Sunscreen composition
The sunscreen composition with Digupigan A and organic sunscreens enhances UVA and UVB protection, addressing the inadequacies of existing sunscreens by improving sun protection factors.
Patent Information
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- Filing Date
- 2025-09-04
- Publication Date
- 2026-03-26
AI Technical Summary
Existing sunscreens do not provide sufficient protection against UV-A and UV-B radiation, necessitating improved compositions with enhanced sun protection factors.
A sunscreen composition comprising compound A, preferably Digupigan A, and/or its extract, combined with organic sunscreens such as butyl methoxydibenzoylmethane, octyl methoxycinnamate, and phenylbenzimidazole sulfonic acid, to enhance UVA and UVB protection.
The composition provides improved sun protection by increasing UVA and UVB absorption, offering better protection against skin damage and hair damage from UV radiation.
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Abstract
Description
[0001] P0000934W01 CPL
[0002] 1
[0003] SUNSCREEN COMPOSITION
[0004] Field of the Invention
[0005] The present invention relates to a sunscreen composition comprising compound A as defined in
[0006] 5 the present invention and organic sunscreen. It was surprisingly found that the composition is capable of providing improved sun protection.
[0007] Background of the Invention
[0008] Solar radiations include about 5% ultraviolet (UV) radiation, wavelength of which is between 200
[0009] 10 nm and 400 nm. It is further divided into three regions: from 320 to 400 nm (UV-A), 280 to 320 nm (UV-B) and from 200 to 280 nm (UV-C). Substantial portion of UV-C radiation is absorbed by ozone. Scientific studies have indicated that exposure to UV-A and UV-B radiation for short period causes pigmentation, reddening of the skin and localized irritation, whereas continued or prolonged exposure can lead to sunburn, formation of wrinkles and age spots. UV radiation is
[0010] 15 also thought to cause significant damage to hair. Therefore, it is desirable to protect the skin and other keratinous substrates of the human body from the harmful effects of both UV-A and UV-B radiation.
[0011] This is often delivered through personal care compositions e.g. cosmetic compositions, which
[0012] 20 provide protection from ultraviolet (UV) radiation. Organic sunscreens e.g. 4-tert-butyl-4'- methoxydibenzoylmethane (BMDM) absorb the UVA radiation. The ability of a sunscreen to provide protection by absorbing UVA radiation is expressed in terms of UVA protection factor (UVAPF). On the other hand, organic sunscreens, e.g. 2-ethylhexyl 2-cyano-3,3-diphenylacrylate (Octocrylene) and octyl methoxycinnamate (MCX) absorb the UVB radiation. The ability of a
[0013] 25 sunscreen to provide protection by absorbing UVB radiation is expressed in terms of sun protection factor (SPF).
[0014] Despite efforts so far, the present inventors have recognized that there are high needs to provide cosmetic composition with improved sun protection. It was surprisingly found that when including
[0015] 30 compound A of the present invention and / or extract comprising the compound A, with organic sunscreen into a composition, the composition is capable of providing improved sun protection.
[0016] Summary of the Invention
[0017] In a first aspect, the present invention is directed to a sunscreen composition comprising:
[0018] 35 (a) compound A having formula I and / or extract comprising the compound A; P0000934W01 CPL wherein: (i) each Ri is independently selected from hydrogen, Ci-Ce alkyl, substituted Ci-Ce alkyl, hydroxy, and OR4, wherein R4is selected from Ci-Ce alkyl, substituted Ci-Ce alkyl,
[0019] 5 monosaccharide and disaccharide; (ii) each R2and R3is independently selected from hydrogen, Ci-Ce alkyl, substituted Ci-Ce alkyl, monosaccharide, and disaccharide; and (b) organic sunscreen.
[0020] All other aspects of the present invention will more readily become apparent upon considering the detailed description and examples which follow.
[0021] Detailed Description of the Invention
[0022] Except in the examples, or where otherwise explicitly indicated, all numbers in this description indicating amounts of material or conditions of reaction, physical properties of materials and / or
[0023] 15 use may optionally be understood as modified by the word “about”.
[0024] All amounts are by weight of the composition, unless otherwise specified.
[0025] It should be noted that in specifying any range of values, any particular upper value can be associated with any particular lower value.
[0026] For the avoidance of doubt, the word “comprising” is intended to mean “including” but not necessarily “consisting of’ or “composed of’. In other words, the listed steps or options need not be exhaustive.
[0027] 25
[0028] The disclosure of the invention as found herein is to be considered to cover all embodiments as found in the claims as being multiply dependent upon each other irrespective of the fact that claims may be found without multiple dependency or redundancy. P0000934W01 CPL
[0029] Where a feature is disclosed with respect to a particular aspect of the invention (for example a composition of the invention), such disclosure is also to be considered to apply to any other aspect of the invention (for example a method of the invention) mutatis mutandis.
[0030] 5 The compound A according to the present invention has formula I as follows: wherein: (i) each Ri is independently selected from hydrogen, Ci-Ce alkyl, substituted Ci-Ce alkyl, hydroxy, and OR4, wherein R4 is selected from Ci-Ce alkyl, substituted Ci-Ce alkyl, monosaccharide and disaccharide; (ii) each R2 and R3 is independently selected from hydrogen, Ci-Ce alkyl, substituted Ci-Ce alkyl, monosaccharide, and disaccharide.
[0031] Preferably, the compound A has the formula I, wherein: (i) each R1 is independently selected from hydrogen, Ci-Ce alkyl, substituted Ci-Ce alkyl, hydroxy, and OR4, wherein R4 is selected from Ci- Ce alkyl, and substituted Ci-Ce alkyl; (ii) each R2 and R3 is independently selected from hydrogen,
[0032] 15 Ci-Ce alkyl, monosaccharide, and disaccharide.
[0033] More preferably, the compound A has the formula I, wherein: (i) each R1 is independently selected from hydrogen, Ci-Ce alkyl, hydroxy, and OR4, wherein R4 is selected from Ci-Ce alkyl; at least one R1 is hydroxy and at least one R1 is OR4 wherein R4 is selected from Ci-Ce alkyl; (ii) each R2 is independently selected from hydrogen and Ci-Ce alkyl; and (iii), and R3 is monosaccharide or disaccharide.
[0034] Even more preferably, the compound A has the formula I, wherein: (i) one R1 is hydrogen, one R1 is hydroxy, and one R1 is OR4 wherein R4is C1-C3 alkyl; (ii) each R2is independently selected
[0035] 25 from hydrogen, methyl, and ethyl; and (iii), and R3 is monosaccharide, preferably 6-membered ring monosaccharide.
[0036] Preferably, the compound A according to the present invention has formula II as follows: P0000934W01 CPL wherein each R2 and R3 is independently selected from hydrogen, Ci-Ce alkyl, substituted Ci-Ce alkyl, monosaccharide, and disaccharide.
[0037] 5 More preferably, the compound A has formula II, wherein each R2 and R3 is independently selected from hydrogen, Ci-Ce alkyl, and monosaccharide.
[0038] Even more preferably, the compound A has formula II, wherein each R2 is independently selected from hydrogen, Ci-Ce alkyl, and R3 is monosaccharide.
[0039] 10
[0040] Still even more preferably, the compound A has formula II, wherein each R2is independently selected from hydrogen, methyl and ethyl, and R3is 6-membered ring monosaccharide.
[0041] Most preferably, the compound A is digupigan A. Digupigan A has structure (III) as follows:
[0042] Preferably, the extract comprising the compound A is Cortex Lycii radicis (Digupi) extract. Cortex Lycii radicis extract refers to a mixture of compounds extracted from Cortex Lycii radicis. The sunscreen composition thus preferably comprises Cortex Lycii radicis extract and organic
[0043] 20 sunscreen.
[0044] Preferably, the extract is an aqueous extract. The term “aqueous extract” means that the extract is obtained by using water, or water mixing with hydrophilic organic solvent as the solvent for P0000934W01 CPL
[0045] 5 extraction. The hydrophilic organic solvent may be selected from C1-C5 alcohol (including polyalcohol), C3-C6 aliphatic ketone; and C2-C5 polyalcohol. Preferably the hydrophilic organic solvent is selected from ethanol, acetone, ethyl acetate, glycerin, isoprene glycol, butylene glycol or a mixture thereof. However, it is preferable that the extract is obtained by solely using water, or
[0046] 5 water mixing ethanol, acetone and / or glycerin as solvent for extraction. More preferably, the extract is obtained by solely using water. Preferably, the extract is solid at 25°C and atmospheric pressure.
[0047] Preferably, the total amount of compound A including those in the extract is 0.00001 to 10% by weight of the composition, more preferably 0.0001 to 5%, even more preferably 0.003 to 2%, still
[0048] 10 even more preferably 0.005 to 1 % and most preferably 0.01 to 0.5% by weight of the composition.
[0049] Preferably, the amount of extract is 0.00001 to 15% by weight of the composition, more preferably 0.0001 to 8%, even more preferably 0.003 to 3%, still even more preferably 0.005 to 1.5% and most preferably 0.01 to 0.8% by weight of the composition. For sake of clarity, the weight of
[0050] 15 extract in the present invention refers to the weight of extract extracted from the plant. Thus, the extracting solvent is excluded.
[0051] Preferably, the amount of the Cortex Lycii radicis (Digupi) extract is 0.00001 to 15% by weight of the composition, more preferably 0.0001 to 8%, even more preferably 0.003 to 3%, still even
[0052] 20 more preferably 0.005 to 1.5% and most preferably 0.01 to 0.8% by weight of the composition.
[0053] The composition comprises organic sunscreens. Sunscreens are known to absorb UV radiations and protect a surface on to which they are applied. Organic sunscreens that may be used in the present invention may be selected from IIV-A, IIV-B organic sunscreens and mixtures thereof.
[0054] 25 Preferably, the organic sunscreen comprises IIV-B organic sunscreens.
[0055] Suitable organic sunscreens may be selected from the group consisting of 2-hydroxy-4- methoxybenzophenone (known also as Benzophenone- 3), octyldimethyl p-aminobenzoic acid, digalloyltrioleate, 2,2-dihydroxy-4-methoxybenzophenone, ethyl-4-(bis(hydroxypropyl))
[0056] 30 aminobenzoate, 2-ethylhexyl-2-cyano-3,3-diphenylacrylate, ethylhexyl salicylate, glyceryl p- aminobenzoate, 3,3,5-trimethylcyclohexylsalicylate, methyl anthranilate, p-dimethyl- aminobenzoic acid, aminobenzoate, 2-ethylhexyl-p-dimethyl- amino-benzoate, 2- phenylbenzimidazole-5-sulfonic acid, 2-(p-dimethylaminophenyl)-5-sulfonicbenzoxazoic acid, 2- ethylhexyl-p-methoxycinnamate, butylmethoxydibenzoylmethane, bis-ethylhexyloxyphenol
[0057] 35 methoxyphenol triazine 2-hydroxy-4- methoxybenzophenone, octyldimethyl-p-aminobenzoic P0000934W01 CPL
[0058] 6 acid, 4- methylbenzylidene camphor, methylene bis-benzotriazolyl tetramethylbutylphenol, dimethicodiethylbenzal malonate, isoamyl methoxycinnamate, octyl triazone, terephthalidene dicamphor sulfonic acid, homosalate, benzophenone-4, benzophenone-5, and mixtures thereof.
[0059] 5 More preferably, the organic sunscreen comprises butyl methoxydibenzoylmethane, octyl methoxycinnamate, oxybenzone, octocrylene, phenylbenzimidazole sulfonic acid, ethylhexyl salicylate or a mixture thereof. Even more preferably, the organic sunscreen comprises octocrylene, phenylbenzimidazole sulfonic acid, ethylhexyl salicylate or a mixture thereof. Still even more preferably, the organic sunscreen comprises octocrylene, ethylhexyl salicylate or a mixture thereof.
[0060] Alternatively, the organic sunscreen more preferably comprises butyl methoxydibenzoylmethane, octyl methoxycinnamate, oxybenzone, or a mixture thereof. Even more preferably the organic sunscreen comprises octyl methoxycinnamate, oxybenzone, or a mixture thereof.
[0061] 15
[0062] Preferably, the organic sunscreen comprises dibenzoylmethane compound, cinnamate compound, benzophenone compound, diphenylacrylate compound, phenylbenzimidazole compound, salicylate, or mixture thereof. More preferably, the organic sunscreen comprises cinnamate compound, benzophenone compound, diphenylacrylate compound,
[0063] 20 phenylbenzimidazole compound, salicylate, or mixture thereof. More preferably, the organic sunscreen is selected from the group consisting of cinnamate compound, benzophenone compound, or mixture thereof. More preferably and alternatively, the organic sunscreen comprises diphenylacrylate compound, phenylbenzimidazole compound, salicylate or mixture thereof.
[0064] 25
[0065] Dibenzoylmethane compound as used herein typically refers that one or more hydrogen in the benzene ring of dibenzoylmethane is replaced by Ci to Ce alkyl group and / or Ci to Ce alkoxy group. Particular preferred dibenzoylmethane compound is selected from the group consisting of 2-methyldibenzoylmethane, 4-isopropyldibenzoyl-methane, butyl methoxydibenzoylmethane (commercially available as Parsol® 1789 or Avobenzone), 2,4-dimethyldibenzoylmethane, 2,5- dimethyldibenzoylmethane, 4,4'-diisopropyl-dibenzoylmethane, 2-methyl-5- isopropyl-4'- methoxydibenzoylmethane, 2-methyl-5-tert-butyl-4'-methoxy- 5 dibenzoyl methane, 2,4-dimethyl- 4'-methoxy dibenzoylmethane, 2,6-dimethyl- 4-tert-butyl-4'-methoxy-dibenzoylmethane, or mixtures thereof. P0000934W01 CPL
[0066] 7
[0067] Cinnamate compound as used herein typically refers to salt, ester of cinnamic acid, one or more hydrogen in the benzene ring of cinnamic acid is replaced by Ci to C alkyl group and / or Ci to C alkoxy group. Particularly preferred cinnamate compound is selected from octyl methoxycinnamate, ethoxyethyl methoxycinnamate, isoamyl methoxycinnamate, or a mixture
[0068] 5 thereof.
[0069] Benzophenone compound as used herein typically refers to compound having benzophenone structure with at least one hydrogen in the benzene ring of benzophenone is substituted, preferably by hydroxy group or Ci to Ce alkoxy group. Particularly preferred benzophenone
[0070] 10 compound is selected from group consisting of benzophenone-1 , benzophenone-2 benzophenone-3, benzophenone-4 benzophenone-5, benzophenone-6, benzophenone-8, benzophenone-9, benzophenone-12, n-hexyl 2-(4-diethylamino-2-hydroxybenzoyl)benzoate, or a mixture thereof.
[0071] 15 Diphenylacrylate compound as used herein typically refers to salt and / or ester, with or without substitution, of diphenyl acrylic acid, preferably with hydrogen on the acrylic acid substituted by cyano group. Particularly preferred diphenylacrylate compound is octocrylene, etocrylene or a mixture thereof.
[0072] 20 Phenylbenzimidazole compound as used herein typically refers to compound having phenylbenzimidazole structure with at least one hydrogen in the benzene ring of phenylbenzimidazole is substituted, preferably by hydroxy group, Ci to Ce alkoxy group, sulfonic acid group, or sulfonate. Particularly preferred phenylbenzimidazole compound is selected from phenylbenzimidazole sulfonic acid, disodium phenyl dibenzimidazole tetrasulfonate or a mixture
[0073] 25 thereof.
[0074] Salicylate as used herein typically refers to salt or ester of salicylic acid. Particularly preferred salicylate is selected from the group consisting of homosalate, ethylhexyl salicylate, dipropylene glycol salicylate, amyl salicylate, phenyl salicylate, benzyl salicylate, menthyl salicylate, glyceryl
[0075] 30 salicylate, TEA salicylate or a mixture thereof.
[0076] A safe and effective amount of organic sunscreen may be used in the compositions useful in the subject invention. The amount of the organic sunscreen is preferably 0.1% to 30%, more preferably 0.5 to 22%, even more preferably from 1% to 16%, and most preferably 1.5 to 10% of
[0077] 35 by weight of the composition. P0000934W01 CPL
[0078] 8
[0079] Preferably, the weight ratio of the compound A to the organic sunscreen is from 1 :400 to 400:1 , more preferably 1 :200 to 100:1 , even more preferably 1 :50 to 20:1 , still even more preferably 1 :8 to 3: 1. Preferably, the weight ratio of the extract to the organic sunscreen is from 1 :400 to 800: 1 ,
[0080] 5 more preferably 1 :100 to 200:1 , even more preferably 1 :20 to 50:1 , still even more preferably 1 :4 to 20:1 , and most preferably 1 :2 to 15:1. Preferably, the weight ratio of the compound A to the total dibenzoylmethane compound, cinnamate compound, benzophenone compound, diphenylacrylate compound, phenylbenzimidazole compound, and salicylate is from 1 :400 to 400:1 , more preferably 1 :200 to 100:1 , even more preferably 1 :50 to 20:1 , still even more preferably 1 :8 to 3:1. Preferably, the weight ratio of the compound A to the total cinnamate compound, benzophenone compound, diphenylacrylate compound, phenylbenzimidazole compound, and salicylate is from 1 :400 to 400:1 , more preferably 1 :200 to 100:1 , even more preferably 1 :50 to 20:1 , still even more preferably 1 :8 to 3:1. Preferably, the weight ratio of the digupigan A to the total cinnamate compound, benzophenone compound, diphenylacrylate
[0081] 15 compound, phenylbenzimidazole compound, and salicylate is from 1 :400 to 400:1 , more preferably 1 :200 to 100: 1 , even more preferably 1 :50 to 20: 1 , still even more preferably 1 :8 to 3: 1 . Preferably, the weight ratio of the extract to the organic sunscreen is from 1 :400 to 800:1 , more preferably 1 :100 to 200:1 , even more preferably 1 :20 to 50:1 , still even more preferably 1 :4 to 20: 1 , and most preferably 1 :2 to 15:1.
[0082] 20
[0083] Preferably, the total amount of cinnamate compound, benzophenone compound, diphenylacrylate compound, phenylbenzimidazole compound, and salicylate is preferably 0.01 % to 30%, more preferably 0.3 to 20%, even more preferably from 1 % to 14%, and most preferably 1 .5 to 10% of by weight of the composition.
[0084] 25
[0085] Preferably, the sunscreen composition comprises (i) compound A; and (ii) organic sunscreen comprising diphenylacrylate compound, phenylbenzimidazole compound, salicylate or mixture thereof. More preferably, the sunscreen composition comprises (i) compound A; and (ii) diphenylacrylate compound and / or salicylate. Preferably, the weight ratio of the compound A to the total diphenylacrylate compound, phenylbenzimidazole compound and salicylate is from 1 :400 to 400:1 , more preferably 1 :200 to 100:1 , even more preferably 1 :50 to 20:1 , still even more preferably 1 :8 to 3: 1. Preferably, the weight ratio of the compound A to the total diphenylacrylate compound and salicylate is from 1 :400 to 400:1 , more preferably 1 :200 to 100:1 , even more preferably 1 :50 to 20:1 , still even more preferably 1 :8 to 3:1.
[0086] 35 P0000934W01 CPL
[0087] 9
[0088] Alternatively, the sunscreen composition preferably comprises (I) Cortex Lycii radicis extract; and (II) organic sunscreen comprising dibenzoylmethane compound, cinnamate compound, benzophenone compound or a mixture thereof. Even more preferably, the sunscreen composition comprises (I) Cortex Lycii radicis extract; and (ii) organic sunscreen comprising cinnamate
[0089] 5 compound, benzophenone compound, or mixture thereof. Preferably, the weight ratio of the compound A to the total dibenzoylmethane compound, cinnamate compound, and benzophenone compound is from 1 :400 to 400:1 , more preferably 1 :200 to 100:1 , even more preferably 1 :50 to 20:1 , still even more preferably 1 :8 to 3:1. Preferably, the weight ratio of the compound A to the total cinnamate compound and benzophenone compound is from 1 :400 to 400:1 , more preferably 1 :200 to 100:1 , even more preferably 1 :50 to 20:1 , still even more preferably 1 :8 to 3:1. Preferably, the weight ratio of the Cortex Lycii radicis extract to the total cinnamate compound, and benzophenone compound is from 1 :800000 to 1000:1 , more preferably 1 :40000 to 300:1 , even more preferably 1 :2000 to 80:1 , still even more preferably 1 :50 to 20:1.
[0090] 15 Preferably, the total amount of cinnamate compound, and benzophenone compound is preferably 0.01 % to 30%, more preferably 0.3 to 20%, even more preferably from 1% to 14%, and most preferably 1 .5 to 10% of by weight of the composition.
[0091] The composition may comprise substituted resorcinol. Substituted resorcinol typically refers to
[0092] 20 that at least one hydrogen on the ring structure and / or on a hydroxy group of the resorcinol replaced with an alkyl group, phenyl alkyl group, or heterocyclic group. Preferably, the substituted resorcinol is 4-substituted resorcinol. Preferably, the substituted resorcinol is selected from 4- ethyl resorcinol, 4-butyl resorcinol, 4-hexyl resorcinol, phenylethyl resorcinol, thiamidol, or a mixture thereof, more preferably, the substituted resorcinol is selected from 4-ethyl resorcinol, 4-
[0093] 25 butyl resorcinol, 4-hexyl resorcinol, or a mixture thereof and even more preferably, the substituted resorcinol comprises 4-hexyl resorcinol. The amount of the substituted resorcinol is preferably in the range of 0.00001 to 10%, more preferably from 0.001 to 5% and most preferably from 0.1 to 0.6% by weight of the total amount of the composition.
[0094] Preferably, the composition comprises Vitamin B3 compounds (including derivatives of vitamin B3). The vitamin B3 compounds comprises niacin, nicotinic acid, niacinamide or a mixture thereof. The most preferred vitamin B3 compound is niacinamide. Amount of Vitamin B3 compounds may be 0.1 to 10%, preferably 0.5 to 5% by weight of the composition. 2-mercaptonicotinoyl glycine may also be included in the composition. Amount of 2-mercaptonicotinoyl glycine may be 0.0001
[0095] 35 to 10%, preferably 0.01 to 1 % by weight of the composition. P0000934W01 CPL
[0096] 10
[0097] Preferably, the composition comprises a glutamate source selected from the group consisting of glutamine, glutamine ester, glutamic acid, pyroglutamic acid, salts, and mixtures thereof. More preferably, the composition comprises pyroglutamic acid and / or salt of pyroglutamic acid. Even
[0098] 5 more preferably, the composition comprises sodium salt of pyroglutamic acid. Preferably, the glutamate source is present in amount of 0.0001 to 10% by weight of the composition, more preferably 0.001 to 6%, even more preferably 0.01 to 3% by weight of the composition.
[0099] The composition may optionally comprise whitening pigment. Whitening pigments are typically particles of high refractive index materials. For example, the whitening pigment may have a refractive index of greater than 1.3, more preferably greater than 1.8 and most preferably from 2.0 to 2.7. Examples of such whitening pigment are those comprising bismuth oxy-chloride, boron nitride, barium sulfate, mica, silica, titanium dioxide, zirconium oxide, aluminium oxide, zinc oxide or combinations thereof. More preferred whitening pigment are particles comprising titanium
[0100] 15 dioxide, zinc oxide, zirconium oxide, mica, iron oxide or a combination thereof. Even more preferred whitening pigment are particles comprising zinc oxide, zirconium oxide, titanium dioxide or a combination thereof as these materials have especially high refractive index. Still even more preferably the whitening pigment is selected from titanium dioxide, zinc oxide or a mixture thereof and most preferred whitening pigment is titanium dioxide. The average diameter of whitening
[0101] 20 pigment is typical from 15 nm to 1 micron, more preferably from 35 nm to 800 nm, even more preferably from 50 nm to 500 nm and still even more preferably from 100 to 300 nm. Amount of whitening pigment may be 0.1 to 15%, preferably 0.5 to 5% by weight of the composition.
[0102] Preferably, the composition comprises polyhydric alcohol. Polyhydric alcohols may be selected
[0103] 25 from group of glycerin, propylyene glycol, dipropylene glycol, polypropylene glycol, polyethylene glycol, sorbitol, hydroxypropyl sorbitol, hexylene glycol, 1 ,3-butylene glycol, isoprene glycol, ethoxylated glycerol, propoxylated glycerol or a mixture thereof. Most preferred polyhydric alcohol is glycerol known also as glycerin. The amount of polyhydric alcohol may range anywhere from 0.1 to 20%, preferably 0.5 to 15% and more preferably 2 and 10% by weight of the composition.
[0104] Preferably, the composition comprises emollient materials. Suitable emollient materials include silicones, hydrocarbons, triglycerides or a mixture thereof. These silicones may be organic, silicone-containing or fluorine-containing, volatile or non-volatile, polar or non-polar. Hydrocarbons may include mineral oil, petrolatum and polyalpha-olefins. Examples of preferred
[0105] 35 volatile hydrocarbons include polydecanes such as isododecane and isodecane (e.g. Permethyl- P0000934W01 CPL
[0106] 11
[0107] 99A which is available from Presperse Inc.) and the C7-C8 through C12-C15 isoparaffins (such as the Isopar Series available from Exxon Chemicals). Illustrative triglycerides but not limiting are sunflower seed oil, cotton oil, canola oil, soybean oil, castor oil, borage oil, olive oil, shea butter, jojoba oil and mixtures thereof. Mono- and di- glycerides may also be useful. Particularly
[0108] 5 preferable are glyceryl monostearate and glyceryl distearate.
[0109] Preferably, the composition comprises moisturizing agents. Particularly preferred moisturizing agents includes, petrolatum, aquaporin manipulating actives, oat kernel flour, substituted urea like hydroxyethyl urea, hyaluronic acid and / or its precursor N-acetyl glucosamine, hyaluronic acid and / or its precursor N-acetyl glucosamine, or a mixture thereof.
[0110] Some compositions may include thickeners. These may be selected from cellulosics, natural gums and acrylic polymers but not limited by this thickening agent types. Among the cellulosics are sodium carboxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl methylcellulose and
[0111] 15 combinations thereof. Suitable gums include xanthan, pectin, karaya, agar, alginate gums and combinations thereof. Among the acrylic thickeners are homopolymers and copolymers of acrylic and methacrylic acids including carbomers such as Carbopol 1382, Carbopol 982, llltrez, Aqua SF-1 and Aqua SF-2 available from the Lubrizol Corporation. Amounts of thickener may range from 0.01 to 3% by weight of the active polymer (outside of solvent or water) in the compositions.
[0112] 20
[0113] In addition, the compositions of the invention may further include 0.5 to 10% by weight of sequestering agents, such as tetra sodium ethylenediaminetetraacetate (EDTA), EHDP or mixtures; opacifiers and pearlizers such as ethylene glycol distearate, titanium dioxide or Lytron 621 (Styrene / Acrylate copolymer); all of which are useful in enhancing the appearance or
[0114] 25 properties of the product.
[0115] The composition may comprise water in amount of 10 to 96% by weight of the composition, more preferably from 25 to 92%, even more preferably from 42 to 88%, most preferably from 55 to 82% by weight of the composition.
[0116] 30
[0117] Preferably, the composition has a viscosity of at least 10 mPa s, more preferably in the range 30 to 10000 mPa s, even more preferably 50 to 5000 mPa s, and most preferably 100 to 2000 mPa s, when measured at 20 degrees C at a relatively high shear rate of about 20 s-1. P0000934W01 CPL
[0118] 12
[0119] Preferably, the composition is an emulsion, more preferably an oil-in-water emulsion. Preferably the composition is a fluid liquid at 25 °C and atmospheric pressure.
[0120] Preferably, the composition is an emulsion, more preferably an oil-in-water emulsion. Preferably,
[0121] 5 the composition is a skin care composition. The skin care composition refers to a composition suitable for topical application to human skin, including leave-on and wash-off products but preferably leave-on compositions. The term “leave-on” as used with reference to compositions herein means a composition that is applied to or rubbed on the skin and left thereon. The term “wash-off” as used with reference to compositions herein means a skin cleanser that is applied to or rubbed on the skin and rinsed off substantially immediately subsequent to application. Preferably the composition is a fluid liquid, and particularly a moisturizer rather than a make-up product. The term "skin" as used herein includes the skin on the face, neck, chest, abdomen, back, arms, under arms, hands, and legs. Preferably “skin” means includes the skin on the face and under arms, more preferably skin means skin on the face other than lips and eyelids.
[0122] 15
[0123] Preferably, the composition is a topical composition. Preferably, the composition may be in the form of cream, lotion, ointment, solution, suspension, emulsion, paste, gel, powder, powder foundation, emulsion foundation, wax foundation, or spray. More preferably, the composition may be formulated in the form of cream, lotion, ointment, emulsion, gel, or a spray.
[0124] 20
[0125] Preferably the use is non-therapeutic. Preferably the method is non-therapeutic. The term non- therapeutic typically means for cosmetic purposes and not curative or therapeutic purposes.
[0126] The following examples are provided to facilitate an understanding of the invention. The examples
[0127] 25 are not intended to limit the scope of the claims.
[0128] Example 1
[0129] This example demonstrates that Digupigan A is capable of providing improved sun protection of sunscreen.
[0130] The samples were solved in methanol with amount according to in Table 1. The UV-Vis spectra of the dissolved samples were measured and recorded on Agilent Cary Series UV-VIS Spectrophotometer using 1 cm quartz cell with scanning wavelength from 200 nm to 600 nm. The
[0131] 35 UVA and UVB absorption for the samples were calculated by the integration of the UV spectrum P0000934W01 CPL
[0132] 13 in the range of 280 nm to 400. The results were shown in Table 1 . The improvement refers to the increase compared with the samples having no Digupigan A.
[0133] 5 Table 1
[0134] As evident in Table 1 , the inclusion of Digupigan A provided an improved sun protection effect to the sunscreens.
[0135] 10 Example 2
[0136] This example demonstrates that Digupi extract is also capable of providing improved sun protection of sunscreen.
[0137] The Digupi extract was prepared by following process. Digupi, procured from Juyaotang Herbal Medicine Co., Ltd, were mixed by water with amount of ten times of Digupi. The mixture was boiled under reflux for two hours. Then, the residue was filtered. Then the extract solution was freeze-dried till all water was removed to obtain the Digupi extract.
[0138] The UVA and UVB absorption were tested by following the same procedure as described in
[0139] 20 Example 1 except the samples of Table 2 were tested. P0000934W01 CPL
[0140] 14
[0141] Table 2
[0142] As evident in Table 2, the inclusion of Digupi extract also provided an improved sun protection 5 effect to the sunscreens.
Claims
P0000934W01 CPL15Claims1. A sunscreen composition comprising:(a) compound A having formula I and / or extract comprising the compound A;wherein: (i) each Ri is independently selected from hydrogen, Ci-Ce alkyl, substituted Ci-Ce alkyl, hydroxyl, and OR4, wherein R4 is selected from Ci-Ce alkyl, substituted Ci-Ce alkyl, monosaccharide and disaccharide; (ii) each R2 and R3 is independently selected from hydrogen, Ci-Ce alkyl, substituted Ci-Ce alkyl, monosaccharide, and disaccharide; and (b) organic sunscreen, wherein the organic sunscreen comprises cinnamate compound, benzophenone compound, diphenylacrylate compound, phenylbenzimidazole compound, salicylate or mixture thereof, and the amount of the organic sunscreen is 0.1 % to 30% by weight of the composition.
2. The composition according to claim 1 wherein the compound A has the formula I, wherein: (i) each R1 is independently selected from hydrogen, Ci-Ce alkyl, hydroxy, and OR4, wherein R4 is selected from Ci-Ce alkyl; at least one R1 is hydroxy and at least one R1 is OR4 wherein R4 is selected from Ci-Ce alkyl; (ii) each R2 is independently selected from hydrogen and Ci-Ce alkyl; and (iii), and R3 is monosaccharide or disaccharide.
3. The composition according to claim 1 or 2 wherein the compound A has formula II as follows:wherein each R2 and R3 is independently selected from hydrogen, Ci-Ce alkyl, substituted Ci- Ce alkyl, monosaccharide, and disaccharide.P0000934W01 CPL164. The composition according to any one of the preceding claims wherein the compound A has formula II, wherein each R2 and R3 is independently selected from hydrogen, Ci-Ce alkyl, and monosaccharide.
5. The composition according to any one of the preceding claims wherein the compound A is digupigan A.
6. The composition according to any one of the preceding claims wherein the extract is Cortex Lycii radicis extract.
7. The composition according to any one of the preceding claims wherein the total amount of compound A is 0.00001 to 10% by weight of the composition, preferably 0.003 to 2% by weight of the composition.
8. The composition according to any one of the preceding claims wherein the organic sunscreens may be selected from the group consisting of 2-hydroxy-4- methoxybenzophenone (known also as Benzophenone-3), octyldimethyl p-aminobenzoic acid, digalloyltrioleate, 2,2-dihydroxy-4-methoxybenzophenone, ethyl-4-(bis(hydroxypropyl)) aminobenzoate, 2-ethylhexyl-2-cyano-3,3-diphenylacrylate, ethylhexyl salicylate, glyceryl p- aminobenzoate, 3,3,5-trimethylcyclohexylsalicylate, methyl anthranilate, p-dimethyl- aminobenzoic acid, aminobenzoate, 2-ethylhexyl-p-dimethyl- amino-benzoate, 2- phenylbenzimidazole-5-sulfonic acid, 2-(p-dimethylaminophenyl)-5-sulfonicbenzoxazoic acid, 2-ethylhexyl-p-methoxycinnamate, butylmethoxydibenzoylmethane, bisethylhexyloxyphenol methoxyphenol triazine 2-hydroxy-4- methoxybenzophenone, octyldimethyl-p-aminobenzoic acid, 4- methylbenzylidene camphor, methylene bis- benzotriazolyl tetramethylbutylphenol, dimethicodiethylbenzal malonate, isoamyl methoxycinnamate, octyl triazone, terephthalidene dicamphor sulfonic acid, homosalate, benzophenone-4, benzophenone-5, or mixtures thereof.
9. The composition according to any one of the preceding claims wherein the organic sunscreen comprises cinnamate compound, benzophenone compound, or mixture thereof.
10. The composition according to any one of the preceding claims wherein the amount of the organic sunscreen is from 1 % to 16% by weight of the composition.P0000934W01 CPL1711 . The composition according to any one of the preceding claims wherein the weight ratio of the compound A to the organic sunscreen is from 1 :400 to 400:1 , preferably 1 :50 to 20:1.
12. A sunscreen composition comprising Cortex Lycii radicis extract and organic sunscreen, wherein the organic sunscreen comprises cinnamate compound, benzophenone compound, diphenylacrylate compound, phenylbenzimidazole compound, salicylate or mixture thereof, and the amount of the organic sunscreen is 0.1 % to 30% by weight of the composition.
13. The composition according to claim 12 wherein the organic sunscreen comprises dibenzoylmethane compound, cinnamate compound, benzophenone compound, or mixture thereof.
Citation Information
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