JP2021104934A - Anhydrous composition for locally delivering active ingredient - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide an anhydrous composition for a keratin substance such as skin, which can provide improved permeability of a cosmetic active ingredient.
The present invention is an anhydrous composition for keratin substances such as skin, wherein (a) at least one oil, (b) at least one organic lipophilic gelling agent, and (c). ) With respect to an anhydrous composition comprising at least one water-soluble particle. The present invention is also a beauty method for keratin substances such as skin, in which the step of applying the anhydrous composition according to the present invention to the keratin substance and the aqueous composition containing water are brought into contact with the applied anhydrous composition. It also relates to methods, including processes. The compositions and cosmetological methods according to the invention are very useful for the topical delivery of active ingredients for keratinous substances such as skin.
[Selection diagram] Fig. 1

Description

The present invention relates to cosmetic compositions for topical delivery of active ingredients, especially cosmetic anhydrous compositions.

Delivery of active ingredients through the skin is one of the important and unmet needs in the cosmetic field. To meet this need, the use of composition containing particles has been proposed. So far, some prior art documents on compositions containing water-soluble particles have been published.

For example, US Pat. No. 6,531,433 (B1) states that (a) at least one water-soluble carbohydrate having an average particle size of about 100 to about 2000 microns, in an amount of about 10 to about 90 percent of the total composition. A non-aqueous personal scrubbing composition comprising at least one water-soluble carbohydrate, which is a monosaccharide or a disaccharide, and (b) a non-aqueous medium in an amount of about 10 to about 90 percent by weight of the total composition. The thing is disclosed.

JP-T-2018-530621 also discloses a non-aqueous cosmetic composition containing 0.01 wt% to 15 wt% polypeptides and angled water-soluble scrub particles with a particle size of 0.01 mm to 2 mm. ing.

In addition, WO2018 / 104428 (A1) added at least a) C _{3 to} C ₁₀ diols, b) hydrophobic silica airgel particles, and c) exfoliative particles in the oily fatty phase to 10 based on the total mass of the composition. Disclosed are anhydrous, especially cosmetic compositions containing in an amount in the range of% to 50% by weight, which exhibit a viscosity of 10 to 20 Pa.s. at a temperature of 25 ° C.

However, there is still a need to improve the local delivery of the active ingredient in cosmetic compositions.

U.S. Pat. No. 6,531,433 (B1) JP-T-2018-530621 WO 2018/104428 (A1) US-A-5783657 US6503522 US6552160 US6399713 US3645705 US3148125 US5500209 US5998570

Charles M. Hansen, Charles Hansen in "Hansen Solubility Parameters: A User's Handbook", CRC Press (2007)

An object of the present invention is to provide an anhydrous composition for a keratin substance such as skin, which can provide improved permeability of a cosmetic active ingredient.

The above object of the present invention is
(a) At least one oil and
(b) With at least one organic lipophilic gelling agent,
(c) This can be achieved with an anhydrous composition containing at least one water-soluble particle.

(b) The organic lipophilic gelling agent may be selected from styrene block copolymers, semi-crystalline polymers, glutamid compounds, polyamides, and mixtures thereof, and is preferably polyamide.

(c) The average primary particle size of the water-soluble particles is 10 μm or more, preferably 30 μm or more, more preferably 50 μm or more, still more preferably 100 μm or more, particularly 200 μm or more, and 1 mm or less, preferably 800 μm or less, more preferably. It may be 600 μm or less, and even more preferably 500 μm or less.

(c) The water-soluble particles may include polysaccharide particles, monosaccharide particles, amino acid particles, sugar alcohol particles, or ascorbic acid particles, and mixtures thereof.

(a) The amount of oil may be 50% by mass or more, preferably 60% by mass or more, more preferably 70% by mass or more, and even more preferably 80% by mass or more, based on the total mass of the anhydrous composition. It is good and 99% by mass or less, preferably 95% by mass or less, more preferably 90% by mass or less, and even more preferably 85% by mass or less.

(b) The amount of the organic lipophilic gelling agent is 1% by mass or more, preferably 2% by mass or more, more preferably 3% by mass or more, still more preferably 4% by mass, based on the total mass of the anhydrous composition. It is 20% by mass or less, preferably 15% by mass or less, more preferably 10% by mass or less, and even more preferably 7% by mass or less.

(c) The amount of the water-soluble particles is 0.01% by mass or more, preferably 0.1% by mass or more, more preferably 0.2% by mass or more, still more preferably 0.5% by mass or more, based on the total mass of the anhydrous composition. It may be 15% by mass or less, preferably 10% by mass or less, more preferably 5% by mass or less, and even more preferably 3% by mass or less.

Linear viscoelasticity (G') profile and loss modulus (G'') of the anhydrous composition on a log scale when measured using a rheometer at 25 ° C. and a frequency of 1 Hz using a 40 mm cone plate. The elastic region may be 10 ^-1 Pa or more, and the strain at the intersection of G'and G'may be more than 4%.

The anhydrous composition preferably has a Hansen solubility parameter δH (hydrogen bond component) of less than 30 at 25 ° C. and a δX (volume-dependent bond parameter: δX = (δD ² + δP ² ) ^1/2 ) of less than 25. It may further contain at least one alcohol.

The amount of alcohol may be 0.5% by mass or more, preferably 1% by mass or more, more preferably 3% by mass or more, still more preferably 5% by mass or more, based on the total mass of the anhydrous composition, and It may be 25% by mass or less, preferably 20% by mass or less, more preferably 15% by mass or less, and even more preferably 10% by mass or less.

The present invention is also a cosmetological method for keratin substances such as skin.
The step of applying the anhydrous composition according to the present invention to the keratin substance, and
It also relates to a method comprising contacting the aqueous composition containing water with the coated anhydrous composition.

The aqueous composition may contain at least one active ingredient for keratinous substances such as skin, preferably selected from a whitening active ingredient, an anti-aging active ingredient, an anti-wrinkle active ingredient, or an antioxidant active ingredient.

The amount of the active ingredient may be 0.1% by mass or more, preferably 0.5% by mass or more, more preferably 1% by mass or more, still more preferably 2% by mass or more, based on the total mass of the aqueous composition. Moreover, it may be 15% by mass or less, preferably 10% by mass or less, more preferably 7% by mass or less, and even more preferably 5% by mass or less.

The amount of water may be 20% by mass or more, preferably 30% by mass or more, more preferably 40% by mass or more, still more preferably 50% by mass or more, and more preferably 50% by mass or more, based on the total mass of the aqueous composition. It may be 90% by mass or less, preferably 80% by mass or less, more preferably 75% by mass or less, and even more preferably 60% by mass or less.

The aqueous composition may be applied to the applied anhydrous composition in the form of a wet sheet mask, mist, spray or topical application.

It is a graph which shows the result of the viscoelasticity measurement about the composition by Example 1.

As a result of diligent studies, the present inventors have surprisingly found that an anhydrous composition containing at least one water-soluble particle and at least one lipophilic gelling agent can improve the permeability of the active ingredient. .. In addition, we have surprisingly found a novel cosmetological method for topical delivery of the active ingredient using the anhydrous composition described above, thereby completing the invention.

Therefore, the anhydrous composition for keratinous substances such as skin according to the present invention is:
(a) At least one oil and
(b) With at least one organic lipophilic gelling agent,
(c) Includes at least one water-soluble particle.

Hereinafter, the composition according to the present invention will be described in detail.

[Composition]

The composition according to the present invention may be a cosmetic composition for a keratin substance, particularly a cosmetic anhydrous composition. The keratin substance may include, for example, the skin of the face, neck and body. Preferably, the composition according to the invention is a skin care composition.

The compositions according to the invention can take various forms such as solutions, gels, lotions, serums, suspensions, dispersions, fluids, emulsions, pastes, creams and the like. The composition is preferably in the form of a gel, i.e. an oil gel, as the composition also comprises an oil and an organic lipophilic gelling agent.

The term "gel" as used herein includes a high concentration liquid which may be a Newtonian fluid or a non-Newtonian fluid. Newtonian fluid means a fluid whose viscosity does not change due to changes in the flow state. Gels also include shear thinned gels.

In a preferred embodiment of the invention, the composition is a gel with non-Newtonian viscosity. In another preferred embodiment of the invention, the composition is shear thinned. Non-Newtonian shear thinned materials change state from gel to liquid in the presence of load shear stress and return to gel in the absence of load shear stress. Shear-thinned materials, by definition, are those in which the viscosity of the material decreases non-linearly as the load shear stress increases.

The gel composition according to the present invention can be defined by its rheological properties. The inventors of the present invention surprisingly have a linear viscoelastic region of storage modulus (G') profile and loss modulus (G'') of 10 ^-1 Pa or more, G'and G''. We have found that a gel composition with a strain of more than 4% at the intersection of the profiles is ideal for the purposes of the present invention. This allows the gel composition to exhibit a favorable shear thinning, thus changing the gel to a nearly water-like thin viscous state under mild shearing conditions, which causes the water-soluble particles to become uniform in the composition. This is to allow dispersion and as soon as the displacement is removed, the gel retains its original high viscosity without a significant increase in viscosity, i.e. without much hysteresis. The gel composition can also provide a bulging texture that the consumer prefers. Moreover, this property can provide the composition with stability and long life, so that the water-soluble particles in the composition do not precipitate for long periods of time.

With respect to hysteresis, in the gel composition according to the invention, the change in final viscosity value under all shear conditions can be less than 10% compared to the initial viscosity value.

The "intersection" of the amplitude sweep, which can also be referred to as the "damping point", is the point where the storage modulus (G') and loss modulus (G'') have the same value. This point is also known as the transition point of the sol-gel state.

Preferably, the gel composition according to the invention has an intersection strain of 8% or more, more preferably 12% or more. In an embodiment of the invention, the intersection of the present invention has a strain of 100% or less, preferably 50% or less, and even more preferably 30% or less.

The linear viscoelastic region is a region in which the value of G'or G'' is constant at a low strain (%). The gel composition has a linear viscoelastic region of G'and G'' on a log scale, preferably above 0 Pa. In an embodiment of the present invention, the gel composition, 10 ⁴ Pa or less, preferably it may have a visco-elastic region of the above logarithmic scale 10 ³ Pa. The linear viscoelastic region can be measured in the same way as at an intersection.

The modulus of elasticity of the linear viscoelastic region and intersection is measured, for example, by graphing the G'and G'' values of the gel composition as a function of strain (%) in the amplitude sweep of shear stress at a constant frequency. be able to. In the present invention, intersections can be measured using a rheometer using a 40 mm cone plate and the following conditions.
Setting interval: 30 μm
Temperature: 25 ° C
Distortion (%): 0.01-1000%
Frequency: 1Hz

In addition, the gel composition according to the invention can exhibit very low hysteresis. Here, hysteresis means the difference between the initial viscosity and the final viscosity after applying a shearing force. For example, hysteresis can be measured by applying a cycle shear force while measuring the viscosity. Since the gel composition according to the present invention can exhibit very low hysteresis, the gel composition can have shape memory gel-like properties.

The compositions according to the invention can be transparent or translucent, which is a consumer preference. This is because the particles cannot be precipitated or suspended in the composition due to the gel properties of the composition. This means that the anhydrous composition according to the present invention can exhibit improved stability because the particles in the composition do not precipitate and the morphology is maintained for a long time. The transparency of the composition can be determined, for example, by measuring the turbidity with a turbidity meter (2100Q portable, Hach). Preferably, the composition has a turbidity of greater than 0, preferably greater than 10 and less than 200, preferably less than 150.

The term "anhydrous composition" as used herein means a composition that is anhydrous and contains less than 3% by weight, less than 1% by weight, or less than 0.1% by weight of water with respect to the total mass of the composition. do.

The anhydrous composition according to the present invention comprises (a) at least one oil, (b) at least one organic lipophilic gelling agent, and (c) at least one water-soluble particle.

The components in the composition will be described in more detail below.

(oil)
The anhydrous composition according to the present invention (a) contains at least one oil. Two or more kinds of (a) oils may be used in combination. Therefore, a single type of oil or a combination of different types of oil can be used.

As used herein, the expression "oil" means an aliphatic compound or substance in the form of a liquid or paste (non-solid) at room temperature (25 ° C.) under atmospheric pressure (760 mmHg). These oils may be volatile or non-volatile, preferably non-volatile.

(a) The oil may be a non-polar oil such as a hydrocarbon oil, a silicone oil; a polar oil such as a vegetable oil or an animal oil and an ester oil or an ether oil; or a mixture thereof.

(a) The oil is preferably selected from the group consisting of plant or animal derived oils, synthetic oils, silicone oils and hydrocarbon oils, and mixtures thereof.

Examples of vegetable oils are, for example, flaxseed oil, camellia oil, macadamia nut oil, corn oil, mink oil, olive oil, avocado oil, southern ka oil, sunflower oil, saflower oil, jojoba oil, sunflower oil, almond oil, abrana seed oil, Sesame oil, soybean oil, peanut oil, and mixtures thereof can be mentioned.

Examples of animal oils include, for example, squalene and squalene.

Examples of synthetic oils include alkane oils such as isododecane and isohexadecane, ester oils, ether oils, and artificial triglycerides.

Ester oils are preferably saturated or unsaturated, and linear or branched C ₁ -C ₂₆ aliphatic monoacid or polyacid, saturated or unsaturated, linear or branched C _{1 to} C ₂₆ Liquid esters with aliphatic monovalent alcohols or polyhydric alcohols, and the total number of carbon atoms of these esters is 10 or more.

Preferably, in the ester of monohydric alcohol, at least one of the alcohol and acid from which the ester of the invention is derived is branched.

Among monoesters of monoacids and monohydric alcohols, ethyl palmitate, ethylhexyl palmitate, isopropyl palmitate, dicaprylyl carbonate, alkyl myristate, such as isopropyl myristate or ethyl myristate, isosetyl stearate, 2-ethylhexyl isononanoate, Examples thereof include isononyl isononanoate, isodecyl neopentate and isostearyl neopentate.

C _{4 to} C ₂₂ dicarboxylic acid or tricarboxylic acid, and _{esters of C 1 to} C ₂₂ alcohols, as well as monocarboxylic acids, dicarboxylic acids or tricarboxylic acids, and non-sugars C _{4 to} C ₂₆ dihydroxy, trihydroxy, tetrahydroxy or penta. Esters of hydroxyalcohol can also be used.

Specific examples include: diethyl sebacate, isopropyl lauroyl sarcosate, diisopropyl sebacate, bis sebacate (2-ethylhexyl), diisopropyl adipate, di-n-propyl adipate, dioctyl adipate, bis adipate. (2-Ethylhexyl), diisostearyl adipate, bis maleate (2-ethylhexyl), triisopropyl citrate, triisocetyl citrate, triisostearyl citrate, glyceryl trilactic acid, glyceryl trioctanoate, trioctyldodecyl citrate, Trioleyl citrate, neopentyl glycol diheptate, and diethylene glycol diisononanoate.

As the ester oil, _{sugar esters and diesters of C 6 to} C ₃₀ , preferably C _{12 to} C ₂₂ fatty acids can be used. The term "sugar" can mean an oxygen-retaining hydrocarbon compound containing or without an aldehyde or ketone functional group and containing several alcohol functional groups containing at least 4 carbon atoms. Recall. These sugars can be monosaccharides, oligosaccharides or polysaccharides.

Examples of suitable sugars that can be mentioned include sucrose (or sucrose), glucose, galactose, ribose, fucose, maltose, fructose, mannose, arabinose, xylose and lactose, and derivatives thereof, especially alkyl derivatives such as methyl. There are derivatives such as methyl glucose.

Fatty acid sugar esters are from the group containing esters or ester mixtures of the aforementioned sugars with linear or branched, saturated or unsaturated _{fatty acids C 6 to} C ₃₀ , preferably C _{12 to} C _22. You can choose in particular. These compounds, when unsaturated, can have 1 to 3 conjugate or unconjugated carbon-carbon double bonds.

Esters due to this modification can also be selected from monoesters, diesters, triesters, tetraesters and polyesters, and mixtures thereof.

These esters include, for example, oleic acid ester, lauric acid ester, palmitic acid ester, myristic acid ester, behenic acid ester, coconut fatty acid ester, stearic acid ester, linoleic acid ester, linolenic acid ester, capric acid ester and arachidonic acid ester. , Or a mixture thereof, for example a mixed ester of oleopalmitic acid, oleostearic acid, and palmitostearic acid, and pentaerythrityl tetraethylhexanoate.

More specifically, monoesters and diesters, especially monooleic or dioleic acids of sucrose, glucose, or methylglucos, stearic acid esters, bechenic acid esters, oleopalmitic acid esters, linoleic acid esters, linolenic acid esters and oleo. Stearic acid ester is used.

An example that can be mentioned is methyl glucose dioleate, a product sold by Amerchol under the name Glucate® DO.

Examples of preferred ester oils include, for example, diisopropyl adipate, dioctyl adipate, 2-ethylhexyl hexanate, ethyl laurate, cetyl octanate, octyldodecyl octanate, isodecyl neopentate, myristyl propionate, 2-ethylhexanoic acid 2. -Ethylhexyl, 2-ethylhexyl octanoate, (caprylic acid / capric acid) 2-ethylhexyl, methyl palmitate, ethyl palmitate, isopropyl palmitate, dicaprilyl carbonate, isopropyl lauroyl sarcosinate, isononyl isononanoate, ethylhexyl palmitate, lauric acid Isohexyl, hexyl laurate, isosetyl stearate, isopropyl isostearate, isopropyl myristate, isodecyl oleate, tri (2-ethylhexanoic acid) glyceryl, tetra (2-ethylhexanoic acid) pentaerythrityl, 2-ethylhexyl succinate, Diethyl sebacate, and mixtures thereof, can be mentioned.

Examples of artificial triglycerides include, for example, caprylic caprylic acid triglyceride, glyceryl trimyristate, glyceryl tripalmitate, glyceryl trilinolenate, glyceryl trilaurate, glyceryl tricaprate, glyceryl tricaprylate, tri (capric acid). / Caprylic acid) glyceryl, and tri (caprylic acid / caprylic acid / linolenic acid) glyceryl.

Examples of silicone oils include linear organopolysiloxanes such as dimethylpolysiloxane, methylphenylpolysiloxane, methylhydrogenpolysiloxane, cyclic organopolysiloxanes such as octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane, etc. Dodecamethylcyclohexasiloxane and the like, as well as mixtures thereof, can be mentioned.

Preferably, the oil phase of the present invention does not contain any silicone oil. In other words, the oil (a) of the present invention can be selected from non-silicone oils.

Hydrocarbon oils can be selected from:
--Linear or branched, optionally cyclic, C _6- C ₁₆ lower alkanes (examples can be hexane, undecane, dodecane, tridecane and isoparaffin, such as isohexadecane, isododecane and isodecan. Included), and
—— Linear or branched hydrocarbons containing more than 16 carbon atoms, such as liquid paraffin, petroleum jelly, polydecene and hydrogenated polyisobutene, such as Parleam®, and squalane.

Preferred examples of hydrocarbon oils include, for example, linear or branched hydrocarbons such as isohexadecane, isododecane, squalane, mineral oil (eg liquid paraffin), paraffin, petrolatum or petrolatum, naphthalene and the like; hydrogenated polyisobutene. , Isoeicosan, and decene / butene copolymers; and mixtures thereof.

(a) The oil may preferably be selected from non-polar hydrocarbon oils in liquid form at room temperature.

(a) The amount of oil may be 50% by mass or more, preferably 60% by mass or more, more preferably 70% by mass or more, and even more preferably 80% by mass or more, based on the total mass of the anhydrous composition. It may be 99% by mass or less, preferably 95% by mass or less, more preferably 90% by mass or less, and even more preferably 85% by mass or less.

(Organic lipophilic gelling agent)
The anhydrous composition according to the present invention contains (b) at least one organic lipophilic gelling agent. Two or more kinds of (b) organic lipophilic gelling agents may be used in combination. Therefore, a single type of organic lipophilic gelling agent may be used, or a combination of different types of organic lipophilic gelling agents may be used.

The term "lipophilic" as used herein, at room temperature (25 ° C.) and atmospheric pressure (10 ⁵ Pa), the substance is soluble in the oil in a concentration of at least 1% by weight relative to the total weight of the oil means.

The term "gelling agent" as used herein means a substance capable of concentrating or gelling an oil.

The (b) organic lipophilic gelling agent used in the present invention can be selected from styrene block copolymers, semi-crystalline polymers, glutamid compounds, polyamides, and mixtures thereof.

Styrene block copolymers are hydrocarbon block copolymers. Styrene block copolymers are obtained from at least one styrene monomer and at least one olefin. The olefin may be, among other things, an elastomeric ethylenically unsaturated monomer. Examples of olefins that can be mentioned are ethylenic carbide monomers containing, among other things, one or two ethylenically unsaturated and containing 2 to 5 carbon atoms, such as ethylene, propylene, butadiene, isoprene or pentadiene. Is included. Advantageously, the styrene block copolymer is an amorphous block copolymer of styrene and olefin.

Block copolymers containing at least one styrene block and at least one block containing units selected from butadiene, ethylene, propylene, butylene and isoprene or mixtures thereof are particularly preferred. According to one preferred embodiment, the styrene block copolymer is hydrogenated after polymerization of the monomers to reduce residual ethylenically unsaturated.

According to one preferred embodiment, the styrene block copolymer is preferably hydrogenated and at least one diblock selected from preferably styrene-ethylene / propylene copolymer, styrene-ethylene butadiene copolymer and styrene-ethylene / butylene copolymer. Contains copolymers. Diblock Polymers are specifically marketed by Kraton Polymers under the name Kraton® G1701E.

According to another preferred embodiment, the styrene block copolymer is preferably hydrogenated, preferably styrene-ethylene / propylene-styrene copolymer, styrene-ethylene / butadiene-styrene copolymer, styrene-isoprene-styrene copolymer and styrene-butadiene. -Contains at least one triblock copolymer selected from styrene copolymers. Triblock Polymers, in particular by Kraton Polymers, are Kraton® G1650, Kraton® G1652, Kraton® G1657, Kraton® DI101, Kraton® DI102 and Kraton®. It is sold under the name DI160.

The term "semi-crystalline polymer" is used herein to include a crystalline moiety, a pendant chain or a block in the main chain and an amorphous moiety in the main chain, and a first-order reversible phase change temperature. In particular, it means a polymer showing a melting point (solid-liquid transition). When the crystalline moiety is a block of polymer backbone, the crystalline block has different chemical properties than that of an amorphous block, in which case the semi-crystalline polymer is, for example, diblock. , Triblock or multi-block type block polymer.

Polymer blocks, as well as crystalline chains or blocks, are amorphous. The term "crystalline chain or block" is considered herein to reversibly change from an amorphous state to a crystalline state, depending on whether the temperature is above or below the melting point, when used alone. Means a chain or block to be

According to a particular embodiment of the invention, the semi-crystalline polymer has C _{14 to} C ₂₄ alkyl (meth) acrylate, C _{11 to} C ₁₅ perfluoroalkyl (meth) acrylate, N-with or without a fluorine atom. (C ₁₄ -C ₂₄ 4 alkyl) (meth) acrylamides, C ₁₄ -C ₂₄ alkyl or vinyl ester having a perfluoroalkyl chain, vinyl ethers having C ₁₄ -C ₂₄ alkyl or perfluoroalkyl chains, C ₁₄ -C ₂₄ alkyl group Selected from C _{14 to} C ₂₄ α-olefins or paraalkyl styrenes having a homopolymer obtained by polymerization of at least one monomer having a crystalline chain, and these monomers and, for example, N. -Selected from copolymers of these monomers obtained by copolymerization with hydrophilic monomers other than methacrylic acid, such as vinylpyrrolidone, hydroxyethyl acrylate, hydroxyethyl methacrylate or acrylic acid. Such copolymers include, for example, C _14- C ₂₄ alkyl acrylates, C _14- C ₂₄ alkyl methacrylates, C _14- C ₂₄ alkyl acrylamides or C _14- C ₂₄ alkyl methacrylamides and N-vinylpyrrolidone, hydroxyethyl acrylates. It may be a copolymer of hydroxyethyl methacrylate or acrylic acid, or a mixture thereof.

The semi-crystalline polymer of the composition of the present invention may be non-crosslinked or partially crosslinked. Preferably, the semi-crystalline polymer of the composition according to the invention is not crosslinked.

According to a particular embodiment of the invention, the semi-crystalline polymer is a homopolymer obtained from the polymerization of a monomer having a crystalline chain selected from _{C 14-} C ₂₄ alkyl acrylates and C _14- C _{24 alkyl methacrylates.} be. In particular, those sold under the name Intelimer (registered trademark) by Landec, which are described in the pamphlet Intelimer (registered trademark) Polymers and Landec IP22, can be mentioned. These polymers are in solid form at room temperature. They carry crystalline side chains and _{correspond to saturated C 14-} C ₂₄ alkyl acrylates or methacrylate homopolymers. More specifically, stearyl acrylate homopolymers (Intelimer IPA-13.1) (INCI name: poly C10-30 alkyl acrylates) or behenyl acrylate homopolymers (Intelimer IPA-13.6) (INCI name: poly C10-30 alkyl acrylates) can be mentioned. Can be done.

The glutamide compound of the present invention is known to contain one of the organic gelling agents. Preferably, the glutamide compounds of the present invention are non-polymers.

Preferably, the glutamid compound is a non-polymer and has a low molecular weight dialkyl N-acylglutamide having a linear alkyl chain, particularly preferably an acyl group such as lauroyl glutamate dibutylamide (or dibutyllauroylglutamide). Di (C2-C6) alkyl N-acylglutamides containing linear C8-C22 alkyl chains and / or low molecular weight dialkyl N-acylglutamides with branched alkyl chains, particularly preferably N-2-. Acyl groups such as ethylhexanoyl glutamate dibutylamide (or dibutylethylhexanoylglutamide) are selected from di (C2-C6) alkyl N-acylglutamides containing branched C8-C22 alkyl chains, as well as mixtures thereof. ..

Preferably, among the non-polymeric glutamid compounds that can be used, at least one selected from (C2-C6) dialkyl N-acylglutamide in which the acyl group contains a linear C8 to C22 alkyl chain, among others. It contains low molecular weight dialkyl N-acylglutamide having a linear alkyl chain (such as lauroyl glutamate dibutylamide (dibutyllauroyl glumid)) and particularly branched C8 to C22 alkyl chains having an acyl group (C2 to C6). ) Dialkyl N-acylglutamide, at least one low molecular weight dialkyl N acylglutamide having a branched alkyl chain (N-2-ethylhexanoyl glutamate dibutylamide (dibutylethylhexanoylglutamide)) ) Etc.), preferably a combination of these two glutamid compounds and a solvent capable of forming a hydrogen bond can be mentioned.

In a preferred embodiment, a glutamide-based compound suitable for use in the present invention is dibutyl lauroyl glutamide known under the trade name GP-1 and sold by Ajinomoto.

For the purposes of the present invention, the term "polyamide" means a compound containing at least 2 repeating amide units, preferably at least 3 repeating amide units, and even better 10 repeating amide units.

In particular, the (b) organic lipophilic gelling agent of the present invention contains at least one polyamide. The inventors of the present invention have surprisingly found that the use of polyamide as an organic lipophilic gelling agent can impart highly favorable viscoelasticity to the composition according to the present invention.

The polyamide of the present invention may be a polyamide polycondensate. The term "polycondensate" is used in the present invention through polycondensation, that is, by chemical reaction between monomers having different functional groups, particularly selected from acid, alcohol, and amine functional groups. Refers to the obtained polymer.

The oleophilic polyamide polycondensate is, in particular, a) a polymer backbone with a repeating pattern of hydrocarbons, with at least one non-pendant amide pattern, and optionally b) 6-120 carbon atoms. It contains at least one pendant fatty chain, preferably containing 8 to 120 carbon atoms, more preferably 12 to 70 carbon atoms, and / or at least 4 carbon atoms, and in these hydrocarbon patterns. You can choose from a polyamide polymer that contains at least one linked, optionally functionalized terminal fat chain.

The term "functionalized chain" refers specifically to the present invention to amides, hydroxyls, ethers, oxyalkylenes, or polyoxyalkylene groups, halogens, groups of which are fluorinated or totally fluorinated, esters. Refers to an alkyl chain containing one or several functional groups or reagents selected from siloxane and polysiloxane. Further, the hydrogen atom of one or several fat chains may be at least partially substituted with a fluorine atom.

The term "repetitive pattern of hydrocarbons" as used in the present invention refers to a pattern containing 2 to 80 carbon atoms, preferably 2 to 60 carbon atoms, having hydrogen atoms and optionally oxygen atoms. The pattern may be linear, branched, or cyclic, and may be saturated or unsaturated. These patterns are also advantageously non-pendant and contain at least one amide group found in the polymer backbone.

Advantageously, the pendant chain is directly linked to at least one of the nitrogen atoms in the polymer backbone.

The lipophilic polyamide polycondensate may contain a silicone pattern or a C _{2 to} C _{3 oxyalkylene pattern between the hydrocarbon patterns.}

Furthermore, the lipophilic polyamide polycondensate of the composition of the present invention advantageously contains 40-98%, more preferably 50-95% fat chains relative to the total number of amide patterns and fat chains.

Preferably, the pendant fat chain is linked to at least one of the nitrogen atoms in the polymer's amide pattern. In particular, the fat chains of this polyamide correspond to 40-98%, more preferably 50-95% of the total number of amide patterns and fat chains.

Advantageously, the lipophilic polyamide polycondensate is less than 100,000 (especially 1000-100,000), especially less than 50,000 (especially 1000-50,000), more specifically 1000-30,000, preferably 2000-20,000, more preferably 2000-10,000. It has a mass average molecular weight in the range of.

The lipophilic polyamide polycondensate is insoluble in water or has a solubility in water of less than 1 g / L or 0.1 g / L, especially at 25 ° C. and atmospheric pressure. In particular, the lipophilic polyamide polycondensate does not contain ionic groups.

Preferred lipophilic polyamide polycondensates that can be used in the present invention include pendant fatty chains having 6 to 120 carbon atoms, more specifically 8 to 120 carbon atoms, particularly 12 to 68 carbon atoms. Alternatively, a polyamide branched by a terminal fat chain can be mentioned, where each terminal fat chain is linked to the polyamide backbone by at least one binding group L. The binding group L can be selected from ester, ether, amine, urea, urethane, thioester, thioether, thiourea, and thiourethane group. Preferably, these polymers contain a fatty chain at each end of the polyamide backbone.

These polymers preferably have a dicarboxylic acid having at least 32 carbon atoms (particularly having 32-44 carbon atoms) and at least 2 carbon atoms (particularly 2-36 carbon atoms). A polymer resulting from polycondensation between a diamine and an amine selected from among triamines having at least 2 carbon atoms (particularly 2-36 carbon atoms). The diacid is preferably a dimer derived from an ethylene unsaturated fatty acid such as oleic acid, linoleic acid, or linolenic acid, which has at least 16 carbon atoms, preferably 16 to 24 carbon atoms. The diamine is preferably diamineethylene, diaminehexylene or diaminehexamethylene. The triamine is, for example, triamineethylene. For polymers containing one or two terminal carboxylic acid groups, these polymers are referred to as at least 4 carbon atoms, preferably 10 to 36 carbon atoms, more preferably 12 to 24, even more preferably 16. It is advantageous to esterify with a monohydric alcohol having ~ 24, for example 18 carbon atoms.

The lipophilic polyamide polycondensate of the composition according to the present invention is particularly prepared by the following formula (A).

[During the ceremony,
n is an integer that varies from 1 to 30
R _'1 represents a fatty chain independently at each occurrence, is selected from alkyl or alkenyl (alcenyl) group having at least 4 carbon atoms, especially 4 to 24 carbon atoms,
R _'2 is independently at each occurrence, a divalent hydrocarbon chain comprising 1 to 52 carbon atoms,
R _'3 is independently in each occurrence a saturated or unsaturated, cyclic or acyclic, if is substituted by and / or optionally is preferably selected from among oxygen and nitrogen one or is interrupted by several heteroatoms that represents a divalent hydrocarbon group containing at least one carbon atom, particularly R _'3, alkylene chain linear or branched (C ₁ Represents ~ C ₈ ), preferably linear alkylene (C ₁ ~ C ₆ ) such as ethylene.
R _'4 is, independently at each occurrence a hydrogen atom, one alkyl group, or R containing from 1 to 10 carbon atoms' ₃ and at least one group selected from a different R' ₄ a direct bond to represent, 'if it is _4, R' base is different R ₃ and R 'nitrogen atom connected to both _4, R' heterocyclic ring defined by ₄ -N-R _'3 with it is part of a formula structure, provided that at least 50% of the R _'4 represents a hydrogen atom,
L, from among the at least one R 'are optionally substituted by ₁ group, an ester or an ether or an amine or urea or urethane or thioester or thioether or thiourea or thiourethane groups such as those defined above Represents a binding group, preferably selected]
Can be selected from the polymers having.

According to certain embodiments, these polymers are selected from polymers in which the linking group L has an ester group, an ester-C (O) -O- or an-OC (O)-representing formula (A). ..

These polymers are more specifically described in Union Camp, US-A-5783657.

Each of these polymers specifically has the following formula (B):

[During the ceremony,
--m indicates an integer number of amide groups such that the number of ester groups corresponds to 10% to 50% of the total number of ester groups and amide groups.
- R ₁ is independently at each occurrence, represents an alkyl group or alkenyl group having at least 4 carbon atoms, especially 4 to 24 carbon atoms,
--R _{2 independently represents C 4 to} C ₄₂ hydrocarbon groups at the time of each appearance, except that 50% of _{R 2 groups represent C 30 to} C ₄₂ hydrocarbon groups.
—— R ₃ is independently saturated or unsaturated at each appearance, cyclic or acyclic, optionally substituted, and / or optionally selected from oxygen and nitrogen. Represents a divalent hydrocarbon group containing at least one carbon atom interrupted by one or several heteroatoms, in particular R ₃ is a linear or branched alkylene chain (C ₁ to Represents C ₈ ), preferably a linear alkylene such as ethylene (C _{1 to} C ₆ ).
--R ₄ is a hydrogen atom, a C _{1 to} C ₁₀ alkyl group, or a direct bond with _{R 3} or another R ₄ (nitrogen linked to both _{R 3} and R _{4) independently at each appearance.} Atoms are part of the heterocyclic structure defined by _{R 4-} NR ₃ ), and at least 50% of _{R 4 represents hydrogen atoms]}
Meet.

In certain cases of formula (B), the terminal fat chain that is optionally functionalized with respect to the present invention is the terminal chain linked to the last nitrogen atom of the polyamide backbone.

In particular, with respect to the present invention, the ester groups of formula (B), which are part of the terminal fat chain and / or the pendant fat chain, correspond to 15-40% of the total number of ester groups and amide groups, particularly 20-35%. do.

In addition, m advantageously represents an integer in the range 1-5, or more specifically an integer greater than 2.

Preferably, R ₁ is a C _{12 to} C ₂₂ , preferably a C _{16 to} C ₂₂ alkyl group. Advantageously, R ₂ may be a divalent hydrocarbon group that is saturated or unsaturated and cyclic or acyclic, in particular R ₂ is a linear or branched chain (C _10- C _42). ) Represents an alkylene chain. Preferably, at least 50%, more preferably at least 75% of the R _{2 groups are groups with 30-42 carbon atoms.} Other R ₂ is, C ₄ ~C _19, further a hydrocarbon group of C ₄ -C _12.

Preferably, R ₃ represents a C ₂ -C ₃₆ hydrocarbon group or a polyoxyalkylene group, R ₄ represents a hydrogen atom. Preferably, R ₃ represents a C _{2 to} C ₁₂ hydrocarbon group.

The hydrocarbon group may be linear, cyclic, or branched and can be a saturated or unsaturated group. Moreover, the alkyl and alkylene groups may be linear or branched and may be saturated or unsaturated groups.

In general, the polymer of formula (B) has the form of a polymer mixture, which mixture can also further contain a compound of formula (B) where n is equal to 0, i.e. a synthetic product corresponding to a diester. Is.

According to a particular preferred embodiment of the invention, a mixture of copolymers of C36 diacid condensed in diamine ethylene is used and the terminal ester group ends the residual acid with cetyl alcohol, stearyl alcohol, or a mixture thereof ( It is produced by esterification with (also called cetylstearyl alcohol) (INCI name: ethylenediamine / stearyl dimerginolate copolymer). Its mass average molar mass is preferably 6000, more preferably 4000. These mixtures are specifically sold by ARIZONA CHEMICAL under the trade names UNICLEAR 80 and UNICLEAR 100 VG in the form of 80% (active material) and 100% (active material) in mineral oil, respectively. These mixtures are also sold by CRODA under the trade name OLEOCRAFT LP-10-PA- (MV) at 99.7% (active material), each with a preservative. They have a softening point of 88 ° C to 94 ° C.

Regarding the polyamide polycondensate satisfying the general formula (A), a polymer containing at least one terminal fat chain linked to the polymer main chain by at least one tertiary amide bonding group (amide-terminated polyamide or Also called ATPA). For more information on these polymers, reference US6503522 can be referred to.

According to a particularly preferred embodiment of the present invention, more specifically, a copolymer of hydrogenated dilinoleic acid, ethylenediamine, di (C14 to C18) alkylamine (INCI name: ethylenediamide / hydrogenated dimer dilinoleic acid copolymer bis-di-C14). ~ C18 alkylamide) is used. This copolymer is specifically marketed by ARIZONA CHEMICAL under the trade name SYLVACLEAR A200V.

Further, according to another embodiment, the polyamide having the formula (A) may be a poly (ester-amide) having an ester terminal (ester-terminal poly (ester-amide) or ETPEA), for example, preparation thereof. May be as described in Ref. US6552160.

According to a particularly preferred embodiment of the present invention, more specifically, a copolymer of linoleic hydride, ethylenediamine, neopentyl glycol, and stearyl alcohol (INCI name: bis-stearylethylenediamine / neopentyl glycol / hydrogenated linoleic acid). Stearyl Copolymer) is used. This copolymer is specifically marketed by ARIZONA CHEMICAL under the trade name SYLVACLEAR C75 V.

Furthermore, the polyamide polycondensate that can be used in the present invention contains at least one terminal fatty chain linked to the polymer main chain by at least one ether or polyether binding group (and). This can also be referred to as an ether-terminated poly (ether) amide). Such polymers are described, for example, in reference US6399713.

The polyamide according to the invention advantageously has a softening temperature of greater than 65 ° C and can range up to 190 ° C. It preferably has a softening temperature in the range of 70-130 ° C, more preferably 80-105 ° C. Polyamides are especially non-waxed polymers.

In addition, the polyamide polycondensate that can be used in the present invention includes a polyamide resin (a compound having more than two carbonyl groups and two amine groups) obtained as a result of the condensation of an aliphatic dicarboxylic acid and a diamine. ), And the carbonyl group and amine group of the adjacent unit pattern are condensed via an amide bond. These polyamide resins are specifically sold under the Versamid brand name by General Mills, Inc. and Henkel Corp. (Versamid 930, 744, or 1655), or the Onamid brand by Olin Mathieson Chemical Corp. Those sold under the name, especially Onamid S or C. These resins have a mass average molar mass in the range of 6000 to 9000. For more information on these polyamides, reference US3645705 and US3148125 can be referred to. More specifically, Versamid 930 or 744 is used.

Also, polyamides sold by Arizona Chemical under the reference name Uni-Rez (2658, 2931, 2970, 2621, 2613, 2624, 2665, 1554, 2623, 2662), and Henkel under the reference name Macromelt 6212. You can also use the products that are on sale. For further information on these polyamides, reference US5500209 can be referred to.

It is also possible to use plant-derived polyamide resins, such as those described in patents US5783657 and US5998570.

Preferably, the lipophilic polyamide polycondensate is a copolymer of C36 diacid condensed in diamine ethylene and the terminal ester group esterifies the terminal of the residual acid with cetyl alcohol, stearyl alcohol, or a mixture thereof. It is caused by that.

(b) The amount of the organic lipophilic gelling agent is 1% by mass or more, preferably 2% by mass or more, more preferably 3% by mass or more, still more preferably 4% by mass, based on the total mass of the anhydrous composition. It may be 20% by mass or less, preferably 15% by mass or less, more preferably 10% by mass or less, and even more preferably 7% by mass or less.

(Water-soluble particles)
The anhydrous composition according to the present invention contains at least one (c) water-soluble particles. Two or more kinds of (c) water-soluble particles may be used in combination. Therefore, a single type of water-soluble particles or a combination of different types of water-soluble particles can be used.

The term "water soluble" as used herein, room temperature (25 ° C.) and atmospheric pressure (10 ⁵ Pa) under at least 1 g / L in water, preferably at least 10 g / L, more preferably the solubility of at least 100 g / L Means a substance having.

Preferably, (c) the water-soluble particles are insoluble in oil, i.e., have a solubility in oil of less than 1 g / L, preferably less than 0.1 g / L.

The water-soluble particles may have any shape regardless of the crystal shape (for example, layered, cubic, hexagonal, orthorhombic, etc.), and may be a plate shape, a spherical shape, an oblong shape, or a polygonal shape.

In a preferred embodiment of the invention, the (c) water-soluble particles of the invention can function as water-soluble scrub particles. (C) Water-soluble particles as scrub particles can physically disintegrate keratin substances such as skin, especially the stratum corneum. In this embodiment, the water-soluble particles can be formed in the form of hard, sharp-edged rough-faced particles. The sharp-edged particles of the present invention can be formed in the form of polypyramids. Further, the rimmed scrub particles may be microneedles formed in the form of tetrahedral or pyramidal microstructures. In addition, each surface of the microneedle may be flat, rough or hollow. Sharp edges or rough surfaces can cause changes in the stratum corneum structure. The functional particles can later be dissolved by contacting the particles with water. After the particles have dissolved, the active ingredient can efficiently penetrate into the skin.

In certain embodiments of the invention, the water-soluble particles can have an aspect ratio of at least 1.1, preferably at least 1.2, more preferably at least 1.5, even more preferably at least 2, especially at least 2.5. In another embodiment of the invention, the water-soluble particles can have an aspect ratio of 2 or less, preferably 1.5 or less, more preferably 1.2 or less. The aspect ratio can be measured by common techniques in the art, such as image analysis using an electron microscope.

In another particular embodiment of the invention, the water-soluble particles have an average roundness determined by the image analysis method of 0.95 or less, preferably 0.9 or less, more preferably 0.85 or less, even more preferably 0.8 or less. Can have. In another embodiment of the invention, the water-soluble particles have an average roundness determined by an image analysis method of 0.7 or greater, preferably 0.8 or greater, more preferably 0.85 or greater, and even more preferably 0.9 or greater. obtain.

The "average roundness" can be determined by an image analysis method. In particular, "average roundness" is obtained by image analysis of scanning electron microscope (SEM) images of more than 2000 particles observed at 1000x magnification by secondary electron detection using a scanning electron microscope (SEM). It may be an arithmetic mean.

The "roundness" of each particle is calculated by the following formula.
C = 4π S / L ²
[In the formula, C represents the roundness, S represents the area (projected area) of the particles in the image, and L represents the length of the circumference (edge) of the particles in the image]
It is a value determined by. As the average roundness approaches 1, the shape of each particle becomes more spherical.

The water-soluble particles can have an average primary particle size of 10 μm or more, preferably 30 μm or more, more preferably 50 μm or more, still more preferably 100 μm or more, and particularly 200 μm or more. The average primary particle size of the water-soluble particles may be 1 mm or less, preferably 800 μm or less, more preferably 600 μm or less, and even more preferably 500 μm or less.

The term "average primary particle size" as used herein refers to the volume average size mean diameter given by the statistical particle size distribution for half of the population, with D50. Is called. For example, the average diameter of the volume average size can be measured with a laser diffraction particle size distribution analyzer, such as the Mastersizer 2000 manufactured by Malvern Corp.

The substance of (c) water-soluble particles of the present invention is not particularly limited as long as it dissolves by contact with an aqueous component such as water. However, in the cosmetological method according to the present invention, the aqueous composition is applied after the composition according to the present invention is applied to the keratin substance, and (c) the water-soluble particles are dissolved and permeate into the keratin substance such as skin. Therefore, preferably, (c) water-soluble particles are composed of components that are beneficial as cosmetics for keratin substances such as skin.

Accordingly, the water-soluble particles may be composed of polysaccharide particles, monosaccharide particles, amino acid particles, sugar alcohol particles, or ascorbic acid particles, and mixtures thereof. Examples of the polysaccharide include disaccharides such as sucrose, lactose and maltose, trisaccharides such as raffinose, and mucopolysaccharides such as hyaluronic acid, chondroitin sulfate and heparin. Monosaccharides can include pentoses, hexoses, and heptoses such as glucose, dextrose, galactose, mannose, and glucuronic acid. Examples of sugar alcohols include sorbitol and glucamine. Vitamin C can be mentioned as ascorbic acid.

(c) The amount of the water-soluble particles is 0.01% by mass or more, preferably 0.1% by mass or more, more preferably 0.2% by mass or more, still more preferably 0.5% by mass or more, based on the total mass of the anhydrous composition. It may be 15% by mass or less, preferably 10% by mass or less, more preferably 5% by mass or less, and even more preferably 3% by mass or less.

(Other ingredients)
-Alcohol The anhydrous composition according to the present invention may contain at least one alcohol. When two or more alcohols are used, they may be the same or different.

The alcohol contained in the composition according to the invention can be characterized by the Hansen solubility parameter. The Hansen solubility parameter is a solubility parameter disclosed by Charles M. Hansen, Charles Hansen in "Hansen Solubility Parameters: A User's Handbook", CRC Press (2007). The solubility parameter used here is a calculated numerical constant and is a tool in predicting the behavior of solvent materials. There are three experimentally and theoretically derived Hansen solubility parameters: dispersion force component (δD), polar or dipole interaction component (δP), and hydrogen bond component (δH). Each of the three parameters (ie, dispersion, polarity and hydrogen bonding) represents a different dissolution property or solvent capacity.

Alcohols have a Hansen solubility parameter δH (hydrogen bond component) that is less than 30 at 25 ° C. and δX (volume-dependent bond parameter: δX = (δD ² + δP ² ) ^1/2 ) that is less than 25 ° C. Is preferable.

The alcohol can be selected from, for example, oleyl alcohol, dodecanol, propylene glycol, diethylene glycol and combinations thereof.

The amount of alcohol may be 0.5% by mass or more, preferably 1% by mass or more, more preferably 3% by mass or more, still more preferably 5% by mass or more, based on the total mass of the anhydrous composition, and It may be 25% by mass or less, preferably 20% by mass or less, more preferably 15% by mass or less, and even more preferably 10% by mass or less.

Surfactants The anhydrous composition according to the invention may contain at least one surfactant selected from amphoteric, anionic, cationic or nonionic surfactants, which can be used alone or as a mixture. good.

Surfactants that can be included in the composition preferably have a low HLB value of 7.0 or less. The term HLB (“hydrophilic lipophilic balance”) is well known to those of skill in the art. When two or more surfactants are used, their HLB values are determined by the mass average of the HLB values of all the surfactants.

Examples of surfactants with low HLB values include, but are not limited to, fatty acid esters of glycol, sorbitol, and / or glycerol, such as polyglyceryl-2 stearate, polyglyceryl distearate-2, polyglyceryl isostearate-2, Polyglyceryl oleate-2, polyglyceryl distearate-3, polyglyceryl hexastearate-5, polyglyceryl pentaoleate-10, glyceryl stearate, sorbitan stearate, glyceryl laurate, acetylated ethylene glycol stearate, and isostearyl succinate. Diglyceryl can be mentioned.

The amount of the surfactant is not limited, but can be 0.1 to 20% by mass with respect to the total mass of the anhydrous composition according to the present invention.

Auxiliary agents The anhydrous compositions according to the invention are physiologically acceptable vehicles, cationic, anionic, nonionic, amphoteric or amphoteric ionic polymers or mixtures thereof, peptides and derivatives thereof, protein hydrolysates, Swelling agents, penetrants, inorganic or organic fillers, antioxidants, neutralizers, metal ion sequestering agents, fragrances, emollients, dispersants, dyes and / or pigments, organic or inorganic UV filters, vitamins or provitamins , Moisturizers, film-forming agents and / or thickeners, ceramides, preservatives, co-preservatives, and topical cosmetic compositions that may be selected from emulsions. Various auxiliaries can also be included.

The amount of the additional component is not limited, but can be 0.1% by mass to 30% by mass based on the total mass of the anhydrous composition according to the present invention.

The compositions according to the invention include (a) at least one oil, (b) at least one organic lipophilic gelling agent, (c) at least one water-soluble particle, and optionally one. It can be produced by mixing with the above other components.

[Cosmetology method]
The present invention is also a cosmetic method for keratin substances such as skin, wherein the anhydrous composition according to the present invention is applied onto the keratin substance, and then an aqueous composition containing water is applied onto the keratin substance. It also relates to a method comprising contacting with the anhydrous composition.

The anhydrous composition used in the first step of this method is the same as that described above. The method for applying the composition to the keratin substance is not particularly limited, and any method known in the art can be adopted. Generally, the composition is applied by hand.

The method according to the invention may include an optional step of massaging the keratinous material coated with the composition according to the invention. This step can promote the water-soluble particles in the composition to disintegrate the surface of keratinous substances, especially the stratum corneum. The massage process may be performed for at least 1 second.

In the step of contacting the aqueous composition with the anhydrous composition applied on the keratin substance, by applying the aqueous composition to the anhydrous composition, the water-soluble particles in the anhydrous composition are dissolved and the active ingredient is contained in the skin. It allows for very effective penetration into the skin.

The aqueous composition in this method comprises water. The amount of water in the aqueous composition is not particularly limited, but is generally 20% by mass or more, preferably 30% by mass or more, more preferably 40% by mass or more, still more preferably, based on the total mass of the aqueous composition. Is 50% by mass or more and 90% by mass or less, preferably 80% by mass or less, more preferably 75% by mass or less, and even more preferably 60% by mass or less.

The aqueous composition may contain other ingredients to meet cosmetic purposes. For example, the aqueous composition can include active ingredients for keratinous substances such as skin, oils, thickeners, emulsifiers, cosmetically acceptable hydrophilic organic solvents, and auxiliaries. Ingredients that can be incorporated into the aqueous composition will be described below.

-Active Ingredients The aqueous composition according to the invention preferably contains at least one active ingredient for keratinous substances such as skin. Two or more active ingredients for keratin substances may be used in combination.

The active ingredient for the keratin substance may be water soluble. More specifically, the active ingredient for keratinous substances has a solubility of at least 1 g / L, preferably at least 10 g / L in water.

The active ingredient for the keratin substance may be an organic compound that exerts any cosmetic or dermatological effect on the keratin substance such as skin. In particular, the active ingredients preferably exhibit cosmetic or dermatological effects on keratinous substances such as the skin after they have penetrated the keratinous substances and improve the condition of the skin. Preferably, the active ingredient is a whitening active ingredient, an anti-aging active ingredient, an anti-wrinkle active ingredient, or an antioxidant active ingredient.

Active ingredients include, in particular, Pro-Xylane (hydroxypropyl tetrahydropyran triol), a Vigna aconitifolia seed extract, such as that sold by Cognis under the reference names Vitoptine LS9529 and Vit-A-Like LS9737.

Other active ingredients include, for example, ascorbic acid and its derivatives, extracts of plants and vegetable proteins and their hydrolysates, algae extracts, especially luminaria, bacterial extracts, salicylic acid, α-hydroxy acids, β-hydroxy acids, For example, salicylic acid, oligopeptides and pseudodipeptides and acyl derivatives thereof, hyaluronic acid and salts thereof, and mixtures thereof can be mentioned.

The amount of the active ingredient may be 0.1% by mass or more, preferably 0.5% by mass or more, more preferably 1% by mass or more, still more preferably 2% by mass or more, based on the total mass of the aqueous composition. Moreover, it may be 15% by mass or less, preferably 10% by mass or less, more preferably 7% by mass or less, and even more preferably 5% by mass or less.

-Oil The aqueous composition according to the present invention may contain at least one oil. If more than one oil is used, they may be the same or different.

The oil that can be blended in the aqueous composition may be the same as the oil (a) described in the anhydrous composition according to the present invention described above.

In particular, the oil used in the aqueous composition can be selected from the group consisting of ester oils, silicone oils, fatty alcohols, and fatty acids.

Ester oils are preferably saturated or unsaturated, and linear or branched C ₁ -C ₂₆ aliphatic monoacid or polyacid, saturated or unsaturated, linear or branched C _{1 to} C ₂₆ Liquid esters with aliphatic monovalent alcohols or polyhydric alcohols, and the total number of carbon atoms of these esters is 10 or more.

Preferably, in the case of an ester of a monohydric alcohol, at least one of the alcohols and acids from which the ester of the invention is derived is branched. Among the monoesters of monoacids and monohydric alcohols, ethyl palmitate, ethylhexyl palmitate, isopropyl palmitate, dicaprylyl carbonate, alkyl myristate, such as isopropyl myristate or ethyl myristate, isosetyl stearate, 2-ethylhexyl isononanoate, Examples thereof include isononyl isononanoate, isodecyl neopentate and isostearyl neopentate.

Specific examples include: diethyl sebacate, isopropyl lauroyl sarcosate, diisopropyl sebacate, bis sebacate (2-ethylhexyl), diisopropyl adipate, di-n-propyl adipate, dioctyl adipate, bis adipate. (2-Ethylhexyl), diisostearyl adipate, bis maleate (2-ethylhexyl), triisopropyl citrate, triisocetyl citrate, triisostearyl citrate, glyceryl trilactic acid, glyceryl trioctanoate, trioctyldodecyl citrate, Trioleyl citrate, neopentyl glycol diheptate, and diethylene glycol diisononanoate.

Examples of silicone oils include linear organopolysiloxanes such as dimethylpolysiloxane, methylphenylpolysiloxane, methylhydrogenpolysiloxane, and cyclic organopolysiloxanes such as cyclohexasiloxane, octamethylcyclotetrasiloxane, decamethyl. Cyclopentasiloxane, dodecamethylcyclohexasiloxane and the like, and mixtures thereof can be mentioned. Preferably, the silicone oil is selected from liquid polydialkylsiloxanes, in particular liquid polydimethylsiloxanes (PDMS, dimethicone), and liquid polyorganosiloxanes containing at least one aryl group. These silicone oils may also be organically modified. Organically modified silicones that can be used in accordance with the present invention are the silicone oils defined above and include in their structure one or more organic functional groups attached via hydrocarbon groups.

The term "fat" in fatty alcohols means that it contains a relatively large number of carbon atoms. Therefore, alcohols having 4 or more, preferably 6 or more, more preferably 12 or more carbon atoms are included in the range of fatty alcohols. Fatty alcohols may be saturated or unsaturated. The fatty alcohol may be linear or branched.

Fatty alcohols are saturated and unsaturated in structure R-OH (in the formula, R contains 4 to 40 carbon atoms, preferably 6 to 30 carbon atoms, more preferably 12 to 20 carbon atoms. It can have saturated, linear and branched groups). In at least one embodiment, R can be selected from _{C 12-} C ₂₀ alkyl groups and C _12- C _{20 alkenyl groups.} R may or may not be substituted with at least one hydroxyl group. Examples of fatty alcohols include lauryl alcohol, cetyl alcohol, stearyl alcohol, isostearyl alcohol, behenyl alcohol, undecylenyl alcohol, myristyl alcohol, octyldodecanol, hexyldecanol, oleyl alcohol, linoleil alcohol, palmitrail alcohol, arachidnyl alcohol, Elsyl alcohol and mixtures thereof can be mentioned. The fatty alcohol is preferably a saturated fatty alcohol. Therefore, the fatty alcohol is a linear or branched, saturated or unsaturated C _{6 to} C ₃₀ alcohol, preferably a linear or branched, saturated C _{6 to} C ₃₀ alcohol, more preferably. You can choose from linear or branched, saturated C _{12 to} C _{20 alcohols.} Examples of saturated fatty alcohols include lauryl alcohol, cetyl alcohol, stearyl alcohol, isostearyl alcohol, behenyl alcohol, undecylenyl alcohol, myristyl alcohol, octyldodecanol, hexyldecanol, and mixtures thereof.

Fatty acids that can be used in the context of the present invention are more specifically selected from saturated or unsaturated carboxylic acids containing 6-30 carbon atoms, particularly 9-30 carbon atoms. The fatty acid is advantageously selected from myristic acid, palmitic acid, stearic acid, behenic acid, oleic acid, linoleic acid, linolenic acid, and isostearic acid.

The amount of oil may be in the range of 5 to 50% by weight, preferably 10 to 40% by weight, more preferably 15 to 30% by weight, based on the total mass of the aqueous composition.

-Thickener The aqueous composition according to the present invention may contain at least one thickener. Two or more thickeners may be combined. The thickener may be hydrophilic or lipophilic.

Oil lip thickeners include carboxyvinyl polymers such as Carbopol products (Carbomer) and Pemulen products (acrylate / C10 to C30 alkyl acrylate copolymers) or polymers having the INCI name "Poly C10 to 30 alkyl acrylates", such as Air Products. An oil-based product that can be selected from Intelimer® products manufactured by Intelimer®, for example, Intelimer® IPA 13-1, which is a polystearyl acrylate, or 30 Intelimer® IPA 13-6, which is a behenyl polymer. Polymer thickeners can be mentioned.

Hydrophilic thickeners include, for example, glucan, modified and non-modified starch (eg, those derived from grains, such as wheat, corn or rice, those derived from vegetables, such as yellow pea, and stalks, such as potatoes or. Cassaba), amylose, amylopectin, glycogen, dextran, cellulose, and their derivatives (methyl cellulose, hydroxyalkyl cellulose, ethyl hydroxyethyl cellulose and carboxymethyl cellulose), mannan, xylan, lignin, araban, galactan, galacturonan, chitin, chitosan, glucurono Kisilane, arabinoxylan, xyloguelucan, glucomannan, pectic acid and pectin, alginate and alginate, arabinogalactan, caragenan, agar, glycosaminoglucan, arabic gum, tragacanto gum, gatti gum, karaya gum, carob gum, galactomannan, eg guar gum Examples thereof include hydrophilic nonionic polysaccharide thickeners which can be selected from their nonionic derivatives (eg, hydroxypropyl guar), xanthan gum, and mixtures thereof.

The amount of thickener may be in the range of 0.01 to 10% by mass, preferably 0.1 to 5% by mass, more preferably 0.5 to 5% by mass, based on the total mass of the aqueous composition.

-Emulsifier The aqueous composition according to the invention may contain at least one emulsifier selected from amphoteric, anionic, cationic or nonionic surfactants used alone or as a mixture. Preferably, the composition comprises at least one nonionic surfactant.

Examples of nonionic surfactants that can be used in the compositions of the present invention include polyethoxylyylated fatty alcohols or polyglycerolylated fatty alcohols, such as ethylene oxide and lauryl alcohol containing 9-50 oxyethylene units in particular. Additives (in CI names Laures-9 to Laures-50), especially Laures-9, eg esters of polyols with saturated or unsaturated chains containing 8-24 carbon atoms and fatty acids, and their oxyalkylenes. Derivatives, i.e. those containing oxyethylene and / or oxypropylene units, such _{as esters of glycerol with C 8-} C ₂₄ fatty acids, such as glyceryl stearate, and oxyalkyleneized derivatives thereof, particularly polyoxyethylene steric acid (mono). , Di, and / or tristearic acid) glyceryl, such as PEG-20 glyceryl triisostearate, polyoxyalkylene glycolyl ester, such as polyoxyethylene glycol, eg ethylene oxide and lauric acid, palmitic acid, stearic acid or behen Additives with acid esters and mixtures thereof, especially those containing 9-100 oxyethylene units, such as PEG-9 to PEG-50 stearate (CTFA name: PEG-9 stearate to PEG-PEGyl stearate). 50), esters of sugars (sucrose, maltose, glucose, fructose, and / or alkylglycos) with C _8- C ₂₄ fatty acids, such as sucrose tristearate, and oxyalkyleneized derivatives thereof, such as sucrose tristearate, Ethers of sugar and C _8- C ₂₄ fatty alcohols, such as caprylyl / capryl glucoside, polyoxyethylene alkyl ether, polyoxyethylene oxypropylene alkyl ether, fatty acid alkanolamide, alkylamine oxide, alkylpolyglycoside and silicone surfactants, For example, polydimethylsiloxane containing an oxyethylene group and / or an oxypropylene group, such as PEG-10 dimethicone, bis-PEG / PPG-14 / 14 dimethicone, bis-PEG / PPG-20 / 20 dimethicone, and PEG / PPG. -20/6 Dimethicone, and polyglyceryl fatty acid esters such as polyglyceryl dicaprate-6, polyglyceryl dioleate-6, polyglyceryl caprylate-6, polyglyceryl oleate Lil-2, polyglyceryl-6 polyricinoleate, and mixtures thereof can be mentioned.

The emulsifier may also include a Gemini surfactant. As a Gemini surfactant, a mixture of dilauramide glutamididine sodium and butylene glycol (INCI name: dilauramide glutamididine sodium) sold by Asahi Kasei Chemicals Co., Ltd. under the trade name of Pellicer LB -30G is used. Can be mentioned.

The amount of emulsifier may be in the range of 0.1 to 30% by mass, preferably 1 to 20% by mass, more preferably 2 to 10% by mass, based on the total mass of the aqueous composition.

-Hydrophilic organic solvent acceptable as cosmetics The aqueous composition according to the present invention may contain at least one hydrophilic organic solvent acceptable as cosmetics. Hydrophilic organic solvents that are acceptable as cosmetics include, for example, substantially linear or branched lower monovalent alcohols having 1 to 8 carbon atoms, such as ethanol, propanol, butanol, isopropanol and iso. Butanol; aromatic alcohols such as benzyl alcohol and phenylethyl alcohol; polyols or polyol ethers such as propylene glycol, dipropylene glycol, isoprene glycol, butylene glycol, glycerin, propanediol, caprylyl glycol, pentylene glycol, sorbitol, ethylene glycol Monomethyl, monoethyl and monobutyl ethers, propylene glycol ethers such as propylene glycol monomethyl ethers, diethylene glycol alkyl ethers such as diethylene glycol monoethyl ethers or monobutyl ethers; polyethylene glycols such as PEG-4, PEG-6 and PEG-8, and Examples thereof include derivatives thereof and combinations thereof.

The amount of hydrophilic organic solvent allowed as a cosmetic is in the range of 1 to 30% by mass, preferably 2 to 20% by mass, more preferably 3 to 10% by mass, based on the total mass of the aqueous composition. You can.

Auxiliary agents The aqueous compositions according to the invention are physiologically acceptable vehicles, cationic, anionic, nonionic, amphoteric or amphoteric ionic polymers or mixtures thereof, peptides and derivatives thereof, protein hydrolysates, Acidifying agents or basicizing agents commonly used in the cosmetic field such as swelling agents, penetrants, inorganic or organic fillers, antioxidants, neutralizers, sodium hydroxide, metal ion sequestering agents such as EDTA, Fragrances, skin softeners, dispersants, organic or inorganic UV filters, dyes and / or pigments, vitamins or provitamins, moisturizers, film-forming agents, ceramides, preservatives such as phenoxyethanol, methylparaben, ethylparaben, propylparaben, and Various supplements conventionally used in compositions for sun care products, which may be selected from chlorphenesin, co-preservatives, and opalescent agents, can also be included.

The amount of the additional component is not limited, but can be 0.1% by weight to 30% by weight based on the total weight of the aqueous composition according to the present invention.

The pH of the aqueous phase of the present invention is not particularly limited. The pH of the aqueous phase may be in the range of 3.0 to 12.0, preferably 4.0 to 9.0. The pH of the aqueous phase of the present invention can be adjusted to a desired value using an acidifying agent or a basicizing agent commonly used in the cosmetics field.

The aqueous composition according to the invention takes various forms such as solutions, gels, lotions, serums, suspensions, dispersions, fluids, emulsions, pastes, creams, emulsions (O / W or W / O types). Can be done.

The aqueous composition according to the invention can be applied to the anhydrous composition according to the invention applied, for example, in the form of a wet sheet mask, mist, spray or topical application on the surface of a keratinous material.

The present invention will be described in more detail by way of examples. However, these examples should not be construed as limiting the scope of the invention.

(Example 1 and Comparative Example 1)
Each anhydrous composition according to Example 1 (Ex.1) and Comparative Example 1 (Comp. Ex.1) was prepared by uniformly mixing the components listed in Table 1 below. .. Their formulations are also shown in Table 1 below. Among the ingredients, sucrose was obtained from Tereos Sucre France with an average primary particle size of 250 μm (product name: SUCRE SEMOULE SURFINE 250). All numerical values for the amount of ingredients are based on the "mass%" of the active ingredient.

[evaluation]
(Rheological characteristics)
The viscous properties of the anhydrous composition according to Example 1 were evaluated using Discovery Hybrid Rheometer 2 (TA instrument) equipped with a 40 mm parallel plate with a setting interval of 30 μm at 25 ° C. Viscoelasticity was measured with a frequency of 1 Hz and a strain (%) variation of 0.01-1000%.

Hysteresis was measured in the same manner as the viscoelasticity analysis above, except that a shear cycle of 0.1-100 seconds- ^{1 was applied and then returned to 100-100 seconds-1.} In the gel composition of the present invention, the change in final viscosity value under all shear conditions is less than 10% compared to the initial viscosity value.

The results of viscoelasticity are shown in Fig. 1. As can be seen in FIG. 1, the intersection of the storage modulus G'and the loss modulus G'was an elastic modulus of 43.5 Pa (Y-axis) and a strain of 17.6% (X-axis). In addition, the linear viscoelastic region of G'showed 102 Pa and the linear viscoelastic region of G'' showed 12.5 Pa.

The composition according to Example 1 showed a very low level of hysteresis, i.e., the change in final viscosity value under all shear conditions was less than 10% compared to the initial viscosity value.

Correspondingly, it can be said that the anhydrous composition according to Example 1 exhibits very favorable viscoelasticity, can provide a comfortable texture with a bulging feel, and can exhibit shape memory gel-like properties. Furthermore, the anhydrous composition according to the present invention can exhibit improved stability, lifetime and transparency because the particles do not precipitate for a long time.

(In vitro permeation experiment)
The compositions according to Example 1 and Comparative Example 1 were evaluated for the transdermal permeation property of the active ingredient by the following Franz cell (static diffusion cell) test.

^{A composition of 5 mg / cm 2} of each of Example 1 and Comparative Example 1 was applied to a specific area of the surface of the full-thickness skin of a pig. The surface of the skin was then manually massaged with a finger covered with a finger cot for 3 minutes. The skin was dried in the air for 2 minutes. A 10 mg / cm ² aqueous composition was then applied onto the skin surface coated with the anhydrous composition and the skin was massaged for 30 seconds. The formulations of the aqueous compositions are listed in Table 2 below. All numerical values for the amount of ingredients are based on the "mass%" of the active ingredient in Table 2. The skin was then attached to Franz cell. Franz cell had a 2 cm ² application area and the cell receptor solution was a 3 mL aqueous NaCl 0.9% (w / w) solution. The receptor solution was stirred during the test. Pig skin was placed between the donor and receptor compartments in the above application area of 2 cm ^2. The temperature of the pig skin was maintained at 32 degrees. After 16 hours, the skin surface was washed with a suitable protocol to ensure the removal of all chemicals remaining on the skin surface, the porcine skin was removed, and then 10 continuous tape strips (DSquam®). The stratum corneum was removed by. The active ingredient (hydroxypropyl tetrahydropyran triol), epidermis, and dermis in the receptor solution were analyzed by LC / MS / MS. Three donors (n = 9) were used in triple repeats for each composition.

^{The average value of the amount of active ingredient (mg / cm 2 of} skin) that passed through the stratum corneum of porcine skin was calculated and shown in Table 3.

The use of the composition according to Example 1 showed excellent permeability of the active ingredient. Therefore, it can be said that the composition and cosmetological method according to the present invention are very useful for the local delivery of the active ingredient for keratin substances such as skin.

Claims (15)

Anhydrous composition for keratinous substances such as skin.
(a) At least one oil and
(b) With at least one organic lipophilic gelling agent,
(c) An anhydrous composition comprising at least one water-soluble particle. (B) The anhydrous composition according to claim 1, wherein the organic lipophilic gelling agent is selected from styrene block copolymers, semi-crystalline polymers, glutamid compounds, polyamides, and mixtures thereof, preferably polyamides. (c) The average primary particle size of the water-soluble particles is 10 μm or more, preferably 30 μm or more, more preferably 50 μm or more, still more preferably 100 μm or more, particularly 200 μm or more, and 1 mm or less, preferably 800 μm or less, more preferably. The anhydrous composition according to claim 1 or 2, which is 600 μm or less, more preferably 500 μm or less. (c) The anhydrous composition according to any one of claims 1 to 3, wherein the water-soluble particles include polysaccharide particles, monosaccharide particles, amino acid particles, sugar alcohol particles, or ascorbic acid particles, and a mixture thereof. .. (a) The amount of oil is 50% by mass or more, preferably 60% by mass or more, more preferably 70% by mass or more, still more preferably 80% by mass or more, and more preferably 80% by mass or more, based on the total mass of the anhydrous composition. The anhydrous composition according to any one of claims 1 to 4, which is 99% by mass or less, preferably 95% by mass or less, more preferably 90% by mass or less, and even more preferably 85% by mass or less. (b) The amount of the organic lipophilic gelling agent is 1% by mass or more, preferably 2% by mass or more, more preferably 3% by mass or more, still more preferably 4% by mass, based on the total mass of the anhydrous composition. The anhydrous according to any one of claims 1 to 5, which is 20% by mass or less, preferably 15% by mass or less, more preferably 10% by mass or less, and even more preferably 7% by mass or less. Composition. (c) The amount of water-soluble particles is 0.01% by mass or more, preferably 0.1% by mass or more, more preferably 0.2% by mass or more, still more preferably 0.5% by mass or more, based on the total mass of the anhydrous composition. The anhydrous composition according to any one of claims 1 to 6, wherein the composition is 15% by mass or less, preferably 10% by mass or less, more preferably 5% by mass or less, and even more preferably 3% by mass or less. Linear viscoelasticity (G') profile and loss modulus (G'') of the anhydrous composition on a log scale when measured using a rheometer at 25 ° C. and a frequency of 1 Hz using a 40 mm cone plate. The anhydrous composition according to any one of claims 1 to 7, wherein the elastic region is 10 ^-1 Pa or more, and the strain at the intersection of G'and G'' is more than 4%. Preferably, the Hansen solubility parameter δ _H (hydrogen bond component) at 25 ° C is less than 30, and δ _X (volume-dependent bond parameter: δ _X = (δ _D ² + δ _P ² ) ^1/2 ) is less than 25. The anhydrous composition according to any one of claims 1 to 8, further comprising at least one alcohol. The amount of alcohol is 0.5% by mass or more, preferably 1% by mass or more, more preferably 3% by mass or more, still more preferably 5% by mass or more, and 25% by mass, based on the total mass of the anhydrous composition. The anhydrous composition according to claim 9, wherein the composition is preferably 20% by mass or less, more preferably 15% by mass or less, and even more preferably 10% by mass or less. A cosmetological method for keratin substances such as skin
The step of applying the anhydrous composition according to any one of claims 1 to 10 to the keratin substance, and
A method comprising contacting an aqueous composition containing water with a coated anhydrous composition. 11. The aqueous composition comprises at least one active ingredient for a keratinous substance such as skin, preferably selected from a whitening active ingredient, an anti-aging active ingredient, an anti-wrinkle active ingredient, or an antioxidant active ingredient. The method described in. The amount of the active ingredient is 0.1% by mass or more, preferably 0.5% by mass or more, more preferably 1% by mass or more, still more preferably 2% by mass or more, and 15% by mass, based on the total mass of the aqueous composition. The method according to claim 12, wherein the method is% or less, preferably 10% by mass or less, more preferably 7% by mass or less, and even more preferably 5% by mass or less. The amount of water is 20% by mass or more, preferably 30% by mass or more, more preferably 40% by mass or more, still more preferably 50% by mass or more, and 90% by mass, based on the total mass of the aqueous composition. The method according to any one of claims 11 to 13, preferably 80% by mass or less, more preferably 75% by mass or less, and even more preferably 60% by mass or less. The method of any one of claims 11-14, wherein the aqueous composition is applied to the applied anhydrous composition in the form of a wet sheet mask, mist, spray, or topical application.

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