CN117045524A - Mild non-irritating cosmetic composition containing azelaic acid and preparation method thereof - Google Patents

Mild non-irritating cosmetic composition containing azelaic acid and preparation method thereof Download PDF

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Publication number
CN117045524A
CN117045524A CN202311034902.2A CN202311034902A CN117045524A CN 117045524 A CN117045524 A CN 117045524A CN 202311034902 A CN202311034902 A CN 202311034902A CN 117045524 A CN117045524 A CN 117045524A
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azelaic acid
cosmetic composition
percent
composition containing
mild non
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CN202311034902.2A
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Inventor
郑祖选
刘凡
申彦晟
姜秉夏
金荣熙
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Cosmax China Cosmetics Co Ltd
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Cosmax China Cosmetics Co Ltd
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Priority to CN202311034902.2A priority Critical patent/CN117045524A/en
Publication of CN117045524A publication Critical patent/CN117045524A/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • A61K8/362Polycarboxylic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/41Amines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/58Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing atoms other than carbon, hydrogen, halogen, oxygen, nitrogen, sulfur or phosphorus
    • A61K8/585Organosilicon compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73Polysaccharides
    • A61K8/731Cellulose; Quaternized cellulose derivatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/81Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
    • A61K8/8129Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by an alcohol, ether, aldehydo, ketonic, acetal or ketal radical; Compositions of hydrolysed polymers or esters of unsaturated alcohols with saturated carboxylic acids; Compositions of derivatives of such polymers, e.g. polyvinylmethylether
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/81Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
    • A61K8/8141Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by only one carboxyl radical, or of salts, anhydrides, esters, amides, imides or nitriles thereof; Compositions of derivatives of such polymers
    • A61K8/8152Homopolymers or copolymers of esters, e.g. (meth)acrylic acid esters; Compositions of derivatives of such polymers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Birds (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Dermatology (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Emergency Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Cosmetics (AREA)

Abstract

The application relates to the field of cosmetics/skin care products, in particular to a mild non-irritating cosmetic composition containing azelaic acid and a preparation method thereof. A mild non-irritating cosmetic composition comprising azelaic acid, the raw materials comprising, in mass percent, at least: 1 to 20 percent of azelaic acid, 15 to 20 percent of softening agent, 0.1 to 5 percent of rheological modifier, 5 to 15 percent of humectant, 0.1 to 5 percent of auxiliary agent, 10 to 30 percent of grease and the balance of water. The mild non-irritating cosmetic composition containing azelaic acid provided by the application has excellent product safety, can still maintain good efficacy on the premise of low irritation, greatly reduces the irritation of the azelaic acid composition in the crowd, requires less azelaic acid when the same efficacy is achieved, obtains a reduction and synergy effect, and has wide market prospect and application value.

Description

Mild non-irritating cosmetic composition containing azelaic acid and preparation method thereof
Technical Field
The application relates to the field of cosmetics/skin care products, in particular to a mild non-irritating cosmetic composition containing azelaic acid and a preparation method thereof.
Background
Azelaic acid is a natural compound, and is widely used in the field of functional cosmetics for improving skin problems such as acne, blackheads and inflammations due to its excellent effects of inhibiting active oxygen free radical properties, anti-inflammatory, reducing synthesis of filiform keratins, preventing excessive keratinization of hair follicles, and the like.
However, azelaic acid is easily dissolved in solvents such as hot water, hot benzene and alcohol, so that azelaic acid exists in a neutralization form in the existing cosmetic/skin care products, and the pH value is high, so that the bioavailability of azelaic acid in the cosmetic/skin care composition is limited.
The prior art (CN 115252449 a) provides an aqueous azelaic acid solution, in which 10% ethanol is used as a cosolvent, and the prepared aqueous azelaic acid solution is claimed to have good stability, and the solution is stable and free from precipitation, so that the aqueous azelaic acid solution can be effectively applied to various cosmetic compositions. However, ethanol is used as a raw material for the preparation, so that the skin is provided with negative effects such as irritation, azelaic acid is used in the range of 10-20, and the skin is sensitive to acne, so that the requirement of a low-irritation product is contrary.
Accordingly, in order to solve the above-mentioned problems, the present inventors have grasped the pain spot in the field of azelaic acid compositions, and have provided a mild non-irritating cosmetic composition comprising azelaic acid which is capable of maintaining excellent efficacy while having low irritation.
Disclosure of Invention
In order to solve the above problems, the first aspect of the present application provides a mild non-irritating cosmetic composition comprising azelaic acid, which comprises, in mass percent, at least the following raw materials: 1 to 20 percent of azelaic acid, 15 to 20 percent of softening agent, 0.1 to 5 percent of rheological modifier, 5 to 15 percent of humectant, 0.1 to 5 percent of auxiliary agent, 10 to 30 percent of grease and the balance of water.
As a preferable scheme, the softening agent is at least one of polyethylene glycol, polymethyl silsesquioxane, hydroxypropyl starch phosphate and polysorbate.
As a preferable scheme, the softening agent is polymethyl silsesquioxane and hydroxypropyl starch phosphate, and the mass ratio of the polymethyl silsesquioxane to the hydroxypropyl starch phosphate is 14-18:1-2.
As a preferable scheme, the softening agent is polymethyl silsesquioxane and hydroxypropyl starch phosphate, and the mass ratio of the polymethyl silsesquioxane to the hydroxypropyl starch phosphate is 14.5-18:1.3-1.5.
As a preferable scheme, the softening agent is polymethyl silsesquioxane and hydroxypropyl starch phosphate, and the mass ratio of the polymethyl silsesquioxane to the hydroxypropyl starch phosphate is 18:1.5.
As a preferred embodiment, the rheology modifier is at least one of acrylic/C10-30 alkanol acrylate cross-linked polymer, dimethylsilylated silica, ethylcellulose, distearyldimethylamine hectorite, hydroxypropyl cellulose, polyvinyl alcohol.
As a preferred embodiment, the rheology modifier is an acrylic/C10-30 alkanol acrylate cross-linked polymer and a dimethylsilylated silica.
As a preferable scheme, the mass ratio of the acrylic acid (ester)/C10-30 alkanol acrylate cross-linked polymer to the dimethylsilylated silica is 0.1-0.2: 0 to 0.8.
As a preferred embodiment, the mass ratio of acrylic acid (esters) of C10-30 alkanol acrylate cross-linked polymer to dimethylsilylated silica is 0.1:0.8.
as a preferred embodiment, the mass ratio of azelaic acid to rheology modifier is 10:0.1 to 1.
As a preferable scheme, the humectant is at least one of propylene glycol, glycerin, butylene glycol, 1, 2-hexanediol, hyaluronic acid and hydrolyzed collagen.
As a preferred embodiment, the humectant is glycerin, 1, 2-hexanediol.
As a preferred embodiment, the oil and fat is at least one of cyclomethicone, cyclopentadimethicone, cyclohexasiloxane, octylmethicone, dimethicone, dioctyl ether, hydrogenated polyisobutene.
As a preferred embodiment, the oils are octyl polymethylsiloxane, polydimethylsiloxane, hydrogenated polyisobutene, cyclohexyl siloxane, dioctyl ether.
As a preferable scheme, the mass ratio of the octyl polymethylsiloxane, the polydimethylsiloxane, the hydrogenated polyisobutene, the cyclohexyl siloxane and the dioctyl ether is 11-22: 0 to 2:1 to 1.5:0 to 3:0 to 1.5.
As a preferred embodiment, the mass ratio of the octyl polymethylsiloxane, polydimethylsiloxane, hydrogenated polyisobutene, cyclohexasiloxane, dioctyl ether is 22:0:1:3:1.5.
as a preferable scheme, the auxiliary agent is at least one of chelating agent, preservative, emulsifying agent, auxiliary emulsifying agent and pH regulator.
As a preferred embodiment, the auxiliary agents are preservatives and pH adjusters.
As a preferred embodiment, the preservative is p-hydroxyacetophenone.
As a preferred embodiment, the pH adjuster is tromethamine.
In a second aspect, the present application provides a process for the preparation of the above-mentioned mild non-irritating cosmetic composition comprising azelaic acid, the steps comprising the steps of: (1) Uniformly mixing part of the softening agent and the grease at room temperature to obtain a phase A, mixing and dissolving the auxiliary agent and part of water to obtain a phase B, mixing part of the humectant and the rheology modifier at 60-80 ℃ and homogenizing to obtain a phase D for later use; (2) Homogenizing the phase B in the phase D for 2-5 min, cooling to 40-45 ℃ after complete homogenization, dispersing the residual soft lubricant and the residual humectant to obtain phase C, and homogenizing the phase D for 2-5 min; (3) Adding the phase D into the phase A, stirring and emulsifying, and adding azelaic acid into the mixture for homogenizing for 4-10 min after homogenizing.
The beneficial effects are that:
1. the mild non-irritating cosmetic composition containing azelaic acid provided by the application has good effect of improving skin problems such as acne, blackheads and inflammation, can effectively inhibit direct irritation of azelaic acid to human skin, has mildness different from other cosmetic compositions containing azelaic acid, and has very wide application value in the cosmetic field.
2. The mild non-irritating cosmetic composition containing azelaic acid provided by the application has excellent product safety, can still maintain good efficacy on the premise of low irritation, greatly reduces the irritation of the azelaic acid composition in the crowd, requires less azelaic acid when the same efficacy is achieved, obtains the effects of reduction and synergy, and has wide market prospect.
3. The mild non-irritating cosmetic composition containing azelaic acid provided by the application can effectively improve the dispersion stability and the fluid state of azelaic acid in the whole system of the composition through the compounding of azelaic acid and a specific rheology modifier, so that the azelaic acid has better penetration effect in skin at a lower content, and the optimal pharmacodynamic performance is obtained.
Drawings
FIG. 1 is a schematic diagram of the results of an anti-acne test of a commercially available 15% azelaic acid anti-acne cream.
Fig. 2 is a schematic diagram showing the acne-removing test result of the composition prepared in example 4 of the present application.
FIG. 3 is a graph showing the results of the test of the erythema removal effect of the composition prepared in example 4 of the present application.
Detailed Description
Example 1
Example 1 in a first aspect there is provided a mild non-irritating cosmetic composition comprising azelaic acid, the raw materials comprising, in mass percent: azelaic acid 10%, softening agent 15.85% (polymethyl silsesquioxane 14.5%, hydroxypropyl starch phosphate 1.35%), rheology modifier 0.1% (acrylic acid (ester)/C10-30 alkanol acrylate cross-linked polymer and dimethyl silyl silica with mass ratio of 1:0), humectant 12.65% (glycerin 12.2%,1, 2-hexanediol 0.45%), assistant 0.375% (pH regulator: tromethamine 0.075%, preservative: p-hydroxyacetophenone 0.3%), grease 14.85% (octyl polymethylsiloxane, polydimethyl siloxane, hydrogenated polyisobutene, cyclohexane siloxane, dioctyl ether with mass ratio of 11:1.8:1.35:0.7:0), water supplementing the rest.
The second aspect provides a preparation method of the composition, comprising the following steps in percentage by mass: (1) Uniformly mixing part of the emollient (polymethyl silsesquioxane) and grease at room temperature to obtain a phase A, mixing and dissolving an auxiliary agent and part of water (10%) to obtain a phase B, mixing part of the humectant (glycerin 5%) and a rheology modifier (acrylic acid (ester)/C10-30 alkanol acrylate cross-linked polymer) to obtain a phase D at 65 ℃ for later use; (2) Homogenizing the B phase in the D phase for 3min, cooling to 45deg.C, dispersing the rest soft lubricant and rest humectant to obtain C phase, homogenizing the D phase for 3min; (3) Adding phase D into phase A, stirring for emulsifying, homogenizing, and adding azelaic acid for 5 min.
Example 2
The specific implementation of this example is the same as example 1, except that: the components comprise: azelaic acid 0.5% (polymethylsilsesquioxane 16%, hydroxypropyl starch phosphate 1.5%), rheology modifier 0.1% (acrylic acid (esters)/C10-30 alkanol acrylate cross-linked polymer and dimethyl silyl silica 1:0), humectant 13.5% (glycerin 13%,1, 2-hexanediol 0.5%), adjuvant 0.38% (pH regulator: tromethamine 0.08%, preservative: p-hydroxyacetophenone 0.3%), grease 16% (octylpolymethylsiloxane, polydimethylsiloxane, hydrogenated polyisobutene, cyclohexasiloxane, dioctyl ether 13:1.5:0:0), water balance.
Example 3
The specific implementation of this example is the same as example 1, except that: azelaic acid 10%, softening agent 17.5% (polymethyl silsesquioxane 16%, hydroxypropyl starch phosphate 1.5%), rheology modifier 0.1% (acrylic acid (esters)/C10-30 alkanol acrylate cross-linked polymer and dimethyl silyl silica 1:0), humectant 13.5% (glycerin 13%,1, 2-hexanediol 0.5%), assistant 0.38% (pH regulator: tromethamine 0.08%, preservative: p-hydroxyacetophenone 0.3%), grease 16.5% (octyl polymethylsiloxane, polydimethylsiloxane, hydrogenated polyisobutene, cyclohexasiloxane, dioctyl ether 13:2:1.5:0:0), water supplementing the rest.
Example 4
The specific implementation of this example is the same as example 1, except that: azelaic acid 10%, softening agent 19.5% (polymethyl silsesquioxane 18%, hydroxypropyl starch phosphate 1.5%), rheology modifier 0.9% (acrylic acid (ester)/C10-30 alkanol acrylate cross-linked polymer and dimethyl silyl silica 1:8), humectant 13.5% (glycerin 13%,1, 2-hexanediol 0.5%), assistant 0.38% (pH regulator: tromethamine 0.08%, preservative: p-hydroxyacetophenone 0.3%), grease 27.5% (octyl polymethylsiloxane, polydimethylsiloxane, hydrogenated polyisobutene, cyclohexasiloxane, dioctyl ether 22:0:1:3:1.5), water supplementing the rest.
Evaluation of Performance
Product safety test
Selecting 30 subjects, and taking example 3 in a plaque tester, wherein a control hole is a blank control; the patch tester added with the test object is stuck to the forearm flexor side of the tested person, and is uniformly stuck to the skin by the light palm pressure for 24 hours; skin irritation and sensitization were observed as in table 1 after 30min, 24 hr, 48 hr, respectively, after removal of the subject plaque tester, and the observations were recorded.
TABLE 1
Table 2 closed patch test results
TABLE 3 Table 3
Subjects for clinical testing:
1. gender: 80% female &20% male
2. Age: 20-40 years old
3. Skin texture: acne muscle
Test/effective population: 60/60
Table 4 content of clinical test

Claims (10)

1. A mild non-irritating cosmetic composition comprising azelaic acid, characterized in that: the raw materials at least comprise the following components in percentage by mass: 1 to 20 percent of azelaic acid, 15 to 20 percent of softening agent, 0.1 to 5 percent of rheological modifier, 5 to 15 percent of humectant, 0.1 to 5 percent of auxiliary agent, 10 to 30 percent of grease and the balance of water.
2. A mild non-irritating cosmetic composition containing azelaic acid according to claim 1, characterized in that: the softening agent is at least one of polyethylene glycol, polymethyl silsesquioxane, hydroxypropyl starch phosphate and polysorbate.
3. A mild non-irritating cosmetic composition containing azelaic acid according to claim 2, characterized in that: the softening agent is polymethyl silsesquioxane and hydroxypropyl starch phosphate, and the mass ratio of the polymethyl silsesquioxane to the hydroxypropyl starch phosphate is 14-18:1-2.
4. A mild non-irritating cosmetic composition containing azelaic acid according to claim 3, wherein: the rheology modifier is at least one of acrylic acid (ester)/C10-30 alkanol acrylate cross-linked polymer, dimethyl silyl silica, ethyl cellulose, distearyl dimethylamine hectorite, hydroxypropyl cellulose and polyvinyl alcohol.
5. The mild non-irritating cosmetic composition containing azelaic acid according to claim 4, wherein: the rheology modifier is acrylic acid (ester)/C10-30 alkanol acrylate cross-linked polymer and dimethyl silyl silica.
6. The mild non-irritating cosmetic composition containing azelaic acid according to claim 5, wherein: the mass ratio of the acrylic acid (ester)/C10-30 alkanol acrylate cross-linked polymer to the dimethylsilylated silica is 0.1-0.2: 0 to 0.8.
7. The mild non-irritating cosmetic composition containing azelaic acid according to claim 6, wherein: the humectant is at least one of propylene glycol, glycerol, butanediol, 1, 2-hexanediol, hyaluronic acid and hydrolyzed collagen.
8. The mild non-irritating cosmetic composition containing azelaic acid according to claim 7, wherein: the oil and fat is at least one of cyclomethicone, cyclopentadimethicone, cyclohexasiloxane, octyl dimethicone, dioctyl ether and hydrogenated polyisobutene.
9. The mild non-irritating cosmetic composition containing azelaic acid according to claim 8, wherein: the auxiliary agent is at least one of chelating agent, preservative, emulsifier, auxiliary emulsifier and pH regulator.
10. A process for the preparation of a mild non-irritating cosmetic composition containing azelaic acid according to claim 9, characterized in that: the method comprises the following steps: (1) Uniformly mixing part of the softening agent and the grease at room temperature to obtain a phase A, mixing and dissolving the auxiliary agent and part of water to obtain a phase B, mixing part of the humectant and the rheology modifier at 60-80 ℃ and homogenizing to obtain a phase D for later use; (2) Homogenizing the phase B in the phase D for 2-5 min, cooling to 40-45 ℃ after complete homogenization, dispersing the residual soft lubricant and the residual humectant to obtain phase C, and homogenizing the phase D for 2-5 min; (3) Adding the phase D into the phase A, stirring and emulsifying, and adding azelaic acid into the mixture for homogenizing for 4-10 min after homogenizing.
CN202311034902.2A 2023-08-16 2023-08-16 Mild non-irritating cosmetic composition containing azelaic acid and preparation method thereof Pending CN117045524A (en)

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