CN110755310B - Active composition for promoting skin microcirculation and preparation method and application thereof - Google Patents
Active composition for promoting skin microcirculation and preparation method and application thereof Download PDFInfo
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics 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
- A61K8/9771—Ginkgophyta, e.g. Ginkgoaceae [Ginkgo family]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
- A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
- A61K31/727—Heparin; Heparan
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/16—Ginkgophyta, e.g. Ginkgoaceae (Ginkgo family)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/42—Amides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/60—Sugars; Derivatives thereof
- A61K8/602—Glycosides, e.g. rutin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/60—Sugars; Derivatives thereof
- A61K8/606—Nucleosides; Nucleotides; Nucleic acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/73—Polysaccharides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
Abstract
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.
Description
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 a polydisaccharide formed by repeatedly and alternately connecting 2-iduronic acid sulfate and glucosamine disulfate through beta-1, 4 and alpha-1, 4 glycosidic bonds, and the relative molecular mass is 15000-30000. Heparin is ubiquitous in mammals. Heparin is obtained from the mucous membrane of the pig duodenum, and the product is usually in the form of its sodium salt. Heparin is a commonly used anticoagulant, and in external use, the heparin has a repairing effect on scars, can effectively promote the proliferation of endothelial cells of local blood vessels of wounds, simultaneously activates the endothelial cells at the damaged parts, can release endogenous WTW, and further enhances the proliferation of the endothelial cells, the generation of new blood vessels, the proliferation of fibroblasts, the generation of granulation tissues and the formation of collagen and matrix, thereby accelerating the healing process of the wounds and preventing the roughening of the skin; can improve microcirculation, recover or increase local blood circulation, and can eliminate dark eye and regulate skin color when used in facial products; the liver essence has antiinflammatory and moisture keeping effects. In some embodiments of the invention, the heparin purity is greater than or equal to 180USP units/mg.
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 also comprises an ultrasonic treatment step, under the promotion of ultrasonic cavitation, on one hand, molecular motion is intensified, collision opportunities among molecules are increased, 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 beta-glucan with molecular weight more than 50 ten thousand daltons, are interrupted, the polymerization degree is reduced, the self-assembly among the molecules is more facilitated, and in addition, the small molecular materials are also beneficial to the osmotic absorption of the 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.
Example 1 active composition for promoting skin microcirculation and preparation thereof
The composition formula comprises:
the preparation method comprises the following steps: mixing hesperidin, panthenol, adenosine, folium Ginkgo extract, and heparin, slowly adding pure water, and stirring until the system is clear and transparent. Then adding proper amount of citric acid to adjust the pH value to be 5.0 +/-0.2, transferring the product into a closed container, carrying out ultrasonic treatment for 60 minutes under the conditions of the frequency of 25Khz and the temperature of 25 ℃, then placing the product into a freezer at the temperature of-25 ℃, freezing for 12 hours, then taking out the product, placing the product into a room temperature for unfreezing for 12 hours, and repeating the freezing-unfreezing for 5 times to obtain the active composition with the supermolecular structure.
Example 2 active composition for promoting skin microcirculation and preparation thereof
The composition formula comprises:
the preparation method comprises the following steps: mixing hesperidin, panthenol, adenosine, folium Ginkgo extract, and heparin, slowly adding pure water, and stirring until the system is clear and transparent. Then adding proper amount of citric acid to adjust the pH value to be 5.0 +/-0.2, transferring the product into a closed container, carrying out ultrasonic treatment for 15 minutes under the conditions of the frequency of 45Khz and the temperature of 25 ℃, then placing the product into a freezer at the temperature of-25 ℃, freezing for 12 hours, then taking out the product, placing the product into a room temperature for unfreezing for 12 hours, and repeating the freezing-unfreezing for 5 times to obtain the active composition with the supermolecular structure.
Example 3 active composition for promoting skin microcirculation and its formulation for preparing the composition:
the preparation method comprises the following steps: mixing hesperidin, panthenol, adenosine, folium Ginkgo extract, and heparin, slowly adding pure water, and stirring until the system is clear and transparent. Then adding proper amount of citric acid to adjust the pH value to be 5.0 +/-0.2, transferring the product into a closed container, carrying out ultrasonic treatment for 35 minutes under the conditions of the frequency of 30Khz and the temperature of 25 ℃, then placing the product into a freezer at the temperature of-25 ℃, freezing for 12 hours, then taking out the product, placing the product into a room temperature for unfreezing for 12 hours, and repeating the freezing-unfreezing for 5 times to obtain the active composition with the supermolecular structure.
Example 4 active composition for promoting skin microcirculation and its preparation composition formula:
the preparation method comprises the following steps: mixing hesperidin, panthenol, adenosine, folium Ginkgo extract, and heparin, slowly adding pure water, and stirring until the system is clear and transparent. Then adding proper amount of citric acid to adjust the pH value to be 5.0 +/-0.2, transferring the product into a closed container, carrying out ultrasonic treatment for 30 minutes under the conditions of the frequency of 35Khz and the temperature of 25 ℃, then placing the product into a freezer at the temperature of-25 ℃, freezing for 12 hours, then taking out the product, placing the product into a room temperature for unfreezing for 12 hours, and repeating the freezing-unfreezing for 5 times to obtain the active composition with the supermolecular structure.
Example 5 active composition for promoting skin microcirculation and preparation of composition formula:
the preparation method comprises the following steps: mixing hesperidin, panthenol, adenosine, folium Ginkgo extract, and heparin, slowly adding pure water, and stirring until the system is clear and transparent. Then adding proper amount of citric acid to adjust the pH value to be 5.0 +/-0.2, transferring the product into a closed container, carrying out ultrasonic treatment for 30 minutes under the conditions of the frequency of 25Khz and the temperature of 25 ℃, then placing the product into a freezer at the temperature of-25 ℃, freezing for 12 hours, then taking out the product, placing the product into a room temperature for unfreezing for 12 hours, and repeating the freezing-unfreezing for 5 times to obtain the active composition with the supermolecular structure.
Example 6 active composition for promoting skin microcirculation and preparation thereof
The composition formula comprises:
the preparation method comprises the following steps: mixing hesperidin, panthenol, adenosine, folium Ginkgo extract, and heparin, slowly adding pure water, and stirring until the system is clear and transparent to obtain active composition.
Example 7 active composition for promoting microcirculation of the skin and preparation thereof
The composition formula comprises:
the preparation method is basically the same as that of example 5.
Example 8 active composition for promoting skin microcirculation and preparation thereof
The composition formula comprises:
the preparation method is basically the same as that of example 5.
Example 9 active composition for promoting skin microcirculation and preparation thereof
The composition formula comprises:
the preparation method is basically the same as that of example 5.
Test example 1 test of skin microcirculation regulating active composition
The purpose of the test is as follows: the microcirculation regulating effect of the skin microcirculation regulating active composition is examined.
The test instrument: laser doppler blood flow (Biopac system, usa), capillary microcirculation (tin-free medical equipment).
Subject: 12 women of age 45-50 were selected and randomized into control and study groups of 6 individuals, with the study group starting at 8 am each day and testing 1 single dose group or composition per day.
The test method comprises the following steps: the subject enters a thermostatic chamber with the temperature of 25 ℃ to ensure that the body adapts to the environmental temperature, and after the test is started, the subject lies on the bed in the supine position and is in a quiet state without any limb movement and severe conscious activity. The probe of the laser Doppler blood flow instrument is adjusted when the middle finger nail is wrinkled, the position of blood perfusion volume about 4.0mL/s is searched and marked, and the later tests are all carried out at the changed position. After the medicine is applied, the security detection probe is fixed, the nail wrinkle blood perfusion amount is recorded after the nail wrinkle blood perfusion amount is stabilized for 5 minutes, and the value is used as a basic value. Every 5 minutes thereafter, 1 minute each, was averaged and observed for 30 minutes. Data are presented as mean ± standard deviation using SPSS11.0 as statistical software, and single-factor analysis of variance (ANOVA) between groups with a statistically significant level P < 0.05.
The results of the tests are shown in table 1 below:
TABLE 11% Change in the amount of blood perfused through the crinkled skin following topical microcirculation-regulating drug concentration: (mL/s)
The above test results show that the compositions of examples 1 to 6 of the present invention have good skin microcirculation regulating ability, blood flow under the same conditions is significantly higher than that of each active ingredient group, and the compositions have a tendency of gradually increasing blood flow over time to a stable value. The composition of example 6, which was not treated to self-assemble by supramolecular recognition, showed no tendency to increase in blood flow velocity with time, although initially high.
Example 10 facial anti-aging essence for promoting skin microcirculation and preparation thereof
The formula is as follows:
the preparation method comprises the following steps: adding xanthan gum as a thickening agent, beta-glucan as a humectant and hyaluronic acid into hot water at 40 ℃, and homogenizing for 5 minutes to fully swell; cooling to room temperature of 25 deg.C, sequentially adding hesperidin, panthenol, adenosine, folium Ginkgo extract, heparin, 1, 2-hexanediol, 1, 2-pentanediol, ethylhexyl glycerol and flos Rosae Davuricae water, and stirring.
Example 11 facial anti-aging essence for promoting skin microcirculation and preparation thereof
The formula is as follows:
the preparation method comprises the following steps: adding xanthan gum as a thickening agent, betaine as a humectant and erythritol into hot water at 40 ℃, and homogenizing for 5 minutes to fully swell; cooling to room temperature of 25 deg.C, sequentially adding hesperidin, panthenol, adenosine, folium Ginkgo extract, heparin, 1, 2-hexanediol, 1, 2-pentanediol, ethylhexyl glycerol and flos Rosae Davuricae water, and stirring.
Example 12 preparation of facial anti-aging essence for promoting skin microcirculation
The formula is as follows:
the preparation method comprises the following steps: adding xanthan gum as a thickening agent, betaine as a humectant and erythritol into hot water at 40 ℃, and homogenizing for 5 minutes to fully swell; cooling to room temperature of 25 deg.C, sequentially adding hesperidin, panthenol, adenosine, folium Ginkgo extract, heparin, 1, 2-hexanediol, 1, 2-pentanediol, ethylhexyl glycerol and flos Rosae Davuricae water, and stirring.
Example 13 facial anti-aging essence for promoting skin microcirculation and preparation thereof
The formulation is the same as in example 10; the preparation method comprises preparing active components of hesperidin, panthenol, adenosine, folium Ginkgo extract and heparin into active composition by the same method as in example 5, and adding other adjuvants to make into essence.
Example 14 facial anti-aging essence for promoting skin microcirculation and preparation thereof
The formulation is the same as in example 11; the preparation method comprises preparing active components of hesperidin, panthenol, adenosine, folium Ginkgo extract and heparin into active composition by the same method as in example 5, and adding other adjuvants to make into essence.
Example 15 facial anti-aging essence for promoting skin microcirculation and preparation thereof
The formulation was the same as in example 12; the preparation method comprises preparing active components of hesperidin, panthenol, adenosine, folium Ginkgo extract and heparin into active composition by the same method as in example 5, and adding other adjuvants to make into essence.
Test example 2 Performance test of facial anti-aging essence for promoting skin microcirculation
1. Stability test
1) Stability of acceleration
A proper amount of the samples prepared in the embodiments 10 to 15 of the invention are put into a centrifuge tube, the tube mouth is sealed, and the samples are centrifuged at 3000rpm for 30 minutes, so that the phenomena of suspended matters, precipitates and oil slick are not observed, and the original appearance is kept.
2) Stability test
The samples prepared in the examples 10 to 15 of the present invention were examined for 3 months at 4 ℃, 25 ℃, 37 ℃ and 60 ℃ for weekly sampling and observation, and the results showed that the samples in the examples 6 to 8 of the present invention maintained clear and transparent appearance under these four conditions, and no suspended matter, precipitation, oil slick, etc. appeared.
2. Safety test (human skin patch test)
Selecting 20 healthy subjects with no allergic history of skin diseases between the ages of 20 and 50, and performing a spot pasting method: selecting a qualified spot tester, dropping about 15 microliters of samples of the embodiments 10-15 of the invention into the spot tester in a closed spot-patch test mode, externally applying a special adhesive tape to the back of a subject, respectively sticking 50 spot testers to each subject, respectively sticking the essence samples of the embodiments 10-15, removing the tested substances after 24 hours, observing skin reactions after 0.5, 6, 12, 24 and 48 hours after removal, and recording the results according to the skin reaction grade standard in the cosmetic hygiene standard.
And (3) test results: the results of the human skin patch test show that all the subjects pass the patch test, and the skin reaction is observed in 0.5, 6, 12, 24 and 48 hours, wherein 0 case has adverse reactions such as skin erythema, pimple and blister, which indicates that the product of the invention is safe and non-irritant.
3. Effect testing
1) Testing of skin moisture loss through skin
30 healthy subjects are selected, the age is 25-50, the room temperature (25 +/-1) DEG C and the relative humidity (40 +/-5)%, and the testers are required to enter the test environment 30 minutes in advance. The tested area (4cm multiplied by 4cm) is marked on the inner side of the arm of the tester, a plurality of areas (1 cm apart) can be marked on the same arm at the same time, and the test samples are distributed randomly. The blank value of each test area is tested, and then the test sample is (2.0 +/-0.1) mg/cm2The amount of (c) was applied in a single application, and the transepidermal water loss (TEWL) was measured in 0, 1,2, 4 hours test area and blank area after application using a skin water loss tester, each area was measured in parallel 5 times, the blank control area was no sample applied. The results are shown in table 2 below:
TABLE 2 skin moisture loss at various times (%)
Test sample | 0 hour | 1 hour | 2 hours | 4 hours | 8 hours |
Blank control group | 16.51 | 16.40 | 16.71 | 16.55 | 16.45 |
Example 10 | 16.60 | 10.84 | 9.64 | 9.75 | 9.21 |
Example 11 | 16.88 | 8.55 | 8.69 | 8.87 | 8.51 |
Example 12 | 16.59 | 9.08 | 8.56 | 8.49 | 8.94 |
Example 13 | 16.37 | 6.21 | 5.23 | 5.01 | 3.56 |
Example 14 | 16.21 | 5.56 | 4.19 | 3.94 | 3.25 |
Example 15 | 16.35 | 6.09 | 4.85 | 3.88 | 3.19 |
As can be seen from table 2 above, the composition of the present invention can significantly reduce skin TEWL, and has the effects of maintaining moisture for a long time, nourishing skin cells, and accelerating self-renewal of skin. In particular, the compositions of examples 13-15 are more effective, mainly due to the fact that the skin water loss is significantly reduced over time, since the supramolecular self-assembling treated compositions slowly release the active agent at a rate when in contact with the skin.
Although the invention has been described in detail hereinabove with respect to a general description and specific embodiments thereof, it will be apparent to those skilled in the art that modifications or improvements may be made thereto based on the invention. Accordingly, such modifications and improvements are intended to be within the scope of the invention as claimed.
Claims (14)
1. An active composition having skin microcirculation promoting effect, wherein the active components comprise:
the preparation method of the active composition with the effect of promoting skin microcirculation comprises the following steps: 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.
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 production method according to claim 4, wherein the pH is adjusted to 4.5 to 6.0; 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 5, wherein the pH is adjusted to between 4.5 and 5.5.
7. The method according to any one of claims 4 to 6, wherein the freezing is performed at a temperature of 0 ℃ to-30 ℃; and/or the time for each thawing is 1-20 hours.
8. The method of claim 7, wherein the time for each freezing is 1 to 20 hours.
9. The method of any one of claims 4-6, 8, further comprising a step of sonication before said freezing.
10. The method of claim 9, wherein the sonication conditions are: the ultrasonic frequency is 20-55KHz, and the ultrasonic treatment time is 15-120 minutes.
11. An active composition prepared by the process of any one of claims 5-10.
12. Use of an active composition according to any one of claims 1 to 3, 11 for the preparation of a pharmaceutical, cosmetic or biological material.
13. A cosmetic comprising the active composition according to any one of claims 1 to 3 or 11.
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CN105395443A (en) * | 2015-11-18 | 2016-03-16 | 关美玲 | Anti-aging eye cream and preparation method thereof |
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CN1907255A (en) * | 2005-08-02 | 2007-02-07 | 赵勤 | Skin caring cream with microcirculation activator |
KR20150083652A (en) * | 2014-01-10 | 2015-07-20 | 주식회사 엘지생활건강 | Composition for Complexion Improvement |
CN105395443A (en) * | 2015-11-18 | 2016-03-16 | 关美玲 | Anti-aging eye cream and preparation method thereof |
CN109498487A (en) * | 2018-11-27 | 2019-03-22 | 广州伽德中医药科技有限公司 | Cosmetic composition and its preparation method and application is repaired in a kind of moisturizing |
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