Composition, use thereof and method for preparing the same
Patent Information
- Application Number
- HK42026125926
- Authority / Receiving Office
- HK · HK
- Patent Type
- Applications
- Current Assignee / Owner
- Filing Date
- 2026-07-09
- Publication Date
- 2026-09-18
- Estimated Expiration
- 2044-08-07
Abstract
Description
(19) State Intellectual Property Office (12) Invention Patent Application (10) Application Publication Number (43) Application Publication Date (21) Application Number 202411085486.3 (22) Application Date 2024.08.08 (71) Applicant ELC Management LLC Address New York, USA (72) Inventors Cao Feng Yao Jizong Zhou Huanjun N. Karaman-Yulukovska Gao Yinghong (74) Patent Agency Beijing Liu Shen Law Firm 11105 Patent Attorney Song Li (51) Int.Cl. A61K 8 / 362 (2006.01) A61K 8 / 88 (2006.01) A61Q 19 / 00 (2006.01) A61Q 19 / 02 (2006.01) A61K 31 / 194 (2006.01) A61K 31 / 20 (2006.01) A61K 47 / 34 (2017.01) A61P 17 / 00 (2006.01) A61P 17 / 10 (2006.01) (54) Title of Invention: Composition, Use Thereof and Method of Preparation Thereof (57) Abstract This invention relates to a composition, the use of said composition in the preparation of topical formulations or cosmetics, and a method for preparing said composition. The composition comprises a linear saturated dicarboxylic acid and polyaspartic acid or a derivative thereof, wherein said polyaspartic acid or a derivative thereof is present in an amount of 0.01% by weight or more, preferably 0.1% by weight or more, more preferably 0.1% by weight to 35% by weight, even more preferably 0.1% by weight to 2% by weight, and even more preferably 0.3% by weight to 0.5% by weight, based on the total weight of said composition. By combining a linear saturated dicarboxylic acid (e.g., azelaic acid) with polyaspartic acid or a derivative thereof, the solubility of the linear saturated dicarboxylic acid (e.g., azelaic acid) in aqueous solution can be improved, thereby enhancing its skin permeability when used, for example, in cosmetics, and thus maximizing its efficacy. Claims 2 pages, Description 9 pages, CN 121489804 A 2026.02.10 CN 1 21 48 98 04 A 1. A composition comprising: a linear saturated dicarboxylic acid, and polyaspartic acid or a derivative thereof, wherein the content of said polyaspartic acid or a derivative thereof is 0.01% by weight or more, preferably 0.1% by weight or more, more preferably 0.1% by weight to 35% by weight, even more preferably 0.1% by weight to 2% by weight, and even more preferably 0.3% by weight to 0.5% by weight, based on the total weight of said composition. 2. The composition of claim 1, wherein the weight ratio of the polyaspartic acid or its derivative to the straight-chain saturated dicarboxylic acid is 0.01:1 to 20:1, particularly 0.1:1 to 5:1, more particularly 0.2:1 to 1:1, and especially 0.3:1 to 0.5:1.3. The composition of claim 1 or 2, wherein the straight-chain saturated dicarboxylic acid is a straight-chain saturated dicarboxylic acid having 6-10 carbon atoms, preferably one or more of azelaic acid, azelaic acid, and sebacic acid, more preferably azelaic acid. 4. The composition of claim 1 or 2, wherein the polyaspartic acid derivative is a polyaspartate salt, such as a physiologically acceptable polyaspartate salt, preferably one or more of sodium polyaspartate, potassium polyaspartate, calcium polyaspartate, magnesium polyaspartate, aluminum polyaspartate, and ammonium polyaspartate, more preferably sodium polyaspartate. 5. The composition of claim 1 or 2, wherein the polyaspartic acid or its derivative is represented by the following formula 1: wherein the sum of the number of repeating units m+n is 2-10000, preferably 10-1000, more preferably 200-500; R1 and R2 are each independently selected from one or more of H, OH and (O)pG, wherein p is 0 or 1, G is selected from substituted or unsubstituted C1-C12 hydrocarbon groups, such as C1-C12 alkyl groups, preferably R1 and R2 are each independently H; and M1 and M2 are each independently selected from one or more of H, metal cations and ammonium cations, preferably the metal is selected from one or more of sodium, potassium, calcium, magnesium and aluminum. 6. The composition of claim 1 or 2, wherein the polyaspartic acid or its derivative has a weight-average molecular weight of 1000-100000, particularly 2000-50000, for example 2000-8000 or 10000-30000, preferably 10000-15000. 7. The composition of claim 1 or 2, wherein the content of the linear saturated dicarboxylic acid is 0.1 wt% to 20 wt%, preferably 0.5 wt% to 10 wt%, more preferably 1 wt% to 5 wt%, based on the total weight of the composition. 8. The composition of claim 1 or 2, wherein the polyaspartic acid or its derivative has a weight-average molecular weight of 10,000 to 15,000, and satisfies one or more of the following characteristics (i)-(ii): (i) the weight ratio of the polyaspartic acid or its derivative to the linear saturated dicarboxylic acid is 0.1:1 to 0.5:1, preferably 0.1:1 to 0.3:1, and (ii) the content of the polyaspartic acid or its derivative is 0.1 wt% to 0.5 wt%, more preferably 0.1 wt% to 0.3 wt%, based on the total weight of the composition. Claims 1 / 2 Page 2 CN 121489804 A 9. The composition according to claim 1 or 2, wherein the composition further comprises a diol, preferably a straight-chain saturated diol, more preferably selected from straight-chain saturated diols having 2-8 carbon atoms, and even more preferably selected from one or more of propylene glycol, butanediol, pentanediol, hexanediol and heptanediol.10. The composition of claim 9, wherein the weight ratio of the diol to the straight-chain saturated dicarboxylic acid is 0.1:1 to 10:1, particularly 1:1 to 5:1, more particularly 2:1 to 5:1. 11. The composition of claim 9, wherein the content of the diol is 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. 12. The composition of claim 1 or 2, wherein the pH of the composition is 3.0 to 6.0, preferably 4.0 to 5.5, more preferably 4.5 to 5.0. 13. The composition of claim 1 or 2, wherein the composition further comprises a solvent, particularly water. 14. The composition of claim 1 or 2, wherein the composition is a topical composition, particularly for treating skin disorders such as pigmentation, melasma, freckles, 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. 15. The composition of claim 1 or 2, wherein the composition is a cosmetic composition, particularly a brightening composition, a spot-reducing composition, an oil-controlling composition, an exfoliating composition, or an acne-reducing composition. 16. The composition of claim 1 or 2, wherein the composition further comprises one or more ingredients 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; oils; inorganic salts; pH adjusters; and anti-inflammatory ingredients. 17. Use of the composition of any one of claims 1-16 for the preparation of topical formulations or cosmetics. 18. A method for preparing a composition according to any one of claims 1-16, comprising: mixing the components contained in the composition. Claims 2 / 2 Page 3 CN 121489804 A Composition, Use Thereof and Preparation Method Technical Field
[0001] The present invention relates to compositions comprising linear saturated dicarboxylic acids and polyaspartic acid (PASP) or derivatives thereof, such as topical compositions or cosmetic compositions. The present invention also relates to the use of the compositions in the preparation of topical formulations or cosmetics and methods for preparing the compositions. Background Art
[0002] Linear saturated dicarboxylic acids are commonly used ingredients in topical formulations or cosmetics. In particular, azelaic acid, as a naturally occurring linear saturated dicarboxylic acid, has been shown to have good efficacy in treating many skin diseases, including acne, hyperpigmentation, melasma, chloasma, pimples, etc.Azelaic acid is also widely used in cosmetics, where it has functions such as anti-oil and anti-acne, brightening and whitening, softening and moisturizing, gentle exfoliation and skin conditioning.
[0003] However, straight-chain saturated dicarboxylic acids (e.g., azelaic acid) used in topical formulations or cosmetics typically have very limited solubility in aqueous solutions, especially at acidic pH values. For example, azelaic acid has a low solubility of only 0.24 g in 100 g of water at 25°C. This solubility problem makes straight-chain saturated dicarboxylic acids such as azelaic acid have very limited solubility in topical or cosmetic formulations, making it difficult to fully penetrate the skin, which greatly limits their efficacy.
[0004] Therefore, there is still a need to find a composition comprising straight-chain saturated dicarboxylic acids that can improve the solubility of straight-chain saturated dicarboxylic acids such as azelaic acid in aqueous solutions, so that they can fully penetrate the skin when used, for example, in topical formulations or cosmetics. Summary of the Invention
[0005] The present invention was made in view of the above-mentioned problems existing in the prior art.
[0006] In a first aspect, the present invention relates to a composition comprising: a linear saturated dicarboxylic acid, and polyaspartic acid or a derivative thereof, wherein the polyaspartic acid or a derivative thereof is present in an amount of 0.01% by weight or more, preferably 0.1% by weight or more, more preferably 0.1% by weight to 35% by weight, even more preferably 0.1% by weight to 2% by weight, and even more preferably 0.3% by weight to 0.5% by weight, based on the total weight of the composition.
[0007] In a second aspect, the present invention relates to the use of the composition for preparing topical formulations or cosmetics.
[0008] In a third aspect, the present invention relates to a method for preparing the composition, comprising: mixing the components contained in the composition.
[0009] The inventors have discovered that when linear saturated dicarboxylic acids and polyaspartic acid or its derivatives are used in combination, especially when polyaspartic acid or its derivatives are added in a specific amount, more preferably in a specific ratio, or when polyaspartic acid or its derivatives of a specific molecular weight are added, the solubility of linear saturated dicarboxylic acids (e.g., azelaic acid) in aqueous solutions, especially in acidic aqueous solutions, is improved. This results in improved skin permeability when used, for example, in cosmetics, thereby enabling the desired therapeutic or cosmetic effects. Detailed Description
[0010] To make the inventive objectives, technical solutions, and beneficial technical effects of this application clearer, the following will provide a detailed description of this application (page 1 / 9, CN 121489804 A). It should be noted that the various aspects, features, embodiments, and advantages described in this application are compatible and / or can be combined together.
[0011] Unless otherwise specified, the technical terms in this specification have the same meaning as commonly understood by those skilled in the art.
[0012] 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.
[0013] 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 within a reasonable physiological judgment without causing excessive toxicity, irritation, allergic reactions or other problems or complications.
[0014] Unless otherwise stated, all amounts referred to herein are amounts by mass, and all percentages are based on the weight percentage of the total composition.
[0015] This invention relates to compositions, their uses and methods of preparation thereof. The invention will be specifically described below.
[0016] Compositions
[0017] In a first aspect, this invention relates to a composition comprising a linear saturated dicarboxylic acid and polyaspartic acid or a derivative thereof.
[0018] Polyaspartic acid or its derivatives belong to protein-like polymers with peptide bond structures, are easily biodegradable, and possess excellent properties such as safety, non-toxicity, low irritation, and environmental friendliness.
[0019] The inventors have discovered that by combining linear saturated dicarboxylic acids (e.g., azelaic acid) with polyaspartic acid or its derivatives, the solubility of the linear saturated dicarboxylic acid (e.g., azelaic acid) in aqueous solutions, especially acidic aqueous solutions, can be improved. This results in improved skin permeability when used, for example, in topical preparations or cosmetics, thereby maximizing its efficacy.
[0020] The content of the polyaspartic acid or its derivatives may be 0.01% by weight or more, preferably 0.1% by weight or more, more preferably 0.1% by weight to 35% by weight, even more preferably 0.1% by weight to 2% by weight, and even more preferably 0.3% by weight to 0.5% by weight, based on the total weight of the composition.For example, the content of the polyaspartic acid or its derivatives may be 0.01 wt%, 0.05 wt%, 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%, 11 wt%. 12 wt%, 13 wt%, 14 wt%, 15 wt%, 16 wt%, 17 wt%, 18 wt%, 19 wt%, 20 wt%, 21 wt%, 22 wt%, 23 wt%, 24 wt%, 25 wt%, 26 wt%, 27 wt%, 28 wt%, 29 wt%, 30 wt%, 31 wt%, 32 wt%, 33 wt%, 34 wt%, 35 wt%, or a range defined by any two thereof, based on the total weight of the composition. When the content of polyaspartic acid or its derivatives is within the above range, the solubility of straight-chain saturated dicarboxylic acids (e.g., azelaic acid) in aqueous solution can be significantly improved.
[0021] Therefore, in one embodiment, the content of the straight-chain saturated dicarboxylic acid may be 0.1 wt% to 20 wt%, preferably 0.5 wt% to 10 wt%, more preferably 1 wt% to 5 wt%, based on the total weight of the composition. For example, the content of the straight-chain saturated dicarboxylic acid may be 0.1 wt%, 0.2 wt%, 0.3 wt%, 0.4 wt%, 0.5 wt%, 0.6 wt%, 0.7 wt%, 0.8 wt%, 0.9 wt%, 1 wt%, 2 wt%, 3 wt%, 4 wt%, 5 wt%, 6 wt%, 7 wt%, 8 wt%, 9 wt%, 10 wt%, 11 wt%, 12 wt%, 13 wt%, 14 wt%, 15 wt%, 16 wt%, 17 wt%, 18 wt%, 19 wt%, 20 wt%, or a range defined by any two thereof, based on the total weight of the composition.
[0022] In one embodiment, the weight ratio of the polyaspartic acid or its derivative to the straight-chain saturated dicarboxylic acid may be from 0.01:1 to 20:1, particularly from 0.1:1 to 5:1, more particularly from 0.2:1 to 1:1, and especially from 0.3:1 to 0.5:1.For example, the weight ratio of the polyaspartic acid or its derivative to the straight-chain saturated dicarboxylic acid can be 0.01:1, 0.05:1, 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. The ratios are 11:1, 12:1, 13:1, 14:1, 15:1, 16:1, 17:1, 18:1, 19:1, 20:1, or any range defined by two or more thereof. The inventors have discovered that when the weight ratio of polyaspartic acid or its derivatives to straight-chain saturated dicarboxylic acids is within the above ranges, the solubility of straight-chain saturated dicarboxylic acids (e.g., azelaic acid) in aqueous solutions, particularly acidic solutions, is significantly improved; when the weight ratio of polyaspartic acid or its derivatives to straight-chain saturated dicarboxylic acids is 0.1:1 or higher, the improvement in solubility is particularly significant in aqueous solutions; and when the weight ratio of polyaspartic acid or its derivatives to straight-chain saturated dicarboxylic acids is 0.3:1 or higher, the solubility of straight-chain saturated dicarboxylic acids (e.g., azelaic acid) in aqueous solutions, particularly acidic solutions, is further improved.
[0023] In one embodiment, the straight-chain saturated dicarboxylic acid may be a straight-chain saturated dicarboxylic acid having 6-10 carbon atoms (e.g., a physiologically acceptable straight-chain saturated dicarboxylic acid), preferably one or more of anthocyanic acid, azelaic acid, and sebacic acid, more preferably azelaic acid. For example, the straight-chain saturated dicarboxylic acid may be one or more of anthocyanic acid, pimelic acid, octanoic acid, azelaic acid, and sebacic acid.
[0024] In one embodiment, the polyaspartic acid derivative may be a polyaspartic acid salt, such as a physiologically acceptable polyaspartic acid salt. The polyaspartic acid salt may be one or more of polyaspartic acid metal salts and polyaspartic acid ammonium salts. For example, the polyaspartic acid salt may be one or more of polyaspartic acid sodium salt, polyaspartic acid potassium salt, polyaspartic acid calcium salt, polyaspartic acid magnesium salt, polyaspartic acid aluminum salt, and polyaspartic acid ammonium salt, more preferably polyaspartic acid sodium salt.
[0025] The polyaspartic acid or its derivatives can generally be represented by the following formula 1:
[0026]
[0027] In formula 1, the sum of the number of repeating units m+n can be 2-10000, preferably 10-1000, 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.
[0028] 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. Specification page 3 / 9 6 CN 121489804 A
[0029] R1 and R2 may each be independently selected from one or more of H, OH and (O)pG, wherein p is 0 or 1, and G is selected from substituted or unsubstituted C1-C12 hydrocarbon groups, such as C1-C12 alkyl, particularly C1-C6 alkyl, such as methyl, ethyl, n- or isopropyl, 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 independently H.
[0030] M1 and M2 may each be independently selected from one or more of H, metal cations and ammonium cations. In a preferred embodiment, the metal is selected from one or more of sodium, potassium, calcium, magnesium and aluminum, more preferably sodium.
[0031] In one embodiment, the weight-average molecular weight of the polyaspartic acid or its derivatives may be 1,000-100,000, particularly 2,000-50,000, for example 2,000-8,000 or 10,000-30,000, preferably 10,000-15,000.For example, the weight-average molecular weight of the polyaspartic acid or its derivatives may be 1000, 2000, 3000, 4000, 5000, 6000, 7000, 8000, 9000, 10000, 11000, 12000, 13000, 14000, 15000, 16000, 17000, 18000, 19000, 20000, 21000, 22000, 23000, 24000, 25000, 26000, 27000, 28000, 29000, 30000, 31000, 32000, or 33000. 34000, 35000, 36000, 37000, 38000, 39000, 40000, 41000, 42000, 43000, 44000, 45000, 46000, 47000, 48000, 49000, 50000, 51000, 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, 77000, 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. The inventors further discovered that when the weight-average molecular weight of the polyaspartic acid or its derivatives used is in the range of 10,000-15,000, the solubility of the straight-chain saturated dicarboxylic acid (e.g., azelaic acid) in aqueous solution can be further improved relative to other molecular weight ranges, such as corresponding polyaspartic acid or its derivatives with lower molecular weights.
[0032] In one embodiment, the weight-average molecular weight of the polyaspartic acid or its derivatives may be 10,000-15,000, and may satisfy one or more of the following characteristics (i)-(ii):
[0033] (i) the weight ratio of the polyaspartic acid or its derivatives to the straight-chain saturated dicarboxylic acid is 0.1:1 to 0.5:1, preferably 0.1:1 to 0.3:1, and
[0034] (ii) the content of the polyaspartic acid or its derivatives is 0.1 wt%-0.5 wt%, more preferably 0.1 wt%-0.3 wt%, based on the total weight of the composition.
[0035] The inventors have found that the solubility of a straight-chain saturated dicarboxylic acid (e.g., azelaic acid) in aqueous solution can be further significantly improved when the weight-average molecular weight of the polyaspartic acid or its derivatives used is in the range of 10,000-15,000 and satisfies one or more of the above characteristics (i)-(ii).
[0036] In one embodiment, 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, and even more preferably pentanediol. The inventors have found that the solubility of a straight-chain saturated dicarboxylic acid (e.g., azelaic acid) in aqueous solution can be further improved when a diol compound is further added to the composition comprising a straight-chain saturated dicarboxylic acid and polyaspartic acid or its derivatives.
[0037] In a further embodiment, when present, the weight ratio of the diol to the straight-chain saturated dicarboxylic acid may be from 0.1:1 to 10:1, particularly from 1:1 to 5:1, and more particularly from 2:1 to 5:1. For example, the weight ratio of the diol to the straight-chain saturated dicarboxylic acid 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 of these ratios. Instruction manual, pages 4 / 9, CN 121489804 A
[0038] 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.
[0039] In one embodiment, the 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 composition may be 3.0-6.0, preferably 4.0-5.5, more preferably 4.5-5.0, for example, 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 found that even under acidic conditions, such as pH within the above range, the linear saturated dicarboxylic acid (e.g., azelaic acid) exhibits enhanced solubility in aqueous solutions by combining it with polyaspartic acid or a derivative thereof.
[0040] In one embodiment, the composition may further comprise a solvent. 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 solvent content may be 10-99% by weight, based on the total weight of the composition. For example, the solvent (e.g., water) content may be 10% by weight, 15% by weight, 20% by weight, 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, 98% by weight, 99% by weight, or a range defined by any two thereof, based on the total weight of the composition. The solvent described herein does not include or differs from the aforementioned diol.
[0041] In one embodiment, 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; oils and fats; inorganic salts; pH adjusters (also known as acid-base regulators); and anti-inflammatory components. 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.
[0042] 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.
[0043] Examples of suitable thickeners include, but are not limited to: xanthan gum, prickly ash gum, guar gum, carrageenan, poloxamer, carbomer, sodium hyaluronate, acrylate / C10-30 alkanol acrylate crosspolymers, etc.
[0044] Examples of suitable oils include, but are not limited to: silicone oils, esters, vegetable oils, synthetic oils (including volatile and non-volatile oils), mineral oils, petrolatum, etc. (Page 5 / 9 of the specification, CN 121489804 A)
[0045] Examples of suitable inorganic salts include, but are not limited to: sodium chloride, magnesium sulfate, zinc chloride.
[0046] Examples of suitable pH adjusters include, but are not limited to: sodium hydroxide, potassium hydroxide, aqueous hydrogen chloride solution.
[0047] 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.
[0048] In one embodiment, the 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, salicylic acid, lactobionic acid, maltodextrin, gluconolactone, etc.
[0049] In one embodiment, the composition may further comprise other additives, provided that these additives are physically and chemically compatible with the components 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, betaine, N-2-hydroxyethyl urea, polyol ethers and esters, low molecular weight polyethylene glycol, lactates, sugars, methyl glucosyl ether, 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.
[0050] In one embodiment, the composition may further include 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, butylene glycol. Examples of suitable chelating agents include, but are not limited to: ethylenediaminetetraacetic acid, ethylene glycol diethyl ether diaminetetraacetic acid, and their physiologically acceptable salts.
[0051] In one embodiment, the composition may be a topical composition, particularly for treating skin disorders such as pigmentation, melasma, freckles, 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.
[0052] In one embodiment, the composition may be a cosmetic composition, particularly a brightening composition, a spot-removing composition, an oil-controlling composition, an exfoliating composition, or an acne-removing composition.
[0053] The inventors have discovered that when a straight-chain saturated dicarboxylic acid, such as azelaic acid, and polyaspartic acid (PASP) or a derivative thereof are used in combination in a topical composition or cosmetic composition, the solubility of the straight-chain saturated dicarboxylic acid, such as azelaic acid, in the composition is significantly improved, thereby significantly improving its skin permeability when applied to the skin, thereby achieving its desired therapeutic or cosmetic effect.
[0054] Uses
[0055] In a second aspect, the present invention relates to the use of compositions according to the first aspect of the invention for the preparation of topical formulations or cosmetics.
[0056] The compositions according to the first aspect of the invention are particularly suitable for the preparation of topical formulations or cosmetics, especially cosmetics. When the compositions according to the first aspect of the invention are used in topical compositions and cosmetic compositions, the skin permeability of the straight-chain saturated dicarboxylic acid, such as azelaic acid, is significantly improved when the topical composition or cosmetic composition is applied to the skin, thereby achieving its desired therapeutic or cosmetic effect.
[0057] However, the use of the composition according to the first aspect of the invention is not particularly limited, for example, the composition can be used for other applications requiring improved solubility of straight-chain saturated dicarboxylic acids (e.g., azelaic acid) in water or skin permeability. Specification 6 / 9 pages 9 CN 121489804 A
[0058] Preparation Method
[0059] In a third aspect, the invention relates to a method for preparing a composition according to the first aspect of the invention, comprising: mixing the components contained in the composition.
[0060] The order of mixing the components is not particularly limited.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 certain order, either all at once or in batches, in a portion of solvent or one solvent, while the remaining components can be 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.
[0061] The components contained in the composition are as described in the above section on the composition, and will not be repeated here.
[0062] Examples
[0063] In order to make the purpose, technical solution and advantages of the present invention clearer, the present invention will be further described in detail below with reference to the examples. It should be understood that the specific examples described herein are only used to explain the present invention and are not intended to limit the present invention.
[0064] I. Source of raw materials
[0065] The sources of the raw materials involved in the examples are shown in Table 1 below.
[0066] Table 1: Sources of each raw material
[0067]
[0068] II. Test methods
[0069] Solubility test
[0070] Transfer 200 μL of the composition sample containing azelaic acid to a 96-well plate and measure the turbidity. Measure the absorbance of the above sample at 700 nm using a microplate reader (INFINITE E PLEX, TECAN, Austria). Higher absorbance indicates higher turbidity, meaning more azelaic acid remains undissolved.
[0071] Skin permeability test
[0072] Place the composition sample containing azelaic acid in a 4°C incubator and let it stand for 1 week before removing it. Transdermal absorption assays were performed using a Franz diffusion cell (Teledyne Technologies). A Strat-M membrane, representing a skin model, was sandwiched between the diffusion cell cap and the diffusion cell. The inner surface of the membrane was immersed in a receiving solution (composed of 0.1% Tween 20, 10% ethanol, and 89.9% PBS buffer). The receiving solution was magnetically stirred at a constant temperature of 25°C. 35 mg of a composition containing azelaic acid was added to the membrane surface and evenly spread using the inner core of a syringe (page 7 / 9, CN 121489804 A, manual). After 8 hours, the receiving solution was collected for quantification by high-performance liquid chromatography (HPLC) analysis of azelaic acid.
[0073] III. Solubility Experiment of Azelaic Acid
[0074] Azelaic acid powder, sodium polyaspartate, and sodium hydroxide were added to water according to the composition shown in Table 2-4 below. The mixture was magnetically stirred at room temperature for 24 hours, and then ultrasonically dispersed until the azelaic acid particles were uniformly dispersed to prepare compositions A-S. The solubility of each composition was tested according to the solubility test method described above to determine the solubility of azelaic acid in it. The solubility test results of azelaic acid in each composition are also shown in Table 2-4 below.
[0075] Table 2
[0076]
[0077] As can be seen from the results in Table 2 above, compared with composition A without added sodium polyaspartate, the solubility of azelaic acid in aqueous solution is improved in compositions B-G with added sodium polyaspartate. With the increase of the weight ratio of sodium polyaspartate to azelaic acid, the solubility of azelaic acid in aqueous solution also increases, especially when the weight ratio of sodium polyaspartate to azelaic acid is 0.1:1 or higher, the improvement in solubility of azelaic acid in aqueous solution is particularly significant. When the weight ratio of sodium polyaspartate to azelaic acid is 0.3:1 or higher, the solubility of azelaic acid in aqueous solution is further improved. The absorbance of composition G is comparable to that of composition H, indicating that all the azelaic acid in it is dissolved.
[0078] Table 3
[0079]
[0080] As can be seen from the results in Table 3 above, both sodium polyaspartate A and sodium polyaspartate B with different molecular weights can solubilize azelaic acid. Furthermore, sodium polyaspartate B with a weight-average molecular weight of 13,000 can further improve the solubility of azelaic acid in aqueous solution compared to sodium polyaspartate A with a weight-average molecular weight of 5,000. In particular, when sodium polyaspartate and azelaic acid are combined in ratios of 0.1:1 and 0.3:1, the solubilizing effect of sodium polyaspartate on azelaic acid is particularly significant. Specification 8 / 9 pages 11 CN 121489804 A
[0081] Table 4
[0082]
[0083]
[0084] As can be seen from the results in Table 4 above, when pentylene glycol is further added, the solubility of azelaic acid in aqueous solution also increases with the increase of the amount of pentylene glycol added. That is, the addition of pentylene glycol further improves the solubility of azelaic acid in aqueous solution.
[0085] IV. Skin Permeability Test of Azelaic Acid
[0086] Azelaic acid powder, sodium polyaspartate A, solubilizer polyethylene glycol-40 hydrogenated castor oil (CREMOPHOR RH-40), and moisturizer 1,3-butanediol were added to water according to the composition shown in Table 5 below. Sodium hydroxide was then added to adjust the pH of the system to 4.5. The mixture was then stirred thoroughly at 50°C until completely dissolved to prepare the compositions of Example 1 and Comparative Example 1. Skin permeability tests were performed on each composition to determine the skin permeability of azelaic acid therein. The results of the skin permeability test of azelaic acid in each composition are also shown in Table 5 below.
[0087] Table 5
[0088]
[0089] Therefore, the above data demonstrate that by using sodium polyaspartate in combination with azelaic acid, the permeability of azelaic acid in the skin is significantly improved, thereby contributing to its efficacy.
[0090] The above description is only an exemplary embodiment of the present invention. It should be noted that those skilled in the art can make improvements to this invention without departing from its inventive concept, and all such improvements fall within the scope of protection of this invention.Instruction manual, 9 / 9 pages, 12 CN 121489804 A Abstract.
Claims
1. A composition comprising: Straight-chain saturated dicarboxylic acids, and Polyaspartic acid or its derivatives, wherein the content of said polyaspartic acid or its derivatives is 0.01% by weight or more, preferably 0.1% by weight or more, more preferably 0.1% by weight to 35% by weight, even more preferably 0.1% by weight to 2% by weight, and even more preferably 0.3% by weight to 0.5% by weight, based on the total weight of said composition.
2. The composition of claim 1, wherein the weight ratio of the polyaspartic acid or its derivative to the straight-chain saturated dicarboxylic acid is 0.01:1 to 20:1, particularly 0.1:1 to 5:1, more particularly 0.2:1 to 1:1, and especially 0.3:1 to 0.5:
1.
3. The composition according to claim 1 or 2, wherein the straight-chain saturated dicarboxylic acid is a straight-chain saturated dicarboxylic acid having 6-10 carbon atoms, preferably one or more of azelaic acid, azelaic acid and sebacic acid, more preferably azelaic acid.
4. The composition of claim 1 or 2, wherein the polyaspartic acid derivative is a polyaspartic acid salt, such as a physiologically acceptable polyaspartic acid salt, preferably selected from one or more of sodium polyaspartic acid, potassium polyaspartic acid, calcium polyaspartic acid, magnesium polyaspartic acid, aluminum polyaspartic acid, and ammonium polyaspartic acid, more preferably sodium polyaspartic acid.
5. The composition of claim 1 or 2, wherein the polyaspartic acid or a derivative thereof is represented by formula 1: The sum of the number of repeating units m+n is 2-10000, preferably 10-1000, and more preferably 200-500; R1 and R2 are each independently selected from H, OH, and (O). p One or more of G, wherein p is 0 or 1, G is selected from substituted or unsubstituted C1-C12 hydrocarbon groups, such as C1-C12 alkyl groups, preferably R1 and R2 are each independently H; and M1 and M2 are each independently selected from one or more of H, metal cations and ammonium cations, preferably the metal is selected from one or more of sodium, potassium, calcium, magnesium and aluminum.
6. The composition of claim 1 or 2, wherein the polyaspartic acid or its derivative has a weight-average molecular weight of 1,000-100,000, particularly 2,000-50,000, for example 2,000-8,000 or 10,000-30,000, preferably 10,000-15,000.
7. The composition of claim 1 or 2, wherein the content of the straight-chain saturated dicarboxylic acid is 0.1%-20% by weight, preferably 0.5%-10% by weight, more preferably 1%-5% by weight, based on the total weight of the composition.
8. The composition of claim 1 or 2, wherein the polyaspartic acid or its derivative has a weight-average molecular weight of 10,000-15,000 and satisfies one or more of the following characteristics (i)-(ii): (i) The weight ratio of the polyaspartic acid or its derivative to the straight-chain saturated dicarboxylic acid is 0.1:1 to 0.5:1, preferably 0.1:1 to 0.3:1, and (ii) The content of the polyaspartic acid or its derivative is 0.1%-0.5% by weight, more preferably 0.1%-0.3% by weight, based on the total weight of the composition.
9. The composition of claim 1 or 2, wherein the composition further comprises a diol, preferably a straight-chain saturated diol, more preferably selected from straight-chain saturated diols having 2-8 carbon atoms, and even more preferably selected from one or more of propylene glycol, butanediol, pentanediol, hexanediol, and heptanediol.
10. The composition of claim 9, wherein the weight ratio of the diol to the straight-chain saturated dicarboxylic acid is 0.1:1 to 10:1, particularly 1:1 to 5:1, and more particularly 2:1 to 5:
1.
11. The composition of claim 9, wherein the content of the diol is 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.
12. The composition of claim 1 or 2, wherein the pH of the composition is 3.0-6.0, preferably 4.0-5.5, more preferably 4.5-5.
0.
13. The composition of claim 1 or 2, wherein the composition further comprises a solvent, particularly water.
14. The composition of claim 1 or 2, wherein the composition is a topical composition, particularly for treating skin disorders such as pigmentation, melasma, freckles, 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.
15. The composition of claim 1 or 2, wherein the composition is a cosmetic composition, particularly a brightening composition, a spot-removing composition, an oil-controlling composition, an exfoliating composition, or an acne-removing composition.
16. The composition of claim 1 or 2, wherein the composition further comprises one or more ingredients 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; oils; inorganic salts; pH adjusters; and anti-inflammatory components.
17. Use of the composition according to any one of claims 1-16 for the preparation of topical formulations or cosmetics.
18. A method for preparing the composition according to any one of claims 1-16, comprising: The components contained in the composition are mixed.