CN100496448C - Oil-in-water emulsion composition - Google Patents

Oil-in-water emulsion composition Download PDF

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CN100496448C
CN100496448C CNB2004100861933A CN200410086193A CN100496448C CN 100496448 C CN100496448 C CN 100496448C CN B2004100861933 A CNB2004100861933 A CN B2004100861933A CN 200410086193 A CN200410086193 A CN 200410086193A CN 100496448 C CN100496448 C CN 100496448C
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oil
acid
emulsion composition
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CN1636549A (en
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井上东彦
渡边启
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Shiseido Co Ltd
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Abstract

To obtain an O/W-type emulsion composition having high emulsion stability with time in a system compounded with an alkoxysalicylic acid compound and having excellent usability. This O/W-type emulsion composition contains (A) an alkoxysalicylic acid or its salt, (B) a long-chain acyl sulfonic acid salt-type anionic surfactant, (C) a higher aliphatic alcohol, (D) water and (E) an oil and satisfies the following requirements; (i) gel having a transition temperature of >=60[deg.]C is formed by the components (B), (C) and (D), (ii) the amount of the component B to form the gel is >=0.1 mass% and <1.0 mass% based on the total amount of the O/W-type emulsion composition, (iii) the molar ratio of the component (B) to the component (C) to form the gel is 1:3 and (iv) the composition contains excessive component (C) or an amphiphilic substance independently of the formation of the gel in an amount of 0.5-10 mass% based on the total amount of the O/W-type emulsion composition.

Description

O/W emulsion composition
Technical field
The present invention relates to O/W emulsion composition mainly as the skin preparations for extenal use use. in more detail, relate to the good O/W emulsion composition of whitening effect excellence and ageing stability and usability.
Background technology
" the whitening " that means the skin of pale beauty at skin preparations for extenal use, particularly is one of most important problem in cosmetics.
Being in the cosmetics of purpose with " whitening ",, can cooperate for example vitamin C or derivatives thereof, arbutin etc. as whitening composition.To the exploration of whitening composition, in recent years more and more in vogue, as one of its achievement, alkoxyl salicylic acid (patent documentation 1) has been proposed as the composition of whitening effect excellence.
But, when in O/W emulsion composition, cooperating the alkoxyl salicylic acid, there is storage stability, particularly temperature (high temperature low temperature) poor stability, change the problem that causes separation or clutch easily along with the time.
In addition, though the applicant has proposed to have improved by the formation that contains α-gel in the foreign minister O/W emulsion composition (patent documentation 2) of usability, high-temperature stability, the stability when having cooperated the alkoxyl salicylic acid is not investigated.
[patent documentation 1] spy opens flat 6-40886 communique
[patent documentation 2] spy opens the 2001-348325 communique
Summary of the invention
In order to solve above-mentioned prior art problems, the object of the present invention is to provide a kind ofly in the system that has cooperated the alkoxyl salicylic acid, to change emulsion stability good along with the time, and the O/W emulsion composition of usability excellence.
In order to solve above-mentioned problem, the invention provides a kind of O/W emulsion composition, it contains following (A)~(E) composition and satisfies following condition (i)~(iv).
(A) composition: the alkoxyl salicylic acid shown in the following general formula (I) or its salt.
(in the formula (I), R represents alkyl).
(B) composition: the long acyl sulfonate type anionic surfactant shown in the following general formula (II).
R 1CO-a-(CH 2)nSO 3M 1 (II)
(in the formula (II), R 1CO-represents that average carbon atom number is 10~22 saturated or unsaturated fatty acid residue (acyl group); A represents-O-or-NR 2-(wherein, R 2The alkyl of expression hydrogen atom or carbon number 1~3); M 1Expression hydrogen atom, alkali metal class, alkaline-earth metal class, ammonium or organic amine; N represents 1~3 integer).
(C) composition: high fatty alcohol.
(D) composition: water.
(E) composition: oil content,
Condition (i): with (B) composition and (C) composition and (D) composition form gel, the transition temperature of the gel of formation is 60 ℃ or more than it.
Condition is (ii): (B) components matching amount that forms above-mentioned gel is with respect to the O/W emulsion composition total amount, is that 0.1 quality % or its are above but less than 1.0 quality %.
Condition is (iii): form (B) composition of above-mentioned gel and (C) mol ratio of the use level of composition be 1:3.
Condition is (iv): contain (C) composition or the amphiphilic species of the surplus that does not participate in gel formation, its use level is 0.5~10 quality % with respect to the O/W emulsion composition total amount.
In addition, the invention provides above-mentioned O/W emulsion composition as paste or emulsion form skin preparations for extenal use.
According to the present invention, provide a kind of and produce excellent whitening effect and stability and the good O/W emulsion composition of usability by alkoxyl salicylic acid or its salt.
Specific embodiments
The alkoxyl salicylic acid of (A) composition that uses among the present invention is shown in the following general formula (I), any hydrogen atom alkoxy (OR) salicylic acid based compound of Qu Daiing of salicylic 3,4 or 5.
Figure C200410086193D00071
In above-mentioned general formula (I), (alkyl OR) (R) is though have no particular limits, and preferred carbon number is 1~6 low alkyl group to constitute alkoxyl.Comprise any of straight chain, side chain.Specifically, methoxyl group), ethyl (corresponding alkoxyl-OR: ethyoxyl), propyl group (corresponding alkoxyl-OR: propoxyl group), isopropyl (corresponding alkoxyl-OR: isopropoxy), butyl (corresponding alkoxyl-OR: butoxy), isobutyl group (corresponding alkoxyl-OR: isobutoxy) etc., but be not limited in these can enumerate methyl (corresponding alkoxyl-OR:.
As the alkoxyl salicylic acid shown in the above-mentioned general formula (I), specifically, can enumerate 3-methoxyl group salicylic acid (2--hydroxyl--3-methoxybenzoic acid), 3-ethyoxyl salicylic acid (2-hydroxyl-3-ethoxybenzoic acid), 4-methoxyl group salicylic acid (2-hydroxyl-4-methoxybenzoic acid), 4-ethyoxyl salicylic acid (2-hydroxyl-4-ethoxybenzoic acid), 4-propoxyl group salicylic acid (2-hydroxyl-4-propoxy benzoic acid), 4-isopropoxy salicylic acid (2-hydroxyl-4-isopropoxy benzoic acid), 4-butoxy salicylic acid (2-hydroxyl-4-butyl phenyl ether formic acid), 5-methoxyl group salicylic acid (2-hydroxy-5-methyl p-methoxybenzoic acid), 5-ethyoxyl salicylic acid (2-hydroxyl-5-ethoxybenzoic acid), 5-propoxyl group salicylic acid (2-hydroxyl-5-propoxy benzoic acid) etc.
The alkoxyl salicylic acid is a known substances, and for example, 5-methoxyl group salicylic acid is with in " Beil ", 10227, and the method for putting down in writing respectively in the 4-methoxyl group salicylic acid " Beil ", 10379 can be easy to synthesize.In addition, Aldrich company (Germany) etc. sells as reagent it on market, also can use it.
The alkoxyl salicylic acid that can cooperate in emulsion composition of the present invention also comprises its salt.If the kind of this salt admissible salt on galenic pharmacy then has no particular limits, for example can enumerate, alkali metal salts such as sodium salt, potassium salt, perhaps alkali earth metal salt such as calcium salt in addition, also can be enumerated the salt of ammonium salt or amino acid salts etc.
(A) composition can cooperate a kind or 2 kinds or more than it.(A) use level of composition should be taken into account the concrete dosage form of skin preparations for extenal use or the selection that other gradation composition suits, though have no particular limits, generally totally be preferably 0.001~20.0 quality %, be preferably 0.01~10.0 quality % especially with respect to preparation.During less than 0.001 quality %, be difficult to give full play to whitening effect, on the other hand, even surpassing 20.0 quality % cooperates, also be difficult to the increase of affirmation along with use level, whitening effect improves, finds on the contrary to exist growth encourage to produce the tendency of the usability that is clamminess, so not preferred.
As the long acyl sulfonate type anionic surfactant of (B) composition among the present invention shown in following general formula (II).
R 1CO-a-(CH 2)nSO 3M 1 (II)
In the general formula (II), R 1CO-represents that average carbon atom number is 10~22 saturated or unsaturated fatty acid residue (acyl group); As R 1CO can enumerate C 11H 23CO, C 12H 25CO, C 13H 27CO, C 14H 29CO, C 15H 31CO, C 16H 33CO, C 17H 35CO, coconut fatty acid residue, PALM FATTY ACID residue etc.In addition, from aspects such as safeties, R 1CO more preferably its average carbon atom number is 12~22 group.
A represents-O-or-NR 2-(wherein, R 2Expression hydrogen atom or carbon number are 1~3 alkyl). they are electron-donating groups.As a, be preferably-O-,-NH-,-N (CH 3)-.
M 1Expression hydrogen atom, alkali metal class, alkaline-earth metal class, ammonium or organic amine.As M 1, can enumerate lithium, potassium, sodium, calcium, magnesium, ammonium, monoethanolamine, diethanolamine, triethanolamine, sodium taurocholate, N methyl taurine sodium etc.
N represents 1~3 integer.
As (B) composition; in above-mentioned general formula (II); a represents-chemical compound of O-, promptly as long acyl isethionate type anionic surfactant, can enumerate Cortex cocois radicis acyl isethinate, stearyl isethionate, lauroyl isethionate, myristoyl isethionate etc.
In the above-mentioned general formula (II); a represents-chemical compound of NH-; promptly, can enumerate N-lauroyl taurate, N-Cortex cocois radicis acyl group-N-ethanol taurate, N-myristoyl taurate, N-stearyl taurate etc. as long acyl taurate type anionic surfactant.
In the above-mentioned general formula (II), a represents-N (CH 3)-chemical compound; promptly, can enumerate N-lauroyl-N methyl taurine salt, N-palmityl-N methyl taurine salt, N-stearyl-N methyl taurine salt, N-Cortex cocois radicis acyl group-N methyl taurine salt etc. as long acyl methyl tauride type anionic surfactant.
Wherein, as (B) composition, be preferably N-stearyl-N methyl taurine salt especially.(B) composition can use a kind or 2 kinds or more than it.
As the high fatty alcohol of (C) composition, the carbon number that preferably has the straight or branched alkyl chain is 12~22 aliphatic alcohol.As (C) composition, can enumerate for example straight chain alcohol of lauryl alcohol, spermol, stearyl alcohol, behenyl alcohol, myristyl alcohol, oleyl alcohol, 16/octadecanol, hardened rapeseed oil alcohol, Jojoba alcohol etc.; Branched-chain alcohos such as perhaps single stearoyl glycerin ether (batilol), 2-decyl tetradecanol, lanolin alcohol, cholesterol, plant sterol, hexyl dodecanol, isooctadecanol, octyldodecanol etc.Preferred straight chain alcohol among the present invention.(C) composition can use a kind or 2 kinds or more than it.The mixture of 2 kinds of preferred uses or its above aliphatic alcohol among the present invention, the fusing point of further preferred this mixture are 60 ℃ or its above combination.If its fusing point is less than 60 ℃, then sometimes according to prescription, the temperature stability of system reduces, emulsion creaming.Among the present invention, the combination of preference such as the pure and mild behenyl alcohol of tristearin.
(C) composition is with the dosage of abundant formation aftermentioned gel, and contains in specific system under the condition of residual components and cooperate.
As the water of (D) composition that uses among the present invention, form the foreign minister.The use level of (D) composition that cooperates among the present invention can suitably determine according to goods, but be preferably 40~95 quality % with respect to O/W emulsion composition total amount among the present invention.
Among the present invention, with above-mentioned (B) composition, (C) composition and (D) composition form gel.It is 60 ℃ or more than it that this combination must make the transition temperature of gel, and more preferably transition temperature is 65 ℃ or more than it.If the transition temperature of this gel is less than 60 ℃, then the temperature stability of system reduces, and the possibility that causes emulsion creaming is arranged, so not preferred under the high temperature.
In addition, this gel constitutes with α-gel.α-gel means the association body that high fatty alcohol and hydrophilic surfactant active form in water, become α-Jie Gou (Fukushima positive two the work " physical chemistry of spermol ", Off レ グ ラ Application ス ジ ャ-Na Le company, 1992) gel.
Form the use level of (B) composition of above-mentioned gel, need be with respect to the O/W emulsion composition total amount for 0.1 quality % or more than it, less than 1.0 quality %.During less than 0.1 quality %, the temperature stability of system reduces, possibility that causes emulsion creaming is arranged, on the other hand, and thick and heavy, the gel that can not obtain satisfying usability of usability during 1.0 quality % or its are coated with when above.
In addition, in above-mentioned gel, form (B) composition of gel and (C) be 1:3 under the mol ratio of the match ratio of composition.
Among the present invention, gel means by (B) composition that forms at aqueous phase and (C) the association body that forms of the membrane structure of composition.(B) composition and (C) composition form the association body and can confirm by DSC (differential scanning calorimetry device).Promptly, mix (B) composition and (C) during composition, the endothermic peak of dispersive sample and (B) composition, (C) composition endothermic peak that dissolving or dispersive sample obtain in water is separately respectively compared, is shown single endothermic peak at high temperature side more in water, but, (C) during composition ratio of components low ((C) composition deficiency), the endotherm peak temperature of association body is low, this temperature raises along with the increase of (C) composition ratio of components, after finishing the association body structure, if (C) composition surplus, when reaching a certain amount of, superfluous (C) occur and become swarming.
Here, the composition that the association body structure is finished, when the hydrophilic surfactant active with single alkyl chain formed the association body with the higher alcohol with single alkyl chain, known to 1 mole of hydrophilic surfactant active, higher alcohol was 3 moles.In the present invention, further contain with (C) composition of the irrelevant surplus of above-mentioned gel formation (below, be designated as " (C 2) composition "), or containing amphiphilic species, its content is 0.5~10 quality % with respect to the O/W emulsion composition total amount.
(C with the irrelevant surplus of above-mentioned gel formation 2) explanation of composition, with (C) composition relevant with above-mentioned gel formation (below, be designated as " (C 1) composition ") explanation identical.Usually, add excessive and C 1The C that composition is identical 2Composition.That is, owing to form (B) composition and the (C of gel 1) the cooperation mol ratio of composition is 1:3, so (the C relevant with α-gel formation 1) content of composition is for multiply by (C on the numeral of 3 times of (B) composition molal quantitys 1) value that obtains of the mean molecule quantity of composition.Therefore, match ratio should be worth (the C of bigger surplus 2) composition, excess components is necessary for 0.5~10 quality % with respect to the O/W emulsion composition total amount.
Also can cooperate (C 2) amphiphilic species beyond the composition, preferably its fusing point is 55 ℃ or its above, more preferably 60 ℃ or its above amphiphilic species.If fusing point is less than 55 ℃, there is the situation that causes emulsion creaming in the then prescription temperature stability reduction of system down.
Amphiphilic species among the present invention is meant the material beyond (C) composition, be to have surface activity but self hydrophobicity has the such surface-active material of general surfactant by force and not, can enumerate for example higher fatty acids, monoglyceride, glycerol monoalkyl ether, monoalkylamine and sterols etc.As object lesson, can enumerate lauric acid, myristic acid, Palmic acid, stearic acid, behenic acid, oleic acid, 12-hydroxy stearic acid, 9-undecylenic acid, the acid of appropriate that, isostearic acid, linoleic acid, linolenic acid, eicosapentaenoic acid (EPA), docosahexenoic acid senior fatty acids such as (DHA); Sterols such as cholesterol, plant sterol; Monoglyceride, glycerol monoalkyl ether, monoalkylamine etc., but be not limited in these examples.Cooperate and the irrelevant (C of gel formation 2) when composition and amphiphilic species, both total use levels are 0.5~10 quality % with respect to the O/W emulsion composition total amount.
With the irrelevant (C of gel formation 2) use level of composition (cooperating (C 2) during amphiphilic species beyond the composition, both total use levels) during less than 0.5 quality %, superfluous (C 2) composition or amphiphilic species crystallization content be few, can not keep sufficient high-temperature stability.In addition, when use level surpassed 10 quality %, according to composition, hardness was too high, and usability is variation also.
In the present invention, except the above-mentioned necessary composition (B) that forms gel, also can cooperate new oiliness nonionic surfactant, cation in the scope of not damaging effect of the present invention is that surfactant, anion are surfactant or amphoteric surfactant.In addition, also can exist and irrelevant (B) composition of gel formation.
As the oil content of (E) composition that in O/W emulsion composition of the present invention, cooperates, in the scope of not damaging stability, can select the material that generally in cosmetics, uses.
As the oil content of expectation, nonpolarity oil content or silicone oils such as preferred hydrocarbons oil content.Nonpolarity oil content means in molecular structure not hydrability functional groups such as ether-containing key, ester bond, amido link, hydroxy, carboxyl.
As hydrocarbon ils, can enumerate liquid paraffin, squalane, Squalene, paraffin, isoparaffin, ceresin etc.
As silicone oil, can enumerate for example chain silicone oils such as dimethyl polysiloxane, methyl phenyl silicone, hydrogenated methyl diene polysiloxanes; Annular siloxanes such as octamethylcy-clotetrasiloxane, decamethylcyclopentaandoxane, ten diformazan basic rings, six siloxanes; Form 3 yuan of cancellated organic siliconresins, organic silicon rubber etc.
For the polarity oil content, in the scope of not damaging stability, can cooperate on a small quantity.Can enumerate liquid fat and ester oil as polar oil.
As liquid fat, can enumerate oleum lini, Camellia oil, macadimia nut oil, Semen Maydis oil, ermine oil, olive oil, American Avocado Tree oil, Camellia oil, Oleum Ricini, safflower oil, Jojoba oil, Oleum helianthi, Semen pruni armeniacae oil, Oleum Brassicae campestris, Oleum sesami, soybean oil, Oleum Arachidis hypogaeae semen, triglycerin, tricaprylin, three different tripalmitins etc.
As ester oil, can enumerate Octanoic acid, hexadecyl ester, lauric acid hexyl ester, isopropyl myristate, octyl palmitate, Standamul 7061, isostearic acid isopropyl ester, different octyl palmitate, Ceraphyl 140A, three-2 ethyl hexanoic acid glyceride, four-2 ethyl hexanoic acid pentaerythritol ester, succinic acid-2-Octyl Nitrite, ethyl sebacate etc.
As the use level of (E) composition, can suitably select according to goods, but be preferably 3~50 quality % with respect to the O/W emulsion composition total amount.In addition, (E) composition among the present invention does not contain (C) composition and the amphiphilic species of above-mentioned necessary composition.
Contain the present invention of above-mentioned necessary composition, in O/W emulsion composition, though form the gel that constitutes by the composition of the composition of (B) composition-(C)-(D), but since (B) composition that cooperates with respect to the emulsification composition total amount less than 1 quality %, the formation amount of gel less, compare with existing emulsion or emulsifiable paste and to have salubrious usability.In addition, because the crystallization coexistence of high-melting-point (C) composition of gel and surplus, therefore, although gel is few, also fully thickening is solidified, can be prevented emulsion creaming.By the present invention,, also can provide ageing stability the good and also good O/W emulsion composition of usability although the amount of surfactant that cooperates is few.
O/W emulsion composition of the present invention can be made the O/W emulsion composition that uses mainly as skin preparations for extenal use such as cosmetics, medicine, cosmeceuticals according to conventional methods, but especially preferably utilizes the skin preparations for extenal use that forms the oil-in-water type paste dosage-form of gel in the employing system in principle.In skin preparations for extenal use,, can cooperate general active ingredient or medicine component according to concrete purpose, under the prerequisite of not damaging the desired effect of the present invention.
As active ingredient, for example, when skin preparations for extenal use of the present invention is used as sunscreen, can in skin preparations for extenal use of the present invention, cooperate, benzoic acid such as para-amino benzoic acid are UV absorbent; Ortho-aminobenzoic acids such as methyl 2-aminobenzoate are UV absorbent; Salicylic acid octyl group ester, salicylic acid phenylester, salicylic acid height
Figure C200410086193D0013143354QIETU
Salicylic acid such as base ester are UV absorbent; P-methoxycinnamic acid isopropyl ester, p-methoxycinnamic acid monooctyl ester, p-methoxycinnamic acid-2-Octyl Nitrite, di-p-methoxy cinnamic acid list-2 ethyl hexanoic acid glyceride, [two (trimethicone) methyl silicane bases of 4--3-methyl butyl]-3,4, cinnamic acid such as 5-trimethoxy cinnamic acid ester are UV absorbent; 2,4-dihydroxy benaophenonel, 2-hydroxyl-4-methoxy benzophenone, 2-hydroxyl-4-methoxy benzophenone-5-sulfonic acid, 2-hydroxyl-4-methoxy benzophenone-benzophenone series UV absorbent such as 5-sodium sulfonate; Urocanic acid, urocanic acid ethyl ester, 2-phenyl-5-Jia base benzoxazole, 2-(2 '-hydroxyl-5 '-aminomethyl phenyl) benzotriazole, the 4-tert-butyl group-4 '-UV absorbent such as methoxy dibenzoyl methylmethane.
In addition, in order to give skin preparations for extenal use moistening effect of the present invention, can cooperate wetting agents such as Polyethylene Glycol, propylene glycol, dipropylene glycol, glycerol, two glycerol, 1,3 butylene glycol, hexanediol, xylitol, Sorbitol, maltol, maltose, D-mannitol, malt sugar, glucose, fructose, lactose, sodium chondroitin sulfate, hyaluronate sodium, adenylic acid sodium, sodium lactate, bile acid sodium, 2-pyrrolidone-5-carboxylic acid, glycosamine, cyclodextrin.
Further, as active ingredient, can cooperate to have the oil-soluble inhibitor vitamins of purposes in addition; Hormones such as estradiol, ethinylestradiol; Amino acidses such as arginine, aspartic acid, cystine, cysteine, methionine, serine, leucine, tryptophan; Antiinflammatories such as allantoin, azulenes, glycyrrhetinic acid; Whitening agents such as arbutin; Astringent such as zinc oxide, tannic acid; Fresheners such as L-menthol, Camphora; Sulfur, lysozyme chloride, pyridoxine hydrochloride, γ-Hi-Z etc.
Further, can cooperate various extracts with multiple drug effect.That is, in skin preparations for extenal use of the present invention, can cooperate The dish extract, Cortex Phellodendri extract, melilotus extract, the Herba lamii barbati extract, the Hemerocallis fulva L. extract, Radix Paeoniae Alba extract, the Saponaria officinalis extract, Fructus Luffae extract, the quinine extract, Herba Saxifragae extract, Radix Sophorae Flavescentis extract, the spatterdock extract, Fructus Foeniculi extract, the Flos Primulae Vittatae extract, rose extract, Radix Rehmanniae extract, citron extract, the Radix Arnebiae (Radix Lithospermi) extract, Aloe extract, the Rhizoma Acori Graminei extract, eucalyptus extracts, Herba Equiseti Hiemalis extract, sage extract, Thymi Serpylli Herba extract, tea extract, seaweed extract, Fructus Cucumidis sativi extract, Flos Caryophylli extract, the Fructus Rubi corchorifolii Immaturus extract, the Herba leucadis ciliatae extract, Radix Dauci Sativae extract, the Aesculus chinensis Bunge extract, the peach extract, the Folium Persicae extract, the Mulberry extract, the Centaurea cyanus extract, the Radix Hamamelidis Mollis extract, intacellin, thymic extract, silkworm silk extract etc.
In addition, the active ingredient that can be engaged in the skin preparations for extenal use of the present invention is not limited to these active ingredient.And, above-mentioned active ingredient except can be separately in skin preparations for extenal use of the present invention, cooperating, according to purpose, also can with 2 kinds or more than it above-mentioned active ingredient appropriate combination cooperate.
As matrix components of the present invention, except above-mentioned necessary composition,, can in the scope of not damaging effect of the present invention, cooperate known matrix components according to concrete desired form.
For example, can in skin preparations for extenal use of the present invention, cooperate lower alcohols such as ethanol, propanol, isopropyl alcohol; Sterols such as cholesterol, sitosterol, plant sterol, lanosterol.
Also can enumerate arabic gum, Tragacanth, galactan, more skin ulcer glue, tragon, karaya, carrageenin, pectin, Qiong Zhi, Fructus cydoniae oblongae seed (Fructus cydoniae oblongae in addition), department of botany's water soluble polymer of algae colloid (brown alga extract), starch (rice, corn, Rhizoma Solani tuber osi, Semen Tritici aestivi), glycyrrhizic acid etc.; The department of microbiology water soluble polymer of xanthan gum, glucosan, succinoglucan, amylase etc.; The animal of collagen protein, casein, albumin, gelatin etc. is a water soluble polymer; The starch of carboxymethyl starch, methyl hydroxypropyl starch etc. is water soluble polymer; The cellulose-based water soluble polymer of methylcellulose, celluloid, ethyl cellulose, methylhydroxypropylcellulose, hydroxyethyl-cellulose, cellulose sodium sulfate, hydroxypropyl cellulose, sodium carboxymethyl cellulose (CMC), crystalline cellulose, cellulose powder etc.; The alginic acid of sodium alginate, propylene glycol alginate etc. is a water soluble polymer; The ethylene of polyvinyl alcohol, polyvinyl methyl ether, polyvinyl pyrrolidone, carboxyl ethylene copolymer (CARBOPOL) etc. is water soluble polymer; The polyoxyethylene of Macrogol 2000 0, Macrogol 4000 000, polyethylene glycol 6000 00 etc. is a water soluble polymer; Copolymerization system water soluble polymers such as poloxalkol; The acrylic acid series water soluble polymer of sodium polyacrylate, polyethyl acrylate, polyacrylamide etc. in addition, can be enumerated polymine, cationic polymer etc.In addition, also can enumerate inorganic water soluble polymers such as bentonite, silicic acid Al Mg (PVC-ガ system), sodium magnesium silicate, Strese Hofmann's hectorite., silicic acid anhydride.
Further, in skin preparations for extenal use of the present invention, can cooperate metal ion blockeres such as alanine, disodium edta, polyphosphate sodium, Polymeric sodium metaphosphate., phosphoric acid; 2-amino-2-methyl-1-propanol, 2-amino-2-methyl-1, nertralizers such as ammediol, potassium hydroxide, sodium hydroxide, L-arginine, L-lysine, triethanolamine, sodium carbonate; The antioxidant of pH regulator agent such as lactic acid, citric acid, glycolic, succinic acid, tartaric acid, dl-malic acid, potassium carbonate, sodium bicarbonate, ammonium bicarbonate etc.
In addition, in skin preparations for extenal use of the present invention, can be used benzoic acid, salicylic acid, carbolic acid, p-Hydroxybenzoate, to antibacterial of chlorine m-cresol, hexachlorophene, alkyl benzyl dimethyl ammonium chloride, chlorhexidine hydrochloride, trichlorine diphenylurea, sensitization element, phenyl phenol, P-hydroxybenzoic acid etc. etc.
In addition, in the scope of not damaging the desired effect of the present invention, as required, can in skin preparations for extenal use of the present invention, cooperate suitable spice, pigment etc.
In addition, above-mentioned matrix components is an illustration, and the matrix components that can cooperate in skin preparations for extenal use of the present invention is not limited to these matrix components.
These matrix components according to the prescription of desired form, can appropriate combination be engaged in the skin preparations for extenal use of the present invention.
Embodiment
Below, enumerate embodiment the present invention is described in further detail, but the present invention is not limited in following embodiment.In addition, use level is represented with quality % with respect to the system that cooperates this composition if do not specify.
(embodiment 1~4, comparative example 1~4)
The O/W emulsion composition that preparation has the compositions of embodiment, comparative example shown in the following table 1 as sample, according to following evaluation criterion, carries out the evaluation of ageing stability, usability with it.Amalgamation result is shown in table 1.
(embodiment 5~7, comparative example 5~7)
The O/W emulsion composition that preparation has the compositions of embodiment, comparative example shown in the following table 2 as sample, according to following evaluation criterion, carries out the evaluation of ageing stability, usability with it.Amalgamation result is shown in table 2.
(method for making)
In table 1,2, mix water-phase component and oil-phase component in the prescription respectively, heat to 80 ℃ oil phase at 80 ℃ aqueous phases, with behind the homomixer uniformly emulsify, be added in that dissolved medicine component stirs in the water, be cooled to room temperature, the preparation O/W emulsion composition.
In addition, " (C) molal quantity of composition in the table 1,2 (* 1)", " (B) molal quantity of composition or surfactant (* 1)" all represent the molal quantity that contains in the 100g O/W emulsion composition.
In addition, (C) composition (quality %) relevant with gel is with (B) composition (in the comparative example (other) surfactant) the mean molecule quantity of molal quantity * 3 * (C) compositions represent.Have (C) composition of single linear alkyl chain and (B) composition of single linear alkyl chain (in the comparative example (other) surfactant) situation under, since known to 3 moles of (C) compositions formation of 1 mole of surfactant association gels, can obtain (C) that have nothing to do with gel by calculating and become component.
(C) components matching amount relevant with the use level of composition of irrelevant (C) composition of gel=(C)-with gel.
[low temperature and high-temperature stability]
Examine the state of each sample after preserving 1 month under-20 ℃ and 50 ℃ with observing, estimate according to following standard.
(evaluation criterion)
Zero: state does not have variation fully
△: see that water separates a little
*: quite a few separation of water
[usability]
According to each data of following standard evaluation.
(evaluation criterion)
Zero: salubrious usability
△: thick and heavy a little usability
*: thick and heavy usability
(method for making)
Mix water-phase component and oil-phase component in the prescription respectively, heat to 80 ℃ oil phase at 80 ℃ aqueous phases, with behind the homomixer uniformly emulsify, be added in that dissolved medicine component stirs in the water, be cooled to room temperature, the preparation O/W emulsion composition.
Figure C200410086193D00171
In table 1, embodiment 1~4 and comparative example 1~4th, the example that the use level of (B) composition, (C) composition is discussed.(B) composition and (C) use level of the composition embodiment 1~4 that satisfies condition of the present invention is good on low temperature and high-temperature stability, usability, but with the use level of irrelevant surplus (C) composition of gel formation comparative example 1 less than 0.5 quality %, poor high temperature stability, (B) use level of composition is less than the comparative example 2 of 0.1 quality %, low temperature and poor high temperature stability, surpass the comparative example 3 of 10 quality % with the use level of irrelevant surplus (C) composition of gel formation, (B) use level of composition is the above comparative examples 4 of 1.0 quality %, and usability is poor.
Figure C200410086193D00191
In table 2, embodiments of the invention 5~7 can obtain effect of the present invention at each of low-temperature stability, high-temperature stability and usability.Comparative example 5 is as surfactant; use N-stearyl-L-sodium glutamate to replace the example of (B) composition; comparative example 6 is to use POE (20) stearyl ether of nonionic surfactant to replace the example of (B) composition as surfactant, but they any low-temperature stability is all poor.Comparative example 7 is to set transition temperature that the cooperation prescription of composition of the composition of (B) composition-(C)-(D) makes gel less than 60 ℃ example, poor high temperature stability.
Utilizability on the industry
O/W emulsion composition of the present invention, be applicable to as the whitening effect excellence and through the time steady The skin preparations for extenal use that qualitative and usability is good uses.

Claims (10)

1. an O/W emulsion composition contains following (A)~(E) composition and satisfies following condition (i)~(iv),
(A) composition: the alkoxyl salicylic acid shown in the following general formula (I) or its salt,
Figure C200410086193C00021
In the formula (I), R represents alkyl,
(B) composition: long acyl sulfonate type anionic surfactant; described surfactant is to be selected from the Cortex cocois radicis acyl isethinate; the stearyl isethionate; the lauroyl isethionate; the myristoyl isethionate; N-lauroyl taurate; N-Cortex cocois radicis acyl group-N-ethanol taurate; N-myristoyl taurate; N-stearyl taurate; N-lauroyl-N methyl taurine salt; N-palmityl-N methyl taurine salt; in N-stearyl-N methyl taurine salt and the N-Cortex cocois radicis acyl group-N methyl taurine salt a kind or 2 kinds or more than it
(C) composition: aliphatic alcohol, be selected from lauryl alcohol, spermol, stearyl alcohol, behenyl alcohol, myristyl alcohol, oleyl alcohol, 16/octadecanol, hardened rapeseed oil alcohol, Jojoba alcohol, batilol, 2-decyl tetradecanol, lanolin alcohol, cholesterol, plant sterol, hexyl dodecanol, isooctadecanol and octyldodecanol
(D) composition: water,
(E) composition: oil content is selected from hydrocarbon ils, silicone oil, liquid fat and ester oil;
Condition (i): with (B) composition and (C) composition and (D) composition form gel, the transition temperature of the gel of formation is at 60 ℃ or more than it,
Condition is (ii): forming the content of (B) composition of above-mentioned gel, with respect to the O/W emulsion composition total amount, is that 0.1 quality % or its are above but less than 1.0 quality %,
Condition is (iii): form (B) composition of above-mentioned gel and (C) mol ratio of component content be 1:3,
Condition is (iv): contain surplus (C) composition or the amphiphilic species that do not participate in gel formation, the total content of superfluous (C) composition and amphiphilic species is 0.5~10 quality % with respect to the O/W emulsion composition total amount.
2. O/W emulsion composition as claimed in claim 1, above-mentioned (B) composition is N-stearyl-N methyl taurine salt.
3. O/W emulsion composition as claimed in claim 1, above-mentioned (C) composition Shi behenyl alcohol and stearyl alcohol.
4. O/W emulsion composition as claimed in claim 1, the content of above-mentioned (E) composition with respect to the O/W emulsion composition total amount, is 3~50 quality %.
5. O/W emulsion composition as claimed in claim 1, above-mentioned (E) composition is the hydrocarbon ils that is selected from liquid paraffin, squalane, Squalene, paraffin, isoparaffin, ceresin.
6. O/W emulsion composition as claimed in claim 1, above-mentioned (E) composition are the silicone oils that is selected from dimethyl polysiloxane, methyl phenyl silicone, hydrogenated methyl diene polysiloxanes, octamethylcy-clotetrasiloxane, decamethylcyclopentaandoxane, ten diformazan basic rings, six siloxanes, forms 3 yuan of cancellated organic siliconresins, organic silicon rubber.
7. O/W emulsion composition as claimed in claim 1, above-mentioned (E) composition is the liquid fat that is selected from oleum lini, Camellia oil, macadimia nut oil, Semen Maydis oil, ermine oil, olive oil, American Avocado Tree oil, Camellia oil, Oleum Ricini, safflower oil, Jojoba oil, Oleum helianthi, Semen pruni armeniacae oil, Oleum Brassicae campestris, Oleum sesami, soybean oil, Oleum Arachidis hypogaeae semen, triglycerin, tricaprylin, three different tripalmitins.
8. O/W emulsion composition as claimed in claim 1, above-mentioned (E) composition are the ester oil that is selected from Octanoic acid, hexadecyl ester, lauric acid hexyl ester, isopropyl myristate, the misery vinegar of Petiolus Trachycarpi, Standamul 7061, isostearic acid isopropyl ester, different octyl palmitate, Ceraphyl 140A, three-2 ethyl hexanoic acid glyceride, four-2 ethyl hexanoic acid pentaerythritol ester, succinic acid-2-Octyl Nitrite, ethyl sebacate.
9. O/W emulsion composition as claimed in claim 1, above-mentioned (E) composition is four-2 ethyl hexanoic acid pentaerythritol ester, squalane and dimethyl polysiloxane.
10. O/W emulsion composition as claimed in claim 1 is paste or emulsion form skin preparations for extenal use.
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