CN1660081A - skin topical - Google Patents
skin topical Download PDFInfo
- Publication number
- CN1660081A CN1660081A CN 200510003793 CN200510003793A CN1660081A CN 1660081 A CN1660081 A CN 1660081A CN 200510003793 CN200510003793 CN 200510003793 CN 200510003793 A CN200510003793 A CN 200510003793A CN 1660081 A CN1660081 A CN 1660081A
- Authority
- CN
- China
- Prior art keywords
- weight
- ascorbic acid
- salt
- skin
- glycol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 230000000699 topical effect Effects 0.000 title description 2
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims abstract description 150
- 238000002360 preparation method Methods 0.000 claims abstract description 82
- 229960005070 ascorbic acid Drugs 0.000 claims abstract description 75
- 235000010323 ascorbic acid Nutrition 0.000 claims abstract description 74
- 239000011668 ascorbic acid Substances 0.000 claims abstract description 74
- KWIUHFFTVRNATP-UHFFFAOYSA-N Betaine Natural products C[N+](C)(C)CC([O-])=O KWIUHFFTVRNATP-UHFFFAOYSA-N 0.000 claims abstract description 54
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- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 57
- 150000003839 salts Chemical class 0.000 claims description 54
- -1 glycol ethers Chemical class 0.000 claims description 38
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims description 37
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Abstract
Provided is a skin care preparation for external use by solubilizing water soluble ascorbic acid stably. This preparation is obtained by blending a low molecular betaine with a skin care preparation for external use containing water soluble ascorbic acid, a glycol ether or a specific polyhydric alcohol for solubilizing the water soluble ascorbic acid stably. Thereby, it is possible to obtain the preparation blended with the water soluble ascorbic acid in a high concentration stably, and to exhibit various activities that the ascorbic acid originally has, in accordance with its blended amount. Also, it is possible to provide the preparation without having a sticky feeling after the application on the skin and having a moist feeling and a good compatibility to the skin.
Description
Technical field
The present invention relates to a kind of ascorbic acid or liquefiable skin preparations for extenal use of its salt of stably making.
Background technology
As everyone knows, ascorbic acid is brought into play so-called anti-inflammatory effect, acne and is improved the synthetic cell-stimulating effects of biotic component such as effect, whitening effect, antiageing effect, antioxidant effect, promotion collagen, suppresses the cell injury of keratinization of epidermis cell under action of ultraviolet radiation or the various effects of the effect of DNA damage, wishes these effects to occur and is widely used as skin preparations for extenal use.But oxidation takes place in ascorbic acid easily under the medium situation that has water to exist of aqueous solution, so seek to reduce the water in the preparation, but problem is a spot of water ascorbic acid can be dissolved fully.For this reason, research is used for making at the skin preparations for extenal use of aqueous the SOME METHODS of ascorbic acid sufficiently solubleization, for example, as everyone knows in the solution that constitutes by the ascorbic acid below 15%, 10～15% water, 47～55% ethoxydiglycol, 22～29% propylene glycol and spice, make stable the dissolving of ascorbic acid (patent documentation 1:WO02/19972)
In addition, in water-free skin preparations for extenal use, also research is used to make the stably liquefiable method of ascorbic acid, for example, in the non-aqueous media that contains stabilization agents such as the dihydroxylic alcohols carrier that constitutes by propylene glycol and butanediol and ethoxydiglycol, make ascorbic acid stably can dissolve (patent documentation 2:WO00/76547).
On the other hand, low molecule betaine by the trimethyl glycine representative, be widely used in skin preparations for extenal use as wetting agent, for example by share carbamide and low molecule betaine, can obtain very excellent pachylosis and improve effect (the patent documentation spy opens flat 9-48720 communique), by cooperating whitening composition, low molecule betaine, silicone oil, improve the percutaneous absorbability (patent documentation 4: the spy opens the 2001-89321 communique) of whitening agent etc.But, about dissolving of ascorbic acid, without any opinion.
Summary of the invention
The present invention will provide a kind of can make in the skin preparations for extenal use that contains ascorbic acid or its salt that ascorbic acid or its salt stably can dissolve, and the skin preparations for extenal use that can carry out the cooperation of the ascorbic acid of high concentration or its salt thus, as problem.
Present inventors etc. concentrate on studies in order to solve above-mentioned problem, found that, in the skin preparations for extenal use that contains ascorbic acid or its salt and glycol ethers or special polyol, by share low molecule betaine, ascorbic acid or its salt stably can be dissolved, the cooperation of high concentration becomes possibility, and then becomes efficient external agent.
That is, the present invention is the skin preparations for extenal use shown in following (1)～(7).
(1) contain the skin preparations for extenal use of following chemical compound:
(A) ascorbic acid or its salt 3 weight % above,
(B) from glycol, glycol ethers, glycerol and diglycerol, select more than a kind or 2 kinds,
(C) low molecule betaine and
(D) water.
(2) contain the skin preparations for extenal use of following chemical compound:
(A) ascorbic acid or its salt 3 weight % above,
(B) from glycol, glycerol and diglycerol, select more than a kind or 2 kinds,
(C) glycol ethers
(D) low molecule betaine and
(E) water.
(3) low molecule betaine is (1) or (2) described skin preparations for extenal use of trimethyl glycine.
(4) contain any described skin preparations for extenal use in (1)～(3) of water 5～35 weight %.
(5) contain the skin preparations for extenal use of following chemical compound:
(A) ascorbic acid or its salt 10～20 weight %,
3～25 weight % more than a kind or 2 kinds that (B) from glycol, glycerol and diglycerol, select,
(C) glycol ethers 45～55 weight %
(D) low molecule betaine 1～5 weight % and
(E) water 5～25 weight %.
(6) contain the skin preparations for extenal use of following chemical compound:
(A) ascorbic acid or its salt 15～20 weight % above,
4～21 weight % more than a kind or 2 kinds that (B) from glycol, glycerol and diglycerol, select,
(C) glycol ethers 50～53 weight %
(D) low molecule betaine 2～4 weight % and
(E) water 10～20 weight %.
(7) further contain any described skin preparations for extenal use at least a (1)～(6 of from whitening composition, anti-inflammatory composition, antioxidant content, aging resistance composition and the composition of preserving moisture, selecting).
Wherein, in this manual, short ofly mention that especially % is meant weight %.
In the present invention, in the skin preparations for extenal use that contains ascorbic acid or its salt, glycol ethers or special polyol,, ascorbic acid or its salt stably can be dissolved by cooperating low molecule betaine.For this reason, can access the skin preparations for extenal use with ascorbic acid or the cooperation of its salt high-concentration stable, ascorbic acid can effectively be brought into play the various effects that it just had originally according to its use level.In addition, can be modulated at the sense and moist feeling and the preparation good to the adaptability of skin are arranged of being applied to not occur being clamminess behind the skin.
The specific embodiment
The ascorbic acid that uses among the present invention can use in the goods or cosmetic field outside medicine, medicine, and as the composition of skin preparations for extenal use and commercially available ascorbic acid, they typically refer to the goods of L body.
In addition, ascorbic acid can use as the salt that pharmaceutically allows, can be exemplified as with the salt of alkaline organic (for example, the salt of front three amine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, pyridiniujm etc. and tertiary amine, alkaline ammonium salt such as arginine etc.) and salt (for example, the ammonium salt of inorganic base, alkali metal salt such as sodium salt, potassium salt, alkali salt such as calcium salt, magnesium salt, aluminum salt etc.) etc., particularly preferred salt is sodium salt, potassium salt.Specifically, can be exemplified as sodium ascorbate, potassium ascorbate etc.
In the present invention, can be used in combination ascorbic acid or its salt more than a kind or 2 kinds.
Skin preparations for extenal use of the present invention can make stable the dissolving of ascorbic acid by cooperating low molecule betaine, so the use level of ascorbic acid is with respect to the skin preparations for extenal use total weight, preferably can be 3～30 weight %, can be in this scope as required the various effects of ascorbic acid or the purposes of skin preparations for extenal use suit to select.In view of effect of the present invention, further preferred 5～25 weight %, the scope of preferred especially 5～20 weight %.
In the present invention, glycol is meant the composition that is used as skin preparations for extenal use in goods outside medicine, medicine or the cosmetic field and is the dihydroxylic alcohols of liquid down at 25 ℃, for example uses general formula C
nH
2n(OH)
2The dihydroxylic alcohols of expression or the condensation polymer of single or the above-mentioned dihydroxylic alcohols more than 2 kinds etc.Specifically, can be exemplified as ethylene glycol, propylene glycol, trimethylene, 1,2-butanediol, 1,3-butanediol, 2,3-butanediol, isopropyl alcohol, 1,2-pentanediol, 1,2-hexanediol, ethohexadiol etc., as condensation polymer, can be exemplified as diethylene glycol, 2,2'-ethylenedioxybis(ethanol)., tetraethylene glycol (TEG), dipropylene glycol, tripropylene glycol etc.Preferred propylene glycol, 1,3 butylene glycol.
In addition, glycerol that uses among the present invention and diglycerol are the known compound that is used for skin preparations for extenal use etc. more.
If the use level of the glycol of Shi Yonging, glycerol or diglycerol is proved effective the present invention in the present invention, then be not particularly limited, can consider the usability of skin or effect and suitable the selection used, but with respect to whole skin preparations for extenal use, usually can be 1～95 weight %, preferred 5～90 weight %, more preferably 10～80 weight %, preferred especially 15～65 weight %.
These glycol, glycerol and diglycerol can make up more than a kind or 2 kinds and use, total amount as glycol, glycerol and diglycerol, with respect to whole skin preparations for extenal use, preferred 30～95 weight %, more preferably 40～90 weight %, further preferred 45～80 weight %, preferred especially 50～75 weight %, if the present invention is proved effective, then is not particularly limited.
Glycol ethers among the present invention is meant that the chemical compound of etherificate takes place one of hydroxyl in the glycol or both, if be used as the chemical compound of skin preparations for extenal use in goods outside medicine, medicine or the cosmetic field, then be not particularly limited, glycol is to be the dihydroxylic alcohols of liquid down at 25 ℃, for example can be to use general formula C
nH
2n(OH)
2The dihydroxylic alcohols or the condensation polymer single or the above-mentioned dihydroxylic alcohols more than 2 kinds of expression.Can be exemplified as ethylene glycol mono-ether, monoalkyl ethers of diethylene glycol, propylene glycol monoether, dipropylene glycol monoether etc., preferred monoalkyl ethers of diethylene glycol.Specifically, can be exemplified as glycol monomethyl methyl ether, ethylene glycol monomethyl ether, glycol monomethyl propyl ether, diglycol monotertiary methyl ether, carbiphene, diglycol monotertiary propyl ether, diglycol monotertiary butyl ether, dihydroxypropane single-ether, propylene glycol monopropyl ether, dipropylene glycol list ethylether, dipropylene glycol list propyl ether etc., preferred diglycol monotertiary methyl ether, carbiphene, diglycol monotertiary propyl ether.
If the use level of the glycol ethers of using among the present invention is proved effective the present invention, then be not particularly limited, can consider the usability of skin or effect and suitable the selection used, but with respect to whole skin preparations for extenal use, usually can be 1～95 weight %, preferred 5～90 weight %, more preferably 10～80 weight %, preferred especially 15～65 weight %.
In the present invention, about the use level of from glycol, glycol ethers, glycerol and diglycerol, selecting more than a kind or 2 kinds, as their total amount, with respect to whole skin preparations for extenal use, preferred 30～95 weight %, more preferably 40～90 weight %, further preferred 45～80 weight %, preferred especially 50～75 weight % if the present invention is proved effective, then are not particularly limited.
And, that more preferably selects from glycol, glycerol and diglycerol is used in combination with glycol ethers more than a kind or 2 kinds, with the total amount of use level as them, with respect to whole skin preparations for extenal use, preferred 30～95 weight %, more preferably 40～90 weight %, further preferred 45～80 weight %, preferred especially 50～75 weight % if the present invention is proved effective, then are not particularly limited.
By containing low molecule betaine and glycol ethers etc., ascorbic acid or its salt is stable dissolving in preparation with the external agent for skin of the present invention.
Low molecule betaine among the present invention be meant molecular weight below 200 and intramolecularly form zwitterionic chemical compound, specifically, can be exemplified as quaternary ammonium base, quaternary phosphonium hydroxide, uncle's sulfonium base etc., they show the character as surfactant hardly.Wherein preferably use the N of following formula (1) expression, N, N-trialkyl aminoacid.
(in the formula, R
1, R
2And R
3Represent the alkyl of carbon number 1～6 independently of each other, n represents 1～6.)
As R
1～R
3, can be extensive use of the straight or branched alkyl of carbon number 1～6.Promptly, can distinguish illustration methyl, ethyl, propyl group, isopropyl, butyl, isobutyl group, sec-butyl, the tert-butyl group, amyl group, isopentyl, neopentyl, tertiary pentyl, hexyl, isohesyl, 3-methyl amyl, 2,2-dimethylbutyl or 2,3-dimethylbutyl etc.Wherein, R
1～R
3Can be identical, also can be different.
Specifically, can be exemplified as the trimethyl glycine, triethyl group glycine, tripropyl glycine, triisopropyl glycine, trimethyl-Beta-alanine of n=2, trimethyl-γ-An Jidingsuan of n=3 of n=1 etc., preferred trimethyl glycine.
In addition, can replace these low molecule betaines, specifically, can be exemplified as the N of n=1, N, N-trimethylalanine, N, N, N-triethyl group alanine, N, N, N-triisopropyl alanine, N, N, N-trimethyl methylalanine, carnitine, acetylcarnitine etc., preferred carnitine.
In skin preparations for extenal use of the present invention, the use level of low molecule betaine is with respect to the skin preparations for extenal use gross weight, preferred 0.5～10 weight %, the various effects of ascorbic acid as required or its salt or the purposes of skin preparations for extenal use can suit to select in this scope.In view of effect of the present invention, further preferred 0.5～9 weight %, the scope of preferred especially 1～8 weight %.Sometimes then can not bring into play effect less than 0.1 weight %, in addition, if surpass 10 weight %, usability variation sometimes.
Skin preparations for extenal use of the present invention can further suppress separating out of ascorbic acid or its salt by hydrous water.
If the use level of the glycol ethers that the present invention uses is proved effective the present invention, then be not particularly limited, can consider the usability of skin or effect and suitable the selection used, but with respect to whole skin preparations for extenal use, usually can be 1～95 weight %, preferred 5～90 weight %, more preferably 10～80 weight %, preferred especially 15～65 weight %.
The cooperation ratio of the water in skin preparations for extenal use of the present invention, the unstability in aqueous solution in view of ascorbic acid or its salt, with respect to 1 weight portion of ascorbic acid or its salt, its cooperation ratio can be below 2 weight portions, more preferably below 1.5 weight portions, further below preferred 1 weight portion.When surpassing 2 weight portions, the trend that can not allow ascorbic acid or its salt to decompose is arranged.
If the use level of the water that cooperates in skin preparations for extenal use of the present invention is proved effective the present invention, then be not particularly limited, but with respect to whole skin preparations for extenal use, its use level is 5～35 weight %.Can in this scope, suit to select to use the viewpoint of the stability of do not associate ascorbic acid or its salt, preferred 5～20 weight %, the scope of preferred especially 8～13 weight %.
As the preferred implementation of skin preparations for extenal use of the present invention, further preferably make up each composition with following use level.
(A) ascorbic acid or its salt 10～20 weight % above,
3～25 weight % more than a kind or 2 kinds that (B) from glycol, glycerol and diglycerol, select,
(C) glycol ethers 45～55 weight %
(D) low molecule betaine 1～5 weight % and
(E) water 5～25 weight %.
As composition, further preferred ascorbic acid in ascorbic acid or its salt, further preferred propylene glycol and diglycerol in glycol, glycerol and diglycerol, as glycol ethers, further preferred carbiphene, as low molecule betaine, further preferred trimethyl glycine.
As the most preferred embodiment of skin preparations for extenal use of the present invention, especially preferably make up each composition with following use level.
(A) ascorbic acid or its salt 15～20 weight % above,
4～21 weight % more than a kind or 2 kinds that (B) from glycol, glycerol and diglycerol, select,
(C) glycol ethers 50～53 weight %
(D) low molecule betaine 2～4 weight % and
(E) water 10～20 weight %.
As composition, further preferred ascorbic acid in ascorbic acid or its salt, further preferred propylene glycol and diglycerol in glycol, glycerol and diglycerol, as glycol ethers, further preferred carbiphene, as low molecule betaine, further preferred trimethyl glycine.
In skin preparations for extenal use of the present invention, except above-mentioned ascorbic acid or its salt, for the various effects that strengthen or additional ascorbic acid or its salt had, in addition, can also make up synthetic promotion composition, blood circulation that whitening composition, anti-inflammatory composition, antimicrobial component, cell-stimulating composition, astringent component, antioxidant content, acne improve biotic components such as composition, aging resistance composition, collagen promote composition, the composition of preserving moisture, aging resistance become to grade various compositions more than a kind or 2 kinds and cooperate, with to additional other the useful effects of skin preparations for extenal use.The composition more than a kind or 2 kinds in whitening composition, anti-inflammatory composition, antioxidant content, aging resistance composition or the composition of preserving moisture preferably.As the combination of these compositions, can enumerate combination, ascorbic acid or its salt and combination, ascorbic acid or its salt of aging resistance composition and the combination of whitening composition and aging resistance composition of combination, ascorbic acid or its salt and the antioxidant content of the combination, ascorbic acid or its salt that particularly preferably are ascorbic acid or its salt and whitening composition and whitening composition and antioxidant content.As these each compositions, the composition as goods outside medicine, the medicine or the skin preparations for extenal use in the cosmetic field can use all the time, and in addition, if the composition that uses future then is not particularly limited, any composition can suit to select to use.
For example,, can be exemplified as arbutin, ellagic acid, phytic acid, lucinol, Ka Momila ET (カ モ ミ ラ ET), vitaminss such as vitamin A or derivatives thereof, vitamin E or derivatives thereof, pantothenic acid or derivatives thereof as whitening composition.Wherein, as preferred composition, can list pantothenic acid or derivatives thereof, ellagic acid, phytic acid, vitamin A or derivatives thereof, vitamin E or derivatives thereof.These whitening compositions can use more than a kind or 2 kinds.
When using above-mentioned whitening composition, be coupled to preferred 0.0003～10 weight % of ratio of skin preparations for extenal use of the present invention, more preferably 0.01～5 weight %.In addition, whitening composition is with respect to the ascorbic acid that contains in the skin preparations for extenal use of the present invention or its salt 100 weight portions, wishes with 0.001～1000 weight portion, preferred 0.005～500 weight portion, more preferably the ratio of 0.01～100 weight portion cooperates.
As the anti-inflammatory composition, can list allantoin, Calamina, enoxolone or derivatives thereof, zinc oxide, Kessazulen, tocopherol acetas, pyridoxine hydrochloride, menthol, Camphora, Oleum Terebinthinae, indometacin, salicylic acid or derivatives thereof etc.Preferably allantoin, enoxolone or derivatives thereof, enoxolone or derivatives thereof, Kessazulen, menthol.
When using above-mentioned anti-inflammatory composition, be coupled to preferred 0.0003～10 weight % of ratio of skin preparations for extenal use of the present invention, more preferably 0.01～5 weight %.In addition, the anti-inflammatory composition is with respect to the ascorbic acid that contains in the skin preparations for extenal use of the present invention or its salt 100 weight portions, wishes with 0.001～1000 weight portion, preferred 0.005～500 weight portion, more preferably the ratio of 0.01～100 weight portion cooperates.
As antioxidant content, can list tocopherol and derivant thereof, Butylated hydroxyanisole, dibenzylatiooluene, sodium sulfite, arabo-ascorbic acid and salt thereof, flavonoid, glutathion, glutathion peroxidase, glutathione-S-transferase, catalase, superoxide dismutase, sulfur oxidation protein, taurine, sulfenyl taurine, hypotaurine etc.Preferably tocopherol and derivant thereof, sulfenyl taurine, hypotaurine, sulfur oxidation protein, flavonoid.
When using antioxidant content, the ratio that is coupled to skin preparations for extenal use of the present invention is generally 0.00001～10 weight %, preferred 0.0001～5 weight %, more preferably 0.001～5 weight %.In addition, with respect to the ascorbic acid that contains in the skin preparations for extenal use of the present invention or its salt 100 weight portions, wish with 0.001～1000 weight portion, preferred 0.005～500 weight portion, more preferably the ratio of 0.01～100 weight portion cooperates.
As the aging resistance composition, can be exemplified as biostearin (vitamin A, retinoic acid, axerophthal etc.), VITAMIN B15, kinetins, p-phenylenediamine (PPD), zingiberaceous plant Rhizoma Curcumae Longae extract, sphingol derivant, silicon, silicic acid, N-methyl-L-serine, methyl dihydroxy pentanone etc.Preferably biostearin (vitamin A, retinoic acid, axerophthal etc.), kinetins.
When using above-mentioned aging resistance composition, be coupled to preferred 0.0003～10 weight % of ratio of skin preparations for extenal use of the present invention, more preferably 0.01～5 weight %.In addition, the aging resistance composition is with respect to the ascorbic acid that contains in the skin preparations for extenal use of the present invention or its salt 100 weight portions, wishes with 0.001～1000 weight portion, preferred 0.005～500 weight portion, more preferably the ratio of 0.01～100 weight portion cooperates.
As the composition of preserving moisture, except being exemplified as aminoacid and derivants thereof such as alanine, serine, leucine, isoleucine, threonine, glycine, proline, hydroxyproline, glycosamine, theanine, peptides such as collagen, collagen peptide, gelatin, glycerol, 1, polyhydric alcohol such as 3-butanediol, propylene glycol, Polyethylene Glycol, sugar alcohols such as Sorbitol, phospholipid such as lecithin, hydrolecithin, mucopolysaccharides such as hyaluronic acid, heparin, chrondroitin, outside the compositions from NMF such as lactic acid, pyrrolidone sodium carboxylate, carbamide, can also be exemplified as polyglutamic acid etc.Preferably alanine, serine, glycine, proline, hydroxyproline, glycosamine, theanine, collagen, collagen peptide, glycerol, 1,3 butylene glycol, hydrolecithin, hyaluronic acid, heparin, chrondroitin, lactic acid, pyrrolidone sodium carboxylate, polyglutamic acid.
When composition is preserved moisture in use,, can enumerate being generally 0.1～10 weight %, preferred 0.5～5 weight %, more preferably 0.5～5 weight % as the ratio that is coupled in the skin preparations for extenal use of the present invention.
Skin preparations for extenal use of the present invention can also further cooperate stabilization agent, surfactant, solvable branch, oils, saccharide or the Transdermal absorption of changing into to promote composition except cooperating above-mentioned each composition.Particularly by cooperating stabilization agent, surfactant, solvable branch or the oils of changing into, can further improve the ascorbic acid in the aqueous solvent or stability, effectiveness, the usability of its salt.
In skin preparations for extenal use of the present invention; do not damage qualities such as appearance stability or viscosity; in addition; in the scope of the amount of not damaging effect of the present invention and matter; in case of necessity in the goods or cosmetic field outside medicine, medicine; can cooperate as external agent composition and normally used various composition, as aminoacid, stimulate palliative, viscosifier, antiseptic, ultraviolet protective agent, coloring agent, dispersant, pH regulator agent, spice etc.Wherein, these compositions can cooperate independent a kind arbitrarily, also can cooperate arbitrarily more than 2 kinds.
Skin preparations for extenal use of the present invention, be to select from above-mentioned glycol, glycerol and diglycerol kind more than a kind or 2 kinds, glycol ethers, ascorbic acid or its salt, low molecule betaine and above-mentioned each any composition mixing cooperation in case of necessity, and then the substrate by cooperating other solvents or normally used external agent etc. in case of necessity, can be modulated into the form of pasty state, cystose, gel, liquid, emulsion state, butyrous, lamellar (the base material load is held), aerosol shape, various needs such as vaporific.They can be by industry method manufacturing commonly used.
Skin preparations for extenal use of the present invention can possess the fluidity of common pH1～8, but, wish that at preferred pH be 2～7, more preferably pH is 2～6 acidic region from the stability of ascorbic acid or its salt, to the viewpoint of the benefit of the low irritant of skin or mucosa and skin usability.
Skin preparations for extenal use of the present invention can be as cosmetics such as foundation cream, lipstick, mascara, eye shadow, eyeliner, brow and manicure materials; Foundation make up materials such as emulsion, vanishing cream, astringent, oil and facial film, detergents such as wash one's face material or cleaning agent, body detergent; Anti-Deodorant, tinea pedis therapeutic agent, pruritus, wound healing agent, wiping agent, detergent, anti-inflammatory analgesic, acne therapeutic agent, hemorrhoid, disinfection sanitizer, whitening agent, ultraviolet protective agent etc. belong to the goods outside medicine, the medicine or the various topical compositions of cosmetic field.According to the action effect to skin, the preparation that preferred the present invention is applied to skin preparations for extenal use crusts such as (crust preparations) uses.
Embodiment
Below, further describe the present invention according to embodiment and test example, but the present invention is not limited to these embodiment etc.
The dissolving of test example 1 ascorbic acid, usability, residual rate test
Solidify in the mixed solution of castor bean oil, water at trimethyl glycine, carbiphene, 1,3 butylene glycol, polyoxyethylene (60) according to the prescription shown in the table 1 (weight %), add ascorbic acid, heating, mixing make its dissolving, the modulation preparation.
＜can dissolve
After placing 1 month under 4 ℃ and the room temperature, each experimental liquid of visualization is judged and is had or not crystallization to separate out with each preparation.
＜usability, effect sense 〉
With 30 testees is object, with regard to following project when on skin, smearing intact each preparation of firm modulation usability and use the effect sense of each preparation after 1 month to estimate.
Usability: the stretching, extension of preparation when smearing, skin affinity, harsh feeling
Effect sense: whitening effects such as the mottle disappearance of spot attenuation, face
The elastic force effect of skin such as that wrinkle becomes is unshowy, pore is unshowy
The skin surface smooth moistening effect that waits that becomes
About above-mentioned project, respectively synthetically to usability, effect sense be satisfied with, satisfied a little, generally, dissatisfied a little, unsatisfied 5 evaluations, when number satisfied and satisfied testee a little is that 20 people are when above, be designated as zero, when number satisfied and satisfied testee a little is 10～19 man-hours, be designated as △, when number satisfied and satisfied testee a little is 9 people when following, be designated as *.
＜residual rate 〉
50 ℃ of 2 weeks of preparation of placing embodiment 1, comparative example 4 down, measure the residual rate (%) of ascorbic acid.
The result is as shown in table 1.
Table 1
| Embodiment 1 | Embodiment 2 | Comparative example 1 | Comparative example 2 | Comparative example 3 | Comparative example 4 | ||
| The L-ascorbic acid | ??5 | ??20 | ??5 | ??20 | ??20 | ??20 | |
| Trimethyl glycine | ??5 | ??3 | ??- | ??- | ??- | ??- | |
| Polyoxyethylene (60) solidifies castor bean oil | ??- | ??- | ??- | ??- | ??3 | ??- | |
| Carbiphene | ??- | ??57 | ??- | ??60 | ??57 | ??- | |
| 1,3 butylene glycol | ??90 | ??- | ??95 | ??- | ??- | ??- | |
| Purified Water | ??- | ??20 | ??- | ??20 | ??20 | ??80 | |
| Can dissolve | Preserved 1 month for 4 ℃ | ??○ | ??○ | ??× | ??× | ??- | ??× |
| Room temperature preservation 1 month | ??○ | ??○ | ??× | ??× | ??- | ??○ | |
| Usability (overall merit) | ??△ | ??○ | ??× | ??× | ??- | ??○ | |
| Effect sense (overall merit) | ??○ | ??○ | ??× | ??× | ??- | ??× | |
| Residual rate (%) | ??99.1 | ??97.5 | ??- | ??- | ??- | ??60.2 | |
In containing the preparation of water, comparative example 2 is the same with comparative example 1, and usability is poor, at usability difference this respect because occur through the time separate out, can not carry out 1 month test.In addition, in comparative example 3, replace trimethyl glycine and the matching surface activating agent, but when modulation, can not dissolve ascorbic acid, thereby do not form preparation.And then.In comparative example 4, the effect sense is poor, and about separate out the crystallization this respect under 4 ℃, residual rate significantly reduces.On the other hand, in embodiment 2, can dissolve, usability, effect sense, residual rate all be gratifying.
Thus, cooperate the present invention of low molecule betaine can stably can dissolve ascorbic acid or its salt, and usability and effect sense are good, simultaneously the residual rate height of ascorbic acid or its salt.
Below, enumerate example of formulations.
Embodiment 3
Ascorbic acid 20
Trimethyl glycine 3
Carbiphene 52.4
Diglycerol 4
Purified Water 20
Spice 0.5
Grapefruit extract 0.1
—————————————————————————————
Add up to 100%
Embodiment 4
Ascorbic acid 15
Trimethyl glycine 3
Carbiphene 50.9
Propylene glycol 20
Purified Water 10
Diglycerol 1
A Sailier (Acerola) extract 0.1
—————————————————————————————
Add up to 100%
Embodiment 5
Ascorbic acid 30
Trimethyl glycine 9
Carbiphene 30.9
Purified Water 30
Fructus Citri tangerinae extract 0.1
—————————————————————————————
Add up to 100%
Claims (5)
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|---|---|---|---|
| JP2004005650 | 2004-01-13 | ||
| JP2004005650 | 2004-01-13 | ||
| JP2004-005650 | 2004-01-13 |
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| CN1660081B CN1660081B (en) | 2011-01-19 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107595663A (en) * | 2017-11-09 | 2018-01-19 | 武汉励合生物医药科技有限公司 | A kind of high-temperature stability skin preparations for extenal use |
| CN109414394A (en) * | 2016-06-28 | 2019-03-01 | 日本乐敦制药株式会社 | Topical composition containing ascorbic acid and/or its salt |
| US20190290575A1 (en) | 2018-03-23 | 2019-09-26 | Mary Kay Inc. | Topical compositions and methods |
| CN111511366A (en) * | 2017-12-27 | 2020-08-07 | 日本乐敦制药株式会社 | Ascorbic acid and/or external composition containing its salt |
| CN111971043A (en) * | 2018-03-30 | 2020-11-20 | 日本乐敦制药株式会社 | Ascorbic acid and/or external composition containing salt thereof |
| CN113747878A (en) * | 2019-04-11 | 2021-12-03 | 雅芳产品公司 | Stabilized ascorbic acid solutions with high water content |
-
2005
- 2005-01-12 CN CN 200510003793 patent/CN1660081B/en not_active Expired - Lifetime
Cited By (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109414394A (en) * | 2016-06-28 | 2019-03-01 | 日本乐敦制药株式会社 | Topical composition containing ascorbic acid and/or its salt |
| US11166938B2 (en) | 2016-06-28 | 2021-11-09 | Rohto Pharmaceutical Co., Ltd. | External composition containing ascorbic acid and/or salts thereof |
| CN107595663A (en) * | 2017-11-09 | 2018-01-19 | 武汉励合生物医药科技有限公司 | A kind of high-temperature stability skin preparations for extenal use |
| CN111511366A (en) * | 2017-12-27 | 2020-08-07 | 日本乐敦制药株式会社 | Ascorbic acid and/or external composition containing its salt |
| US12263239B2 (en) | 2017-12-27 | 2025-04-01 | Rohto Pharmaceutical Co., Ltd. | External composition containing ascorbic acid and/or salt thereof |
| US20190290575A1 (en) | 2018-03-23 | 2019-09-26 | Mary Kay Inc. | Topical compositions and methods |
| CN112218616A (en) * | 2018-03-23 | 2021-01-12 | 玫琳凯有限公司 | Topical compositions and methods |
| US11701322B2 (en) | 2018-03-23 | 2023-07-18 | Mary Kay Inc. | Topical compositions and methods |
| CN111971043A (en) * | 2018-03-30 | 2020-11-20 | 日本乐敦制药株式会社 | Ascorbic acid and/or external composition containing salt thereof |
| CN113747878A (en) * | 2019-04-11 | 2021-12-03 | 雅芳产品公司 | Stabilized ascorbic acid solutions with high water content |
| CN113747878B (en) * | 2019-04-11 | 2024-03-08 | 雅芳产品公司 | Stable ascorbic acid solution with high water content |
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