Skin external preparation
By combining niacinamide, edelweiss extract, and sesame extract in a topical skin formulation, the uncertainties surrounding the combined effects of plant extracts were resolved, resulting in a more effective anti-aging effect.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- NOEVIR CO LTD
- Filing Date
- 2021-08-25
- Publication Date
- 2026-06-05
AI Technical Summary
The combined effects of plant extracts in existing topical skin agents are unpredictable, making it difficult to achieve higher anti-aging effects with smaller amounts.
By combining niacinamide with Edelweiss extract and Sesamum indicum extract, and adjusting their proportions in topical skin formulations, the anti-aging effects can be synergistically enhanced.
It enhances the production of filaggrin, ceramides, and collagen, reduces elastin breakdown, and significantly improves the anti-aging effect of topical skin agents.
Smart Images
Figure BDA0003228669960000061
Abstract
Description
Technical Field
[0001] This invention relates to a topical skin agent. Background Technology
[0002] As people age, they experience various signs of aging such as age spots, wrinkles, and sagging. The causes are known to include a decreased skin barrier function, reduced moisture content, disrupted metabolism, and reduced or degraded production of collagen and elastin. Various proposals have been put forward to prevent and improve these conditions (Japanese Patent No. 4780817, Japanese Unexamined Patent Application Publication No. 2001-261568, and Japanese Unexamined Patent Application Publication No. 2005-8571).
[0003] Niacinamide is a type of B vitamin that is water-soluble, also known as nicotinic acid amide. Its effects on improving rough skin, whitening, and anti-aging are well-known, and cosmetics containing niacinamide are widely available.
[0004] Leontopodium alpinum is an alpine plant classified as belonging to the genus Leontopodium in the family Asteraceae. Extracts of this plant have been disclosed for use in topical dermatological preparations (Japanese Patent Application Publication No. 2001-288032). Lamiumabum is a perennial herb classified as belonging to the genus Lamium in the family Lamiaceae. Extracts of this plant have been disclosed for use in topical dermatological preparations (Japanese Patent Application Publication No. Hei 10-330221).
[0005] In addition, extensive research has been conducted on the use of plant extracts in cosmetics. However, the effects of using plant extracts together do not necessarily synergistically enhance each other; rather, they may have additive or offsetting effects. The resulting effects are unpredictable, and there is a high demand for using plant extracts in smaller quantities to achieve greater results.
[0006] Existing technical documents
[0007] Patent documents
[0008] Patent Document 1: Japanese Patent No. 4780817
[0009] Patent Document 2: Japanese Patent Application Publication No. 2001-261568
[0010] Patent Document 3: Japanese Patent Application Publication No. 2005-8571
[0011] Patent Document 4: Japanese Patent Application Publication No. 2001-288032
[0012] Patent Document 5: Japanese Patent Application Publication No. 10-330221 Summary of the Invention
[0013] The problem with this invention is to provide a topical skin agent containing niacinamide and specific plant extracts that exhibits high anti-aging effects.
[0014] The present invention provides a topical skin preparation containing the following (A) to (C).
[0015] (A) Nicotinamide, (B) Edelweiss extract, and (C) Sesamum indicum extract.
[0016] The topical skin formulation of the present invention achieves a high anti-aging effect by combining nicotinamide with specific plant extracts. Detailed Implementation
[0017] The specific embodiments of the present invention will be described below.
[0018] [Niacinamide]
[0019] Niacinamide is a type of B vitamin that is water-soluble and is also known as nicotinamide.
[0020] The nicotinamide used in this invention is any nicotinamide commonly used in topical skin preparations, and there are no particular limitations on its raw materials, manufacturing methods, purification methods, etc.
[0021] The amount of nicotinamide used in this invention in the topical skin preparation is 0.001% to 20% by mass relative to the total amount of the topical skin preparation, preferably 0.01% to 15% by mass, and more preferably 0.1% to 10% by mass.
[0022] [Edelweiss]
[0023] Leontopodium alpinum is an alpine plant belonging to the genus Leontopodium in the family Asteraceae.
[0024] The Edelweiss extract used in this invention can be any Edelweiss extract commonly used in topical skin preparations. It can be an extract directly derived from the plant or a commercially available Edelweiss extract. Examples of commercially available Edelweiss extracts include: EDELEWEISS GC (ALPAFLOR), EDELEWEISS EP, and EDELEWEISS B (DSM Nutrition Japan).
[0025] The amount of Edelweiss extract used in this invention in the topical skin preparation is preferably 0.00001% to 5% by mass relative to the total amount of the topical skin preparation, and more preferably 0.00001% to 1% by mass.
[0026] The components of usable Edelweiss include, for example, leaves, stems, flowers, buds, and the whole above-ground part, with the whole above-ground part being preferred.
[0027] [Short-stalked wild sesame]
[0028] Short-stalked wild sesame (scientific name: Lamium album) is a perennial herb belonging to the genus Lamium in the family Lamiaceae.
[0029] The *Sesamum indicum* extract used in this invention can be a type of *Sesamum indicum* extract commonly used in topical skin preparations. It can be an extract directly derived from the plant or a commercially available *Sesamum indicum* extract. Examples of commercially available *Sesamum indicum* extracts include Pharcolex *Sesamum indicum* B (ICHIMARU PHARCOS Co., Ltd.).
[0030] The amount of the short-stalked wild sesame extract used in this invention in the topical skin preparation is preferably 0.00001% to 5% by mass relative to the total amount of the topical skin preparation, and more preferably 0.00001% to 1% by mass.
[0031] The usable components of short-stalked wild sesame include, for example, leaves, stems, flowers, flower buds, and the whole above-ground plant, with the whole above-ground plant being preferred.
[0032] When preparing the above extracts, the original plant material can be used directly or after drying. As extraction solvents, one or more polar organic solvents can be selected from water, methanol, ethanol, propanol, isopropanol, etc.; polyols such as 1,3-butanediol, propylene glycol, dipropylene glycol, and glycerol; ethers such as diethyl ether and propyl ether; esters such as ethyl acetate and butyl acetate; and ketones such as acetone and methyl ethyl ketone. Physiological saline, phosphate buffer, and phosphate-buffered saline can also be used. The extracts obtained using the above solvents can be used directly, but the concentrated, dried, and solidified substances can also be reconstituted in water or polar solvents; or purified by decolorization, deodorization, and desalting within a range that does not impair their skin physiological function and enhances their effects; or used after fractionation using column chromatography. Furthermore, substances obtained by hydrolyzing the extract using acids, alkalis, enzymes, etc., can also be used. Additionally, for preservation, the purified material can be lyophilized and then dissolved in a solvent before use. In addition, vesicles or microcapsules containing liposomes can also be used. There are no particular limitations on the extraction process as long as it allows the soluble components of the raw material to dissolve into the extraction solvent; it can be carried out using conventional methods. For example, the raw material can be immersed in an extraction solvent of 5 to 30 times its mass, and the soluble components can be extracted at room temperature or under reflux. After extraction, the residue is removed by filtration, thus obtaining an extract. When the solvent is removed by distillation from the obtained extract, a paste-like concentrate is obtained. Further drying of this concentrate yields a dried product.
[0033] In the topical skin preparations used in this invention, in addition to the ingredients described above, any ingredients commonly used in cosmetics and quasi-drugs may be incorporated to the extent that they do not impair the effectiveness of this invention. Specifically, examples include: oils, surfactants, thickeners, preservatives, fragrances, moisturizers, antioxidants, anti-inflammatory agents, antibacterial agents, etc.
[0034] The dosage form of the topical skin agent used in this invention is not particularly limited and can be any dosage form such as aqueous, oil-based, or emulsified.
[0035] The topical skin agents used in this invention can be prepared by conventional methods.
[0036] The topical skin agents used in this invention can be in the form of lotions, emulsions, or ointments.
[0037] [Example]
[0038] The present invention will now be specifically described using examples, but the scope of the invention is not limited thereto. It should be noted that, unless otherwise specified, the amount of each component is expressed as a percentage by mass.
[0039] First, a method for preparing the plant extracts used in the examples is shown.
[0040] [Edelweiss Extract]
[0041] The dried aerial parts of *Edelweiss* were soaked in a 70% (v / v) aqueous ethanol solution, filtered, and the solvent was removed by distillation. The freeze-dried material was then used as *Edelweiss* extract.
[0042] [Sesamum indicum extract]
[0043] The dried aerial parts of *Sesamum indicum* were soaked in water, filtered, and the solvent was removed by distillation. The freeze-dried material was then used as *Sesamum indicum* extract.
[0044] [Experiment using human epidermal keratinocytes]
[0045] Human epidermal keratinocytes were divided into 3×10 5 Cells were seeded at a density of 6-well plates and cultured overnight in Humedia-KG2 medium. The medium was then replaced with fresh medium containing any concentration of dissolved dried plant extract powder, and cultured for 24 hours at 37°C in a 5% CO2 incubator. RNA was extracted from the collected cells using a commercially available RNA extraction kit (Quick Gene RNA Cultured Cell HC Kit S). After cDNA synthesis, gene expression was confirmed by real-time PCR using the SYBR Green method with the primers listed below. GAPDH was used as an internal standard. mRNA expression levels are expressed as relative values with the expression level without the addition of each plant extract set to 1. The effects are shown in Tables 3–5.
[0046] [Experiment using human skin fibroblasts]
[0047] Human skin fibroblasts were divided into 5×10 5 Cells were seeded at a density of 0.5% FBS in 6-well plates and cultured overnight in DMEM medium containing 5% FBS. The medium was then replaced with DMEM medium containing 0.5% FBS dissolved in dried plant extract powder at any concentration, and cultured for 24 hours at 37°C in a 5% CO2 incubator. RNA was extracted from the collected cells using a commercially available RNA extraction kit (Quick Gene RNA Cultured Cell HC Kit S). After cDNA synthesis, gene expression was confirmed by real-time PCR using the SYBR Green method with the primers listed below. GAPDH was used as an internal standard. mRNA expression levels are expressed as relative values with the expression level without the addition of each plant extract set to 1. The effects are shown in Table 6.
[0048] The primer sequences used are shown in Table 1.
[0049] [Table 1]
[0050]
[0051] In the example, the extracts were dissolved in the culture medium in the amounts shown in Table 2, with each extract having a concentration (w / v%) of the amount shown.
[0052] [Table 2]
[0053] Example 1 Comparative Example 1 Comparative Example 2 Comparative Example 3 Nicotinamide 0.033 0.1 - - Leontopodium alpinum extract 0.013 - 0.04 - Short fruited St. John's wort extract 0.013 - - 0.04
[0054] [Table 3]
[0055] Gene Control Comparative Example 1 Comparative Example 2 Comparative Example 3 Example 1 FLG 1.00 1.21 0.82 1.06 1.86
[0056] As shown above, in Example 1, in which nicotinamide was used in combination with Edelweiss extract and Sesamum indicum extract, the expression of the filaggrin-related gene FLG was synergistically increased compared with Comparative Examples 1-3, which were used alone.
[0057] [Table 4]
[0058] Gene Control Comparative Example 1 Comparative Example 2 Comparative Example 3 Example 1 SMPD1 1.00 1.97 2.30 0.92 3.27 SGMS1 1.00 1.66 1.45 1.47 2.32 GBA 1.00 1.34 2.28 1.04 2.50
[0059] As shown above, in Example 1, in which nicotinamide was used in combination with Edelweiss extract and Sesamum indicum extract, the expression of ceramide-related genes SMPD1, SGMS1, and GBA was synergistically increased compared with Comparative Examples 1-3, which were used alone.
[0060] [Table 5]
[0061] Gene Control Comparative Example 1 Comparative Example 2 Comparative Example 3 Example 1 COL7A1 1.00 1.74 1.65 1.49 4.17 COL17A1 1.00 0.95 1.05 1.06 1.56
[0062] As shown above, in Example 1, in which nicotinamide was used in combination with Edelweiss extract and Sesamum indicum extract, the expression of collagen production-related genes COL7A1 and COL17A1 was synergistically increased compared with Comparative Examples 1-3, which were used alone.
[0063] [Table 6]
[0064] Gene Control Comparative Example 1 Comparative Example 2 Comparative Example 3 Example 1 MME 1.00 0.91 0.75 0.81 0.69
[0065] As shown above, in Example 1, in which nicotinamide was used in combination with Edelweiss extract and Sesamum indicum extract, the expression of the elastin degradation-related gene MME was synergistically reduced compared with Comparative Examples 1-3, which were used alone.
[0066] Based on the above results, the topical skin agent of the present invention exhibits a high anti-aging effect by synergistically increasing the expression of genes related to filaggrin production, ceramide production, and collagen production, and synergistically decreasing the expression of genes related to elastin degradation.
[0067] [Example 2] Emulsion
[0068] (1) Squalane: 10.0 (wt%)
[0069] (2) Methylphenyl polysiloxane: 4.0
[0070] (3) Hydrogenated palm kernel oil: 0.5
[0071] (4) Hydrogenated soybean lecithin: 0.1
[0072] (5) Polyoxyethylene sorbitan monostearate (20E.O.): 1.3
[0073] (6) Sorbitan monostearate: 1.0
[0074] (7) Glycerin: 4.0
[0075] (8) Methylparaben: 0.1
[0076] (9) Carboxyvinyl polymer: 0.15
[0077] (10) Purified water: The remaining portion set to 100
[0078] (11) Arginine (1% aqueous solution): 20.0
[0079] (12) Nicotinamide: 4.0
[0080] (13) Edelweiss extract: 0.01
[0081] (14) Extract of short-stalked wild sesame: 0.01
[0082] Preparation method: Dissolve the oil phase components (1) to (6) by heating at 80°C. On the other hand, dissolve the aqueous phase components (7) to (10) by heating at 80°C. Add the oil phase components while stirring, and emulsify them evenly using a homogenizer. After cooling, add (11) to (14) in sequence at 40°C and mix evenly.
[0083] [Example 3] Toner
[0084] (1) Ethanol: 15.0 (wt%)
[0085] (2) Polyoxyethylene (40E.O.) hydrogenated castor oil: 0.3
[0086] (3) Spices: 0.1
[0087] (4) Purified water: The remaining portion set to 100
[0088] (5) Citric acid: 0.02
[0089] (6) Sodium citrate: 0.1
[0090] (7) Glycerin: 1.0
[0091] (8) Hydroxyethyl cellulose: 0.1
[0092] (9) Nicotinamide: 6.0
[0093] (10) Edelweiss extract: 0.005
[0094] (11) Extract of short-stalked wild sesame: 0.005
[0095] Preparation: Dissolve (2) and (3) in (1). Then add (4) to (11) in sequence, stir thoroughly and mix evenly.
[0096] [Example 4] Cream
[0097] (1) Squalane: 10.0 (wt%)
[0098] (2) Stearic acid: 2.0
[0099] (3) Hydrogenated palm kernel oil: 0.5
[0100] (4) Hydrogenated soybean lecithin: 0.1
[0101] (5) Cetyl alcohol: 3.6
[0102] (6) Lipophilic glyceryl monostearate: 2.0
[0103] (7) Glycerin: 10.0
[0104] (8) Methylparaben: 0.1
[0105] (9) Arginine (20% by mass aqueous solution): 15.0
[0106] (10) Purified water: The remaining portion set to 100
[0107] (11) Carboxyvinyl polymer (1% aqueous solution by mass): 15.0
[0108] (12) Nicotinamide: 0.4
[0109] (13) Edelweiss extract: 0.05
[0110] (14) Extract of short-stalked wild sesame: 0.05
[0111] Preparation method: Dissolve the oil phase components (1) to (6) by heating at 80°C. On the other hand, dissolve the aqueous phase components (7) to (10) by heating at 80°C. Add the oil phase components while stirring, and emulsify them evenly using a homogenizer. After adding (11) and stirring, cool the mixture, and add (12) to (14) at 40°C, and mix evenly.
[0112] [Example 5] Beauty Serum
[0113] (1) Purified water: The remaining portion (by mass) of 100.
[0114] (2) Glycerin: 10.0
[0115] (3) Sucrose fatty acid esters: 1.3
[0116] (4) Carboxyvinyl polymer (1% aqueous solution by mass): 17.5
[0117] (5) Sodium alginate (1% aqueous solution): 15.0
[0118] (6) Polyglycerol monolaurate: 1.0
[0119] (7) Phytosterol macadamia oleate: 3.0
[0120] (8) Phytosterols / Ocyldodecyl lauroyl glutamate: 2.0
[0121] (9) Hydrogenated palm oil: 2.0
[0122] (10) Squalane (derived from olive): 1.0
[0123] (11) Sagerol: 0.75
[0124] (12) Beeswax: 1.0
[0125] (13) Jojoba oil: 1.0
[0126] (14) 1,3-Butanediol: 10.0
[0127] (15) L-arginine (10% by mass aqueous solution): 2.0
[0128] (16) Nicotinamide: 2.0
[0129] (17) Edelweiss extract: 0.1
[0130] (18) Extract of short-stalked wild sesame: 0.1
[0131] Preparation: The aqueous phase components (1) to (6) are mixed and heated to dissolve at 75°C. Meanwhile, the oil phase components (7) to (14) are mixed and heated to dissolve at 75°C. Next, the oil phase components are added to the aqueous phase components for pre-emulsification, and then emulsified uniformly using a high-speed mixer. After cooling, (15) is added at 50°C, and (16) to (18) are added at 40°C, and then mixed uniformly.
[0132] [Example 6] Aqueous Gel
[0133] (1) Carboxyvinyl polymer: 0.5 (wt%)
[0134] (2) Purified water: The remaining portion set to 100
[0135] (3) Sodium hydroxide (10% by mass aqueous solution): 0.5
[0136] (4) Glycerin: 10.0
[0137] (5) 1,3-Butanediol: 10.0
[0138] (6) Ethanol: 10.0
[0139] (7) Methylparaben: 0.1
[0140] (8) Spices: 0.1
[0141] (9) Nicotinamide: 4.0
[0142] (10) Edelweiss extract: 0.01
[0143] (11) Extract of short-stalked wild sesame: 0.01
[0144] Preparation method: Add (1) to (2), stir evenly, then add (3). After stirring evenly, add (5) which has been dissolved in (4) beforehand. After stirring evenly, add (6) to (11) which have been mixed beforehand, and stir evenly to mix. sequence list <110> Novia Co., Ltd. <120> Topical skin agents <130> KP2016 <150> JP2020-141481 <151> 2020-08-25 <160> 16 <210> 1 <211> 20 <212> DNA <213> Artificial sequence <220> <223> Primers <400> 1 GGAATTTCGG CAAATCCTGA 20 <210> 2 <211> twenty one <212> DNA <213> Artificial sequence <220> <223> Primers <400> 2 TGCTTTCTGT GCTTGTGTCC 21 <210> 3 <211> 20 <212> DNA <213> Artificial sequence <220> <223> Primers <400> 3 CTGACCCAGG CAAACATACC 20 <210> 4 <211> 20 <212> DNA <213> Artificial sequence <220> <223> Primers <400> 4 TGCGATATAC CAGGTTGTGC 20 <210> 5 <211> 20 <212> DNA <213> Artificial sequence <220> <223> Primers <400> 5 TGGCACGCTG TACCTGTATC 20 <210> 6 <211> 20 <212> DNA <213> Artificial sequence <220> <223> Primers <400> 6 CACCTCCAGC AATGAGCTTC 20 <210> 7 <211> twenty two <212> DNA <213> Artificial sequence <220> <223> Primers <400> 7 CAATTGGGTG CGTAACTTTG TC 22 <210> 8 <211> twenty three <212> DNA <213> Artificial sequence <220> <223> Primers <400> 8 AAAACGTGTC CTTGGTGATG TCT 23 <210> 9 <211> 20 <212> DNA <213> Artificial sequence <220> <223> Primers <400> 9 AGCCTGGCGT CTCTTACATC 20 <210> 10 <211> 20 <212> DNA <213> Artificial sequence <220> <223> Primers <400> 10 ACGGTGAGCA TTGTCTTGAG 20 <210> 11 <211> twenty one <212> DNA <213> Artificial sequence <220> <223> Primers <400> 11 AATTCAGAGG CATCGTTGGA C 21 <210> 12 <211> twenty two <212> DNA <213> Artificial sequence <220> <223> Primers <400> 12 CCGGCAGTAT GTAAGTAAGA CG 22 <210> 13 <211> 20 <212> DNA <213> Artificial sequence <220> <223> Primers <400> 13 CCTTCTTTAG TGCCCAGCAG 20 <210> 14 <211> 20 <212> DNA <213> Artificial sequence <220> <223> Primers <400> 14 TGAGTCCACC AGTCAACGAG 20 <210> 15 <211> 20 <212> DNA <213> Artificial sequence <220> <223> Primers <400> 15 CCACTCCTCC ACCTTTGACG 20 <210> 16 <211> 20 <212> DNA <213> Artificial sequence <220> <223> Primers <400> 16 CACCCTGTTG CTGTAGCCAA 20
Claims
1. A topical skin preparation comprising the following (A) to (C): (A) Nicotinamide, (B) Edelweiss extract, and (C) Extract of short-stalked wild sesame.