Cosmetic composition and preparation method thereof

Abstract

The invention provides a cosmetic composition and a preparation method thereof. In particular, the cosmetic composition comprises: a linear saturated dicarboxylic acid having 4 to 10 carbon atoms; mandelic acid or a derivative thereof; and polyaspartic acid or a derivative thereof. The cosmetic composition according to the technical scheme of the invention contains higher content of straight-chain saturated dicarboxylic acid with 4-10 carbon atoms, and has excellent cutin removal and acne inhibition effects when azelaic acid is used as the straight-chain saturated dicarboxylic acid with 4-10 carbon atoms.

Description

Technical Field

[0001] This invention relates to the field of cosmetic technology, and more specifically, it provides a cosmetic composition and a method for preparing the same. Background Technology

[0002] Lower straight-chain saturated dicarboxylic acids (e.g., succinic acid, glutaric acid, adipic acid, pimelic acid, octanoic acid, azelaic acid, and sebacic acid) are widely used in cosmetics as pH adjusters, moisturizers, and skin conditioning agents. However, these lower straight-chain saturated dicarboxylic acids generally have low solubility in water, which limits their application to some extent.

[0003] Furthermore, among these lower straight-chain saturated dicarboxylic acids, azelaic acid has a variety of uses, including but not limited to: improving skin pigmentation, anti-aging, improving skin texture, reducing sebum secretion, antimicrobial properties, reducing erythema and inflammation, and promoting skin repair. Due to these properties, azelaic acid is widely used in various skincare products, such as cleansers, toners, serums, creams, and masks.

[0004] Healthy skin has a slightly acidic surface, so most skincare products use a slightly acidic system. This slightly acidic environment helps maintain healthy skin, including its natural defense mechanisms and microbial balance. However, azelaic acid has relatively low solubility in water, especially under slightly acidic conditions. Due to its low solubility, special formulation techniques are usually required to prepare azelaic acid to a concentration and form suitable for cosmetic use. For example, existing technologies use glycol compounds as solvents for azelaic acid. However, these methods involve the use of large amounts of glycols, which may cause side effects such as skin irritation and stickiness. In addition, some non-glycolic acid ingredients are also used as solubilizers to improve the solubility and stability of azelaic acid. For example, CN108187070A discloses a method for preparing a hydroxypropyl-β-cyclodextrin / azeliaic acid complex; US6734210B2 discloses a water-soluble salt of a mixture of azeliaic acid and chitosan; CN117843472A discloses a composition of azeliaic acid and tranexamic acid; and CN113248364A relates to a combination of azeliaic acid and alkaloids. However, these prior art methods all require pretreatment to prepare the azeliaic acid complex, the process is complex, and the specific effect of the complex in the complete formulation is unclear.

[0005] Therefore, it is of great significance to develop a cosmetic composition with a high content of low-grade straight-chain saturated dicarboxylic acids (especially azelaic acid) and its preparation method. Summary of the Invention

[0006] Based on the technical problems described above, the purpose of this invention is to provide a cosmetic composition and its preparation method. The cosmetic composition according to the technical solution of this invention contains a high content of a straight-chain saturated dicarboxylic acid with 4 to 10 carbon atoms, and when azelaic acid is used as the straight-chain saturated dicarboxylic acid with 4 to 10 carbon atoms, it has excellent exfoliating and acne-inhibiting effects.

[0007] The inventor completed this invention through in-depth and meticulous research.

[0008] According to one aspect of the present invention, a cosmetic composition is provided, the cosmetic composition comprising:

[0009] Straight-chain saturated dicarboxylic acids having 4 to 10 carbon atoms;

[0010] Mandelic acid or its derivatives; and

[0011] Polyaspartic acid or its derivatives.

[0012] According to another aspect of the present invention, a method for preparing a cosmetic composition is provided, the method comprising: mixing a straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms, mandelic acid or a derivative thereof, and polyaspartic acid or a derivative thereof.

[0013] Compared with the prior art in this field, the advantages of the present invention are as follows:

[0014] 1. Improve the solubility of straight-chain saturated dicarboxylic acids with 4 to 10 carbon atoms under weakly acidic conditions: The present invention significantly improves the solubility of straight-chain saturated dicarboxylic acids (especially azelaic acid) with 4 to 10 carbon atoms under acidic pH conditions by combining polyaspartic acid or its derivatives with mandelic acid or its derivatives.

[0015] 2. No pretreatment step required: Compared with the prior art, the method according to the present invention can achieve effective dissolution of azelaic acid without pretreatment, which simplifies the preparation process;

[0016] 3. Synergistic effect of exfoliation and acne inhibition: In the presence of polyaspartic acid or its derivatives, the combination of azelaic acid and mandelic acid or their derivatives shows excellent synergistic effect in exfoliation and acne inhibition;

[0017] 4. Safety and irritation: Compared with existing technologies that use large amounts of glycol as solvents for azelaic acid, the present invention reduces potential skin irritation and discomfort. Detailed Implementation

[0018] It should be understood that, without departing from the scope or spirit of this disclosure, those skilled in the art can conceive of various other embodiments and can modify them based on the teachings of this specification. Therefore, the following specific embodiments are not intended to be limiting.

[0019] Unless otherwise specified, all figures used in this specification and claims to indicate feature dimensions, quantities, and physical properties should be understood to be modified by the term "about" in all cases. Therefore, unless stated to the contrary, the numerical parameters listed in the foregoing specification and appended claims are approximations, and those skilled in the art can appropriately modify these approximations to obtain the desired characteristics using the teachings disclosed herein. The use of numerical ranges indicated by endpoints includes all numbers within that range and any range within that range; for example, 1 to 5 includes 1, 1.1, 1.3, 1.5, 2, 2.75, 3, 3.80, 4, and 5, etc.

[0020] Unless otherwise specified, the technical terms used in this specification have the same meaning as commonly understood by those skilled in the art.

[0021] As used herein, the term "dicarboxylic acid" means that a dicarboxylic acid can be prepared by synthetic methods or isolated from natural sources, and can be in mixed forms or in pure or substantially pure forms. All physical forms of dicarboxylic acids, including crystalline, semi-crystalline, and amorphous forms, are within the scope of this invention.

[0022] As used herein, the term “physiologically acceptable” has the meaning known in the art and refers to compounds, materials, compositions and / or dosage forms that are suitable for contact with human and animal tissues without causing excessive toxicity, irritation, allergic reactions or other problems or complications, within a reasonable physiological judgment.

[0023] Cosmetic Composition

[0024] As mentioned above, lower straight-chain saturated dicarboxylic acids (e.g., succinic acid, glutaric acid, adipic acid, pimelic acid, octanoic acid, azelaic acid, and sebacic acid) have limited applications to some extent due to their low solubility in water. In particular, azelaic acid has limited solubility in aqueous solutions, especially at acidic pH levels, which restricts its use in skincare products. Insufficient solubility may result in azelaic acid not being evenly distributed in the product or failing to effectively penetrate the skin, affecting the product's efficacy. Effectively formulating azelaic acid into skincare products presents a challenge due to its solubility. While existing techniques have attempted to improve the solubility of azelaic acid using glycols or other solubilizers, these methods have limitations. For example, glycols may cause skin irritation and discomfort, while non-glycol solubilizers require pretreatment to prepare the complex, and their effectiveness in the final product formulation is unclear.

[0025] The inventors of this invention have discovered that by using a combination of mandelic acid or its derivatives and polyaspartic acid or its derivatives in specific amounts, the solubility of lower straight-chain saturated dicarboxylic acids (e.g., succinic acid, glutaric acid, adipic acid, pimelic acid, octanoic acid, azelaic acid, and sebacic acid) in skin care products can be significantly improved, especially the solubility under acidic pH conditions.

[0026] Specifically, the present invention provides a cosmetic composition comprising:

[0027] Straight-chain saturated dicarboxylic acids having 4 to 10 carbon atoms;

[0028] Mandelic acid or its derivatives; and

[0029] Polyaspartic acid or its derivatives.

[0030] According to certain preferred embodiments of the invention, the straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms (e.g., physiologically acceptable straight-chain saturated dicarboxylic acids having 4 to 10 carbon atoms) is selected from one or more of succinic acid, glutaric acid, adipic acid, pimelic acid, octanoic acid, azelaic acid, and sebacic acid. The straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms is preferably a straight-chain saturated dicarboxylic acid having 6 to 10 carbon atoms, most preferably one or more of azelaic acid, azelaic acid, and sebacic acid. More preferably, the straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms is azelaic acid.

[0031] According to certain preferred embodiments of the present invention, the cosmetic composition comprises, by weight 100%, 0.1-20% by weight, preferably 0.5-10% by weight, more preferably 1-5% by weight, and most preferably 1-2% by weight of the linear saturated dicarboxylic acid having 4 to 10 carbon atoms. The inventors of the present invention have surprisingly discovered that, in the presence of polyaspartic acid or its derivatives, a specific amount of azelaic acid and a specific amount of mandelic acid or its derivatives exhibit a synergistic effect in exfoliation and acne suppression.

[0032] The inventors of this invention discovered in their research that simultaneously adding mandelic acid or a derivative thereof and polyaspartic acid or a derivative thereof to an aqueous system can enhance the solubility of straight-chain saturated dicarboxylic acids having 4 to 10 carbon atoms under acidic conditions. Mandelic acid or a derivative thereof that can be used in this invention has a structure represented by the following general formula (I):

[0033]

[0034] in:

[0035] R1 and R2 are each independently hydrogen, halogen atom, hydroxyl group, or carbonyl group; and

[0036] R3 is hydrogen or a metal cation.

[0037] In the above general formula (I), the halogen atom is selected from one or more of fluorine, chlorine, and iodine atoms. Furthermore, in the above general formula (I), the metal cation is a sodium cation or a potassium cation.

[0038] According to certain preferred embodiments of the present invention, the mandelic acid or its derivative is mandelic acid.

[0039] According to the technical solution of the present invention, mandelic acid or its derivatives are added to the skin care system in combination with polyaspartic acid or its derivatives, thereby improving the solubility of the straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms under weakly acidic conditions. Furthermore, by specifically controlling the ratio of the straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms (especially azelaic acid), mandelic acid or its derivatives, and polyaspartic acid or its derivatives, the straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms (especially azelaic acid), mandelic acid or its derivatives can achieve a synergistic effect in exfoliation and acne inhibition. Preferably, based on 100% of the total weight of the cosmetic composition, the cosmetic composition contains 0.5-10% by weight, preferably 0.5-8% by weight, more preferably 0.5-4% by weight of the mandelic acid or its derivatives.

[0040] As described above, the inventors of this invention discovered in their research that the solubility of the straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms under acidic conditions can be enhanced by simultaneously adding mandelic acid or a derivative thereof and polyaspartic acid or a derivative thereof to an aqueous system. According to certain embodiments of the invention, the polyaspartic acid derivative may be a polyaspartate salt, such as a physiologically acceptable polyaspartate salt. The polyaspartate salt may be selected from one or more of polyaspartic metal salts and polyaspartic ammonium salts. For example, the polyaspartate salt may be selected from one or more of sodium polyaspartate, potassium polyaspartate, calcium polyaspartate, magnesium polyaspartate, aluminum polyaspartate, and ammonium polyaspartate, more preferably sodium polyaspartate.

[0041] The polyaspartic acid or its derivatives that can be used in this invention have a structure represented by the following general formula (II):

[0042]

[0043] in:

[0044] The sum of m and n is 2 to 10000, preferably 10-1000, and more preferably 200-500. For example, the sum of the number of repeating units m+n can be 2, 10, 50, 100, 150, 250, 300, 350, 400, 450, 500, 550, 600, 650, 700, 750, 800, 850, 900, 950, 1000, 2000, 3000, 4000, 5000, 6000, 8000, 10000, or a range defined by any two of them;

[0045] The ratio of m to n can be (0-100):(100-0), for example, it can be 0, 10:90, 20:80, 30:70, 40:60, 50:50, 60:40, 70:30, 80:20, 90:10, or a range defined by any two of them.

[0046] R1 and R2 can be independently selected from H, -OH, and -(O). p One or more of G, wherein p is 0 or 1, and G is selected from substituted or unsubstituted C1-C12 hydrocarbon groups, such as C1-C12 alkyl groups, particularly C1-C6 alkyl groups, such as methyl, ethyl, n- or iso-propyl, n-, iso-, tert- or sec-butyl, n-, iso-, tert- or sec-pentyl, or n-, iso-, tert- or sec-hexyl. In a preferred embodiment, R1 and R2 may each be H independently.

[0047] M1 and M2 can each be independently selected from one or more of H, metal cations, and ammonium cations.

[0048] Preferably, the metal cation is selected from one or more of sodium cation, potassium cation, calcium cation, magnesium cation and aluminum cation.

[0049] Preferably, in order to achieve the technical effect of the present invention, in the above general formula (II), the sum of m and n is an integer from 10 to 50; R1 and R2 are H; M1 and M2 are independently selected from one or more of H, metal cations and ammonium cations, wherein the metal cation is selected from one or more of sodium cations, potassium cations, calcium cations, magnesium cations and aluminum cations.

[0050] Preferably, the polyaspartic acid or its derivative is sodium polyaspartate.

[0051] Preferably, the weight-average molecular weight of the sodium polyaspartate is in the range of 300 to 100,000, particularly 2,000-50,000, for example, 2,000-10,000. For example, the weight-average molecular weight of the polyaspartic acid or its derivatives may be 1,000, 2,000, 3,000, 4,000, 5,000, 6,000, 7,000, 8,000, 9,000, 10,000, 11,000, 12,000, 13,000, 14,000, 15,000, 16,000, 17,000, 18,000, 19,000, 20,000, 21,000, 22,000, 23,000, or 24,000. 25000, 26000, 27000, 28000, 29000, 30000, 31000, 32000, 33000, 34000, 35000, 36000, 37000, 38000, 39000, 40000, 41000, 42000, 43000, 44000, 45000, 46000, 47000, 48000, 49000, 50000, 5 1000, 52000, 53000, 54000, 55000, 56000, 57000, 58000, 59000, 60000, 61000, 62000, 63000, 64000, 65000, 66000, 67000, 68000, 69000, 70000, 71000, 72000, 73000, 74000, 75000, 76000, 77 000, 78000, 79000, 80000, 81000, 82000, 83000, 84000, 85000, 86000, 87000, 88000, 89000, 90000, 91000, 92000, 93000, 94000, 95000, 96000, 97000, 98000, 99000, 100000, or a range defined by any two of them.

[0052] According to the technical solution of the present invention, polyaspartic acid or its derivatives are added to the skin care system in combination with mandelic acid or its derivatives, thereby improving the solubility of the straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms under weakly acidic conditions. Furthermore, by specifically controlling the ratio of the straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms (especially azelaic acid), mandelic acid or its derivatives, and polyaspartic acid or its derivatives, the straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms (especially azelaic acid), mandelic acid or its derivatives can achieve a synergistic effect in exfoliation and acne inhibition. Preferably, based on 100% of the total weight of the cosmetic composition, the cosmetic composition contains 0.02-50% by weight, preferably 0.05-20% by weight, more preferably 0.1-5% by weight, even more preferably 0.1-1% by weight, and most preferably 0.1-0.3% by weight of polyaspartic acid or its derivatives.

[0053] According to certain preferred embodiments of the present invention, in order to achieve the synergistic effect of the straight-chain saturated dicarboxylic acid (especially azelaic acid) having 4 to 10 carbon atoms, mandelic acid, or derivatives thereof on exfoliation and acne inhibition while increasing the solubility of the straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms under weakly acidic conditions, the cosmetic composition comprises, by weight 100%, the following:

[0054] 1-2% by weight of the straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms (especially azelaic acid);

[0055] 0.5-4% by weight of the said mandelic acid or its derivatives; and

[0056] 0.1-0.3% by weight of polyaspartic acid or its derivatives.

[0057] In addition to the linear saturated dicarboxylic acids, mandelic acid or their derivatives, and polyaspartic acid or their derivatives having 4 to 10 carbon atoms mentioned above, the cosmetic compositions according to the present invention may also contain one or more other ingredients to achieve one or more additional functions, provided that the presence of these other ingredients does not impair the effects of the present invention.

[0058] Specifically, the cosmetic composition according to the invention may further comprise one or more solvents. The solvent may be a physiologically acceptable solvent suitable for use in topical formulations or cosmetics. The solvent may be water or an organic solvent (including solvents miscible with water), preferably water. The organic solvent is selected from one or more of ethanol, propylene glycol, etc. For example, the solvent content may be 25-95% by weight, based on the total weight of the composition. For example, the solvent (e.g., water) content may be 25% by weight, 30% by weight, 35% by weight, 40% by weight, 45% by weight, 50% by weight, 55% by weight, 60% by weight, 65% by weight, 70% by weight, 75% by weight, 80% by weight, 85% by weight, 90% by weight, 95% by weight, or a range defined by any two thereof, based on the total weight of the composition.

[0059] According to certain preferred embodiments of the invention, the cosmetic composition further comprises a solubilizer. Specific examples of solubilizers that can be used in the invention include polyethylene glycol-40 hydrogenated castor oil (CREMOPHOR RH-40). Preferably, the cosmetic composition contains 2-5% by weight of the solubilizer, based on 100% of the total weight of the cosmetic composition.

[0060] Preferably, the cosmetic composition according to the invention may further contain one or more plant extracts, such as extracts from various plants (e.g., chamomile, green tea, etc.).

[0061] Preferably, the cosmetic composition according to the invention may further contain one or more sunscreens, such as UVA and UVB chemical sunscreens, physical sunscreens, etc.

[0062] Preferably, the cosmetic composition according to the present invention may further contain one or more vitamins and antioxidants, such as vitamins E, C, A, D, K and their derivatives.

[0063] Preferably, the cosmetic composition according to the present invention may further contain one or more preservatives, such as quaternary ammonium compounds, parabens, etc.

[0064] Preferably, the cosmetic composition according to the invention may further contain one or more colorants, such as inorganic or organic pigments for providing color.

[0065] In some embodiments, the composition may further comprise a diol (e.g., a physiologically acceptable diol), preferably a straight-chain alkane diol, more preferably selected from straight-chain alkane diols having 2-8 carbon atoms, such as one or more selected from ethylene glycol, propylene glycol, butanediol, pentanediol, hexanediol, heptahydrate, and octanediol, with pentanediol being even more preferred. The inventors have found that when a diol compound is further added to a cosmetic composition comprising a straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms, mandelic acid or a derivative thereof, and polyaspartic acid or a derivative thereof, the solubility of a straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms (e.g., azelaic acid) in aqueous solution can be further improved.

[0066] In a further embodiment, when present, the weight ratio of the diol to a straight-chain saturated dicarboxylic acid (e.g., azelaic acid) having 4 to 10 carbon atoms may be 0.1:1 to 10:1, particularly 1:1 to 5:1, and more particularly 2:1 to 5:1. For example, the weight ratio of the diol to the straight-chain saturated dicarboxylic acid (e.g., azelaic acid) having 4 to 10 carbon atoms may be 0.1:1, 0.15:1, 0.2:1, 0.25:1, 0.3:1, 0.35:1, 0.4:1, 0.45:1, 0.5:1, 0.55:1, 0.6:1, 0.65:1, 0.7:1, 0.75:1, 0.8:1, 0.85:1, 0.9:1, 0.95:1, 1:1, 2:1, 3:1, 4:1, 5:1, 6:1, 7:1, 8:1, 9:1, 10:1, or a range defined by any two thereof.

[0067] In a further embodiment, when present, the content of the diol may be 0.1 wt% to 70 wt%, for example 1 wt% to 50 wt%, particularly 1 wt% to 10 wt%, more particularly 2 wt% to 5 wt%, based on the total weight of the composition. For example, the content of the diol may be 0.1 wt%, 0.15 wt%, 0.2 wt%, 0.25 wt%, 0.3 wt%, 0.35 wt%, 0.4 wt%, 0.45 wt%, 0.5 wt%, 0.55 wt%, 1 wt%, 1.5 wt%, 2 wt%, 2.5 wt%, 3 wt%, 3.5 wt%, 4 wt%, 4.5 wt%, 5 wt%, 5.5 wt%, 6 wt%, 6.5 wt%, 7 wt%, 7.5 wt%, 8 wt%, 8.5 wt%, 9 wt%, 9.5 wt%, 10 wt%, 20 wt%, 30 wt%, 40 wt%, 50 wt%, 60 wt%, 70 wt%, or a range defined by any two thereof, based on the total weight of the composition.

[0068] In some embodiments, the cosmetic composition may be an acidic composition. For example, the pH of the acidic composition may be a physiologically acceptable pH value. For example, the pH of the cosmetic composition may be 3.0-6.0, preferably 4.0-5.5, more preferably 4.5-5.0, for example, it may be 3.0, 3.5, 4.0, 4.5, 5.0, 5.5, 6.0, 6.5, or a range defined by any two thereof. The inventors have discovered that even under acidic conditions, such as pH within the above-mentioned range, the linear saturated dicarboxylic acid (e.g., azelaic acid) having 4 to 10 carbon atoms exhibits enhanced solubility in aqueous solutions by combining it with mandelic acid or a derivative thereof, polyaspartic acid or a derivative thereof.

[0069] In some embodiments, the composition may further comprise one or more components selected from: surfactants, such as cationic surfactants, anionic surfactants, amphoteric surfactants and / or nonionic surfactants; thickeners, such as polysaccharide thickeners, silicone elastomers and / or acrylate polymers; and anti-inflammatory ingredients. The components may be appropriately selected depending on the intended use and are not particularly limited thereto. The amounts of each component are not particularly limited and can be selected independently and appropriately according to the intended use. For example, the amounts of each component can be 0.05-10% by weight, such as 0.05% by weight, 0.1% by weight, 0.2% by weight, 0.3% by weight, 0.4% by weight, 0.5% by weight, 1% by weight, 1.5% by weight, 2% by weight, 2.5% by weight, 3% by weight, 3.5% by weight, 4% by weight, 4.5% by weight, 5% by weight, 5.5% by weight, 6% by weight, 6.5% by weight, 7% by weight, 7.5% by weight, 8% by weight, 8.5% by weight, 9% by weight, 9.5% by weight, 10% by weight, or a range defined by any two thereof, based on the total weight of the composition.

[0070] Examples of suitable surfactants include, but are not limited to: polysorbate-20, polysorbate-40, polysorbate-60, lecithin, hydrogenated lecithin, stearyl alcohol polyether-20, PEG-100 stearate, PEG-40 hydrogenated castor oil, polyglycerol-10 laurate, polyglycerol-10 oleate, polyglycerol-10 stearate, polyglycerol-5 oleate, polyglycerol-6 stearate, PPG-6-decyltetradecyl alcohol polyether-30, PPG-26-butanol polyether-26, etc.

[0071] Examples of suitable thickeners include, but are not limited to: xanthan gum, guar gum, carrageenan, poloxamer, carbomer, sodium hyaluronate, acrylate / C10-30 alkanol acrylate crosspolymers, etc. Specific examples of thickeners that can be used as synthetic polymers in this invention include those manufactured by Vanderbilt Minerals. NF (a type of xanthan gum) is a powdered polymer with thickening, stabilizing, and texture-modifying properties.

[0072] Suitable oils and fats include, but are not limited to: silicone oils, esters, vegetable oils, synthetic oils (including volatile and non-volatile oils), mineral oils, petrolatum, etc.

[0073] Examples of suitable anti-inflammatory ingredients include, but are not limited to: salicylic acid and its physiologically acceptable salts, dipotassium glycyrrhizate, 4-tert-butylcyclohexanol, witch hazel extract, bisabolol, olive leaf extract, etc.

[0074] In some embodiments, the cosmetic composition may further comprise a chemical peeling agent, examples of suitable chemical peeling agents including glycolic acid, citric acid, lactic acid, malic acid, pyruvic acid, tartaric acid, mandelic acid, salicylic acid, lactobionic acid, maltodextrin, gluconolactone, etc.

[0075] In some embodiments, the cosmetic composition may further comprise other additives, provided that these additives are physically and chemically compatible with the ingredients in the composition, dissolve in the composition, and do not impair the therapeutic or cosmetic properties of the composition. Examples of such other additives include, but are not limited to, moisturizing compounds, vitamins, antioxidants, and film-forming polymers. Examples of suitable moisturizing compounds include, but are not limited to, butylene glycol, betaine, N-2-hydroxyethyl urea, polyol ethers and esters, low molecular weight polyethylene glycol, lactates, sugars, methyl gluconate, sodium pyrrolidone carboxylate, sodium hyaluronate, panthenol, and hyaluronic acid. Examples of suitable vitamins include, but are not limited to, tocopherol phosphate, vitamin B2 and its derivatives, vitamin B3 and its derivatives such as niacinamide, and vitamin C and its derivatives. Examples of suitable antioxidants include, but are not limited to, green tea extract, grape seed extract, flavonoids, inositol and its derivatives, glutathione, cysteine ​​and its derivatives, proline, and carnitine and its derivatives. Preferably, the cosmetic composition according to the invention may also comprise one or more moisturizing agents, such as glycerin, butylene glycol, and pentylene glycol. Specific examples of butylene glycol that can be used in this invention include 1,3-butanediol produced by KH NEOCHEM. Preferably, the cosmetic composition contains 40-50% by weight of a moisturizer, based on 100% of the total weight of the cosmetic composition.

[0076] In some embodiments, the composition may further comprise other ingredients as needed, including but not limited to: skin penetration enhancers, chelating agents, preservatives, colorants, inorganic salts, pH adjusters, fragrances, etc. Examples of suitable skin penetration enhancers include, but are not limited to: tetrahydropiperine, isosorbide dimethyl ether, hexanediol, and butylene glycol. Examples of suitable chelating agents include, but are not limited to: ethylenediaminetetraacetic acid (EDTA), ethylene glycol diethyl ether diaminetetraacetic acid (EDTA), and their physiologically acceptable salts. Examples of suitable inorganic salts include, but are not limited to: sodium chloride, magnesium sulfate, and zinc chloride. Examples of suitable pH adjusters include, but are not limited to: sodium hydroxide, potassium hydroxide, and aqueous solutions of hydrogen chloride.

[0077] In one embodiment, the cosmetic composition may be a topical composition, particularly for treating skin disorders such as pigmentation, melasma, dark spots, acne, or pimples; for increasing the penetration of active ingredients; for promoting epidermal exfoliation; for brightening skin tone and reducing hyperpigmentation; for controlling oil production; for enhancing skin barrier function; or for making skin smooth and soft.

[0078] In one embodiment, the cosmetic composition may be a brightening composition, a spot-removing composition, an oil-controlling composition, an exfoliating composition, or an acne-removing composition.

[0079] The cosmetic compositions according to the present invention can be designed in various forms such as lotions, gels, powders, and foams to suit different skin types and skincare needs. Lotions can be water-in-oil or oil-in-water types, gels provide a refreshing feel, powders are used for setting makeup or absorbing oil, and foams are often used for gentle cleansing. Furthermore, the packaging and application methods of the cosmetic compositions according to the present invention are extremely diverse, including portable and easy-to-use sprays and aerosols.

[0080] Preferably, the cosmetic composition is a skin care composition.

[0081] Preparation method

[0082] According to another aspect of the present invention, a method for preparing a cosmetic composition is provided, the method comprising: uniformly mixing the above-described straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms, mandelic acid or a derivative thereof, and polyaspartic acid or a derivative thereof, along with optional water and additives.

[0083] There are no particular limitations on the mixing methods that can be used in this invention, and the mixing methods conventionally used in this invention can be used. For example, there are no particular limitations on the mixing order of the components. For example, the components can be mixed together or sequentially; all components can be added and dissolved in the total amount of solvent in a certain order, either all at once or in batches; or some components can be added and dissolved in a portion of solvent or a solvent in a certain order, while the remaining components are added and dissolved in another portion of solvent in a certain order, either all at once or in batches, and then the resulting solutions are combined.

[0084] The components contained in the cosmetic composition are as described in the section on the composition above, and will not be repeated here.

[0085] The following detailed description is intended to illustrate the contents of this disclosure by way of example and not by way of limitation.

[0086] Specific embodiment 1 is a cosmetic composition, the cosmetic composition comprising:

[0087] Straight-chain saturated dicarboxylic acids having 4 to 10 carbon atoms;

[0088] Mandelic acid or its derivatives; and

[0089] Polyaspartic acid or its derivatives.

[0090] Specific embodiment 2 is a cosmetic composition according to specific embodiment 1, wherein the straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms is azelaic acid.

[0091] Specific embodiment 3 is a cosmetic composition according to specific embodiment 1, wherein, based on the total weight of the cosmetic composition as 100%, the cosmetic composition contains 0.1-20% by weight, preferably 0.5-10% by weight, more preferably 1-5% by weight, and most preferably 1-2% by weight of the straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms.

[0092] Specific embodiment 4 is a cosmetic composition according to specific embodiment 1, wherein the mandelic acid or its derivative has a structure represented by the following general formula (I):

[0093]

[0094] in:

[0095] R1 and R2 are each independently hydrogen, halogen atom, hydroxyl group, or carbonyl group; and

[0096] R3 is hydrogen or a metal cation.

[0097] Specific embodiment 5 is a cosmetic composition according to specific embodiment 4, wherein the metal cation is a sodium cation or a potassium cation.

[0098] Specific embodiment 6 is a cosmetic composition according to specific embodiment 1, wherein the mandelic acid or its derivative is mandelic acid.

[0099] Specific embodiment 7 is a cosmetic composition according to specific embodiment 1, wherein, based on the total weight of the cosmetic composition as 100%, the cosmetic composition contains 0.5-10% by weight, preferably 0.5-8% by weight, more preferably 0.5-4% by weight of the mandelic acid or its derivatives.

[0100] Specific embodiment 8 is a cosmetic composition according to specific embodiment 1, wherein the polyaspartic acid or its derivative has a structure represented by the following general formula (II):

[0101]

[0102] in:

[0103] The sum of m and n is 2 to 10000, preferably 10-1000, and more preferably 200-500;

[0104] R1 and R2 are independently selected from H, -OH, and -(O). p One or more of G, where p is 0 or 1, and G is selected from substituted or unsubstituted C1-C. 12 hydrocarbon groups;

[0105] M1 and M2 are independently selected from one or more of H, metal cations, and ammonium cations.

[0106] Specific embodiment 9 is a cosmetic composition according to specific embodiment 8, wherein the metal cation is selected from one or more of sodium cation, potassium cation, calcium cation, magnesium cation or aluminum cation.

[0107] Specific embodiment 10 is a cosmetic composition according to specific embodiment 1, wherein the polyaspartic acid or its derivative is sodium polyaspartic acid.

[0108] Specific embodiment 11 is a cosmetic composition according to specific embodiment 10, wherein the weight average molecular weight of the sodium polyaspartate is in the range of 300 to 100,000, preferably 2,000 to 50,000, and more preferably 2,000 to 10,000.

[0109] Specific embodiment 12 is a cosmetic composition according to specific embodiment 1, wherein, based on the total weight of the cosmetic composition as 100%, the cosmetic composition contains 0.02-50% by weight, preferably 0.05-20% by weight, more preferably 0.1-5% by weight, even more preferably 0.1-1% by weight, and most preferably 0.1-0.3% by weight of polyaspartic acid or its derivatives.

[0110] Specific embodiment 13 is a cosmetic composition according to specific embodiment 1, wherein, based on the total weight of the cosmetic composition as 100%, the cosmetic composition comprises:

[0111] 1-2% by weight of the straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms;

[0112] 0.5-4% by weight of the said mandelic acid or its derivatives; and

[0113] 0.1-0.3% by weight of polyaspartic acid or its derivatives.

[0114] Specific embodiment 14 is a cosmetic composition according to specific embodiment 1, wherein the cosmetic composition further contains 25-95% by weight of water, based on 100% of the total weight of the cosmetic composition.

[0115] Specific embodiment 15 is a cosmetic composition according to specific embodiment 1, wherein the cosmetic composition further comprises a solubilizer.

[0116] Specific embodiment 16 is a cosmetic composition according to specific embodiment 1, wherein the cosmetic composition further comprises a moisturizer.

[0117] Specific embodiment 18 is a cosmetic composition according to specific embodiment 1, wherein the cosmetic composition is a skin care composition.

[0118] Specific embodiment 19 is a method for preparing a cosmetic composition, the method comprising: mixing a straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms, mandelic acid or a derivative thereof, and polyaspartic acid or a derivative thereof according to any one of embodiments 1-18.

[0119] The present invention will now be described in more detail with reference to embodiments. It should be noted that these descriptions and embodiments are intended to facilitate understanding of the invention and are not intended to limit the invention. The scope of protection of the present invention is defined by the appended claims.

[0120] Example

[0121] In this invention, unless otherwise specified, all reagents used are commercially available products and are used directly without further purification.

[0122] Table 1 Raw Material List

[0123]

[0124] Azelaic acid solubility performance test

[0125] Example 1 (E1)

[0126] 1 g of azelaic acid powder, 0.5 g of mandelic acid, and 0.1 g of sodium polyaspartate (weight average molecular weight 5000) were added to water, followed by the addition of sodium hydroxide to adjust the pH of the system to 4.9. The mixture was then stirred for 24 hours and sonicated to completely and uniformly disperse the azelaic acid powder, thereby obtaining cosmetic composition 1. In cosmetic composition 1, based on 100% of the total weight of cosmetic composition 1, the cosmetic composition 1 contains 1% by weight of azelaic acid, 0.5% by weight of mandelic acid, and 0.1% by weight of sodium polyaspartate.

[0127] Next, the solubility of azelaic acid in the cosmetic composition 1 was characterized. Specifically, 200 μL of cosmetic composition 1 was taken using a pipette. The obtained sample was added to a 96-well plate for turbidity determination. Subsequently, the absorbance of the sample was measured at a wavelength of 700 nm using an ELISA reader (INFINITE E PLEX, TECAN, Austria). The absorbance value was recorded; a higher absorbance value indicates higher turbidity of the sample, meaning that more azelaic acid remained undissolved. According to the experimental results of the present invention, when the normalized absorbance value based on Comparative Example 1 (C1) is less than or equal to 0.6, the solubility of azelaic acid in the cosmetic composition is considered to have reached a "high" level.

[0128] The proportions of each component in Example 1 above and the results of the azelaic acid solubility test (absorbance value) are shown in Table 2 below.

[0129] Examples 2-8 (E2-E8) and Comparative Examples 1-4 (C1-C4)

[0130] Examples 2-8 and Comparative Examples 1-4 were conducted in a manner similar to Example 1, except that the proportions of the various components were changed as shown in Table 2 below to obtain cosmetic compositions 2-8 and comparative cosmetic compositions 1-4, respectively. Mandelic acid was not used in the raw materials of Comparative Examples 1-3.

[0131] The solubility of azelaic acid in cosmetic compositions 2-8 and comparative cosmetic compositions 1-4 was characterized according to the azelaic acid solubility characterization method described in detail in Example 1. The proportions of each component in Examples 2-8 and Comparative Examples 1-4 and the obtained azelaic acid solubility test results (absorbance values) are shown in Table 2 below.

[0132]

[0133] The data in Table 2 clearly show that the solubility of azelaic acid increases with increasing amounts of sodium polyaspartate and mandelic acid. The normalized absorbance values ​​decrease with increasing amounts of sodium polyaspartate and mandelic acid, indicating a decrease in turbidity in the solution, i.e., a reduction in undissolved azelaic acid. The experimental results demonstrate a synergistic effect between azelaic acid and mandelic acid in the presence of sodium polyaspartate, which further enhances the solubility of azelaic acid.

[0134] Increasing the amount of sodium polyaspartate and mandelic acid can effectively improve the solubility of azelaic acid in cosmetic compositions, which is of great significance for preparing skin care products with uniform distribution of active ingredients. Exfoliation test (exfoliated skin) Peeling effect test)

[0135] Example 9 (E9)

[0136] 2g of azelaic acid powder, 4g of mandelic acid, 0.3g of sodium polyaspartate (weight average molecular weight 5000), 5g of solubilizer polyethylene glycol 40 hydrogenated castor oil (CREMOPHOR RH-40), and 50g of moisturizer 1,3-butanediol were added to water, followed by the addition of sodium hydroxide to adjust the pH of the system to 4.5. The mixture was then stirred thoroughly at 50°C until completely dissolved, thus obtaining cosmetic composition 9. In cosmetic composition 9, based on 100% of the total weight of cosmetic composition 9, the cosmetic composition 9 contains 2% by weight of azelaic acid, 4% by weight of mandelic acid, and 0.3% by weight of sodium polyaspartate. Furthermore, tests showed that the solubilizer polyethylene glycol 40 hydrogenated castor oil (CREMOPHOR RH-40) and the moisturizer 1,3-butanediol did not negatively affect the solubility, exfoliating, and acne-inhibiting properties of azelaic acid.

[0137] Subsequently, the exfoliation efficacy of the cosmetic composition 9 was tested according to the following steps. Specifically, the exfoliated skin was incubated overnight in an incubator after cleaning. The next day, the exfoliated skin was equilibrated at room temperature for several hours, and the exfoliated skin was then subjected to an incubation period of 145 mm. 210 μL of the cosmetic composition was applied to the area of ​​the sample. Four hours later, the excised skin was rinsed with water, and the rinse fluid was collected. The eluted cells were labeled with a fluorescent dye (NanoOrange, ThermoFisher). Cell images were taken using a Keyence Fluorescence Microscope, and the number of eluted cells was counted using image analysis (Keyence software).

[0138] The proportions of each component in Example 9 above and the test results of the exfoliation effect of the obtained skin are shown in Table 3 below.

[0139] Comparative Examples 5-7 (C5-C7)

[0140] Comparative Examples 5-7 were prepared in a manner similar to that of Example 9, except that the proportions of the various components were changed as shown in Table 3 below to obtain comparative cosmetic compositions 5-7.

[0141] The exfoliation effect of comparative cosmetic compositions 5-7 was characterized according to the exfoliation effect characterization method described in Example 9. The proportions of each component in the above comparative examples 5-7 and the obtained exfoliation effect test results are shown in Table 3 below.

[0142] Table 3 shows the proportions of each component in Example 9 (E9) and Comparative Examples 5-7 (C5-C7) and the test results of the exfoliative skin peeling effect.

[0143]

[0144] Wherein: the symbol "—" indicates that the corresponding component is not present.

[0145] The data in Table 3 demonstrate that the combination of azelaic acid and mandelic acid or their derivatives exhibits excellent synergistic effects in exfoliation and acne suppression in the presence of polyaspartic acid or its derivatives. This synergistic effect may contribute to the development of more effective skincare products that can more effectively remove dead skin cells and promote skin renewal.

[0146] Acne Inhibition Test (Propionibacterium acnes inhibition zone test)

[0147] Example 10 (E10)

[0148] 1 g of azelaic acid powder, 4 g of mandelic acid, 0.3 g of sodium polyaspartate (weight average molecular weight 5000), 2 g of solubilizer polyethylene glycol 40 hydrogenated castor oil (CREMOPHOR RH-40), and 40 g of moisturizer 1,3-butanediol were added to water, followed by the addition of sodium hydroxide to adjust the pH of the system to 4.5. The mixture was then stirred thoroughly at 50°C until completely dissolved, thus obtaining cosmetic composition 10. In cosmetic composition 10, based on 100% of the total weight of cosmetic composition 10, the cosmetic composition 10 contains 1% by weight of azelaic acid, 4% by weight of mandelic acid, and 0.3% by weight of sodium polyaspartate. Furthermore, testing showed that the solubilizer polyethylene glycol 40 hydrogenated castor oil (CREMOPHOR RH-40) and the moisturizer 1,3-butanediol did not negatively affect the solubility, exfoliating, and acne-inhibiting properties of azelaic acid.

[0149] Subsequently, the cosmetic composition 10 was subjected to a Propionibacterium acnes inhibition zone test. The Propionibacterium acnes inhibition zone test is a commonly used laboratory test to evaluate the inhibitory effect of active ingredients in cosmetic formulations on Propionibacterium acnes. Specifically, Propionibacterium acnes (C. acnes; BNCC336649, Beina Biotechnology Co., Ltd.) was incubated at 37°C until the absorbance (OD600) reached approximately 0.1, indicating that the bacteria had grown to a sufficient concentration. The cultured Propionibacterium acnes was evenly swabbed onto an agar plate. Holes were punched in the agar plate using a 6mm agar punch, with consistent depth and diameter to ensure experimental accuracy. 100 μL of the cosmetic composition 10 sample was added to the punched holes. The agar plate was incubated in an anaerobic environment at 37°C for 96 hours to promote bacterial growth. After incubation, the inhibition zone around each hole was observed. The inhibition zone refers to the area where bacteria cannot grow, and its size reflects the antibacterial effect of the active ingredient in the cosmetic formulation. Measure and record the diameter of the inhibition zone around each well. Generally, the larger the diameter of the inhibition zone, the better the antibacterial effect of the sample.

[0150] The proportions of each component in Example 10 above and the acne inhibition test results are shown in Table 4 below.

[0151] Comparative Examples 8-10 (C8-C10)

[0152] Comparative Examples 8-10 were prepared in a manner similar to that of Example 10, except that the proportions of the various components were changed as shown in Table 4 below to obtain comparative cosmetic compositions 8-10.

[0153] The acne-inhibiting properties of comparative cosmetic compositions 8-10 were characterized according to the acne-inhibiting test characterization method described in detail in Example 10. The proportions of each component in the above comparative examples 8-10 and the results of the obtained acne-inhibiting properties are shown in Table 4 below.

[0154] Table 4 shows the proportions of each component in Example 10 (E10) and Comparative Examples 8-10 (C8-C10) and the results of the Propionibacterium acnes inhibition zone experiment.

[0155]

[0156]

[0157] Wherein: the symbol "—" indicates that the corresponding component is not present.

[0158] Table 4 above shows the inhibitory effects of different formulations on Propionibacterium acnes using the inhibition zone test. As can be seen from Table 4, compared to C9 and C10, the diameter of the inhibition zone in Example 10 was significantly larger, indicating a synergistic effect between azelaic acid and mandelic acid, which can more effectively inhibit the growth of Propionibacterium acnes.

[0159] Although specific embodiments have been shown and described herein, those skilled in the art will understand that various alternative and / or equivalent embodiments can be used instead of the shown and described specific embodiments without departing from the scope of the invention. This application is intended to include any improvements or modifications to the specific embodiments discussed herein. Therefore, the invention is limited only to the claims and their equivalents.

[0160] Those skilled in the art will understand that various modifications and alterations can be made without departing from the scope of the invention. Such modifications and alterations are intended to fall within the scope of the invention as defined in the appended claims.

Claims

1. A cosmetic composition comprising: Straight-chain saturated dicarboxylic acids having 4 to 10 carbon atoms; Mandelic acid or its derivatives; and Polyaspartic acid or its derivatives.

2. The cosmetic composition according to claim 1, wherein the straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms is azelaic acid.

3. The cosmetic composition according to claim 1, wherein, based on 100% of the total weight of the cosmetic composition, the cosmetic composition comprises 0.1-20% by weight, preferably 0.5-10% by weight, more preferably 1-5% by weight, and most preferably 1-2% by weight of the straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms.

4. The cosmetic composition according to claim 1, wherein the mandelic acid or its derivative has a structure represented by the following general formula (I): in: R1 and R2 are each independently hydrogen, halogen atom, hydroxyl group, or carbonyl group; and R3 is hydrogen or a metal cation.

5. The cosmetic composition according to claim 4, wherein the metal cation is a sodium cation or a potassium cation.

6. The cosmetic composition according to claim 1, wherein the mandelic acid or its derivative is mandelic acid.

7. The cosmetic composition according to claim 1, wherein, based on 100% of the total weight of the cosmetic composition, the cosmetic composition comprises 0.5-10% by weight, preferably 0.5-8% by weight, more preferably 0.5-4% by weight of the mandelic acid or its derivatives.

8. The cosmetic composition according to claim 1, wherein the polyaspartic acid or a derivative thereof has a structure represented by the following general formula (II): in: The sum of m and n is 2 to 10000, preferably 10-1000, and more preferably 200-500; R1 and R2 are independently selected from H, -OH, and -(O). p One or more of G, where p is 0 or 1, and G is selected from substituted or unsubstituted C1-C. 12 hydrocarbon groups; M1 and M2 are independently selected from one or more of H, metal cations, and ammonium cations.

9. The cosmetic composition according to claim 8, wherein the metal cation is selected from one or more of sodium cations, potassium cations, calcium cations, magnesium cations, and aluminum cations.

10. The cosmetic composition according to claim 1, wherein the polyaspartic acid or its derivative is sodium polyaspartate.

11. The cosmetic composition according to claim 10, wherein the sodium polyaspartate has a weight-average molecular weight in the range of 300 to 100,000, preferably 2,000 to 50,000, and more preferably 2,000 to 10,000.

12. The cosmetic composition according to claim 1, wherein, based on 100% of the total weight of the cosmetic composition, the cosmetic composition comprises 0.02-50% by weight, preferably 0.05-20% by weight, more preferably 0.1-5% by weight, even more preferably 0.1-1% by weight, and most preferably 0.1-0.3% by weight of polyaspartic acid or its derivatives.

13. The cosmetic composition according to claim 1, wherein, based on 100% of the total weight of the cosmetic composition, the cosmetic composition comprises: 1-2% by weight of the straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms; 0.5-4% by weight of the said mandelic acid or its derivatives; and 0.1-0.3% by weight of polyaspartic acid or its derivatives.

14. The cosmetic composition according to claim 1, wherein the cosmetic composition further comprises 25-95% by weight of water, based on 100% of the total weight of the cosmetic composition.

15. The cosmetic composition according to claim 1, wherein the cosmetic composition further comprises a solubilizer.

16. The cosmetic composition according to claim 1, wherein the cosmetic composition further comprises a moisturizer.

17. The cosmetic composition according to claim 1, wherein the cosmetic composition is a skin care composition.

18. A method for preparing a cosmetic composition, the method comprising: Mix a straight-chain saturated dicarboxylic acid having 4 to 10 carbon atoms, mandelic acid or a derivative thereof, and polyaspartic acid or a derivative thereof, according to any one of claims 1-17.

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