CN116407460A - Skin external composition and application of sialic acid in preparation of antiallergic preparation - Google Patents

Skin external composition and application of sialic acid in preparation of antiallergic preparation Download PDF

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CN116407460A
CN116407460A CN202111644960.8A CN202111644960A CN116407460A CN 116407460 A CN116407460 A CN 116407460A CN 202111644960 A CN202111644960 A CN 202111644960A CN 116407460 A CN116407460 A CN 116407460A
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essential oil
sialic acid
composition
skin
preparation
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李翔宇
项威
李慕梓
王纪
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Cabio Biotech Wuhan Co Ltd
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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
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60Sugars; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7012Compounds having a free or esterified carboxyl group attached, directly or through a carbon chain, to a carbon atom of the saccharide radical, e.g. glucuronic acid, neuraminic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • 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
    • A61K8/92Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A61K8/922Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
    • 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
    • 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
    • A61Q19/005Preparations for sensitive skin
    • 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
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/59Mixtures
    • A61K2800/592Mixtures of compounds complementing their respective functions
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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Abstract

The application provides a skin external composition and application of sialic acid in preparing an antiallergic agent, and the composition can relieve, treat and improve anaphylactic reaction caused by plant essential oil by compounding the sialic acid and the plant essential oil; the application can inhibit the action of sensitization components in the skin external preparation by adding sialic acid into the anti-sensitization preparation, thereby inhibiting skin irritation reaction and improving skin anaphylaxis to realize the anti-allergy effect. In addition, sialic acid has small irritation in a certain dosage range and has good application prospect.

Description

Skin external composition and application of sialic acid in preparation of antiallergic preparation
Technical Field
The application relates to the technical field of preparations, in particular to a skin external composition and application of sialic acid in preparation of an antiallergic preparation.
Background
The skin is the tissue covered outside the muscle on the surface of the body, is the largest organ of the human body, and mainly plays the roles of protecting the body, perspiration, feeling cold and hot, pressure and the like. The skin covers the whole body, protects all tissues and organs in the human body from being affected by external substances such as pathogenic microorganisms and mechanical injuries such as physics and the like, and effectively resists external stimulus; the skin also keeps the loss of water, electrolyte, nutrient substances and the like of the human body, effectively maintains the stability of the internal environment of the human body, and is a natural barrier for protecting the human body.
With the enhancement of living standard and self-maintenance consciousness of people, various skin problems brought by sensitive skin are also attracting attention in addition to basic care effects on skin such as whitening, moisturizing and the like. The cosmetics on the market are various, but the quality is uneven, and due to the addition of chemical components and heavy metals, the skin allergy appearance and the possibility of receiving external stimulus are improved, and the consciousness of skin health and the antiallergic cognition of people are gradually improved.
The skin allergy is usually itching, and may be accompanied by red swelling, dry scraps, blisters, scab and exudation, etc., and the shape and size of the lesions are different. Occasionally, symptoms such as skin tightness, numbness, swelling, etc. may occur. Aiming at the problems, a large number of preparations are developed at home and abroad, however, the efficacy is not ideal, hormone products are used in many cases, and the defects of strong dependence and great side effect exist.
Disclosure of Invention
In view of this, the present application provides a composition for external use on skin and the use of sialic acid in the preparation of antiallergic agents.
In a first aspect, the present application provides a skin external composition comprising sialic acid and a plant essential oil.
Optionally, in the composition, the mass ratio of the sialic acid to the plant essential oil is greater than or equal to 1:20.
Optionally, in the composition, the mass percentage of sialic acid is 0.05% -2%; and/or the mass percentage of the plant essential oil is 0.1-20%.
Optionally, the sialic acid is selected from: at least one of sialic acid monomer, polysialic acid, sialic acid metal salt or sialic acid derivative.
Optionally, the plant essential oil comprises at least one of floral essential oil, citrus essential oil, vanilla essential oil, woody essential oil, spicy essential oil or resin essential oil.
Optionally, the plant essential oil comprises spicy essential oil and/or vanilla essential oil, and the mass percentage of the spicy essential oil and/or vanilla essential oil is 0.1% -15% based on the total mass of the composition.
Optionally, the plant essential oil comprises, in parts by weight:
0.1 to 1 part of cinnamon essential oil;
0.1 to 1 part of butyl essential oil;
0.2 to 2 parts of neroli essential oil; and/or
0.1 to 2 portions of rose essential oil.
Optionally, the composition comprises 0 to 6 parts of surfactant and 40 to 60 parts of base oil; and/or, 30-50 parts of moisturizing emollient.
Optionally, the skin external composition is any one of a toning lotion, an essence, an emulsion, a face cream, an eye cream, a facial mask, a sun cream, a bath lotion, a facial cleanser, a foundation or a BB cream.
In a second aspect, the present application also provides the use of sialic acid in the manufacture of a formulation for preventing allergic reactions in skin.
Optionally, the ingredients that cause the skin to develop an allergic reaction include: at least one of essence, preservative, heavy metal, coloring agent, plant essential oil or surfactant.
The beneficial effects are that:
the application provides a skin external composition which can relieve, treat and improve anaphylactic reaction caused by plant essential oil by compounding sialic acid and the plant essential oil. The application also provides an application of sialic acid in preparing an antiallergic preparation, and the application can inhibit the action of the sensitization components in the external skin preparation by adding sialic acid into the antiallergic preparation, so that the skin irritation reaction is inhibited, the skin allergy reaction is improved, and the antiallergic effect is realized. In addition, sialic acid has small irritation in a certain dosage range and has good application prospect.
Drawings
In order to more clearly illustrate the technical solutions in the embodiments of the present application, the drawings that are required to be used in the description of the embodiments will be briefly described below.
FIG. 1 is a picture of the skin condition of each group 6 hours after removal of the test object in the skin external composition allergy test in the example of the present application.
Detailed Description
In order to make the technical problems, technical solutions and technical effects to be solved by the present application more apparent, the present application will be described in further detail below in conjunction with specific embodiments, and it is apparent that the described embodiments are only some embodiments of the present application, but not all embodiments. All other embodiments, which can be made by those skilled in the art based on the embodiments herein without making any inventive effort, are intended to be within the scope of the present application.
Some terms and expressions used in the context of the present application are incorporated in order to facilitate understanding of the present application.
The term "sialic acid" is known as "N-acetylneuraminic acid (N-Acetylneuraminic acid)", and is a naturally occurring carbohydrate with a CAS number of 131-48-6. The chemical formula is C 11 H 19 NO 9 . It was originally isolated from submaxillary gland mucins and is therefore named. The sialic acid can be produced by synthesis (e.g. chemical synthesis, enzymatic synthesis), natural extraction (e.g. from egg white, submaxin or placenta), and fermentation, wherein the fermentation can produce sialic acid monomers or polysialic acid, as desiredIt is clear that the origin of sialic acid does not affect the implementation of the examples of the present application.
The term "skin" is understood to mean the layers that comprise it from the uppermost layer or stratum corneum to the lowermost layer or dermis (both included). These layers contain different types of cells, such as, inter alia, keratinocytes, fibroblasts, melanocytes and adipocytes. In the examples of the present application, the term "skin" refers mainly to mammalian skin, in particular to human skin, including scalp.
The term "allergic reaction" refers to a hypersensitive reaction induced by an immune mechanism. Allergy can be humoral (antibodies) or mediated by cellular immune mechanisms. Allergy is an allergy of an organism, which is an abnormal reaction of a person to normal substances (allergens) and occurs only when the allergens come into contact with people with allergic constitution, and for the embodiment of the application, allergy mainly refers to skin allergy, and the allergens mainly are chemical substances, for example, sensitization components in skin external preparations, such as: essence, preservative, heavy metal, plant essential oil, pigment or surfactant. The sensitization components mainly have the functions of correcting taste, preserving, beautifying and needing stability of the preparation, the sensitization sources of different people are different, the skin barrier is damaged after long-term use or contact with the corresponding sensitization components, the skin is allergic or allergic skin diseases are caused, and the function of inhibiting the sensitization components is particularly important.
The plant essential oil has the effects of health care and taste correction, is a component commonly used in skin external preparations, but because of the complexity of the component, the risk of allergy is caused, and most essential oils are subjected to strict proportion and higher dilution ratio in the use process to reduce the risk of allergy, but the problem of skin allergy still cannot be avoided due to individual difference, and especially the frequency of allergy caused by spicy and vanilla essential oils such as cinnamon, bay, rosemary and the like is higher.
In view of this, the inventors have unexpectedly found that sialic acid can be used in a composition to prevent and alleviate potential allergic reactions caused by other ingredients, and thus the present application provides a composition for external use on skin, comprising sialic acid and a plant essential oil.
In some embodiments, the composition comprises 0.05 to 2 parts sialic acid by weight and the plant essential oil is 0.1 to 6 parts. In this ratio range, sialic acid has a good antiallergic effect after both are compounded.
In some embodiments, the mass ratio of the sialic acid to the plant essential oil in the composition is greater than or equal to 1:20, e.g., 1:2-20. If the sialic acid ratio is too small, it is difficult to suppress allergic symptoms caused by the essential oil. It is understood that the mass ratio of the sialic acid to the plant essential oil can be any number greater than or equal to 1:20, for example: 1:0.5, 1: 1. 1: 2. 1: 3. 1: 4. 1: 5. 1: 6. 1: 7. 1: 8. 1: 9. 1: 10. 1: 11. 1: 12. 1: 13. 1: 14. 1: 15. 1: 16. 1: 17. 1: 18. 1: 19. 1:20, etc., or greater than or equal to 1:20, other unlisted values. However, if the pursuing ratio is too large, the content of the plant essential oil is limited due to the influence of the upper limit of the sialic acid addition amount, and the application value of the essential oil is reduced.
In addition, reference is made to the method described in CN112535292a for the method of adding sialic acid to essential oils.
In some embodiments, the composition comprises 0.05% to 2% sialic acid by mass. If the mass percentage of the sialic acid is too large, the preparation difficulty is increased, and if the mass percentage of the sialic acid is too small, the content of the added plant essential oil is smaller, so that the application value of the composition is reduced. It is understood that the mass percentage of sialic acid may be specifically: 0.05%, 0.1%, 0.5%, 1%, 1.5%, 2%, etc., or other values not listed therebetween. Wherein the upper limit of the mass of sialic acid is set based on current regulations for sialic acid in cosmetic applications.
In some embodiments, in the composition, the mass percentage of the plant essential oil is 0.1% -20%, and if the content of the plant essential oil is too small, the application value of the essential oil is reduced; if the content of the plant essential oil is too large, sialic acid is difficult to suppress allergic symptoms caused by the essential oil. It can be understood that the mass percentage of the plant essential oil is arbitrarily taken in the range of 0.1% -20%, for example: 0.1%, 0.5%, 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, 11%, 12%, 13%, 14%, 15%, 16%, 17%, 18%, 19%, 20%, etc., or other unlisted values in the range of 0.1% to 20%. The upper limit of 20% in the plant essential oil is mainly based on practical application effect and commercial value.
In some embodiments, the composition further comprises a base oil and a moisturizing emollient, wherein the mass percent of sialic acid in the composition is 0.05% -2%, the plant essential oil is 0.1% -20%, the surfactant is 0% -6% and the base oil is 40% -60%; and/or, 30% -50% of the moisturizing emollient.
In some embodiments, the sialic acid is selected from: at least one of sialic acid monomer, polysialic acid, sialic acid metal salt or sialic acid derivative. The Sialic acid (Sialic acid) is an acidic amino sugar containing 9 carbon atoms and having a pyranose structure, and is also called N-acetylneuraminic acid, nidus Collocaliae acid and nidus Collocaliae essence.
In some embodiments, the plant essential oil comprises at least one of an floral essential oil, a citrus essential oil, a vanilla essential oil, a woody essential oil, a spicy essential oil, or a resinous essential oil. In some embodiments, the floral essential oil comprises at least one of a rose essential oil, a jasmine essential oil, a geranium essential oil, a chamomile essential oil, or an orange flower essential oil; the citrus essential oil comprises at least one of bergamot essential oil, grapefruit essential oil, lemon essential oil or orange essential oil; the vanilla essential oil comprises at least one of herba Ocimi essential oil, herba Salvia officinalis essential oil, herba Euphorbiae Humifusae essential oil, herba Melissae axillaris essential oil, herba Rosmarini officinalis essential oil or herba Thymi essential oil; the wood essential oil comprises at least one of cedar essential oil, cypress essential oil, juniper berry essential oil, myrtle essential oil, sandalwood essential oil or pine essential oil; the spicy essential oil comprises: at least one of cinnamon essential oil, bay essential oil, black pepper essential oil, clove essential oil, sweet-flour essential oil or nutmeg essential oil; the resin essential oil comprises: at least one of an essential oil of milk, an essential oil of myrrh or an essential oil of benzoin.
The plant essential oils in the external preparation are often formulated with various essential oils based on efficacy considerations, for example, in some embodiments, the plant essential oils include spicy and/or vanilla essential oils, and in some embodiments, the spicy and/or vanilla essential oils are present in an amount of 0.1-15% by mass based on the total mass of the composition. The application aims at solving the risk of allergy caused by Gao Zhimin essential oil containing, for example, spicy essential oil and vanilla essential oil. Therefore, for the external preparation containing the essential oil with high sensitization, the sialic acid and the sialic acid are compounded to have obvious antiallergic effect.
In some embodiments, the plant essential oil comprises, in parts by weight:
0.1 to 1 part of cinnamon essential oil;
0.1 to 1 part of butyl essential oil;
0.2 to 2 parts of neroli essential oil; and/or
0.1 to 2 portions of rose essential oil.
In some embodiments, the composition further comprises 0 to 6 parts of a surfactant, 40 to 60 parts of a base oil; and/or, 30-50 parts of moisturizing emollient. The base oil is also called a base oil, and can lubricate the skin. Unlike plant essential oils, the base oils are mainly non-volatile oils extracted from seeds, flowers, rhizomes or fruits of plants, commonly known as jojoba oil, sweet almond oil, grape seed oil, rose hip oil, olive oil, etc. In addition, some of the mineral oils can be used as base oils, and the mineral oils are mixtures of refined liquid hydrocarbons obtained from petroleum, which are obtained by normal pressure and reduced pressure fractionation, solvent extraction and dewaxing, and hydrofinishing, and are also commonly known as white oils. Specifically, the base oil is jojoba oil and white oil, the surfactant is polyoxyethylene lauryl alcohol ether, and the moisturizing emollient is vitamin E, isooctyl palmitate, squalene and/or squalane.
In some embodiments, the skin external composition is any one of a lotion, a serum, a lotion, a cream, an eye cream, a mask, a sunscreen, a body wash, a facial cleanser, a foundation, or a BB cream.
Correspondingly, the embodiment of the application also provides application of sialic acid in preparing a preparation for preventing skin from anaphylactic reaction, wherein the preparation mainly refers to a skin external preparation.
Sialic acid can prevent skin from allergic reaction by inhibiting sensitization components in the skin external preparation and/or other sensitization components contacted with the skin from acting on the skin, so that the purpose of preventing allergy is achieved, and therefore, the application provided by the application can inhibit allergic reaction from the source and prevent adverse effects on the skin caused by methods such as hormone treatment and the like; on the other hand, the inventor experiments prove that sialic acid has no irritation to skin in a certain dosage range, so the sialic acid can be used as a mild additive in a preparation. It should be noted that there is no additional limitation in the sensitization component in the present application, and the sensitization component may be a sensitization component having a stimulatory effect in a skin external preparation known to those skilled in the art, or other sensitization components with which skin contacts, for example, in some specific embodiments, the sensitization component includes: at least one of essence, preservative, heavy metal, coloring agent, plant essential oil or surfactant, or other chemical raw materials, such as 2, 4 dinitrochlorobenzene, and is not limited in particular.
As an example, the fragrances are mainly industrial fragrances that are irritating to the skin, and among fragrances for cosmetics or skin care products, the fragrances are classified mainly into floral fragrances, fruity fragrances, and also other fragrant fragrances, including but not limited to: flos Jasmini sambac essence, flos Rosae Rugosae essence, herba Violae essence, flos Osmanthi Fragrantis essence, flos Linderae essence or flos Baihua essence, etc., and the fruit flavor essence includes but is not limited to: orange flavored essence, lemon flavored essence, including but not limited to: ginseng-flavored essence, grass-flavored essence, sandalwood-flavored essence, and the like.
As examples, the preservative mainly includes alcohols, acids, parabens, formaldehyde-releasing substances, methyl chloroisothiazolinone and mixture of methyl isothiazolinone (CMIT/MIT), iodopropynyl butyl carbamate (IPBC). Wherein the alcohols include, but are not limited to, at least one of phenoxyethanol or benzyl alcohol; the acids include, but are not limited to: at least one of benzoic acid, salicylic acid, boric acid and sorbic acid. The parabens include, but are not limited to, at least one of methyl paraben, ethyl paraben, propyl paraben, butyl paraben, jin Yibing paraben, and isobutyl paraben; the formaldehyde releasing species include, but are not limited to, at least one of 1, 3-dimethylol-5, 5 dimethylhydantoin (DMDMH), imidazolidinyl urea, diazoimidazolidinyl urea, quaternary ammonium salt-15 (DOW ici ltm 200), and sodium hydroxymethylglycinate.
As an example, the plant essential oil mainly includes: floral, citrus, vanilla, woody, spicy, or resinous, the floral essential oil comprising at least one of a rose essential oil, a jasmine essential oil, a geranium essential oil, a chamomile essential oil, or a neroli essential oil; the citrus essential oil comprises at least one of bergamot essential oil, grapefruit essential oil, lemon essential oil or orange essential oil; the vanilla essential oil comprises at least one of herba Ocimi essential oil, herba Salvia officinalis essential oil, herba Euphorbiae Humifusae essential oil, herba Melissae axillaris essential oil, herba Rosmarini officinalis essential oil or herba Thymi essential oil; the wood essential oil comprises at least one of cedar essential oil, cypress essential oil, juniper berry essential oil, myrtle essential oil, sandalwood essential oil or pine essential oil; the spicy essential oil comprises: at least one of cinnamon essential oil, black pepper essential oil, clove essential oil, sweet flour essential oil or nutmeg essential oil; the resin essential oil comprises: at least one of an essential oil of milk, an essential oil of myrrh or an essential oil of benzoin.
As examples, the surfactants include, but are not limited to: anionic surfactants, cationic surfactants, amphoteric surfactants, or nonionic surfactants. Wherein the anionic surfactant comprises: at least one of fatty acid soap, sodium dodecyl sulfate, sodium laureth sulfate, sodium cetyl polyoxyethylene ether phosphate and soybean lecithin (lecithin); cationic surfactants include primary, secondary, tertiary and quaternary ammonium salts of higher alkyl groups, such as at least one of octadecyl trimethyl ammonium chloride, C12-14 alkyl dimethyl benzyl ammonium chloride, dioctadecyl dimethyl sodium chloride. The amphoteric surfactant includes: at least one of cocoamidopropyl betaine and imidazoline. The nonionic surfactant includes: at least one of sorbitan monolaurate, ethylene oxide adduct, laureth, cocodiethanolamide, oleic acid monoglyceride, polyoxyethylene castor oil, and polyoxyethylene lanolin.
As an example, the heavy metal includes at least one of lead, mercury, or arsenic.
By way of example, the colorant includes p-phenylenediamine.
In some embodiments, sialic acid may be applied to at least the skin to achieve the following effects:
(1) Inhibit skin irritation. Specifically, inhibiting skin irritation includes alleviating side effects such as tightening, numbness, swelling, pain, burning or itching of the skin due to the sensitization component, and preventing the generation of sensitive skin.
(2) Improving skin allergic reactions; by "ameliorating" in embodiments of the present application is meant any action, such as symptoms, that at least reduces the severity of a parameter associated with the disorder being treated. Since sialic acid is antiallergic, it can improve symptoms such as erythema, pimple, eczema, acne or urticaria due to skin allergy.
As an application for suppressing allergic reaction, the sialic acid can be used for preparing skin external preparations including, but not limited to, skin care products such as toner, lotion, essence, face cream, eye cream, body cream, sun-screening agent, hand cream, lip balm; can also be used for preparing cosmetics such as foundation, barrier cream, lipstick, etc.; also useful in medicine, including: any one of ointment, lotion, dressing, cream and emulsion. In these skin care products, cosmetics or medicines, sialic acid may be present together with other active ingredients for repairing skin barrier and suppressing skin irritation and allergy caused by sensitization ingredients.
In embodiments of the present application, sialic acid may be derived from synthetic free sialic acid or natural material extracts. The natural material extract may be nidus Collocaliae extract. In this application, free sialic acid, which is prepared and isolated purified by biosynthetic or chemical synthetic methods known in the art, may be selected. In some embodiments, synthetic sialic acid is desirable for this application, for sialic acid purity and sialic acid component safety, stability considerations.
In some embodiments, the sialic acid is selected from: at least one of sialic acid monomer, polysialic acid, sialic acid metal salt and sialic acid derivative. For example, in some specific embodiments, the metal sialic acid salt can be sodium or zinc sialic acid salt; in other embodiments, the sialic acid can also be attached to the ends of glycoproteins, glycolipids, and oligosaccharides in the form of an α -glycosidic linkage.
The present application also provides a method for preventing allergy, which is mainly by adding sialic acid to an external preparation containing an sensitizing ingredient, and applying an effective dose of the external preparation to the skin and/or mucous membrane.
The external skin preparation described in the present application is a generic term for all ingredients commonly used outside the skin, and may be, for example, cosmetics or medicines. The cosmetic can be basic cosmetic, facial make-up cosmetic, body cosmetic, head care product, etc., and the dosage form is not particularly limited, and can be reasonably selected according to different purposes. The skin external preparation described herein may further comprise other active ingredients, which are preferably one or more of a moisturizing active ingredient, an antioxidant active ingredient, an oil control active ingredient, a whitening active ingredient, and an anti-aging active ingredient. The other active ingredient is present in amounts conventional in the art.
In the present invention, the form of the external skin preparation may be any suitable product form including, but not limited to, one or more of essential oils, aerosol sprays, creams, emulsions, solids, liquids, dispersions, foams, gels, lotions, mousses, ointments, powders, patches, pomades, hand pump sprays, sticks, masks and wet tissues. The skin external preparation of the present invention may be a cosmetic, dermatological or pharmaceutical topical application product, and the preparation method thereof may be a conventional preparation method in the art, as is well known.
In some embodiments, the skin and/or mucosa is selected from at least one of the following: neck, chest, shoulder, abdomen, arms, thighs, crotch, buttocks, waist and/or face.
The following is a detailed description of the technical aspects of the present application using examples.
Examples: sialic acid containing compositions
The compositions were formulated in the proportions shown in table 1 below, wherein the white oils used in examples 1 to 4 and comparative example 1 were used as base oils, and sialic acid was uniformly dispersed in the oils by a method of homogenization after sonication to prepare oiling agents; example 5 and comparative example 2 were formulated as emulsions with deionized water. The cinnamon essential oil in the raw material contains more than 75% of cinnamaldehyde, more than 99% of p-phenylenediamine and 98.3% of sialic acid.
TABLE 1 formulation of antiallergic composition
Figure BDA0003444806830000101
Skin external composition allergy test
1. Purpose of experiment
The composition was examined for the ability of sialic acid to inhibit potential allergic symptoms in the presence of a sensitization material.
2. Experimental animals and apparatus as above
3. Test reagent
Examples 1 to 4 and comparative examples 1 and 2 in Table 1, the blank was white oil or deionized water.
4. Test method
(1) Test group
Guinea pigs were randomly divided into 7 groups of 5 animals each, with females ranging from 2 to 3 animals by body weight and sex.
(2) Test preparation
The guinea pig is dehaired at the left and right sides of the back 24h before administration, the area is 5cm×5cm, and dehaired skin is marked whether damaged or not, if damaged, the skin is replaced for standby.
(3) Formal experiments
The test skin area on the left side of dehairing is respectively smeared with 0.1mL of test reagent, the right side is smeared with 0.1mL of white oil or water which is a corresponding blank sample, and after administration, the test skin area is covered by two layers of medical gauze and one layer of glass paper, and is fixedly bound by medical adhesive tape. After 6 hours, the fixing adhesive tape, the glass paper and the medical gauze are removed, and the medical gauze is cleaned and wiped dry by warm water.
5. Test results
After the test objects are removed, the appearance behavior of all guinea pigs is normal, and no abnormal manifestation such as diet, urination and defecation and the like and no immediate toxic reaction are observed after 0.5h, 6h, 24h and 48 h. Within fourteen days after administration of the test substance, no delayed toxic reaction is seen daily, and the animal is in good state and has no poisoning manifestation and death condition.
The evaluation method comprises the following steps: average score per animal calculated for each animal = sum of erythema and edema score for each animal/subject animal, skin irritation intensity was determined in table 2, and experimental results are shown in table 3 and figure 1.
TABLE 2
Figure BDA0003444806830000111
TABLE 3 acute allergy stimulation test results
Time Example 1 Example 2 Example 3 Example 4 Comparative example 1 Comparative example 2 Blank space
0.5h 0 0 0 0 0.4 0.1 0
6h 0 0 0.4 0 0.4 0.2 0
24h 0 0 0 0 0 0 0
48h 0 0 0 0 0 0 0
As can be seen from Table 3, the effects of examples 1 to 4 were less than those of comparative examples 1 and 2 on skin allergy risk, and it was confirmed that sialic acid had an antiallergic effect in the presence of a substance liable to sensitize.
From FIG. 1, cases where a positive reaction was generated in example 3 and cases where a positive reaction was generated in the control group were seen, and edema or erythema state was seen in the observation of 6 hours.
Essential oil preparation
Experimental purposes taking plant essential oil as an example, an antiallergic essential oil skin care product is provided, and specific materials of the skin care product are shown in the following table 4.
TABLE 4 Table 4
Raw and auxiliary materials Mass percent (%)
Isooctyl palmitate 41.45
Jojoba oil 27
White oil 28
VE 1.5
Cinnamon essential oil 0.5
Butyl essential oil 0.5
Neroli essential oil 0.5
Rose essential oil 3
Sialic acid 0.05
In the preparation, sialic acid is evenly dispersed in oil after grinding and homogenizing to obtain oil suspension. The present application is illustrative of the above dosage forms only, and the choice and amount of excipients for all dosage forms is not limited thereto, and may be suitably adjusted by those skilled in the art. The present invention is applicable to various external preparations, and is not exemplified herein.
Skin external application experiment
The purpose of the experiment is as follows: according to the principle of random control, volunteer efficacy evaluation is carried out on self-made skin care products, and the efficacy of the skin care products on allergy prevention is evaluated.
Trial product: the formulation of Table 4 was formulated into skin care products.
The experimental steps are as follows: 20 volunteers with ages of 20-45 years are selected, 8 men and 12 women are selected, and the skin closed patch test is performed for the people with high physical sensitivity and pregnant women.
The tested sample is the above-mentioned essential oil skin care product, the above-mentioned essential oil skin care product without sialic acid separately, the control sample is the above-mentioned essential oil skin care product without sialic acid and plant essential oil.
The test sample and the control sample of the essential oil skin care product without sialic acid were placed into a plaque laboratory at an amount of about 0.025mL. The plaque test with the sample was applied to the forearm of the subject on the curved side (left arm tested and right arm control) with hypoallergenic tape, and applied to the skin with gentle pressure with the palm for 6 hours.
After the spot-stick test is completed for 48 hours, no positive reaction is confirmed by the tested person, and then the tested sample and the control sample of the essential oil skin care product containing sialic acid are placed into a spot tester cell, wherein the dosage is about 0.025mL. The plaque test with the sample was applied to the forearm of the subject on the curved side (left arm tested and right arm control) with hypoallergenic tape, and applied to the skin with gentle pressure with the palm for 6 hours.
Skin reactions were observed according to the criteria of Table 1 30min, 6h, 24h after removal of the plaque assay. And the observations were recorded. The scoring criteria are shown in Table 5 and the test results are filled in total score/number of subjects and the results are shown in Table 6.
TABLE 5 skin response grading Standard for skin seal Patch test
Figure BDA0003444806830000131
TABLE 6 test results
Figure BDA0003444806830000132
As can be seen from table 6, no positive skin reaction occurs in all control cases, the allergic phenomenon occurs in the group of essential oils containing no sialic acid, which indicates that the plant essential oil is indeed a potential allergic stimulus and easily causes skin allergic reaction, and the essential oil added with sialic acid does not have positive reaction and has an antiallergic effect, which indicates that a certain amount of sialic acid and plant essential oil are compounded to have an antiallergic effect.
The application of the skin external composition and sialic acid in preparing the anti-sensitization preparation provided by the invention is described in detail. The principles and embodiments of the present application are described herein with specific examples, and the description of the above examples is only for helping to understand the technical solutions and core ideas of the present application; those of ordinary skill in the art will appreciate that: the technical scheme described in the foregoing embodiments can be modified or some technical features thereof can be replaced by equivalents; such modifications and substitutions do not depart from the spirit of the corresponding technical solutions from the scope of the technical solutions of the embodiments of the present application.

Claims (11)

1. A composition for external use on the skin, characterized in that it comprises sialic acid and a plant essential oil.
2. The composition of claim 1, wherein the mass ratio of sialic acid to plant essential oil in the composition is greater than or equal to 1:20.
3. The composition according to claim 1, wherein the mass percentage of sialic acid in the composition is 0.05% to 2%; and/or the mass percentage of the plant essential oil is 0.1-20%.
4. The composition of claim 1, wherein the sialic acid is selected from the group consisting of: at least one of sialic acid monomer, polysialic acid, sialic acid metal salt or sialic acid derivative.
5. The composition of claim 1, wherein the plant essential oil comprises at least one of a floral essential oil, a citrus essential oil, a vanilla essential oil, a woody essential oil, a spicy essential oil, or a resinous essential oil.
6. The composition according to claim 5, wherein the plant essential oil comprises spicy and/or vanilla essential oil, the spicy and/or vanilla essential oil being present in an amount of 0.1-15% by mass based on the total mass of the composition.
7. The composition of claim 6, wherein the plant essential oil comprises, in parts by weight:
0.1 to 1 part of cinnamon essential oil;
0.1 to 1 part of butyl essential oil;
0.2 to 2 parts of neroli essential oil; and/or
0.1 to 2 portions of rose essential oil.
8. The composition of claim 7, wherein the composition comprises 0 to 6 parts of surfactant, 40 to 60 parts of base oil; and/or, 30-50 parts of moisturizing emollient.
9. The composition according to claim 7, wherein the skin external composition is any one of a lotion, an essence, an emulsion, a face cream, an eye cream, a mask, a sun cream, a body wash, a facial cleanser, a foundation, or a BB cream.
10. Use of sialic acid in the preparation of a formulation for preventing skin allergy.
11. The use according to claim 10, wherein the components that cause the skin to develop an allergic reaction comprise: at least one of essence, preservative, heavy metal, coloring agent, plant essential oil or surfactant.
CN202111644960.8A 2021-12-30 2021-12-30 Skin external composition and application of sialic acid in preparation of antiallergic preparation Pending CN116407460A (en)

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