CN102188710A - Composition for external use - Google Patents
Composition for external use Download PDFInfo
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- CN102188710A CN102188710A CN2011100514694A CN201110051469A CN102188710A CN 102188710 A CN102188710 A CN 102188710A CN 2011100514694 A CN2011100514694 A CN 2011100514694A CN 201110051469 A CN201110051469 A CN 201110051469A CN 102188710 A CN102188710 A CN 102188710A
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Abstract
The present invention provides a composition for external use, which comprises a component (A) and a component (B). The composition has excellent absorbility of the effect component in skin. Particularly, the composition has excellent absorbility of water-soluable effective component which is absorbed through skin and has inferior absorbility in the skin. In the composition for external use, the component (A) represents glycol ether or a derivative thereof; and component (B) represents polyhydroxy acid or a pharmaceutically acceptable salt.
Description
Technical field
The present invention relates to the topical composition of the endermic absorbability excellence of effective ingredient.
Background technology
The external agent that is applicable to skin has various dosage forms such as patch, ointment, cream, lotion, solid formulation, but owing to be blocked in and be used for stoping the allotrylic horny layer that comes from the outside, be engaged in during useful component in the external agent is difficult for penetrating to the skin effectively.Therefore, for the effective ingredient that promotes skin preparations for extenal use and cosmetics has carried out various researchs to the percutaneous absorption of skin, and known several improve the chemical compound of the Percutaneously absorbable of effective ingredient.
For example, as the external agent of the Percutaneously absorbable that improves effective ingredient, known have a liposome (patent documentation 1) that contains lecithin and hydrophilic non-ionic surfactant, and the absorption that contains phospholipid and special polyol promotes compositions (patent documentation 2) etc.In addition, the known pair of ethoxydiglycol cyclohexanedicarboxyester ester has (patent documentations 3) such as permeability facilitations of excellent aqueous soluble active constituent.In addition, the applicant also absorbs the percutaneous that utilizes glycol ether and studies, and carries out the invention (patent documentation 4) that absorbs by combination glycol ether and phosphoric acid promoted percutaneous so far.
Patent documentation 1: Japanese kokai publication sho 62-95134 communique
Patent documentation 2: Japanese kokai publication hei 10-194994 communique
Patent documentation 3: TOHKEMY 2009-35497 communique
Patent documentation 4: TOHKEMY 2006-213695 communique
Summary of the invention
Problem of the present invention is, the topical composition of the absorbability excellence of effective ingredient in skin is provided.
The inventor repeats research in order to solve above-mentioned problem, find to comprise (A) glycol ether or derivatives thereof and (B) topical composition of polyhydroxy acid or its pharmaceutically useful salt can significantly improve the permeability of effective ingredient in skin.
In addition, find that also the permeability of this effective ingredient compares and can be improved synergistically with the situation of each separate constituent of above-mentioned (B) composition with above-mentioned (A) composition.
The present invention is based on that above-mentioned discovery finishes, and following topical composition is provided.
First, a kind of topical composition comprise following (A) composition and (B) composition,
(A) glycol ether or derivatives thereof; With
(B) polyhydroxy acid or its pharmaceutically useful salt.
Second, according to first described topical composition, with respect to the total amount of compositions, contain (A) composition of 0.001～70 weight % that has an appointment.
The 3rd, according to first or second described topical composition, with respect to the total amount of compositions, contain (B) composition of 0.01～25 weight % that has an appointment.
The 4th, according to any described topical composition in first～the 3rd, the glycol ether or derivatives thereof is diethylene glycol monoethyl ether or two ethoxydiglycol cyclohexanedicarboxyester ester.
The 5th, according to any described topical composition in first～the 4th, polyhydroxy acid is the chemical compound that is selected from the group that the saccharic acid by hexonic acid, tartaric acid and above-mentioned acid constitutes.
The 6th, according to any described topical composition in first～the 5th, further contain aqueous soluble active constituent.
The 7th, a kind of comprise following (A) composition and (B) compositions of composition in the application of preparation in the transdermal absorption accelerator,
(A) glycol ether or derivatives thereof; With
(B) polyhydroxy acid or its pharmaceutically useful salt.
The 8th, a kind of absorbefacient method of aqueous soluble active constituent in skin that improve, this method will comprise following (A) composition and (B) compositions and the aqueous soluble active constituent mixing of composition,
(A) glycol ether or derivatives thereof; With
(B) polyhydroxy acid or its pharmaceutically useful salt.
Comprise the topical composition of the present invention of above-mentioned (A) composition and above-mentioned (B) composition, the permeability of effective ingredient in skin is extremely good, can fully obtain the original effect of effective ingredient.Particularly, the general endermic absorbability of water soluble ingredient is poor, but topical composition of the present invention permeability, the absorbability of such water soluble ingredient all can be brought up to can the actual degree of using as cosmetics or skin preparations for extenal use.
In addition, contain the topical composition basis of acid and the combination of other compositions usually, might strengthen the skin irritation that acid causes, but topical composition of the present invention can not strengthen the skin irritation of acid, usability excellence.In addition, topical composition of the present invention does not have or almost not to the infringement of skin.
Description of drawings
Fig. 1 is the percutaneous permeability facilitation effect for the water soluble fluorescence material, the synergistic figure of two ethoxydiglycol cyclohexanedicarboxyester ester of expression and gluconic acid.
The specific embodiment
Below, the present invention is described in detail.
(A) glycol ether or derivatives thereof
Glycol ether
As glycol ether, can enumerate the monoether of ethylene glycol, diethylene glycol, propylene glycol or dipropylene glycol and methanol, ethanol or propanol.
As preferred glycol ether, can enumerate glycol monoethyl ether, ethylene glycol monoethyl ether, ethylene glycol ether, diethylene glycol monomethyl ether, diethylene glycol monoethyl ether, diglycol monotertiary propyl ether, dihydroxypropane single-ether, propylene glycol monopropyl ether, dipropylene glycol list ether, dipropylene glycol list propyl ether etc., wherein preferred glycol monoethyl ether, diethylene glycol monoethyl ether, more preferably diethylene glycol monoethyl ether.
Derivant
As the derivant of glycol ether, can enumerate the glycol ether of above-mentioned explanation and the ester of monoacid or binary acid.Wherein, preferably with the ester of binary acid.Can enumerate saturated straight chain dicarboxylic acids such as succinic acid, 1,3-propanedicarboxylic acid, adipic acid, 1,5-pentanedicarboxylic acid., suberic acid, Azelaic Acid, decanedioic acid, dodecanedioic acid as binary acid; 2,2,4-trimethyladipic acid, 2,4, saturated side chain dicarboxylic acids such as 4-trimethyladipic acid; 1,2-cyclohexane cyclohexanedimethanodibasic, 1,3-cyclohexane cyclohexanedimethanodibasic, 1, cyclic dicarboxylic acid such as 4-cyclohexane cyclohexanedimethanodibasic, phthalic acid, M-phthalic acid, p-phthalic acid (ester ring type dicarboxylic acids, aromatic dicarboxylic acid) etc.In the middle of these, from infiltration facilitation effect excellence, obtain easily and cheap viewpoint is considered, in the middle of succinic acid, adipic acid, Azelaic Acid, decanedioic acid, dodecanedioic acid and the cyclic dicarboxylic acid in the middle of the preferred saturated straight chain dicarboxylic acids 1,4-cyclohexane cyclohexanedimethanodibasic, phthalic acid, p-phthalic acid.Wherein, more preferably succinic acid, adipic acid, 1,4-cyclohexane cyclohexanedimethanodibasic, most preferably 1,4-cyclohexane cyclohexanedimethanodibasic.
The glycol ether or derivatives thereof can be used alone or make up two or more the use.
(B) polyhydroxy acid or its pharmaceutically useful salt
As polyhydroxy acid, can enumerate carbon number and be 3～15, hydroxyl value is that 2～10 (preferred 2～6) and carboxyl number are the chemical compound of 1～2 (preferred 1).
As the concrete example of this polyhydroxy acid, can enumerate the such dihydroxypropionic acid of glyceric acid (hydroxyl value 2, carboxyl number 1); Erythronic acid, the such trihydroxy-butyric acid (hydroxyl value 3, carboxyl number 1) of threonic acid THREONIC ACID.; Ribonic acid, arabonic acid, xylonic, the such tetrahydroxy valeric acid (hydroxyl value 4, carboxyl number 1) of LYXONIC ACID; Allonic acid, altronic acid, gluconic acid, mannonic acid, gulonate, idonic acid, galactobionic acid Galactonic acid, the such hexonic acid (hydroxyl value 5, carboxyl number 1) of talonic acid; Glucoheptonic acid, the such hexahydroxy enanthic acid (hydroxyl value 6, carboxyl number 1) of galactoheptose acid; Tartaric acid (hydroxyl value 2, carboxyl number 2) etc.In addition, the saccharic acid of the such sugar of above-mentioned polyhydroxy acid and galactose, glucose, maltose is also contained in the polyhydroxy acid of the present invention.
Wherein, the saccharic acid (particularly lactobionic acid, 4-O-alpha-D-Glucopyranosyl-D-gluconic acid) of the such sugar of preferred hexonic acid (particularly gluconic acid), tartaric acid or these acid and galactose, glucose, maltose.
For salt,, can enumerate for example sodium salt, potassium salt, zinc salt, iron salt etc. so long as pharmaceutically useful salt gets final product.
Polyhydroxy acid or its pharmaceutically useful salt can be used alone or make up two or more the use.
(A) composition and (B) preferred compositions of composition
As (A) composition and (B) preferred compositions of composition, can enumerate the combination shown in the following table 1.
[table 1]
| (A) composition | (B) composition |
| Diethylene glycol monoethyl ether | Gluconic acid |
| Diethylene glycol monoethyl ether | Lactobionic acid |
| Diethylene glycol monoethyl ether | 4-O-alpha-D-Glucopyranosyl-D-gluconic acid |
| Diethylene glycol monoethyl ether | Tartaric acid |
| Two ethoxydiglycol cyclohexanedicarboxyester ester | Gluconic acid |
| Two ethoxydiglycol cyclohexanedicarboxyester ester | Lactobionic acid |
| Two ethoxydiglycol cyclohexanedicarboxyester ester | 4-O-alpha-D-Glucopyranosyl-D-gluconic acid |
| Two ethoxydiglycol cyclohexanedicarboxyester ester | Tartaric acid |
(A) composition and (B) consumption of composition
The content of above-mentioned (A) composition is with respect to preferably about 0.001～70 weight % of the total amount of compositions, 0.01～60 weight % more preferably from about, further preferred about 0.1～50 weight %, preferred especially about 0.1～30 weight %.If when the content of glycol ether or derivatives thereof in above-mentioned scope, then can obtain sufficient osmotic effect, can obtain good usability.
The content of above-mentioned (B) composition is with respect to preferably about 0.01～25 weight % of the total amount of compositions, more preferably from about 0.05～15 weight %, especially preferably about 0.1～5 weight %.If when the content of polyhydroxy acid or its pharmaceutically useful salt in above-mentioned scope, then can obtain sufficient osmotic effect, can obtain almost non-stimulated good usability.
In addition, as the glycol ether or derivatives thereof of (A) composition with as the ratio of the polyhydroxy acid of (B) composition or its pharmaceutically useful salt can for, with respect to the glycol ether or derivatives thereof of conduct (A) composition of 1 weight portion, be about 0.004～250 weight portion as polyhydroxy acid or its pharmaceutically useful salt of (B) composition.If (A) composition then can obtain sufficient synergy with (B) components in proportions aspect osmosis in above-mentioned scope.
Effective ingredient
Topical composition of the present invention can contain various effective ingredient.Kind to effective ingredient does not limit especially, can be in slightly water-soluble composition, the water soluble ingredient any one, usually the water soluble ingredient of preferred poor permeability in skin.
In the present invention, " water soluble ingredient " be meant, served as when thermal agitation mixes 30 seconds at interval with 5 minutes in water, under 20 ℃ of temperature, and (promptly 5 minutes serve as that vibration at interval mixed after 6 times in 30 seconds) dissolves the composition more than the 1g/L in 30 minutes.
Effective ingredient can be used alone, and perhaps makes up two or more the use.
As the concrete example that contains aqueous soluble active constituent, can enumerate for example antioxidant content, anti-aging composition, anti-inflammatory component, whitening composition, cell activation composition, vitamins, the blood circulation that are used as cosmetic composition usually and promote composition, the composition of preserving moisture, prevention and/or the composition of repair, anti-saccharifying composition, peptide or derivatives thereof, aminoacid or derivatives thereof, water solublity sphingolipid, hydroquinone glucosides and esters thereof etc. with DNA damage.
As the water solublity antioxidant content, can enumerate composition from plant (for example Fructus Vitis viniferae, Radix Ginseng, Symphytum officinale etc.); Procyanidin, ascorbic acid and derivant thereof, glucityl Hesperidin etc.
As water solublity anti-aging composition, can enumerate hydrolyzed soybean protein, Rhizoma Curcumae Longae extract etc.
As the water solublity anti-inflammatory component, can enumerate composition from plant (for example Symphytum officinale); Allantoin, glycyrrhizic acid or derivatives thereof etc.
As the water solublity whitening composition, can enumerate for example arbutin; Hydroquinone; Kojic acid; The butyl resorcinol; The ascorbic acid or derivatives thereof; The plant component of tranamic acid etc. or Pear Power effect (for example plant extract).
As water solublity cell activation composition, can enumerate composition from plant (for example Pericarpium Citri tangerinae); Amino acids such as γ-An Jidingsuan, episilon amino caproic acid; Vitaminss such as thiamine, riboflavin, pyridoxine hydrochloride, pantothenic acid class; Alpha-hydroxy such as glycol acid, lactic acid acids etc.
As water-soluble vitamins, can enumerate vitamin B2 classes such as riboflavin; Nicotinic acid classes such as niacinamide usp; Vitamin c class such as ascorbic acid (ascorbic acid and derivant thereof); Vitamin B1 classes such as thiamine salt hydrochlorate, thiamine cetyl hydrochlorate, thiamine rhodanate, thiamine dilauryl hydrochlorate, thiamine nitrate, thiamine monophosphate, thiamine lysinate, thiamine triphosphate, thiamine phosplate phosphate, thiamine phosplate, thiamine bisphosphate, thiamine bisphosphate hydrochlorate, thiamine triguaiacyl phosphate, thiamine triguaiacyl phosphate monophosphate; Vitamin B6 classes such as pyridoxine hydrochloride, acetic acid pyridoxol, pyridoxal hydrochloride, 5 '-pyridoxal 5-phosphate, hydrochloric acid pyridoxamine; Vitamin B12 classes such as cobalamin; Folic acid classes such as folic acid; The pantothenic acid class of pantothenylol etc.; Biotin classes such as biotin; In addition, biostearin sample effector such as carnitine etc.
As water solublity blood circulation facilitation composition, can enumerate composition from plant (for example Radix Ginseng); The glucityl Hesperidin.
As the water solublity composition of preserving moisture, can enumerate composition from plant (for example Herba Imperatae); Aminoacid that alanine is such and derivant thereof; Collagen, such protein or peptide and the hydrolysate thereof of elastin laminin; The polyhydric alcohol that glycerol is such; The sugar alcohol that Sorbitol is such; The phospholipid that lecithin is such; The mucopolysaccharide that hyaluronic acid is such; The composition that lactic acid is such from NMF; Polyglutamic acid; MPC polymer (for example, LIPIDURE (registered trade mark) etc.) etc. has the macromolecule of phospholipid polar group; Polyoxy propylidene methyl glucosamine; Trimethyl glycine (betanin); The ethoxy urea; Sorbitol etc.
As water miscible composition, can enumerate composition from animal (for example artemia) with prevention and/or repair of DNA damage; Composition from plant (for example Radix Ranunculi Ternati); Nucleic acid compositions such as DNA, DNA salt, RNA, RNA salt.
As the anti-saccharifying composition of water solublity, can enumerate for example plant extract (for example, axil is given birth to Herba Buddlejae Lindleyanae leaf extract (water, ethanol equal solvent are given birth to the Herba Buddlejae Lindleyanae leaf to axil and carried out the material that extracting obtains, and are also referred to as the Herba Buddlejae Lindleyanae extract)); Fruit, fruit juice or their extract of Indian currant (ア system ラ one) (more than, TOHKEMY 2006-028090 number, TOHKEMY 2006-62989 number etc.); L-arginine (TOHKEMY 2001-039816); Carnosine (" the disconnected マ ニ ュ ア Le of the up-to-date skin Skin of beauty treatment め ?", Off レ グ ラ Application ス ジ ャ one Na Le society, distribution on August 15th, 2006); The extract of grape leaf (TOHKEMY 2006-273811 number); The extract of seed of Fructus Vitis viniferae (TOHKEMY 2003-212770 number); Folium Perillae, Herba thymi vulgaris, Herba Rosmarini Officinalis extract (above, TOHKEMY 2004-250445 number) etc.
As the water-soluble peptide or derivatives thereof, can enumerate elastin laminin and decompose peptide, collagen decomposition peptide, soybean protein decomposition peptide etc.
As the water-soluble amino acid or derivatives thereof, can enumerate betanin (trimethyl glycine), arginine, lysine, serine, glycine, threonine, glutamic acid, glutamine, agedoite, aspartic acid, cysteine, cystine, histidine, taurine, γ-An Jidingsuan, GABOB, carnitine, carnosine etc.
As water solublity hydroquinone glucosides and esters thereof, can enumerate arbutin, alpha-arbutin etc.
In addition, also preferred ferulate and water soluble ingredients such as derivant, intacellin, glutathion, Hinokitiol, caffeine, rutin and glucosides thereof, Hesperidin and glucosides thereof thereof.
As particularly preferred aqueous soluble active constituent, can enumerate ascorbic acid, ascorbic acid derivates, glycyrrhizic acid, arbutin, hydroquinone, kojic acid, butyl resorcinol, glucityl Hesperidin, elastin laminin decomposition peptide, soybean protein decomposition peptide, nicotiamide, carnosine etc.
In addition, effective ingredient can also be the composition as the effective ingredient use of medicine.Topical composition of the present invention is considered from the aspect that can be suitable as smears, patch, except the antiinflammatory that acts on skin, disinfectant, antibacterial, wound healing agent etc., the analgesics that can absorb through skin, antipyretic, anti-arrhythmic agents, hypotensive agent, bronchodilator, antitumor agent, anti-tussive agents, diuretic, hormone agent etc. widely composition as the effective ingredient that contains aqueous soluble active constituent.
Effective ingredient also can be electronegative composition, even such composition is so long as topical composition of the present invention just can penetrate to the skin effectively or by skin absorbs.
In addition, effective ingredient is preferably the composition of lower molecular weight, and for example molecular weight is 50～1000, particularly can further penetrate to the skin effectively in 50～500 o'clock or by skin absorbs.
Content of effective is different and different according to its kind, but with respect to the total amount of topical composition, more than preferred about 0.001 weight %, more preferably from about more than the 0.01 weight %, and then more preferably more than the 0.1 weight %.In addition, content of effective is with respect to the total amount of topical composition, below preferred about 40 weight %, more preferably from about below the 30 weight %, and then more preferably from about below the 20 weight %.Effective ingredient contains such amount, also can permeate effectively or absorb in the skin.
Other compositions
Topical composition of the present invention can be with the substrate that is generally used for cosmetics or carrier and the additive that adds as required as cosmetic composition.
Use form to cosmetic composition does not limit especially, can enumerate for example astringent, emulsion, cream, beautifying liquid, Sun block cosmetics, facial film, hand cream, health breast, the such basic cosmetics of health frost; Cleansing milk, cleansing product, bath foam, shampoo, hair conditioner, the such washing of nursing frost apply some make up etc.
In addition, can enumerate liquor, suspending agent, Emulsion, cream, ointment, gel etc. as the form of cosmetic composition.Wherein, consider preferred Emulsion, cream, ointment, gel from the aspect that annexs moistening effect.
In addition, in the scope of not damaging effect of the present invention, can add for example surfactant, thickening agent, preservative agent, pH regulator agent, chelating agen, stabilizing agent, stimulation palliative, antiseptic, coloring agent, dispersant, spice, pearly luster imparting agent etc. in the cosmetic composition and can add known additive in the cosmetics to.Additive can be used alone or make up two or more the use.
Topical composition of the present invention can be with the substrate that is generally used for medicine external agent or carrier and the additive that adds as required as pharmaceutical composition.
Form to pharmaceutical composition does not limit especially, can enumerate for example liquor, suspending agent, Emulsion, cream, ointment, gel, liniment, lotion or paste etc.
In addition, in the scope of not damaging effect of the present invention, can add for example antioxidant, antiseptic, stabilizing agent, chelating agen, amphoteric surfactant, cationic surfactant, wetting agent, Reducing agent, pH regulator agent, powdery type, UV absorbent, whitening agent, buffer agent or inorganic salts, propellant, lower alcohol (ethanol, isopropyl alcohol etc.), freshener, aromatic, spice or pigment etc. in the pharmaceutical composition and can add known additive in the medicine external agent to.Additive can be used alone or make up two or more the use.
Using method
Topical composition of the present invention can be coated with common using method, access times according to the kind of effective ingredient, dosage form etc.
In addition, as mentioned above,, can improve the permeability of effective ingredient in skin and hair, therefore contain (A) glycol ether or derivatives thereof by combination (A) composition and (B) composition; (B) compositions of the above-mentioned explanation of polyhydroxy acid or its pharmaceutically useful salt can be used to prepare transdermal absorption accelerator.
In addition, the present invention comprises the absorptive method of raising aqueous soluble active constituent in skin, and this method will contain (A) composition and (B) compositions and effective ingredient (particularly aqueous soluble active constituent) mixing of composition.
[embodiment]
Below, enumerate embodiment and further describe the present invention, but the present invention is not limited by these embodiment.
(1) evaluation of percutaneous permeability
(1-1) preparation of topical composition sample
Prepared the topical composition of forming shown in the following table 2.
[table 2]
Unit in the table 2 is g.
In addition, fluorescein sodium is the water soluble fluorescence material.
(1-2) dermal osmosis test method
Freezing Corii Sus domestica (5 centimetres of about 3 cm x) was left standstill 2 hours in 33 ℃ of calorstats, thaw and constant temperatureization.This Corii Sus domestica is placed in the plate, left standstill 2 hours with putting into 33 ℃ of calorstats under the aluminium foil light blocking state after closing the lid, fully apply topical composition afterwards.
Then, in order to measure the fluorescence intensity that is present in the fluorescein sodium in this part horny layer, use 1.8 centimetres of wide adhesive tapes to carry out adhesive tape sticking 15 times.The adhesive tape that is stained with on the horny layer that adhesive tape sticking is crossed carries out 30 minutes ultrasonic Treatment, as the fluorescent strength determining sample after being recovered in the conical pipe that adds the alcoholic acid 10mL capacity of 3mL one by one.Each sample is directly got 100 μ L respectively in 96 hole microwell plates, utilize fluorescence microplate reader under excitation wavelength 485nm, mensuration wavelength 538nm, to measure fluorescence intensity.The cuticular fluorescence intensity level that obtains from the 4th of skin surface number to the 15 adhesive tape is accumulated as the infiltrative index in skin.And, from the fluorescence intensity level of the adhesive tape of first to the 3rd of skin surface number since the state of coating per sample produce big error and by except, therefore be not included in the accumulation.And the Corii Sus domestica of the freezing Corii Sus domestica that uses in this test for obtaining as residue from edible Carnis Sus domestica is not the Corii Sus domestica of obtaining for this test is massacred again.
(1-3) result
The dermal osmosis result of the test is illustrated among Fig. 1.The longitudinal axis of Fig. 1 is the relative value who becomes the fluorescence intensity accumulated value of permeability index, for will not comprising the relative value that any one the value of topical composition of comparative example 3 in two ethoxydiglycol cyclohexanedicarboxyester ester and the gluconic acid was made as at 100% o'clock.
In the topical composition of the embodiment 1 that contains two ethoxydiglycol cyclohexanedicarboxyester ester and gluconic acid, compare with the topical composition of comparative example 2 with the comparative example 1 that contains each chemical compound separately, fluorescence intensity accumulated value as the permeability index is big as can be known, and the permeability in skin is very high.In addition, by making up two ethoxydiglycol cyclohexanedicarboxyester ester and gluconic acid, percutaneous permeability is improved synergistically as can be known.
(2) evaluation of excitement
(2-1) preparation of sample
The sample of forming shown in the preparation following table 3.
[table 3]
Unit in the table 3 is g.
(2-2) test method
The adult is after (male, women) one group of three volunteer wash one's face with cleansing milk, at around eyes coated sample 10 μ L, and after excitement estimated, sample washed off.
Excitement is estimated by following four standards.
0 is non-stimulated
1 sense stimulation slightly
2 feel faint stimulation
3 sensation intense stimulus
(2-3) result
The result is illustrated in the following table 4.
[table 4]
| Embodiment 2 | Comparative example 4 | Comparative example 5 | Comparative example 6 | Comparative example 7 | |
| The volunteer 1 | 0 | 0 | 2 | 0 | 0 |
| The volunteer 2 | 1 | 0 | 3 | 0 | 0 |
| The volunteer 3 | 0 | 0 | 2 | 3 | 0 |
When lactic acid made up with two ethoxydiglycol cyclohexanedicarboxyester ester, the excitement that lactic acid causes strengthened, even but make gluconic acid and two ethoxydiglycol cyclohexanedicarboxyester ester combinations also can not strengthen excitement.Hence one can see that, and the topical composition that contains gluconic acid and two ethoxydiglycol cyclohexanedicarboxyester ester has excellent usability.
The prescription example
Shown in the prescription of topical composition of the present invention is for example following.Numerical value unit in the prescription example is " weight % ".
Example of formulations 1 washing liquid
Example of formulations 2 beautifying liquids
Example of formulations 3 beautifying liquids
Example of formulations 4 beautifying liquids
Example of formulations 5 emulsions
Example of formulations 6 emulsions
Example of formulations 7 washing liquids
Example of formulations 8 cream
Example of formulations 9 cream
Example of formulations 10 washing liquids
Example of formulations 11 emulsions
Example of formulations 12 beautifying liquids
Example of formulations 13 beautifying liquids
Example of formulations 14 beautifying liquids
Example of formulations 15 cream
Example of formulations 16 washing liquids
Example of formulations 17 emulsions
Topical composition of the present invention can be suitable as cosmetics or medicine external agent etc. because the permeability of water soluble ingredient in skin is high.
Claims (8)
1. topical composition comprises following (A) composition and (B) composition,
(A) glycol ether or derivatives thereof; With
(B) polyhydroxy acid or its pharmaceutically useful salt.
2. topical composition according to claim 1 with respect to the total amount of compositions, contains (A) composition of 0.001～70 weight % that has an appointment.
3. topical composition according to claim 1 and 2 with respect to the total amount of compositions, contains (B) composition of 0.01～25 weight % that has an appointment.
4. according to any described topical composition in the claim 1～3, the glycol ether or derivatives thereof is diethylene glycol monoethyl ether or two ethoxydiglycol cyclohexanedicarboxyester ester.
5. according to any described topical composition in the claim 1～4, polyhydroxy acid is the chemical compound that is selected from the group that the saccharic acid by hexonic acid, tartaric acid and above-mentioned acid constitutes.
6. according to any described topical composition in the claim 1～5, further contain aqueous soluble active constituent.
7. one kind comprises following (A) composition and (B) application of compositions in the preparation transdermal absorption accelerator of composition,
(A) glycol ether or derivatives thereof; With
(B) polyhydroxy acid or its pharmaceutically useful salt.
8. one kind is improved the absorbefacient method of aqueous soluble active constituent in skin, and this method will comprise following (A) composition and (B) compositions and the aqueous soluble active constituent mixing of composition,
(A) glycol ether or derivatives thereof; With
(B) polyhydroxy acid or its pharmaceutically useful salt.
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| JP2010044723 | 2010-03-01 | ||
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| CN (1) | CN102188710A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN110114061A (en) * | 2016-12-28 | 2019-08-09 | 小林制药株式会社 | Topical composition |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5826075B2 (en) * | 2012-03-08 | 2015-12-02 | 株式会社ナリス化粧品 | Cosmetics |
| JP6813165B2 (en) * | 2016-07-26 | 2021-01-13 | ピアス株式会社 | Pseudo eyebrow forming cosmetics |
| JP6813166B2 (en) * | 2016-07-26 | 2021-01-13 | ピアス株式会社 | Tanning agent |
| JP6195402B1 (en) * | 2017-03-17 | 2017-09-13 | ウィントレーディング株式会社 | Eyebrows formation method |
| JP7071830B2 (en) * | 2018-01-30 | 2022-05-19 | 株式会社コーセー | External skin preparation or cosmetics |
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| CN101102797A (en) * | 2005-01-07 | 2008-01-09 | 日本乐敦制药株式会社 | Composition for external use |
| CN101553213A (en) * | 2006-12-06 | 2009-10-07 | 尼普洛外用药品株式会社 | Pharmaceutical composition for external application and adhesive skin patch |
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| JP2001064205A (en) * | 1999-06-25 | 2001-03-13 | Dai Ichi Seiyaku Co Ltd | Medication composition |
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- 2011-03-01 CN CN2011100514694A patent/CN102188710A/en active Pending
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| CN101102797A (en) * | 2005-01-07 | 2008-01-09 | 日本乐敦制药株式会社 | Composition for external use |
| CN101553213A (en) * | 2006-12-06 | 2009-10-07 | 尼普洛外用药品株式会社 | Pharmaceutical composition for external application and adhesive skin patch |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN110114061A (en) * | 2016-12-28 | 2019-08-09 | 小林制药株式会社 | Topical composition |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2011201848A (en) | 2011-10-13 |
| JP5739679B2 (en) | 2015-06-24 |
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