WO2019100923A1 - 一种护肤组合物及其应用、保健品 - Google Patents

一种护肤组合物及其应用、保健品 Download PDF

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WO2019100923A1
WO2019100923A1 PCT/CN2018/113403 CN2018113403W WO2019100923A1 WO 2019100923 A1 WO2019100923 A1 WO 2019100923A1 CN 2018113403 W CN2018113403 W CN 2018113403W WO 2019100923 A1 WO2019100923 A1 WO 2019100923A1
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powder
parts
concentrated
skin
skin care
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PCT/CN2018/113403
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English (en)
French (fr)
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贺瑞坤
张旭光
陈天玲
汪玉芳
肖健
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汤臣倍健股份有限公司
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Publication of WO2019100923A1 publication Critical patent/WO2019100923A1/zh

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/42Cucurbitaceae (Cucumber family)
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23GCOCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
    • A23G3/00Sweetmeats; Confectionery; Marzipan; Coated or filled products
    • A23G3/34Sweetmeats, confectionery or marzipan; Processes for the preparation thereof
    • A23G3/36Sweetmeats, confectionery or marzipan; Processes for the preparation thereof characterised by the composition containing organic or inorganic compounds
    • A23G3/364Sweetmeats, confectionery or marzipan; Processes for the preparation thereof characterised by the composition containing organic or inorganic compounds containing microorganisms or enzymes; containing paramedical or dietetical agents, e.g. vitamins
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23GCOCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
    • A23G3/00Sweetmeats; Confectionery; Marzipan; Coated or filled products
    • A23G3/34Sweetmeats, confectionery or marzipan; Processes for the preparation thereof
    • A23G3/36Sweetmeats, confectionery or marzipan; Processes for the preparation thereof characterised by the composition containing organic or inorganic compounds
    • A23G3/48Sweetmeats, confectionery or marzipan; Processes for the preparation thereof characterised by the composition containing organic or inorganic compounds containing plants or parts thereof, e.g. fruits, seeds, extracts
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/105Plant extracts, their artificial duplicates or their derivatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/01Hydrocarbons
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/32Burseraceae (Frankincense family)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/87Vitaceae or Ampelidaceae (Vine or Grape family), e.g. wine grapes, muscadine or peppervine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/88Liliopsida (monocotyledons)
    • A61K36/886Aloeaceae (Aloe family), e.g. aloe vera
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/88Liliopsida (monocotyledons)
    • A61K36/896Liliaceae (Lily family), e.g. daylily, plantain lily, Hyacinth or narcissus
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23VINDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00Food compositions, function of food ingredients or processes for food or foodstuffs

Definitions

  • the invention relates to the technical field of health care products, in particular to a skin care composition, an application thereof and a health care product.
  • Free Radicals aging theory was first proposed by Denham Harman in 1955. The theory holds that: free radicals have a strong oxidizing power. When the free radical metabolism in the body is in an unbalanced state, excessive free radicals will cause damage to the body, and the unsaturated fatty acids will be oxidized into lipid peroxidase (lipid peroxidase, LPO), the final product malonic dialdehyde (MDA) is a strong cross-linking agent, and cross-links with biomacromolecules such as proteins and nucleic acids to form a poorly soluble substance, lipofuscin. After entering the middle-aged and old age, as the age increases, the amount of lipofuscin in the skin gradually increases, which makes the dark yellow color of the skin become more serious.
  • MDA malonic dialdehyde
  • Non-enzymatic glycosylation in vivo means that the aldehyde or keto group of a reducing sugar reacts with a free amino group in a macromolecule such as a protein to form a reversible or irreversible conjugate under conditions uncatalyzed by the enzyme - a higher glycosylation terminal
  • AGEs Advanced glycation end-products
  • Dyer et al found that skin aging is associated with non-enzymatic glycosylation.
  • the dermis of the skin is rich in collagen and elastin.
  • the amino acids in the protein molecule are easily non-enzymatically glycosylated with the aldehyde or keto group of glucose in the extracellular fluid.
  • the reaction and as the age increases, the AGEs progressively increase, and the browning of the AGEs forms a brown-yellow bio-waste, which accumulates in the dermis layer of the skin, causing the skin to lose its opacity and yellowing and dullness.
  • the increase of AGEs in the skin causes collagen to form intermolecular crosslinks, which not only reduces the elasticity and permeability of the skin, but also weakens the diffusion properties of nutrients and wastes, and reduces the solubility of collagen, making it difficult to be hydrolyzed by collagenase.
  • the skin elasticity is reduced, and the wrinkles are not easily calmed and deepened, thereby accelerating the aging process of the skin.
  • Modern medicine solves the problem of dark yellow skin and delays aging. It mainly starts from the above two aspects: 1 inhibiting non-enzymatic glycosylation reaction, eliminating the harm of carbonyl compounds to the skin; 2 scavenging free radicals, avoiding lipid peroxidation, reducing the production of carbonyl compounds And the formation of dark yellow skin.
  • the present invention provides the following technical solutions:
  • the skin care composition provided by the invention comprises concentrated melon powder, acerola cherry powder and concentrated olive juice lyophilized powder.
  • the skin care composition comprises the following components in parts by weight:
  • the composition further comprises aloe vera gel, grape seed extract and lycopene.
  • the skin care composition comprises the following components in parts by weight:
  • the invention adopts a composition composed of three kinds of natural edible and edible plant extracts of concentrated melon powder, acerola cherry powder and concentrated olive juice lyophilized powder, which exhibits synergistic effect in whitening and anti-aging, and can effectively inhibit The formation of tyrosine, scavenging free radicals, and improving skin photodamage indicate that the composition of the present invention has a remarkable effect of whitening and delaying aging.
  • the addition of Aloe vera gel, grape seed extract and lycopene can significantly enhance the whitening and anti-aging effects.
  • Cantaloupe is also known as melon or melon.
  • the fruit of the cucurbitaceae has a multi-chamber and multi-fruit, much like a berry.
  • the content of antioxidant substances in cantaloupe is extremely high. It is mainly based on SOD and vitamin C. It can eliminate free radicals in the body, relieve aging, and also has certain anti-ultraviolet effect. It can reduce the formation and precipitation of pigments. Beauty and beauty effects. Especially in the sunny season, it can avoid pigmentation and protect the skin from sunscreen, whitening and wrinkle.
  • Olive (Canarium album (Lour.) Raeusch.), also known as the sapling, also known as the sorghum, the olive family of olive genus. Nanjing people call it green fruit, Lingnan people call it olives, whether it is oysters or boiled juice, it can produce thirst, cure throat, relieve fish sputum and throat. Olives are rich in nutrients, and the flesh contains protein, carbohydrates, fat, vitamin C and minerals such as calcium, phosphorus and iron. Using modern biotechnology analysis, the main active substance in olives is polyphenols. The research shows that olive polyphenols have strong free radical scavenging ability and high antioxidant activity. The free radical scavenging ability of olive polyphenols is higher than that of artificial Synthetic antioxidants BHA and ascorbic acid.
  • Hydroxytyrosol also known as 3,4-dihydroxyphenylethanol, is a natural antioxidant widely found in the foliage and fruits of the olive plant of the olive family, especially in the olive groves of the Mediterranean. High in content, it is the active ingredient of olive oil. Numerous studies have shown that hydroxytyrosol has a strong antioxidant effect (Aeschbach et al. 1994; Visioli et al. 1998), which prevents auto-oxidation of polyunsaturated fatty acids (Tsinidou et al. 1995). Hydroxytyrosol has a higher ability to scavenge free radicals than other synthetic and natural antioxidants.
  • hydroxytyrosol can reduce the level of ROS and lipid peroxidation in HepG2 cells caused by t-butyl hydroperoxide, and prevent the decrease of glutathione caused by t-butyl hydroperoxide.
  • Glutathione is an endogenous major antioxidant secreted by cells that directly neutralizes free radicals and reactive oxygen species.
  • vitamin C 100 grams of fresh fruit vitamin C content of 3500 mg, equivalent to 500 times that of apples, 100 times of citrus, 600 times of grapes, 200 times of pears, 12 times of kiwi, is known as the king of vitamin C.
  • Aloe vera gel made from Aloe vera leaves, is made by draining, peeling, blanching, sterilizing, etc.
  • Aloe vera gel freeze-dried powder moisturizes dry skin, removes acne, removes wrinkles It has unique and magical effects in restoring skin elasticity, improving human immunity, scavenging free radicals, and alleviating pain in inflamed and damaged skin.
  • Grape seed is the seed of grape, is the waste of wine and other products, after drying, the product obtained after separating grape skin and grape stem, accounts for 4% to 6% of the whole grape quality. Grape seed is rich in amino acids, vitamins, minerals and dietary fiber and many other nutrients and a variety of active ingredients, such as catechins and proanthocyanidins and other polyphenols, with health and beauty effects.
  • Lycopene a type of carotenoid, is found in foods such as tomatoes, watermelons, grapefruits, and papayas. Lycopene is a natural biological antioxidant extracted from tomato and has a unique long-chain molecular structure. Studies have shown that the antioxidant capacity of lycopene is 100 times that of vitamin E. A lycopene molecule can remove thousands of singlet oxygen. Lycopene is the carotenoid that quenches singlet oxygen and scavenges hydrogen peroxide and has the strongest free radical. The ability to inhibit and destroy singlet oxygen is twice that of carotene. Therefore, lycopene can prevent lipid oxidation by quenching singlet oxygen, protect biofilm from free radical damage, and protect the face and delay aging.
  • the skin care composition comprises the following components in parts by weight:
  • the skin care composition comprises the following components in parts by weight:
  • the skin care composition comprises the following components in parts by weight:
  • the skin care composition comprises the following components in parts by weight:
  • the skin care composition comprises the following components in parts by weight:
  • the concentrated melon powder, the conifer cherry powder, the concentrated olive juice lyophilized powder, the aloe vera gel and the grape seed extract may be a lyophilized powder or a concentrate.
  • the amount of efficacy of the concentrate and the lyophilized powder should be equal to the amount of the original extract component.
  • the present invention also provides the use of the skin care composition for the preparation of a medicament or a health care product having whitening and anti-aging effects.
  • the present invention also provides a medicament having a whitening anti-aging effect, comprising the skin care composition and a pharmaceutically acceptable adjuvant.
  • the present invention also provides a health care product having whitening and anti-aging effects, including acceptable excipients in the skin care composition and health care product.
  • the acceptable excipient in the health supplement is selected from the group consisting of isomalt, microcrystalline cellulose, magnesium stearate, maltitol, resistant dextrin, stevioside, pregelatinized starch, silica. One or two or more.
  • the acceptable auxiliary materials in the health care product are 20-40 parts of isomalt, 20-40 parts of microcrystalline cellulose, and magnesium stearate 1 in parts by weight. - 5 servings.
  • the acceptable excipients in the health supplement are 20-40 parts of maltitol, 20-40 parts of resistant dextrin, and 1-5 parts of stevioside.
  • the acceptable auxiliary materials in the health care product are 20-40 parts of pregelatinized starch, 0.5-2 parts of magnesium stearate, and 0.5-2 of silica. Share.
  • the dosage form of the health food is a tablet, a capsule, a pill, a granule, a powder, and an oral solution.
  • the health care product is a tablet candy.
  • Compressed candy is a product obtained by directly compressing powder, granules by granulation or dry powder mixing (no granulation).
  • the main types are ordinary compressed sugar, coated compressed sugar, multi-layered candy, effervescent tablet Sugar and chewing type compressed sugar.
  • the packaging of fashionable and convenient compressed candy has become one of the fastest growing candy products in the candy market in recent years due to its rich taste, fresh breath or health care function.
  • composition of the three kinds of natural edible and edible plant extracts which are concentrated melon powder, conifer cherry powder and concentrated olive juice lyophilized powder, exhibit synergistic effect in whitening and anti-aging. It can effectively inhibit the formation of tyrosine, scavenge free radicals, and improve skin photodamage.
  • the addition of Aloe vera gel, grape seed extract and lycopene can significantly enhance the whitening and anti-aging effects.
  • the invention discloses a skin care composition and an application thereof, a health care product, and those skilled in the art can learn from the contents of the paper and appropriately improve the process parameters. It is to be understood that all such alternatives and modifications are obvious to those skilled in the art and are considered to be included in the present invention.
  • the method and the application of the present invention have been described by the preferred embodiments, and it is obvious that the method and application described herein may be modified or appropriately modified and combined without departing from the scope of the present invention. The technique of the present invention is applied.
  • compositions of Examples 1 to 6 and Comparative Examples 1 to 6 were diluted with water to obtain a sample liquid having a final concentration of 10 mg/mL.
  • Comparative Example 1 30.41 77.89 54.15 Comparative Example 2 29.28 76.46 52.87 Comparative Example 3 30.86 79.23 55.05 Comparative Example 4 31.37 80.02 55.70 Comparative Example 5 33.43 82.91 58.17 Comparative Example 6 32.74 80.74 56.74
  • the tyrosinase inhibition rate and the DPPH clearance rate of the groups 1 to 6 were significantly better than those of the single drug group and the comparative group 1 to 6, and had a remarkable whitening effect.
  • Example 8 Protective effect of the composition of the invention on photodamage of rat skin
  • Grouping of animals 120 Wistar rats, 5 weeks old, weighing 122.5 ⁇ 5.5g, male and female, were fed in separate cages according to the standard conditions of clean animals. They were randomly divided into 15 groups, including normal control group, model control group, single drug group and test group, with 8 rats in each group, administered intragastrically (0.83 g/kg) according to the administration method shown in Table 3, and continuously administered. After 4 weeks, the rats were given normal drinking water during the test, and normal granule feed was normally fed.
  • Animal hair removal + UVA irradiation Rats were moderately anesthetized with ether inhalation, and the back hair was cut to 1 mm with an ophthalmic scissors, and then the remaining rat hair was shaved with an electric shaver, and the hair removal area was about 5.0 ⁇ 4.5 cm. Hair removal 6 h before irradiation.
  • Specimen samples rats were anesthetized by ether inhalation 24 hours after irradiation. The skin at the center of the back hair removal area was removed by skin biopsy. The subcutaneous tissue was removed as much as possible. After washing with physiological saline, 10% neutral formalin and liquid nitrogen were placed respectively. Save in standby. After the specimens were taken, conventional 10% formalin was fixed, paraffin-embedded 4 ⁇ m serial sections, and conventional HE staining.
  • Detection of skin MDA content, superoxide dismutase (SOD) activity, and glutathione peroxidase (GSH-Px) activity After the last UVA ten UVB irradiation experiment, the rats were sacrificed and the rat back irradiation area was taken. Part of the skin, the subcutaneous fat was removed and weighed, made into a 10% tissue homogenate, centrifuged at 3000 rpm for 10 minutes, and the supernatant was taken for determination of each index.
  • SOD superoxide dismutase
  • GSH-Px glutathione peroxidase
  • UVA+UVB irradiation could significantly increase the MDA content in the skin tissue homogenate of rats, and the SOD activity and glutathione peroxidase (GSH-Px) activity were significantly decreased.
  • UVA+UVB irradiation+Examples 1 to 6 significantly reduced the content of MDA in skin tissue homogenate (P ⁇ 0.05), and significantly increased SOD activity and GSH-Px activity (P ⁇ 0.05).
  • the composition of Example 4 has the best effect on ultraviolet rays.
  • the content of MDA, SOD activity and GSH-Px activity in the skin tissue homogenate of the comparative groups 1 to 6 were not significantly different from those of the model group, indicating that the composition of the comparative group had no significant effect on ultraviolet protection.
  • the AGE Reader skin AGEs fluorescence spectrometer
  • AF skin autofluorescence
  • compositions described in Examples 2 to 6 were subjected to a whitening anti-aging efficacy test, and the results were the same as or similar to those of Example 1, and there was no significant difference (P>0.05).

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Abstract

一种具有美白、抗衰老功效的护肤组合物,包括:浓缩香瓜粉、针叶樱桃粉和浓缩橄榄汁冻干粉。实验结果表明,本发明选用包括浓缩香瓜粉、针叶樱桃粉和浓缩橄榄汁冻干粉这三种天然药食同源的药材组成的组合物在美白、延缓衰老方面具有协同增效作用,能够有效地抑制酪氨酸形成、清除自由基、改善皮肤光损伤。以上结果表明,本发明提供的护肤组合物具有显著地美白、延缓衰老的作用,可用于制备具有美白、抗衰老作用的药物或保健品。

Description

一种护肤组合物及其应用、保健品
本申请要求于2017年11月21日提交中国专利局、申请号为201711163108.2、发明名称为“一种护肤组合物及其应用、保健品”的中国专利申请的优先权,其全部内容通过引用结合在本申请中。
技术领域
本发明涉及保健品技术领域,具体涉及一种护肤组合物及其应用、保健品。
背景技术
现代医学对肤色暗黄生化本质的认识:关于皮肤衰老的机理研究得非常多,先后出现过很多学说,但能够较为合理地揭示肤色暗黄问题的主要有自由基衰老学说、非酶糖基化衰老学说。
肤色暗黄与自由基衰老学说:自由基(Free Radicals)衰老学说最早是由Denham Harman于1955年提出来的。该学说认为:自由基具有极强的氧化能力,当机体内的自由基代谢处于不平衡状态时,过量的自由基就会引起机体损伤,将不饱和脂肪酸氧化成过氧化脂质(lipid peroxidase,LPO),其终产物丙二醛(malonic dialdehyde,MDA)是很强的交联剂,与蛋白质、核酸等生物大分子交联,形成难溶性物质-脂褐素。人进入中老年之后,随着年龄的增大,皮肤内脂褐素类物质的量逐渐增多,从而使肤色暗黄现象愈发严重。
肤色暗黄与非酶糖基化衰老学说:非酶糖基化衰老学说(又称美拉德反应衰老学说),作为分子水平的又一个重要的衰老学说,是近年来衰老机制研究的重点。生物体内非酶糖基化反应是指在无酶催化的条件下,还原性糖的醛基或酮基与蛋白质等大分子中的游离氨基反应生成可逆或不可逆结合物-高级糖基化终末产物(Advanced glycation end-products,AGEs)的过程。Dyer等发现皮肤衰老与非酶糖基化有关,皮肤的真皮层中富含胶原蛋白和弹性蛋白,蛋白质分子中的氨基酸容易与细胞外液中葡萄糖的醛基或酮基发生非酶糖基化反应,且随着年龄的 增长,AGEs进行性增加,AGEs发生褐变后形成棕黄色的生物垃圾,堆积在皮肤的真皮层,令肌肤失去剔透感而泛黄、暗沉。此外,皮肤中AGEs增加,使胶原蛋白形成分子间交联,不但降低了皮肤的弹性和通透性,使养料及废物的扩散性能减弱,而且降低了胶原的可溶性使其难以被胶原酶水解,造成皮肤弹性下降,皱纹不易平复且不断加深,从而加快皮肤的衰老过程。
现代医学解决肤色暗黄、延缓衰老问题主要从以上两方面入手:①抑制非酶糖基化反应,消除羰基化合物对肌肤的危害;②清除自由基、避免脂质过氧化,减少羰基化合物的产生和肤色暗黄的形成。
目前市场上具有美白、抗衰老功效的保健品种类繁多、品质参差不齐,能够有效解决肤色暗黄、延缓衰老问题,且效果显著的保健品并不多见。
发明内容
本发明的目的在于提供一种具有美白、延缓衰老功效的护肤组合物及其应用、保健品。
为实现上述发明目的,本发明提供如下技术方案:
本发明提供的护肤组合物,包括浓缩香瓜粉、针叶樱桃粉和浓缩橄榄汁冻干粉。
作为优选,以重量份计,所述护肤组合物包括如下组分:
浓缩香瓜粉10-50份、针叶樱桃粉10-40份和浓缩橄榄汁冻干粉1-15份。
作为优选,所述组合物还包括库拉索芦荟凝胶、葡萄籽提取物和番茄红素。
作为优选,以重量份计,所述护肤组合物包括如下组分:
浓缩香瓜粉10-50份、针叶樱桃粉10-40份、浓缩橄榄汁冻干粉1-15份、库拉索芦荟凝胶1-10份、葡萄籽提取物1-5份和番茄红素0.1-1份。
本发明选用浓缩香瓜粉、针叶樱桃粉和浓缩橄榄汁冻干粉这三种天然药食两用植物提取物组成的组合物在美白、延缓衰老方面表现出协同 增效作用,能够有效地抑制酪氨酸形成、清除自由基、改善皮肤光损伤,表明本发明所述组合物美白、延缓衰老的效果显著。在上述几味药材的基础上,添加库拉索芦荟凝胶、葡萄籽提取物和番茄红素,能够更显著的增强美白、延缓衰老的作用。
香瓜又称甘瓜或甜瓜,葫芦科植物的果实肉质,具多室及多种子,和浆果很像。香瓜中抗氧化性物质含量极高,以SOD和维生素C为主,能起到清除体内自由基,缓解衰老,也有一定的抗紫外线的功效,降低色素的形成和沉淀,能起到很好的美容养颜功效。尤其是在阳光充足的季节,能够避免色素沉着,起到防晒、增白、抗皱之保护皮肤的作用。
橄榄(Canarium album(Lour.)Raeusch.)又名山榄,又称谏果,橄榄科橄榄属乔木植物。南京人称它为青果,岭南人称作橄榄,不论生啖或是煮汁,它都能生津止渴、治咽喉瘸、解鱼熬之毒和喉闻骨鲠。橄榄营养丰富,果肉内含蛋白质、碳水化合物、脂肪、维生素C以及钙、磷、铁等矿物质。用现代生物技术分析,橄榄中主要活性物质为多酚类化学成,研究证明橄榄多酚具有较强的自由基清除能力及较高的抗氧化活性,橄榄多酚的自由基清除能力高于人工合成抗氧化剂BHA和抗坏血酸。羟基酪醇(hydroxytyrosol),又名3,4-二羟基苯乙醇,是一种天然抗氧化剂,广泛存在于橄榄(olive)科橄榄属植物的枝叶及果实中,特别是地中海地区的橄榄树中含量较高,是橄榄油的有效成分。大量的研究表明羟基酪醇具有很强的抗氧化作用(Aeschbach et al.1994;Visioli et al.1998),可阻止多不饱和脂肪酸的自氧化(Tsinidou et al.1995)。羟基酪醇对自由基的清除能力比其他一些合成的和天然的抗氧剂的抗氧化能力都高,例如,它是维生素E抗氧化性的10倍、二丁基羟基甲苯(BHT)的1000多倍。Goya等研究发现羟基酪醇能够降低由叔丁基过氧化氢所引起HepG2细胞内的ROS水平和脂质过氧化水平增高,阻止了叔丁基过氧化氢所导致的谷胱甘肽下降。谷胱甘肽为细胞所分泌的内生性主要抗氧化物质,能直接中和自由基和活性氧分子。
针叶樱桃,金虎尾科(Malpighiaceae)金虎尾属(Malpighia)凹缘金虎尾(M.emarginata)的果实。主产于巴西,其维生素C、维生素P(芦 丁)、超氧化歧化酶(SOD)含量均雄冠世界所有水果,有“三王之果”之称。特别是维生素C,100克鲜果维生素C含量3500毫克,相当于苹果的500倍,柑橘的100倍,葡萄的600倍,梨的200倍,猕猴桃的12倍,被誉为维C之王。
库拉索芦荟凝胶,以库拉索芦荟叶片为原料,经沥醌清洗、去皮、漂烫、杀菌等步骤制成,芦荟凝胶冻干粉在滋润干燥肌肤、祛斑除痘、削除皱纹、恢复皮肤弹性,提高人体免疫力,清除自由基,缓解发炎和受损皮肤的疼痛等方面有着独特神奇的功效。
葡萄籽,葡萄籽是葡萄的种子,是葡萄酒和其他产品的下脚料,经晒干后分离葡萄皮、葡萄梗后所得产物,占整粒葡萄质量的4%~6%。葡萄籽含有丰富的氨基酸、维生素、矿物质和膳食纤维等多种营养物物质以及多种活性成分,如儿茶素类和原花青素类等多酚类物质,具有保健、美容之功效。
番茄红素,是类胡萝卜素的一种,主要存在于番茄、西瓜、葡萄柚和木瓜等食品中。番茄红素是从番茄中提取的天然生物抗氧化剂,有较独特的长链分子结构。研究表明番茄红素的抗氧化能力是维生素E的1 0 0倍。一个番茄红素分子可以清除数千个单线态氧。番茄红素是淬灭单线态氧和清除过氧化氢、自由基最强的类胡萝卜素,抑制、破坏单线态氧能力是胡萝卜素的2倍。因此番茄红素可以通过淬灭单线态氧预防脂类氧化,保护生物膜免受自由基的伤害,达到保护容颜,延缓衰老的作用。
在本发明提供的一些具体实施例中,以重量份计,所述护肤组合物包括如下组分:
浓缩香瓜粉30份、针叶樱桃粉20份、浓缩橄榄汁冻干粉15份、库拉索芦荟凝胶4份、葡萄籽提取物1份和番茄红素0.1份。
在本发明提供的一些具体实施例中,以重量份计,所述护肤组合物包括如下组分:
浓缩香瓜粉50份、针叶樱桃粉10份、浓缩橄榄汁冻干粉1份、库拉索芦荟凝胶4份、葡萄籽提取物1份和番茄红素0.1份。
在本发明提供的一些具体实施例中,以重量份计,所述护肤组合物 包括如下组分:
浓缩香瓜粉10份、针叶樱桃粉40份、浓缩橄榄汁冻干粉12份、库拉索芦荟凝胶4份、葡萄籽提取物1份和番茄红素0.1份。
在本发明提供的一些具体实施例中,以重量份计,所述护肤组合物包括如下组分:
在本发明提供的一些具体实施例中,以重量份计,所述护肤组合物包括如下组分:
浓缩香瓜粉50份、针叶樱桃粉10份、浓缩橄榄汁冻干粉1份。
本发明提供的护肤组合物中,浓缩香瓜粉、针叶樱桃粉、浓缩橄榄汁冻干粉、库拉索芦荟凝胶和葡萄籽提取物可以是冻干粉,也可以是浓缩物,所述浓缩物和所述冻干粉的功效量应与所述原提取物成分份量相等。
本发明还提供了所述护肤组合物在制备具有美白、抗衰老功效的药物或保健品中的应用。
本发明还提供了一种具有美白抗衰老作用的药物,包括所述护肤组合物和药学上可接受的辅料。
本发明还提供了一种具有美白、抗衰老作用的保健品,包括所述护肤组合物和保健品中可接受的辅料。
作为优选,所述保健品中可接受的辅料选自异麦芽酮糖醇、微晶纤维素、硬脂酸镁、麦芽糖醇、抗性糊精、甜菊糖苷、预胶化淀粉、二氧化硅中的一种或两种以上。
在本发明提供的一些具体实施例中,以重量份计,所述保健品中可接受的辅料为异麦芽酮糖醇20-40份、微晶纤维素20-40份、硬脂酸镁1-5份。
在本发明提供的一些具体实施例中,以重量份计,所述保健品中可接受的辅料为麦芽糖醇20-40份、抗性糊精20-40份、甜菊糖苷1-5份。
在本发明提供的一些具体实施例中,以重量份计,所述保健品中可接受的辅料为预胶化淀粉20-40份、硬脂酸镁0.5-2份、二氧化硅0.5-2份。
本发明中,保健食品的剂型为片剂、胶囊剂、丸剂、颗粒剂、粉剂剂、口服液剂。
作为优选,所述保健品为压片糖果。压片糖果是粉末、颗粒经制粒或干粉混合(无需制粒)直接压片而成的产品,主要类型有普通压片糖、包衣压片糖、多层压片糖、泡腾压片糖以及咀嚼型压片糖。包装时尚、方便的压片糖果以其产品口味丰富、具清新口气或保健功能等特点,成为近年来糖果市场发展最快的糖果品类之一。
实验结果表明,本发明选用浓缩香瓜粉、针叶樱桃粉和浓缩橄榄汁冻干粉这三种天然药食两用植物提取物组成的组合物在美白、延缓衰老方面表现出协同增效作用,能够有效地抑制酪氨酸形成、清除自由基、改善皮肤光损伤。在上述几味药材的基础上,添加库拉索芦荟凝胶、葡萄籽提取物和番茄红素后能够明显的增强美白、延缓衰老的作用。
具体实施方式
本发明公开了一种护肤组合物及其应用、保健品,本领域技术人员可以借鉴本文内容,适当改进工艺参数实现。特别需要指出的是,所有类似的替换和改动对本领域技术人员来说是显而易见的,它们都被视为包括在本发明。本发明的方法及应用已经通过较佳实施例进行了描述,相关人员明显能在不脱离本发明内容、精神和范围内对本文所述的方法和应用进行改动或适当变更与组合,来实现和应用本发明技术。
对所公开的实施例的说明,使本领域专业技术人员能够实现或使用本发明。对这些实施例的多种修改对本领域的专业技术人员来说将是显而易见的,本文中所定义的一般原理可以在不脱离本发明的精神或范围的情况下,在其它实施例中实现。因此,本发明将不会被限制于本文所示的这些实施例,而是要符合与本文所公开的原理和新颖特点相一致的最宽的范围。
下面结合实施例,进一步阐述本发明:
实施例1本发明护肤组合物
浓缩香瓜粉10份、针叶樱桃粉40份、浓缩橄榄汁冻干粉12份,混合,即得。
实施例2本发明护肤组合物
浓缩香瓜粉50份、针叶樱桃粉10份、浓缩橄榄汁冻干粉1份,混合即得。
实施例3本发明护肤组合物
浓缩香瓜粉30份、针叶樱桃粉20份、浓缩橄榄汁冻干粉15份,混合即得。
实施例4本发明护肤组合物
浓缩香瓜粉30份、针叶樱桃粉20份、浓缩橄榄汁冻干粉15份、库拉索芦荟凝胶4份、葡萄籽提取物1份、番茄红素0.1份,混合即得。
实施例5本发明护肤组合物
浓缩香瓜粉50份、针叶樱桃粉10份、浓缩橄榄汁冻干粉1份、库拉索芦荟凝胶4份、葡萄籽提取物1份和番茄红素0.1份,混合即得。
实施例6本发明护肤组合物
浓缩香瓜粉10份、针叶樱桃粉40份、浓缩橄榄汁冻干粉12份、库拉索芦荟凝胶4份、葡萄籽提取物1份和番茄红素0.1份,混合即得。
比较例1~6的护肤组合物
比较例1~6的护肤组合物,如表1所示。
表1比较例1~6的护肤组合物
Figure PCTCN2018113403-appb-000001
Figure PCTCN2018113403-appb-000002
实施例7体外试验
将实施例1~6和比较例1~6的组合物,加水稀释,得到终浓度为10mg/mL的样品液。
(1)抑制酪氨酸酶活性的测定:在各试管中分别加入磷酸盐缓冲液(PBS)和样品液、酪氨酸酶溶液,混合均匀,于恒温水浴(37℃)反应10min,分别迅速移入多巴溶液1mL,混匀,放回水浴中反应5min,当反应至5min时马上测各收拾样品在475nm处的吸光度,计算供试药液对酪氨酸酶的抑制率。
(2)DPPH自由基清除率的测定:精密移取DPPH自由基溶液、样品液和无水乙醇各2mL于同一试管中,混匀后避光静置20min,分别测定517nm处的吸光度,计算供试药液对DPPH的清除率。
结果如表2所示。
表2不同配方酪氨酸酶抑制率、DPPH清除率结果
组别 酪氨酸酶抑制率% DPPH清除率% 综合评分%
浓缩香瓜粉组 28.06 75.98 52.02
针叶樱桃粉组 25.1 71.23 48.17
浓缩橄榄汁冻干粉组 27.4 73.84 50.62
实施例1组 36.74 83.19 59.97
实施例2组 40.27 89.95 65.11
实施例3组 39.01 87.84 63.43
实施例4组 49.99 94.81 72.40
实施例5组 45.39 92.75 69.07
实施例6组 43.74 91.39 67.57
比较例1组 30.41 77.89 54.15
比较例2组 29.28 76.46 52.87
比较例3组 30.86 79.23 55.05
比较例4组 31.37 80.02 55.70
比较例5组 33.43 82.91 58.17
比较例6组 32.74 80.74 56.74
注:综合评分=酪氨酸酶抑制率×50%+DPPH清除率×50%。
根据表2数据可知,实施例1~6组对酪氨酸酶抑制率及DPPH清除率均明显优于单药各组和比较例1~6组,具有显著的美白作用。
实施例8本发明组合物对大鼠皮肤光损伤的防护作用
动物分组:取Wistar大鼠120只,5周龄,体重122.5±5.5g,雌雄各半,按清洁动物标准条件雌雄分笼喂养。随机分为15组,包括正常对照组、模型对照组、单药组和试验组,每组8只,按照表3所示的给药方式灌胃给药(0.83g/kg),连续给药4周,试验期间大鼠正常饮水,正常饲喂普通基础颗粒饲料。
表3分组与给药方式
Figure PCTCN2018113403-appb-000003
Figure PCTCN2018113403-appb-000004
实验方法:
动物脱毛+UVA照射:将大鼠用乙醚吸入法适度麻醉,以眼科剪刀剪短背部鼠毛至1mm,然后用电动剃须刀将剩余鼠毛剃净,脱毛区约5.0×4.5cm。照射前6h脱毛。
标本取材:照射后24h乙醚吸入法麻醉大鼠,以皮肤活检术取下背部脱毛区中央处皮肤,尽量去除皮下组织,生理盐水洗净后分别置入10%中性福尔马林和液氮中保存备用。标本取材后,常规10%福尔马林固定,石蜡包埋4μm连续切片,常规HE染色。
皮肤MDA含量、超氧化物歧化酶(SOD)活性、谷胱甘肽过氧化物酶(GSH-Px)活性的检测:末次UVA十UVB照射实验结束后,处死大鼠,取大鼠背部照射区部分皮肤,去除皮下脂肪称重,制成10%组织匀浆,以3000转/分钟的速度离心10分钟,取上清液进行各指标测定。
结果如表4所示。
表4丙二醛(MDA)含量及抗氧化酶活性测定(n=8,x±s)
Figure PCTCN2018113403-appb-000005
Figure PCTCN2018113403-appb-000006
注:与正常对照组比较: P<0.05, ▲▲P<0.01;与模型对照组比较:*P<0.05,**P<0.01
结果显示,与对照组比较,UVA+UVB照射可使大鼠皮肤组织匀浆中MDA含量显著增高,SOD活性和谷胱甘肽过氧化物酶(GSH-Px)活性均显著降低。与UVA+UVB照射组比较,UVA+UVB照射+实施例1~6组能够显著降低皮肤组织匀浆中MDA的含量(P<0.05),显著提高SOD活性和GSH-Px活性(P<0.05)。其中,实施例4的组合物对对紫外线防护效果最好。比较例1~6组的皮肤组织匀浆中MDA的含量、SOD活性和GSH-Px活性与模型组对比,未达显著差异,这表明,比较例组的组合物对对紫外线防护效果不明显。
实施例9美白抗衰功效测试试验
本实验使用荷兰DiagnOptics的AGE Reader(皮肤AGEs荧光光谱仪),通过无创法测定受试者皮肤自体荧光(skin autofluorescence,AF)参考值判断实施例1是否可以降低皮肤组织中AGEs含量。入选受试者 20人,女性,平均年龄28岁。受试期间口服实施例1的组合物,连续服用1个月。检测服用前后皮肤AGEs含量,结果如表5所示:
表5受试者服用前后肝功能变化比较(n=20,x±s)
  受试人数 AF值
服用前 20 1.8±0.3
服用后 20 1.5±0.2**
注:服用前后对比,**P<0.01
由表5结果可知,与服用前相比,受试者服用本发明实施例1的组合物后皮肤自体荧光值显著下降(P<0.01),表明本发明提供的组合物能够显著延缓皮肤衰老。
取实施例2~6所述的组合物进行美白抗衰功效测试试验,结果与实施例1相同或相近,无显著性差异(P>0.05)。
实施例10本发明护肤组合物片剂的制备
(1)称量、备料:称取实施例4所述组合物、异麦芽酮糖醇30份、微晶纤维素30份、硬脂酸镁3份,备用。
(2)混合:将上述除硬脂酸镁外的原料混合25min,然后加入硬脂酸镁再混合5min。
(3)压片:用压片机将上述混合料进行压片,0.5g/片,得到素片。
(4)包衣:称取配方量包衣剂,配置成适宜的固形物含量,在配桨锅中搅拌30~45分钟;搅拌完成后,对素片进行包衣,至片面基本成膜、颜色一致。
实施例11本发明护肤组合物粉剂的制备
(1)称量、称取实施例5所述组合物、麦芽糖醇30份、抗性糊精30份、甜菊糖苷3份,备用。
(2)混合:先将甜菊糖苷与抗性糊精混合10分钟,至颜色均匀后,再加入实施例5所述的组合物和麦芽糖醇,混合30分钟至完全均匀后出料。
(3)分装:按要求调整好设备,再将60mm空白铝箔膜准确安装于颗粒包装机上,待空机调试完毕后下料进行包装,至装量、外型符合要求才正式分装,净重量控制在每袋4克,每袋装量差异±4.5%,每10分钟检查一次装量差异,随时抽检外观和密封性。密封性用密封试验仪进行检测,真空度应小于或等于-60kpa,测试时间应该大于或等于3分钟。外袋上不得有粉粘结,不得有泄漏。
实施例12本发明护肤组合物硬胶囊的制备
(1)备料、混合:称取实施例6所述组合物、预胶化淀粉30份、硬脂酸镁1.5份、二氧化硅1.5份,备用。
(2)填充:混合好的物料在全自动填充剂上填充,装量0.5g/粒。
以上所述仅是本发明的优选实施方式,应当指出,对于本技术领域的普通技术人员来说,在不脱离本发明原理的前提下,还可以做出若干改进和润饰,这些改进和润饰也应视为本发明的保护范围。

Claims (10)

  1. 一种护肤组合物,其特征在于,包括浓缩香瓜粉、针叶樱桃粉和浓缩橄榄汁冻干粉。
  2. 根据权利要求1所述的护肤组合物,其特征在于,以重量份计,包括如下组分:
    浓缩香瓜粉10-50份、针叶樱桃粉10-40份和浓缩橄榄汁冻干粉1-15份。
  3. 根据权利要求1或2所述的护肤组合物,其特征在于,还包括库拉索芦荟凝胶、葡萄籽提取物和番茄红素。
  4. 根据权利要求3所述的护肤组合物,以重量份计,包括如下组分:
    浓缩香瓜粉10-50份、针叶樱桃粉10-40份、浓缩橄榄汁冻干粉1-15份、库拉索芦荟凝胶1-10份、葡萄籽提取物1-5份和番茄红素0.1-1份。
  5. 根据权利要求3或4所述的护肤组合物,其特征在于,所述浓缩香瓜粉、所述针叶樱桃粉、所述浓缩橄榄汁冻干粉、所述库拉索芦荟凝胶、所述葡萄籽提取物为冻干粉或浓缩物。
  6. 权利要求1~5任一项所述的护肤组合物在制备具有美白、抗衰老功效的药物或保健品中的应用。
  7. 一种具有美白抗衰老作用的药物,其特征在于,包括如权利要求1至5任一项所述的组合物和药学上可接受的辅料。
  8. 一种具有美白、抗衰老作用的保健品,其特征在于,包括如权利要求1至5任一项所述的组合物和保健品中可接受的辅料。
  9. 根据权利要求8所述的保健品,其特征在于,所述保健品中可接受的辅料选自异麦芽酮糖醇、微晶纤维素、硬脂酸镁、麦芽糖醇、抗性糊精、甜菊糖苷、预胶化淀粉、二氧化硅中的一种或两种以上。
  10. 根据权利要求8所述的保健品,其特征在于,其剂型为片剂、胶囊剂、丸剂、颗粒剂、粉剂剂、口服液剂。
PCT/CN2018/113403 2017-11-21 2018-11-01 一种护肤组合物及其应用、保健品 WO2019100923A1 (zh)

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CN113521136A (zh) * 2021-08-04 2021-10-22 上海楷达生物科技有限公司 一种有助于皮肤美白和除皱的组合物
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