CN115463044B - Brightening composition containing supermolecule azelaic acid and preparation method thereof - Google Patents

Brightening composition containing supermolecule azelaic acid and preparation method thereof Download PDF

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Publication number
CN115463044B
CN115463044B CN202111213497.1A CN202111213497A CN115463044B CN 115463044 B CN115463044 B CN 115463044B CN 202111213497 A CN202111213497 A CN 202111213497A CN 115463044 B CN115463044 B CN 115463044B
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azelaic acid
supermolecule
agent
solvent
preparation
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CN202111213497.1A
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CN115463044A (en
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聂敏仪
郑家成
洪嘉峻
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Guangzhou Hua Chu Xian Biotech Co ltd
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Guangzhou Hua Chu Xian Biotech Co ltd
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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
    • A61K8/44Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • 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
    • A61K8/67Vitamins
    • A61K8/673Vitamin B group
    • A61K8/675Vitamin B3 or vitamin B3 active, e.g. nicotinamide, nicotinic acid, nicotinyl aldehyde
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/59Mixtures
    • A61K2800/592Mixtures of compounds complementing their respective functions

Abstract

The invention relates to the field of A61K8/9789, in particular to a brightening composition containing supermolecule azelaic acid and a preparation method thereof, wherein the preparation raw materials comprise: supermolecule azelaic acid, assistant and solvent. The invention solves the problem of low solubility of the supermolecule azelaic acid with various cosmetic compositions in high addition amount in the prior art by adjusting the pH value of the system, the prepared brightening composition has long-acting low temperature resistant and high temperature resistant effects and good stability.

Description

Brightening composition containing supermolecule azelaic acid and preparation method thereof
Technical Field
The invention relates to the field of A61K8/9789, in particular to a brightening composition containing supermolecule azelaic acid and a preparation method thereof.
Background
Azelaic acid is also called azalea acid, is an organic compound with various effects of brightening, anti-inflammatory, oil control and the like, has extremely low solubility in water (about 2.4g/L in water), and affects the use as an effect product. The azelaic acid is directly added in the form of fine powder in the market, the low solubility of the azelaic acid leads to granular feel and poor sensory use of the product, or the azelaic acid is added in the form of modification or solubilization, but the property of the azelaic acid is inevitably partially changed to influence the efficacy, or the solvent which is not needed by the formula is introduced, so that the product does not accord with the direction of the current mainstream of consumption which is advocated green, environment-friendly and simplified.
CN110623949a discloses a whitening and thinning skin-action composition containing azelaic acid monometal salt and Mo Nuoben parts and a preparation method thereof, wherein azelaic acid is ground into fine powder or modified azelaic acid derivative is used and added into the composition, the former cannot dissolve azelaic acid, the efficacy is greatly reduced, and the latter changes the properties of azelaic acid, and the consumption is increased, so that the cost is increased.
CN112624918A discloses a eutectic crystal of azelaic acid and organic base and a preparation method thereof, wherein the eutectic crystal of azelaic acid and organic base is used for improving the water solubility of the former, and although the water solubility of azelaic acid is improved, the application of azelaic acid in an aqueous system is still limited. This application only tested the use of eutectic azelaic acid added at 0.5%, but products with too low efficacy are not readily available in the market, so it is very necessary to find a formulation stabilization method with a use level of 0.5% or more.
Disclosure of Invention
In a first aspect, the present invention provides a lightening composition comprising supramolecular azelaic acid prepared from the following raw materials: supermolecule azelaic acid, assistant and solvent.
As a preferred embodiment, the auxiliary agent includes at least one of sodium hydroxide, arginine, lysine, and histidine.
The present invention is not particularly limited to the auxiliary agent, and any of the above substances which can be used as an alkaline pH adjustor in the cosmetic field may be used.
The auxiliary agent is mainly used for adjusting the pH value of the system, thereby adjusting the solubility of the supermolecule azelaic acid in the system and the compatibility of the supermolecule azelaic acid with other substances.
As a preferred embodiment, the solvent comprises water and/or an aqueous solution of a plant extract.
As a preferred embodiment, the weight ratio of the supramolecular azelaic acid to the auxiliary agent is 1: (0.25-1.2).
As a preferred embodiment, the pH of the lightening composition is from 6.0 to 7.0.
Azelaic acid has extremely low solubility in water, and azelaic acid fine powder or other solvent added to assist dissolution is generally adopted in the prior art, but granular feel or unnecessary solvent components can be brought to influence the application in the field of cosmetics.
Supermolecule azelaic acid is a supermolecule eutectic compound formed by polymerizing azelaic acid and nicotinamide by using supermolecule self-assembly technology and supermolecule modification technology, and the successful preparation of supermolecule azelaic acid can improve the solubility of the supermolecule azelaic acid in water, but only improves partial solubility compared with untreated azelaic acid, the solubility of the supermolecule azelaic acid in water is still not high, white crystals are extremely easy to agglomerate and separate out in the form of particles, and the dosage, the formula, the system, the pH and compatibility raw materials are limited to certain requirements.
The applicant has unexpectedly found that by adjusting the pH of the cosmetic composition to be slightly alkaline, the solubility of supramolecular azelaic acid in the present system can be adjusted, and the resulting composition has high-temperature, low-temperature stability, in particular at-10 ℃ and 45 ℃ for 3 months, without any precipitation. Considering that the pH value of the system is unsuitable for the pH value of skin when the pH value is more than 7, the system is unsuitable for the production of cosmetic compositions, and the cold resistance of the composition containing supermolecule azelaic acid is remarkably reduced when the pH value is less than 6, the composition can be separated out at-10 ℃, and the application prospect is not provided. The applicant speculates that the reason may be that at a pH of 6-7, the ionization of supramolecular azelaic acid is accelerated and the tightness of the copolymerization of azelaic acid and nicotinamide is improved, whereas at a pH of less than 6, the non-covalent forces between the azelaic acid and nicotinamide eutectic compound are reduced, the two are separated from each other, the copolymerization forces are reduced, azelaic acid returns to the free state, and the solubility is reduced.
As a preferred embodiment, the preparation raw material further comprises: moisturizing agent, brightening agent and soothing agent.
As a preferred embodiment, the humectant comprises at least one of hydrolyzed sodium hyaluronate, glucosyl glycerate, beta-glucan, ceramide, dipropylene glycol, glycerin, 1, 3-propanediol, 1, 2-hexanediol, decanediol, nonanediol, octanediol.
Preferably, the humectant is hydrolyzed sodium hyaluronate, glyceroglycosides, beta-glucan, ceramide, glycerol.
Preferably, the weight ratio of the hydrolyzed sodium hyaluronate, the glyceroglycosides, the beta-glucan, the ceramide and the glycerol is (0.03-0.1): (0.1-2): (0.1-2): (0.05-0.5): (5-15).
Preferably, the weight ratio of the hydrolyzed sodium hyaluronate to the glyceroglycosides to the beta-glucan to the ceramide to the glycerol is 0.07:0.5:1.5:0.3:10.
the applicant finds that the supermolecule azelaic acid selected by the invention has better compatibility with hydrolyzed sodium hyaluronate, glyceroglycosides, beta-glucan, ceramide and glycerin, can fully exert the moisturizing effect, and does not influence the moisturizing effect of the composition due to the fluctuation of pH value.
As a preferred embodiment, the brightening agent includes at least one of nicotinamide, tranexamic acid, vitamin C, and arbutin.
Preferably, the brightening agent is nicotinamide or tranexamic acid.
Preferably, the weight ratio of nicotinamide to tranexamic acid is (1-5): (0.5-2).
The optimal pH value of nicotinamide is 6, and the optimal pH value of tranexamic acid is 7-8, however, in order to adapt to the solubility of supramolecular azelaic acid, the pH value of a system is required to be maintained at 6-7, which leads to limited lightening effect of nicotinamide and tranexamic acid and influences the lightening effect of the composition. The applicant has unexpectedly found that when nicotinamide and tranexamic acid are mixed in a weight ratio of (1-5): when (0.5-2) is compounded, the lightening effect of the composition can be remarkably improved under the condition that the pH value is 6-7, and the reason the applicant speculates is that under the condition that the proportion, the composition and the supermolecule azelaic acid can have synergistic action, the respective optimal pH values are balanced, the low-temperature dissolution effect of the supermolecule azelaic acid is met, and the lightening effect of nicotinamide and tranexamic acid is fully exerted.
As a preferred embodiment, the soothing agent includes at least one of allantoin, paeonia extract, aloe extract, juglans mandshurica extract, linseed extract, centella extract, scutellaria baicalensis extract, rose extract, lavender extract.
The present invention is not particularly limited to soothing agents, and any one or more of the above extracts may be incorporated into the composition to provide a soothing effect.
As a preferred embodiment, the preparation raw material further comprises: essential oil and antiseptic.
The present invention is not particularly limited to essential oils, and essential oils commonly used in the cosmetic arts to enhance the fragrance of the composition may include, but are not limited to, rose essential oils.
The present invention is not particularly limited to preservatives, and preservatives commonly used in the cosmetic arts that provide preservative efficacy to the composition may include, but are not limited to, phenoxyethanol, and chlorpheniramine.
In a second aspect, the present invention provides a process for the preparation of a lightening composition comprising supramolecular azelaic acid, said process comprising: adding humectant into solvent, heating for dissolving, cooling, adding supermolecule azelaic acid and relieving agent dissolved by adjuvant and solvent, and stirring.
Compared with the prior art, the invention has the following beneficial effects:
1. the invention solves the problem that azelaic acid with high addition amount is difficult to be separated out in water and at low temperature, and provides a new solution for the application of azelaic acid in the cosmetic field.
2. The invention solves the problem of reduced solubility of the supermolecule azelaic acid and various cosmetic compositions in the prior art by adjusting the pH value of the system, and the prepared brightening composition has long-acting low-temperature resistance and high-temperature resistance effects and good stability.
3. The weight ratio of nicotinamide to tranexamic acid is (1-5): (0.5-2) and solves the balance of the effects of dissolving and brightening supermolecule azelaic acid, nicotinamide and tranexamic acid at the pH value of 6-7.
4. The brightening composition prepared by the invention has very remarkable brightening effect after two weeks of use, and can exist stably for a long time.
5. The brightening composition prepared by the invention has good solubility, no granular feel and no introduction of other solvents, and accords with the concept of current green cosmetics.
Drawings
Figures 1-3 are all results of the lightening effect test.
Fig. 4 is the stability test results of example 1 and comparative example 1.
Detailed Description
The material information in the present invention is as follows:
hydrolyzed sodium hyaluronate was purchased from Muvana organisms
Beta-glucan was purchased from Sizithrombi
Paeonia lactiflora extract was purchased from Cia Siraibang Biotechnology Co., ltd
Rose essential oils were purchased from Guangzhou City, jia beautification cosmetics Co., ltd
Example 1
In a first aspect, this example provides a lightening composition comprising supramolecular azelaic acid prepared from the following raw materials in parts by weight: 3 parts of supermolecule azelaic acid, 0.75 part of auxiliary agent, 75 parts of solvent, 14.87 parts of humectant, 5 parts of brightening agent, 0.6 part of soothing agent, 0.2 part of essential oil and 0.4 part of preservative.
The auxiliary agent is sodium hydroxide.
The solvent is water.
The humectant is hydrolyzed sodium hyaluronate, glyceroglycosides, beta-glucan, ceramide and glycerin, and the weight ratio of the humectant to the glycerol is 0.07:0.5:1.5:0.3: and 10, compounding.
The brightening agent is nicotinamide and tranexamic acid, and the weight ratio of the brightening agent to tranexamic acid is 3:2, compounding.
The soothing agent is allantoin and paeonia lactiflora (latin academy Paeonia lactiflora pall.) extract with a weight ratio of 1:5, compounding.
The essential oil is rose (La Ding Xueming: rosa rugosa Thunb.) essential oil.
The preservative is phenoxyethanol.
The pH of the lightening composition was 6.01.
In a second aspect, this embodiment provides a process for preparing a lightening composition comprising supramolecular azelaic acid, the process comprising: adding humectant into solvent, heating for dissolving, cooling, adding supermolecule azelaic acid and relieving agent dissolved by aid and solvent, adding brightening agent, continuously adding the rest raw materials, and stirring uniformly.
Comparative example 1
In a first aspect, this comparative example provides a lightening composition comprising supramolecular azelaic acid, the specific embodiment being the same as example 1, except that 0 parts of auxiliary agent is present, the lightening composition having a pH of 4.7.
In a second aspect, this comparative example provides a process for preparing a lightening composition comprising supramolecular azelaic acid, the embodiments being as in example 1.
Performance testing
Whitening effect test: 10 female volunteers aged 25-35 years were selected for skin ITA value, and 5g of the lightening composition of example 1 was applied uniformly to the face after cleansing with clear water every day, and the skin ITA value was measured for 2 weeks after adhering to the face. Test data for 10 volunteers are shown in table 1.
The ITA value test method comprises the following steps: images were taken using visual-CR and analyzed using Mirror Photo Tools.
TABLE 1
Volunteer numbering ITA value before use ITA value after 2 weeks Difference value
1 38.34 40.11 1.77
2 36.68 37.09 0.41
3 37.14 37.9 0.76
4 38.19 38.64 0.45
5 32.79 34.72 1.93
6 33.71 36.87 3.16
7 40.25 42.85 2.6
8 43.65 44.6 0.95
9 35.19 35.96 0.77
10 36.04 36.46 0.42
And (3) brightness enhancement effect test: 3 female volunteers aged 25-30 years were selected, and the brightening composition of example 1 was applied to the face uniformly after cleansing with clear water in the morning and evening every day, and the face was kept for 2 weeks, and the pictures of the face before and after 2 weeks were recorded by photographing in the plain state, respectively, see fig. 1-3, the left picture before use, and the right picture after 2 weeks of use.
Stability test the compositions of example 1, comparative example 1 were placed in an environment at-10 ℃ for 3 months and the appearance of the composition after 3 months was recorded by photographing, see fig. 4.

Claims (2)

1. A lightening composition comprising supramolecular azelaic acid, characterized in that the raw materials for the preparation comprise: 3 parts of supramolecular azelaic acid, 0.75 part of auxiliary agent, 75 parts of solvent, 14.87 parts of humectant, 5 parts of brightening agent, 0.6 part of soothing agent, 0.2 part of essential oil and 0.4 part of preservative;
the supermolecular azelaic acid is a supermolecular eutectic compound formed by polymerizing azelaic acid and nicotinamide;
the auxiliary agent is sodium hydroxide;
the solvent is water;
the humectant is hydrolyzed sodium hyaluronate, glyceroglycosides, beta-glucan, ceramide and glycerin, and the weight ratio of the humectant to the glycerol is 0.07:0.5:1.5:0.3:10, compounding;
the brightening agent is nicotinamide and tranexamic acid, and the weight ratio of the brightening agent to tranexamic acid is 3:2, compounding;
the soothing agent is allantoin and paeonia lactiflora extract in a weight ratio of 1:5, compounding;
the essential oil is rose essential oil;
the preservative is phenoxyethanol;
the pH of the lightening composition was 6.01.
2. A process for the preparation of a lightening composition comprising supramolecular azelaic acid according to claim 1, characterized in that it comprises: adding humectant into solvent, heating for dissolving, cooling, adding supermolecule azelaic acid and relieving agent dissolved by aid and solvent, adding brightening agent, continuously adding the rest raw materials, and stirring uniformly.
CN202111213497.1A 2021-10-19 2021-10-19 Brightening composition containing supermolecule azelaic acid and preparation method thereof Active CN115463044B (en)

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EP1663148A2 (en) * 2003-08-25 2006-06-07 Foamix Ltd. Penetrating pharmaceutical foam
CN104718214A (en) * 2012-05-31 2015-06-17 国立科学研究中心 Improved organic-inorganic hybrid solid having a modified outer surface
CN106852126A (en) * 2014-06-04 2017-06-13 阿尔邦国际有限公司 Transparent composition and method for delivering skin nursing active component
CN112624918A (en) * 2020-12-18 2021-04-09 深圳市萱嘉生物科技有限公司 Eutectic of azelaic acid and organic base as well as preparation method and application thereof

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Publication number Priority date Publication date Assignee Title
US20160144038A1 (en) * 2014-11-20 2016-05-26 Broda International, LLC Water-soluble supramolecular complexes

Patent Citations (5)

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Publication number Priority date Publication date Assignee Title
EP1663148A2 (en) * 2003-08-25 2006-06-07 Foamix Ltd. Penetrating pharmaceutical foam
CN104718214A (en) * 2012-05-31 2015-06-17 国立科学研究中心 Improved organic-inorganic hybrid solid having a modified outer surface
CN106852126A (en) * 2014-06-04 2017-06-13 阿尔邦国际有限公司 Transparent composition and method for delivering skin nursing active component
EP3151923A4 (en) * 2014-06-04 2018-01-03 Arbonne International LLC Clear compositions and methods for the delivery of active ingredients for skin care
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