CN117426991A - Composition comprising sweet wormwood extract and efficacy active substance and application thereof - Google Patents

Composition comprising sweet wormwood extract and efficacy active substance and application thereof Download PDF

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Publication number
CN117426991A
CN117426991A CN202210836208.1A CN202210836208A CN117426991A CN 117426991 A CN117426991 A CN 117426991A CN 202210836208 A CN202210836208 A CN 202210836208A CN 117426991 A CN117426991 A CN 117426991A
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extract
sweet wormwood
skin
bisabolol
composition
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陈默
孙懿
赵亚
贾海东
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Shanghai Jahwa United Co Ltd
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Shanghai Jahwa United Co Ltd
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Priority to CN202210836208.1A priority Critical patent/CN117426991A/en
Priority to PCT/CN2023/106475 priority patent/WO2024012385A1/en
Publication of CN117426991A publication Critical patent/CN117426991A/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/7034Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/28Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
    • A61K36/282Artemisia, e.g. wormwood or sagebrush
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics 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
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/005Preparations for sensitive skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/10Washing or bathing preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/74Biological properties of particular ingredients
    • A61K2800/78Enzyme modulators, e.g. Enzyme agonists
    • A61K2800/782Enzyme inhibitors; Enzyme antagonists

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Abstract

The present invention provides the use of a composition comprising an extract of Artemisia annua and an efficacy active selected from dipotassium glycyrrhizinate and bisabolol for anti-sensitization, anti-inflammatory and/or anti-irritant skin. The invention also relates to the use of a composition comprising an extract of Artemisia annua and an active agent selected from dipotassium glycyrrhizinate and bisabolol for the preparation of a skin external preparation having anti-allergic, anti-inflammatory and/or anti-irritant effects on the skin.

Description

Composition comprising sweet wormwood extract and efficacy active substance and application thereof
Technical Field
The invention belongs to the field of phytochemistry, and in particular relates to a composition containing sweet wormwood extract and efficacy active substances and application thereof in external preparations or cosmetics for skin.
Background
Allergy is the condition that foreign substances enter the human body, and the immune system of the organism recognizes the foreign substances as foreign substances, so that the immune system is disturbed, and allergy, inflammation and the like are caused. Allergic reactions can be classified into types I, II, III and IV according to the mechanism, while hyaluronidase is a participant in type I allergic reactions and has strong correlation with inflammation and allergy.
Hyaluronidase is a specific lyase of hyaluronic acid, and hyaluronic acid shows physiological functions of various traditional Chinese medicines in the body, such as skin moistening, wound healing promotion, etc. According to research reports, some anti-allergic and anti-inflammatory drugs have strong inhibition of hyaluronidase activity, and therefore, inhibition of hyaluronidase activity is used as an index for researching anti-inflammatory effects.
Herba Artemisiae Annuae is whole herb of Artemisia annua L. Bitter and cold in property. It enters liver, gallbladder and kidney meridians. Has effects of clearing deficiency heat, relieving summer heat and preventing malaria. The sweet wormwood herb contains an antimalarial component artemisinin, can directly kill plasmodium, and modern researches show that the sweet wormwood herb extract has the functions of bacteriostasis, disinsection, antipyresis, anti-inflammatory and immunity regulation, and also has 5 flavonoid components with antioxidant activity, including quercetin and the like.
The water-soluble licorice is a white or quasi-white fine powder, has multiple effects of bacteriostasis, anti-inflammation, detoxification, anti-sensitization, deodorization and the like, and is widely applied to industries of medicines, daily chemicals, foods and the like. The production process of dipotassium glycyrrhizinate, which is commonly used at present, is to use licorice as a raw material extract, produce monoammonium glycyrrhizinate through ammonia, and produce dipotassium glycyrrhizinate through ion exchange, and in the cosmetic field, the dipotassium glycyrrhizinate can go deep into the skin and keep high activity, whiten and efficiently resist oxidation, effectively inhibit the activities of various enzymes in the melanin production process, particularly inhibit the activity of tyrosinase, and simultaneously have the effects of preventing rough skin, resisting inflammation and resisting bacteria.
Bisabolol is also an organic compound, is a nontoxic sesquiterpene alcohol existing in natural essential oil, and is mainly applied to skin protection and care cosmetics as an active ingredient to protect and care allergic skin, and research shows that bisabolol has anti-inflammatory effect and certain inhibition activity. Can effectively inhibit the production of peroxidase, and has good inhibition effect on acute inflammation or chronic inflammation bisabolol. Three-dimensional skin models prove that the bisabolol can inhibit the release of leukotrienes and interleukins caused by phorbol esters, thereby reducing the stimulation of external factors and ultraviolet rays to the skin of a human body and playing a role in preventing and inhibiting the occurrence and treatment of inflammation.
The invention surprisingly found that compounding the sweet wormwood extract with efficacy actives (e.g., dipotassium glycyrrhizinate, bisabolol) has excellent hyaluronidase inhibition effect. Therefore, the composition comprising the sweet wormwood herb extract and the efficacy active substance can be added into the external skin preparation as a compound efficacy additive to assist in relieving itching, eczema and the like.
Disclosure of Invention
In one aspect, there is provided the use of a composition comprising an extract of Artemisia annua and an efficacy active selected from dipotassium glycyrrhizinate and bisabolol for anti-sensitization, anti-inflammatory and/or anti-irritant skin.
In a preferred embodiment, the sweet wormwood extract is prepared by an ultrasonic extraction method. In a preferred embodiment, the sweet wormwood extract is extracted with water as solvent.
In a preferred embodiment, the efficacy active is dipotassium glycyrrhizinate, and the weight ratio of sweet wormwood extract to dipotassium glycyrrhizinate is 1:10 to 10:1.
In a preferred embodiment, the efficacy active is bisabolol, the weight ratio of sweet wormwood extract to bisabolol being from 2:1 to 55:1.
In a preferred embodiment, the anti-inflammatory, anti-allergic and/or anti-irritant effect is achieved by inhibition of hyaluronidase; or to aid in the relief of itching and/or eczema problems.
In another aspect, the present invention provides the use of a composition comprising an extract of Artemisia annua and an efficacy active selected from dipotassium glycyrrhizinate and bisabolol for the preparation of a skin external preparation having skin anti-sensitization, anti-inflammatory and/or anti-irritant effect.
In a preferred embodiment, the skin external agent is selected from the group consisting of: face cream, milky lotion, jelly, lotion, essence, pack, eye cream, aerosol cleansing foam, spray, body wash, and facial cleanser.
Brief description of the drawings
Fig. 1 shows the results of positive control hyaluronidase inhibition experiments.
FIG. 2 shows the results of the hyaluronidase inhibition experiment of example 2.
FIG. 3 shows the results of the hyaluronidase inhibition experiment of example 3.
FIG. 4 shows the results of the hyaluronidase inhibition experiment of example 4.
FIG. 5 shows the results of the hyaluronidase inhibition experiment of example 6.
FIG. 6 shows the results of the hyaluronidase inhibition experiment of example 7.
FIG. 7 shows the results of the hyaluronidase inhibition experiment of example 8.
FIG. 8 shows the results of the hyaluronidase inhibition experiment of example 9.
FIG. 9 shows the results of the hyaluronidase inhibition experiment of example 10.
FIG. 10 shows the results of the hyaluronidase inhibition experiment of example 11.
Detailed Description
The invention aims at providing a composition comprising an artemisia annua extract and an efficacy active. Specifically, the sweet wormwood extract and the efficacy active substance are combined, so that the sweet wormwood extract has better hyaluronidase inhibition effect. Therefore, the composition containing the sweet wormwood herb extract and the efficacy active substance can be used as a compound efficacy additive to be added into skin care products for assisting in relieving itching, eczema and the like.
In order to provide a more concise description, some quantitative representations presented herein are not modified by the term "about". It will be understood that each quantity given herein is intended to refer to an actual given value, whether or not the term "about" is explicitly used, and is also intended to refer to approximations of such given values, including approximations of such given values resulting from experimental and/or measurement conditions, as reasonably deduced by one of ordinary skill in the art.
To provide a more concise description, some quantitative expressions herein are recited as a range from about X to about Y. It should be understood that when a range is recited, the range is not limited to the recited upper and lower limits, but rather, includes the entire range of about X to about Y amounts or any amount therebetween.
Artemisia annua extract
Herba Artemisiae Annuae is whole herb of Artemisia annua L. Bitter and cold in property. It enters liver, gallbladder and kidney meridians. Has effects of clearing deficiency heat, relieving summer heat and preventing malaria. The sweet wormwood herb contains an antimalarial component artemisinin, can directly kill plasmodium, and modern researches show that the sweet wormwood herb extract has the functions of bacteriostasis, disinsection, antipyresis, anti-inflammation and immunity regulation, and also has 5 flavonoid components with antioxidant activity, including quercetin and the like.
In some embodiments, the sweet wormwood extract is extracted using an ultrasonic extraction method. The ultrasonic extraction characteristics include: 1. shortening extraction time, wherein each ultrasonic treatment only needs 20min-30min, and conventional extraction is basically carried out for 1h-1.5h;2. extracting at normal temperature without damaging thermosensitive components; 3. the cell wall is broken directly, and the extraction of the effective components is complete. In a preferred embodiment, the process parameters of the ultrasonic extraction are as follows: extracting for 2 times each for 20min, ultrasonic for 3s, and clearance for 3s.
In some embodiments, the extraction solvent is water (e.g., deionized water). In some embodiments, the extraction process includes an alcohol precipitation step. For example, ethanol precipitation is achieved with 95% ethanol. In some embodiments, the extraction process includes a filtration step. In some embodiments, the extraction process includes a centrifugation step. In some embodiments, the extraction process further comprises a concentration step. For example, to a solids content of 5 to 20% by weight. In a specific embodiment, the concentration is to a solids content of 10.94% by weight.
Efficacy actives
The invention surprisingly found that the combination of the sweet wormwood extract and the efficacy active substance (such as dipotassium glycyrrhizinate or bisabolol) has better synergistic effect in the aspects of skin anti-sensitization, anti-inflammation and/or anti-irritation. Thus, the sweet wormwood extract can be used in combination with the efficacy active to achieve anti-sensitization, anti-inflammatory and/or anti-irritant effects on the skin.
In some embodiments, the efficacy extract is dipotassium glycyrrhizinate. Dipotassium glycyrrhizinate is an organic compound, has multiple effects of bacteriostasis, anti-inflammation, detoxification, anti-allergy, deodorization and the like, and is widely applied to industries of medicines, daily chemicals, foods and the like. In the field of cosmetics, dipotassium glycyrrhizinate can penetrate into the skin and keep high activity, whiten and resist oxidation efficiently, effectively inhibit the activity of various enzymes in the melanin production process, particularly inhibit the activity of tyrosinase, and simultaneously have the effects of preventing skin roughness, resisting inflammation and resisting bacteria.
In some embodiments, the present invention provides a composition comprising sweet wormwood extract and dipotassium glycyrrhizinate, wherein the weight ratio of sweet wormwood extract to dipotassium glycyrrhizinate is 1:10 to 10:1. In a preferred embodiment, the weight ratio of sweet wormwood extract to dipotassium glycyrrhizinate is 2:5 to 5:2. In a preferred embodiment, the weight ratio of sweet wormwood extract to dipotassium glycyrrhizinate is from 8:5 to 10:1.
In some embodiments, the efficacy extract is bisabolol. Bisabolol is an organic compound capable of protecting and caring allergic skin. Research shows that the bisabolol has not only anti-inflammatory effect, but also certain inhibition activity. Can effectively inhibit the production of peroxidase, and has good inhibition effect on acute inflammation or chronic inflammation bisabolol. Three-dimensional skin models prove that the bisabolol can inhibit the release of leukotrienes and interleukins caused by phorbol esters, thereby reducing the stimulation of external factors and ultraviolet rays to the skin of a human body and playing a role in preventing and inhibiting the occurrence and treatment of inflammation. Bisabolol is an oil-soluble component which can be layered when meeting water, so suspending agents (such as tween) are often added to make the bisabolol become suspension when preparing, and the experiment can be ensured to be normally carried out. Typically, the amount of tween added is 10%.
In some embodiments, the present invention provides a composition comprising sweet wormwood extract and bisabolol, wherein the weight ratio of sweet wormwood extract to bisabolol is 1:10 to 10:1. In a preferred embodiment, the weight ratio of sweet wormwood extract to bisabolol is 1:5 to 5:1. In a preferred embodiment, the weight ratio of sweet wormwood extract to bisabolol is from 2:1 to 55:1. For example, the weight ratio of sweet wormwood extract to bisabolol may be 10.94:5, 10.94:1, or 54.7:1.
External preparation for skin
The composition containing the sweet wormwood herb extract and the efficacy active substance can be used as a composite efficacy additive to be applied to external skin preparations. In some embodiments, the skin external agent is selected from the group consisting of: facial cleanser, toning lotion, emulsion, cream, gel and facial mask. Different amounts are added according to the different types of formulations.
In another aspect, a skin external preparation is provided, comprising a composition of an extract of Artemisia annua and an active substance of efficacy and an excipient acceptable in the cosmetic field.
The external skin preparation is a general concept of all ingredients commonly used outside the skin, and may be, for example, a cosmetic composition or a pharmaceutical composition. The cosmetic composition may be basic cosmetic, facial makeup cosmetic, body cosmetic, hair care cosmetic, etc., and its dosage form is not particularly limited and may be reasonably selected according to different purposes. The cosmetic composition also contains various cosmetically acceptable medium or matrix excipients depending on dosage form and purpose.
The external preparation for skin contains a dermatologically acceptable carrier or vehicle (e.g., a lotion, a cream, an ointment, a cleanser, etc.). The person of ordinary skill in the art will be able to select a carrier that will dissolve or disperse these components at the concentrations described above, in accordance with common general knowledge in the art. When a carrier is used, the carrier should not cause inactivation of the sweet wormwood extract or the efficacy active, and should not cause any adverse effect on the skin when used.
The person of ordinary skill in the art will be able to select suitable carriers, including, for example, water, alcohols, oils, etc., based on common general knowledge and their ability to dissolve or disperse in the active ingredient at a concentration most suitable for treatment.
The skin external preparation of the present invention may be in the form of a topical application product which can be externally applied to the skin and can be prepared by those ordinary techniques well known in the art. The carrier may take a variety of practical forms, such as creams, dressings, gels, lotions, ointments or liquids, including compositions for application and cleansing, and incorporating them into a carrier material such as a dry or wet spread, hydrogel matrix, or adhesive (or non-adhesive) patch by methods well known in the art. Preferably, the carrier is a gel or a moisturizing lotion, or an application in dry or wet form.
Typical carriers include emulsions comprising water and/or an alcohol and an emollient, wherein the emollient is, for example, a hydrocarbon oil and wax, silicone oil, hyaluronic acid, a vegetable, animal or marine fat or oil, a glyceride derivative, a fatty acid, or fatty acid ester or alcohol ether, lanolin and its derivatives, a polyol or ester, a wax ester, a sterol, a phospholipid, and the like, and typically also an emulsifier (nonionic, cationic or anionic), although some emollients themselves have emulsifying properties. In addition, these same components may be formulated into creams, gels, or solid sticks using different proportions of their components and/or by incorporating thickeners such as gums or other forms of hydrocolloids.
The skin external agent of the present invention may contain additional components commonly found in skin care compositions, such as emollients, skin conditioning agents, emulsifiers, preservatives, antioxidants, fragrances, chelating agents, and the like, as long as they are physically and chemically compatible with the other components in the skin external agent.
In some embodiments of the skin external preparation of the present invention, one or more preservatives may be used. Suitable preservatives include p-hydroxyacetophenone, alkyl C1-C4 p-hydroxybenzoates and phenoxyethanol. The preservative is used in an amount of about 0.5 to about 2 wt%, preferably about 0.5 to 1 wt%, based on the total weight of the composition.
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 hydroxyanisole, phenyl-alpha-naphthylamine, hydroquinone, propyl gallate, nordihydroguaiaretic acid, vitamin E or derivatives of vitamin E, vitamin C and its derivatives, calcium pantothenate, green tea extracts and mixed polyphenols, and mixtures of the foregoing. The antioxidants are used in an amount ranging from about 0.02 to 0.5 weight percent, more preferably from about 0.002 to 0.1 weight percent, based on the total weight of the composition.
In some embodiments of the skin external preparations of the present invention, one or more emollients may be used that act as lubricants to reduce flaking and improve the appearance of the skin by their ability to remain on the skin surface or in the stratum corneum. Typical emollients include fatty esters, fatty alcohols, mineral oils, polyether siloxane copolymers, and the like. Examples of suitable emollients include, without limitation, polypropylene glycol ("PPG") -15 stearyl ether, PPG-10 cetyl ether, steareth-10, oleth-8, PPG-4 lauryl ether, vitamin E acetate, lanolin, cetyl alcohol, cetostearyl alcohol ethyl hexanoate, cetostearyl alcohol, glyceryl stearate, octyl hydroxystearate, dimethylpolysiloxane, and combinations thereof. Cetyl alcohol, cetostearyl alcohol ethyl hexanoate, cetostearyl alcohol, glycerol stearate, and combinations thereof are preferred. When used, the emollient is in an amount ranging from about 0.1 to about 30 weight percent, preferably from about 1 to about 30 weight percent, based on the total weight of the composition.
In some embodiments of the skin external preparation of the present invention, one or more moisturizers may be used. Humectants, also known as humectants, help to enhance the effectiveness of emollients, reduce flaking, stimulate removal of constituent scales and enhance skin feel. Polyols may be used as humectants including, but not limited to, glycerin, polyalkylene glycols, alkylene polyols and derivatives thereof, including butylene glycol, propylene glycol, dipropylene glycol, polyglycerol, polyethylene glycol and derivatives thereof, sorbitol, hydroxypropyl sorbitol, hexylene glycol, 1, 3-dibutylene glycol, 1,2, 6-hexanetriol, ethoxylated glycerin, propoxylated glycerin and combinations thereof. When used, the humectant is present in an amount of about 0.1 to about 20 weight percent, preferably about 1 to about 15 weight percent, based on the total weight of the composition.
In some embodiments of the skin external preparation of the present invention, one or more emulsifiers may be used. The emulsifier may be used in an effective stabilizing amount. Preferably, the emulsifier is used in an amount of about 1.0 to about 10.0 wt%, more preferably about 3.0 to about 6.0 wt%, based on the total weight of the composition. Any emulsifier that is 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-linked polymers, and combinations thereof.
In some embodiments of the skin external preparation of the present invention, one or more pH adjusting agents may be used. The pH adjuster useful in the skin external preparation of the present invention includes tromethamine. When used, the pH adjustor is used in an amount of about 0.1 to about 2 weight percent, preferably about 0.1 to about 1 weight percent, based on the total weight of the composition.
In some embodiments of the invention, the skin external preparation comprises acrylic/C10-30 alkanol acrylate cross-linked polymer, glycerol, p-hydroxyacetophenone, glycerol stearate and lecithin, cetyl/stearyl alcohol, cetostearyl alcohol ethyl hexanoate, tromethamine or combinations thereof.
In some embodiments of the invention, the composition of sweet wormwood extract and efficacy active in the skin external preparation is used in an amount of 0.001% -0.2% (w/w), preferably 0.007% -0.1% (w/w), more preferably 0.007% -0.08% (w/w), most preferably 0.007% -0.056% (w/w).
Examples
The invention will be further illustrated by the following examples. It is noted herein that the examples are given solely for the purpose of illustration and are not to be construed as limitations on the scope of the invention, since many insubstantial modifications and variations will become apparent to those skilled in the art in light of the above teachings. The test methods in the following examples, in which specific conditions are not specified, are generally conducted under conventional conditions or under conditions recommended by the manufacturer. All percentages and parts are by weight unless otherwise indicated.
The experimental materials used in the following examples are as follows:
name of the name Specification of specification Manufacturer' s
Herba Artemisiae Annuae Producing area Anhui Beijing and Anhui decoction piece factory
Deionized water Homemade
Ethanol 95%
Centrifugal machine DL-5M Lu Xiangyi
Dipotassium glycyrrhizinate Japanese pill
Bisabolol Merck KGaA
Tween 20 Shanghai Uama trade development Limited
Glacial acetic acid Analytical grade Chinese medicine reagent
Anhydrous sodium acetate Analytical grade Chinese medicine reagent
Example 1: preparation of sweet wormwood herb extract
Weighing 100g of sweet wormwood, ultrasonically extracting for 2 times by using 1-time deionized water, filtering, decocting and concentrating, adding a certain amount of 95% ethanol for alcohol precipitation (the final concentration is 70%), filtering by using filter paper (New star qualitative filter paper with the specification of 60 cm), concentrating the filtrate at 55 ℃, standing overnight at 4 ℃, taking out at 3 ℃ and centrifuging for 15min (Lu Xiangyi, DL-5M) at 3500rpm, filtering by using filter paper, and finally preparing into a solution with the solid content of 10.94% for later use.
Example 2: preparation of sweet wormwood herb extract
10.94g of the sweet wormwood herb extract sample with the solid content of 10.94% prepared in the example 1 is taken, and deionized water is added to prepare a solution with the solid content of 1% for later use.
Example 3: preparation of dipotassium glycyrrhizinate solution
10g of dipotassium glycyrrhizinate is taken, deionized water is added to prepare 1% dipotassium glycyrrhizinate solution for standby.
Example 4: preparation of bisabolol solution
Taking 59ml of glacial acetic acid, adding water to dilute to 1000ml, uniformly stirring by using a glass rod, and diluting by using 10 times of water to prepare 0.1mol/L solution A for later use. 8.203g of anhydrous sodium acetate is taken and dissolved in 1000ml of water, and is stirred uniformly by a glass rod, and then diluted by 10 times of water to prepare 0.1mol/L solution B for standby. According to solution A: the volume ratio of the solution B is 16:1, and finally the solution B is prepared into an acetic acid-sodium acetate Buffer solution (hereinafter referred to as Buffer solution) with the pH of 3.5 for standby.
Taking 10g of bisabolol, adding tween 20 (10%) and Buffer solution, and mixing well to prepare 1% bisabolol solution suspension for later use.
Example 5: preparation of sweet wormwood herb extract
Taking the sweet wormwood extract with the solid content of 10.94% prepared in the example 1, adding deionized water to prepare a solution with the solid content of 4% for later use.
Example 6: preparation of sweet wormwood herb extract
The extract of example 5: the solution of example 3 was mixed uniformly in a weight ratio of 1:1 for use.
Example 7: preparation of sweet wormwood herb extract
The extract of example 5: the solution of example 3 was mixed well in a weight ratio of 2:5 for use.
Example 8: preparation of sweet wormwood herb extract
The extract of example 5: the solution of example 3 was mixed well in a weight ratio of 5:2 for use.
Example 9: preparation of sweet wormwood herb extract
The extract of example 1: the solution of example 4 was mixed well in a weight ratio of 1:1 for use.
Example 10: preparation of sweet wormwood herb extract
The extract of example 1: the solution of example 4 was mixed well in a weight ratio of 1:5 for use.
Example 11: preparation of sweet wormwood herb extract
The extract of example 1: the solution of example 4 was mixed well in a weight ratio of 5:1 for use.
Example 12: evaluation of hyaluronidase Activity inhibition
Taking 59ml of glacial acetic acid (national medicine reagent, analytical grade), adding water to dilute to 1000ml, stirring uniformly by using a glass rod, and diluting by using 10 times of water to prepare 0.1mol/L solution A for later use. 8.203g anhydrous sodium acetate (national medicine reagent, analytical grade) is taken and dissolved in 1000ml water, and is stirred uniformly by a glass rod, and then diluted by 10 times of water to prepare 0.1mol/L solution B for standby. According to solution A: the volume ratio of the solution B is 16:1, and finally the solution B is prepared into an acetic acid-sodium acetate Buffer solution (hereinafter referred to as Buffer solution) with the pH of 3.5 for standby.
0.1411g of hyaluronidase (activity is greater than or equal to 560units/mg, sigma) is prepared into a hyaluronidase solution with the enzyme activity being greater than or equal to 7900units/ml by using 10ml Buffer solution for clinical preparation.
0.1387g of anhydrous calcium chloride (national drug reagent, analytical grade) was prepared into a calcium chloride solution of 12.5mmol/L with 100ml of water for use.
0.12g of sodium hyaluronate (Dongchen group) is prepared into 1.2mg/ml sodium hyaluronate solution by using 100ml Buffer solution for standby.
0.4g of sodium hydroxide (national medicine reagent, analytical grade) is taken and prepared into 0.4mol/L sodium hydroxide solution by 25ml of water for later use.
30.55g of potassium tetraborate (national medicine reagent, analytical grade) is taken and prepared into 0.4mol/L potassium borate solution by 250ml of water for later use.
41.4ml of concentrated hydrochloric acid (national medicine reagent, analytical grade) is taken and 8.5ml of water is used for preparing 10mol/L hydrochloric acid solution for standby.
4g of p-dimethylaminobenzaldehyde (national reagent, analytical grade) is taken, 350ml of glacial acetic acid is added, and 50ml of 10mol/L hydrochloric acid is added to prepare 10mg/ml of p-dimethylaminobenzaldehyde solution for later use.
The prepared extracts or solutions of examples 2-11 were diluted with buffer, tested according to the method of Table 1, absorbance was measured at 585nm, and IC was calculated 50
TABLE 1
Experimental results:
the inhibition rate of hyaluronidase was calculated according to the following formula:
where T is the sample, T0 is the sample control, C is the blank, and C0 is the blank control.
TABLE 2
TABLE 3 Table 3
TABLE 4 Table 4
From the results of the hyaluronic acid activity inhibition experiments, the extracts of example 2 and example 3 have a certain hyaluronidase inhibition ability as a single drug, and the extract of example 4 has no hyaluronidase inhibition ability. However, when the sweet wormwood extract is compounded with dipotassium glycyrrhizinate and bisabolol, the capacity of inhibiting the activity of hyaluronidase is improved to a certain extent.
Meanwhile, according to the results of inhibiting the concentration of the hyaluronidase according to the mixture ratio of different compound ratios, the mixture ratio of the sweet wormwood extract and the dipotassium glycyrrhizinate in the embodiment 8 is 5:2, the mixture ratio of the sweet wormwood extract and the dipotassium glycyrrhizinate in the embodiment 7 is 2:5, and the IC is shown as follows 50 Concentration is smaller than positive control cromolyn sodium IC 50 Concentration, preferred example 8, sub-selected example 7.
In addition, the compounding ratio of the sweet wormwood extract and the bisabolol in the embodiment 11 is 5:1, the compounding ratio of the sweet wormwood extract and the bisabolol in the embodiment 9 is 1:1, and the IC is the same as that of the embodiment 50 The concentrations are larger than the positive control sodium cromoglycate IC 50 The concentrations are still smaller than the single drug, and example 11, and example 9 can be preferred.
Further analysis shows that the actual sweet wormwood IC in different compound ratios after conversion is obtained due to different weight ratios of sweet wormwood in examples 6-11 50 The concentrations are shown in tables 3 and 4, and it can be found that the actual Artemisia annua IC in examples 6, 8 to 11 50 The concentration is smaller than that of the sweet wormwood IC alone 50 The concentration is reduced, so that the efficacy addition amount of the formula is reduced, and the cost is reduced.
The preparations of examples 6 to 11 were used for the preparation of external preparations for skin. The external preparation for skin is preferably a cosmetic composition such as a lotion, essence, cream, etc. The weight percentage of the preparation in the external skin preparation is 0.001% -0.2% (w/w). Preferably 0.007% to 0.1% (w/w). More preferably, the weight percentage is 0.007% -0.08% (w/w). Most preferably 0.007% to 0.056% (w/w) by weight.
The following are specific examples of applications of the preparations of examples in skin external preparations, and formulations and preparation methods of these dosage forms. Specific applications are as follows:
example 13: preparation of face cream
Example 14: preparation of the emulsion
Example 15: preparation of jelly
Example 16: preparation of toning lotion
Example 17: preparation of essence
Example 18: preparation of facial mask
Example 19: preparation of eye cream
Example 20: preparation of aerosol (cleaning foam)
Example 21: preparation of the spray
Example 22: preparation of bath lotion
Example 23: preparation of facial cleanser

Claims (10)

1. Use of a composition comprising an extract of sweet wormwood and an efficacy active selected from dipotassium glycyrrhizinate and bisabolol for anti-sensitization, anti-inflammatory and/or anti-irritant skin.
2. The use according to claim 1, wherein the sweet wormwood extract is prepared by ultrasonic extraction.
3. The use according to claim 1, wherein the sweet wormwood extract is extracted with water as solvent.
4. The use according to claim 1, wherein the efficacy active is dipotassium glycyrrhizinate and the weight ratio of sweet wormwood extract to dipotassium glycyrrhizinate is 1:10 to 10:1.
5. The use according to claim 1, wherein the efficacy active is bisabolol, the weight ratio of artemisia annua extract to bisabolol is from 2:1 to 55:1.
6. The use according to any one of claims 1 to 5, wherein the anti-inflammatory, anti-allergic and/or anti-irritant effect is achieved by inhibition of hyaluronidase.
7. Use according to any one of claims 1-5 for aiding in the relief of itching and/or eczema problems.
8. Use of a composition comprising an extract of sweet wormwood herb and an efficacy active selected from dipotassium glycyrrhizinate and bisabolol for the preparation of a skin external preparation having anti-allergic, anti-inflammatory and/or anti-irritant effects on the skin.
9. The use according to claim 8, wherein the external skin preparation is selected from the group consisting of: face cream, milky lotion, jelly, lotion, essence, pack, eye cream, aerosol cleansing foam, spray, body wash, and facial cleanser.
10. The use according to claim 8, wherein the skin external preparation comprises 0.001-0.2% by weight of a composition comprising sweet wormwood extract and an efficacy active.
CN202210836208.1A 2022-07-15 2022-07-15 Composition comprising sweet wormwood extract and efficacy active substance and application thereof Pending CN117426991A (en)

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Family Cites Families (8)

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CN105496904A (en) * 2016-01-25 2016-04-20 王晶怡 Toning lotion for hypersensitive skin
US20180177706A1 (en) * 2016-12-23 2018-06-28 L'oreal Compositions containing hyaluronic acid and synergistic anti-hyaluronidase actives
CN106726789A (en) * 2017-03-14 2017-05-31 四川蓝伯特生物科技股份有限公司 A kind of sweet wormwood bacterium-suppressing shower lotion and preparation method thereof
CN107440974A (en) * 2017-09-21 2017-12-08 广州添意时企业管理有限公司 A kind of oil-controlling facial mask liquid and preparation method thereof
CN107753666A (en) * 2017-11-10 2018-03-06 无比滴(广东)药业有限公司 A kind of easypro shield liquid for preventing and treating infant eczema
CN109276497A (en) * 2018-11-12 2019-01-29 重庆菩璞生物科技有限公司 A kind of application of the composition comprising Artemisinin in skin care item
CN113855718A (en) * 2021-09-30 2021-12-31 上海家化联合股份有限公司 Artemisia apiacea extract and application thereof
CN116035986A (en) * 2022-06-29 2023-05-02 广州凡岛网络科技有限公司 Scalp repair composition applied to cosmetic formula

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