CN106456484A - External preparation - Google Patents

Abstract

Provided is an external preparation containing (A) tranexamic acid or a salt thereof, (B) a saccharide, and (C) a compound represented by formula (I) or a salt thereof. (In formula (I), Ra indicates a C7-19 linear alkyl group or a group represented by NRdRe, Rd and Re each independently indicate a hydrogen atom or optionally substituted alkyl group, Rb and Rc each independently indicate a hydrogen atom, optionally substituted alkyl group, or group represented by formula (II). Here, Rb and Rc may bond to each other to form a ring. Substituents are a hydroxyl group, carboxy group, alkyl group, or group represented by formula (III). In formula (II), Rf indicates a hydrogen atom or an alkyl group optionally substituted by a hydroxyl group.

Description

External preparation

Technical field

The present invention relates to a kind of external preparation.

Background technology

It is known that tranexamic acid has pigmentation inhibitory action etc., it is used in various cosmetics because of whitening etc. In.On the other hand, tranexamic acid is under the conditions of being exposed to daylight, high temperature etc., there is a problem of through when colour.Additionally, at the same time The problem that coloring occurs is there is also during using tranexamic acid with carbohydrate.

As suppression simultaneously using the method for tranexamic acid and coloring during carbohydrate, such as, in patent document 1, disclose A kind of cosmetic composition is it is characterised in that in the composition containing tranexamic acid class and carbohydrate, adding and be selected from inorganic acid Class or its salt, organic acid or its salt, alcohols, vitamins or derivatives thereof, chelating agent and from plant, marine alga or animal One of composition or two or more.

Prior art literature

Patent document

Patent document 1：Japanese Unexamined Patent Publication 2014-062077 publication

Content of the invention

The technical problem to be solved in the present invention

In cosmetic composition described in patent document 1, mainly sodium pyrosulfite is used as inorganic salts.But It is that sodium pyrosulfite has metachronism and has a case that unpleasant odour, be not suitable for perfume-free preparation.Even if additionally, using fragrant Material also cannot cover this smell.

The present invention forms in view of the above circumstances, its object is to provide a kind of external preparation, and its suppression is containing tranexamic acid With in the external preparation of carbohydrate because through when the coloring that leads to.

Solve the technological means of technical problem

It was found by the inventors of the present invention that by containing (A) tranexamic acid (hereinafter referred to as " (A) composition ") and (B) carbohydrate Add the compound or its salt shown in (C) formula (I) (hereinafter referred to as further in the composition of (hereinafter referred to as " (B) composition ") " (C) composition "), it is capable of the coloring of composite inhibiting.The present invention is formed based on above-mentioned opinion.

The present invention for example provides following [1]～[11].

[1] a kind of external preparation, its contain the compound shown in (A) tranexamic acid or its salt, (B) carbohydrate, (C) formula (I) or Its salt,

[chemical formula 1]

In formula (I), R^aRepresent straight chained alkyl or the-NR of carbon number 7～19^dR^eShown group, R^dAnd R^eEach independent Ground represents the alkyl can with hydrogen atom or substituent, R^bAnd R^cRepresent the alkyl can with hydrogen atom, substituent independently of one another Or the group shown in formula (II), wherein, R^bAnd R^cRing can be bonded together to form mutually, described substituent be hydroxyl, carboxyl, alkyl or Group shown in formula (III)；

[chemical formula 2]

In formula (II), R^fThe alkyl that expression can be replaced by hydrogen atom or hydroxyl.

[chemical formula 3]

[2] external preparation according to [1], wherein, the compound shown in formula (I) is the compound shown in formula (1),

[chemical formula 4]

In formula, R¹Any one in expression (2)～group shown in (23), n represents 6～18 integer.

[chemical formula 5]

[chemical formula 6]

[chemical formula 7]

[3] external preparation according to [1], wherein, the compound shown in formula (I) is the compound shown in formula (24),

[chemical formula 8]

In formula, R^b、R^c、R^dAnd R^eWith the R in formula (I)^b、R^c、R^dAnd R^eSynonymous.

[4] external preparation according to [1], wherein, described (C) composition is selected from N- decoyl glycine (N- Capryloylacylglycine), N- capryl-L-PROLINE, N- stearyl-Pidolidone, allantoin and Alcloxa (alcloxa) at least one and in their group of salt composition.

[5] external preparation according to any one of [1]～[4], described (B) composition is selected from monose, disaccharides, oligosaccharides And at least one in the group of glucoside composition.

[6] a kind of external preparation, it is for whitening, suppression or to improve inflammation or the external preparation improving pachylosis, and it contains There is the compound or its salt shown in (A) tranexamic acid or its salt, (B) carbohydrate, (C) formula (I).

[7] external preparation in whitening, suppression or improves inflammation or improves application in pachylosis, and this external preparation contains (A) Compound or its salt shown in tranexamic acid or its salt, (B) carbohydrate, (C) formula (I).

[8] external preparation preparation for whitening, for suppress or improve inflammation or for improve pachylosis medicament in Application, this external preparation contains the compound or its salt shown in (A) tranexamic acid or its salt, (B) carbohydrate, (C) formula (I).

[9] a kind of method for whitening, suppression or improve the method for inflammation or improve the method for pachylosis, it includes making to contain The external preparation having the compound or its salt shown in (A) tranexamic acid or its salt, (B) carbohydrate, (C) formula (I) is used for the operation of skin.

[10] a kind of method of the coloring of suppression external preparation, its by make external preparation contain (A) tranexamic acid or its salt, (B) compound or its salt shown in carbohydrate, (C) formula (I) and suppress the coloring of external preparation.

[11] a kind of method of coloring of suppression external preparation and pH change, it contains (A) tranexamic acid by making external preparation Or the compound or its salt shown in its salt, (B) carbohydrate, (C) formula (1) and suppress the coloring of external preparation and pH change.

Invention effect

In accordance with the invention it is possible to provide a kind of external preparation, in this external preparation containing tranexamic acid and carbohydrate it is suppressed that Because heat or through when and the coloring that leads to.

Specific embodiment

Hereinafter, the mode (hereinafter referred to as " present embodiment ") for implementing the present invention is described in detail.Additionally, The present invention is not limited by implementation below institute.

The external preparation of present embodiment contains the compound shown in (A) tranexamic acid or its salt, (B) carbohydrate, (C) formula (I) Or its salt,

[chemical formula 9]

In formula (I), R^aRepresent straight chained alkyl or the-NR of carbon number 7～19^dR^eShown group, R^dAnd R^eEach independent Ground represents the alkyl can with hydrogen atom or substituent, R^bAnd R^cRepresent the alkyl can with hydrogen atom, substituent independently of one another Or the group shown in formula (II), wherein, R^bAnd R^cRing can be bonded together to form mutually, above-mentioned substituent be hydroxyl, carboxyl, alkyl or Group shown in formula (III)；

[chemical formula 10]

In formula (II), R^fThe alkyl that expression can be replaced by hydrogen atom or hydroxyl.

[chemical formula 11]

(A) tranexamic acid or its salt

Tranexamic acid is also known as the compound of trans -4- (amino methyl) hexamethylene -1- carboxylic acid for one kind, can pass through Known method synthesizes it is also possible to the mode of commercially available product obtains.

As the salt of tranexamic acid, as long as or physiologically allowing in pharmacology (in pharmacy) as external preparation, then no It is particularly limited to.As the salt of tranexamic acid, for example, can include the alkali metal salts such as sodium salt, sylvite；The alkaline earth eka-gold such as calcium salt, magnesium salts Belong to salt；Zinc salt；Molysite；Ammonium salt；The salt being formed with basic amino acids such as arginine, lysine, histidine, ornithines；With single second Salt that the amine such as hydramine, diethanol amine, triethanolamine are formed etc..As the salt of tranexamic acid, wherein, particular certain cancers, sylvite, three second Alcohol amine salt, arginine salt, more preferably sodium salt.

Tranexamic acid or its salt can be used alone one kind, also can be combined using two or more.

With regard to the content of (A) composition in the external preparation of present embodiment, such as using the total amount of external preparation as benchmark, (A) The total content of composition is preferably generally 0.01～5 weight %, more preferably 0.1～3 weight %, more preferably 0.5～2 weight Amount %.(A) if the described scope of the content of composition, then the effect that the present invention brings can be improved further.(A) content of composition If described scope, then additionally it is possible to obtain tranexamic acid or whitening that its salt has, anti-in addition to the effect that the present invention brings Inflammation, improve pachylosis and other effects.

(B) carbohydrate

As carbohydrate, as long as can be used for the carbohydrate of common composition for external application, it is not particularly limited, for example Monose, disaccharides, oligosaccharides, polysaccharide, glucoside and sugar alcohol can be included.

As monose, for example, can include four carbohydrates such as D- erythrulose, D- erythrose, D- threose；D-R, L- The valeral carbohydrates such as arabinose, D- wood sugar, D- lyxose, L- lyxose, D-ribose；D- xylulose, L- xylulose, D- core ketone The pentanone carbohydrates such as sugar, L- ribulose；The hexanal carbohydrates such as D- galactolipin, L- galactolipin, D-Glucose, D- talose, D-MANNOSE； The hexanone carbohydrate such as L- sorbose, D-Tag, D-Psicose, D-Fructose；The side chain carbohydrates such as D- apiose, D- hamamelose； The pentoses such as ribose, arabinose, wood sugar；The hexoses such as glucose, galactolipin, fructose；The amino sugars such as aminoglucose, galactosamine；Or Derivative of these monose etc..

As disaccharides, oligosaccharides and its glucoside, the equal oligosaccharides containing a kind of above-mentioned monose or derivatives thereof can be included Or containing two or more heterooligosaccharides.As equal oligosaccharides, for example, can include the wood such as xylobiose, xylotriose, Xylotetrose, wooden pentasaccharides Oligosaccharide kind；The galactooligosacchari(es classes such as agarobiose, carrabiose (carrabiose)；Maltose, maltotriose, maltotetraose, Maltopentaose, isomaltose, sophorose (sophorose), cellobiose, cellotriose, cellotetrose, cellopentaose, trehalose, The grape oligosaccharide kind such as neotrehalose, isotrehalose；Mannooligo saccharide；Inulobiose, inulin trisaccharide, inulin tetrose, inulin pentasaccharides Deng fructo oligosaccharide etc..As heterooligosaccharide, vicianose, isoprimeverose, mountain cloth disaccharide (sambubiose), primrose can be included Sugar, lycotetraose, solabiose (solabiose), melibiose, manninotriose, lactose, short-tube lycoris disaccharides, short-tube lycoris trisaccharide, table fiber two Sugar, sucrose, turanose, maltulose, different ketose, erlose (erlose), ketose, gentianose, Lactulose, epigentiobiose, isolychnose, umbelliferose, sesame seed candy, gossypose, lychnose, robinobiose (robinobiose), hila disaccharides (silanobiose), rutinose, chacotriose, solatriose, alpha-glucans oligosaccharides are (poly- Right be 2～10 glucose oligomers) etc..

As polysaccharide, xanthans, cellulose, guar gum, starch (starch), the mould glycan of short stalk can be included (pullulan), glucan, levulan, mannosan, agar, carragheen, chitin, chitosan, pectin, alginic acid The polysaccharide such as (alginic acid), starch (amylum), glycogen, hyaluronic acid.These sugar are also included by methyl, second in polysaccharide The substituted derivatives such as base, ethoxy, hydroxypropyl, acetyl group, stearic epoxide, glycerine, propane diols.These substituents can be single Replaced solely or with multiple combination.As the polysaccharide with substituent, hydroxyethyl cellulose, ethoxy second specifically can be included Base cellulose, molar substitution degree, HES, methylcellulose, methyl, methyl starch, ethyl cellulose, second Base guar gum, hydroxyethyl starch, hydroxypropyl cellulose, HPG, hydroxypropul starch, HEMC, hydroxyl second Ylmethyl guar gum, hydroxyethyl methyl starch, hydroxypropyl methyl cellulose, hydroxypropylmethyl guar, hydroxypropyl methyl starch, Stearic epoxide hydroxypropyl methyl cellulose, acetylation hyaluronic acid, propylene glycol alginate, hyaluronic acid propylene diester etc..

As glucoside, for example can include ursin, ascorbic acid glucoside, glucose ceramide, anthocyanin, Rutin, aurantiamarin, daidzin etc..

As glycitols, for example can include xylitol, trehalose, maltitol, mannitol, sorbierite, subconjunctival capillaries alcohol, Ah Draw primary sugar alcohol, ribitol, galactitol, glucitol, erythrite.

In these carbohydrates, preferably glucose, arabinose, galactolipin, mannose, maltose, fructose, lactose, α-Portugal Chitosan oligosaccharide, carragheen, dextrin, pectin, hyaluronic acid, Sodium Hyaluronate, hyaluronan sodium, hydrolysis hyaluronic acid, thoroughly Bright matter acid hydroxypropyl three ammonium, hydrolysis zinc hyaluronate, Sodium Hyaluronate cross-linked polymer, hyaluronic acid PG, chondroitin sulfate, can Soluble collagen, curdlan, xanthans, carragheen, methylcellulose, ethyl cellulose, carboxymethylcellulose calcium, methylol Cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, cationized cellulose, alginate, ring Dextrin, glucan, the mould glycan of short stalk, ursin, ascorbic acid glucoside etc..As carbohydrate, more preferably glucose, malt Sugar, fructose, lactose, alpha-glucans oligosaccharides, hyaluronic acid, hyaluronic acid, Sodium Hyaluronate, hyaluronan sodium, hydrolysis are thoroughly Bright matter acid, hyaluronic acid hydroxypropyl three ammonium, hydrolysis zinc hyaluronate, Sodium Hyaluronate cross-linked polymer, hyaluronic acid PG, xanthan Glue, carragheen, methylcellulose, ethyl cellulose, carboxymethylcellulose calcium, hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl Cellulose, hydroxypropyl methyl cellulose, cationized cellulose, alginate, ursin, ascorbic acid glucoside etc..As Carbohydrate, more preferably glucose, maltose, fructose, lactose, alpha-glucans oligosaccharides, carboxymethylcellulose calcium, hydroxy ethyl fiber Element, hydroxypropyl methyl cellulose, alginate, methylcellulose, ursin, ascorbic acid glucoside etc..

Carbohydrate can be used alone one kind, also can be combined using two or more.

With regard to the content of (B) composition in the external preparation of present embodiment, in terms of total amount, (B) composition is preferably 0.01～7 weight Amount %, more preferably 0.05～5 weight %, more preferably 0.1～3 weight %.(B) if the content of composition is in described model Enclose, then can improve the effect that the present invention brings further.

(C) compound or its salt shown in formula (I)

R in the formula (I) of (C) composition of present embodiment^aRepresent straight chained alkyl or the-NR of carbon number 7～19^dR^eInstitute The group showing.R^dAnd R^eRepresent hydrogen atom or alkyl independently of one another, alkyl can have substituent.As this substituent, permissible It is hydroxyl, carboxyl, alkyl or the group shown in formula (III), preferably hydroxyl, carboxyl, alkyl or the group shown in formula (III), The more preferably group shown in formula (III).

[chemical formula 12]

R in formula (I)^bAnd R^cRepresent hydrogen atom, alkyl or the group shown in formula (II) independently of one another, alkyl can have Substituted base.As this substituent, can be hydroxyl, carboxyl, alkyl or the group shown in formula (III), preferably hydroxyl, carboxyl Or alkyl, R^bAnd R^cRing can be bonded together to form mutually.

[chemical formula 13]

In formula (II), R^fThe alkyl that expression can be replaced by hydrogen atom or hydroxyl.

Compound shown in formula (I) is preferably the compound shown in formula (1) or formula (24).

[chemical formula 14]

In formula (1), R¹Any one in expression (2)～group shown in (23), n represents 6～18 integer.

[chemical formula 15]

In formula (24), R^b、R^c、R^dAnd R^eAs mentioned above.

R in formula (1)¹As long as being not particularly limited for any one in formula (2)～group shown in (23).This embodiment party The external preparation of formula when containing the compound shown in formula (1) as (C) composition, except suppression external preparation coloring effect in addition to, The change of the pH of external preparation can also be suppressed.The pH of external preparation is due to becoming the former of external preparation variable color because of contained active ingredient Because, or due to intervening the viscosity of external preparation and becoming due to use feeling or Character change, therefore preferably unchanged.From entering one The angle of the external preparation coloring of step suppression present embodiment and pH change is set out, the R in formula (1)¹Be preferably formula (2), formula (3), Formula (9), formula (10), formula (11), formula (22) or the group shown in formula (23), more preferably formula (2), formula (9) or formula (11).Formula (1) n in the compound shown in is preferably 6～18, more preferably 7～18.From the external application further suppressing present embodiment The angle of agent coloring and pH change is set out, as the compound shown in formula (1), such as preferably N- decoyl glycine, N- caprinoyl Base-L-PROLINE and N- stearyl-Pidolidone.

The angle colouring from the external preparation further suppressing present embodiment, as the chemical combination shown in formula (24) Thing, for example preferably allantoin ((2,5- dioxo -4- imidazolidinyl) urea) or its salt or imidazolidinyl urea (N, N '-methylene Two [N '-(3- methylol -2,5- dioxo -4- imidazolidinyl) urea), more preferably allantoin or its salt.

As C) salt of composition, as long as or physiologically allowing in pharmacology (in pharmacy) as external preparation, then no special Do not limit.As the salt of (C) composition, for example, can include the alkali metal salts such as sodium salt, sylvite；The alkaline-earth metals such as calcium salt, magnesium salts Salt；The aluminium salt such as hydroxyl aluminium salt；Zinc salt；Molysite；Ammonium salt；With the basic amino acid shape such as arginine, lysine, histidine, ornithine The salt becoming；Salt being formed with amine such as MEA, diethanol amine, triethanolamines etc..As the salt of (C) composition, wherein, preferably Sodium salt, sylvite, triethanolamine salt, arginine salt, more preferably sodium salt.As the salt of allantoin, preferably Alcloxa (allantois Plain aluminium chloride).

(C) composition can be used alone one kind it is also possible to be applied in combination two or more.

The content of (C) composition in the external preparation of present embodiment, such as on the basis of the total amount of external preparation, (C) composition Total content is preferably generally 0.01～10 weight %, more preferably 0.05～8 weight %, more preferably 0.1～5 weight Amount %.When (C) composition is allantoin, Alcloxa, imidazolidinyl urea or its salt, its content with the total amount of external preparation is for example Benchmark, total content preferably 0.01～5 weight % of (C) composition, more preferably 0.05～2 weight %, more preferably 0.1 ～1 weight %.(C) if the content of composition is in described scope, the effect that the present invention brings can be improved further.

With regard to the content of (C) composition in the external preparation of present embodiment, (B) can suitably be adjusted according to the carbohydrate using Divide the interpolation ratio with (C) composition.For every 1 weight portion (B) composition, the content of (C) composition is preferably 0.05～5 weight portion, more It is preferably 0.1～4 weight portion, more preferably 0.15～3.0 weight portion.If with respect to (B) composition with the ratio of described scope Example contains (C) composition, then can fully suppress the external preparation of present embodiment to colour or pH change, have and can suppress anti-with coloring The tendency of the smell answered and produce.

The preparation method of the compound shown in formula (I) is not particularly limited.The preparation method of the compound shown in formula (I), For example can be by the compound with amino be prepared derivative with the compound condensation with carboxyl.Change shown in formula (1) The preparation method of compound is not particularly limited.The preparation method of the compound shown in formula (1), for example, can pass through the ammonia of amino acid The carboxyl of base and aliphatic acid is condensed and prepares derivative.The preparation method of the compound shown in formula (24) is not particularly limited.Formula (24) preparation method of the compound shown in, for example, can prepare derivative by carrying out oxidation processes to urea.

The external preparation of present embodiment can be any one in medicine, quasi drug or cosmetics.Outside present embodiment Preferably it is applicable to the skin preparations for extenal use of skin with agent.

Form for the external preparation of the present embodiment of medicine is not particularly limited, for example, can include liquor, hang Turbid dose, emulsion, creme, ointment, gel, liniment, lotion (lotion), aerosol etc..These preparations can change according to the 16th Positive method described in Pharmacopeia of Japan preparation general provisions etc. is prepared.As the form of external preparation, wherein preferably liquor, suspended Agent, emulsion, creme, ointment, gel, lotion and aerosol, more preferably liquor, suspension, creme, emulsion and gel Agent.

As during for quasi drug or external preparation used for cosmetic, it can be the external preparation identical with described medicine Form.Additionally, in addition, as the form of external preparation, patch can be included or make liquid contain the sheet being immersed on non-woven fabrics Agent etc..As the form for quasi drug or external preparation used for cosmetic, wherein preferably liquor, suspension, emulsion, creme, Ointment, gel, lotion and sheet agent, more preferably liquor, suspension, creme, emulsion and gel.

The external preparation of present embodiment, when containing oiliness base with aqueous base as creme and emulsion, can be W/ O-shaped or O/W type.The external preparation of present embodiment is preferably O/W type.

As the purposes served as when quasi drug or external preparation used for cosmetic, for example, can include toner, emulsion, coagulate Glue, creme, beautifying liquid, sun-proof apply some make up, the basis such as facial mask (pack), facial mask (mask), hand lotion, shin moisturizer, face cream Cosmetics；Mildy wash, makeup removal products, agent of shaving, body lotion, shampoo, smooth liquid (rinse), hair conditioner (treatment) etc. are clear Wash and apply some make up；The lips such as lip-stick, lipstick apply some make up；The makeup cosmetic such as foundation cream, mascara；Hair remover；And bathing use Agent etc..

The external preparation of present embodiment, in addition to described composition, can contain and be generally used for medicine, quasi drug or cosmetic The base of product or carrier.Additionally, the external preparation of present embodiment can contain additive as needed.

As the base contained by the external preparation of present embodiment or carrier, for example can include atoleine, saualane, The hydrocarbon such as vaseline, gelled hydrocarbon (Plastibase etc.), ceresine, alpha-olefin oligomer, liquid paraffin,light；Polymethyl siloxane, Cross-linking type polymethyl siloxane, high polymerization polymethyl siloxane, cyclic silicone, alkyl-modified silicone, the alkyl-modified silicon of cross-linking type Ketone, amino modified silicone, polyether modified silicone, polyglycerol-modified silicone, crosslinked polyether modified silicone, cross-linking type alkyl, polyether Modified silicone, silicone alkyl chain modified polyether modified silicone, silicone alkyl chain modified polyglycerol-modified silicone, polyethers altogether altogether The silicone oil such as modified side chain silicone, polyglycerol-modified side chain silicone, silicon Acrylote, phenyl modified silicone, organic siliconresin；16 The higher alcohols such as alcohol, cetostearyl alcohol, octadecanol, tadenan；Cholesterine, phytosterol, phytosterol hydroxy stearic acid The sterols such as ester；SIMMONDSIA CHINENSIS SEED OIL, meadow sweet seed oil, sunflower oil, grape-kernel oil, Chinese toon oil, saualane, shea butter, rice germ The vegetable oil such as oil；Lanolin, orange even fin salmon (Orange roughy) animal oil such as oil, saualane, house oil；Ethyl cellulose, hydroxyl The modified natural polymers such as propyl cellulose, hydroxypropyl methyl cellulose, JR-125, acetylation hyaluronic acid； Polyvinylpyrrolidone, carboxyl ethylene polymer, acrylic arid methacrylic acid alkyl ester copolymer etc. synthesize macromolecule；OK a karaoke club The natural polymers such as glue, alginic acid, cellulose, guar gum, smoke tree, glucan, gellan gum, hyaluronic acid；Polyethylene butyl ester； Polyethylene glycol；Dioxane；Butanediol adipate polyester；Isopropyl myristate, myristic acid octyldodecyl ester, palm fibre Palmitic acid isopropyl propionate, cetyl palmitate, isononyl isononanoate, pentaerythrite four (2 ethyl hexanoic acid) ester, SIMMONDSIA CHINENSIS SEED OIL, three (pungent Acid/capric acid) esters such as glyceride；The polysaccharides such as dextrin, maltodextrin；The lower alcohols such as ethanol, isopropanol；The carbon of described above is former Subnumber 2～6, the polyalcohol of hydroxyl value 2～4；The glycol ether of described above；Butanedioic acid, glycolic, gluconic acid, citric acid etc. Organic acid；And the aqueous base such as water etc..As the base contained by the external preparation of present embodiment or carrier, wherein it is preferably many First alcohol, higher alcohol, hydrocarbon, esters and silicone oil, more preferably polyalcohol.

As the preferred example of the external preparation of present embodiment, as base, liquor containing polyalcohol, suspended can be included Agent, creme, emulsion and gel.

Base or carrier can be used alone one kind, also can be combined using two or more.

In the range of the effect not damaging the present invention, can be added in the external preparation of present embodiment medicine, quasi drug, Or the known additive adding in cosmetics.As additive, for example, can include antioxidant, surfactant, thickening Agent, preservative agent, pH adjusting agent, stabilizer, stimulation palliative, preservative, colouring agent, freshener, spices, pearling agent etc..

As antioxidant, for example, can include dibutyl hydroxy toluene, butylated hydroxy anisole, sorbic acid, sulfurous acid Sodium, ascorbic acid, ascorbic acid derivates, tocopherol, Tocopheryl derivatives, arabo-ascorbic acid, L-cysteine hydrochloride etc..

As surfactant, for example, can include sorbitan list isostearate, sorbitan mono laurate Ester, sorbitan monopalmitate, sorbitan monostearate, five -2 ethyl hexanoic acid two glycerine sorbitan, The sorbitan fatty acid ester classes such as four -2 ethyl hexanoic acid two glycerine sorbitan；The propane diols such as propylene glycol monostearate Fatty acid ester；Polyoxyl 40 hydrogenated castor oil (HCO-40), Nikkol HCO50 (HCO-50), polyoxyethylene The rilanit special derivatives such as 60 rilanit specials (HCO-60), Nikkol HCO80；Polyoxyethylene (20) sorb Sugar alcohol acid anhydride monolaurate (TWEEN-20), polyoxyethylene (20) sorbitan monostearate (polysorbate 60), polyoxyethylene (20) sorbitan monooleate (polysorbate 80), the different tristearin of polyoxyethylene (20) sorbitan The polyoxyethylene sorbitan fatty acid ester class such as acid esters；Polyoxyethylene list coconut oil fat acid glyceride；Glycerine alkyl ether；Whale The alkyl glucosides such as wax stearyl glucoside；The polyoxyalkylenes such as PCE, polyoxyethylene docosyl ether Alkyl ether；The amines such as stearylamine, oleyl amine；Polyoxyethylene methyl polysilicone alkyl copolymer, lauryl PEG-9 polydimethylsiloxanes The silicone surfactant such as ethyl dimethyl silicone polymer, KF-6028；Phosphorus The natural surfactants such as fat, surfactant peptides, saponin(e；The fat such as stearmide alcohol, stearamide propyl diethylamine Fat acid amido amine；The alkylamines such as Alamine 304, dimethyl stearamine, D2EHA di 2 ethylhexyl amine；Stearamide propyl diformazan Betaines amphoteric surfactantes such as amine, lauryl hydroxyl sulfo betaine etc..

As thickener, for example, can include guar gum, locust bean gum, carragheen, hyaluronic acid, xanthans, polyethylene Alcohol, polyvinylpyrrolidone, carboxyl ethylene polymer, acrylic arid methacrylic acid alkyl ester copolymer, polyethylene glycol, bentonite, Alginic acid, polyethylene glycol (macrogol), sodium chondroitin sulfate, methylcellulose, ethyl cellulose, hydroxyethyl cellulose, hydroxyl The cellulose families such as methylcellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, carboxymethylcellulose calcium, carboxyethyl cellulose Thickener etc..

As preservative or preservative agent, for example, can include benzoic acid, Sodium Benzoate, dehydroactic acid, dehydroactic acid sodium, right Hydroxybenzoic acid isobutyl ester, p-Hydroxybenzoic acid isopropyl ester, butyl p-hydroxybenzoate, ethyl-para-hydroxybenzoate, to hydroxyl Propyl benzoate, benzyl p-hydroxybenzoate, methyl p-hydroxybenzoate, phenoxetol, benzylalcohol, methaform, sorbic acid and Its salt, chlorhexidine gluconate, alkanediol, fatty acid glyceride etc..

As pH adjusting agent, for example, can include inorganic acid (hydrochloric acid, sulfuric acid, phosphoric acid, polyphosphoric acid, boric acid etc.), organic acid (lactic acid, sodium lactate, acetic acid, citric acid, sodium citrate, tartaric acid, malic acid, butanedioic acid, sodium succinate, oxalic acid, gluconic acid, Fumaric acid, propionic acid, aspartic acid, EACA, glutamic acid, tarine etc.), glucolactone, ammonium acetate, inorganic Alkali (sodium acid carbonate, sodium carbonate, potassium hydroxide, NaOH, calcium hydroxide, magnesium hydroxide etc.) and organic base (MEA, three Monoethanolamine, diisopropanolamine (DIPA), lysine, triisopropanolamine etc.) etc..

As stabilizer, for example, can include Sodium Polyacrylate, dibutyl hydroxy toluene, butylated hydroxy anisole etc..

As stimulating palliative, for example, can include Radix Glycyrrhizae extract, sodium alginate, 2- methylacryoyloxyethyl phosphoric acid Choline etc..

As chelating agent, for example, can include ethylenediamine tetra-acetic acid (edetic acid(EDTA)), (sodium salt is (according to ground for edetate Sour sodium：Pharmacopeia of Japan, EDTA-2Na etc.), sylvite etc.), phytic acid, gluconic acid, polyphosphoric acid, metaphosphoric acid etc..As chelating agent, its In be preferably edetate sodium.

As colouring agent, for example, can include inorganic pigment, natural colouring matter etc..

As freshener, can include menthol, TK-10, thin lotus base glycerol base ether, menthyl lactate, Camphor, eugenol, peppermint oil, Japanese peppermint oil etc..

As pearling agent, for example, can include glycol distearate, ethylene glycol monostearate, triethylene glycol two hard Resin acid ester etc..As pearling agent, wherein preferably glycol distearate.

Additive can be used alone one kind, also can be combined using two or more.

In the range of the effect not damaging the present invention, the external preparation of present embodiment can contain other active ingredients. As active ingredient specific example, for example can include moisturizing ingredient, anti-inflammatory composition, antimicrobial component, vitamins, peptide Or derivatives thereof, amino acid or derivatives thereof, cell activation composition, anti-aging composition, blood circulation promote composition, cutin softening Composition, whitening composition, astringent component, ultraviolet protection composition (UV absorbing component, ultraviolet scattering composition) etc..

As moisturizing ingredient, for example, can include：The lipids such as ceramide, cholesterine, phosphatide；Chamomile extract, mulberry Shen extract, cordate houttuynia extract, ginseng extract, witch hazel extract, cowberry leaf extract, tea extract, purple perilla extraction The plant extract extract such as thing；Hyaluronic acid, Sodium Hyaluronate, hyaluronan, hyaluronan sodium, heparan, soft The mucopolysaccharides such as ossein, sodium chondroitin sulfate；The high scores such as collagen, elastin laminin, keratin, chitin, chitosan Sub- compound；Glycerine, 1,3 butylene glycol, propane diols, polyethylene glycol and two glycerine trehaloses (diglycerine trehalose) Deng polyalcohol；Alanine, serine, leucine, isoleucine, threonine, glycine, proline, hydroxy-proline, glucose The amino acid such as amine, aspartic acid, theanine, arginine；The NMFs such as sodium lactate, urea, pyrrolidone sodium carboxylate；Mountain The sugar alcohols such as pears alcohol；The phosphatide such as lecithin, hydrolecithin；Polyglutamic acid；MPC polymer (for example, LIPIDURE (registration mark) Deng) etc. there is the macromolecule of phosphatide polar group；PP 25；Trimethylglycine (glycine betaine)；Ethoxy Urea；Acrylic acid acrylamide dimethyldiallylammonium chloride copolymer etc..As NMF, wherein, if considering to use Sense, then the preferably lipid such as ceramide, cholesterine, phosphatide；Mulberry extract, cordate houttuynia extract, ginseng extract, cowberry The plant extracts such as leaf (bilbery leaf) extract.

As anti-inflammatory composition, for example, can include from plant (for example, grape, asia ginseng and rehabilitation power flower etc.) Composition, allantoin, glycyrrhizic acid or derivatives thereof, acidifying zinc, puridoxine hydrochloride, salicylic acid or derivatives thereof and epsilon-amino oneself Acid, OPC, tocopherol or derivatives thereof, ascorbic acid or derivatives thereof, aurantiamarin, glucityl aurantiamarin, erythrothioneine, Sodium hydrogensulfite, arabo-ascorbic acid or its salt, flavonoids, glutathione, glutathione peroxidase, glutathione-S- turn Move enzyme, catalase, superoxide dismutase, thioredoxin, taurine, thiolaurine, hypotaurine etc..

As antibacterial or sterilization component, for example can include Chlorhexidine, salicylic acid, benzalkonium chloride, rivanol, Sulfur, Resorcinol, ethanol, benzethonium chloride, Adapalene, benzoyl peroxide, clindamycin, cresols, gluconic acid and its derivative Thing, PVP-I, KI, iodine, isopropyl methyl phenol, triclocarban, triclosan, photosensitive plain No. 101, photosensitive plain No. 201, The alkanediols such as p-hydroxybenzoate, phenoxetol, 1,2- pentanediol, fatty acid glyceride, azelaic acid, salt dialkylaminobenzoic acid two Amino glycine, chlorhexidine gluconate, p-phenolsulfonic acid's zinc etc..

As vitamins, for example, can include：The retinols such as retinol, retinyl acetate, retinyl palmitate Derivative, retinene, retinoic acid, retinoic acid methyl esters, retinoic acid ethyl ester, retinol retinoic acid ester, d- Delta-Tocopherol retinoic acid ester The retinoid such as (tocopheryl retinoate), alpha-tocopherol retinoic acid ester, betatocopherol retinoic acid ester；β-carrot The provitamin As such as element, alpha-carotene, gamma carotene, δ-carrotene, lycopene, luteole, kryptoxanthin, echinenone Class；Delta-Tocopherol, dl- alpha-tocopherol, dl- alpha-tocopherol acetate, dl- alpha-tocofecol succinic acid ester, dl- alpha-tocopherol amber The vitamin E class such as acid esters calcium, tocopheryl nicotinate；Riboflavin, FMN, flavin adenine dinucleotide (FAD), riboflavin The vitamin B2 classes such as butyrate, Riboflavin Tetrabutyrate, riboflavin 5 '-sodium phosphate, riboflavin four nicotinate；Dl- α-fertility The nicotinic acid classes such as phenol nicotinate, nicotinic acid benzyl ester, methyl nicotinate, nicotinic acid Beta-Butoxy ethyl ester, 1- (4- aminomethyl phenyl) ethyl nicotinate；Anti- Bad hematic acid stearate, Vitamin C dipalmitate, Ascorbyl Tetraisopalmitate (ascorbic acid four 2- hexyldecanoic acid Ester), ascorbic acid, sodium ascorbate, hydroascorbic acid, NAP, MAP, Vitamin C The vitamin Cs such as sour glucoside, ascorbigen (ascorbigen)-A, ascorbyl stearate, ascorbyl palmitate Class；The vitamin D class such as hesperidin methyl, ergocalciferol, vitamine D3；The vitamin K class such as phylloquinone, farnoquinone；Hexichol Formyl thiamine, dibenzoyl thiamine, thiamine salt hydrochlorate, thiamine cetyl hydrochloride, thiamine sulphur cyanogen Hydrochlorate, thiamine lauryl hydrochloride, thiamine nitrate, thiamine monophosphate, thiamine lysine salt, thiamine three phosphorus Hydrochlorate, thiamine phosplate phosphate, thiamine phosplate, thiamine bisphosphate, thiamine bisphosphate hydrochloride, The vitamin B1 classes such as thiamine triguaiacyl phosphate, thiamine triguaiacyl phosphate monophosphate；Puridoxine hydrochloride, acetic acid pyridoxol, hydrochloric acid The vitamin B6 classes such as pyridoxal, P5P, hydrochloric acid pyridoxamine；Cyanocobalamin, hydroxocobalamine, deoxyadenosyl cobalamin Deng vitamin B12 class；The folic acid class such as folic acid, pteroylglutamic acid；The nicotinic acid class such as nicotinic acid, niacin hydroxyacyl amine；Pantothenic acid, calcium pantothenate, basis are many The pantothenic acid classes such as raw alcohol (panthenol), D- lactobacillus bulgaricus factor (pantecine), D- pantethine, coacetylase, pantothenic acid alcohol ethylether；Raw The biotin classes such as thing element, biocytin (bioticine)；Ascorbic acid, sodium ascorbate, hydroascorbic acid, ascorbic acid The vitamin c class of the ascorbic acid derivates such as sodium phosphate, MAP；Gamma oryzanol, carnitine, forulic acid, α- Vitaminoid action factor such as lipoic acid, orotic acid etc..

As peptide or derivatives thereof, for example, can include keratin and decompose peptide, hydrolysis of keratin, collagen, be derived from fish Collagen, Atelocollagen albumen, gelatin, elastin laminin, elastin laminin decompose peptide, collagen decompose peptide, hydrolysis glue Former albumen, chlorination hydroxypropyl ammonium Hydrolyzed Collagen, Elastin peptide, conchiolin decompose peptide, hydrolysis conchiolin, silkworm Silk-fibroin decompose peptide, hydrolysis silk, lauroyl hydrolysis silk sodium, soybean protein decompose peptide, hydrolytic soya bean protein, wheat gluten, Wheat gluten decomposes peptide, hydrolyzed wheat protein, caseinolytic peptide, acylated peptide (palmitoyl oligopeptide, palmityl penta peptide, palmityl Tetrapeptide etc.) etc..

As amino acid or derivatives thereof, for example, can include glycine betaine (trimethylglycine), proline, hydroxyl dried meat ammonia Acid, arginine, lysine, serine, glycine, alanine, phenylalanine, Beta-alanine, threonine, glutamic acid, paddy ammonia Acid amides, asparagine, aspartic acid, cysteine, cystine, methionine, leucine, isoleucine, valine, group ammonia Acid, taurine, GABA, gamma-amino-beta-hydroxy butyric acid, carnitine, carnosine, creatine etc..

As cell activation composition, for example, can include the amino acidses such as GABA, EACA；Retinol, The vitamins such as thiamine, riboflavin, puridoxine hydrochloride, pantothenic acid class；The Alpha-hydroxy acids such as glycolic, lactic acid；Tannin；Class is yellow Ketone；Saponin(e；Allantoin；Photosensitive plain No. 301 etc..

As anti-aging composition, for example can include pangamic acid, kinetin, ursolic acid, turmeric extract, sphingol derive Thing, silicon, silicic acid, N- methyl-L-serine, mevalonolactone etc..

As blood circulation facilitation composition, for example can include from (for example asia ginseng, Angelica Keiskei, Arnica, Ginkgo, fennel, prolong life grass, Nasturtium officinale, chamomile, Rome chamomile, carrot, felwort, burdock, rice, hawthorn, mushroom, Europe Continent hawthorn, hackmatack, Ligusticum wallichii, Swertia patens, thyme, cloves, dried orange peel, Radix Angelicae Sinensis, peach kernel, dragon spruce, ginseng, garlic, butcher's broom, Grape, tree peony, horse chestnut, lemon balm, shaddock, coix seed, rosemary, fructus rosae, dried orange peel, Radix Angelicae Sinensis, dragon spruce, peach, apricot, English walnut or Corn) composition；Glucityl aurantiamarin etc..

As keratolytic ingredient, for example, can include urea, salicylic acid, glycolic, gluconic acid, tartaric acid, phytic acid, wool Fat, lactic acid, lactate, citric acid, Sulfur etc..

As whitening composition, for example, can include：Ursin；Hydroquinones；Kojic acid；Ellagic acid；Phytic acid；Rucinol (rucinol)；Chamomile ET；Ascorbic acid or derivatives thereof；Vitamin E or derivatives thereof；Pantothenic acid or derivatives thereof；There is U.S. Plant component (for example, plant extract or essential oil) of white effect etc..

As astringent component, for example, can include：Alum, chlorination hydroxyl aluminium, aluminium chloride, allantoin aluminium salt, zinc sulfate, to benzene sulphur The slaines such as sour zinc, acidifying zinc, alum；The organic acids such as tannic acid, citric acid, lactic acid, butanedioic acid；Menthol, ethanol etc..

As UV absorbing component, for example, can include methoxy cinnamic acid 2- Octyl Nitrite, 2- [4- (diethylamino Base) -2- hydroxy benzoyl] hexyl-benzoate, 2,4,6- tri- [4- (2- ethylhexyl Epoxide carbonyl) anilino-] -1,3,5- three Piperazine, dimethoxybenzyliden oxo-imidazole alkane propionic acid 2- Octyl Nitrite, 2,4- pair-[{ 4- (2- ethylhexyl epoxide) -2- hydroxyl Base }-phenyl] -6- (4- methoxyphenyl) -1,3,5- triazine, tert-butyl group methoxy dibenzoyl methane, diphenyl methylene dioxy Pungent for imidazolidine propionic acid Octyl Nitrite, ethylhexyl triazoline, p-aminobenzoic acid and its derivative, p-(dimethylamino)-benzoic acid Ester, ethylene glycol salicylate, dihydroxy benaophenonel etc..

Scatter composition as ultraviolet, for example, can include zinc oxide, titanium oxide, iron oxide, cerium oxide, zirconium oxide, silicon The inorganic compounds such as sour titanium, zinc silicate, silicic acid anhydride, silicic acid cerium, aqueous silicic acid；With aqueous silicic acid, aluminium hydroxide or mica, talcum Cover the material of above-mentioned inorganic compound Deng inorganic particle；By above-mentioned inorganic compound and polyamide, polyethylene, polyester, The material that the resin powder such as polystyrene or nylon is composited；Using silicone oil, aliphatic acid aluminium salt etc. to above-mentioned inorganization Compound carries out material of processing etc..

As cleaning composition, for example, can include polyoxyalkylene alkyl (or thiazolinyl) ether sulfate, alkyl (or thiazolinyl) sulphur Hydrochlorate, higher fatty acid salt (palmitic acid, laurate, myristic acid, stearic acid etc.), ether carboxylate, Amide Ether Carboxylates, alkyl Phosphate ester salt, N- acyl amino hydrochlorate (N- lauroyl NaAsp, potassium hydroxide/N- fatty acid distribution of coconut oil acyl glutamic acid Potassium, fatty acid distribution of coconut oil acylglycine sodium, myristoyl glutamic acid etc.), polyoxyalkylene fatty acid amide ether sulfate, acyl group Change isethionate, be acylated the anion surfactants such as taurate；Can addition alkylene oxide, to have straight or branched long The cationic surfactants such as the single or double long chain alkyl ammonium salt of alkyl group；Carboxybetaine, sulfobetaines, imidazoline are sweet Dish alkali (2- alkyl-N- carboxymethyl group-N- hydroxyethyl imidazolines glycine betaine, N- fatty acid distribution of coconut oil acyl group-N- Carboxvmethoxv second Base-N- carboxymethyl group ethylene diamine=sodium etc.), the amphoteric surfactant such as amide betaine.

These other active ingredients can be used alone one kind, also can be combined using two or more.

The external preparation of present embodiment can be the external preparation of container sealing.As container shapes, for example can illustrate vial-type, Tubular type, pot type, point medicine bottle formula, force feed device formula, bag, aluminium foil encapsulation etc..Additionally, as container material, such as it is poly- right to illustrate Polyethylene terephthalate, polypropylene, polyethylene (HDPE, LDPE and LLDPE etc.), ABS resin, ethylene vinyl alcohol, polyphenyl Ethene, glass, metal (aluminium etc.) etc..In addition, it is contemplated that the intensity of these materials, flexibility, weatherability, housing in a reservoir Stability of composition etc., can apply various coating treatments or by for example mixing this etc. to the container containing these materials A little combinations of materials are using as container material or will be laminated as container material by the layer that these materials are constituted.Additionally, ability Field technique personnel are in order to adjust preparation discharge rate from container, or in order to reduce the attachment to container for the preparation, can suitably select Select the nozzle of container and the bore of preparation discharge unit and material.

As the using method of the external preparation of present embodiment, it is according to the state of the skin using object, age, sex And different, for example can include following method.Using method can be, by daily for the external preparation of present embodiment for several times (for example, 1～5 time, preferably 1～3 time) in appropriate amount (such as 0.05～5g) be coated on skin.Additionally, making daily with tranexamic acid Consumption is, for example, 0.00001～0.05g, and the mode of preferably 0.0001～0.02g, more preferably 0.0002～0.01g is coated with External preparation.Additionally, for example, 1～6 month coating phase of external preparation, preferably 3～6 months.

With regard to the external preparation of present embodiment, the physiologically active of tranexamic acid can be expected it is adaptable to have skin speckle, inflammation Deng people.In addition, the external preparation of present embodiment is also applied for the people with various disease of skin or skin problem.This Outward, in order to prevent skin problem, the external preparation of present embodiment also using the people with normal skin as suitable use object.

The external preparation of the present invention is had whitening, suppression or improves inflammation or improve due to the physiologically active of tranexamic acid The effect of pachylosis.Accordingly it is also possible to obtain the invention of following each embodiments.

As an embodiment of the invention, provide a kind of external preparation of the present invention, it is used for whitening, the suppression of inflammation Or the improvement of improvement or pachylosis.

As an embodiment of the invention, provide the external preparation of the present invention for whitening, the suppression of inflammation or change Application in the kind or improvement of pachylosis.

As an embodiment of the invention, provide the external preparation of the present invention preparation for whitening, for suppression or Improve inflammation or be used for improving the application in the medicament of pachylosis.

As an embodiment of the invention, provide a kind of method for whitening, suppression or method or the improvement improving inflammation The method of pachylosis, it comprises for the external preparation of the present invention to be suitable for (coating) operation on skin.

Additionally, the external preparation of the present invention be inhibited by Yin Re or through when and the coloring of external preparation that causes.

Accordingly, as an embodiment of the invention, provide a kind of method of the coloring of suppression external preparation, outer by making Contain the compound or its salt shown in (A) tranexamic acid or its salt, (B) carbohydrate, (C) formula (I) with agent, suppress this external preparation Color.

Further, the external preparation of the present invention be inhibited by Yin Re or through when and the coloring of external preparation that causes and the change of pH Change.

Accordingly, as an embodiment of the invention, provide a kind of method that coloring of suppression external preparation and pH change, Contain the compound or its salt shown in (A) tranexamic acid or its salt, (B) carbohydrate, (C) formula (1) by making external preparation, suppress this outer Changed with the coloring and pH of agent.

Required composition, other additives and their the content as above institute contained in the external preparation of described each embodiment State.

Embodiment

Hereinafter, enumerate embodiment the present invention is specifically described, but the present invention is not limited by these embodiments.

[test example 1：The mensure of the aberration of external preparation, smell and pH change]

(1) experimental liquid is prepared

Experimental liquid used in embodiment and comparative example to be entered than mixing various medicines with the interpolation shown in table 1～table 3 Row is prepared.

(2) test method

The experimental liquid of preparation is filled in the glass container of 20mL capacity, measures 25 with following shown condition determinations The aberration of the experimental liquid at DEG C, smell, pH.Afterwards, experimental liquid is transferred to 60 DEG C of thermostat, is incubated 1 week.After 1 week, will be At 60 DEG C, the experimental liquid of insulation takes out, thermostatic at 25 DEG C, carries out various mensure again.

(color difference measurement)

1mL experimental liquid is put into glass cell (CM-A97, thickness 2mm), by spectral photometric colour measuring meter CM-5 (KONICA MINOLTA, INC. system) measure aberration.Measured value is used using purified water as Δ b* during blank group.By following calculating Formula calculates the change of aberration.

(variable quantity of aberration)=(measured value of the experimental liquid after being incubated at the 60 DEG C)-(mensure of the experimental liquid before insulation Value)

(evaluation of smell)

The smell of experimental liquid is evaluated in the following manner.

±：Even if after being incubated at 60 DEG C, it is not changed in the smell before insulation.

+：After being incubated at 60 DEG C, smell smartens.

(evaluation of pH)

The pH of experimental liquid uses pH meter (HORIBA Ph METER F-52, hole field makes society of institute system) to measure.The change of pH Calculated by following calculating formulas.

(variable quantity of pH)=(pH of the experimental liquid after being incubated at 60 DEG C)-(pH of the experimental liquid before insulation)

(overall merit)

The result of the aberration, smell and pH of the experimental liquid evaluated before and after being incubated at 60 DEG C is compared, and this is compared Relatively result is evaluated in the following manner.

◎：With respect to the comparative example as comparison, the evaluation of mensure is all good；

○：With respect to the comparative example as comparison, 2 in the evaluation of mensure are good；

△：With respect to the comparative example as comparison, 1 in the evaluation of mensure is good；

×：With respect to the comparative example as comparison, 1 in the evaluation of mensure, is not had to be good.

Additionally, the comparative example as comparison is：Embodiment 1 is comparative example 1, embodiment 2 is comparative example 2, embodiment 3 is ratio Compared with example 3, embodiment 4 be comparative example 4, comparative example 5～7 and embodiment 5～6 be comparative example 3, embodiment 7 be comparative example 8.

(3) result of the test

Result of the test is as shown in Table 1 to Table 3.If with the experimental liquid (comparative example 1～4) containing only (A) composition and (B) composition Or the experimental liquid (comparative example 5～7) containing the amino acid different from (C) composition etc. is compared, in (A) composition and (B) composition Outside also contain the aberration finding experimental liquid in the experimental liquid (embodiment 1～6) of (C) composition and pH change is significantly inhibited, The tendency that the change of smell is also significantly inhibited.In addition understand, by employing the experimental liquid as (B) composition for the glucoside Add (C) composition, the suppression color of experimental liquid and the change of pH in (comparative example 8 and embodiment 7).

[table 1]

[table 2]

[table 3]

[test example 2：The mensure 1 of the aberration of external preparation]

(1) experimental liquid is prepared

Each composition is weighed according to table 4, prepares the experimental liquid of embodiment 8 and comparative example 9.The experimental liquid of embodiment 8 is equivalent to It is added with the experimental liquid of the allantoin of (C) composition in the experimental liquid of comparative example 9.

Each composition is respectively using following material.

Tranexamic acid：(HUNAN DONGTING PHARMACEUTICAL society system)

Glucan oligosaccharides：BIOECOLIA (Solabia society system)

The mould glycan of short stalk：(Lin Yuan society system)

Allantoin：(PERMACHEM AISA society system)

[table 4]

(2) test method：Evaluation by the coloring of accelerated test

The experimental liquid that every 10mL is prepared is filled to the glass container of 20mL capacity, with following shown mensure bars Part, measures the aberration of 25 DEG C of experimental liquid.Then, experimental liquid is transferred to 70 DEG C of thermostat, is incubated 1 week.After 1 week, take out At 70 DEG C, the experimental liquid of insulation, thermostatic at 25 DEG C, carries out the mensure of aberration and the visual valuation of coloring.

(color difference measurement)

1mL experimental liquid is put in glass cell (CM-A97, thickness 2mm), aberration is by spectral photometric colour measuring meter CM-5 (KONICA MINOLTA, INC. system) determines b value.Measured value is used using purified water as Δ b* during blank group.By under The calculating formula stated calculates the change of aberration.

(variable quantity (Δ b value) of aberration)=(measured value (b after accelerated test of the experimental liquid after being incubated at 70 DEG C Value))-(measured value (the b value before accelerated test) of the experimental liquid before insulation)

Represent index by the use of b value as transparent feel.Therefore Δ b value less then it represents that coloring fewer.

(visual valuation)

According to following fraction, with the coloring of the experimental liquid after visual valuation accelerated test.

1：Basic non-coloring

2：Slightly colour

3：Coloring

4：Slightly colour by force

5：Strong coloring

(3) result of the test

Result of the test is as shown in table 5.Experimental liquid containing allantoin (embodiment 8) (is compared with the experimental liquid without allantoin Compared with example 9) compare that Δ b value is little, therefore display pass through the experimental liquid of accelerated test coloring few.Additionally, containing after accelerated test The experimental liquid of allantoin, compared with the experimental liquid not containing allantoin, displays that on visual valuation coloring is few.

[table 5]

	Comparative example 9	Embodiment 8
			B value (before accelerated test)	2.34	2.68
B value (after accelerated test)	15.69	12.61
			Δ b value (after accelerated test-accelerated test before)	13.35	9.93
Visual valuation after accelerated test	4	1

[test example 3：The mensure 2 of the aberration of external preparation]

(1) preparation of experimental liquid

Each composition is weighed according to table 6, prepares the experimental liquid of embodiment 9 and comparative example 10.The experimental liquid of embodiment 9 is equivalent to Add the experimental liquid of the allantoin of (C) composition in the composition for external application of comparative example 10.

Each composition is respectively using following material.

Tranexamic acid：(HUNAN DONGTING PHARMACEUTICAL society system)

Glucan oligosaccharides：BIOECOLIA (Solabia society system)

Allantoin：(PERMACHEM AISA society system)

[table 6]

		Comparative example 10	Embodiment 9
				(A) composition	Tranexamic acid	1	1
(B) composition	Glucan oligosaccharides	1	1
				(C) composition	Allantoin	-	0.2
	Purified water	98	97.8
					Total	100	100

(2) test method：Evaluation by the coloring of accelerated test

The experimental liquid that every 10mL is prepared is filled to the glass container of 20mL capacity, with following shown mensure bars Part, measures the aberration of 25 DEG C of experimental liquid.Then, experimental liquid is transferred to 60 DEG C of thermostat, is incubated 1 week.After 1 week, take out At 60 DEG C, the experimental liquid of insulation, thermostatic at 25 DEG C, carries out the mensure of aberration and the visual valuation of coloring.

(color difference measurement)

1mL experimental liquid is put in glass cell (CM-A97, thickness 2mm), aberration is by spectral photometric colour measuring meter CM-5 (KONICA MINOLTA, INC. system) determines b value.Measured value is used using purified water as Δ b* during blank group.By under The calculating formula stated calculates the change of aberration.

(variable quantity (Δ b value) of aberration)=(measured value (b after accelerated test of the experimental liquid after being incubated at 60 DEG C Value))-(measured value (the b value before accelerated test) of the experimental liquid before insulation)

(visual valuation)

According to following fraction, with the coloring of the experimental liquid after visual valuation accelerated test.

1：Basic non-coloring

2：Slightly colour

3：Coloring

4：Slightly colour by force

5：Strong coloring

(3) result of the test

Result of the test is as shown in table 7.Experimental liquid containing allantoin (embodiment 9) and the experimental liquid not containing allantoin (comparative example 10) compares that Δ b value is little, and therefore display is few by the coloring of the experimental liquid of accelerated test.Additionally, after accelerated test Experimental liquid containing allantoin, compared with the experimental liquid not containing allantoin, displays that on visual valuation coloring is few.

[table 7]

	Comparative example 10	Embodiment 9
			B value (before accelerated test)	1.79	2.06
B value (after accelerated test)	18.36	10.6
			Δ b value (after accelerated test-accelerated test before)	16.57	8.54
Visual valuation after accelerated test	4	2

Formulation Example

Prepare external preparation according to following formula.Additionally, each numerical value of Formulation Example represents weight %.

Formulation Example 1 (toner)

Formulation Example 2 (emulsion)

Formulation Example 3 (white)

Claims (5)

1. a kind of external preparation, it contains the compound or its salt shown in (A) tranexamic acid or its salt, (B) carbohydrate, (C) formula (I),

[chemical formula 1]

In formula (I), R^aRepresent straight chained alkyl or the-NR of carbon number 7～19^dR^eShown group, R^dAnd R^eTable independently of one another Show the alkyl can with hydrogen atom or substituent, R^bAnd R^cRepresent to there is hydrogen atom, the alkyl of substituent or formula independently of one another (II) group shown in, wherein, R^bAnd R^cRing can be bonded together to form mutually, described substituent is hydroxyl, carboxyl, alkyl or formula (III) group shown in,

[chemical formula 2]

In formula (II), R^fThe alkyl that expression can be replaced by hydrogen atom or hydroxyl,

[chemical formula 3]

2. external preparation according to claim 1, wherein, the compound shown in described formula (I) is the chemical combination shown in formula (1) Thing,

[chemical formula 4]

In formula, R¹Any one in expression (2)～group shown in (23), n represents 6～18 integer,

[chemical formula 5]

[chemical formula 6]

[chemical formula 7]

3. external preparation according to claim 1, wherein, the compound shown in described formula (I) is the chemical combination shown in formula (24) Thing,

[chemical formula 8]

In formula, R^b、R^c、R^dAnd R^eWith the R in formula (I)^b、R^c、R^dAnd R^eSynonymous.

4. external preparation according to claim 1, wherein, described (C) composition is selected from N- decoyl glycine, N- caprinoyl In the group of base-L-PROLINE, N- stearyl-Pidolidone, allantoin and Alcloxa and their salt composition at least A kind of.

5. the external preparation according to any one of Claims 1 to 4, wherein, described (B) composition be selected from monose, disaccharides, At least one in the group of oligosaccharides and glucoside composition.