CN115813801A - Ascorbic acid transdermal absorption composition and application thereof - Google Patents
Ascorbic acid transdermal absorption composition and application thereof Download PDFInfo
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- CN115813801A CN115813801A CN202211683245.XA CN202211683245A CN115813801A CN 115813801 A CN115813801 A CN 115813801A CN 202211683245 A CN202211683245 A CN 202211683245A CN 115813801 A CN115813801 A CN 115813801A
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- Prior art keywords
- ascorbic acid
- parts
- acid
- composition
- phase
- Prior art date
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- 229960005070 ascorbic acid Drugs 0.000 title claims abstract description 99
- 239000000203 mixture Substances 0.000 title claims abstract description 83
- 235000010323 ascorbic acid Nutrition 0.000 title claims abstract description 80
- 239000011668 ascorbic acid Substances 0.000 title claims abstract description 80
- 238000010521 absorption reaction Methods 0.000 title claims abstract description 20
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- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 claims abstract description 36
- 239000011732 tocopherol Substances 0.000 claims abstract description 35
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- 229960003471 retinol Drugs 0.000 description 1
- 235000020944 retinol Nutrition 0.000 description 1
- 229960004889 salicylic acid Drugs 0.000 description 1
- 230000006641 stabilisation Effects 0.000 description 1
- 238000011105 stabilization Methods 0.000 description 1
- 230000000087 stabilizing effect Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 229960000984 tocofersolan Drugs 0.000 description 1
- 229960000401 tranexamic acid Drugs 0.000 description 1
- GYDJEQRTZSCIOI-LJGSYFOKSA-N tranexamic acid Chemical compound NC[C@H]1CC[C@H](C(O)=O)CC1 GYDJEQRTZSCIOI-LJGSYFOKSA-N 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 235000009492 vitamin B5 Nutrition 0.000 description 1
- 239000011675 vitamin B5 Substances 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
- 235000008939 whole milk Nutrition 0.000 description 1
- 229940118846 witch hazel Drugs 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
- 238000004383 yellowing Methods 0.000 description 1
- 239000002076 α-tocopherol Substances 0.000 description 1
- 235000004835 α-tocopherol Nutrition 0.000 description 1
Abstract
The application provides an ascorbic acid transdermal absorption composition, which comprises ascorbic acid and polar oil derived from amino acid, and further comprises p-coumaric acid derivative and tocopherol. The ascorbic acid transdermal absorption combination improves the stability of ascorbic acid and the transdermal efficiency of ascorbic acid, and provides an ascorbic acid product and a technology with good and stable skin feeling for consumers.
Description
Technical Field
The application belongs to the technical field of cosmetics, and particularly relates to an ascorbic acid transdermal absorption composition and application thereof.
Background
Vitamin C, commonly known as ascorbic acid, has a chemical name of 2,3,5, 6-tetrahydroxy-2-hexene-4-lactone, and because two adjacent carbon-carbon double bonds at the 2 nd position and the 3 rd position in a molecule simultaneously have a hydroxyl group, namely an enol structure, the vitamin C is relatively unstable chemically and has strong reducibility, protons are easily dissociated to form dehydroascorbic acid, and diketone gulonic acid can be formed through further hydrolysis, so that the physiological activity is lost. It has been shown that ascorbic acid is very sensitive to light, oxygen, water, temperature, pH, metal ions, etc., and is easily hydrolyzed to deactivate particularly in an aqueous solution, and is accompanied by discoloration such as yellowing or even browning. (Sheraz M A, khan M F, ahmed S, et al.Stablility and Stabilization of Ascorbic acid.2015.)
In 2005, repailico corporation applied a patent for stabilizing ascorbic acid compositions (US 2005154054 A1) which stabilized a 15% aqueous solution of ascorbic acid by using up to 20% alcohol ether and around 10% alkyl glycol, and examined the thermal stability at 45 ℃ for 4 weeks, the retention of ascorbic acid after 4 weeks was still up to 82% of the initial value. The addition of a large amount of alcohol ether solvent can better maintain the stability of the ascorbic acid, but can bring about very sticky skin feel and strong irritation to users. If the addition amount of the alcohol ether solvent is reduced, the stability of the ascorbic acid is difficult to ensure.
In recent years, with the development of cosmetic packaging technology, products in which ascorbic acid is separated from a solution appear on the market, namely, the ascorbic acid is packaged separately in a powder form and is mixed with the solution before use, and the mode can well maintain the long-term stability of the ascorbic acid.
Disclosure of Invention
In view of the above problems in the prior art, the present application provides a composition comprising ascorbic acid, which has improved stability by adding polar oil based on amino acid derivatives and has an effect of promoting the transdermal absorption of ascorbic acid. The composition of the present application may include tocopherol and/or p-coumaric acid derivatives to further enhance the stability of ascorbic acid without the need to add a large amount of alcohol ether solvent to dissolve the p-coumaric acid derivatives, with fresh skin feel, and in particular, the present application relates to the following aspects:
1. an ascorbic acid transdermal absorption composition, wherein the composition comprises ascorbic acid and polar oil derived from amino acid.
2. The composition according to item 1, wherein the amino acid-derived polar oil-and-fat-based oil-and-fat comprises one or more of isopropyl N-lauroyl glutamate, phytosterol/octyldodecanol lauroyl glutamate, and phytosterol/behenyl alcohol/octyldodecanol lauroyl glutamate.
3. The composition according to item 1 or 2, wherein the composition comprises 3 to 25 parts by mass of ascorbic acid and 2 to 20 parts by mass of an amino acid-derived polar oil-and-fat.
4. The composition according to any one of items 1 to 3, wherein the composition further comprises a p-coumaric acid derivative, preferably in an amount of 0.1 to 3 parts by mass.
5. The composition of item 4, wherein the p-coumaric acid derivative comprises one or both of ferulic acid and caffeic acid.
6. The composition according to any one of items 1 to 5, wherein the composition further comprises tocopherol, preferably, the tocopherol is contained in an amount of 0.1 to 5 parts by mass.
7. The composition according to any one of items 1 to 6, wherein the composition further comprises an emulsifier, preferably, the emulsifier is contained in an amount of 0.5 to 5 parts by mass.
8. The composition of claim 7, wherein the emulsifier comprises one or more of ceteareth-25, ceteareth-20, polyacrylate-1, and laureth-4.
9. The composition according to any one of items 1 to 8, wherein the composition further comprises a cosmetically acceptable adjuvant and/or efficacy ingredient.
10. Use of a composition according to any one of items 1 to 9 to increase the stability and/or promote the transdermal absorption of ascorbic acid.
The ascorbic acid transdermal absorption composition improves the stability of ascorbic acid and the transdermal efficiency of ascorbic acid, avoids the sticky use feeling caused by using a large amount of alcohol ether as a solvent, and provides an ascorbic acid product and a stable technology with good skin feeling for consumers.
Detailed Description
The present application is further described below in conjunction with the following examples, which are intended to be illustrative and explanatory only and are not restrictive of the application.
Unless defined otherwise, technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art. Although methods and materials similar or equivalent to those described herein can be used in experimental or practical applications, the materials and methods are described below. In case of conflict, the present specification, including definitions, will control, and the materials, methods, and examples are illustrative only and not intended to be limiting. The present application is further described with reference to the following specific examples, which should not be construed as limiting the scope of the present application.
The application provides an ascorbic acid transdermal absorption composition, which comprises ascorbic acid and polar oil derived from amino acid.
The polar grease derived from the amino acid comprises one or more than two of isopropyl N-lauroyl glutamate, phytosterol/octyldodecanol lauroyl glutamate and phytosterol/behenyl alcohol/octyldodecanol lauroyl glutamate.
In a specific embodiment, the amino acid-based polar oil-and-fat is isopropyl N-lauroyl glutamate.
In a specific embodiment, the composition comprises 3 to 25 parts by mass of ascorbic acid, for example, 3 parts, 4 parts, 5 parts, 6 parts, 7 parts, 8 parts, 9 parts, 10 parts, 11 parts, 12 parts, 13 parts, 14 parts, 15 parts, 16 parts, 17 parts, 18 parts, 19 parts, 20 parts, 21 parts, 22 parts, 23 parts, 24 parts, 25 parts, etc., preferably 10 to 20 parts; the amount of the polar oil-and-fat derived from amino acid may be, for example, 2 to 20 parts, preferably 2 to 15 parts, more preferably 3 to 10 parts, based on 2 to 20 parts of the polar oil-and-fat derived from amino acid, such as 2 parts, 3 parts, 4 parts, 5 parts, 6 parts, 7 parts, 8 parts, 9 parts, 10 parts, 11 parts, 12 parts, 13 parts, 14 parts, 15 parts, 16 parts, 17 parts, 18 parts, 19 parts, or 20 parts.
In a particular embodiment, the composition further comprises a p-coumaric acid derivative.
In the present application, the p-coumaric acid derivative includes one or both of ferulic acid and caffeic acid.
In a particular embodiment, the p-coumaric acid derivative is ferulic acid.
In a particular embodiment, the p-coumaric acid derivative is caffeic acid.
In a specific embodiment, the composition further comprises 0.1 to 3 parts of p-coumaric acid derivative, for example, 0.1 part, 0.2 part, 0.3 part, 0.4 part, 0.5 part, 0.6 part, 0.7 part, 0.8 part, 0.9 part, 1 part, 1.1 part, 1.2 part, 1.3 part, 1.4 part, 1.5 part, 1.6 part, 1.7 part, 1.8 part, 1.9 part, 2 parts, 2.1 part, 2.2 part, 2.3 part, 2.4 part, 2.5 part, 2.6 part, 2.7 part, 2.8 part, 2.9 part, 3 part, etc., preferably 0.5 to 1 part, by mass.
In a particular embodiment, the composition further comprises tocopherol.
Among them, tocopherol is a hydrolysate of vitamin E, and natural tocopherol is D-tocopherol (D-form), which has 8 isomers such as alpha, beta, gamma, delta, etc., wherein the activity of alpha-tocopherol is the strongest. The tocopherol mixed concentrate used as an antioxidant is a mixture of various isomers of natural tocopherol. The tocopherol has wide application in whole milk powder, cream or margarine, meat products, aquatic products, dehydrated vegetables, fruit juice beverages, frozen foods, instant foods and the like, and especially has important significance as an antioxidant and a nutrition enhancer of infant foods, curative effect foods, fortified foods and the like.
In a specific embodiment, the composition further comprises tocopherol in an amount of 0.1 to 5 parts, for example, 0.1 part, 0.2 part, 0.3 part, 0.4 part, 0.5 part, 0.6 part, 0.7 part, 0.8 part, 0.9 part, 1 part, 1.1 part, 1.2 part, 1.3 part, 1.4 part, 1.5 part, 1.6 part, 1.7 part, 1.8 part, 1.9 part, 2 parts, 2.5 parts, 3 parts, 3.5 parts, 4 parts, 4.5 parts, 5 parts, etc., preferably 0.5 to 3 parts, by mass.
In a particular embodiment, the ascorbic acid is present in the composition in an amount of 3wt% to 25wt%, for example 3wt%, 4wt%, 5wt%, 6wt%, 7wt%, 8wt%, 9wt%, 10wt%, 11wt%, 12wt%, 13wt%, 14wt%, 15wt%, 16wt%, 17wt%, 18wt%, 19wt%, 20wt%, 21wt%, 22wt%, 23wt%, 24wt%, 25wt%, etc., preferably 10wt% to 20wt%.
In a specific embodiment, the content of the amino acid-derived polar oil-and-fat based on the amino acid in the composition is 2wt% to 20wt%, for example, may be 2wt%, 3wt%, 4wt%, 5wt%, 6wt%, 7wt%, 8wt%, 9wt%, 10wt%, 11wt%, 12wt%, 13wt%, 14wt%, 15wt%, 16wt%, 17wt%, 18wt%, 19wt%, 20wt%, etc., preferably 2wt% to 15wt%, more preferably 3wt% to 10wt%.
In a particular embodiment, the p-coumaric acid derivative is present in the composition in an amount of 0.1wt% to 3wt%, and may be, for example, 0.1wt%, 0.2wt%, 0.3wt%, 0.4wt%, 0.5wt%, 0.6wt%, 0.7wt%, 0.8wt%, 0.9wt%, 1wt%, 1.1wt%, 1.2wt%, 1.3wt%, 1.4wt%, 1.5wt%, 1.6wt%, 1.7wt%, 1.8wt%, 1.9wt%, 2wt%, 2.1wt%, 2.2wt%, 2.3wt%, 2.4wt%, 2.5wt%, 2.6wt%, 2.7wt%, 2.8wt%, 2.9wt%, 3wt%, etc., preferably 0.5wt% to 1wt%;
in a particular embodiment, the tocopherol is present in the composition in an amount of 0.1wt% to 5wt%, e.g., can be 0.1wt%, 0.2wt%, 0.3wt%, 0.4wt%, 0.5wt%, 0.6wt%, 0.7wt%, 0.8wt%, 0.9wt%, 1wt%, 1.1wt%, 1.2wt%, 1.3wt%, 1.4wt%, 1.5wt%, 1.6wt%, 1.7wt%, 1.8wt%, 1.9wt%, 2wt%, 2.5wt%, 3wt%, 3.5wt%, 4wt%, 4.5wt%, 5wt%, etc., preferably 0.5wt% to 3wt%.
The compositions herein may further comprise an emulsifier, wherein the emulsifier may be one commonly used in the cosmetic arts, and may be routinely selected by those skilled in the art.
In a specific embodiment, the emulsifier comprises one or more of ceteareth-25, ceteareth-20, polyacrylate-1, laureth-4.
In a specific embodiment, the emulsifier is present in the composition in an amount of 0.5 to 5 parts by weight, and may be, for example, 0.5 part, 1 part, 1.5 parts, 2 parts, 2.5 parts, 3 parts, 3.5 parts, 4 parts, 4.5 parts, 5 parts, etc.
In a particular embodiment, the emulsifier is present in the composition in an amount of 0.5wt% to 5wt%, for example 0.5wt%, 1wt%, 1.5wt%, 2wt%, 2.5wt%, 3wt%, 3.5wt%, 4wt%, 4.5wt%, 5wt%, etc.
In a particular embodiment, the composition comprises 3wt% to 25wt% ascorbic acid, 0.1wt% to 5wt% tocopherol, 0.1wt% to 3wt% p-coumaric acid derivative, 2wt% to 20wt% amino acid-based derived polar oil and 0.5wt% to 5wt% emulsifier.
In a particular embodiment, the composition comprises 10wt% to 20wt% ascorbic acid, 0.5wt% to 3wt% tocopherol, 0.5wt% to 1wt% p-coumaric acid derivative, 2wt% to 15wt% amino acid-based derived polar oil and 0.5wt% to 5wt% emulsifier.
In a particular embodiment, the composition comprises 5wt% to 20wt% ascorbic acid, 0.1wt% to 5wt% tocopherol, 0.1wt% to 2wt% p-coumaric acid derivative, 3wt% to 15wt% amino acid-based derived polar oil, 0.5wt% to 5wt% emulsifier and 0.01wt% to 5wt% glycerol.
In a particular embodiment, the composition consists of ascorbic acid, tocopherol, a p-coumaric acid derivative, an amino acid-derived polar oil-and-fat, and water.
In a specific embodiment, the ascorbic acid transdermal absorption composition is composed of 5wt% to 20wt% ascorbic acid, 0.1wt% to 5wt% tocopherol, 0.1wt% to 2wt% p-coumaric acid derivative, 3wt% to 20wt% amino acid-derived polar oil-based oil, and water.
In a particular embodiment, the composition consists of ascorbic acid, tocopherol, p-coumaric acid derivative, polar oil based on amino acid derivatives, emulsifier and water.
In a particular embodiment, the composition consists of 5wt% to 20wt% ascorbic acid, 0.1wt% to 5wt% tocopherol, 0.1wt% to 2wt% p-coumaric acid derivative, 3wt% to 20wt% amino acid-based derived polar oil, 0.5wt% to 5wt% emulsifier and water.
Further, the composition also comprises auxiliary materials and/or functional components which are acceptable in cosmetics.
For the auxiliary materials, including solvents, thickeners, antiseptics, pH regulators, essences, etc. commonly used in cosmetics, for example, the solvents may be water, alcohols, oil ester solvents acceptable in the cosmetic field, and the solvents may not include glycol ethers, alkyl glycols; the thickener can be thickener commonly used in cosmetic field, such as cellulose, xanthan gum, guar gum, poloxamer, etc.; the preservative may be a cosmetically acceptable preservative such as alcohol preservatives, phenol preservatives, paraben preservatives, organic acid preservatives, quaternary amine preservatives, etc.; the acid-base regulator can be acid, alkali, inorganic salt and the like acceptable in the field of cosmetics; as the essence, there may be mentioned animal essence, plant essence, synthetic essence, etc. acceptable in the field of cosmetics.
The effective components comprise whitening components, moisture-keeping components, wrinkle-removing components, anti-aging components, oil-controlling acne-removing components, repairing components and the like which are commonly used in cosmetics. For example, the whitening ingredients commonly used in the cosmetic field include, but are not limited to, resorcinol compounds, fruit acids and derivatives thereof, vitamin C and derivatives thereof, azelaic acid, arbutin and derivatives thereof, kojic acid and derivatives thereof, tranexamic acid, pantothenic acid derivatives, biological whitening agents, natural animal and plant extracts, and the like; moisturizing ingredients commonly used in the cosmetic field include, but are not limited to, hyaluronic acid, vitamin B5, hydroxyethyl urea, betaine, lecithin, polyols, amino acids, xylitol, and the like; wrinkle-removing components commonly used in the cosmetic field include, but are not limited to, vitamin C, alpha alcohol, vitronectin, peptide, etc.; anti-aging ingredients commonly used in the cosmetic field include, but are not limited to, retinol, boscalid, fullerene, etc.; oil-controlling and acne-removing ingredients commonly used in the cosmetic field include, but are not limited to, salicylic acid, fruit acid, niacinamide, witch hazel, and the like; typical repair ingredients commonly used in the cosmetic field include, but are not limited to, ceramide, ectoin, allantoin, centella asiatica, chamomile, and the like.
In one embodiment of the present application, the composition further comprises glycerin as a moisturizing ingredient.
The application also provides the application of the composition in improving the stability of the ascorbic acid and/or promoting the transdermal absorption of the ascorbic acid.
Examples
The experimental methods used in the following examples are all conventional methods unless otherwise specified.
Example 1
Weighing 15g of L-ascorbic acid and 0.5g of polyacrylate-1, adding into 77.5g of water, stirring uniformly, and heating to 60 ℃ to be used as an A phase; weighing 1g tocopherol, 0.5g ferulic acid, 3.5g isopropyl N-lauroyl sarcosinate, and 2g ceteareth-25, heating to 60 deg.C to melt and obtain phase B, adding phase B into phase A, homogenizing at 3000rpm for 3min, and cooling to obtain ascorbic acid composition.
Example 2
Weighing 15g of L-ascorbic acid and 0.5g of polyacrylate-1, adding into 76g of water, uniformly stirring, and heating to 60 ℃ to be used as an A phase; weighing 1g tocopherol, 2.0g ferulic acid, 3.5g isopropyl N-lauroyl sarcosinate, and 2g ceteareth-25, heating to 60 deg.C to melt and obtain phase B, adding phase B into phase A, homogenizing at 3000rpm for 3min, and cooling to obtain ascorbic acid composition.
Example 3
Weighing 15g of L-ascorbic acid and 0.5g of polyacrylate-1, adding the L-ascorbic acid and the polyacrylate-1 into 71g of water, uniformly stirring, and heating to 60 ℃ to be used as an A phase; weighing 1g tocopherol, 2.0g ferulic acid, 10g isopropyl N-lauroyl sarcosinate, and 2g ceteareth-25, heating to 60 deg.C to melt and obtain phase B, adding phase B into phase A, homogenizing at 3000rpm for 3min, and cooling to obtain ascorbic acid composition.
Example 4
Weighing 15g of L-ascorbic acid and 0.5g of polyacrylate-1, adding into 78g of water, uniformly stirring, and heating to 60 ℃ to be used as an A phase; weighing 0.5g tocopherol, 0.5g ferulic acid, 3.5g N-lauroyl sarcosine isopropyl ester, 2g ceteareth-25, heating to 60 deg.C to melt and obtain phase B, adding phase A, homogenizing at 3000rpm for 3min, and cooling to obtain ascorbic acid composition.
Example 5
Weighing 5g of L-ascorbic acid and 0.5g of polyacrylate-1, adding the mixture into 87.5g of water, uniformly stirring, and heating to 60 ℃ to be used as an A phase; weighing 1g tocopherol, 0.5g ferulic acid, 3.5g N-lauroyl sarcosine isopropyl ester, 2g ceteareth-25, heating to 60 deg.C to melt and obtain phase B, adding phase B, homogenizing at 3000rpm for 3min, and cooling.
Example 6
Weighing 20g of L-ascorbic acid and 0.5g of polyacrylate-1, adding into 72.5g of water, uniformly stirring, and heating to 60 ℃ to be used as an A phase; weighing 1g tocopherol, 0.5g ferulic acid, 3.5g isopropyl N-lauroyl sarcosinate, and 2g ceteareth-25, heating to 60 deg.C to melt and obtain phase B, adding phase B into phase A, homogenizing at 3000rpm for 3min, and cooling to obtain ascorbic acid composition.
Example 7
Weighing 15g of L-ascorbic acid and 0.5g of polyacrylate-1, adding into 76.5g of water, stirring uniformly, and heating to 60 ℃ to be used as an A phase; weighing 2g tocopherol, 0.5g ferulic acid, 3.5g N-lauroyl sarcosine isopropyl ester, 2g ceteareth-25, heating to 60 deg.C to melt and obtain phase B, adding phase A, homogenizing at 3000rpm for 3min, and cooling.
Example 8
Weighing 15g of L-ascorbic acid and 0.5g of polyacrylate-1, adding into 77.5g of water, stirring uniformly, and heating to 60 ℃ to be used as an A phase; weighing 1g of tocopherol, 0.5g of ferulic acid, 3.5g of phytosterol/octyldodecanol lauroyl glutamate and 2g of ceteareth-25, heating to 60 ℃ for melting to obtain phase B, adding A into the phase B, homogenizing at 3000rpm for 3min, and cooling to obtain the ascorbic acid composition.
Example 9
Weighing 15g of L-ascorbic acid, 3g of glycerol and 0.5g of polyacrylate-1, adding the mixture into 74.5g of water, uniformly stirring, and heating to 60 ℃ to obtain a phase A; weighing 1g tocopherol, 0.5g ferulic acid, 3.5g isopropyl N-lauroyl sarcosinate, and 2g ceteareth-25, heating to 60 deg.C to melt and obtain phase B, adding phase B into phase A, homogenizing at 3000rpm for 3min, and cooling to obtain ascorbic acid composition.
Example 10
Weighing 15g of L-ascorbic acid, adding the L-ascorbic acid into 77.5g of water, uniformly stirring, and heating to 60 ℃ to be used as an A phase; weighing 1g tocopherol, 0.5g ferulic acid, 3.5g isopropyl N-lauroyl sarcosinate, and 2.5g ceteareth-25, heating to 60 deg.C to melt to obtain phase B, adding phase A, homogenizing at 3000rpm for 3min, and cooling to obtain ascorbic acid composition.
Example 11
Weighing 15g of L-ascorbic acid and 0.5g of polyacrylate-1, adding into 77.5g of water, stirring uniformly, and heating to 60 ℃ to be used as an A phase; weighing 1g tocopherol, 0.5g caffeic acid, 3.5g isopropyl N-lauroyl sarcosinate, and 2g ceteareth-25, heating to 60 deg.C to melt to obtain phase B, adding phase A, homogenizing at 3000rpm for 3min, and cooling to obtain ascorbic acid composition.
Example 12
Weighing 15g of L-ascorbic acid, adding the L-ascorbic acid into 80g of water, uniformly stirring, and heating to 60 ℃ to be used as an A phase; weighing 1g of tocopherol, 0.5g of ferulic acid and 3.5g of N-lauroyl sarcosine isopropyl ester, heating to 60 ℃ to melt to obtain a B phase, adding the B phase into the A phase, homogenizing at 3000rpm for 3min, and cooling to obtain the ascorbic acid composition.
Comparative example 1
Weighing 15g of L-ascorbic acid, 3g of glycerol and 0.5g of polyacrylate-1, adding into 77.5g of water, uniformly stirring, and heating to 60 ℃ to obtain phase A; weighing 1g tocopherol, 0.5g ferulic acid, 3.5g propylene glycol ether, and 2g ceteareth-25, heating to 60 deg.C to melt and obtain phase B, adding phase A, homogenizing at 3000rpm for 3min, and cooling to obtain ascorbic acid composition.
Comparative example 2
Weighing 15g of L-ascorbic acid and 0.5g of polyacrylate-1, adding into 80g of water, uniformly stirring, and heating to 60 ℃ to be used as an A phase; weighing 1g tocopherol, 0.5g ferulic acid, 1g isopropyl N-lauroyl sarcosinate, and 2g ceteareth-25, heating to 60 deg.C to melt and obtain phase B, adding phase B into phase A, homogenizing at 3000rpm for 3min, and cooling to obtain ascorbic acid composition.
Comparative example 3
Weighing 15g of L-ascorbic acid, adding the L-ascorbic acid into 85g of water, uniformly stirring, heating to 60 ℃, and cooling to obtain the ascorbic acid composition.
Specific conditions of the above examples and comparative examples are shown in table 1.
TABLE 1
Test examples
Test example 1 stability test
The stability tests were carried out on the samples prepared in the above examples and comparative examples. Specifically, the ascorbic acid compositions prepared in the above examples and comparative examples were dispensed into colorless and transparent PET vials, and placed in a Binder 45 ℃ ± 2 ℃ oven without being shielded from light to examine the high temperature stability for 28 days, after the set examination time, the emulsion was taken out of the oven and left at room temperature and returned to room temperature, the content of ascorbic acid was quantified by HPLC, and the content of ascorbic acid measured was divided by the initial content of ascorbic acid to obtain the retention ratio of ascorbic acid, and the results are shown in table 2.
TABLE 2
| Retention ratio | |
| Example 1 | 92.50％ |
| Example 2 | 93.10％ |
| Example 3 | 92.70％ |
| Example 4 | 90.30％ |
| Example 5 | 91.90％ |
| Example 6 | 92.60％ |
| Example 7 | 93.40％ |
| Example 8 | 91.90％ |
| Example 9 | 92.55％ |
| Example 10 | 92.47％ |
| Example 11 | 92.52％ |
| Example 12 | 88.6% (oil-water split phase) |
| Comparative example 1 | 84.10％ |
| Comparative example 2 | 80.5% (ferulic acid with precipitation) |
| Comparative example 3 | 42％ |
As can be seen from table 2, the amino acid-derived polar oils and fats used in the examples and the propylene glycol ether used in comparative example 1 both dissolve p-coumaric acid derivatives such as ferulic acid, but the amino acid-derived polar oils and fats used in the examples can improve the stability of ascorbic acid as compared with comparative example 1. And the alcohol ether solvent of comparative example 1 is inferior in stability against ascorbic acid to the amino acid-derived polar oil used in the examples at the same amount.
Test example 2 in vitro transdermal absorption test
The ascorbic acid compositions of the present application were tested for in vitro transdermal absorption by the Franz diffusion cell method, using pigskin as a carrier, which was fixed between the supply and receiving chambers of the Franz diffusion cell, the diffusion cell was fixed in a transdermal absorption diffusion apparatus, and the transdermal experiments were carried out by adding samples of the ascorbic acid compositions prepared in examples and comparative examples to the skin surface in the chamber, with the magnetic stirrer and thermostatic water bath turned on. The receiving solution is selected from 20% polyethylene glycol (PEG) + PBS aqueous solution, and the transdermal amounts of ascorbic acid and ferulic acid are respectively determined in 2h, 4h, 8h and 24 h. The cumulative transdermal quantity Q is calculated by the formula: q = [ Cn x V +. Sigma Ci x V0]/S (i =1 \8230; n-1), where Q is the cumulative transdermal mass, S is the effective diffusion area, V is the volume of the receiving fluid in the receiving chamber, V0 is the volume per sample, ci is the concentration of the drug in the receiving fluid from the first sampling to the last sampling, and Cn is the concentration of the sample measured at the nth sampling point. The results of the transdermal amount of ascorbic acid accumulated as a function of time in the composition are shown in Table 3 below.
TABLE 3 cumulative transdermal amounts of ascorbic acid in ascorbic acid compositions over various periods of time
As can be seen from table 3, in the case that the amount of ascorbic acid added in the compositions of examples 1 to 4 and 7 to 12 is the same as that of comparative example 3, the examples have higher transdermal absorption amount of ascorbic acid, which indicates that the composition of the present application has the effect of significantly improving the transdermal absorption of ascorbic acid. Examples 1 and 8 compared with comparative example 1, the transdermal absorption amount of ascorbic acid in the ascorbic acid composition can be significantly increased based on the amino acid-derived polar oil compared with propylene glycol ether.
Claims (10)
1. An ascorbic acid transdermal absorption composition, comprising ascorbic acid and a polar oil based on amino acid derivatives.
2. The composition according to claim 1, wherein the polar oil based on amino acid derivatives comprises one or more of isopropyl N-lauroyl glutamate, phytosterol/octyldodecanol lauroyl glutamate, and phytosterol/behenyl/octyldodecanol lauroyl glutamate.
3. The composition according to claim 1 or 2, wherein the composition comprises 3 to 25 parts by mass of the ascorbic acid and 2 to 20 parts by mass of the amino acid-derived polar oil-and-fat.
4. The composition according to any one of claims 1 to 3, further comprising a p-coumaric acid derivative, preferably in an amount of 0.1 to 3 parts by weight.
5. The composition of claim 4, wherein the p-coumaric acid derivative comprises one or both of ferulic acid and caffeic acid.
6. The composition according to any one of claims 1 to 5, wherein the composition further comprises tocopherol, preferably in an amount of 0.1 to 5 parts by weight.
7. The composition according to any one of claims 1 to 6, further comprising an emulsifier, preferably in an amount of 0.5 to 5 parts by weight.
8. The composition of claim 7, wherein the emulsifier comprises one or more of ceteareth-25, ceteareth-20, polyacrylate-1, and laureth-4.
9. Composition according to any one of claims 1 to 8, characterized in that it further comprises cosmetically acceptable adjuvants and/or functional ingredients.
10. Use of a composition according to any one of claims 1 to 9 for increasing the stability and/or promoting the transdermal absorption of ascorbic acid.
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