Anti-acne sunscreen composition, preparation method of anti-acne sunscreen composition and application of anti-acne sunscreen composition
By combining salicylic acid and other anti-acne ingredients, UV filters and stabilizing polymers in the sunscreen composition, the greasy and instability of the sunscreen composition on oily skin in the prior art is solved, achieving high levels of SPF, stable and comfortable sun protection.
Patent Information
- Application Number
- CN202411291565.X
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2019-02-28
- Publication Date
- 2024-12-17
AI Technical Summary
Existing sunscreen compositions are difficult to maintain the comfort of oily skin while increasing the level of UV protection and often lead to greasiness, viscosity and instability, especially when high levels of sunscreen filters are included.
Anti-acne agent system containing salicylic acid and other anti-acne ingredients such as octanyl salicylic acid, hydroxyethylpiperazine ethanesulfonic acid, octadecene diacid or nicotinamide, combined with UV filter system and stabilization polymerization The composition system forms a high SPF sunscreen composition to ensure the stability and ease of application of the composition.
Achieve high levels of UV protection, control oil secretion, reduce skin gloss, provide matte results, and maintain skin comfort and stability.
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Abstract
Description
[0001] This application is a divisional application of a Chinese invention patent application with an international application date of February 28, 2019, an international application number of PCT / BR2019 / 050064, an application number of 201980093052.9 entering the Chinese national phase, and an invention name of “Anti-acne sunscreen composition, a method for preparing an anti-acne sunscreen composition, and a use of an anti-acne sunscreen composition”. Field of the Invention
[0002] The present invention relates to an anti-acne sunscreen composition, comprising: (a) an anti-acne agent system, the anti-acne agent system comprising salicylic acid and at least one additional anti-acne ingredient, (b) a UV filter system, the UV filter system comprising at least two UV filters, and (c) a stabilizing polymer system. The present invention also relates to a method for preparing the anti-acne sunscreen composition and the use thereof. Background of the Invention
[0004] Photoprotection of keratin materials, including both skin and hair, is considered very important to prevent sun damage, sunburn, photoaging, and to reduce the chance of developing skin cancer caused by exposure to ultraviolet ("UV") radiation. There are generally two types of UVA / UVB sunscreen compositions used to achieve photoprotection, namely inorganic UV filters and organic UV filters.
[0005] The degree of UV protection provided by a sunscreen composition is directly related to the amount and type of UV filters contained therein. The higher the amount of UV filters, the higher the degree of UV protection (UVA / UVB).
[0006] In particular, sunscreen compositions must provide good protection against the sun, as measured by the sun protection factor (SPF) value, while at the same time having a pleasing sensory perception, such as a smooth, non-greasy feel upon application. However, this combination of properties is difficult to achieve, particularly since many sunscreen active ingredient compounds themselves have an oily or greasy feel, and increasing their content often results in the final product suffering from this effect.
[0007] Furthermore, most organic sunscreen filters are oily and / or oil-soluble materials and high levels of such sunscreen filters in sunscreen products make the products less attractive due to their greasy skin feel, stickiness, long drying time and leaving a shiny residue on the skin after application.
[0008] Furthermore, they are often unstable due to the high levels of sunscreen filters associated with large amounts of fillers to ensure good sensory and / or additional active ingredients to achieve additional beneficial effects in O / W emulsions.
[0009] The drawbacks associated with a greasy skin feel will directly affect oily skin. It is known that the main determinant of skin oiliness is the secretion of the sebaceous glands. The sebaceous glands are formed by pyknotic cells and are located in the dermis. The cells release their lipid content in the hair follicles on the surface of the skin. This content is called "sebum" or tallow, and is therefore a whole secretion, containing 92-100% lipids (EBLING & ROOK, 1979).
[0010] Sebum secretions are composed of several types of fats: triglycerides, free fatty acids, esterified waxes, squalene, and cholesterol.
[0011] There are more glands and they are larger in certain areas of the skin. These areas are the "T-zone" (including the forehead, nose, and chin), back, chest, ears, armpits, genitals, and scalp.
[0012] Oily skin is shiny, thick, has dilated infundibulum of pilosebaceous glands (pores), especially in seborrheic areas, and is prone to developing acne (Cunliffe & Cotterill, 1975). This clinical aspect is aesthetically unpleasant and implies the need to develop specific products for oily skin.
[0013] Acne is a very common skin problem that affects a portion of the world population, mainly in the age group of 11-25 years. It is characterized by comedones, papules, pustules, cysts or scars, mainly located in the "seborrheic areas" - the areas of the body with the highest number of sebaceous glands - the central area of the face, the back and the chest (VIGLIOGLIA & RUBIN, 1991).
[0014] In pathophysiology, it is observed as an important factor in increased glandular sebum secretion, hyperkeratinization of hair follicles and subsequent obstruction, leading to accumulation of keratin and sebum in the hair follicles and bacterial colonization in addition to inflammation (SAMPAIO & RIVITTI, 2000).
[0015] The origin is not completely understood; however, it is known that in addition to changes in the local microbiota (increase in the bacterial population, especially Propionibacterium acnes), genetic aspects as well as emotional, immune, hormonal, and environmental factors are involved in the development or exacerbation of the condition.
[0016] Therefore, products for oily skin should have the purpose of regulating sebum secretion without deeply removing oil, as this will release a rebound effect and increase fat production. They can also work by reducing flora and hyperkeratosis (CLAR, 1994). The most suitable carriers are oil-water emulsions and gels, which should not contain comedogenic or acneogenic ingredients.
[0017] An important anti-acne active ingredient is salicylic acid, which is known to have keratolytic and anti-inflammatory properties. Furthermore, it is recognized that incorporating such a compound into a high SPF composition is difficult because it tends to break the composition into phases.
[0018] The inventors of the present invention have successfully overcome the problems of the prior art and surprisingly disclosed a stable sunscreen composition using an anti-acne agent system comprising salicylic acid and at least one additional anti-acne ingredient selected from the group consisting of octanoyl salicylic acid, hydroxyethylpiperazineethanesulfonic acid, octadecenedioic acid, niacinamide and combinations thereof, the sunscreen composition having a high SPF (UVA and UVB protection), exhibiting oil control, and thus exhibiting an anti-acne effect. Summary of the invention
[0019] The present invention relates to a novel anti-acne sunscreen composition with high SPF, a method for preparing the anti-acne sunscreen composition and use thereof.
[0020] In addition, due to the combination of (a) the anti-acne agent system, (b) the UV filter system and (c) the stabilizing polymer system, the anti-acne sunscreen composition of the present invention is stable over time, exhibits a high level of UV protection to protect the skin from sun damage, easy application, good spreadability, less shine and a matte effect. BRIEF DESCRIPTION OF THE DRAWINGS
[0021] Figures 1(a) to (c) demonstrate the results of stability testing of the anti-acne sunscreen composition of the present invention, according to Example 3, which shows the stability of the ingredients after 1 month at room temperature, 4°C and 45°C (Figure 1(b)) and after 2 months at room temperature, 4°C and 45°C (Figure 1(c)) when compared to the composition as prepared (Figure 1(a)). DETAILED DESCRIPTION
[0022] In one embodiment, the anti-acne sunscreen composition of the present invention comprises:
[0023] (a) an anti-acne agent system comprising salicylic acid and at least one additional anti-acne ingredient selected from the group consisting of capryloyl salicylic acid, hydroxyethylpiperazineethanesulfonic acid, octadecenedioic acid, niacinamide, and combinations thereof;
[0024] (b) UV filter system;
[0025] (c) a stabilizing polymer system selected from the group consisting of xanthan gum, acrylates / acrylic acid C 10-30Alkyl ester crosspolymers and ammonium acryloyldimethyltaurate / vp copolymers and combinations thereof.
[0026] In a preferred embodiment, the anti-acne agent system is present in an amount ranging from 0.5 wt % to 5.0 wt % relative to the total weight of the composition, preferably in an amount ranging from about 1 wt % to about 4 wt %, more preferably from about 2 wt % to about 3 wt % based on the total weight of the composition.
[0027] In a preferred embodiment, the salicylic acid of the anti-acne agent system is present in a range of 0.25 wt % to 1.0 wt % relative to the total weight of the composition, preferably in a range of about 0.35 wt % to about 0.75 wt %, more preferably about 0.4 wt % to about 0.5 wt % based on the total weight of the composition.
[0028] In a preferred embodiment, at least one additional anti-acne ingredient is present in a range of 0.2 wt. % to 4.0 wt. % relative to the total weight of the composition, preferably in a range of about 1.25 wt. % to about 3.5 wt. %, more preferably about 2.0 wt. % to about 2.8 wt. % based on the total weight of the composition.
[0029] In a preferred embodiment, the UV filter system of the present invention is selected from the group consisting of phenylbenzimidazolesulfonic acid, butyl methoxydibenzoylmethane, titanium dioxide, ethylhexyl triazone, terephthalylidene dicamphorsulfonic acid, octocrylene, homosalate, bis-ethylhexyloxyphenol methoxyphenyl triazine, silica (and) titanium dioxide, methylene bis-benzotriazolyl tetramethylbutylphenol (and) polyglyceryl 10 laurate and combinations thereof.
[0030] In a preferred embodiment, the UV filter system is present in an amount in the range of 0.1 wt.-% to 50 wt.-% relative to the total weight of the composition, preferably in an amount in the range of about 1 wt.-% to about 40 wt.-%, more preferably about 1 wt.-% to about 30 wt.-%, based on the total weight of the composition.
[0031] In a preferred embodiment, the stabilizing polymer system is present in an amount in the range of 0.1 wt % to 5 wt % relative to the total weight of the composition, preferably in an amount in the range of about 0.2 wt % to about 3 wt %, more preferably about 0.5 wt % to about 1.5 wt % based on the total weight of the composition.
[0032] In another preferred embodiment, when the polymer system comprises xanthan gum, acrylate / acrylic acid C 10-30When the combination of alkyl ester crosspolymer and ammonium acryloyldimethyltaurate / vp copolymer.
[0033] In a preferred embodiment, the anti-acne sunscreen composition of the present invention further comprises a cosmetically acceptable ingredient selected from the group consisting of additional sunscreens, fragrances / flavors, preservatives, solvents, active ingredients, surfactants, fatty compounds, vitamins, fillers, silicones, polymers, pigments, buffers, masking agents, and mixtures thereof.
[0034] In a preferred embodiment, the sunscreen composition of the present invention may exhibit a sun protection factor in the range of 30 to 90.
[0035] In various embodiments, the sunscreen compositions of the present invention can exhibit a sun protection factor of 30, 35, 40, 45, 50, 55, 60, 65, 70, 75, 80, 85, and 90.
[0036] In one embodiment, the sunscreen composition of the present invention may exhibit a sun protection factor of 30.
[0037] In one embodiment, the sunscreen composition of the present invention may exhibit a sun protection factor of 50.
[0038] In one embodiment, the sunscreen composition of the present invention may exhibit a sun protection factor of 60.
[0039] In one embodiment, the sunscreen composition of the present invention may exhibit a sun protection factor of 70.
[0040] In one embodiment, the sunscreen composition of the present invention may exhibit a sun protection factor of 80.
[0041] In one embodiment, the sunscreen composition of the present invention may exhibit a sun protection factor of 90.
[0042] The anti-acne sunscreen composition of the present invention can be used as a daily skin product.
[0043] The anti-acne sunscreen composition of the present invention is stable over time, yet exhibits a high level of UV protection to protect the skin from sun damage, ease of application, good spreadability, less shine, and a matte finish.
[0044] In another embodiment, the anti-acne sunscreen composition of the present invention exhibits anti-aging effects.
[0045] In another preferred embodiment, the present invention relates to the use of the composition for preparing a product for preventing sunburn.
[0046] The present invention also relates to methods of preparing sunscreen compositions for preventing sunburn that provide the above-mentioned properties to consumers.
[0047] the term
[0048] As used herein, the expression "at least" means one or more, and thus includes individual components as well as mixtures / combinations.
[0049] Other than in the working examples, or where otherwise indicated, all numbers expressing quantities of ingredients and / or reaction conditions are to be understood as modified in all instances by the term "about," meaning within + / - 5% of the indicated number.
[0050] As used herein, all ranges provided are meant to be included in each specific range within a given range, and combinations of subranges therebetween. Thus, a range of 1-5 specifically includes 1, 2, 3, 4, and 5, and subranges such as 2-5, 3-5, 2-3, 2-4, 1-4, etc. All ranges and values disclosed herein are inclusive and combinable. For example, any value or point described herein that falls within the range described herein can be used as a minimum or maximum value, etc., for deriving a subrange.
[0051] Anti-acne system
[0052] Salicylic acid
[0053] Salicylic acid or 2-hydroxybenzoic acid or parahydroxybenzoic acid is a BHA (Beta Hydroxy Acid) known for its keratolytic properties.
[0054] The salicylate cleavage formed by the alcohol (OH) and acid (COOH) functional groups is largely responsible for the exfoliating action of salicylic acid.
[0055]
[0056] Salicylic acid acts specifically on the corneum granules that are responsible for the cohesion of the stratum corneum cells. It induces a chemical breakage of these bonds, inducing cell-by-cell shedding of the stratum corneum cells.
[0057] In addition to the fact that this exfoliant helps remove dead cells filled with melanin, it is also added to the formula to promote the absorption of ceramides. In fact, due to their lipid chemical structure, ceramides tend to bind to epidermal lipids and have difficulty diffusing into the skin.
[0058] Additional Anti-Acne Ingredients
[0059] Suitable anti-acne ingredients for use in the present invention may be selected from the group consisting of capryloyl salicylic acid, hydroxyethylpiperazineethane sulfonic acid, octadecenedioic acid, niacinamide and alpha-hydroxy-acids such as glycolic acid and combinations thereof.
[0060] UV filter system
[0061] Additional non-limiting suitable UV filters of the present invention can be as follows:
[0062] Oil-soluble organic sunscreen ingredients
[0063] "Oil-soluble organic sunscreen ingredient" means any organic compound for screening UV radiation which is completely soluble or miscible in the oil phase in molecular form or which is soluble in the oily fatty phase in colloid form, for example in the form of micelles.
[0064] Non-limiting examples of oil-soluble organic sunscreen ingredients useful in the present invention include, for example, cinnamic acid derivatives; anthranilates; salicylic acid derivatives; dibenzoylmethane derivatives; camphor derivatives; benzophenone derivatives; diphenylacrylate derivatives; triazine derivatives; benzotriazole derivatives; benzalmalonate derivatives, especially those cited in patent US5624663; benzimidazole derivatives; imidazoline; bis-benzoxazolyl derivatives, such as those described in patents EP669323 and US246326 4; para-aminobenzoic acid (PABA) derivatives; methylene bis (hydroxyphenylbenzotriazole) derivatives, such as those described in applications US5237071, US5166355, GB2303549, DE19726184 and EP893119; benzoxazole derivatives, such as those described in patent applications EP0832642, EP1027883, EP1300137 and DE10162844; shielding polymers and shielding siloxanes, such as, in particular, patent application WO 93 / 04665; dimers derived from alkyl-styrene, such as those described in patent application DE 19855649; 4,4-diarylbutadiene, such as those described in patent applications EP0967200, DE19746654, DE19755649, EP-A-1008586, EP1133980 and EP1133981, merocyanine derivatives, such as those described in patent applications WO 04 / 006878, WO 05 / 058269 and WO 06 / 032741; and mixtures thereof, the entire contents of said patents and patent applications being incorporated by reference in their entirety.
[0065] As examples of other suitable oil-soluble organic sunscreen ingredients, mention may be made of those indicated below by their INCI names:
[0066] Cinnamic acid derivatives:
[0067] Examples of suitable cinnamic acid derivatives include, but are not limited to, ethylhexyl methoxycinnamate, isopropyl methoxycinnamate, isoamyl methoxycinnamate, DEA methoxycinnamate, diisopropyl methylcinnamate, dimethoxycinnamate glyceryl ethylhexanoate.
[0068] Dibenzoylmethane derivatives:
[0069] Examples of suitable dibenzoylmethane derivatives include, but are not limited to, butyl methoxydibenzoylmethane and isopropyl dibenzoylmethane.
[0070] Salicylic acid derivatives:
[0071] Examples of suitable salicylic acid derivatives include, but are not limited to, trimethicone salicylate, ethylhexyl salicylate, dipropylene glycol salicylate, and TEA salicylate.
[0072] β,β-Diphenylacrylate derivatives:
[0073] Examples of suitable β,β-diphenylacrylate derivatives include, but are not limited to, octocrylene and etocrylene.
[0074] Benzophenone derivatives:
[0075] Examples of suitable benzophenone derivatives include, but are not limited to, benzophenone-1, benzophenone-2, benzophenone-3 or oxybenzone, benzophenone-4, benzophenone-5, benzophenone-6, benzophenone-8, benzophenone-9, benzophenone-12, n-hexyl 2-(4-diethylamino-2-hydroxybenzoyl)benzoate or as a mixture with octyl methoxycinnamate.
[0076] Benzylidene camphor derivatives:
[0077] Examples of suitable benzylidene camphor derivatives include, but are not limited to, manufactured 3-benzylidene camphor, 4-methylbenzylidene camphor, manufactured polyacrylamidomethylbenzylidene camphor.
[0078] Phenylbenzotriazole derivatives:
[0079] Examples of suitable phenylbenzotriazole derivatives include, but are not limited to, drometrizole trisiloxane, methylene bis-benzotriazolyl tetramethylbutyl-phenol or in micronized form as an aqueous dispersion.
[0080] Triazine derivatives:
[0081] Examples of suitable triazine derivatives include, but are not limited to, bis-ethylhexyloxyphenol methoxyphenyl triazine, ethylhexyl triazone, diethylhexyl butyramido triazone, 2,4,6-tris(di-neopentyl 4'-aminobenzylidenemalonate)-s-triazine, 2,4,6-tris(diisobutyl 4'-aminobenzylidenemalonate)-s-triazine, 2,4-bis(di-neopentyl 4'-aminobenzylidenemalonate)-6-(n-butyl 4'-aminobenzoate)-s-triazine, US Pat. No. 6,225,467, patent WO2004 / 085412 (see compounds 6 and 9) or the literature "Symmetrical Triazine Derivatives" IP.COM Journal, IP.COM Inc., West Symmetrical triazine shielding agents described in Henrietta, NY, US (September 2, 2004), especially 2,4,6-tris(biphenyl)-1,3,5-triazine (especially 2,4,6-tris(biphenyl-4-yl)-1,3,5-triazine and 2,4,6-tris(terphenyl)-1,3,5-triazine included in patent applications WO 06 / 035000, WO 06 / 034982, WO 06 / 034991, WO 06 / 035007, WO 2006 / 034992 and WO 2006 / 034985)).
[0082] Anthranilic acid derivatives:
[0083] Examples of suitable anthranilic acid derivatives include, but are not limited to, methyl anthranilate.
[0084] Imidazoline derivatives:
[0085] Examples of suitable imidazoline derivatives include, but are not limited to, ethylhexyl dimethoxybenzylidene dioxoimidazolinium propionate.
[0086] Benzalmalonate derivatives:
[0087] Examples of suitable benzalmalonate derivatives include, but are not limited to, polyorganosiloxanes containing benzalmalonate functional groups, such as polysilicone-15.
[0088] 4,4-Diarylbutadiene derivatives:
[0089] Examples of suitable 4,4-diarylbutadiene derivatives include, but are not limited to, 1-dicarboxy(2,2'-dimethylpropyl)-4,4-diphenyl-butadiene.
[0090] Benzooxazole derivatives:
[0091] Examples of suitable benzoxazole derivatives include, but are not limited to, 2,4-bis[5-(1-dimethylpropyl)benzoxazol-2-yl-(4-phenyl)imino]-6-(2-ethylhexyl)imino-1,3,5-triazine and mixtures thereof.
[0092] Preferably, the oil-soluble organic sunscreen ingredient will be selected from butyl methoxydibenzoylmethane, ethylhexyl salicylate, ethylhexyl triazone, octocrylene, drometrizole trisiloxane, bis-ethylhexyloxyphenol methoxyphenyl triazine and mixtures thereof.
[0093] The oil-soluble organic sunscreen ingredient is preferably present in the composition according to the present invention in an amount of about 3 wt. % to about 25 wt. %, preferably in an amount of about 5 wt. % to about 20 wt. % and most preferably in an amount of about 7 wt. % to about 18 wt. %, based on the total weight of the composition.
[0094] Water-soluble organic sunscreen ingredients
[0095] "Water-soluble organic sunscreen ingredient" means any organic compound for screening UV radiation which is completely soluble or miscible in a liquid aqueous phase in molecular form or which is soluble in a liquid aqueous phase in colloid form, for example in the form of micelles.
[0096] Non-limiting examples of water-soluble organic sunscreen ingredients useful in the present invention include, for example, terephthalylidene dicamphor sulfonic acid, phenylbenzimidazole sulfonic acid, benzophenone-4, aminobenzoic acid (PABA), 4-bis(polyethoxy)-para-aminobenzoic acid polyethoxyethyl ester (PEG-25PABA), camphor benzalkoniummethosulfate, methylene bis-benzotriazolyl tetramethylbutylphenol (Bisoctrizole), phenyl dibenzimidazole tetrasulfonate disodium (Bisdisulizoledisodium) and tris-biphenyl triazine; their derivatives and corresponding salts; naphthalene bisimide derivatives such as those described in European Patent Application EP1990372 A2 (the entire contents of which are incorporated herein by reference); and cinnamamide amine cationic quaternary salts and derivatives such as those described in U.S. Pat. No. 5,601,811 (the entire contents of which are incorporated herein by reference), and mixtures thereof.
[0097] In particular, the salts of the compounds that can be used according to the invention are selected from: salts of alkali metals (e.g. sodium or potassium); salts of alkaline earth metals (e.g. calcium, magnesium or strontium); metal (e.g. zinc, aluminum, manganese or copper) salts; ammonium salts of formula NH4+; quaternary ammonium salts; salts of organic amines, such as methylamine, dimethylamine, trimethylamine, triethylamine, ethylamine, 2-hydroxyethylamine, bis(2-hydroxyethyl)amine or tris(2-hydroxyethyl)amine; lysine salts or arginine salts. Preferably, a salt selected from sodium salts, potassium salts, magnesium salts, strontium salts, copper salts, manganese salts or zinc salts is used. Preferably, a sodium salt is used.
[0098] Preferably, the water-soluble organic sunscreen ingredient will be selected from terephthalylidene dicamphor sulfonic acid, methylene bis-benzotriazolyl tetramethylbutylphenol and mixtures thereof.
[0099] The water-soluble organic sunscreen ingredient is preferably present in the composition according to the present invention in an amount of about 0.1 wt. % to about 10 wt. %, preferably in an amount of about 0.5 wt. % to about 8 wt. % and most preferably in an amount of about 1 wt. % to about 7 wt. %, based on the total weight of the composition.
[0100] Silica-encapsulated titanium dioxide sunscreen ingredient
[0101] "Silica-encapsulated titanium dioxide sunscreen ingredient" means spherical beads formed by encapsulating titanium dioxide particles in silica.
[0102] Non-limiting examples of silica-encapsulated titanium dioxide sunscreen ingredients useful in the present invention include, for example, titanium dioxide encapsulated with silica, such as the name Silica (and) Titanium Dioxide, having a silica:titanium dioxide composition of about 55:45 and a particle size of about 2 microns to about 7 microns.
[0103] The silica-encapsulated titanium dioxide sunscreen ingredient is preferably present in the composition according to the present invention in an amount of about 1 wt % to about 10 wt %, preferably in an amount of about 2 wt % to about 10 wt % and most preferably in an amount of about 5 wt % to about 10 wt %, based on the total weight of the composition.
[0104] Suitable UV filter systems according to the invention include terephthalylidene dicamphor sulfonic acid, octocrylene and butyl methoxydibenzoylmethane sulfonic acid.
[0105] Stabilized polymer systems
[0106] The stabilized polymer system of the present invention comprises xanthan gum, acrylate / acrylic acid C 10-30 Alkyl ester crosspolymer, ammonium acryloyldimethyltaurate / vp copolymer and combinations thereof.
[0107] Other polymers
[0108] In addition to the stabilizing polymer system, the anti-acne sunscreen composition according to the invention may also comprise further polymers.
[0109] Suitable additional polymers of the present invention are selected from rheology modifier polymers and anionic polymers, which may be water soluble or water dispersible at pH 7 and room temperature (25° C.). According to the present invention, suitable polymers of the present invention may be as follows.
[0110] The rheology modifier polymer is pre-neutralized and is preferably selected from taurate polymers. Such polymers contain an ionic monomer portion, 2-acrylamido-2-methylpropanesulfonic acid (AMPS) and an additional less polar monomer portion (vinyl pyrrolidone or beheneth-25 methacrylate). These polymers are used as thickeners and stabilizers for oil-in-water emulsions and form extremely stable emulsions already at low concentrations. In particular, these polymers can be used in combination with almost any oil phase, including silicone oils, hydrocarbons / waxes and ester oils.
[0111] Examples of taurate polymers are acrylates / vinyl isodecanoate crosspolymer (such as Stabylen 30), acrylates / acrylic acid C 10-30 Alkyl esters crosspolymer (such as Pemulen TR1 and TR2), carbomer (Aqua SF-1), ammonium acryloyldimethyltaurate / VP copolymer (such as Aristoflex AVC), ammonium acryloyldimethyltaurate / beheneth-25 methacrylate crosspolymer (such as Aristoflex HMB), acrylates / ceteth-20 itaconate copolymer (such as Structure 3001), polyacrylamide (such as Sepigel 305), nonionic thickener (such as Aculyn 46), or mixtures thereof.
[0112] Acrylic polymer powders that can be used in the present invention include, for example, acrylic polymer powders such as methyl methacrylate cross-linked polymers.
[0113] Anionic polymers can be polymers with anionic groups distributed along the polymer backbone. The anionic groups can include carboxylates, sulfonates, sulfates, phosphates, nitrates or other negatively charged or ionizable groups, which can be arranged as pendant groups of the backbone or can be incorporated into the backbone itself.
[0114] The anionic polymer may comprise at least one ethylenically unsaturated carboxylic acid type hydrophilic unit and at least one exclusively unsaturated carboxylic acid (C 10 -C 30)Alkyl ester type hydrophobic unit.
[0115] In certain exemplary and non-limiting embodiments, the copolymer is selected from copolymers produced by polymerization of:
[0116] (1) at least one monomer of formula (I):
[0117] CH 2 =CH(R 1 )COOH (I)
[0118] Where R 1 Selected from H or CH 3 or C 2 H 5 , providing acrylic acid, methacrylic acid or ethacrylic acid monomers, and
[0119] (2) at least one unsaturated carboxylic acid (C 10 -C 30 ) Alkyl ester type monomer (corresponding to the monomer of formula (II)):
[0120] CH 2 =CH(R 2 )COOR 3 (II)
[0121] For example, unsaturated carboxylic acid (C 10 -C 30 ) Non-limiting examples of alkyl esters are selected from lauryl acrylate, stearyl acrylate, decyl acrylate, isodecyl acrylate, dodecyl acrylate and the corresponding methacrylates, such as lauryl methacrylate, stearyl methacrylate, decyl methacrylate, isodecyl methacrylate and dodecyl methacrylate, and mixtures thereof.
[0122] In addition, the cross-linked polymer can be selected according to another exemplary embodiment. For example, such a polymer can be selected from a polymer produced by polymerization of a mixture of monomers, the monomers comprising:
[0123] (1) Acrylic acid,
[0124] (2) an ester of the above formula (II), wherein R2 is selected from H or CH3, R3 represents an alkyl group having 12 to 22 carbon atoms, and
[0125] (3) A crosslinking agent which is a well-known copolymerizable polyethylenically unsaturated monomer such as diallyl phthalate, allyl (meth)acrylate, divinylbenzene, (poly)ethylene glycol dimethacrylate and methylenebisacrylamide.
[0126] For example, you can choose acrylate / acrylic C 10 -C30 Alkyl Esters Copolymer (INCI name: Acrylates / Acrylate C 10-30 Alkyl ester crosspolymers), such as the products PEMULEN TR1, PEMULEN TR2, CARBOPOL 1382 and CARBOPOL EDT 2020.
[0127] Anionic polymers useful herein include, for example: polyacrylic acid; polymethacrylic acid; parboxyvinyl polymer; acrylate copolymers, such as acrylate / acrylic acid C 10-30 Alkyl ester crosspolymer, acrylic acid / vinyl ester copolymer / acrylates ninyl isodecanoate crosspolymer, acrylates / palmeth-25 acrylate copolymer, acrylates / steareth-20 itaconate copolymer, and acrylates / celeth-20 itaconate copolymer; sulfonate / ester polymers such as polysulfonic acid, sodium polystyrene sulfonate, copolymers of methacrylic acid and acrylamidomethylpropane sulfonic acid, and copolymers of acrylic acid and acrylamidomethylpropane sulfonic acid; carboxymethylcellulose; carboxy guar gum; copolymers of ethylene and maleic acid; and acrylate siloxane polymers. In some cases, anionic polymers include, for example, carbomer and CARBOPOL 980; acrylates / acrylic acid C 10-30 Alkyl ester crosspolymers such as Pemulen TR-1, PEMULEN TR-2, CARBOPOL 1342, CARBOPOL 1382 and CARBOPOL ETD 2020; sodium carboxymethylcellulose such as the CMC series; and acrylate copolymers such as Capigel; acrylate copolymers such as CARBOPOL Aqua SF-1 as an aqueous dispersion, acrylate crosspolymer-4 such as CARBOPOL Aqua SF-2 as an aqueous dispersion.
[0128] In one embodiment, the anionic polymer of the present invention is a carbomer, such as CARBOPOL 980. Exemplary nonionic polymers can be shown below:
[0129] (i) Hydroxyethylcellulose, for example the products NATROSOL 250HHR PC or NATROSOL 250HHR CS;
[0130] (ii) cellulose modified with groups comprising at least one fatty chain; examples that may be mentioned include:
[0131] - with a group containing at least one fatty chain (such as an alkyl, arylalkyl or alkylaryl group, or a mixture thereof, wherein the alkyl group is preferably C 8 -C 22 ) modified hydroxyethyl cellulose, such as the product NATROSOLPlus Grade 330CS (C 16 alkyl), or the product BERMOCOLL EHM 100; methyl hydroxyethyl cellulose; methyl ethyl hydroxyethyl cellulose, known as the product STRUCTURE CEL 8000M; or hydroxypropyl cellulose, known as the product KLUCEL MFPHARM hydroxypropyl cellulose;
[0132] - hydroxyethylcellulose modified with alkylphenyl polyalkylene glycol ether groups, such as the product Amercell polymer HM-1500 (nonylphenyl polyethylene glycol (15) ether); or
[0133] (iii) Hydroxypropyl guar, such as hydroxypropyl guar and hydroxypropyl guar modified with groups containing at least one fatty chain, such as the product Esaflor HM 22 (C 22 Alkyl chain), and product RE210-18 (C 14 Alkyl chain) and RE205-1(C 20 alkyl chain).
[0134] pigment
[0135] The anti-acne sunscreen composition of the present invention may further comprise a pigment. Suitable pigments for use in the sunscreen composition of the present invention may be coated or uncoated.
[0136] Coated pigments are pigments that have been surface treated with compounds of one or more chemical, electronic, mechanochemical and / or mechanical properties, such as, for example, those described in Cosmetics & Toiletries, February 1990, Vol. 105, pp. 53-64, such as amino acids, beeswax, fatty acids, fatty alcohols, anionic surfactants, lecithin, sodium, potassium, zinc, iron or aluminum salts of fatty acids, (titanium or aluminum) metal alkoxides, polyethylene, siloxanes, proteins (collagen, elastin), alkanolamines, silicon oxides, metal oxides or sodium hexametaphosphate.
[0137] More particularly, the coated pigment is titanium oxide coated with silica (such as the product silica and iron oxide, silica and alumina), alumina (such as the product alumina and aluminum stearate, alumina and aluminum laurate), iron oxide and iron stearate, zinc oxide and zinc stearate, silica, alumina and siloxane, silica, alumina, aluminum stearate and siloxane, alumina and siloxane, and the like.
[0138] Mention may also be made of mixtures of metal oxides, in particular titanium dioxide and ceria, including silica-coated equal weight mixtures of titanium dioxide and ceria, and also mixtures of alumina-silica-coated and siloxane-coated titanium dioxide and zinc dioxide, or mixtures of alumina-coated, silica-coated and glycerol-coated titanium dioxide and zinc dioxide.
[0139] Additionally, uncoated titanium oxides, zinc oxides, and cerium oxides may be used in the sunscreen compositions of the present invention.
[0140] Additional Ingredients
[0141] In addition to the essential components described above, the compositions of the present invention may also contain any conventional cosmetically acceptable ingredients, which may be chosen, among others, from such agents as additional sunscreens, fragrances / fragrances, preservatives, solvents, active ingredients, surfactants, fatty compounds, vitamins, fillers, silicones, pigments, buffers, masking agents and mixtures thereof.
[0142] A person skilled in the art will take care to choose the optional further ingredients and / or their amounts such that the advantageous properties of the composition according to the invention are not or not substantially adversely affected by the envisaged addition.
[0143] Non-limiting examples of preservatives that may be used in accordance with the present invention include phenoxyethanol.
[0144] As examples of oil-absorbing fillers, suitable fillers for the present invention may be: mica, silica, kaolin, corn (corn) starch, magnesium oxide, nylon-12, nylon-66, cellulose, polyethylene, talc, talc (and) methicone, talc (and) dimethicone, perlite, sodium silicate, pumice, PTFE, polymethyl methacrylate, rice (rice) starch, aluminum starch octenylsuccinate, modified potato starch, alumina, silica silylate, sodium calcium borosilicate, magnesium carbonate, hydrated silica, dimethicone / vinyl dimethicone crosspolymer, sodium carboxymethyl starch.
[0145] Additionally, the compositions of the present invention may contain polymer fillers, such as polylactic acid.
[0146] Non-limiting suitable fatty compounds of the present invention include isononyl isononanoate, diisopropyl sebacate, isopropyl n-lauroyl sarcosinate, and stearyl alcohol.
[0147] Suitable solvents include, but are not limited to, water, alcohols, glycols and polyols, such as glycerol, water, caprylyl glycol, pentylene glycol, propylene glycol, butylene glycol, benzoic acid C 12-15 Alkyl esters and mixtures thereof.
[0148] In various embodiments, the solvent is present in a concentration of about 15 wt % to 100 wt %, or about 20 wt % to about 80 wt %, or about 30 wt % to about 70 wt %, or about 35 wt % to about 75 wt %, or preferably about 40 wt % to about 70 wt % and more preferably about 45 wt % to about 65 wt %, including ranges and sub-ranges therebetween, based on the total weight of the combinations and / or compositions of the present disclosure.
[0149] Suitable additional active ingredients include, but are not limited to, disodium EDTA, triethanolamine, and mixtures thereof.
[0150] Non-limiting examples of additional surfactants suitable for use are fatty acids, glycerides other than glyceryl stearate, alkoxylated fatty alcohols such as stearic acid, laureth-12, laureth-21, glyceryl isostearate, disodium stearoyl glutamate, potassium cetyl phosphate, poloxamer 338, sodium methyl stearoyl taurate, and mixtures thereof.
[0151] Exemplary fat or oil materials include, but are not limited to, esters, fatty acids, synthetic oils, and hydrocarbons / paraffins, such as stearyl alcohol, myristic acid, palmitic acid, silicones, mineral oils, vegetable / vegetable oils, and mixtures thereof.
[0152] Non-limiting examples of vitamins suitable for use in the compositions of the present invention include tocopherol.
[0153] Examples of silicones useful in the compositions of the present invention are, but are not limited to, dimethicone and caprylylmethicone.
[0154] The additional ingredients may comprise 60 to 85 wt%, such as 60 to 82 wt% or such as 65 to 80 wt% of the total weight of the composition of the invention.
[0155] Method for preparing anti-acne sunscreen composition
[0156] The stability of complex systems containing large amounts of sunscreen filters can be easily affected by acidic active ingredients. In order to ensure the stability of the emulsion, the anti-acne active ingredients must be included in the formulation in the correct sequence.
[0157] The anti-acne sunscreen composition according to the present invention (Examples 2 and 8) can be obtained as follows:
[0158] Step (A): adding oil phase;
[0159] Step (B): heating to 75°C;
[0160] Step (C): mixing thoroughly;
[0161] Step (D): adding an oily active ingredient (at least one additional anti-acne ingredient);
[0162] Step (E): mixing thoroughly;
[0163] Step (F): Add TiO 2 ;
[0164] Step (G): mixing thoroughly;
[0165] Step (H): transfer of secondary phase B (aqueous phase) - 10 minutes;
[0166] Step (I): emulsification;
[0167] Step (J): gelation - adding a stabilizing polymer system;
[0168] Step (K): adding phase E (neutralization);
[0169] Step (L): mixing thoroughly;
[0170] Step (M): Check pH (and adjust if necessary): pH target ≥ 6.0;
[0171] Step (N): adding phase F (filler);
[0172] Step (O): Mix thoroughly until uniform;
[0173] Step (P): adding phase G (filter);
[0174] Step (Q): mixing thoroughly;
[0175] Step (R): Add phase H (salicylic acid + alcohol)
[0176] Step (S): mixing thoroughly;
[0177] Step (T): The batch ends.
[0178] Example
[0179] By way of non-limiting illustration, the invention will now be described with reference to the following examples.
[0180] Examples 1 to 7
[0181] As shown below, suitable compositions according to the prior art are such as Example 1 (ie, EX.1), and suitable compositions according to the present invention are such as Examples 2 to 7 (ie, EX.2 to EX.7):
[0182] Table 1 - Compositions of the prior art and the present invention
[0183]
[0184]
[0185] Example 8
[0186] Stability test
[0187] In order to demonstrate the stability of the composition according to the invention, a test was carried out with the composition of Example 3 (invention), wherein the composition was analyzed after 1 month and 2 months at specific temperatures (room temperature, 4° C. and 45° C.). The aspects analyzed were appearance, viscosity, pH, microscopy under non-polarized light and microscopy under polarized light, and the results after 1 and 2 months were compared with the composition after preparation ( FIG. 1( a) ).
[0188] The results for the composition of the present invention showed perfect ingredient stability, with no phase separation after 1 month at room temperature, 4°C, and 45°C (Figure 1(b)). No phase separation was observed after 2 months at room temperature, 4°C, and 45°C (Figure 1(c)).
[0189] Example 9
[0190] Sun Protection Factor
[0191] To evaluate the sun protection factor (SPF) of the compositions according to the invention, tests were carried out with the compositions of Examples 2, 3 and 7 (according to the invention).
[0192] According to the selected method and evaluation criteria, in order to determine the SPF, the product is 2mg / cm 2 SPF when applied.
[0193] The sun protection factor is calculated as the ratio of the minimum erythema dose (MEDp) obtained when the product is used to the minimum erythema dose (MEDu) obtained when the product is not used.
[0194] SPF=MEDp / MEDu
[0195] The minimum erythema dose was defined as the energy required to produce the first perceptible, well-defined redness reaction with clear boundaries, assessed 16 to 24 hours after exposure to the solar simulator with 6 UV escalation doses (15% progression). Testing was performed on at least 10 subjects to meet statistical criteria.
[0196] Based on the test results, it was concluded that the anti-acne sunscreen composition of Example 2 had an average SPF of 65.2. In addition, the anti-acne sunscreen composition of Example 3 exhibited an average SPF of 48.3.
[0197] The composition of Example 7 exhibited an average SPF of 100.5.
[0198] Example 10
[0199] Sensory test
[0200] In order to evaluate the sensory properties (dry feel to the touch, less oily feel and less residue), sensory tests were carried out with a composition according to the prior art (Example 1) and with a composition according to the invention (Example 3).
[0201] The compositions of Example 1 and Example 3 were each applied to half of the face of 6 volunteers having combination to oily skin. The application evaluation was performed immediately and 4 hours after the product application.
[0202] Both products were easy to apply and absorb. The texture of the composition of Example 1 was smoother, waxy and slightly greasy. The same product exhibited cuddles during application by 3 volunteers. Without an immediate effect (visual 2 minutes), the composition of Example 3 produced a more uniform visual effect, with a matte visual effect, dry touch and a more comfortable feel.
[0203] After a period of 4 hours, the composition of Example 3 leaves the skin softer, drier and more pleasant to the touch. In visual analysis, the results between the two compositions are very close, both with good lightness control. The composition of Example 1 exhibits rubbing mud after the hand gesture of the volunteer.
[0204] The results show that the composition according to the invention (Example 3) has improved visual and tactile results when compared to the prior art (Example 1).
[0205] Embodiment 11
[0206] Process for preparing a composition according to the prior art
[0207] A non-limiting example of preparing the compositions according to Examples 2 to 7 can be shown below:
[0208] Step (A): adding oil phase;
[0209] Step (B): heating to 75°C;
[0210] Step (C): mixing thoroughly;
[0211] Step (D): adding oily active ingredients (anti-acne ingredients, including salicylic acid);
[0212] Step (E): mixing thoroughly;
[0213] Step (F): Add TiO 2 ;
[0214] Step (G): mixing thoroughly;
[0215] Step (H): transfer phase B (aqueous phase), 10 min;
[0216] Step (I): emulsification;
[0217] Step (J): gelation - adding a stabilizing polymer system;
[0218] Step (K): mixing thoroughly;
[0219] Step (L): adding phase E (neutralization);
[0220] Step (M): mixing thoroughly;
[0221] Step (N): Check pH (and adjust if necessary): pH target ≥ 6.0;
[0222] Step (O): adding phase F (filler);
[0223] Step (P): Mix thoroughly until uniform;
[0224] Step (Q): adding phase G (filter);
[0225] Step (R): mixing thoroughly;
[0226] Step(S): Batch ends.
[0227] An anti-acne sunscreen composition cannot be properly obtained by such a method because the formulation breaks immediately after the gelling step.
[0228] It was also observed that salicylic acid interfered with the stability of the emulsion when salicylic acid was added in step (D).
Claims
1. An anti-acne sunscreen composition, comprising: (a) an anti-acne agent system comprising salicylic acid and at least one additional anti-acne ingredient selected from the group consisting of capryloyl salicylic acid, hydroxyethylpiperazineethanesulfonic acid, octadecenedioic acid, niacinamide, and combinations thereof, wherein the anti-acne agent system is present in an amount of 4.5 wt%, 5 wt%, 5.55 wt%, 5.7 wt%, 5.75 wt%, or 6.8 wt% relative to the total weight of the composition; (b) a UV filter system selected from the group consisting of phenylbenzimidazole sulfonic acid, butyl methoxydibenzoylmethane, titanium dioxide, ethylhexyl triazone, terephthalylidene dicamphor sulfonic acid, octocrylene, trimethylol salicylate, bis-ethylhexyloxyphenol methoxyphenyl triazine, silica (and) titanium dioxide, methylene bis-benzotriazolyl tetramethylbutylphenol (and) polyglyceryl 10 laurate, and combinations thereof; (c) a stabilizing polymer system selected from the group consisting of xanthan gum, acrylates / acrylic acid C 10-30 alkyl ester crosspolymer and ammonium acryloyldimethyltaurate / vp copolymer and combinations thereof, wherein the stabilizing polymer system is present in an amount ranging from 3.1 wt % to 5 wt % based on the total weight of the composition, The anti-acne sunscreen composition exhibits a sun protection factor in the range of 45 to 90.
2. The anti-acne sunscreen composition according to claim 1, wherein the salicylic acid of the anti-acne agent system is present in an amount ranging from 0.25 wt% to 1 wt% based on the total weight of the composition.
3. The anti-acne sunscreen composition of claim 1, wherein the at least one additional anti-acne ingredient of the anti-acne agent system is present in an amount of 4.0 wt%, 4.2 wt%, 4.55 wt%, 4.6 wt%, 5.5 wt% or 6.45 wt% based on the total weight of the composition.
4. The anti-acne sunscreen composition according to claim 1, wherein the UV filter system is present in an amount ranging from 0.1 wt. % to 50 wt. %, based on the total weight of the composition.
5. The anti-acne sunscreen composition of claim 1, wherein the anti-acne sunscreen composition further comprises a cosmetically acceptable ingredient selected from the group consisting of additional sunscreens, fragrances / fragrances, preservatives, solvents, active ingredients, surfactants, fatty compounds, vitamins, fillers, silicones, polymers, pigments, buffers, masking agents, and mixtures thereof.
6. The anti-acne sunscreen composition of claim 1, wherein the anti-acne sunscreen composition exhibits a sun protection factor of 50.
7. The anti-acne sunscreen composition of claim 1, wherein the anti-acne sunscreen composition exhibits a sun protection factor of 60.
8. The anti-acne sunscreen composition of claim 1, wherein the anti-acne sunscreen composition exhibits a sun protection factor of 70.
9. The anti-acne sunscreen composition of claim 1, wherein the anti-acne sunscreen composition exhibits a sun protection factor of 80.
10. The anti-acne sunscreen composition of claim 1, wherein the anti-acne sunscreen composition exhibits a sun protection factor of 90.
11. A method for preparing an anti-acne sunscreen composition, the anti-acne sunscreen composition comprising: (a) an anti-acne agent system comprising salicylic acid and at least one additional anti-acne ingredient selected from the group consisting of capryloyl salicylic acid, hydroxyethylpiperazineethanesulfonic acid, octadecenedioic acid, niacinamide, and combinations thereof, wherein the anti-acne agent system is present in an amount of 4.5 wt%, 5 wt%, 5.55 wt%, 5.7 wt%, 5.75 wt%, or 6.8 wt% relative to the total weight of the composition; (b) a UV filter system selected from the group consisting of phenylbenzimidazole sulfonic acid, butyl methoxydibenzoylmethane, titanium dioxide, ethylhexyl triazone, terephthalylidene dicamphor sulfonic acid, octocrylene, trimethylol salicylate, bis-ethylhexyloxyphenol methoxyphenyl triazine, silica (and) titanium dioxide, methylene bis-benzotriazolyl tetramethylbutylphenol (and) polyglyceryl 10 laurate, and combinations thereof; (c) a stabilizing polymer system selected from the group consisting of xanthan gum, acrylates / C10-30 alkyl acrylate crosspolymer and ammonium acryloyldimethyltaurate / vp copolymer, and combinations thereof, wherein the stabilizing polymer system is present in an amount ranging from 3.1 wt % to 5 wt % based on the total weight of the composition, wherein the anti-acne sunscreen composition exhibits a sun protection factor in the range of 45 to 90, and The method comprises the following steps: Step (A): adding oil phase; Step (B): heating to 75°C; Step (C): mixing thoroughly; Step (D): adding an oily active ingredient (at least one additional anti-acne ingredient); Step (E): mixing thoroughly; Step (F): adding TiO2; Step (G): mixing thoroughly; Step (H): transfer of secondary phase B (aqueous phase) - 10 minutes; Step (I): emulsification; Step (J): gelation - adding a stabilizing polymer system; Step (K): adding phase E (neutralization); Step (L): mixing thoroughly; Step (M): Check pH (and adjust if necessary): pH target ≥ 6.0; Step (N): adding phase F (filler); Step (O): Mix thoroughly until uniform; Step (P): adding phase G (filter); Step (Q): mixing thoroughly; Step (R): Add phase H (salicylic acid + alcohol) Step(s): Mix thoroughly Step (T): The batch ends.
12. Use of an anti-acne sunscreen composition, the anti-acne sunscreen composition comprising: (a) an anti-acne agent system comprising salicylic acid and at least one additional anti-acne ingredient selected from the group consisting of capryloyl salicylic acid, hydroxyethylpiperazineethanesulfonic acid, octadecenedioic acid, niacinamide, and combinations thereof, wherein the anti-acne agent system is present in an amount of 4.5 wt%, 5 wt%, 5.55 wt%, 5.7 wt%, 5.75 wt%, or 6.8 wt% relative to the total weight of the composition; (b) a UV filter system selected from the group consisting of phenylbenzimidazole sulfonic acid, butyl methoxydibenzoylmethane, titanium dioxide, ethylhexyl triazone, terephthalylidene dicamphor sulfonic acid, octocrylene, trimethylol salicylate, bis-ethylhexyloxyphenol methoxyphenyl triazine, silica (and) titanium dioxide, methylene bis-benzotriazolyl tetramethylbutylphenol (and) polyglyceryl 10 laurate, and combinations thereof; (c) a stabilizing polymer system selected from the group consisting of xanthan gum, acrylates / C10-30 alkyl acrylate crosspolymer and ammonium acryloyldimethyltaurate / vp copolymer, and combinations thereof, wherein the stabilizing polymer system is present in an amount ranging from 3.1 wt % to 5 wt % based on the total weight of the composition, The use is for preparing a product for use as a sunscreen and anti-acne daily product, wherein the product exhibits a sun protection factor in the range of 45 to 90 to protect the skin from damage by the sun.
13. Use according to claim 12, wherein the use is for the preparation of a product which exhibits easy application, good spreadability, less white film, less shine, which does not melt at high temperatures on the face, has an imperceptible touch, and combines high protection and smoothness of the skin and is stable over time.
