CZ20011582A3 - Skin lightening composition - Google Patents

Abstract

Disclosed is a composition comprising: (a) an ascorbic acid compound; (b) a charged, reflective particulate material a preferred embodiment of which is coated Titanium dioxide; (c) a structuring compound whose preferred embodiment is a combination of a surfactant and a fatty alcohol; and a cosmetically-acceptable carrier. Preferred use of such composition is a skin whitening composition. Herein, ascorbic acid compound means ascorbic acid or derivatives thereof which have formula: (II) wherein R<2> and R<3> are independently selected from hydrogen and linear or branched alkyl of 1 to about 8 carbons; M<1> is a metal; and x is an integer of from 1 to about 3. More preferably, R<2> and R<3> are independently selected from hydrogen and linear or branched alkyl of 1 to about 3 carbons; M<1> is sodium, potassium, magnesium, or calcium.

Description

Skin lightening agent

Technical field

The present invention relates to skin lightening compositions. In particular, it is a topical skin lightening agent.

BACKGROUND OF THE INVENTION

Customers often use cosmetic products to care for their skin as well as to improve the health and / or physical appearance of their skin. Rough and / or cracked skin and hyperpigmentation (such as age spots, freckles and brown areas related to exposure to sunlight, skin aging or human skin damage) are those areas that customers typically want to treat. Skin lightening is of particular interest in some Asian populations.

Ultraviolet radiation (UF) tends to cause sunburn, leading to skin darkening and / or hyperpigmentation. It is generally known that conditions that lead to defective or missing tyrosinase, an enzyme involved in the formation of melanin, lead to hyperpigmentation, e.g., albinism. UF rays, as a result of exposure to sunlight, promote the formation of the melanin complex in melanocytes located in the basal layer of the epidermis. Melanin is gradually released from melanocyte dendrites, then diffuses keratinocytes, leading to hyperpigmentation of the skin. This hyperpigmentation may exist in the form of spots, freckles, large spots, unwelcome general darkening and / or inconsistencies in the basal skin.

A variety of compounds and / or additives, such as ascorbic acid and derivatives thereof, kojic acid and derivatives thereof, hydroquinone, arbutin, and a variety of extracts such as licorice are known and usually available for use in skin lightening. Recently, highly sophisticated synthetic ingredients useful for skin lightening are also available in a variety of product forms from a variety of product forms.

L-ascorbic acids (eg, vitamin C) are useful ingredients as skin lightening and / or uniformity agents, as well as a reducing agent, a UF absorbing agent, and an inhibitor of melanin formation in cosmetics. However, it is also known that L-ascorbic acid tends to be unstable in the formulation, resulting in an (undesirable) yellowish coloration of the composition which may eventually start to brown. This may lead to a deterioration in the price of the product.

Some combinations have been suggested to stabilize compositions containing ascorbic acid. Japanese Patent Publication (Kokai) A2 H1-213212, Imamura et al., Issued August 28, 1989, discloses stable cosmetic compositions containing ascorbic acid and gluconic acid derivatives. Japanese Patent A2 H1-305009, Yamada et al., Issued December 8, 1989, discloses stable cosmetic compositions containing ascorbic acid derivatives and cyclodextrin. Japanese Patent A2 H3-63208, Sato, issued March 19, 1991, discloses compositions comprising ascorbic acid and phenoxyethanol. These combinations tend to provide acceptable stability of the compositions, but a change in product appearance to yellow to brown is still observed, especially when stored. Thus, it would be desirable to stabilize the ascorbic acid compositions, especially as the amount of ascorbic acid present in the formulation is increased simultaneously.

Accordingly, there is a need for a stable skin lightening composition that contains increased amounts of the ascorbic acid compound as well as persistent pleasant aesthetic properties of the article. None of the prior art has provided all of the advantageous and beneficial properties of the present invention.

SUMMARY OF THE INVENTION

The present invention relates to a composition comprising:

a) ascorbic acid compound,

(b) charged, reflective bulk material;

(c) a structuring compound; and

d) a cosmetically acceptable carrier.

These and other features, aspects and advantages of the present invention will be better understood from the following description and the appended claims.

Although this specification ends with the claims that underline and clearly claim the present invention, it is believed that the present invention will be better understood from the following description.

All percentages, ratios, and amounts of ingredients referred to herein are based on the actual total amount of the composition unless otherwise indicated.

All measurements herein are performed at 25 ° C unless otherwise noted.

All publications, patent applications, and patents issued herein are hereby incorporated by reference in their entirety. Citation of any reference does not imply acceptance of any determination as to its availability as a field of technology for the claimed invention.

Comprising herein means that other steps and other components that do not affect the final result can be added. The term includes terms consisting of and essentially consisting of.

Topical application here means applying or spreading the material onto the skin surface.

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Lightening the skin herein means changing the appearance of the skin to a brighter, lighter and / or whiter appearance, and improving hyperpigmentation when compared to the previous treatment.

Cosmetically acceptable herein means that the compositions or components thereof so described are suitable for use in contact with the human skin without undue toxicity, incompatibility, instability, allergic response and the like.

A safe and effective amount herein means an amount of a compound or composition that is sufficient to significantly induce positive beneficial effects, preferably a positive skin appearance or skin feel including the beneficial effects independently described herein, but low enough to cause serious side effects, thus, for example, it has provided a reasoned benefit-risk balance in a reasonable assessment by a skilled expert.

Mixtures herein mean that they comprise a simple combination of materials and any compounds that may be derived from that combination.

All ingredients, such as the active ingredients and other ingredients useful in the present invention, may be categorized or described by their cosmetic and / or therapeutic beneficial effects or by their postulated mode of action. However, it is to be understood that the active and other ingredients useful in the present invention may, in some cases, provide more than one beneficial cosmetic and / or therapeutic effect or cause more than one mode of action. Thus, the classification is made here for convenience and is not intended to limit the component to a particular application or list of applications.

The present invention relates to a composition comprising an ascorbic acid compound, a charged, reflective bulk material, a structuring compound, and a cosmetically acceptable carrier.

Without wishing to be bound by theory, it is believed that the great reducing capacity of the ascorbic acid compound provides cell respiration support, enzyme activation and antioxidation. Further, it is believed that topical application of the ascorbic acid compound tends to reduce the oxidized melanin complex itself and its precursors as well as inhibit tyrosinase activity in the melanosome. As a result, it is also contemplated that compositions comprising the ascorbic acid compound can provide beneficial effects to the skin, such as preventing melanin production and reducing age spots, large spots and / or freckles associated with skin hyperpigmentation.

Increasing the concentration of ascorbic acid in the compositions will typically improve the effectiveness of the composition. For example, increasing the amount of ascorbic acid in the skin lightening composition will result in improved skin lightening. Unfortunately, it has been difficult to increase these amounts in the past, since compositions having these increased amounts of ascorbic acid tend to be unstable, especially inedible by their physical properties, as the appearance of the product turns yellow to brown. However, we have now discovered that by incorporating the structuring compound into the composition, the original physical properties of the ascorbic acid compound and its composition may persist, although the composition contains relatively high amounts of the ascorbic acid compound. This stability improvement is particularly effective in an aqueous composition.

A. Ascorbic Acid Compound: The composition of the present invention comprises an ascorbic acid compound. The ascorbic acid compound is selected according to its compatibility with the other ingredients. The ascorbic acid compound may be included in the composition as a substantially pure material, for example, may be an extract obtainable by suitable physical and / or chemical isolation from natural (e.g., plant) sources.

The composition of the present invention preferably comprises from 1.0% to 10.0% by weight. % of an ascorbic acid compound, more preferably from 2.0 to 5.0 wt.

Ascorbic acid compound herein refers to ascorbic acid or derivatives of formula I in w (I).

wherein V and W are each independently -OH and R ¹ is

-CH (OH) -CH ₂ OH, and salts thereof.

Preferably, the ascorbic acid compound useful herein is an ascorbic acid salt or derivative thereof, such as a non-toxic alkali metal salt, an alkaline earth metal salt, and an ammonium salt, usually known to the skilled artisan, but not limited to, sodium, potassium, lithium, calcium, magnesium, bamat, ammonium and protamine salt, which are produced by methods well known in the art.

More preferably, the ascorbic acid salt useful herein is a metal ascorbate of the following formula (II)

wherein R ² and R ³ are independently selected from hydrogen and a linear or branched alkyl of 1 to 8 carbon atoms, M ¹ is a metal and x is a number from 1 to

More preferably, R ² and R ³ are independently selected from hydrogen and C 1 -C 3 linear or branched alkyl, and M ¹ is sodium, potassium, magnesium or calcium.

Examples of preferred salts of the ascorbic acid of formula II include monovalent metal salts (e.g. sodium ascorbate, potassium ascorbate), divalent metal salts (e.g. magnesium ascorbate, calcium ascorbate) and trivalent metal ascorbic salts (e.g. aluminum ascorbate).

Preferably, the ascorbic acid salt useful according to the invention is a water-soluble ascorbyl ester of the following formula III

wherein A is sulfate or phosphate, R ⁴ and R ⁵ are independently selected from hydrogen and C 1 -C 8 linear or branched alkyl, M ² is metal and y is from 1 to 3. More preferably R ⁴ and R 5 ⁵ are independently selected from hydrogen and C 1 -C 3 linear or branched alkyl, and M ² is sodium, potassium, magnesium or calcium.

Examples of water-soluble salt derivatives include, but are not limited to, ester salts of L-ascorbyl phosphate, such as sodium L-ascorbyl phosphate, potassium L-ascorbyl phosphate, magnesium L-ascorbyl phosphate, calcium L-ascorbyl phosphate and aluminum L-ascorbyl phosphate. L-Ascorbyl sulfate ester salts may also be used. Examples are sodium L-ascorbyl sulphate, potassium L-ascorbyl sulphate, magnesium L-ascorbyl sulphate, calcium L-ascorbyl sulphate and aluminum L-ascorbyl sulphate.

B) Charged, Reflective, Bulk Material: The compositions of the present invention also essentially comprise from 0.01% to 5.0%, preferably from 0.1% to 5.0%, more preferably from 0.5% to 2%. 0 wt. by weight of the composition of the charged, reflective bulk material (charged material).

♦ ··

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The charged material preferably comprises a reflective bulk material, such as titanium dioxide, which is coated with a coating material that imparts a net charge that is greater than the zeta potential of the uncoated metal oxide. The charged material may be dispersed in the carrier.

Without wishing to be bound by theory, it is believed that reflective bulk materials, such as titanium dioxide, usually have a relatively high surface activity that creates instability of the formulation. In addition, these reflective bulk materials tend to agglomerate, e.g., form clumps, resulting in precipitation of the reflective bulk material. These problems can be solved by coating the reflective bulk material (metal oxide) with a coating material that imparts a net charge that is greater than the zeta potential of the uncoated reflective bulk material. Typically, the coating material imparts a zeta potential that is greater than ± 20 mV (eg, either in the positive or negative direction) at a pH of from 4 to 8.5. Other such coating materials provide reflective bulk materials with steric hindrance, thereby preventing agglomeration of such charged materials. This provides stability to the composition and prevents agglomeration of the reflective bulk materials (metal oxide). The particles and their charges are well known to those skilled in the art and are well documented in R. J. Hunter: Zeta Potential in Colloid Sciences: Principles and Application (1981), published by Academie Press; J. N. Israelachvili: Intermolecular and Surface Forces: With Applications to Colloidal and Biological Systems (1985), published by Academie Press; and Hoogeven N.G. et al., Colloids and Surfaces, Physiochemical and Engineering Aspects, 1966, 177, 77. All of these publications are incorporated herein by reference in their entirety.

All charged materials preferably have a pure cationic charge or a pure anionic charge. It is believed that since all particles have the same charge, repulsive forces prevent agglomeration and induce even distribution in the hydrophilic phase. As a result, i) lower concentrations of the reflective bulk material provide maximum reflection of visible light in the composition, ii) do not produce an aesthetic negative impact, such as a chalk or rough feel, and iii) reduce instability of the composition. Usage 9 9 9 9 9 9 9 9 9 9 9 9 Thus, the charged materials provide effective pn coverage to a relatively low amount of charged materials.

Charged materials useful in the compositions of the present invention will typically have a refractive index of at least 2, more preferably of at least 2.5, e.g. from 2 to 3. The refractive index can be determined by conventional methods. For example, a method of determining the refractive index that is applicable according to the present invention is described in JA Dean (ed.): Lange's Handbook of Chemistry, 14th Edition, McGraw Hill, New York 1982, Part 9, Refractometry, which is hereby incorporated by reference in its entirety. link.

Preferred charged materials are those having a primary particle size of from 100 nm to 300 nm, more preferably from 10 to 250 nm in pure form (i.e., substantially pure powder form prior to coupling with any carrier). Preferred charged materials have a primary particle size when dispersed in the composition of from 100 nm to 1000 nm, more preferably from 100 nm to 400 nm, even more preferably from 200 nm to 300 nm. The primary particle size can be determined using 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, which is incorporated herein by reference.

The particles may have a variety of shapes, including spherical, spherical, elliptical, lamellar, irregular, acicular and rod-like, provided that the desired refractive index is achieved. The bulk material can exist in a variety of physical forms, including rutile, anatase, or combinations thereof.

i) Reflective Bulk Material: Reflective Bulk Material herein is a metal oxide, preferably comprising particles of inorganic material such as titanium dioxide, zinc oxide, zirconia, alumina and combinations thereof, more preferably titanium dioxide, zinc oxide and combinations thereof ( the combinations are meant to include particles that contain one or more of these materials as well as mixtures of such bulk materials), and most preferably the particles consist essentially of titanium dioxide.

The reflective bulk material may be a composite, eg deposited on a core or mixed with other materials such as, but not limited to, silica, silicone resin, mica, and nylon.

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Inorganic bulk materials, such as titanium dioxide, zinc oxide, zirconia or alumina, are commercially available from a variety of sources. One example of a suitable bulk material includes Tronox ™ (titanium dioxide series) and SAT-T CR837 (rutile titanium dioxide) available from U.S. Pat. Cosmetics, CR-50 titanium dioxide available from Ishihara Sangyo Kaisha and JA-1 titanium dioxide available from Tayca Corporation.

The compositions may contain other inorganic or organic bulk materials. However, it is preferred that the bulk materials in the compositions of the invention consist essentially of the bulk material described in this section.

ii) Coating Material: The reflective bulk materials described herein are preferably coated with a coating material which gives them a net charge that is greater than the zeta potential of the uncoated reflective bulk material. Thus, any coating material can be used as long as the net charge (cationic or anionic) imparted to the reflective bulk material is greater than that of the unprocessed reflective bulk material. However, all of the particles in the composition are preferably treated with the same net charge, e.g. no cationic and anionic coating materials are mixed to achieve favorable properties resulting from repulsive forces between the reflective particles. It is understood by one skilled in the art that, however, small amounts of oppositely charged coating materials can be used as long as the overall repulsive forces are maintained.

Non-limiting examples of coating materials that impart 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, hydroxypropylchitosan, quatemium-80, polyquatemium-7, and mixtures thereof.

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0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 ** 0

Non-limiting examples of coating materials that impart 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 copolymer, polysioloxane, dimethicone copolyol phosphate, dimethicone copolyol, dimethicone copolyol, dimethicone copolyol, dimethicone copolyol, dimethicone copolyol hydroxystearate, phosphate ester, sodium chondroiton sulphate, sodium hyaluronate, ammonium hyaluronate, sodium algenate, ammonium laurate, sodium laurate, potassium laurate, ammonium myristate, sodium myristate, potassium palmitate, palmitate, palmitate ammonium, sodium stearate, potassium stearate, ammonium oleate, sodium oleate, potassium oleate, and mixtures thereof. More preferred are anionic coating materials selected from the group consisting of ammonium polyacrylate, sodium polyacrylate, and mixtures thereof.

Charged materials (eg, treated with a coating material) are available in substantially pure, powdered form or pre-dispersed in various types of carriers including, but not limited to, water, organic hydrophilic diluents such as lower monohydric alcohols (e.g. (1-4 carbon atoms) and low molecular weight glycols and polyols, including propylene glycol, polyethylene glycol (e.g., 200-600 g / mol), polypropylene glycol (e.g., 425-2025 g / mol), glycerol, butylene glycol, 1,2,4-butanetriol, sorbitol esters, 1,2,6-hexanetriol, ethanol, isopropanol, sorbitol esters, butanediol, propanol ether, ethoxylated ethers, propoxylated ethers, and combinations thereof. The charged bulk materials are preferably pre-dispersed in water, glycerin, butylene glycol, propylene glycol, and mixtures thereof. Examples of commercially available charged bulk materials include Kobo BG60DC (titanium dioxide and butylene glycol-treated chitosan pre-dispersion), Kobo GLW75CAP (titanium dioxide-treated ammonium polyacrylate pre-dispersion, water and glycerin), Kobo GLW75CAP-MP (pre-dispersion). 99 99 99 999 99 ammonium acrylate treated with titanium dioxide, water, glycerine, methylparaben and propylparaben), all available from Kobo Products Inc., Established in South Plainfield, NJ

C. Structuring Compound: The composition of the present invention comprises a structuring compound. A structuring compound herein refers to a compound that forms an organized structure, a gel cross-linked system, so that the system may exist in hydrophobic or hydrophilic components. The structuring compound is believed to assist in achieving good rheological properties of the composition that contribute to the stability and pleasant aesthetic properties of the composition. The structuring compound is preferably present in an amount of from 1.0% to 10.0%, more preferably from 2.0% to 8.0% by weight. means.

Preferably, the structuring compound comprises a fatty alcohol and an amphiphilic surfactant. Without wishing to be bound by theory, it is believed that the fatty alcohol together with the amphiphilic surfactant is oriented to form a lamellar structure, resulting in the persistence of the oil and water phases. It is also believed that such an organized structure, called a fatty acid gel cross-linked system, contributes to the stability of the composition.

The fatty alcohols useful herein means a linear or branched, saturated fatty alcohol selected from the group consisting of linear or branched, saturated C 12 -C30 fatty alcohols, linear or branched, saturated C 12 -C30 diols. and mixtures thereof. Preferred fatty alcohols are cetyl alcohol, stearyl alcohol and mixtures thereof. The fatty alcohols useful in the present invention are preferably present in the composition in an amount of from 1.0% to 10.0%, more preferably from 1.0% to 5.0% by weight.

Amphiphilic surfactants useful herein include surfactants, any of a variety of nonionic, cationic, anionic, zwitterionic and amphoteric surfactants and mixtures of these surfactants.

Aktivních ·· · · · ··· φφφ · · ··· · φφφφ · φ active agents. Examples of a variety of other surfactants useful in the invention are described in McCutcheoris Detergents and Emulsifiers, North American Edition (1986), published by Allured Publishing Corporation, which is incorporated herein by reference in its entirety. See also U.S. Patent No. 4,800,197, issued to Kowcz et al

On January 24, 1989, which is hereby incorporated by reference in its entirety, for examples of surfactants useful herein. Preferably, the amphiphilic surfactants useful according to the invention are present in the composition in an amount of from 1.0% to 10.0%, more preferably from 2.0% to 6.0% by weight.

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 moiety is esterified at one end with a fatty acid and etherified (e.g., linked via an ether bond) at the other end with a fatty alcohol). These materials have the general formula R ² CO (X ¹ ) ZOR ³ , wherein R ² and R ^{3 are} independently C 10 -C 30 alkyl, X ¹ is -OCH ₂ CH ₂ derived from, for example, ethylene glycol or oxide or -OCH ₂ CHCH ₃ from propylene glycol or oxide and z is from 6 to 100.

Other examples of such 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 thawate, PEG-200 glyceryl thalowate, PEG-8 dilaurate, PEG-10 distearate, glyceryl monostearate, glyceryl distearate, glyceryl monolaurate, glyceryldilaurate and mixtures thereof.

The structuring compound may further comprise a thickening co-agent. Examples of thickening agents useful in the invention are polysaccharides and materials that are primarily derived from natural sources such as gums.

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A variety of polysaccharides known in the art can be used. Polysaccharides, as used herein, means a component comprising a backbone of repeating sugar (i.e., carbohydrate) units. Non-limiting examples of polysaccharides include those selected from the group consisting of cellulose, carboxymethylhydroxyethylcellulose, cellulose acetate propionate carboxylate, hydroxyethylcellulose, hydroxyethyl ethylcellulose, hydroxypropylmethylcellulose, hydroxypropylmethylcellulose, methyl hydroxyethylcellulose, cellulose sulphate, microcrystalline cellulose, microcrystalline cellulose, microcrystalline cellulose, microcrystalline cellulose.

Alkyl substituted celluloses are also useful in the present invention. In these polymers, the hydroxyl groups of the cellulosic polymer are hydroxyalkylated (preferably hydroxyethylated or hydroxypropyllated) to form hydroxyalkylated celluloses, which are then further modified in an ether bond by a straight chain or branched chain alkyl group of 10 to 30 carbon atoms. These polymers typically are straight chain or branched chain alkyl ethers of C 10 -C 30 alcohols. Examples of alkyl groups useful in the invention include those selected from the group consisting of stearyl, isostearyl, lauryl, myristyl, cetyl, isocetyl, cocoyl (i.e., alkyl groups derived from coconut oil alcohols), palmityl, oleyl, linoleyl, linolenyl, ricinoleyl, behenyl and mixtures thereof. Of the alkyl hydroxyalkyl cellulose ethers, a preferred material having the CTFA designation is cetyl hydroxyethylcellulose, which is an ether of cetyl alcohol and hydroxyethylcellulose. This material is sold under the trade name Natroso ^(R) CS Plus by Aqualon Corporation.

Other useful polysaccharides include scleroglucans containing a linear chain of (less than three) linked glucose units with less than 6 linked glucose every three units, a commercially available example of which is Clearogel ™ CS11 from Michel Mercier Products Inc. (Mountainside, N.J.).

Non-limiting examples of gums include materials that are selected from the group consisting of acacia, agar, algin, alginic acid, ammonium alginate, amylopec. 4 4 4 4 4 4 tin, calcium alginate, calcium carrageenan, carnitine, carrageenan, dextrin, gelatin, gelatin gum, guar gum, guar hydroxypropyltrimonium chloride, hectorite, hyaluronic acid, hydrated silica, hydroxypropyl chitosan, hydroxypropyl guar, caraya gum, caraya gum gums, natto gums, potassium alginate, potassium carrageenan, propylene glycol alginate, sodium carboxymethyldextran, sodium carrageenan, gum tragacanth, xanthan gum, and mixtures thereof.

D. Cosmetically Acceptable Carrier: The composition of the present invention comprises a cosmetically acceptable carrier. A cosmetically acceptable carrier herein means one or more compatible solid or liquid fillers, diluents, extenders, and the like which is cosmetically acceptable as defined herein. Compatible herein means that the components of the compositions of the present invention are capable of being mixed with each other in such a way that there is no interaction that would substantially reduce the effectiveness of the composition under otherwise conventional conditions of use.

The cosmetically acceptable carrier useful herein is selected from the group consisting of a hydrophobic component, a hydrophilic liquid carrier, a pH adjusting agent, water, and mixtures thereof. The type of carrier used according to the present invention depends on the type of product desired and may contain several types of carriers including, but not limited to, solutions, aerosols, emulsions (including oil in water and water in oil), gels, solids and liposomes .

1) Hydrophobic component: Hydrophobic components useful in the present invention include lipid, oil, oily or other hydrophobic component. The hydrophobic component is used as a humectant.

A variety of suitable hydrophobic components are known and can be used herein. Numerous examples can be found in Sagarin: Cosmetics, Science and Technology, Second Edition, 1972, 1, 32-43. Non-limiting examples of suitable hydrophobic ingredients include: &lt; tb &gt; ______________________________________ &lt; tb &gt; 9 include mineral oil, petrolatum, straight and branched hydrocarbons of 7 to 40 carbon atoms, esters of alcohols having 1 to 30 carbon atoms, glycerides, alkylene glycol esters, propoxylated and ethoxylated derivatives, sugar esters, vegetable oils and hydrogenated vegetable oils, animal fats and oils, alkyl esters of 4 to 20 carbon atoms of propylene glycols, esters of carboxylic acids of 1 to 20 carbon atoms with polypropylene glycols, and dialkyl (8 to 30 carbon atoms) ethers. Examples of hydrophobic ingredients useful in the present invention are disclosed in U.S. Patent No. 5,306,521, Letton et al., Issued April 26, 1994, in the Gauge Index, Tenth Edition, item 7048, p. 1033 (1983), and in the International Cosmetic Ingredient Dictionary , Fifth Edition, Vol. 1, pp. 415-417 (1993).

The sugar ester of the fatty acids useful according to the invention is a monoester or polyester of 1 to 30 carbons of sugars and one or more carboxylic acid moieties, preferably a sucrose polyester in which the degree of esterification is 7 to 8 and wherein the fatty acid groups are mono- and / or or a di-unsaturated acid of 18 carbon atoms and behenic acid in a molar ratio of unsaturated to behenic from 1: 7 to 3: 5, more preferably octaester of sucrose, wherein there are 7 parts of behenic fatty acid and 1 part of oleic acid, e.g. sucrose cottonseed fatty acid ester.

Preferably, the composition comprises from 2.0 to 95.0 wt. % hydrophobic components, more preferably from 40.0 to 85.0 wt. The hydrophobic component may include an additive derived from animals, plants or diesel and is natural or synthetic (eg, man-made).

2) Hydrophilic Liquid Carrier: The composition of the present invention may comprise a hydrophilic liquid carrier (HLC). A preferred HLC may comprise a dermatologically acceptable, non-aqueous, hydrophilic diluent. Non-limiting examples of hydrophilic diluents are polyhydroxy alcohols such as low molecular weight monovalent alcohols (i.e., 1 to 6 carbon atoms) and low molecular weight glycols and polyols, including propylene glycol, butylene glycol, hexylene glycol, dipropylene glycol, polyethylene glycol (e.g. molecular weight 100 to 1000 g / mol), poles 17 propylene glycol (e.g. having a molecular weight of 425 up to 2025 g / mol), glycerol, 1,2,4-butanetriol, 1,2,6-hexanetriol, and combinations thereof.

The composition preferably comprises from 30% to 95% HLC, more preferably from 40% to 90% by weight. HLC includes water and one or more water-soluble or dispersible components. The exact amount of water in the composition will vary within such ranges as will be determined by the desired and optional selected ingredients.

3) pH Adjusting Agents: The cosmetically acceptable useful composition of the invention may comprise a pH adjusting agent. The pH adjusting agent according to the invention means any component which is used to raise or lower the total pH of the composition to an optimum pH, thereby preventing decomposition of the components (especially the ascorbic acid compound). The optimum pH depends on the choice of the ascorbic acid compound. For example, if the composition comprises magnesium L-ascorbyl phosphate (MAP), the optimum pH is 7.0 to 8.0. Suitable pH adjusting agents of the invention include acetate, phosphate, citrate, triethanolamine and carbonate. Frequently, a combination of the preceding agents is also used to adjust the pH of the composition to a specific optimal pH. The total weight amount of the pH adjusting agent is from 0.01% to 5.0%, preferably from 0.5% to 2.0% by weight. by weight of the whole composition.

4) Other Active Ingredients: The cosmetically acceptable useful composition of the invention may further comprise other active ingredients that are capable of functioning in various ways to enhance the beneficial properties of the ascorbic acid compound and / or to provide other beneficial effects. Examples of such agents include, but are not limited to, a vitamin B ₃ compound, antioxidants and radical scavengers, anti-inflammatory agents, antimicrobial agents, sun filters, and sun blockers and chelating agents. Other active agents useful in the present invention include vitamin A (eg, retinoid, which is commercially available from a number of sources, for example, from Sigma Chemical Company (St. Louis, Mo.) and Boerhinger Mannheim (Indianapolis, In.) And described in the U.S. Pat. No. 4,677,120, Parish et al., issued Jan. 30, 1987; U.S. Patent No. 4,885,311, Parish et al., issued December 5, 1989; U.S. Patent No. 5,049,584 to Purcell et al. U.S. Pat. No. 4,404,356, Purcell et al., Issued September 17, 1991; , issued January 23, 1992, and U.S. Reissue No. 34,075, Purcell et al., issued September 22, 1992), and vitamin K.

i) Vitamin B ₃ Compounds: The vitamin B ₃ compound enhances the skin-enhancing properties of the present invention, particularly in controlling skin condition, including controlling skin aging features, more particularly wrinkles, lines and pores. The vitamin B ₃ compound is preferably present in an amount of 0.01% to 50%, more preferably from 0.1% to 10%, even more preferably from 0.5% to 10% and even more preferably from 1% to 5% by weight.

The vitamin B ₃ compound herein is a compound of the general formula

wherein R is -CONH ₂ (eg niacinamide), -COOH (eg nicotinic acid) or CH ₂ OH (eg nicotinyl alcohol), derivatives thereof and salts of any of the foregoing compounds.

Examples of derivatives of the preceding vitamin B ₃ compounds include nicotinic acid esters, including non-vasodilatory esters of nicotinic acid, nicotinylamine acids, carboxylic acid and nicotinyl alcohol esters, nicotinic acid N-oxide and niacinamide N-oxide.

Suitable nicotinic esters include nicotinic acid esters of 1 to 22 carbon atoms, preferably 1 to 16 carbon atoms, more preferably 1 to 6 carbon alcohols. The alcohols preferably exist with straight chain, branched chain, cyclic or acyclic, saturated or unsaturated (including aromatic) and substituted or unsubstituted. The esters are preferably non-vasodilating. As used herein, the term non-vasodilatory means that the ester usually does not provide a visible blush response upon application of the compositions to the skin of the subject (in the majority of the general population).

there is no skin reddening response, although such compounds may cause vasodilation invisible to the naked eye (i.e., the ester does not cause the skin to flush). Non-vasodilating nicotinic acid esters include tocopherol nicotinate and inositol hexanicotinate; tocopherol nicotinate is preferred.

Other derivatives of the vitamin B ₃ compound are derivatives of niacinamide resulting from the substitution of one or more hydrogen of the amide group. Non-limiting examples of niacinamide derivatives useful herein include nicotinylamino acids derived, for example, from the reaction of an activated nicotinic acid compound (e.g., nicotinic azide or nicotinyl chloride) with an amino acid and organic carboxylic acid esters (e.g., 1 to 18 carbon atoms) with nicotinyl alcohol. Specific examples of such derivatives include nicotinuric acid (C ₈ H ₈ N ₂ O ₃ ) of the formula

O O

II. II

C-NH-CH ₂ COH and nicotinyl hydroxamic acid (C ₆ H ₆ N2O2) of formula

Examples of nicotinyl alcohol esters include nicotinyl alcohol esters with carboxylic acids such as salicylic acid, acetic acid, glycolic acid, palmitic acid and the like. Other non-limiting examples of vitamin B3 compounds useful herein are 2-chlomicotinamide, 6-aminonicotinamide,

6-methylnicotinamide, N-methylnicotinamide, Ν, Ν-dimethylnicotinamide, N- (hydroxymethyl) -nicotinamide, quinolinic acid imide, nicotinanilide, N-benzylnicotinamide, N-ethylnicotinamide, nifenazone, nicotinaldehyde, isonicotinic acid methy · 4 4 4 4 4 4 4 cotinic acids, thionicotinamide, nialamide, 1- (3-pyridylmethyl) urea, 2-mercaptonicotinic acid, nicomol and niaprazine .

Non-limiting examples of vitamin B ₃ compounds are well known in the art and are commercially available from numerous sources, eg, Sigma Chemical Company (St. Louis, Mo.), ICN Biomedicals, Inc. (Irvin, Ka.) And Aldrich Chemical Company (Milwaukee, Wi.).

One or more vitamin B ₃ compounds may be used according to the invention. Preferred vitamin B ₃ compounds are niacinamide and tocopherol nicotinate. More preferred is niacinamide.

When used, salts, derivatives and derivatives of salts of niacinamide are preferably those having substantially the same activity as niacinamide in the methods of controlling the skin condition described herein.

Also useful herein are salts of the vitamin B ₃ compound. Non-limiting examples of salts of the vitamin B ₃ compound useful herein include organic and inorganic salts such as inorganic salts with anionic inorganic particles (e.g., chloride, bromide, iodide, and carbonate, preferably chloride), and salts with organic carboxylic acids (among which include salts of mono-, di- and tri-carboxylic acids having 1 to 18 carbon atoms (e.g., acetate, salicylate, glycolate, lactate, malate, citrate, preferably monocarboxylic acid salts such as acetate). These and other salts of the vitamin B ₃ compound can be readily prepared by a skilled artisan, for example, according to W. Wenner: The Reaction of L-Ascorbic and D-losascorbic Acid 26. Wenner describes the synthesis of niacinamide ascorbic acid salt.

In a preferred embodiment, the ring nitrogen atom of the vitamin B ₃ compound is chemically substantially free (eg, unbound and / or unprotected) or becomes substantially chemically free upon delivery to the skin (alternatively chemically free here alternatively). 44 • 44 44444 ·

44 · 4 4 4 4 · 44 denotes uncomplexed). More preferably, the vitamin B ₃ compound is substantially uncomplexed. Therefore, if the composition comprises a vitamin B ₃ compound in salt or other complexed form, the complex is preferably substantially reversible, more preferably substantially reversible, upon delivery of the composition to the skin. For example, such a complex would be substantially reversible at a pH of 5.0 to 6.0. This reversibility can be readily determined by one skilled in the art.

More preferably, the vitamin B ₃ compound is substantially uncomplexed in the composition prior to delivery to the skin. Examples of approaches to minimizing or preventing the formation of undesirable complexes include omitting materials that form substantially irreversible or other complexes with the vitamin B ₃ compound, pH adjustment, ionic strength adjustment, the use of surfactants and formulation, wherein the vitamin B ₃ compound and materials which form complexes with it exist in different phases. These approaches are well known to those skilled in the art.

Thus, in a preferred embodiment, the vitamin B ₃ compound comprises a limited amount in the form of a salt and more preferably is substantially free of salts of the vitamin B ₃ compound. The vitamin B ₃ compound preferably contains less than 50 wt. such salts, more preferably substantially free of any salt form. The vitamin B ₃ compound in the compositions of the invention having a pH of from 4 to 7 typically contains less than 50% salt.

The vitamin B ₃ compound may be included as a substantially pure material or as an extract obtained by suitable physical and / or chemical isolation from natural sources (eg, plant). The vitamin B ₃ compound is preferably substantially pure, more preferably substantially pure.

ii) Antioxidants and Radical Scavengers: Antioxidants and radical scavengers are especially useful agents to achieve UV protection that can cause increased scaling or structural changes in the stratum coral • ·· ·· φ φ φ φ φ φ · · ♦ · · Φ φφφ

Ochrany φ ΦΦΦΦ φ φ neum and protection against other environmental agents that may cause skin damage.

Antioxidants and radical scavengers such as tocopherol (vitamin E), tocopherol sorbate, tocopherol acetate, other tocopherol esters, butylated hydroxybenzoic acids and their salts, 6-hydroxy-2,5,7,8-tetramethylchroman-2- can be used. carboxylic acid (commercially available under the tradename Trolox ^(R) ), gallic acid and its alkyl esters, especially propyl gallate, uric acid and its salts and alkyl esters, sorbic acid and its salts, amines (ie Ν, Ν-diethylhydroxylamine, aminoguanidine) , mercaptan compounds (i.e. glutathione), dihydroxyfumaric acid and its salts, lycin pidolate, arginine pilolate, nordihydroguaiaretic acid, bioflavonoids, lysine, methionine, proline, dismutase peroxide, silymarin, tea extracts, peels / melanin extracts / seeds extracts. Preferred antioxidants / preferred radical scavengers are selected from tocopherolsorbate and other tocopherol esters, more preferably tocopherolsorbate. For example, the use of tocopherolsorbate in topical formulations and the applicability of the present invention is described in U.S. Patent No. 4,847,071, Bissett et al., Issued July 11, 1989.

(iii) Anti-inflammatory agents: Anti-inflammatory agents enhance the skin's beneficial properties, for example by contributing to uniformity and acceptable skin tone and / or skin color.

Preferably, the anti-inflammatory agent includes a steroidal anti-inflammatory agent and a non-steroidal anti-inflammatory agent. A preferred steroidal anti-inflammatory agent for use herein is hydrocortisone.

A variety of compounds of this class are known to those skilled in the art. For a detailed description of the chemical structure, synthesis, side effects, etc. of non-steroidal anti-inflammatory agents, reference may be made to standard texts, including Anti-Inflammatory and Anti-Rheumatic Drugs, D. Rainsdorf, Vol. I to III, CRC Press, Boca Rarton ( 1985), and Anti-Infammatory Agents, Chemistry and Pharma, 44, 4444, 4 cology, 1, RA Scherrer et al., Academic Press, New York (1974), both incorporated herein by reference.

Also useful are so-called born anti-inflammatory agents. These agents may advantageously be obtained as an extract by suitable physical and / or chemical isolation from natural sources (ie plants, fungi, by-products of microorganisms). For example, alpha-bisabolol, aloe vera, Manistha (extracted from plants of the genus Rubia, especially Rubia Cordifolia), Guggal (extracted from plants of the genus Commiphora, especially Commiphora Mukul), cola extract, chamomile and cornea extract of the order Gorgonaria can be used.

Other anti-inflammatory agents useful herein include compounds of the genus licorice (plant of the genus Glycyrrhiza glabra), including enoxolone and 3-O- (2-OBD-gucopyranosyl-αD-glucopyranosyl) -enoxolone, and derivatives thereof (e.g., salts and esters) . Suitable salts of the foregoing compounds include metal salts and ammonium salts. Suitable esters include saturated or unsaturated esters of acids of 2 to 24 carbon atoms, preferably of 10 to 24 carbon atoms, more preferably of 16 to 24 carbon atoms.

iv) Antimicrobial Agent: Antimicrobial agents, as used herein, means a compound that is capable of killing microbes, preventing microbial development or preventing the pathogenic action of microbes. Antimicrobial agents are useful, for example, in the control of acne. Preferred antimicrobial agents useful in the present invention are benzoyl peroxide, erythromycin, tetracycline, clindamycin, nonandioic acid, resorcinol-phenoxyethanol with sulfur, and Irgasan ™ DP 300 (Ciba Geigy Corp., USA). A safe and effective amount of an antimicrobial agent may be added to the compositions of the present invention, preferably an amount of from 0.001% to 10%, more preferably from 0.01% to 5%, even more preferably from 0.05% to 2%.

(v) Sun filters and sun blockers: Sun filters and sun blockers generally prevent excessive scaling and structure changes due to ultraviolet exposure and may be added to the composition of the present invention, according to the present invention. filtry φ φ φ φ φ . Suitable sun filters and sun blockers may be organic or inorganic.

A variety of conventional sun filters and sun blockers are suitable for use in the present invention. See U.S. Patent No. 5,087,445 to Haffey et al., Issued Feb. 11, 1992; U.S. Patent No. 5,073,372 to Turner et al., Issued December 17, 1991; U.S. Patent No. 5,073,371 to Turner et al. , issued December 17, 1991, and Segarin et al., Chapter VIII, page 189 et seq., Cosmetics Science and Technology 1972, which describes numerous suitable sun filters and sun blockers. Preferred of these sun filters and sun blockers that are useful in the compositions are those selected from 2-ethylhexyl-pmethoxycinnamate (commercially available as PARSOL MCX), butylmethoxydibenzoylmethane, 2-hydroxy-4-methoxybenzophenone, 2-phenylbenzimidiazole -5-sulfonic acids, octyldimethyl-p-aminobenzoic acid, occtrylene, 2-ethylhexyl-N, N-dimethyl-p-aminobenzoate, p-aminobenzoic acid, 2-phenylbenzimidazole-5-sulfonic acid, octocrylene, oxybenzone, homomethylsalicylate, octylsalicylate 4,4'-methoxy-tert-butyldibenzoylmethane, 4-isopropyl-dibenzoylmethane, 3-benzylidene camphor, 3- (4-methylbenzylidene) camphor, titanium dioxide, zinc oxide, silica, iron oxide, Eusolex ™ 6300, Octocrylene, Parsol 1789 and mixtures thereof.

Agents such as those described in U.S. Patent No. 4,937,370 to Sabatelli, issued June 26, 1990, and U.S. Patent No. 4,999,186 to Sabatelli, are particularly useful in the compositions as sun filters and sunblocks. , issued March 12, 1991. The sun filters and sun blockers described in this invention have two distinct chromophore moieties in a single molecule that exhibit different ultraviolet absorption spectra. One of the chromophore parts absorbs predominantly in the UFB region and the other absorbs strongly in the UFA region. These sun filters and sunblocks provide higher efficiency, broader UF absorption, lower skin penetration, and longer-lasting performance relative to conventional sunblocks and sunblocks.

• 4 * φ · φ φ φ · φ φ φ φ φ φ φ φ φ

The exact amounts will depend on the selected sun filter and the desired sun protection factor (SPF). SPF is typically used to measure photoprotection by a sunscreen against erythema. See Federal Register, Aug. 25, 1978, 43 (166), 38206-38269.

A sunscreen or sun blocker according to the invention can also be added to improve the skin, in particular to increase its resistance to water washing or wiping. Preferred sun filters and sun blockers that will provide these beneficial properties are ethylene-acrylic acid copolymers. Compositions comprising this copolymer are described in U.S. Patent No. 4,663,157, Brock, issued May 5, 1987.

vi) Chelating Agents: The term chelating agent, as used herein, means a compound that reacts to remove a metal ion from the system by forming a complex so that the metal ion cannot readily participate in chemical reactions or catalyze chemical reactions. The inclusion of a chelating agent is particularly useful for providing protection against UV radiation, which may contribute to unnecessary scale formation or skin structure changes, and other environmental agents that may cause skin damage.

Examples of chelating agents useful in the present invention are described in U.S. Patent No. 5,487,884 to Bissett et al., Issued Jan. 30, 1996, PCT application 91/16035 and PCT application 91/16034 to Bush et al. Published Oct. 31, 1995. Preferred chelating agents are fluordioxime and derivatives thereof.

4) Other Ingredients: In addition to the ingredients described above, the 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 or flattening agents, including koji-acid, and • this to the skin. Arbutin, WO 95/23780, Kvalnes et al., Published Sep. 8, 1995, skin conditioners, skin penetration enhancers, protective agents for skin, skin soothing agents, skin healing agents, ultraviolet light absorbers or light scattering agents, masking agents, anti-acne agents, anti-androgens, depilatory agents, keratolytic / peeling and cell release agents / peeling agents such as salicylic acid, panthenolic humectants, such as D-panthenol, soluble or colloidal soluble humectants, such as hyaluronic acid and starch grafted sodium polyacrylates such as Sanwet ™ IM-1000, IM-1500 and IM-2500, available from Celanase Superabsorbent Materials, Portsmith, Va., USA, which are described in U.S. Patent No. 4,076,663, proteins, polypeptides and derivatives thereof, organic hydroxy acids, astringent drugs, external analgesics, film-forming agents, absorbents including oil absorbents such as clays and polymer absorbents, abrasives, anti-caking agents, antifoams, binders, biological additive, bulking agents , coloring agents, perfumes, essential oils and their solubilizing agents, natural extract and compounds that stimulate collagen production.

E. Method of Making the Compositions: The compositions of the present invention are generally made by any method conventionally used for obtaining skin care compositions, particularly skin lotions known in the art. Such methods typically include mixing the components in one or more stages to a relatively uniform state with heating or cooling or without heating or cooling, and the like. Typical methods are described, for example, in Harry's Cosmeticology, 7th Edition, Harry & Wilkinson (Hill Publishers, London 1982).

DETAILED DESCRIPTION OF THE INVENTION

The following examples further describe and represent embodiments within the scope of the present invention. These examples are given for the purpose of illustration only and are not to be construed as limiting the present invention since many variations thereof are possible without departing from the spirit and scope of the invention. Where possible they are * 4 * 444

4 4

4 4 4 4 • «3

4

444

4 4 ♦ ··

4 4

444 components identified by their chemical or CTFA name or otherwise defined below.

The compositions set forth below can be made by any conventional method known in the art. Suitable methods and resource kits are as follows:

(units:% by weight)

chemical name AND (B) C magnesium ascorbyl phosphate 4,000 3,000 - sodium ascorbyl phosphate - - 2,000 KOBO GLW75CAP ^MP-1 0.670 1,330 2,000 stearyl alcohol - 1,500 - cetylakohol - - 1,500 xanthan gum 0.2000 0.020 0.500 a fatty acid ester of a sugar - 1,000 0.500 glycerol 5,000 9,000 7,000 glyceryl monostearate - 3,000 3,000 PEG 100 stearate 0.300 - - Ceteareth-10 - 0.400 0.200 Steareth-21 - 0.200 0.300 isononyl isononanoate 6,000 5,000 3,000 sodium citrate 1,000 1,000 1,000 water add to 100

The above-described compositions are conveniently produced as follows:

«· · · · · · · · · · · · · Φ φ φ φ φ φ φ φ φ φ φ φ φ φ φ φ

(1) dissolve the water-soluble components up to the ascorbic acid compound and sodium citrate and heat the solution to 75 ° C;

(2) mixing a separate aqueous solution of the ascorbic acid compound and sodium citrate and cooling the mixture below 40 ° C;

3) mixing ad 1) and ad 2) and maintaining the temperature at 75 ° C,

4) the mixture of structuring compounds and oil components is heated to 80 ° C;

5) a mixture of 4) is added to the aqueous phase ad 3) followed by high pressure homogenization, and

6) KOBO GLW75CAP-MP and glycerin are added to the mixture of 5) at 30 ° C.

The embodiments described and represented by the preceding examples have many advantages. For example, the composition of the invention contains increased amounts of the skin lightening ascorbic acid compound while exhibiting an improved aesthetic product, such as the appearance of a product that does not change to yellow or brown, even when stored for extended periods of time.

It is to be understood that the foregoing detailed description of the examples and embodiments of the present invention are given by way of illustration only, and that numerous modifications and variations will be apparent to those skilled in the art without departing from the spirit and scope of the invention. These obvious modifications and variations are intended to be included within the scope of the appended claims.

Claims (8)

PATENT CLAIMS 1. A composition for lightening the skin, comprising: a) ascorbic acid compound, (b) charged, reflective bulk material; (c) a structuring compound; and d) a cosmetically acceptable carrier. The composition of claim 1, wherein the structuring compound comprises a fatty alcohol and an amphiphilic surfactant. The composition of claim 2, wherein the cosmetically acceptable carrier is selected from the group consisting of a hydrophobic component, a hydrophilic liquid carrier, a pH adjusting agent, and mixtures thereof. The composition of claim 2, wherein the cosmetically acceptable carrier further comprises at least one other active agent selected from the group consisting of vitamin B ₃ compounds, antioxidants and radical scavengers, anti-inflammatory agents, antimicrobial agents, sun filters, and sun blockers, and chelating agents. The composition of claim 5, wherein the structuring compound further comprises a thickening agent selected from the group consisting of gums and polysaccharides. 6. A skin lightening composition comprising: a) from 1.0% to 10.0 wt. ascorbic acid compounds, b) from 0.01 to 5.0 wt. charged, reflective, loose material, c) from 1.0% to 10.0% of a structuring compound; and d) from 30.0 to 95.0 wt. a cosmetically acceptable carrier. Composition according to claim 6, characterized in that the structuring compound comprises from 1.0% to 10.0% by weight. % of fatty alcohol and from 1.0% to 10.0% by weight of a fatty alcohol; an amphiphilic surfactant. A composition according to claim 7 wherein the cosmetically acceptable carrier comprises from 2.0% to 95.0% by weight of the composition. % hydrophobic components, from 30.0% to 95.0% by weight; % of hydrophilic liquid carrier; and from 0.01 to 5.0 wt. pH adjusting agents.