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CN108158993A - A kind of removing acnes and controlling oil micro emulsion gels and preparation method and application - Google Patents

A kind of removing acnes and controlling oil micro emulsion gels and preparation method and application Download PDF

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Publication number
CN108158993A
CN108158993A CN201810031753.7A CN201810031753A CN108158993A CN 108158993 A CN108158993 A CN 108158993A CN 201810031753 A CN201810031753 A CN 201810031753A CN 108158993 A CN108158993 A CN 108158993A
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Prior art keywords
micro emulsion
parts
oil
emulsion gels
removing acnes
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Inventor
秦昆明
石芸
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Lianyungang Herbal Medicine Technology Co Ltd
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Lianyungang Herbal Medicine Technology Co Ltd
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Priority to CN201810031753.7A priority Critical patent/CN108158993A/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/107Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/164Amides, e.g. hydroxamic acids of a carboxylic acid with an aminoalcohol, e.g. ceramides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • A61K31/375Ascorbic acid, i.e. vitamin C; Salts thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/455Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/60Salicylic acid; 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
    • A61K31/7028Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • 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
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • A61K33/24Heavy metals; Compounds thereof
    • A61K33/30Zinc; Compounds thereof
    • 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
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • 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
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • A61K8/365Hydroxycarboxylic acids; Ketocarboxylic acids
    • 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
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4906Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
    • A61K8/4913Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having five membered rings, e.g. pyrrolidone carboxylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/63Steroids; Derivatives thereof
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    • 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
    • A61K8/67Vitamins
    • A61K8/673Vitamin B group
    • 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
    • A61K8/67Vitamins
    • A61K8/673Vitamin B group
    • A61K8/675Vitamin B3 or vitamin B3 active, e.g. nicotinamide, nicotinic acid, nicotinyl aldehyde
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    • 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
    • A61K8/67Vitamins
    • A61K8/676Ascorbic acid, i.e. vitamin C
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/008Preparations for oily skin

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Abstract

The invention discloses a kind of removing acnes and controlling oil micro emulsion gels and preparation method thereof, the micro emulsion gels are by 0.1 part to 2 parts of salicylic acid, 0.1 part to 3 parts of niacinamide, 0.1 part to 3 parts of ascorbic acid, 0.01 part to 0.1 part of bisabolol, 0.01 part to 0.2 part of zinc pyrrolidone carboxylate, 0.01 part to 0.5 part of panthenol, 0.01 part to 0.2 part of dipotassium glycyrrhizinate, 1 part to 20 parts of oil phase, 1 part to 15 parts of surfactant, 1 part to 10 parts of cosurfactant, 0.1 part to 10 parts of gel matrix material, 0.1 part to 5 parts of pH adjusting agent, 0.1 part to 1 part of preservative, deionized water is made.Micro emulsion gels provided by the invention can increase transdermal penetration rates, promote the Transdermal absorption of more active constituents by percutaneous drug delivery, the purpose of slow release long-acting can be played, product stability is good, has good acne-removing, preparation process is simple, is suitble to industrialized production.

Description

A kind of removing acnes and controlling oil micro emulsion gels and preparation method and application
Technical field
The invention belongs to medicine, cosmetic technical fields, and in particular to a kind of removing acnes and controlling oil micro emulsion gels and its preparation Method.
Background technology
The degree of active constituent absorbing transmission from skin determines its effect in cosmetics, and any cosmetics will be by suitable The effect of carrier competence exertion should have.That is, the composition and property of the cosmetic base, directly affect its active ingredient It absorbs.
Micro emulsion (microemulsion, ME) is one kind by water phase, oil phase, surfactant and cosurfactant institute group Into appearance clear, size droplet diameter be less than 100nm's and the sufficiently stable liquid system of thermodynamics and kinetics.It is micro- The emulsion droplet size of breast is minimum, can freely be dispersed among another liquid and form dispersion system of colloid, emulsion droplet shape is more For spherical shape, and size is substantially uniform, good fluidity, though placement for a long time at a certain temperature, heating, high pressure sterilization, from Heart separation will not be allowed to be layered.Micro emulsion is as active ingredient carrier and Transdermal absorption bleeding agent, compared with emulsion, micro emulsion Grain size is small to nanoscale and to distribute very evenly.Therefore, microemulsion formulation can be blended preferably with active ingredient and uniformly Distribution makes the effect of its Transdermal absorption more preferable, bioavilability higher;Meanwhile microemulsion formulation property is more stablized, and prepares more Industrialization easy to implement.
Gelling agent can in the long time with site of action close adhesion, so as to increase the Transdermal absorption of active ingredient Amount.Gelling agent hygroscopicity is strong, and simultaneously energy absorptive tissue diffusate can be mixed with aqueous solution, is conducive to the removing of skin secretion, and And it is easily dried after smearing.Gelling agent stability and gas permeability are preferable, and chemical property stablizes safety, and nonirritant and allergy is anti- It should.Meanwhile gelling agent do not have it is greasy, it is easy to use, pollution clothes and will not be readily cleaned.
For micro emulsion gels as cutaneous penetration carrier, it has concentrated micro emulsion to the thorough dispersed, gel of drug to skin Adhesiveness, the Deformation Flow under external force, drug is enable preferably uniformly to be applied to skin surface.Micro emulsion gels and skin After contact, drug can be made to discharge for a long time at high concentrations, increase drug transdermal rate, there is better Transdermal absorption effect Fruit, and skin irritation is small, so as to achieve the purpose that improve drug effect and safety.Micro emulsion gels as a kind of novel form, Have both the two-fold advantage of microemulsion and gelling agent, drug solubility can be significantly improved, increase preparation adhesion, improve biological utilisation Degree.
With the continuous improvement of living standards, than more serious, life stress increasingly increases for environmental pollution, and part blueness is caused to be lacked Year and adult suffer from whelk situation it is more and more, not only affect daily life, but also cause spirit negative with economically Load.Whelk is medically known as acne, is a kind of common sebaceous glands chronic disease, pathogenic factor is mainly that smegma is prosperous It contains, leads to what clogging of pores was formed.Whelk is a kind of common disease and frequently-occurring disease, except with hypersteatosis mutually outside the Pass, also and Endocrine-immunity and hair follicle hyperkeratinization are related, in addition, the anaerobic bacterias such as propionibacterium acnes, staphylococcus epidermis etc. are aerobic The mixed infection of bacterium is also closely related with its morbidity.At present, many product for resolving poxes in the market use hormone, antibiotic etc. into Point, it is larger to skin irritation, drug resistance of the skin to acne bacillus is easily caused, safety is under suspicion.And it existing dispels In acne product, often only single selection natural extract carrys out anti-inflammation and sterilization, and there is no carried out for the reason of causing acne The comprehensively regulating of multicomponent, multiple target point and multimachine, so the speed that takes effect is slow.
The acne-removing composition of natural botanical source uses more in recent years, and CN104688811A is disclosed to be carried containing spina gleditsiae Take the acne-removing composition of the ingredients such as object, white willow bark extract, aloe extract, Fructus Forsythiae berry extract, purslane extract.Knot Fruit shows has certain sterilizing rate to propionibacterium acnes, but it uses various plants extracts, it is difficult to be formed stable Cosmetic composition.Therefore, it is necessary to finding one kind has apparent anti-acne effect, and can stablize the acne-removing composition of preservation.
Invention content
The object of the present invention is to provide a kind of stability and absorbability are good, it is safe, nonirritant, Transdermal absorption is good, Microemulsion gel preparation easy to apply and preparation method thereof and the application in cosmetics are prepared.
Technical solution:In order to achieve the goal above, the technical solution that the present invention takes is:
A kind of removing acnes and controlling oil micro emulsion gels, it is made of the raw material of following parts by weight:
0.1 part to 2 parts of salicylic acid, 0.1 part to 3 parts of niacinamide, 0.1 part to 3 parts of ascorbic acid, 0.01 part of bisabolol is extremely 0.1 part, 0.01 part to 0.2 part of zinc pyrrolidone carboxylate, 0.01 part to 0.5 part of panthenol, 0.01 part to 0.2 part of dipotassium glycyrrhizinate, 1 part to 20 parts of oil phase, 1 part to 15 parts of surfactant, 1 part to 10 parts of cosurfactant, 0.1 part to 10 parts of gel-type vehicle, 0.1 part to 5 parts of pH adjusting agent, 0.1 part to 1 part of preservative, appropriate deionized water.
Preferably, above-described removing acnes and controlling oil micro emulsion gels, the oil phase is jojoba seed oil, soybean Oil, peppermint oil, peanut oil, olive oil, castor oil, linseed oil, coconut oil, ethyl oleate, ethyl linoleate, palmitic acid isopropyl One or more of ester, isopropyl myristate, caprylic/capric triglyceride, isopropyl laurate or Monooctamoin Mixture.
Preferably, above-described removing acnes and controlling oil micro emulsion gels, the surfactant is lecithin, pool Lip river Sha Mu, Emulsifier EL-60, Labraso, polyoxyethylene aliphatic alcohol ether, polyethylene glycol hydrogenated castor-oil plant One kind in oil, Arlacel-20, Arlacel-40, Arlacel-60, Arlacel-80, Tween-20, Tween-40, Tween-60 or Tween-80 or Several mixtures.
Preferably, above-described removing acnes and controlling oil micro emulsion gels, the cosurfactant for absolute ethyl alcohol, 1,2- propylene glycol, glycerine, normal propyl alcohol, n-butanol, n-amyl alcohol, isopropanol, isobutanol, isoamyl alcohol, 1- hexanols, 2- hexanols, 1- The mixture of one or more of octanol, sec-n-octyl alcohol, polyethylene glycol, polyethylene glycol 400.
Preferably, above-described removing acnes and controlling oil micro emulsion gels, the gel matrix material are Methyl cellulose Element, ethyl cellulose, hydroxypropyl methylcellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, sodium carboxymethylcellulose, sodium alginate, Acritamer 940, Carbopol, chitosan, ulcerlmin, polyvinylpyrrolidone, polyvinyl alcohol, tragacanth, poloxamer, The mixture of one or more of gelatin.
Preferably, above-described removing acnes and controlling oil micro emulsion gels, the pH adjusting agent is hydrochloric acid, hydroxide One or more of sodium, triethanolamine, diethanol amine, ethylenediamine, lauryl amine, meglumine, tromethamine, sodium bicarbonate The pH of gelling agent is adjusted to 6~8 by mixture.
Preferably, above-described removing acnes and controlling oil micro emulsion gels, which is characterized in that the preservative is oxybenzene Methyl esters, ethyl hydroxy benzoate, methyl hydroxybenzoate, ethylparaben, propylben, bi-imidazolidinyl urea, chloreresol, sorbic acid, mountain The mixture of one or more of potassium sorbate, anesin, Phenoxyethanol.
As more preferred scheme, the oil phase is isopropyl myristate;The surfactant is polyoxyethylene Castor oil;The cosurfactant is 1,2- propylene glycol;The gel matrix material is Acritamer 940;The pH adjusting agent For triethanolamine;The preservative is ethyl hydroxy benzoate.
The present invention screens the active component of item anti-acne by many experiments, the experimental results showed that with salicylic acid, niacinamide, resisting Bad hematic acid, bisabolol, zinc pyrrolidone carboxylate, panthenol and dipotassium glycyrrhizinate multicomponent composition carry out antibacterial activity research, As a result it shows:According to 0.1 part to 2 parts of salicylic acid, 0.1 part to 3 parts of niacinamide, 0.1 part to 3 parts of ascorbic acid, bisabolol 0.01 part to 0.1 part, 0.01 part to 0.2 part of zinc pyrrolidone carboxylate, 0.01 part to 0.5 part of panthenol, 0.01 part of dipotassium glycyrrhizinate After being mixed to 0.2 part of ratio, it can inhibit the activity of propionibacterium acnes.It is antipruritic and other effects so as to play anti-acne.
The preparation method of removing acnes and controlling oil micro emulsion gels of the present invention, includes the following steps:
(1) parts by weight as described in claim 1 take salicylic acid, niacinamide, ascorbic acid, bisabolol, pyrrolidines Keto carboxylic acid zinc, panthenol, dipotassium glycyrrhizinate, surfactant, cosurfactant and oil phase are added under the conditions of being stirred at room temperature It is uniformly mixed in deionized water and obtains micro emulsion;
(2) parts by weight as described in claim 1 take gel-type vehicle and preservative, are added in deionized water, overnight Fully swelling, be uniformly dispersed to obtain Blank gel;
(3) micro emulsion that step (1) is prepared with the Blank gel that step (2) is prepared is mixed, stirs evenly, add Enter pH adjusting agent, adjust after pH is 6 to 8 to get micro emulsion gel.
The preparation process of the present invention is simple, easily operated, and gel matrix material drugloading rate used is big, lasting medicine;It is used A variety of materials can uniformly coordinate with main ingredient, and no incompatibility will not be remained, is readily cleaned on the skin, nontoxic stingless to skin Swash.Micro emulsion drug delivery system can form micro emulsion of the grain size in 10-100nm, can increase the solubility of drug, which can Increase the transdermal penetration rates of drug.
In the present invention, salicylic acid, niacinamide, ascorbic acid, bisabolol, zinc pyrrolidone carboxylate, panthenol, glycyrrhizic acid two Potassium can be rapidly permeated into skin, so as to reach removing acnes and controlling oil, go the effect of print is except trace, moisturizing moisturizing.
Application of the removing acnes and controlling oil micro emulsion gels of the present invention in removing acnes and controlling oil cosmetics are prepared.
The present invention is the study found that salicylic acid, niacinamide, ascorbic acid, bisabolol, zinc pyrrolidone carboxylate, panthenol, sweet The multicomponent combination of oxalic acid dipotassium can obtain excellent anti-acne and oil-control effect, and due to definite ingredients, easily controllable, should Combination can be used for preparing stable cosmetics.Based on this discovery, applicant select the multicomponent combination as primary efficacy into Point, will have the characteristics that skin compatibility is good, grain size is small, the micro emulsion of easy Transdermal absorption and with preparing simple, stable quality, attached The gelling agent for the advantages that putting forth effort strong, good penetrability organically combines, and prepares a kind of microemulsion gel preparation and cosmetics, dispels so as to reach The effect of print is except trace, moisturizing moisturizing is gone in acne oil-control.Many deficiencies of the prior art can be overcome.
Advantageous effect:Removing acnes and controlling oil micro emulsion gels provided by the invention have the following advantages:
1. the present invention is for the first time with salicylic acid, niacinamide, ascorbic acid, bisabolol, zinc pyrrolidone carboxylate, panthenol and sweet Oxalic acid dipotassium prepares a kind of microemulsion gel preparation and cosmetics as main composition.
2. microemulsion thermodynamic stability is good:Under the collective effect of surfactant and cosurfactant, it can be formed Thermodynamically stable dispersion, when storage, will not be layered and stability can be greatly improved.Microemulsion Transdermal absorption is imitated Fruit is good:The emulsion droplet size that the present invention is prepared is between 10-100nm, and structure is similar with human body cell membrane structure, has very Good skin compatibility, can be transported to skin base layer by active constituent.
3rd, the microemulsion bioavilability that the present invention is prepared is higher:After active constituent is wrapped up by micro emulsion, Ke Yida To the effect of slow controlled release, so as to extend the action time of active constituent, so as to substantially increase bioavilability.
4. the gelling agent that the present invention is prepared is easy to coating uniformly, it is readily cleaned, not pollution clothes, can effectively improves To the adhesiveness of skin, and have the function of to promote Drug Percutaneous Absorption.
Specific embodiment
It is as described below, only it is presently preferred embodiments of the present invention, limitation in any form is not done to the present invention, therefore All contents without departing from technical solution of the present invention, technical spirit according to the present invention is made to the above embodiment any simply to repair Change, equivalent variations and modification, in the range of still falling within technical solution of the present invention.
The selection of 1 micro emulsion surfactant of embodiment and cosurfactant
The HLB value for preparing the surfactant of O/W type micro emulsions is 8~18.Present invention screening is using Tween 80 and polyoxy second For alkene castor oil respectively as surfactant, screening absolute ethyl alcohol, 1,2-PD, glycerine, polyethylene glycol-400, which are used as, helps table Face activating agent, surfactant are 3 according to mass ratio with cosurfactant:1 mixing is as mixed surfactant.Nutmeg Isopropyl propionate is oil phase, and blending surface activity is with it according to 9:1、8:2、7:3、6:4、5:5、4:6、3:7、2:8、1:9(w/w) Mixing carries out screening experiment, and water is added dropwise at room temperature, and using system, by clarifying, change is muddy, becomes clear critical point by muddiness as judgement Standard screens suitable surfactant (note:"+" expression can form clear microemulsion;" one " represents muddy, it is impossible to be formed micro- Breast).The experimental results showed that:When isopropyl myristate is oil phase, two different surfactants help surface to live from different Property agent can form microemulsion system, when surfactant is Tween 80, it is bigger to form micro emulsion viscosity, and during one section of placement Between can become cloudy, and micro emulsion clear formed by Emulsifier EL-60, and stability is good.Therefore the present invention preferably polyoxy second Alkene castor oil is surfactant, and four kinds of cosurfactants can be formed with isopropyl myristate and Emulsifier EL-60 The micro emulsion (being shown in Table 1) of clear.
The different micro emulsions that 1 surfactant of table is formed from cosurfactant
The screening of 2 gel-type vehicle of embodiment
The present invention with《Chinese Pharmacopoeia》Middle gelling agent appearance is index, answers uniform, exquisiteness, glue is kept not do at room temperature It dries up or liquefies, screening obtains optimum substrate material.Respectively with Acritamer 940, methylcellulose, hypromellose, hydroxyl first Base sodium cellulosate, chitosan, sodium alginate are added in for matrix system in blank micro emulsion, and in (40 ± 1) DEG C swelling, gel is prepared (being shown in Table 2).It is better than other gel-type vehicles by Acritamer 940 gel-type vehicle can be obtained in table.Therefore, the preferred carbomer of the present invention 940 gel-type vehicles.
The phenomenon that table 2 adds in different gel-type vehicles
3 micro emulsion gels percutaneous penetration of embodiment
Healthy male white mouse 20g or so is taken, the hair on skin of abdomen is carefully cut off with scissors, the neck that breaks is put to death, and removes abdomen Portion's skin.The skin stripped down is laid on glass plate, cuticula is downward, with single back of the body blade carefully reject subcutaneous fat and Then adhesion object is rinsed well repeatedly with physiological saline, be cut into appropriate size, and checks the integrality of skin.Experiment every time Before, it checks the integrality of mouse skin, must not there is any breakage.
Between skin is fixed on upper and lower two Room of diffusion cell, upward, acceptable solution is physiological saline (acceptance pool to cuticula Volume is 7mL), supply pool adds in sample to be tested (salicylic acid, niacinamide, ascorbic acid, bisabolol) 1g, is covered with preservative film Cover Chi Kou.Device is placed in (37 ± 0.01) DEG C water bath with thermostatic control, while speed of agitator:200r/min, timing, respectively at 1,2, 4th, 6,8,10,12,0.5mL is sampled for 24 hours, while add mutually synthermal isometric fresh acceptable solution.The sample detection drug of taking-up Content, calculate accumulation infiltration capacity, obtain steady-state permeation rate (the μ gcm of micro emulsion, micro emulsion gel and ordinary gel with method-2·h-1) (being shown in Table 3).
3 different dosage forms penetrating absorption result (n=3) of table
By with upper table 3 the experimental results showed that, the micro emulsion gel for preparing of the present invention has better Transdermal Absorption Energy.
Embodiment 4
1st, a kind of removing acnes and controlling oil micro emulsion gels, it is made of the raw material of following weight g numbers:
Salicylic acid 2g, niacinamide 2g, ascorbic acid 2g, bisabolol 0.1g, zinc pyrrolidone carboxylate 0.2g, panthenol 0.5g, dipotassium glycyrrhizinate 0.2g, isopropyl myristate 2g, Emulsifier EL-60 3g, 1,2-PD 1g, Acritamer 940 0.5g, triethanolamine 0.1g, ethyl hydroxy benzoate 0.1g, appropriate deionized water.
2nd, a kind of preparation method of removing acnes and controlling oil micro emulsion gels, includes the following steps:
(1) by salicylic acid 2g, niacinamide 2g, ascorbic acid 2g, bisabolol 0.1g, zinc pyrrolidone carboxylate 0.2g are general Alcohol 0.5g, dipotassium glycyrrhizinate 0.2g, isopropyl myristate 2g, Emulsifier EL-60 3g, 1,2-PD 1g, at room temperature It is stirred, adds in and load medicine micro emulsion is uniformly mixed so as to obtain into deionized water;
(2) Acritamer 940 0.5g, the ethyl hydroxy benzoate 0.1g of recipe quantity are weighed, is added in deionized water, is fully swollen, divides Dissipate uniform Blank gel;
(3) Blank gel that the micro emulsion that step (1) prepares is prepared with step (2) is mixed evenly, used The triethanolamine of 0.1g is adjusted after pH is 6-8 to get micro emulsion gels.
Embodiment 5
1st, a kind of removing acnes and controlling oil micro emulsion gels, it is made of the raw material of following weight g numbers:
Salicylic acid 2g, niacinamide 1g, ascorbic acid 2g, bisabolol 0.1g, zinc pyrrolidone carboxylate 0.2g, panthenol 0.3g, dipotassium glycyrrhizinate 0.1g, isopropyl myristate 8g, Emulsifier EL-60 5g, 1,2-PD 2g, Acritamer 940 4g, triethanolamine 0.3g, ethyl hydroxy benzoate 0.2g, appropriate deionized water.
2nd, a kind of preparation method of removing acnes and controlling oil micro emulsion gels, includes the following steps:
(1) by salicylic acid 2g, niacinamide 1g, ascorbic acid 2g, bisabolol 0.1g, zinc pyrrolidone carboxylate 0.2g are general Alcohol 0.3g, dipotassium glycyrrhizinate 0.1g, isopropyl myristate 8g, Emulsifier EL-60 5g, 1,2-PD 2g is at room temperature Stirring adds in into deionized water uniformly mixed be prepared into and carries medicine micro emulsion;
(2) Acritamer 940 4g, the ethyl hydroxy benzoate 0.2g of recipe quantity are weighed, is added in deionized water, fully swelling, dispersion It is uniform to obtain Blank gel;
(3) Blank gel that the micro emulsion that step (1) prepares is prepared with step (2) is mixed evenly, with three Ethanol amine 0.3g is adjusted after pH is 6-8 to get micro emulsion gels.
6 Absorption in vitro test experience of embodiment
Healthy male white mouse 20g or so is taken, the hair on skin of abdomen is carefully cut off with scissors, the neck that breaks is put to death, and removes abdomen Portion's skin.The skin stripped down is laid on glass plate, cuticula is downward, with single back of the body blade carefully reject subcutaneous fat and Then adhesion object is rinsed well repeatedly with physiological saline, be cut into appropriate size, and checks the integrality of skin.Experiment every time Before, it checks the integrality of mouse skin, must not there is any breakage.
Between skin is fixed on upper and lower two Room of diffusion cell, upward, acceptable solution is physiological saline (acceptance pool to cuticula Volume is 7mL), supply pool adds in the micro emulsion gels 1g that embodiment 4 is prepared, and Chi Kou is covered with preservative film.Device is put In (37 ± 0.01) DEG C water bath with thermostatic control, while speed of agitator:200r/min, timing, respectively at 1,2,4,6,8,10,12, 0.5mL is sampled for 24 hours, while adds mutually synthermal isometric fresh acceptable solution.The content of the micro emulsion gels detection drug of taking-up, Accumulation infiltration capacity is calculated, steady-state permeation rate (the μ gcm of micro emulsion, micro emulsion gel and ordinary gel are obtained with method-2·h-1) (be shown in Table 4)。
4 embodiment of table, 1 micro emulsion gels penetrating absorption result (n=3)
7 anti-acne of embodiment or the activity experiment for inhibiting propionibacterium acnes
Screening test:To the inhibiting effect of propionibacterium acnes
Sample preparation:Each 1g of sample, salicylic acid single component 20mg prepared by Example 4 and embodiment 5.It takes a certain amount of Sample, be separately added into 1,3 one butanediol of 50mL deionized waters or 50mL, be uniformly mixed, it is spare.
Drug sensitive test:Inoculation:1-2 propionibacterium acnes colony inoculation of picking is on LB plating mediums, 37 DEG C Aerobic culture for 24 hours, the purebred P.acne of aerobic culture for 24 hours is rinsed with sterile saline, flushing liquor is put into sterile test tube; Using Maxwell turbidimetry than turbid, opacity tube is with shaking 10-12 times is before needed, first than turbid to 3*108/ mL, then use normal saline dilution To 105-106/ mL is spare.LB plating mediums are inoculated with:The swab stick of sterilizing is dipped into bacterium solution, extra bacterium solution is gone in being squeezed on tube wall, The even spread on LB plating mediums, and a circle is swept along plate edge ring, cover plate, dry 2-3min.By sterile steel bowl (a diameter of 6mm) is put down gently on plating medium, filling it up with ready sample liquid, is put into 37 DEG C of aerobic cultures for 24 hours, is found nothing in plate Bacterial growth continues 37 DEG C of aerobic cultures and sees have inhibition zone to be formed afterwards for 24 hours.
Antibacterial circle diameter is measured, is judged as a result, 3 groups of antibacterial circle diameter values are averaged, antibacterial susceptibility grade classification:Suppression Collarium diameter is more than 20mm for Gao Min, quick in 10-20mm, is drug resistance less than 10mm.
Result of the test:It is shown in Table 5
5 antibacterial Comparative result result of table
It can be seen that micro emulsion gels prepared by the present invention have propionibacterium acnes exact inhibiting effect, and imitate Fruit and the more significant difference of salicylic acid.

Claims (9)

1. a kind of removing acnes and controlling oil micro emulsion gels, which is characterized in that it is made of the raw material of following parts by weight:
0.1 part to 2 parts of salicylic acid, 0.1 part to 3 parts of niacinamide, 0.1 part to 3 parts of ascorbic acid, 0.01 part to 0.1 of bisabolol Part, 0.01 part to 0.2 part of zinc pyrrolidone carboxylate, 0.01 part to 0.5 part of panthenol, 0.01 part to 0.2 part of dipotassium glycyrrhizinate, oil phase 1 part to 20 parts, 1 part to 15 parts of surfactant, 1 part to 10 parts of cosurfactant, 0.1 part to 10 parts of gel-type vehicle, pH tune Save 0.1 part to 5 parts of agent, 0.1 part to 1 part of preservative, appropriate deionized water.
2. removing acnes and controlling oil micro emulsion gels according to claim 1, which is characterized in that the oil phase for jojoba seed oil, Soybean oil, peppermint oil, peanut oil, olive oil, castor oil, linseed oil, coconut oil, ethyl oleate, ethyl linoleate, palmitic acid are different One kind or several in propyl ester, isopropyl myristate, caprylic/capric triglyceride, isopropyl laurate or Monooctamoin The mixture of kind.
3. removing acnes and controlling oil micro emulsion gels according to claim 1, which is characterized in that the surfactant is lecithin Fat, poloxamer, Emulsifier EL-60, Labraso, polyoxyethylene aliphatic alcohol ether, polyoxyethylene hydrogen Change in castor oil, Arlacel-20, Arlacel-40, Arlacel-60, Arlacel-80, Tween-20, Tween-40, Tween-60 or Tween-80 One or more of mixtures.
4. removing acnes and controlling oil micro emulsion gels according to claim 1, which is characterized in that the cosurfactant is anhydrous Ethyl alcohol, 1,2- propylene glycol, glycerine, normal propyl alcohol, n-butanol, n-amyl alcohol, isopropanol, isobutanol, isoamyl alcohol, 1- hexanols, 2- hexanols, The mixture of one or more of 1- octanols, sec-n-octyl alcohol, polyethylene glycol, polyethylene glycol 400.
5. removing acnes and controlling oil micro emulsion gels according to claim 1, which is characterized in that the gel matrix material is methyl Cellulose, ethyl cellulose, hydroxypropyl methylcellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, sodium carboxymethylcellulose, seaweed Sour sodium, Acritamer 940, Carbopol, chitosan, ulcerlmin, polyvinylpyrrolidone, polyvinyl alcohol, tragacanth, pool Lip river The mixture of one or more of Sha Mu, gelatin.
6. removing acnes and controlling oil micro emulsion gels according to claim 1, which is characterized in that the pH adjusting agent is hydrochloric acid, hydrogen One kind or several in sodium oxide molybdena, triethanolamine, diethanol amine, ethylenediamine, lauryl amine, meglumine, tromethamine, sodium bicarbonate The mixture of kind, 6~8 are adjusted to by the pH of gelling agent.
7. removing acnes and controlling oil micro emulsion gels according to claim 1, which is characterized in that the preservative for methyl hydroxybenzoate, Ethyl hydroxy benzoate, methyl hydroxybenzoate, ethylparaben, propylben, bi-imidazolidinyl urea, chloreresol, sorbic acid, sorbic acid The mixture of one or more of potassium, anesin, Phenoxyethanol.
8. the preparation method of removing acnes and controlling oil micro emulsion gels described in claim 1, which is characterized in that include the following steps:
(1) parts by weight as described in claim 1 take salicylic acid, niacinamide, ascorbic acid, bisabolol, pyrrolidones carboxylic Sour zinc, panthenol, dipotassium glycyrrhizinate, surfactant, cosurfactant and oil phase, be added under the conditions of being stirred at room temperature from It is uniformly mixed in sub- water and obtains micro emulsion;
(2) parts by weight as described in claim 1 take gel-type vehicle and preservative, are added in deionized water, overnight abundant Swelling, be uniformly dispersed to obtain Blank gel;
(3) micro emulsion that step (1) is prepared with the Blank gel that step (2) is prepared is mixed, stirred evenly, add in pH Conditioning agent is adjusted after pH is 6 to 8 to get micro emulsion gel.
9. application of claim 1 to the 8 any one of them removing acnes and controlling oil micro emulsion gels in removing acnes and controlling oil cosmetics are prepared.
CN201810031753.7A 2018-01-12 2018-01-12 A kind of removing acnes and controlling oil micro emulsion gels and preparation method and application Pending CN108158993A (en)

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CN108703895A (en) * 2018-08-21 2018-10-26 赵宏伟 A kind of long-acting moisturizing gel and preparation method of percdation
CN110585117A (en) * 2019-09-16 2019-12-20 五邑大学 Thermo-sensitive gel preparation of phloretin and preparation method and application thereof
CN110742833A (en) * 2019-11-28 2020-02-04 广州环亚化妆品科技有限公司 Acne-removing, whitening and anti-aging essential oil composition as well as preparation method and application thereof
CN111000795A (en) * 2019-12-26 2020-04-14 山西瑞博隆生物科技有限公司 Compound microemulsion gel containing soybean isoflavone nano-microspheres and preparation method thereof
CN111870590A (en) * 2020-08-13 2020-11-03 广州市科能化妆品科研有限公司 Liquid acne removing patch and preparation method thereof
CN112315883A (en) * 2020-11-24 2021-02-05 哈尔滨敷尔佳科技发展有限公司 Skin care composition for controlling oil and removing acne and preparation and application thereof
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CN112603993A (en) * 2020-12-19 2021-04-06 江苏诺瓦立医疗用品有限公司 Gel for treating inflammatory acne based on chitosan and preparation method thereof
CN113908064A (en) * 2020-07-08 2022-01-11 河南净好运医疗科技有限公司 Gel matrix and preparation method thereof
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CN115634181A (en) * 2022-11-07 2023-01-24 广州东耀化妆品有限公司 A kind of antibacterial composition and application thereof against Propionibacterium acnes
CN116059121A (en) * 2021-11-03 2023-05-05 安佳医药(广州)有限公司 Wrapped salicylic acid
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CN108703895A (en) * 2018-08-21 2018-10-26 赵宏伟 A kind of long-acting moisturizing gel and preparation method of percdation
CN110585117A (en) * 2019-09-16 2019-12-20 五邑大学 Thermo-sensitive gel preparation of phloretin and preparation method and application thereof
US20210093724A1 (en) * 2019-09-30 2021-04-01 Concept Matrix Solutions Topical anti-acne composition
CN110742833A (en) * 2019-11-28 2020-02-04 广州环亚化妆品科技有限公司 Acne-removing, whitening and anti-aging essential oil composition as well as preparation method and application thereof
CN111000795A (en) * 2019-12-26 2020-04-14 山西瑞博隆生物科技有限公司 Compound microemulsion gel containing soybean isoflavone nano-microspheres and preparation method thereof
CN113908064A (en) * 2020-07-08 2022-01-11 河南净好运医疗科技有限公司 Gel matrix and preparation method thereof
CN111870590A (en) * 2020-08-13 2020-11-03 广州市科能化妆品科研有限公司 Liquid acne removing patch and preparation method thereof
CN111870590B (en) * 2020-08-13 2023-12-15 广州市科能化妆品科研有限公司 Liquid acne-removing patch and preparation method thereof
CN112315883B (en) * 2020-11-24 2023-01-06 哈尔滨敷尔佳科技股份有限公司 Skin care composition for controlling oil and removing acne and preparation and application thereof
CN112315883A (en) * 2020-11-24 2021-02-05 哈尔滨敷尔佳科技发展有限公司 Skin care composition for controlling oil and removing acne and preparation and application thereof
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FR3119324A1 (en) * 2021-02-04 2022-08-05 L'oreal COMPOSITION TO IMPROVE THE APPEARANCE OF KERATINOUS MATERIALS
CN116059121A (en) * 2021-11-03 2023-05-05 安佳医药(广州)有限公司 Wrapped salicylic acid
CN115634181A (en) * 2022-11-07 2023-01-24 广州东耀化妆品有限公司 A kind of antibacterial composition and application thereof against Propionibacterium acnes
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