CN1159753A - Anti-acne cosmetic compositions - Google Patents

Anti-acne cosmetic compositions Download PDF

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Publication number
CN1159753A
CN1159753A CN95195386A CN95195386A CN1159753A CN 1159753 A CN1159753 A CN 1159753A CN 95195386 A CN95195386 A CN 95195386A CN 95195386 A CN95195386 A CN 95195386A CN 1159753 A CN1159753 A CN 1159753A
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Prior art keywords
cosmetic composition
acne
water
composition
weight
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CN95195386A
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G·S·布里格斯
T·B·克罗克
G·D·T·史密斯
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Procter and Gamble Co
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Procter and Gamble Co
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/191—Carboxylic acids, e.g. valproic acid having two or more hydroxy groups, e.g. gluconic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/194—Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
    • A61K31/203—Retinoic acids ; Salts thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/60—Salicylic acid; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04—Dispersions; Emulsions
    • A61K8/06—Emulsions
    • A61K8/066—Multiple emulsions, e.g. water-in-oil-in-water
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/113—Multiple emulsions, e.g. oil-in-water-in-oil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/08—Anti-ageing preparations

Abstract

An anti-acne cosmetic composition in the form of a multiple phase water-in-oil emulsion and process for preparing thereof, wherein the composition comprises two or more aqueous phases and a coalescence inhibitor for preventing coalescence of the aqueous phases and wherein at least a first aqueous phase comprises the anti-acne active in the form of an aqueous/alcoholic solution. The composition exhibits moisturisation, anti-acne activity and skin anti-ageing benefits, together with product and colour stability.

Description

The cosmetic composition of anti-acne
Technical background
The present invention relates to cosmetic composition.Relate in particular to painted cosmetic composition, said composition provides effect and the prescription and the colour stability of humidification effect, improved anti-acne activity and the anti aging effect of excellence.
Background of invention
Skin is made up of several cellular layers, and its covering and protection form the keratin and the collagen fiber albumen of skin texture skeleton.The outermost layer of these cellular layers is called horny layer, and known is the protein Shu Zucheng of 25 nanometers that is surrounded by the layer of 8 nanometer thickness by skin.Anion surfactant and organic solvent infiltrate the cutin tunic usually and destroy its integrity by degreasing (sloughing the class ester in the horny layer).This skin surface structural damage causes harsh feeling and may finally make surfactant or solvent and keratin reaction, produces pain.
Suitable water content gradient is important to its function in the now cognitive maintenance horny layer.Most water is considered to cuticular flexibility agent sometimes, comes from the body.If humidity is too low,, there is not adequate moisture to keep organizing normal pliability, skin will become squamous and producing Pruritus in outer layer of stratum corneum as at cold day.When cuticular moisture content was inadequate, percutaneous permeability also had certain reduction.On the other hand, the too many moisture content of skin outer layer will cause horny layer finally to absorb the doubly bound water of himself weight of 3-5.This makes puffiness of skin wrinkling, causes skin that the permeability of moisture content or other polar molecule is approximately increased by 2 to 3 times.
Need compositions like this, although it is in washing, the deleterious interaction that runs in work and the amusement still can help horny layer to keep its barrier and water retaining function is in optimum state.
Traditional cosmetic emulsion and detergent composition in the document, for example, " Sagarin cosmetic science and technology ", the 2nd edition, volume 1, Wiley Interscience publishes (1972) and " encyclopedia of chemical technology ", the third edition, in the volume 7, the known advantage of skin moistening, barrier and water conservation (humidification) in various degree that provides.Yet also there is serious adverse (being that skin often feels greasy) in they and has relatively poor rubbing to wipe infiltration, absorption and persistence characteristic aspect dermal sensation.
Also need to provide a kind of like this cosmetic composition, it brings color and luster but also the humidification effect is provided not only for the skin of user.Colored cosmetic compositions can be used for the color harmony quality of even skin, and hides hole, defective, microgroove etc.
Simultaneously, also need to provide a kind of active humidifying composite of topical anti-acne that has.Known have chemical compound lot to work as them to embody the anti-acne performance when being locally applied to skin.It is normally used that to have the active keratolytic of anti-acne be salicylic acid.But because salicylic acid is water insoluble substantially, it is difficult to be incorporated into the aqueous phase of emulsion compositions.The variable color (because salicylic acid and colorant, especially reaction of the colorant of titanium oxide type) that provides salicylic acid can produce on the one hand compositions the colorant oil phase from containing of emulsion compositions.In addition, in requiring the high compositions of water content (as skin moisturizing compositions), salicylic acid trends towards being settled out from solution.Therefore, need provide salicylic acid with soluble form and not have salicylic acid from water and from solution, be settled out.
Therefore, a target of the present invention provides a kind of cosmetic composition that anti-acne is active and increase the profit effect that embodies.
Another target of the present invention provides the cosmetic composition with the multi-phase emulsion form with improved products and color stability.
Summary of the invention
According to one aspect of the present invention, a kind of anti-acne cosmetic composition with each phase water-in-oil emulsion form is provided, wherein compositions comprises:
(a) two or more waters; With
(b) prevent the anti-coalescent that water is coalescent;
Wherein at least the first water comprises the anti-acne active ingredient with water/alcoholic solution form.
According to the present invention, a kind of preparation anti-acne method for compositions also is provided, this method may further comprise the steps:
(a) with anti-acne active ingredient water-soluble/alcoholic solution prepares first water;
(b) first water is mixed with oil phase; With
(c) subsequently one or more other waters are added to the gained mixture forming heterogeneous water-in-oil emulsion, first and/or other aqueous phase be dissolved with anti-coalescent.
Compositions of the present invention provides the effect of anti-acne activity and anti aging effect, and improved products and color stability and excellent humidification effect, skin feel and outward appearance.
All content and ratio are all in composition total weight, except as otherwise noted.The detailed description of invention
Compositions of the present invention is the heterogeneous water-in-oil emulsion that comprises two or more waters.At least the first water includes the anti-acne active ingredient with water/alcoholic solution form.The active component that is applicable to this comprises salicylic acid, tretinoin, Azelaic Acid, lactic acid, glycolic, acetone acid, flavonoid and its derivant and salt, and composition thereof.
The anti-acne active ingredient that is used for this compositions is preferably from salicylic acid and Azelaic Acid and composition thereof, more preferably salicylic acid.The content of anti-acne active ingredient be composition weight about 0.1% to about 10%, preferred about 0.1% to about 5%, more preferably from about 0.5% to about 3%.
Anti-acne active ingredient is dissolved in water or alcoholic solution, and alcoholic solution for example is based on C 2-C 6The solution of alcohol, two pure and mild many alcohol, preferred alcohol is selected from ethanol, dipropylene glycol, butanediol, hexanediol and its mixture.The preferred content with about 1% to about 20% of alcohol is present in the compositions.Water/the alcoholic solution of final anti-acne active ingredient preferably has under the room temperature (25 ℃) less than about pK a+ 1 pH value, wherein pK aIt is the logarithm acidity constant of fully protonated anti-acne active ingredient.In preferred embodiments, the pH of final solution is less than about pK a
Therefore, the logarithm acidity constant is defined by following balance
H ++ H N-1A=H nA is H wherein nA is fully protonated acid, and n is the proton number in the protonated fully acid, H N-1A is the conjugate base corresponding to the acid of loss proton.
So this equilibrated acidity constant (K n) be: [ H n A ] [ H + ] [ H n - 1 A ]
And pK a=log10 K n
For the purpose of this description, acidity constant is that zero condition is given a definition 25 ℃ and ionic strength.Desirable literature value under the possible situation (seeing " stability constant of metal-ionic complex ", Special Publication No.25, chemistry meeting, London); When query occurring, use glass electrode by these values of potentiometric determination.
The pK of tart anti-acne active ingredient used herein aBe preferably about 1 to about 6, more preferably from about 1 to about 4.5, particularly about 1.5 to about 4.0.
The pH preferably about 1 of the water/alcoholic solution of final anti-acne active ingredient is to about 7, and more preferably from about 2 to about 5, particularly about 2 to about 4.Less than about 5 o'clock, there was not sour unsettled material in preferred water, as acrylic acid/ethyl acrylate copolymer and polymethyl acid glyceride at pH value.
Another basis is the anti-coalescent that prevents that water is coalescent in the said composition.Preferred anti-coalescent is electrolyte or electrolyte mixture, is preferably sodium chloride.The content of anti-coalescent is about 0.05% to about 5%, preferred about 0.01% to about 2% of composition weight.
Compositions of the present invention is the form that comprises the heterogeneous water-in-oil emulsion of two or more waters.As mentioned above, the present composition comprises at least one first water, and this comprises the anti-acne active ingredient with water/alcoholic solution form mutually.This first water preferably comprises the water that is no more than about 20% weight.Compositions of the present invention also comprises second water, and this preferably comprises the water at least about 15% weight of compositions mutually.The present composition preferably comprises about altogether 30% to about 50% heavy water and about 1% to about 15% heavy alcoholic solvent.The amount of the anti-acne active ingredient that said composition comprises usually surpasses the dissolubility that its at room temperature (25 ℃) in the equivalent mixture of water and solvent is measured.But feature of the present invention is: by the heterogeneous form and the anti-coalescent of use of aforesaid compositions, the anti-acne material can soluble form be prepared, and its content surpasses its normal dissolubility in single-phase water/pure system.
The present composition preferably comprises the complexant based on ketopyrrolidine.In order to help the dissolving of anti-acne active ingredient, added complexant, and it also is that a kind of film forming matter of aqueous phase interface is to prevent the coalescent of water phase based on ketopyrrolidine.Here based on the complexant of ketopyrrolidine preferably from polyvinyl pyrrolidone complexant or C 1-C 4Alkyl polyvinyl pyrrolidone complexant, its molecular weight (all sticking) about 1500 be to about 1,500,000, preferred about 3000 to about 700,000, and more preferably from about 5000 to about 100,000.Suitable example based on the complexant of ketopyrrolidine is polyvinyl pyrrolidone (PVP) (or claiming povidone) and butylation polyvinyl pyrrolidone.Here most preferred complexant based on ketopyrrolidine is the polyvinyl pyrrolidone complexant.PVP can be commercial with Luviskol (RTM) trade name from BASF Corp.Here preferred PVP complexant is the Luviskol K17 of viscosity-average molecular weight about 9,000.Other complexant based on ketopyrrolidine that is applicable to this comprises C 1-C 18Alkyl or hydroxyalkyl ketopyrrolidine are as the lauryl ketopyrrolidine.
Content based on the complexant of ketopyrrolidine in the said composition is about 0.1% to about 10%, preferred about 0.1% to about 5% of composition weight.Anti-acne active ingredient is about 10: 1 to about 1: 10 with weight ratio based on the complexant of ketopyrrolidine, preferred about 5: 1 to about 1: 5.
Also comprise about 0.01% to about 5% in the preferred embodiment of the invention, preferred about 0.1% to about 1%, especially about 0.1% to about 0.5% heavy acid or its salt, this acid or salt are less than or equal to the pK of respective acids (as citric acid, boric acid) and salt and its mixture at pH value aWater soluble under the situation of value.From helping the dissolved angle of anti-acne active ingredient, it is useful that these materials are used in combination with complexant based on ketopyrrolidine.From this viewpoint, particularly preferably be the sodium salt of citric acid.In preferred embodiments, the dissolubility of acid or its salt is at least 5% weight by weight (25 ℃).
The present composition is with the form of heterogenetic water-in-oil emulsion, contain two or more, the interior water of preferred two separations.Oil phase comprises the mixture of volatile polysiloxanes and nonvolatile polysiloxanes in preferred embodiments.The amount of the silicone oil that is comprised is about 50% (weight) of about 1%-.The volatile silicone oils that is fit to comprises ring-type and the poly-organopolysiloxane (used term " volatile " is meant those materials that the vapour pressure that can measure is arranged under environmental condition) of straight chain volatility here.
At people's such as Todd " used for cosmetic Y 7175 fluid ", can find description among the 91 Cosmeticsand Tioletries 27-32 (1976) about various Y 7175s.
Preferred cyclic polysiloxanes comprises and contains about 9 silicon atoms of about 3-, preferably contains the polydimethylsiloxane of about 5 silicon atoms of about 4-.Preferred straight chain silicone oil comprises the polydimethylsiloxane that contains about 9 silicon atoms of about 3-.The straight chain Y 7175 generally has the viscosity less than about 5 centistokes (25 ℃), and the ring-type material has the viscosity less than about 10 centistokes.The example that is applicable to silicone oil of the present invention comprises: Dow Corning 344, Dow Corning 21330, Dow Corning345 and Dow Corning 200 (being made by Dow Corning Corporation): Silicone 7207 and Silicone7158 (being made by Union Carbide Corporation), SF:202 (being made by General Electric Co. Limited) and SWS-03314 (being made by Stauffer chemical company).
The non-volatile polysiloxanes that is fit to preferably has an appointment 1, and 000-is about 2,000,000mm 2S -1The average viscosity of (25 ℃), more preferably from about 10,000-is about 1,800,000mm 2S -1, further preferred about 100,000-is about 1,500,000mm 2S -1Yet can also use more low viscous nonvolatile siloxanes regulator.Can measure viscosity by means of the glass capillary tube viscometer that the method for testing CTM0004 of Dow Corning Corporation on the 20th provided by July in 1970.The fixedness polysiloxane fluid that is applicable to this comprises polysiloxanes that poly-alkylsiloxane, poly-aryl siloxanes, polyoxyethylene alkyl aryl radical siloxane, amino-functional replace, polyether siloxane copolymer and composition thereof.Being used for polysiloxanes of the present invention can comprise as methyl, hydroxyl, oxirane, expoxy propane base, amino and carboxy blocking with any amount of molecule part.Yet, can use other polyorganosiloxane fluid of skin adjusting function.Operable nonvolatile poly-alkylsiloxane liquid comprises for example polydimethylsiloxane.These polysiloxanes are can be by the Viscasil that obtains as General Electric Co. Limited (RTM) series and Dow Corning 200 series of products that obtained by Dow Corning Corporation.Be preferably about 10mm at 25 ℃ range of viscosities 2S -1-Yue 100,000mm 2S -1Operable polyoxyethylene alkyl aryl radical siloxane liquid also comprises for example PSI.These polysiloxanes are can be by SF1075 aminomethyl phenyl liquid that obtains as General Electric Co. Limited or the 556 cosmetics-stage fluids that obtained by DOW CORNING.Operable polyether siloxane copolymer comprises as a kind of dimethyl polysiloxane of poly(propylene oxide) modification (as Dow Corning DC-1248), can also use the mixture of oxirane or oxirane and expoxy propane to carry out described modification.
The document of describing the polyorganosiloxane fluid that is fit to comprises authorized the patent USA 3964500 of Drakoff on June 22nd, 1976 by the patent USA2826551 of Green; The patent USA 4364837 of Pader; Patent GBA 849433 with Woolston.In addition, 1984 " silicone compounds " by Petrarch Systems Inc. classification provides large-scale (but being not whole) inventory of the silicone liquid that is fit to.
The preferred nonvolatile polysiloxanes that is applicable to this comprises poly-diorganosiloxane polyoxyalkylene copolymers, and it contains at least one poly-diorganosiloxane segment and at least one polyoxyalkylene segment, and described poly-diorganosiloxane segment is mainly by R bSiO (4-b)/2Siloxane unit is formed, the b value of 0-about 3 of having an appointment wherein, each silicon has average about 2 R bases all siloxane units in copolymer, and R is selected from methyl, ethyl, vinyl, phenyl and a kind ofly makes described polyoxyalkylene chain paragraph key be incorporated into bilvalent radical on the poly-diorganosiloxane segment, all R bases be methyl at least about 95%; And described polyoxyalkylene segment has at least about 1000 mean molecule quantity and by the polyoxypropylene unit of about 50% (mole) of about 0-and the polyoxyethylene unit of about 100% (mole) of about 50-and forms, at least one end of described polyoxyalkylene segment is bonded on the described poly-diorganosiloxane segment, and any end that is not bonded to the described polyoxyalkylene segment on the described poly-diorganosiloxane segment all uses a kind of termination base to come saturated; The weight ratio of poly-diorganosiloxane segment and polyoxyalkylene segment is about 2-about 8 in the described copolymer.This base polymer has been described among the USA 4268499.
Be applicable to poly-diorganosiloxane-polyoxyalkylene copolymers that this more preferably following formula is represented:
Figure A9519538600111
Wherein select weight ratio that X and Y make poly-diorganosiloxane segment and polyoxyalkylene segment about 8, mol ratio a: (a+b) be that about 0.5-is about 1, and R to be the chain termination base, particularly to be selected from hydrogen for about 2-; Hydroxyl; Alkyl such as methyl, ethyl, propyl group, butyl, benzyl; Aryl such as phenyl; Alkoxyl such as methoxyl group, ethyoxyl, propoxyl group, butoxy; Benzyloxy; Aryloxy group such as phenoxy group; Alkenyloxy such as ethyleneoxy and propenyloxy group; Acyloxy such as acetoxyl group, acryloxy and propionyloxy and amino as dimethylamino.
Segmental quantity and mean molecule quantity should make the poly-diorganosiloxane segment in the copolymer and the weight ratio of polyoxyalkylene segment be preferably about 2.5-about 4.0 in the copolymer.
The copolymer that is fit to is the commercially available Wacker-Chemie company limited that originates from, address Gesehaftsbereich S, the commodity of Postfach D-8000 Munich 22 are called the product of Belsil (RTM) and originate from the Th.Goldschmidt company limited, address Tego House, Victoria Road, Ruislip, Middlesex, the commodity of HA40YL are called the product of Abil (RTM).What be applicable to this particularly preferably is Belsil (RTM) 6031, Abil (RTM) B88183 and DC3225C.Here the CTFA name of preferred polysiloxanes is called dimethicone copolymerization polyol.
The polysiloxanes oil phase preferably contains about 25%, the non-volatile polysiloxanes of about 15% (weight) of 5%-more preferably from about of about 2%-of compositions.
The very preferred composition of the another kind of the compositions here is wetting agent or wetting agent mixture.Wetting agent here or wetting agent mixture be about 30% with the heavy about 0.1%-of compositions, preferably about 5%-amount about 25%, that be more preferably about 10%-about 20% exists.Wetting agent or wetting agent mixture preferably are present in one or more aqueous phases.
Wetting agent to small part can be sneaked in the oil phase of water-in-oil emulsion to form a kind of heterogeneous Water-In-Oil (wetting agent) oil-in-water dispersion liquid.In these embodiments, based on compositions, it is about 10% that oil phase contains the 0.1%-that has an appointment, more preferably from about the wetting agent of 0.1%-about 3% (weight).Wetting agent can add in the oil phase with the form with a kind of graininess oleophylic or hydrophobic carrier mixtures of material.
The wetting agent that is fit to comprises sorbitol, panthenol, propylene glycol, butanediol, hexanediol, oxyalkylated glucosan derivative, as Glucam (RTM) E-20, hexanetriol, glucose ether, and composition thereof.Carbamide also is a kind of wetting agent that is fit to add one or more inner aqueous phases.
The panthenol humidizer can be selected from D-panthenol ((R)-2; 4-dihydroxy-N-(3-hydroxypropyl))-3,3-amide dimethyl butyrate), DL-panthenol, calcium pantothenate, royal jelly, pantethine (panthetine), pantetheine, pantoyl benzyl ethyl ether, pangamic acid, pyridoxin, pantoyl lactose and vitamin B complex.
Here preferred humectants is a glycerol.The chemical name of glycerol is 1,2, the 3-glycerol, and it is a commercial product.
Here comprise colorant or coloring material for mixing thing in the embodiment preferred.The colorant that is applicable to this can be inorganic matter and/or Organic substance.The material that is also included within the colorant term scope has weak color or weak glossy material, as unglazed lacquer, and light scattering agent.The example of the colorant that is fit to has iron oxides class, acyl glutamic acid iron oxides class, ultramarine blue, D﹠amp; C dyestuff, carmine and composition thereof.
The compositions here can also be added with at least a unglazed lacquer.The effect of unglazed lacquer is to cover skin defect and reduce light.The Silicon stone beadlet that the inorganic reagent that allows in these class cosmetics (promptly be included in the third edition " CTFA used for cosmetic composition dictionary " those) is crossed as Silicon stone, hydration Silicon stone, siloxane treated, Muscovitum, Talcum, polyethylene, titanium dioxide, bentonite, hectorite, Kaolin, Chalk, kieselguhr, zinc oxide (USP or superfine) etc. can use.Be specially adapted to as unglazed lacquer be the low gloss colorant, as be enclosed with BaSO 4Metatitanic acid Muscovitum (titanium dioxide parcel Muscovitum).Particularly preferably be Talcum, polyethylene, hydration Silicon stone, Kaolin, titanium dioxide and composition thereof as in the inorganic constituents of unglazed lacquer low gloss colorant.The material that is suitable as light scattering agent generally can be described as have an appointment below 100 microns, preferably the inorganic spherical material of about 50 micron grain sizes of about 5-, for example spherical silica particles.
The total concentration of colorant can be the compositions gross weight about 0.1 to about 25% (weight), preferred about 1 to 10% (weight), definite concentration depends on to a certain extent for reaching the specific coloring material for mixing thing that required tone is chosen.Preferred compositions contains has an appointment 2% to the titanium dioxide of about 20% (weight) and 5% titanium dioxide to about 10% (weight) most preferably from about.
From the angle of humidification, dermal sensation, skin appearance and the emulsion compatibility, the preferred here colorant that uses is the colorant of handling.Colorant can be with for example lysine, type siloxane, lauroyl class, collagen protein, polyethylene, lecithin and ester oil are handled as aminoacid.Preferred colorant is the colorant that siloxanes (polysiloxanes) is handled.
In the preferred embodiment of the invention, water is present in the interior aqueous phase of two separations, and anti-acne active ingredient exists only in an aqueous phase.This is high and not have the stable compositions that the anti-acne active component is settled out solution be useful especially for water content is provided.
Compositions of the present invention also can contain crosslinked hydrophobic acrylate of a kind of graininess or methacrylate copolymer.This copolymer is used in particular for reducing light and the control oiliness helps to provide effective humidification benefit simultaneously.Crosslinked hydrophobic polymer is preferably copolymer point formation, and it has homodisperse and is trapped in the interior at least a active component of copolymer dot matrix.Alternative plan is that hydrophobic polymer can adopt porous particle shape, its surface area (N 2-BET) at about 50-500, preferred 100-300m 2/ g scope and absorption active component is within it arranged.
Hydrophobic polymer amount crosslinked during use is about 10% (weight) of about 0.1%-, and preferably described polymer is sneaked in the outer oil phase that contains polysiloxanes.One or more or its mixture in wetting agent, softening agent, humidizer and the sunscreen that active component can be the oil that is fit to skin, be fit to skin.Polymer masses is a powder shape, and described powder is particulate mixed system.The powder particle system forms dot matrix, and this dot matrix comprises that average diameter is less than the aggregation of about 1 micron unit grain, the fused unit grain of average diameter in about 20-100 micrometer range and the fused aggregation group of average diameter in about 200-1200 micrometer range gathering groups.
The powder material of the present invention that can be used as the carrier of active component can broadly be described as crosslinked " absorbing the back " hydrophobic polymer dot matrix.Preferably wrapped up and be dispersed with the active component of a kind of solid, liquid or gas form in this powder.Dot matrix is granular pattern and constitutes free-pouring dispersed solids granule when the carrying active material.This dot matrix can contain the active material of scheduled volume.The polymer architecture formula is as follows:
Figure A9519538600141
Wherein X is 80: 20 with the ratio of Y, and R ' is-CH 2CH 2-and R " be-(CH 2) 11CH 3
Hydrophobic polymer is highly cross-linked polymer, particularly highly cross-linked polymethacrylate copolymer.(USA) make and sell with trade mark POLYTRAP (RTM) by Midland, close supporting root by Dow Corning Corporation for this material.It is that a kind of ultralight free-flow white lead is last and this granule can absorb a large amount of lipophile liquids and some water seeking liquid keeps the free flowing powder characteristic simultaneously.Mealy structure is made up of the dot matrix less than 1 micron unit grain, and described unit grain is melt into the aggregation of 20-100 micron and this aggregation loosely and is clustered to and is of a size of about 1200 microns bulky grain of about 200-or gathering groups.This polymer powder can contain nearly its heavy 4 times liquid, emulsion, dispersion or fused solid.
Can utilize a rustless steel mixing container and a spoon to realize that active substance is adsorbed onto on the polymer powder, wherein active substance be added in the powder and active substance is called in the polymer powder lightly with spoon.Low viscous liquid can be by adding this liquid in the sealable container that fills this polymer and this material that rolls is absorbed till reaching evenly.Also can use more complicated mixing apparatus such as ribbon blender or double cone mixer.The preferred active component that is applicable to this is a glycerol.The weight ratio of wetting agent and carrier is about 1: 4 to about 3: 1.
Microsponges 5647 also is suitable as highly cross-linked polymethacrylate copolymer.It adopts and is generally spheric crosslinked hydrophobic polymer particle type, and its aperture is that about 0.05 μ m of 0.01-and surface area are 200-300m 2/ g.And it preferably is loaded with the wetting agent of above-mentioned amount.
Compositions of the present invention also can contain hydrophilic gellant, and described gelling dosage is preferably about 10%, the 0.02%-about 2% and in particular for 0.02%-about 0.5% more preferably from about of about 0.01%-.Gellant preferably has at least about 4000mPaS, more preferably at least about 10,000mPaS and particularly at least 50, the viscosity of 000mPaS (1% aqueous solution, 20 ℃, BrookfieldRVT).
The hydrophilic gelling agent that is fit to generally can be described as polymer water-soluble or that colloid is water-soluble, and comprises cellulose ether (for example hydroxyethyl-cellulose, methylcellulose, hydroxypropyl emthylcellulose), polyvinyl alcohol, polyquaternium-10, guar gum, hydroxypropyl guar gum and synthesising biological polymeric gel.
Other the gellant that is applicable to this is oily gellant, as trihydroxy stearin, hydroxy stearic acid magnalium.This gellant benefits the stability that provides excellent under room temperature and high temperature especially.
The compositions here can contain softening agent in addition.The softening agent that is fit to compositions of the present invention comprises natural and synthetic oils, and described grease separation is from mineral oil, vegetable oil and animal oil, fat and wax, fatty acid ester, aliphatic alcohol, aklylene glycol and polyalkylene glycol ethers and ester, fatty acid and composition thereof.
The softening agent that is applicable to this comprises the C that for example nonessential hydroxyl replaces 8-C 50Unsaturated fatty acid and ester thereof, C 8-C 30The C of satisfied fatty acid 1-C 24Ester such as isopropyl myristate; hexadecylic acid cetyl ester and dodecyl tetradecylic acid octyl group ester (Wickenol 142); Cera Flava; saturated and undersaturated aliphatic alcohol such as docosanol and hexadecanol; hydrocarbon such as mineral oil; oil and isotriacontane; fat Isosorbide Dinitrate (authorizing the United States Patent (USP) 3988255 of Seiden referring on October 26th, 1976); lanoline and lanolin derivative such as lanolin alcohol; ethoxylation; hydroxylated and acetylizad lanoline; cholesterol and derivant thereof, animal and plant triglyceride such as almond oil; Oleum Arachidis hypogaeae semen; wheat germ oil; Semen Lini oil; simmondsia oil; Apricot kernel oil; walnut oil; palm kernel oil; pistachio nut oil; Oleum sesami; rapeseed oil; cade oil; Semen Maydis oil; Semen Persicae oil; poppy seed oil; Oleum Pini; Oleum Ricini; Oleum Glycines; American Avocado Tree oil; safflower oil; Oleum Cocois; hazelnut oil; olive oil; Semen Vitis viniferae oil; C with sunflower seed oil and dimeric dibasic acid and trimer acid 1-C 24Ester such as dimeric dibasic acid diisopropyl ester, two different stearic malates, two different stearic dimeric dibasic acid esters and three different stearic trimerization acid esters.
Preferred softening agent is selected from hydro carbons such as 2-Methylpentadecane, mineral oil, vaseline and isotriacontane, lanolin alcohol and stearyl alcohol.These softening agents can use separately or use and the amount of about 1%-about 30% (weight) that can the compositions gross weight is present in the compositions of the present invention with form of mixtures, preferably with the amount existence of about 15% (weight) of about 5%-.
Compositions also can contain other material on demand, as spice, filler such as nylon, sunscreen, preservative agent, protein, antioxidant, chelating agen and water-in-oil emulsifier.
The another kind of nonessential composition of cosmetic composition is one or more ultraviolet absorbers.The ultraviolet absorber that often is called sunscreen can exist based on the concentration of about 12% (weight) of the about 1%-of compositions gross weight.Ultraviolet absorber preferably accounts for about 2%-8% (weight).Ultraviolet absorber more preferably can about 4%-about 6% (weight) concentration be present in the compositions.Be applicable in this ultraviolet absorber preferred especially, benzophenone-3, octyldimethyl PABA (Padimate O) and composition thereof.
Here a kind of nonessential still preferred composition is one or more other chelating agen.Chelating agen preferably is present in the compositions with the concentration based on the about 0.02%-of compositions gross weight about 0.10% (weight).Chelating agen preferably exists with the concentration based on about 0.07% (weight) of the about 0.03%-of compositions gross weight.Can be comprised in one of chelating agen in the compositions is tetrasodium ethylenediamine tetraacetate.
The another kind of nonessential still preferred composition of cosmetic composition is one or more preservative agents.Based on the compositions gross weight, preservative agent concentration is about 0.8% (weight) of about 0.05%-in the background color compositions, about 0.3% (weight) of preferably about 0.1%-.The preservative agent that is applicable to this comprises sodium benzoate and propyl parabene and composition thereof.
Cosmetic composition of the present invention can the humidification emulsifiable paste, lotion or gel and coloured composition such as painted humidizer, substrate material and the liquid form that hides material.
Following table is used to illustrate compositions of the present invention: example I II III IV V VI VII
Wt Wt Wt Wt Wt Wt Wt
％ ％ ％ ％ ％ ％ ％ A. 1.00 0.0 0.0 0.0 0.0 0.0 2.0 8.57 8.0 8.3 9.0 12.0 8.57 8.57 / ( 90∶10 ) 12.00 12.5 11.5 12.1 12.3 11.00 12.1 Laureth-7 0.75 0.75 0.0 0.75 0.0 0.75 0.75 ( 33％ ) 0.0 0.0 2.0 0.0 0.0 0.0 0.0 -3 0.0 0.0 0.0 0.0 0.0 2.0 0.0 / 0.0 0.0 0.0 4.0 0.0 5.0 0.0 3.0 0.0 3.0 0.0 4.0 0.0 0.0 B. ( ) 2.0 2.0 2.5 2.0 3.0 3.5 2.6 ( 、 ) 2.0 2.0 1.0 1.5 1.8 2.1 1.0 0.1 0.0 0.0 0.0 0.0 0.0 0.1 3.38 4.5 5.0 0.7 0.7 0.7 3.38 0.6 0.0 0.0 0.0 0.6 0.0 0.0 0.0 0.0 0.0 0.0 0.5 0.0 0.0 2.0 2.0 1.0 2.0 2.0 2.0 2.0 ( ) I II III IV V VI VII
Wt Wt Wt Wt Wt Wt Wt
% % % % % % % C. SILIBIONE OIL 70047 V20 0.5 0.5 0.5 0.5 0.5 0.5 0.5 D. iron oxide yellows 0.5 0.6 0.52 0.53 0.61 0.54 0.5 iron oxide reds 0.28 0.3 0.31 0.25 0.27 0.2 0.3 iron black 0.05 0.1 0.07 0.05 0.06 0.07 0.1 E. synthetic wax, 0.1 0.5 0.5 0.1 0.0 0.0 0.0 behenic acids, 20 esters, 0.3 0.0 0.0 0.3 0.5 0.3 0.3 stearic acid 0.0 0.0 0.0 0.0 0.0 0.0 2.5 palmitic acids, 0.0 0.0 0.0 0.0 0.0 2.5 0.0 silicas 0.1 0.0 0.1 0.0 0.1 0.0 0.1 (Spheron P1500) F. trihydroxy stearins, 0.3 0.3 0.5 0.6 0.0 0.0 0.0 SILIBIONE OIL 70047 V20s, 1.0 1.0 0.0 0.0 1.0 1.0 1.0 beeswaxs, 1.5 1.2 0.0 0.0 1.3 0.0 0.0 Abil WED9,0.0 3.0 0.0 0.0 0.0 0.0 0.0 example I II III IV V VI VII
Wt Wt Wt Wt Wt Wt Wt
％ ％ ％ ％ ％ ％ ％ G. 0.05 0.0 0.0 0.0 0.0 0.05 0.05 BHT 0.05 0.0 0.0 0.0 0.0 0.05 0.05 H. 7.55 7.6 7.7 7.65 7.6 7.4 7.63 4.0 5.5 4.0 8.0 4.5 5.0 4.0 1 1 1 2 2 2 0.0 0.0 0.0 0.0 0.0 0.0 0.0 5 6.0 5.0 6.5 7.00 8.0 6.0 5.0 ( Luviskol K17 ) 1 2 1.5 1 1 1 2 0.3 0.3 0.3 0.2 0.4 0.3 0.4 I. 12.0 12.2 11.5 11.8 12.0 12.1 12.2 0.2 0.2 0.2 0.2 0.1 0.2 0.1 EDTA 0.04 0.04 0.04 0.04 0.04 0.04 0.04 4 4 4 4 4 4 4 J -------------------100------------------- 0.2 0.3 0.2 0.3 0.3 0.3 0.4 ( Luviskol K17 ) 0.5 0.0 0.0 0.6 1.0 0.8 0.0 EDTA 0.06 0.06 0.06 0.06 0.06 0.06 0.06 6.0 6.0 6.0 6.0 6.0 6.0 6.0 0.1 0.0 0.1 0.2 0.0 0.0 0.0 K. 0.0 0.0 0.0 0.0 10.0 0.0 0.0 I II III IV V VI VII
Wt Wt Wt Wt Wt Wt Wt
% % % % % % %L. propane diols 0.0 0.0 0.0 2.0 0.0 0.0 0.0 xanthans 0.0 0.0 0.0 0.08 0.0 0.0 0.0M. essential oils 0.0 0.0 0.0 0.20 0.0 0.0 0.0 aromatic oil 0.0 0.25 0.0 0.20 0.0 0.0 0.0 Retinol Palmitates 0.0 0.05 0.0 0.0 0.0 0.0 0.0N. Aloe Vera Gels 0.0 0.0 3.0 0.0 0.0 0.0 0.0 chamomile extracts 0.0 0.0 0.1 0.0 0.0 0.0 0.0
*Contain about 1% propylene glycol
Each listed in table composition has divided in groups, and composition of each group mixes before in the composition that joins all the other groups according to the step that proposes below.
The first step, with phase A mixture of ingredients shear-mixed stir about 5 minutes to evenly.Under high speed shear is mixed, the material of phase B is added among the A gradually, and mix 20 minutes to dispersity.
Phase C is slowly added in the mixture of phase A and B with subsequently the composition of D mutually, and high shear mixing is to dispersity simultaneously.Add Silicon stone and it is distributed in the mixture this moment.
Before adding phase E component, the gained batch of material is heated to 90 ℃.Container is cooled to 55 ℃, and adds pre-mixed phase F.Batch mixture is until evenly.Mixture is cooled to 30 ℃ and add phase G.
Be prepared as follows phase H: at first the polyvinyl pyrrolidone complexant is dissolved in alcoholic solvent, dissolves anti-acne active ingredient then, dissolve all the other components subsequently, add the solution of citric acid or salt at last.Then phase I is added phase H, and the gained mixture is added to oil phase.Phase J with premix also is added to oil phase then.
At last, add phase K, L, M and N as diluent.
Resulting composition is prepared packing.
The compositions of embodiment has embodied humidification effect, anti-acne activity, function of anti-skin aging and has improved prescription and color stability, skin feel and outward appearance.

Claims (26)

1. anti-acne cosmetic composition with heterogeneous water-in-oil emulsion form, wherein said composition comprises:
(a) two or more waters; With
(b) prevent the anti-coalescent that water is coalescent; Wherein at least the first water comprises the anti-acne active ingredient with water/alcoholic solution form.
2. according to the anti-acne cosmetic composition of claim 1, wherein anti-coalescent is electrolyte or electrolytical mixture.
3. according to the anti-acne cosmetic composition of claim 2, wherein electrolyte is a sodium chloride.
4. according to each anti-acne cosmetic composition of claim 1 to 3, wherein the content of anti-coalescent is about 0.05% to about 5% of composition weight.
5. according to each anti-acne cosmetic composition of claim 1 to 4, wherein the content of anti-coalescent is about 0.01% to about 1% of composition weight.
6. according to each anti-acne cosmetic composition of claim 1 to 5, wherein first water contains 20% the water that is no more than composition weight.
7. according to each anti-acne cosmetic composition of claim 1 to 6, wherein second water contains about 15% water of composition weight at least.
8. according to each anti-acne cosmetic composition of claim 1 to 7, it comprises about 30% Total Water to about 50% weight, with about 1% alcoholic solvent to about 15% weight, wherein the amount of the anti-acne active ingredient that comprises of compositions has surpassed the dissolubility of this active component in the equivalent mixture of water and alcohol.
9. according to each anti-acne cosmetic composition of claim 1 to 8, wherein anti-acne active ingredient is selected from salicylic acid, tretinoin, Azelaic Acid, lactic acid, glycolic, acetone acid, flavonoid and its derivant and composition thereof.
10. according to each anti-acne cosmetic composition of claim 1 to 9, comprise about 0.1% anti-acne active ingredient to about 10% weight.
11., comprise about 1% the silicone oil that is selected from Y 7175, non-volatile polysiloxanes and its mixture to about 50% weight according to each anti-acne cosmetic composition of claim 1 to 10.
12. according to the anti-acne cosmetic composition of claim 11, viscosity was less than poly-organopolysiloxane of linearity of about 5 centistokes and composition thereof when viscosity was less than the poly-organopolysiloxane of the ring-type of about 10 centistokes and 25 ℃ when wherein volatile silicone oils was selected from 25 ℃.
13. according to the anti-acne cosmetic composition of claim 12, wherein volatile silicone oils is selected from and contains about 3 to about 9 silicon atoms, preferred about 4 to the annular dimethyl polysiloxane of about 5 silicon atoms with contain the about 3 line style polydimethylsiloxane to about 9 silicon atoms.
14. according to the anti-acne cosmetic composition of claim 13, wherein non-volatile silicone oil comprises and contains at least one poly-diorganosiloxane fragment and the segmental poly-diorganosiloxane-polyoxyalkylene copolymers of at least one polyoxyalkylene.
15. according to the anti-acne cosmetic composition of claim 14, wherein poly-diorganosiloxane-polyoxyalkylene copolymers is the dimethicone polyol.
16., comprise about 0.1% wetting agent in addition to about 30% weight according to each anti-acne cosmetic composition of claim 1 to 15.
17. according to the anti-acne cosmetic composition of claim 16, wherein wetting agent is a glycerol.
18., comprise about 0.01% to the colorant of about 10% weight or mix colorant according to each anti-acne cosmetic composition of claim 1 to 17.
19. according to each anti-acne cosmetic composition of claim 1 to 18, wherein anti-acne active ingredient is a salicylic acid.
20., comprise about 0.1% polyvinyl pyrrolidone complexant in addition to about 10% weight according to each anti-acne cosmetic composition of claim 1 to 19.
21., comprise about 0.01% citric acid or its salt in addition to about 5% weight according to each anti-acne cosmetic composition of claim 1 to 20.
22. according to the anti-acne cosmetic composition of claim 21, wherein silicone oil comprise composition weight about 2% to about 25%, preferred about 5% to about 15% non-volatile polysiloxanes.
23. according to each anti-acne cosmetic composition of claim 1 to 22, comprise about 1% softening agent in addition to about 15% weight, it is natural or artificial oil, be selected from mineral oil, vegetable oil and animal oil, fat and waxiness, fatty acid ester, aliphatic alcohol, aklylene glycol and polyalkylene glycol ethers and ester, fatty acid and composition thereof.
24. according to the anti-acne cosmetic composition of claim 23, wherein softening agent is selected from isopropyl palmitate, isostearic acid isopropyl ester, di-2-ethylhexyl maleate, two sad propylene glycol ester/didecyl acid propylene glycol esters, Trivent OCG/tricaprin, isotriacontane, mineral oil, the different pelargonate of cetearyl and lanolin alcohol and composition thereof.
25. according to each anti-acne cosmetic composition of claim 1 to 24, wherein the pH value of the water/alcoholic solution of anti-acne active ingredient is about 1 to about 7, preferred about 2 to about 5, more preferably from about 2 to about 4.
26., may further comprise the steps according to each the preparation method of anti-acne cosmetic composition of claim 1 to 25:
(a) with anti-acne active ingredient water-soluble/alcoholic solution prepares first water;
(b) first water is mixed with oil phase; With
(c) subsequently one or more other waters are added to the gained mixture forming heterogeneous water-in-oil emulsion, first and/or other aqueous phase be dissolved with anti-coalescent.
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