Stabilization of composition comprising polyhydroxy acid, beta-hydroxy acid and peptide with polyol

Abstract

The present invention relates to a composition comprising: (a) at least one first compound selected from polyhydroxy acids and salts thereof; (b) at least one second compound selected from p-hydroxy acids and salts thereof; (c) at least one peptide; and (d) at least one polyol. The composition according to the present invention is stable.

Description

[0001] DESCRIPTION

[0002] TITLE OF INVENTION

[0003] STABILIZATION OF COMPOSITION COMPRISING POLYHYDROXY ACID, BETAHYDROXYACID AND PEPTIDE WITH POLYOL

[0004] TECHNICAL FIELD

[0005] The present invention relates to a composition, preferably a cosmetic composition, and more preferably a skin care cosmetic composition.

[0006] BACKGROUND ART

[0007] Peptides are short amino acid sequences some of which have activity or a function useful for antiaging skin care, such as anti-wrinkle activity. These peptides, generally simply referred to as “peptides” in the skin care field, are well known active agents to be added to skin care products for improving the appearance of the surface of the skin.

[0008] On the other hand, peeling is also a well-known means for improving the appearance of the surface of the skin, in particular for treating visible and / or tactile irregularities of the human skin, and for example to attenuate defects of pigmentation such as skin freckles or the marks due to acne or varicella, or to smooth irregularities in the texture of the skin, in particular wrinkles or minor wrinkles.

[0009] This peeling has the effect of removing part of the skin to be treated (the epidermis and possibly upper layer of dermis) by chemical methods such as the application of compositions containing a peeling agent(s) stimulating the desquamation of the skin, for example alpha-hydroxy acids (AHAs) such as glycolic acid or beta-hydroxy acids (BHAs) such as salicylic acid, or else other active substances such as retinoic acid, resorcinol, trichloroacetic acid or phenol.

[0010] DISCLOSURE OF INVENTION

[0011] Polyhydroxy acids (PHAs) are also useful as peeling agents. In general, PHAs have a larger molecule size than AHAs.

[0012] However, it has been found that, if PHA is used in combination with peptide and BHA, in a composition, the composition becomes unstable.

[0013] An objective of the present invention is to provide a stable composition comprising PHA in combination with peptide and BHA.

[0014] The above objective of the present invention can be achieved by a composition comprising:

[0015] (a) at least one first compound selected from polyhydroxy acids and salts thereof;

[0016] (b) at least one second compound selected from p-hydroxy acids and salts thereof;

[0017] (c) at least one peptide; and

[0018] (d) at least one polyol.

[0019] The (a) first compound may be in the form of a lactone. It is preferable that the (a) first compound be gluconolactone. The amount of the (a) first compound(s) in the composition according to the present invention may be from 0.01% to 20% by weight, preferably from 0.1% to 15% by weight, and more preferably from 1% to 10% by weight, relative to the total weight of the composition.

[0020] The (b) second compound may be represented by the following formula (I): in which:

[0021] Ri represents a hydrogen atom, or a saturated, linear, branched or cyclized aliphatic, alkoxy, ester or ketoxy chain, an unsaturated hydrocarbon chain carrying one or more conjugated or unconjugated double bonds, these chains containing from 1 to 22 carbon atoms and being capable of being substituted with at least one substituent chosen from halogen atoms, trifluoromethyl group, hydroxyl group in free form or esterified with an acid having from 1 to 6 carbon atoms and alternatively with a carboxyl functional group, which is free or esterified with a lower alcohol having from 1 to 6 carbon atoms;

[0022] R2 represents a hydroxyl group, or an ester functional group of the following formula (II): where R4 represents a saturated aliphatic group or an alkenyl group having from 1 to 18 carbon atoms; and

[0023] R3 represents a hydrogen atom, or a saturated or unsaturated linear or branched hydrocarbon chain having from 2 to 30 carbon atoms, optionally containing one or more substituents.

[0024] It is preferable that the (b) second compound be salicylic acid.

[0025] The amount of the (b) second compound(s) in the composition according to the present invention may be from 0.01% to 10% by weight, preferably from 0.05% to 5% by weight, and more preferably from 0.1 % to 1 % by weight, relative to the total weight of the composition.

[0026] It is preferable that the (c) peptide be selected from the group consisting of acetyl hexapeptide-8, dipeptide diaminobutyroyl benzylamide diacetate, and a mixture thereof.

[0027] The amount of the (c) peptide(s) in the composition according to the present invention may be from 0.0001% to 1% by weight, preferably from 0.0005% to 0.5% by weight, and more preferably from 0.001 % to 0.1 % by weight, relative to the total weight of the composition.

[0028] The (d) polyol may be selected from glycols, preferably selected from the group consisting of propyleneglycol, butyleneglycol, pentyleneglycol, hexyleneglycol and mixtures thereof, and more preferably selected from the group consisting of butyleneglycol, pentyleneglycol, and a mixture thereof.

[0029] The amount of the (d) polyol(s) in the composition according to the present invention may be from 1% to 20% by weight, preferably from 2% to 15% by weight, and more preferably from 3% to 10% by weight, relative to the total weight of the composition.

[0030] The composition according to the present invention may comprise (e) at least one hydrophilic thickener.

[0031] The amount of the (e) hydrophilic thickener(s) in the composition according to the present invention may be from 0.001% to 5% by weight, preferably from 0.01% to 3% by weight, and more preferably from 0.1% to 1% by weight, relative to the total weight of the composition.

[0032] The composition according to the present invention may comprise no a-hydroxy acid.

[0033] The present invention also relates to a cosmetic process for treating a keratin substance, preferably for treating the skin, and more preferably for peeling the skin, comprising the step of applying the composition according to the present invention.

[0034] BEST MODE FOR CARRYING OUT THE INVENTION

[0035] After diligent research, the inventors have discovered that it is possible to provide a stable composition which comprises PHA in combination with peptide and BHA.

[0036] Thus, one aspect of the present invention is a composition comprising:

[0037] (a) at least one first compound selected from polyhydroxy acids and salts thereof;

[0038] (b) at least one second compound selected from P-hydroxy acids and salts thereof;

[0039] (c) at least one peptide; and

[0040] (d) at least one polyol.

[0041] A composition comprising the (a) first compound in combination with the (b) second compound and the (c) peptide, without the (d) polyol, is unstable such that the composition becomes cloudy, separates into different phases, causes precipitation, or changes in color, in particular at higher temperature or under the cycle of from hot to cold conditions and vice versa.

[0042] On the other hand, the composition according to the present invention comprising the (d) polyol, with the (a) first compound, the (b) second compound, and the (c) peptide is stable. Thus, the composition according to the present invention can prevent or reduce becoming cloudy, separating into different phases, causing precipitation, or changing in color, in particular at higher temperature or under the cycle of from hot to cold conditions and vice versa.

[0043] Accordingly, the composition according to the present invention is stable, and can be safely stored even under hot conditions or a long period of time such as from summer to winter.

[0044] The composition according to the present invention can also provide additional effects.

[0045] It is known that the (d) polyol such as glycerin cause a sticky feeling to touch. The term “sticky” here means a property which provides a tacky feeling to the skin. The composition according to the present invention includes the (d) polyol for stabilizing the composition. The greater the amount of the (d) polyol is used, the more the composition is stabilized. However, even if the amount of the (d) polyol is increased, surprisingly, the stickiness of the composition according to the present invention is not increased (rather, in general, decreased). In other words, the stickiness of the composition can be reduced, and therefore, the composition according to the present invention can provide a less sticky feeling to the touch.

[0046] Thus, the composition according to the present invention can provide an excellent feeling, such as a less sticky feeling, during and / or after application of the composition.

[0047] Nevertheless, the use of too great an amount of the (d) polyol tends to increase stickiness due to its own properties. Therefore, it is preferable that the amount of the (d) polyol in the composition according to the present invention is 15% by weight or less, and more preferably 10% by weight or less, relative to the total weight of the composition.

[0048] The composition according to the present invention is useful for peeling off the superficial layer of the stratum comeum or homy layer of the skin.

[0049] Thus, the composition according to the present invention can provide cosmetic effects of exfoliating the skin, improving the condition of the skin, and the like, in terms of both the appearance and the feel to the touch of the skin, including smoothing the skin, refining and brightening the skin tone, reducing blemishes, pores and blackheads.

[0050] The composition according to the present invention is also useful for reducing wrinkles and / or fine lines on the skin, resulting in improving the appearance of the surface of the skin.

[0051] Thus, the composition according to the present invention can also provide cosmetic effects of, for example, anti-aging.

[0052] Hereinafter, the present invention will be explained in a more detailed manner.

[0053] [Composition]

[0054] The composition according to the present invention includes:

[0055] (a) at least one first compound selected from polyhydroxy acids and salts thereof;

[0056] (b) at least one second compound selected from P-hydroxy acid and salts thereof;

[0057] (c) at least one peptide; and

[0058] (d) at least one polyol.

[0059] (Polyhydroxy Acid)

[0060] The composition according to the present invention comprises (a) at least one first compound selected from polyhydroxy acids and salts thereof. If two or more first compounds are used, they may be the same or different.

[0061] The term “polyhydroxy acid” here means an organic compound which has at least one carboxyl group and a plurality of hydroxy groups. The number of carboxyl groups in the polyhydroxy acid is not limited, but one or two carboxyl groups are preferable, and one carboxyl group is more preferable. The number of hydroxyl groups in the polyhydroxy acid is also not limited, but 2 to 10 are preferable, and 2 to 6 are more preferable. The number of carbon atoms in the polyhydroxy acid is not limited, but 3 to 11 are preferable, and 3 to 8 are more preferable.

[0062] The above organic compound may be aliphatic or aromatic. In other words, the polyhydroxy acid may be selected from aliphatic polyhydroxy acids or aromatic polyhydroxy acids. It is preferable that the aliphatic polyhydroxy acid be selected from sugar acids.

[0063] Examples of the polyhydroxy acid include, dihydroxy propanoic acid such as glyceric acid; trihydroxy butanoic acid such as erythronic acid and threonic acid; tetrahydroxy pentanoic acid such as ribonic acid, arabinoic acid, xylonic acid, and lyxonic acid; pentahydroxy hexanoic acid such as allonic acid, altronic acid, gluconic acid, mannoic acid, gulonic acid, idonic acid, galactonic acid, and talonic acid; hexahydroxy heptanoic acid such as glucoheptanoic acid, galactoheptonic acid; tartaric acid; lactobionic acid, maltobionic acid, and mixtures thereof.

[0064] It is preferable that the (a) first compound be in the form of a lactone. The lactone ring of the (a) first compound in the form of a lactone may be saturated. Examples of the (a) first compound include, gluconolactone, ribonolactone, and a mixture thereof.

[0065] It is more preferable that the (a) first compound be gluconolactone. As gluconolactone, a commercially available product, such as Glucono-delta-Lactone F5010 marketed by Jungbunzlauer, may be used.

[0066] The type of the salt is not limited. Examples of the salt include alkaline metal salts such as sodium salt and potassium salt; alkaline earth metal salts such as calcium salt and magnesium salt; zinc salts; iron salts; ammonium salts; amine salts such as monoethanolamine salt, diethanolamine salt and triethanolamine salt; and mixtures thereof. Sodium salt is preferable. If two or more salts are used, they may be the same or different.

[0067] The amount of the (a) first compound(s) in the composition according to the present invention is 0.01% by weight or more, preferably 0.1% by weight or more, and more preferably 1% by weight or more, relative to the total weight of the composition.

[0068] On the other hand, the amount of the (a) first compound(s) in the composition according to the present invention may be 20% by weight or less, preferably 15% by weight or less, and more preferably 10% by weight or less, relative to the total weight of the composition.

[0069] The amount of the (a) first compound(s) in the composition according to the present invention may be from 0.01% to 20% by weight, preferably from 0.1% to 15% by weight, and more preferably from 1% to 10% by weight, relative to the total weight of the composition.

[0070] (P-Hydroxy Acid)

[0071] The composition according to the present invention comprises (b) at least one second compound selected from p-hydroxy acids and salts thereof. If two or more second compounds are used, they may be the same or different.

[0072] The term “P-hydroxy acid” or “BHA”, here means a carboxylic acid which has at least one hydroxyl group on the beta carbon atom.

[0073] As P-hydroxy acids, mention may be made, without limitation, of salicylic acid and its derivatives. Salicylic acid and its derivatives may be represented by the following formula (I): in which:

[0074] Ri represents a hydrogen atom, or a saturated, linear, branched or cyclized aliphatic, alkoxy, ester or ketoxy chain, an unsaturated hydrocarbon chain carrying one or more conjugated or unconjugated double bonds, these chains containing from 1 to 22 carbon atoms and being capable of being substituted with at least one substituent chosen from halogen atoms, trifluoromethyl group, hydroxyl group in free form or esterified with an acid having from 1 to 6 carbon atoms and alternatively with a carboxyl functional group, which is free or esterified with a lower alcohol having from 1 to 6 carbon atoms;

[0075] R2 represents a hydroxyl group, or an ester functional group of the following formula (II): where R4 represents a saturated aliphatic group or an alkenyl group having from 1 to 18 carbon atoms;

[0076] R3 represents a hydrogen atom, or a saturated or unsaturated linear or branched hydrocarbon chain having from 2 to 30 carbon atoms, optionally containing one or more substituents. The hydrocarbon chain may be chosen from alkyl and alkenyl radicals containing from 2 to 30 carbon atoms, which are optionally substituted. The substituent may be in particular a hydroxyl radical.

[0077] When R3 is a hydrogen atom, it is also possible to use salts of the acids of the above formula (I), and in particular salts obtained by salification with a base.

[0078] As a base which is capable of salifying the salicylic acid derivatives of the above formula (I), mention may be made of, without limitation, inorganic bases such as alkali metal hydroxides (sodium and potassium hydroxides) or ammonium hydroxides or better still the organic bases such as primary, secondary, tertiary or cyclic organic amines and more especially amino acids. By way of example of bases, mention may be made of glycine, lysine, arginine, taurine, histidine, alanine, valine, cysteine, trihydroxymethylaminomethane (TRISTA) and triethanolamine.

[0079] According to a specific embodiment of the present invention, as derivatives of the above formula (I), those where the radical Ri contains at least 4 carbon atoms are used in the composition of the present invention are preferred. It is for example formed of a saturated linear alkyl or alkoxy radical having from 4 to 11 carbon atoms.

[0080] As derivatives of the above formula (I) in which Ri is formed of a saturated, linear alkyl or alkoxy radical having from 4 to 11 carbon atoms, R2 is a hydroxyl group, and R3 is a hydrogen atom, mention may be made for example of 5-n-octanoylsalicylic (CTFAname: Capryloyl Salicylic Acid), 5-n-decanoylsalicylic, 5-n-dodecanoylsalicylic, 5-n-octylsalicylic, 5-n-heptyloxysalicylic, 5-tert-octylsalicylic, 5-butoxysalicylic, 5-ethoxysalicylic, 5 -methoxysalicylic, 5-propoxysalicylic, 5 -methylsalicylic, 5 -ethylsalicylic and 5-propylsalicylic acids, and mixtures thereof, these acids being generally salified with a base, the compounds described in the document EP-A-570230 may also be used.

[0081] When Ri represents a hydrogen atom, and R2 represents a hydroxyl group, the derivative of the above formula (I) is a salicylic acid ester. It includes preferably esters of fatty alcohols such as esters of dodecyl, hexadecyl, stearyl, cetyl, myristyl, linoleyl, octyl, oleyl and tridecyl alcohols, or also esters of butyl, propyl and ethyl alcohols or alternatively the esters of polyols such as the esters of propylene glycol, butylene glycol, ethylene glycol or glycerol, or mixtures of these esters. This may include in particular cetyl salicylate, dodecyl salicylate and tridecyl salicylate.

[0082] As the (b) second compound, salicylic acid is preferable.

[0083] The amount of the (b) second compound(s) in the composition according to the present invention may be 0.01% by weight or more, preferably 0.05% by weight or more, and more preferably 0.1% by weight or more, relative to the total weight of the composition.

[0084] On the other hand, the amount of the (b) second compound(s) in the composition according to the present invention may be 10% by weight or less, preferably 5% by weight or less, and more preferably 1% by weight or less, relative to the total weight of the composition.

[0085] The amount of the (b) second compound(s) in the composition according to the present invention may be from 0.01% to 10% by weight, preferably from 0.05% to 5% by weight, and more preferably from 0.1 % to 1 % by weight, relative to the total weight of the composition.

[0086] (Peptide)

[0087] The composition according to the present invention comprises (c) at least one peptide. If two or more peptides are used, they may be the same or different.

[0088] The term “peptide” here means a chain of amino acid monomers linked by amide bonds. In some embodiments, a peptide includes from 2 amino acid residues to 50 amino acids residues (e.g., from 2 to 20 amino acid residues, from 2 to 10 amino acid residues, or from 5 to 10 amino acid residues).

[0089] It is preferable that the (c) peptide be selected from oligopeptides having from about 2 to 20, preferably from about 4 to 10, or most preferably 5 to 6 amino acids.

[0090] Examples of the (c) peptide include, but are not limited to dipeptides, tripeptides, tetrapeprides, pentapeptides, hexapeptides, and heptapeptides.

[0091] The (c) peptide may be substituted with acyl groups such as acetyl, palmitoyl, and the like. Suitable acyl groups include acetyl, palmitoyl, or myristoyl.

[0092] It is preferable that the (c) peptide have anti-wrinkle activity for skin. The anti-wrinkle activity may be based on the relaxation of shrinkage of muscles to make wrinkles on the skin. The relaxation may be caused by blocking acetylchorine at the synapses at between nerves and muscles.

[0093] In one embodiment of the present invention, examples of the (c) peptide may include any one or more selected from acetyl hexapeptides (e.g., acetyl hexapeptide-3, -37, -38, and -51), acetyl tetrapeptides (e.g., acetyl tetrapeptide-2, -3, -5, -7, -8, -9, -11, and -15), and combinations thereof.

[0094] Specific examples of the (c) peptide include hexapeptides 1-60, said range including each whole integer between 1 and 60, and hexapeptides that are acetylated, palmitoylated or myristoylated such as acetyl hexapeptides 1, 2, 3, 5, 7, 8, 9, 11, 15, 19, 20, 22, 24, 30, 31, 37, 38, 39, 40, and 51.

[0095] Particularly preferred is acetyl hexapeptide- 8 which is obtained by the acetylation of hexapeptide- 8, that is a synthetic peptide containing arginine, glutamic acid, glutamine, and methionine.

[0096] Acetyl hexapeptide- 8 has the following amino acid sequence:

[0097] Ac-Glu-Glu-Met-Gln-Arg-Arg-NH2 wherein

[0098] Ac: Acetyl,

[0099] Glu: L-a-glutamyl group,

[0100] Met: L-methionyl group,

[0101] Gin: L-Glutaminyl group, and

[0102] Arg: L- Arginyl group.

[0103] Acetyl hexpeptide-8 can be purchased from Lipotec S.A. under the tradename Argireline®.

[0104] Further Specific examples of the (c) peptide include the compounds represented by the following formula (III): wherein

[0105] - n represents 0, 1 or 2,

[0106] - R1and R4, independently of each other, are selected from the group consisting of H, Ci-Ce alkyl, amidino and tetra-Ci -Cs-alkylamidinium,

[0107] - R2is H or Ci-Ce-alkyl, or R1and R2together with the residue to which they are bound form a 5- to 7-membered, saturated ring;

[0108] - R3is selected from the group consisting of Ci-Ce alkyl, arCi-Ce alkyl, and heteroaryl Ci-Ce alkyl, and

[0109] - R5is H and, when n is 1, also NH2, or R5and R1together with the residue to which they are bound form a 5- to 7-membered, saturated ring, or a cosmetically acceptable salt thereof The term “Ci-Ce alkyl” as used herein refers to unbranched Ci-Ce alkyl or branched C3-C6 alkyl groups such as methyl, ethyl, n-propyl, 1 -methylethyl, n-butyl, 1 -methylpropyl, 2-methylpropyl, 1,1 -dimethylethyl, n-pentyl, 1 -methylbutyl, 2-methylbutyl, 3 -methylbutyl, 2,2-dimethylpropyl, 1- ethylpropyl, n-hexyl, 1,1 -dimethylpropyl, 1,2-dimethylpropyl, 1 -methylpentyl, 2-methylpentyl, 3- methylpentyl, 4-methylpentyl, 1,1 -dimethylbutyl, 1 ,2-dimethylbutyl, 1,3 -dimethylbutyl, 2,2- dimethylbutyl, 2,3-dimethylbutyl, 3, 3 -dimethylbutyl, 1 -ethylbutyl, 2-ethylbutyl, 1,1,2- trimethylpropyl, 1,2,2-trimethylpropyl, 1 -ethyl- 1 -methylpropyl, and l-ethyl-2-methylpropyl groups.

[0110] The term “arCi-Cg alkyl” as used herein refers to a Ci-Ce alkyl-aryl wherein the term ‘aryl’ is e.g. a phenyl, indanyl or naphthyl group. The “arCi-Cg alkyl” may be referred to as “Ci-Cg aralklyl” group. The examples of “arCi-Cg alkyl” or “Ci-Cg aralklyl” group include a benzyl group.

[0111] The term “heteroaryl Ci-Cg alkyl” as used herein refers to a Ci-Cg alkyl-heteroaryl wherein the term “heteroaryl” refers to a 5- or 6-membered aromatic ring containing one or more heteroatoms, viz., N, O or S; these heteroaromatic rings may be fused to other aromatic systems.

[0112] Examples for the 5- to 7-membered, saturated ring, that R1and R2or R1and R5, respectively, may form together with the residue to which they are bound, are pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, azepinyl, oxazolidinyl, thiazolidinyl and 1,2,3,4-tetrahydroquinolinyl.

[0113] It is well understood, that the present invention encompasses the compounds of formula (III) as optically pure isomers such as e.g. as pure enantiomers or stereoisomers as well as mixtures of different isomers such as e.g. as racemates, or mixtures of diastereoisomers.

[0114] It is well understood, that the term “cosmetically acceptable salt” refers to non-toxic acid addition salts, i.e. salts that are physiologically acceptable and may be used in contact with skin, lips, hair or gums without causing any undesirable or deleterious effects. Preferably, the term “or a cosmetically acceptable salt thereof’ refers to compounds of formula (III) in the form of an acid addition salt such as in the form of a chloride, an acetate, a mesylate or a trifluoro acetate salt. Alternatively, the salt may be formed by reaction with an alkali or earth alkaline base resulting in the respective alkali or earth alkaline salt such as in particular the respective lithium, sodium, potassium, magnesium or calcium salts.

[0115] It is preferable that the compounds of the above formula (III) be in the form of their acetates or trifluoroacetates. Such salts are easily prepared by a person skilled in the art.

[0116] It is preferable that R1, R4and R5be H.

[0117] It is preferable that R2be H or a methyl group, and more preferably H.

[0118] It is preferable that R3be an arCi-Cg alkyl group, and more preferably a benzyl group.

[0119] It is preferable that “n” be 0 or 1, and more preferably 1.

[0120] It is preferable that, in the above formula (III), R1, R2, R4and R5be H, R3be a benzyl group, and “n” be 1.

[0121] The compounds of formula (III) can be prepared as e.g. disclosed in US-A-2009 / 0111731. It is particularly preferable that the compound of the above formula (III) be dipeptide having the sequence: H-(beta-Ala)-Pro-Dab-NH-benzyl, in particular as diacetate. This compound is also known as Dipeptide Diaminobutyroyl Benzylamide Diacetate (INCI) [CAS 823202-99-9], and is commercially available as SYN®-AKE from DSM Nutritional products Ltd., which is a solution of from 0.2% to 0.3% by weight of dipeptide diaminobutyroyl benzylamide diacetate.

[0122] It is preferable that the (c) peptide be selected from the group consisting of acetyl hexapeptide-8, dipeptide diaminobutyroyl benzylamide diacetate, and a mixture thereof.

[0123] The amount of the (c) peptide(s) in the composition according to the present invention may be 0.0001% by weight or more, preferably 0.0005% by weight or more, and more preferably 0.001% by weight or more, relative to the total weight of the composition.

[0124] On the other hand, the amount of the (c) peptide(s) in the composition according to the present invention may be 1% by weight or less, preferably 0.5% by weight or less, and more preferably 0.1% by weight or less, relative to the total weight of the composition.

[0125] The amount of the (c) peptide(s) in the composition according to the present invention may be from 0.00001% to 1% by weight, preferably from 0.0005% to 0.5% by weight, and more preferably from 0.001% to 0.1% by weight, relative to the total weight of the composition.

[0126] (Polyol)

[0127] The composition according to the present invention comprises (d) at least one polyol. If two or more polyols are used, they may be the same or different.

[0128] The term “polyol” here means an alcohol having two or more hydroxy groups, and does not encompass a saccharide or a derivative thereof. The derivative of a saccharide includes a sugar alcohol which is obtained by reducing one or more carbonyl groups of a saccharide, as well as a saccharide or a sugar alcohol in which the hydrogen atom or atoms in one or more hydroxy groups thereof has or have been replaced with at least one substituent such as an alkyl group, a hydroxyalkyl group, an alkoxy group, an acyl group or a carbonyl group.

[0129] The (d) polyol used in the present invention is in the form of a liquid at ambient temperature such as 25°C under atmospheric pressure (760 mmHg or 105 Pa).

[0130] The (d) polyol may be a C2-24 polyol, preferably a C2-9 polyol comprising at least 2 hydroxy groups, and preferably a C4-6 polyol comprising 2 to 5 hydroxy groups.

[0131] The (d) polyol may be a natural or synthetic polyol. The (d) polyol may have a linear, branched or cyclic molecular structure.

[0132] The (d) polyol may be selected from glycerins and derivatives thereof, and glycols and derivatives thereof. The (d) polyol may be selected from the group consisting of glycerin, diglycerin, polyglycerin, ethyleneglycol, diethyleneglycol, propyleneglycol, dipropyleneglycol, butyleneglycol, pentyleneglycol, hexyleneglycol, C6-C24 polyethyleneglycol, 1,3-propanediol, 1,4- butanediol, 1,5-pentanediol, and mixtures thereof. The (d) polyol may not be glycerin.

[0133] It is preferable that the (d) polyol be selected from glycols, more preferably selected from the group consisting of propyleneglycol, butyleneglycol, pentyleneglycol, hexyleneglycol and mixtures thereof, and even more preferably selected from butyleneglycol, pentylene glycol and a mixture thereof.

[0134] The amount of the (d) polyol(s) in the composition used in the present invention may be 1% by weight or more, preferably 2% by weight or more (or more than 2% by weight), and more preferably 3% by weight or more, relative to the total weight of the composition.

[0135] On the other hand, the amount of the (d) polyol(s) in the composition used in the present invention may be 20% by weight or less, preferably 15% by weight or less, more preferably 10% by weight or less, and even more preferably 8% by weight or less, relative to the total weight of the composition.

[0136] The amount of the (d) polyol(s) in the composition used in the present invention may range from 1% to 20% by weight, preferably from 2% to 15% by weight, more preferably from 3% to 10% by weight (or more than 3% to 10% by weight), and even more preferably from 3% to 8% by weight, relative to the total weight of the composition.

[0137] (Hydrophilic Thickener)

[0138] The composition according to the present invention may comprise (e) at least one hydrophilic thickener. If two or more hydrophilic thickeners are used, they may be the same or different.

[0139] The (e) hydrophilic thickener can thicken the composition according to the present invention, if the composition comprises water.

[0140] Hydrophilic thickeners that may be mentioned include carboxyvinyl polymers such as the Carbopol products (carbomers) and the Pemulen products (acrylate / C10-C30-alkyl acrylate copolymer); polyacrylamides, for instance those sold under the names Sepigel 305 (CTFAname: polyacrylamide / C13-C14 isoparaffin / Laureth 7) sold by the company SEPPIC; acryloyldimethyl taurate copolymers, for instance, Simulgel FL (CTFA name: hydroxy ethylacrylate / sodium acryloyldimethyl taurate copolymer / polysorbate 60), Simulgel 800 (CTFAname: sodium polyacryloyldimethyl taurate / polysorbate 80 / sorbitan oleate) or Simulgel 600 (CTFAname: acrylamide / sodium acryloyldimethyl taurate copolymer / isohexadecane / polysorbate 80) sold by the company SEPPIC; 2-acrylamido-2 -methylpropanesulfonic acid polymers and copolymers, optionally neutralized, for instance poly(2-acrylamido-2 -methylpropanesulfonic acid) sold by the company Clariant under the trade name Hostacerin AMPS (CTFA name: ammonium polyacryloyldimethyl taurate) copolymers of 2-acrylamido-2-methylpropanesulfonic acid and of hydroxyethyl acrylate, for instance Simulgel NS and Sepinov EMT 10 sold by the company SEPPIC; cellulose derivatives such as hydroxyethylcellulose, methylcellulose, hydroxypropylmethylcellulose, carboxymethylcelulose and mixtures thereof.

[0141] It is preferable that the (e) hydrophilic thickener be selected from cellulose derivatives.

[0142] It is more preferable that the (e) hydrophilic thickener be hydroxyethylcellulose.

[0143] The amount of the (e) hydrophilic thickener (s) in the composition according to the present invention may be 0.001% by weight or more, preferably 0.01% by weight or more, and more preferably 0.1% by weight or more, relative to the total weight of the composition.

[0144] On the other hand, the amount of the (e) hydrophilic thickener(s) in the composition according to the present invention may be 5% by weight or less, preferably 3% by weight or less, and more preferably 1% by weight or less, relative to the total weight of the composition.

[0145] The amount of the (e) hydrophilic thickener(s) in the composition according to the present invention may be from 0.001% to 5% by weight, preferably from 0.01% to 3% by weight, and more preferably from 0.1% to 1% by weight, relative to the total weight of the composition.

[0146] (Additional Ingredient)

[0147] The composition according to the present invention may comprise (f) at least one additional ingredient selected from water; a-hydroxy acids and salts thereof, which is different from the (a) first compound; pH adjusting agent; and mixtures thereof. If two or more additional ingredients are used, they may be the same or different.

[0148] Water:

[0149] The composition according to the present invention may comprise water.

[0150] The amount of the water in the composition according to the present invention may be 50% by weight or more, preferably 60% by weight or more, and more preferably 70% by weight or more, relative to the total weight of the composition.

[0151] On the other hand, the amount of the water in the composition according to the present invention may be 95% by weight or less, preferably 90% by weight or less, and more preferably 85% by weight or less, relative to the total weight of the composition.

[0152] The amount of the water in the composition according to the present invention may be from 50% to 95% by weight, preferably from 60% to 90% by weight, and more preferably from 70% to 85% by weight, relative to the total weight of the composition.

[0153] Alpha-Hydroxy Acid (AHA):

[0154] The composition according to the present invention may comprise at least one a-hydroxy acid.

[0155] If two or more a-hydroxy acids are used, they may be the same or different.

[0156] The term “a-hydroxy acid”, or “AHA”, here means a carboxylic acid which has at least one carboxyl group and at least one hydroxyl group separated by one carbon atom. Thus, in other words, AHA is a carboxylic acid which has at least one hydroxyl group on the adjacent (alpha) carbon atom.

[0157] The a-hydroxy acid may be selected from, for example glycolic acid, lactic acid, malic acid, citric acid, mandelic acid, and mixtures thereof, preferably from glycolic acid, citric acid, and a mixture thereof, more preferably from glycolic acid.

[0158] The amount of a-hydroxy acid(s) in the composition according to the present invention may be 0.001% by weight or more, preferably 0.01% by weight or more, and more preferably 0.1% by weight or more, relative to the total weight of the composition.

[0159] On the other hand, the amount of the a-hydroxy acid(s) in the composition according to the present invention may be 5% by weight or less, preferably 3% by weight or less, and more preferably 1% by weight or less, relative to the total weight of the composition.

[0160] The amount of the a-hydroxy acid(s) in the composition according to the present invention may be from 0.001% to 5% by weight, preferably from 0.01% to 3% by weight, and more preferably from 0.1 % to 1 % by weight, relative to the total weight of the composition.

[0161] In some embodiments, it may be preferable in terms of reducing possible skin irritation that the composition according to the present invention include no a-hydroxy acid. pH Adjusting Agent:

[0162] The composition according to the present invention may comprise at least one pH adjusting agent. If two or more pH adjusting agents are used, they may be the same or different.

[0163] The pH adjusting agent can control the pH of the composition according to the present invention.

[0164] The pH of the composition according to the present invention may be less than 7, preferably 6 or less, and more preferably 5 or less. The pH of the composition according to the present invention may be 3.0 or more, preferably 3.5 or more, and more preferably 4.0 or more. Thus, the pH of the composition according to the present invention may be from 3.0 to less than 7, preferably from 3.5 to 6, and more preferably from 4.0 to 5.

[0165] As the pH adjusting agent, at least one acidifying agent and / or at least one basifying agent (alkaline agent) may be used.

[0166] The acidifying agents can be, for example, inorganic or organic acids, for instance hydrochloric acid, phosphoric acid, sulfonic acid, and carboxylic acids such as lactic acid.

[0167] The basifying agent or alkaline agent can be, for example, any inorganic or organic basic agents which are commonly used in cosmetic products such as ammonia; alkanolamines such as mono-, di- and tri-ethanolamine, isopropanolamine; metal hydroxide such as alkaline metal hydroxide (e.g., sodium and potassium hydroxides); urea, guanidine and their derivatives; and diamines such as those described in the structure below:

[0168] R1 R3 zN-R-N R2 R4 wherein

[0169] R denotes an alkylene such as propylene optionally substituted by a hydroxyl or a C1-C4 alkyl radical, and Ri, R2, R3, and R4 independently denote a hydrogen atom, an alkyl radical, or a C1-C4 hydroxyalkyl radical, which may be exemplified by 1,3-propanediamine, and derivatives thereof. Alkaline metal hydroxide such as potassium hydroxide is preferable.

[0170] The amount of the pH adjusting agent(s) in the composition according to the present invention may be 0.001% by weight or more, preferably 0.01% by weight or more, and more preferably 0.1% by weight or more, relative to the total weight of the composition.

[0171] On the other hand, the amount of the pH adjusting agent(s) in the composition according to the present invention may be 15% by weight or less, preferably 10% by weight or less, and more preferably 5% by weight or less, relative to the total weight of the composition.

[0172] The amount of the pH adjusting agent(s) in the composition according to the present invention may be from 0.001% to 15% by weight, preferably from 0.01% to 10% by weight, and more preferably from 0.1% to 5% by weight, relative to the total weight of the composition.

[0173] (Other Ingredients)

[0174] The composition according to the present invention may also include various adjuvants conventionally used in cosmetic compositions, such as anionic, cationic, nonionic, and amphoteric or zwitterionic polymers; anionic, cationic, nonionic, and amphoteric surfactants, antioxidants, coloring agents, chelating agents, sequestering agents, fragrances, dispersing agents, conditioning agents, film-forming agents, preservatives, co-preservatives, and mixtures thereof, except for the ingredients as explained above.

[0175] The amount of the adjuvant(s) in the composition according to the present invention may be 0.01 % by weight or more, preferably 0.1% by weight or more, and more preferably 1% by weight or more, relative to the total weight of the composition.

[0176] On the other hand, the amount of the adjuvant(s) in the composition according to the present invention may be 15% by weight or less, preferably 10% by weight or less, and more preferably 5% by weight or less, relative to the total weight of the composition.

[0177] Thus, the amount of the adjuvant(s) in the composition according to the present invention may range from 0.01% to 15% by weight, preferably from 0.1% to 10% by weight, and more preferably from 1% to 5% by weight, relative to the total weight of the composition.

[0178] (Embodiments)

[0179] According to a preferred embodiment, the composition according to the present invention comprises, relative to the total weight of the composition: from 0.01% to 20% by weight of (a) at least one polyhydroxy acid; from 0.01% to 10% by weight of (b) at least one P-hydroxy acid; from 0.0001% to 1% by weight of (c) at least one peptide; and from 1% to 20% by weight of (d) polyol.

[0180] According to another preferred embodiment, the composition according to the present invention comprises, relative to the total weight of the composition: from 0.1% to 15% by weight of (a’) gluconolactone; from 0.05% to 5% by weight of (b’) salicylic acid; from 0.0005% to 0.5% by weight of (c’) at least one peptide having anti-wrinkle activity for skin; and from 2% to 15% by weight of (d’) polyol selected from glycols.

[0181] According to another preferred embodiment, the composition according to the present invention comprises, relative to the total weight of the composition: from 1% to 10% by weight of (a’) gluconolactone; from 0.1% to 1% by weight of (b’) salicylic acid; from 0.001% to 0.1% by weight of (c’) at least one peptide selected from the group consisting of acetyl hexapeptide-8, dipeptide diaminobutyroyl benzylamide diacetate, and a mixture thereof; and from 3% to 10% by weight of (d’) polyol selected from the group consisting of butyleneglycol, pentyleneglycol and a mixture thereof.

[0182] According to another preferred embodiment, the composition according to the present invention comprises, relative to the total weight of the composition: from 1% to 10% by weight of (a’) gluconolactone; from 0.1% to 1% by weight of (b’) salicylic acid; from 0.001% to 0.1% by weight of (c’) at least one peptide selected from the group consisting of acetyl hexapeptide-8, dipeptide diaminobutyroyl benzylamide diacetate, and a mixture thereof; and from 3% to 10% by weight of (d’) polyol selected from the group consisting of butyleneglycol, pentyleneglycol and a mixture thereof, provided that the composition comprises no a-hydrox acid.

[0183] [Preparation]

[0184] The composition according to the present invention can be prepared by mixing the essential ingredient(s) as explained above, and optional ingredient(s), if necessary, as explained above.

[0185] The method and means to mix the above essential and optional ingredients are not limited. Any conventional method and means can be used to mix the above essential and optional ingredients to prepare the composition according to the present invention.

[0186] [Form]

[0187] The form of the composition according to the present invention is not limited. Thus, the composition according to the present invention may be in the form of, for example, a solution, a gel or an emulsion. However, it is preferable that the composition according to the present invention not be in the form of an emulsion. It is preferable that the composition according to the present invention be in the form of a liquid such as a solution.

[0188] The composition according to the present invention may be transparent or translucent.

[0189] The transparency may be measured by measuring the turbidity (for example, turbidity can be measured with a 2100Q (marketed by Hach Company) having a round cell (25 mm in diameter and 60 mm height) and a tungsten filament lamp which can emit visible light (between 400 and 800 nm, preferably from 400 to 500 nm). The measurement can be performed on the undiluted composition. The blank may be determined with distilled water.

[0190] The composition according to the present invention may have a turbidity of 50 NTU or less, preferably 40 NTU or less, more preferably 30 NTU or less, more preferably 20 NTU or less, more preferably 10 NTU or less, and even more preferably 5 NTU or less.

[0191] [Process and Use]

[0192] It is preferable that the composition according to the present invention be a cosmetic composition, preferably a skin cosmetic composition, and more preferably a skin care cosmetic composition.

[0193] The skin here encompasses facial skin, neck skin, and scalp. The composition according to the present invention may also be used for mucosae such as lips, and the like. As the composition according to the present invention includes (a) at least one first compound selected from polyhydroxy acids and salts thereof, the composition according to the present invention can be used for skin peeling while providing reduced skin discomfort such as reduced skin irritation. In other words, the composition according to the present invention is useful as a skin peeling composition. The skin peeling here means peeling the superficial surface of the skin, in particular the homy layer of the skin.

[0194] The composition according to the present invention can be used for a non-therapeutic process, such as a cosmetic process, for treating a keratin substance, preferably for treating the skin, and more preferably for peeling the skin, by being applied to the keratin substance.

[0195] Thus, the present invention also relates to a cosmetic process for treating a keratin substance, preferably for treating the skin, and more preferably for peeling the skin, comprising the step of applying the composition according to the present invention to the keratin substance in particular the skin.

[0196] The present invention may also relate to a use of the composition according to the present invention as a cosmetic product or in a cosmetic product such as skin care products. In other words, the composition according to the present invention can be used, as it is, as a cosmetic product.

[0197] Alternatively, the composition according to the present invention can be used as an element of a cosmetic product. For example the composition according to the present invention can be added to or combined with any other elements to form a cosmetic product.

[0198] The care product may be in the form of a solution, a gel, a lotion, and the like.

[0199] Another aspect of the present invention may relate to a use of (d) at least one polyol in a composition comprising:

[0200] (a) at least one first compound selected from polyhydroxy acids and salts thereof;

[0201] (b) at least one second compound selected from p-hydroxy acids and salts thereof; and

[0202] (c) at least one peptide, in order to stabilize the composition.

[0203] In addition, another aspect of the present invention may relate to a use of (d) at least one polyol in a composition comprising:

[0204] (a) at least one first compound selected from polyhydroxy acids and salts thereof;

[0205] (b) at least one second compound selected from p-hydroxy acids and salts thereof; and

[0206] (c) at least one peptide, wherein the amount of the (d) polyol in the composition is from 1% to 20% by weight, preferably from 2% to 15% by weight, and more preferably from 3% to 10% by weight, relative to the total weight of the composition, in order to reduce the stickiness of the composition.

[0207] The above explanations regarding the ingredients (a) to (d), as well as the optional ingredients, for the composition according to the present invention can apply to those for the above use according to the present invention. The explanations regarding the preparation and forms of the composition according to the present invention can also apply to those of the composition described in the above use according to the present invention. Another aspect of the present invention may relate to a process or method for stabilizing a composition comprising:

[0208] (a) at least one first compound selected from polyhydroxy acids and salts thereof;

[0209] (b) at least one second compound selected from p-hydroxy acids and salts thereof; and

[0210] (c) at least one peptide, characterized by adding (d) at least one polyol to the composition.

[0211] In addition, another aspect of the present invention may relate to a process or method for reducing the stickiness of a composition comprising:

[0212] (a) at least one first compound selected from polyhydroxy acids and salts thereof;

[0213] (b) at least one second compound selected from P-hydroxy acids and salts thereof; and

[0214] (c) at least one peptide, characterized by adding (d) at least one polyol to the composition, wherein the amount of the (d) polyol in the composition is from 1% to 20% by weight, preferably from 2% to 15% by weight, and more preferably from 3% to 10% by weight, relative to the total weight of the composition.

[0215] The above explanations regarding the ingredients (a) to (d), as well as the optional ingredients, for the composition according to the present invention can apply to those for the above process or method according to the present invention. The explanations regarding the preparation and forms of the composition according to the present invention can also apply to those of the composition described in the above process or method according to the present invention.

[0216] EXAMPLES

[0217] The present invention will be described in more detail by way of examples which however should not be construed as limiting the scope of the present invention.

[0218] [Examples 1-4 and Comparative Example 1]

[0219] The following compositions according to Examples 1-4 and Comparative Example 1, shown in Table 1 , were prepared by mixing the components shown in Table 1. The numerical values for the amounts of the components shown in Table 1 are all based on “% by weight” as raw material(s) unless indicated otherwise (AM: active material). In Table 1 , the total amount of polyols (butyleneglycol and pentyleneglycol) is shown in the line of “Amount of Polyol”.

[0220] Table 1

[0221] * 1 : ARGIRELINE® AMPLIFIED PEPTIDE SOLUTION (LIPOTEC) *2: SYN®-AKE (DSM NUTRITIONAL PRODUCTS)

[0222] [Evaluations]

[0223] (Stability)

[0224] Each of the compositions according to Examples 1-4 and Comparative Example 1 was filled into a glass bottle and was held at a temperature of 55°C for 1 day, followed by changing the temperature from -20°C to 20°C for 10 days (10 cycles). Each sample was then investigated for the degree of change in aspect (color and homogeneity) and evaluated in accordance with the following criteria:

[0225] Good: No change in aspect was observed

[0226] Poor: Changes in aspect (cloudiness and phase separation) were observed.

[0227] The results are shown in Table 1.

[0228] (Non-Stickiness)

[0229] Seven professional panelists evaluated the “non-sticky feeling” after application of the compositions according to Examples 1-4 and Comparative Example 1. Each panelist took each composition in their hands, then applied it onto their faces to evaluate the non-sticky feeling after application, and scored it from 1 (not sticky) to 5 (very sticky), in which the composition according to Example 2 was used as a standard as a score of 3. Then, the results were averaged. The results are shown in Table 1.

[0230] [Example 5]

[0231] The following composition according to Example 5, shown in Table 2, was prepared by mixing the components shown in Table 2. The numerical values for the amounts of the components shown in Table 2 are all based on “% by weight” as raw material(s) unless indicated otherwise (AM: active material).

[0232] Table 2

[0233] * 1 : ARGIRELINE® AMPLIFIED PEPTIDE SOLUTION (LIPOTEC)

[0234] *2: SYN®-AKE (DSM NUTRITIONAL PRODUCTS) The composition according to Example 5 is stable and can be safely stored even under hot conditions or a long period of time such as from summer to winter.

[0235] Moreover, the composition according to Example 5 can provide an excellent feeling, such as a less sticky feeling, during and / or after application of the composition.

Claims

CLAIMS1. A composition, comprising:(a) at least one first compound selected from polyhydroxy acids and salts thereof;(b) at least one second compound selected from fl-hydroxy acids and salts thereof;(c) at least one peptide; and(d) at least one polyol.

2. The composition according to Claim 1 , wherein the (a) first compound is in the form of a lactone.

3. The composition according to Claim 1 or 2, wherein the (a) first compound is gluconolactone.

4. The composition according to any one of Claims 1 to 3, wherein the amount of the (a) first compound(s) in the composition is from 0.01% to 20% by weight, preferably from 0.1% to 15 % by weight, and more preferably from 1 % to 10% by weight, relative to the total weight of the composition.

5. The composition according to any one of Claims 1 to 4, wherein the (b) second compound is represented by the following formula (I):in which:Ri represents a hydrogen atom, or a saturated, linear, branched or cyclized aliphatic, alkoxy, ester or ketoxy chain, an unsaturated hydrocarbon chain carrying one or more conjugated or unconjugated double bonds, these chains containing from 1 to 22 carbon atoms and being capable of being substituted with at least one substituent chosen from halogen atoms, trifluoromethyl group, hydroxyl group in free form or esterified with an acid having from 1 to 6 carbon atoms and alternatively with a carboxyl functional group, which is free or esterified with a lower alcohol having from 1 to 6 carbon atoms;R2 represents a hydroxyl group or an ester functional group of the following formula (II):where R4 represents a saturated aliphatic group or an alkenyl group having from 1 to 18 carbon atoms;R3 represents hydrogen or a saturated or unsaturated linear or branched hydrocarbonchain having from 2 to 30 carbon atoms, optionally containing one or more substituents.

6. The composition according to any one of Claims 1 to 5, wherein the (b) second compound is salicylic acid.

7. The composition according to any one of Claims 1 to 6, wherein the amount of the (b) second compound(s) in the composition is from 0.01 % to 10% by weight, preferably from 0.05% to 5% by weight, and more preferably from 0.1% to 1% by weight, relative to the total weight of the composition.

8. The composition according to any one of Claims 1 to 7, wherein the (c) peptide is selected from the group consisting of acetyl hexapeptide- 8, dipeptide diaminobutyroyl benzylamide diacetate, and a mixture thereof.

9. The composition according to any one of Claims 1 to 8, wherein the amount of the (c) peptide(s) in the composition is from 0.0001% to 1% by weight, preferably from 0.0005% to 0.5% by weight, and more preferably from 0.001% to 0.1% by weight, relative to the total weight of the composition.

10. The composition according to any one of Claims 1 to 9, wherein the (d) polyol is selected from glycols, preferably selected from the group consisting of propyleneglycol, butyleneglycol, pentyleneglycol, hexyleneglycol and mixtures thereof, and more preferably selected from the group consisting of butyleneglycol, pentyleneglycol and a mixture thereof.

11. The composition according to any one of Claims 1 to 10, wherein the amount of the (d) polyol(s) in the composition is from 1% to 20% by weight, preferably from 2% to 15% by weight, and more preferably from 3% to 10% by weight, relative to the total weight of the composition.

12. The composition according to any one of Claims 1 to 11 , wherein the composition comprises (e) at least one hydrophilic thickener.

13. The composition according to Claim 1 , wherein the amount of the (e) hydrophilic thickener in the composition is from 0.001% to 5% by weight, preferably from 0.01% to 3% by weight, and more preferably from 0.1% to 1% by weight, relative to the total weight of the composition.

14. The composition according to any one of Claims 1 to 13, wherein the composition comprises no a-hydroxy acid.

15. A cosmetic process for treating a keratin substance, preferably for treating the skin, and more preferably for peeling the skin, comprising the step of applying the composition according to any one of Claims 1 to 14 to the keratin substance.

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