MXPA01008140A - Cosmetic compositions containing vitamin b3. - Google Patents

Cosmetic compositions containing vitamin b3.

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Publication number
MXPA01008140A
MXPA01008140A MXPA01008140A MXPA01008140A MXPA01008140A MX PA01008140 A MXPA01008140 A MX PA01008140A MX PA01008140 A MXPA01008140 A MX PA01008140A MX PA01008140 A MXPA01008140 A MX PA01008140A MX PA01008140 A MXPA01008140 A MX PA01008140A
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Mexico
Prior art keywords
vitamin
weight
cosmetic composition
further characterized
niacinamide
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Application number
MXPA01008140A
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Spanish (es)
Inventor
Magda El-Nokaly
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Procter & Gamble
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Publication of MXPA01008140A publication Critical patent/MXPA01008140A/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67Vitamins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q15/00Anti-perspirants or body deodorants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/0295Liquid crystals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67Vitamins
    • A61K8/673Vitamin B group
    • A61K8/675Vitamin B3 or vitamin B3 active, e.g. nicotinamide, nicotinic acid, nicotinyl aldehyde
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/92Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q1/00Make-up preparations; Body powders; Preparations for removing make-up
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q1/00Make-up preparations; Body powders; Preparations for removing make-up
    • A61Q1/02Preparations containing skin colorants, e.g. pigments
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q1/00Make-up preparations; Body powders; Preparations for removing make-up
    • A61Q1/02Preparations containing skin colorants, e.g. pigments
    • A61Q1/04Preparations containing skin colorants, e.g. pigments for lips
    • A61Q1/06Lipsticks
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q1/00Make-up preparations; Body powders; Preparations for removing make-up
    • A61Q1/02Preparations containing skin colorants, e.g. pigments
    • A61Q1/10Preparations containing skin colorants, e.g. pigments for eyes, e.g. eyeliner, mascara
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q1/00Make-up preparations; Body powders; Preparations for removing make-up
    • A61Q1/12Face or body powders for grooming, adorning or absorbing

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  • Life Sciences & Earth Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Cosmetics (AREA)

Abstract

The present invention relates to topical cosmetic compositions composed primarily of lipophilic materials as the continuous phase and containing vitamin B3 compounds. Such compositions are useful in improving the stability and skin penetration of compositions containing vitamin B3 compounds.

Description

COSMETIC COMPOSITIONS CONTAINING VITAMIN B3 COMPOUNDS FIELD OF THE INVENTION The present invention relates to topical cosmetic compositions composed primarily of lipophilic materials such as continuous phase and containing vitamin B3 compounds.
BACKGROUND OF THE INVENTION Niacin, also known as vitamin B3, is the common name for icotinic acid. The physiologically active form of niacin is niacinamide, also a member of the family of vitamin B3 compounds. Niacin and niacinamide (nicotinic acid amide) function in the body as components of two coenzymes: nicotinamide adenine dinucleotide (NAD) and nicotinamide adenine dinucleotide phosphate (NADP). Until recently, these vitamin B3 compounds were used exclusively to treat niacin and pellagra deficiency. However, nowadays, vitamin B3 compounds have also found use in the area of active skin care. British Patent 1 370,236 discloses skin lightening compositions containing 0.5% to 10% niacin. In the same way, the patent of E.U.A. 4,096,240 describes the use of 0.1% to 10% niacinamide to lighten the skin. It has also been found that vitamin B3 compounds are useful for regulating the texture of human skin. See PCT application WO 97/39733, by Oblong et al. In addition, the inventors of the present have observed that incorporating vitamin B3 compounds solubilized in water-in-oil cosmetic vehicles improves the penetration of vitamin B3 compounds into the skin, thereby improving their skin-regulating properties. However, since most vitamin B3 compounds are soluble in polar solvents, they can create stability problems when formulated in cosmetic compositions composed primarily of lipophilic materials of (ie, forming a lipophilic continuous phase). In formulating these compositions, the polar solvents (eg, polyhydric alcohols, water) necessary to dissolve the vitamin B3 compounds have to be separated from the lipophilic materials, causing the formation of layers of mass of untidy appearance. In addition, in formulating the lipophilic bar compositions (e.g., lipsticks), this separation phase manifests as liquid droplets along the surface of the stick composition. This can negatively accept consumer acceptance. Thus, there is a need for cosmetic compositions comprising vitamin B3 compounds that provide improved skin penetration of the vitamin B3 compound and provide good compositional stability. The inventors of the present have observed that the stability of the cosmetic compositions comprising a vitamin B3 compound, a polar solvent and a lipophilic continuous phase can be improved by incorporating a surfactant or surfactant mixture having a Krafft point of or less of 20 ° C and forms association structures so that the association structures thermodynamically link the humectant / polar solvent and absorbed homogeneously in the lipophilic matrix. Therefore, an aspect of the present invention is to provide cosmetic compositions comprising a lipophilic continuous phase and solubilized vitamin B3 compounds. Another aspect of the present invention is to provide cosmetic compositions comprising solubilized vitamin B3 compounds that provide improved skin penetration of the vitamin B3 compound. A further aspect of the present invention is to provide cosmetic stick compositions comprising solubilized vitamin B3 compounds. Yet another aspect of the present invention is to provide cosmetic stick compositions comprising a lipophilic continuous phase and solubilized vitamin B3 compounds stabilized by association structures. Another aspect of the present invention is to provide cosmetic stick compositions that improve the penetration of vitamin B3 compounds into the skin. These and other aspects will become evident from the detailed description that appears below.
BRIEF DESCRIPTION OF THE INVENTION The present invention relates to topical cosmetic compositions useful for providing improved skin penetration of a vitamin B3 compound, comprising: from about 0.01% to about 50% by weight of the composition, of vitamin B3 compound; from about 1% to about 90%, by weight of the composition, of the emollient component comprising from 0.1% to 100% by weight of the emollient component of an oil that is liquid at room temperature; from about 0.1% to about 80% by weight of the composition, of a stabilizing system, comprising: (i) from about 0.1% to about 90% by weight of the stabilizing system, of a solidifying agent; and (ii) from about 0.01% to about 30% by weight of the stabilizer system, of a surfactant, wherein the surfactant has a Krafft point of at least 20 ° C and forms association structures; and from about 0.01% to about 90% of the composition, of a polar solvent. All percentages, parts and ratios are based on the total weight of the cosmetic compositions of the present invention, unless otherwise specified. All weights, while belonging to the aforementioned ingredients, are based on the active level and, therefore, do not include vehicles or by-products that may be included in commercially available materials, unless otherwise specified.
DETAILED DESCRIPTION OF THE INVENTION Definition As used herein, the term "cosmetics" includes makeup, foundation for makeup, and skin care products. The term "makeup" refers to the products that give color to the face, including base for makeup, dark and tanned, that is, mascara, eyeliners, eyebrow color, eye shadows, blushes, lip colors, etc. Skin care products are those that are used to treat or care for, or in some way moisturize, improve, or cleanse the skin. Products that are contemplated with the phrase "skin care products" include, but are not limited to, adhesives, bandages, toothpaste, anhydrous occlusive humectants, antiperspirants, deodorants, laundry detergents in powder form, fabric softener fabric, patches that supply occlusive drugs, nail polishes, powders, fabrics, cloths, solid emulsion compact articles, anhydrous conditioners for hair, and the like. The term "foundation for makeup" refers to liquids, cream, foam, powder, or similar products created or reintroduced by cosmetic companies to match the overall color of the skin. The base for makeup is made to work better on moisturized and / or oily skin. As used herein, the term "association structure" refers to an aggregation of surfactant and / or polymer molecules so that they are oriented to form an ordered mixed-body structure. An association structure is also known in the art as a liquid crystalline phase. A requirement for the formation of a liquid crystal is the hydrocarbon portion of an amphiphilic molecule is transformed to a state with a disorder such as exists in the liquid state. Despite the high degree of short-range disorder in these structures there is a large-scale order of at least one dimension. As used herein, the term "solid materials" refers to any solidifying ingredient capable of absorbing the association structures. The solids include waxes, solid fats, clays, fillers, powders, UV absorbers, suspending agents, wax emulsifiers or pigments commonly used to thicken or solidify the cosmetic compositions. As used herein, "color (s) or colorant (s)" include pigments, colorants, colors, lacquers and pearlescents. The colors are measured on an anhydrous weight basis. As used in this, the term, "lecithin" refers to a material that is a phosphatide. Phosphatides of natural or synthetic occurrence can be used. Phosphatidyl choline or lecithin is a glycerin esterified with a single colloidal ether of phosphoric acid and two fatty acids, usually a long saturated or unsaturated fatty acid chain, having 16 to 20 carbons and up to 4 fold bonds. Other phosphatides capable of forming succession structures, preferably lamellar or hexagonal liquid crystals, can be used in place of lecithin or in combination with it. Other phosphatides are glycerol esters with two fatty acids as in lecithin, but the choline is replaced by ethanolamine (a cephalin), or serine (an α-aminopropanol acid); phosphatidyl serine) or an inositol (phosphatidyl inositol). As used herein, the term "surfactant" refers to an organic compound below molecular weight or non-polymeric monomer of an amphiphilic nature, i.e., it has hydrophilic and hydrophobic groups and shows a marked tendency to absorb on a surface or interface and decrease the surface tension. The surfactants are emulsifiers are divided nonionic (uncharged) anionic (negative charge) cationic (positive charge) and amphoteric (both charges) based on whether or not to ionize the aqueous medium. The surfactants are monomers and are derived from natural oil and fats and crude oil. The term "surfactant" as used herein refers to mixtures of surfactants as well as to a single organic compound. As used herein, "polar solvent" refers to a polar material capable of forming an association structure with a surfactant. Some examples of polar solvents include glycerin, panthenol (preferably panthenol mixed with glycerin or alcohol), propylene glycol, butylene glycol, hexylene glycol, water, alcohols, alkanediols, polyethylene glycols, sorbitol, maltilal and mixtures thereof. As used herein, the term "comprising" means that the composition may contain other ingredients that are compatible with the composition and that preferably do not substantially disrupt the association structures of the present invention. The term encompasses the terms "consisting of" and "consisting essential of". As used herein, the term "room temperature" refers to the temperature also known in the art as "room temperature" and typically refers to about 20 ° C. Generally the ambient temperature can vary from about 18 ° C to about 27 ° C, preferably from about 20 ° C to about 25 ° C, depending on variables such as geographical location, ie sub-tropical vs. temperate regions.
ESSENTIAL COMPONENTS * Component of vitamin B3 The compositions of the present invention comprise a safe and effective amount of a natural or synthetic cylindrical crystalline vitamin B3 compound. The compositions of the present invention preferably comprise from above 0.01% to about 50%, more preferably from about 0.1% to about 30%, even more preferably from 0.5% to about 20%, more preferably from about 1% to about 10%. % of the vitamin B3 compound. As used herein, "vitamin B3 compound" means a "compound having the formula: wherein R is -CONH2 (for example, niacinamide), -COOH (for example, nicotinic acid) or -CH2OH (for example, nicotinyl alcohol), derivatives thereof and salts of any of the foregoing. Examples of derivatives of the above vitamin B3 compounds include esters of nicotinic acid, including non-vasodilating esters of nicotinic acid, nicotinyl amino acids, and nicotinyl alcohol esters of carboxylic acids. Suitable esters of nicotinic acid include esters of C 1 -C 22 nicotinic acid. preferably C1-C16, more preferably CrC6 alcohols. 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-blushing. As used herein "non-blushing" means that the ester does not commonly produce a visible flow response after application to the skin of the target compositions (the majority of the general population does not experience a visible flow response, although said compounds may cause vasodilation not visible to the exposed eye). Alternatively, a nicotinic acid material that is blushing at high doses can be used at a lower dose to reduce the blushing effect. Non-blushing nicotinic acid esters include tocopherol nicotinate and inositol hexanicotinate. Other derivatives of the vitamin B3 compound are the niacinamide derivatives that result from the substitution of one or more of the hydrogens of the amide group. Non-limiting examples of niacinamide derivatives 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 esters of Nicotinyl alcohol of organic carboxylic acids (e.g., d-C18). Specific examples of such derivatives include nicotinuric acid having the following chemical structures: nicotinuric acid: nicotinylhydroxamic acid: Examples of nicotinyl alcohol esters include nicotinyl alcohol esters of carboxylic acids, salicylic acid, acetic acid, glycolic acid, palmitic acid, and the like. Other non-limiting examples of the vitamin B3 compounds useful herein are 2-chloronicotinamide, 6-aminonicotinamide, 6-methylnicotinamide, n-methyl-nicotinamide, n, n-diethylnicotinamide, n- (hydroxymethyl) -nicotinamide, metric of quinolinic acid, nicotinanilide, n-benzylnicotinamide, n-ethylnicotinamide, nifenazone, nicotinaldheido, isonicotinic acid, methylisonicotinic acid, thionicotinamide, nialamide, 1- (3-pyridylmethyl) urea, 2-mercaptonicotinic acid, nicomol, and niaprazine. Examples of the above vitamin B3 compounds are well known in the art and are commercially available from a number of sources, for example, the Sigma Chemical Company (St. Louis, MO); ICN Biomedicals, Inc. (Irvin, CA) and the Aldrich Chemical Company (Milwaukee, Wl). One or more vitamin B3 compounds can be used herein. The preferred compounds of vitamin B3 are niacinamide and tocopherol nicotinate. Niacinamide is the most preferred. When they used, salts, derivatives, and derivatives of niacinamide salts are preferably those which have substantially the same efficacy as niacinamide in the skin condition regulation methods described herein. The salts of the vitamin B3 compound are also useful herein. Non-limiting examples of salts of the vitamin B3 compound useful herein include organic or inorganic salts, such as inorganic salts with anionic inorganic species (eg, chloride, bromide, iodide, carbonate, preferably chloride), and carboxylic acid salts organic (including mono-, di- and tricarboxylic acid salts of C1-C18, for example, acetate, salicylate, glycolate, lactate, malate, citrate, preferably salts of monocarboxylic acid such as acetate). These and other salts of the vitamin B3 compound can be easily prepared by the person skilled in the art, for example, as described by W. Wenner, "The Reaction of L-Ascorbic and D-lsoascorbic Acid with Nicotinic Acid and Its Amide" , J. Organic Chemistry, Vol. 14, 22-26 (1949), which is incorporated herein by reference. Wenner describes the synthesis of the ascorbic acid salt of niacinamide. In a preferred embodiment, the ring nitrogen of the vitamin B3 compound is chemically free in substantial form (eg, unbound and / or unimpeded), or after the supply to the skin chemically becomes substantially free ("chemically free"). free "hereinafter refers alternatively to" without combination "). More preferably, the vitamin B3 compound is not essentially combined. Therefore, if the composition contains the vitamin B3 compound in a salt or other combination form, said combination is preferably substantially reversible, more preferably essentially reversible, in the delivery of the composition to the skin. For example, said combination must be substantially reversible at a pH of about 5.0 to about 6.0. Said reversibility can be easily determined by the person skilled in the art.
More preferably, the vitamin B3 compound is not substantially combined in the composition prior to delivery to the skin. Examples of approaches to minimize or avoid the formation of undesirable combinations include the omission of materials whose form is substantially irreversible or other combinations with the vitamin B3 compound, pH adjustment, ionic strength adjustment, the use of surfactants, and formulations in where the vitamin B3 compound and materials whose combination therein is in different phases. Such approaches are within the skill level of the person skilled in the art. Therefore, in a preferred embodiment, the vitamin compound B3 contains a limited amount of the salt form and preferably is substantially free of salts of a vitamin B3 compound. Preferably the vitamin B3 compound contains less than 50% of said salt, and more preferably is essentially free of the salt form. The vitamin B3 compound in the present compositions having a pH of about 4 to about 7 typically contains less than about 50% of the salt form. The vitamin B3 compound can be included as the substantially pure material, or as an extract obtained by adequate physical and / or chemical isolation from natural sources (e.g., plants). The vitamin B3 compound is preferably substantially pure, more preferably essentially pure.
The vitamin B3 compounds that exist in crystalline form are particularly preferred for use herein.
Emollient Compound The compositions of the present invention further comprise an emollient suitable for suspending or otherwise dispersing the crystalline vitamin B3 compound therein. Any emollient that is known or otherwise suitable for use in cosmetic applications, and that is also compatible with the crystalline vitamin B3 compound in the composition, can be used in the composition of the present invention. Preferred emollients for use in the composition of the present invention are those materials that are mentioned in personal care techniques such as fats, oils, fatty alcohols, fatty acids, fatty acid esters, and combinations thereof, and which they aid in the application and adhesion, produce shine and / or provide occlusive wetting. Emollients suitable for use in the present invention include isostearic acid derivatives, isopropyl palmitate, lanolin oil, diisopropyl dimerate, maleate soybean oil, octyl palmitate, isopropyl isostearate, cetyl lactate, cetyl ricinoleate, acetate of tocopheryl, acetylated lanolin alcohol, cetyl acetate, phenyltrimethicone, glyceryl oleate, tocopheryl linoleate, wheat germ glycerides, arachidyl propionate, myristyl lactate, decyl oleate, propylene glycol ricinoleate, isopropyl lanolate, pentaerythrityl tetrastearate , neopentilglycol dicaprylate / dicaprate, hydrogenated cocoglycerides, isononyl isononanoate, isotridecyl isononanoate, myristyl myristate, triisocetyl citrate, cetyl alcohol, octyl dodecanol, oleyl alcohol, panthenol, lanolin alcohol, linoleic acid, linolenic acid, sucrose esters of fatty acids, octyl hydroxystearate and me zclas of them. Examples of other suitable emollients are described in Cosmetic Bench Reference, pp. 1.19-1.22 (1996), whose descriptions are incorporated herein by reference. Oils suitable for use in the compositions of the present invention include esters, triglycerides, hydrocarbons and silicones. These can be a single material or a mixture of one or more materials. They will usually comprise from about 0.1% to about 100%, preferably from about 5% to about 90%, and more preferably from about 70% to about 90% of the emollient component. The oils act as emollients and may also provide viscosity, tackiness, and entrainment properties to cosmetic compositions such as lipsticks. Examples of suitable oils include caprylic triglycerides, capric triglyceride, isostearic triglyceride; adipic triglyceride; Propylene glycol myristyl acetate; lanolin; lanolin oil; polybutene, isopropyl palmitate; mypropyl myristate; isopropyl isostearate; Diethyl sebacate; diisopropyl adipate; tocopheryl acetate; tocopheryl linoleate; hexadecyl stearate; ethyl lactate; cetyl oleate; cetyl ricinoleate; oleyl alcohol; hexadecyl alcohol; octyl hydroxystearate; octyl dodecanol; wheat germ oil; hydrogenated vegetable oils; Castor oil; petrolatum; modified lanolins; branched chain hydrocarbons; alcohols and esters; corn oil; cottonseed oil; olive oil; palm kernel oil; rapeseed oil; safflower oil; jojoba oil; ass grass oil; mineral oil of avocado oil; yellow or white butter, octylpalmitate, soybean oil with maleate; glycerol trioctanoate, diisopropyl dimerate, and volatile and non-volatile silicone oils including phenyl trimethicone. Preferred oils for use herein are acetyglycerides, octanoates and decanoates of alcohols and polyalcohols, such as glycol and glycerol, the recinoleates of alcohols and polyalcohols such as cetyl ricinoleate, PG-3 distearate, polyglycerol ethers, polyglycerol esters, triglycerides capríliicos, capric triglycerides, isostearic triglyceride, adipic triglyceride, phenyl timethicone, lanolin oil, polybutens, isopropyl palmitate, isopropyl isostearate, cetyl ricinoleate, octyl dodecanol, oleyl alcohol, hydrogenated vegetable oils, castor oil, modified lanolins , octyl palmitate, lanolin oil, maleate soybean oil, cetyl ricinoleate, glyceryl trioctanoate, diisopropyl dimerate, synthetic lanolin derivatives and branched chain alcohols, sucrose esters of fatty acids, octyl hydroxystearate and mixtures of the same. Preferably, the oils used are selected so that the majority (at least about 75%, preferably at least about 80%, and more preferably at least 99%) of the types of oils used have solubility parameters that do not differ by more than about 1 to about 0.1, preferably about 0.8 to about 0.1. The emollient component comprises from about 1% to about 90%, preferably from about 10% to about 80%, more preferably from about 20% to about 70%, and more preferably from about 40% to about 60%, of cosmetic composition.
Stabilizing System The compositions of the present invention further comprises a stabilizing system. The phrase "stabilizing system", as used herein, refers to a system that prevents coalescence of polar solvent droplets and / or in the case of bar compositions, their migration to the bar surface. a) Solidifying agent The cosmetic compositions of the present invention may further comprise a solidifying agent for solidifying or trapping any liquid base material in the cosmetic compositions. (As used herein, the term "solidify" refers to the physical and / or chemical alteration of the liquid base material to form a solid or semi-solid at ambient conditions, i.e., to form a final composition having a structure stable physics and deposited on the skin during normal conditions of use). As will be appreciated by those skilled in the art, the selection of the particular solidification agent to be used in cosmetic compositions will depend on the particular type of composition desired, ie, gel or wax-based, the desired rheology, the base material used liquid and other materials to be used in the composition. The solidifying agent is preferably present at a concentration of from about 1% to about 90%, more preferably from about 1% to about 50%, even more preferably from about 5% to about 40%, more preferably from about 3% to approximately 20%. The wax-based cosmetic stick forms of the invention preferably contain from about 5% to about 50% (by weight) of the solidification agent with wax. The term "wax solidification agent", as used herein, refers to a solidification material having similar characteristics to wax. Said materials with wax can also serve as emollients. Among the wax materials useful herein are high melting waxes, ie, having a melting point of about 65 ° C to about 125 ° C, such as beeswax, spermaceti, carnauba, laurel berry, candelilla, montan, ozokerite, ceresin, paraffin, synthetic waxes such as Fisher-Tropsch waxes, microcrystalline wax and mixtures thereof. Ceresin, ozokerite, white beeswax, synthetic waxes, and mixtures thereof, are among the preferred high-melting waxes useful herein. The compositions having waxes, among those which are useful herein, are described in the U.S. patent. 4,049,792, Elsnau, filed September 20, 1977, incorporated herein by reference in its entirety). Low-melting waxes, having a melting point of about 37 ° C to about 75 ° C, are preferred for use in the wax-based stick embodiments of the invention. In the form of wax bars containing volatile silicon oils as liquid base material, they preferably contain from about 10% to about 35%, more preferably from about 10% to about 20% (by weight), of a wax low melting point. Such materials include fatty acids, fatty alcohols, fatty acid esters and fatty acid amides, which have fatty chains of from about 8 to about 10 carbon atoms, and mixtures thereof. Preferred wax-like materials include cetyl alcohol, palmitic acid, stearyl alcohol, behenamide, sucrose esters of bait fatty acids, polyethylene glycol mono and digraso acid esters, and mixtures thereof. Stearyl alcohol, cetyl alcohol, and mixtures thereof, are particularly preferred. The fatty acids, fatty alcohols, and other wax-like materials useful in this invention are described in the following references, which are all incorporated herein by reference: U.S. Pat. 4,151, 272, Geary, et al., Filed April 24, 1979; patent of E.U.A. 4,229, 432, Geria, filed October 21, 1980; and patent of E.U.A. 4,280, 994, Turney, filed July 28, 1981; "The Chemistry and Technology of Waxes", A.H. Warth, second edition, reprinted in 1960, Reinhold Publishing Corporation, pp. 391-393 and 421; "The Petroleum Chemicals Industry", R.F. Goldstein and A. L. Waddeam, third edition (1967), E & F.N. Span Ltd., pp 33-40; "The Chemistry and Manufacture of Cosmetics", M.G. DeNavarre, second edition (1970), Van Nostrand & Company, pp 354-376; and in "Encyclopedia of Chemical Technology :, Vol. 24, Kirk-Othmer, third edition (1979) pp 466-481. Preferred wax-like materials useful as solidifying agents in the wax bars of the present are described in US Patent 4,126,679, Davy, et al., issued November 21, 1978, which is incorporated herein in its entirety Preferred mixtures of wax-like materials comprise fatty alcohols containing carbon chains around from 14 to about 18 carbon atoms, and alcohols having chain lengths of 20 carbons or more, wherein the final mixture contains from about 1% to about 3% (by weight) of the longer chain fatty alcohols. The compositions containing these fatty alcohol mixtures are described in European Patent Specification No. 117,070, May, published August 29, 1984 (incorporated by reference herein). biopolymers such as those described in European application No. 522624, to Dunphy et al., incorporated herein by reference in its entirety. The gel bar embodiments of this invention preferably contain from about 3% to about 30%, preferably from about 3% to about 10% (by weight) of a solidification agent. The particular amount of the solidifying agent that will be used will depend on the particular solidification agent and the liquid base material used, and the desired physical characteristics of the gel stick. The solidification agents useful in the gel-bar mode of this invention are, in general, surface active compounds that form networks by immobilizing or solidifying the liquid base materials in a gel. Such solidifying agents include: soaps, such as sodium and potassium salts of higher fatty acids, ie, acids having from 12 to 22 carbon atoms; amides of higher fatty acids; higher fatty acid amides of alkylaminos; acetals of dibenzaldehyde-monosorbitol; alkali metal salts and ferrous alkali metal salts of acetates, propionates and lactates; waxes, such as candelillas and caranauba; and mixtures thereof. Among these preferred solidifying agents for use in the gel stick embodiments of this invention, are sodium stearate, sodium palmitate, aluminum stearate, aluminum-magnesium hydroxystearate, and mixtures thereof. Gel stick compositions containing solidifying agents among those useful herein are described in the following patent documents, all incorporated herein by reference in their entirety: US Patent 2,900,306, Slater, issued August 18. of 1959; U.S. Patent 3,255,082, Barton, issued June 7, 1966 U.S. Patent 4,137,306, Rubino et al., issued January 30, 1979 U.S. Patent 4,154,816, Roehl, et al., issued May 15, 1979 from US 4,226,899, Yuhas, issued October 7, 1980; U.A. Patent 4,346,079, Roehl, issued August 24, 1982; U.A. Patent 4,383,988, Teng, et al., issued May 17, 1983; European Patent Specification No. 107,330, Luebbe, et al., published May 2, 1984; and patent application of E. U. A. serial number 630, 790, DiPietro, filed July 13, 1984. Preferred solidifying agents useful in the gel bar embodiments of the present invention are described in European Patent Specification No. 24, 365 Sampson et al., Published on March 4, 1981, incorporated herein by reference in its entirety. Conventional thickeners are also useful herein as solidifying agents. Examples of suitable thickeners include, but are not limited to, natural polymeric materials such as locust bean gum, sodium alginate, sodium caffeinate, egg albumin, gelatin agar, carrageenan gum sodium alginate, xanthan gum, quince seed, tragacanth gum, starch, chemically modified starches and the like, semi-synthetic polymeric materials, such as cellulose ethers (for example hydroxyethylcellulose, methylcellulose, carboxymethylcellulose, hydroxypropylmethylcellulose), polyvinylpyrrolidone, polyvinyl alcohol, guar gum, guar gum, hydroxypropyl, soluble starch, cationic celluloses, cationic guands and the like and synthetic polymeric materials, such as carboxyvinyl polymers, polyvinylpyrrolidone, polyvinyl alcohol of polyacrylic acid polymers, polymethacrylic acid polymers, polyvinyl acetate polymers, polyvinyl chloride polymers, polymer s of polyvinylidene chloride and the like. Inorganic thickeners such as aluminum silicates such as, for example, bentonites, or a mixture of polyethylene glycol and polyethylene glycol stearate or distearate can also be used. Natural polymers or biopolymers and their use, is described further in European application No. 522624, to Dunphy et al. Additional examples of natural polymers or biopolymers can be found in Cosmetic Bench Reference, pp. 1.40-1.42, which is incorporated herein by reference. Also useful are hydrophilic gelling agents such as copolymers of acrylic acid / ethyl acrylate and the carboxyvinyl polymers sold by B.F. Goodrich Company with the commercial name of Carbopol Registered TM resins. These resins consist essentially of a colloidally water-soluble polyether-polyalkenyl crosslinked polymer of acrylic acid crosslinked with 0.75% to 2.00% of an entanglement agent such as for example polyallyl sucrose or polyallyl pentaerythritol. Examples include Carbopol 934, Carbopol 940, Carbopol 950, Carbopol 980, Carbopol 951 and Carbopol 981. Carbopol 934 is a water-soluble polymer of acrylic acid crosslinked with about 1% of a polyallyl ether of sucrose having an average of about 5.8 groups allyl for each sucrose molecule. Also suitable for use herein are carbomers sold under the tradename "Carbopol Ultrez 10, Carbopol ETD2020, Carbopol 1382, Carbopol 1342 and Pemulen TR-1 (CTFA designation: Acrylates / 10-30 AIkil Acrylate Crosspolymer). of the above polymers are also useful herein Other gelling agents suitable for use herein include oleogels such as trihydroxystearin Hydrophobically modified celluloses are also useful for use herein These celluloses are described in detail in US Pat. 4,228,277 and 5,101, 646, both incorporated herein by reference in their entirety Additional examples of suitable gelling agents or gelling agents can be found in Cosmetic Bench Reference, page 1.27, which is incorporated herein by reference. the theory, it is believed that the agent solidifies in combination with the emollient, ac It acts as an occlusive on the skin by forming continuous or discontinuous double-layer or multiple-layer films on the skin. The term "occlusive", as used herein, refers to avoiding or obstructing something, in this case, avoid the removal of moisture (by means of evaporation) and the vitamin B3 compound (by means of the bond to the film) from a surface of the skin. b) Surfactant The compositions of the present invention further comprise a surfactant. Surfactants suitable for use in the compositions of the present invention are those which can form association structures, preferably lamellar or hexagonal reverse liquid crystals, at room temperature when mixed with a polar solvent. Ambient temperature as used herein is typically referred to at about 20 ° C. Generally the ambient temperature can vary from about 18 ° C to about 27 ° C, preferably from about 20 ° C to about 25 ° C, depending on variables such as geographical location, ie sub-tropical regions see their temperate regions. One skilled in the art can determine if the association structures form are formed at ambient temperatures. Suitable surfactants to be used generally have a Krafft point below room temperature at about 20 ° C or generally at or below about 18 ° C at about 27 ° C, preferably at or below about 20 ° C at about 25 ° C. ° C. The definition of the Krafft point is well known in the art and one skilled in the art can determine the Krafft point of the surfactant. In general terms, the Krafft point is the melting point of the hydrocarbon chains of the surfactants. It can also be expressed as the temperature at which the solubility of an association colloid in water suddenly increases because the critical concentration of micelles is exceeded and micelles are formed. See Ekwall., P., "Composition, Properties and Structure of Liquid Cristalline Phases in Systems of Amphyphilic Compounds" Advances in Liquid Crystals Vol. I, Chapter I, p.81. In the preparation of a sample combination of a surfactant and polar solvent to demonstrate the ability to form association structures, the surfactant needs to be sufficiently soluble in the polar solvent so that an association structure can be formed at room temperature. One skilled in the art is capable of determining compatible interactions. Any surfactant that forms association structures at room temperature and is suitable for use in cosmetics is suitable for use herein. Surfactants suitable for use in cosmetics do not present dermatological or toxicological problems. The anionic, nonionic, amphoteric cationic surfactants and mixtures thereof are suitable for use. Preferably the anionic, nonionic, cationic, amphoteric surfactants and their mixtures having a Krafft point of at least room temperature are used. Most preferably, nonionic, cationic, amphoteric surfactants and their mixtures having a Krafft point of at least room temperature are used. Suitable surfactants for use herein are found in the U.S.A. No. 5,843,407 to El-Nokaly, included herein by way of reference. The association structures of the present invention are also useful for improving the skin penetration of the vitamin B3 compound. Without being bound by any theory, it is believed that the association structures act as an occlusive or trapping matrix in the skin by forming continuous or discontinuous films of double or multiple layers on the skin. The term "occlusive", as used herein, refers to avoiding or obstructing something, in this case, preventing the removal of moisture (by evaporation) and the vitamin B3 compound (by film bonding the surface of the The term "trapping matrix" as used herein, refers to unilamellar, multilamellar vesicles, cylindrical micelles, hexagonal liquid crystals, lamellar liquid crystals or cubic phase liquid crystals capable of binding to the skin. the vitamin B3 compounds and, in this way, maintains the contact of the skin with the vitamin B3 compound. In addition, since the association structures of the present invention are thermodynamically stable, it is believed that the entrapped or bound polar solvent is released slowly over time. The slow release of the polar solvent thus helps maintain the vitamin B3 compound in solubilized form, thereby improving the skin penetration of the vitamin B3 compound. The occlusive effect is further increased with the addition of wax or wax type (or gel type) solidification agents described above. The surfactants can be used at levels from 4% to about 97% to about 97%, preferably from about 5% to about 95%, most preferably from about 20% to about 90% and most preferably about 30%. % to about 70% of the association structure.
Polar Solvent The solvents useful for making the association structures of the present invention include any polar solvent. In general, "polar solvents" refers to solvents that contain hydroxyl and / or carbonyl groups and also have high dielectric constants and a strong polarity. Suitable polar solvents include: water; alcohols, such as ethanol, propyl alcohol, isopropyl alcohol, hexanol, and benzyl alcohol; polyols, such as propylene glycol, polypropylene glycol, butylene glycol, hexylene glycol, maltitol, sorbitol, and glycerin; Panthenol dissolved in glycerin; flavoring oils, and their mixtures. Mixtures of these solvents can also be used. The preferred polar solvents are polyhydric alcohols and water. Examples of preferred solvents include glycerin, panthenol in glycerin, glycols such as propylene glycol and butylene glycol, polyethylene glycols, water and mixtures thereof. The most preferred polar solvents to be used are alcohols, glycerin, panthenol, propylene glycol, butylene glycol and mixtures thereof. The cosmetic compositions of the present invention will comprise from about 0.01% to about 90%, preferably from about 0.1% to about 60%, most preferably from about 1% to about 30% and most preferably from about 3% to about 18% by weight of the polar solvent composition. Preferably, the solvents are used in relation to the association structures at levels from about 3% to about 96%, preferably from about 5% to about 95%, most preferably from about 10% to about 80% and most preferably from about 30% to about 70% by weight of the association structure.
Preparation of the association structure The formation of the association structure, ie, cylindrical inverse micelles and / or liquid crystals and the concentration at which these association structures occur depend on a variety of factors, including the specific types of surfactant , solvent, temperature, solubility of the surfactant in the solvent, and concentration of the surfactant in the carrier. The purity of the surfactant affects the level of concentration at which the association structures are formed and particularly the preferred form of laminar liquid crystals. The polar solvent and surfactant are mixed together. The formation of association structure, particularly the preferred hexagonal or lamellar liquid crystalline state, is accelerated by mechanical agitation. The mixture can be enhanced either by hand (ie using hand tools) or with useful mechanical equipment for domestic, institutional or industrial cosmetic preparation. Extruders can be used that provide a cutting operation with mixing. The most preferred one is the liquid crystal of a phase. It is preferred that a substantially single-phase liquid crystal, single phase liquid crystal or single phase liquid crystal (preferably at least 90%) be used. The separation and therefore the detection of the association structure of the excess liquid or solid (solvent or solution) can be achieved by ultracentrifugation. It should be performed using sufficiently high centrifugal force (preferably on the scale of about 20,000 revolutions per minute to about 60,000 revolutions per minute from about an hour to about sixteen hours using a Beckman L8-80 centrifuge equipped with an SW60TÍ engine or applying approximately 300,000 * g for approximately one hour) to induce the formation of observable phase limits for a period of time. Under these conditions a good separation of the individual phases is obtained. The volume of each phase is determined by calibration of the centrifuge tube and thus the volume fraction of the individual phase is calculated. Optionally, the compositions of the present invention may include additional colloidal structures. Non-limiting examples of colloidal structures, emulsions and gel networks. A detailed description of these and other useful colloidal structures is found in Niels J. Krog, Food Emulsifiers, p. 141 188, marcel Dekker, Inc., (1997), which is incorporated herein by reference in its entirety.
OPTIONAL COMPONENTS Color Certain embodiments of the present invention, preferably lipstick or lip paints, may further comprise from about 1% to about 90%, preferably about 1% to about 35%, more preferably from about 1% to about 20% and more preferably from about 5% to about 15% color, on a weight basis of anhydrous pigment. These are usually aluminum, barium or calcium salts or lacquers. Preferably, the dyes are present in about 0.1% to about 4% or nacre of about 0% to about 20%. The pigments are typically dispersed in emollients for good dispersion of the pigments when incorporated into the lip compositions, and thus provide a uniform color distribution. Excellent pigment dispersion can be achieved by using association structures, preferably lamellar liquid crystals, as a means to incorporate the colors / pigments in the cosmetic compositions of the present invention. A preferred method for incorporating dry pigments comprises the steps of: (a) preparing a mixture consisting basically of: (1) a polar solvent; and (2) a surfactant selected from the group consisting of amphoteric, cationic, anionic and nonionic surfactants having a Krafft a point or below the ambient temperature and mixtures thereof; and (b) stirring said mixture until the association structures are formed; (c) add and mix dry pigments until a homogenous mixture is obtained; (d) grinding the mixture until a uniform particle size is achieved; (e) add and mix the mixture of (c) to the remaining ingredients until a homogenous mixture is obtained. If the ingredients of the cosmetic composition are processed so that the association structures are formed in situ, the preferred method of incorporating the dry pigments is to suspend them in one or more of the liquid emollient ingredients. The colors / pigments suitable for use herein are all inorganic and organic colors / pigments suitable for use in lipstick compositions. Lacquers are also a pigment that is extended or reduced with a solid diluent or an organic pigment that is prepared by the precipitation of a water-soluble dye or an absorption surface, which is generally an aluminum hydrate. There is no certainty in some cases if the soluble dye is precipitated on the surface of the aluminum hydrate to produce a dyed inorganic pigment or is precipitated merely in the presence of the substrate. A lacquer is also formed from a precipitation of an insoluble salt from an acid dye or a basic dye. The calcium and barium lakes can also be used here. Lacquers suitable for use in the present invention include red aluminum lacquer 3, red aluminum lacquer 21, red aluminum lacquer 27, red aluminum lacquer 28, red aluminum lacquer 33, yellow aluminum lacquer 5, yellow aluminum lacquer 6, yellow aluminum lacquer 10, aluminum lacquer orange 5 and blue aluminum lacquer 1, red barium lacquer 6, red calcium lacquer 7. Other colors and pigments can also be included in lipsticks such as dyes and nacres, dioxides of titanium, dyes Red 6, Red 21, Coffee, Berber and Siena color, lime carbonate, talcum, iron oxides and titanate micas. Preferably, the color component is particulate solids having an average primary particle size diameter of less than about 5 microns, preferably 2 microns, more preferably 1 micron. Without being limited by any theory, it is believed that the solid particles are placed themselves at the interface of scattered droplets (ie, the discontinuous phase) and the continuous phase serves as a barrier, preventing coalescence of scattered droplets and, therefore, improving stabilization. A more detailed explanation of this phenomenon is described in S. E. Friberg and Káre Larsson, Food Emulsions, p. 36-41, Marcel Dekker, Inc. (1997), included herein as a reference in its entirety. The dispersants can also be used in conjunction with the colors and pigments of the present invention. Examples of suitable dispersants include, but are not limited to, those described in U.S. Pat. 5,688,493, incorporated herein by reference in its entirety.
Other additives Other optional ingredients that may be present in the cosmetic compositions of the present invention include flavor oils, fat-soluble vitamins such as vitamin A and E, vitamin A esters (eg, acetate, propionate or palmitate) or vitamin E (e.g., acetate or sorbate), sunscreens such as octyl methoxycinnamate, butyl methoxydibenzoylmethane, titanium dioxide and zinc oxide, germicides such as triclosan, anti-inflammatory agents such as hydrocortisone, lipid materials such as ceramides and liposomes and other active ingredients for skin care. The cosmetic compositions may comprise ingredients conventionally employed in cosmetic compositions, such as mascara, make-up base or lip care products. This includes active ingredients for skin care, such as pharmaceutically active ingredients.
The active ingredients for skin care in both water-soluble and water-insoluble forms can be added to the cosmetic compositions of the present invention. These include but are not limited to vitamin C and its derivatives (eg, ascorbyl palmitate, ascorbyl phosphate and its salts such as magnesium or sodium), vitamin D, panthenol, calconas, flavonones, retinoic acid, titanium dioxide, oxides of iron, zinc oxide, beta-glycerietic acid; chamomile oil; ginko biloba extract; pyroglutamic acid, salts or esters; sodium hyaluronate; 2-hydroxyoctanoic acid; sulfur; salicylic acid; carboxymethylcysteine, and mixtures thereof.
These additives, both fat soluble and water soluble, will be present in amounts of less than about 10% by weight, generally in the range of about 0.01% to about 5%, preferably about 0.01% about 3%, more preferably about 0.1% to about 1% by weight.
Organic binders such as stearic acid, paraffin, butyl acetate, ethylene vinyl acetate copolymer, butyl methacrylic acid ester, dibutyl phthalate, polyester and mixtures thereof may be used in the present invention.
Flavor oils such as peppermint oil, orange oil, citrus fruit oil, wintergreen oil, can be used together with alcohol or glycerin. Flavor oils are generally mixed in a solvent such as ethanol to dilute the flavor. The flavor oils useful herein may be derived from natural sources or may be prepared synthetically. Generally, flavor oils are mixtures of ketone, alcohols, fatty acids, esters and terpenes. The term "flavor oil" is generally recognized in the art as a liquid that is derived from botanical sources, i.e. leaves, bark, or peel of fruits or vegetables, and which are generally insoluble in water. The flavor oil used can vary from 0% to about 5%, preferably from about 0.01% to about 5%, preferably from about 0.01% to about 1%.
Additional humectants may also be included in the compositions of the present invention. Preferred humectants include pyrrolidone carboxylic acid, sodium lactate or lactic acid, urea, guanidine, glyceric acid and its salts (eg, calcium salt), petrolatum, collagen, ether, α-hydroxypropyl glyceryl, α-hydroxy acids (eg. example, ethylglycolic acid, leucic acid, mandelic acid, glycolic acid), glucosamines, and elastin fibers, D-panthenol, allantoin and hyaluronic acid and chondroitin sulfate. Examples of suitable humectants can be found in Cosmetic Bench Reference, p. 1.30-1.32 (1996), which is incorporated herein by reference.
Also useful herein are emulsifiers commonly known as binding agents. When used, the total concentration of the emulsifier can be from about 0.1% to about 30%, preferably from about 1% to about 15%, more preferably from about 1% to about 15% and more preferably about 1 % to about 5% by weight of the composition. Examples of suitable emulsifiers can be found in the patent of E.U.A. 5,085,856 to Dunphy et al.; Japanese Patent Publication Sho 61-83110; European patent application EP 522624 to Dunphy et al .; patent of E.U.A. 5,688,831 to El-Nokali et al. Examples of other suitable emulsifiers can be found in Cosmetic Bench Reference, pp. 1.22, 1.24-1.26 (1996), all incorporated herein by reference in their entirety. A preferred embodiment of the present invention preferably comprises: a) from about 1% to about 10% niacinamide, b) from about 0.1% to about 50%, preferably from about 0.1% to about 15% polar solvent c ) from about 0.1% to about 20% surfactants of the cosmetic composition and d) from about 0.1% to about 50% of an oil that is liquid at room temperature. The surfactants are preferably a mixture in which from about 50% to about 75% of the mixture is made of surfactants having a Krafft point of at or below room temperature and form association structures at room temperature and about 25% to about 50% of the mixture is made of surfactants that are coupling agents. Another preferred mixture of surfactants which can form surfactant association structures which act as a coupling agent is lecithin, PG-3 diisostearate, sorbitan monooleate, cholesterol 12-hydroxystearate and dipentaerythritol fatty acid ester.
A preferred optional component is ethylcellulose (Ethocel). Ethylcellulose is generally preferred for use at levels of about 5% and more preferably 1%.
Another preferred optional component is silica. Silica is generally preferred for use at levels of about 1% and about 5%. The hypoallergenic compositions can be made from the liquid crystal, wax, oils and colors of the present. These compositions should not contain fragrances, flavor oils, lanolin, sunscreens, particularly PABA or other potential sensitizers or sensitizers and irritants. The compositions of the present invention can also be made in long-lasting or non-transferable cosmetic compositions. Detailed discussions of such lipsticks are found in Japanese Patent Publication Hei No. 6-199630 and European Patent Application 748622, both incorporated herein by reference in their entirety. Additional optional materials that can be incorporated into the compositions of the present invention can be found in the PCT application WO 97/39733, for Oblong et al.
MANUFACTURING METHODS The present invention encompasses methods for preparing stable cosmetic compositions comprising vitamin B3 compounds. Conventional formulation and mixing techniques can be used and generally comprise dissolving vitamin B3 compounds in a polar solvent and adding the solution to a hydrophobic base composed of an emollient component, and a stabilizing system comprising a solidifying agent and a surfactant, producing a composite cosmetic composition as already descd. In a preferred embodiment, this invention provides a method for improving skin penetration of vitamin B3 compounds, especially in radii and improving the stability of the product. The conventional formulation and mixing techniques are descd in detail in Harrv's Cosmeticoloav. pp. 119-141 and 314-354 (J.B. Wilkinson and R.J. Moore T ed 1982). and Cosmetics: Science and Technology, pp. 1-104 and 307-422 (M.S. Balsam and E. Sagarin 2nd ed. 1972), which are hereby included in their entirety by way of reference.
METHODS OF USE The cosmetic compositions of the present invention are suitably adapted for use in the treatment of skin and lips, especially in the form of a lipstick or lip balm to apply a permanent or semi-permanent color to the lips, ideally with a lustrous finish or shining The cosmetic compositions can also be used to treat the skin and / or lips with a skin care agent for protection against exposure to adverse weather, including wind and rain, dry and / or hot environments, contaminated environments (e.g. , ozone, smoke, and the like), or exposure to excessive doses of sunlight. The compositions are also useful for providing sun protection, moisturizing and / or conditioning for the hair and skin, improving the feeling of the skin, regulating the texture of the skin, reducing fine lines and wrinkles, reducing the greasy shine on the skin. hair or skin, lightening the skin and reducing the smell of the skin and hair. The cosmetic compositions can, accordingly, be applied to the skin and / or lips in the traditional manner using a convenient handle or applicator to provide a decorative and / or protective film thereto.
EXAMPLES The cosmetic formulations illustrated in Examples I-X illustrate the specific embodiments of the cosmetic compositions of the present invention, but are not intended to be limiting thereof. Those skilled in the art will be able to make other modifications without departing from the spirit and scope of this invention. These exemplified embodiments of the cosmetic compositions of the present invention provide skin penetration improvements of the vitamin B3 compound as well as improve the stability of the cosmetic composition. All the exemplified compositions can be prepared by conventional formulation and mixing techniques. The amounts of the components are listed as percentages by weight and exclude minor materials such as diluents, fillers and the like. The formulations listed, therefore, comprise the listed components and any minor material related to these components.
EXAMPLE I Composition for lipstick Ingredient% by weight Castor oil 18.5 Isopropyl palmitate 11.6 Caprylic / capric / isostearic / adipic triglyceride 7.0 Lanolin 7.0 Red aluminum lacquer 21 7.0 Candelilla wax 6.6 Myristyl ether propylene glycol acetate 6.0 Caprylic / capric triglyceride 5.8 Glycerol 5.0 Water 5.0 Niacinamide 1.0 Titanium dioxide 4.7 Beeswax 4.1 Monoglyceride 3.5 Lanolin oil 2.5 Ozokerite wax 2.5 Phospholipid (soy lecithin) 1.0 Polybutene 0.8 Carnauba wax 0.4 The above ingredients were added to a stainless steel vessel equipped with a heat source. The ingredients were heated to approximately 85 ° C and mixed until homogeneous. This mixture was poured into a mold and cooled to room temperature. The lipstick is applied to the lips to provide color, moisture and improved penetration to the skin of niacinamide.
EXAMPLE li- Composition for Lipstick Ingredient Amount (percent by weight) Carnauba 1.50 Ozoquedite 6.00 Candelilla 4.00 Hydrogenated vegetable oil 5.00 Acetylated lanolin 4.00 Isopropyl isostearate 11.90 Isostearic acid 10.00 Propylparaben 0.10 Cetyl risinoleate 10.00 Ascorbyl Palmitate 1.00 Silica L-700 1.00 Polybutene 2.00 Petrolatum 5.50 Phase Structure of Association Monooleato sucrose 14.00 Niacinamide 2.00 Glycerin 12.00 Pigments 9.00 The ingredients for the Association Structure Phase, except for the pigments, are mixed until the association structures are formed. Once the association structures have been formed, the pigments are added and milled in a three-rmill. The mixture is mixed with other ingredients and mixed until a homogeneous mixture is obtained. (Or alternatively, the above components add and mix together at the same time). This mixture is heated to 85 ° C and poured into a mold at room temperature.
The lipstick is applied to the lips to provide color, moisturization and penetration to the improved skin of niacinamide.
EXAMPLE III- Composition for lipstick Inqredient Amount (percent by weight) Carnauba 1.50 Ozoquedite 6.00 Candelilla 4.00 Hydrogenated vegetable oil 9.00 Isopropyl palmitate 9.40 Stereostaric acid 11.50 Acetylated lanolin 4.00 Propylparaben • 0.10 Cetyl risinoleate 10.00 Ascorbyl Palmitate 1.00 Silica L-700 1.00 Polybutene 2.00 Petrolatum 5.50 Phase of Structure of Associate Monoeroleate of sucrose 12.00 Niacinamide 2.00 Glycerin 12.00 Pigments 9.00 The composition is prepared and used as in Example II.
EXAMPLE IV- Composition for Lipstick Ingredient Quantity (weight percent) Carnauba 1.50 Ozoquedita 5.50 Candelilla 4.00 Hydrogenated vegetable oil 8.50 Acetylated lanolin 4.00 Propylparaben 0.10 Cetyl Risinoleate 10.00 Ascorbyl Palmitate 1.00 Polybutene 2.00 Copolymer1 of polysiloxane 5.97 Petrolatum 5.97 Lanolin anhydrous 5.97 Lecithin Association Structure Phase 22.95 Niacinamide 2.50 Panthenol 1.00 Glycerin 6.00 Pigments 9.00 Water 4.04 1 # 1154-141-1, supplied by GE Silicones. The composition is prepared as in Example II.
EXAMPLE V- Antiperspirant bar Ingredient Quantity (percent by weight) di-n-butylamide of N-lauroyl-L-glutamic acid1 4 12-hydroxystearic acid 2 Water 2.0 Niacinamide 2 Lecithin 0.1 Light mineral oil2 21.1 Diisopropyl sebacate2 40.8 Aluminum zirconium 25 Talc 3 1GP supplied by Ajinomoto, Inc. 2 White benolite mineral oil supplied by Witco Chemical Corp. 3Schercemol DIS supplied by Scher Cherfficals Inc.
In a stainless steel container, the niacinamide is dissolved in water and combined with lecithin to form the association structures. Separately, the gelling agent and the liquid base material are combined in a vessel equipped with a heat source. The mixture is heated to about 80 ° C and about 130 ° C with stirring, until the mixture forms a homogeneous, molten solution. Preferably, the homogeneous, molten solution is allowed to cool to a mixing temperature; typically between about 65 ° C and 120 ° C. (Alternatively, the mixture can simply be heated to mixing temperature until the mixture forms a homogeneous, molten solution, however, this alternative method typically takes longer than heating to high temperatures and then cooling). The mixture of niacinamide, active antiperspirant and other ingredients, such as perfumes and colors, is added in the homogeneous solution, melted in the aforementioned container with agitation. The mixture is allowed to cool until it begins to thicken and is then poured into containers allowing them to cool to room temperature. (Although not preferred, the antiperspirant active can alternatively be added together with the gelling agent and the liquid base material in the first step). An antiperspirant composition, formed as mentioned, is applied to the area under the arm of a human, and reduces perspiration in the applied area and improves odor in this area.
EXAMPLE VI Solid antiperspirant bar Ingredient apuaaa r / oep weight »Stearyl alcohol 9.8 Niacinamide 0.1 Lecithin 1.0 Butylene glycol 1.2 Hydrogenated castor oil mp at 86 ° C 4.0 Aluminum chlorohydroxide 40.0 Isopar 'V" 1 42.9 Perfume 1.0 1 (lsopar "V" average molecular weight 197 BP scale , 255-301 degrees centigrade) In a stainless steel vessel, niacinamide is dissolved in butylene and combined with lecithin to form the association structures. Separately, isoparaffin liquids, water insoluble liquid emollients, surface active agent, and water-insoluble waxes are combined and heated to a temperature sufficient to form a solution of these materials, followed by the addition of the active astringent antiperspirant salts with moderate agitation. After the addition of the niacinamide mixture and the salts, other optional ingredients such as talc may be added and mixed to form a homogeneous suspension. The suspension is cooled to a temperature above the solidification point and then poured into suitable containers. An antiperspirant composition, formed as mentioned, is applied to the area under the arm of a human, and reduces perspiration in the applied area and improves odor in this area.
EXAMPLE VII Antiperspirant cream Inqredient Quantity (% by weight) Cyclomethicone (D5) 41.5 Dimethicone (350 cs) 4.0 Cab-O-Sill HS-51 4.0 Microtensile FN5102 6.0 Natrosol3 2.0 Lecithin 0.5 Niacinamide 0.5 Glycerin 3.0 Isoeicosano4 13.0 Reach AZ5 26.7 Perfume 0.8 1 Colloidal silica thickener material , sold by Cabot Corporation. 2 Low density polyethylene powder, sold by U.S. I Chemicals. 3Hydroxyethylcellulose, sold by Hercules, Inc. 42, 2, 4, 4, 6, 6, 8, 8-dimethyl-10-methylundecane, obtained from Permethyl Corporation, Frazier, PA. 5 Complex of zirconium-aluminum-glycine hydroxychloride, particulate antiperspirant active material, sold by Reheis Chemical Company Cyclomethicone dimethicone, isoeicosan and perfume are added to a stainless steel mixing vessel. Then Cab-O-Sill is added, followed by microteno and natrosol and, finally, the active antiperspirant. The composition is vigorously stirred after the addition of each particulate material. The composition is milled, using a Black &White die-cutter. Decker (model 4420, type 4) with a Cowles dispersion blade of 6.35 cm in diameter at approximately 6,000 revolutions per minute, for approximately 5 minutes. The penetration force value of the milled composition is about 300 grams at 25 ° C and 50% relative humidity. The antiperspirant cream formulation, formed as mentioned, is applied to the area under a human's arm, and reduces perspiration in the applied area and improves odor in this area.
EXAMPLE HIV Mascara Ingredient Quantity (% by weight) Carnauba wax 3.00 Glyceryl monostearate1 7.50 White beeswax 3.75 C18-C362 triglycerides 5.50 Rosinate glycerol hydrogenated3 0.15 Propylparaben 0.10 Paraffin wax 118/125 2.25 Paraffin wax 2.25 Lecithin4 2.25 Stearic acid 3X 4.00 Oleic acid 0.75 Triethanolamine 1.25 Cetylphosphate potassium5 1.00 Shellac, NF 3.00 Trietalonamine 0.47 Trisodium EDTA 0.10 Oxide of black iron 7.00 Dimethicone 0.20 Methylparaben 0.20 Ethylparaben 0.15 Phenoxyethanol 0.80 Alkyl alcohol 40B, test 190 4.00 Diazolidinil urea 0.20 Deionized water 44.78 d1 -panthenol 0.35 Niacinamide 5.00 total 100.00 available as Emerest 2400 from Henkel / Emery- available as Syncrowax HGL-C from Croda, Inc-3 available as Foral 105 from Hercules, Inc- 4 available as Centrolex F from Central Soya, Inc- 5 available as Amphisol K from Giltudan- Las Waxes and fats are mixed in a container equipped with a heat source. The waxes and fats are heated and mixed at low speed using a conventional mixer to liquefy the mixture. Continue mixing until the mixture is homogeneous. Pigments are added to the homogeneous mixture. The mixing speed is increased to high and the pigments are mixed for 30 to 35 minutes until they are uniformly dispersed. Mixing is continued while the emulsifiers are added. In a second vessel equipped with a heat source, water is added followed by niacinamide, lecithin and any other component dispersible in water. The mixture is heated and mixed at a temperature of about 80 to 95 ° C. Additional water is added as necessary to compensate for water loss. The aqueous and lipophilic mixtures are combined and mixed using a dispersing type mixer. Mixing is continued until the mixture is cooled to a temperature of about 65 to 70 ° C. The preservatives are added by mixing, allowing the mixture to cool to 45 to 47 ° C. Any remaining component is added with mixing. The combined mixture is cooled to a temperature above the solidification point and then poured into suitable containers.
The mascara composition is applied to the eyelashes and / or eyebrows to provide softness, wetting and conditioning.
EXAMPLE 9 Mascara Inherent Amount (% by weight) Carnauba wax 2.00 Glyceryl monostearate1 8.50 White beeswax 3.25 Triglycerides of C17-C362 5.50 Hydrogenated glycerol 0.15 Rosinate3 Propylparaben 0.10 Paraffin wax 118/125 2.25 Paraffin wax 2.25 Lecithin4 2.50 Stearic acid 3X 4.00 Acid oleic 0.75 Trietalonamine 2.00 Cetyl phosphate of potassium5 1.00 Deionized water 41.03 Shellac, NF 3.00 Triethanolamine 0.47 Copolymer PVP / VA6 0.25 Oxide of black iron 10.00 Simethicone 0.20 Methylparaben 0.20 Ethylparaben 0.15 Phenoxyethanol 0.80 Ethyl alcohol 40B, test 190 4.00 Diazolidinyl urea 0.20 EDTA trisodium 0.10 d1 -pantenol 0.35 Niacinamide 5.00 total 100.00 1 available as Emerest 2400 from Henkel / Emery-2 available as Syncrowax HGL-C from Croda, Inc-3 available as Foral 105 from Hercules, Inc-4 available as Central Solex from Central Soya, Ino-5 available as Amphisol K from Giltudan - 6 available as PVP A S-630 from ISP The mascara is prepared and used as in example 8.
EXAMPLE 10 Lipsticks Ej. Xa Ej. Xb INGREDIENT T.% T.% Polybutene 4,536 4,536 Lanolin oil 18,342 18,342 Octoxiglyceryl Behenate 18,342 18,342 Stearic Heptanoate 8,856 8,856 Jojoba oil 8,856 8,856 Castor oil 19.28 24.08 Butylated hydroxytoluene 0.054 0.054 Butylated hydroxyanisole 0.054 0.054 Microcrystalline wax 6.84 6.84 Polyethylene 500 6.84 6.84 Association phase Lecithin 0.475 0.475 Water 6 1.2 Niacínamida 1 1 Cholesterol 0.475 0.475 Dicetyl Phosphate 0.05 0.05 In a suitable vessel, castor oil, polybutene, lanolin oil, octoxiglyceryl behenate, stearyl heptanoate, jojoba oil, butylated hydroxytoluene, butylated hydroanisol, microcrystalline wax, polyethylene 500 are added to an equipped container or with a heat source. and heated to a temperature of about 100 to 110 ° C to form a molten material. The molten material is mixed until it becomes homogeneous. Separately, the niacinamide is dissolved in the polar solvent (ie water). Then the niacinamide solution is mixed with lecithin, cholesterol and dicetyl phosphate to form association structures. The association structure / niacinamide mixture is added to the mixture containing castor oil and mixed until they become uniform. The mixture is removed from the air by vacuum and poured into the appropriate mold. The mixture is cooled to room temperature and incorporated into the appropriate container. The lipstick is applied to the lips to provide color, wetting and improved penetration of niacinamide.
EXAMPLE XI Solid compact emulsion Ingredient% p / p Part A Ciclomethicone 245 14.00 Cyclo / dimethicone copolyol (DC5225C) 1 15.00 isononyl ionsonanoate 3.00 Abil Quat 3272 1.00 Part B Laureth 7 (Rhodasurf L-790) 2 0.50 Propylparaben 0.25 Part C MT-600 5.07 Tronox 4.06 Glycerin 4.53 Suspension of black iron oxide 0.10 Suspension yellow iron oxide 1.87 Suspension of red iron oxide 0.33 Zinc oxide 5.00 Niacinamide 5.00 Lecithin 1.00 Methylparaben 0.12 Deionized water 27.33 Part D Talc treated with dimethicone 5.00 Polytrap 1.34 Copolymers of ethylene acrylic acid (EA-209) 3 2.00 Wax de'ozoquetita 3.50 Available from Dow Corning 1 Available from Rhone Poulenc Available from Rhone Poulenc In a suitable container, the ingredients of part C are combined and ground using a Silverson L4R at high speed (preferably from about 9,000 to 10,000 rpm) with 1"disintegrating screen at least for? A or until the mixture is uniform In a separate container, the ingredients of part A are combined and mixed using a Silverson L4R at approximately 3,000 rpm with 2"emulsion screen. The ingredients of part B are combined separately and, before the propylparaben is completely dissolved, part B is added to part A using a Silverson L4R at approximately 3,000 to 4,000 rpm with a 2"emulsion screen, mixing is continued until the mixture is uniform. it is added while maintaining a proper tumbling (ie, using a mixer speed of approximately 6,000 to 8,000 rpm) and then heated to a temperature of about 80 ° C. oxoquerite wax is added to the heated mixture by mixing until the mixture The mixture is then evacuated by vacuum and poured into the appropriate mold.The mixture is cooled to room temperature and incorporated into the proper packaging.The compact solid emulsion is applied to the skin to reduce fine lines and texture. the skin as well as reduce the greasy shine.g.
EXAMPLE XI Long-lasting cosmetic emulsion (Example of association structure) A. Prepare a mixture (part A) by combining in a suitable container the following ingredients: Ingredient% by weight Resin MQ1 43.7 PM99A2 56.3 1 Trimethylsiloxysilicate available from GE. 2 Isododecane available from Presperse.
The mixture is mixed using conventional mixing techniques until the MQ resin dissolves.
Procedures: B. Prepare a mixture (part B) by combining in a suitable container the following ingredients: Ingredient% by weight Silicone rubber SE30 50.0 PM99A 50.0 1 Available from GE.
The mixture is mixed using conventional mixing techniques until the silicone rubber SE30 dissolves.
C. A cosmetic emulsion composition containing part A and part B is prepared by combining the following ingredients: Ingredients% by weight Part A 36.89 Part B 19.00 Pigments 10.00 PM99A * 1.41 Propylparaben 0.20 Bentona ISD 15.00 Water 10.00 Niacinamide 5.00 Lecithin 2.00 Laponite 0.5 1 Available under the trade name Centrolex F by Central Soya In a suitable container, the mixture of part A together with the pigments, propylparaben and PM99A are combined and mixed using an Ultra Turrax T25 homogenizer at approximately 8,000 rpm for approximately 10 minutes or until the mixture is uniform (taking care not to ignite the PM99A ). Bentona ISD is added to the blend combination at approximately 8,000 rpm until the mixture is uniform. The water, niacynamide and lecithin are mixed together in a separate vessel to form association structures and then added to the cosmetic mixture with agitation. The XLS laponite is added to the mixture and mixed using a Ross homogenizer at approximately 3,500 rpm until it is uniform. The mixture of part B is added to the cosmetic mixture and mixed initially at high speed, preferably 1600 rpm, to facilitate dispersion using an IKA mixer. Once sufficient dispersion has been achieved, the speed of the mixer is reduced, preferably to about 1,000 rpm, and the cosmetic mixture is allowed to mix uniformly. The cosmetic mixture is poured into a suitable container and tightly closed for storage, preferably at room temperature. The composition of the cosmetic emulsion is applied to the skin to improve the texture of the skin and provide better penetration into the skin of niacinamide.

Claims (10)

NOVELTY OF THE INVENTION CLAIMS
1. A topical cosmetic composition, useful for improving skin penetration of vitamin B3 compounds, characterized in that it comprises: a) from 0.01% to 50% by weight of the composition, of a vitamin B3 compound; b) from 1% to 90%, preferably from 1% to 80% by weight of the emollient composition, of an oil that is liquid at room temperature; c) from 0.1% to 80% by weight, of a stabilizing system, whose stabilizing system comprises; i) from 0.1% to 90%, by weight of the stabilizing system, of a solidifying agent; and ii) from 0.01% to 30%, by weight of the stabilizing system, of a surfactant, wherein the surfactant has a Krafft point of or less than 20C and forms association structures; Y; d) from 0.01% to 90%, by weight of the composition, of a polar solvent.
2. The cosmetic composition according to claim 1, further characterized in that the vitamin B3 compound is selected from the group consisting of niacinamide, niacinamide derivatives, non-vasodilating esters of nicotinic acid and combinations thereof, preferably niacinamide, nicotinate of tocopherol, and combinations thereof, preferably niacinamide.
3. The cosmetic composition according to claim 1 or 2, further characterized in that the association structure is selected from the group consisting of cylindrical reverse micelles, lyotropic liquid crystals and mixtures thereof, preferably selected from unilamellar vesicles, vesicles multilamellar, reverse cylindrical micelles, hexagonal liquid crystals, liquid cubic crystals, liquid lamellar crystals and mixtures thereof, more preferably are selected from the group consisting of lamellar liquid crystals, reverse hexagonal liquid crystals and mixtures thereof.
4. The cosmetic composition according to claim 3, further characterized in that the aggregates of reverse micelles form spherical network structures, elongated structures, cylindrical structures, vesicles, filamentous structures, or mixtures thereof.
5. The cosmetic composition according to any of claims 1 to 4, further characterized in that the association structure comprises 0.1% to 75%, preferably 5% to 65% of the cosmetic composition.
6. The cosmetic composition according to any of claims 1 to 5, further characterized in that said polar solvent comprises from 10% to 80% of the association structure and wherein said surfactant comprises from 30% to 80% of the structure of association.
7. The cosmetic composition according to any of claims 1 to 6, further characterized in that the polar solvent is selected from the group consisting of water, glycerin, propylene glycol, butylene glycol, hexylene glycol, alcohol, panthenol and mixtures thereof.
8. - The cosmetic composition according to any of claims 1 to 7, further characterized in that the oil is selected in such a way that at least 99% of the types of oils used have solubility parameters that do not differ by more than 0.1 to 1.5.
9. The cosmetic composition according to any of claims 1 to 8, further characterized in that said composition is further characterized in that it comprises from 0.1% to 90%, preferably from 1% to 35%, by weight of the composition, of a color component insoluble in water.
10. A method for improving the skin penetration of vitamin B3 compound by applying a safe and effective amount of the composition to the skin as claimed in claim 1.
MXPA01008140A 1999-02-12 2000-02-10 Cosmetic compositions containing vitamin b3. MXPA01008140A (en)

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EP1152742A1 (en) 2001-11-14

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