WO2021102874A1 - Composition d'écran solaire huile dans l'eau - Google Patents
Composition d'écran solaire huile dans l'eau Download PDFInfo
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- WO2021102874A1 WO2021102874A1 PCT/CN2019/121808 CN2019121808W WO2021102874A1 WO 2021102874 A1 WO2021102874 A1 WO 2021102874A1 CN 2019121808 W CN2019121808 W CN 2019121808W WO 2021102874 A1 WO2021102874 A1 WO 2021102874A1
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
- A61K2800/41—Particular ingredients further characterized by their size
- A61K2800/413—Nanosized, i.e. having sizes below 100 nm
Definitions
- the present invention describes an improved oil-in-water (O/W) sunscreen composition containing at least one organic UV filter and titan dioxide (nano) .
- UVA and UVB filters are summarized in most industrialized countries in the form of positive lists such as for instance Annex 7 of the German Cosmetics Regulation.
- the effect of UV filters in a cosmetic preparation has to be determined; in general the sun protection factor (SPF) is used to characterize the sun protection potential of a cosmetic composition intended for the use as a sunscreen means.
- the sun protection factor (SPF) indicates the increased time of exposure to the sun's rays made possible through use of the sunscreen composition. It is the ratio of the erythema threshold time with sunscreen composition to erythema threshold time without sunscreen composition.
- a cosmetic composition may be characterized by SPF values of 20 -50.
- SPF values 20 -50.
- a high amount of UV filters especially organic UV filters, has to be used in said compositions.
- High amounts of UV filters worsen the cosmetic properties of a composition, which may become highly viscous, sometimes even pasty-like. After usage of such a composition the skin feeling is described as greasy and oily. Also, skin irritations have been observed after the application of sun screen compositions containing high amounts of organic UV filters.
- high amounts of UV filters make sunscreen compositions more and more expensive. And finally, there are restrictions in relation to the amount and kind of UV filters depending on different countries.
- SPF booster means a compound or composition that increases the SPF of a given preparation when used together with a UV filter. Frequently, the compound or composition being effective as a SPF booster does not function as an UV filter itself or only to a negligible extent.
- SPF booster to increase the SPF of a given sunscreen composition is already disclosed in prior art.
- a great variety of substances and mixtures of substances have been described to be effective as SPF booster, only a few will be mentioned below.
- SPF boosters namely diesters of carboxylic acids and alcohols having 2 to 10 carbon atoms; 2-propyl heptyloctanoate; sodium acrylate homopolymers, having an average molecular weight of 2,500,000 to 3,500,000 Dalton and the 1 %by weight solution of said sodium acrylate homopolymers having a pH value of 5.5 to 7.5; silica particles not being modified or coated and having an average by number diameter of 2 to 15 ⁇ m.
- SPF boosters namely VitisVinifera Seed Oil; trimethylsiloxysilicate; talc; stearoxytrimethylsilane + stearyl alcohol; sodium polystyrene sulfonate; sodium hyaluronate; polysorbate 65; polysorbate 40; polymethylsilsesquioxane; phenethyl benzoate; Ginkgo Biloba extract; OenotheraBiennis Oil; octadecenedioic acid; methyl palmitate; GlycyrrhizaInflata Root Extract; Glycine Soja (isoflavone) ; ArctiumLappa Extract; diethylhexyl 2, 6-naphthalate; ceramide 3; caprylic/capricglycerides; Di-C12-13 alkyl tartrate.
- SPF boosters are disclosed, which are selected from hollow particles.
- Polymers and copolymers of (meth) acrylic acid, (meth) acrylates, and/or styrene; glass; silica are the materials, said particles are made therefrom.
- the hollow latex particles may be constituted of a copolymer of styrene and (meth) acrylic acid or one of its alkyl esters, known under the INCI name Styrene/Acrylates Copolymer, which may be purchased under the trade name Sunspheres TM Powder by the company Rohm &Haas.
- a SPF booster is described, which is composed of a particulate material that is virtually insoluble and a water-soluble or water-dispersible, interfacially-active polymer.
- the interfacially-active polymer may be chosen from lignosulfonate, lignin, oxylignin, alkali metal salts of humic acid, alkali metal salts of tannic acid, proteins, hydrophobically-modified water-soluble or water-dispersible polymers, and water-soluble or water-dispersible, amphiphilic copolymers.
- the particulate materials may be chosen from titanium dioxide, zinc oxide, alumina, cerium oxide, silica, bentonite, talc, aluminum hydroxide, calcium sulfate, and polymeric latex particles.
- a commercially available mixture of said SPF booster is sold under the trade name UV from AMCOL International Corporation.
- UV filters are quite expensive and by reducing the amount of UV filters the costs of a product may be decreased.
- TiO 2 having a primary particle size between 10 and 100 nm, could bring about improvements in sun screen compositions.
- Said TiO 2 is also called titan dioxide (nano) .
- the INCI name of titan dioxide particles having a primary particle size of 1 to 100 nm is titan dioxide (nano) .
- titan dioxide is described as a micro pigment, wherein the UV protection is achieved by physical effects, namely the reflection and scattering of UV light. This dual effect may also be described by UV shielding and SPF boosting in one molecule.
- titan dioxide nano
- US 2013/0266621 A1 and CN 106983671 A are already disclosed, e.g. in US 2013/0266621 A1 and CN 106983671 A.
- the sunscreen composition comprises an aqueous phase, the total amount of water ranges from 45 to 95 %by weight, preferably 60 to 85 %by weight, in relation to the total weight of the composition.
- isoamyl laurate is contained in the sunscreen composition. Especially isoamyl laurate is proved to be an advantageous solvent for the one or more UV filter (s) .
- Isoamyl laurate may be purchased as Mackaderm LIA from Solvay or Dermofeel Sensolv from Evonik Dr. Straetmans.
- isoamyl laurate is contained in an amount of 0.1 to 5.0 %by weight, preferably 0.5 to 3.0 %by weight, in relation to the total weight of the composition.
- the sunscreen composition of the present invention contains at least one organic UV filter; however to provide a composition having a sufficient and broad photo protective potential, advantageously a combination of organic UV filters is present, which absorb sun rays in a range of about 280 to about 400 nm. This may be achieved by a suitable combination of so called UV A and UV B filters or by using broadband filters or combinations thereof.
- the sun screen composition according to the present invention contains at least one organic UV B filter, said filter may be an oil-soluble or water-soluble one.
- suitable oil-soluble organic UV B filters are:
- suitable water-soluble organic UV B filters are:
- the sun screen composition according to the present invention contains at least one organic UV A filter, said filter may be chosen from
- the at least one organic UV filter is contained in a total amount of 1.0 to 35.0 %by weight, preferably 2.0 to 30.0 %by weight, in relation to the total weight of the composition.
- titan dioxide is contained in the composition of the present invention, which may be purchased from Tayca as MT-500B or MT-700B or from Brenntag as Kronos 1171.
- the particle size of titan dioxide is in the range of 15 to 100 nm, preferably 30 to 80 nm.
- the particle size may be determined by sedimentation, especially photo sedimentation, sieve analysis, light microscopy or laser diffraction analysis.
- the titan dioxide particles are uncoated.
- further inorganic pigments based on metal oxides, which are insoluble or sparingly soluble in water are contained in the composition of the present invention, it is preferred that said pigments are uncoated, too. It is most preferred, if, in relation to titan dioxide, only uncoated titan dioxide (nano) and no further inorganic pigments based on metal oxides, which are insoluble or sparingly soluble in water, are contained in the composition of the present invention.
- Titan dioxide (nano) is contained in an amount of 0.1 to 10 %by weight, preferably 0.2 to 5 %by weight, in relation to the total weight of the composition.
- the sunscreen composition contains the UV filters Butyl Methoxydibenzoylmethane, Ethylhexyl Salicylate, Octocrylene, 3, 3, 5-Trimethylcyclohexyl salicylate, and Phenylbenzimidazole Sulfonic Acid.
- UV filters Butyl Methoxydibenzoylmethane, Ethylhexyl Salicylate, 3, 3, 5-Trimethylcyclohexyl salicylate, and Phenylbenzimidazole Sulfonic Acid are contained.
- UV B filters Octocrylene and/or 2-hydroxy-4-methoxybenzophenone are not contained in the composition of the invention.
- the sunscreen composition of the present invention contains at least one film-former.
- Film-formers are added to skin care compositions in order to contribute to build a film on the skin after the evaporation of the solvent; the film helps to prevent transepidermal water loss and/or maintain a good barrier for ultraviolet radiation protection.
- the film on the skin shall also support the water resistance of the product.
- an oil soluble film-former is used.
- the oil soluble film-former may be selected from PEG-240/HDI Copolymer Bis-Decyltetradeceth-20 Ether, Vinyl Pyrolidone/Triacontene Copolymer, Acrylates/OctylacrylamideCopolymer, Acrylates Copolymer, Hydroxyesters Acrylates Copolymer, Dimethicone + Dimethicone Crosspolymer, VP/Hexadecene Copolymer. It is preferred, if at least one dimethicone crosspolymer is contained in the composition of the present invention.
- silicones are synthetic polymers containing silicium atoms connected via oxygen atoms.
- the functional unit consisting of silicium atom and oxygen atom is called siloxane.
- Dimethicones many siloxane units are arranged in a linear way, each silicium atom having two methyl residues and the silicium atoms at the ends having three methyl residues. Dimethicones are varying in length. The differing length accounts for differing viscosity values. Therefore dimethicones can be characterized by these values. Dimethicones, or silicone fluids, as they are also called, may be purchased having varying values of viscosity.
- Viscosity values between 1 centistokes (cst) and 1,000,000 cst.
- the lower viscosity products are miscible for example with mineral oil and isopropyl myristate and are useful for aerosol applications.
- the dimethicone products having 100 –500 cst are the traditional silicones used as additives in skin care formulations and products characterized by higher viscosities are used in barrier products or in hair products.
- the viscosity values are referring to those values which are given by the suppliers of the respective silicone components to characterize these components.
- the viscosity values may be determined according to CTM 0004 (Dow Corning) or DIN 53019 (Wacker) .
- dimethicone crosspolymers are generated.
- Said crosspolymers are silicone elastomers being characterized by a network.
- Dimethicone crosspolymers may be effective as rheology modifiers in O/W-and W/O-emulsions and influence the texture of the compositions they are contained in.
- dimethicone crosspolymers are effective as film-formers, helping to build a film on the skin ensuring an even distribution of UV filters contained in said film.
- the one or more dimethicone crosspolymer (s) is contained in a total amount of 1.0 to 10.0 %by weight, preferably 3.0 to 5.0 %by weight, in relation to the active content of the dimethicone crosspolymers and in relation to the total weight of the composition.
- Dimethicone crosspolymers are available as combinations with cyclopentasiloxane or low viscosity dimethicone, which may be volatile or non-volatile.
- a preferred dimethicone crosspolymer is a blend of dimethicone and dimethicone crosspolymer, available as Dowsil 9041 Silicon Elastomer Blend from Dow Corning. According to the invention it is preferred, if the blend of dimethicone and dimethicone crosspolymer is contained in a total amount of 1.0 to 10 %by weight, preferably 3.0 to 5.0 %by weight, in relation to the total weight of the composition.
- a natural film former may be contained; a preferred example of such a film former is Capryloyl Glycerin/Sebacic Acid Copolymer, which may be purchased from Inolex under trade name LexFilm Sun Natural.
- emulsions are heterogeneous systems, which consist of two liquids which are immiscible or have only limited miscibility with one another and which are usually referred to as phases.
- one of the two liquids is dispersed in the form of very fine droplets in the other liquid.
- the liquids pure or as solutions
- O/W emulsion oil-in-water emulsion
- the basic character of an O/W emulsion exemplified by electrical conductivity, sensory properties, ability of the continuous phase to be stained, is determined by the water.
- W/O emulsion water-in-oil emulsion, e.g. butter
- the basic character is determined by the oil.
- one or more emulsifier (s) is/are contained in general.
- Emulsifiers help to combine two immiscible liquids (for example oil in water) in a way to result in a stable preparation, an emulsion. For that reason emulsifiers have to have an amphiphilic character, the hydrophobic part interacts with the oily or lipid phase and the hydrophilic part interacts with the aqueous phase. By stirring or homogenizing the generated droplets are dispersed in the respective environment, namely aqueous droplets in a lipid environment or lipid droplets in an aqueous environment. Primarily, emulsifiers do not have a detersive, surfactant character.
- Emulsifiers reduce the interfacial tension between the two phases and, besides reducing the interfacial work, also achieve a stabilization of the emulsion formed. They stabilize the formed emulsion by means of interfacial films, as well as by forming steric or electrical barriers, as a result of which the merging (coalescence) of the emulsified particles is prevented.
- HLB values are suitable to characterize emulsifiers, said values specify the hydrophilicity of a given emulsifier.
- the HLB value may be determined by the following formula:
- HLB 20 ⁇ (1-M lipophile /M)
- M lipophile represents the molar mass of the lipophilic fraction of a given emulsifier and M represents the molar mass of the total emulsifier.
- emulsifiers with an HLB value up to about 8 are considered to be W/O-emulsifiers.
- O/W-emulsifiers have HLB values greater than 8.
- the sunscreen composition of the present invention contains at least one O/W-emulsifier.
- the at least one O/W emulsifier may be chosen from Ceteareth-12, ceteareth-20, ceteareth-25, ceteareth-3, ceteth-10, ceteth-2, ceteth-20, cetyl phosphate, cetylstearyl alcohol in combination with PEG-20 stearate, glyceryl stearate citrate, glyceryl stearate in combination with PEG-100 stearate, glyceryl stearate in combination with PEG-30 stearate, glyceryl stearate SE, isosteareth-10, isosteareth-20, isostearyldiglyceryl succinate, laureth-23, laureth-4 phosphate, laureth-4, methyl glucose sesquistearate, PEG-100 stearate, PEG-20 glyceryl stearate, PEG-20 stearate, PEG-20 methyl glucose sesquistearate, PEG-30 stearate, PEG-40 stea
- sodium stearoyl glutamate is contained in the composition according to the present invention.
- the at least one O/W emulsifier is contained in a total amount of 0.2 to 1.2 %by weight, preferably 0.3 to 0.9 %by weight, in relation to the total weight of the composition.
- the sunscreen composition comprises an oily phase, which may contain the oil soluble film-former, isoamyl laurate and oil-soluble UV filters.
- the oily phase is present in an amount of 6.5 to 55 %by weight, more preferably 7.0 to 45 %by weight, in relation to the total weight of the composition.
- the composition may additionally contain at least one thickener in order to adjust the viscosity, especially of the aqueous phase.
- at least one thickener are:
- - organic, natural compounds such as, for example, agar agar, carrageen, tragacanth, gum arabic, alginates, pectins, polyoses, guar gum, carob bean flower, starch, dextrins, gelatins, casein,
- inorganic compounds such as, for example, polysilicic acids, clay minerals, such as montmorillonites, zeolites, silicas.
- xanthan (CAS No. 11138-66-2) , also called xanthan gum may be contained.
- Xanthan gum is an anionic heteropolysaccharide, which is generally formed by fermentation from maize sugar and is isolated as the potassium salt. It is produced by Xanthomonas campestris and some other species under aerobic conditions with a molecular weight of 2 ⁇ 10 6 to 24 ⁇ 10 6 .
- Xanthan is formed from a chain having ⁇ -1, 4-bonded glucose (cellulose) with side chains.
- the structure of the subgroups ( "repeat units” ) consists of glucose, mannose, glucuronic acid, acetate and pyruvate.
- Xanthan gum may be purchased from CP Kelcounder the trade name Keltrol CG-F. If xanthan gum is contained in the composition of the present invention, xanthan gum is contained in an amount of 0.05 to 5 %by weight, preferably 0.1 to 3.0 %by weight, in relation to the total weight of the composition.
- acrylate-based thickeners may be contained in the composition of the present invention.
- These acrylate-based thickeners may be polymers of acrylic acid, in particular those chosen from the group of carbomers or Carbopols ( is actually a registered trade mark of the Lubrizol Company) .
- Carbopols are compounds of the general structural formula
- Carbopols also includes acrylate-alkyl acrylate copolymers, for example those characterized by the following structure:
- R' is an alkyl radical
- x and y are numbers which symbolize the respective stoichiometric content of each comonomer.
- composition of the present invention may contain copolymers, having a comparable structure as the acrylate-alkyl acrylate copolymers, but R’ being an alkyl radical having 10 to 30 carbon atoms.
- Said copolymers comprise one or more monomers of acrylic acid, of methacrylic acid and one or more C10-30 alkyl acrylates monomers.
- the INCl name of such compounds is "Acrylates/C 10-30 Alkyl Acrylate Crosspolymer" .
- Particularly advantageous are those available under the trade names Pemulen TR1, Pemulen TR2 and Pemulen EZ-4U polymeric emulsifier from Lubrizol.
- the at least one Acrylates/C10-30 Alkyl Acrylate Crosspolymer is contained in the composition of the present invention, the at least one Acrylates/C10-30 Alkyl Acrylate Crosspolymer is contained in an amount of 0.1 to 1.5 %by weight, preferably 0.15 to 0.4 %by weight, in relation to the total weight of the composition.
- the thickeners xanthan gum and/or Acrylates/C10-30 Alkyl Acrylate Crosspolymer are contained in the composition of the present invention.
- the composition may additionally contain at least one moisturizer.
- moisturizers refer to substances or substance mixtures that give cosmetic preparations the property that, after application and distribution on the skin surface, the release of moisture from the corneal layer of the epidermis (also referred to as transepidermal water loss (TEWL) ) is reduced and/or the hydration of the corneal layer is positively influenced.
- TEWL transepidermal water loss
- the at least one moistuizer is contained in an amount of 1.0 to 10.0 %by weight, preferably 2.0 to 5.0 %by weight, in relation to the total weight of the composition.
- the composition may additionally contain at least one preservative. All preservatives, which are allowed and suitable for cosmetic compositions may be contained. However, it is preferred, if methylparaben, ethylparaben, and Phenoxyethanol, or mixtures thereof, more preferably Phenoxyethanol are contained. Other preservatives may also be used, for example Benzyl Alcohol. These preservatives may be used alone or in combination or in combination with the above mentioned preferred preservatives.
- the at least one preservative is preferably contained in a total amount of 0.1 to 0.9 %by weight, more preferably 0.4 to 0.8 %by weight, relative to the total weight of the composition.
- the values are referring to the active content of the preservatives.
- the composition may additionally contain cosmetic auxiliaries, which are usually used in such compositions, e.g. preservative aids, complexing agents, electrolytes, perfumes, pigments which have a coloring action, fats, further oils, waxes or other common constituents of a cosmetic composition.
- cosmetic auxiliaries which are usually used in such compositions, e.g. preservative aids, complexing agents, electrolytes, perfumes, pigments which have a coloring action, fats, further oils, waxes or other common constituents of a cosmetic composition.
- the pH value of the composition according to the present invention may be adjusted by all means suitable for cosmetic compositions. However, it is preferred, if suitable amounts of inorganic base, e.g. sodium hydroxide, are contained to adjust the pH value to a value from 7.0 to 7.8, more preferably 7.2 to 7.8.
- inorganic base e.g. sodium hydroxide
- the composition according to the invention preferably has a viscosity of 2900 to 4000 mPa ⁇ s, more preferably 2900 to 3900 mPa ⁇ s.
- the viscosity is determined by using a Rheomat R123 at 25°C.
- composition of the present invention may be prepared by any technique known or effective to prepare an O/W-emulsion.
- the process to prepare the composition of the present invention comprises conventional formulating and mixing techniques. However, it is preferred, if the composition according to the present invention is prepared by the following method:
- Test areas on subjects’ backs are coated with test product. Between product application and irradiation a waiting time of 15 minutes is realized. Irradiation is carried out by 6 different doses. The resultant erythema is used to ascertain the minimum erythema dose (MED) .
- the individual Sun Protection Factor (SPF) is determined from the ratio of MEDU (MED of untreated skin) and MED (MED of protected skin) of the area treated with the product in question.
- the SPF result is expressed as the arithmetical mean of the individual SPF values obtained from the total number of subjects used.
- isoamyl laurate at least one film-former, preferably a dimethicone crosspolymer, and titan dioxide (nano)
- a sunscreen composition having a reduced amount of UV filter (s) and at the same time reaching an SPF significantly greater than 50.
- Isoamyl laurate supports the solubility of the UV filter (s) , especially oil-soluble one (s)
- the film-former helps to build a film on the skin, and thereby distributing the oil droplets and the UV filters evenly on the skin. Because of the lipophilic character of said components the resulting film gets water resistant.
- the components isoamyl laurate, UV filter (s) , film-former, and titan dioxide (nano) are interacting and supporting each other in such a way that a well-balanced sunscreen composition results, having a reduced amount of UV filter (s) and reaching high SPF values.
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Abstract
L'invention concerne une composition d'écran solaire sous forme d'une émulsion H/E qui contient au moins un filtre UV organique et du dioxyde de titane (nano), ayant une quantité réduite de filtre(s) UV et un SPF supérieur à 50.
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CN117503626A (zh) * | 2023-11-09 | 2024-02-06 | 植物医生(广东)生物科技有限公司 | 植物来源的防晒增效组合物、防晒产品、制备方法和应用 |
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WO2010093573A2 (fr) * | 2009-02-11 | 2010-08-19 | Amcol International Corporation | Compositions d'écrans solaires comprenant des agents actifs écrans solaires particulaires qui présentent un renforcement du facteur de protection solaire |
US8815218B2 (en) * | 2009-04-20 | 2014-08-26 | Dr. Straetmans Gmbh | Cosmetic or dermatological preparation |
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CN117503626B (zh) * | 2023-11-09 | 2024-04-16 | 植物医生(广东)生物科技有限公司 | 植物来源的防晒增效组合物、防晒产品、制备方法和应用 |
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