WO2025226072A1 - Composition cosmétique transparente à teneur élevée en acide azélaïque - Google Patents

Composition cosmétique transparente à teneur élevée en acide azélaïque

Info

Publication number
WO2025226072A1
WO2025226072A1 PCT/KR2025/005609 KR2025005609W WO2025226072A1 WO 2025226072 A1 WO2025226072 A1 WO 2025226072A1 KR 2025005609 W KR2025005609 W KR 2025005609W WO 2025226072 A1 WO2025226072 A1 WO 2025226072A1
Authority
WO
WIPO (PCT)
Prior art keywords
cosmetic composition
azelaic acid
skin
mixture
present
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
PCT/KR2025/005609
Other languages
English (en)
Korean (ko)
Inventor
서희승
문선영
박천호
정동진
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Cosmax Inc
Original Assignee
Cosmax Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Cosmax Inc filed Critical Cosmax Inc
Publication of WO2025226072A1 publication Critical patent/WO2025226072A1/fr
Pending legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/362—Polycarboxylic acids
    • 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
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • 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
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34—Alcohols
    • A61K8/345—Alcohols containing more than one hydroxy group
    • 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
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/365—Hydroxycarboxylic acids; Ketocarboxylic acids
    • 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
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/007—Preparations for dry skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
    • A61K2800/26—Optical properties
    • A61K2800/262—Transparent; Translucent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/48—Thickener, Thickening system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/49—Solubiliser, Solubilising system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/52—Stabilizers
    • A61K2800/524—Preservatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
    • A61K2800/805—Corresponding aspects not provided for by any of codes A61K2800/81 - A61K2800/95

Definitions

  • the present invention relates to a transparent liquid type cosmetic composition containing azelaic acid and a sodium base, and more particularly, to a transparent liquid type cosmetic composition containing azelaic acid in a high content, including a sodium base, an amino acid, and a polyol that increase the solubility of azelaic acid.
  • Azelaic acid has been used to alleviate a wide range of physiological and chronic conditions, including acne, pigmentation, hair loss, wrinkles, hyperhidrosis, inflammatory skin diseases, and infectious skin diseases.
  • azelaic acid Currently known formulations of azelaic acid are dispersion formulations, which deliver azelaic acid in an undissolved state. Undissolved azelaic acid is not readily absorbed when applied to the skin, and as a result, an excessive amount of azelaic acid is required to exhibit an effect.
  • a fully dissolved azelaic acid composition is required, as dissolved azelaic acid is more readily absorbed than the undissolved form and is therefore less irritating to the skin, thus reducing the risk of adverse skin irritation effects.
  • azelaic acid is somewhat soluble in water, cosmetic oils, and alcohols, each of these solvents has significant limitations. Water can only dissolve azelaic acid in very small amounts, so a solution containing water and azelaic acid can contain only about 0.24% by weight (w/w) of azelaic acid, which is insufficient to be effective. Furthermore, azelaic acid is also poorly or completely soluble in cosmetic oils. Furthermore, while alcohol is a good solvent, the presence of large amounts of isopropyl alcohol in topical compositions can negatively affect the skin, hindering its effectiveness. In fact, some alcohols, such as ethyl alcohol, tend to destabilize azelaic acid under standard temperature and atmospheric pressure conditions, making it difficult to formulate cosmetic compositions that are effective on the skin as a whole.
  • the formulation must remain stable under standard temperature and atmospheric pressure conditions; however, the art has not yet developed a cosmetic composition that is stable and completely dissolves azelaic acid under standard temperature and atmospheric pressure conditions.
  • a transparent liquid type cosmetic composition containing azelaic acid, sodium chloride, amino acid, and polyol contains a high content of azelaic acid, is optimized for troubled skin, and exhibits a refreshing feeling as well as an excellent skin moisture improvement effect.
  • the purpose of the present invention is to provide a transparent liquid type cosmetic composition containing azelaic acid and a sodium base.
  • Another object of the present invention is to provide a composition for external application to the skin comprising azelaic acid and a sodium salt.
  • Another object of the present invention is to provide a method for producing a transparent liquid type cosmetic composition or composition for external application to the skin containing a high content of azelaic acid, comprising the following steps:
  • a step of preparing a composition by mixing the first mixture and the second mixture and then mixing the third mixture.
  • Another object of the present invention is to provide a transparent liquid type cosmetic composition that contains azelaic acid and a sodium base and a high content of azelaic acid, and is optimized for skin troubles and exhibits a refreshing feeling and an excellent skin moisture improvement effect.
  • Another object of the present invention is to provide a cosmetic composition comprising azelaic acid, sodium base and amino acid.
  • Another object of the present invention is to provide a cosmetic composition comprising azelaic acid, sodium base and polyol.
  • the present invention relates to a transparent liquid type cosmetic composition containing azelaic acid and a sodium salt, and the inventors of the present invention have completed the present invention by confirming that the transparent liquid type cosmetic composition not only contains azelaic acid in a high content by including a sodium salt, an amino acid, and a polyol that increase the solubility of azelaic acid, but also exhibits a refreshing feeling optimized for troubled skin, an excellent skin moisture improvement effect, and a significant anti-acne effect.
  • One aspect of the present invention is a high-azelaic acid cosmetic composition
  • azelaic acid and a sodium base.
  • the cosmetic composition is a liquid, gel, cream, lotion, paste, emulsion, dispersion, foam, toner, skin, toner, serum, essence, eye cream, nourishing cream, massage cream, hand cream, ointment, external ointment for skin, liquid soap, solid soap, scrub, detergent, cleansing foam, cleansing gel, cleansing lotion, cleansing cream, cleansing water, cleansing oil, body cleanser, body lotion, patch, mask, pack, shampoo, rinse, conditioner, treatment, hair pack, hair tonic, hair fixer stick, scalp ampoule, sunscreen, sunscreen, BB cream, CC cream, tone-up cream, makeup base, makeup primer, foundation, pact, concealer, powder, spray, atomizer, aerosol, eye shadow, eyebrow, eyeliner, balm, stick, sun stick, It may be one or more formulations selected from the group consisting of highlighter sticks, contour sticks, lip balms, lipsticks, lip tints, lip glosses, lip oils, lip lacquers, lip creams, and lip crayons, but
  • the cosmetic composition may be a transparent formulation. In another embodiment of the present invention, the cosmetic composition may be a liquid formulation. In yet another embodiment of the present invention, the cosmetic composition may be a transparent liquid formulation.
  • azelaic acid refers to an organic substance having a structure represented by the following chemical formula 1, which can be used as a precursor for various products, including polymers and plasticizers, as well as a component of hair and skin conditioner compositions. Azelaic acid is also known to be effective in treating acne and can be used as a whitening agent for freckles and inflammatory pigmentation.
  • sodium base in this specification may be used interchangeably with “sodium salt” and means a compound that includes sodium (Na) within the compound.
  • amino acid in this specification means an organic compound having an amino group (in the form of -NH3 + , which is protonated under biological conditions), a carboxyl group (in the form of -COO - , which is deprotonated under biological conditions) and a specific side chain (R group), and also includes amino acid derivatives.
  • amino acid derivative refers to a compound derived from an amino acid by replacing, adding, or removing an amino group, carboxyl group, side chain group, or other group attached to a central atom of the amino acid.
  • betaine is a trimethylated derivative of the amino acid glycine, which is an amino acid derivative containing a glycine backbone with three methyl groups attached to the nitrogen atom.
  • the amino acid derivative of the present invention may include, but is not necessarily limited to, any one or more of betaine, betaine salicylate, glycocyamine, acetylcysteine, sodium PCA, glycolic acid, and lactic acid.
  • the cosmetic composition may contain azelaic acid in an amount of 0.1 to 30 wt%, 0.1 to 25 wt%, 0.1 to 20 wt%, 0.2 to 30 wt%, 0.2 to 25 wt%, 0.2 to 20 wt%, 0.3 to 30 wt%, 0.3 to 25 wt%, 0.3 to 20 wt%, 0.4 to 30 wt%, 0.4 to 25 wt%, 0.4 to 20 wt%, 0.5 to 30 wt%, or 0.5 to 25 wt%, based on the total cosmetic composition, and for example, may contain 0.5 to 20 wt%, but is not limited thereto.
  • the cosmetic composition may contain the azelaic acid in an amount of 0.5 to 20 wt%, 0.5 to 15 wt%, 0.5 to 10 wt%, 1 to 20 wt%, 1 to 15 wt%, 1 to 10 wt%, 5 to 20 wt%, 5 to 15 wt%, 5 to 10 wt%, 10 to 20 wt%, 10 to 15 wt%, or 15 to 20 wt%, for example, but not limited to, 10 to 15 wt%, 10 to 16 wt%, or 10 to 17 wt%.
  • the sodium base may include at least one selected from the group consisting of sodium hydroxide, sodium citrate, and sodium carbonate, but is not limited thereto.
  • the cosmetic composition may contain the sodium base in an amount of 0.05 to 30 wt%, 0.05 to 28 wt%, 0.05 to 26 wt%, 0.05 to 24 wt%, 0.05 to 22 wt%, 0.05 to 20 wt%, 0.1 to 30 wt%, 0.1 to 28 wt%, 0.1 to 26 wt%, 0.1 to 24 wt%, or 0.1 to 22 wt%, based on the total cosmetic composition, and for example, may contain 0.1 to 20 wt%, but is not limited thereto.
  • the cosmetic composition may contain the sodium base in an amount of 0.1 to 20 wt%, 0.1 to 15 wt%, 0.1 to 10 wt%, 0.5 to 20 wt%, 0.5 to 15 wt%, 0.5 to 10 wt%, 1 to 20 wt%, 1 to 15 wt%, 1 to 10 wt%, 2 to 20 wt%, 2 to 15 wt%, 2 to 10 wt%, 3 to 20 wt%, 3 to 15 wt%, 3 to 10 wt%, 4 to 20 wt%, 4 to 15 wt%, or 4 to 10 wt%, for example, 4 to 8 wt% or 0.5 to 8 wt%, but is not limited thereto.
  • the cosmetic composition may additionally contain an amino acid.
  • the amino acid may include at least one selected from the group consisting of betaine, betaine salicylate, and arginine, but is not limited thereto.
  • Betaine in this specification refers to a substance rated Level 1 by the Environmental Working Group (EWG), also known as trimethylglycine (TMG), which has excellent skin penetration ability and can help soothe and moisturize the skin.
  • EWG Environmental Working Group
  • TMG trimethylglycine
  • betaine may be betaine; or a physiologically or cosmetically acceptable salt thereof, such as, but not limited to, betaine salicylate.
  • Arginine in this specification is an amino acid used in the biosynthesis of proteins, and may be used interchangeably with “arginine” or “arginine”.
  • the cosmetic composition may contain the amino acid in an amount of 0.1 to 20 wt%, 0.2 to 20 wt%, 0.3 to 20 wt%, or 0.4 to 20 wt% relative to the total cosmetic composition, for example, 0.5 to 20 wt%, but is not limited thereto.
  • the cosmetic composition may contain the amino acid in an amount of 0.05 to 20 wt%, 0.05 to 15 wt%, 0.05 to 10 wt%, 0.05 to 5 wt%, 0.1 to 20 wt%, 0.1 to 15 wt%, 0.1 to 10 wt%, 0.1 to 5 wt%, 0.5 to 20 wt%, 0.5 to 15 wt%, 0.5 to 10 wt%, 0.5 to 5 wt%, 1 to 20 wt%, 1 to 15 wt%, 1 to 10 wt%, 1 to 5 wt%, 2 to 20 wt%, 2 to 15 wt%, or 2 to 10 wt%, for example, 0.1 to 10 wt%, 0.1 to 5 % by weight, or 2 to 5 wt%, but is not limited thereto.
  • the cosmetic composition may additionally contain a polyol.
  • the polyol may include propylene glycol.
  • the cosmetic composition may contain the polyol in an amount of 0.05 to 20 wt%, 0.05 to 15 wt%, 0.05 to 10 wt%, 0.1 to 20 wt%, 0.1 to 15 wt%, 0.1 to 10 wt%, 0.5 to 20 wt%, 0.5 to 15 wt%, 0.5 to 10 wt%, 1 to 20 wt%, 1 to 15 wt%, 1 to 10 wt%, 2 to 20 wt%, 2 to 15 wt%, 2 to 10 wt%, 5 to 20 wt%, 5 to 15 wt%, 5 to 10 wt%, 8 to 20 wt%, 8 to 15 wt%, or 8 to 10 wt%, based on the total cosmetic composition, for example, 8 to It may contain, but is not limited to, 12% by weight.
  • the cosmetic composition may additionally include at least one selected from the group consisting of a solvent, a thickener, and a preservative, but is not limited thereto.
  • the solvent may be a polyol, specifically a C1 to C6 polyol, and may include, for example, at least one selected from the group consisting of propylene glycol, ethoxy diglycol, glycerin, propanediol, and dipropylene glycol.
  • thickening agent in this specification may mean an ingredient used to maintain the viscosity and stability of a cosmetic composition, and in the present invention, the thickening agent may be at least one selected from the group consisting of glyceryl acrylate/acrylic acid copolymer, carbomer, and xanthan gum, and may be, for example, xanthan gum, but is not limited thereto.
  • preservative in this specification may mean an ingredient used to prevent deterioration of a cosmetic composition and maintain purity, and in the present invention, the preservative may be at least one selected from the group consisting of pentylene glycol, 1,2-hexanediol, ethylhexyl glycerin, caprylyl glycol, and phenoxyethanol, and may be, for example, 1,2-hexanediol, but is not limited thereto.
  • the cosmetic composition may additionally contain a moisturizer.
  • the moisturizer may be at least one selected from the group consisting of sodium hyaluronate, sodium PCA (sodium pyrrolidone carboxylate), sodium lactate, sodium gluconate, sodium chondroitin sulfate, sodium polyacrylate, hyaluronic acid, glycerin, and propanediol, but is not necessarily limited thereto.
  • the cosmetic composition may be one in which azelaic acid does not precipitate at low temperature (4°C).
  • the cosmetic composition may be one in which azelaic acid is dissolved at a low temperature (4°C).
  • dissolution refers to the process by which a component disperses and mixes in a solvent to form a homogeneous solution. Dissolution ensures that the component is evenly distributed within the cosmetic, prevents precipitation under various temperature conditions, and becomes biologically available for skin absorption.
  • the usability of the manufactured cosmetic composition was evaluated, and as a result, it was specifically confirmed that the cosmetic composition of the comparative example was sticky and showed an unpleasant usability, whereas the cosmetic composition of the example showed a refreshing usability without being sticky.
  • the cosmetic composition manufactured above was evaluated for water activity, inflammatory lesion improvement effect, and anti-acne effect, and as a result, the cosmetic composition of the example not only showed an excellent inflammatory lesion improvement effect compared to the cosmetic composition of the comparative example, but also showed an excellent skin moisture improvement effect by increasing skin moisture by about 101.5%, and it was specifically confirmed that it exhibited a significant anti-acne effect.
  • the cosmetic composition may be used for moisturizing the skin, promoting moisturizing the skin, improving skin moisture, and/or improving skin inflammation.
  • compositions for external application to the skin comprising azelaic acid and a sodium base.
  • Topical skin preparation refers to a product that is applied directly to the skin to provide skin treatment, improvement, protection, soothing, relief, or cosmetic benefits, and encompasses cosmetics and dermatological cosmetics. Topical skin preparations can primarily exert local effects on the skin surface or specific areas, and the active ingredients contained in the preparation can penetrate through the skin barrier.
  • composition for external application to the skin according to the present invention contains the same ingredients as the cosmetic composition according to another embodiment of the present invention described above, in order to avoid excessive complexity of the description herein, redundant contents are cited and the description thereof is omitted.
  • Another aspect of the present invention is a method for producing a transparent liquid type cosmetic composition or composition for external application to the skin containing a high content of azelaic acid, comprising the following steps:
  • a step of preparing a composition by mixing the first mixture and the second mixture and then mixing the third mixture.
  • the cosmetic composition or the composition for external application to the skin may contain the azelaic acid in an amount of 0.1 to 30 wt%, 0.1 to 25 wt%, 0.1 to 20 wt%, 0.2 to 30 wt%, 0.2 to 25 wt%, 0.2 to 20 wt%, 0.3 to 30 wt%, 0.3 to 25 wt%, 0.3 to 20 wt%, 0.4 to 30 wt%, 0.4 to 25 wt%, 0.4 to 20 wt%, 0.5 to 30 wt% or 0.5 to 25 wt% relative to the total cosmetic composition or the composition for external application to the skin, and for example, may contain 0.5 to 20 wt%, but is not limited thereto.
  • the cosmetic composition or the composition for external application to the skin may contain the azelaic acid in an amount of 0.5 to 20 wt%, 0.5 to 15 wt%, 0.5 to 10 wt%, 1 to 20 wt%, 1 to 15 wt%, 1 to 10 wt%, 5 to 20 wt%, 5 to 15 wt%, 5 to 10 wt%, 10 to 20 wt%, 10 to 15 wt%, or 15 to 20 wt%, based on the total cosmetic composition or the composition for external application to the skin, and for example, may contain 10 to 15 wt%, but is not limited thereto.
  • the sodium base may include at least one selected from the group consisting of sodium hydroxide, sodium citrate, and sodium carbonate, but is not limited thereto.
  • the cosmetic composition or the composition for external application to the skin may contain the sodium salt in an amount of 0.05 to 30 wt%, 0.05 to 28 wt%, 0.05 to 26 wt%, 0.05 to 24 wt%, 0.05 to 22 wt%, 0.05 to 20 wt%, 0.1 to 30 wt%, 0.1 to 28 wt%, 0.1 to 26 wt%, 0.1 to 24 wt%, or 0.1 to 22 wt% relative to the total cosmetic composition or the composition for external application to the skin, and for example, may contain 0.1 to 20 wt%, but is not limited thereto.
  • the cosmetic composition or the composition for external application of the skin may contain the sodium salt in an amount of 0.1 to 20 wt%, 0.1 to 15 wt%, 0.1 to 10 wt%, 0.5 to 20 wt%, 0.5 to 15 wt%, 0.5 to 10 wt%, 1 to 20 wt%, 1 to 15 wt%, 1 to 10 wt%, 2 to 20 wt%, 2 to 15 wt%, 2 to 10 wt%, 3 to 20 wt%, 3 to 15 wt%, 3 to 10 wt%, 4 to 20 wt%, 4 to 15 wt%, or 4 to 10 wt%, based on the total cosmetic composition or the composition for external application of the skin, and for example, may contain 4 to 8 wt% or 0.5 to 8 wt%, but is not limited thereto. It is not.
  • the first mixture may additionally include an amino acid.
  • the amino acid may include at least one selected from the group consisting of betaine, betaine salicylate, and arginine, but is not limited thereto.
  • the cosmetic composition or the composition for external application to the skin may contain the amino acid in an amount of 0.1 to 20 wt%, 0.2 to 20 wt%, 0.3 to 20 wt%, or 0.4 to 20 wt% relative to the total cosmetic composition or the composition for external application to the skin, and for example, may contain 0.5 to 20 wt%, but is not limited thereto.
  • the cosmetic composition or the composition for external application of the skin may contain the amino acid in an amount of 0.05 to 20 wt%, 0.05 to 15 wt%, 0.05 to 10 wt%, 0.05 to 5 wt%, 0.1 to 20 wt%, 0.1 to 15 wt%, 0.1 to 10 wt%, 0.1 to 5 wt%, 0.5 to 20 wt%, 0.5 to 15 wt%, 0.5 to 10 wt%, 0.5 to 5 wt%, 1 to 20 wt%, 1 to 15 wt%, 1 to 10 wt%, 1 to 5 wt%, 2 to 20 wt%, 2 to 15 wt%, or 2 to 10 wt%, based on the total cosmetic composition or the composition for external application of the skin, for example, 2 to 5 May include, but is not limited to, weight %.
  • the solvent in the second mixture may be a polyol.
  • the polyol may include propylene glycol.
  • the step of preparing the second mixture may be heating and dissolving at a temperature of 55°C to 95°C, 55°C to 90°C, 55°C to 85°C, 60°C to 95°C, 60°C to 90°C, 60°C to 85°C, 65°C to 95°C, or 65°C to 90°C, and for example, heating and dissolving at a temperature of 65°C to 85°C, but is not limited thereto.
  • a first mixture was prepared by mixing purified water, an amino acid, a thickener, and a preservative
  • a second mixture was prepared by dissolving azelaic acid in a solvent by heating at 75°C, and then purified water and a sodium salt were mixed to prepare a third mixture. Thereafter, the first mixture and the second mixture were mixed, and then the third mixture was mixed to prepare a high-azelaic acid transparent liquid type cosmetic composition.
  • the cosmetic composition can form a transparent liquid type formulation while containing a high content of azelaic acid, including a sodium salt and an amino acid that increase the solubility of azelaic acid, and has a refreshing feeling of use, an excellent skin moisture improvement effect, an excellent inflammatory lesion improvement effect, and a significant anti-acne effect, and is suitable for human use because it does not irritate the skin.
  • azelaic acid including a sodium salt and an amino acid that increase the solubility of azelaic acid
  • the description of the cosmetic composition in the aspect of the method for producing the cosmetic composition or the composition for external application to the skin can also be applied to the composition for external application to the skin, and therefore, the replacement of the cosmetic composition with the composition for external application to the skin is also included in the present invention.
  • the overlapping contents of the method for manufacturing the transparent liquid type high-content azelaic acid cosmetic composition and the transparent liquid type high-content azelaic acid cosmetic composition are omitted in consideration of the complexity of this specification.
  • the present invention relates to a transparent cosmetic composition containing azelaic acid and a sodium base, wherein the transparent cosmetic composition of the present invention not only contains azelaic acid in a high content, but also has the effect of being optimized for troubled skin, providing a refreshing feeling of use, and improving skin moisture.
  • Figure 1 shows the results of confirming the usability and solubility of cosmetic composition Example 1 manufactured according to one manufacturing example of the present invention.
  • Figure 2 shows the results of confirming the usability and solubility of comparative example 1 of a cosmetic composition manufactured according to one manufacturing example of the present invention.
  • Figure 3 shows the results of measuring the water activity of Example 1 of a cosmetic composition manufactured according to one experimental example of the present invention.
  • Figures 4 and 5 show graphs and photographs showing the evaluation results of improvement in inflammatory lesions of Example 1 of a cosmetic composition manufactured according to one experimental example of the present invention.
  • Figure 6 shows the results of confirming the low-temperature (4°C) stability of cosmetic compositions manufactured according to one manufacturing example of the present invention, Example 1, and Comparative Examples 6 to 8.
  • Figures 7 and 8 show the results of an anti-acne test of a cosmetic composition manufactured according to an experimental example of the present invention.
  • the present invention relates to a transparent liquid type cosmetic composition containing azelaic acid and a sodium base.
  • % used to indicate the concentration of a particular substance is (wt/wt)% for solid/solid, (wt/vol)% for solid/liquid, and (vol/vol)% for liquid/liquid, unless otherwise stated.
  • Cosmetic compositions containing azelaic acid were prepared as shown in Tables 1 to 3 below (unit: weight %).
  • Example 1 Comparative Example 4 Comparative Example 5 First mixture purified water To 100 To 100 To 100 amino acids Betaine 2 0 0 0 Arginine 0 5 0 0 thickener xanthan gum 0.5 0.5 0.5 0.5 antiseptic 1,2-hexanediol 2 2 2 2 Second mixture menstruum Propylene glycol 10 10 10 azelaic acid 10 15 10 15 Third mixture (sodium base solution) purified water 20 20 20 20 20 20 20 20 sodium base sodium hydroxide 4 0 4 0 Sodium citrate 0 8 0 8
  • purified water, betaine as an amino acid, xanthan gum as a thickener, and 1,2-hexanediol as a preservative were sequentially added to a homomixer and mixed at 3,500 rpm for 10 minutes to prepare a first mixture. Thereafter, propylene glycol as a solvent, azelaic acid, and PEG-60 hydrogenated castor oil as a surfactant were separately dissolved by heating to 75°C to prepare a second mixture, which was then added to a homomixer and mixed at 3,500 rpm for 10 minutes.
  • each cosmetic composition of Examples 1 to 4 and Comparative Examples 1 to 8 was stored at temperature conditions of 4°C, 25°C, and 45°C for one week to check whether a precipitated substance was present, which is shown in FIG. 1, FIG. 2, and Table 4 below.
  • Example 1 when comparing the cosmetic compositions of Example 1 and Comparative Examples 1 to 3 containing the same amount of azelaic acid, there was a difference in whether precipitation occurred under temperature conditions of low temperature (4°C) and room temperature (25°C) depending on whether the base included in the cosmetic composition was a sodium base, confirming that the sodium base had the effect of increasing the solubility of azelaic acid. At this time, even though a surfactant was used to dissolve azelaic acid in Comparative Examples 2 and 3, the solubility was significantly superior in Example 1.
  • the inventors of the present invention confirmed that propylene glycol as a solvent has the effect of increasing the solubility of azelaic acid.
  • this does not mean that propylene glycol must be included as a solvent, and that other polyols must not be included as solvents other than propylene glycol.
  • the cosmetic composition of the present invention includes propylene glycol as a solvent, which is a polyol, and may further include butylene glycol, butanediol, 1,2-hexanediol, and/or pentylene glycol.
  • the cosmetic composition of the present invention can provide a transparent liquid type cosmetic composition containing a high content of azelaic acid without causing precipitation, since it includes an amino acid, sodium base, and/or polyol that increases the solubility of azelaic acid.
  • Example 1 Comparative Example 2
  • Comparative Example 3 Comparative Example 3
  • each cosmetic composition was applied to the face and the stickiness was evaluated, and the results are shown in Table 5 below.
  • Example 1 in order to evaluate stickiness, a stickiness test was conducted by applying the cosmetic composition of Example 1 or Comparative Example 1 on the back of the hand, placing a sprinkle on it, and visually observing the extent to which the sprinkle was stuck. As a result, compared to the case where the cosmetic composition of Comparative Example 1 was applied, the extent to which the sprinkle was stuck was significantly less when the cosmetic composition of Example 1 was applied, confirming that the usability of Example 1 was excellent without stickiness.
  • the cosmetic composition of the present invention can provide a transparent liquid type cosmetic composition that contains a high content of azelaic acid while providing a refreshing feeling of use, since it includes an amino acid, sodium base, and/or polyol that increases the solubility of azelaic acid.
  • Example 1 To evaluate water activity, one 33-year-old professional panelist washed the test area (inner side of the lower arm) with soap and waited for 10 minutes in a constant temperature and humidity room (22 ⁇ 2°C, 40 to 60% RH). Then, the cosmetic composition of Example 1 was applied, and 10 minutes later, the skin moisture content (A.U., Arbituary Unit) was measured using a measuring device (Epsilon, BiOX) to confirm the water activity, which is shown in Fig. 3.
  • the cosmetic composition of the present invention can provide a transparent liquid type cosmetic composition that contains a high content of azelaic acid while exhibiting an excellent skin moisture improvement effect, since it includes an amino acid, sodium base, and/or polyol that increases the solubility of azelaic acid.
  • Example 1 To evaluate the improvement of inflammatory lesions, the cosmetic composition of Example 1 was used on five expert panelists aged 24 to 35 years to evaluate whether inflammatory lesions improved for 4 weeks, and the results are shown in Figs. 4 and 5.
  • the evaluation items are as follows:
  • Pimple A firm lump on the skin measuring approximately 0.5 cm to 1.0 cm in diameter, which is an intermediate form between inflammatory and non-inflammatory acne lesions.
  • Pustule An inflammatory acne lesion that is a raised, pus-filled pocket.
  • the cosmetic composition of the present invention includes an amino acid, sodium base, and/or polyol that increases the solubility of azelaic acid, and thus can provide a transparent liquid type cosmetic composition that can be used for improving acne by showing an excellent inflammatory lesion improvement effect while containing a high amount of azelaic acid.
  • the colonies were counted after the Minimum Inhibitory Concentration (MIC) assay.
  • MIC Minimum Inhibitory Concentration
  • 180 ⁇ L of a culture solution of Cutibacterium acnes (C. acnes ), the acne-causing bacteria was dispensed into 20 ⁇ L of the sample, and the experiment was conducted by diluting the final concentration to 1.0 wt% when the sample with an active substance (i.e., azelaic acid) content of 10 wt% was treated.
  • an active substance i.e., azelaic acid
  • Example 1 In the negative control group, no treatment was performed with the sample, and in the positive control group, 250 ⁇ g/mL of the antibiotic tetracycline hydrochloride was used as the sample, and in the experimental group, the cosmetic composition of Example 1 was used as the sample.
  • Example 1 According to the present invention, it was confirmed that the cosmetic composition of Example 1 according to the present invention exhibited a significant anti-acne effect.
  • a primary irritation evaluation was conducted on a panel of 31 female volunteers aged 19 to 59 years for the cosmetic composition of Example 1.
  • the test substance was applied to the back of the subjects using an IQ UltraTM chamber for 24 hours, and the degree of skin irritation was evaluated according to the judgment criteria of the PCPC Guideline (Personal Care Products Council, USA) 30 minutes and 24 hours after removal of the patch.
  • the cosmetic composition of Example 1 a test substance, did not show any skin irritation reaction 30 minutes and 24 hours after removal of the patch, and the average irritation index was 0.00. Therefore, the cosmetic composition of Example 1 was judged to be suitable for use on human skin, as it is a substance with an irritation category corresponding to an average irritation index of 0.00.
  • the cosmetic composition having a high azelaic acid content of the present invention includes a sodium base, an amino acid, and/or a polyol that increases the solubility of azelaic acid, thereby providing a transparent liquid type cosmetic composition having excellent formulation stability that does not cause precipitation under various temperature conditions despite containing a high content of azelaic acid, and has a refreshing feeling of use without stickiness, an excellent skin moisture improvement effect, an excellent inflammatory lesion improvement effect, and a significant anti-acne effect, and has been specifically confirmed to be suitable for human use because it does not irritate the skin, suggesting that it can be usefully used as a cosmetic composition.
  • the present invention relates to a transparent liquid type cosmetic composition containing azelaic acid and a sodium salt, wherein the transparent liquid type cosmetic composition of the present invention not only contains azelaic acid in a high content, but also provides a refreshing feeling optimized for troubled skin and has a skin moisture improvement effect, including a sodium salt, an amino acid, and a polyol that increase the solubility of azelaic acid.

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Abstract

La présente invention concerne une composition cosmétique de type liquide transparent contenant un acide azélaïque et une base sodique, et présentant une teneur élevée en acide azélaïque. Une composition cosmétique de type liquide transparent selon la présente invention présente non seulement une teneur élevée en acide azélaïque due à l'inclusion d'une base de sodium, d'un acide aminé et d'un polyol qui augmentent la solubilité de l'acide azélaïque, mais est également optimisée pour la peau troublée, fournit une sensation rafraîchissante, et a un effet d'amélioration de l'hydratation de la peau.
PCT/KR2025/005609 2024-04-26 2025-04-25 Composition cosmétique transparente à teneur élevée en acide azélaïque Pending WO2025226072A1 (fr)

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Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20090041426A (ko) * 2006-08-11 2009-04-28 파나세아 바이오테크 리미티드 활성제를 전달하기 위한 미립자 및 이의 조제방법 및 조성물
KR20150079144A (ko) * 2013-12-31 2015-07-08 동의대학교 산학협력단 아젤릭산을 포함하는 기능성 화장료 조성물
KR101605517B1 (ko) * 2014-02-14 2016-03-22 주식회사 씨앤피코스메틱스 여드름 개선용 화장료 조성물 제조방법 및 이에 의해 제조된 화장료 조성물
CN115252449A (zh) * 2022-08-17 2022-11-01 上海臻臣化妆品有限公司 壬二酸水溶液及其制备方法、化妆品组合物
CN115463044A (zh) * 2021-10-19 2022-12-13 广州花出见生物科技有限公司 一种含有超分子壬二酸的提亮组合物及其制备方法

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20090041426A (ko) * 2006-08-11 2009-04-28 파나세아 바이오테크 리미티드 활성제를 전달하기 위한 미립자 및 이의 조제방법 및 조성물
KR20150079144A (ko) * 2013-12-31 2015-07-08 동의대학교 산학협력단 아젤릭산을 포함하는 기능성 화장료 조성물
KR101605517B1 (ko) * 2014-02-14 2016-03-22 주식회사 씨앤피코스메틱스 여드름 개선용 화장료 조성물 제조방법 및 이에 의해 제조된 화장료 조성물
CN115463044A (zh) * 2021-10-19 2022-12-13 广州花出见生物科技有限公司 一种含有超分子壬二酸的提亮组合物及其制备方法
CN115252449A (zh) * 2022-08-17 2022-11-01 上海臻臣化妆品有限公司 壬二酸水溶液及其制备方法、化妆品组合物

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