CN102846599B - Topical composition - Google Patents

Abstract

The present invention provides a kind of topical composition, contains（a）Selected from least one of the ascorbic acid for being 3 ~ 40 weight % by quinhydrones and its derivative, retinoid and total amount relative to composition and its group that salt is constituted compound with（b）The polyglycerol-modified siloxanes of cross-linking type while capable of inhibiting coloring, use feeling and has good stability although containing (a) ingredient.

Description

Topical composition

Technical field

The present invention relates to steadily this kind of containing quinhydrones or derivatives thereof, retinoid or ascorbic acid or its salt The topical composition of normally unstable ingredient.

Background technology

Known quinhydrones is widely used as pigmented therapeutic agent caused by a variety of causes due to its strong reduction, but It is easy to be aoxidized by light and heat etc. and brown stain occurs.Then, the various methods for making quinhydrones stablize are studied all the time.For example, non-special The method that sharp document 1 teaches the method for addition sodium sulfite and adds sodium sulfite and citric acid.Also, non-patent literature 2 teach the method for the compound ointment bases (mono- ス of プ ラ ス チ ベ) of adding liquid paraffin wax and polyethylene and cooperation Vitamin C Acid and the method being stored at 4 DEG C.

But these methods are unable to fully coloring caused by inhibiting the oxidation of quinhydrones.

Also, taught in patent document 1 containing quinhydrones and 65 weight % or more selected from by ethylene glycol, ethylene glycol In one or more kinds of skin preparations for extenal use in the group that ether, glycerine and diglycerol are constituted cooperation ascorbic acid or its When salt, the coloring of skin preparations for extenal use can inhibit.

Although the skin preparations for extenal use coloring of patent document 1 can be adequately suppressed, due to the addition of these polyalcohols, preparation Viscosity reduce, according to the dosage form of preparation, sagging (liquid ダ レ) phenomenon occurs when use and is difficult with sometimes.Also, in order to Sagging is prevented, if a large amount of thickeners as water soluble polymer of addition, preparation is tacky, or fold occurs in coating Deng use feeling variation.

Patent document 1：Japanese Unexamined Patent Publication 2006-328064

Non-patent literature 1：Mono- Na Le of medical ジ ヤ, Vol.20, N.10,1929-1934,1984

Non-patent literature 2：JJSHP, Vol.24, No.7,8,801-804,1988

Invention content

Problem of the present invention is that providing containing selected from by quinhydrones and its derivative, retinoid and about 3 ~ 40 weights Measure the compound in the ascorbic acid of % and its group of salt composition, while inhibiting coloring, the good topical composition of use feeling.

The present inventor is solves as a result, finding containing selected from by quinhydrones and its spreading out that the above subject is constantly studied In the topical composition of compound in the group that the ascorbic acid and its salt of biology, retinoid and about 3 ~ 40 weight % are constituted Coordinate the polyglycerol-modified siloxanes of cross-linking type, thus while the coloring of composite inhibiting, obtains not tacky good use Sense, so inhibit through when ingredient detach.

It is completed the present invention is based on above-mentioned opinion, topical composition below is provided.

A kind of 1st topical composition of, containing (a) be selected from by quinhydrones and its derivative, retinoid and relative to At least one of the group that the ascorbic acid and its salt that the total amount of composition is 3 ~ 40 weight % are constituted compound and (b) cross-linking type Polyglycerol-modified siloxanes.

Topical compositions of 2nd as described in the 1st, relative to the total amount of composition, containing 0.01 ~ 90 weight % (b) ingredient.

Topical compositions of 3rd as described in the 1st or the 2nd, contains quinhydrones and/or its derivative as (a) ingredient When, relative to the quinhydrones and/or its derivative of 1 parts by weight, contain (b) ingredient of 0.0005 ~ 9000 parts by weight.

Topical compositions of the 3-1 as described in any one in the 1st ~ the 3rd, relative to the total amount of composition, Quinhydrones containing 0.01 ~ 20 weight % and/or its derivative.

Topical compositions of 4th as described in the 1st or the 2nd, when containing retinoid as (a) ingredient, relatively In the retinoid of 1 parts by weight, contain (b) ingredient of 0.002 ~ 900000 parts by weight.

Topical compositions of the 4-1 as described in the 1st, the 2nd or the 4th contains relative to the total amount of composition The retinoid of 0.00001 ~ 5 weight %.

Topical compositions of 5th as described in the 1st or the 2nd, the Vitamin C of 3 ~ 40 weight % is contained as (a) ingredient When acid and/or its salt, relative to the ascorbic acid and/or its salt of 1 parts by weight, contain (b) ingredient of 0.00025 ~ 30 parts by weight.

Topical compositions of the 5-1 as described in the 1st, the 2nd or the 5th contains 3 relative to the total amount of composition The ascorbic acid and/or its salt of ~ 40 weight %.

6th is as described in any one in the 1st ~ 3,3-1, the 4th, 4-1, the 5th and 5-1 Topical composition, further contain cross-linking type organopolysiloxane.

Topical compositions of 7th as described in the 6th contains the friendship of 0.1 ~ 95 weight % relative to the total amount of composition Connection type organopolysiloxane.

Topical compositions of 8th as described in the 6th or the 7th contains relative to (b) ingredient of 1 parts by weight The cross-linking type organopolysiloxane of 0.0001 ~ 900 parts by weight.

Appointing in 8-1 such as the 1st ~ 3,3-1, the 4th, 4-1, the 5th, 5-1 and the 6th ~ 8 Topical composition described in meaning one contains 20 weight % water below relative to the total amount of composition.

A kind of 9th coloring inhibiting method of topical composition of is given birth to being selected from containing (a) by quinhydrones and its derivative, dimension At least one of the group that the ascorbic acid and its salt that plain A classes and total amount relative to composition are 3 ~ 40 weight % are constituted is changed It closes and adds the polyglycerol-modified siloxanes of (b) cross-linking type in the topical composition of object.

Due to being selected from by the ascorbic acid and its salt structure of quinhydrones and its derivative, retinoid and about 3 ~ 40 weight % At group in compound it is unstable, the composition containing these compounds would generally occur through when coloring or discoloration. In the problem, topical composition of the invention is polyglycerol-modified by containing cross-linking type other than above-mentioned unstable compound Siloxanes, to become the composition for being difficult to colour or change colour.

Even if also, the topical composition of the present invention is largely thickened as water soluble polymer without using additional Agent, it may have appropriate viscosity and be not likely to produce sagging.Also, no tacky and fold good use feeling can be obtained.

In turn, topical composition of the invention due to through when the isolated inhibition of ingredient, it is highly stable.

Also, the cold technique when topical composition of the present invention can pass through preparation without heating, uniformly mixes each ingredient, by This can avoid being selected from and is made of quinhydrones and its derivative, the ascorbic acid of retinoid and about 3 ~ 40 weight % and its salt It is compound in group, modified caused by heating or decompose.

Description of the drawings

Fig. 1 is the photo before and after heating to each composition of embodiment 1 ~ 5 and comparative example 1.

Fig. 2 is the photo before and after heating to each composition of embodiment 6,7 and comparative example 1.

Fig. 3 is the photo before and after heating to each composition of embodiment 8 ~ 13 and comparative example 1.

Fig. 4 is the photo before and after heating to each composition of embodiment 14 ~ 17 and comparative example 1.

Specific implementation mode

The detailed description below present invention.

The topical composition of the present invention is to be selected from quinhydrones and its derivative, retinoid and about 3 ~ 40 weights containing (a) Measure the compound and the polyglycerol-modified siloxanes of (b) cross-linking type of at least one of the ascorbic acid of % and its group of salt composition Composition.

Quinhydrones

Quinhydrones it is commercially available enter commercially available product.

The derivative of quinhydrones

For the derivative of quinhydrones, can example quinhydrones and sugar condensation product and to quinhydrones import a carbon atom number be 1 ~ The glucosides such as the alkyl quinhydrones of 4 alkyl and the condensation product of sugar are as preferred hydroquinone derivatives.

The sugar of glucosides can enumerate D-Glucose, D- galactolipins, D-MANNOSE, D-Tag, D-Fructose, L- sorboses, D- The hexoses such as Tagatose and D-Psicose；L-arabinose, D- xyloses, D-ribose, D- xyluloses, D- lyxoses and D- ribulose Equal pentoses；The amino sugar of D- aminoglucoses, D-Gal, sialic acid and muramic acid etc.；And D- glucuronic acids, D- galas Uronic acids such as uronic acid, D-MANNOSE aldehydic acid and L- iduronic acids (acetylation etc.) etc..

And, it is possible to use the pharmaceutical salt of quinhydrones glucosides, it can be cited for example that the alkali metal salts such as sodium salt and sylvite；Calcium The alkaline-earth metals such as salt and magnesium salts；Ammonium salt；The organic amine salts such as triethylamine salt, triethanolamine salt and monoethanolamine salt；And bad ammonia Alkaline amino acid salts such as hydrochlorate and alginate etc..

Quinhydrones glucosides can be derived by the way that glycosidase is added in the solution that quinhydrones is constituted with sugar and brings it about effect. For example, ursin can be by being synthesized in the solution that quinhydrones is constituted with D-Glucose using the enzyme reaction of β-glucosyl enzym.Tool Body, such as can be prepared by the method for Japanese Unexamined Patent Publication 5-176785 bulletins record.

Also, quinhydrones glucosides can obtain as follows.That is, acetylation sugar and hydrogen as obtained from carrying out acetylation to sugar Quinone forms glycosidic bond in the presence of glycosidase, and then is obtained except deacetylate by basic hydrolysis.

Also, quinhydrones glucosides can be extracted from various plant extracts, such as ursin from black bearberry or cowberry.

Hydroquinone derivatives can also be made using being added in food as butylated hydroxy anisole, as antioxidant Ingredient.

The preferred glucosides of hydroquinone derivatives, the glucosides of more preferable hexose, wherein it is preferred that ursin.

Quinhydrones and its derivative can be used alone one kind, or combination is two or more uses.

The topical composition of the present invention contains content when quinhydrones and/or its derivative, excellent relative to the total amount of composition It is selected as about 0.01 weight % or more, even more preferably about 0.1 weight % or more, even more preferably from about 0.5 weight % or more.If In above range, then the effects that can fully obtaining the whitening function that quinhydrones and hydroquinone derivatives have.

Also, the content of the quinhydrones and/or its derivative in composition, relative to the total amount of composition, preferably from about 20 Weight % hereinafter, even more preferably about 10 weight % hereinafter, even more preferably from about 5 weight % or less.If within the above range, Composition through when coloring or discoloration be inhibited, while obtaining sufficient physiological activity, can obtain have at The composition of this advantage.

Retinoid

The retinoid of the present invention includes retinol, retinene, retinoic acid, their dehydrogenation body, their ester and Wei Sheng Plain A originals etc..

Ester can enumerate retinyl acetate, retinyl propionate, retinol butyrate, retinol caprylate, retinol Laurate, retinyl palmitate, retinol stearate, retinol myristinate, retinol oleate, retinol are sub- Numb acid esters, retinene palmitate, retinene acetic acid esters, retinene propionic ester, retinoic acid methyl esters, regards retinol linoleate Yellow acid ethyl ester, retinol retinoic acid ester and tocopherol retinoic acid ester (can be any one isomers in α, β, γ and δ) etc.. Provitamin A can enumerate alpha-carotene, beta carotene, gamma carotene, δ-carrotene, lycopene, zeaxanthin, Beta-cryptoxanthin and echinenone etc..

Wherein, preferably retinol, retinoic acid and their ester (retinyl palmitate, retinyl acetate etc.).

Retinoid can be the vitamin A of the natural goods such as driven object material separation, or chemically synthesized dimension life Plain A.Also, retinoid can also be used in the form of oleovitamin A.Oleovitamin A can be extraction in driven object, essence The natural oil of system, or oleovitamin A made of retinoid is dissolved in vegetable oil etc..Representative as the latter Example can enumerate the oleovitamin A (containing more than 30000 vitamin A units (IU) in per 1g) described in Japanese Pharmacopoeia, preferably sharp With the oleovitamin A for containing 1,000,000 IU, 1,500,000 IU or 1,700,000 IU in every 1g.

Retinoid can be used alone one kind, or combination is two or more uses.

The topical composition of the present invention contains content when retinoid, relative to the total amount of composition, preferably 0.00001 weight % or more, more preferably 0.0001 weight % or more, and then more preferably 0.001 weight % or more.If above-mentioned In range, then it can play collagen possessed by retinoid and generate facilitation, the proliferation function of keratinocyte, angling The physiological actions such as the effects that differentiation of cell inhibits the metabolism brought to promote or antioxidation.

Also, content when containing retinoid, relative to the total amount of composition, preferably 5 weight % hereinafter, more preferably 3 weight % hereinafter, be more preferably 2 weight % or less in turn.If within the above range, obtain sufficient physiological action, It can obtain the composition with cost advantage.

When retinoid is contained in the composition in the form of oleovitamin A, the content and ratio of said vitamin A classes Rate is the weight for the oleovitamin A being dissolved in retinoid in vegetable oil etc..

Ascorbic acid and its salt

Ascorbic acid may be any one in L- bodies, D- bodies and their mixture.Wherein, from whitening function and From the viewpoint of the physiological activity such as generation facilitation of collagen effect is good, preferably L-AA.Ascorbic acid can be bought Commercially available product.

Also, ascorbate can enumerate sodium salt, sylvite, calcium salt, magnesium salts, phosphate and molysite etc..

The topical composition of the present invention is when containing ascorbic acid and/or its salt, relative to the total amount of composition, in composition Ascorbic acid and/or the content of its salt be about 3 weight % or more, at this moment, will produce through when coloring phenomenon.Ascorbic acid And/or the content of its salt, relative to the total amount of composition, preferably from about 4 weight % or more, even more preferably about 5 weight % or more.If Within the above range, then can fully obtain whitening function, wrinkle inhibiting effect and relaxation inhibiting effect etc. ascorbic acid or its The physiological action of salt.

Also, the content of the ascorbic acid and/or its salt in composition is about 40 weight % relative to the total amount of composition Hereinafter, preferably from about 30 weight % or less.If within the above range, obtain sufficient physiological action, can obtain have at The composition of this advantage.

Quinhydrones and its derivative, the ascorbic acid of retinoid and about 3 ~ 40 weight % and its salt can be used alone one Kind, or combination is two or more uses.

For example, the case where as contained quinhydrones and/or its derivative and retinoid, for (i) quinhydrones and/or its derivative Object, (ii) retinoid and (iii) ascorbic acid or its salt, containing (i) (ii) (iii) it is two or more when, total amount Relative to the total amount of composition, preferably from about 0.00001 weight % or more, even more preferably about 0.001 weight % or more, so it is more excellent It is selected as about 0.01 weight % or more.Also, total amount of its total amount relative to composition, preferably from about 65 weight % are hereinafter, more preferably It is about 30 weight % hereinafter, being even more preferably about 25 weight % or less in turn.

The polyglycerol-modified siloxanes of cross-linking type

The polyglycerol-modified siloxanes of cross-linking type is with glyceryl cross-linking type organopolysiloxane polymer.The present invention In, the polyglycerol-modified siloxanes of cross-linking type further includes the total modified silica of alkyl co-modified siloxanes of cross-linking type polyglycereol etc. Alkane.

The polyglycerol-modified siloxanes of cross-linking type can also be in the form of the composition (such as starchiness) containing liquid finish It uses.For example, 0.65mm of the polyglycerol-modified siloxanes of cross-linking type more than dead weight can be made²/ second (25 DEG C) ~ 100.0mm²/ the second The glycerine such as the hydrocarbon ils or tricaprylin of low viscosity silicone, atoleine, saualane or the Permethyl 99A of (25 DEG C) etc. It is swollen in ester oil or ester oil.

Cross-linking type polyglycerol-modified siloxanes can be used alone or appropriately combined two or more use.

The present invention the polyglycerol-modified siloxanes of cross-linking type can use for example be documented in Japanese Patent No. 4187198 or The polyglycerol-modified siloxanes of cross-linking type in each bulletin of person's Japanese Patent No. 4490817.

Specifically, the polyglycerol-modified siloxanes of cross-linking type indicated by the following general formula (1) can be enumerated.

R¹ _aR² _bSiO_(4-a-b)/2 (1)

In formula, R¹It is to replace alkyl to indicate organic selected from alkyl, aryl, aralkyl and the fluorine for being 1 ~ 30 by carbon atom number The identical type of group or different types of organic group, can specifically enumerate methyl, ethyl, propyl, butyl, amyl, oneself The alkyl such as base, heptyl, octyl, nonyl and decyl；The naphthenic base such as cyclopenta and cyclohexyl；The aryl such as phenyl and tolyl；Benzene first The aralkyl such as base and phenethyl；And the fluorine such as trifluoro propyl and 17 fluorine decyls substitution alkyl etc..Also, a is 1.0≤a≤2.5 Number, b be 0.001≤b≤1.5 number.

In formula, R¹It may further be the organic group of the chain alkyl indicated containing the following general formula (2).

-C_mH_2m-O-(C₂H₄O)_c(C₃H₆O)_dR³ (2)

In formula, R³It is 1 valency alkyl or R that carbon atom number is 5 ~ 30⁴The organic group that (CO)-is indicated, R⁴It is carbon atom The alkyl that number is 1 ~ 30, c and d are respectively 0 ~ 50 integer, the integer that m is 0 ~ 15.That is, R¹It is residual for alkoxy, ester group, alkene ether Base or alkenyl esters residue.Wherein, no matter which type of number c and d is, it is poor to be possible to hydrolytic resistance when m is 0, if m be 15 with On, then it is oily smelly too strong, therefore m is preferably 3 ~ 11.

As R¹, as m=0, c=0, d=0, the alkoxy that carbon atom number is 5 ~ 30, such as octadecane epoxide can be enumerated With the higher alkoxies such as stearic oxygroup.Alternatively, the ester group of oleic acid, stearic acid and behenic acid etc. can be enumerated.

When m is 1 or more, c=0, d=0, m is particularly preferably 3,5 or 11, at this point, R¹For allyl ether, pentenyl ether or Person's undecenyl ether residue, although according to R³It is different and different, but such as allyl stearyl ether residue, allyl two can be enumerated Lauryl ether residue or endecatylene base oil ether residue etc..When c or d is non-zero, R¹For there is alkane by polyoxyalkylene The group of oxygroup or ester group.

Particularly preferred these wholes R¹50% or more be methyl, further preferred 70% or more be methyl, or 100% methyl.

R²The hydrophilic radical indicated for the following general formula (3).

-Q-O-X (3)

In formula, Q indicates that the carbon atom number containing ehter bond and ester bond is 3 ~ 20 bivalent hydrocarbon radical, it can be cited for example that- (CH₂)₂-、-(CH₂)₃-、-CH₂CH(CH₃)CH₂-、-(CH₂)₄-、-(CH₂)₅-、-(CH₂)₆-、-(CH₂)₇-、-(CH₂)₈-、- (CH₂)₂-CH(CH₂CH₂CH₃)-、-CH₂-CH(CH₂CH₃)-、-(CH₂)₃-O-(CH₂)₂-、-(CH₂)₃-O-(CH₂)₂-O- (CH₂)₂-、-(CH₂)₃-O-CH₂CH(CH₃)-and-CH₂CH(CH₃)-COO(CH₂)₂Etc..

X is glycerine.

As R²Following residues can be enumerated.

(in formula, Q is identical as the Q in formula (3), the integer that the s in formula is 1 ~ 20.Also, a part for hydroxyl can be by alcoxyl Base or ester group substitution.)

(in formula, Q is identical as the Q in formula (3), the integer that the t in formula is 1 ~ 20.Also, a part for hydroxyl can be by alcoxyl Base or ester group substitution.)

(in formula, Q is identical as the Q in formula (3).Also, a part for hydroxyl can be replaced by alkoxy or ester group.)

Also, it as the concrete example of the polyglycerol-modified siloxanes of workable cross-linking type in the present invention, can enumerate following logical Formula (a1) and/or the organic hydride polysiloxanes of the following general formula (a2) expression, the following general formula (b1) indicate sweet with alkenyl Organopolysiloxane with alkenyl that oily derivative, general formula (b2) indicate and selected from the following general formula (b3) expression with alkenyl Hydrocarbon at least one compound among, the ingredient that is indicated using the following general formula (a1) or (b1) carried out addition polymerization as neccessary composition and obtained The organopolysiloxane polymer arrived.

(a1):R¹ _aR² _bH_cSiO_(4-a-b-c)/2

(a2):R¹ _dH_eSiO_(4-d-e)/2

(b1):

(b2):R¹ _pR³ _qSiO_(4-p-q)/2

(b3):R³(CH₂)_rR³

Above-mentioned (a1) ingredient is by average composition formula R¹ _aR² _bH_cSiO_(4-a-b-c)/2It indicates.In formula, R¹It is substitution or non-substituted Carbon atom number be 1 ~ 30 and without alkenyl 1 valency alkyl.They are alkyl, aryl, aralkyl or halohydrocarbyl, as tool Body example can enumerate methyl, ethyl, propyl, butyl, amyl, hexyl, heptyl, octyl, nonyl, decyl, stearyl and 22 The alkyl such as alkyl；Cyclopenta and cyclohexyl etc. are saturated alicyclic type hydrocarbon；The aryl such as phenyl and tolyl；The aralkyl such as phenethyl； And the fluorine such as trifluoro propyl, nine fluorine hexyls and 17 fluorine decyls substitution alkyl etc..

R²1 valence groups indicated for following formula, with glycerol derivatives.

C in formula_XH_2XIn, X be 2 ~ 20 bivalent hydrocarbon radical, s be 1 ~ 20 integer, preferably 1 ~ 10.C_XH_2XThe concrete example of base, - (CH can be enumerated₂)₂-、-(CH₂)₃-、-CH₂CH(CH₃)CH₂-、-(CH₂)₄-、-(CH₂)₅-、-(CH₂)₆-、-(CH₂)₇-、- (CH₂)₈-、-(CH₂)₂-CH(CH₂CH₂CH₃)-and-CH₂-CH(CH₂CH₃)-etc..

If describing the preparation method of above-mentioned glycerol derivatives, such as by keeping glycerine and allyl glycidyl ether anti- It answers, the glycerol derivatives with 1 mole of allyl can be synthesized, polyglycerol derivatives then can be by making allylin Several moles of glycidol reactions are made to obtain for starting material.R is conventionally made by addition reaction²It imported into the allyl Base polyglycereol.

(a1) ingredient is by general formula R¹ _aR² _bH_cSiO_(4-a-b-c)/2It indicates.Wherein, a is 1 ~ 2.3, and preferably 1.2 ~ 2.1, b is 0.001 ~ 1, preferably 0.005 ~ 0.5, c are 0.001 ~ 1, preferably 0.005 ~ 0.5.When a is less than 1, since the degree of cross linking became Height, cannot contain with dead weight identical weight more than fluid oil, be more than 2.3 when, since the degree of cross linking becomes too low, it is difficult to form three Tie up cross-linked structure.

Since the degree of cross linking is lower when c is less than 0.001, it is difficult to three-dimensional crosslinking structure is formed, since the degree of cross linking becomes when more than 1 It is excessively high, it cannot contain and fluid oil more than dead weight identical weight.Also, a+b+c is 1.5 ~ 2.6, preferably 1.8 ~ 2.2.From It is smoothed out from the viewpoint of polymerisation, which is preferably straight-chain or predominantly straight-chain, but can also For there is R as its Component units¹SiO_3/2Or SiO₂Deng, straight-chain, branch-like or ring-type containing element branches unit Any one.

(a1) concrete example of ingredient can enumerate the compound indicated by following formula.

(in formula, R¹、R²Indicate above-mentioned group, x, y are 0 or 1 and x+y=1,0≤l≤100,0≤m≤100,0≤n≤ 100、0≤w≤100、0≤l+m+n≤200。)

(in formula, R¹、R²Indicate that above-mentioned group, x, y are 0 or 1 and x+y=1,0≤l '≤100,0≤m '≤100,0≤n ' ≤ 100, the bivalent hydrocarbon radical that+n '≤200 0≤l '+m ', Q expression oxygen atoms or carbon atom number are 2 ~ 20.)

(in formula, R¹、R²Indicate above-mentioned group, 0≤g≤8,0≤h≤8,0≤i≤8,3≤g+h+i≤8.)

(a2) ingredient is by general formula R¹ _dH_eSiO_(4-d-e)/2It indicates.D is 1 ~ 2.3, and preferably 1.2 ~ 2.1, e is 0.001 ~ 1, excellent It is selected as 0.005 ~ 0.5.Become excessively high due to the degree of cross linking when d is less than 1, cannot contain with fluid oil more than dead weight identical weight, When more than 2.3, since the degree of cross linking becomes too low, it is difficult to form three-dimensional crosslinking structure.Since the degree of cross linking becomes when e is less than 0.001 It is too low, it is difficult to form three-dimensional crosslinking structure, since the degree of cross linking becomes excessively high when more than 1, cannot contain with dead weight identical weight with On fluid oil.From the viewpoint of being smoothed out polymerisation, which is preferably straight-chain or is mainly straight Chain, but may be that there is R as its Component units¹SiO_3/2Or SiO₂Deng, straight-chain containing element branches unit, point Branch shape or it is cricoid any one.

(a2) concrete example of ingredient can enumerate the compound indicated by following formula.

(in formula, R¹Indicate above-mentioned group, the case where x, l, n, w are with above-mentioned (a1) ingredient is identical.)

(in formula, R¹Indicate above-mentioned group, the case where x, l ', n ' are with above-mentioned (a1) ingredient is identical.)

(in formula, R¹Indicate above-mentioned group, g, i and identical, 3≤g+i≤8 the case where above-mentioned (a1) ingredient.)

(b1) ingredient is glycerol derivatives indicated by following formula, with alkenyl.

R³It is the alkenyl that carbon atom number is 2 ~ 20, is unsaturated aliphatic hydrocarbon or ester ring type unsaturated hydrocarbons.R³It is preferably logical Formula C_YH_2Y-1The alkyl with alkenyl indicated, the integer that Y is 2 ~ 20.As-C_YH_2Y-1Base can enumerate vinyl, 1- third Alkenyl, allyl, isopropenyl, 1- cyclobutenyls, 2- cyclobutenyls, 3- cyclobutenyls, 2- methacrylics, 2- pentenyls, 4- amylenes Base, 5- hexenyls and 10- undecenyls.Among them, preferably Y=2 or 3 vinyl and allyl.G be glycerine or Polyglycereol, the alkenyl (R in glycerol derivatives³) it is preferably in derivative end.Also, f be 2 ~ 10 integer, preferably 2 or Person 3.Also, the integer that s is 1 ~ 20.Such (b1) ingredient passes through the glycerine either hydroxyl of polyglycereol and alkenyl alcohol or alkenyl The etherification reaction of glycidol ether synthesizes.

(b2) ingredient is by general formula R¹ _pR³ _qSiO_(4-p-q)/2It indicates.R³For in the alkenyl described in (b1) ingredient.P is 1 ~ 2.3, Preferably 1.2 ~ 2.1, q is 0.001 ~ 1, preferably 0.005 ~ 0.5.Since the degree of cross linking becomes excessively high when p is less than 1, cannot contain With dead weight identical weight more than fluid oil, be more than 2.3 when, since the degree of cross linking becomes too low, it is difficult to form three-dimensional crosslinking structure. Since the degree of cross linking becomes too low when q is less than 0.001, it is difficult to three-dimensional crosslinking structure is formed, since the degree of cross linking became when more than 1 Height cannot contain and fluid oil more than dead weight identical weight.From the viewpoint of being smoothed out polymerisation, organic poly- silicon Oxygen alkane is preferably straight-chain or predominantly straight-chain, but may be to have R as its Component units¹SiO_3/2Or SiO₂Deng, Straight-chain, branch-like containing element branches unit or it is cricoid any one.

(b2) concrete example of ingredient can enumerate the compound of following formula expression.

(in formula, R¹、R³Indicate above-mentioned group.Z is 0 or 1,0≤k≤100,0≤l+k≤200.)

(in formula, R¹、R³Indicate above-mentioned group.Z is 0 or 1,0≤k '≤100 ,+k '≤200 0≤l '.)

(in formula, R¹、R³Indicate above-mentioned group.1≤j≤8、3≤g+j≤8.)

(b3) ingredient is by general formula R³(CH₂)_rR³It indicates.R³For in the alkenyl described in (b1) ingredient.The integer that r is 0 ~ 20. (b3) ingredient can enumerate diene such as butadiene, pentadiene, hexadiene, heptadiene, octadiene and nonadiene etc., particularly preferably Hexadiene.

Workable organopolysiloxane polymer includes any one in (a1) and (b1) ~ (b3) or more in the present invention Combination, combination more than any one in (a1+a2) and (b1) ~ (b3), the combination of (a2) and (b1), (a2) and (b1) with (b2) combination of combination or (a2) and (b1) and (b2) and (b3).

It is poly- that the concrete example of the polyglycerol-modified siloxanes of cross-linking type can enumerate (dimethyl silicone polymer/polyglycereol -3) crosslinking Close object etc..It is commercially available by chemical industry society as the commodity containing (dimethyl silicone polymer/polyglycereol -3) cross-linked polymer KSG-710 etc..

Also, (the poly- diformazan of lauryl as the concrete example of the alkyl co-modified siloxanes of cross-linking type polyglycereol, can be enumerated Radical siloxane/polyglycereol -3) cross-linked polymer etc..As poly- containing (lauryl dimethicone/polyglycereol -3) crosslinking The commodity for closing object, by chemical industry society commercially available KSG-810, KSG-820, KSG-830 and KSG-840 etc..Also, may be used also Enumerate (- 3/ lauryl polydimethylsiloxanes base ethyl dimethyl silicone polymer of polyglycereol) cross-linked polymer etc..As containing (poly- - 3/ lauryl polydimethylsiloxanes base ethyl dimethyl silicone polymer of glycerine) cross-linked polymer commodity, by SHIN-ETSU HANTOTAI's chemical industry Society commercially available KSG-820Z and KSG-850Z etc..

The weight average molecular weight of the polyglycerol-modified siloxanes of cross-linking type used in the present invention is preferably from about 500 ~ 200,000, Even more preferably about 1,000 ~ 100,000.

Relative to the total amount of composition, the content of the polyglycerol-modified siloxanes of cross-linking type is preferably from about 0.01 weight % or more, Even more preferably about 0.5 weight % or more, even more preferably from about 1 weight % or more.If within the above range, can fully inhibit The coloring of composition.

Also, relative to the total amount of composition, the content of the polyglycerol-modified siloxanes of cross-linking type be preferably from about 90 weight % with Under, even more preferably about 50 weight % are hereinafter, even more preferably from about 20 weight % or less.If within the above range, being filled Point coloring inhibition, and inhibit through when ingredient detach, the good composition of use feeling can be obtained.

When the topical composition of the present invention contains quinhydrones and/or its derivative, relative to quinhydrones and/or its 1 weight of derivative Part is measured, the content of the polyglycerol-modified siloxanes of cross-linking type is preferably from about 0.0005 parts by weight or more, even more preferably about 0.01 weight Part or more, it is more than even more preferably from about 0.5 parts by weight.If within the above range, can fully composite inhibiting coloring.

Also, it is preferred relative to quinhydrones and/or its 1 parts by weight of derivative, the content of the polyglycerol-modified siloxanes of cross-linking type It is about 9000 parts by weight hereinafter, even more preferably about 900 parts by weight are hereinafter, below even more preferably from about 10 parts by weight.If In above range, then obtain adequately colouring inhibition, and inhibit through when ingredient detach, good group of use feeling can be obtained Close object.

When the topical composition of the present invention contains retinoid, relative to 1 parts by weight of retinoid, cross-linking type polyglycereol The content of modified siloxane is preferably from about 0.002 parts by weight or more, more than even more preferably about 0.01 parts by weight, even more preferably It is about 1 parts by weight or more.If within the above range, can fully composite inhibiting coloring.

Also, relative to 1 parts by weight of retinoid, the content of the polyglycerol-modified siloxanes of cross-linking type is preferably from about 900000 parts by weight hereinafter, even more preferably about 10000 parts by weight hereinafter, below even more preferably from about 1000 parts by weight.If Within the above range, then obtain adequately colouring inhibition, and inhibit through when ingredient detach, it is good use feeling to be obtained Composition.

When the topical composition of the present invention contains ascorbic acid and/or its salt, relative to ascorbic acid and/or its 1 weight of salt Part is measured, the content of the polyglycerol-modified siloxanes of cross-linking type is preferably from about 0.00025 parts by weight or more, even more preferably about 0.05 weight Part or more, it is more than even more preferably from about 0.1 parts by weight.If within the above range, can fully composite inhibiting coloring.

Also, it is preferred relative to ascorbic acid and/or its 1 parts by weight of salt, the content of the polyglycerol-modified siloxanes of cross-linking type It is about 30 parts by weight hereinafter, even more preferably about 20 parts by weight are hereinafter, below even more preferably from about 5 parts by weight.If above-mentioned In range, then obtain adequately colouring inhibition, and inhibit through when ingredient detach, the good combination of use feeling can be obtained Object.

Cross-linking type organopolysiloxane

The topical composition of the present invention can further contain cross-linking type organopolysiloxane and (remove the polyglycerol-modified silicon of cross-linking type Except oxygen alkane), thus, it is possible to further enhance coloring to inhibit, and the better composition of use feeling can be become.Cross-linking type is organic poly- Siloxanes can be the cross-linking type organopolysiloxane of modification (in addition to the polyglycerol-modified siloxanes of cross-linking type), or non- Modified cross-linking type organopolysiloxane, but preferably non-modified cross-linking type organopolysiloxane.

The substance that cross-linking type organopolysiloxane preferably obtains as follows.That is, having more than two ethylene to react in molecule The crosslinking agent at position act on on the hydrogen atom of the silicon atom Direct Bonding of organopolysiloxane, to forming cross-linked structure and Obtained cross-linking type organopolysiloxane.There is the substance of more than two ethylene reactive sites can enumerate in molecule to have in molecule There are two polyoxyalkylene, α and the ω-in the organopolysiloxane of the above vinyl, molecule with more than two allyls Alkenyl diene etc..

In turn, which also can in the molecule contain selected from by polyoxyalkylene part, alkyl Partly, at least one of group that alkenyl part, aryl moiety and fluoroalkyl moiety are constituted partly is modified.

Also, cross-linking type organopolysiloxane is preferably with respect to 0.65 ~ 10.0mm²The low viscosity silicone of/s, containing certainly Weight more than low viscosity silicone and be swollen.

The concrete example of cross-linking type organopolysiloxane can enumerate Dimethicone Crosspolymer (9040Silicone Elastomer Blend、9045 Silicone Elastomer Blend、9041 Silicone Elastomer Blend、 9546 Silicone Elastomer Blend、9027 Silicone Elastomer Blend、EL-8040ID Silicone Organic Blend；The Shang one ニ Application グ societies systems of Wei East レ ダ ウ Us of Yi), (dimethyl silicone polymer/vinyl Dimethyl silicone polymer) cross-linked polymer (KSG-15, KSG-16, KSG-1610；It is chemical industry society system above), Silicone Elastomer Blend、E-506S、S-508、BY29-129、PF-2001；Shang one ニ of Wei East レ ダ ウ Us of Yi Application グ societies system), (dimethyl silicone polymer/phenyl vinyl dimethyl silicone polymer) cross-linked polymer (KSG-18A；SHIN-ETSU HANTOTAI Learn industrial society's system), (vinyldimethicone/lauryl dimethicone) cross-linked polymer (KSG-41, KSG- 42、KSG-43、KSG-44；Above be chemical industry society system), (dimethyl silicone polymer PEG-10/15)) cross-linked polymeric Object (KSG-210, KSG-240；Above be chemical industry society system), (PEG-15/ lauryl dimethicones) crosslinking Polymer (KSG-310, KSG-320, KSG-330, KSG-340；Above be chemical industry society system), (PEG-15/ lauryls Polydimethylsiloxanes base ethyl dimethyl silicone polymer) cross-linked polymer (KSG-320Z, KSG-350Z；It is SHIN-ETSU HANTOTAI's chemistry above Industrial society's system) and (lauryl polydimethylsiloxanes base ethyl dimethyl silicone polymer/bi-vinyl dimethyl silicone polymer) friendship Linked polymer (KSG-042Z, KSG-045Z；It is chemical industry society system above) etc..

Relative to the total amount of composition, the content of cross-linking type organopolysiloxane is preferably from about 0.1 weight % or more, more excellent It is selected as about 0.5 weight % or more, even more preferably from about 1 weight % or more.If within the above range, can more effectively inhibit The coloring of composition.

Also, relative to the total amount of composition, the content of cross-linking type organopolysiloxane be preferably from about 95 weight % hereinafter, Even more preferably about 70 weight % are hereinafter, even more preferably from about 60 weight % or less.If within the above range, can obtain tacky Feel repressed use feeling it is good, inhibit through when ingredient separation composition.

Also, relative to polyglycerol-modified 1 parts by weight of siloxanes of cross-linking type, the content of cross-linking type organopolysiloxane is preferred It is about 0.0001 parts by weight or more, more than even more preferably about 0.01 parts by weight, more than even more preferably from about 0.5 parts by weight. If the repressed composition of sticky feeling within the above range, can be obtained.

Also, relative to polyglycerol-modified 1 parts by weight of siloxanes of cross-linking type, the content of the polyglycerol-modified siloxanes of cross-linking type Preferably from about 900 parts by weight hereinafter, even more preferably about 100 parts by weight hereinafter, below even more preferably from about 30 parts by weight.If Within the above range, then can obtain through when ingredient separation be suppressed, the good composition of the repressed use feeling of sticky feeling.

Water

The topical composition of the present invention can contain water, and can be free of has water, but preferably comprises water.Water when containing water Total amount of the content relative to composition, if more than 0 weight %, preferably 0.5 weight % or more, more preferably 1 weight % with On.If within the above range, can inhibit through when ingredient precipitation, become stable composition.

Also, relative to the total amount of composition, the content of water be preferably 20 weight % hereinafter, more preferably 15 weight % with Under, it is even more preferably 10 weight % or less.If within the above range, can obtain adequately colouring inhibition, and pass through When ingredient separation be suppressed, become the good composition of use feeling.

pH

The pH of the topical composition of the present invention is preferably from about 1 ~ 10, even more preferably about 2 ~ 8, even more preferably from about 2 ~ 7 Acidic region.If sufficient effect in the range, can be obtained.

Hardness

The hardness of the topical composition of the present invention is not particularly limited, but preferably from about 1 ~ 200g, even more preferably about 10 ~ 180g, even more preferably from about 30 ~ 140g.If in the range, good use feeling can be obtained without sagging phenomenon.

The hardness of the present invention is to be measured using rheometer (trade name " NRM-2002J ", motionless Industrial Co., Ltd's system) Value.Specifically, substance after preparation being put into plastics 50g tanks is as sample, with above-mentioned rheometer by columned diameter The elasticity of compression of 30mm takes over peak when entering 1cm using the speed of 2cm/min as hardness.

Dosage form

The topical composition of the present invention can will be selected from by quinhydrones and its derivative, retinoid and about 3 ~ 40 weight % Ascorbic acid and its at least one of the group polyglycerol-modified siloxanes of compound, cross-linking type that constitutes of salt and then according to need In the cross-linking type organopolysiloxane wanted, with cosmetics either quasi- drug usually used base or carrier and as needed Additive be mixed together, so as to form the topical composition of cosmetics or quasi- drug.

The form of topical composition is not particularly limited, it can be cited for example that liquid agent, suspending agent, emulsion, creme, ointment Agent, gelling agent, liniment, lotion, aerosol, stylus and Formulation made of making liquid be infiltrated up in non-woven fabrics etc..Wherein, excellent Select emulsion, creme, ointment, gelling agent and lotion, more preferable creme and gelling agent.

Can be w/o type when containing oiliness base and aqueous base as creme, emulsion, or O/W types, but It is preferred that w/o type.

The present invention topical composition specific purposes it can be cited for example that, toner, lotion, gel, creams, beauty Liquid, it is sun-proof apply some make up, the basic cosmetics such as facial mask, facial mask, hand lotion, skin cream and skin cream；And facial cleanser, makeup removing Product, bath foam, shampoo, hair conditioner and conditioning liquid（treatment）Equal washings apply some make up.

Base or carrier

As base or carrier, it can be cited for example that atoleine, saualane, vaseline, gelled hydrocarbon (white oil and poly- Compound ointment bases (mono- ス of プ ラ ス チ ベ) of ethylene etc.), ceresine, α-alkene is through the hydrocarbon such as oligomer and light liquid paraffin；First Based polysiloxane, high polymer methylpolysiloxane, annular siloxane, alkyl modified siloxane, amino modified siloxanes, polyethers change Property siloxanes, that polyglycerol-modified siloxanes, silicone alkyl chain are total to modified polyether modified siloxane, silicone alkyl chain is total Modified polyglycerol-modified siloxanes, polyether-modified branch siloxanes, polyglycerol-modified branch siloxanes, acrylic siloxanes, The silicone oils such as phenyl modified siloxanes and silicone resin；Cetanol, 18 hexadecanols, stearyl alcohol and tadenan are contour Grade alcohol；The cellulose derivatives such as ethyl cellulose, hydroxypropyl cellulose and hydroxypropyl methyl cellulose；Polyvinylpyrrolidone Ketone, carrageenan, poly- vinyl butyrate, polyethylene glycol, twoAlkane, butanediol adipate polyester, isopropyl myristate, Pork and beans Cool acid octyldodecyl, isopropyl palmitate, cetyl base ester, isononyl isononanoate, four (2 ethyl hexanoic acid) seasons The esters such as Doutrate and jojoba oil；The polysaccharides such as dextrin and maltodextrin, the lower alcohols such as ethyl alcohol and isopropanol, ethylene glycol list Methyl ether, ethylene glycol monoethyl ether, ethylene glycol ether, diethylene glycol monomethyl ether, diethylene glycol monoethyl ether, diethylene glycol monopropyl ether, diethylene glycol (DEG) The glycol such as monobutyl ether, dihydroxypropane single-ether, propylene glycol monopropyl ether, dipropylene monoethylether and dipropylene glycol list propyl ether Ether；The polyalcohols such as polyethylene glycol, propylene glycol, 1,3 butylene glycol, glycerine, isoprene, diglycerol and dipropylene glycol and Aqueous base such as water etc..

Quinhydrones and its derivative, retinoid and ascorbic acid and its salt especially become unstable in water, therefore The topical composition of the present invention is adapted as the composition that base or carrier contain water, even if being free from the combination of water Also effect can be obtained in object.

Wherein, preferred polyol, higher alcohol, hydrocarbon, esters and silicone oil, more preferable polyalcohol.In polyalcohol, preferably 1,3-BDO, propylene glycol, isoprene, glycerine, diglycerol, dipropylene glycol and 1,2- pentanediols, more preferable 1, 3- butanediols, propylene glycol, glycerine, diglycerol and 1,2- pentanediols.The composition preferred example of the present invention, can enumerate and contain There is polyalcohol as the creme of base, gelling agent and emulsion.

Either carrier can be used alone and one kind or can combine two or more use base.

Additive

In the topical composition of the present invention, within the scope of the effect of the invention, cosmetics, quasi- drug can be added In addible well known additive, for example, antioxidant, surfactant, thickener, preservative agent, pH adjusting agent, stabilization Agent, counter-stimulus, preservative, colorant, fragrance and pearling agent etc..

As antioxidant, it can be cited for example that dibutyl hydroxy toluene, butylated hydroxyanisole (BHA), sorbic acid, sulfurous acid Sodium, ascorbic acid, ascorbic acid derivates, tocopherol, Tocopheryl derivatives, arabo-ascorbic acid and L-cysteine hydrochloride Deng.

As surfactant, it can be cited for example that sorbitan list isostearate, sorbitan Dan Yue Cinnamic acid ester, span 40, sorbitan monostearate, (the 2- ethyl hexyls of sorbitan five Acid) the sorbitan fatty acid esters class such as double glyceride and sorbitan four (2 ethyl hexanoic acid) double glyceride, the third two The methyl glycol fatty acid esters class such as alcohol monostearate, Crodaret 40 (HCO-40), polyethylene glycol hydrogenated castor-oil plant The equal rilanit specials of 50 (HCO-50) of oil, polyoxyethylene hydrogenated castor oil 60 (HCO-60) and Crodaret 80 spread out Biology, polyoxyethylene (20) sorbitan monolaurate (polysorbate20), polyoxyethylene (20) Sorbitan Alcohol monostearate (polysorbate60), polyoxyethylene (20) dehydrated sorbitol mono-fatty acid ester (polysorbate80) and poly- The polyoxyethylene sorbitan fatty acid esters classes such as ethylene oxide (20) sorbitan isostearate, polyoxyethylene list coconut palm Fatty acid oil glyceride, glycerine alkyl ether, alkyl-glucoside, the polyoxyalkylene alkyls such as polyoxyethylene cetyl base ether are stearic The amines such as amine and oleyl amine and polyoxyethylene methyl polysiloxane copolymer, lauryl PEG-9 polydimethylsiloxanes base ethyls Siloxane type surfactants such as dimethyl silicone polymer and PEG-9 polydimethylsiloxanes base ethyl dimethyl silicone polymers etc..

Other than cellulose thickener, when containing thickener, such as guar gum, locust bean gum, carrageenan, Huang can be enumerated Virgin rubber, polyvinyl alcohol, polyvinylpyrrolidone, carboxyl vinyl polymer, acrylic arid methacrylic acid alkyl ester copolymer, Polyethylene glycol, bentonite, alginic acid, macrogol and sodium chondroitin sulfate etc..

As preservative or preservative agent, it can be cited for example that benzoic acid, sodium benzoate, dehydroactic acid, dehydroactic acid sodium, P-Hydroxybenzoic acid isobutyl ester, p-Hydroxybenzoic acid isopropyl ester, butyl p-hydroxybenzoate, ethyl-para-hydroxybenzoate, to hydroxyl Yl benzoic acid propyl ester, benzyl p-hydroxybenzoate, methyl p-hydroxybenzoate, phenoxetol, benzyl alcohol, methaform, sorb Acid and its salt, chlorhexidine gluconate and alkane diol etc..

As pH adjusting agent, it can be cited for example that inorganic acid (hydrochloric acid and sulfuric acid etc.), organic acid (lactic acid, sodium lactate, lemon Acid, sodium citrate, succinic acid and sodium succinate etc.), inorganic base (potassium hydroxide and sodium hydroxide etc.) and organic base (three ethyl alcohol Amine, diisopropanolamine (DIPA) and triisopropanolamine etc.) etc..

As stabilizer, it can be cited for example that Sodium Polyacrylate, dibutyl hydroxy toluene and butylated hydroxy anisole etc..

As counter-stimulus, licorice and sodium alginate etc. can be enumerated.

Additive can be used alone one kind, or can combine two or more use.

Other active ingredients

The topical composition of the present invention can contain other active ingredients in the range of not interfering effect of the present invention.Make For the concrete example of active ingredient, it can be cited for example that moisturizing ingredient, anti-inflammatory component, antimicrobial component, vitamins, peptide or its derivative Object, amino acid or derivatives thereof, cell-activating ingredient, anti-aging ingredient, the ingredient that promotes blood circulation, keratolytic ingredient, U.S. Bai Chengfen and converging grades.

As moisturizing ingredient, it can be cited for example that glycerine, 1,3-BDO, propylene glycol, polyethylene glycol and diglycerol The polyalcohols such as trehalose；Sodium Hyaluronate, hyparinoids from animal organs, sodium chondroitin sulfate, collagen, elastin laminin, keratin, chitin With the high-molecular compounds such as chitosan；The amino acid such as glycine, aspartic acid and arginine；Sodium lactate, urea and pyrrole The natural moisturizing factor such as pyrrolidone carboxylic acid's sodium；The lipids such as ceramide, cholesterine and phosphatide；Chamomile extract, North America gold thread Plant extracts such as prunus mume extract, tea extraction and extractive of perilla etc..

As anti-inflammatory component, it can be cited for example that from plant (such as comfrey) ingredient, allantoin, glycyrrhizic acid or Its derivative, zinc oxide, puridoxine hydrochloride, tocopherol acetate, salicylic acid or derivatives thereof and ε-aminocaproic acid etc..

As antibacterial or sterilization component, it can be cited for example that chlorhexidine, salicylic acid, benzalkonium chloride, rivanol, sulphur, Resorcinol, ethyl alcohol, benzethonium chloride, Adapalene, benzoyl peroxide, clindomycin, cresols, gluconic acid and its derivative Object, povidone iodine, potassium iodide, iodine, isopropyl methyl phenol, triclocarban, triclosan, it is plain No. 101 photosensitive, plain No. 201 photosensitive, P-hydroxybenzoate, phenoxetol, 1,2- pentanediols, salt dialkylaminobenzoic acid diamino glycine, chlorhexidine gluconate and to hydroxyl Base ZINC P-PHENOLSULFONATE etc..

As vitamins, it can be cited for example that dl- alpha-tocopherols, dl- alpha-tocopherol acetates, dl- alpha-tocopherol ambers The vitamin Es class such as amber acid esters and dl- alpha-tocofecol succinic acid calcium；Riboflavin, flavin mononucleotide, flavin adenine dinucleotide The vitamin B2s classes such as acid, Riboflavine Tertrabutyrate, four nicotinate of Riboflavin Tetrabutyrate, riboflavin 5 '-sodium phosphate and riboflavin； Dl- Tocopheryl Nicotinates, niacin benzene methyl, methyl nicotinate, niacin Beta-Butoxy ethyl ester and niacin 1- (4- aminomethyl phenyls) second The niacin class such as ester；The vitamin Ds classes such as hesperidin methyl, vitamin D2 and courage calcium ostelin；The dimensions such as phylloquinone and farnoquinone are given birth to Plain K classes；γ-Hi-Z, dibenzoylthiamine element, dibenzoyl thiamine, thiamine salt hydrochlorate, thiamine cetyl Hydrochloride, thiamine rhodanate, thiamine lauryl hydrochloride, thiamine nitrate, thiamine monophosphate, thiamine rely Propylhomoserin salt, thiamine triphosphate, thiamine phosplate phosphate, thiamine phosplate, thiamine bisphosphate, thiamines The vitamin B1s classes such as plain bisphosphate hydrochloride, thiamine triguaiacyl phosphate and thiamine triguaiacyl phosphate monophosphate；Hydrochloric acid pyrrole is trembled The vitamin B6s classes such as alcohol, acetic acid pyridoxol, pyridoxal hydrochloride, pyridoxime 5'-phosphate and hydrochloric acid pyridoxamine；Cyanocobalamin, hydroxycobalamin With the vitamin B12s class such as desoxyadenossine cobalt amine；The folic acid class such as folic acid and pteroylglutamic acid；The niacin class such as niacin and niacin hydroxyacyl amine； The pantothenic acid such as pantothenic acid, calcium pantothenate, panthenol (panthenol), D- pantetheines, D- pantethines, coacetylase and pantothenyl ethyl ether Class；The biotins class such as biotin and biocytin；And the vitaminoid actions such as carnitine, ferulic acid, alpha-lipoic acid and orotic acid Factor etc..

As peptide or derivatives thereof, it can be cited for example that keratin decomposes peptide, hydrolysis of keratin, collagen, collagen, lacks end Collagen, gelatin, elastin laminin, elastin laminin decompose peptide, decomposition of collagen peptide, hydrolytic collagen, hydroxypropyl ammonium chloride hydrolytic collagen, bullet Property protein breakdown peptide, conchiolin decompose peptide, hydrolysis conchiolin, fibroin and decompose peptide, hydrolysis silk, lauroyl water Solve silk sodium, soybean protein decomposes peptide, hydrolytic soya bean protein, wheat gluten, wheat gluten decompose peptide, hydrolyzed wheat protein, junket Protein breakdown peptide and acylation peptide (palmitoyl oligopeptide, Matrixyl and palmityl tetrapeptide etc.) etc..

As amino acid or derivatives thereof, it can be cited for example that glycine betaine (trimethylglycine), proline, hydroxyl dried meat ammonia Acid, arginine, lysine, serine, glycine, alanine, phenylalanine, Beta-alanine, threonine, glutamic acid, glutamy Amine, asparagine, aspartic acid, cysteine, cystine, methionine, leucine, isoleucine, valine, histidine, ox Sulfonic acid, γ-aminobutyric acid, γ-amino-β-hydroxybutyric acid, carnitine, carnosine and creatine etc..

As cell-activating ingredient, it can be cited for example that the amino acids such as γ-aminobutyric acid and ε-aminocaproic acid；Depending on Huang The vitamins such as alcohol, thiamines, riboflavin, puridoxine hydrochloride and pantothenic acid class；The Alpha-hydroxies acids such as glycolic and lactic acid；Tannin；Class Flavones；Saponin；Allantoin and photosensitive plain No. 301 etc..

As anti-aging ingredient, it can be cited for example that pangamic acid, kinetin, ursolic acid, Turmeric P.E, sphingol derive Object, silicon, silicic acid, N- methyl-L-serines and mevalonolactone etc..

As the action component that promotes blood circulation, it can be cited for example that from plant (such as ginseng, Angelica Keiskei, mountain gold Vehicle, ginkgo, fennel, rabdosia japonica (エ Application メ イ ソ ウ), オ ラ Application ダ カ シ, chamomile, Rome chamomile, carrot, dragon Courage, burdock, rice, hawthorn, mushroom, sharp thorn hawthorn, hackmatack, Rhizoma Chuanxiong, Japanese Swertia patens, thyme, cloves, dried orange peel, Radix Angelicae Sinensis, Peach kernel, orange peel, carrot, garlic, butcher's broom, grape, tree peony, horse chestnut, balm, shaddock, coix seed, rosemary, rose Fruit, dried orange peel, Radix Angelicae Sinensis, orange peel, peach, apricot, walnut or corn) ingredient；And glucityl aurantiamarin etc..

As keratolytic ingredient, it can be cited for example that urea, salicylic acid, glycolic, tartaric acid, phytic acid and sulphur etc..

As whitening composition, it can be cited for example that tocopherol etc..

As astringent component, it can be cited for example that zinc paraphenol sulfonate, zinc oxide, menthol and ethyl alcohol etc..

Other active ingredients can be used alone, or can combine two or more use.

Application method

The application method of the topical composition of the present invention is different according to the state for the skin for using object, age and gender etc. And it is different, however for example can be the following method.

That is, appropriate (for example, about 0.05 ~ 5g) to skin (such as 1 ~ 5 time, preferably 1 ~ 3 time) each coating for several times in 1 day. Also, one day dosage of quinhydrones and/or its derivative for example comes coating composition, vitamin A with about 0.005 ~ 5000mg One day dosage of class for example carrys out coating composition with about 0.00005 ~ 5000mg, the ascorbic acid of about 3 ~ 40 weight % and/or One day dosage of its salt for example carrys out coating composition with about 1 ~ 100000mg.Coating duration be, for example, about 3 ~ 365 days, preferably About 7 ~ 180 days.

Other

The present invention includes a kind of suppressing method, by containing selected from by quinhydrones and its derivative, retinoid z and Addition cross-linking type is poly- in the composition of the compound of at least one of the group that the ascorbic acid and its salt of about 3 ~ 40 weight % is constituted Glycerin modification siloxanes, inhibit tacky either ingredient to detach and inhibit through when composition coloring or discoloration.Each ingredient Type and usage amount, the character of composition etc. are as described in the explanation that the topical composition to the present invention carries out.

[embodiment]

Hereinafter, enumerating embodiment is described in more detail the present invention, but the present invention is not limited to these examples.

(1) preparation of composition

At normal temperatures, A ingredients shown in aftermentioned table 1 ~ 3 are mixed with B component, the mixture and cross-linking type is organic poly- Siloxanes mixes, to prepare topical composition.

(2) accelerated test

Above-mentioned each composition is fitted into the screw socket bottle of glass system, 2 days are stood in 25 DEG C or 60 DEG C of thermostat.

Before and after heating 2 days at 60 DEG C, appearance is visually observed.Also, 20 how old ~ 30 men and women how old are tested Person 2 is applied to wrist or face, and has rated use feeling.

As a result together it is shown in table 1 ~ 3.Also, the photo of the front and back composition of heating is shown in Fig. 1 ~ 4.

[table 1]

(unit:w/w%)

[table 2]

(unit:w/w%)

[table 3]

(unit:w/w%)

The ingredient of commodity in table 1 ~ 3 is shown in following.

KSG-710：The mixture of (dimethyl silicone polymer/polyglycereol -3) cross-linked polymer and dimethyl silicone polymer

KSG-810：The mixture of (lauryl dimethicone/polyglycereol -3) cross-linked polymer and mineral oil

KSG-210：The mixing of (dimethyl silicone polymer/(PEG-10/15)) cross-linked polymer and dimethyl silicone polymer Object

KF-6104：- 3 polydimethylsiloxanes base ethyl dimethyl silicone polymer of polyglycereol

KSG-15：(Dimethicone/Vinyl Dimethicone) cross-linked polymer and cyclopentasiloxane Mixture

KSG-045Z：(lauryl polydimethylsiloxanes base ethyl dimethyl silicone polymer/bi-vinyl polydimethylsiloxanes Alkane) cross-linked polymer and cyclopentasiloxane mixture

KSG-16：(Dimethicone/Vinyl Dimethicone) cross-linked polymer and polydimethylsiloxanes The mixture of alkane

KSG-19：(Dimethicone/Vinyl Dimethicone) cross-linked polymer and polydimethylsiloxanes The mixture of alkane

KSG-016F：(Dimethicone/Vinyl Dimethicone) cross-linked polymer and poly dimethyl silicon The mixture of oxygen alkane

KSG-43：(ethylene dimethyl silicone polymer/lauryl dimethicone) cross-linked polymer and triethyl group oneself The mixture of acid glyceride (ト リ メ チ Le ヘ キ サ ノ イ Application)

By table 1 ~ 3 it is found that the coloring of the composition of the embodiment of the present invention is suppressed, better stability of preparation, and use feeling is good It is good.On the other hand, the group of the comparative example 1 of the polyglycerol-modified siloxanes of cross-linking type is replaced using crosslinked polyether modified siloxane The yellow coloring for closing object is strong.Also, the use of the composition of the comparative example 2 of the polyglycerol-modified siloxanes of straight chain type it is slimy make With sense.Also, similarly, using the group of the polyglycerol-modified siloxanes of straight chain type and the comparative example 3 of cross-linking type organopolysiloxane It closes object and ingredient separation has occurred.

Example of formulations described below.Unit is weight %.

1 creams of example of formulations

2 creams of example of formulations

3 creams of example of formulations

Industrial availability

The topical composition of the present invention contain it is normally unstable selected from by quinhydrones and its derivative, retinoid and Compound in the group that the ascorbic acid and its salt of about 3 ~ 40 weight % is constituted, can inhibit to colour.Also, stablizes and use Sense is good, therefore is useful as cosmetics or quasi- drug.

Claims (6)

1. a kind of topical composition, it is 3~40 weights to be selected from by quinhydrones, retinol and total amount relative to composition containing (a) It measures at least one of the group of ascorbic acid composition of % compound and (b) is selected from by (dimethyl silicone polymer/polyglycereol -3) Cross-linked polymer, (lauryl dimethicone/polyglycereol -3) cross-linked polymer and (the poly- diformazan of -3/ lauryl of polyglycereol Base siloxy ethyl dimethyl silicone polymer) at least one of the group polyglycerol-modified silica of cross-linking type that constitutes of cross-linked polymer Alkane, the content of water be 8 weight % hereinafter,

When containing quinhydrones as (a) ingredient, relative to the quinhydrones of 1 parts by weight, (b) ingredient containing 0.5~900 parts by weight,

When containing retinol as (a) ingredient, relative to the retinol of 1 parts by weight, (b) ingredient containing 1~1000 parts by weight,

When containing the ascorbic acid of 3~40 weight % as (a) ingredient, relative to the ascorbic acid of 1 parts by weight, containing 0.1~ (b) ingredient of 20 parts by weight.

2. topical composition according to claim 1 contains 0.01~90 weight %'s relative to the total amount of composition (b) ingredient.

3. topical composition according to claim 1, when containing quinhydrones as (a) ingredient, the hydrogen relative to 1 parts by weight Quinone, (b) ingredient containing 0.5~10 parts by weight.

4. topical composition according to claim 1, when containing the ascorbic acid of 3~40 weight % as (a) ingredient, phase For the ascorbic acid of 1 parts by weight, (b) ingredient containing 0.1~5 parts by weight.

5. according to the topical composition described in any one in Claims 1 to 4, further contain selected from by (poly dimethyl Siloxanes/vinyldimethicone) cross-linked polymer, (vinyldimethicone/lauryl poly dimethyl silicon Oxygen alkane) cross-linked polymer and (lauryl polydimethylsiloxanes base ethyl dimethyl silicone polymer/bi-vinyl polydimethylsiloxanes Alkane) at least one of the group cross-linking type organopolysiloxane that constitutes of cross-linked polymer,

Relative to the total amount of composition, the cross-linking type organopolysiloxane containing 1~60 weight %,

Relative to (b) ingredient of 1 parts by weight, the cross-linking type organopolysiloxane containing 0.5~30 parts by weight.

6. a kind of coloring inhibiting method of topical composition is selected to containing (a) by quinhydrones, retinol and relative to composition Total amount be 3~40 weight % at least one of the group topical composition of compound that constitutes of ascorbic acid in add (b) Selected from by (dimethyl silicone polymer/polyglycereol -3) cross-linked polymer, (lauryl dimethicone/polyglycereol -3) crosslinking In the group that polymer and (- 3/ lauryl polydimethylsiloxanes base ethyl dimethyl silicone polymer of polyglycereol) cross-linked polymer are constituted At least one polyglycerol-modified siloxanes of cross-linking type with coloring inhibition, the content of the water of the topical composition is 8 Weight % hereinafter,

When containing quinhydrones as (a) ingredient, relative to the quinhydrones of 1 parts by weight, (b) ingredient containing 0.5~900 parts by weight,

When containing retinol as (a) ingredient, relative to the retinol of 1 parts by weight, (b) ingredient containing 1~1000 parts by weight,

When containing the ascorbic acid of 3~40 weight % as (a) ingredient, relative to the ascorbic acid of 1 parts by weight, containing 0.1~ (b) ingredient of 20 parts by weight.