阅读说明：本技术 促进皮肤微循环的活性组合物及其制备方法与应用 (Active composition for promoting skin microcirculation and preparation method and application thereof ) 是由 孙乐青 于 2019-11-15 设计创作，主要内容包括：本发明涉及一种促进皮肤微循环的活性组合物及其制备方法与应用。本发明提供的具有促进皮肤微循环作用的活性组合物的活性组分为橙皮苷、泛醇、腺苷、银杏叶提取物和肝素,该组合物之间通过不同机理而起到协同增效作用,相对于单个活性组分,组合物具有显著的促进皮肤微循环的优势；各组分协同增效,能够有效且持续地促进皮肤微循环,加速皮肤自我更新,启动抗老修护,加速细胞增殖代谢,抚平皱纹细纹,淡化色斑暗斑,改善皮肤的整体质感和外观。(The invention relates to an active composition for promoting skin microcirculation and a preparation method and application thereof. The active components of the active composition with the effect of promoting skin microcirculation are hesperidin, panthenol, adenosine, a ginkgo leaf extract and heparin, the compositions have a synergistic interaction effect through different mechanisms, and compared with a single active component, the composition has the advantage of remarkably promoting skin microcirculation; the components have synergistic effect, and can effectively and continuously promote skin microcirculation, accelerate skin self-renewal, start anti-aging repair, accelerate cell proliferation and metabolism, smooth wrinkles and fine lines, fade color spots and dark spots, and improve the overall texture and appearance of the skin.)

1. An active composition with skin microcirculation promoting effect comprises hesperidin, panthenol, adenosine, folium Ginkgo extract and heparin.

2. Active composition according to claim 1, characterized in that its active components comprise:

3. active composition according to claim 1, characterized in that its active components comprise:

preferably, the active components thereof comprise:

4. a method for preparing an active composition for promoting skin microcirculation according to any of claims 1 to 3, which comprises: preparing a clear and transparent system by using purified water as a solvent and hesperidin, panthenol, adenosine, a ginkgo leaf extract and heparin as active components; adjusting the pH value to 4.5-6.5; freezing and then thawing, allowing intermolecular self-assembly of the active components to form a supramolecular structured composition.

5. The method of claim 4, wherein the pH is adjusted to 4.5-6.0, preferably 5.0 ± (0.2-0.5); and/or the presence of a gas in the gas,

repeatedly freezing and thawing for 1-10 times to allow the active ingredient to fully perform intermolecular self-assembly.

6. The method of claim 4 or 5, wherein the freezing is performed at 0 ℃ to-30 ℃, preferably for 1-20 hours per freezing; and/or the time for each thawing is 1-20 hours.

7. The method of any one of claims 4 to 6, further comprising a step of ultrasonication before the freezing; preferably, the conditions of the ultrasonic treatment are: ultrasonic frequency is 20-55Khz, and ultrasonic treatment time is 15-120 minutes.

8. An active composition prepared by the method of any one of claims 4-7.

9. Use of an active composition according to any one of claims 1 to 3, 7 for the preparation of a pharmaceutical, cosmetic or biological material.

10. A cosmetic comprising the active composition according to any one of claims 1 to 3 or 7;

preferably, the cosmetic comprises the following components in parts by weight:

Technical Field

The invention relates to an active composition for promoting skin microcirculation, and also provides a preparation method and application of the active composition.

Background

The capillary network of the skin is a complex dynamic system that plays a very important role in skin color, thermoregulation, skin metabolism and transdermal transport. The microcirculation transports the hemoglobin to the skin, the microcirculation is accelerated, sufficient oxygen and nutrient substances are provided for keratinocytes and the like of the skin, metabolites of the cells and various harmful substances such as superoxide anions and the like are removed in time, the oxidation of collagen fibers is reduced, various cells of the skin maintain good functions, the moisture of the stratum corneum is sufficient, and the bright and glossy surface of the skin is maintained. Therefore, the development of the skin care product capable of improving skin microcirculation plays an important role in delaying skin aging and improving skin color.

Disclosure of Invention

The invention provides an active composition with the effect of promoting skin microcirculation, the composition has a synergistic effect through different mechanisms, and compared with a single active component, the composition has the advantage of remarkably promoting the skin microcirculation.

The inventor researches and discovers that the hesperidin, the panthenol, the adenosine, the ginkgo biloba extract and the heparin which are used as active components are combined for external use, and the components have synergistic interaction, so that the skin micro-circulation can be effectively and continuously promoted, the self-renewal of the skin is accelerated, the anti-aging repair is started, the cell proliferation and metabolism are accelerated, the fine wrinkles and lines are smoothed, the color spots and dark spots are lightened, and the overall texture and appearance of the skin are improved.

Specifically, the invention firstly provides an active composition with the effect of promoting skin microcirculation, and the active components of the composition comprise hesperidin, panthenol, adenosine, ginkgo biloba extract and heparin.

Further, the active composition with the effect of promoting skin microcirculation comprises the following active components:

still further, the active composition having the effect of promoting skin microcirculation comprises the following active components:

in some preferred embodiments of the present invention, the active ingredients in the active composition having the effect of promoting skin microcirculation include:

in some embodiments of the present invention, the active composition for promoting skin microcirculation is composed of or prepared from hesperidin, panthenol, adenosine, ginkgo biloba extract and heparin as active ingredients.

The brief introduction of the five active components is as follows:

hesperetin (Hesperetin) belongs to flavanone compounds, Hesperidin (Hesperidin) is the rutinoside of Hesperetin, and the Hesperidin and the rutinoside are the main effective components of Citrus aurantium of Rutaceae, and are abundant in pericarpium Citri Tangerinae, lemon peel, fructus Aurantii, fructus Citri Tangerinae and fructus Citri Sarcodactylis. The hesperetin and hesperidin can be prepared from pericarpium Citri Tangerinae. Hesperidin and hesperetin have vitamin P-like effect, can enhance vitamin C, can be used as antioxidant for food, medicine and cosmetic, and can prevent fat oxidation and rancidity, and has the same effect when administered in vitro; hesperidin and hesperetin can improve blood flow of subcutaneous capillary, promote hair growth, and improve black eye, and can be used in skin care product in winter to prevent cold injury; the hesperetin has strong antibacterial effect, can inhibit the generation of dental plaque when being used in the toothpaste, has the dosage of 0.1-0.01 percent, and simultaneously eliminates halitosis; hesperidin has anti-inflammatory effect, and can inhibit intercellular adhesion to prevent skin diseases such as vesicular disease, keratosis, and dyskeratosis; hesperidin and hesperetin can also be used as weight reducing agent. In some embodiments of the invention, the hesperidin purity is > 95%.

Panthenol can be used as an isodynamic substance of vitamin B5, participates in the same metabolic process in organisms, and can be used as a nutritional supplement and a reinforcing agent. Although only panthenol has biological activity, for moisturizing skin care, the panthenol and racemic panthenol have the same effect, have a lasting moisturizing function, and can prevent hair from splitting and damaging, increase hair density, stimulate hair growth and improve hair quality luster; nail care appears to improve nail hydration, imparting flexibility to the nail; panthenol has strong transdermal permeability, can promote blood circulation, has anti-inflammatory effect, can stimulate epithelial cell growth, promote wound healing, and has anti-inflammatory effect. In some embodiments of the invention, the panthenol purity is 98% or more.

Adenosine (Adenosine) is a purine substance, is an important biochemical metabolite in animals, and is widely present in plants, such as Liliaceae (Liliaceae) leek (alliumturosum) leaves and Hubei mountain ophiopogon roots (liliopesipitata). Is prepared by a microbial fermentation method at present. Adenosine is white spun silk-shaped crystal (methanol), has a melting point of 235-236 ℃, is easily soluble in water and is almost insoluble in an organic solvent, and is a nutritional aid and widely compatible with skin care emulsions for conditioning skin, resisting aging, preventing wrinkles, whitening and the like; has effects in stimulating hair growth and inhibiting dandruff generation; can interfere the synthesis of virus nucleic acid, is an antiviral active ingredient of traditional Chinese medicine, and has antibacterial and anti-inflammatory effects; has pharmacological action of promoting coronary blood volume, is a clinical vasodilator, and has wide activity on nervous system. In some embodiments of the invention, the adenosine is greater than or equal to 99.5% pure.

Ginkgo biloba leaf extract (GBE) is a product which is prepared by taking ginkgo biloba leaves as a raw material, adopting a proper solvent and enriching extracted effective components. Various preparations prepared by taking GBE as a raw material are widely applied to the fields of medicines, health-care products, food additives, functional beverages, cosmetics and the like. The product is one of the most successful cases of botanical drugs (belonging to traditional Chinese medicines) developed by modern science and technology. The ginkgo biloba extract can be prepared by the techniques commonly used in the art. In some embodiments of the present invention, the ginkgo biloba extract has a ginkgo biloba total flavonoid content of greater than or equal to 24.0%.

Heparin (Heparin) is polydisaccharide formed by repeatedly and alternately connecting 2-iduronic acid and glucosamine disulfate through β -1, 4 and α -1, 4 glycosidic bonds, the relative molecular mass is 15000-30000, Heparin is commonly present in mammals, Heparin is taken from mucous membranes of duodenum of pigs, and the Heparin is usually in the form of sodium salt.

Generally, the active composition with the effect of promoting skin microcirculation can be prepared by taking hesperidin, panthenol, adenosine, a ginkgo leaf extract and heparin as active components by adopting a conventional method in the field, for example, the components are taken according to the proportion, purified water is added after mixing, and the mixture is stirred until the system is clear and transparent; or further freeze drying, pulverizing into 50-300 mesh granules, and storing.

Surprisingly, it has been found that the sustained release effect of the active components of the active composition can be achieved after the supramolecular recognition self-assembly treatment, which has the advantage of significantly prolonging the duration of action compared to the individual components or compositions not subjected to the supramolecular recognition self-assembly treatment.

Specifically, the present invention also provides a preparation method of the above active composition, comprising: preparing a clear and transparent system by using purified water as a solvent and hesperidin, panthenol, adenosine, a ginkgo leaf extract and heparin as active components; adjusting the pH value to 4.5-6.5; freezing and then thawing, allowing intermolecular self-assembly of the active components to form a supramolecular structured composition.

The clear and transparent system can be prepared by, for example, mixing hesperidin, panthenol, adenosine, folium Ginkgo extract, and heparin in formula ratio, slowly adding pure water, and stirring until the system is clear and transparent.

Further, the pH of the clear and transparent system is adjusted to be between 4.5 and 6.0, more preferably between 5.0 ± (0.2 and 0.5). Researches show that the intermolecular force in the system is stronger in the pH range, and the intermolecular recognition and self-assembly are more facilitated.

In some embodiments of the invention, the pH of the clear transparent system is adjusted to 4.5, 4.8, 5.0, 5.2, or 5.5.

pH adjusting agents commonly used in the art, such as citric acid, salicylic acid, lactic acid, glycolic acid, and the like, may be used.

Further, the freezing treatment is preceded by an ultrasonic treatment step, under the promotion of ultrasonic cavitation, on one hand, molecular motion is intensified, collision opportunities among molecules are increased, and preliminary complexation or self-assembly is generated among the molecules, on the other hand, materials with larger polymerization degree, such as a small amount of β -glucan with molecular weight more than 50 ten thousand daltons, are broken, so that the polymerization degree is reduced, and the self-assembly among the molecules is facilitated, and in addition, small molecular materials are also beneficial to the permeation and absorption of skin.

In some embodiments of the present invention, the sonication conditions are: ultrasonic frequency is 20-55Khz, and ultrasonic treatment time is 15-120 minutes.

In some embodiments of the invention, the sonication is performed at room temperature (20-25 ℃).

In some embodiments of the present invention, the freezing is performed under a closed condition, which has an advantage of using a cyclic directional freezing-thawing (DFT) method, which is a biomimetic biosynthesis technique for inducing intermolecular self-assembly by changing external conditions, and has a main advantage of ensuring the biological activity of the base material, and after entering the skin, the base material slowly and spontaneously releases the self-assembly to release the active substance, thereby reducing the irritation of the active substance to the skin, and further, the active substance which is difficult to enter the skin can be complexed with the active substance with strong skin permeability by the self-assembly to promote the active substance to enter the deep layer of the skin to exert the biological activity.

Further, in the above preparation method, freezing and thawing may be repeated 1 to 10 times (for example, 5 times) to allow the active ingredient to sufficiently undergo intermolecular self-assembly.

In some embodiments of the invention, the freezing is carried out at a temperature of from 0 ℃ to-30 ℃, for example-25 ℃, preferably for a time period of from 1 to 20 hours, for example 12 hours, per freezing.

In some embodiments of the invention, the time for each thaw is 1 to 20 hours.

The invention also comprises an active composition prepared by the supermolecule recognition self-assembly treatment.

The invention also comprises the application of the active composition with the function of promoting skin microcirculation in the aspects of preparing medicines, cosmetics, biological materials and the like.

Specifically, the invention also provides a cosmetic which contains the active composition with the effect of promoting skin microcirculation or takes the active composition with the effect of promoting skin microcirculation as a main active ingredient. The cosmetic has microcirculation regulating function, and also has lasting moisture keeping effect, and can be used as skin care product.

In some embodiments of the present invention, the main active ingredients for promoting skin microcirculation in the cosmetic are hesperidin, panthenol, adenosine, ginkgo biloba extract and heparin, and the cosmetic comprises the following components in parts by weight:

the humectant and thickener can be selected conventionally in the art. For example, the humectant can be selected from glycerol, xylitol, erythritol, betaine, ceramide, hyaluronic acid, Tremella polysaccharide, etc., and the thickener can be selected from xanthan gum, carbomer, hydroxyethyl cellulose, flaxseed gum, etc.

The raw materials and auxiliary materials used in the invention can be obtained commercially.

The active composition provided by the invention better promotes skin microcirculation by exerting a synergistic effect among the components. Some of the embodiments provide a supramolecular-recognized self-assembled active composition which can also play a sustained release role, and has the advantage of remarkably prolonging the action time. The active composition can be directly applied and used, and can also be used as an active ingredient to be added into other skin care products for use. The active composition provided by the invention is used for preparing skin care products, is safe and non-irritant, can obviously reduce skin TEWL, and has the effects of keeping moisture for a long time, nourishing skin cells and accelerating self renewal of skin.

Detailed Description

The following examples are intended to illustrate the invention but are not intended to limit the scope of the invention. The examples do not show the specific techniques or conditions, according to the technical or conditions described in the literature in the field, or according to the product specifications. The reagents or instruments used are conventional products available from regular distributors, not indicated by the manufacturer.

Hesperidin is purchased from Beijing GmbH of Kuer chemical technology, and has a purity of more than 95%; panthenol is purchased from basf (china) ltd and has a purity of 98%; adenosine was purchased from Shanghai Michelin Biochemical Co., Ltd, and had a purity of 99.5%; the folium Ginkgo extract is obtained from Shanghai Michelin Biochemical technology limited, and purified at a ratio of 10:1, and the content of total flavonoids in folium Ginkgo is not less than 24.0%; heparin was purchased from Shanghai Aladdin Biotechnology Ltd with a purity of 180USP units/mg or more.