WO2024012386A1 - Composition containing artemisia annua l. extract and oil-soluble component, and use thereof - Google Patents
Composition containing artemisia annua l. extract and oil-soluble component, and use thereof Download PDFInfo
- Publication number
- WO2024012386A1 WO2024012386A1 PCT/CN2023/106478 CN2023106478W WO2024012386A1 WO 2024012386 A1 WO2024012386 A1 WO 2024012386A1 CN 2023106478 W CN2023106478 W CN 2023106478W WO 2024012386 A1 WO2024012386 A1 WO 2024012386A1
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- WO
- WIPO (PCT)
- Prior art keywords
- extract
- oil
- artemisia annua
- skin
- preparation
- Prior art date
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
- A61K8/9783—Angiosperms [Magnoliophyta]
- A61K8/9789—Magnoliopsida [dicotyledons]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
Definitions
- the present invention belongs to the field of phytochemistry, and specifically relates to a composition containing Artemisia annua extract and oil-soluble components and its application in external skin agents or cosmetics.
- Allergic reactions can be divided into types I, II, III, and IV according to their mechanisms, and hyaluronidase is a participant in type I allergic reactions and has a strong correlation with inflammation and allergy.
- Hyaluronidase is a specific cleavage enzyme of hyaluronic acid, and hyaluronic acid displays a variety of physiological functions of traditional Chinese medicine in the body, such as moisturizing and promoting wound healing. According to research reports, some anti-allergic and anti-inflammatory drugs strongly inhibit hyaluronidase activity. Therefore, inhibition of hyaluronidase activity is used as an indicator to study anti-inflammatory effects.
- Artemisia annua is the whole plant of Artemisia annua L. in the Asteraceae family. Bitter and cold in nature. Returns to the liver, gallbladder, and kidney meridians. It has the effect of clearing away heat, relieving heat and cutting off malaria.
- Artemisia annua contains the anti-malarial component artemisinin, which can directly kill malaria parasites.
- Artemisia annua extract has antibacterial and insecticidal, antipyretic and anti-inflammatory, and immune-regulating effects. It also has five kinds of flavonoids with antioxidant activity. Ingredients, including quercetin, etc.
- Schizonepeta is the above-ground part of Schizonepeta tenuifolia Briq. in the family Lamiaceae. Purgit and slightly warm in nature. Returns to the lung and liver meridians. It has the effect of dispersing wind, resolving rash and sores. Its water decoction can enhance skin blood circulation and has a weak antipyretic effect; it has a strong antibacterial effect on Staphylococcus aureus; its methanol extract has certain analgesic and anti-inflammatory effects.
- Peony seed oil also known as peony oil
- peony oil is made from peony seeds and is processed through squeezing or other extraction techniques. The final product is made through a series of extraction processes.
- hyaluronidase inhibition According to the chemical composition of hyaluronidase inhibition, it can be roughly divided into polysaccharides, proteins, alkaloids, terpenes, etc.
- traditional Chinese medicine extracts also include oil-soluble components such as volatile oils and lignans. To date, there have been no reports of hyaluronidase inhibitory activity among these oil-soluble ingredients.
- the present invention unexpectedly found that compounding Artemisia annua extract and oil-soluble components (for example, oil-soluble components such as Schizonepeta sapiens and peony seed oil) has an excellent hyaluronidase inhibitory effect. Therefore, a composition containing artemisia annua extract and oil-soluble ingredients can be added as a compound functional additive to external skin preparations to assist in relieving itching, eczema, etc.
- oil-soluble components for example, oil-soluble components such as Schizonepeta sapiens and peony seed oil
- the present invention provides the application of a composition comprising an Artemisia annua extract and an oil-soluble component in skin anti-allergy, anti-inflammation and/or anti-irritation, wherein the oil-soluble component is selected from the group consisting of Schizonepeta sapiens extract and an oil-soluble component. Peony seed oil.
- the Artemisia annua extract is prepared by ultrasonic extraction. In a preferred embodiment, the Artemisia annua extract is extracted using water as a solvent.
- the oil-soluble component is Schizonepeta parsnip extract, and the weight ratio of Artemisia annua extract to Schizonepeta sapiens extract is 4:1 to 30:1.
- the oil-soluble component is peony seed oil, and the weight ratio of the Artemisia annua extract to the peony seed oil is 3:1 to 33:1.
- the anti-inflammatory, anti-allergic and/or anti-irritant effects are achieved by inhibiting hyaluronidase; or used to assist in relieving itching and/or eczema problems.
- the present invention provides the use of a composition comprising an Artemisia annua extract and an oil-soluble component in the preparation of a skin external preparation with skin anti-allergic, anti-inflammatory and/or anti-irritant effects, wherein the oil-soluble component Selected from Nepeta parsnip extract and peony seed oil.
- the external skin agent is selected from the group consisting of: cream, lotion, gel, lotion, essence, facial mask, eye cream, aerosol cleansing foam, spray, shower gel, and facial cleanser.
- Figure 1 shows the results of the positive control hyaluronidase inhibition experiment.
- Figure 2 shows the results of the hyaluronidase inhibition experiment of Example 2.
- Figure 3 shows the results of the hyaluronidase inhibition experiment in Example 3.
- Figure 4 shows the results of the hyaluronidase inhibition experiment of Example 4.
- Figure 5 shows the results of the hyaluronidase inhibition experiment of Example 5.
- Figure 6 shows the results of the hyaluronidase inhibition experiment of Example 6.
- Figure 7 shows the results of the hyaluronidase inhibition experiment of Example 7.
- Figure 8 shows the results of the hyaluronidase inhibition experiment of Example 8.
- Figure 9 shows the results of the hyaluronidase inhibition experiment of Example 9.
- Figure 10 shows the results of the hyaluronidase inhibition experiment of Example 10.
- the object of the present invention is to provide a composition containing Artemisia annua extract and oil-soluble components. Specifically, the combination of Artemisia annua extract and oil-soluble ingredients has a better effect on inhibiting hyaluronidase. Therefore, the composition containing Artemisia annua extract and oil-soluble ingredients can be added to skin care products as a compound functional additive to help relieve itching, eczema, etc.
- Artemisia annua L. is the whole plant of Artemisia annua L. in the Asteraceae family. Bitter and cold in nature. Returns to the liver, gallbladder, and kidney meridians. It has the effect of clearing away heat, relieving heat and cutting off malaria.
- Artemisia annua contains the anti-malarial ingredient artemisinin, which can directly kill malaria parasites.
- Artemisia annua extract has antibacterial and insecticidal, antipyretic and anti-inflammatory, and immune-regulating effects. It also has five types of antioxidant activity. Flavonoids, including quercetin, etc.
- an ultrasonic extraction method is used to extract the Artemisia annua extract.
- Ultrasonic extraction characteristics Including: 1. Shorten the extraction time, each ultrasound only takes 20min-30min, and conventional extraction is basically 1h-1.5h; 2. Extraction at room temperature, without destroying heat-sensitive components; 3. Direct cell wall breaking, and the active ingredients are more completely extracted.
- the process parameters of ultrasonic extraction are as follows: extraction twice, 20 minutes each time, ultrasonic for 3 seconds, and gap of 3 seconds.
- the extraction solvent is water (eg, deionized water).
- the extraction process includes an alcohol precipitation step. For example, 95% ethanol is used to achieve alcohol precipitation.
- the extraction process includes a filtering step.
- the extraction process includes a centrifugation step.
- the extraction process also includes a concentration step. For example, concentrate to a solid content of 5-20% by weight. In a specific embodiment, the solid content is concentrated to 10.94% by weight.
- the present invention unexpectedly found that the compounding of artemisia annua extract and oil-soluble ingredients (such as Schizonepeta parsnip extract and peony seed oil) has a better synergistic effect on skin anti-sensitivity, anti-inflammation and/or anti-irritation. Therefore, Artemisia annua extract can be used in combination with oil-soluble ingredients to achieve anti-allergic, anti-inflammatory and/or anti-irritant effects on the skin.
- oil-soluble ingredients such as Schizonepeta parsnip extract and peony seed oil
- the functional extract is Nepeta parsnip extract.
- the Schizonepeta parsnip extract is prepared using a supercritical extraction method. For example, it can be prepared using the HA220-50-06 supercritical extraction equipment of Jiangsu Nantong Huaan Supercritical Extraction Co., Ltd.
- the preparation of the Nepeta parsnip extract further includes a re-dissolving step. For example, absolute ethanol is used to achieve redissolution.
- the preparation of the Nepeta parsnip extract further includes a concentration step.
- the extract can be concentrated to an infusion.
- the preparation of the Schizonepeta parsnip extract further includes the step of adding anhydrous sodium sulfate.
- the preparation of Nepeta parsnip extract further includes a filtration step.
- cotton absorbent cotton ordinary grade, Shanghai Honglong
- the preparation of the Nepeta parsnip extract further includes an elution step.
- rice bran oil is used to achieve elution.
- Rice bran oil is a type of base oil.
- the preparation of Nepeta parsnip extract further includes The step of adding Tween 20 and pH 3.5 acetic acid-sodium acetate buffer (i.e. Buffer buffer). Oil-soluble ingredients will stratify when they meet water, so suspending agents (such as Tween) are often added during preparation to make them into suspensions to ensure that the experiment can proceed normally. Generally, the amount of Tween added is 10%. In a specific embodiment of the present invention, the Schizonepeta parsnip oil extract is finally formulated to have a solid content of 1%.
- the present invention provides a composition comprising an extract of Artemisia annua and an extract of Schizonepeta parsnip, wherein the weight ratio of the Artemisia annua extract to the Schizonepeta sapiens extract is 4:1 to 30:1. In a preferred embodiment, the weight ratio of the Artemisia annua extract to the Schizonepeta parsnip extract is 10:1 to 30:1. In a preferred embodiment, the weight ratio of the Artemisia annua extract to the Schizonepeta parsnip extract is 10:1 to 25:1.
- the functional extract is peony seed oil.
- Peony seed oil also known as peony oil, is made from peony seeds as raw materials, and is finally made through a series of extraction processes by pressing or other extraction techniques.
- the peony seed oil provided by Heze Hi-Tech Peony Application Research Institute is used. Oil-soluble ingredients will stratify when they meet water, so suspending agents (such as Tween) are often added during preparation to make them into suspensions to ensure that the experiment can proceed normally. Generally, the amount of Tween added is 10%.
- the present invention provides a composition comprising artemisia annua extract and peony seed oil, wherein the weight ratio of artemisia annua extract and peony seed oil is 3:1 to 33:1. In a preferred embodiment, the weight ratio of Artemisia annua extract to peony seed oil is 10:1 to 33:1.
- composition comprising artemisia annua extract and oil-soluble components of the present invention can be used as a compound functional additive in external skin preparations.
- the external skin agent is selected from: facial cleanser, lotion, lotion, cream, gel, and facial mask. Different dosages are added according to different types of preparations.
- an external preparation for skin which includes a composition of an Artemisia annua extract and an oil-soluble component and an excipient acceptable in the field of cosmetics.
- the external agent for skin is a general term for all ingredients commonly used on the outside of the skin, and may be, for example, a cosmetic composition or a pharmaceutical composition.
- the cosmetic composition may include basic cosmetics, facial makeup cosmetics, body cosmetics, hair care cosmetics, etc. There are no special restrictions on the dosage form and can be selected appropriately according to different purposes.
- the cosmetic composition also contains different cosmetically acceptable media or matrix excipients depending on the dosage form and purpose.
- Topical skin preparations contain a dermatologically acceptable carrier or vehicle (e.g., lotions, creams, soft ointments, detergents, etc.).
- a dermatologically acceptable carrier or vehicle e.g., lotions, creams, soft ointments, detergents, etc.
- a carrier capable of dissolving or dispersing these components at the concentrations described above based on common knowledge in the art.
- a carrier When a carrier is used, it should not cause inactivation of the Artemisia annua extract or oil-soluble ingredients and should not cause any adverse effects on the skin when used.
- the skin external preparation of the present invention may be in the form of a topical application product, which can be applied externally to the skin, and can be prepared by those ordinary techniques known in the art.
- the carrier may take various practical forms, such as creams, dressings, gels, lotions, ointments or liquids, which comprise the composition for application and cleansing, and they may be added to, for example, dry or A wet applicator, hydrogel matrix, or adhesive (or non-adhesive) patch material carrier.
- the carrier is a gel or moisturizing lotion, or an application in dry or wet form.
- Typical carriers include emulsions containing water and/or alcohol and an emollient, such as hydrocarbon oils and waxes, silicone oils, hyaluronic acid, vegetable, animal or marine fats or oils, glyceride derivatives, Fatty acids, or fatty acid esters or alcohols or alcohol ethers, lanolin and its derivatives, polyols or esters, wax esters, sterols, phospholipids, etc., generally emulsifiers (nonionic, cationic or anionic), Although some emollients have emulsifying properties of their own. Additionally, these same components may be formulated into creams, gels, or solid sticks using different ratios of their components and/or by incorporating thickening agents such as gums or other forms of hydrophilic colloids.
- an emollient such as hydrocarbon oils and waxes, silicone oils, hyaluronic acid, vegetable, animal or marine fats or oils, glyceride derivatives, Fatty acids
- the skin external preparation of the present invention may contain additional components commonly found in skin care compositions, such as emollients, skin conditioners, emulsifiers, preservatives, antioxidants, fragrances, chelating agents, etc., as long as they are compatible with the skin.
- additional components commonly found in skin care compositions, such as emollients, skin conditioners, emulsifiers, preservatives, antioxidants, fragrances, chelating agents, etc., as long as they are compatible with the skin.
- the other components of the topical preparation are physically and chemically compatible.
- one or more preservatives may be used. Suitable preservatives include parahydroxyacetophenone, C1-C4 alkyl parabens and phenoxyethanol.
- the preservative is present in an amount of from about 0.5 to about 2% by weight, preferably from about 0.5 to 1% by weight, based on the total weight of the composition.
- one or more antioxidants may be used. Suitable antioxidants include butylated hydroxytoluene (BHT), ascorbyl palmitate (BHA), butylated hydroxyaniline Ether, phenyl-alpha-naphthylamine, hydroquinone, propyl gallate, nordihydroguaiaretic acid, vitamin E or derivatives of vitamin E, vitamin C and its derivatives, calcium pantothenate, green tea extract and Mixed polyphenols, and mixtures of the substances mentioned above.
- the antioxidant is used in an amount ranging from about 0.02 to 0.5% by weight, more most preferably from about 0.002 to 0.1% by weight, based on the total weight of the composition.
- one or more emollients may be used that act as a lubricant to reduce flaking by their ability to remain on the skin surface or in the stratum corneum, Improves the appearance of skin.
- Typical emollients include fatty esters, fatty alcohols, mineral oils, polyethersiloxane copolymers, and the like.
- emollients include, without limitation, polypropylene glycol ("PPG")-15 octadecyl ether, PPG-10 cetyl ether, Steareth-10, Oleth-8, PPG-4 dodecane Ether, vitamin E acetate, lanolin, cetyl alcohol, cetearyl ethyl hexanoate, cetostearyl alcohol, glyceryl stearate, octyl hydroxystearate, dimethylpolysiloxane alkanes, and their combinations. Cetyl alcohol, cetearyl ethylhexanoate, cetearyl alcohol, glycerol stearate and combinations thereof are preferred.
- the emollient may be present in an amount ranging from about 0.1 to about 30%, preferably from about 1 to about 30% by weight, based on the total weight of the composition.
- one or more humectants may be used.
- Moisturizers are also called humectants, which help to increase the effectiveness of emollient, reduce flaking, stimulate the removal of flaky skin and improve skin feel.
- Polyols can be used as humectants, including but not limited to, glycerin, polyalkylene glycols, alkylene polyols and their derivatives, including butylene glycol, propylene glycol, dipropylene glycol, polyglycerol, polyethylene glycol Alcohols and their derivatives, sorbitol, hydroxypropyl sorbitol, hexanediol, 1,3-dibutanediol, 1,2,6-hexanetriol, ethoxylated glycerin, propoxylated glycerin, and their combinations.
- the humectant is present in an amount from about 0.1 to about 20% by weight, preferably from about 1 to about 15% by weight, based on the total weight of the composition.
- one or more emulsifiers may be used.
- Emulsifiers can be used within an effective stabilizing amount.
- the emulsifier is used in an amount from about 1.0 to about 10.0% by weight, more preferably from about 3.0 to about 6.0% by weight, based on the total weight of the composition.
- Any emulsifier compatible with the components of the composition may be used.
- Suitable emulsifiers include stearic acid, cetyl alcohol, glyceryl stearate, lecithin, stearyl alcohol, Steareth-2, Steareth-20, acrylic/C10-30 alkanol acrylate cross-links Polymers, and their combinations.
- one or more pH adjusters may be used.
- Useful pH adjusters in the skin external preparations of the present invention include tromethamine.
- the pH adjuster is present in an amount of from about 0.1 to about 2% by weight, preferably from about 0.1 to about 1% by weight, based on the total weight of the composition.
- the skin external preparation includes acrylic/C10-30 alkanol acrylate crosspolymer, glycerin, p-hydroxyacetophenone, glyceryl stearate and lecithin, /stearyl alcohol, cetearyl ethylhexanoate, tromethamine or combinations thereof.
- the dosage of the composition of Artemisia annua extract and oil-soluble ingredients in the external skin preparation is 0.001%-0.2% (w/w), and the preferred weight percentage is 0.007%-0.1% (w /w), the more preferred weight percentage is 0.007%-0.08% (w/w), and the most preferred weight percentage is 0.007%-0.056% (w/w).
- Buffer buffer acetic acid-sodium acetate buffer
- potassium tetraborate (national medicine reagent, analytical grade) and use 250ml of water to prepare a 0.4mol/L potassium borate solution for later use.
- T is the sample
- T0 is the sample control
- C is the blank
- C0 is the blank control
- IC50 ⁇ 10 mg/ml is excellent, IC50 ⁇ 30 mg/ml is good, IC50 ⁇ 50 mg/ml is average, and IC50 ⁇ 50 mg/ml has basically no application value.
- the extract of Example 2 has a certain ability to inhibit hyaluronidase as a single drug
- the extract of Example 3 has no ability to inhibit hyaluronidase
- the extract of Example 4 has a weak ability to inhibit hyaluronidase.
- the ability to inhibit hyaluronic acid is improved to a certain extent. force.
- Example 5 the compound ratio of Artemisia annua extract and Schizonepeta parsnip oil in Example 5 is 1:1, and the compound ratio of Artemisia annua extract and Schizonepeta parsnip oil in Example 7 is 1:1.
- the oil compounding ratio is 7:3.
- the IC 50 concentrations are greater than the IC 50 concentrations of the positive control sodium cromoglycate, they are still less than the single drug.
- Example 5 is preferred, and Example 7 is second preferred.
- the preparations of Examples 5-10 can be used in the preparation of external preparations for skin.
- the skin external preparation is preferably a cosmetic composition, such as lotion, essence, cream, etc.
- the weight percentage of the preparation in the skin external preparation is 0.08%-1% (w/w).
- the preferred weight percentage is 0.12%-0.64% (w/w).
- a more preferred weight percentage is 0.24%-0.5% (w/w).
- the most preferred weight percentage is 0.32%-0.48% (w/w).
Abstract
The present invention provides a use of a composition containing an Artemisia annua L. extract and an oil-soluble component in skin anti-allergy, anti-inflammation and/or anti-irritation, wherein the oil-soluble component is selected from a Herba Schizonepetae-Radix Saposhnikoviae extract and peony seed oil. The present invention also relates to a use of a composition containing an Artemisia annua L. extract and an oil-soluble component in preparation of a skin external preparation having a skin anti-allergy, anti-inflammation and/or anti-irritation effect, wherein the oil-soluble component is selected from a Herba Schizonepetae-Radix Saposhnikoviae extract and peony seed oil.
Description
本发明属于植物化学领域，具体涉及包含青蒿提取物和油溶性成分的组合物及其在皮肤外用剂或化妆品中的应用。The present invention belongs to the field of phytochemistry, and specifically relates to a composition containing Artemisia annua extract and oil-soluble components and its application in external skin agents or cosmetics.
过敏是由于外源物质进入人体，机体的免疫系统将此类物质识别为异物，致使免疫系统紊乱，引起过敏、炎症等症状。过敏反应根据其机理可分为I、II、III、IV型，而透明质酸酶是I型过敏反应的参与者，与炎症、过敏有强相关性。Allergy occurs when foreign substances enter the human body, and the body's immune system recognizes such substances as foreign bodies, causing immune system disorders and causing symptoms such as allergies and inflammation. Allergic reactions can be divided into types I, II, III, and IV according to their mechanisms, and hyaluronidase is a participant in type I allergic reactions and has a strong correlation with inflammation and allergy.
透明质酸酶是透明质酸的特异性裂解酶，而透明质酸在机体内显示出多种中药的生理功能，如润肤、促进伤口愈合等。根据研究报道，一些抗敏、抗炎药物有强抑制透明质酸酶活性，因此，抑制透明质酸酶活性作为研究抗炎作用的指标。Hyaluronidase is a specific cleavage enzyme of hyaluronic acid, and hyaluronic acid displays a variety of physiological functions of traditional Chinese medicine in the body, such as moisturizing and promoting wound healing. According to research reports, some anti-allergic and anti-inflammatory drugs strongly inhibit hyaluronidase activity. Therefore, inhibition of hyaluronidase activity is used as an indicator to study anti-inflammatory effects.
青蒿，为菊科黄花蒿Artemisia annua L.的全草。性苦、寒。归肝、胆、肾经。有清虚热，解暑截疟的作用。青蒿含有抗疟成分青蒿素，可直接杀灭疟原虫，现代研究表明青蒿提取物具有抑菌杀虫、解热抗炎、调节免疫的作用，同时还具有5种抗氧化活性的黄酮类成分，包括槲皮素等。Artemisia annua is the whole plant of Artemisia annua L. in the Asteraceae family. Bitter and cold in nature. Returns to the liver, gallbladder, and kidney meridians. It has the effect of clearing away heat, relieving heat and cutting off malaria. Artemisia annua contains the anti-malarial component artemisinin, which can directly kill malaria parasites. Modern research shows that artemisia annua extract has antibacterial and insecticidal, antipyretic and anti-inflammatory, and immune-regulating effects. It also has five kinds of flavonoids with antioxidant activity. Ingredients, including quercetin, etc.
荆芥，为唇形科荆芥Schizonepeta tenuifolia Briq.的地上部分。性辛、微温。归肺、肝经。具有发表散风，透疹消疮的作用。其水煎剂可增强皮肤血液循环，有微弱解热作用；对金黄色葡萄球菌具有较强抑菌作用；其甲醇提取物具有一定的镇痛和抗炎作用。Schizonepeta is the above-ground part of Schizonepeta tenuifolia Briq. in the family Lamiaceae. Pungent and slightly warm in nature. Returns to the lung and liver meridians. It has the effect of dispersing wind, resolving rash and sores. Its water decoction can enhance skin blood circulation and has a weak antipyretic effect; it has a strong antibacterial effect on Staphylococcus aureus; its methanol extract has certain analgesic and anti-inflammatory effects.
防风，为伞形科防风Saposhnikovia divaricate(Turez.)Schischk.的根。性辛、甘，微温。归膀胱、肝、脾经。能够发表散风，胜湿止痛，止痉止泻。防风富含挥发油、甘露醇、酚类、多糖等，具有解热、抗炎镇痛、抗惊厥作用，鲜汁对金黄色葡萄球菌有一定抗菌作用，煎剂则对痢疾杆菌有抑制作用。Windproof, the root of Saposhnikovia divaricate(Turez.)Schischk. Pungent, sweet, slightly warm in nature. Returns to the bladder, liver, and spleen meridians. It can dispel wind, overcome dampness and relieve pain, relieve spasm and diarrhea. Fructus sapsense is rich in volatile oil, mannitol, phenols, polysaccharides, etc. It has antipyretic, anti-inflammatory, analgesic, and anticonvulsant effects. The fresh juice has a certain antibacterial effect on Staphylococcus aureus, and the decoction has an inhibitory effect on Shigella dysenteriae.
牡丹籽油，又称牡丹油，由牡丹籽为原料，经压榨或其他提取技术经过一
系列提取工艺最终制成。Peony seed oil, also known as peony oil, is made from peony seeds and is processed through squeezing or other extraction techniques. The final product is made through a series of extraction processes.
按照透明质酸酶抑制的化学组成大致可分为多糖类、蛋白质类、生物碱类、萜类等。中药提取物除了包括水溶性成分之外，还包括诸如挥发油、木脂素类等油溶性成分。迄今为止，尚未见到这些油溶性成分具有透明质酸酶抑制活性的报道。According to the chemical composition of hyaluronidase inhibition, it can be roughly divided into polysaccharides, proteins, alkaloids, terpenes, etc. In addition to water-soluble components, traditional Chinese medicine extracts also include oil-soluble components such as volatile oils and lignans. To date, there have been no reports of hyaluronidase inhibitory activity among these oil-soluble ingredients.
本发明意外地发现，将青蒿提取物和油溶性成分(例如，如荆芥防风、牡丹籽油的油溶性成分)复配，具有优异的抑制透明质酸酶的作用。因此，包含青蒿提取物和油溶性成分的组合物可以作为复配型功效添加剂加入到皮肤外用剂中，以辅助止痒、湿疹问题等。The present invention unexpectedly found that compounding Artemisia annua extract and oil-soluble components (for example, oil-soluble components such as Schizonepeta sapiens and peony seed oil) has an excellent hyaluronidase inhibitory effect. Therefore, a composition containing artemisia annua extract and oil-soluble ingredients can be added as a compound functional additive to external skin preparations to assist in relieving itching, eczema, etc.
发明内容Contents of the invention
一方面，本发明提供了包含青蒿提取物和油溶性成分的组合物在皮肤抗敏、抗炎和/或抗刺激中的应用，其中，所述油溶性成分选自荆芥防风提取物和牡丹籽油。In one aspect, the present invention provides the application of a composition comprising an Artemisia annua extract and an oil-soluble component in skin anti-allergy, anti-inflammation and/or anti-irritation, wherein the oil-soluble component is selected from the group consisting of Schizonepeta sapiens extract and an oil-soluble component. Peony seed oil.
在优选的实施方式中，所述青蒿提取物采用超声提取法制备。在优选的实施方式中，所述青蒿提取物采用水作为溶剂提取。In a preferred embodiment, the Artemisia annua extract is prepared by ultrasonic extraction. In a preferred embodiment, the Artemisia annua extract is extracted using water as a solvent.
在优选的实施方式中，所述油溶性成分是荆芥防风提取物，青蒿提取物与荆芥防风提取物的重量比为4∶1至30∶1。在优选的实施方式中，所述油溶性成分是牡丹籽油，青蒿提取物与牡丹籽油的重量比为3∶1至33∶1。In a preferred embodiment, the oil-soluble component is Schizonepeta parsnip extract, and the weight ratio of Artemisia annua extract to Schizonepeta sapiens extract is 4:1 to 30:1. In a preferred embodiment, the oil-soluble component is peony seed oil, and the weight ratio of the Artemisia annua extract to the peony seed oil is 3:1 to 33:1.
在优选的实施方式中，所述抗炎、抗敏和/或抗刺激作用通过抑制透明质酸酶实现；或者用于辅助止痒和/或湿疹问题。In a preferred embodiment, the anti-inflammatory, anti-allergic and/or anti-irritant effects are achieved by inhibiting hyaluronidase; or used to assist in relieving itching and/or eczema problems.
另一方面，本发明提供了包含青蒿提取物和油溶性成分的组合物在制备具有皮肤抗敏、抗炎和/或抗刺激作用的皮肤外用剂中的应用，其中，所述油溶性成分选自荆芥防风提取物和牡丹籽油。On the other hand, the present invention provides the use of a composition comprising an Artemisia annua extract and an oil-soluble component in the preparation of a skin external preparation with skin anti-allergic, anti-inflammatory and/or anti-irritant effects, wherein the oil-soluble component Selected from Nepeta parsnip extract and peony seed oil.
在优选的实施方式中，所述皮肤外用剂选自：面霜、乳液、啫喱、化妆水、精华液、面膜、眼霜、气雾洁面泡、喷雾、沐浴露、洗面奶。In a preferred embodiment, the external skin agent is selected from the group consisting of: cream, lotion, gel, lotion, essence, facial mask, eye cream, aerosol cleansing foam, spray, shower gel, and facial cleanser.
附图简要说明Brief description of the drawings
图1显示了阳性对照透明质酸酶抑制实验的结果。
Figure 1 shows the results of the positive control hyaluronidase inhibition experiment.
图2显示了实施例2透明质酸酶抑制实验的结果。Figure 2 shows the results of the hyaluronidase inhibition experiment of Example 2.
图3显示了实施例3透明质酸酶抑制实验的结果。Figure 3 shows the results of the hyaluronidase inhibition experiment in Example 3.
图4显示了实施例4透明质酸酶抑制实验的结果。Figure 4 shows the results of the hyaluronidase inhibition experiment of Example 4.
图5显示了实施例5透明质酸酶抑制实验的结果。Figure 5 shows the results of the hyaluronidase inhibition experiment of Example 5.
图6显示了实施例6透明质酸酶抑制实验的结果。Figure 6 shows the results of the hyaluronidase inhibition experiment of Example 6.
图7显示了实施例7透明质酸酶抑制实验的结果。Figure 7 shows the results of the hyaluronidase inhibition experiment of Example 7.
图8显示了实施例8透明质酸酶抑制实验的结果。Figure 8 shows the results of the hyaluronidase inhibition experiment of Example 8.
图9显示了实施例9透明质酸酶抑制实验的结果。Figure 9 shows the results of the hyaluronidase inhibition experiment of Example 9.
图10显示了实施例10透明质酸酶抑制实验的结果。Figure 10 shows the results of the hyaluronidase inhibition experiment of Example 10.
本发明目的在于提供一种包含青蒿提取物和油溶性成分的组合物。具体地，将青蒿提取物与油溶性成分组合后，具有更优的抑制透明质酸酶的作用。因此，包含青蒿提取物和油溶性成分的组合物可作为复配型功效添加剂加入到护肤品中使用，以辅助止痒、湿疹问题等。The object of the present invention is to provide a composition containing Artemisia annua extract and oil-soluble components. Specifically, the combination of Artemisia annua extract and oil-soluble ingredients has a better effect on inhibiting hyaluronidase. Therefore, the composition containing Artemisia annua extract and oil-soluble ingredients can be added to skin care products as a compound functional additive to help relieve itching, eczema, etc.
为了提供更简明的描述，本文给出的一些数量表述没有用术语“约”修饰。应当理解，无论是否明确地使用了术语“约”，本文所给出的每个量都意在指代实际的给定值，并且还意在指代由本领域的普通技术人员可合理推测出的这些给定值的近似值，包括这些给定值的由实验和/或测量条件所引起的近似值。In order to provide a more concise description, some quantitative expressions given herein are not qualified by the term "about." It will be understood that, whether or not the term "about" is expressly used, each quantity given herein is intended to refer to the actual given value, and is also intended to refer to a value that may reasonably be inferred by one of ordinary skill in the art. Approximations of these given values include approximations of these given values resulting from experimental and/or measurement conditions.
为了提供更简洁的描述，本文中一些数量表述被叙述为约X量至约Y量的范围。应当理解，当叙述范围时，该范围并不限制于所叙述的上下界限，而应包括约X量至约Y量的整个范围或它们之间的任何量。In order to provide a more concise description, some quantities expressed herein are stated as ranging from about X amount to about Y amount. It should be understood that when a range is recited, the range is not limited to the upper and lower limits recited, but should include the entire range from about X amount to about Y amount or any amount therebetween.
青蒿提取物Artemisia annua extract
青蒿为菊科黄花蒿Artemisia annua L.的全草。性苦、寒。归肝、胆、肾经。有清虚热，解暑截疟的作用。青蒿含有抗疟成分青蒿素，可直接杀灭疟原虫，现代研究表明，青蒿提取物具有抑菌杀虫、解热抗炎、调节免疫的作用，同时还具有5种抗氧化活性的黄酮类成分，包括槲皮素等。Artemisia annua L. is the whole plant of Artemisia annua L. in the Asteraceae family. Bitter and cold in nature. Returns to the liver, gallbladder, and kidney meridians. It has the effect of clearing away heat, relieving heat and cutting off malaria. Artemisia annua contains the anti-malarial ingredient artemisinin, which can directly kill malaria parasites. Modern research shows that artemisia annua extract has antibacterial and insecticidal, antipyretic and anti-inflammatory, and immune-regulating effects. It also has five types of antioxidant activity. Flavonoids, including quercetin, etc.
在一些实施方式中，采用超声提取法提取青蒿提取物。超声提取特点
包括：1.缩短提取时间，每次超声只需要20min-30min，常规提取基本上1h-1.5h；2.常温提取，不破坏热敏成分；3.直接细胞破壁，有效成分提取较完全。在优选的实施方式中，超声提取的工艺参数如下：提取2次，每次20min，超声3s，间隙3s。In some embodiments, an ultrasonic extraction method is used to extract the Artemisia annua extract. Ultrasonic extraction characteristics Including: 1. Shorten the extraction time, each ultrasound only takes 20min-30min, and conventional extraction is basically 1h-1.5h; 2. Extraction at room temperature, without destroying heat-sensitive components; 3. Direct cell wall breaking, and the active ingredients are more completely extracted. In a preferred embodiment, the process parameters of ultrasonic extraction are as follows: extraction twice, 20 minutes each time, ultrasonic for 3 seconds, and gap of 3 seconds.
在一些实施方式中，提取溶剂是水(例如，去离子水)。在一些实施方式中，提取过程包括醇沉步骤。例如，采用95％的乙醇实现醇沉。在一些实施方式中，提取过程包括过滤步骤。在一些实施方式中，提取过程包括离心步骤。在一些实施方式中，提取过程还包括浓缩步骤。例如，浓缩至固含5-20重量％。在一个具体的实施方式中，浓缩至固含10.94重量％。In some embodiments, the extraction solvent is water (eg, deionized water). In some embodiments, the extraction process includes an alcohol precipitation step. For example, 95% ethanol is used to achieve alcohol precipitation. In some embodiments, the extraction process includes a filtering step. In some embodiments, the extraction process includes a centrifugation step. In some embodiments, the extraction process also includes a concentration step. For example, concentrate to a solid content of 5-20% by weight. In a specific embodiment, the solid content is concentrated to 10.94% by weight.
油溶性成分oil soluble ingredients
本发明意外地发现，青蒿提取物和油溶性成分(例如荆芥防风提取物和牡丹籽油)复配，在皮肤抗敏、抗炎和/或抗刺激方面有较好的协同作用。因此，可以将青蒿提取物与油溶性成分组合使用，实现皮肤抗敏、抗炎和/或抗刺激效果。The present invention unexpectedly found that the compounding of artemisia annua extract and oil-soluble ingredients (such as Schizonepeta parsnip extract and peony seed oil) has a better synergistic effect on skin anti-sensitivity, anti-inflammation and/or anti-irritation. Therefore, Artemisia annua extract can be used in combination with oil-soluble ingredients to achieve anti-allergic, anti-inflammatory and/or anti-irritant effects on the skin.
在一些实施方式中，功效提取物是荆芥防风提取物。在一些实施方式中，荆芥防风提取物采用超临界萃取方法制备。例如，可以采用江苏南通市华安超临界萃取有限公司的HA220-50-06型超临界萃取设备制备得到。在一些实施方式中，荆芥防风提取物的制备还包括再溶解的步骤。例如，采用无水乙醇实现再溶解。在一些实施方式中，荆芥防风提取物的制备还包括浓缩步骤。例如，可以将提取物浓缩至浸膏。在一些实施方式中，荆芥防风提取物的制备还包括加入无水硫酸钠的步骤。加入无水硫酸钠的作用是去除超临界萃取及加入无水乙醇后残余的水分，确保整个体系达到无水状态。每批次药材含水量会有所不同，因此1％～20％是通常加入量的范围，根据残余水分多少酌情添加。在一些实施方式中，荆芥防风提取物的制备还包括过滤步骤。例如，采用棉花(脱脂棉花普通级，上海宏隆)进行过滤。在一些实施方式中，荆芥防风提取物的制备还包括洗脱步骤。例如，采用米糠油实现洗脱。米糠油属于基础油的一种，超临界萃取物的量往往少，浓度高，因此往往需要用基础油稀释，米糠油作为天然来源，跟温和无刺激。在一些实施方式中，荆芥防风提取物的制备还包括
加入吐温20和pH 3.5的乙酸-乙酸钠缓冲液(即Buffer缓冲液)的步骤。油溶性成分遇水会分层，因此配制时常常加入助悬剂(例如吐温)使其成为混悬液，确保实验能正常进行。一般情况下，吐温加入量为10％。在本发明的具体实施方式中，最终配制成固含1％的荆芥防风油提取物。In some embodiments, the functional extract is Nepeta parsnip extract. In some embodiments, the Schizonepeta parsnip extract is prepared using a supercritical extraction method. For example, it can be prepared using the HA220-50-06 supercritical extraction equipment of Jiangsu Nantong Huaan Supercritical Extraction Co., Ltd. In some embodiments, the preparation of the Nepeta parsnip extract further includes a re-dissolving step. For example, absolute ethanol is used to achieve redissolution. In some embodiments, the preparation of the Nepeta parsnip extract further includes a concentration step. For example, the extract can be concentrated to an infusion. In some embodiments, the preparation of the Schizonepeta parsnip extract further includes the step of adding anhydrous sodium sulfate. The function of adding anhydrous sodium sulfate is to remove the residual moisture after supercritical extraction and the addition of absolute ethanol, ensuring that the entire system reaches an anhydrous state. The moisture content of each batch of medicinal materials will be different, so 1% to 20% is the usual range of adding amount. Add as appropriate according to the residual moisture. In some embodiments, the preparation of Nepeta parsnip extract further includes a filtration step. For example, cotton (absorbent cotton ordinary grade, Shanghai Honglong) is used for filtration. In some embodiments, the preparation of the Nepeta parsnip extract further includes an elution step. For example, rice bran oil is used to achieve elution. Rice bran oil is a type of base oil. The amount of supercritical extract is often small and the concentration is high, so it often needs to be diluted with base oil. As a natural source, rice bran oil is mild and non-irritating. In some embodiments, the preparation of Nepeta parsnip extract further includes The step of adding Tween 20 and pH 3.5 acetic acid-sodium acetate buffer (i.e. Buffer buffer). Oil-soluble ingredients will stratify when they meet water, so suspending agents (such as Tween) are often added during preparation to make them into suspensions to ensure that the experiment can proceed normally. Generally, the amount of Tween added is 10%. In a specific embodiment of the present invention, the Schizonepeta parsnip oil extract is finally formulated to have a solid content of 1%.
在一些实施方式中，本发明提供了包含青蒿提取物与荆芥防风提取物的组合物，其中，青蒿提取物与荆芥防风提取物的重量比为4∶1至30∶1。在优选的实施方式中，青蒿提取物与荆芥防风提取物的重量比为10∶1至30∶1。在优选的实施方式中，青蒿提取物与荆芥防风提取物的重量比为10∶1至25∶1。In some embodiments, the present invention provides a composition comprising an extract of Artemisia annua and an extract of Schizonepeta parsnip, wherein the weight ratio of the Artemisia annua extract to the Schizonepeta sapiens extract is 4:1 to 30:1. In a preferred embodiment, the weight ratio of the Artemisia annua extract to the Schizonepeta parsnip extract is 10:1 to 30:1. In a preferred embodiment, the weight ratio of the Artemisia annua extract to the Schizonepeta parsnip extract is 10:1 to 25:1.
在一些实施方式中，功效提取物是牡丹籽油。牡丹籽油又称牡丹油，由牡丹籽为原料，经压榨或其他提取技术经过一系列提取工艺最终制成。在具体的实施方式中，采用菏泽市高科牡丹应用研究所提供的牡丹籽油。油溶性成分遇水会分层，因此配制时常常加入助悬剂(例如吐温)使其成为混悬液，确保实验能正常进行。一般情况下，吐温加入量为10％。In some embodiments, the functional extract is peony seed oil. Peony seed oil, also known as peony oil, is made from peony seeds as raw materials, and is finally made through a series of extraction processes by pressing or other extraction techniques. In a specific implementation, the peony seed oil provided by Heze Hi-Tech Peony Application Research Institute is used. Oil-soluble ingredients will stratify when they meet water, so suspending agents (such as Tween) are often added during preparation to make them into suspensions to ensure that the experiment can proceed normally. Generally, the amount of Tween added is 10%.
在一些实施方式中，本发明提供了包含青蒿提取物与牡丹籽油的组合物，其中，青蒿提取物与牡丹籽油的重量比为3∶1至33∶1。在优选的实施方式中，青蒿提取物与牡丹籽油的重量比为10∶1至33∶1。In some embodiments, the present invention provides a composition comprising artemisia annua extract and peony seed oil, wherein the weight ratio of artemisia annua extract and peony seed oil is 3:1 to 33:1. In a preferred embodiment, the weight ratio of Artemisia annua extract to peony seed oil is 10:1 to 33:1.
皮肤外用剂Skin external preparations
本发明包含青蒿提取物与油溶性成分的组合物可以作为复合功效添加剂应用于皮肤外用剂中。在一些实施方式中，所述皮肤外用剂选自：洁面乳、化妆水、乳液、膏霜、啫喱、面膜。根据制剂的不同类型添加不同的用量。The composition comprising artemisia annua extract and oil-soluble components of the present invention can be used as a compound functional additive in external skin preparations. In some embodiments, the external skin agent is selected from: facial cleanser, lotion, lotion, cream, gel, and facial mask. Different dosages are added according to different types of preparations.
另一方面，提供了一种皮肤外用剂，所述皮肤外用剂包含青蒿提取物与油溶性成分的组合物及化妆品领域可接受的赋形剂。On the other hand, an external preparation for skin is provided, which includes a composition of an Artemisia annua extract and an oil-soluble component and an excipient acceptable in the field of cosmetics.
所述皮肤外用剂是通常用于皮肤外部的所有成分的统称概念，例如可以是化妆品组合物或药物组合物。所述化妆品组合物中可以是基础化妆品、面部妆容化妆品、身体用化妆品、头发护理用化妆品等，对其剂型无特殊限制，根据不同目的可合理选择。所述化妆品组合物中根据剂型和目的的不同还含有不同的化妆品学层面允许的介质或基质赋形剂。The external agent for skin is a general term for all ingredients commonly used on the outside of the skin, and may be, for example, a cosmetic composition or a pharmaceutical composition. The cosmetic composition may include basic cosmetics, facial makeup cosmetics, body cosmetics, hair care cosmetics, etc. There are no special restrictions on the dosage form and can be selected appropriately according to different purposes. The cosmetic composition also contains different cosmetically acceptable media or matrix excipients depending on the dosage form and purpose.
皮肤外用剂含有皮肤学上可接受的载体或媒介物(例如，洗液、面霜、软
膏、清洁剂等等)。本领域普通技术人员能够根据本领域公知常识，选择能够以上文所述的浓度溶解或分散这些组分的载体。当使用一种载体时，该载体应当不会导致青蒿提取物或油溶性成分的灭活，而且在使用时不会在皮肤上带来任何相反的作用。Topical skin preparations contain a dermatologically acceptable carrier or vehicle (e.g., lotions, creams, soft ointments, detergents, etc.). Those of ordinary skill in the art can select a carrier capable of dissolving or dispersing these components at the concentrations described above based on common knowledge in the art. When a carrier is used, it should not cause inactivation of the Artemisia annua extract or oil-soluble ingredients and should not cause any adverse effects on the skin when used.
本领域普通技术人员能够根据公知常识和它们以最适用于处理时活性组分的浓度而溶解或分散在活性组分中的能力来选择适宜的载体，所述载体例如包括水、醇类、油等。One of ordinary skill in the art will be able to select suitable carriers, including, for example, water, alcohols, oils, etc., based on common knowledge and their ability to dissolve or disperse the active ingredient in a concentration most suitable for treatment. wait.
本发明的皮肤外用剂可以是局部施用产品的形式，其能够从外部施用在皮肤上，并能够以本领域公知的那些普通技术制备。载体可以具有各种实际的形式，例如面霜，敷料，凝胶，洗液，软膏或者液体，其包括敷用和清洗掉的组合物，以及用本领域公知的方法将它们加入到例如干的或湿的涂抹物，水凝胶基质，或粘性(或非粘性)贴片的材料载体中。优选地，载体是一种凝胶或增加水分的洗剂，或者以干或湿的形式的涂抹物。The skin external preparation of the present invention may be in the form of a topical application product, which can be applied externally to the skin, and can be prepared by those ordinary techniques known in the art. The carrier may take various practical forms, such as creams, dressings, gels, lotions, ointments or liquids, which comprise the composition for application and cleansing, and they may be added to, for example, dry or A wet applicator, hydrogel matrix, or adhesive (or non-adhesive) patch material carrier. Preferably, the carrier is a gel or moisturizing lotion, or an application in dry or wet form.
典型的载体包括包含水和/或醇和润肤剂的乳剂，其中润肤剂是例如烃的油和蜡，硅油，透明质酸，植物、动物或海洋生物的脂肪或油，甘油酯衍生物，脂肪酸、或脂肪酸酯或醇或醇醚，羊毛脂及其衍生物，多元醇或酯，蜡酯，甾醇，磷脂等等，一般还有乳化剂(非离子的，阳离子的或阴离子的)，尽管一些润肤剂本身具有乳化特性。另外，可以利用其组分的不同比例和/或通过掺入例如树胶或其他形式的亲水胶体的增稠剂将这些相同组分配制成面霜、凝胶、或固体棒。Typical carriers include emulsions containing water and/or alcohol and an emollient, such as hydrocarbon oils and waxes, silicone oils, hyaluronic acid, vegetable, animal or marine fats or oils, glyceride derivatives, Fatty acids, or fatty acid esters or alcohols or alcohol ethers, lanolin and its derivatives, polyols or esters, wax esters, sterols, phospholipids, etc., generally emulsifiers (nonionic, cationic or anionic), Although some emollients have emulsifying properties of their own. Additionally, these same components may be formulated into creams, gels, or solid sticks using different ratios of their components and/or by incorporating thickening agents such as gums or other forms of hydrophilic colloids.
本发明的皮肤外用剂可以包含在皮肤护理组合物中通常能找到的附加组分，例如润肤剂、皮肤调节剂、乳化剂、防腐剂、抗氧化剂、香料、螯合剂等，只要它们与皮肤外用剂中其他的组分在物理上和化学上相容即可。The skin external preparation of the present invention may contain additional components commonly found in skin care compositions, such as emollients, skin conditioners, emulsifiers, preservatives, antioxidants, fragrances, chelating agents, etc., as long as they are compatible with the skin. The other components of the topical preparation are physically and chemically compatible.
在本发明的皮肤外用剂的一些实施方式中，可使用一种或多种防腐剂。适宜的防腐剂包括对羟基苯乙酮、C1-C4对羟基苯甲酸烷基酯和苯氧基乙醇。基于组合物总重量，防腐剂的用量为大约0.5至大约2重量％，优选大约0.5至1重量％。In some embodiments of the topical skin preparations of the present invention, one or more preservatives may be used. Suitable preservatives include parahydroxyacetophenone, C1-C4 alkyl parabens and phenoxyethanol. The preservative is present in an amount of from about 0.5 to about 2% by weight, preferably from about 0.5 to 1% by weight, based on the total weight of the composition.
在本发明的皮肤外用剂的一些实施方式中，可使用一种或多种抗氧化剂。适宜的抗氧化剂包括丁化羟基甲苯(BHT)、抗坏血酸棕榈酸酯(BHA)、丁羟茴
醚、苯基-α-萘基胺、氢醌、没食子丙酯、去甲二氢愈创木酸、维生素E或维生素E的衍生物、维生素C及其衍生物、泛酸钙、绿茶提取物和混合的多酚，以及上面所述的物质的混合物。所使用的抗氧化剂是组合物总重量的大约0.02至0.5重量％，更最优选的是从大约0.002至0.1重量％的用量范围。In some embodiments of the skin external preparation of the present invention, one or more antioxidants may be used. Suitable antioxidants include butylated hydroxytoluene (BHT), ascorbyl palmitate (BHA), butylated hydroxyaniline Ether, phenyl-alpha-naphthylamine, hydroquinone, propyl gallate, nordihydroguaiaretic acid, vitamin E or derivatives of vitamin E, vitamin C and its derivatives, calcium pantothenate, green tea extract and Mixed polyphenols, and mixtures of the substances mentioned above. The antioxidant is used in an amount ranging from about 0.02 to 0.5% by weight, more most preferably from about 0.002 to 0.1% by weight, based on the total weight of the composition.
在本发明的皮肤外用剂的一些实施方式中，可使用一种或多种润肤剂，通过其保持在皮肤表面上或在角质层中的能力，起到润滑剂的作用，以减少剥落，改善皮肤的外观。典型的润肤剂包括脂肪酯、脂肪醇、矿物油、聚醚硅氧烷共聚物等等。适宜的润肤剂的例子非限定地包括，聚丙二醇(“PPG”)-15十八烷基醚，PPG-10十六烷基醚，Steareth-10，Oleth-8，PPG-4十二烷基醚，维生素E醋酸酯，羊毛脂，鲸蜡醇，鲸蜡硬脂醇乙基己酸酯，十六十八醇，甘油硬脂酸酯，羟基硬脂酸辛脂，二甲基聚硅氧烷，以及它们的组合。鲸蜡醇，鲸蜡硬脂醇乙基己酸酯，十六十八醇，甘油硬脂酸酯以及它们的组合是优选的。使用时，润肤剂是基于组合物总重量的大约0.1至大约30重量％，优选大约1至大约30重量％的用量范围。In some embodiments of the skin topicals of the present invention, one or more emollients may be used that act as a lubricant to reduce flaking by their ability to remain on the skin surface or in the stratum corneum, Improves the appearance of skin. Typical emollients include fatty esters, fatty alcohols, mineral oils, polyethersiloxane copolymers, and the like. Examples of suitable emollients include, without limitation, polypropylene glycol ("PPG")-15 octadecyl ether, PPG-10 cetyl ether, Steareth-10, Oleth-8, PPG-4 dodecane Ether, vitamin E acetate, lanolin, cetyl alcohol, cetearyl ethyl hexanoate, cetostearyl alcohol, glyceryl stearate, octyl hydroxystearate, dimethylpolysiloxane alkanes, and their combinations. Cetyl alcohol, cetearyl ethylhexanoate, cetearyl alcohol, glycerol stearate and combinations thereof are preferred. When used, the emollient may be present in an amount ranging from about 0.1 to about 30%, preferably from about 1 to about 30% by weight, based on the total weight of the composition.
在本发明的皮肤外用剂的一些实施方式中，可使用一种或多种保湿剂。保湿剂也称为湿润剂，其有助于提高润肤剂的效果，减少剥落，刺激组成的鳞皮的去除和提高皮肤触感。可使用多元醇作为保湿剂，包括但并不限于，甘油，聚亚烷基二醇，亚烷基多元醇及其衍生物，包含丁二醇、丙二醇、双丙二醇，聚丙三醇，聚乙二醇及其衍生物，山梨醇，羟丙基山梨醇，己二醇，1，3-二丁二醇，1，2，6-己三醇，乙氧基化甘油，丙氧基化甘油，以及它们的组合。使用时，基于组合物的总重量，保湿剂的用量为大约0.1至大约20重量％，优选是大约1至大约15重量％。In some embodiments of the skin external preparation of the present invention, one or more humectants may be used. Moisturizers are also called humectants, which help to increase the effectiveness of emollient, reduce flaking, stimulate the removal of flaky skin and improve skin feel. Polyols can be used as humectants, including but not limited to, glycerin, polyalkylene glycols, alkylene polyols and their derivatives, including butylene glycol, propylene glycol, dipropylene glycol, polyglycerol, polyethylene glycol Alcohols and their derivatives, sorbitol, hydroxypropyl sorbitol, hexanediol, 1,3-dibutanediol, 1,2,6-hexanetriol, ethoxylated glycerin, propoxylated glycerin, and their combinations. When used, the humectant is present in an amount from about 0.1 to about 20% by weight, preferably from about 1 to about 15% by weight, based on the total weight of the composition.
在本发明的皮肤外用剂的一些实施方式中，可使用一种或多种乳化剂。乳化剂可在有效稳定量的范围内使用。优选地，在组合物总重量的基础上，以大约1.0至大约10.0重量％，更优选的是大约3.0至大约6.0重量％的用量来使用乳化剂。可以使用任何与组合物中的组分相容的乳化剂。适宜的乳化剂包括硬脂酸，鲸蜡醇，甘油硬脂酸酯，卵磷脂，十八烷醇，Steareth-2，Steareth-20，丙烯酸(酯)类/C10-30烷醇丙烯酸酯交联聚合物，以及它们的组合。In some embodiments of the skin external preparation of the present invention, one or more emulsifiers may be used. Emulsifiers can be used within an effective stabilizing amount. Preferably, the emulsifier is used in an amount from about 1.0 to about 10.0% by weight, more preferably from about 3.0 to about 6.0% by weight, based on the total weight of the composition. Any emulsifier compatible with the components of the composition may be used. Suitable emulsifiers include stearic acid, cetyl alcohol, glyceryl stearate, lecithin, stearyl alcohol, Steareth-2, Steareth-20, acrylic/C10-30 alkanol acrylate cross-links Polymers, and their combinations.
在本发明的皮肤外用剂的一些实施方式中，可使用一种或多种pH调节剂。
本发明的皮肤外用剂中有益的pH调节剂包括氨丁三醇。使用时，基于组合物的总重量pH调节剂的用量为大约0.1至大约2重量％，优选是大约0.1至大约1重量％。In some embodiments of the skin external preparation of the present invention, one or more pH adjusters may be used. Useful pH adjusters in the skin external preparations of the present invention include tromethamine. When used, the pH adjuster is present in an amount of from about 0.1 to about 2% by weight, preferably from about 0.1 to about 1% by weight, based on the total weight of the composition.
在本发明的一些实施方式中，皮肤外用剂包含丙烯酸(酯)类/C10-30烷醇丙烯酸酯交联聚合物、甘油、对羟基苯乙酮、甘油硬脂酸酯和卵磷脂、十六/十八醇、鲸蜡硬脂醇乙基己酸酯、氨丁三醇或它们的组合。In some embodiments of the present invention, the skin external preparation includes acrylic/C10-30 alkanol acrylate crosspolymer, glycerin, p-hydroxyacetophenone, glyceryl stearate and lecithin, /stearyl alcohol, cetearyl ethylhexanoate, tromethamine or combinations thereof.
在本发明的一些实施方式中，皮肤外用剂中青蒿提取物与油溶性成分的组合物的用量为0.001％-0.2％(w/w)，优选的重量百分比为0.007％-0.1％(w/w)，更优选的重量百分比为0.007％-0.08％(w/w)，最优选的重量百分比为0.007％-0.056％(w/w)。In some embodiments of the present invention, the dosage of the composition of Artemisia annua extract and oil-soluble ingredients in the external skin preparation is 0.001%-0.2% (w/w), and the preferred weight percentage is 0.007%-0.1% (w /w), the more preferred weight percentage is 0.007%-0.08% (w/w), and the most preferred weight percentage is 0.007%-0.056% (w/w).
实施例Example
下面结合具体实施例，以进一步阐述本发明。有必要在此指出的是，实施例只用于对本发明进行进一步的说明，不能理解为对本发明保护范围的限制，该领域的技术熟练人员可以根据上述本发明的内容做出一些非本质的改进和调整。下列实施例中未注明具体条件的试验方法，通常按照常规条件，或按照制造厂商所建议的条件。除非另有说明，所有的百分比和份数按重量计。The present invention will be further described below in conjunction with specific embodiments. It is necessary to point out here that the examples are only used to further illustrate the present invention and cannot be understood as limiting the protection scope of the present invention. Those skilled in the field can make some non-essential improvements based on the above content of the present invention. and adjustments. Test methods without specifying specific conditions in the following examples usually follow conventional conditions or conditions recommended by the manufacturer. All percentages and parts are by weight unless otherwise stated.
以下实施例中采用的实验材料如下：
The experimental materials used in the following examples are as follows:
The experimental materials used in the following examples are as follows:
实施例1：青蒿提取物的制备Example 1: Preparation of Artemisia annua Extract
称取青蒿100g，用1倍去离子水超声提取2次，过滤，煎煮浓缩，加入一定量95％乙醇醇沉(终浓度70％)，滤纸(新星牌定性滤纸，规格60*60cm)过滤，滤液于55℃条件下浓缩，4℃静置过夜，取出3℃ 3500rpm条件下离心15min(卢湘仪，DL-5M)，滤纸过滤，最终配制成固含10.94％溶液，备用。Weigh 100g of Artemisia annua, extract it twice with 1x deionized water by ultrasonic, filter, boil and concentrate, add a certain amount of 95% ethanol to precipitate (final concentration 70%), filter paper (Xinxing brand qualitative filter paper, specification 60*60cm) Filter, concentrate the filtrate at 55°C, let it stand overnight at 4°C, take out and centrifuge at 3°C and 3500rpm for 15min (Lu Xiangyi, DL-5M), filter with filter paper, and finally prepare a solution with a solid content of 10.94% for later use.
实施例2：青蒿提取物的制备Example 2: Preparation of Artemisia annua Extract
取实施例1制备的固含10.94％青蒿提取物样品10.94g，加入去离子水，配制成固含1％溶液，备用。Take 10.94g of the Artemisia annua extract sample prepared in Example 1 with a solid content of 10.94%, add deionized water to prepare a solution with a solid content of 1%, and set aside.
实施例3：荆芥防风提取物的制备Example 3: Preparation of Schizonepeta parsnip extract
取59ml冰醋酸加水稀释至1000ml，用玻璃棒搅拌均匀，再用10倍水稀释配制成0.1mol/L的溶液A，备用；取8.203g无水乙酸钠溶于1000ml水中，用玻璃棒搅拌均匀，再用10倍水稀释配制成0.1mol/L的溶液B，备用；按溶液A∶溶液B体积比16∶1，最终配制成pH3.5的乙酸-乙酸钠缓冲液(以下简称Buffer缓冲液)，备用。Take 59ml of glacial acetic acid and dilute it to 1000ml with water, stir it evenly with a glass rod, then dilute it 10 times with water to prepare a 0.1mol/L solution A, and set it aside; take 8.203g of anhydrous sodium acetate and dissolve it in 1000ml of water, and stir it evenly with a glass rod. , and then dilute it with 10 times of water to prepare a 0.1 mol/L solution B for later use; according to the volume ratio of solution A: solution B 16:1, finally prepare a pH 3.5 acetic acid-sodium acetate buffer (hereinafter referred to as Buffer buffer) ),spare.
称取荆芥∶防风(1∶1)1400g，打粗粉，用超临界萃取设备(江苏南通市华安超临界萃取有限公司，HA220-50-06)萃取(萃取溶剂仅为C02，萃取釜温度45℃，萃取釜压力16MPa，分离釜温度35℃，分离釜压力4MPa)至无油状态。加入无水乙醇溶解，于55℃旋转蒸发仪上浓缩至浸膏。加入10％无水硫酸钠，去除超临界萃取及加入无水乙醇后残余的水分，确保整个体系达到无水状态。4℃静置过夜，棉花(脱脂棉花普通级，上海宏隆)过滤，用米糠油洗脱溶解，加入吐温20(10％)，与Buffer缓冲液混匀，最终配制成固含1％的荆芥防风油溶液混悬液，备用。
Weigh 1400g of Schizonepeta: Fangfeng (1:1), grind into coarse powder, and extract with supercritical extraction equipment (Jiangsu Nantong Huaan Supercritical Extraction Co., Ltd., HA220-50-06) (the extraction solvent is only C02, the temperature of the extraction kettle 45℃, extraction kettle pressure 16MPa, separation kettle temperature 35℃, separation kettle pressure 4MPa) to an oil-free state. Add absolute ethanol to dissolve, and concentrate on a 55°C rotary evaporator to extract. Add 10% anhydrous sodium sulfate to remove the residual moisture after supercritical extraction and adding absolute ethanol to ensure that the entire system reaches an anhydrous state. Let it stand overnight at 4°C, filter with cotton (ordinary grade of skim cotton, Shanghai Honglong), elute and dissolve with rice bran oil, add Tween 20 (10%), mix with Buffer, and finally prepare a solution of Jingpa with a solid content of 1%. Mustard parsnip oil solution suspension, set aside.
实施例4：牡丹籽油的制备Example 4: Preparation of peony seed oil
取牡丹籽油10g，加入吐温20(10％)和Buffer缓冲液混匀，最终配制成固含1％的牡丹籽油溶液混悬液，备用。Take 10g of peony seed oil, add Tween 20 (10%) and Buffer, mix well, and finally prepare a peony seed oil solution suspension with a solid content of 1% for later use.
实施例5：青蒿提取物的制备Example 5: Preparation of Artemisia annua Extract
将实施例1提取物：实施例3提取物按照重量比1∶1混合制备，备用。Prepare by mixing the extract of Example 1: the extract of Example 3 at a weight ratio of 1:1 and set aside.
实施例6：青蒿提取物的制备Example 6: Preparation of Artemisia annua Extract
将实施例1提取物：实施例3提取物按照重量比3∶7混合制备，备用。Mix the extract of Example 1 and the extract of Example 3 according to a weight ratio of 3:7 and prepare for later use.
实施例7：青蒿提取物的制备Example 7: Preparation of Artemisia annua Extract
将实施例1提取物：实施例3提取物按照重量比7∶3混合制备，备用。Mix the extract of Example 1 and the extract of Example 3 according to a weight ratio of 7:3 and set aside.
实施例8：青蒿提取物的制备Example 8: Preparation of Artemisia annua Extract
将实施例1提取物：实施例4提取物按照重量比1∶1混合制备，备用。Mix the extract of Example 1: the extract of Example 4 at a weight ratio of 1:1 and prepare for later use.
实施例9：青蒿提取物的制备Example 9: Preparation of Artemisia annua Extract
将实施例1提取物：实施例4提取物按照重量比1∶3混合制备，备用。Mix the extract of Example 1 and the extract of Example 4 according to a weight ratio of 1:3 and set aside.
实施例10：青蒿提取物的制备Example 10: Preparation of Artemisia annua Extract
将实施例1提取物：实施例4提取物按照重量比3∶1混合制备，备用。Mix the extract of Example 1 and the extract of Example 4 according to a weight ratio of 3:1 and prepare for later use.
实施例11：透明质酸酶活性抑制评价Example 11: Evaluation of hyaluronidase activity inhibition
取59ml冰醋酸(国药试剂，分析纯)加水稀释至1000ml，用玻璃棒搅拌均匀，再用10倍水稀释配制成0.1mol/L的溶液A，备用。取8.203g无水乙酸钠(国药试剂，分析纯)溶于1000ml水中，用玻璃棒搅拌均匀，再用10倍水稀释配制成0.1mol/L的溶液B，备用。按溶液A∶溶液B体积比16∶1，最终配制成pH3.5的乙酸-乙酸钠缓冲液(以下简称Buffer缓冲液)，备用。
Take 59ml of glacial acetic acid (Chinese medicine reagent, analytical grade), add water and dilute to 1000ml, stir evenly with a glass rod, then dilute 10 times with water to prepare 0.1mol/L solution A, set aside. Dissolve 8.203g anhydrous sodium acetate (Chinese medicine reagent, analytical grade) in 1000ml water, stir evenly with a glass rod, then dilute it 10 times with water to prepare a 0.1mol/L solution B, set aside. According to the volume ratio of solution A: solution B of 16:1, the acetic acid-sodium acetate buffer solution (hereinafter referred to as Buffer buffer) with pH 3.5 is finally prepared for later use.
取透明质酸酶(活力≥560units/mg，sigma)0.1411g，用10ml Buffer缓冲液配制成酶活≥7900units/ml的透明质酸酶溶液，临用配制。Take 0.1411g of hyaluronidase (activity ≥560 units/mg, sigma) and use 10 ml Buffer to prepare a hyaluronidase solution with enzyme activity ≥ 7900 units/ml for immediate use.
取无水氯化钙(国药试剂，分析纯)0.1387g，用100ml水配制成12.5mmol/L的氯化钙溶液，备用。Take 0.1387g of anhydrous calcium chloride (Chinese medicine reagent, analytical grade) and use 100ml of water to prepare a 12.5mmol/L calcium chloride solution for later use.
取透明质酸钠(东辰集团)0.12g，用100ml Buffer缓冲液配制成1.2mg/ml的透明质酸钠溶液，备用。Take 0.12g of sodium hyaluronate (Dongchen Group) and use 100ml Buffer to prepare a 1.2mg/ml sodium hyaluronate solution for later use.
取氢氧化钠(国药试剂，分析纯)0.4g，用25ml水配制成0.4mol/L的氢氧化钠溶液，备用。Take 0.4g of sodium hydroxide (national medicine reagent, analytical grade) and use 25ml of water to prepare a 0.4mol/L sodium hydroxide solution for later use.
取四硼酸钾(国药试剂，分析纯)30.55g，用250ml水配制成0.4mol/L的硼酸钾溶液，备用。Take 30.55g of potassium tetraborate (national medicine reagent, analytical grade) and use 250ml of water to prepare a 0.4mol/L potassium borate solution for later use.
取浓盐酸(国药试剂，分析纯)41.4ml，用8.5ml水配制成10mol/L的盐酸溶液，备用。Take 41.4 ml of concentrated hydrochloric acid (Chinese medicine reagent, analytical grade) and use 8.5 ml of water to prepare a 10 mol/L hydrochloric acid solution for later use.
取对二甲氨基苯甲醛(国药试剂，分析纯)4g，先加入350ml冰醋酸，再加入50ml 10mol/L盐酸，配制成10mg/ml的对二甲氨基苯甲醛溶液，备用。Take 4g of p-dimethylaminobenzaldehyde (Chinese medicine reagent, analytical grade), first add 350ml of glacial acetic acid, and then add 50ml of 10mol/L hydrochloric acid to prepare a 10mg/ml p-dimethylaminobenzaldehyde solution for later use.
取制备好的实施例2-10提取物或溶液，以缓冲液各自稀释，按表1方法进行试验，于585nm处测吸光值，最终计算其IC50。Take the prepared extracts or solutions of Examples 2-10, dilute them with buffers, conduct the test according to the method in Table 1, measure the absorbance value at 585 nm, and finally calculate its IC 50 .
表1
Table 1
Table 1
实验结果：Experimental results:
根据以下公式计算透明质酸酶的抑制率：
Calculate the inhibition rate of hyaluronidase according to the following formula:
Calculate the inhibition rate of hyaluronidase according to the following formula:
其中T为样品，T0为样品对照，C为空白，C0为空白对照。Among them, T is the sample, T0 is the sample control, C is the blank, and C0 is the blank control.
根据皮肤外用剂场景下的实际应用，可以认为IC50＜10mg/ml属于优秀，IC50＜30mg/ml属于良好，IC50＜50mg/ml属于一般，IC50≥50mg/ml基本上没有应用价值。According to the actual application in the scenario of skin external use, it can be considered that IC50 <10 mg/ml is excellent, IC50 <30 mg/ml is good, IC50 <50 mg/ml is average, and IC50 ≥ 50 mg/ml has basically no application value.
表2
Table 2
Table 2
表3
table 3
table 3
表4
Table 4
Table 4
由透明质酸活性抑制实验结果可知，实施例2提取物作为单味药具有一定的抑制透明质酸酶能力，实施例3提取物无抑制透明质酸酶能力，实施例4提取物具有较弱地抑制透明质酸能力。然而，当青蒿提取物与荆芥防风油、牡丹籽油复配时，均在一定程度上改善抑制透明质酸酶活性的能
力。It can be seen from the results of the hyaluronic acid activity inhibition experiment that the extract of Example 2 has a certain ability to inhibit hyaluronidase as a single drug, the extract of Example 3 has no ability to inhibit hyaluronidase, and the extract of Example 4 has a weak ability to inhibit hyaluronidase. The ability to inhibit hyaluronic acid. However, when Artemisia annua extract is compounded with Schizonepeta parsnip oil and peony seed oil, the ability to inhibit hyaluronidase activity is improved to a certain extent. force.
同时，根据不同复方比例配比抑制透明质酸酶浓度结果可知，实施例5即青蒿提取物与荆芥防风油复配比例为1∶1，实施例7即青蒿提取物与荆芥防风油复配比例为7∶3，IC50浓度虽均大于阳性对照色甘酸钠IC50浓度，但仍均小于单味药，可优选实施例5，次选实施例7。At the same time, according to the results of inhibiting hyaluronidase concentration based on different compound ratios, it can be seen that the compound ratio of Artemisia annua extract and Schizonepeta parsnip oil in Example 5 is 1:1, and the compound ratio of Artemisia annua extract and Schizonepeta parsnip oil in Example 7 is 1:1. The oil compounding ratio is 7:3. Although the IC 50 concentrations are greater than the IC 50 concentrations of the positive control sodium cromoglycate, they are still less than the single drug. Example 5 is preferred, and Example 7 is second preferred.
进一步分析可知，由于实施例5～10中青蒿重量占比不同，换算后不同复方配比中实际青蒿IC50浓度如表3、表4所示，可以发现实施例5～7、10中实际青蒿IC50浓度均小于单独青蒿IC50浓度，从而在本质上降低了配方功效添加量，进而可以降低成本。Further analysis shows that due to the different weight proportions of Artemisia annua in Examples 5 to 10, the actual IC 50 concentrations of Artemisia annua in different compound ratios after conversion are shown in Table 3 and Table 4. It can be found that in Examples 5 to 7 and 10 The actual IC 50 concentration of Artemisia annua is less than the IC 50 concentration of Artemisia annua alone, which essentially reduces the amount of added efficacy in the formula, thereby reducing costs.
实施例5-10的制备物可用于皮肤外用剂的制备。所述皮肤外用剂优选为化妆品组合物，例如化妆水、精华液、乳霜等。所述制备物在皮肤外用剂中的重量百分比为0.08％-1％(w/w)。优选的重量百分比为0.12％-0.64％(w/w)。更优选的重量百分比为0.24％-0.5％(w/w)。最优选的重量百分比为0.32％-0.48％(w/w)。The preparations of Examples 5-10 can be used in the preparation of external preparations for skin. The skin external preparation is preferably a cosmetic composition, such as lotion, essence, cream, etc. The weight percentage of the preparation in the skin external preparation is 0.08%-1% (w/w). The preferred weight percentage is 0.12%-0.64% (w/w). A more preferred weight percentage is 0.24%-0.5% (w/w). The most preferred weight percentage is 0.32%-0.48% (w/w).
以下是实施例的制备物在皮肤外用剂中的具体应用例，以及这些剂型的配方和制备方法。以下各表中“-”表示无添加。The following are specific application examples of the preparations of the Examples in external skin preparations, as well as the formulations and preparation methods of these dosage forms. "-" in the following tables indicates no addition.
实施例12：面霜的制备
Example 12: Preparation of facial cream
Example 12: Preparation of facial cream
实施例13：乳液的制备
Example 13: Preparation of emulsion
Example 13: Preparation of emulsion
实施例14：啫喱的制备
Example 14: Preparation of gel
Example 14: Preparation of gel
实施例15：化妆水的制备
Example 15: Preparation of lotion
Example 15: Preparation of lotion
实施例16：精华液的制备
Example 16: Preparation of Essence
Example 16: Preparation of Essence
实施例17：面膜的制备
Example 17: Preparation of facial mask
Example 17: Preparation of facial mask
实施例18：眼霜的制备
Example 18: Preparation of eye cream
Example 18: Preparation of eye cream
实施例19：气雾(清洁泡)的制备
Example 19: Preparation of aerosol (cleaning bubble)
Example 19: Preparation of aerosol (cleaning bubble)
实施例20：喷雾的制备
Example 20: Preparation of spray
Example 20: Preparation of spray
实施例21：沐浴露的制备
Example 21: Preparation of shower gel
Example 21: Preparation of shower gel
实施例22：洗面奶的制备
Example 22: Preparation of facial cleanser
Example 22: Preparation of facial cleanser
Claims (10)
- 包含青蒿提取物和油溶性成分的组合物在皮肤抗敏、抗炎和/或抗刺激中的应用，其中，所述油溶性成分选自荆芥防风提取物和牡丹籽油。Application of a composition comprising artemisia annua extract and oil-soluble ingredients in skin anti-sensitivity, anti-inflammatory and/or anti-irritation, wherein the oil-soluble ingredients are selected from the group consisting of Schizonepeta parsnip extract and peony seed oil.
- 如权利要求1所述的应用，其中，所述青蒿提取物采用超声提取法制备。The application according to claim 1, wherein the Artemisia annua extract is prepared by ultrasonic extraction.
- 如权利要求1所述的应用，其中，所述青蒿提取物采用水作为溶剂提取。The application according to claim 1, wherein the Artemisia annua extract is extracted using water as a solvent.
- 如权利要求1所述的应用，其中，所述油溶性成分是荆芥防风提取物，青蒿提取物与荆芥防风提取物的重量比为4∶1至30∶1。The application according to claim 1, wherein the oil-soluble component is Schizonepeta parsnip extract, and the weight ratio of Artemisia annua extract to Schizonepeta sapiens extract is 4:1 to 30:1.
- 如权利要求1所述的应用，其中，所述油溶性成分是牡丹籽油，青蒿提取物与牡丹籽油的重量比为3∶1至33∶1。The application according to claim 1, wherein the oil-soluble component is peony seed oil, and the weight ratio of the artemisia annua extract to the peony seed oil is 3:1 to 33:1.
- 如权利要求1-5中任一项所述的应用，其中，所述抗炎、抗敏和/或抗刺激作用通过抑制透明质酸酶实现。The use according to any one of claims 1 to 5, wherein the anti-inflammatory, anti-allergic and/or anti-irritant effects are achieved by inhibiting hyaluronidase.
- 如权利要求1-5中任一项所述的应用，用于辅助止痒和/或湿疹问题。The application according to any one of claims 1 to 5, for assisting in relieving itching and/or eczema problems.
- 包含青蒿提取物和油溶性成分的组合物在制备具有皮肤抗敏、抗炎和/或抗刺激作用的皮肤外用剂中的应用，其中，所述油溶性成分选自荆芥防风提取物和牡丹籽油。Use of a composition comprising an Artemisia annua extract and an oil-soluble component in the preparation of a skin external preparation with skin anti-allergic, anti-inflammatory and/or anti-irritating effects, wherein the oil-soluble component is selected from the group consisting of Schizonepeta sapiens extract and Peony seed oil.
- 如权利要求8所述的应用，其中，所述皮肤外用剂选自：面霜、乳液、啫喱、化妆水、精华液、面膜、眼霜、气雾洁面泡、喷雾、沐浴露、洗面奶。The application according to claim 8, wherein the external agent for skin is selected from the group consisting of: facial cream, lotion, gel, lotion, essence, facial mask, eye cream, aerosol cleansing foam, spray, shower gel, and facial cleanser.
- 如权利要求8所述的应用，其中，所述皮肤外用剂包含0.08-1重量％的包含青蒿提取物和油溶性成分的组合物。 The application according to claim 8, wherein the external skin preparation contains 0.08-1% by weight of a composition containing Artemisia annua extract and oil-soluble ingredients.
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| 邓薇 等 (DENG, WEI ET AL.): "针对敏感性皮肤的中药应用概况 (Commonly used Traditional Chinese Medicine for Sensitive Skin)", 中国现代中药 (MODERN CHINESE MEDICINE), vol. 17, no. 1, 31 January 2015 (2015-01-31), XP055970980, DOI: 10.13313/j.issn.1673-4890.2015.1.022 * |
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