Whitening composition with enhanced penetration and synergy

Abstract

The invention discloses a whitening composition for promoting penetration and enhancing efficacy, comprising: a whitening component; a Chinese medicine extract; and a polyol, wherein the Chinese medicine extract is prepared by the following raw materials: Poria, Tribulus, Ampelopsis, Paeonia, Atractylodes, Bletilla striata and Dictamni, wherein the weight ratio of Poria: Tribulus: Ampelopsis: Paeonia: Atractylodes: Bletilla striata: Dictamni is 1:1-4:4-10:8-10:1-4:1-4:1-4, wherein the polyol is a mixture of butanediol and ethylhexylglycerol in a weight ratio of 9:1. The invention also relates to a freeze-dried product comprising the whitening composition and skin whitening applications of the whitening composition and the freeze-dried product.

Description

Technical Field

[0001] The present invention relates to the fields of natural drug chemistry and cosmetics, and in particular to a traditional Chinese medicine composition with whitening, anti-oxidation and skin-lightening effects, a preparation method and application of the traditional Chinese medicine composition. Background Art

[0002] Traditional Chinese medicine is a treasure of the Chinese nation. It has made indelible contributions to the prosperity of the Chinese nation for thousands of years and has received more and more attention and attention from people around the world. However, due to the disconnection between traditional Chinese medicine theory and modern scientific theory and the relatively backward research methods of Chinese medicine, the development and utilization of Chinese medicine resources have been greatly affected and restricted. The development of Chinese medicine is currently mainly limited to finding effective ingredients from existing Chinese medicines and developing various extraction methods to enrich and optimize effective ingredients. However, improving the development potential, application efficiency and new application scenarios of Chinese medicine based on existing Chinese medicine resources has not yet attracted widespread attention. In particular, combining the advantages of traditional Chinese medicine with modern cosmetic formulation technology to realize the modernization of Chinese medicine is an important means to promote the development of Chinese medicine.

[0003] Modern Chinese herbal cosmetics, with their adherence to the wisdom of traditional Chinese medicine and holistic concepts, use Chinese herbal ingredients that not only enhance the functionality of Chinese herbal cosmetics, but also make them multifunctional, and have natural properties, i.e., high safety, low toxicity and side effects, and easy utilization and absorption, which have broad development and application prospects. With the progress of society and the development of science and technology, people's understanding of skin problems continues to deepen, such as the mechanism of aging, whitening mechanism, sensitive mechanism, etc. Chinese people believe that having fair, shiny, and translucent skin can cover the aging of the face.

[0004] The current research hotspot is the role and effectiveness of the entire whitening chain, which includes but is not limited to 1) the stimulation of reactive oxygen species under the action of ultraviolet rays; 2) the activating factor that stimulates melanocytes produced in keratinocytes; 3) the stimulation pathway of melanocyte activating factor; 4) the production of tyrosinase protein in melanocytes; 5) tyrosinase activation and its reaction chain; 6) the transfer of melanin carried by melanosomes; 7) the metabolism of melanin transferred into keratinocytes; from the perspective of the mechanism and mechanism of whitening, the above main links must be regulated to prevent possible pigmentation, the formation of spots and spots, and dull skin.

[0005] Although the TCM theory system and molecular biology belong to two different thought systems, the material basis for studying life activities is the same, and they are the products of human understanding and exploration of life and health to varying degrees. For example, TCM theory believes that the aging mechanism is the view that "when qi and blood are not harmonious, all diseases will arise", that is, qi deficiency and blood stasis are the root cause of aging. Modern medicine believes that qi deficiency and blood stasis are caused by poor microcirculation, poor blood fluidity, and poor metabolism inside the skin. Therefore, studying TCM theory and TCM from the molecular level and applying TCM theory and other new achievements of modern TCM to modern biological technology are of great significance to promoting the integration of Chinese and Western medicine and promoting the development of medicine in beauty and skin care. From the perspective of modern medical research, Chinese herbal medicines are rich in nutrients such as proteins, lipids, amino acids, polysaccharides, pectin, vitamins, trace elements, organic acids, alkaloids, saponins, etc., which have skin care effects such as promoting cell proliferation and metabolism, improving skin microcirculation, enhancing the body's antioxidant capacity, resisting ultraviolet damage, inhibiting whitening link reactions, moisturizing and repairing the skin barrier. From the perspective of traditional Chinese medicine, Chinese herbal medicine can regulate the balance of yin and yang, regulate qi and blood, regulate internal organs and delay aging. Therefore, the social and economic benefits of applying Chinese herbal medicine to the development of cosmetics are promising.

[0006] The present invention unexpectedly discovered that a Chinese herbal medicine extract comprising Poria cocos, Tribulus terrestris, Ampelopsis pilosula, Paeonia lactiflora, Atractylodes macrocephala, Bletilla striata and Dictamni cortex has the effects of whitening, anti-oxidation and brightening skin tone, and can also be combined with additional whitening ingredients for application in cosmetics. Summary of the invention

[0007] In one aspect, the present invention provides a whitening composition for promoting penetration and enhancing efficacy, comprising:

[0008] Whitening ingredients;

[0009] Chinese herbal medicine extracts; and

[0010] Polyols,

[0011] The Chinese medicine extract is prepared from the following raw materials: Poria, Tribulus, Bletilla striata, Paeonia lactiflora, Atractylodes macrocephala, Bletilla striata and Dictamni cortex, wherein the weight ratio of Poria: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex is 1:1-4:4-10:8-10:1-4:1-4:1-4,

[0012] Wherein, the polyol is a mixture of butanediol and ethylhexylglycerol in a weight ratio of 9:1.

[0013] In a preferred embodiment, the whitening ingredient is selected from: niacinamide, ascorbyl glucoside or a combination thereof.

[0014] In a preferred embodiment, the weight ratio of Poria cocos:Tribulus terrestris:Bletilla striata:Paeonia lactiflora:Atractylodes macrocephala:Bletilla striata:Cortex Dictamni is 1:1-2:4-8:8-10:1-4:1-4:1-2.

[0015] In a preferred embodiment, the Chinese herbal medicine extract is prepared by solvent extraction. In a more preferred embodiment, the solvent extraction adopts a water extraction and alcohol precipitation method.

[0016] In a preferred embodiment, the weight ratio of the Chinese herbal medicine extract to the polyol is 1:10.

[0017] In a preferred embodiment, the whitening composition of the present invention comprises 10-50% by weight of the Chinese herbal medicine extract.

[0018] In another aspect, the present invention also relates to a freeze-dried product of the whitening composition.

[0019] In yet another aspect, the present invention also relates to use of the whitening composition or freeze-dried product in skin whitening.

[0020] In yet another aspect, the present invention also relates to an external skin preparation comprising the whitening composition or the freeze-dried product. BRIEF DESCRIPTION OF THE DRAWINGS

[0021] The present invention is further described below in conjunction with the accompanying drawings.

[0022] Figure 1 The HPLC spectrum of PGG of the Chinese medicine extract of Example 4 is shown.

[0023] Figure 2 Results for the apparent chromaticity of the model melanin content are shown.

[0024] Figure 3 The results of the laser Raman confocal microscopy on the permeability are shown. The left side of the figure represents Example 43, and the right side represents Nicotinamide VB3. DETAILED DESCRIPTION OF THE INVENTION

[0026] The purpose of the present invention is to improve the efficacy of the traditional Chinese medicine complex by synergistic combination, increase the content of active ingredients through an extraction process, improve the special smell and color of the traditional Chinese medicine complex, improve the bioavailability of the traditional Chinese medicine complex, and combine it with modern cosmetic technology to provide a traditional Chinese medicine composite product with better skin pigmentation inhibition effect. The product can be directly used on the skin and can also be added to the cosmetic formula as an effective additive, thereby greatly improving the efficacy of the cosmetic application and having a low cost.

[0027] The invention is based on the research results of multiple ancient books and modern Chinese herbal medicine, and multiple ancient Chinese medicine prescriptions are compounded to obtain a beauty prescription with better compound Chinese medicine compatibility theory. The invention adopts Poria cocos, Tribulus terrestris, Ampelopsis pilosula, Paeonia lactiflora, Atractylodes macrocephala, Bletilla striata and Dictamni to obtain Chinese medicine extracts.

[0028] The present invention uses modern Chinese herbal medicine extraction methods and processes to pre-treat the ancient Chinese medicine prescription. In a preferred embodiment, the Chinese herbal medicine extract of the present invention includes crushing the Chinese herbal medicine raw materials before solvent extraction. For example, a high-speed universal crusher (FW100 model) can be used to crush the mixture of Chinese herbal medicine raw materials.

[0029] The present invention also utilizes concentration, purification and other processes to improve and increase the content of active substances in the Chinese medicine compound extract. In some embodiments, a Chinese medicine extraction and concentration tank (TNH type) is used to achieve concentration.

[0030] The present invention utilizes cosmetic technology to further improve the bioavailability of active ingredients of Chinese herbal medicine to the skin and enhance the whitening effect.

[0031] Unless otherwise defined, all scientific and technical terms used herein have the same meaning as those commonly understood by those of ordinary skill in the art to which the present invention belongs. In addition, all publications, patent applications, patents and other references mentioned herein are incorporated herein by reference. Unless otherwise indicated, percentages refer to weight percentages.

[0032] Chinese herbal medicine

[0033] Peony is the dried root of Paeonia lactiflora Pall, a plant of the Ranunculaceae family. It contains paeoniflorin, paeonol, paeonin, benzoic acid, volatile oil, fatty oil, resin, tannin, sugar, starch, mucilage, protein, β-sitosterol and triterpenes.

[0034] Ampelopsis japonica (Thunb.) Makino is a dried root tuber of the grape family Ampelopsis japonica (Thunb.) Makino, which contains mucilage and starch.

[0035] Tribulus terrestris is the dried mature fruit of Tribulus terrestris L., a plant of the Tribulaceae family. The roots and leaves contain saponins, and the aglycones include diosgenin, gitogenin, chlorogenin, and ruscogenin. The leaves also contain kaempferol and a variety of kaempferol glycosides.

[0036] Atractylodes is the dried rhizome of Atractylodes macrocephala Koldz. of the Asteraceae family. It contains 1.4% volatile oil, the main components of which are atractylol, atractylon, etc., and also contains vitamin A.

[0037] Poria cocos is the dried sclerotium of the Polyporaceae fungus Poria cocos (Schw.) Wolf, which contains β-Pachyman, which accounts for about 93% of the dry weight, and triterpenoid compounds such as acetylated pachymic acid, tumulosic acid, and 3β-hydroxylanostatrienoic acid [3β-Hydroxylanosta-7,9(11),24-trien-21-oil acid]. In addition, it also contains gum, chitin, protein, fat, sterol, lecithin, glucose, adenine, histidine, choline, β-Pachyman decomposing enzyme, lipase, protease, etc.

[0038] Dictamnus dasycarpus Turcz. is a dried root bark of the Rutaceae plant, containing Dictamnine, Dictamnolactone, Obaculactone, Limonin, Sitosterol, Obacunonic acid, Trigonelline, Choline, Fraxinellone. It also contains Campesterol, Skimmianin, γ-Fagarin, Dasycarpamin. The above-ground part contains Psoralen and Xanthotoxin.

[0039] Bletilla striata is the dried tuber of Bletilla striafa (Thunb.) Reichb.f., a plant of the orchid family. Its fresh tuber contains 14.6% water, 30.48% starch, and 1.5% glucose. It also contains volatile oil and mucilage. The root contains Bletilla mannan, which is a glucomannan composed of 4 parts of mannose and 1 part of glucose.

[0040] Following the idea of ​​traditional Chinese medicine beauty formula, the formula is still based on the ingredients that nourish both yin and yang, namely Paeonia lactiflora Pall and Ampelopsis japonica (Thunb Vlakino) as the main medicines; the auxiliary medicines are Tribulus terrestris L and Atractylodes macrocephala Koidz, which are warming Chinese herbs; Poria cocos (Schw.) Wolf and Dictamnus dasycarpus Turcz are added as adjuvants; and Bletilla striata Thunb Reichb.f. is used as the guiding medicine. The formula is identified with reference to the 2015 edition of the Chinese Pharmacopoeia, Volume 1, and the Flora of China. The formula is simplified as much as possible to form a simple formula for balanced beauty, so as to meet the requirements of later extraction and purification technologies.

[0041] Chinese herbal extracts

[0042] This application is the first to combine Poria cocos, Tribulus terrestris, Bletilla striata, Paeonia lactiflora, Atractylodes macrocephala, Bletilla striata and Dictamni to extract, and the various herbs in the obtained compound Chinese medicine extract complement each other to achieve the effects of anti-glycation, anti-yellowing, whitening and brightening skin color.

[0043] In some embodiments, the weight ratio of raw materials Poria cocos: Tribulus terrestris: Ampelopsis radix: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex in the Chinese medicine extract of the present invention is 1:1-4:4-10:8-10:1-4:1-4:1-4. In a specific embodiment, the weight ratio of raw materials Poria cocos: Tribulus terrestris: Ampelopsis radix: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex in the Chinese medicine extract of the present invention is 1:4:10:10:1:4:4. In a specific embodiment, the weight ratio of raw materials Poria cocos: Tribulus terrestris: Ampelopsis radix: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex in the Chinese medicine extract of the present invention is 1:2:8:10:4:1:2. In a specific embodiment, the weight ratio of raw materials Poria cocos: Tribulus terrestris: Ampelopsis radix: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex in the Chinese medicine extract of the present invention is 1:1:10:10:4:1:1. In a specific embodiment, the weight ratio of the raw materials Poria cocos: Tribulus terrestris: Ampelopsis radix: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex in the Chinese medicine extract of the present invention is 1:1:4:10:4:1:1. In a specific embodiment, the weight ratio of the raw materials Poria cocos: Tribulus terrestris: Ampelopsis radix: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex in the Chinese medicine extract of the present invention is 1:1:4:10:2:1:1. In a specific embodiment, the weight ratio of the raw materials Poria cocos: Tribulus terrestris: Ampelopsis radix: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex in the Chinese medicine extract of the present invention is 1:2:4:8:4:1:2.

[0044] The Chinese medicinal extract of the present invention can be added into cosmetics as an effective additive to achieve the effects of anti-glycation, yellowing, whitening and brightening skin tone.

[0045] Extraction method

[0046] The Chinese herbal extract of the present invention is prepared by solvent extraction. Common extraction solvents include, but are not limited to, water (e.g., deionized water) and organic solvents (e.g., ethanol). There are other extraction methods, including microwave extraction, supercritical carbon dioxide extraction, ultrasonic extraction, enzyme extraction, etc.

[0047] In some embodiments, the Chinese medicine extract of the present invention is prepared by water extraction and alcohol precipitation. For example, the Chinese medicine extract of the present invention is extracted by boiling with deionized water, and then precipitated with alcohol to obtain a filtrate to obtain the desired Chinese medicine extract. In a specific embodiment, ethanol is used in the alcohol precipitation process. In some embodiments, the extraction process of water extraction and alcohol precipitation lasts for 1-24 hours. In some embodiments, the extraction process of water extraction and alcohol precipitation lasts for 12-16 hours.

[0048] In some embodiments, the Chinese medicine extract of the present invention uses alcohol as an extraction solvent. For example, the Chinese medicine extract of the present invention can be extracted with ethanol. In a preferred embodiment, the extraction process is carried out under boiling conditions (e.g., 80 ± 10 ° C). In a preferred embodiment, 70% by volume ethanol can be used for extraction. In some embodiments, the alcohol extraction process lasts for 2-4 hours.

[0049] Post-treatment products of Chinese herbal medicine extracts and polyols

[0050] The present invention combines the Chinese herbal medicine extract with polyol to form a post-processed product. In a preferred embodiment, the Chinese herbal medicine extract and the polyol are combined in a weight ratio of 1:10.

[0051] The term "polyol" used in the present invention refers to a water-soluble polyol having two or more hydroxyl groups in the molecule, including but not limited to: glycerol, diglycerol, butylene glycol, pentanediol, propylene glycol, ethylhexylglycerol, polyethylene glycol, sorbitol, etc. Polyols are commonly used as moisturizers in cosmetics, absorbing moisture from the environment, replenishing it into the skin, and increasing the water content of the skin surface. Polyols can be used alone, or they can be used in combination. For example, two or more polyols can be used in combination.

[0052] In some embodiments, the herbal extract of the present invention is combined with a mixture of pentylene glycol and propylene glycol in a weight ratio of 9: 1. In some embodiments, the herbal extract of the present invention is combined with a mixture of polyethylene glycol and caprylyl glycol in a weight ratio of 5:5.

[0053] From the perspective of softening the cell membrane layer and the stratum corneum, butylene glycol, pentylene glycol, and ethylhexylglycerol are preferred. Therefore, in a preferred embodiment, the Chinese herbal extract is combined with a mixture of butylene glycol and ethylhexylglycerol in a weight ratio of 9:1.

[0054] Whitening composition

[0055] The post-processed product formed by combining the Chinese herbal medicine extract with the polyol can be further combined with a whitening component to form a whitening composition.

[0056] Vitamin C / derivatives are safe whitening ingredients with strong antioxidant properties. They can improve facial dullness, while effectively inhibiting the activity of tyrosinase and the formation of melanin, providing a root whitening effect.

[0057] Nicotinamide is a water-soluble vitamin and a member of the vitamin B family. It can be converted from nicotinic acid in vivo and has a vitamin effect. Ascorbic acid 2-glucoside (AA2G) is a derivative of vitamin C and also has a vitamin effect. However, the transdermal permeability of nicotinamide and ascorbic acid 2-glucoside has always been one of the core issues that have not been resolved.

[0058] Combining the active ingredients ascorbyl glucoside and / or niacinamide with the post-processed product of the Chinese herbal extract and polyols of the present invention can significantly improve the gloss and transparency of the skin, making the skin "translucent white" and the surface clean and bright. Whitening active ingredients, vitamin C / derivatives, and niacinamide can inhibit melanin from the source, and the combined niacinamide further cuts off the transmission of melanin to the epidermal cells of the skin to prevent spots, and at the same time can help the skin to remove endogenous yellowing and improve dullness, so that the whitening / brightening effect of the product can be maximized.

[0059] The present invention provides a whitening composition comprising niacinamide and / or ascorbyl glucoside.

[0060] In some embodiments, the whitening composition of the present invention comprises 1-5 wt% nicotinamide. In a preferred embodiment, the whitening composition of the present invention comprises 3 wt% nicotinamide.

[0061] In some embodiments, the whitening composition of the present invention comprises 0.1-2 wt% ascorbyl glucoside. In a preferred embodiment, the whitening composition of the present invention comprises 0.1-1 wt% ascorbyl glucoside.

[0062] In some embodiments, the whitening composition of the present invention comprises 10-50% by weight of the post-treatment. In some embodiments, the whitening composition of the present invention comprises 10-30% by weight of the post-treatment. In some embodiments, the whitening composition of the present invention comprises 30-50% by weight of the post-treatment.

[0063] Freeze-dried products

[0064] The present invention also relates to a freeze-dried product of a Chinese herbal medicine extract. In some embodiments, the freeze-dried product may be an amorphous powder.

[0065] In some embodiments, freeze-drying is performed using a vacuum freeze dryer model FD-2 produced by Beijing Boyikang Laboratory Instrument Co., Ltd.

[0066] In some embodiments, freeze drying is set at -80 to -40°C, vacuum degree 1 to 30Pa, time 8 hours, sublimation drying is set at -20 to +20°C, vacuum degree 1 to 30Pa, time 6 hours, and the water content is controlled between 0 and 6%; analytical drying is set at -10 to +20°C, vacuum degree 1 to 30Pa, time 3 hours, and the water content is controlled between 0 and 6%.

[0067] Skin topical products

[0068] The present invention also relates to an external skin preparation, which comprises the whitening composition of the present invention or a lyophilized product thereof, and a cosmetically, dermatologically or pharmaceutically acceptable excipient.

[0069] In some preferred embodiments, the amount of the whitening composition is 0.001-50% (w / w), preferably 1-20% (w / w), more preferably 2-10% (w / w), and most preferably 3-8% (w / w), based on the total weight of the external skin preparation.

[0070] The skin external application composition is a general concept of all ingredients usually used on the outside of the skin, for example, it can be a cosmetic composition or a pharmaceutical composition. The cosmetic composition can be a basic cosmetic, a facial makeup cosmetic, a body cosmetic, a hair care cosmetic, etc. There is no special restriction on its dosage form, and it can be reasonably selected according to different purposes.

[0071] This skin external preparation can be formulated into any suitable product form. Such product forms include, but are not limited to, aerosol sprays, creams, emulsions, solids, liquids, dispersions, foams, gels, lotions, mousses, ointments, powders, patches, pomades, solutions, hand-pump sprays, sticks, facial masks and wet tissues. This skin external preparation can be conveniently used for preparation or as a cosmetic, dermatological or pharmaceutical topical application product by various methods well known in the art.

[0072] The skin topical composition of the present invention may include one or more of the following ingredients: antiallergic agents, antimicrobial agents, antioxidants, chelating agents, colorants, depigmenting agents, emollients, emulsifiers, exfoliants, film formers, fragrances, moisturizers, insect repellents, lubricants, pharmaceutically active agents, moisturizers, photostabilizers, preservatives, skin care agents, skin penetration enhancers, sunscreens, stabilizers, surfactants, thickeners, viscosity regulators, vitamins or any combination thereof.

[0073] The cosmetic, dermatological or pharmaceutically acceptable excipients that can be used for the skin topical composition of the present invention are in the form of an aqueous phase, an oil phase, a gel, a wax-in-water emulsion, an oil-in-water emulsion or an oil-in-water emulsion. The aqueous phase is a mixture of one or more water-soluble or dispersible components, which can be liquid, semi-solid or solid at room temperature (25° C.). The excipient includes or can be in the form of a suspension, dispersion or solution in water or a water-alcohol excipient, which can contain a thickener or a gelling agent. Those skilled in the art can select a suitable product form based on the knowledge mastered by those skilled in the art, the components contained therein.

[0074] The composition may include an aqueous phase, which may contain water or a mixture of water and at least one hydrophilic organic solvent, such as an alcohol, especially a linear or branched lower monohydric alcohol containing 2 to 5 carbon atoms, such as ethanol or propanol; a polyol, such as propylene glycol, sorbitol, glycerol, panthenol or polyethylene glycol, and mixtures thereof.

[0075] When the composition of the invention is in the form of an emulsion, the composition may also optionally contain a surfactant.

[0076] The composition may also comprise a film-forming polymer, such as polyurethanes, polyacrylic acid homopolymers or copolymers, polyesters, hydrocarbon-based resins and / or silicone resins. The polymer may be dissolved or dispersed in a cosmetically acceptable vehicle and optionally combined with a plasticizer.

[0077] The composition of the present invention may also comprise an oil phase, which contains an oil-soluble or oil-dispersible component that is liquid at room temperature (25° C.) and / or an oily or waxy substance at room temperature, such as wax, semisolid, gum and a mixture thereof. The oil phase may also contain an organic solvent.

[0078] Suitable oily substances are usually liquid at room temperature and include: hydrocarbon-based oils of animal origin, such as fully hydrogenated squalene; hydrocarbon-based vegetable oils, such as liquid C4-10 fatty acid triglycerides, for example heptanoic acid or caprylic acid triglycerides, or oils, for example sunflower oil, corn oil, soybean oil, grape seed oil, castor oil, avocado oil, caprylic / capric triglycerides, jojoba oil; linear or branched hydrocarbons of mineral or synthetic origin, for example liquid paraffin and its derivatives, vaseline; synthetic esters and ethers, in particular esters of fatty alcohols, for example isopropyl myristate, 2-ethylhexyl palmitate, 2-octyldodecyl stearate, isostearyl isostearate; hydroxylated esters, for example isostearyl lactate, hydroxy octyl stearate, octyl hydroxystearate, octyldodecyl hydroxystearate, heptanoates, caprylates and caprates of fatty alcohols; polyol esters, such as propylene glycol dicaprylate, neopentyl glycol diheptanoate, diethylene glycol diisononanoate and pentaerythritol esters; fatty alcohols containing C12-26, such as octyldodecanol, 2-butyloctanol, 2-hexyldecanol, 2-undecylpentadecanol, oleyl alcohol; fluorinated oils and / or fluorinated silicone oils based on partial hydrocarbons, silicone oils, volatile or non-volatile linear or cyclic polymethylsiloxanes that are liquid or semisolid at room temperature, such as cyclopolydimethylsiloxanes and polydimethylsiloxanes, which optionally contain phenyl groups, such as phenyltrimethicone, siloxanes and mixtures thereof.

[0079] The composition of the present invention may further comprise any components commonly used in the cosmetic field. These components include preservatives, aqueous phase thickeners (extract biopolymers, synthetic polymers) and fat phase thickeners, fragrances, hydrophilic and lipophilic active agents and mixtures thereof.

[0080] The composition of the present invention may also contain an additional particulate phase, which may be a pigment and / or pearlescent agent and / or filler used in cosmetic compositions.

[0081] Pigments may be present in the composition, suitable inorganic pigments include titanium, zirconium and cerium oxides as well as zinc oxide, iron oxide and ferric blue; suitable organic pigments include barium, strontium, calcium and aluminium lakes and carbon black.

[0082] Pearlescent agents may be present in the composition. Suitable pearlescent agents include mica coated with titanium oxide, iron oxide or natural pigments.

[0083] Fillers may be present in the composition, suitable fillers include talc, silica, zinc stearate, mica, kaolin, nylon powder, polyethylene powder, Teflon, starch, boron nitride, copolymer microspheres, such as silicone resin microspheres.

[0084] The oil phase of the composition of the present invention may comprise one or more waxes, gums or mixtures thereof. Waxes include hydrocarbon-based waxes, fluoro waxes and / or silicone waxes and may be derived from plant, mineral, animal and / or synthetic sources. Suitable waxes include beeswax, carnauba wax, candelilla wax, paraffin wax, microcrystalline wax, ozokerite wax; synthetic waxes include polyethylene wax, silicone wax containing C16-45. Gums are generally polydimethylsiloxane or sodium carboxymethylcellulose or extracts, and semisolid substances are generally hydrocarbon-based compounds, such as lanolin and its derivatives.

[0085] The composition of the present invention can be formulated into any suitable product form. Such product forms include, but are not limited to, aerosol sprays, creams, emulsions, solids, liquids, dispersions, foams, gels, lotions, mousses, ointments, powders, patches, pomades, solutions, hand-pump sprays, sticks, facial masks, and wet wipes. The composition of the present invention can be conveniently used to prepare or as a cosmetic, dermatological, or pharmaceutical topical application product by various methods well known in the art.

[0086] The skin topical composition of the present invention may include one or more of the following ingredients: antiallergic agents, antimicrobial agents, antioxidants, chelating agents, colorants, depigmenting agents, emollients, emulsifiers, exfoliants, film formers, fragrances, moisturizers, insect repellents, lubricants, pharmaceutically active agents, moisturizers, photostabilizers, preservatives, skin care agents, skin penetration enhancers, sunscreens, stabilizers, surfactants, thickeners, viscosity regulators, vitamins or any combination thereof. DETAILED DESCRIPTION

[0087] The present invention will be further described below in conjunction with specific examples. However, it should be understood that these examples are only used to illustrate the present invention and do not constitute a limitation of the scope of the present invention. The test methods in the following examples that do not specify specific conditions are usually based on conventional conditions or the conditions recommended by the manufacturer. Unless otherwise stated, all percentages and parts are by weight.

[0088] The medicinal raw materials used in the following examples were all purchased from "Anhui Bozhou Jingwan Chinese Medicine Pieces Factory", and the incoming materials were in the form of "Chinese herbal medicine pieces"; the biological reagents used were all purchased from Shanghai Jahwa Biotechnology Co., Ltd.

[0089] The experimental instruments used in the following examples are as follows:

[0090] 1. Fixed stirrer (IKA RW20)

[0091] 2. Constant temperature water bath Shanghai Yiheng Scientific Instrument Co., Ltd. HWS 28

[0092] 3. Weighing balance METTLER TOLEDO PL602-S

[0093] 4. Electric constant temperature CO2 incubator (Thermo, 150i)

[0094] 5. Refrigerator

[0095] 6. Minolta CR-300 colorimeter

[0096] 7. Waters 2690HPLC, Waters 2487 dual wavelength absorption detector

[0097] 8. High-speed universal pulverizer (FW100 model)

[0098] 9. Chinese herbal medicine extraction and concentration tank (TNH type)

[0099] 10. UV-Vis spectrophotometer (Thermo Fisher)

[0100] 11. Vacuum freeze dryer, model FD-2, Beijing Boyikang Laboratory Instrument Co., Ltd.

[0101] 12. Clean bench (Suzhou Antai, SW-CJ-IF)

[0102] 13. Microplate reader (BioTek, Epoch)

[0103] 14. Inverted microscope (Olympus, CKX41)

[0104] 15. Upright microscope (Olympus, BX53)

[0105] Example 1: Preparation of Chinese herbal medicine extract

[0106] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex in a weight ratio of 1:4:10:10:1:4:4, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 12 kg of deionized water and boil in an extraction concentration tank, keep it slightly boiling for 1 hour, filter, extract the residue once, filter again, combine the two filtrates, concentrate to 1.5 kg, cool, add 70% volume concentration of ethanol while stirring, let stand for 12 hours, filter, and concentrate the filtrate under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared in a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0107] Example 2: Preparation of Chinese herbal medicine extract

[0108] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex according to the weight ratio = 1:2:8:10:4:1:2, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 12 kg of deionized water and boil in an extraction and concentration tank, keep it slightly boiling for 1 hour, filter, extract the residue once, filter again, combine the two filtrates, concentrate to 1.5 kg, cool, add ethanol to 70% ethanol volume concentration while stirring, let stand for 12 hours, filter, and concentrate the filtrate under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0109] Example 3: Preparation of Chinese herbal medicine extract

[0110] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex in a weight ratio of 1:1:10:10:4:1:1, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 12 kg of deionized water and boil in an extraction and concentration tank, keep it slightly boiling for 1 hour, filter, extract the residue once, filter again, combine the two filtrates, concentrate to 1.5 kg, cool, add ethanol to 70% ethanol volume concentration while stirring, let stand for 12 hours, filter, and concentrate the filtrate under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0111] Example 4: Preparation of Chinese herbal medicine extract

[0112] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex according to the weight ratio = 1:1:4:10:4:1:1, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 12 kg of deionized water and boil in an extraction concentration tank, keep it slightly boiling for 1 hour, filter, extract the residue once, filter again, combine the two filtrates, concentrate to 1.5 kg, cool, add ethanol to 70% ethanol volume concentration while stirring, let stand for 12 hours, filter, and concentrate the filtrate under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) according to a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0113] Example 5: Preparation of Chinese herbal medicine extract

[0114] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Cortex Dictamni in a weight ratio of 1:1:4:10:2:1:1, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 12 kg of deionized water and boil in an extraction and concentration tank, keep it slightly boiling for 1 hour, filter, extract the residue once, filter again, combine the two filtrates, concentrate to 1.5 kg, cool, add ethanol while stirring to a volume concentration of 70% ethanol, let stand for 12 hours, filter, and concentrate the filtrate under reduced pressure to a dry solid to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0115] Example 6: Preparation of Chinese herbal medicine extract

[0116] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex according to the weight ratio = 1:2:4:8:4:1:2, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 12 kg of deionized water and boil in an extraction concentration tank, keep it slightly boiling for 1 hour, filter, extract the residue once, filter again, combine the two filtrates, concentrate to 1.5 kg, cool, add ethanol while stirring to 70% ethanol volume concentration, let stand for 12 hours, filter, and concentrate the filtrate under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0117] Example 7: Preparation of Chinese herbal medicine extract

[0118] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex in a weight ratio of 1:4:10:10:1:4:4, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 10 kg of ethanol solution (70% volume concentration) and boil in an extraction and concentration tank, keep the temperature at 80°C for 2 hours, filter, extract the residue once, filter again, combine the two filtrates, filter, and concentrate the filtrate under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared in a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0119] Example 8: Preparation of Chinese herbal medicine extract

[0120] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Cortex Dictamni in a weight ratio of 1:2:8:10:4:1:2, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 10 kg of ethanol solution (70% volume concentration) and boil in an extraction and concentration tank, keep the temperature at 80°C for 2 hours, filter, extract the residue once, filter again, combine the two filtrates, and concentrate the filtrates under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0121] Example 9: Preparation of Chinese herbal medicine extract

[0122] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex in a weight ratio of 1:1:10:10:4:1:1, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 10 kg of ethanol solution (70% volume concentration) and boil in an extraction and concentration tank, keep the temperature at 80°C for 2 hours, filter, extract the residue once, filter again, combine the two filtrates, and concentrate the filtrates under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0123] Example 10: Preparation of Chinese herbal medicine extract

[0124] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Cortex Dictamni in a weight ratio of 1:1:4:10:4:1:1, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 10 kg of ethanol solution (70% volume concentration) and boil in an extraction and concentration tank, keep the temperature at 80°C for 2 hours, filter, extract the residue once, filter again, combine the two filtrates, and concentrate the filtrates under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0125] Example 11: Preparation of Chinese herbal medicine extract

[0126] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Cortex Dictamni in a weight ratio of 1:1:4:10:2:1:1, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 10 kg of ethanol solution (70% volume concentration) and boil in an extraction and concentration tank, keep the temperature at 80°C for 2 hours, filter, extract the residue once, filter again, combine the two filtrates, and concentrate the filtrates under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0127] Example 12: Preparation of Chinese herbal medicine extract

[0128] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Cortex Dictamni in a weight ratio of 1:2:4:8:4:1:2, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 10 kg of ethanol solution (70% volume concentration) and boil in an extraction and concentration tank, keep the temperature at 80°C for 2 hours, filter, extract the residue once, filter again, combine the two filtrates, and concentrate the filtrates under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0129] Example 13: Preparation of Chinese herbal medicine extract (Comparative Example)

[0130] Weigh Poria cocos and grind it into 1 kg of coarse powder with a high-speed universal grinder, add 12 kg of deionized water and boil it in an extraction and concentration tank, keep it slightly boiling for 1 hour, filter, extract the residue again, filter again, combine the two filtrates, concentrate to 1.5 kg, cool, add ethanol to 70% ethanol volume concentration while stirring, let it stand for 12 hours, filter, and concentrate the filtrate under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared in a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0131] Example 14: Preparation of Chinese herbal medicine extract (Comparative Example)

[0132] Weigh 1 kg of coarse powder obtained by grinding Tribulus terrestris with a high-speed universal grinder, add 12 kg of deionized water and boil in an extraction and concentration tank, keep it slightly boiling for 1 hour, filter, extract the residue again, filter again, combine the two filtrates, concentrate to 1.5 kg, cool, add ethanol to 70% ethanol volume concentration while stirring, let stand for 12 hours, filter, and concentrate the filtrate under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0133] Example 15: Preparation of Chinese herbal medicine extract (Comparative Example)

[0134] Weigh 1 kg of coarse powder obtained by grinding the white mulberry with a high-speed universal grinder, add 12 kg of deionized water and boil in an extraction and concentration tank, keep it slightly boiling for 1 hour, filter, extract the filter residue once, filter again, combine the two filtrates, concentrate to 1.5 kg, cool, add ethanol to 70% ethanol volume concentration while stirring, let stand for 12 hours, filter, and concentrate the filtrate under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0135] Example 16: Preparation of Chinese herbal medicine extract (Comparative Example)

[0136] Weigh 1 kg of coarse powder obtained by grinding peony with a high-speed universal grinder, add 12 kg of deionized water and boil in an extraction and concentration tank, keep it slightly boiling for 1 hour, filter, extract the residue again, filter again, combine the two filtrates, concentrate to 1.5 kg, cool, add ethanol to 70% ethanol volume concentration while stirring, let stand for 12 hours, filter, and concentrate the filtrate under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared in a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0137] Example 17: Preparation of Chinese herbal medicine extract (Comparative Example)

[0138] Weigh 1 kg of coarse powder obtained by grinding Atractylodes macrocephala with a high-speed universal grinder, add 12 kg of deionized water and boil in an extraction and concentration tank, keep it slightly boiling for 1 hour, filter, extract the residue again, filter again, combine the two filtrates, concentrate to 1.5 kg, cool, add ethanol to 70% ethanol volume concentration while stirring, let stand for 12 hours, filter, and concentrate the filtrate under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared in a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0139] Example 18: Preparation of Chinese herbal medicine extract (Comparative Example)

[0140] Weigh 1 kg of coarse powder from Bletilla striata and grind it with a high-speed universal grinder, add 12 kg of deionized water and boil it in an extraction and concentration tank, keep it slightly boiling for 1 hour, filter, extract the residue again, filter again, combine the two filtrates, concentrate to 1.5 kg, cool, add ethanol to 70% ethanol volume concentration while stirring, let stand for 12 hours, filter, and concentrate the filtrate under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0141] Example 19: Preparation of Chinese herbal medicine extract (Comparative Example)

[0142] Weigh the Dictamni cortex and grind it into 1kg of coarse powder by a high-speed universal grinder, add 12kg of deionized water and boil it in an extraction and concentration tank, keep it slightly boiling for 1 hour, filter, extract the residue again, filter again, combine the two filtrates, concentrate to 1.5kg, cool, add ethanol to 70% ethanol volume concentration while stirring, let it stand for 12 hours, filter, and concentrate the filtrate under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared in a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0143] Example 20: Preparation of Chinese herbal medicine extract (Comparative Example)

[0144] Weigh Poria cocos and grind it into 1 kg of coarse powder by high-speed universal grinder, add 10 kg of ethanol solution (70% volume concentration) and boil it in an extraction and concentration tank, keep the temperature at 80°C for 2 hours, filter, extract the residue again, filter again, combine the two filtrates, and concentrate the filtrates under reduced pressure to a dry solid state to obtain the Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared in a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0145] Example 21: Preparation of Chinese herbal medicine extract (Comparative Example)

[0146] Weigh Tribulus terrestris and grind it into 1 kg of coarse powder by high-speed universal grinder, add 10 kg of ethanol solution (70% volume concentration) and boil it in an extraction and concentration tank, keep the temperature at 80°C for 2 hours, filter, extract the residue once, filter again, combine the two filtrates, and concentrate the filtrates under reduced pressure to a dry solid state to obtain the Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared in a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0147] Example 22: Preparation of Chinese herbal medicine extract (Comparative Example)

[0148] Weigh 1 kg of coarse powder obtained by grinding the white mulberry with a high-speed universal grinder, add 10 kg of ethanol solution (70% volume concentration) in an extraction and concentration tank, boil, maintain the temperature at 80°C for 2 hours, filter, extract the residue once, filter again, combine the two filtrates, and concentrate the filtrates under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0149] Example 23: Preparation of Chinese herbal medicine extract (Comparative Example)

[0150] Weigh 1 kg of coarse powder obtained by grinding peony with a high-speed universal grinder, add 10 kg of ethanol solution (70% volume concentration) in an extraction and concentration tank, boil, maintain the temperature at 80°C for 2 hours, filter, extract the residue once, filter again, combine the two filtrates, and concentrate the filtrates under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared in a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0151] Example 24: Preparation of Chinese herbal medicine extract (Comparative Example)

[0152] Weigh 1 kg of coarse powder from Atractylodes macrocephala and grind it with a high-speed universal grinder, add 10 kg of ethanol solution (70% volume concentration) and boil it in an extraction and concentration tank, keep the temperature at 80°C for 2 hours, filter, extract the residue once, filter again, combine the two filtrates, and concentrate the filtrates under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared in a weight ratio of 9:1) at a weight ratio of 1:10, stir until evenly mixed, and set aside.

[0153] Example 25: Preparation of Chinese herbal medicine extract (Comparative Example)

[0154] Weigh 1 kg of coarse powder from Bletilla striata and grind it with a high-speed universal grinder, add 10 kg of ethanol solution (70% volume concentration) and boil it in an extraction and concentration tank, keep the temperature at 80°C for 2 hours, filter, extract the residue once, filter again, combine the two filtrates, and concentrate the filtrates under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until evenly mixed, and set aside.

[0155] Example 26: Preparation of Chinese herbal medicine extract (Comparative Example)

[0156] Weigh the Dictamni cortex and grind it into 1 kg of coarse powder by a high-speed universal grinder, add 10 kg of ethanol solution (70% volume concentration) and boil it in an extraction and concentration tank, keep the temperature at 80°C for 2 hours, filter, extract the residue once, filter again, combine the two filtrates, and concentrate the filtrates under reduced pressure to a dry solid state to obtain the Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared in a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0157] Example 27: Preparation of Chinese herbal medicine extract (Comparative Example)

[0158] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex according to the weight ratio = 1:0:10:10:1:4:4, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 12 kg of deionized water and boil in an extraction and concentration tank, keep it slightly boiling for 1 hour, filter, extract the residue once, filter again, combine the two filtrates, concentrate to 1.5 kg, cool, add ethanol to 70% ethanol volume concentration while stirring, let stand for 12 hours, filter, and concentrate the filtrate under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) according to a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0159] Example 28: Preparation of Chinese herbal medicine extract

[0160] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex according to the weight ratio = 1:2:0:10:4:1:2, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 12 kg of deionized water and boil in an extraction and concentration tank, keep it slightly boiling for 1 hour, filter, extract the residue once, filter again, combine the two filtrates, concentrate to 1.5 kg, cool, add ethanol to 70% ethanol volume concentration while stirring, let stand for 12 hours, filter, and concentrate the filtrate under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) according to a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0161] Example 29: Preparation of Chinese herbal medicine extract

[0162] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex in a weight ratio of 1:1:10:0:4:1:1, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 12 kg of deionized water and boil in an extraction and concentration tank, keep it slightly boiling for 1 hour, filter, extract the residue once, filter again, combine the two filtrates, concentrate to 1.5 kg, cool, add ethanol to 70% ethanol volume concentration while stirring, let stand for 12 hours, filter, and concentrate the filtrate under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0163] Example 30: Preparation of Chinese herbal medicine extract

[0164] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex according to the weight ratio = 1:1:4:10:0:1:1, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 12 kg of deionized water and boil in an extraction and concentration tank, keep it slightly boiling for 1 hour, filter, extract the residue once, filter again, combine the two filtrates, concentrate to 1.5 kg, cool, add ethanol to 70% ethanol volume concentration while stirring, let stand for 12 hours, filter, and concentrate the filtrate under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0165] Example 31: Preparation of Chinese herbal medicine extract

[0166] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex according to the weight ratio = 1:1:4:10:2:0:1, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 12 kg of deionized water and boil in an extraction and concentration tank, keep it slightly boiling for 1 hour, filter, extract the residue once, filter again, combine the two filtrates, concentrate to 1.5 kg, cool, add ethanol while stirring to 70% ethanol volume concentration, let stand for 12 hours, filter, and concentrate the filtrate under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0167] Example 32: Preparation of Chinese herbal medicine extract

[0168] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Cortex Dictamni in a weight ratio of 1:2:4:8:4:1:0, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 12 kg of deionized water and boil in an extraction and concentration tank, keep it slightly boiling for 1 hour, filter, extract the residue once, filter again, combine the two filtrates, concentrate to 1.5 kg, cool, add ethanol to 70% ethanol volume concentration while stirring, let stand for 12 hours, filter, and concentrate the filtrate under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0169] Example 33: Preparation of Chinese herbal medicine extract

[0170] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Cortex Dictamni in a weight ratio of 0:2:4:8:4:1:0, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 12 kg of deionized water and boil in an extraction and concentration tank, keep it slightly boiling for 1 hour, filter, extract the residue once, filter again, combine the two filtrates, concentrate to 1.5 kg, cool, add ethanol while stirring to a volume concentration of 70% ethanol, let stand for 12 hours, filter, and concentrate the filtrate under reduced pressure to a dry solid to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0171] Example 34: Preparation of Chinese herbal medicine extract

[0172] Weigh Poria cocos: Tribulus terrestris: Ampelopsis radix: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex in a weight ratio of 1:0:10:10:1:4:4, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 10 kg of ethanol solution (70% volume concentration) and boil in an extraction and concentration tank, keep the temperature at 80°C for 2 hours, filter, extract the residue once, filter again, combine the two filtrates, and concentrate the filtrates under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0173] Example 35: Preparation of Chinese herbal medicine extract

[0174] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Cortex Dictamni in a weight ratio of 1:2:0:10:4:1:2, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 10 kg of ethanol solution (70% volume concentration) and boil in an extraction and concentration tank, keep the temperature at 80°C for 2 hours, filter, extract the residue once, filter again, combine the two filtrates, and concentrate the filtrates under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0175] Example 36: Preparation of Chinese herbal medicine extract

[0176] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Cortex Dictamni in a weight ratio of 1:1:10:0:4:1:1, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 10 kg of ethanol solution (70% volume concentration) and boil in an extraction and concentration tank, keep the temperature at 80°C for 2 hours, filter, extract the residue once, filter again, combine the two filtrates, and concentrate the filtrates under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0177] Example 37: Preparation of Chinese herbal medicine extract

[0178] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Cortex Dictamni in a weight ratio of 1:0:4:10:0:1:1, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 10 kg of ethanol solution (70% volume concentration) and boil in an extraction and concentration tank, keep the temperature at 80°C for 2 hours, filter, extract the residue once, filter again, combine the two filtrates, and concentrate the filtrates under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0179] Example 38: Preparation of Chinese herbal medicine extract

[0180] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Cortex Dictamni in a weight ratio of 1:0:4:10:2:0:1, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 10 kg of ethanol solution (70% volume concentration) and boil in an extraction and concentration tank, keep the temperature at 80°C for 2 hours, filter, extract the residue once, filter again, combine the two filtrates, and concentrate the filtrates under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0181] Example 39: Preparation of Chinese herbal medicine extract

[0182] Weigh Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Cortex Dictamni in a weight ratio of 1:2:0:8:4:1:0, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 10 kg of ethanol solution (70% volume concentration) and boil in an extraction and concentration tank, keep the temperature at 80°C for 2 hours, filter, extract the residue once, filter again, combine the two filtrates, and concentrate the filtrates under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0183] Example 40: Preparation of Chinese herbal medicine extract

[0184] Weigh Poria cocos: Tribulus terrestris: Ampelopsis radix: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Cortex Dictamni in a weight ratio of 0:2:0:8:4:1:0, mix and grind with a high-speed universal grinder to obtain 1 kg of coarse powder, add 10 kg of ethanol solution (70% volume concentration) and boil in an extraction and concentration tank, keep the temperature at 80°C for 2 hours, filter, extract the residue once, filter again, combine the two filtrates, and concentrate the filtrates under reduced pressure to a dry solid state to obtain a Chinese medicine complex extract. Disperse the above extracts in a mixed liquid of butanediol: ethylhexylglycerol (pre-prepared at a weight ratio of 9:1) at a weight ratio of 1:10, stir until uniformly mixed, and set aside.

[0185] Test Example 1: Active substance detection

[0186] The extracts of the Chinese medicinal compound of Examples 1 to 40 were taken to detect the content of active ingredients therein.

[0187] The chemical structure of active drug ingredients is the key to drug transdermal penetration. Fat-soluble drugs easily penetrate the stratum corneum, skin barrier, and cell membrane, but diffuse slowly in the active epidermis due to the relatively high water content. Water-soluble drugs penetrate the stratum corneum cell membrane and skin barrier slowly, but diffuse quickly in the active epidermis. Generally, when selecting active ingredients for functional drugs, attention is paid to the molecular structure of the ingredients, and drug ingredients with moderate oil / water distribution are selected as much as possible, or water-soluble and fat-soluble ingredients are used together, which often achieves better results.

[0188] 1,2,3,4,6-O-galloylglucose (PGG) is a polyphenol compound composed of 5 gallic acids and 1 glucose bonded by an ester bond. It has a relative molecular weight of 940, good hydrophilicity and lipophilicity, and strong physiological activity, such as anti-tumor, anti-oxidation, anti-leukemia, anti-allergy, and hypoglycemic functions. It exists in many traditional Chinese medicinal materials.

[0189] High performance liquid chromatography determination:

[0190] The chromatographic conditions and system suitability test used a C18 universal Eclipse XDB-C18 (4.6x250mm, 5μm) column; acetonitrile-0.1% dilute phosphoric acid (25:75) as the mobile phase; after gradient elution, the detection wavelength was 230nm; the column temperature was 35℃; the flow rate was 0.8mL / min; the injection volume was 10μL. The theoretical plate number calculated according to the 1,2,3,4,6-O-galloylglucose (PGG) peak should not be less than 200,000.

[0191] Preparation of reference solution: accurately weigh the PGG reference substance dried to constant weight, add methanol to make a mixed solution containing 0.2 mg per 1 mL, and shake well.

[0192] Preparation of the sample to be tested: 1 mL of each of the Chinese medicinal extracts of Examples 1 to 3 and the crude product of the enzymatic hydrolysis reaction of Examples 4 to 6 were accurately weighed, placed in a 5 mL volumetric flask, diluted to the mark with methanol, and shaken to obtain the sample.

[0193] For determination, 10 μL of the reference solution and the sample solution to be tested were accurately drawn and injected into the high performance liquid chromatograph, and the HPLC spectrum was recorded to obtain Figure 1 .

[0194] The results of measuring the contents of Examples 1 to 40 are shown in Table 1 below.

[0195] Table 1: PGG content in Chinese herbal extracts of Examples 1 to 40

[0196]

[0197]

[0198] The results show that after different extraction processes, the Chinese herbal compound extracts of Examples 1 to 6 obtained a higher amount of PGG, especially Example 2, which reached 0.4006 mg / ml, 96% higher than Example 6. For Examples 7 to 12, the alcohol extraction process, even with the same compatibility ratio of Chinese herbal medicines, has a lower content of active ingredient PGG as a whole, especially Example 8 with the same ratio, which is about 13.7% lower than Example 2; similarly, in the water extraction and alcohol precipitation process of Examples 1 to 6, even with the same ratio and compatibility, the overall PGG content is higher than that of the alcohol extraction process of Examples 7 to 12.

[0199] Comparing the extracts with different proportions, especially when one or more of the seven Chinese herbal medicines are deleted, the PGG content obtained by water extraction and alcohol precipitation or alcohol extraction process is generally lower than the situation where the seven herbs are present together, such as Example 14, where PGG was not detected. Comparing the PGG content obtained in Example 2 with that obtained in Examples 13 to 40, it is basically between 2 and 100 times; in general, the seven different Chinese herbal medicines obtained by combining in different proportions have large differences in active substance content between different combinations and proportions, and there are also large differences in active substance content for different extraction processes.

[0200] Examples 41-112: Compounding of extracts and whitening ingredients

[0201] According to the weight ratio in Table 2, the sample of Example 2, nicotinamide (VB3), ascorbyl glucoside (AA2G) and water were weighed and stirred to obtain 100 g of solution for later use.

[0202] Table 2: Example solutions prepared according to weight ratio

[0203]

[0204]

[0205]

[0206] Test Example 2: Whitening efficacy test based on melanin model

[0207] The 3D melanin skin model used in this test ( Batch number: MS220304, Guangdong Boxi Biotechnology Co., Ltd.), prepare 6-well plates, add 3.7 mL of M-TA culture medium to each well, transfer the models on the third day of gas-liquid surface culture, that is, the day of model reception (Day 0), to the marked 6-well plates; each experimental group requires 6 models (for the determination of apparent chromaticity, L*b* value and melanin content), transfer all 6-well plates with models to the CO 2Culture in an incubator (37°C, 5% CO 2 ). Using UVB (50mJ / cm 2 ) as the stimulus condition, the measurement of apparent chromaticity places the colorimetric card just below the SLR camera, and uses tweezers to place a single model in the color circle of the colorimetric card and take a photo. The SLR camera parameters are set to manual photography mode, the focal length is adjusted to 5.8mm, the aperture is set to f / 8, the aperture is adjusted to F22, the shutter speed is set to 1 / 80s, and the ISO is set to 1600. L* value and b* value test, the model after the apparent chromaticity test is completed, the L* value and b* value are tested. The specific test operation is as follows: place the model on a flat and hard white plane with the stratum corneum facing up, and according to the instructions for use of the colorimeter, align the colorimeter detection hole vertically with the model surface for detection, repeat the reading three times for each model, and record the data, and take the average value as the L* value and b* value reading of the single model. The tested model is placed in a clean EP tube for melanin content determination. Melanin content test 1) Place the model in a 1.5mL EP tube, label it, add 1mL PBS buffer to each tube, vortex shaker for 3min, centrifuge at 2000r / min, and discard the supernatant; 2) Add 200μL distilled water, 500μL anhydrous ethanol and 500μL ether to the EP tube in step (1) in sequence, mix well, let stand at room temperature for 20min, and centrifuge at 3000r / min.

[0208] 5min, discard the supernatant; 3) add 1mL of 1mol / L NaOH aqueous solution containing 10% DMSO and heat in a water bath at 80℃ for 40min to completely dissolve the melanin particles; 4) After the heat incubation, pipette 200μL of supernatant into the corresponding wells of a clearly labeled 96-well plate, read the OD value at 405nm, and test two parallels for each model on the 96-well plate.

[0209] GraphPad Prism was used for statistical analysis, and the results were expressed as Mean ± SD. The t-test was used for statistical analysis among the groups. All statistical analyses were two-tailed. P < 0.05 was considered to be significantly different, and P < 0.01 was considered to be extremely significantly different.

[0210] Table 3: Whitening efficacy (melanin content) results of Examples 41 to 112 based on the melanin model

[0211]

[0212]

[0213]

[0214]

[0215] The core factors affecting skin transparency, lightness and whiteness include 1) the content of melanin in the skin; 2) (endogenous) dark yellowing of the skin base; 3) skin inflammation caused by oxidative factors; 4) skin barrier function and water content; According to the research on the factors affecting the dark yellow and dull skin of Chinese women, with the increase of age, the facial brightness of Chinese women decreases significantly, and the yellowness increases significantly. Dark yellowing is a characteristic change that distinguishes Chinese women from Caucasian women and Mexican women. The main factors affecting the "dark" and "yellow" skin are the synthesis of melanin and protein carbonylation, and both reactions can be induced by oxidative stress. Under normal physiological conditions, the body has a complete antioxidant defense mechanism (enzyme antioxidant system and non-enzyme antioxidant system). Nowadays, with the deterioration of the natural environment and the intensification of competition in modern society, urban people are accompanied by various unhealthy lifestyles (staying up late, improper diet, lack of exercise or excessive exercise), and the body is in a sub-healthy state and cannot provide enough antioxidants, which in turn causes oxidative stress.

[0216] Vitamin C / derivatives are safe whitening ingredients with strong antioxidant properties. They can improve facial dullness, while effectively inhibiting the activity of tyrosinase and the formation of melanin, providing a root whitening effect.

[0217] Nicotinamide is a water-soluble vitamin, which is a member of the vitamin B family. It can be converted from nicotinic acid in vivo, and both have vitamin effects. However, nicotinic acid is prone to cause a series of problems such as skin itching, redness and allergies, so the present invention uses more than 99% high-purity nicotinamide to avoid the mixing of nicotinic acid to the greatest extent. Nicotinamide can effectively prevent the transmission of melanin, thereby bringing whitening and spot-lightening effects. In the literature, it is reported that the use of vitamin C combined with nicotinamide has achieved relatively satisfactory results in the treatment of chloasma. In addition, the two can cause an increase in the level of endogenous antioxidant NAD(P)H, which has the effect of helping the deep layer of the skin to resist glycation, thereby endogenously regulating the skin's dark yellowing phenomenon. However, the transdermal permeability of niacinamide combined with AA2G has always been one of the core issues that have not been resolved.

[0218] The first thing that needs to be studied to realize the core efficacy of Chinese herbal cosmetics is the transdermal absorption and utilization of active ingredients. When the water content in the stratum corneum of the skin is lower than 10%, the keratinocytes are arranged more tightly, reducing the effective penetration area of ​​the skin and the space for substances to penetrate the skin, thereby reducing the degree and efficiency of transdermal absorption of drugs. In this skin environment, even if the dosage of the drug is increased, the effect is not much improved. Therefore, the first thing to do for functional cosmetics is to restore the water content of the skin to a normal level or a moist state. The stratum corneum contains 10% or more water, and the other layers of the epidermis contain 10% to 47%. When the water content in the epidermis reaches 10% to 50%, the compact keratinocytes become porous and plump, increasing the effective area of ​​the skin and the contact cross-section, and the transdermal absorption rate of the drug is greatly improved. In the environment of moisturizing the skin, the drug will play a better role. Modern biological research shows that Poria, Tribulus terrestris and Bletilla striata all have a clear effect of inhibiting tyrosinase activity, Atractylodes macrocephala and Bletilla striata (and) have a clear antioxidant effect, and White Peony Root has a certain effect of promoting blood circulation, promoting metabolism, and making the skin even and bright.

[0219] The present invention is the first to use the highly effective moisturizing ingredients, small molecule polyols (butylene glycol) and ethylhexylglycerin, to moisturize the skin, strengthen the skin barrier, and increase the water content of the skin. Butylene glycol is a classic functional moisturizing ingredient in cosmetics. Butylene glycol is a small molecule ingredient with a molecular weight of only 90g / mol, and it has good skin moisturizing and permeability. The "twin" "permeability" technology combining ethylhexylglycerin and butylene glycol can help the skin achieve double penetration and significantly increase the effect of moisturization, and can significantly increase the "permeability" effect of active substances. Double-effect moisturizing, fast water absorption, water lock, bright and white skin. The combination of active substances ascorbyl glucoside, niacinamide and Chinese herbal whitening compound can significantly improve the gloss and transparency of the skin. It is the "translucent white" essence of the skin, and the surface is even and translucent. Whitening herbal active ingredients, vitamin C / derivatives, and niacinamide can inhibit melanin from the source and resist oxidation. Combined with niacinamide, it can further cut off the transmission of melanin to the skin's epidermal cells and prevent pigmentation. At the same time, it can help the skin remove endogenous yellowing and improve dullness, maximizing the whitening / brightening effect of the product.

[0220] The differences in melanin inhibition effects were compared when the same concentration of Chinese herbal compound extracts were combined with different proportions of whitening ingredients.

[0221] From the results of Examples 41 to 112 (see Table 3), most of the examples and compositions have the effect of inhibiting melanin. From the perspective of relative improvement rate, the preferred combination of 7 Chinese herbal medicines improves by more than 12%, which is also positively correlated with the content of PGG in the extracts of the same examples. Examples 2, 4, 8, and 10 are post-processed products of preferred Chinese herbal extracts. By combining with specific whitening ingredients, the improvement rate of the example extracts in inhibiting melanin content is greatly improved, such as Example 43 is increased to 50.67%, Example 44 is increased to 46.27%, Example 54 is increased to 42.41%, and Example 62 is increased to 50%. The average improvement ratio exceeds 30%, indicating that the use of the selected two substances for compounding can greatly improve the efficacy of the Chinese herbal compound extract in inhibiting melanin content.

[0222] Comparing the melanin-inhibiting abilities of the two whitening ingredients at the same ratio, it is generally found that the melanin-inhibiting effects are not high, which indicates that the active ingredients of the Chinese herbal complex play a greater role in promoting the effects of melanin-inhibiting effects.

[0223] At the same time, there is a certain correlation between the post-processing products of the extracts of Examples 2, 4, 8, and 10 and the aforementioned higher content of PGG. The addition of polyols can greatly improve the utilization rate of the active ingredients of Chinese herbal medicines by cells, which is a possible working mechanism.

[0224] from Figure 2 The apparent chromaticity of the suppressed melanin content can be seen more intuitively, and Example 43 is significantly improved compared with NC and PC.

[0225] Test Example 3: Permeability test based on laser Raman confocal method

[0226] A confocal Raman microscope system (Thermo, DXR2Xi model) equipped with a 532nm (He-Ne laser) laser source, a semiconductor-cooled CCD detector (1024×800 pixels) and a 25μm confocal pinhole was used; the laser beam was used with a 50x telephoto objective (NA0.50BD) to obtain sample parameters. Before measurement, a silicon plate (520.5cm -1 ) for standard single-point calibration. All spectra were obtained between 50 and 3400 cm -1The Raman spectrum of each point is obtained by XY scanning. The laser power for scanning the sample is 3.5mW, and the integration time for each point of the spectrum is 0.05sec. All Raman spectral data are preprocessed (cosmic ray removal, background removal, smoothing and noise reduction). The Raman image is obtained by using XZ Raman deep imaging. The experiment starts with single spectrum acquisition. After obtaining a single spectrum, the single spectrum is first preprocessed and the spectral quality is evaluated to explore the experimental conditions. Subsequently, a point-by-point scanning method is used for deep scanning imaging. The spectral data acquisition step is 2μm, the scanning area is 8μm×100μm (4×50 pixels), and the spectral integration time is 0.05 seconds for each pixel.

[0227] All spectra were recorded by OMSNIC of Thermo Fisher SCIENTIFIC for data processing. Data were analyzed using R (i386 4.0.3). Raman spectra were baseline corrected, SG second-order smoothed, and normalized before statistical analysis; K-means clustering was used to analyze spectral changes in Raman imaging profiles. K-means is a data processing method that classifies spectral data based on the similarity of spectral data. Each spectrum is regarded as a point in a two-dimensional space, so the similarity between spectra can be mathematically defined by similarity coefficients and distances. First, the number of clusters k is set, and the spectra to be clustered are divided into k categories. The sum of the distances of all spectra in each category to the cluster center is minimized iteratively, that is, the similarity between similar spectra is the highest. K-means clustering starts with a random cluster distribution of k clusters, and then iteratively solves them according to their minimum distance to the average spectrum of the cluster. This work is carried out until a stable arrangement is reached, and a color map is constructed to more clearly observe the differences in skin tissue with depth. The advantages of this algorithm are fast calculation speed, simple process, and wide applicability. In order to obtain reliable results, the collected Raman spectra must be preprocessed, and the original spectra must be processed including removing cosmic rays, removing baseline background, and smoothing and noise reduction. During the experiment, in order to ensure the accuracy of the experimental data, the Raman spectrum must be preprocessed. Because during the measurement process, there will be interference from fluorescence background, cosmic rays, and Gaussian noise or Poisson noise, which will affect the collection and acquisition of Raman information. In order to obtain undisturbed data, these influencing factors must be eliminated, so baseline correction is required. After baseline correction, the spectrum is smoothed, and the Savitzky-Golay filter (based on the least squares convolution fitting algorithm) is used to smooth the spectral mechanical energy.

[0228] The skin tissue used in the experimental test (six-week-old, male suckling pig abdomen, purchased from Chongqing Meisheng Trading Co., Ltd.). The purchased suckling pig abdomen skin was frozen and stored in a refrigerator at -25°C. Before the experiment, the frozen skin sample was thawed in a culture dish filled with PBS (pH=7.4, 5ml), with the skin epidermis facing up and exposed to the air and the dermis part immersed in PBS buffer. The size of the skin sample was kept at 1.5×1.5cm 2 During the entire experimental measurement process, the lower end of the skin sample is always in contact with the PBS buffer. After the skin sample is completely thawed, it needs to be placed in a PBS solution for 2 hours to ensure that oil and moisture no longer overflow from the skin surface. The laboratory room temperature is maintained at 25±2°C and the air humidity is maintained at 45±5%. The skin sample is always kept moistened at the lower end during the entire experiment. Take 2.5μL of the sample from the above embodiment and drop it on the center of each skin sample, and then start single spectrum measurement and Raman imaging. The confocal microscopy and polarization Raman imaging time of a single sample is controlled within 3 hours to ensure that the barrier function of the sample will not change due to changes in humidity and temperature.

[0229] The laser Raman confocal permeability test and evaluation of Example 43 were carried out, and compared with the solution of the whitening component not preferred by the present invention (ie, VB3 of the same concentration), the results are as follows: Figure 3 shown. Figure 3 For the intuitive presentation of Raman spectrum, the scale of skin depth (leftmost) and the maximum and minimum directions of the degree scale are added. From the scale, we can see that yellow indicates the maximum penetration and blue indicates the minimum penetration. On the cross-section of the skin, it is from the skin surface to the deep layer of the skin, that is, 0-100μm. As can be seen from the left picture, after 120 minutes, the substance can basically penetrate to a depth of 60-100μm; compared with the picture on the right, we can see that after 120 minutes, most of the substance still remains in the skin surface layer of 0-20μm.

[0230] From the penetration result data, it can be seen that the penetration efficiency of Example 43 is significantly improved, that is, within the same period of time, the penetration efficiency of the whitening component in Example 43 is higher and the penetration is deeper.

[0231] The main effective substances in Chinese herbal compound additives are flavonoids, polyphenols, polysaccharides, etc. The distribution and content of specific components mostly depend on the extraction method and means. Moreover, since most substances are not easy to preserve, improper storage is prone to oxidation, decomposition, volatilization, deterioration and other problems, resulting in the loss of effective substances. Advanced freeze-drying technology can also be used in the later stage of the preparation process, so that the active ingredients in the extract can be better preserved, and the original flavor of the active ingredients can be retained to a greater extent, especially the heat-sensitive active ingredients. In addition, because it is operated in a vacuum and oxygen-free environment, some easily oxidized active ingredients (such as oils and fats) can also be protected. When operated in a vacuum and low temperature, the growth of microorganisms and the action of enzymes are inhibited, and they can be stored for a long time at room temperature without adding any preservatives, reducing the erosion of microorganisms and extending the shelf life of the product.

[0232] In summary, the extracts obtained in the examples according to the wisdom of traditional Chinese medicine are combined and matched in specific whitening combinations to obtain examples 41 to 112, which have better whitening effects in inhibiting melanin production.

[0233] The skin external preparation is preferably a cosmetic composition, such as a toner, an essence, a cream, etc. The weight percentage of the composite extract in the skin external preparation is 0.001%-50% (w / w). The preferred weight percentage is 1%-20% (w / w). The more preferred weight percentage is 2%-10% (w / w). The most preferred weight percentage is 3%-8% (w / w).

[0234] The following are examples of specific applications of Chinese herbal extracts in skin topical preparations, and the formulations and preparation methods of these dosage forms. In the following tables, "-" means no addition.

[0235] Application Example 1: Preparation of facial cream

[0236]

[0237]

[0238] Application Example 2: Preparation of Emulsion

[0239]

[0240] Application Example 3: Preparation of Gel

[0241]

[0242]

[0243] Application Example 4: Preparation of lotion

[0244]

[0245] Application Example 5: Preparation of Essence

[0246]

[0247]

[0248] Application Example 6: Preparation of facial mask

[0249]

[0250]

[0251] Application Example 7: Preparation of Eye Cream

[0252]

[0253] Application Example 8: Preparation of Shower Gel

[0254]

[0255]

[0256] Application Example 9: Preparation of Facial Cleanser

[0257]

[0258]

[0259] Embodiments 82 to 121 of the present invention can also be used alone as low-temperature freeze-dried products.

[0260] The cosmetics prepared by using the composition of the present invention have the same or better use effects as the commercially available products.

[0261] The present invention illustrates the detailed method of the present invention through the above-mentioned embodiments, but the present invention is not limited to the above-mentioned detailed method, that is, it does not mean that the present invention must rely on the above-mentioned detailed method to be implemented. Those skilled in the art should understand that any improvement of the present invention, equivalent replacement of various raw materials of the product of the present invention, addition of auxiliary components, selection of specific methods, etc., all fall within the protection scope and disclosure scope of the present invention.

Claims

1. A whitening composition for promoting penetration and enhancing efficacy, comprising: 3% by weight of niacinamide, 0.1-1% by weight of ascorbyl glucoside, 10% by weight of a mixture of a Chinese herbal medicine extract and a polyol, The balance is water, in, The Chinese medicine extract is prepared from the following raw materials: Poria cocos, Tribulus terrestris, Bletilla striata, Paeonia lactiflora, Atractylodes macrocephala, Bletilla striata and Dictamni cortex, wherein the weight ratio of Poria cocos: Tribulus terrestris: Bletilla striata: Paeonia lactiflora: Atractylodes macrocephala: Bletilla striata: Dictamni cortex is 1:2:8:10:4:1:2, and the Chinese medicine extract is prepared by water extraction and alcohol precipitation method, wherein the polyol is a mixture of butanediol and ethylhexylglycerol in a weight ratio of 9:1, and Wherein, the weight ratio of the traditional Chinese medicine extract to the polyol is 1:

10.

2. A freeze-dried product of the whitening composition according to claim 1.

3. Use of the whitening composition according to claim 1 or the freeze-dried product according to claim 2 in skin whitening for non-therapeutic purposes. 4 . A skin external preparation comprising the whitening composition according to claim 1 or the freeze-dried product according to claim 2 .

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