JP2003502435A - Nicotinamide compositions having reduced tackiness - Google Patents

Abstract

(57) Abstract: The present invention is directed to a topical application leave-on skin care composition comprising: a) an vitamin B ₃ compounds 1 to 10%; and b) i) a weight average molecular weight (MW) 100-1000 branched chain hydrocarbons; and ii) 3-10% of a highly malleable oil selected from liquid ester emollients of formula I Wherein R ¹ is selected from H or CH ₃ , R ² , R ³ , R ⁴ are each independently selected from C ₁ -C ₂₀ straight or branched chain alkyl, and x is 1-20 And a mixture thereof); 0.3 to 4% of an anti-adhesive selected from polyalphaolefin having a molecular weight (MW) of 260 to 1000 in a dermatologically acceptable carrier of the composition, preferably A skin care composition comprising polydecene and an occluding agent selected from petrolatum, cetyl ricinoleate and lanolin. Compositions of the invention, preferably oil-in-water emulsions, containing less than 4% anionic or amphoteric surfactants are useful for maintaining the natural appearance of the skin and are undesirable, such as skin stickiness. It can be applied topically without cosmetic effects. The present invention relates to the further use polydecene or vaseline in order to reduce the tackiness of leave-on skin care compositions comprising 1-10% of a vitamin B ₃ compound.

Description

Detailed Description of the Invention

The present invention relates to the field of topical compositions that improve the appearance and feel of human skin. The present invention particularly relates to leave-on skin care compositions, and more particularly to oil-in-water emulsions that have low tack and are effective in controlling skin condition.

Background A wide variety of compounds have been demonstrated in the art as useful in controlling fine skin lines, wrinkles, and other undesirable skin surface morphologies. For example, vitamin ₃ compounds, especially nicotinic acid amide, regulate skin conditions including wrinkles, wrinkles, and other aging and skin surface irregularities or roughness that are closely associated with light-damaged skin. It has recently become apparent that it offers significant advantages for doing so. However, such substances, when used in clinically effective concentrations,
May cause undesired short-term cosmetic effects, especially sticky or tacky sensations on areas applied to the skin.

Many substances cause a sticky feel on the skin at high concentrations; glycerin is one of the more commonly known ones. Therefore, in the art, there are many methods for reducing the stickiness.

EP-A-692,242 discloses the use of hollow deformable particles having a particle size of 1-250 μm to suppress the sticky feel of compositions predominantly in fatty substances.

WO 92/19217 describes a cosmetic composition in the form of an aqueous gel containing glycerin, a panthenol humectant and a polyglyceryl methacrylate (PGMA) lubricant. This composition is said to have reduced tack. Similarly, WO 93/24101 describes a cosmetic composition composed inter alia of polyhydric alcohols, especially glycerin, and PGMA. It is described herein that trimethylglycine (betaine) is effective from the standpoint of providing improved skin feel and tack reduction effects.

Simultaneous genus PCT application numbers PCT / US98 / 22483 and PCT / US99
/ 04748 discloses that the stickiness of the vitamin B ₃ compound can be offset by the organic fine particles.

Furthermore, it is well known in the art to add emollients containing petrolatum and branched hydrocarbons to vitamin B ₃ compounds, as for example in WO 98/52530.

Co-affiliated PCT application number PCT / US98 / 21521 describes a cosmetic composition having improved rubbing and absorption properties, as well as improved moisturizing properties, skin feel, skin flexibility, and skin smoothness properties. It is disclosed. Examples in said specification include isohexadecane and nicotinic acid amide.

Presently, certain hydrocarbon emollients have been identified that are effective in reducing the stickiness or stickiness of vitamin B ₃ compositions. It may be considered that this substance is surprisingly oily in itself, increasing the stickiness rather than offsetting it.

It is an object of the present invention to provide a vitamin B ₃ composition that is effective in controlling skin conditions and has a reduced stickiness or tackiness.

SUMMARY OF THE INVENTION The present invention relates to a topical leave-on skin care composition which comprises: a) about 1 to about 10% vitamin B ₃ ; b) a highly malleable oil selected from: i) A branched chain hydrocarbon having a weight average molecular weight of about 100 to about 1000; ii) a liquid ester emollient of formula I

[0012]

[Chemical 2]

[0013] (R in the formula¹Is H or CH₃Selected from R², R³, R^Four Are each independently C ₁ ~ C₂₀Selected from straight chain or branched chain alkyl, x is an integer from 1 to 20, and
Then a mixture of them)   iii) a mixture of these; c) a dermatologically acceptable carrier Containing petrolatum, cetylricinoleate and lanolin
An occlusive drug selected from the group consisting of poly (alph
And an anti-adhesive agent of 0.3% to 4% selected from
It

A second aspect of the invention relates to the use of polydecene to reduce the tack of leave-on skin care compositions containing from about 1 to about 10% vitamin B ₃ compounds.
A third aspect of the present invention relates to the use of petroleum jelly to reduce the tackiness of including leave-on skin care composition from about 1 to about 10% of the vitamin B ₃ compound.

The composition is preferably an oil-in-water emulsion, useful for maintaining the natural skin appearance and applied topically without undesirable cosmetic effects such as a sticky feel on the skin. Applicable. Generally, the composition of the present invention is less than about 4%,
It preferably contains less than about 1% anionic, amphoteric or zwitterionic surfactant.

[0016] All percentages and ratios used in the detailed description herein of the invention are by weight of the total composition, and all measurements, unless otherwise stated, are carried out at 25 ° C.. All publications cited in this specification are incorporated herein by reference.

As used herein, the term “leave on” for a skin care composition, after the composition has been applied to the skin, without the rinsing step, the composition is preferably applied to the skin for at least about 15 minutes, More preferably, it is intended to be used to remain for at least about 1 hour, most preferably at least several hours.

The active agents and other components useful herein may be categorized or described herein for their cosmetic and / or therapeutic benefit, or by the mode of action they have. . However, it is understood that the active agents and other components useful herein may in some cases provide multiple cosmetic and / or therapeutic benefits, or act in multiple modes of action. Should be. Therefore, the classification herein is for convenience only and is not intended to limit the components to any particular application or listed application.

The compositions of the present invention are useful for the control of skin conditions including visible and / or tactile discontinuities of the skin, especially those closely related to aging of the skin such as wrinkles. . Such discontinuities are induced or caused by endogenous and / or exogenous factors. Extrinsic factors include ultraviolet light (eg, from sun exposure), environmental pollution,
Includes wind, heat, low humidity, strong surfactants, abrasives, etc. Intrinsic factors include aging and other biochemical changes within the skin.

The vitamin B ₃ compound first essential component of the compositions of the present invention is from about 1 to about 10%, preferably about 2% to 8%, more preferably from about 3 to about 7% vitamin B ₃ compound. Such compounds, when used on their own, may cause a sticky feel, especially at higher concentrations. As used herein, "vitamin B ₃ compound" means a compound having the following structural formula:

[0021]

[Chemical 3]

Wherein R is —CONH ₂ (ie nicotinic acid amide), —COOH (ie nicotinic acid) or —CH ₂ OH (ie nicotinyl alcohol); derivatives thereof; and any of the foregoing. It is salt.

Typical derivatives of the vitamin B ₃ compound include nicotinic acid ester including non-vasodilator of nicotinic acid, nicotinyl amino acid, nicotinyl alcohol ester of carboxylic acid, nicotinic acid N-oxide and nicotinic acid. Amide N-
An oxide is mentioned. The term “non-vasodilatory” as used herein does not normally cause a visible flushing reaction after application of the ester to the skin in the composition of interest (such compounds are of macroscopic invisible vasodilation). It is possible, but it means that the majority of the general population does not have a visible flushing reaction, ie the ester is non-reddening). Non-vasodilators of nicotinic acid include tocopherol nicotinate and inositol hexanicotinate; tocopherol nicotinate is preferred.

Other derivatives of vitamin B ₃ compounds are nicotinic acid amide derivatives obtained as a result of substituting one or more of the amide hydrogens. Examples of nicotinic acid amide derivatives useful in the present invention include, for example, active nicotinic acid compounds (eg, nicotinic azide or nicotinyl chloride), amino acids, and nicotinyl alcohol esters of organic carboxylic acids (eg, carbon number). 1-18) and nicotinyl amino acids derived from the reaction thereof. Specific examples of such derivatives, nicotinuric acid _{(C 8 H 8 N 2 O} 3) and nicotinyl hydroxamic acid _{(C 6 H 6 N 2 O} 2) can be mentioned. Representative nicotinyl alcohol esters include carboxylic acid, salicylic acid,
Mention may be made of nicotinyl alcohol esters such as acetic acid, glycolic acid and palmitic acid. Examples of other vitamin B ₃ compounds useful herein are 2-chloronicotinic acid amide, 6-methyl nicotinamide, N- methyl - nicotine acid amide, and Naiapurajin.

Vitamin B ₃ compounds are well known in the art and can be found in a number of sources including Sigma Chemical Company, St. Louis, Mo .; ICN Biomedicals, Inc. , Irvine, California, USA and Aldrich Chemical Company
, Milwaukee, Wisconsin, USA).

One or more vitamin B ₃ compounds can be used herein.
Preferred vitamin B ₃ compounds are niacinamide and tocopherol nicotinate. Nicotinic acid amide is more preferred.

Salts of vitamin B ₃ compounds are also useful in the present invention. Useful examples include organic or inorganic salts such as inorganic salts having an anionic inorganic species (eg chloride) and organic carboxylates. These and other salts of Vitamin B ₃ compounds are known to those skilled in the art, eg W. Wenner "Reaction of nicotinic acid and its amide with L-ascorbic acid and D-isoascorbic acid" (Organic Chemistry, No. 14, pp. 22-26,
It can be easily prepared as described in (1949). Wenner describes the synthesis of ascorbate of nicotinamide.

In a preferred embodiment, the endocyclic nitrogen of the vitamin B ₃ compound is uncomplexed or undelivered after delivery to the skin. More preferably the vitamin B ₃ compound is essentially uncomplexed. Therefore, if the composition contains as a complex or otherwise the vitamin B ₃ compound as a salt, when the composition is delivered to the skin, such complexes preferably is substantially reversible. Such a complex has a pH of about 5
． It should be substantially reversible from 0 to about 6.0. One of ordinary skill in the art can readily determine such reversibility. Preferably the vitamin B ₃ compound containing the less than 50% in the form of a salt.

The vitamin B ₃ compound may be included as a substantially pure substance, or an extract obtained by suitable physical and / or chemical separation from natural (eg, plant) sources. Vitamin B ₃ compound is preferably substantially pure, substantially means that it does not contain the impurities resulting from the original material. Such compounds are
It is provided as a solution with any antioxidants or other stabilizers.

Highly Spreading Oil A highly preferred composition of the present invention further comprises 3-10%, preferably about 3-8%.
, More preferably about 4 to about 6% of a highly malleable oil selected from: i) a branched chain hydrocarbon having a weight average molecular weight of about 100 to about 1000 and ii) a liquid ester emollient of formula I

[0031]

[Chemical 4]

In the formula, R ¹ is selected from H or CH ₃ , and R ² , R ³ and R ⁴ are each independently C ₁ to
C _{20 is} selected from straight or branched chain alkyl and x is an integer from 1 to 20

These highly malleable oils are useful for delivering vitamin B ₃ compounds to the skin.

Suitable examples of branched chain hydrocarbons include isododecane, isohexadecane and isoeicosane. Preferred is isohexadecane. Poly (alpha olefin) anti-adhesives are described in further detail herein below,
It is generally a branched chain hydrocarbon. When these anti-adhesives are used,
Those amounts are considered to be included in the above-mentioned highly malleable oil concentrations.

Suitable ester emollient materials of formula I above include methyl isostearate, isopropyl isostearate, isostearyl neopentanoate, isononyl isononanoate, isodecyl octanoate, isodecyl isononanoate, Tridecyl isononanoate, myristyl octanoate, octyl pelargonate, octyl isononanoate, myristyl myristate, myristyl neopentanoate, isostearyl neopentanoate, myristyl octanoate, myristyl propionate, isopropyl myristate and Mention may be made of mixtures thereof.

Preferred ester emollients for use herein are isononyl isononanoate, isostearyl neopentanoate, methyl isostearate, isopropyl isostearate, isopropyl stearate, isopropyl myristate and mixtures thereof. .

Particularly preferred highly malleable oils for use herein are isohexadecane, isononyl isononanoate, methyl isostearate, isopropyl isostearate, or mixtures thereof.

Even more preferred for use herein is a mixture of highly malleable oils containing isohexadecane and isopropyl isostearate. Such mixtures are particularly preferred when the composition of the present invention contains a high concentration of glycerin.

The ester emollient material is preferably present in the composition at about 0.1 to about the weight of the composition.
About 10%, preferably about 0.1 to about 8%, particularly preferably about 0.5 to about 5%
Present in a concentration of.

Anti-Adhesive Agent A further essential ingredient of the composition of the present invention is about 0.3 to about 4%, preferably about 0.
5 to about 2.5%, even more preferably about 1 to about 2% molecular weight about 260 to about 10.
No. 00 poly (alpha olefin) anti-adhesive and an anti-adhesive selected from petrolatum, cetyl ricinoleate and lanolin. Poly (
It is clear that (alpha-olefin) anti-adhesives and occlusive anti-adhesives act by different mechanisms but have not been fully elucidated. Nevertheless, both of which are effective in reducing the stickiness of the closely related skin to high concentrations of vitamin B ₃ compound. A mixture of anti-adhesives is not excluded, but a better effect is obtained when the anti-adhesive is selected from one of the two.

Suitable poly (alpha olefins) as described above have about 6 to about 14 carbon atoms, preferably about 6 to about 12 carbon atoms, especially about 8 to about 12 carbon atoms.
It can be derived from alkene monomers. The poly (alpha olefins) useful herein are preferably hydrogenated poly (alpha olefin) oligomers. Examples of 1-alkene monomers useful herein for preparing polyalphaolefin oligomers include 1-hexene, 1-octene, 1-decene, 1-dodecene, 1-tetradecene, 4-methyl-1. -Branched chain isomers such as pentene, and combinations thereof. Most preferred are 1-octene to 1-dodecene oligomers or combinations thereof. Especially preferred is polydecene. A suitable polydecene oil is Mobil Chem.
ical Company, New Jersey 08818, Edison, PO Box 3140
) Under the trade name Puresyn 4 (registered trademark), and BP Amoco (BP A
moco, Illinois 60601-7125, Chicago, Randolph Drive, 200E
) Under the trade name Silkflow 364NF (Silkflo364NF) (registered trademark). The most preferred anti-sticking agent is petrolatum.

Carrier The composition of the invention comprises a dermatologically acceptable carrier suitable for topical application to the skin, such that the essential substances and optional ingredients can be delivered to the skin in suitable concentrations. Essential substances and other optional substances are integrated. The carrier acts as a diluent, dispersant, solvent, etc. for the particulate matter and active agent, ensuring that it can be applied or dispensed at a suitable concentration to the selected target.

Topical compositions useful in the subject invention may be made into a wide variety of product forms as are known in the art. These include, but are not limited to, lotions, creams, gels, sprays, ointments, and mousses. Highly preferred carriers are liquids or semi-solids. Preferably the carrier is in the form of a lotion, cream or gel, more preferably one having sufficient consistency or yield point so that the organic particles do not settle. The carrier is itself inert and the carrier itself may have dermatological benefits. The carrier must also be physically and chemically compatible with the essential ingredients described herein and not excessively impair the stability, effectiveness or other advantages associated with the compositions of the present invention. .

A preferred carrier contains a dermatologically acceptable hydrophilic diluent. Suitable hydrophilic diluents include water, C ₁ -C ₄ monohydric alcohols and propylene glycol, polyethylene glycol (eg molecular weight 200-600), polypropylene glycol (eg molecular weight 425-2025), glycerol, butylene glycol. , 1,2,4-butanetriol, sorbitol ester, 1,2,6-
Hexanetriol, ethanol, isopropanol, sorbitol ester,
Included are organic hydrophilic diluents such as ethoxylated ethers, low molecular weight glycols including propoxylated ethers and polyhydric alcohols, and combinations thereof. The diluent is preferably a liquid. Water is a particularly preferred diluent. The composition preferably comprises at least about 60% hydrophilic diluent.

Preferred carriers are hydrophilic phases, especially aqueous phases, and hydrophobic phases, such as emulsions composed of lipids, oils or oily substances. As is well known to those skilled in the art, the hydrophilic phase is dispersed in the hydrophobic phase, and vice versa, to form a hydrophilic or hydrophobic dispersed continuous phase, respectively, with the composition components. Become. In the emulsification technique, the term "dispersed phase" is a term well known to those skilled in the art and means that the phase exists as small particles or droplets suspended or surrounded by a continuous phase.
The dispersed phase is also known as the internal or discontinuous phase. The emulsion is
It may be or may include a water-in-oil emulsion, such as an oil-in-water emulsion or a water-in-silicone emulsion (eg, as in 3 or other multi-phase emulsions). Oil-in-water emulsions typically contain about 1% to about 50% (preferably about 1% to about 30%) of the dispersed hydrophobic phase and about 1% to about 99% (preferably about 40% to about 40%). 90%) of the continuous hydrophilic phase; water-in-oil emulsions typically contain about 1% to about 98% (preferably about 40% to about 90%) dispersed hydrophilic phase and about 1%. To about 50% (preferably about 1% to about 30%) of a continuous hydrophobic phase. The emulsion is also G.I. M. GM Eccleston's Application of Emulsion Stability Principle to Mobile and Semi-solid O / W Emulsions (Applic
ation of Emulsion Stability Theories to Mobile and Semisolid O / W Emulsio
ns) ”Cosmetics & Toiletries, Vol. 101, November 1996, 73-92.
It may include a gel network as described on page. The preferred composition for the present invention is an oil-in-water emulsion.

Preferred compositions have an apparent viscosity of about 5,000 to about 200,000 mPa.s (
Sentipoise). For example, preferred lotions have an apparent viscosity of about 10,000 to about 40,000 mPa.s, and preferred creams have an apparent viscosity of about 30,000 to about 200,000 mPa.s. The apparent viscosity is measured by Brookfield DVII RV viscometer, spindle TD, 5 rpm,
Alternatively, it can be measured using a viscometer equivalent thereto. Viscosity is determined for a composition after it has been prepared and has been allowed to stabilize under conditions of 25 ° C +/- 1 ° C and ambient pressure, generally for at least 24 hours. After rotating the spindle for 30 seconds, 25 ℃ +/- 1
The apparent viscosity of the composition is measured at a temperature of ° C.

The compositions of the present invention typically have a pH of 9.5 or less, and usually a pH of about 4.5 to about 9,
More preferably, it is blended in the range of about 5 to about 8.5.

Certain compositions, especially those containing additional actives such as salicylic acid, require lower pH, which is desirable for the additional actives to be sufficiently effective. Such compositions are typically formulated to have a pH of about 2.5 to about 5, more preferably about 2.7 to about 4.

Optional Ingredients Optional ingredients are physically and chemically compatible with the essential ingredients described herein, and are of excessive stability, efficacy, or other use associated with the compositions of the present invention. The topical compositions of the present invention may further comprise a wide variety of optional ingredients without compromising the advantages. The optional components may be dispersed or dissolved in the carrier of the present composition.

As an optional ingredient, an emollient, an oil absorbent, an antimicrobial agent, a binder, a buffer, a modifier, a cosmetic astringent, an external analgesic, a film-forming agent, a moisturizer, an opacifying agent, and a fragrance. ,
Pigments, skin smoothing and healing agents, preservatives, propellants, skin permeation aids, solvents, suspensions, emulsifiers, detergents, thickeners, solubilizers, waxes, sunscreens, sunles.
s tanning) agent, antioxidant and / or radical scavenger, chelating agent,
Anti-acne agents, anti-inflammatory agents, exfoliants / exfoliants, organic hydroxy acids, vitamins and natural extracts. A non-limiting example of such a substance is "Harry's Cosmetics".
Cosmeticology ", 7th Edition, Harry & Wilkinson (Hill Publishers, London, 1982);" Drug Form-Dispersion Systems (P
harmaceutical Dosage Forms- Disperse ”, Lieberman, Rieger & Banker, Volume 1 (1988) & Volume 2 (1989) (Marcel Decker, Inc.); Manufacturing (The Che
mistry and Manufacture of Cosmetics), 2nd Edition, deNavarre
(Van Nostrand, 1962-1965); and "The Handbook of Cosmetic Science and Technol.
ogy) ”1st edition, Knowlton & Pearce, (Elsevier (E
lsevier), 1993).

Organic Particulate Materials Preferred compositions of the present invention have a refractive index of about 1.3 to about 1.7 and are dispersed in the composition and have a volume average particle size of about 5 to 30 μm, preferably about 8 to about 25 μm. Including organic particulate matter. Without being bound by theory, an organic particulate material that is at least equal in diameter to the oil layer on the skin formed by the composition of the present invention is a non-greasy oil that improves the overall skin feel and offsets the sticky feeling. It is believed to act as a lubricant.

The volume average particle size is measured in the neat form of the present particulate material, ie in the form of a powder that is essentially pure and prior to binding with the carrier of the present invention. However, each method of measuring particle size may require particulate matter dispersed in an inert carrier, such as refined oil, to measure the particle size distribution. The particle size is Coulter Counter or ASTM
Name E20-85 "Standard Practice for Particle Size Analysis of Particles in the Range of 0.2-75 μm by Optical Microscope
Particulate Substances in the Range of 0.2 to 75 Micrometers by Optical
Microscopy) "(ASTM Volume 14.02, 1993).

Refractive index is measured by conventional methods. For example, a refractive index measuring method applicable to the present invention is described in J. A. McGraw (Langue's Handbook of Chemistry), 14th edition, edited by Dean (JA Dean)
Hill), New York, 1992, Section 3, Refractometry.
The index of refraction is preferably in the range of about 1.35 to about 1.6, which range closely matches the index of refraction of the skin.

The composition of the present invention is preferably about 0.1% to about 10%, more preferably about 0.1%.
It comprises from 3% to about 5%, particularly preferably from about 0.5% to about 2% organic particulate material.

Preferred microparticles are free-flowing, porous, especially spherical particle materials. Suitable organic particulates include polymethylsilsesquioxane as referred to above,
Mention may be made of polyamide, polythene, polyacrylonitrile, polyacrylic acid, polymethacrylic acid, polystyrene, polytetrafluoroethylene (PTFE) and poly (vinylidene chloride). Copolymers derived from monomers of the aforementioned materials can also be used. Preferred are polyamides, especially nylons. Particularly preferred for use in the present invention are porous nylon particles having a volume average particle size in the range of about 15 to about 25 μm. Suitable nylon particles are Elf Atchem SA (Atoc
hem), Paris, France, under the trade name Orgasol®.

The composition may contain other inorganic or organic particulate materials. However, it is preferred that the organic particulates of the composition of the present invention consist essentially of the particulate material described in this section entitled "Organic particulate material".

Inhibitor Pigment Another preferred composition component of the present invention is a green platelet inhibitor pigment having a TiO ₂ layer thickness of about 120 to about 160 nm or an integral multiple thereof. Preferably, the retarding pigment material comprises TiO ₂ coated platelet mica. The color of the reflected light will vary depending on the layer thickness. The suppression pigment material used in the present invention comprises at least a proportion of the pigment material such that the thickness of the TiO ₂ layer is about 120 to about 160 nm or an integral multiple thereof.
When the pigment itself is applied to the skin, the light reflection from the pigment platelets results in an overall green appearance. Without being bound by theory, the inclusion of low concentrations of inhibitor pigments
The pigment itself is believed to help offset the reddish areas of the skin without giving it an unnatural green appearance. In this way, the suppressive pigment helps to provide an overall uniform skin tone. Preferred suppressor pigments for use in the compositions of the present invention have a TiO ₂ layer having a thickness of about 150 nm and about 250 nm, preferably about 150 nm. Suitable examples are the tradename Timiron® supplied by Merck, in particular Chimilon Silk Green, or the tradename Flamenco® supplied by Mearl, Especially flamenco satin green.

Inhibitor pigments are generally used in the present invention in a concentration of about 0.05 to about 1.5%, preferably about 0.1 to about 1%, more preferably about 0.2 to about 0.5%. Exists in.

Inorganic Delustering Agents Inorganic delustering agents such as titanium oxide or zinc oxide are useful in the compositions of the present invention. Matting agents, when present in the present invention, are used at concentrations of 3% or less to avoid unwanted skin whitening or an unnatural "dull" appearance. Preferred for use in the present invention are titanium dioxide and especially anatase titanium dioxide.

Anatase type titanium oxide has a density of about 3.90 g / cm ³ and has a tetragonal cubic close-packed structure. The refractive index of anatase type titanium dioxide is 2.55. Anatase type titanium dioxide is a product name of Kobo (Kobo Products Inc.)
Kobo) BTD11S2, Whittaker, Clark, Daniel (Whittaker, Cla
rk, Daniels), South Plainfield, New Jersey, USA (New Jerse
y, South Plainfield) under the trade name TiO ₂ 9729 under the name Cardre I
nc., South Plainfield, NJ, USA) under the trade name Cardre 70429.

Preferred matting agents for use in the present invention in terms of skin feel, skin appearance, and compatibility with emulsions are surface-treated pigments. The pigments may be treated with compounds such as amino acids such as lysine, silicones, lauroyl, collagen, polyethylene, lecithin, and ester oils. The most preferred matting agents are organosilicone (polysiloxane) treated pigments such as polysiloxane treated titanium dioxide. Most preferred is polysiloxane treated anatase titanium dioxide. The function of the surface treatment is to make the pigment hydrophobically modified so that it becomes "wettable" in the oil phase of the oil-in-water emulsion.

The total concentration of inorganic matting agent is about 0 to about 3%, and preferably about 0.1 to about 2.
It may be 5%, preferably about 0.25% to about 2%.

Panthenol Highly preferred, but an optional component of the composition of the invention is panthenol.
Panthenol is also useful in regulating skin conditions, but in addition it can impart short-term benefits such as moisturizing properties. Panthenol is preferably used at a concentration of 0.1% to about 5%, more preferably about 0.5% to about 3%.

Retinoid The composition of the present invention contains any retinoid. Retinoids are useful in regulating skin condition. As used herein, "retinoid" refers to all natural and / or synthetic analogs of vitamin A or retinol-like compounds that have the biological activity of vitamin A in the skin, as well as the geometric and stereoisomeric forms of these compounds. The body is included. The retinoid is preferably retinol, retinol ester (for example, retinyl palmitate, retinyl acetate, C ₂ -C ₂₂ alkyl ether of retinol such as retinyl propionate), retinal, and / or retinoic acid (all-trans retinoic acid and / or Or 13-cis-retinoic acid) or its esters such as tocopheryl retinoate. Preferably, a retinoid other than retinoic acid is used. These compounds are well known in the art and are commercially available from a number of sources, such as Sigma Chemical Company, St. Louis, Mo., and Boerhiger Mannheim, Indianapolis, Ind. There is. Other retinoids useful herein are those of US Pat. No. 4,677,120 of Parish et al. (6 June 1987).
U.S. Pat. No. 4,885,311 (issued Dec. 5, 1989) to Parrish et al., U.S. Pat. No. 5,049,584 (Purcell) issued Sep. 17, 1991 (September 17, 1991) Issued), U.S. Pat. No. 5,124,356 (issued June 23, 1992) to Purcell et al. And Issue 34,075 (reissued September 22, 1992) issued to Purcell et al. Preferred retinoids are retinol esters such as retinyl palmitate, retinyl acetate, and retinyl propionate. Most preferred are retinyl propionate and retinyl palmitate.

The composition preferably comprises from about 0.005% to about 2%, more preferably from 0.01%.
It contains about 2% retinoid. Retinol is most preferably about 0.01% to
Used in an amount of about 0.15%; the retinol ester is most preferably about 0.0
Used in an amount of 1% to about 2% (eg about 1%); retinoic acid is most preferably used in an amount of about 0.01% to about 0.25%; tocopheryl retinoate is preferably used. Used in an amount of 0.01% to about 2%.

[0066] The topical compositions of the emollient subject invention is generally from about 1% to about 50%, preferably from about 3% to about 15% of a dermatologically acceptable emollient. Emollients tend to make the skin smooth, increase the smoothness and suppleness of the skin, prevent or reduce dryness of the skin and / or protect the skin. Emollients are typically oily or waxy substances that are immiscible with water. The highly malleable oils and anti-adhesive agents of the present invention also act as emollients. A wide variety of other suitable emollients are well known and can be used herein. Sagarin's "Cosmetics, Science and Technology"
and Technology), Second Edition, Volume 1, pages 32-43 (1972), includes examples of many substances suitable as emollients. Illustrative examples of emollients include: i) straight and branched chain hydrocarbons having from about 7 to about 40 carbon atoms such as dodecane, squalane, cholesterol, hydrogenated polyisobutylene, isohexadecane. and branched hydrocarbons C ₇ -C _40, such as isoparaffins C ₇ -C _40. ii) alcohol esters of C ₁ -C ₃₀ C ₁ to carboxylic acids -C ₃₀ and C ₂ -C ₃₀ dicarboxylic acids, for example isononyl isononanoate, isopropyl myristate,
Myristyl propionate, isopropyl stearate, behenyl behenate, dioctyl maleate, diisopropyl adipate and diisopropyl dilinoleate. These include the aforementioned ester emollients. iii) Mono-, di- and toglycerides of C ₁ -C ₃₀ carboxylic acids and their ethoxylated derivatives such as capryl / caprin triglyceride, PEG-6 capryl /
Kaprint glyceride. iv) Alkylene glycol esters of C ₁ -C ₃₀ carboxylic acids, such as ethylene glycol mono- and diesters, and propylene glycol mono- and diesters of C ₁ -C ₃₀ carboxylic acids, such as ethylene glycol distearate. v) sugars and C ₁ -C ₃₀ mono- and polyesters of related substances. Such esters are derived from sugars or polyhydric alcohol moieties and one or more carboxylic acids. Depending on the constituent acids and sugars, these esters can be liquid or solid at room temperature. Examples include: glucose tetraoleate, galactose tetraoleate of oleic acid, sorbitol tetraoleate, sucrose tetraoleate, sucrose pentaoleate, sucrose hexaoleate, sucrose heptaoleate, sucrose octaoleate, carboxylic ester moieties. Is a palmitooleate and arachidate sorbitol hexaester in a molar ratio of 1: 2, and an esterified carboxylic acid moiety is a laurate in a molar ratio of 1: 3: 4,
The octaesters of sucrose are the linoleates and behenates. Other materials include sucrose cottonseed oil or soybean oil fatty acid esters. Other examples of such substances are described in WO 96/16636. A particularly preferred material is known by the INCI name Sucrose Polycotton Seedate. vi) Organopolysiloxane oil Organopolysiloxane oil is volatile, non-volatile,
Or it may be a mixture of volatile and non-volatile silicones. The term "non-volatile" as used in this context is liquid at ambient conditions and has a flash point of about 100 ° C.
The silicone as described above (under 1 atmosphere) is referred to. The term "volatile" as used in this context refers to all other silicone oils. Suitable organopolysiloxanes can be selected from a wide variety of silicones with a wide range of volatility and viscosities. Nonvolatile polysiloxanes are preferred. Suitable silicones are disclosed in US Pat. No. 5,069,897 (issued December 3, 1991).
Preferred for use herein are organopolysiloxanes selected from the group consisting of polyalkyl siloxanes, alkyl substituted dimethicones, dimethiconols, polyalkylaryl siloxanes, and mixtures thereof. More preferred for use herein are polyalkyl siloxanes and cyclomethicones. Among the polyalkyl siloxanes, dimethicone is preferred. vii) Vegetable oils and hydrogenated vegetable oils. Examples of vegetable oils and hydrogenated vegetable oils are safflower oil, castor oil, coconut oil, cottonseed oil, menhaden oil, palm kernel oil, palm oil, peanut oil, soybean oil, rapeseed oil, linseed oil, bran oil, pine oil, sesame oil, sunflower. Included are seed oils, partially and wholly hydrogenated oils of the above materials, and mixtures thereof. viii) Animal fats and oils, for example lanolin and its derivatives such as cod liver oil, acetylated lanolin and isopropyllanolate. Lanolin oil is preferred. ix) The alkyl ether of polypropylene glycol C ₄ -C ₂₀ as useful, carboxylic acid esters of C ₁ -C ₂₀ polypropylene glycol, and there are alkyl ethers of di -C ₈ -C _30, as an example PPG-14 butyl ether, PPG-15 stearyl ether, dioctyl ether, dodecyl octyl ether, and mixtures thereof.

Humectants Highly preferred optional ingredients are humectants, especially hydric alcohol type humectants. Typical polyhydric alcohols include polyalkylene glycols, more preferably alkylene polyols and their derivatives, such as propylene glycol, dipropylene glycol, polypropylene glycol, polyethylene glycol and their derivatives, sorbitol, hydroxypropyl sorbitol. , Erythritol, threitol, pentaerythritol, xylitol, glucitol, mannitol, hexylene glycol butylene glycol (eg 1
, 3-butylene glycol), hexanetriol (eg, 1,2,6-hexanetriol), glycerin, ethoxylated glycerin, and propoxylated glycerin.

Also useful herein are sodium-2-pyrrolidone-5-carboxylate, guanidine; glycolic acid and glycolates (eg, ammonium and quaternary alkylammonium); lactic acid and lactates (eg, ammonium and Quaternary alkylammonium); any form of aloe vera (eg, aloe vera gel); hyaluronic acid and their derivatives (eg, salt derivatives such as sodium hyaluronate); lactamide monoethanolamine; acetamide monoethanol. Amines; ureas; panthenol; sodium pyroglutamate (NaPCA), water soluble glyceryl polyacrylic (methacrylic) acid lubricants (such as Hispagel®) and mixtures thereof.

The compounds listed above may be incorporated alone or in combination. Preferred moisturizers are selected from glycerin, glyceryl polyacrylate, urea, and mixtures thereof. Most preferred is glycerin, which can be used at a concentration of about 1 to about 15%, preferably about 4 to about 14%. It is well known in the art that glycerin produces a sticky feel at these concentrations. It has been clarified that the advantage of reducing the sticky feeling of the vitamin B ₃ compound imparted by the anti-sticking agent of the present invention also reduces the sticky feeling or tackiness of glycerin. For body or face lotions and creams, a glycerin concentration of about 7 to about 15% is suitable, with a preferred concentration of about 9 to about 14%. For hand lotions and creams, a concentration of about 4 to about 8% is preferred,
More preferably, it is about 5 to about 7%.

A particularly preferred formulation of the present invention has a total nicotinamide and glycerin content of about 7%.
To about 16%, preferably about 9 to about 15%, total nicotinic acid amide and glycerin concentrations are preferably about 8 to about 12% for hand use, and for face and / or body use. Preferably includes about 12 to about 15% both nicotinamide and glycerin.

Emulsifier / Surfactant The composition herein preferably comprises an emulsifier and / or a surfactant, usually to help disperse and suspend the discontinuous phase in the continuous phase. Surfactants can also be useful if the product is intended for cleansing the skin. For convenience, hereinafter emulsifiers will be referred to by the term "surfactant", and thus "surfactant" will be used for purposes such as emulsifiers or other surfactants such as skin washes. Shall be used to represent the surface activator. Well-known or previously known surfactants can be used in the composition provided the selected surfactant physically and chemically matches the essential ingredients of the composition and provides the desired properties. Suitable surfactants include silicone materials, non-silicone materials and mixtures thereof.

The composition of the present invention preferably comprises from about 0.05% to about 15% of a surfactant or mixture of surfactants. The exact surfactant or surfactant mixture selected is
It will depend on the pH of the composition and other components present.

Preferred surfactants are nonionic. Among the nonionic surfactants useful herein are those broadly defined as condensation products of long chain alcohols such as condensation products of _C8-30 alcohols with sugars or starch polymers, ie glycosides. is there. Such compounds can be represented by the formula (S) _n —O—R, where S is a sugar moiety such as glucose, fructose, mannose, and galactose; n is from about 1 to about 1000. And R is a C _8-30 alkyl group. Examples of long chain alcohols from which an alkyl group can be derived include decyl alcohol, cetyl alcohol, stearyl alcohol, lauryl alcohol,
Examples thereof include myristyl alcohol and oleyl alcohol. Preferred examples of such surfactants include those where S is a glucose moiety, R is a _C8-20 alkyl group, and n is an integer from about 1 to about 9. Commercially available examples of such surfactants include decyl polyglucoside (Henkel to A
Commercially available as PG325CS), lauryl polyglucoside (from Henkel to APG6
00CS and 625CS) and cetearyl polyglucoside (commercially available from Seppic Corp. as Montanov 68).

Other useful nonionic surfactants include condensation products of alkylene oxides and fatty acids (ie, alkylene oxide esters of fatty acids). These materials have the general formula RCO has the (X) _n OH, alkyl groups of the formula R is C _{10 to 30,} X is (from i.e. ethylene glycol or oxide) -OCH ₂ CH ₂
Or —OCH ₂ CHCH ₃ (ie, derived from propylene glycol or oxide), and n is an integer from about 6 to about 200. Other nonionic surfactants are condensation products of alkylene oxides and 2 moles of fatty acids (ie alkylene oxide diesters of fatty acids). These materials have the general formula RCO (X) _n OO
Has a CR, alkyl group wherein R is C _{10 to 30,} X is -OCH ₂ CH ₂ (i.e.,
It is derived from ethylene glycol or oxide) or -OCH ₂ CHCH ₃ (ie derived from propylene glycol or oxide), and n is from about 6 to about 100 integer. Other nonionic surfactants are condensation products of alkylene oxides and aliphatic alcohols (ie alkylene oxide ethers of aliphatic alcohols). These materials have the general formula R (X) _n OR ', where R is C _10
30 alkyl group, X is -OCH ₂ CH ₂ (i.e. derived from ethylene glycol or oxide) or -OCH ₂ CHCH ₃ - is (i.e. derived from propylene glycol or oxide), and n is from about 6 to R is an integer of about 100
'Is H or a _C10-30 alkyl group. In addition, other nonionic surfactants are condensation products of alkylene oxides with fatty acids and fatty alcohols [ie, the polyalkylene oxide moiety is esterified with a fatty acid at one end and an aliphatic alcohol at the other end]. Are etherified (ie, attached via an ether bond)]. These materials have the general formula RCO (X) _n OR ', where R and _R'are C _10-30 alkyl groups, and X is -OCH ₂ CH ₂ (ie derived from ethylene glycol or oxide) or -OCH. ₂ CHCH ₃ — (derived from propylene glycol or oxide), and n is an integer of about 6 to about 100, and examples thereof include ceteth-6, ceteth-10, ceteth-12, ceteareth-6, ceteareth- 10, ceteareth-12, steareth-6, steareth-1
0, steareth-12, PEG-6 stearic acid, PEG-10 stearic acid,
PEG-100 stearic acid, PEG-12 stearic acid, PEG-20 glyceryl stearate, PEG-80 glyceryl tallowate, PEG-10 glyceryl stearate, PEG-30 glyceryl cocoate, PEG-80 glyceryl cocoate, PEG-200 glyceryl tallowate 200 , PEG-8 dilaurate, PEG-10 distearate, and mixtures thereof.

Still other useful nonionic surfactants include polyhydroxy fatty acid amide surfactants, which are described in more detail in WO98 / 04241.

Preferred nonionic surfactants are steareth-2, steareth-21, ceteareth-20, ceteareth-12, sucrose cocoate, steareth-100.
, PEG-100 stearate, and mixtures thereof.

[0077]   Other suitable nonionic surfactants for use herein include sugar esters and
And polyester, alkoxylated sugar ester and polyester, C₁~ C₃₀The fat
Alcohol C₁~ C₃₀Fatty acid ester of C₁~ C₃₀C of aliphatic alcohol ₁ ~ C₃₀Alkoxylated derivative of fatty acid ester of C₁~ C₃₀Fatty alcohol
An alkoxylated ether of C,₁~ C₃₀Polyglyceryl ester of fatty acid, poly
C of polyhydric alcohol₁~ C₃₀Ester of C, polyhydric alcohol C₁~ C₃₀Ether
Rukyl phosphate, polyoxyalkylene fatty ether phosphate, fatty acid
Mention may be made of amides, acyl lactylates and mixtures thereof. Siri like this
Examples of corn-free surfactants include polysorbate 20, polyethylene glycol.
Cole 5 soy sterol, steareth-20, ceteareth-20, PPG-2me
Chill glucose ether distearate, ceteth-10, polysorbate 80,
Polysorbate 60, glyceryl stearate, sorbitan monolaurate, po
Lioxyethylene 4-lauryl ether sodium stearate, polyglyceryl
-4 isostearate, hexyl laurate, PPG-2 methyl glucose a
Teldistearate, PEG-100 stearate and mixtures thereof.
Be done.

Other emulsifiers useful herein are fatty acid esters mixed with the mixture sorbitan or a mixture of sorbitol fatty acid ester and sucrose fatty acid ester as the main component, said fatty acid being in each case preferably C _{8 to} C ₂₄ , and further preferably a C _{1 0} ~C _20. Preferred fatty acid ester emulsifier is a sorbitan or sorbitol C ₁₆ -C ₂₀ fatty acid esters, sucrose C ₁₀ -C ₁₆ fatty acid esters, especially mixtures of sorbitan stearate and sucrose cocoate. This is an IC
It is commercially available from I under the trade name Arlatone 2121.

Hydrophilic surfactants useful herein include, alternatively or additionally, a wide variety of cationic, anionic, zwitterionic and amphoteric surfactants as are known in the art. Both can be mentioned. For example, McCutcheon's "Detergents and Emulsifiers," North American version (1986), Aloud (
Allured Publisher; US Pat. No. 5,011,681 (Ciotti et al.,
Issued April 30, 1991, U.S. Pat. No. 4,421,769 (Dixon (
Dixon) et al., Issued Dec. 20, 1983), and US Pat. No. 3,755,56.
See No. 0 (Dickert et al., Published August 28, 1973).

[0080]   Anionic, amphoteric and zwitterionic surfactants can be used herein.
Are generally more suitable for rinse-off cleaning compositions, and
Their concentration is kept below 4%, preferably below 1%. Representative anion world
Alcoyl isethionate (for example, C₁₂~ C₃₀), Alkyl
And alkyl ether sulfates and salts thereof, alkyl and alkyl ethers
Terphosphates and their salts, alkylmethyl taurates (eg C ₁₂ ~ C₃₀), And soaps of fatty acids (eg alkali metal salts such as sodium or
Or potassium salt). Representative amphoteric sexes used in the compositions of the present invention and
Alkyl imino acetate, imino dialkanoate as the zwitterionic surfactant
And aminoalkanoates, imidazolinium and ammonium derivatives.
To be Other suitable amphoteric and zwitterionic surfactants are betaines, sultaines, hydrides.
Roxysultaine, alkyl sarcosinic acid (for example, C₁₂~ C₃₀) And alkano
It is selected from the group consisting of irsarcosine acid.

Preferred emulsions of the present invention include silicone-containing emulsifiers or surfactants. A wide variety of silicone emulsifiers are useful herein. Such silicone emulsifiers are generally originally modified organopolysiloxanes,
Also known to those skilled in the art as silicone surfactants. Useful silicone emulsifiers include dimethicone copolyol. These materials are polydimethylsiloxanes, such as those containing moieties derived from both ethylene oxide and propylene oxide, such as containing polyethylene oxide chains, polypropylene oxide chains, and mixtures thereof as polyether side chains. It has been modified to contain as an ether chain. In other instances, dimethicone copolyol and alkyl-modified, i.e., compounds which contain C ₂ -C ₃₀ pendant side chains. Still other useful dimethicone copolyols include materials with a variety of cations, anions, zwitterions, and zwitterpendant moieties.

Thickener components (including thickeners and gelling agents) The compositions of the present invention are also preferably from about 0.1% to about 5%, more preferably about 0%.
． It can also include 1 to about 3%, and most preferably about 0.25 to about 2% thickener component.

Preferred thickener components include cellulose, carboxymethyl hydroxyethyl cellulose, propionic acid carboxylic acid cellulose acetate, hydroxyethyl cellulose, hydroxyethyl ethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, methyl hydroxyethyl cellulose, microcrystalline cellulose, sodium cellulose sulfate. , And mixtures thereof, such as cellulose and its derivatives. Alkyl-substituted celluloses are also useful herein. Among these polymers, the hydroxy groups of the cellulose polymer is hydroxyalkylated to make a hydroxyalkyl cellulose (preferably hydroxyethylated or hydroxypropylated), C ₁₀ -C ₃₀ further through an ether bond Is modified with a straight chain or branched chain alkyl group.
Typically these polymers are a linear or branched chain alcohols of C ₁₀ -C _30, ethers of hydroxyalkyl cellulose. Examples of alkyl groups useful herein include stearyl, isostearyl, lauryl, myristyl, cetyl, isocetyl, cocoyl (ie, alkyl groups derived from alcohol of coconut oil),
And those selected from the group consisting of palmityl, oleyl, linoleyl, linolenyl, ricinoleyl, behenyl, and mixtures thereof.

Other thickeners include acacia, agar, algin, alginic acid, ammonium alginate, amylopectin, calcium alginate, carrageenan calcium, carnitine, carrageenan, dextrin, gelatin, gellan gum, guar gum, hydroxypropyltrimonium chloride guar, and hector. Light, hyaluronic acid, silicon hydroxide, hydroxypropyl chitosan, hydroxypropyl guar, karaya gum, kelp, locust bean gum, natto gum, potassium alginate, carrageenan potassium, propylene glycol alginate, sclerotium gum, carboxymethyl dextran sodium, carrageenan sodium, Tragacanth gum,
Xanthan gum, and mixtures thereof. In addition, B. F. Also useful are acrylic acid / ethyl acrylic acid copolymers and carboxyvinyl polymers sold under the tradename Carbopol resin by the BF Goodrich Company. Suitable carbopol resins are disclosed in WO98. / 220
No. 85.

Preferred compositions of the present invention are thickener components selected from carboxylic acid polymers, cross-linked polyacrylates, polyacrylamides, xanthan gum and mixtures thereof, more preferably selected from polyacrylamide polymers, xanthan gum and mixtures thereof. including. Preferred polyacrylamides are predispersed in a water immiscible solvent such as mineral oil and contain a surfactant (HLB about 7 to about 10) to help promote water dispersibility of the polyacrylamide. Most preferred for use in the present invention is the CTFA designated nonionic polymer, which is available from Seppic.
Polyacrylamide and isoparaffin and laureth 7 sold under the trade name Sepigel 305 from the Corporation.

Anti-Inflammatory Agent A safe and effective amount of anti-inflammatory agent is provided, preferably from about 0.1% to about 5% of the composition.
More preferably about 0.1% to about 2% may be added to the compositions of the subject invention. Anti-inflammatory agents enhance the skin appearance benefits of the present invention, eg, such agents contribute to a more uniform and desirable skin tone or color. The exact amount of anti-inflammatory agent used in the composition will depend on the particular anti-inflammatory agent, as the potency of such agents varies widely.

Anti-inflammatory agents useful herein include steroids such as hydrocortisone;
Non-steroidal anti-inflammatory drugs (NSAIDS) such as ibuprofen; panthenol and ethers and their ester derivatives such as panthenol ethyl ether, panthenyl triacetate; pantothenic acid and salts and their ester derivatives, especially calcium pantothenate Aloe vera, bisabolol, allantoin and licorice (Glycyrrhiza glabra) family (glycyrrhetinic acid,
Glycyrrhizic acid, and derivatives thereof, including salts such as ammonium glycyrrhizinate and esters such as stearylglycyrrhetinic acid esters)
Compounds of Particularly preferred in the present invention are panthenol, pantothenic acid and their ether, ester or salt derivatives, and mixtures thereof,
Suitable concentrations are about 0.1 to about 5%, preferably about 0.5 to about 3%. Panthenol is particularly preferred.

Sunscreens and Sunscreens The compositions of the subject invention may contain sunscreens. Suitable sunscreens can be organic or inorganic. Particularly preferred organic sunscreens include butylmethoxydibenzoylmethane, 2-ethylhexyl-p-methoxycinnamate, phenylbenzimidazole sulfonic acid, and octocrylene. Inorganic sunscreens include zinc oxide and titanium dioxide. The amount of sunscreen agent is typically about 1% to about 20%, and more typically about 2% to about 10%. The exact amount will vary depending on the sunscreen agent selected and the desired sun protection factor (SPF). To improve the skin directness of the compositions useful in the subject invention, especially to increase resistance to washing or scrubbing with water,
A drug may be added to any of the above compositions. A preferred drug that provides such an effect is a copolymer of ethylene and acrylic acid. Compositions containing such copolymers are disclosed in Brock, U.S. Pat. No. 4,663,157 (issued May 5, 1987).

Antioxidants / Radical Scavengers The compositions of the subject invention can further comprise antioxidants / radical scavengers. Antioxidants / radical scavengers are particularly useful for protection from UV radiation, which increases scale-like flaking or tissue changes in the stratum corneum, and from other environmental chemicals that can cause skin damage. . Suitable amounts are from about 0.1% to about 10% of the composition, more preferably from about 1% to about 5%.

Ascorbic acid (vitamin C) and its salts, ascorbyl esters of fatty acids,
Ascorbic acid derivatives (eg magnesium ascorbyl phosphate), β-carotene, tocopherol (vitamin E), tocopherol sorbate, tocopherol acetate, other tocopherol esters, butylated hydroxybenzoic acid and its salts, gallic acid and its alkyl esters , Especially propyl gallate, uric acid and its salts and alkyl esters, sorbic acid and its salts, amines (eg N,
N-diethylhydroxylamine, amino-guanidine), sulfhydryl compounds (eg glutathione), dihydroxyfumaric acid and its salts, bioflavonoids, lysine, methionine, proline, superoxide dismutase, silymarin, tea extract, grape skin / seed Antioxidants / radical scavengers such as extracts, melanin, and rosemary extracts may be used. Preferred antioxidant /
The radical scavenger is selected from tocopherol acetate, tocopherol sorbate and other tocopherol esters, more preferably tocopherol acetate.

[0091] It chelating agent chelating agent is included, in order to protect from UV radiation, such as to contribute dander or tissue changes in the stratum corneum, and from other environmental chemicals like can cause damage to the skin Especially useful for. A suitable amount is from about 0.01% of the composition.
It is about 1%, more preferably about 0.05% to about 0.5%. Representative chelating agents used herein are disclosed in US Pat. No. 5,487,884. The preferred chelating agents used in the compositions of the subject invention are ethylenediaminetetraacetic acid (EDTA), furyldioximes and their derivatives.

Descaling Agent / Release Agent A safe and effective amount of the release agent is more preferably from about 0.1% to about 10% of the composition.
%, Even more preferably about 0.2% to about 5%, even more preferably about 0.5% to about 4%.
% May be added to the composition of the subject invention. Exfoliants enhance the effect on the appearance of the skin according to the invention. For example, exfoliants tend to improve skin texture (eg, smoothness). A wide variety of stripping agents are known in the art, and suitable for use herein include salicylic acid, glycolic acid, lactic acid, 5-octanoylsalicylic acid, hydroxyoctanoic acid, hydroxycaprylic acid, and lanolin fatty acid. Organic hydroxy acids such as One suitable release system for use herein comprises a sulfhydryl compound and a zwitterionic surfactant, and is disclosed in WO 9
6/01101. Other exfoliation systems suitable for use herein include salicylic acid and a zwitterionic surfactant, and WO95 / 13.
048. Salicylic acid is preferred.

Skin Lightning Agent The compositions of the present invention may also include a skin lightening agent. When used, the composition preferably comprises about 0.1% to about 10% skin lightening agent, more preferably about 0.2% to about 5%, even more preferably about 0.5% to about 2%. . Suitable skin lightening agents are known in the art and include kojic acid, arbutin, ascorbic acid and their derivatives such as magnesium ascorbyl phosphate. Suitable skin lightening agents for use herein include those described in WO95 / 34280 and WO95 / 23780.

Preparation of Compositions The compositions of the present invention are generally prepared by conventional methods such as are known in the art of making topical compositions. Such methods generally involve mixing the components in one or more steps, with or without heating, cooling, vacuum application, etc., to achieve a relatively uniform state.

Methods of Regulating Skin Condition The compositions of the present invention are suitable for controlling the condition of mammalian skin, particularly human skin, and more particularly the skin of body parts other than the hands or face. Useful for controlling visible and / or palpable discontinuities of the skin, such as visual and / or palpable discontinuities of the skin, and more particularly age-related discontinuities. . Controlling skin condition involves topically applying to the skin a safe and effective amount of a composition of the invention. The amount of composition applied, the number of applications and the period of use depend on the activity level of a given composition and the degree of modulation desired, for example the degree of skin aging present in a subject and the rate of further skin aging. Taking into account, it will vary widely.

The compositions of the present invention can be used in a wide range of amounts to provide skin appearance and / or feel benefits. Once per application, the amount of the present compositions which are commonly used in compositions mg / skin cm ^2, and from about 0.1 mg / cm ² to about 10 mg / cm ^2.
A particularly useful application amount is about 2 mg / cm ² . Generally, application will be on the order of about once per day, but application rates can range from about once per week to about three times per day or more.

The compositions of the present invention provide an improvement in the condition of the skin which is substantially visible immediately after application of the composition to the skin. Such abrupt improvement may include masking or masking skin imperfections such as discontinuities in the skin (including those associated with skin aging such as enlarged pores), and / or It also includes providing a more uniform skin tone or color.

The compositions according to the invention, which contain active substances for long-term conditioning of the skin, give a visible improvement in the skin by prolonged topical application of the composition. "Long-term topical application" and the like include continuous topical application of the composition for a longer period of time, generally at least about 1 week, more preferably at least about 1 month, within the shelf life of the object. . Generally, application will be on the order of about once per day for such extended periods, but application rates can range from about once per week to about three times per day or more.

[0099]

【Example】

The following examples further describe and explain embodiments within the scope of the present invention. The examples are given for the purpose of demonstration and are not to be construed as limiting the invention. When applicable, components are represented by CTFA names. All examples are oil-in-water emulsion compositions made using conventional compounding techniques. The surface-treated titanium dioxide is mixed via the oil phase component, while the nylon particles and the suppressor pigment are added via the aqueous phase. Examples 1-8 are representative hand and body lotions according to the present invention.

[0100]

[Table 1]

[0101]

[Table 2]

Upon application of the above example to the subject's hand, at a rate of 2 mg / cm ² skin, there is a substantially immediate visual improvement in the appearance of the skin, eg a reduction in the noticeability of pores and a more uniform. Provides skin tone. Apply once or twice a day at the same rate from 3 to
By continuing for 6 months, the fineness of the skin surface was improved, including the reduction of fine lines and wrinkles, and a substantially immediate improvement in appearance was observed. A facial skin cream is prepared from the following ingredients.

[0103]

[Table 3]

¹ Orgasol® 2002 EXD NATCOS. ² Green suppression content ³ BP Silkflo 364 NF ⁴ Arlatone from ICI Arlatone 2121 ⁵ GE Tospearl 145a from silicone

─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. ⁷ Identification code FI theme code (reference) A61K 47/14 A61K 47/14 47/32 47/32 47/44 47/44 A61P 17/00 A61P 17 / 00 43/00 107 43/00 107 (31) Priority claim number 0001234.4 (32) Priority date January 19, 2000 (January 19, 2000) (33) Priority claim United Kingdom (GB) ( 81) Designated countries EP (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE), OA (BF, BJ, CF, CG, CI, CM, GA, GN, GW, ML, MR, NE, SN, TD, TG), AP (GH, GM, KE, LS, MW, SD, SL, SZ, TZ, UG, ZW), EA (AM, Z, BY, KG, KZ, MD, RU, TJ, TM), AE, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CR, CU, CZ, DE, DK, DM, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC , LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, TZ, UA, UG, US, UZ, VN, YU, ZA, ZW (72) Inventor Crook, Teresa Barbara United Kingdom, Surrey, GU 17, 9 Elwai, Camberley, Holly, Hill, Bloomsbury, Way 65 (72) Ming Man, Paul Elliott England, Hearts, Ahl 5, 5 T, Harpenden, Top Street, Way 13 (72) Inventor Opry, Conner James England, Sally, Tidwell 9, 1 Younu, Richmond, Sheen, Park 21, Top, Floor, Flat F Term (Reference) 4C076 AA16 BB31 CC18 CC29 DD34A EE03A EE51A EE55A FF16 FF17 4C083 AA112 AB242 AC011 AC012 AC072 AC121 AC122 AC182 AC242 AC341 AC351 AD1522 AD2021 AD021 AD2021 AD2021 AD2021 AD021 AD2021 AD021 AD2021 AD021 AD2021 AD021 AD2021 AD2021 AD2021 AD2021 AD2021 AD2021 AD021 AD2021 AD631 AD662 CC02 CC04 CC05 DD23 DD31 EE12 4C086 AA01 AA02 BC19 MA03 MA05 MA07 MA09 MA21 MA28 MA63 NA14 ZA89 ZB22

Claims (15)

[Claims] 1. A topical leave-on skin care composition: a) from about 1 to about 10% of the vitamin B _3; b) high malleability oil is selected from the following: i) from about 100 to about a weight average molecular weight A branched chain hydrocarbon having 1000; ii) a liquid ester emollient of formula I Where R ¹ is selected from H or CH ₃ , R ² , R ³ and R ⁴ are each independently selected from C _{1 to} C ₂₀ straight or branched chain alkyl and x is 1 An integer of ˜20); and iii) mixtures thereof; c) an occlusive drug containing a dermatologically acceptable carrier and selected from petrolatum, cetyl ricinoleate and lanolin. Poly (with a molecular weight (MW) of 260 to 1000
A leave-on skin care composition comprising 0.3% to 4% of an anti-adhesive agent selected from alpha olefins). 2. The composition according to claim 1, wherein the vitamin B ₃ compound is nicotinic acid amide. 3. A composition according to claim 1, wherein the vitamin B ₃ compound is present in a concentration of 3-8%. 4. The composition of claim 1, wherein the highly malleable oil is a branched chain hydrocarbon. 5. A composition according to claim 4, wherein the branched chain hydrocarbon is isohexadecane. 6. The composition of claim 1, wherein the branched chain hydrocarbon is present in a concentration of 3% to 7%. 7. The composition according to claim 1, wherein the anti-adhesive agent is a poly (alpha olefin) having a molecular weight of 260 to 1000. 8. The composition according to claim 6, wherein the anti-adhesive agent is polydecene. 9. The composition according to claim 1, wherein the anti-adhesive agent is petrolatum. 10. Composition according to any one of the preceding claims, wherein the anti-adhesive agent is present in a concentration of 0.5-2.5%, preferably 1-2%. 11. A composition according to any one of the preceding claims further comprising 4-14% glycerin. 12. The composition of claim 1, further comprising 0.1 to 10% of an organic particulate material dispersed in the composition and having a volume average particle size in the range of 5 to 30 μm and a refractive index of 1.3 to 1.7. Composition. 13. Particles of an organic fine particle substance are porous and have a volume average particle size of 15 to 2.
The composition according to claim 12, which is nylon particles in the range of 5 μm. 14. Use of polydecene for reducing the stickiness of a leave-on skin care composition comprising 1 to 10% of a vitamin B ₃ compound. 15. Use of petrolatum for reducing the sticky feel of a leave-on skin care composition comprising 1 to 10% of a vitamin B ₃ compound.