WO2022142669A1 - Composition anti-âge de médecine traditionnelle chinoise, sa méthode de préparation, son utilisation à des fins non thérapeutiques et son utilisation dans la préparation d'un produit cosmétique - Google Patents

Composition anti-âge de médecine traditionnelle chinoise, sa méthode de préparation, son utilisation à des fins non thérapeutiques et son utilisation dans la préparation d'un produit cosmétique Download PDF

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WO2022142669A1
WO2022142669A1 PCT/CN2021/127252 CN2021127252W WO2022142669A1 WO 2022142669 A1 WO2022142669 A1 WO 2022142669A1 CN 2021127252 W CN2021127252 W CN 2021127252W WO 2022142669 A1 WO2022142669 A1 WO 2022142669A1
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extract
chinese medicine
traditional chinese
weight
medicine composition
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PCT/CN2021/127252
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English (en)
Chinese (zh)
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孙懿
陈默
赵亚
李玲玉
祝乐
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上海家化联合股份有限公司
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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)
    • A61K36/88Liliopsida (monocotyledons)
    • 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)
    • A61K36/23Apiaceae or Umbelliferae (Carrot family), e.g. dill, chervil, coriander or cumin
    • A61K36/232Angelica
    • 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)
    • A61K36/23Apiaceae or Umbelliferae (Carrot family), e.g. dill, chervil, coriander or cumin
    • A61K36/236Ligusticum (licorice-root)
    • 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)
    • A61K36/25Araliaceae (Ginseng family), e.g. ivy, aralia, schefflera or tetrapanax
    • A61K36/258Panax (ginseng)
    • 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)
    • A61K36/62Nymphaeaceae (Water-lily 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)
    • A61K36/70Polygonaceae (Buckwheat family), e.g. spineflower or dock
    • A61K36/704Polygonum, e.g. knotweed
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9794Liliopsida [monocotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/18Antioxidants, e.g. antiradicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/08Anti-ageing preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2236/00Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • A61K2236/30Extraction of the material
    • A61K2236/33Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
    • A61K2236/333Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using mixed solvents, e.g. 70% EtOH

Definitions

  • the invention relates to the field of natural medicinal chemistry and cosmetics, in particular to a traditional Chinese medicine composition with anti-aging effect, a preparation method and application of the traditional Chinese medicinal composition.
  • Non-enzymatic glycosylation of NEG is a series of complex non-enzymatic reactions in which reducing sugars are directly combined with protein residues to produce Schiff bases (Schiff), which are cleaved to glucosamine rearrangement (Amadori) products, followed by dehydration, cyclic It is further degraded into a series of reactive aldehyde and ketone compounds (reactive carbonyl compounds RCS).
  • RCS has higher activity than reducing sugars, and can quickly combine with free amino groups of proteins to eventually generate irreversible brown-yellow fluorescent substances, which are collectively referred to as advanced glycation end products (AGEs). ).
  • Human skin tissue contains a large amount of collagen and elastin. These two proteins are metabolized slowly and contain more lysine and hydroxylysine, which provide the material basis for NEG reaction. Skin proteins and reducing sugars generate NEG to form AGEs, which increase with age. With the progressive increase of AGEs, collagen forms intermolecular cross-links, which not only reduces the permeability of connective tissue, but also weakens the diffusion properties of nutrients and wastes, and increases tissue ductility and hardness; it reduces the solubility of collagen and is difficult to be absorbed by collagen Enzymatic hydrolysis results in decreased skin elasticity and wrinkles, which deepen with age.
  • Oxidation is a crucial step in the formation of AGEs.
  • the intermediate products formed by AEGs—active carbonyl groups are all derived from the oxidative degradation or auto-oxidation of Amadori products.
  • AGEs can directly reduce the activity of antioxidant enzymes in the body. Increase skin oxidative stress levels. Overall, oxidative stress can promote the NEG process, and AGEs can increase the level of oxidative stress.
  • many antioxidants have been confirmed to have anti-glycation activity, such as: ascorbic acid, tocopherol, sodium selenite, riboflavin, zinc, manganese, etc.
  • a mixture of green tea, vitamin C (VC), vitamin E (VE), acetylcysteine, and rutin can inhibit the non-enzymatic glycation of collagen in mouse skin.
  • AGEs are: carboxymethyl lysine (CML), carboxyethyl lysine (CEL), pentoside, glycosylated collagen, pyrrolidine and dilysyl imidazoline derivatives Wait. Most of them have fluorescence specificity (such as pentosides, glycosylated limbs), and some do not have fluorescent properties (such as CML, CEL). Therefore, the most typical evaluation of anti-glycation efficacy is to use biochemical reaction methods, that is, to use models such as bovine serum albumin-glucose (BSA-glucose) and bovine serum albumin-pyruvaldehyde (BSA-MGO) to evaluate by fluorescence spectrophotometry.
  • BSA-glucose bovine serum albumin-glucose
  • BSA-MGO bovine serum albumin-pyruvaldehyde
  • the present invention unexpectedly found that the traditional Chinese medicine composition comprising the extracts of saffron, ginseng, lotus, Polygonum cuspidatus, Chuanxiong and Angelica has excellent antioxidant and good anti-glycation effects.
  • the present invention provides an anti-aging traditional Chinese medicine composition, which comprises:
  • the saffron extract, ginseng extract, lotus flower extract, Polygonum cuspidatum extract, Chuanxiong extract, and Angelica extract are prepared by solvent ultrasonic extraction.
  • the weight ratio of the saffron extract, ginseng extract, lotus flower extract, Polygonum cuspidatum extract, Chuanxiong extract, and angelica extract is 0.1-0.5:1-3:1-2: 0.5-2:1-2:1-2. In a more preferred embodiment, the weight ratio of the saffron extract, ginseng extract, lotus extract, Polygonum cuspidatum extract, Chuanxiong extract, and Angelica extract is 0.1:3:2:2:1:1 .
  • the extract of the present invention is extracted with ethanol, preferably 70% ethanol by volume.
  • the present invention also relates to the application of a traditional Chinese medicine composition comprising saffron extract, ginseng extract, lotus extract, polygonum extract, chuanxiong extract, and angelica extract for non-therapeutic purposes against skin aging.
  • a traditional Chinese medicine composition comprising saffron extract, ginseng extract, lotus extract, polygonum extract, chuanxiong extract, and angelica extract for non-therapeutic purposes against skin aging.
  • the anti-aging of the skin is achieved by anti-oxidation and/or anti-glycosylation.
  • the present invention also relates to the application of a traditional Chinese medicine composition comprising saffron extract, ginseng extract, lotus extract, polygonum extract, chuanxiong extract, and angelica extract in the preparation of cosmetics for anti-aging skin .
  • the anti-aging of the skin is achieved by anti-oxidation and/or anti-glycosylation.
  • the present invention also relates to a preparation method of a traditional Chinese medicine composition comprising saffron extract, ginseng extract, lotus flower extract, Polygonum cuspidatum extract, Chuanxiong extract, and Angelica sinensis extract, the method comprising:
  • the saffron extract, ginseng extract, lotus flower extract, Polygonum cuspidatum extract, Chuanxiong extract and Angelica sinensis extract were prepared by solvent ultrasonic extraction method;
  • the saffron extract, the ginseng extract, the lotus flower extract, the Polygonum cuspidatum extract, the Chuanxiong extract and the angelica extract were combined according to parts by weight.
  • the present invention provides an external preparation for skin comprising a traditional Chinese medicine composition of saffron extract, ginseng extract, lotus flower extract, Polygonum cuspidatum extract, Chuanxiong extract and Angelica sinensis extract.
  • the external preparation for skin comprises 0.01-5% by weight of the traditional Chinese medicine composition.
  • Figure 1 shows the results of the relative expression levels of advanced glycation end products (AGEs).
  • BC represents blank control
  • NC represents negative control
  • PC represents positive control.
  • Figure 2 shows the results of immunohistochemical detection.
  • the microscope used was OLMPUS BX53, and the magnifications were 20x objective ⁇ 10x eyepiece and 40x objective ⁇ 10x eyepiece.
  • the picture of expression analysis is the picture of 40x objective lens ⁇ 10x eyepiece.
  • anti-aging includes alleviating, reducing, preventing, improving or eliminating the presence of, for example, fine lines and wrinkles, loss of elasticity, skin unevenness, red scars and age spots.
  • wrinkles include fine lines, micro wrinkles, or coarse wrinkles.
  • wrinkles include, but are not limited to, fine lines around the eyes (eg, "crow's feet"), forehead and cheek wrinkles, brow lines, and laugh lines around the mouth.
  • loss of elasticity includes loss of elasticity or structural integrity of skin or tissue, including but not limited to sagging, sagging, and loose tissue. Loss of elasticity or tissue structural integrity can be caused by a variety of factors including, but not limited to, disease, aging, hormonal changes, mechanical trauma, environmental damage, or as a result of the application of products such as cosmetic or pharmaceuticals to the tissue.
  • skin unevenness refers to a skin condition associated with diffuse or mottled hyperpigmentation, which may be classified as hyperpigmentation, such as post-inflammatory hyperpigmentation.
  • red scar refers to a skin condition associated with redness or erythema.
  • age spots refers to skin conditions associated with discontinuous pigmentation, such as small areas of darker pigmentation that can develop on the face and hands.
  • cosmetic refers to a cosmetic substance or article that maintains, restores, imparts, stimulates, or enhances the appearance of the body, or appears to enhance beauty or rejuvenation, particularly as it relates to the appearance of tissue or skin.
  • a “cosmetically effective amount” refers to an amount of a physiologically active compound or composition sufficient to treat one or more signs of skin aging, but sufficiently low to avoid serious side effects.
  • the cosmetically effective amount of a compound or composition will vary with the specific condition being treated, the age and physical condition of the end user, the severity of the condition being treated/prevented, the duration of the treatment, the nature of the other treatment, The particular compound or product/composition employed, the particular cosmetically acceptable carrier employed, and the like.
  • the anti-aging traditional Chinese medicine composition of the present invention comprises saffron extract.
  • Saffron the stigma of Crocus sativus L. of the Iridaceae family. Aliases are saffron, saffron and so on. Sexual sweet, flat. Heart, liver meridian. It has the effect of promoting blood circulation and removing blood stasis, dispersing depression and opening knots. Modern research shows that saffron has antioxidant, anticoagulant and immune regulation effects.
  • saffron extract Although the application of saffron extract is disclosed in the prior art, the efficacy of saffron extract is not disclosed, and the efficacy and application of the compound extract containing saffron in the present invention are not disclosed.
  • CN110812299A discloses a toner containing saffron and its preparation process.
  • CN106821932A discloses a cosmetic containing saffron extract, which does not disclose the efficacy of saffron extract.
  • CN110279640A discloses that saffron extract has a whitening effect.
  • the traditional Chinese medicine composition of the present invention comprises 1-10 parts by weight, preferably 1-2 parts by weight of saffron extract.
  • the anti-aging traditional Chinese medicine composition of the present invention comprises ginseng extract.
  • Ginseng the root of Panax ginseng C.A.Mey. Also known as yellow ginseng, jade essence, blood ginseng, baby ginseng and so on. Sweet, lukewarm. Returns the lung, spleen, heart and kidney meridians. It has the effect of invigorating vitality and rejuvenating the mind. It has been reported in the literature that the main components of ginseng and its preparations are ginsenosides, which have significant promoting effects in improving learning ability and facilitation of memory, and can also inhibit Staphylococcus aureus and improve autoimmunity. Not only that, ginseng also has antioxidant, anti-aging and anti-inflammatory effects.
  • CN110787075A is a skin care oil composition containing ginseng root extract and ginseng seed oil, wherein the efficacy of ginseng root or ginseng seed oil is not disclosed.
  • the traditional Chinese medicine composition of the present invention comprises 15-40 parts by weight, preferably 15-35 parts by weight of ginseng extract.
  • the anti-aging traditional Chinese medicine composition of the present invention comprises lotus flower extract.
  • the lotus is the bud of Nelumbo nucifera Gaertn. Also known as hanli, hibiscus, hibiscus. Bitter, sweet, flat. Return to the liver and stomach meridians. Lotus can disperse blood stasis and stop bleeding, dispel dampness and eliminate wind.
  • the lotus is rich in flavonoids, which are good antioxidants and bacteriostatic agents. The lotus flavonoids can clear superoxide anion free radicals and hydroxyl free radicals.
  • lotus actives are disclosed in the prior art, lotus, especially the efficacy of lotus/lotus extract, and the efficacy and application of the compound extract containing lotus/lotus in the present invention are not disclosed.
  • lotus especially the efficacy of lotus/lotus extract, and the efficacy and application of the compound extract containing lotus/lotus in the present invention are not disclosed.
  • CN105534815B discloses a skin care composition containing lotus active ingredients, but the specific efficacy of the lotus active ingredients is not disclosed.
  • the traditional Chinese medicine composition of the present invention comprises 15-35 parts by weight, preferably 20-30 parts by weight of lotus flower extract.
  • the anti-aging traditional Chinese medicine composition of the present invention comprises Polygonum cuspidatum extract.
  • Polygonum cuspidatum is the rhizome and root of Liaoke Polygonum cuspidatum Sieb.Et Zucc. Also known as spot stick, bitter stick, acid stick, etc. Sexually bitter, slightly cold. Returns liver, gallbladder, lung meridian. Polygonum cuspidatum has the effect of promoting blood circulation and removing blood stasis, clearing away heat and detoxifying. Modern pharmacology shows that Polygonum cuspidatum contains resveratrol glycosides, which can effectively inhibit lipid peroxidation caused by free radical generating system, and also have antibacterial and antiviral effects.
  • CN111870572A discloses the antioxidant effect of Polygonum cuspidatum extract and its application.
  • the traditional Chinese medicine composition of the present invention comprises 15-30 parts by weight, preferably 15-25 parts by weight of Polygonum cuspidatum extract.
  • the anti-aging traditional Chinese medicine composition of the present invention comprises Chuanxiong extract.
  • Chuanxiong the rhizome of Ligusticum chuanxiong Hort. also known as xiong fragrant fruit, husk Jingxiong et al. Sexual pungent, warm. Return liver, gallbladder, pericardium meridian.
  • Chuanxiong mainly has the functions of promoting blood circulation and removing blood stasis, promoting qi and relieving stagnation, dispelling wind and relieving pain.
  • the main ingredient is ligustrazine, which has the functions of anti-oxidation, anti-inflammatory, promoting blood microcirculation and improving immunity.
  • the traditional Chinese medicine composition of the present invention comprises 10-25 parts by weight, preferably 10-15 parts by weight of the Chuanxiong extract.
  • the anti-aging traditional Chinese medicine composition of the present invention comprises angelica extract.
  • Angelica sinensis the root of Angelica sinensis (Oliv.) Diels of Umbelliferae. Alias Gangui, Mawei Angelica, Yungui, etc. Sweet, acrid, bitter, warm in nature. Returns liver, heart and spleen meridians. Has the effect of invigorating blood and nourishing blood. Angelica mainly contains volatile oils, organic acids, etc., which can play an antioxidant and anti-inflammatory role.
  • the traditional Chinese medicine composition of the present invention comprises 10-25 parts by weight, preferably 10-15 parts by weight of Angelica sinensis extract.
  • This application is the first time to combine saffron extract, ginseng extract, lotus flower extract, Polygonum cuspidatum extract, Chuanxiong extract and angelica extract, and the various herbs in the obtained compound traditional Chinese medicine composition complement each other to achieve anti-aging , Improve the efficacy of the skin.
  • the traditional Chinese medicine composition of the present invention is suitable for the field of cosmetics.
  • the present inventors have unexpectedly found that the traditional Chinese medicine composition comprising saffron extract, ginseng extract, lotus flower extract, Polygonum cuspidatum extract, Chuanxiong extract and Angelica sinensis extract has anti-oxidative and/or anti-glycosylation effects. Therefore, the traditional Chinese medicine composition of the present invention can be used as a functional additive in cosmetics to assist in improving skin aging, oxidation, wrinkles and the like.
  • the weight ratio of saffron extract, ginseng extract, lotus flower extract, Polygonum cuspidatum extract, Chuanxiong extract and Angelica extract in the traditional Chinese medicine composition of the present invention is 0.1-0.5:1-3 :1-2:0.5-2:1-2:1-2.
  • the weight ratio of saffron extract, ginseng extract, lotus flower extract, polygonum extract, chuanxiong extract and angelica extract is 0.1:3:2:2:1:1.
  • the traditional Chinese medicine extract of the present invention is prepared by a solvent ultrasonic extraction method.
  • ethanol can be used as the extraction solvent.
  • 70% by volume ethanol can be used for extraction.
  • the extraction process can be performed in steps. For example, in the first step, 95 vol% ethanol is used for ultrasonic extraction, centrifugal filtration, and the filtrate is discarded; in the second step, 70 vol% ethanol is used for ultrasonic extraction, centrifugal filtration, and the filtrate is concentrated, and the desired extract is obtained after filtration.
  • the extraction step is carried out for a maximum of 24 hours, but can be shorter. For example, the extraction process can be performed for 30 minutes to 1 hour.
  • the present invention also relates to a skin external preparation, which comprises a traditional Chinese medicine composition of saffron extract, ginseng extract, lotus extract, polygonum extract, chuanxiong extract and angelica extract, as well as cosmetics, dermatology or pharmaceutically acceptable excipients.
  • the dosage of the traditional Chinese medicine composition of saffron extract, ginseng extract, lotus flower extract, Polygonum cuspidatum extract, Chuanxiong extract and Angelica extract 0.001-20% (w/w), preferably 0.008-10% (w/w), more preferably 0.01-5% (w/w), most preferably 0.01-2% (w/w).
  • the skin external preparation composition is a general concept of all ingredients generally used on the outside of the skin, and may be, for example, a cosmetic composition or a pharmaceutical composition.
  • the cosmetic composition can be basic cosmetic, facial cosmetic, body cosmetic, hair care cosmetic, etc. There is no special restriction on the dosage form thereof, and can be reasonably selected according to different purposes.
  • This external preparation for skin can be formulated into any suitable product form.
  • product forms include, but are not limited to, aerosol sprays, creams, lotions, solids, liquids, dispersions, foams, gels, lotions, mousses, ointments, powders, patches, pomades, solutions , hand pump sprays, sticks, masks and wipes.
  • topical preparations for skin can be conveniently used for the preparation or topical application as cosmetic, dermatological or pharmaceutical products by various methods well known in the art.
  • the skin external preparation composition of the present invention may include one or more of the following ingredients: antiallergic agent, antimicrobial agent, antioxidant, chelating agent, colorant depigmenting agent, emollient, emulsifier, epidermal exfoliating agent, Films, fragrances, humectants, insect repellents, lubricants, pharmaceutically active agents, moisturizing agents, lightfasteners, preservatives, skin care agents, skin penetration enhancers, sunscreens, stabilizers, surfactants, thickening agents agents, viscosity modifiers, vitamins, or any combination thereof.
  • Cosmetic, dermatologically or pharmaceutically acceptable excipients that can be used in the skin external preparation composition of the present invention are water phase, oil phase, gel, wax-in-water emulsion, oil-in-water emulsion, or water-in-oil in the form of an emulsion.
  • the aqueous phase is a mixture of one or more water-soluble or dispersible components, which may be liquid, semi-solid or solid at room temperature (25°C).
  • Excipients include or may be in the form of suspensions, dispersions or solutions in aqueous or hydro-alcoholic vehicles, which may contain thickening or gelling agents. Those skilled in the art can select the appropriate product form and the components contained therein based on the knowledge possessed by those skilled in the art.
  • the composition may include an aqueous phase, which may contain water or a mixture of water and at least one hydrophilic organic solvent, such as an alcohol, especially containing 2-5 carbon atoms linear or branched lower monohydric alcohols such as ethanol or propanol; polyols such as propylene glycol, sorbitol, glycerol, panthenol or polyethylene glycol and mixtures thereof.
  • an aqueous phase which may contain water or a mixture of water and at least one hydrophilic organic solvent, such as an alcohol, especially containing 2-5 carbon atoms linear or branched lower monohydric alcohols such as ethanol or propanol; polyols such as propylene glycol, sorbitol, glycerol, panthenol or polyethylene glycol and mixtures thereof.
  • the composition may also optionally contain a surfactant.
  • the composition may also comprise film-forming polymers such as polyurethane, polyacrylic homo- or copolymers, polyesters, hydrocarbon-based resins and/or silicone resins.
  • film-forming polymers such as polyurethane, polyacrylic homo- or copolymers, polyesters, hydrocarbon-based resins and/or silicone resins.
  • the polymer can be dissolved or dispersed in a cosmetically acceptable vehicle and optionally combined with a plasticizer.
  • compositions of the present invention may also comprise an oil phase containing oil-soluble or oil-dispersible components that are liquid at room temperature (25°C) and/or oily or waxy substances at room temperature, such as Waxes, semisolids, gums and mixtures thereof.
  • the oil phase may also contain organic solvents.
  • suitable oily substances include: hydrocarbon-based oils of animal origin, such as perhydrosqualene; hydrocarbon-based vegetable oils, such as liquid triglycerides of C4-10 fatty acids, such as heptanoic acid or caprylic triglycerides, or oils such as sunflower oil, corn oil, soybean oil, grapeseed oil, castor oil, avocado oil, caprylic/capric triglycerides, jojoba oil; Chain or branched hydrocarbons, such as liquid paraffin and its derivatives, petrolatum; synthetic esters and ethers, especially esters of fatty alcohols, such as isopropyl myristate, 2-ethylhexyl palmitate, hard 2-Octyldodecyl fatty acid, isostearyl isostearate; hydroxylated esters such as isostearyl lactate, octyl hydroxystearate, octyl hydroxystearate, hydroxystea
  • composition of the present invention may further contain any components commonly used in the cosmetic field. These components include preservatives, aqueous phase thickeners (extract biopolymers, synthetic polymers) and fatty phase thickeners, fragrances, hydrophilic and lipophilic actives, and mixtures thereof.
  • compositions of the present invention may also contain additional particulate phases, which may be pigments and/or pearlescent agents and/or fillers used in cosmetic compositions.
  • Pigments may be present in the composition, suitable inorganic pigments include titanium oxide, zirconium oxide and cerium oxide and zinc oxide, iron oxide and iron blue; suitable organic pigments include barium, strontium, calcium and aluminum lakes and carbon black.
  • Pearlescent agents may be present in the composition, suitable pearlescent agents include mica coated with titanium oxide, iron oxide or natural pigments.
  • Fillers may be present in the composition, suitable fillers include talc, silicon dioxide, zinc stearate, mica, kaolin, nylon powder, polyethylene powder, Teflon, starch, boron nitride, copolymers Microspheres, such as silicone resin microbeads.
  • the oily phase of the compositions of the present invention may comprise one or more waxes, gums or mixtures thereof.
  • Waxes include hydrocarbon-based waxes, fluorowaxes, and/or silicone waxes, and can be derived from vegetable, mineral, animal, and/or synthetic sources. Suitable waxes include beeswax, carnauba wax, candelilla wax, paraffin wax, microcrystalline wax, ozokerite; synthetic waxes include polyethylene waxes, silicone waxes containing C16-45.
  • the gums are typically polydimethylsiloxane or sodium carboxymethylcellulose or extracts, and the semi-solid materials are typically hydrocarbon-based compounds such as lanolin and its derivatives.
  • compositions of the present invention may be formulated into any suitable product form.
  • product forms include, but are not limited to, aerosol sprays, creams, lotions, solids, liquids, dispersions, foams, gels, lotions, mousses, ointments, powders, patches, pomades, solutions , hand pump sprays, sticks, masks and wipes.
  • the compositions of the present invention can be conveniently used in the preparation or topical application of products as cosmetic, dermatological or pharmaceutical products by various methods well known in the art.
  • the skin external preparation composition of the present invention may include one or more of the following ingredients: antiallergic agent, antimicrobial agent, antioxidant, chelating agent, colorant depigmenting agent, emollient, emulsifier, epidermal exfoliating agent, Films, fragrances, humectants, insect repellents, lubricants, pharmaceutically active agents, moisturizing agents, lightfasteners, preservatives, skin care agents, skin penetration enhancers, sunscreens, stabilizers, surfactants, thickening agents agents, viscosity modifiers, vitamins, or any combination thereof.
  • Embodiment 7 the preparation of traditional Chinese medicine composition
  • the mass ratio of the extract of Example 1 the extract of Example 2: the extract of Example 3: the extract of Example 4: the extract of Example 5: the extract of Example 6 (0.1:3:2:2:1:1 ) mixed to prepare a traditional Chinese medicine composition, and finally prepared into a 1% solid content solution for later use.
  • Embodiment 8 the preparation of Chinese medicine composition
  • the mass ratio of the extract of Example 1 the extract of Example 2: the extract of Example 3: the extract of Example 5: the extract of Example 6 (0.1:3:2:1:1) was mixed to prepare a traditional Chinese medicine composition, and finally It was prepared into a 1% solid solution for later use.
  • Embodiment 9 the preparation of Chinese medicine composition
  • the mass ratio of the extract of Example 1 the extract of Example 3: the extract of Example 5: the extract of Example 6 (0.1:2:1:1) was mixed to prepare a traditional Chinese medicine composition, and finally formulated into a 1% solid content solution, spare.
  • the mass ratio of the extract of Example 1 the extract of Example 2: the extract of Example 3: the extract of Example 4: the extract of Example 5: the extract of Example 6 (0.5:1:2:1:1:1 ) mixed to prepare a traditional Chinese medicine composition, and finally prepared into a 1% solid content solution for later use.
  • the mass ratio of the extract of Example 1 the extract of Example 2: the extract of Example 3: the extract of Example 4: the extract of Example 5: the extract of Example 6 (0.2:1:1:0.5:1:1 ) mixed to prepare a traditional Chinese medicine composition, and finally prepared into a 1% solid content solution for later use.
  • the mass ratio of the extract of Example 1 the extract of Example 2: the extract of Example 3: the extract of Example 4: the extract of Example 5: the extract of Example 6 (0.1:2:1:0.5:1:1 ) mixed to prepare a traditional Chinese medicine composition, and finally prepared into a 1% solid content solution for later use.
  • DPPH diphenylpicroyl free radical
  • ethanol solution is dark purple and has strong absorption near 517nm.
  • free radical scavengers the light absorption of DPPH is weakened due to its single electron pairing.
  • the fading degree of DPPH ethanol solution has a quantitative relationship with the number of electrons it accepts, which can evaluate the ability of antioxidants to scavenge free radicals or the magnitude of antioxidant activity. The greater the inhibition rate, the better the antioxidant effect.
  • Example 1-12 Take the prepared extract of Example 1-12 and prepare it with distilled water to make 2ml each of 12.5ug/ml, 62.5ug/ml and 312.5ug/ml, and carry out the test according to the following method. After 40min reaction at room temperature, absorbance is measured at 517nm value. Among them, DPPH was purchased from Sigma Company (sigma), and the active substance concentration was 60ug/ml.
  • T is the sample
  • T0 is the sample control
  • C is the blank
  • C0 is the blank control
  • Example 10 extract Two traditional Chinese medicines were removed from the extract of Example 9, and one traditional Chinese medicine was removed from the extract of Example 8, but the antioxidant effect of the extract of Example 9 was better than that of the extract of Example 8. It was speculated that the extract of Example 2 was The fresh ginseng extract has no significant antioxidant activity, and the proportion of the extract in Example 8 is relatively large. When the six drugs are compounded, they have a synergistic effect.
  • Tissue processing The skin tissue (from the leg of a 45-year-old male; purchased from Guangdong Boxi Biotechnology Co., Ltd.) was frozen in a liquid nitrogen tank, then taken out and thawed in hot water at 37°C, and then placed in a liquid nitrogen tank. Quick-freeze in liquid nitrogen, repeat 5 times. The skin was taken, placed in a 24-well plate, washed three times with PBS buffer containing double antibodies (purchased from Boster), and then the tissue was soaked in 75% ethanol for 5 minutes, and then washed three times with PBS buffer containing double antibodies , and finally placed in PBS buffer containing double antibody for 24h.
  • PBS buffer containing double antibodies purchased from Boster
  • UVA irradiated tissues In order to accelerate the saccharification reaction, 1 ml/well of PBS buffer was added to the 24-well plate. Except for the blank control group, other tissues in the incubation system were irradiated 7 days before the saccharification reaction, and the dose was 10J/well. cm 2 of UVA irradiation (UVA irradiator, the average intensity of UVA irradiator irradiation is 13.38mw/s, and the irradiation time of 10J/cm2 is 12min 27s), after the irradiation, the 24 wells were sealed with parafilm. The plate was sealed and placed in a 45°C oven for 72 h, and the reaction was repeated once after 72 h.
  • the blank control (BC) is PBS buffer solution containing double antibody
  • the negative control group (NC) is PBS buffer solution containing double antibody + 0.5mM methylglyoxal
  • the positive control group (PC) is PBS buffer containing double antibody Solution + 0.5mM methylglyoxal + 3mM aminoguanidine sulfate
  • experimental group (S) is PBS buffer solution + 0.5mM methylglyoxal + carnosine/Extract 7 containing double antibody.
  • the experimental group (S) was divided into S1 group and S2 group.
  • S1 is equivalent to an external source control product (currently generally recognized by consumers)
  • group S2 is the extract of the present invention.
  • the BC group was replaced with PBS buffer solution containing double antibodies;
  • the NC group was replaced with PBS buffer solution containing 0.5Mm methylglyoxal and double antibodies;
  • the PC group was replaced with 0.5Mm methylglyoxal and 3mM aminoguanidine PBS buffer solution of sulfate and double antibody;
  • group S was replaced with PBS buffer solution containing 0.5Mm methylglyoxal, 0.625% carnosine/Extract 7 and double antibody, each group set 3 parallels, when the sample was collected Tissues were fixed with 4% formaldehyde followed by immunohistochemistry.
  • the primary antibody kit in immunohistochemical detection was Anti-Carboxymethyl Lysine antibody [NF-1G], purchased from abcam.
  • the secondary antibody kit was VECTASTAIN ABC Kit (mouse IgG), purchased from Vector Laboratories.
  • Dewaxing of baked slices The paraffin slices were placed in a baking machine at 70°C, and baked for 4 hours.
  • Dewaxing and hydration Immerse the sections in xylene for 10 min, replace the xylene and repeat once, and then soak in absolute ethanol, 95% ethanol, and 75% ethanol for 5 min. Washed with PBS buffer 3 times, 5 min each time.
  • Antigen retrieval put the paraffin sections into 0.01M sodium citrate antigen retrieval solution, use high pressure to repair, take out after cooling, wash 3 times with PBS buffer, 5min each time.
  • Block peroxidase add 1 drop of 3% hydrogen peroxide to each section, incubate at room temperature for 30 min to block the activity of endogenous peroxidase, wash with PBS buffer three times, 5 min each time.
  • Serum blocking dropwise add serum homologous to the secondary antibody for blocking at 37°C for 1 h.
  • Primary antibody incubation add primary antibody working solution dropwise, incubate at 4°C overnight, and wash with PBS buffer three times for 5 min each time.
  • Secondary antibody incubation Add the secondary antibody working solution dropwise, incubate at 4°C for 1 h, and wash with PBS buffer for 3 times, 5 min each time.
  • ABC complex incubation dropwise add ABC complex solution, incubate at room temperature for 30 min, and wash with PBS buffer three times, 5 min each time.
  • DAB staining add 1 drop of freshly prepared DAB solution to each section and observe under microscope for 5-30s.
  • Dehydration Dehydrate the slices with 75% ethanol, 95% ethanol, absolute ethanol, and anhydrous ethanol in sequence for 5 minutes, then soak the slices in xylene for 10 minutes, replace the xylene, repeat once, dry, mount with neutral resin, and dry. dry, watch.
  • the relative expression of AGEs in the isolated skin the expression of AGEs in the isolated skin/the average expression of AGEs in the isolated skin of the control group
  • S1 is 0.625% carnosine
  • S2 is 0.625% Example 7 extract.
  • the extracts of Example 7 and Examples 9-12 were used in the preparation of external preparations for skin.
  • the external preparation for skin is preferably a cosmetic composition, such as lotion, essence, cream and the like.
  • the weight percentage of the composite extract in the external preparation for skin is 0.0001%-20% (w/w).
  • the preferred weight percent is 0.001% to 10% (w/w).
  • a more preferred weight percentage is 0.001%-5% (w/w).
  • the most preferred weight percent is 0.01%-5% (w/w).

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Abstract

Sont divulgués une composition anti-âge de médecine traditionnelle chinoise, un agent d'utilisation externe associé, sa méthode de préparation, son utilisation contre le vieillissement de la peau à des fins non thérapeutiques, et son utilisation dans la préparation d'un produit cosmétique contre le vieillissement de la peau. La composition comprend : de 1 à 10 parties en poids d'un extrait de safran, de 15 à 40 parties en poids d'un extrait de ginseng, de 15 à 35 parties en poids d'un extrait de lotus, de 15 à 30 parties en poids d'un extrait de rhizome de renouée de Sakhaline, de 10 à 25 parties en poids d'un extrait de rhizome de racine de livèche, et de 10 à 25 parties en poids d'un extrait de racine d'Angelica sylvestris chinensis. L'extrait de safran, l'extrait de ginseng, l'extrait de lotus, l'extrait de rhizome de renouée de Sakhaline, l'extrait de rhizome de racine de livèche, et l'extrait de racine d'Angelica sylvestris chinensis sont préparés en utilisant une méthode d'extraction par solvant et ultrasons.
PCT/CN2021/127252 2020-12-29 2021-10-29 Composition anti-âge de médecine traditionnelle chinoise, sa méthode de préparation, son utilisation à des fins non thérapeutiques et son utilisation dans la préparation d'un produit cosmétique WO2022142669A1 (fr)

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