturizing cream and keratin softening cream
  • gels such as moisturizing gel, whitening gel, and all-in-one gel
  • beauty serums such as moisturizing essence, whitening essence, moisturizing serum, and whitening serum
  • sunscreens such as sun protect, sun protector, UV care milk, and sunscreen
  • packs and masks such as peel-off packs, powder packs, washing packs, oil packs, and cleansing masks
  • makeup removers such as cleansing foam, cleansing cream, cleansing milk, cleansing lotion, cleansing gel, and cleansing oil
  • facial cleansers such as paste facial cleansing foam, gel facial cleansing foam, foam facial cleansing foam, facial cleansing powder, cosmetic soap, transparent soap, medicated soap, liquid soap, and shaving soap.
  • makeup cosmetics include lipstick, lip gloss, foundation, blusher, face powder, concealer, eyeliner, mascara, eye shadow, eyebrow pencil, eyebrow pencil, nail enamel, enamel remover, and nail treatment.
  • aromatic cosmetics include perfume, perfume, perfume, perfume, perfume, perfume, perfume, eau de perfume, eau de toilette, eau de cologne, perfume paste, aromatic powder, perfumed soap, body lotion, and bath oil.
  • body cosmetics include body cleansers such as body shampoos, deodorant cosmetics such as deodorant lotions, deodorant powders, deodorant sprays and deodorant sticks, bleaches, depilatories, bath additives, and insect repellents such as insect repellent sprays.
  • topical skin preparations of the present invention from the viewpoint of their moisturizing effect and improved usability, lotions, milky lotions, creams, gels, beauty essences, packs, makeup removers, facial cleansers, etc. are preferred.
  • Preferred dosage forms of the topical skin preparation of the present invention include emulsion-type cosmetics such as oil-in-water (O/W) type, water-in-oil (W/O) type, W/O/W type, and O/W/O type, oil-based cosmetics, solid cosmetics, liquid cosmetics, paste-type cosmetics, stick-type cosmetics, volatile oil-type cosmetics, powder cosmetics, jelly-type cosmetics, gel-type cosmetics, paste-type cosmetics, emulsified polymer-type cosmetics, sheet-type cosmetics, mist-type cosmetics, and spray-type cosmetics.
  • the topical skin preparation of the present invention is an emulsion
  • the continuous phase may be either an aqueous phase or an oil phase.
  • a composition is prepared in which the continuous phase is an aqueous phase.
  • the present invention will be described below based on examples, but the present invention is not limited to the following examples.
  • the average particle size of the liposomes was 100 to 150 nm.
  • ⁇ Test substance> Niacinamide having a purity of 98% by mass or more was used.
  • B D-pantothenyl alcohol having a purity of 98% by mass or more was used.
  • C 3-O-ethyl ascorbic acid having a purity of 95% by mass was used.
  • D As the pine bark extract, a hot water extract (dried powder) of the bark of French maritime pine was used.
  • E1 Glutathione used was of reduced type with a purity of 98% by mass or more.
  • E2 N-stearoylphytosphingosine (ceramide NP) was used as the ceramide.
  • (F) Hydrogenated soybean phospholipid Hydrogenated soybean lecithin (purity 100% by mass) was used.
  • Bilberry leaf extract was prepared by extracting bilberry leaf extract powder using water and 1,3-butylene glycol as an extraction solvent in a mass ratio of 1:1. The purity was 0.2% by mass, with the remainder being water and 1,3-butylene glycol.
  • Astaxanthin was derived from Haematococcus algae and had a purity of 50% by mass, with the remainder being tri(caprylic acid/capric acid)glyceryl.
  • As the Centella asiatica leaf extract a purified extract with a purity of 100% by mass was used.
  • (H1) Phytosterol Phytosterol with a purity of 100% by mass was used.
  • Example 1 The components used were (A) to (D), (E1), (E2), (F), and (H1) to (H12).
  • Step 1 Preparation of liposomes
  • (F), (H1), and (H3) were mixed at 85° C. (Liquid 1).
  • the mixing was performed by adding (H1) and (H3) to (F) in that order.
  • (C), (D), (E1), and (E2) were mixed with (H12) in an amount corresponding to 13% by mass based on the total amount of the topical skin preparation at 85° C. (Liquid 2).
  • Example 2 An external skin preparation was obtained in the same manner as in Example 1, except that the amount of (A) niacinamide was changed and (E1) ceramide or (E2) glutathione was not used.
  • Example 4 A skin topical preparation was obtained in the same manner as in Example 1, except that the amount of (A) niacinamide was changed.
  • Example 5 Bilberry leaf extract was added together with (A), (B), (H2), (H4) to (H12) in the second step. Except for this, a skin external preparation was obtained in the same manner as in Example 4.
  • Example 6 (g1) Astaxanthin, (g3) Centella asiatica leaf extract, (g4) Bisglyceryl ascorbic acid, (g5) Tocopherol, and (g6) Lactic acid were added together with (A), (B), (H2), and (H4) to (H12) in the second step. Except for this, a skin topical preparation was obtained in the same manner as in Example 5.
  • the moisture content of the stratum corneum was measured using a skin epidermal moisture content measuring device SKICON-200EX (manufactured by IBS Co., Ltd.) This skin epidermal moisture content measuring device evaluates the moisture content of the stratum corneum as the skin conductance (electrical conductivity, unit: ⁇ S). The higher the stratum corneum moisture content, the greater the moisturizing effect.
  • Production Examples 1 to 5 The beauty essences described in Production Examples 1 to 5 were prepared in the same manner as in Example 1.
  • the beauty essences of Production Examples 1 to 5, like the Examples, have excellent moisturizing effects, smoothness upon application, and excellent transparency and firmness of the skin after use.
  • the skin external preparation of the present invention is industrially useful since it has an excellent moisturizing effect, is smooth when applied, and leaves the skin transparent and firm after use.

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Abstract

Cette préparation externe pour la peau contient les éléments (A), (B), (C), (D), (E) et (F) suivants. (C), (D) et (E) sont chacun une composition incluse dans un liposome contenant, en tant que composant constitutif de la membrane, (F) un phospholipide de soja hydrogéné.　(A) de la niacinamide.　(B) de l'alcool D-pantothényle.　(C) du 3-O-éthyl ascorbate.　(D) un extrait d'écorce de pin.　(E) au moins un élément choisi parmi le glutathion et les céramides.　(F) un phospholipide de soja hydrogéné.　En outre, il est préférable que la préparation externe pour la peau contienne (G) au moins un élément choisi parmi des antioxydants, des agents hydratants, des agents anti-inflammatoires, des agents de blanchiment, des vitamines et des agents de pelage.
PCT/JP2023/018955 2023-05-22 2023-05-22 Préparation externe pour la peau WO2024241430A1 (fr)

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JP2005220084A (ja) * 2004-02-06 2005-08-18 Kose Corp アセロラ種子抽出物含有組成物
JP2006193512A (ja) * 2004-12-13 2006-07-27 Toyo Shinyaku:Kk 外用剤
JP2012201670A (ja) * 2011-03-28 2012-10-22 Toyo Shinyaku Co Ltd 外用剤
WO2015152384A1 (fr) * 2014-04-03 2015-10-08 ポーラ化成工業株式会社 Inhibiteur de la mélanogenèse comprenant de l'alcool d-pantothénylique, et produit cosmétique de blanchiment de la peau contenant ledit inhibiteur
JP2016160242A (ja) * 2015-03-04 2016-09-05 杏林製薬株式会社 セラミド類含有リポソーム分散液
WO2016158704A1 (fr) * 2015-03-27 2016-10-06 株式会社コーセー Composition de liposomes
JP2023016083A (ja) * 2021-07-21 2023-02-02 日本精化株式会社 ３－ｏ－エチルアスコルビン酸含有化粧料又は皮膚外用剤

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