Composition and application thereof

Abstract

The invention discloses a composition and application thereof, and the composition comprises synephrine or a pharmaceutically acceptable salt thereof, and further comprises naringin, neohesperidin and / or hesperidin. The composition prepared by compounding the synephrine or the pharmaceutically acceptable salt thereof with the naringin, the neohesperidin and / or the hesperidin has the effects of relieving, repairing, resisting wrinkles, easing pain, relieving itching or resisting allergy when being used as a functional component of a skin care product; when being used as a functional component of a scalp care product, the shampoo has the effects of removing dandruff, removing oil, relieving itching or preventing alopecia.

Description

Technical Field

[0001] The present invention relates to the technical field of chemical engineering, and in particular to a composition and application thereof. Background Art

[0002] Synephrine, CAS: 94-07-5, molecular formula C9H 13 NO2, also known as synephrine, hydroxyephrine, sinephrine, sympathol, and deoxyepinephrine. Synephrine, when salted, is readily soluble in water, poorly soluble in ethanol, and virtually insoluble in chloroform and ether. Reported uses of synephrine include: acting as a natural stimulant, increasing blood pressure, resisting shock, enhancing metabolism, increasing calorie expenditure, improving performance, promoting weight loss, and dilating the trachea and bronchi.

[0003] Hesperidin, CAS: 520-26-3, molecular formula: C 28 H 34 O 15 The reported effects of hesperidin include maintaining osmotic pressure, enhancing capillary toughness, shortening bleeding time, lowering cholesterol, and anti-oxidation.

[0004] Neohesperidin (CAS: 13241-33-3, molecular formula: C28H34O15). The reported effects of neohesperidin include antioxidant, anti-allergic, and improving skin microcirculation.

[0005] Naringin, CAS: 10236-47-2, molecular formula: C 27 H 32 O 14 The reported effects of naringin include antioxidant, anti-inflammatory, lipid-lowering, blood sugar-lowering, and anti-cancer. Summary of the Invention

[0006] In view of the deficiencies in the prior art, the present invention aims to provide a composition and use thereof.

[0007] The purpose of the present invention is achieved through the following technical solutions:

[0008] In a first aspect, the present invention provides a composition comprising synephrine or a pharmaceutically acceptable salt thereof, and further comprising naringin, neohesperidin and / or hesperidin.

[0009] Preferably, the ratio of the weight of synephrine or its pharmaceutically acceptable salt to the total weight of naringin, neohesperidin and / or hesperidin is (1:30) to (15:1).

[0010] Preferably, the composition comprises the following components in parts by weight:

[0011] 1.0-2.0 parts of synephrine or a pharmaceutically acceptable salt thereof;

[0012] 0.1-2.0 parts of naringin;

[0013] Neohesperidin and / or hesperidin 0.1-2.0 parts.

[0014] Preferably, the weight ratio of naringin to neohesperidin and / or hesperidin is (10:1) to (1:10).

[0015] In a second aspect, the present invention provides a use of the aforementioned composition in preparing a skin care product with soothing, repairing, anti-wrinkle, analgesic, antipruritic or anti-allergic effects.

[0016] In a third aspect, the present invention provides a use of the aforementioned composition in preparing a scalp care product having anti-dandruff, degreasing, anti-itching or anti-hair loss effects.

[0017] In a fourth aspect, the present invention provides a use of a citrus fruit extract in preparing a skin care product with soothing, repairing, anti-wrinkle, analgesic, antipruritic or anti-allergic effects, wherein the citrus fruit extract comprises the aforementioned composition;

[0018] Wherein, the mass ratio of total flavonoids to total alkaloids in the citrus fruit extract is (1:30) to (15:1).

[0019] In a fifth aspect, the present invention provides a use of a citrus fruit extract in preparing a scalp care product having anti-dandruff, degreasing, anti-itching or anti-hair loss effects, wherein the citrus fruit extract comprises the aforementioned composition;

[0020] Wherein, the mass ratio of total flavonoids to total alkaloids in the citrus fruit extract is (1:30) to (15:1).

[0021] Preferably, in the citrus fruit extract, the content of synephrine is 0.1-3.0%, the content of naringin is 0.1-1.5%, and the content of neohesperidin or hesperidin is 0.1-1.5%.

[0022] Preferably, the citrus fruit extract further comprises at least one of hesperetin, naringenin, tangeretin, rutin, nobiletin, eriocin, and quercetin; and the content of hesperetin, naringenin, tangeretin, rutin, nobiletin, eriocin, and quercetin is 0.001 to 1.0% respectively.

[0023] Compared with the prior art, the present invention has the following significant effects:

[0024] The composition prepared by compounding synephrine or a pharmaceutically acceptable salt thereof, naringin, neohesperidin and / or hesperidin in the present invention has soothing, repairing, anti-wrinkle, analgesic, antipruritic and anti-allergic effects when used as an effective ingredient in skin care products; and has anti-dandruff, degreasing, antipruritic or anti-hair loss effects when used as an effective ingredient in scalp care products.

[0025] The present invention further adopts a composition obtained by compounding synephrine, naringin, and neohesperidin in a specific ratio, and the IC50 result for TRPV3 is 18.39-26.64%. After 4 weeks of use, the dandruff reduction rate and scalp oil content reduction rate reach 31.62-46.26% and 35.27-41.52%, respectively, further improving the anti-dandruff, degreasing, anti-itching and anti-hair loss effects. BRIEF DESCRIPTION OF THE DRAWINGS

[0026] Other features, objects and advantages of the present invention will become more apparent upon reading the detailed description of non-limiting embodiments with reference to the following drawings:

[0027] Figure 1 To verify the VISIA photographs and red zone analysis results of the typical subjects in Example 1;

[0028] Figure 2 To verify the results of fluorescence microscopy in Example 2;

[0029] Figure 3 Schematic diagram of scalp area division in Verification Example 5. DETAILED DESCRIPTION

[0030] The present invention will be described in detail below with reference to specific embodiments. The following embodiments will help those skilled in the art to further understand the present invention, but are not intended to limit the present invention in any form. It should be noted that, for those skilled in the art, several variations and improvements can be made without departing from the scope of the present invention. These all fall within the scope of protection of the present invention.

[0031] In a specific embodiment of the present invention, a composition is provided, comprising synephrine or a pharmaceutically acceptable salt thereof, wherein the weight percentage of synephrine or a pharmaceutically acceptable salt thereof is 1-99%. Specifically, the weight percentage is any one of 1%, 5%, 10%, 15%, 20%, 25%, 30%, 35%, 40%, 45%, 50%, 55%, 60%, 65%, 70%, 75%, 80%, 85%, 90%, 95%, and 99%, or a range formed by any two of the following values.

[0032] The composition further comprises naringin, wherein the weight percentage of naringin and / or hesperidin is 0.1-99%. Specifically, the weight percentage is any one of 0.1%, 0.5%, 1%, 5%, 10%, 15%, 20%, 25%, 30%, 35%, 40%, 45%, 50%, 55%, 60%, 65%, 70%, 75%, 80%, 85%, 90%, 95%, and 99%, or a range formed by any two of the weight percentages.

[0033] The composition further comprises neohesperidin and / or hesperidin, wherein the weight percentage of neohesperidin and / or hesperidin is 0.1-99%. Specifically, the weight percentage is any one of 0.1%, 0.5%, 1%, 5%, 10%, 15%, 20%, 25%, 30%, 35%, 40%, 45%, 50%, 55%, 60%, 65%, 70%, 75%, 80%, 85%, 90%, 95%, and 99%, or a range formed by any two of the above values.

[0034] Specifically, the composition is selected from any one of the following combinations:

[0035] 1) A combination of synephrine or a pharmaceutically acceptable salt thereof, naringin, and neohesperidin; based on 100% by weight of the composition, the weight percentage of synephrine or a pharmaceutically acceptable salt thereof is 1-99%, the weight percentage of naringin is 0.1-98.9%, and the weight percentage of hesperidin is 0.1-98.9%. In one embodiment, the ratio of the weight of synephrine or a pharmaceutically acceptable salt thereof to the total weight of naringin and neohesperidin is (1:30) to (15:1). In a further embodiment, the composition comprises the following components in the following weight proportions: 1-2 parts synephrine or a pharmaceutically acceptable salt thereof; 0.1-2.0 parts naringin; and 0.1-2.0 parts neohesperidin. More preferably, the composition comprises the following weight proportions of the components: 1-2 parts synephrine or a pharmaceutically acceptable salt thereof; 0.2-0.5 parts naringin; and 0.4-0.8 parts neohesperidin. In a further embodiment, the weight ratio of naringin to neohesperidin is (10:1) to (1:10), for example, 10:1, 5:1, 2:1, 1.5:1, 1:1, 1:1.5, 1:2, 1:5, and 1:10. More preferably, the weight ratio of naringin to neohesperidin is (2:1) to (1:2).

[0036] 2) A combination of synephrine or a pharmaceutically acceptable salt thereof, naringin, and hesperidin; based on 100% by weight of the composition, the weight percentage of synephrine or its pharmaceutically acceptable salt is 1-99%, the weight percentage of naringin is 0.1-98.9%, and the weight percentage of hesperidin is 0.1-98.9%. In one embodiment, the ratio of the weight of synephrine or its pharmaceutically acceptable salt to the total weight of naringin and hesperidin is (1:30) to (15:1). In a further embodiment, the composition comprises the following components in parts by weight: 1-2 parts synephrine or its pharmaceutically acceptable salt; 0.1-2.0 parts naringin; and 0.1-2.0 parts hesperidin. More preferably, the composition comprises the following components in parts by weight: 1-2 parts synephrine or its pharmaceutically acceptable salt; 0.2-0.5 parts naringin; and 0.4-0.8 parts hesperidin. In a further embodiment, the weight ratio of naringin to hesperidin is (10:1) to (1:10), for example, 10:1, 5:1, 2:1, 1.5:1, 1:1, 1:1.5, 1:2, 1:5, and 1:10. More preferably, the weight ratio of naringin to hesperidin is (2:1) to (1:2).

[0037] In a specific embodiment of the present invention, the composition may also be a plant extract comprising synephrine or a pharmaceutically acceptable salt thereof, and further comprising naringin, neohesperidin and / or hesperidin, such as a citrus fruit extract.

[0038] In a specific embodiment of the present invention, the citrus fruit extract may further include at least one of hesperetin, naringenin, tangeretin, rutin, nobiletin, eriocin, and quercetin; and the content of hesperetin, naringenin, tangeretin, rutin, nobiletin, eriocin, and quercetin is 0.001 to 1.0% respectively.

[0039] Specific efficacy experiments have verified that the aforementioned composition has soothing, repairing, anti-wrinkle, analgesic, antipruritic, anti-allergic or anti-aging effects; and specific efficacy experiments have also verified that the aforementioned composition has anti-dandruff, degreasing, antipruritic or anti-hair loss effects on the scalp.

[0040] In the detailed description of the present application, the composition of the present application can further include other efficacy ingredients. The other efficacy ingredients include plant extracts such as Magnolia Officinalis Extract, Sophora Flavescens Extract, Artemisia Argyi Extract, Styrax Extract, Illicium Verum Extract, Paubera Coffeae Extract, Albizia Lebbeck Extract, Elettaria Cardamomum Extract, Youngia japonica Extract, Salix Alba Extract, Betula Alba Extract, Imperata Cylindra Extract, Syzygium Aromaticum Extract, Atractylodes Macrocephala Extract, Pulsatilla Koreana Extract, Aristolochia Longa Extract, Mentha Arvensis Extract, Cedrus Atlantica Extract, Schisandra Chinensis Extract, Chamaecyparis Obtusa Extract, Artemisia Scoparia Extract, Crocus Sativus Extract, Atractylodes Lancea Extract, Amomum Subulatum Extract, Amomum Xanthioides Extract, Melilotus Officinalis Extract, Biota Orientalis Extract, Camellia Sinensis Leaf Extract, Bupleurum Falcatum Extract, Acorus Calamus Extract, Hedera Helix Extract, Pulsatilla Koreana Extract, Angelica Gigas Extract, Plantago Asiatica Extract, Aquilaria Agallocha Extract, Chrysanthemum Extract, Aquilaria Sinensis Extract, Panax Notoginseng Extract, Phellodendron Amurense Extract, Zanthoxylum Peppers Extract, Zanthoxylum Bungeanum Extract, Zanthoxylum Nitidum Extract, Zanthoxylum Piperitum Extract, Zanthoxylum Schinifolium Extract, Zanthoxylum Simile Extract, Zanthoxylum Xanthoporum Extract, Zanthoxylum Zanthoxyloides Extract, Zizyphus Jujuba Extract, Salvia Miltiorrhiza Extract, Crataegus Monogyna Extract, Ginkgo Biloba Leaf / Stem Extract, Angelica Archangelica Extract, Codonopsis Lanceolata Extract, Canavalia Gladiata Extract, Rehmannia Glutinosa Extract, Hippophae Rhamnoides Extract, Ruscus Aculeatus Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia Nudicaulis Extract, Scrophularia NudicaScutellaria baicalensis extract, anise fruit extract, fennel extract, radix scutellariae extract, millettia vine extract, centella asiatica extract, pseudoalteromonas ferment extract, quinquefolia root extract, dandelion extract, sisal extract, ginger extract, turmeric extract, gynostemma pentaphyllum extract, yeast lysate extract, yeast extract, elderberry extract, golden lotus extract, dendrobium nobile extract, golden chamomile extract, desmodium officinale extract, urea leaf / root / stem extract, schizonepeta tenuifolia extract, murraya officinalis leaf extract, platycodon grandiflorum extract, artemisia selengensis extract, chrysanthemum extract, chicory extract, kava root extract, sophora flavescens root extract, bitter melon fruit extract, quassia extract, aloe barbadensis extract, peppermint flower / leaf / stem extract, horseradish root extract, pepper extract, forsythia extract, lotus extract, lotus leaf extract, lotus seed extract, trumpet creeper extract, spearmint flower / leaf / stem extract, reed root extract, aloe extract, arundo donax stem extract, deer antler extract, cypress branch extract, monk fruit extract, podocarpus extract, basil flower / leaf / stem extract, mung bean extract, purslane extract, calla lily / stem extract, ophiopogon extract, cyperus rotundus extract, myrrh extract, acacia fruit extract, rosemary extract, codonopsis pilosula extract, jasmine extract, mother clove extract, matricaria extract, peony extract, oroxylum extract, hibiscus bark extract, akebia extract, costus root extract, artemisia selengensis extract, schisandra chinensis Extract, lemon extract, burdock root extract, oregano extract, privet fruit extract, thyme extract, salvia miltiorrhiza extract, clove extract, madder root extract, inula flower extract, agrimony extract, horse chestnut extract, barberry rhizome / root extract, loquat fruit / leaf extract, hops extract, brewer's yeast extract, grape seed extract, grapefruit seed extract, dandelion extract, horse chestnut extract, madder extract, rose extract, zanthoxylum fruit extract, artemisia annua extract, ginseng root extract, honeysuckle flower extract, cypress leaf extract, chuanxiong root extract, angelica extract, coptis root extract, coptis root extract, cistanche extract, nutmeg extract, Lactic acid bacteria fermentation extract, frankincense extract, Panax notoginseng extract, Akebia trifoliata stem extract, mulberry fruit extract, mulberry leaf extract, mistletoe extract, camellia extract, yam extract, cornus officinalis extract, peony extract, cnidium monnieri extract, thyme extract, holy basil leaf extract, acorus calamus extract, pomegranate flower extract, pomegranate seed extract, dianthus extract, cornflower extract, sage extract, water mint extract, milk thistle extract, sappanwood extract, jujube seed extract, pseudoginseng extract, myrtle fruit extract, tenacious grass leaf extract, honeysuckle extract, gastrodia elata extract, asparagus extract, radix schizonepetae extract, smilax china extract, marigold flower extract, fenugreek extract, forsythia suspensa bud / flower extract,Biscuit flower extract, Linderae serrata extract, Ficus microcarpa extract, Soapberry extract, Evodia rutaecarpa fruit extract, Gallnut nut extract, Acanthopanax cortex extract, Schisandra chinensis fruit extract, American ginseng extract, Sambucus nigra flower extract, Cinnamomum cassia bark extract, Leonurus tenuifolia extract, Senna angustifolia leaf extract, Prunella vulgaris extract, Prickly pear extract, Opuntia cactus extract, Citrus citrus peel extract, Lemongrass extract, Bergamot fruit extract, Bergamot leaf extract, Hypericum suspensa extract, Wheat extract, Apricot extract, Bearberry extract, Meadowfoam extract, Pinus tabacum Dill Extract, Cynanchum wilfordii Extract, Scrophulariaceae Extract, Inula Flower Extract, Snow Lotus Extract, Urtica Dioica Extract, Mushroom Extract, Bacillus / Soy Ferment Extract, Bacillus / Rice Bran Extract / Soy Extract Ferment Filtrate, Avena Sativa Extract, Sage Leaf Extract, Rhubarb Extract, Polygonatum Rhizome / Root Extract, Wallwort Extract, Soybean Extract, Crataegus Pinnatifida Fruit Extract, Motherwort Extract, Bupleurum Chinense Extract, Ginkgo Nut Extract, Ginkgo Biloba Leaf Extract, Epimedium Extract, Neem Extract, Myrrh Resin Extract, cherry leaf extract, poppy seed extract, camellia oil tea extract, camellia oil tea seed extract, grapefruit peel extract, grapefruit seed extract, houttuynia cordata extract, elm spirea flower extract, poppy flower extract, cinnamon extract, polygonatum extract, guaiac wood extract, cilantro fruit / leaf extract, mint leaf extract, angelica sinensis, extract, polygala tenuifolia extract, evening primrose extract, Vietnamese benzoin resin extract, costus root extract, Yunnan coptis root extract, jujube fruit extract, soapberry extract, soapberry thorn extract, soap tree bark extract, oriental extract , at least one of camphor leaf extract, long-petaled almond extract, long-crowned selfheal extract, Kalanchoe flower extract, palmate rhubarb extract, Zhejiang horse chestnut extract, pearl extract, sesame extract, rhizome of anemarrhena extract, gardenia flower extract, stemona erecta extract, Chinese rehmannia root extract, poria extract, japonica ginseng extract, bamboo leaf pepper extract, lithospermum officinale extract, mirabilis jalapa extract, perilla frutescens extract, rosewood extract, wisteria extract, ganoderma lucidum extract, and palm extract, or at least one of the main active ingredients in any of the foregoing extracts.

[0041] In a specific embodiment of the present invention, the composition can be applied to a skin care product, wherein the dosage form of the skin care product includes any one of a cream, lotion, essence, water, foam, and spray. The skin care product also includes at least one of the following components: an emollient, a humectant, a thickener, a chelating agent, an emulsifier, a co-emulsifier, an antioxidant, a pH adjuster, a skin conditioner, a surfactant, a fragrance, a preservative, a solvent, and a solubilizing agent.

[0042] In a specific embodiment of the present invention, the composition is added to the skin care product in an amount of 0.01-20% by weight.

[0043] In a specific embodiment of the present invention, the composition can also be used in scalp care products, including any one of shampoo, shampoo cream, conditioner, hair mask, and scalp care lotion. The scalp care product also includes at least one of the following components: a surfactant, a humectant, a thickener, a chelating agent, an emulsifier, a co-emulsifier, an antioxidant, a pH adjuster, a skin conditioner, a viscosity modifier, a foaming agent, a fragrance, a preservative, a solvent, a solubilizer, and a pigment.

[0044] In a specific embodiment of the present invention, the composition is added to a skin care product or a scalp care product at a weight ratio of 0.01-20%.

[0045] The raw materials, reagents, etc. used in the following examples are all conventional commercial products or can be prepared by conventional methods, and the present invention does not impose any particular limitations thereto.

[0046] Example 1

[0047] This embodiment provides a composition comprising the following components in parts by weight: 1.5 parts of synephrine, 0.3 parts of neohesperidin, and 0.6 parts of naringin.

[0048] Example 2

[0049] This embodiment provides a composition comprising the following components in parts by weight: 1 part of synephrine, 0.5 part of neohesperidin, and 0.5 part of naringin.

[0050] Example 3

[0051] This embodiment provides a composition comprising the following components in parts by weight: 1 part of synephrine, 0.4 part of neohesperidin, and 0.8 part of naringin.

[0052] Example 4

[0053] This embodiment provides a composition comprising the following components in parts by weight: 2 parts of synephrine, 0.2 parts of neohesperidin, and 0.4 parts of naringin.

[0054] Example 5

[0055] This embodiment provides a composition comprising the following components in parts by weight: 1.5 parts of synephrine, 0.5 parts of neohesperidin, and 0.5 parts of naringin.

[0056] Example 6

[0057] This embodiment provides a composition comprising the following components in parts by weight: 1.5 parts of synephrine, 0.3 parts of hesperidin, and 0.6 parts of naringin.

[0058] Example 7

[0059] This embodiment provides a composition comprising the following components in parts by weight: 1 part of synephrine, 0.8 part of neohesperidin, and 0.2 part of naringin.

[0060] Example 8

[0061] This embodiment provides a composition comprising the following components in parts by weight: 1 part of synephrine, 0.1 part of neohesperidin, and 1.1 parts of naringin.

[0062] Example 9

[0063] This embodiment provides a composition comprising the following components in parts by weight: 2.3 parts of synephrine, 0.1 parts of neohesperidin, and 0.2 parts of naringin.

[0064] Example 10

[0065] This embodiment provides a composition comprising the following components in parts by weight: 0.8 part of synephrine, 0.5 part of neohesperidin, and 0.8 part of naringin.

[0066] Example 11

[0067] This embodiment provides a composition comprising the following components in parts by weight: 6 parts of synephrine, 0.2 parts of neohesperidin, and 0.2 parts of naringin.

[0068] Example 12

[0069] This embodiment provides a composition comprising the following components in parts by weight: 0.1 part of synephrine, 1.0 part of neohesperidin, and 2.0 parts of naringin.

[0070] Example 13

[0071] This embodiment provides a composition comprising the following components in parts by weight: 0.8 part of synephrine, 0.5 part of neohesperidin, 0.8 part of naringin, and 0.3 part of polymethoxyflavonoids.

[0072] Example 14

[0073] This embodiment provides a composition comprising the following components in parts by weight: 3 parts of synephrine, 0.5 parts of neohesperidin, and 0.5 parts of naringin.

[0074] Example 15

[0075] This embodiment provides a composition comprising the following components in parts by weight: 2 parts of synephrine, 0.2 parts of neohesperidin, and 2 parts of naringin.

[0076] Example 16

[0077] This embodiment provides a composition comprising the following components in parts by weight: 1.5 parts of synephrine, 2 parts of neohesperidin, and 0.2 parts of naringin.

[0078] Example 17

[0079] This embodiment provides a citrus fruit extract obtained by conventional extraction methods. The citrus fruit extract comprises the following components: 1.5% synephrine, 0.5% neohesperidin, and 1% naringin. The contents of each component were determined by HPLC.

[0080] Comparative Example 1

[0081] This comparative example provides a composition comprising the following components in parts by weight: 0 parts of synephrine, 1.0 parts of neohesperidin, and 1.2 parts of naringin.

[0082] Comparative Example 2

[0083] This comparative example provides a composition comprising the following components in parts by weight: 0.7 parts of synephrine, 0 parts of neohesperidin, and 1.5 parts of naringin.

[0084] Comparative Example 3

[0085] This comparative example provides a composition comprising the following components in parts by weight: 1.7 parts of synephrine, 0.5 parts of neohesperidin, and 0 parts of naringin.

[0086] Comparative Example 4

[0087] This comparative example provides a composition comprising the following components in parts by weight: 2 parts of synephrine, 0 parts of neohesperidin, and 0 parts of naringin.

[0088] Comparative Example 5

[0089] This comparative example provides a composition comprising the following components in parts by weight: 0 parts of synephrine, 1 part of neohesperidin, and 1 part of naringin.

[0090] Efficacy verification

[0091] Verification Example 1: Lactic Acid Stimulation Human Efficacy Evaluation Test

[0092] Principle: Skin irritation reactions can be clinically manifested as erythema, small bumps, burning and stinging, itching, etc. The severity of the irritation is closely related to the secretion of cytokines and damage to tissue structure. Sensitive skin refers to a syndrome in which discomfort (stinging, burning, pain, itching and tingling) occurs in response to routine stimulation (no abnormal sensation occurs under normal conditions). This discomfort cannot be explained by any skin lesions related to skin diseases. Symptoms of skin sensitivity include skin irritation reactions, and persistent skin irritation reactions can aggravate skin sensitivity symptoms. Lactic acid sting test, capsaicin test, patch test, histamine test, etc. are often used as human evaluation methods for skin sensitivity and skin irritation.

[0093] This experiment targeted the nasolabial folds and cheeks, areas of sensitive skin. After immediately applying lactic acid and a sample, subjects were asked to assess their subjective ratings of various discomforts following the irritation. The efficacy of the sample was evaluated by analyzing changes in the red zone using the VISIA facial analyzer. Lactic acid, at a certain concentration and for a certain duration, can cause a stinging sensation without adverse consequences, making it suitable for testing skin sensitivity. The nasolabial folds and cheeks have high keratin permeability, rich accessory organs, and a rich neural network, making the stinging sensation more pronounced. This lactic acid stinging test can provide a reference for the diagnosis and treatment of sensitive skin, and can also be used to evaluate the effectiveness of samples in alleviating sensitive skin.

[0094] The compositions prepared in Example 1 and Example 2 were used as test samples 1 and 2. Water and butanediol were used as solvents (44% water, 36% butanediol, 20% composition) to prepare a 20% composition solution. The solution was then diluted with water to a 1% composition concentration to obtain the corresponding test sample solutions 1 and 2.

[0095] Subjects aged 18-60 with healthy skin who are sensitive to lactic acid stimulation were recruited. The method for determining sensitive skin was as follows: After cleansing and balancing, a 10% lactic acid solution was applied to the test area and a timer was started. The lactic acid sting score was recorded by questioning 2.5 minutes and 5 minutes later. A total score of 3 or higher at both 2.5 and 5 minutes was considered sensitive skin.

[0096] Recruited subjects who were sensitive to lactic acid stimulation were randomly smeared with test sample solution 1 or test sample solution 2 on the left and right sides of their cheeks, once daily in the morning and evening for seven consecutive days. Lactic acid irritation was assessed before application (day 0) and seven days after application (day 7). A 4-point scale (0: no sensation, 1: mild, 2: moderate, 3: severe) was used to score the irritation. Scores were recorded 1 to 5 minutes after stimulation. VISIA images were taken and the red area analyzed.

[0097] Compared with before use, the lactic acid stimulation score of the test sample solution 1 after 7 days of use decreased by 52.49%, 50.83%, 51.05%, 49.47%, and 43.61% at 1, 2, 3, 4, and 5 min, respectively; the lactic acid stimulation score of the test sample solution 2 after 7 days of use decreased by 65.12%, 70.87%, 56.15%, 54.70%, and 51.96% at 1, 2, 3, 4, and 5 min, respectively.

[0098] The VISIA photograph and the red area analysis result of a typical subject are shown in Figure 2 Compared with before use, the cheek red area feature count and score of the subject after 7 days of use of the test sample solution 1 Figure 1 (a)) and after 7 days of use of the test sample solution 2 Figure 1 (b)) were all reduced, and the percentile was all increased, indicating that the skin sensitivity was reduced after use of the compositions prepared in Example 1 and Example 2.

[0099] Verification Example 2: TRPV1 stimulation reaction test

[0100] Principle: The soothing efficacy refers to the help in improving the state of skin irritation, and the repairing efficacy refers to the help in maintaining the normal state of the application site. Different types of experimental methods can be used for verification. The activation reaction of TRPV1 of keratinocytes with high expression of TRPV1 under the action of different stimulants is used to test the efficacy of CR.

[0101] The mechanism of occurrence of skin sensitivity or irritation includes that the stimulant first passes through the stratum corneum to cause damage to the barrier function, induces the primary reaction of the cutaneous receptor in the epidermis of the skin, and then activates the cascade amplification reaction in the dermis, and finally causes various clinical symptoms of the skin. Among them, the cutaneous receptor is increasingly studied in sensitive skin. The transient receptor potential receptor (TRP) is related to various biological functions, including temperature sensation, vascular inflammation, irritation, intracellular ion homeostasis, and nerve cell signal transduction, and is an important target for skin sensitivity. TRPV1 is a non-selective cation channel with high permeability to calcium ions, and it is the first member of the TRP superfamily found in mammals. It is mainly expressed at the end of the central and peripheral small sensory neurons, and is also found in different brain regions such as the cerebellum, hypothalamus, cerebral cortex, olfactory bulb, midbrain, and hippocampus. It plays an important role in regulating nociceptive stimulation. Recent studies have also found that TRPV1 plays an important role in pain and neurogenic inflammation, and its overactivation and overexpression can induce sensitive skin discomfort. Therefore, TRPV1 is considered as a means to judge sensitive skin, and the regulation of TRPV1 helps to improve skin irritation and maintain the normal state of the skin, and repair sensitive skin.

[0102] The detection of TRPV1 overactivation mainly includes TRPV1 channel activation and changes in TRPV1 expression. After TRPV1 is activated by capsaicin, vanillin, phenoxyethanol, low pH, etc., it causes extracellular Ca 2+ Fluo-8 / AM, a commonly used fluorescent probe for calcium ions, can be used to quantitatively detect Ca influx and transduce pain signals in the peripheral nervous system. 2+ Changes in Ca influx can be detected by FlexStation 3 or fluorescence microscopy, allowing for quantification of Ca 2+ Influx intensity. The intensity of the fluorescence signal is related to the intracellular free Ca 2+ Proportional to concentration.

[0103] Experimental methods:

[0104] 1) The compositions prepared in Example 2, Example 5, Example 14, Comparative Example 4, and Comparative Example 5 were used as test samples. Water and butanediol were used as solvents (44% water, 36% butanediol, and 20% composition) to prepare a 20% composition solution, which was then diluted with water to a composition concentration gradient of 0.5%, 0.25%, 0.125%, and 0.06% of each test substance.

[0105] 2) Construction of HaCaT-TRPV1-OE cells: The human TRPV1 mRNA CDS sequence (GenBank: AY131289.1) and the lentiviral system vector pCDH-CMV-MCS-EF1α-Puro were first constructed into a co-expression vector by double enzyme digestion. The lentivirus was then used to infect normal HaCaT cells. After puromycin selection and cell function verification, a HaCaT cell line with high TRPV1 expression, namely HaCaT-TRPV1-OE cells, was obtained.

[0106] 3) HaCaT-TRPV1-OE cells were digested with trypsin to prepare a cell suspension and the concentration was adjusted to 2-2.5×10 5 / ml, 500 μl per well was inoculated into a 24-well plate containing a cell slide and incubated overnight in a carbon dioxide incubator at 37°C and 5% CO2. Different concentrations of the test substances were added, followed by Fluo-8 / AM dye (final concentration 5 μM) and incubated for 30 minutes. The stimulator (5 μM nicotinamide) was then added for 10 minutes. The culture medium was discarded, the cell slide was removed, and the slide was sealed and photographed under a fluorescence microscope.

[0107] Test results: The results are as follows Figure 2 As shown ( Figure 2 , F represents the composition of Comparative Example 5, A represents the composition of Comparative Example 4, AF3:1 represents the composition of Example 14, AF1.5:1 represents the composition of Example 5, and AF1:1 represents the composition of Example 2). Figure 2 The results show that the composition of Example 2 has an effect on Ca 2+ The results show that the composition of Example 2 has an effect on Ca

[0108] Verification Example 3: Anti-wrinkle efficacy test

[0109] Principle: With age, the epidermis of the skin becomes thin, the elastic fibers disappear, and then wrinkles appear, and skin aging occurs. Skin aging is the most obvious and most obvious manifestation of body aging, and can be used as a predictor of life expectancy and health. Fibroblasts are the most abundant cell type in the dermis, which directly or through interaction with other cells leads to skin aging. Human fibroblasts are cells with vigorous functional activity, with large cells and nuclei, clear outlines, large and obvious nuclei, weakly basophilic cytoplasm, and obvious protein synthesis and secretion activity. Human dermal fibroblasts are responsible for synthesizing most of the skin collagen fibers. An increase in the number of cells helps to increase collagen fiber synthesis and improve skin elasticity to resist aging. Type I collagen (COL I) and type III collagen (COL III) exist in the dermis, and type I collagen accounts for about 80% of the total collagen in the dermis. The content of COL I and COL III in the skin decreases with age. The extracellular matrix component (ECM) of the dermal layer mainly contains collagen, structural glycoprotein, polysaccharide, etc., and together with fibroblasts forms a complex network structure to maintain the structure of the skin and is closely related to skin aging. Therefore, the cell proliferation capacity, the content of COL I, COL III, and each protein in the ECM in the cell can be used as a key indicator for cell aging detection.

[0110] Experimental method:

[0111] Test sample solutions 1 and 2 were prepared using the method in Verification Example 1.

[0112] HDF-a cells (Sciencell 2320) were inoculated at 5*10 4 The cells were inoculated in a 12-well plate at 5*10

[0113] The test results showed that compared with the control group, the expression of COL I increased by 89% and 102% after the cells were treated with test sample solutions 1 and 2.

[0114] Verification Example 4: TRPV3 stimulation response test

[0115] Literature reports that TRPV3 is a thermosensitive transient receptor potential channel belonging to the same TRPV family as TRPV1 (TRPV1 has been shown to be associated with acute pruritus, but not with the severity of scalp pruritus). TRPV3 plays a role in scalp pruritus and is also abundantly expressed in keratinocytes and scalp hair follicles. Activation of TRPV3 inhibits hair growth in humans. Hair loss is associated with premature differentiation of follicular keratinocytes, characterized by premature denaturation of keratin and keratin, increased production of deiminated proteins, increased apoptosis, and decreased expression of transcriptional regulators known to regulate hair follicle differentiation (Foxn1, Msx2, Dlx3, and Gata3). These abnormalities occur in the inner root sheath and medial proximal region of the hair shaft, where TRPV3 is highly expressed and associated with impaired hair tract and shaft formation. Therefore, TRPV3 can be used to evaluate the efficacy of suppressing scalp pruritus and preventing hair loss.

[0116] Experimental plan:

[0117] Construction of HaCaT-TRPV3-OE cells: The human TRPV3 mRNA CDS sequence (GenBank: NM_001258205.2) and the lentiviral system vector pCDH-CMV-MCS-EF1α-Puro were first constructed into a co-expression vector by double enzyme digestion. The lentivirus was then used to infect normal HaCaT cells. After puromycin selection and cell function verification, a HaCaT cell line with high TRPV3 expression, namely HaCaT-TRPV3-OE cells, was obtained.

[0118] HaCaT-TRPV3-OE cells were seeded at 3.5w / well in a black 96-well plate and cultured overnight. The next day, the culture medium was discarded, 200μL 1×HHBS was added to each well and washed once, 75μL 1×HHBS and 25μL Ca- AM working solution was incubated in a CO2 incubator for 60 min ± 5 min. After staining, 200 μL of 1× HHBS was added to each well and gently washed twice. 75 μL of 1× HHBS and 25 μL of sample at different concentrations were added to each well and incubated in a cell culture incubator for 10 min. After incubation, FlexStation3 automatically added 25 μL of stimulant to each well and collected the signal.

[0119] The 1×HHBS used was prepared by diluting 10×HBSS into 1×HBSS using sterile water, and then adding an appropriate amount of HEPES to a concentration of 20 mM.

[0120] The samples used included agonists, antagonists, and test substances, all of which were prepared with 1×HHBS at corresponding concentrations.

[0121] TRPV3 antagonist: Ruthenium red, starting with a concentration of 100 μM, diluted to 8 concentration points, with a dilution factor of 2.

[0122] Test substance: The compositions of Examples 1-14 and Comparative Examples 1-5 were prepared into 20% solutions using water and butanediol as solvents (44% water, 36% butanediol, 20% composition), and then diluted with water to a final concentration of 2% of the test substance. The solution was then diluted down by 8 points, with a dilution factor of 2.

[0123] The citrus fruit extract of Example 15 was prepared into a 20% solution using water and butylene glycol as solvents (44% water, 36% butylene glycol, 20% citrus fruit extract), and then diluted with water to a final concentration of 2% of the test substance. The solution was then diluted down by 8 points, with a dilution factor of 2.

[0124] The stimulus used was a TRPV3 agonist, specifically 2-aminoethyldiphenylborinate (2-APB) at a final concentration of 200 μM.

[0125] The IC50 results obtained from the final test are shown in Table 2.

[0126] Table 2

[0127] Test substance IC50 Ruthenium red 27.99％ Example 1 25.09％ Example 2 18.39％ Example 3 26.64％ Example 4 23.72％ Example 5 20.86％ Example 6 28.42％ Example 7 26.55％ Example 8 29.76％ Example 9 28.81％ Example 10 30.26％ Example 11 35.43％ Example 12 41.71％ Example 13 32.67％ Example 14 39.82％ Example 15 27.37％ Example 16 28.09％ Example 17 26.43％ Comparative Example 1 45.29％ Comparative Example 2 42.04％ Comparative Example 3 38.77％ Comparative Example 4 53.91％ Comparative Example 5 55.20％

[0128] Verification Example 5: Evaluation Test of Anti-dandruff and Anti-oiling Efficacy

[0129] Inclusion criteria: ① Subjects had experienced moderate or higher levels of scalp itching, dandruff, or scalp redness and swelling for at least three consecutive months; ② Hair length >3 cm, no severe hair loss, and hair root growth covering at least 70% of the scalp; ③ Dandruff grade >3 or redness >3 at the end of the recruitment and conditioning periods; ④ Good health, healthy, non-allergic skin, and no history of cosmetic allergies. Exclusion criteria: ① Pregnant or breastfeeding women; ② Medical conditions that could affect outcome assessment (such as psoriasis and contact dermatitis); ③ Other scalp injuries or allergies. All subjects provided signed informed consent.

[0130] Test process: pre-conditioning period of 2 weeks, test period of 4 weeks. 0w), after the pre-conditioning period (T 2w ), 2 weeks after the test period (T 4w ), 4 weeks after the test period (T 6w ) Regularly track and record the degree of dandruff and oiliness of the subjects.

[0131] Conditioning shampoo: A commercially available shampoo without dandruff and oil removal properties (provided by the testing agency)

[0132] There were 19 types of shampoos in the test period: the compositions of Examples 1-14 and Comparative Examples 1-5 were prepared using water and butylene glycol as solvents (44% water, 36% butylene glycol, 20% composition) to prepare a 20% solution of the composition. Then, the 20% solution of each composition prepared above was added to commercially available shampoo at a final composition concentration of 1%, forming test shampoo samples 1-19.

[0133] Dandruff evaluation: The scalp is divided into 12 areas ( Figure 3 ), the expert evaluator selected the 4 most severe dandruff areas for evaluation at each time point, and took the average score of the 4 areas. The higher the score, the more severe the dandruff and the more severe the scalp redness and swelling. Test time point: T 0w 、T 2w 、T 4w 、T 6w . Staff are required to collect photos of the relevant areas.

[0134] Dandruff evaluation criteria: 0 points - no dandruff; 1 point - small powdery grayish-white rough scales; 2 points - small to medium-sized scales; 3 points - large, thin scales loosely attached to the scalp; 4 points - large, sticky scales; 5 points - thick white to yellow scales tightly attached to the scalp.

[0135] Scalp oil secretion analysis: Under standard experimental conditions, a test area was screened and labeled for each volunteer. Following the instrument's operating instructions, the test was repeated three times for each test point, and the average value was calculated.

[0136] Collection Method: The SEBUMETER measures scalp oil content to assess scalp oil secretion. Testing conditions strictly follow a 30-minute sitting position in a laboratory at 22°C + 1°C and 50% + 5% relative humidity. The SEBUMETER is then used to measure each area three times.

[0137] The PHOTOS method is a globally recognized oil content test based on the principle of photometry. A special 0.1mm thick matte tape absorbs oil from the skin, becoming translucent. The tape's light transmittance changes; the more oil absorbed, the greater the light transmittance, allowing the oil content of the skin to be measured. Its greatest advantage is its small size and ease of use, allowing testing of any area of ​​the skin. This indirect measurement of oil gland secretions allows for differentiation between different skin types, enabling accurate understanding of changes in oil content caused by both internal and external factors.

[0138] According to different time points (T 2W 、T 6W The dandruff score test results and scalp oil content results of the scalp were used to calculate the dandruff reduction rate and scalp oil content reduction rate using the following formula:

[0139] Decline rate / %=(T 6W Test value-T 2W Test value) / T 2W Test value × 100%

[0140] The results are shown in Table 3.

[0141] Table 3

[0142]

[0143] The present invention has many specific application paths, and the above is only a preferred embodiment of the present invention. It should be noted that the above embodiments are only used to illustrate the present invention and are not intended to limit the scope of protection of the present invention. For those skilled in the art, several improvements can be made without departing from the principles of the present invention, and these improvements should also be considered as the scope of protection of the present invention.

Claims

1. A composition, characterized in that The invention comprises synephrine or a pharmaceutically acceptable salt thereof, and further comprises naringin, neohesperidin and / or hesperidin.

2. The composition according to claim 1, characterized in that The ratio of the weight of synephrine or its pharmaceutically acceptable salt to the total weight of naringin, neohesperidin and / or hesperidin is (1:30) to (15:1).

3. The composition according to claim 2, characterized in that The composition comprises the following components in parts by weight: 1.0-2.0 parts of synephrine or a pharmaceutically acceptable salt thereof; 0.1-2.0 parts of naringin; Neohesperidin and / or hesperidin 0.1-2.0 parts.

4. The composition according to claim 2 or 3, characterized in that The weight ratio of the naringin to the neohesperidin and / or hesperidin is (10:1) to (1:10).

5. Use of the composition according to any one of claims 1 to 4 in preparing a skin care product with soothing, repairing, anti-wrinkle, analgesic, antipruritic or anti-allergic effects.

6. Use of the composition according to any one of claims 1 to 4 in the preparation of a scalp care product with anti-dandruff, degreasing, anti-itching or anti-hair loss effects.

7. Use of a citrus fruit extract in preparing a skin care product with soothing, repairing, anti-wrinkle, analgesic, antipruritic or anti-allergic effects, characterized in that: The citrus fruit extract comprises the composition of claim 1; Wherein, the mass ratio of total flavonoids to total alkaloids in the citrus fruit extract is (1:30) to (15:1).

8. Use of a citrus fruit extract in preparing a scalp care product with anti-dandruff, degreasing, anti-itching or anti-hair loss effects, characterized in that: The citrus fruit extract comprises the composition of claim 1; Wherein, the mass ratio of total flavonoids to total alkaloids in the citrus fruit extract is (1:30) to (15:1).

9. The use according to claim 7 or 8, characterized in that The citrus fruit extract contains 0.1-3.0% synephrine, 0.1-1.5% naringin, and 0.1-1.5% neohesperidin or hesperidin.

10. The use according to claim 7 or 8, characterized in that The citrus fruit extract further comprises at least one of hesperetin, naringenin, tangeretin, rutin, nobiletin, eriocin and quercetin; the content of each of hesperetin, naringenin, tangeretin, rutin, nobiletin, eriocin and quercetin is 0.001-1.0%.

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