Classifications

• • 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
  • A61K8/67—Vitamins
• • 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
  • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
  • A61K8/29—Titanium; Compounds 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
  • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
  • A61K8/11—Encapsulated compositions
• • 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
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/34—Alcohols
  • A61K8/342—Alcohols having more than seven atoms in an unbroken chain
• • 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
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/39—Derivatives containing from 2 to 10 oxyalkylene groups
• • 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
  • A61K8/67—Vitamins
  • A61K8/673—Vitamin B group
  • A61K8/675—Vitamin B3 or vitamin B3 active, e.g. nicotinamide, nicotinic acid, nicotinyl aldehyde
• • 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
  • A61K8/67—Vitamins
  • A61K8/676—Ascorbic acid, i.e. vitamin C
• • 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
  • A61K8/84—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
  • A61K8/86—Polyethers
• • 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
  • A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
• • 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
  • A61K2800/41—Particular ingredients further characterized by their size
  • A61K2800/412—Microsized, i.e. having sizes between 0.1 and 100 microns

Definitions

• the present invention relates to a topical composition.
• it relates to a topical skin lightening composition.
• Rough and/or broken skin and hyperpigmentations are areas consumers typically seek to treat. Skin lightening is of particular interest in certain Asian populations.
• UV rays Irradiation of ultra-violet (UV) rays tends to cause sun-burning, resulting in skin darkening and/or hyperpigmentation. It is generally known that conditions which result in defective or missing tyrosinase, an enzyme involved in the formation of melanin, lead to hyperpigmentation, e.g. albinism.
• the irradiation of UV rays as a consequence of exposure to sunlight promotes a melanin complex formation in melanocytes located in the basal layer of the epidermis. Melanin is subsequently released from the dendrites of the melanocytes, then diffused to keratinocytes, resulting in hyperpigmentation of the skin.
• hyperpigmentation may take the form of spots, freckles, blotches, unwelcome general darkening and/or unevenness of the basal skin.
• a wide variety of compounds and/or ingredients e.g., ascorbic acid and derivatives thereof, kojic acid and derivatives thereof, hydroquinone, arbutine, and a variety of extracts such as glycyrrhiza, are known and are commonly- available for skin-lightening use.
• hi-tech synthetic ingredients useful for skin-lightning are also available in a wide variety and array of product forms.
• L-ascorbic acids e.g., Vitamin C
• Vitamin C a compound that is useful ingredients as skin-lightening and/or evenness agents as well as a reductant, UV-absorbent and melanin- formation inhibitor in cosmetics.
• L-ascorbic acid tends to be unstable in formulation, resulting in imparting a (undesirable) yellowish color to the composition which may eventually become brownish. This may lead deterioration of a product value.
• the present invention is directed to a composition
• a composition comprising: (a) an ascorbic acid compound; (b) a charged, reflective particulate material;
• skin lightening refers altering the appearance of the skin to a brighter, lighter, and/or whiter appearance, and improving hyperpigmentation as compared to pre-treatment.
• compositions or components thereof so described are suitable for use in contact with human skin without undue toxicity, incompatibility, instability, allergic response, and the like.
• 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, e.g., 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.
• ingredients such as actives and other ingredients useful herein may be categorized or described by their cosmetic and/or therapeutic benefit or their postulated mode of action. However, it is to be understood that the active and other ingredients useful herein can, in some instances, provide more than one cosmetic and/or therapeutic benefit or operate via more than one mode of action. Therefore, classifications herein are made for the sake of convenience and are not intended to limit an ingredient to the particularly stated application or applications listed.
• the present invention is directed to a composition
• a composition comprising an ascorbic acid compound, a charged, reflective particulate material, a structuring compound, and a cosmetically-acceptable carrier.
• an ascorbic acid compound provides promotion of cell respiration, enzyme activation and anti-oxidation.
• topical application of the ascorbic acid compound tends to reduce oxidized melanin complex itself and its precursors, as well as inhibit tyrosinase activity in the melanosome. Consequently, it is also believed that compositions containing the ascorbic acid compound can provide skin benefits such as the prevention of melanin production and the reduction of age spots, blotches and/or freckles associated with skin hyperpigmentation.
• compositions having such increased levels of ascorbic acid tend to be unstable, particularly uneatable in physical properties, such as product appearance changing to yellow or brown.
• a structuring compound in a composition can sustain the original physical properties of an ascorbic acid compound and the composition thereof, even when the composition contains relatively high levels of the ascorbic acid compound. Such improvement of stability is particularly effective in an aqueous composition.
• composition of the . present invention includes an ascorbic acid compound.
• the ascorbic acid compound is selected depending upon its compatibility with the other ingredients.
• the ascorbic acid compound may be included as a substantially pure material, for example, which may be an extract obtained by suitable physical and/or chemical isolation from natural (e.g., plant) sources.
• composition of the present invention preferably contains from about 1.0% to about 10.0% of the ascorbic acid compound, more preferably from about 2.0% to about 5.0%.
• ascorbic acid compound means ascorbic acid or derivatives thereof which have the formula (I):
• V and W are independently -OH; R 1 is - CH(OH)-CH2OH; and salts thereof.
• the ascorbic acid compound useful herein is an ascorbic acid salt or derivative thereof, such as the non-toxic alkali metal, alkaline earth metal and ammonium salts commonly known by those skilled in the art including, but not limited to, the sodium, potassium, lithium, calcium, magnesium, barium, ammonium and protamine salts which are prepared by methods well known in the art.
• an ascorbic acid salt or derivative thereof such as the non-toxic alkali metal, alkaline earth metal and ammonium salts commonly known by those skilled in the art including, but not limited to, the sodium, potassium, lithium, calcium, magnesium, barium, ammonium and protamine salts which are prepared by methods well known in the art.
• the ascorbic acid salt useful herein is a metal ascorbate having the following formula (II):
• R2 and R ⁇ are independently selected from hydrogen and linear or branched alkyl of 1 to about 8 carbons; M ⁇ is a metal; and x is an integer of from 1 to about 3. More preferably, R2 and R3 are independently selected from hydrogen and linear or branched alkyl of 1 to about 3 carbons; M ⁇ is sodium, potassium, magnesium, or calcium.
• Examples of other preferred ascorbic acid salts having formula (II) include monovalent metal salts (e.g., sodium ascorbate, potassium ascorbate), divalent metal salts (e.g., magnesium ascorbate, calcium ascorbate) and trivelent metal salts (e.g., aluminum ascorbate) of ascorbic acid.
• monovalent metal salts e.g., sodium ascorbate, potassium ascorbate
• divalent metal salts e.g., magnesium ascorbate, calcium ascorbate
• trivelent metal salts e.g., aluminum ascorbate
• the ascorbic acid salt useful herein is a water soluble ascorbyl ester having the following formula (III):
• A is sulfate or phosphate; R ⁇ and R ⁇ are independently selected from hydrogen and linear or branched alkyl of 1 to about 8 carbons; M2 is a metal; and y is an integer of 1 to about 3. More preferably, R 4 and R5 are independently selected from hydrogen and linear or branched alkyl of 1 to about 3 carbons; M ⁇ is sodium, potassium, magnesium, or calcium.
• Exemplary water soluble salt derivatives include, but are not limited to, L- ascorbyl phosphate ester salts such as sodium L-ascorbyl phosphate, potassium
• L-ascorbyl phosphate magnesium L-ascorbyl phosphate, calcium L-ascorbyl phosphate, aluminum L-ascorbyl phosphate.
• L-ascorbyl sulfate ester salts can also be used. Examples are sodium L-ascorbyl sulfate, potassium L-ascorbyl sulfate, magnesium L-ascorbyl sulfate, calcium L-ascorbyl sulfate and aluminum
• compositions of the present invention also essentially comprise from about 0.01% to about 5.0%, preferably from about 0.1% to about 5.0%, more preferably from about 0.5% to about 2.0%, by weight of the composition, of a charged, reflective particulate material ("charged material").
• charged material a charged, reflective particulate material
• the charged material preferably comprises a reflective particulate material such as titanium dioxide which is coated with a coating material that confers a net charge that is greater than the zeta potential of the uncoated metallic oxide.
• a reflective particulate material such as titanium dioxide
• Such charged material can be dispersed throughout the carrier.
• reflective particulate materials such as titanium dioxide
• these reflective particulate materials have a tendency to agglomerate, e.g., clump together, resulting in precipitation of the reflective particulate materials.
• the coating material confers a zeta potential that is greater than about ⁇ 20 mV (e.g., either in the positive or negative direction) at pH from about 4 to about 8.5. Further such coating materials provide reflective particulate materials with steric hindrance, resulting in preventing agglomeration of such charged materials. This provides formulation stability and prevents agglomeration of the reflective particulate materials (metallic oxide). Particulates and their charges are well known to those of ordinary skill in the art, and are well described in R.J Hunter, Zeta Potential in Colloid Science: Principles and Application (1981), published by Academic Press; J.N.
• the charged materials all have a net cationic charge or a net anionic charge. It is believed that because all of the particles have the same charge, the repulsive forces prevent agglomeration and induce even distribution throughout the hydrophilic phase. As a result, (i) lower concentrations of the reflective particulate material give maximum visible light reflection in a composition, (ii) aesthetic negative impact such as chalky and gritty feel are not created, and (iii) formulation instabilities are decreased. Thus, the use of charged materials provide efficient coverage at relatively low levels of the charged materials.
• the charged materials useful in the compositions of the present invention will generally have a refractive index of at least about 2, more preferably at least about 2.5, e.g., from about 2 to about 3.
• Refractive index can be determined by conventional methods. For example, a method for determining the refractive index which is applicable to the present invention is described in J. A. Dean, Ed., Lange's Handbook of Chemistry, 14th Ed., McGraw Hill, New York, 1992, Section 9, Refractometry, incorporated herein by reference in its entirety.
• Preferred charged materials are those having an primary particle size of from about 100 nm to about 300 nm, more preferably from about 100 to about 250 nm in the neat form (i.e., in the essentially pure, powder form prior to combination with any carrier). Preferred charged materials have a primary particle size when dispersed in the composition of from about 100 nm to about 1000 nm, more preferably from about 100 nm to about 400 nm, even more preferably from about 200 nm to about 300 nm.
• Primary particle size can be determined using the ASTM Designation E20 - 85 "Standard Practice for Particle Size Analysis of Particulate Substances in the Range of 0.2 to 75 Micrometers by Optical Microscopy", ASTM Volume 14.02, 1993, incorporated herein by reference.
• the particles may have a variety of shapes, including spherical, spheroidal, elliptical, lamellar, irregular, needle and rod-like, provided that the desired refractive index is provided.
• the particulate can be in a variety of physical forms, including rutile, anatase or a combination thereof.
• the reflective particulate material herein is metallic oxide, preferably comprises particles of inorganic material such as titanium dioxide, zinc oxide, zirconium dioxide, aluminum oxide, and combinations thereof, more preferably titanium dioxide, zinc oxide and combinations thereof (combinations are intended to include particles which comprise one or more of these materials, as well as mixtures of these particulate materials) and most preferably, the particles consist essentially of titanium dioxide.
• the reflective particulate material may be a composite, e.g., deposited on a core or mixed with other materials such as, but not limited to, silica, silicone resin, mica, and nylon.
• Inorganic particulate materials e.g., titanium dioxide, zinc oxide, zirconium dioxide, or aluminum oxide are commercially available from a number of sources.
• a suitable particulate material comprises TronoxTM (titanium dioxide series) and SAT-T CR837 (a rutile Titanium dioxide) available from U. S. Cosmetics, titanium dioxide CR-50 available from Ishihara Sangyo Kaisha, and titanium dioxide JA-1 available from Tayca Corporation.
• compositions may contain other inorganic or organic particulate materials.
• particulates in the compositions of the invention consist essentially of the particulate material described in this section.
• Coating Material The reflective particulate materials described hereinbefore are preferably coated with a coating material that confers a net charge that is greater than the zeta potential of the uncoated reflective particulate material. Therefore, any coating material can be used as long as the net charge (cationic or anionic) conferred to the reflective particulate is greater than the untreated reflective particulate material. However, all of the particulates within a composition are preferably treated with the same net charge, e.g., no mixing of cationic and anionic coating materials, to benefit from the repulsive forces between the reflective particulates. It is understood by one skilled in the art, however, that small amounts of oppositely charged coating materials may be used, as long as, the overall repulsive forces are maintained.
• Nonlimiting examples of coating materials that confer a cationic charge include cationic polymers (natural and/or synthetic) and cationic surfactants.
• Preferred cationic coating materials are selected from the group consisting of chitosan, hydroxypropyl chitosan, quaternium-80, polyquaternium-7, and mixtures thereof.
• Nonlimiting examples of coating materials that confer an anionic charge include anionic polymers (natural and/or synthetic) and anionic surfactants.
• Preferred anionic coating materials are selected from the group consisting of ammonium polyacrylate, sodium polyacrylate, potassium polyacrylate, ethylene acrylic acid copolymer, hydrolyzed wheat protein polysiloxane copolymer, dimethicone copolyol phosphate, dimethicone copolyol acetate, dimethicone copolyol laurate, dimethicone copolyol stearate, dimethicone copolyol behenate, dimethicone copolyol isostearate, dimethicone copolyol hydroxystearate, phosphate ester, sodium chondroiton sulfate, sodium hyaluronate, ammonium hyaluronate, sodium algenate, ammonium algenate, ammonium laurate, sodium laurate, potassium
• the charged materials are available in essentially neat, powdered form, or predispersed in various types of carriers, including but not limited to water, organic hydrophilic diluents such as lower monovalent alcohols (e.g., C1.4) and low molecular weight glycols and polyols, including propylene glycol, polyethylene glycol (e.g., Molecular Weight 200-600 g/mole), polypropylene glycol (e.g., Molecular Weight 425-2025 g/mole), glycerol, butylene glycol, 1 ,2,4-butanetriol, sorbitol esters, 1 ,2,6-hexanetriol, ethanol, isopropanol, sorbitol esters, butanediol, ether propanol, ethoxylated ethers, propoxylated ethers and combinations thereof.
• organic hydrophilic diluents such as lower monovalent alcohols (e.g., C1.4) and
• the charged particulate materials are predispersed in water, glycerin, butylene glycol, propylene glycol, and mixtures thereof.
• Examples of commercially available charged particulate materials include Kobo BG60DC (a predispersion of chitosan treated titanium dioxide and butylene glycol), Kobo GLW75CAP (a predispersion of ammonium polyacrylate treated titanium dioxide, water, and glycerin), Kobo GLW75CAP-MP (a predispersion of ammonium polyacrylate treated titanium dioxide, water, glycerin, methylparaben, and propylparaben) all available from Kobo Products Inc., located in South Plainfield, NJ. C. Structuring Compound
• the composition of the present invention comprises a structuring compound.
• structuring compound refers to a compound which forms an organized structure, a gel network system, such that the system can exist in hydrophobic or hydrophilic components. It is believed that the structuring compound assists in providing good rheological characteristics to the composition which contribute to the stability and pleasant aesthetic characteristics of the composition.
• the structuring compound is present from about 1.0% to about 10.0%, more preferably from about 2.0% to about 8.0% in the composition.
• the structuring compound comprises a fatty alcohol and an amphiphilic surfactant. While not wishing to be bound by theory, it is believed that the fatty alcohol, together with the amphiphilic surfactant, is oriented in order to form a lamellar structure, resulting in sustaining oil and water phases. It is also believed such an organized structure, called "fatty alcohol gel network system,” contribute to stability of the composition.
• the fatty alcohols useful herein are an linear or branched, saturated fatty alcohol, selected from the group consisting of linear or branched, saturated C-J2- 30 fatty alcohols, linear or branched, saturated C-
• Preferred fatty alcohols are cetyl alcohol, stearyl alcohol, and mixtures thereof.
• the fatty alcohols useful herein present from about 1.0% to 10.0% in the composition, more preferably from about 1.0% to about 5.0%.
• amphiphilic surfactant useful herein includes surfactants, any of a wide variety of nonionic, cationic, anionic, zwitterionic, amphoteric as well as mixtures of these surfactants. Examples of a broad variety of additional surfactants useful herein are described in McCutcheon's Detergents and Emulsifiers, North American Edition (1986), published by Allured Publishing Corporation, which is incorporated herein by reference in its entirety. Also see U.S. Patent No. 4,800,197, to Kowcz et al., issued January 24, 1989, which is incorporated herein by reference in its entirety, for exemplary surfactants useful herein. Preferably, the amphiphilic surfactants useful herein present from about 1.0% to 10.0% in the composition, more preferably from about 2.0% to about 6.0%.
• Preferred nonionic surfactants useful herein are the condensation products of alkylene oxides with both fatty acids and fatty alcohols (e.g., wherein the polyalkylene oxide portion is esterified on one end with a fatty acid and etherified (e.g., connected via an ether linkage) on the other end with a fatty alcohol).
• These materials have the general formula R 2 CO( ⁇ 1) z OR3 wherein R2 and R3 are independently alkyl of from about 10 to about 30 carbons; ⁇ 1 is - OCH2CH2 derived from, for example ethylene glycol or oxide or -OCH2CHCH3- derived from propylene glycol or oxide; and z is an integer from about 6 to about 100.
• alkylene oxide derived nonionic surfactants include ceteth-6, ceteth-10, ceteth-12, ceteareth-6, ceteareth-10, ceteareth-12, ceteareth-20, steareth-6, steareth-10, steareth-12, steareth-20, steareth-21 , steareth-100, PEG-6 stearate, PEG-10 stearate, PEG-12 stearate, PEG-100 stearate, PEG-10 glyceryl stearate, PEG-20 glyceryl stearate, PEG-30 glyceryl cocoate, PEG-80 glyceryl cocoate, PEG-80 glyceryl tallowate, PEG-200 glyceryl tallowate, PEG-8 dilaurate, PEG-10 distearate, glyceryl monostearate, gylceryl distearate, glyceryl monolaurate, gly
• the structuring compound may further contain a co-thickener.
• exemplary co-thickeners useful herein are polysaccharides and materials which are primarily derived from natural sources such as gums.
• Polysaccharides as used herein means an ingredient containing a backbone of repeating sugar (i.e. carbohydrate) units.
• Nonlimiting examples of such polysaccharides include those selected from the group consisting of cellulose, carboxymethyl hydroxyethylcellulose, cellulose acetate propionate carboxylate, hydroxyethylcellulose, hydroxyethyl ethylcellulose, hydroxypropylcellulose, hydroxypropyl methylcellulose, methyl hydroxyethylcellulose, microcrystalline cellulose, sodium cellulose sulfate, and mixtures thereof.
• alkyl substituted celluloses are also useful herein.
• 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 Cio-30 straight chain or branched chain alkyl group through an ether linkage.
• 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, lauryl, 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 among the alkyl hydroxyalkyl cellulose ethers is the material given the CTFA designation cetyl hydroxyethylcellulose, which is the ether of cetyl alcohol and hydroxyethylcellulose. This material is sold under the tradename Natrosol® CS Plus from Aqualon Corporation.
• polysaccharides include scleroglucans comprising a linear chain of (less than 3) linked glucose units with a less than 6 linked glucose every three units, a commercially available example of which is ClearogelTM CS11 from Michel Mercier Products Inc. (Mountainside, NJ).
• Nonlimiting examples of the gums include materials selected from the group consisting of acacia, agar, algin, alginic acid, ammonium alginate, amylopectin, calcium alginate, calcium carrageenan, camitine, carrageenan, dextrin, gelatin, gellan gum, guar gum, guar hydroxypropyltrimonium chloride, hectorite, hyaluroinic acid, hydrated silica, hydroxypropyl chitosan, hydroxypropyl guar, karaya gum, kelp, locust bean gum, natto gum, potassium alginate, potassium carrageenan, propylene glycol alginate, sclerotium gum, sodium carboyxmethyl dextran, sodium carrageenan, tragacanth gum, xanthan gum, and mixtures thereof.
• P. Cosmeticallv-Acceptable Carrier P.
• composition of the present invention comprises a cosmetically- acceptable carrier.
• cosmetically-acceptable carrier means one or more compatible solid or liquid fillers, diluents, extenders and the like, which are cosmetically acceptable 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 cosmetically-acceptable carrier useful herein is selected from the group consisting of a hydrophobic component, a hydrophilic liquid carrier, a pH adjuster, water, and mixtures thereof.
• the type of the carrier utilized in the present invention depends on the type of the product desired and may comprise several types of carriers including, but not limited to, solutions, aerosols, emulsions (including oil-in-water or water-in-oil), gels, solids, and liposomes.
• Hydrophobic components useful in the present invention include a lipid, oil, oily or other hydrophobic component.
• the hydrophobic component is used as an emollient.
• suitable hydrophobic components include mineral oil, petrolatum, C7_4Q straight and branched hydrocarbons, C-
• hydrophobic components useful herein are set forth in U.S. Patent 5,306,514, Letton et al., issued April 26, 1994; Merck Index, Tenth Edition, Entry 7048, p. 1033 (1983); and International Cosmetic Ingredient Dictionary, Fifth Edition, vol. 1 , p.415-417 (1993).
• a fatty acid sugar ester useful herein is C-j_3o monoester or polyester of sugars and one or more carboxylic acid moieties, preferably a sucrose polyester in which the degree of esterification is 7-8, and in which the fatty acid moieties are C ⁇ s mono- and/or di-unsatu rated and behenic, in a molar ratio of unsaturates:behenic of 1 :7 to 3:5, more preferably the octaester of sucrose in which there are about 7 behenic fatty acid moieties and about 1 oleic acid moiety in the molecule, e.g., sucrose ester of cottonseed oil fatty acids.
• the composition contains from about 2.0% to about 95.0% of the hydrophobic component, more preferably from about 40.0% to about 85.0%.
• the hydrophobic component may include an ingredient derived from animals, plants, or petroleum and which is natural or synthetic (e.g., man-made).
• composition of the present invention may contain a hydrophilic liquid carrier (HLC).
• HLC hydrophilic liquid carrier
• Preferred HLC can contain a dermatologically acceptable, non- aqueous hydrophilic diluent.
• hydrophilic diluents are polyhydric alcohols such as low molecular weight monovalent alcohols (i.e., C-j.
• glycols and polyols including propylene glycol, butylene glycol, hexylene glycol, dipropylene glycol, polyethylene glycol (e.g., Molecular Weight 200-1000 g/mole), polypropylene glycol (e.g., Molecular Weight 425-2025 g/mole), glycerol, 1 ,2,4-butanetriol, 1 ,2,6-hexanetriol, and combinations thereof.
• the composition contains from about 30% to about 95% of
• the HLC includes water and one or more water soluble or dispersible ingredients. The exact amount of water in the formulation will vary with the ranges of the required and optional components chosen.
• the cosmetically-acceptable useful herein may contain a pH adjuster.
• pH adjuster refers to any component which is employed to increase or decrease the overall pH of the composition to an optimum pH, thereby preventing decomposition of ingredients (particularly the ascorbic acid compound).
• An optimum pH is subject to the selection of the ascorbic acid compound.
• MAP magnesium L-ascorbyl phosphate
• Suitable pH adjusters herein include acetate, phosphate, citrate, triethanolamine and carbonate. A combination of the foregoing are often employed to adjust to a specific optimal pH for the composition.
• the total level by weight of total composition of the pH adjuster is from about 0.01% to about 5.0%, preferably, from about 0.5% to about 2.0%.
• the cosmetically-acceptable useful herein may further contain other actives capable of functioning in different ways to enhance the benefits of the ascorbic acid compound and/or to provide other benefits.
• 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 are commercially available from a number of sources, for example, Sigma Chemical Company (St. Louis, MO), and Boerhinger Mannheim (Indianapolis, IN) and described in U.S. Patent 4,677,120, Parish et al., issued Jun. 30, 1987; U.S.
• Vitamin B3 Compounds The vitamin B3 compound enhances the skin appearance benefits of the present invention, especially in regulating skin condition, including regulating signs of skin aging, more especially wrinkles, lines, and pores.
• the vitamin B 3 compound 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), -COOH (e.g., nicotinic acid) or - CH2OH (e.g., nicotinyl alcohol); derivatives thereof; and salts of any of the foregoing.
• -CONH2 e.g., niacinamide
• -COOH e.g., nicotinic acid
• CH2OH e.g., nicotinyl alcohol
• 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., 1 to about 18 carbons).
• nicotinuric acid C8H8N2O3
• nicotinyl hydroxamic acid C6H6N2O2
• 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, nialamide, 1-(3-pyridylmethyl) urea, 2-mercaptonicotinic acid, nicomol, and nia
• Nonlimiting examples of the above vitamin B 3 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).
• 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-j.-jg carboxylic acid salts, e.g., acetate, salicylate, glycolate, lactate, malate, citrate, preferably monocarboxylic acid salts such as acetate).
• anionic inorganic species e.g., chloride, bromide, iodide, carbonate, preferably chloride
• organic carboxylic acid salts including mono-, di- and tri- C-j.-jg carboxylic acid salts, e.g., acetate, salicylate, glycolate, lactate, malate, citrate, preferably monocarboxylic
• 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.
• such complex is preferably substantially reversible, more preferably essentially reversible, upon delivery of the composition to the skin.
• 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 B 3 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, butylated hydroxy benzoic acids and their salts, 6-hydroxy-2,5,7,8-tetramethylchroman-2- carboxylic acid (commercially available under the tradename Trolox®), gallic acid and its alkyl esters, especially propyl gallate, uric acid and its salts and alkyl esters, sorbic acid and its salts, amines (i.e., N,N-diethylhydroxylamine, amino- guanidine), sulfhydryl compounds (i.e., glutathione), dihydroxy fumaric acid and its salts, lycine pidolate, arginine pilolate, nordihydroguaiaretic acid, bioflavonoids, lysine, methionine, proline, superoxide dismutase, sily
• 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-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.
• Additional anti-inflammatory agents useful herein include compounds of the licorice (the plant genus/species Glycyrrhiza glabra) family, including glycyrrhetic acid, glycyrrhizic acid, and derivatives thereof (e.g., salts and esters).
• Suitable salts of the foregoing compounds include metal and ammonium salts.
• Suitable esters include C2-24 saturated or unsaturated esters of the acids, preferably CI Q-24- more preferably C ⁇
• 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 or inorganic.
• 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, 2-phenylbenzimidazole-5-sulfonic acid, octyldimethyl-p-aminobenzoic acid, octocrylene, 2-ethylhexyl N,N-dimethyl-p-aminobenzoate, p-aminobenzoic acid, 2-phenylbenzimidazole-5-sulfonic acid, octocrylene, oxybenzone, homomenthyl salicylate, octyl salicylate, 4,4'-methoxy-t-butyldibenzoylmethane, 4-isopropyl dibenzoylmethane, 3-benzy
• 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
• a sunscreen or sunblock herein may also be added to improve the skin, particularly to enhance their resistance to being washed off by water, or rubbed off.
• Preferred sunscreens and sunblocks which will provide this benefit are a copolymer of ethylene and acrylic acid. Compositions comprising this copolymer are disclosed in U.S. Patent 4,663,157, Brock, issued May 5, 1987.
• Chelators 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 solubilizable preservatives including Germall 115, methyl, ethyl, propyl and butyl esters of hydroxybenzoic acid, benzyl alcohol, EDTA, Bronopol (2-bromo-2-nitropropane-1 ,3-diol) and phenoxypropanol; other skin lightening/evenness agents including kojic acid and arbutin; WO95/23780, Kvalnes et al, published September 8, 1995; skin-conditioning agents; skin penetration enhancing agents; skin protectants; skin soothing agents; skin healing agents; ultraviolet light absorbers or scattering agents; sequestrants; anti-acne agents; anti-androgens; depilation agents; keratolytic agents/ desquamation agents/ exfoliants such as salicylic acid; panthenol moisturizer such as D
• 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 shown below can be prepared by any conventional method known in the art. Suitable methods and formulations are as follows:
• compositions above described are suitably made as follows: (1) Dissolve water soluble contents except for an ascorbic acid compound and sodium citrate, and heat the solution up to about 75 °C; (2) Mix a separate water solution of a ascorbic acid compound and sodium citrate and cool the mixture to below about 40° C, (3 Mix (1) and (2) and keep the temperature at about 75 °C; (4) Heat a mixture of the structuring compounds and the oil components to about 80 °C; (5) Add the mixture (4) into the water phase (3) followed by high pressure homogenizing;and (6) Add KOBO GLW75CAP-MP and glycerin to the mixture (5) at about 30°C.
• composition herein contains increased levels of ascorbic acid compound for skin lightening, while exhibiting improved product aesthetic such as product appearance unchanging to yellow or brown, even if maintained in storage for extended periods of time.

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