Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/55—Phosphorus compounds
  • A61K8/553—Phospholipids, e.g. lecithin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
  • A61K8/73—Polysaccharides
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
  • A61K8/73—Polysaccharides
  • A61K8/731—Cellulose; Quaternized cellulose derivatives
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
  • A61K8/73—Polysaccharides
  • A61K8/737—Galactomannans, e.g. guar; Derivatives thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
  • A61K8/81—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
  • A61K8/8129—Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by an alcohol, ether, aldehydo, ketonic, acetal or ketal radical; Compositions of hydrolysed polymers or esters of unsaturated alcohols with saturated carboxylic acids; Compositions of derivatives of such polymers, e.g. polyvinylmethylether
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
  • A61K8/81—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
  • A61K8/817—Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by a single or double bond to nitrogen or by a heterocyclic ring containing nitrogen; Compositions or derivatives of such polymers, e.g. vinylimidazol, vinylcaprolactame, allylamines (Polyquaternium 6)
  • A61K8/8176—Homopolymers of N-vinyl-pyrrolidones. Compositions of derivatives of such polymers
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
  • A61K2800/26—Optical properties
  • A61K2800/262—Transparent; Translucent
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
  • A61K2800/54—Polymers characterized by specific structures/properties
  • A61K2800/542—Polymers characterized by specific structures/properties characterized by the charge
  • A61K2800/5422—Polymers characterized by specific structures/properties characterized by the charge nonionic

Definitions

• the present invention relates to a transparent composition.
• it relates to a transparent composition for moisturizing the skin.
• Phospholipids are known in cosmetics and/or pharmaceuticals, as ingredients which provide moisture retaining of skin. Such phospholipids includes ingredients derived from natural sources and synthetic ingredients. Recently, phospholipids has been useful in various formulation, particularly in emulsion (aqueous composition), due to the structural properties as emulsifying agents and/or solubilizing agents. But phospholipid containing compositions that feel less greasy on the consumer's skin may be unacceptable to consumers because they are less spreadable and do not feel as "rich” when applied to the skin. In addition, due to their property as emulsifying agents, the phospholipids are commonly used in compositions that are not transparent.
• the present invention is directed to a transparent composition
• a transparent composition comprising a phospholipid, a water-soluble nonionic polymer, an oily component, and a cosmetically-acceptable carrier, wherein the concentration of the water-soluble nonionic polymer is less than 2.0% by weight of the composition.
• compositions containing the specified ingredients are useful for topical application and for providing improved transparency and spreadability of products and good skin feel such as moisturizing the skin without greasy feeling to skin.
• composition of the present invention is stable in storage even at high temperature (about 40 degC).
• topical application means to apply or spread a material onto the surface of the skin.
• cosmetically-acceptable carrier means one or more compatible dermatologically-acceptable solid or liquid filler diluents or encapsulating substances.
• compositions or components thereof so described are suitable for use in contact with human skin without undue toxicity, incompatibility, instability, irritation allergic response, and the like, commensurate with a reasonable benefit/risk ratio.
• safety and effective amount means an amount of a compound or composition sufficient to significantly induce a positive benefit, preferably a positive skin appearance or feel benefit, including independently the benefits disclosed herein, but low enough to avoid serious side effects, i.e., to provide a reasonable benefit to risk ratio, within the scope of sound judgment of the skilled artisan.
• mixtures is meant to include a simple combination of materials and any compounds that may result from their combination.
• compositions comprising a phospholipid, a water-soluble nonionic polymer, an oily component, and a cosmetically-acceptable carrier.
• transparent composition means that the composition has transparency sufficient to see the other side when the composition is in a clear glass or plastic bottle which has about 1cm of diameter.
• the transparent composition of the present invention has an apparent viscosity of from about 2 to about 10,000 centipoise (cps), preferably from about 3 to about 500 cps of viscosity, more preferably from about 4 to about 200 cps.
• Such viscosity can be determined using a CJV 5000 Viscometer (AND, Tokyo, Japan). The viscosity is determined on the composition after the composition has been allowed to stabilize following its preparation, generally at least 24 hours under conditions of 25°C +/- 1 °C and ambient pressure after preparation of the composition. Viscosity is measured with the composition at a temperature of 25°C +/- 1 °C.
• the transparent composition of the present invention contains a phospholipid component.
• a phospholipid component generally known as amphiphilic surfactant derived from natural sources, tends to emulsify and/or solubilize a composition with water and/or oils, due to being an amphiphilic component.
• Nonlimiting examples of phospholipids useful herein includes synthetic phospholipids such as dialloylphosphatidylcholine and dipalmitoyl phosphatidylcholine, phosphatidylcholine, phosphatidylinositol, phosphatidylethanolamine, phosphatidylserine, and sphingomyelin; natural phospholipds include egg yolk lecithin and soybean lecithin extracted from egg yolk and soybean.
• the phospholipid used herein is lecithin. More specifically, “Lecithin” is 1 ,2-diacyl-sn-glycero-3-phosphocholone and derivatives thereof, which does not mean a “lecithin” as a group which are commercially and industrially available phospholipids.
• the phospholipid component is present in the composition from about from about 0.05% to about 5.0%, preferably from about 0.1% to about 1.0%.
• the transparent composition of the present invention contains a water- soluble nonionic polymer.
• the water-soluble nonionic polymer herein is primarily a thickening agent. Without intending to be limited by theory, it is believed that anionic or cationic water-soluble polymers tend to interact with the phospholipids of this invention, resulting in an emulsion. Consequently, the emulsified composition is no longer transparent.
• the water-soluble polymer described below can be provided in the form of both solid and liquid.
• the liquid form of the polymer may be provided in a water solution.
• the water solution is also transparent.
• the concentration of the water-soluble nonionic polymer is less than 2.0% by weight of the composition, preferably from about 0.01 % to about 2.0 %.
• Water-soluble nonionic polymers useful herein include polysaccharides, gums, polyacrylamide, and mixtures thereof. Extract materials which are derived from natural sources (e.g., locust bean gum) can be included as water-soluble polymeric thickening agent. Locust bean gum is available from Pentapharm Ltd, (Basel, Switzerland).
• polysaccharides refers to water-soluble nonionic polymers containing a backbone of a repeating mono saccharide (i.e., carbohydrate) units.
• polysaccharides include those selected from the group consisting of cellulose, hydroxyethylcellulose, hydroxyethyl ethylcellulose, hydroxypropylcellulose, hydroxypropyl methylcellulose, methyl hydroxyethylcellulose, and mixtures thereof. Also useful herein are the alkyl substituted celluloses.
• the hydroxy groups of the cellulose polymer is hydroxyalkylated (preferably hydroxyethylated or hydroxypropylated) to form a hydroxyalkylated cellulose which is then further modified with a C-
• these polymers are ethers of C ⁇ o-30 straight or branched chain alcohols with hydroxyalkylcelluloses.
• alkyl groups useful herein include those selected from the group consisting of stearyl, isostearyl, lauryi, myristyl, cetyl, isocetyl, cocoyl (i.e., alkyl groups derived from the alcohols of coconut oil), palmityl, oleyl, linoleyl, linolenyl, ricinoleyl, behenyl, and mixtures thereof.
• Preferred water-soluble nonionic polymers are hydroxyethylcellulose and cetyl hydroxyethylcellulose.
• Gums useful herein include materials which are primarily derived from natural sources. Examples of these gums include materials selected from the group consisting of amylopectin, amylose, dextrin, guar gum, hydroxypropyl guar, konjac mannan, locust bean gum, pullulan, sclerotium gum, tamarind seed gum, and mixtures thereof; preferably locust bean gum, pullulan, sclerotium gum, and termarind seed gum. Purified gums are preferable.
• Polvacrylamide Polymers Polyacrylamide polymers are also useful. Such nonionic polyacrylamide polymers include substituted branched or unbranched polymers.
• polymers can be formed from a variety of monomers including acrylamide and methacrylamide which are unsubstituted or substituted with one or two alkyl groups (preferably C ⁇ .5).
• Preferred are acrylate amide and methacrylate amide monomers in which the amide nitrogen is unsubstituted, or substituted with one or two C-j.s alkyl groups (preferably methyl, ethyl, or propyl), for example, acrylamide, methacrylamide, N- methacrylamide, N-methylmethacrylamide, N,N-dimethylmethacrylamide, N- isopropylacrylamide, N-isopropylmethacrylamide, and N,N-dimethylacrylamide.
• Crosslinked poly(N-vinylpyrrolidones) useful herein include those described in US Patent No. 5,139,770, Shih et al. issued August 18, 1992, and US Patent No. 5,073,614, Shih et al. issued December 17, 1991 , both patents of which are incorporated by reference herein in their entirety.
• Such crosslinked poly(N-vinylpyrrolidones) typically contain from about 0.25% to about 1 % by weight of a crosslinking agent selected from the group consisting of divinyl ethers and diallyl ethers of terminal diols containing from about 2 to about 12 carbon atoms, divinyl ethers and diallyl ethers of polyethylene giycols containing from about 2 to about 600 units, dienes having from about 6 to about 20 carbon atoms, divinyl benzene, vinyl and allyl ethers of pentaerythritol, and the like.
• a crosslinking agent selected from the group consisting of divinyl ethers and diallyl ethers of terminal diols containing from about 2 to about 12 carbon atoms, divinyl ethers and diallyl ethers of polyethylene giycols containing from about 2 to about 600 units, dienes having from about 6 to about 20 carbon atoms, divinyl benzene
• these gelling agents typically have a viscosity from about 25,000 cps to about 40,000 cps when measured as a 5% aqueous solution at 25°C using a Brookfield RVT viscometer with Spindle #6 at 10 rpm.
• Commercially available examples of these polymers include ACP-1120, ACP-1179, and ACP-1180, available from International Specialty Products (Wayne, NJ).
• the transparent composition of the present invention contains an oily component.
• the oily component is used as an emollient.
• the oily component is present in the composition from about 0.05% to about 15.0%, preferably from about 0.1 % to about 8.0%.
• the level of the oily component depends on the desired form of the composition, such as a lotion or a gel.
• the concentration of the oily component may be higher than in a low viscosity composition.
• low viscosity compositions e.g., lotion
• High viscosity compositions e.g., gel
• oily component is a mixture of two or more of the oily components described below.
• suitable oily components include:
• Mineral oil which is also known as petrolatum liquid, is a mixture of liquid hydrocarbons obtained from petroleum. See The Merck Index, Tenth Edition, Entry 7048, p. 1033 (1983) and International Cosmetic Ingredient Dictionary, Fifth Edition, vol. 1 , p.415-417 (1993), which are incorporated by reference herein in their entirety.
• Petrolatum which is also known as petroleum jelly, is a colloidal system of nonstraight-chain solid hydrocarbons and high-boiling liquid hydrocarbons, in which most of the liquid hydrocarbons are held inside the micelles. See The Merck Index, Tenth Edition, Entry 7047, p. 1033 (1983); Schindler, Drug. Cosmet. Ind., 89, 36-37, 76, 78-80, 82 (1961 ); and International Cosmetic Ingredient Dictionary, Fifth Edition, vol. 1 , p. 537 (1993), which are incorporated by reference herein in their entirety.
• (iiO Straight and branched chain hydrocarbons having from about 7 to about 40 carbon atoms include dodecane, isododecane, squalane, cholesterol, hydrogenated polyisobutylene, docosane (i.e., a C-22 hydrocarbon), hexadecane, isohexadecane (a commercially available hydrocarbon sold as Permethyl® 101 A by Presperse, South Plainfield, NJ). Also useful are the C7.40 isoparaffins, which are 07.40 branched hydrocarbons.
• Nonlimiting examples include diisopropyl sebacate, diisopropyl adipate, isopropyl myristate, isopropyl palmitate, methyl paimitate, myristyl propionate, 2-ethylhexyl palmitate, isodecyl neopentanoate, di-2-ethylhexyl maleate, cetyl palmitate, myristyl my state, stearyl stearate, isopropyl stearate, methyl stearate, cetyl stearate, behenyl behenate, dioctyl maleate, dioctyl sebacate, diisopropyl adipate, cetyl octanoate, diisopropyl dilinoleate.
• .C3Q carboxylic acids For example, ethylene glycol mono- and di- esters, and propylene giycol mono- and di- esters of C-I-3Q carboxylic acids e.g., ethylene glycol distearate.
• (viO C ⁇ _3Q mono- and polv- esters of sugars and related materials These esters are derived from a sugar or polyol moiety and one or more carboxylic acid moieties. Depending on the constituent acid and sugar, these esters can be in either liquid or solid form at room temperature. The ester materials are further described in, US Patent No.
• vegetable oils and hydrogenated vegetable oils include safflower oil, castor oil, coconut oil, cottonseed oil, menhaden oil, palm kernel oil, palm oil, peanut oil, soybean oil, rapeseed oil, linseed oil, rice bran oil, pine oil, sesame oil, sunflower seed oil, hydrogenated safflower oil, hydrogenated castor oil, hydrogenated coconut oil, hydrogenated cottonseed oil, hydrogenated menhaden oil, hydrogenated palm kernel oil, hydrogenated palm oil, hydrogenated peanut oil, hydrogenated soybean oil, hydrogenated rapeseed oil, hydrogenated linseed oil, hydrogenated rice bran oil, hydrogenated sesame oil, hydrogenated sunflower seed oil, and mixtures thereof.
• the transparent compositions of the present invention contain a cosmetically-acceptable carrier.
• the carrier can include a polyhydric alcohol and/or water solvent; preferably water.
• the composition contains from about 60% to about 99.8% of the carrier, preferably from about 80% to about 99.5%.
• the carrier includes water and lower alkyl alcohols.
• Lower alkyl alcohols useful herein are C- ⁇ alkyl monohydric alcohols; preferably C2-3 alkyl alcohols.
• Preferred lower alkyl alcohols include ethyl alcohol, isopropyl alcohol, and mixtures thereof.
• Preferred polyhydric alcohols useful herein include, but are not limited to, polyalkylene glycols, more preferably alkylene polyols and their derivatives including glycerin, propylene glycol, dipropylene glycol, tripropylene glycol, polyethylene glycol and derivatives thereof, sorbitol, hydroxypropyl sorbitol, erythritol, threitol, pentaerythritol, xylitol, glucitol, mannitol, hexylene glycol, 1 ,3- butylene glycol, 1 ,2,6-hexanetriol, glycerol, ethoxylated glycerol, propoxylated glycerol, soluble collagen, gelatin, and mixtures thereof.
• Preferred moisturizing agents are glycerin, 1 ,3-butylene glycol, glucose, trimethylglycine, urea, or mixtures thereof; more preferably
• Optional Components may further comprises optional components.
• optional components means one or more compatible solid or liquid fillers, diluents, extenders and the like, which are commonly used in cosmetics as defined herein.
• compatible herein means that the components of the compositions of this invention are capable of being commingled with each other, in a manner such that there is no interaction which would substantially reduce the efficacy of the composition under ordinary use situations.
• the optional components useful herein include an active and inactive components.
• the type of the optional components utilized in the present invention depend on the type of product desired and may comprise several types of carriers including, but not limited to, oil-in-water or water-in-oil emulsions. 1 ) Actives
• the optional components useful herein may comprise active components.
• actives include, but are not limited to, a vitamin B3 compound, anti-oxidants and radical scavengers, anti-inflammatory agents, antimicrobial agents, sunscreens and sunblocks, and chelators.
• Other actives useful herein include vitamin A (e.g., retinoid which is commercially available from a number of sources, for example, Sigma Chemical Company (St.
• Vitamin B3 compounds enhance skin appearance by improving skin condition, including treating signs of skin aging, more especially wrinkles, lines, and pores. Vitamin B3 compounds are preferably present from about 0.01% to about 50%, more preferably from about 0.1% to about 10%, even more preferably from about 0.5% to about 10%, and still more preferably from about 1 % to about 5%.
• Vitamin B3 compound means a compound having the formula:
• R is -CONH2 (e.g., niacinamide), -CH2OH (e.g., nicotinyl alcohol); and derivatives thereof.
• Exemplary derivatives of the foregoing vitamin B3 compounds include nicotinic acid esters, including non-vasodilating esters of nicotinic acid, nicotinyl amino acids, nicotinyl alcohol esters of carboxylic acids, nicotinic acid N-oxide and niacinamide N-oxide.
• Suitable esters of nicotinic acid include nicotinic acid esters of from 1 to about 22 carbons, preferably 1 to about 16 carbons, more preferably alcohols from about 1 to about 6 carbons.
• the alcohols are suitably straight-chain or branched chain, cyclic or acyclic, saturated or unsaturated (including aromatic), and substituted or unsubstituted.
• the esters are preferably non-vasodilating.
• non-vasodilating means that the ester does not commonly yield a visible flushing response after application to the skin in the subject compositions (the majority of the general population would not experience a visible flushing response, although such compounds may cause vasodilation not visible to the naked eye, i.e., the ester is non-rubifacient).
• Non-vasodilating esters of nicotinic acid include tocopherol nicotinate and inositol hexanicotinate; tocopherol nicotinate is preferred.
• derivatives of the vitamin B3 compound are derivatives of niacinamide resulting from substitution of one or more of the amide group hydrogens.
• Nonlimiting examples of derivatives of niacinamide useful herein include nicotinyl amino acids, derived, for example, from the reaction of an activated nicotinic acid compound (e.g., nicotinic acid azide or nicotinyl chloride) with an amino acid, and nicotinyl alcohol esters of organic carboxylic acids (e.g.,
• 8)- Specific examples of such derivatives include nicotinuric acid (C8H8N2O3) and nicotinyl hydroxamic acid (C6H6N2O2), which have the following chemical structures: nicotinuric acid:
• nicotinyl alcohol esters include nicotinyl alcohol esters of the carboxylic acids salicylic acid, acetic acid, glycolic acid, palmitic acid and the like.
• vitamin B3 compounds useful herein are 2- chloronicotinamide, 6-aminonicotinamide, 6-methylnicotinamide, n-methyl- nicotinamide, n,n-diethylnicotinamide, n-(hydroxymethyl)-nicotinamide, quinolinic acid imide, nicotinanilide, n-benzylnicotinamide, n-ethylnicotinamide, nifenazone, nicotinaldehyde, isonicotinic acid, methyl isonicotinic acid, thionicotinamide, niaiamide, 1-(3-pyridylmethyl) urea, 2-mercaptonicotinic acid, nicomol, and
• Nonlimiting examples of the above vitamin B3 compounds are well known in the art and are commercially available from a number of sources, e.g., the Sigma Chemical Company (St. Louis, MO); ICN Biomedicals, Inc. (Irvin, CA) and Aldrich Chemical Company (Milwaukee, Wl).
• One or more vitamin B3 compounds may be used herein.
• Preferred vitamin B3 compounds are niacinamide and tocopherol nicotinate. Niacinamide is more preferred.
• salts, derivatives, and salt derivatives of niacinamide are preferably those having substantially the same efficacy as niacinamide in the methods of regulating skin condition described herein.
• Salts of the vitamin B3 compound are also useful herein.
• Nonlimiting examples of salts of the vitamin B3 compound useful herein include organic or inorganic salts, such as inorganic salts with anionic inorganic species (e.g., chloride, bromide, iodide, carbonate, preferably chloride), and organic carboxylic acid salts (including mono-, di- and tri- C ⁇
• anionic inorganic species e.g., chloride, bromide, iodide, carbonate, preferably chloride
• organic carboxylic acid salts including mono-, di- and tri- C ⁇
• Wenner "The Reaction of L-Ascorbic and D-losascorbic Acid with Nicotinic Acid and Its Amide", J. Organic Chemistry, Vol. 14, 22-26 (1949). Wenner describes the synthesis of the ascorbic acid salt of niacinamide.
• the ring nitrogen of the vitamin B3 compound is substantially chemically free (e.g., unbound and/or unhindered), or after delivery to the skin becomes substantially chemically free ("chemically free” is hereinafter alternatively referred to as "uncomplexed”). More preferably, the vitamin B3 compound is essentially uncomplexed. Therefore, if the composition contains the vitamin B3 compound in a salt or otherwise complexed form, such complex is preferably substantially reversible, more preferably essentially reversible, upon delivery of the composition to the skin. For example, such complex should be substantially reversible at a pH of from about 5.0 to about 6.0. Such reversibility can be readily determined by one having ordinary skill in the art.
• the vitamin B3 compound is substantially uncomplexed in the composition prior to delivery to the skin.
• Exemplary approaches to minimizing or preventing the formation of undesirable complexes include omission of materials which form substantially irreversible or other complexes with the vitamin B3 compound, pH adjustment, ionic strength adjustment, the use of surfactants, and formulating wherein the vitamin B3 compound and materials which complex therewith are in different phases. Such approaches are well within the level of ordinary skill in the art.
• the vitamin B3 compound contains a limited amount of the salt form and is more preferably substantially free of salts of a vitamin B3 compound.
• the vitamin B3 compound contains less than about 50% of such salt, and is more preferably essentially free of the salt form.
• the vitamin B3 compound in the compositions hereof having a pH of from about 4 to about 7 typically contain less than about 50% of the salt.
• the vitamin B3 compound may be included as the substantially pure material, or as an extract obtained by suitable physical and/or chemical isolation from natural (e.g., plant) sources.
• the vitamin B3 compound is preferably substantially pure, more preferably essentially pure.
• Anti-oxidants and radical scavengers are especially useful for providing protection against UV radiation which can cause increased scaling or texture changes in the stratum corneum and against other environmental agents which can cause skin damage.
• Anti-oxidants and radical scavengers such as tocopherol (vitamin E), tocopherol sorbate, tocopherol acetate, other esters of tocopherol, propyl gallate, alkyl esters of uric acid, amines (i.e., N,N-diethylhydroxylamine, amino- guanidine), sulfhydryl compounds (i.e., glutathione), lycine pidolate, arginine pilolate, bioflavonoids, lysine, methionine, praline, superoxide dismutase, silymarin, tea extracts, grape skin/seed extracts, melanin, and rosemary extracts may be used.
• tocopherol vitamin E
• tocopherol sorbate tocopherol acetate
• other esters of tocopherol propyl gallate
• alkyl esters of uric acid amines (i.e., N,N-diethyl
• Preferred anti-oxidants/radical scavengers are selected from tocopherol sorbate and other esters of tocopherol, more preferably tocopherol sorbate.
• tocopherol sorbate for example, the use of tocopherol sorbate in topical compositions and applicable to the present invention is described in U.S. Patent 4,847,071 , Bissett et al, issued July 11 , 1989.
• Anti-lnflammatorv Agents Anti-inflammatory agents enhance the skin appearance benefits, by for example, contribution of uniformity and acceptable skin tone and/or color.
• the anti-inflammatory agent includes a steroidal anti- inflammatory agent and an non-steroidal anti-inflammatory agent.
• Preferred steroidal anti-inflammatory for use is hydrocortisone.
• Such agents may suitably be obtained as an extract by suitable physical and/or chemical isolation from natural sources (i.e., plants, fungi, by-products of microorganisms).
• natural sources i.e., plants, fungi, by-products of microorganisms.
• alpha bisabolol, aloe vera, Manjistha (extracted from plants in the genus Rubia, particularly Rubia Cordifolia), and Guggal (extracted from plants in the genus Commiphora, particularly Commiphora Mukul), kola extract, chamomile, and sea whip extract may be used.
• Antimicrobial agents means a compound capable of destroying microbes, preventing the development of microbes or preventing the pathogenic action of microbes. Antimicrobal agents are useful, for example, in controlling acne.
• Preferred antimicrobial agents useful in the present invention are benzoyl peroxide, erythromycin, tetracycline, clindamycin, azelaic acid, sulfur resorcinol phenoxyethanol, and IrgasanTM DP 300 (Ciba Geigy Corp., U.S.A.).
• a safe and effective amount of an antimicrobial agent may be added to compositions of the present invention, preferably from about 0.001% to about 10%, more preferably from about 0.01% to about 5%, still more preferably from about 0.05% to about 2%.
• Sunscreens and Sunblocks generally prevent excessive scaling and texture changes of the stratum corneum by exposure of ultraviolet light and may be added to the composition of the present invention. Suitable sunscreens and sunblocks may be organic.
• sunscreens and sunblocks which are useful in the compositions are those selected from 2-ethylhexyl-p-methoxycinnamate (commercially available as PARSOL MCX), butylmethoxydibenzoyl-methane, 2- hydroxy-4-methoxybenzo-phenone, octocrylene, oxybenzone, homomenthyl salicylate, octyl salicylate, 4,4'-methoxy-t-butyldibenzoylmethane, 4-isopropyl dibenzoylmethane, 3-benzylidene camphor, 3-(4-methylbenzylidene) camphor, EusolexTM 6300, Octocrylene, Parsol 1789, and mixtures thereof.
• 2-ethylhexyl-p-methoxycinnamate commercially available as PARSOL MCX
• butylmethoxydibenzoyl-methane 2- hydroxy-4-methoxybenzo
• sunscreens and sunblocks such as those disclosed in U.S. Patent 4,937,370, Sabatelli, issued June 26, 1990, and U.S. Patent 4,999,186, Sabatelli, issued March 12, 1991.
• the sunscreens and sunblocks disclosed therein have, in a single molecular, two distinct chromophore moieties which exhibit different ultraviolet radiation absorption spectra.
• One of the chromophore moieties absorbs predominantly in the UVB radiation range and the other absorbs strongly in the UVA radiation range.
• These sunscreens and sunblocks provide higher efficacy, broader UV absorption, lower skin penetration and longer lasting efficacy relative to conventional sunscreens and sunblocks.
• SPF Sun Protection Factor
• chelator refers to a compound that reacts for removing a metal ion from a system by forming a complex so that the metal ion cannot readily participate in or catalyze chemical reactions.
• the inclusion of a chelator is especially useful for providing protection against UV radiation which can contribute to excessive scaling or skin texture changes and against other environmental agents which can cause skin damage.
• chelators that are useful herein are disclosed in U.S. Patent 5,487,884, Bissett et al, issued January 30, 1996; PCT application 91/16035 and 91/16034, Bush et al, published October 31 , 1995.
• Preferred chelators are furildioxime and derivatives thereof.
• composition of the present invention may further include preservatives and preservative enhancers such as water-soluble or solubiiizable preservatives including Germall 115, methyl, ethyl, propyl and butyl esters of hydroxybenzoic acid, benzyl alcohol, EDTA, Bronopol (2-bromo-2-nitropropane-1 ,3-diol), phenoxyethanpl, and phenoxypropanol; antifoaming agents; binders; biological additives; bulking agents; coloring agents; perfumes, essential oils, and solubiiizers thereof; natural extracts; compounds which stimulate collagen production.
• preservatives and preservative enhancers such as water-soluble or solubiiizable preservatives including Germall 115, methyl, ethyl, propyl and butyl esters of hydroxybenzoic acid, benzyl alcohol, EDTA, Bronopol (2-bromo-2-nitropropane-1
• compositions of the present invention are generally prepared by any method conventionally used for providing skin care compositions, particularly for skin lotions, that are known in the art. Such methods typically involve mixing of the ingredients in one or more steps to a relatively uniform state, with or without heating, cooling, and the like. Typical methods are described in, for example are described in Harry's Cosmeticology, 7th Ed., Harry & Wilkinson (Hill Publishers, London 1982).
• compositions above described are suitably made as follows:
• phase B ingredients to phase A mixture and mix at about 70-75°C.
• phase C additive phase C into mixture of phase A-B at about 70-75°C.
• the oil-in-water transparent composition comprising lecithin, water-soluble nonionic polymer, and oily component herein provide improved transparency and spreadability of products and good skin feel such as moisturizing the skin without greasy feeling to skin.

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• 1999
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