Non-greasy sunscreen composition
A sunscreen composition combining fine zinc oxide and specific UV filters addresses the issues of stickiness and solubility, providing high SPF protection while minimizing sand adhesion and ensuring stable UV filter solubility.
Patent Information
- Application Number
- JP2022523313
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- Priority Date
- 2019-11-05
- Filing Date
- 2020-11-03
- Publication Date
- 2025-06-09
- Estimated Expiration
- 2040-11-03
AI Technical Summary
Modern sunscreens face challenges with stickiness, leading to sand adhesion on the skin, and solubility issues with high UV filter content, particularly with triazine derivatives, which can result in insufficient protection when users apply less product to avoid stickiness.
A topical sunscreen composition combining fine zinc oxide with specific surface coatings, along with the UV filters 2,4-bis{[4-(2-ethylhexyloxy)-2-hydroxy]phenyl}-6-(4-methoxyphenyl)-1,3,5-triazine, 2-phenylbenzimidazole-5-sulfonic acid, and 2,4,6-tris[anilino(p-carbo-2'-ethyl-1'-hexyloxy)]-1,3,5-triazine, to provide high sun protection factor (SPF 20 or higher) while minimizing sand adhesion and ensuring stable solubility of UV filters.
The composition effectively reduces sand adhesion to the skin and ensures stable solubility of UV filters, providing high SPF protection without the drawbacks of stickiness and solubility issues in existing sunscreens.
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Abstract
Description
Detailed Description of the Invention
[0001] The present invention relates to a topical preparation comprising a combination of UV filters of a specific zinc oxide, 2,4-bis{[4-(2-ethylhexyloxy)-2-hydroxy]phenyl}-6-(4-methoxyphenyl)-1,3,5-triazine (INCI: bisethylhexyloxyphenol methoxyphenyl triazine), 2-phenylbenzimidazole-5-sulfonic acid and / or one or more salts thereof, and 2,4,6-tris[anilino(p-carbo-2'-ethyl-1'-hexyloxy)]-1,3,5-triazine (INCI: ethylhexyl triazone).
[0002] It is well known that ultraviolet (UV) rays in sunlight have an effect of damaging the skin. In addition to well-known acute damage (sunburn), there are also long-term damages such as an increased risk of developing skin cancer. Furthermore, exposure to ultraviolet rays is involved in most of the wrinkles and spots on people's faces. Therefore, in order to protect the skin from the harmful effects of ultraviolet rays, various photoprotective UV filter substances that can be incorporated into topical sunscreen preparations have been developed.
[0003] Modern sunscreens need to effectively and safely protect the skin from the harmful effects of ultraviolet rays. Therefore, generally, sunscreens contain various UV-B (wavelength: 280 - 320 nm) and UV-A (wavelength: 320 - 400 nm) filters. However, these filters often make the sunscreen sticky, which means that sand adheres to the skin where the cream is applied, especially when used at the beach. The higher the UV filter content of the preparation, the more serious this problem becomes. To address the stickiness problem, consumers tend to reduce the amount of sunscreen used, which leads to insufficient protection.
[0004] Even if attempts have been made to develop sunscreen compositions with reduced greasiness, this problem has not yet led to a fully satisfactory solution, particularly with regard to formulations characterized by a particularly high sun protection factor.
[0005] Therefore, there is still a need to develop new sunscreen formulations with reduced greasiness.
[0006] Therefore, it would be advantageous if a sunscreen composition having anti-sand adhesion property, more particularly a sunscreen composition having a high sun protection factor (SPF 20 or higher) and particularly low sand adhesion property, were available.
[0007] In addition to greasiness / sand adhesion, a further problem with cosmetic sunscreen compositions is that when the amount of UV filter is made very high, it does not exhibit particularly good solubility in the formulation. In particular, when attempting to develop formulations with a high sun protection factor and a high UV filter content, developers face the problem of the solubility of triazine derivatives. To date, to solve this problem, octocrylene, a liquid UV-B filter, has been used as a UV filter and a solvent.
[0008] The drawback of the prior art in that case is that octocrylene, despite being approved by the approval authorities, is not in a situation where there is no room for discussion regarding its use, and it receives a "bad rating" in the product scoring based on the evaluation of certain consumer magazines (e.g., the German Oko-test). The reason for this bad evaluation is that certain scientists have doubts that this UV filter may have a hormone-like effect. Even though sunscreen compositions containing this UV filter have been used worldwide for decades and it has been shown that there is no adverse effect on the human body, there is still a desire among consumers to avoid formulations containing this type of ingredient.
[0009] Therefore, it is desirable to develop a sunscreen composition having anti-sand adhesion properties that overcomes the drawbacks of the prior art, has a high UV protection index, and in which organic UV filters such as triazine derivatives are stably dissolved. Ideally, this should be achievable without using octocrylene as a solvent and stabilizer.
[0010] Therefore, the present invention provides a topical sunscreen composition. This topical composition a.) fine zinc oxide, preferably having an average particle size Dn50 selected in the range of 30 to 200 nm, as determined by laser diffraction, and a surface coating selected from the group consisting of triethoxycaprylylsilane, octyltrimethoxysilane, and dimethicone; b.) 2,4-bis{[4-(2-ethylhexyloxy)-2-hydroxy]phenyl}-6-(4-methoxyphenyl)-1,3,5-triazine (INCI: bisethylhexyloxyphenol methoxyphenyltriazine); c.) 2-phenylbenzimidazole-5-sulfonic acid and / or one or more salts thereof; d.) at least one of 2,4,6-tris[anilino(p-carbo-2'-ethyl-1'-hexyloxy)]-1,3,5-triazine (INCI: ethylhexyltriazone) and comprises a combination of UV filters.
[0011] The term fine zinc oxide refers to any zinc oxide particles suitable for use as a UV filter, i.e., zinc oxide having a particle size that is basically useful for incorporation into a sunscreen composition. Advantageously, the fine zinc oxide consists of particles having a primary particle size of less than about 300 nm, such as less than about 200 nm or less than about 150 nm. Most preferably, in all embodiments of the present invention, the average particle size of the fine zinc oxide according to the present invention is selected in the range of 30 to 200 nm, more preferably in the range of 75 to 150 nm, and most preferably in the range of 90 to 130 nm. Even more preferred ranges include 30 nm to 150 nm and 30 nm to 130 nm.
[0012] As used herein, the term "average particle diameter" refers to the median diameter Dn50 (also known as Dn0.5) of a number-based particle size distribution determined by laser diffraction using, for example, a Horiba particle size distribution analyzer LA-960 or a Malvern Mastersizer 2000 (ISO 13320:2009).
[0013] The zinc oxide according to the present invention preferably further has a Dn1 > 20 nm (1% is below this diameter).
[0014] According to the present invention, it is also advantageous that the zinc oxide particles are surface-coated. The surface coating may include providing a thin hydrophilic or hydrophobic inorganic or organic layer on the metal oxide particles by methods known per se. According to the present invention, various surface coatings may also include water. By performing a surface treatment, hydrophilic, amphiphilic or hydrophobic properties are imparted to the metal oxide.
[0015] Examples of inorganic surface coatings suitable for the purposes of the present invention include, for example, aluminum oxide (Al 2 O 3 ), aluminum hydroxide Al(OH) 3 , aluminum oxide hydrate (alias: alumina, CAS number: 1333-84-2), sodium hexametaphosphate (NaPO 3 ), 6 sodium metaphosphate (NaPO 3 ), n silicon dioxide (SiO 2 ) (alias: silica, CAS number: 7631-86-9) and iron oxide (Fe 2 O 3 ). These inorganic surface coatings may be present alone, in combination and / or in combination with organic coating materials.
[0016] Examples of organic surface coatings suitable for use in the present invention include aluminum stearate of vegetable or animal origin, stearic acid of vegetable or animal origin, lauric acid, dimethylpolysiloxane (also known as dimethicone), methylpolysiloxane (methicone), simethicone (a mixture of dimethylpolysiloxane with an average chain length of about 200 to about 350 dimethylsiloxane units and silica gel), triethoxycaprylylsilane, and octyltrimethoxysilane. These organic surface coatings can exist alone, in combination, and / or in combination with inorganic coating materials. Preferably, the zinc oxide according to the present invention is uncoated or coated with dimethicone, methicone, or triethoxycaprylylsilane, and most preferably, the zinc oxide according to the present invention is surface-coated with triethoxycaprylylsilane.
[0017] Preferably, the amount of the coating is selected in the range of 0.1 to 25% by weight, preferably in the range of 0.25 to 10% by weight, most preferably in the range of 0.5 to 7.5% by weight, and even more preferably in the range of 1 to 5% by weight based on the weight of the uncoated zinc oxide.
[0018] More preferably, the zinc oxide is a white powder composed of zinc oxide existing as a wurtzite crystal structure.
[0019] Zinc oxide particles and preliminary dispersions of zinc oxide particles for use according to the present invention are available, for example, as PARSOL® ZX (2 - 3.5% triethoxycaprylylsilane-coated) from DSM Nutritional Products Ltd or ZnO-C-DS4 (dimethicone-coated) from Kobo.
[0020] A particularly advantageous zinc oxide according to the present invention is obtained by recrystallizing zinc oxide particles by dissolving zinc oxide in water under strongly acidic conditions (e.g., HCl) and at high temperature and then neutralizing with NaOH, coating the thus obtained particles with triethoxycaprylylsilane, and then performing dehydration, drying, and pulverization.
[0021] Most preferably, in all embodiments according to the present invention, zinc oxide is a white powder composed of zinc oxide existing as a wurtzite crystal structure coated with triethoxycaprylylsilane, the zinc oxide content thereof is 96 to 98%, the triethoxycaprylylsilane content is 2 to 3.5%, and the average particle size is 90 to 130 nm, which is commercially available as PARSOL (registered trademark) ZX.
[0022] In all embodiments of the present invention, the amount of fine zinc oxide is preferably in the range of 0.1% by weight to 20% by weight, more preferably in the range of 0.5% by weight to 15% by weight, most preferably in the range of 1% by weight to 10% by weight, for example, in the range of 5% by weight to 10% by weight, based on the total weight of the topical composition.
[0023] In all embodiments of the present invention, the amount of 2,4-bis{[4-(2-ethylhexyloxy)-2-hydroxy]phenyl}-6-(4-methoxyphenyl)-1,3,5-triazine (INCI: bisethylhexyloxyphenol methoxyphenyltriazine) is preferably in the range of 0.1% by weight to 10% by weight, more preferably in the range of 0.5% by weight to 7.5% by weight, most preferably in the range of 1% by weight to 5% by weight, based on the total weight of the topical composition.
[0024] In all embodiments of the present invention, the amount of 2-phenylbenzimidazole-5-sulfonic acid and / or one or more salts thereof is preferably in the range of 0.1% by weight to 10% by weight, more preferably in the range of 0.5% by weight to 7.5% by weight, most preferably in the range of 1% by weight to 5% by weight, based on the total weight of the topical composition.
[0025] In all embodiments of the present invention, the amount of 2,4,6-tris[anilino(p-carbo-2'-ethyl-1'-hexyloxy)]-1,3,5-triazine (INCI: ethylhexyltriazone) is preferably in the range of 0.1% by weight to 10% by weight, more preferably in the range of 0.5% by weight to 7.5% by weight, most preferably in the range of 1% by weight to 5% by weight, based on the total weight of the topical composition.
[0026] As used herein, the term "topical" is understood to mean, in particular, external application to the skin, scalp, eyelashes, eyebrows, nails, mucous membranes and keratinous substances such as hair, preferably human skin.
[0027] Since the topical composition according to the present invention is intended for topical application, it is well understood that the topical composition according to the present invention comprises a physiologically acceptable medium, i.e., a medium compatible with keratinous substances such as skin, mucous membranes and keratin fibers. In particular, the physiologically acceptable medium is a cosmetically acceptable carrier.
[0028] As used herein, the term "cosmetically acceptable carrier" refers to all carriers, excipients and / or diluents conventionally used in topical cosmetic compositions such as skin care formulations.
[0029] The exact amount of the carrier will depend on the actual amount of the UV filter and all other optional components (e.g., other active ingredients) that those skilled in the art would classify as different from the carrier.
[0030] In an advantageous embodiment, the topical composition according to the present invention comprises a carrier in an amount of 50% to 99%, preferably 60% to 98%, more preferably 70% to 98%, particularly 80% to 95% based on the total weight of the topical composition.
[0031] In a particular advantageous embodiment, the carrier further consists of water in an amount of at least 40% by weight, more preferably at least 50% by weight, most preferably at least 55% by weight, particularly 55 to 90% by weight.
[0032] In particular, the topical composition according to the present invention is a cosmetic or pharmaceutical composition, preferably a cosmetic (non-therapeutic) composition.
[0033] In one embodiment, the topical composition according to the invention is applied in particular to mammalian keratinous tissues such as human skin or human scalp and hair.
[0034] As used in this application, the term "cosmetic composition" refers to the cosmetic compositions defined under the heading "Kosmetika" in Roempp Lexikon Chemie, 10th edition 1997, Georg Thieme Verlag Stuttgart, New York and the cosmetic compositions disclosed in A. Domsch, "Cosmetic Compositions", Verlag fuer chemische Industrie (ed. H. Ziolkowsky), 4th edition, 1992.
[0035] Preferred topical compositions according to the invention are skin care formulations, decorative formulations and functional formulations.
[0036] Examples of skin care formulations are in particular light protection formulations, anti-aging formulations, formulations for treating photoaging, body oils, body lotions, body gels, treatment creams, skin protection ointments, skin powders, moisturizing gels, moisturizing sprays, face and / or body moisturizers, sunless tanning formulations (i.e., compositions for artificially tanning and / or browning the human skin without using sunlight), such as self-tanning creams and skin whitening formulations.
[0037] Examples of decorative formulations are in particular lipsticks, eyeshadows, mascaras, dry and wet makeup formulations, blushes and / or face powders.
[0038] Examples of functional formulations are cosmetic or pharmaceutical compositions containing active ingredients such as hormone formulations, vitamin formulations, plant extract formulations, anti-aging formulations and / or antimicrobial (antibacterial or antifungal) formulations, but are not limited thereto.
[0039] In certain embodiments, the topical compositions according to the invention are photoprotective formulations (sun care products, sunscreens), such as sunscreen lotions, sunscreen milks, sunscreen creams, sunscreen oils, sunblocks or tropical’s or day care creams having a SPF (Sun Protection Factor). Particular interest is directed to sunscreen creams, sunscreen lotions, sunscreen milks and sunscreen formulations.
[0040] The compositions of the invention (including the carrier) may include conventional auxiliaries and additives such as preservatives / antioxidants, fatty substances / oils, organic solvents, silicones, thickeners, emollients, emulsifiers, defoamers, aesthetic components such as fragrances, surfactants, fillers, anionic, cationic, nonionic or amphoteric polymers or mixtures thereof, propellants, acidifying or basifying agents, dyes, colorants / coloring agents, abrasives, absorbents, chelating agents and / or sequestering agents, essential oils, skin refreshing agents, astringents, pigments or any other components customarily incorporated into compositions of this type.
[0041] According to the invention, the compositions according to the invention may include components for skin whitening, sunburn prevention, treatment of hyperpigmentation, acne, wrinkles, fine lines, atrophy and / or inflammation prevention or reduction, chelating agents and / or sequestering agents, anti-cellulite and slimming (e.g., phytic acid), firming, moisturizing and revitalizing, self-tanning, calming, and agents for improving elasticity and skin barrier properties, and / or further UV filter substances, and further components such as carriers and / or excipients or diluents conventionally used in topical compositions.
[0042] Unless otherwise stated, the excipients, additives, diluents, etc. described below are suitable for the topical compositions according to the invention. The required amounts of cosmetic and dermatological auxiliaries and additives can be readily determined by a person skilled in the art based on the desired product.
[0043] Additional ingredients, when considered appropriate, can be added to the oil phase, to the aqueous phase or separately. The mode of addition can be readily adapted by a person skilled in the art.
[0044] Examples of cosmetic excipients, diluents, adjuvants, additives and active ingredients commonly used in the skin care industry and suitable for use in the cosmetic compositions of the present invention are described, for example, in the International Cosmetic Ingredient Dictionary & Handbook by the Personal Care Product Council (http: / / www.personalcarecouncil.org / ), which is viewable by, for example, the ONLINE INFO BASE (http: / / online.personalcarecouncil.org / jsp / Home.jsp), but are not limited thereto.
[0045] The cosmetic active ingredients useful herein can, in some cases, provide more than one benefit or act by more than one mechanism of action.
[0046] Of course, the person skilled in the art will select the above-mentioned optional additional ingredients, adjuvants, diluents and additives and / or their amounts, taking care that the advantageous properties inherent in the combinations according to the invention are not or are substantially not adversely affected by one or more of the envisaged additions.
[0047] The topical composition according to the invention can be in the form of a suspension or dispersion in a solvent or fatty substance, or in the form of an emulsion or microemulsion (in particular oil-in-water (O / W), water-in-oil (W / O), silicone-in-water (Si / W) or water-in-silicone (W / Si) type, PIT-emulsion, multiple emulsion (e.g., oil-in-water-in-oil (O / W / O) or water-in-oil-in-water (W / O / W) type), Pickering emulsion, hydrogel, alcoholic gel, lipogel, single-phase or multiphase solution or vesicle dispersion), or in other conventional forms that can also be applied as a beauty pack or as a spray by means of a pen.
[0048] The topical composition according to the invention is preferably in the form of an oil-in-water (O / W) emulsion comprising an oily phase dispersed in an aqueous phase in the presence of an O / W emulsion. The preparation of such O / W emulsions is well known to those skilled in the art and is illustrated in the examples.
[0049] In an advantageous embodiment, the O / W emulsifier is a phosphate ester emulsifier. Among the preferred phosphate ester emulsifiers are C 8~10 alkyl ethyl phosphate, C 9~15 alkyl phosphate, cetareth-2 phosphate, cetareth-5 phosphate, cetes-8 phosphate, cetes-10 phosphate, cetyl phosphate, (C 6-10 ) pareth-4 phosphate, (C 12-15 ) pareth-2 phosphate, (C 12-15 ) pareth-3 phosphate, cetareth-2 phosphate DEA, cetyl phosphate DEA, oleth-3 phosphate DEA, cetyl phosphate potassium, deceth-4 phosphate, deceth-6 phosphate and trilauryl-4 phosphate. A specific phosphate ester emulsifier according to the invention is, for example, cetyl phosphate potassium commercially available as Amphisol® K from DSM Nutritional Products Ltd Kaiseraugst.
[0050] More preferred O / W emulsifiers according to the present invention include dipolyhydroxystearic acid PEG-30, lauric acid PEG-4, dioleic acid PEG-8, oleic acid PEG-40 sorbitol, PEG-7 glyceryl cocoate, PEG-20 glyceryl almond fatty acid, PEG-25 hydrogenated castor oil, glyceryl stearate (and) stearic acid PEG-100, olive oil fatty acid PEG-7, oleic acid PEG-8, lauric acid PEG-8, PEG-60 glyceryl almond fatty acid, sesquistearic acid PEG-20 methyl glucose, stearic acid PEG-40, stearic acid PEG-100, lauric acid PEG-80 sorbitan, steareth-2, steareth-12, oleth-2, ceteth-2, laureth-4, oleth-10, oleth 10 / polyoxyethylene (10) oleyl ether, ceteth-10, isosteareth-20, cetareth-20, oleth-20, steareth-20, steareth-21, ceteth-20, isoceteth-20, laureth-23, steareth-100, glyceryl stearate citrate, glyceryl stearate (self-emulsifying type), stearic acid, salts of stearic acid, and polyglyceryl-3 methyl glucose distearate. Even more preferred emulsifiers are sorbitan oleate, sorbitan sesquioleate, sorbitan isostearate, sorbitan trioleate, lauryl glucoside, decyl glucoside, sodium stearoyl glutamate, sucrose polystearate, and hydrated polyisobutene. Further, one or more synthetic polymers can be used as emulsifiers. For example, (VP / eicosene) copolymer, (acrylates / acrylic acid alkyl (C10-30)) crosspolymer, (acrylates / steareth-20 methacrylate) copolymer, (PEG-22 / dodecyl glycol) copolymer, (PEG-45 / dodecyl glycol) copolymer, and mixtures thereof.
[0051] Another particularly suitable type of O / W emulsifier is, for example, olive oil fatty acid sorbitan (chemical composition: sorbitan esters and cetearyl esters of olive oil fatty acids), known as cetearyl and OLIVEM 1000 under the trade name of olive oil fatty acid sorbitan, which is a non-ionic self-emulsifying system derived from olive oil.
[0052] Commercially available polymer emulsifiers, such as hydrophobically modified polyacrylic acids such as (acrylates / alkyl acrylates (C10-30)) cross-polymer sold under the trade names Pemulen® TR-1 and TR-2 from Noveon, are even more suitable.
[0053] Another particularly suitable type of emulsifier is the polyglycerol ester or diester of fatty acids, also called polyglyceryl ester / diester (i.e., a polymer in which fatty acids are bonded by esterification with polyglycerol), such as Isolan GPS [INCI name (diisostearic acid / polyhydroxystearic acid / sebacic acid) polyglyceryl-4 (i.e., a diester of a mixture of isostearic acid, polyhydroxystearic acid and sebacic acid and polyglyceryl-4)] commercially available from Evonik or Dehymuls PGPH (INCI dipolyhydroxystearic acid polyglyceryl-2) commercially available from Cognis.
[0054] Also, polyethylene glycol ethers such as Brij 72 (polyoxyethylene (2) stearyl ether) or Brij 721 (polyoxyethylene (21) stearyl ether) available from Croda, for example, are also suitable.
[0055] Particularly advantageous O / W emulsifiers according to the invention are one or more of polyglyceryl-3 methylglucose distearate, lauryl glucoside (and) polyglyceryl-2 dipolyhydroxystearate, glyceryl stearate citrate, sodium cetearyl sulfate, cetearyl glucoside; polyglyceryl-6 stearate (and) polyglyceryl-6 behenate, cetearyl olive oil fatty acid (and) sorbitan olive oil fatty acid, araalkyl alcohol (and) behenyl alcohol (and) arachidyl glucoside, cetearyl alcohol (and) coconut oil alkyl glucoside, coconut oil alkyl glucoside (and) coconut alcohol, PEG-100 stearate (and) glyceryl stearate, sodium stearoyl glutamate, steareth-20, steareth-21, steareth-25, steareth-2, ceteth-25 and ceteth-6 (all described by their INCI names).
[0056] The most preferred O / W emulsifiers according to the invention are one or more of ceteth-6 (optionally in a mixture with stearyl alcohol) and ceteth-25.
[0057] This at least one O / W or Si / W emulsifier is preferably used in an amount in the range of 0.5 to 10% by weight, particularly in the range of 0.5 to 5% by weight, most particularly in the range of 0.5 to 4% by weight, based on the total weight of the composition.
[0058] Suitable W / O or W / Si emulsifiers according to the present invention are polyglyceryl-2 dipolyhydroxystearate, PEG-30 dipolyhydroxystearate, cetyl dimethicone copolyol, polyglyceryl-3 diisostearate, polyglycerol ester of oleic acid / isostearic acid, polyglyceryl-6 ricinoleate, polyglyceryl-4 oleate, polyglyceryl-4 oleate / coconut oil fatty acid PEG-8-PG, magnesium stearate, sodium stearate, potassium laurate, potassium ricinoleate, sodium coconut fatty acid, sodium tallow fatty acid, sodium castor oil fatty acid, sodium oleate and mixtures thereof. More suitable W / Si emulsifiers are lauryl polyglyceryl-3 polydimethylsiloxyethyl dimethicone, and / or PEG-9 polydimethylsiloxyethyl dimethicone, and / or cetyl PEG / PPG-10 / 1 dimethicone, and / or PEG-12 dimethicone crosspolymer, and / or PEG / PPG-18 / 18 dimethicone. A particularly suitable W / O emulsifier for use in the compositions according to the present invention is PEG-30 dipolyhydroxystearate. At least one W / O emulsifier is preferably used in an amount of about 0.001 to 10% by weight, more preferably 0.2 to 7% by weight, based on the total weight of the composition.
[0059] The topical compositions according to the present invention more preferably contain at least one surfactant adjuvant, such as those selected from the group consisting of, for example, monoglycerides and diglycerides and / or fatty alcohols. The surfactant adjuvant is generally used in an amount selected from the range of 0.1 to 10% by weight, in particular in the range of 0.5 to 7% by weight, most particularly in the range of 1 to 5% by weight, based on the total weight of the composition. Specific suitable surfactant adjuvants are selected from the list of alkyl alcohols such as cetyl alcohol (Lorol C16, Lanette 16), cetearyl alcohol (Lanette O), stearyl alcohol (Lanette 18), behenyl alcohol (Lanette 22), glyceryl stearate, glyceryl myristate (Estol 3650), hydrogenated coco-glyceryl (Lipocire Na10) and mixtures thereof.
[0060] In certain advantageous embodiments according to the present invention, the emulsifier is selected from the group consisting of cetearyl-6 and / or cetearyl-25, and the surfactant adjuvant is selected from the group consisting of behenyl alcohol, cetyl alcohol, cetearyl alcohol and / or stearyl alcohol.
[0061] The composition in the form of an O / W emulsion according to the present invention can be provided, for example, in any formulation form of an O / W emulsion, such as in the form of a lotion, milk or cream, which are prepared according to conventional methods. The composition which is the subject of the present invention is intended for topical application and can in particular constitute a dermatological or cosmetic composition, for example intended to protect human skin from the adverse effects of ultraviolet rays (such as preventing wrinkles, anti-aging, moisturizing, protection from sunlight, etc.).
[0062] According to an advantageous embodiment of the present invention, the composition constitutes a cosmetic composition and is intended for topical application to the skin.
[0063] Finally, the subject of the present invention is a method for cosmetically treating keratinous substances such as the skin in particular, and the composition as defined above is applied in particular to said keratinous substances such as the skin. This method is particularly suitable for protecting the skin from the adverse effects of ultraviolet rays such as sunburn and / or photoaging.
[0064] In an advantageous aspect of the present invention, the topical composition according to the present invention does not contain (i.e., is free of) 3-(4-methylbenzylidene)-camphor, 2-hydroxy-4-methoxybenzophenone (INCI: oxybenzone) and ethylhexyl 2-cyano-3,3-diphenylacrylate (INCI: octocrylene).
[0065] In another advantageous aspect of the present invention, the topical composition according to the present invention further comprises one or more of dibutyl adipate, dicaprylyl carbonate, alkyl (C12-15) benzoate, caprylyl carbonate, glyceryl tri(caprylate / caprate), and mixtures thereof, preferably alkyl (C12-15) benzoate and / or dicaprylyl carbonate.
[0066] In a further advantageous aspect of the present invention, the topical composition of the present invention further comprises a preservative and / or a co-preservative preferably selected from the group consisting of phenoxyethanol, ethylhexylglycerin, hexylglycerin, glyceryl caprylate, caprylyl glycol, 1,2-hexanediol, propanediol, propylene glycol, p-hydroxyacetophenone, and mixtures thereof, most preferably selected from the group consisting of p-hydroxyacetophenone, phenoxyethanol, hexylglycerin, and mixtures thereof. When the preservative or co-preservative is present, they are preferably used in an amount of 0.01 to 2% by weight, more preferably 0.05 to 1.5% by weight, and most preferably 0.1 to 1.0% by weight based on the total weight of the composition.
[0067] In another advantageous aspect, the topical composition according to the present invention does not contain any parabens, benzethonium chloride, piroctone olamine, lauroyl arginate, methylisothiazolinone, chloromethylisothiazolinone, bronopol, benzalkonium chloride, formaldehyde-releasing compounds, salicylic acid, triclosan, DMDM hydantoin, chlorphenesin, and IPBC (iodopropynyl butylcarbamate).
[0068] In a further advantageous aspect, the topical composition of the present invention further comprises one or more of glycerin or polyhydroxystearic acid and mixtures thereof.
[0069] In a more advantageous embodiment, the topical composition of the present invention further comprises a thickening agent, preferably a gum such as xanthan gum or Caesalpinia spinosa gum or a polyacrylate such as polyacrylate crosspolymer-6 and mixtures thereof.
[0070] The topical composition according to the present invention generally has a pH in the range of 3 to 10, preferably in the range of 4 to 8, and most preferably in the range of 4 to 7. The pH can be easily adjusted as necessary using a suitable acid, such as citric acid, or a base, such as NaOH, according to standard methods in the art.
[0071] The topical composition according to the present invention may further contain one or more emollient agents that soothe and soften the skin. As an example, the emollient agent may be dicaprylyl carbonate or alkyl benzoate (C 12-15 )). Further emollient agents are silicone (dimethicone, cyclomethicone), vegetable oil (grape seed, sesame seed, jojoba, etc.), butter (cocoa butter, shea butter), alcohol (stearyl alcohol, cetyl alcohol) and petrolatum derivatives (petrolatum, mineral oil).
[0072] In yet another embodiment, the topical composition of the present invention may include one or more of potassium cetyl phosphate as an emulsifier and / or dibutyl adipate, dicaprylyl carbonate and alkyl benzoate (C12-15).
[0073] In other embodiments, the topical composition of the present invention can contain one or more fragrances selected from limonene, citral, linalool, α-isomethylionone, geraniol, citronellol, 2-isobutyl-4-hydroxy-4-methyltetrahydropyran, 2-tert-pentylcyclohexyl acetate, 3-methyl-5-phenyl-1-pentanol, 7-acetyl-1,1,3,4,4,6-hexamethyltetralin, adipic acid diester, cinnamal, amyl salicylate, α-amylcinnamaldehyde, α-methylionone, butylphenylmethylpropanal, cinnamal, amylcinnamyl alcohol, anis alcohol, benzoin, benzyl alcohol, benzyl benzoate, benzyl cinnamate, benzyl salicylate, bergamot oil, bitter orange oil, butylphenylmethylpropional, shouzhuk seed oil, cedrol, cinnamal, cinnamyl alcohol, citronellyl methylcrotonate, citrus oil, coumarin, diethyl succinate, ethyl linalool, eugenol, Evernia furfuracea extract, Usnea barbata extract, farnesol, guaiacwood oil, hexyl cinnamal, hexyl salicylate, hydroxycitronellal, lavender oil, lemon oil, linalyl acetate, mandarin oil, PCA menthyl, methyl heptenone, nikuzuku kernel oil, rosemary oil, sweet orange oil, terpineol, tonka bean oil, triethyl citrate, vanillin.
[0074] In other embodiments, the topical composition of the present invention can contain at least one salt of 2-phenylbenzimidazole-5-sulfonic acid.
[0075] In other embodiments, the composition can have an SPF of at least 20, preferably at least 30.
[0076] The topical composition of the present invention can be made with a surprisingly low total amount of UV filter.
[0077] In addition to the claimed combination of UV filters, the formulations of the present invention can contain one or more further UV filters. According to the invention, these are preferably phenylenedi(2-benzimidazolyl)-3,3’,5,5’-tetrasulfonate; 1,4-di(2-oxo-10-sulfo-3-bornylidene methyl) benzene and its salts; 4-(2-oxo-3-bornylidene methyl)-benzenesulfonate; 2-methyl-5-(2-oxo-3-bornylidene methyl) sulfonate; 2,2’-methylene-bis(6-(2H-benzotriazol-2-yl)-4-(1,1,3,3-tetramethylbutyl)phenol); 2-(2H-benzotriazol-2-yl)-4-methyl-6-[2-methyl-3-[1,3,3,3-tetramethyl-1-[(trimethylsilyl)oxy]disiloxanyl]propyl]-phenol; 3-benzylidenecamphor; terephthalylidenedicamphorsulfonic acid; 2-ethylhexyl 4-(dimethylamino)benzoate; amyl 4-(dimethylamino)benzoate; di(2-ethylhexyl) 4-methoxybenzalmalonate; isoamyl 4-methoxycinnamate; hexyl 2-(4’-diethylamino-2’-hydroxybenzoyl)benzoate, ethylhexyl salicylate, homomenthyl salicylate, 2-ethylhexyl 2-hydroxybenzoate; dimethicone / diethyl 2-benzylidenemalonate; 3-(4-(2,2-bis-ethoxycarbonylvinyl)-phenoxy)propenyl)methoxysiloxane / dimethylsiloxane copolymer; 4-(tert-butyl)-4’-methoxydibenzoylmethane, 1,4-di(benzoxazol-2’-yl)benzene and 2,4,6-triphenyl-4-yl-1,3,5-triazine can be selected.
[0078] In an embodiment, the present invention does not contain 1,4-di(benzoxazol-2’-yl)benzene, especially micronized 1,4-di(benzoxazol-2’-yl)benzene.
[0079] According to the present invention, advantageously, the topical composition is in the form of an emulsion or a dispersion, preferably in the form of an emulsion, more preferably in the form of an O / W emulsion.
[0080] When the topical composition of the present invention is in the form of an O / W emulsion, the formulation advantageously contains one or more O / W emulsifiers selected from glyceryl citrate stearate, glyceryl stearate (self-emulsifying type), stearic acid, stearate, polyglyceryl-3-methylglucose distearate, sodium cetearyl sulfate, potassium cetyl phosphate, polyglyceryl-10 stearate, and sodium stearyl glutamate.
[0081] According to the present invention, advantageously, these O / W emulsifiers of the present invention can be present in the formulation at a concentration of 0.001 to 10% by weight, preferably 0.1 to 7% by weight, based on the total weight of the formulation.
[0082] According to the present invention, preferably, the formulation contains potassium cetyl phosphate as an emulsifier.
[0083] According to the present invention, more advantageously, the formulation contains cetyl alcohol, stearyl alcohol, and / or glyceryl stearate.
[0084] According to the present invention, advantageously, the formulation of the present invention does not contain polyethylene glycol, polyethylene glycol ether, and polyethylene glycol ester (so-called PEG derivatives).
[0085] The formulation of the present invention may advantageously contain a humectant. A humectant is a compound or a mixture of compounds that imparts to the cosmetic formulation the quality of reducing the water loss of the stratum corneum (also referred to as transepidermal water loss (TEWL)) and / or having a favorable effect on the hydration of the stratum corneum after the cosmetic formulation is applied to or spread on the skin surface.
[0086] Non-limiting examples of humectants that are advantageous for use in the present invention include glycerol, lactic acid and / or lactate, particularly sodium lactate, butylene glycol, propylene glycol, biosaccharide gum-1, adzuki bean, ethylhexyl oxyglycerol, pyrrolidone carboxylic acid, and urea. In particular, it is more advantageous to use a polymeric humectant from the group of polysaccharides that are water-soluble and / or water-swellable and / or gellable by the force of water. Particularly advantageous are, for example, hyaluronic acid, chitosan and / or fucose-rich polysaccharides, and the fucose-rich polysaccharides are registered in the Chemical Abstracts with the registration number 178463-23-5 and are available, for example, from SOLABIAS.A. under the name Fucogel® 1000. The humectant can also be advantageously used, for example, as an anti-wrinkle active ingredient for protecting the skin from the types of changes caused by skin aging.
[0087] Although not essential, advantageously, the cosmetic formulation of the present invention may further comprise a filler that, for example, further improves the sensory and aesthetic properties of the formulation and has an effect of evoking or enhancing, for example, a velvety or silk-like feel. Fillers that are advantageous in the context of the present invention are starch and starch derivatives (for example, tapioca starch, phosphate-crosslinked starch, aluminum octenyl succinate starch, sodium, etc.), pigments that essentially show neither an ultraviolet filter effect nor a coloring effect (for example, boron nitride, etc.), and / or Aerosils® (CAS No. 7631-86-9), and / or talc, and / or polyethylene, nylon, and dimethylsilylated silica.
[0088] As an advantageous embodiment of the formulation of the present invention, embodiments in which the formulation contains one or more oils selected from dibutyl adipate, dicaprylyl carbonate, and / or alkyl (C12-15) benzoate, diisopropyl sebacate, dicaprylyl carbonate, dialkyl (C12-13) tartrate, butyl octyl salicylate, diethylhexyl malonate silicylene, hydrogenated castor oil dimer acid ester, triheptanoin, alkyl (C12-13) lactate, alkyl (C16-17) benzoate, propyl heptyl caprylate, glyceryl tri(caprylate / caprate), diethylhexyl naphthalenedicarboxylate, octyldodecanol, and ethylhexyl coconut oil fatty acid are also included.
[0089] According to the present invention, formulations containing dibutyl adipate, dicaprylyl carbonate and / or alkyl (C12-15) benzoate are preferred.
[0090] The aqueous phase of the formulation according to the invention advantageously contains conventional cosmetic adjuvants, such as, in each case individually or in combination, alcohols, especially those with a low carbon number, preferably ethanol and / or isopropanol or polyols with a low carbon number and their ethers, preferably propylene glycol, glycerol, electrolytes, self-tanning agents and, in addition to these, especially one or more thickeners, advantageously silicon dioxide, aluminium silicate, polysaccharides and / or their derivatives, such as hyaluronic acid, xanthan gum, hydroxypropylmethylcellulose, thickeners which can be selected from the group consisting of, especially preferably, polyacrylates, preferably polyacrylates from the group of polyacrylates known as Carbopol (examples of which include Carbopol types 980, 981, 1382, 2984 and 5984). Further advantageous thickeners according to the invention are, in addition to those having the INCI name (acrylates / acrylic acid alkyl (C10 - 30)) crosspolymer (for example Pemulen TR 1, Pemulen TR 2, Carbopol 1328 from NOVEON), Aristoflex AVC (INCI: (acryloyldimethyltaurine ammonium / VP) copolymer) and Simugel NS (INCI: (hydroxyethyl acrylate / acryloyldimethyltaurine Na) copolymer and squalane and polysorbate 60).
[0091] In this regard, according to the invention, it is preferred that the formulation contains xanthan gum, crosslinked acrylate / acrylic acid alkyl (C10 - 30) polymer, (hydroxyethyl acrylate / acryloyldimethyltaurine Na) copolymer and squalane and polysorbate 60 and / or vinylpyrrolidone / hexadecene copolymer.
[0092] According to the invention, it is particularly advantageous for the formulation to contain at least 2.5% by weight of glycerol, based on the total weight of the formulation.
[0093] According to the present invention, it is advantageous for the formulation to contain one or more alkanediols from the group of 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol, 1,2-decanediol, 2-methyl-1,3-propanediol.
[0094] According to the present invention, it is advantageous for the formulation of the present invention to contain ethanol, phenoxyethanol and / or ethylhexylglycerin.
[0095] According to the present invention, it is advantageous for the formulation of the present invention to contain a film-forming agent. The film-forming agent in the meaning of the present invention is a substance having various configurations characterized by having the following properties: When the film-forming agent is dissolved in water or another suitable solvent and this solution is applied to the skin, the film-forming agent forms a film after the solvent has evaporated, and this film basically serves to fix a light-shielding substance on the skin and enhance the water resistance of the product.
[0096] It is particularly advantageous to select the film-forming agent from the group of polymers based on polyvinylpyrrolidone (PVP).
[0097] For example, copolymers of vinylpyrrolidone such as (VP / hexadecene) copolymer and (VP / eicosene) copolymer available under the trade names Antaron V216 and Antaron V220 from GAF Chemicals Corporation are particularly preferred.
[0098] Similarly, other polymeric film formers such as sodium polystyrene sulfonate available under the trade name Flexan 130 from National Starch and Chemical Corp. and / or polyisobutene available under the trade name Rewopal PIB1000 from Rewo are also advantageous. Examples of further suitable polymers are polyacrylamide (Seppigel 305), polyvinyl alcohol, PVP, PVP / VA copolymer, polyglycol, acrylate / octylacrylamide copolymer (Dermacryl 79). It is similarly advantageous to use hydrogenated castor oil dimer linoleic acid (CAS 646054-62-8, INCI hydrogenated castor oil dimer linoleic acid) available under the name Risocast DA-H from Kokyu Alcohol Kogyo or otherwise PPG-3 benzyl ether myristate (CAS 403517-45-3) available under the trade name Crodamol STS from Croda Chemicals.
[0099] According to the present invention, the formulations of the present invention are used as a UV protection composition in addition to protecting the skin from aging (especially protecting the skin from UV-induced aging).
[0100] According to the present invention, the combination of UV filters of the present invention is also used to reduce the adhesion of sand to cosmetic formulations (especially sunscreen compositions). In particular, in this case, according to the present invention, in order to reduce the adhesion of sand to cosmetic formulations (especially sunscreen compositions), zinc oxide, 2,4-bis{[4-(2-ethylhexyloxy)-2-hydroxy]phenyl}-6-(4-methoxyphenyl)-1,3,5-triazine (INCI: bisethylhexyloxyphenol methoxyphenyltriazine), 2-phenylbenzimidazole-5-sulfonic acid and / or one or more salts thereof, and 2,4,6-tris[anilino(p-carbo-2'-ethyl-1'-hexyloxy)]-1,3,5-triazine (INCI: ethylhexyltriazone) are used in combination. In this connection, particularly preferably, the zinc oxide has an average particle diameter Dn50 selected in the range of 50 to 200 nm, preferably in the range of 75 to 150 nm, most preferably in the range of 90 to 130 nm, determined by laser diffraction, and a surface coating selected from the group consisting of triethoxycaprylylsilane, octyltrimethoxysilane, and dimethicone, preferably triethoxycaprylylsilane and dimethicone, most preferably triethoxycaprylylsilane.
[0101] The following examples are provided to further illustrate the compositions and effects of the present invention. These examples are merely illustrative and are not intended to limit the scope of the present invention in any way.
[0102] [Examples] Formulations outlined in Table 1 were prepared according to standard methods in the art. Then, the sand adhesion prevention property was tested according to the method outlined below. - Apply 2 mg / cm of cream to the PMMA plate 2 and spread it evenly - Dry at 40 °C for 15 minutes - Measure the weight of the PMMA plate - Place sand (Kultpfoetchen 5kg - terrarium sand, natural beige, particle size 0.4 - 0.8 mm) in a petri dish, place the plate with the cream film side facing the sand, place a weight (500 g) on the plate, and leave it for 5 minutes. - Remove the PMMA plate and rotate it 180° without shaking the plate. - Measure the weight of the PMMA plate. - Determine the amount of sand adhering to the plate. - Repeat the test for each sample using four plates.
[0103] The results are shown in Table 1.
[0104]
Table 1
[0105] As can be read from Table 1, by using the combination according to the present invention, the adhesion of sand to the plate is reduced compared to the reference product.
Claims
Claim 1. A topical composition which is a W / O emulsion or an O / W emulsion, comprising: a.) fine zinc oxide having an average particle diameter Dn50 selected in the range of 30 to 200 nm, as determined by laser diffraction, and a surface coating selected from the group consisting of triethoxycaprylylsilane, octyltrimethoxysilane, and dimethicone; b.) 2,4-bis{[4-(2-ethylhexyloxy)-2-hydroxy]phenyl}-6-(4-methoxyphenyl)-1,3,5-triazine; c.) 2-phenylbenzimidazole-5-sulfonic acid and / or one or more salts thereof; d.) 2,4,6-tris[anilino(p-carbo-2'-ethyl-1'-hexyloxy)]-1,3,5-triazine; wherein the combination of UV filters is included, the amount of the fine zinc oxide is selected in the range of 0.1% to 20% by weight based on the total weight of the composition, the amount of 2,4-bis{[4-(2-ethylhexyloxy)-2-hydroxy]phenyl}-6-(4-methoxyphenyl)-1,3,5-triazine is selected in the range of 0.1% to 10% by weight based on the total weight of the composition, the amount of 2-phenylbenzimidazole-5-sulfonic acid and / or one or more salts thereof is selected in the range of 0.1% to 10% by weight based on the total weight of the composition, the amount of 2,4,6-tris[anilino(p-carbo-2'-ethyl-1'-hexyloxy)]-1,3,5-triazine is selected in the range of 0.1% to 10% by weight based on the total weight of the composition, a topical composition that does not contain 3-(4-methylbenzylidene)camphor, 2-hydroxy-4-methoxybenzophenone, and ethylhexyl 2-cyano-3,3-diphenylacrylate. Claim 2. The topical composition according to claim 1, wherein the fine zinc oxide has an average particle diameter selected in the range of 50 to 200 nm, as determined by laser diffraction. Claim 3. The topical composition according to claim 1 or 2, wherein the fine zinc oxide is surface-coated with triethoxycaprylylsilane. Claim 4. The topical composition according to any one of claims 1 to 3, wherein the amount of the fine zinc oxide is selected in the range of 5% to 10% by weight based on the total weight of the composition. Claim 5. The topical composition according to any one of claims 1 to 4, comprising one or more of ceteth-6 and ceteth-25 as an emulsifier.
6. The topical composition according to any one of claims 1 to 5, comprising one or more of dibutyl adipate, dicaprylyl carbonate, and alkyl (C12-15) benzoate.
7. The topical composition according to any one of claims 1 to 6, comprising one or more of ethanol, p-hydroxyacetophenone, phenoxyethanol, and ethylhexylglycerin.
8. The topical composition according to any one of claims 1 to 7, comprising one or more of xanthan gum, crosslinked acrylate / alkyl acrylate (C10-30) polymer, (hydroxyethyl acrylate / acryloyldimethyltaurine Na) copolymer, squalane, polysorbate 60, and (VP / hexadecene) copolymer.
9. The topical composition according to any one of claims 1 to 8, comprising one or more of cetyl alcohol, cetearyl alcohol, stearyl alcohol, and glyceryl stearate.
10. The topical composition according to any one of claims 1 to 9, having an SPF of at least 20.
11. Use of fine zinc oxide to reduce the stickiness of a topical composition comprising 2,4-bis{[4-(2-ethylhexyloxy)-2-hydroxy]phenyl}-6-(4-methoxyphenyl)-1,3,5-triazine, 2-phenylbenzimidazole-5-sulfonic acid and / or one or more salts thereof, and 2,4,6-tris[anilino(p-carbo-2'-ethyl-1'-hexyloxy)]-1,3,5-triazine, wherein the fine zinc oxide has an average particle diameter Dn50 selected in the range of 30 to 200 nm as determined by laser diffraction, and a surface coating selected from the group consisting of triethoxycaprylylsilane, octyltrimethoxysilane, and dimethicone, the amount of the fine zinc oxide is selected in the range of 0.1% to 20% by weight based on the total weight of the composition, the amount of 2,4-bis{[4-(2-ethylhexyloxy)-2-hydroxy]phenyl}-6-(4-methoxyphenyl)-1,3,5-triazine is selected in the range of 0.1% to 10% by weight based on the total weight of the composition. The amount of the 2-phenylbenzimidazole-5-sulfonic acid and / or one or more salts thereof is selected in the range of 0.1% by weight to 10% by weight based on the total weight of the composition, The amount of the 2,4,6-tris[anilino(p-carbo-2'-ethyl-1'-hexyloxy)]-1,3,5-triazine is selected in the range of 0.1% by weight to 10% by weight based on the total weight of the composition, The composition is a W / O emulsion or an O / W emulsion, Use where the composition does not contain 3-(4-methylbenzylidene)camphor, 2-hydroxy-4-methoxybenzophenone, and ethylhexyl 2-cyano-3,3-diphenylacrylate. [
12. ] A method for reducing the stickiness and / or sand adhesion to the skin of a topical composition comprising at least one of 2,4-bis{[4-(2-ethylhexyloxy)-2-hydroxy]phenyl}-6-(4-methoxyphenyl)-1,3,5-triazine, 2-phenylbenzimidazole-5-sulfonic acid and / or one or more salts thereof, and 2,4,6-tris[anilino(p-carbo-2'-ethyl-1'-hexyloxy)]-1,3,5-triazine, comprising the step of incorporating fine zinc oxide into the topical composition before applying the composition to the skin, The fine zinc oxide has an average particle diameter Dn50 selected in the range of 30 to 200 nm determined by laser diffraction and a surface coating selected from the group consisting of triethoxycaprylylsilane, octyltrimethoxysilane, and dimethicone, The amount of the fine zinc oxide is selected in the range of 0.1% by weight to 20% by weight based on the total weight of the composition, The amount of the 2,4-bis{[4-(2-ethylhexyloxy)-2-hydroxy]phenyl}-6-(4-methoxyphenyl)-1,3,5-triazine is selected in the range of 0.1% by weight to 10% by weight based on the total weight of the composition, The amount of the 2-phenylbenzimidazole-5-sulfonic acid and / or one or more salts thereof is selected in the range of 0.1% by weight to 10% by weight based on the total weight of the composition, The amount of the 2,4,6-tris[anilino(p-carbo-2'-ethyl-1'-hexyloxy)]-1,3,5-triazine is selected in the range of 0.1% by weight to 10% by weight based on the total weight of the composition, The composition is a W / O emulsion or an O / W emulsion, The composition does not contain 3-(4-methylbenzylidene) camphor, 2-hydroxy-4-methoxybenzophenone, and ethylhexyl 2-cyano-3,3-diphenylacrylate, a method.
Citation Information
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