CN115813801A - A kind of ascorbic acid transdermal absorption composition and its application - Google Patents
A kind of ascorbic acid transdermal absorption composition and its application Download PDFInfo
- Publication number
- 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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- China
- Prior art keywords
- parts
- ascorbic acid
- composition
- acid
- tocopherol
- Prior art date
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Abstract
本申请提供一种抗坏血酸透皮吸收组合物,其包括抗坏血酸和基于氨基酸衍生的极性油脂,进一步还包括对香豆酸衍生物和生育酚。本申请的抗坏血酸透皮吸收组合提高了抗坏血酸的稳定性以及抗坏血酸的透皮效率,为消费者提供了一种肤感良好且稳定的抗坏血酸产品和技术。The present application provides an ascorbic acid transdermal absorption composition, which includes ascorbic acid and amino acid-based polar oils, and further includes p-coumaric acid derivatives and tocopherol. The ascorbic acid transdermal absorption combination of the present application improves the stability of ascorbic acid and the transdermal efficiency of ascorbic acid, and provides consumers with a good and stable ascorbic acid product and technology with good skin feeling.
Description
技术领域technical field
本申请属于化妆品技术领域,具体涉及一种抗坏血酸透皮吸收组合物及其用途,所述组合物是一种稳定的具有促进抗坏血酸吸收作用的化妆品组合物。The application belongs to the technical field of cosmetics, and in particular relates to an ascorbic acid transdermal absorption composition and its application. The composition is a stable cosmetic composition capable of promoting ascorbic acid absorption.
背景技术Background technique
维生素C,俗称抗坏血酸,化学名为2,3,5,6-四羟基-2-己烯-4-内酯,因分子中第2位和第3位两个相邻的碳碳双键同时具有一个羟基基团,即烯醇式结构,化学上较为不稳定,具有很强的还原性,容易解离出质子,形成脱氢抗坏血酸,进一步水解可形成二酮古洛糖酸,从而失去生理活性。有研究指出,抗坏血酸对光、氧气、水、温度、pH、金属离子等十分敏感,尤其在水溶液中较容易水解而失活,同时伴随变色的发生,如变黄甚至变成棕色等。(Sheraz M A,Khan M F,Ahmed S,et al.Stability and Stabilization of AscorbicAcid.2015.)Vitamin C, commonly known as ascorbic acid, has a chemical name of 2,3,5,6-tetrahydroxy-2-hexene-4-lactone, because the two adjacent carbon-carbon double bonds at the 2nd and 3rd positions in the molecule are simultaneously It has a hydroxyl group, that is, an enol structure. It is chemically unstable and has strong reductivity. It is easy to dissociate protons and form dehydroascorbic acid. Further hydrolysis can form diketogulonic acid, thus losing physiological active. Studies have pointed out that ascorbic acid is very sensitive to light, oxygen, water, temperature, pH, metal ions, etc., especially in aqueous solution, it is easy to be hydrolyzed and inactivated, and it is accompanied by discoloration, such as yellowing or even browning. (Sheraz M A, Khan M F, Ahmed S, et al. Stability and Stabilization of Ascorbic Acid. 2015.)
2005年,美国修丽可公司申请了一个稳定抗坏血酸组合物的专利(US2005154054A1),其通过使用高达20%的醇醚和10%左右的烷基二醇来稳定15%的抗坏血酸水溶液,在45℃下考察了4周的热稳定性,4周后抗坏血酸的保留率仍高达初始值的82%。大量的醇醚溶剂的加入,虽然能够较好地保持抗坏血酸的稳定性,但会给使用者带来十分黏腻的肤感以及较强的刺激感。如果降低醇醚溶剂的添加量,又难以保证抗坏血酸的稳定性。In 2005, SkinCeuticals of the United States applied for a patent for a stable ascorbic acid composition (US2005154054A1), which stabilized a 15% ascorbic acid aqueous solution by using up to 20% of alcohol ether and about 10% of alkyl glycol. Investigated the thermal stability of 4 weeks, the retention rate of ascorbic acid was still as high as 82% of the initial value after 4 weeks. Although the addition of a large amount of alcohol ether solvent can better maintain the stability of ascorbic acid, it will bring a very sticky skin feeling and strong stimulation to the user. If reduce the addition amount of alcohol ether solvent, be difficult to guarantee the stability of ascorbic acid again.
近年来,随着化妆品包装技术的发展,市场上出现了抗坏血酸和溶液分离的产品,即抗坏血酸以粉末的形式单独包装,使用前和溶液混合,这种方式能够很好的保持抗坏血酸的长期稳定性,但其缺点也显而易见,对包材的要求较高,大大增加了产品的成本,且使用感多有不便。In recent years, with the development of cosmetic packaging technology, ascorbic acid and solution separation products have appeared on the market, that is, ascorbic acid is packaged separately in the form of powder, and mixed with the solution before use. This method can well maintain the long-term stability of ascorbic acid , but its shortcomings are also obvious. The requirements for packaging materials are high, which greatly increases the cost of the product, and it is inconvenient to use.
发明内容Contents of the invention
针对现有技术存在的上述问题,本申请提供一种包含抗坏血酸的组合物,通过加入基于氨基酸衍生的极性油脂提升抗坏血酸的稳定性,并且该组合物具有促进抗坏血酸透皮吸收的作用。本申请的组合物可以包括生育酚和/或对香豆酸衍生物,进一步提升抗坏血酸的稳定性,不需要添加大量的醇醚溶剂来溶解对香豆酸衍生物,肤感清爽,具体来说,本申请涉及如下方面:To solve the above-mentioned problems in the prior art, the present application provides a composition containing ascorbic acid, the stability of ascorbic acid is improved by adding polar oil derived from amino acid, and the composition has the 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 improve the stability of ascorbic acid without adding a large amount of alcohol ether solvent to dissolve the p-coumaric acid derivatives, and the skin feels refreshing, specifically , this application involves the following aspects:
1.一种抗坏血酸透皮吸收组合物,其中,所述组合物包括抗坏血酸和基于氨基酸衍生的极性油脂。1. An ascorbic acid transdermal absorption composition, wherein the composition comprises ascorbic acid and polar oil derived from amino acid.
2.根据项1所述的组合物,其中,所述基于氨基酸衍生的极性油脂包括N-月桂酰基谷氨酸异丙酯、植物甾醇/辛基十二醇月桂酰谷氨酸酯、以及植物甾醇/山嵛醇/辛基十二醇月桂酰谷氨酸酯中的一种或两种以上。2. The composition according to item 1, wherein the polar oil based on amino acid derivatization includes isopropyl N-lauroyl glutamate, phytosterol/octyldodecyl lauroyl glutamate, and One or more of phytosterol/behenyl alcohol/octyldodecanol lauroyl glutamate.
3.根据项1或2所述的组合物,其中,按质量份数计,所述组合物包括抗坏血酸3-25份,基于氨基酸衍生的极性油脂2-20份。3. The composition according to item 1 or 2, wherein, in terms of parts by mass, the composition includes 3-25 parts of ascorbic acid and 2-20 parts of amino acid-derived polar oil.
4.根据项1-3中任一项所述的组合物,其中,所述组合物还包括对香豆酸衍生物,优选的,按质量份数计,所述对香豆酸衍生物的含量为0.1-3份。4. The composition according to any one of items 1-3, wherein the composition also includes a p-coumaric acid derivative, preferably, in parts by mass, the p-coumaric acid derivative The content is 0.1-3 parts.
5.根据项4所述的组合物,其中,所述对香豆酸衍生物包括阿魏酸、咖啡酸中的一种或两种。5. The composition according to item 4, wherein the p-coumaric acid derivative comprises one or both of ferulic acid and caffeic acid.
6.根据项1-5中任一项所述的组合物,其中,所述组合物还包括生育酚,优选的,按质量份数计,所述生育酚的含量为0.1-5份。6. The composition according to any one of items 1-5, wherein the composition further comprises tocopherol, preferably, the content of the tocopherol is 0.1-5 parts by mass.
7.根据项1-6中任一项所述的组合物,其中,所述组合物还包括乳化剂,优选的,按质量份数计,所述乳化剂的含量为0.5-5份。7. The composition according to any one of items 1-6, wherein the composition further comprises an emulsifier, preferably, the content of the emulsifier is 0.5-5 parts by mass.
8.根据项7所述的组合物,其中,所述乳化剂包括鲸蜡硬脂醇聚醚-25、鲸蜡硬脂醇聚醚-20、聚丙烯酸酯-1、月桂醇聚醚-4中的一种或两种以上。8. The composition according to item 7, wherein the emulsifier comprises ceteareth-25, ceteareth-20, polyacrylate-1, laureth-4 one or more of them.
9.根据项1-8中任一项所述的组合物,其中,所述组合物还包括化妆品上可接受的辅料和/或功效成分。9. The composition according to any one of items 1-8, wherein the composition further comprises cosmetically acceptable excipients and/or functional ingredients.
10.项1-9中任一项所述的组合物在提高抗坏血酸的稳定性和/或促进抗坏血酸透皮吸收中的用途。10. Use of the composition described in any one of items 1-9 in improving the stability of ascorbic acid and/or promoting the transdermal absorption of ascorbic acid.
本申请的抗坏血酸透皮吸收组合物,提高了抗坏血酸的稳定性以及抗坏血酸的透皮效率,且避免了使用大量醇醚作为溶剂带来的粘腻的使用感,为消费者提供了一种肤感良好且稳定的抗坏血酸产品和技术。The ascorbic acid transdermal absorption composition of the present application improves the stability of ascorbic acid and the transdermal efficiency of ascorbic acid, avoids the sticky feeling of use caused by using a large amount of alcohol ether as a solvent, and provides consumers with a skin feeling Good and stable ascorbic acid products and technology.
具体实施方式Detailed ways
下面结合实施例进一步说明本申请,应当理解,实施例仅用于进一步说明和阐释本申请,并非用于限制本申请。The present application will be further described below in conjunction with the examples. It should be understood that the examples are only used to further illustrate and explain the present application, and are not intended to limit the present application.
除非另外定义,本说明书中有关技术的和科学的术语与本领域内的技术人员所通常理解的意思相同。虽然在实验或实际应用中可以应用与此间所述相似或相同的方法和材料,本文还是在下文中对材料和方法做了描述。在相冲突的情况下,以本说明书包括其中定义为准,另外,材料、方法和例子仅供说明,而不具限制性。以下结合具体实施例对本申请作进一步的说明,但不用来限制本申请的范围。Unless otherwise defined, technical and scientific terms in this specification have the same meaning as commonly understood by a person skilled in the art. Although methods and materials similar or identical to those described herein can be employed in experiments or practical applications, the materials and methods are described herein below. In case of conflict, the present specification, including definitions, will control and the materials, methods, and examples are presented for purposes of illustration only and not limitation. The present application will be further described below in conjunction with specific examples, but they are not used to limit the scope of the present application.
本申请提供一种抗坏血酸透皮吸收组合物,所述组合物包括抗坏血酸和基于氨基酸衍生的极性油脂。The present application provides an ascorbic acid transdermal absorption composition, which comprises ascorbic acid and polar oil derived from amino acid.
所述基于氨基酸衍生的极性油脂包括N-月桂酰基谷氨酸异丙酯、植物甾醇/辛基十二醇月桂酰谷氨酸酯、以及植物甾醇/山嵛醇/辛基十二醇月桂酰谷氨酸酯中的一种或两种以上。The amino acid-based polar oils include isopropyl N-lauroyl glutamate, phytosterol/octyldodecyl lauroyl glutamate, and phytosterol/behenyl/octyldodecyl lauryl One or two or more of acylglutamic acid esters.
在一个具体的实施方式中,所述基于氨基酸衍生的极性油脂为N-月桂酰基谷氨酸异丙酯。In a specific embodiment, the amino acid-based polar oil is isopropyl N-lauroyl glutamate.
在一个具体的实施方式中,按质量份数计,所述组合物包括抗坏血酸3-25份,例如可以为3份、4份、5份、6份、7份、8份、9份、10份、11份、12份、13份、14份、15份、16份、17份、18份、19份、20份、21份、22份、23份、24份、25份等,优选为10-20份;基于氨基酸衍生的极性油脂2-20份,例如可以为2份、3份、4份、5份、6份、7份、8份、9份、10份、11份、12份、13份、14份、15份、16份、17份、18份、19份、20份等,优选为2-15份,更优选3-10份。In a specific embodiment, in terms of parts by mass, the composition includes 3-25 parts of ascorbic acid, such as 3 parts, 4 parts, 5 parts, 6 parts, 7 parts, 8 parts, 9 parts, 10 parts 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 10-20 parts; 2-20 parts based on amino acid-derived polar oils, 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, 20 parts, etc., preferably 2-15 parts, more preferably 3-10 parts.
在一个具体的实施方式中,所述组合物还包括对香豆酸衍生物。In a specific embodiment, the composition further includes p-coumaric acid derivatives.
在本申请中,对香豆酸衍生物包括阿魏酸、以及咖啡酸中的一种或两种。In the present application, p-coumaric acid derivatives include one or both of ferulic acid and caffeic acid.
在一个具体的实施方式中,所述对香豆酸衍生物为阿魏酸。In a specific embodiment, the p-coumaric acid derivative is ferulic acid.
在一个具体的实施方式中,所述对香豆酸衍生物为咖啡酸。In a specific embodiment, the p-coumaric acid derivative is caffeic acid.
在一个具体的实施方式中,按质量份数计,所述组合物还包括对香豆酸衍生物0.1-3份,例如可以为0.1份、0.2份、0.3份、0.4份、0.5份、0.6份、0.7份、0.8份、0.9份、1份、1.1份、1.2份、1.3份、1.4份、1.5份、1.6份、1.7份、1.8份、1.9份、2份、2.1份、2.2份、2.3份、2.4份、2.5份、2.6份、2.7份、2.8份、2.9份、3份等,优选为0.5-1份。In a specific embodiment, in terms of parts by mass, the composition further includes 0.1-3 parts of p-coumaric acid derivatives, such as 0.1 parts, 0.2 parts, 0.3 parts, 0.4 parts, 0.5 parts, 0.6 parts parts, 0.7 parts, 0.8 parts, 0.9 parts, 1 part, 1.1 parts, 1.2 parts, 1.3 parts, 1.4 parts, 1.5 parts, 1.6 parts, 1.7 parts, 1.8 parts, 1.9 parts, 2 parts, 2.1 parts, 2.2 parts, 2.3 parts, 2.4 parts, 2.5 parts, 2.6 parts, 2.7 parts, 2.8 parts, 2.9 parts, 3 parts, etc., preferably 0.5-1 parts.
在一个具体的实施方式中,所述组合物还包括生育酚。In a specific embodiment, said composition further comprises tocopherol.
其中,生育酚,是维生素E的水解产物,天然的生育酚都是D-生育酚(右旋型),它有α、β、γ、δ等8种同分异构体,其中以α-生育酚的活性最强。作为抗氧化剂使用的生育酚混合浓缩物,是天然生育酚的各种同分异构体的混合物。在全脂乳粉、奶油或人造奶油、肉制品、水产加工品、脱水蔬菜、果汁饮料、冷冻食品及方便食品等中具有广泛的应用,尤其是生育酚作为婴儿食品、疗效食品、强化食品等的抗氧化剂和营养强化剂更具有重要的意义。Among them, tocopherol is the hydrolysis product of vitamin E, and the natural tocopherol is D-tocopherol (dextrorotary), which has 8 isomers such as α, β, γ, and δ, among which α- Tocopherol is the most active. The tocopherol mixed concentrate used as an antioxidant is a mixture of various isomers of natural tocopherol. It is widely used in whole milk powder, butter or margarine, meat products, processed aquatic products, dehydrated vegetables, juice drinks, frozen foods and convenience foods, especially tocopherol as baby food, curative food, fortified food, etc. Antioxidants and nutritional fortifiers are more important.
在一个具体的实施方式中,按质量份数计,所述组合物还包括生育酚的含量为0.1-5份,例如可以为0.1份、0.2份、0.3份、0.4份、0.5份、0.6份、0.7份、0.8份、0.9份、1份、1.1份、1.2份、1.3份、1.4份、1.5份、1.6份、1.7份、1.8份、1.9份、2份、2.5份、3份、3.5份、4份、4.5份、5份等,优选为0.5-3份。In a specific embodiment, in terms of parts by mass, the composition further includes 0.1-5 parts of tocopherol, such as 0.1 part, 0.2 part, 0.3 part, 0.4 part, 0.5 part, 0.6 part , 0.7, 0.8, 0.9, 1, 1.1, 1.2, 1.3, 1.4, 1.5, 1.6, 1.7, 1.8, 1.9, 2, 2.5, 3, 3.5 parts, 4 parts, 4.5 parts, 5 parts, etc., preferably 0.5-3 parts.
在一个具体的实施方式中,在所述组合物中,抗坏血酸的含量为3wt%-25wt%,例如可以为3wt%、4wt%、5wt%、6wt%、7wt%、8wt%、9wt%、10wt%、11wt%、12wt%、13wt%、14wt%、15wt%、16wt%、17wt%、18wt%、19wt%、20wt%、21wt%、22wt%、23wt%、24wt%、25wt%等,优选为10wt%-20wt%。In a specific embodiment, in the composition, the content of ascorbic acid is 3wt%-25wt%, such as 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%-20wt%.
在一个具体的实施方式中,在所述组合物中,基于氨基酸衍生的极性油脂的含量为2wt%-20wt%,例如可以为2wt%、3wt%、4wt%、5wt%、6wt%、7wt%、8wt%、9wt%、10wt%、11wt%、12wt%、13wt%、14wt%、15wt%、16wt%、17wt%、18wt%、19wt%、20wt%等,优选为2wt%-15wt%,更优选3wt%-10wt%。In a specific embodiment, in the composition, the content of polar oil derived from amino acid is 2wt%-20wt%, such as 2wt%, 3wt%, 4wt%, 5wt%, 6wt%, 7wt% %, 8wt%, 9wt%, 10wt%, 11wt%, 12wt%, 13wt%, 14wt%, 15wt%, 16wt%, 17wt%, 18wt%, 19wt%, 20wt%, etc., preferably 2wt%-15wt%, More preferably 3wt%-10wt%.
在一个具体的实施方式中,在所述组合物中,对香豆酸衍生物的含量为0.1wt%-3wt%,例如可以为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%等,优选为0.5wt%-1wt%;In a specific embodiment, in the composition, the content of p-coumaric acid derivatives is 0.1wt%-3wt%, such as 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%-1wt%;
在一个具体的实施方式中,在所述组合物中,生育酚的含量为0.1wt%-5wt%,例如可以为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%等,优选为0.5wt%-3wt%。In a specific embodiment, in the composition, the content of tocopherol is 0.1wt%-5wt%, such as 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%-3wt%.
本申请的组合物还可以进一步包括乳化剂,其中所述乳化剂可以是化妆品领域常用的乳化剂,本领域技术人员可以在现有技术中进行常规选择。The composition of the present application may further include an emulsifier, wherein the emulsifier may be an emulsifier commonly used in the field of cosmetics, and those skilled in the art may make routine selections in the prior art.
在一个具体的实施方式中,所述乳化剂包括鲸蜡硬脂醇聚醚-25、鲸蜡硬脂醇聚醚-20、聚丙烯酸酯-1、月桂醇聚醚-4中的一种或两种以上。In a specific embodiment, the emulsifier includes one of ceteareth-25, ceteareth-20, polyacrylate-1, laureth-4 or Two or more.
在一个具体的实施方式中,所述组合物中,按质量份数计,所述乳化剂为0.5-5份,例如可以为0.5份、1份、1.5份、2份、2.5份、3份、3.5份、4份、4.5份、5份等。In a specific embodiment, in the composition, the emulsifier is 0.5-5 parts by mass, for example, 0.5 parts, 1 part, 1.5 parts, 2 parts, 2.5 parts, 3 parts , 3.5 parts, 4 parts, 4.5 parts, 5 parts, etc.
在一个具体的实施方式中,在所述组合物中,所述乳化剂的含量为0.5wt%-5wt%,例如可以为0.5wt%、1wt%、1.5wt%、2wt%、2.5wt%、3wt%、3.5wt%、4wt%、4.5wt%、5wt%等。In a specific embodiment, in the composition, the content of the emulsifier is 0.5wt%-5wt%, such as 0.5wt%, 1wt%, 1.5wt%, 2wt%, 2.5wt%, 3wt%, 3.5wt%, 4wt%, 4.5wt%, 5wt%, etc.
在一个具体的实施方式中,所述组合物包括3wt%-25wt%抗坏血酸、0.1wt%-5wt%生育酚、0.1wt%-3wt%对香豆酸衍生物、2wt%-20wt%基于氨基酸衍生的极性油脂和0.5wt%-5wt%乳化剂。In a specific embodiment, the composition includes 3wt%-25wt% ascorbic acid, 0.1wt%-5wt% tocopherol, 0.1wt%-3wt% p-coumaric acid derivatives, 2wt%-20wt% amino acid derivatives Polar oil and 0.5wt%-5wt% emulsifier.
在一个具体的实施方式中,所述组合物包括10wt%-20wt%抗坏血酸、0.5wt%-3wt%生育酚、0.5wt%-1wt%对香豆酸衍生物、2wt%-15wt%基于氨基酸衍生的极性油脂和0.5wt%-5wt%乳化剂。In a specific embodiment, the composition includes 10wt%-20wt% ascorbic acid, 0.5wt%-3wt% tocopherol, 0.5wt%-1wt% p-coumaric acid derivatives, 2wt%-15wt% amino acid derivatives Polar oil and 0.5wt%-5wt% emulsifier.
在一个具体的实施方式中,所组合物包括5wt%-20wt%抗坏血酸、0.1wt%-5wt%生育酚、0.1wt%-2wt%对香豆酸衍生物、3wt%-15wt%基于氨基酸衍生的极性油脂、0.5wt%-5wt%乳化剂和0.01wt%-5wt%甘油。In a specific embodiment, the composition includes 5wt%-20wt% ascorbic acid, 0.1wt%-5wt% tocopherol, 0.1wt%-2wt% p-coumaric acid derivatives, 3wt%-15wt% Polar oil, 0.5wt%-5wt% emulsifier and 0.01wt%-5wt% glycerin.
在一个具体的实施方式中,所述收组合物由抗坏血酸、生育酚、对香豆酸衍生物、基于氨基酸衍生的极性油脂和水组成。In a specific embodiment, the collection composition is composed of ascorbic acid, tocopherol, p-coumaric acid derivatives, polar oils based on amino acid derivatization, and water.
在一个具体的实施方式中,所述抗坏血酸透皮吸收组合物由5wt%-20wt%抗坏血酸、0.1wt%-5wt%生育酚、0.1wt%-2wt%对香豆酸衍生物、3wt%-20wt%基于氨基酸衍生的极性油脂和水组成。In a specific embodiment, the ascorbic acid transdermal absorption composition consists of 5wt%-20wt% ascorbic acid, 0.1wt%-5wt% tocopherol, 0.1wt%-2wt% p-coumaric acid derivatives, 3wt%-20wt% % based on amino acid derived polar oils and water composition.
在一个具体的实施方式中,所述组合物由抗坏血酸、生育酚、对香豆酸衍生物、基于氨基酸衍生的极性油脂、乳化剂和水组成。In a specific embodiment, the composition consists of ascorbic acid, tocopherol, p-coumaric acid derivatives, amino acid-based polar oils, emulsifiers and water.
在一个具体的实施方式中,所述组合物由5wt%-20wt%抗坏血酸、0.1wt%-5wt%生育酚、0.1wt%-2wt%对香豆酸衍生物、3wt%-20wt%基于氨基酸衍生的极性油脂、0.5wt%-5wt%乳化剂和水组成。In a specific embodiment, the composition is composed of 5wt%-20wt% ascorbic acid, 0.1wt%-5wt% tocopherol, 0.1wt%-2wt% p-coumaric acid derivatives, 3wt%-20wt% amino acid-based It consists of polar oil, 0.5wt%-5wt% emulsifier and water.
进一步的,所述组合物还包括化妆品上可接受的辅料和/或功效成分。Further, the composition also includes cosmetically acceptable excipients and/or functional ingredients.
对于辅料,包括化妆品常用的溶剂、增稠剂、防腐剂、酸碱调节剂、香精等,例如,所述溶剂可以是化妆品领域可接受的水、醇、油酯类溶剂,所溶剂可以不包括乙二醇醚类、烷基二醇类;所述增稠剂可以是化妆品领域常用的增稠剂,如纤维素、黄原胶、瓜儿胶、泊洛沙姆等;对于防腐剂可以是化妆品领域可接受的防腐剂,如醇类防腐剂、酚类防腐剂、尼泊尔金类防腐剂、有机酸防腐剂、季胺类防腐剂等;对于酸碱调节剂可以是化妆品领域可接受的酸、碱、无机盐等;对于香精,可以是化妆品领域可接受的动物性香精、植物性香精、合成香精等。For auxiliary materials, including solvents, thickeners, preservatives, acid-base regulators, essences, etc. commonly used in cosmetics, for example, the solvents can be water, alcohol, and oily ester solvents acceptable in the field of cosmetics, and the solvents may not include Ethylene glycol ethers, alkyl glycols; The thickener can be a thickener commonly used in the field of cosmetics, such as cellulose, xanthan gum, guar gum, poloxamer, etc.; for preservatives, it can be Acceptable preservatives in the field of cosmetics, such as alcohol preservatives, phenolic preservatives, Nepal gold preservatives, organic acid preservatives, quaternary ammonium preservatives, etc.; acid-base regulators can be acceptable acids in the field of cosmetics , alkali, inorganic salt, etc.; for essence, it can be acceptable animal essence, plant essence, synthetic essence, etc. in the field of cosmetics.
对于功效成分,包括化妆品常用的美白成分、保湿成分、祛皱成分、抗衰成分、控油祛痘成分、修复成分等。例如,化妆品领域常用的美白成分包括但不限于间苯二酚类化合物、果酸及其衍生物、维生素C及其衍生物、壬二酸、熊果苷及其衍生物、曲酸及其衍生物、氨甲环酸、泛酸衍生物、生物美白制剂、天然动植物提取物等;化妆品领域常用的保湿成分包括但不限于透明质酸、维生素B5、羟乙基脲、甜菜碱、卵磷脂、多元醇类、氨基酸、木糖醇等;化妆品领域常用的祛皱成分包括但不限于维C、A醇、玻色因、胜肽等;化妆品领域常用的抗衰成分包括但不限于视黄醇、玻色因、富勒烯等;化妆品领域常用的控油祛痘成分包括但不限于水杨酸、果酸、烟酰胺、金缕梅等;化妆品领域常用的修复成分包括但不限于神经酰胺、依克多因、尿囊素、积雪草、洋甘菊等。For functional ingredients, it includes whitening ingredients, moisturizing ingredients, anti-wrinkle ingredients, anti-aging ingredients, oil control and acne ingredients, and repairing ingredients commonly used in cosmetics. For example, commonly used whitening ingredients in the field of cosmetics include but are not limited to resorcinol compounds, fruit acids and their derivatives, vitamin C and its derivatives, azelaic acid, arbutin and its derivatives, kojic acid and its derivatives substances, tranexamic acid, pantothenic acid derivatives, biological whitening preparations, natural animal and plant extracts, etc.; commonly used moisturizing ingredients in the field of cosmetics include but are not limited to hyaluronic acid, vitamin B5, hydroxyethyl urea, betaine, lecithin, Polyols, amino acids, xylitol, etc.; anti-wrinkle ingredients commonly used in the cosmetic field include but not limited to vitamin C, A alcohol, Bosein, peptides, etc.; anti-aging ingredients commonly used in the cosmetic field include but not limited to retinol , Boseine, fullerene, etc.; oil control and acne-removing ingredients commonly used in the field of cosmetics include but not limited to salicylic acid, fruit acid, niacinamide, witch hazel, etc.; repairing ingredients commonly used in the field of cosmetics include but not limited to ceramide, Ectoine, allantoin, centella asiatica, chamomile, etc.
在本申请一个具体实施方式中,所述组合物还包含作为保湿成分的甘油。In a specific embodiment of the present application, the composition further comprises glycerin as a moisturizing ingredient.
本申请还提供上述的组合物在提高抗坏血酸的稳定性和/或促进抗坏血酸透皮吸收中的用途。The present application also provides the use of the above-mentioned composition in improving the stability of ascorbic acid and/or promoting the transdermal absorption of ascorbic acid.
实施例Example
下述实施例中所使用的实验方法如无特殊要求,均为常规方法。The experimental methods used in the following examples are conventional methods unless otherwise specified.
实施例1Example 1
称取15g L-抗坏血酸、0.5g聚丙烯酸酯-1加入77.5g水中搅拌均匀,升温至60℃作为A相;称取1g生育酚、0.5g阿魏酸、3.5g N-月桂酰肌氨酸异丙酯、2g鲸蜡硬脂醇聚醚-25加热至60℃融化作为B相,B加入A均质3000rpm、3min,降温即得抗坏血酸组合物。Weigh 15g L-ascorbic acid, 0.5g polyacrylate-1, add 77.5g water and stir evenly, heat up to 60°C as phase A; weigh 1g tocopherol, 0.5g ferulic acid, 3.5g N-lauroyl sarcosine Isopropyl ester and 2g of ceteareth-25 were heated to 60°C and melted as phase B, and B was added to A to homogenize at 3000 rpm for 3 minutes, and the temperature was lowered to obtain the ascorbic acid composition.
实施例2Example 2
称取15g L-抗坏血酸、0.5g聚丙烯酸酯-1加入76g水中搅拌均匀,升温至60℃作为A相;称取1g生育酚、2.0g阿魏酸、3.5g N-月桂酰肌氨酸异丙酯、2g鲸蜡硬脂醇聚醚-25加热至60℃融化作为B相,B加入A均质3000rpm、3min,降温即得抗坏血酸组合物。Weigh 15g L-ascorbic acid, 0.5g polyacrylate-1, add 76g water and stir evenly, heat up to 60°C as phase A; weigh 1g tocopherol, 2.0g ferulic acid, 3.5g N-lauroyl sarcosine iso Propyl ester and 2g of ceteareth-25 were heated to 60°C and melted as phase B, and B was added to A to homogenize at 3000 rpm for 3 minutes, and the temperature was lowered to obtain the ascorbic acid composition.
实施例3Example 3
称取15g L-抗坏血酸、0.5g聚丙烯酸酯-1加入71g水中搅拌均匀,升温至60℃作为A相;称取1g生育酚、2.0g阿魏酸、10g N-月桂酰肌氨酸异丙酯、2g鲸蜡硬脂醇聚醚-25加热至60℃融化作为B相,B加入A均质3000rpm、3min,降温即得抗坏血酸组合物。Weigh 15g L-ascorbic acid, 0.5g polyacrylate-1, add 71g water and stir evenly, heat up to 60°C as phase A; weigh 1g tocopherol, 2.0g ferulic acid, 10g N-lauroyl sarcosine isopropyl Esters and 2g ceteareth-25 were heated to 60°C and melted as phase B, B was added to A homogeneously at 3000 rpm for 3 minutes, and the ascorbic acid composition was obtained after cooling down.
实施例4Example 4
称取15g L-抗坏血酸、0.5g聚丙烯酸酯-1加入78g水中搅拌均匀,升温至60℃作为A相;称取0.5g生育酚、0.5g阿魏酸、3.5g N-月桂酰肌氨酸异丙酯、2g鲸蜡硬脂醇聚醚-25加热至60℃融化作为B相,B加入A均质3000rpm、3min,降温即得抗坏血酸组合物。Weigh 15g L-ascorbic acid, 0.5g polyacrylate-1, add 78g water and stir evenly, heat up to 60°C as phase A; weigh 0.5g tocopherol, 0.5g ferulic acid, 3.5g N-lauroyl sarcosine Isopropyl ester and 2g of ceteareth-25 were heated to 60°C and melted as phase B, and B was added to A to homogenize at 3000 rpm for 3 minutes, and the temperature was lowered to obtain the ascorbic acid composition.
实施例5Example 5
称取5g L-抗坏血酸、0.5g聚丙烯酸酯-1加入87.5g水中搅拌均匀,升温至60℃作为A相;称取1g生育酚、0.5g阿魏酸、3.5g N-月桂酰肌氨酸异丙酯、2g鲸蜡硬脂醇聚醚-25加热至60℃融化作为B相,B加入A均质3000rpm、3min,降温即得。Weigh 5g L-ascorbic acid, 0.5g polyacrylate-1, add 87.5g water and stir evenly, heat up to 60°C as phase A; weigh 1g tocopherol, 0.5g ferulic acid, 3.5g N-lauroyl sarcosine Isopropyl ester and 2g of ceteareth-25 were heated to 60°C and melted as phase B, and B was added to A to homogenize at 3000 rpm for 3 minutes, and the temperature was lowered.
实施例6Example 6
称取20g L-抗坏血酸、0.5g聚丙烯酸酯-1加入72.5g水中搅拌均匀,升温至60℃作为A相;称取1g生育酚、0.5g阿魏酸、3.5g N-月桂酰肌氨酸异丙酯、2g鲸蜡硬脂醇聚醚-25加热至60℃融化作为B相,B加入A均质3000rpm、3min,降温即得抗坏血酸组合物。Weigh 20g L-ascorbic acid, 0.5g polyacrylate-1, add 72.5g water and stir evenly, heat up to 60°C as phase A; weigh 1g tocopherol, 0.5g ferulic acid, 3.5g N-lauroyl sarcosine Isopropyl ester and 2g of ceteareth-25 were heated to 60°C and melted as phase B, and B was added to A to homogenize at 3000 rpm for 3 minutes, and the temperature was lowered to obtain the ascorbic acid composition.
实施例7Example 7
称取15g L-抗坏血酸、0.5g聚丙烯酸酯-1加入76.5g水中搅拌均匀,升温至60℃作为A相;称取2g生育酚、0.5g阿魏酸、3.5g N-月桂酰肌氨酸异丙酯、2g鲸蜡硬脂醇聚醚-25加热至60℃融化作为B相,B加入A均质3000rpm、3min,降温即得。Weigh 15g L-ascorbic acid, 0.5g polyacrylate-1, add 76.5g water and stir evenly, heat up to 60°C as phase A; weigh 2g tocopherol, 0.5g ferulic acid, 3.5g N-lauroyl sarcosine Isopropyl ester and 2g of ceteareth-25 were heated to 60°C and melted as phase B, and B was added to A to homogenize at 3000 rpm for 3 minutes, and the temperature was lowered.
实施例8Example 8
称取15g L-抗坏血酸、0.5g聚丙烯酸酯-1加入77.5g水中搅拌均匀,升温至60℃作为A相;称取1g生育酚、0.5g阿魏酸、3.5g植物甾醇/辛基十二醇月桂酰谷氨酸酯、2g鲸蜡硬脂醇聚醚-25加热至60℃融化作为B相,B加入A均质3000rpm、3min,降温即得抗坏血酸组合物。Weigh 15g L-ascorbic acid, 0.5g polyacrylate-1, add 77.5g water and stir evenly, raise the temperature to 60°C as phase A; weigh 1g tocopherol, 0.5g ferulic acid, 3.5g phytosterol/octyldodecane Alcohol lauroyl glutamate and 2g of ceteareth-25 were heated to 60°C and melted as phase B, and B was added to A to homogenize at 3000 rpm for 3 minutes, and the temperature was lowered to obtain the ascorbic acid composition.
实施例9Example 9
称取15g L-抗坏血酸、3g甘油、0.5g聚丙烯酸酯-1加入74.5g水中搅拌均匀,升温至60℃作为A相;称取1g生育酚、0.5g阿魏酸、3.5g N-月桂酰肌氨酸异丙酯、2g鲸蜡硬脂醇聚醚-25加热至60℃融化作为B相,B加入A均质3000rpm、3min,降温即得抗坏血酸组合物。Weigh 15g of L-ascorbic acid, 3g of glycerin, 0.5g of polyacrylate-1, add 74.5g of water and stir evenly, raise the temperature to 60°C as phase A; weigh 1g of tocopherol, 0.5g of ferulic acid, 3.5g of N-lauroyl Isopropyl sarcosinate and 2g of ceteareth-25 were heated to 60°C and melted as phase B, and B was added to A to homogenize at 3000 rpm for 3 minutes, and the temperature was lowered to obtain the ascorbic acid composition.
实施例10Example 10
称取15g L-抗坏血酸加入77.5g水中搅拌均匀,升温至60℃作为A相;称取1g生育酚、0.5g阿魏酸、3.5g N-月桂酰肌氨酸异丙酯、2.5g鲸蜡硬脂醇聚醚-25加热至60℃融化作为B相,B加入A均质3000rpm、3min,降温即得抗坏血酸组合物。Weigh 15g of L-ascorbic acid, add it to 77.5g of water and stir evenly, heat up to 60°C as phase A; weigh 1g of tocopherol, 0.5g of ferulic acid, 3.5g of N-lauroyl sarcosinate isopropyl ester, 2.5g of cetyl wax Steareth-25 was heated to 60°C and melted as phase B, B was added to A homogeneously at 3000 rpm for 3 minutes, and the temperature was lowered to obtain the ascorbic acid composition.
实施例11Example 11
称取15g L-抗坏血酸、0.5g聚丙烯酸酯-1加入77.5g水中搅拌均匀,升温至60℃作为A相;称取1g生育酚、0.5g咖啡酸、3.5g N-月桂酰肌氨酸异丙酯、2g鲸蜡硬脂醇聚醚-25加热至60℃融化作为B相,B加入A均质3000rpm、3min,降温即得抗坏血酸组合物。Weigh 15g of L-ascorbic acid, 0.5g of polyacrylate-1, add 77.5g of water and stir evenly, raise the temperature to 60°C as phase A; weigh 1g of tocopherol, 0.5g of caffeic acid, 3.5g of N-lauroyl sarcosine iso Propyl ester and 2g of ceteareth-25 were heated to 60°C and melted as phase B, and B was added to A to homogenize at 3000 rpm for 3 minutes, and the temperature was lowered to obtain the ascorbic acid composition.
实施例12Example 12
称取15g L-抗坏血酸加入80g水中搅拌均匀,升温至60℃作为A相;称取1g生育酚、0.5g阿魏酸、3.5g N-月桂酰肌氨酸异丙酯加热至60℃融化作为B相,B加入A均质3000rpm、3min,降温即得抗坏血酸组合物。Weigh 15g L-ascorbic acid, add 80g water and stir evenly, heat up to 60°C as phase A; weigh 1g tocopherol, 0.5g ferulic acid, 3.5g N-lauroyl sarcosine isopropyl ester and heat to 60°C to melt as In phase B, B was added to A to homogenize at 3000 rpm for 3 minutes, and the temperature was lowered to obtain the ascorbic acid composition.
对比例1Comparative example 1
称取15g L-抗坏血酸、3g甘油、0.5g聚丙烯酸酯-1加入77.5g水中搅拌均匀,升温至60℃作为A相;称取1g生育酚、0.5g阿魏酸、3.5g丙二醇醚、2g鲸蜡硬脂醇聚醚-25加热至60℃融化作为B相,B加入A均质3000rpm、3min,降温即得抗坏血酸组合物。Weigh 15g of L-ascorbic acid, 3g of glycerin, 0.5g of polyacrylate-1, add 77.5g of water and stir evenly, raise the temperature to 60°C as phase A; weigh 1g of tocopherol, 0.5g of ferulic acid, 3.5g of propylene glycol ether, 2g Ceteareth-25 was heated to 60°C and melted as phase B, B was added to A homogeneously at 3000 rpm for 3 minutes, and the temperature was lowered to obtain the ascorbic acid composition.
对比例2Comparative example 2
称取15g L-抗坏血酸、0.5g聚丙烯酸酯-1加入80g水中搅拌均匀,升温至60℃作为A相;称取1g生育酚、0.5g阿魏酸、1g N-月桂酰肌氨酸异丙酯、2g鲸蜡硬脂醇聚醚-25加热至60℃融化作为B相,B加入A均质3000rpm、3min,降温即得抗坏血酸组合物。Weigh 15g L-ascorbic acid, 0.5g polyacrylate-1, add 80g water and stir evenly, heat up to 60°C as phase A; weigh 1g tocopherol, 0.5g ferulic acid, 1g N-lauroyl sarcosine isopropyl Esters and 2g ceteareth-25 were heated to 60°C and melted as phase B, B was added to A homogeneously at 3000 rpm for 3 minutes, and the ascorbic acid composition was obtained after cooling down.
对比例3Comparative example 3
称取15g L-抗坏血酸加入85g水中搅拌均匀,升温至60℃作为,降温即得抗坏血酸组合物。Weigh 15g of L-ascorbic acid and add it to 85g of water, stir evenly, raise the temperature to 60°C, and lower the temperature to obtain the ascorbic acid composition.
上述实施例和对比例的具体条件如表1所示。The concrete conditions of above-mentioned embodiment and comparative example are as shown in table 1.
表1Table 1
试验例Test case
试验例1稳定性测试Test Example 1 Stability Test
将上述实施例和对比例制备得到的样品进行稳定性测试。具体地,将如上所述实施例和对比例制备得到的抗坏血酸组合物分装到无色透明的PET材质小瓶中,分别放置于Binder 45℃±2℃烘箱中不避光条件下考察28天的高温稳定性,到达设置考察时间后从烘箱中取出乳液常温放置并恢复至室温,使用HPLC定量抗坏血酸的含量,使用所测的抗坏血酸的含量除以初始的抗坏血酸含量,得到抗坏血酸的保留比率,得到的结果如表2所示。The samples prepared in the above examples and comparative examples were subjected to a stability test. Specifically, the ascorbic acid compositions prepared in the above-mentioned examples and comparative examples were divided into colorless and transparent PET vials, and placed in a Binder oven at 45°C±2°C without light protection for 28 days. High temperature stability, after reaching the set investigation time, take out the emulsion from the oven and place it at room temperature and return to room temperature, use HPLC to quantify the content of ascorbic acid, divide the measured ascorbic acid content by the initial ascorbic acid content, and obtain the retention ratio of ascorbic acid. The results are shown in Table 2.
表2Table 2
从表2中可以看出,实施例中使用的氨基酸衍生的极性油脂和对比例1中使用的丙二醇醚均能溶解阿魏酸这样的对香豆酸衍生物,但是相较于对比例1,实施例使用的氨基酸衍生的极性油脂能够提高抗坏血酸的稳定性。且在相同用量下,对比例1的醇醚类溶剂对抗坏血酸的稳定性要差于实施例中使用的氨基酸衍生的极性油脂。As can be seen from Table 2, the amino acid derived polar oil used in the examples and the propylene glycol ether used in Comparative Example 1 can dissolve p-coumaric acid derivatives such as ferulic acid, but compared with Comparative Example 1 , the amino acid-derived polar oil used in the examples can improve the stability of ascorbic acid. And under the same dosage, the alcohol ether solvent of Comparative Example 1 is less stable to ascorbic acid than the amino acid-derived polar oil used in the examples.
试验例2体外透皮吸收测试Test example 2 in vitro transdermal absorption test
通过Franz扩散池法对本申请的抗坏血酸组合物进行体外透皮吸收的测试,使用猪皮作为载体,将其固定在Franz扩散池的供给室和接收室之间,将扩散池固定于透皮吸收扩散仪中,在开启磁搅拌子和恒温水浴的情况下,向室中皮肤表面加入实施例和对比例制备的抗坏血酸组合物样品进行透皮实验。接收液选择含有20%聚乙二醇(PEG)+PBS的水溶液,并分别在2h、4h、8h、24h测定抗坏血酸、阿魏酸的透皮量。累积透皮量Q计算公式为:Q=[Cn x V+∑Ci x V0]/S(i=1…n-1),其中Q为累积透皮量,S为有效扩散面积,V为接收室中接收液体积,V0为每次取样的体积,Ci为第一次至上次取样时接收液中药物浓度,Cn为第n个取样点测得的样品浓度。组合物中抗坏血酸累积透皮量随时间变化结果如下表3。The ascorbic acid composition of the present application is tested for in vitro transdermal absorption by the Franz diffusion cell method. Pig skin is used as a carrier, which is fixed between the supply chamber and the receiving chamber of the Franz diffusion cell, and the diffusion cell is fixed on the transdermal absorption diffusion cell. In the instrument, under the condition of turning on the magnetic stirring bar and the constant temperature water bath, the ascorbic acid composition samples prepared in the examples and the comparative examples were added to the skin surface in the chamber to carry out the transdermal test. As the receiving solution, an aqueous solution containing 20% polyethylene glycol (PEG)+PBS was selected, and the transdermal amounts of ascorbic acid and ferulic acid were measured at 2h, 4h, 8h, and 24h, respectively. The formula for calculating the cumulative transdermal volume Q is: Q=[Cn x V+∑Ci x V0]/S(i=1...n-1), where Q is the cumulative transdermal volume, S is the effective diffusion area, and V is the receiving chamber V0 is the volume of each sampling, Ci is the drug concentration in the receiving solution from the first sampling to the last sampling, and Cn is the sample concentration measured at the nth sampling point. The cumulative transdermal amount of ascorbic acid in the composition changes with time as shown in Table 3.
表3抗坏血酸组合物中抗坏血酸不同时间的累计透皮量The cumulative transdermal amount of ascorbic acid in different time in table 3 ascorbic acid composition
从表3中可以看出,实施例1-4、7-12和对比例3相比,组合物中抗坏血酸添加量相同的情况下,实施例具有更高的抗坏血酸的透皮吸收量,说明本申请的组合物具有显著提升抗坏血酸的透皮吸收的效果。实施例1、8和对比例1相比,基于氨基酸衍生的极性油脂相比于丙二醇醚,可以显著提高抗坏血酸组合物中抗坏血酸的透皮吸收量。As can be seen from Table 3, compared with Example 1-4, 7-12 and Comparative Example 3, under the same situation of the ascorbic acid addition amount in the composition, the embodiment has a higher transdermal absorption of ascorbic acid, indicating that this The applied composition has the effect of significantly improving the transdermal absorption of ascorbic acid. Compared with Examples 1 and 8 and Comparative Example 1, the amino acid-derived polar oil can significantly increase the transdermal absorption of ascorbic acid in the ascorbic acid composition compared with propylene glycol ether.
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