CN1443056A - External preparations for beautifying skin - Google Patents

External preparations for beautifying skin Download PDF

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Publication number
CN1443056A
CN1443056A CN01813107A CN01813107A CN1443056A CN 1443056 A CN1443056 A CN 1443056A CN 01813107 A CN01813107 A CN 01813107A CN 01813107 A CN01813107 A CN 01813107A CN 1443056 A CN1443056 A CN 1443056A
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Prior art keywords
rosa
extract
centifolia
water
acid
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CN1229094C (en
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古屋理香子
茂吕修
伊福欧二
海盐健一
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Shiseido Co Ltd
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Shiseido Co Ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9789—Magnoliopsida [dicotyledons]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/74—Biological properties of particular ingredients
    • A61K2800/78—Enzyme modulators, e.g. Enzyme agonists
    • A61K2800/782—Enzyme inhibitors; Enzyme antagonists

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Microbiology (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Mycology (AREA)
  • Botany (AREA)
  • Biotechnology (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Cosmetics (AREA)
  • Medicines Containing Plant Substances (AREA)

Abstract

External preparations for beautifying the skin, which contain as the active ingredient R. centifolia L. or R. gallica L. var. centifolia (L.) Reg., both of which belong to the genus Rosa of the family Rosaceae, or solvent extracts thereof. The preparations exhibit inhibitory activities against tyrosinase and the production of cyclic AMP (cAMP), have excellent melanism-inhibiting and beautifying effects, and are excellent in safety.

Description

Dermatologic preparation for beautifying
Technical field
The present invention relates to contain the Dermatologic preparation for beautifying of specified plant extract.Dermatologic preparation for beautifying of the present invention has the active effect of restraint of tyrosinase simultaneously and suppresses the effect that cyclic adenosine monophosphate (cAMP) produces, and have excellent inhibition melanocyte and generate effect, white-skinned face function, and safety is good.
Background technology
Pigment calmnesses such as the chloasma of skin, freckle are because hormone secretion is unusual, ultraviolet, inflammatory stimulus etc., cause the means of information transmission activation that produces melanocyte in the tegumentary chromatophore, the main enzyme that produces the melanocyte generation is a tryrosinase, activity expression is hyperfunction, and melanocyte produces in the excessive calmness of epidermis as a result.
As the method that prevents this chloasma, freckle, all be that the main enzyme that adopts the inhibition melanocyte to produce is the material of tyrosinase activity all the time.Particularly, express the frost that mixes by kojic acid, ellagic acid etc. that necessary copper ion is the mechanism of action, dew etc. at local coating to catch tyrosinase activity exactly; The frost that the hydroquinone derivative who have the structure that is similar to substrate tyrosine at local coating, plays a role as the tryrosinase competitive inhibitor, resorcinol derivatives etc. mix, dew etc.; Perhaps as the material with above-mentioned mechanism of action in addition, using melanocyte precursor DOPA quinone is reduced into DOPA is the L-ascorbic acid that suppresses the melanocyte mechanism of production.
Aforementioned substances is to the tryrosinase that is produced or expresses the DOPA quinone produced by tyrosinase activity and play a role, rather than the generation of restraint of tyrosinase.Therefore, has the more weak difficult point of effect itself and persistence thereof.In addition, L-ascorbic acid predecessor and the poor stability in substrate are in order to obtain essential a large amount of use of the effect that fully prevents chloasma, freckle.
In recent years, the various active component that contained in the plant extraction liquid are subjected to concern.Headed by the Polyphenols antioxidation that is contained in most plants, various effects such as antitumor have been reported.Plant extraction liquid to the Pear Power effect has also carried out various researchs.
As the plant of the Pear Power effect that is contained in Rosaceae (Rosaceae) Rosa (Rosa), known have Fructus Rosae Laevigatae, a Fructus rosae multiflorae etc.These plant extraction liquids also are active in its mechanism of action with restraint of tyrosinase, can not satisfy the requirement of whitening function and persistence aspect thereof.
On the other hand, as to the means of information transmission effect, to the material that its generation suppresses itself, reported to have the inhibiting か I of nitric oxide approach ょ く, have the inhibiting Chamomile of プ mouth テ ィ Application カ ィ ネ one ス C approach etc.But it is less that their pipeline participates in the melanocyte generation, is difficult to be suppressed significantly melanocyte generation effect, needs the agent of the better plant extract drug effect of exploitation.
Present inventors are on the basis of above-mentioned situation, further investigate repeatedly, found that the specified plant extract has the active effect of restraint of tyrosinase simultaneously and highly participates in the adenylate cyclase enzymatic pathway inhibition effect that melanocyte produces, have good whitening effect, the good melanogenic effect of inhibition, thereby finished the present invention.
Disclosure of an invention
That is to say that the present invention is a Dermatologic preparation for beautifying, it is characterized in that containing the Rosa centifolia L (R.centifolia L. or R.gallica L.var.centifolia (L.) Reg.) that belongs to the Rosaceae Rosa or its solvent extractable matter as effective ingredient.
The invention provides Melanogenesis inhibitor, tyrosinase activity inhibitor and cyclic adenosine monophosphate (cAMP) and produce inhibitor, it is characterized in that containing above-mentioned plant or its solvent extractable matter as effective ingredient.
The best mode that carries out an invention
Describe the present invention below.
Dermatologic preparation for beautifying of the present invention, Melanogenesis inhibitor, tyrosinase activity inhibitor, cyclic adenosine monophosphate (cAMP) produce inhibitor and contain the Rosa centifolia L that belongs to the Rosaceae Rosa or its solvent extractable matter as effective ingredient.
Used Rosa centifolia L (English name: Cabbage Rose among the present invention, Provance Rose) be from the Greece Rome epoch to the Renaissance epoch mainly in the garden-variety of south of europe cultivation, by its English name promptly as can be known this flower be the hose-in-hose hybrid of common head cabbage shape originate from (R.biferaX R.alba).
Rosa centifolia L can use with form that live or dried, but from viewpoints such as usability, preparationizations, preferably uses with the form of dried powder or solvent extractable matter.
The use position of Rosa centifolia L is flower or herb preferably, also can use other position.
The solvent extractable matter of above-mentioned plant can obtain by conventional method, for example can by with extract that solvent floods or reflux after, filtering and concentrating obtains.As long as extracting solvent is that the solvent that is generally used for extracting can arbitrarily use, for example can be separately separately or be used in combination with organic solvent classes such as alcohols such as water, methanol, ethanol, propylene glycol, 1,3 butylene glycol, glycerol, aqueous alcohols, chloroform, dichloroethanes, carbon tetrachloride, acetone, ethyl acetate, hexane etc.Also can use the extracting solution former state that will obtain by above-mentioned solvent extraction or concentrate after extracting solution by absorption method for example spent ion exchange resin remove material behind the impurity; After the post absorption with porous polymer (for example Amberlite XAD-2), with methanol or alcohol extraction, the material that obtains after concentrating.Also can use in addition by apportion design extract of obtaining of water/ethyl acetate extraction etc. for example.
The above-mentioned plant extract that makes thus safe has excellent whitening effect, suppresses melanocyte and generate effect, the active effect of restraint of tyrosinase and suppress cyclic adenosine monophosphate (cAMP) and tell on.
When above-mentioned plant extract was mixed into Dermatologic preparation for beautifying, preferably its combined amount was counted 0.000001-5.0% weight with dry weight in external agent total amount, more preferably 0.00001-3.0% weight, especially preferably 0.00001-1.0% weight.
When above-mentioned plant extract is mixed into Dermatologic preparation for beautifying, except that these extracts, in the scope of not overslaugh effect of the present invention, can suitably be mixed for other composition of skin preparations for extenal use such as common cosmetics, pharmaceuticals as required, for example oil content, wetting agent, UV absorbent, antioxidant, surfactant, antiseptic, wetting agent, spice, water, alcohol, viscosifier etc.
As above-mentioned UV absorbent, can suitably add 2-hydroxyl-4-methoxyl group benzophenone, 2-hydroxyl-4-methoxyl group benzophenone-5-sodium sulfonate, benzotriazole base butylphenol sodium sulfonate, di-2-ethylhexylphosphine oxide-benzophenone derivatives such as benzotriazole base tetramethyl butyl phenol as required; Methoxy cinnamic acid derivants such as p-methoxycinnamic acid monooctyl ester, di-p-methoxy cinnamic acid list-2 ethyl hexanoic acid glyceride, isopentyl trimethoxy cinnamic acid trisiloxanes ester; Urocanic acid, uncle 4--4 '-methoxy dibenzoyl methylmethane, diethyl hexyloxy phenol methoxyphenyl triazine, ethylhexyl triazinone, Phenylbenzimidazolesulfonic acid etc.
And, can also suitably add the edetic acid disodium as required, the edetic acid trisodium, sodium citrate, sodium polyphosphate, Polymeric sodium metaphosphate., sequestering agents such as gluconic acid, caffeine, tannin, verapamil, tranamic acid and derivant thereof, Radix Glycyrrhizae extract, グ ラ Block リ ジ Application, various crude drugs, tocopherol acetate, medicines such as glycyrrhizic acid and derivant thereof or its salt, vitamin C, magnesium ascorbyl phosphate, ascorbic acid glucoside, arbutin, kojic acid, resorcinol, ellagic acid, other whitening agent such as chamomile extract, glucose, fructose, mannose, sucrose, saccharides such as trehalose etc.
Dermatologic preparation for beautifying of the present invention can be used as cosmetics, medicine and the medicine analog etc. that exodermis is suitable for, and is particularly suitable for being widely used as cosmetics.Its dosage form is so long as be applicable to the dosage form of skin and get final product, applicable to solution system, can dissolve dosage form arbitrarily such as system, emulsification system, powder dispersion system, water-oily two coating systems, water-oil-powder three coating systems, ointment, gel, aerosol.
In addition, the use form of Dermatologic preparation for beautifying of the present invention also is arbitrarily, for example can be used as that faces such as astringent, emulsion, frost, facial film apply some make up, foundation cream, also can be used as cosmetics, fragrant cosmetics, baths etc. in addition.
The form that Dermatologic preparation for beautifying of the present invention can use is not limited to above-mentioned dosage form and uses form.
Embodiment
The present invention will be described in more detail to enumerate embodiment below, but technical scope of the present invention is not limited by these embodiment at all.In addition, combined amount all is a % weight.
Before embodiment, tyrosinase activity inhibition effect, the cyclic adenosine monophosphate (cAMP) to plant extract of the present invention produces the inhibition effect earlier, melanocyte generates the experimental technique and the evaluation methodology that suppress effect and whitening effect and describes.[experimental technique and evaluation methodology]
1. the preparation of sample
Colored water heating extraction with the 50g Rosa centifolia L obtains extracting solution.This extracting solution is concentrated, obtain the 5g plant extract.
Above-mentioned plant extract is dissolved in 70% ethanol, makes its concentration reach 2% weight, make the solution that contains plant extract.This is contained the solution dilution of plant extract, adjust concentration, carry out following experiment used as sample solution.
2. cell culture processes
The B16 melanoma cultured cell of mice is taken from use.At CO 2In the incubator (95% air, 5% carbon dioxide), under 37 ℃ of conditions, (α-MSH) the Dulbecco MEM culture medium of (10nM) is cultivated with containing 10%FBS and theophylline (0.09mg/ml) or melanotropin.
3. tyrosinase activity suppresses effect measuring
To be seeded in above-mentioned 2 method cultured cells on 96 orifice plates, and cultivate and add sample solution after 24 hours, and make its ultimate density (extracting dry thing conversion concentration) reach 10 -7-10 -5% weight continues to cultivate again.Cultivate after 3 days and wash, add the PBS that contains 1%Triton, add DOPA again, make its ultimate density reach 1mM with PBS.
Measure the absorbance (475nm) that adds after 0 minute and 60 minutes.With the sample (reference substance that does not add plant extract; 70% ethanol) compare, estimate according to following determinating reference.In addition, as a reference example, Flos rosae multiflorae (Rosacanina L.) extract (ethanol extraction) that belongs to the Rosaceae Rosa is equally carried out experiment same as described above.The result is as shown in table 1.In addition, provided in the table 1 to use and contain melanotropin (result of the culture medium of α-MSH), the result when using theophylline is the same.
(determinating reference)
Zero: its tyrosinase activity inhibitory action is better than reference substance.
△: its tyrosinase activity inhibitory action is better a little than reference substance.
*: no tyrosinase activity inhibitory action.Table 1
Sample solution Sample solution concentration (% weight)
???0 ????10 -7 ????10 -6 ????10 -5
The Rosa centifolia L extract ???× ????△ ????○ ????○
The Flos rosae multiflorae extract ???× ????× ????× ????×
4. the vision of melanocyte amount is judged (melanocyte generates and suppresses effect)
To be seeded in above-mentioned 2 method cultured cells on 96 orifice plates, and cultivate and add sample solution after 24 hours, and make its ultimate density (extracting dry thing conversion concentration) reach 10 -2-10 -5% weight continues to cultivate again.Cultivate after 3 days, on the lid of 96 orifice plates, place diffuser plate, with the melanocyte amount in the handstand microscope observing cell, with the sample (reference substance that does not add plant extract; 70% ethanol) compare, estimate according to following determinating reference.In addition, as a reference example, the Flos rosae multiflorae extract (ethanol extraction) that belongs to the Rosaceae Rosa is equally carried out experiment same as described above.The result is as shown in table 2.In addition, provided in the table 2 to use and contain melanotropin (result of the culture medium of α-MSH), the result when using theophylline is the same.
(determinating reference)
Zero: than reference substance white (it is good that melanocyte generates inhibitory action).
△: than reference substance white slightly (it is better that melanocyte generates inhibitory action).
*: with reference substance same white (no melanocyte generates inhibitory action).Table 2
Sample solution Sample solution concentration (% weight)
???0 ????10 -5 ????10 -4 ????10 -3 ????10 -2
The Rosa centifolia L extract ???× ????× ????△ ????○ ????○
The Flos rosae multiflorae extract ???× ????× ????× ????× ????×
5. cyclic adenosine monophosphate (cAMP) produces and suppresses effect measuring
The B16 melanoma cultured cell that to take from mice is seeded on 12 orifice plates, at CO 2In the incubator (95% air, 5% carbon dioxide), under 37 ℃ of conditions, cultivate with the Dulbecco MEM culture medium that contains 10%FBS.Cultivate sucking-off culture medium after 24 hours, add melanotropin (α-MSH, 0.1nM) and added sample solution and made its ultimate density reach 10 -1-10 -3The serum-free medium of % weight (extracting dry thing conversion concentration).Cultivate after 30 minutes, remove culture medium,, move in the 1.5mL microtubule, after boiling, measure with the cyclic adenosine monophosphate (cAMP) that cyclic adenosine monophosphate (cAMP) mensuration apparatus (manufacturing of ア マ シ ャ system society) is measured in this solution with TE buffer collecting cell.In addition, as a reference example, the Flos rosae multiflorae extract (ethanol extraction) that belongs to the Rosaceae Rosa is equally carried out experiment same as described above.With the sample (reference substance that does not add plant extract; 70% ethanol) compare, estimate according to following determinating reference.The result is as shown in table 3.
(determinating reference)
Zero: it is better than reference substance that its cyclic adenosine monophosphate (cAMP) produces inhibitory action.
△: it is better a little than reference substance that its cyclic adenosine monophosphate (cAMP) produces inhibitory action.
*: no cyclic adenosine monophosphate (cAMP) produces inhibitory action.Table 3
Sample solution Sample solution concentration (% weight)
???0 ???10 -3 ???10 -2 ??5×10 -2 ???10 -1
The Rosa centifolia L extract ???× ???× ???△ ??○ ???○
The Flos rosae multiflorae extract ???× ???× ???× ??× ???×
6. whitening effect test
(test method)
With 20 skin of back that are exposed to the tester of sunlight in summer following 4 hours (2 hours on the 1st, 2 days) is object, and sooner or later show test sample solution under each primary coating every day, applied for 4 weeks altogether, according under show determinating reference evaluation.The meansigma methods of 20 testers' scoring is as shown in table 4.(test sample solution)
Blending constituent (% weight)
(pure phase)
95% ethanol 25.0
Polyoxyethylene (25 moles) hardened castor oil ether 2.0
Methyl parahydroxybenzoate 0.1
Dibenzylatiooluene 0.01
Spice 0.05
(water)
Glycerol 2.0
1,3 butylene glycol 1.0
Ion exchange water surplus medicine is (as shown in table 4.Combined amount in the table is represented dry weight.) (preparation method)
Allocate respectively water, alcohol mutually after, mix, make its dissolving.(evaluation methodology)
According to the color desalination effect after the following determinating reference judgement use.
(scoring)
4: after continuously coating uses, can obviously confirm color desalination effect.
3: after continuously coating uses, can confirm color desalination effect.
2: after continuously coating uses, can confirm color desalination effect a little.
1: after continuously coating uses, can not confirm color desalination effect.Table 4
Comparative example Embodiment
??1 ??2 ??3 ??4 ??5 ??6 ??1 ??2
Rosa centifolia L ??- ??- ??- ??- ??- ??- ??0.1 ??1.0
Flos rosae multiflorae ??1.0 ??- ??- ??- ??- ??- ??- ??-
Fructus rosae multiflorae ??- ??1.0 ??- ??- ??- ??- ??- ??-
Ascorbic acid ??- ??- ??3.0 ??- ??- ??- ??- ??-
Magnesium L-ascorbyl-2-phosphate ??- ??- ??- ??1.0 ??- ??- ??- ??-
Ascorbic acid phosphoric acid esters sodium ??- ??- ??- ??- ??1.0 ??- ??- ??-
Intacellin ??- ??- ??- ??- ??- ??1.0 ??- ??-
Scoring ??1.00 ??1.10 ??1.10 ??1.35 ??1.35 ??1.15 ??1.60 ??2.20
As shown in Table 4, the present invention's product have good whitening effect.Particularly mix example and compare, can confirm that also the present invention's product have good whitening effect with known ascorbic acid derivates, intacellin with skin-whitening effect.
Below the mixing example of the Dermatologic preparation for beautifying of the present invention of the various dosage forms form with embodiment is described.The combined amount of plant extract is dry residual volume.3 ( ％ ) ( 1 ) 6.0 ( 2 ) 2.0 ( 3 ) ( 20 ) 1.5 ( 4 ) 7.0 ( 5 ) 0.03 ( 6 ) 7.0 ( 7 ) 3.0 ( 8 ) ( ) 1.0 ( 9 ) 0.1 ( 10 ) 0.1 ( 11 ) 0.01 ( 12 ) 0.1 ( 13 ) 72.16 ( )
(4), (6), (7), (8) are joined in (13), 70 ℃ of (waters) .On of and heating remains on the other hand, (1)-(3), (5), (9)-(12) are mixed, 70 ℃ of (oil phases) .Oil phase of heating for dissolving remains on is added water carry out pre-emulsifying, behind the homogeneous mixer uniformly emulsify, fully stir, 30 ℃ of be cooled to, obtain foundation cream cream. embodiment 4 neutral white blending constituent (% weight) (1) stearyl alcohols 5.0 (2) stearic acid 2.0 (3) hydrogenated lanolins 2.0 (4) oxybenzones 2.0 (5) saualane 5.0 (6) 2-octyldodecanols, 6.0 (7) polyoxyethylene (25 moles) spermaceti alcohol ethers 3.0 (8) monostearins 2.0 (9) intacellins 0.1 (10) propane diols 2.0 (11) 1; 3-butanediol 3.0 (12) Rosa centifolia extracts (water extract) 5.0 (13) spices 0.2 (14) 1,2-pentanediol 0.5 (15) butyl p-hydroxybenzoate 0.1 (16) hypotaurine 0.01 (17) ion exchange water 65.69 (preparation method)
(9)-(12), (16) are joined in (17), 70 ℃ of (waters) .On of and heating remains on the other hand, (1)-(8), (13)-(15) are mixed, 70 ℃ of (oil phases) .Oil phase of heating for dissolving remains on is added water carry out pre-emulsifying, behind the homogeneous mixer uniformly emulsify, fully stir, 30 ℃ of be cooled to, obtain neutral frost. embodiment 5 cold cream blending constituents (% weight) (1) solid paraffin 5.0 (2) beeswaxs 5.0 (3) vaseline 5.0 (4) atoleines 20.0 (5) saualanes 10.0 (6) monostearin 2.0 (7) polyoxyethylene (20 moles) anhydro sorbitol one 2.0 laurates (8) kojic acids 2.0 (9) Uvinul MS 40 sodium 3.5 (10) soap powder 0.1 (11) borax 0.2 (12) Rosa centifolia extract (water extract) 0.1 (13) ion exchange water 44.55 (14) spices 0.2 (15) ethyl-para-hydroxybenzoate 0.2 (16) butyl p-hydroxybenzoate 0.1 (17) butylated hydroxytoluene 0.05 (preparation method)
(8); (10); (11) and (12) are joined in (13); 70 ℃ of (waters) .On of and heating for dissolving remains on the other hand; (1)-(7); (9); (14)-(17) are mixed; 70 ℃ of (oil phases) .While stirring of heating for dissolving remains on oil phase is slowly added water; react.After reaction finishes; fully stir after the emulsifying; 30 ℃ of simultaneously of be cooled to, 2.0 hectorites (2) polyoxyethylene polymethyl siloxane polymer, 0.1 (3) atoleine, 10.0 (4) vaseline, 5.0 (5) Octanoic acid, hexadecyl esters, 20.0 (6) Pidolidone soda, 0.01 (7) dipropylene glycol, 5.0 (8) methyl p-hydroxybenzoates, 0.2 (9) Sodium Hyaluronate, 0.05 (10) vitamin E acetate, 0.02 (11) Rosa centifolia extract (water extract), 2.0 (12) ion exchange waters 55.62 (preparation method) that obtain cold cream by the homogeneous mixer uniformly emulsify. embodiment 6 nourishing cream blending constituents (% weight) (1) dimethyl distearyl ammonium chloride is processed
After (2), (3), (5) are warming up to 50 ℃, add in (4), (10) consoluet oil phase part and add (1), make its homodisperse, making (6), (7), (8), (9), (11) be dissolved in the aqueous portion that forms in (12) heats to 50 ℃, and add in the oil mixture, after carrying out homodisperse by HM, be cooled to room temperature, obtain water-in-oil emulsion composition.
Embodiment 7 emulsion blending constituents (% weight) (1) polyoxyethylene (10 moles) monooleate 2.0 (2) OctMets 3.5 (3) atoleines 2.0 (4) ring five (dimethyl siloxane) 1.0 (5) saualanes 3.0 (6) 1; 3-butanediol 5.0 (7) ursin 2.0 (8) sodium hydrogensulfites 0.03 (9) glycerine 2.0 (10) ethanol 5.0 (11) carboxyl vinyl polymers 0.3 (12) hydroxypropyl cellulose 0.1 (13) potassium hydroxide 0.15 (14) ethyl-para-hydroxybenzoate 0.1 (15) 1,2-pentanediol 1.0 (16) Rosa centifolia extracts (water extract) 0.5 (17) ion exchange water 72.02 (18) spices 0.3 (preparation method)
(16) and (7) heated to be dissolved in (17) and (10), and dissolving (6), (8), (9), (11)-(13) remain on 70 ℃ (waters) again.On the other hand, (1)-(5), (14), (15), (18) are mixed, heating for dissolving remains on 70 ℃ (oil phases).Oil phase is added water, carry out pre-emulsifying, carry out uniformly emulsify, fully stir after the emulsifying, be cooled to 30 ℃ simultaneously, obtain emulsion by homogeneous mixer.
8 ( ％ ) ( 1 ) ( 20 ) ( 2 1.0 ) ( 2 ) 3.5 ( 3 ) “シリコンKF96” ( 20cs ) 2.0 ( ) ( 4 ) ( ) 3.0 ( 5 ) 4- 0.3 ( 6 ) ( 2- ) 1.0 ( 7 ) 2.0 ( 8 ) 0.03 ( 9 ) 2.0 ( 10 ) 3.0 ( 11 ) 0.3 ( 12 ) 0.1 ( 13 ) 0.1 ( 14 ) 1,2- 2.0 ( 15 ) 0.2 ( 16 ) ( ) 0.1 ( 17 ) 79.37 ( )
(16) and (7) heated to be dissolved in (17) and (10), and dissolving (6), (8), (9), (11)-(13), (15) remain on 70 ℃ (waters) again.On the other hand, (1)-(5), (14) are mixed, heating for dissolving remains on 70 ℃ (oil phases).Oil phase is added water, carry out pre-emulsifying, carry out uniformly emulsify, fully stir after the emulsifying, be cooled to 30 ℃ simultaneously, obtain emulsion by homogeneous mixer.
9 ( ％ ) ( 1 ) ( 20 ) ( 2 ) 1.0 ( 2 ) -2- 2.0 ( 3 ) “シリコンKF96” ( 20cs ) 2.0 ( ) ( 4 ) 3.0 ( 5 ) 1,3- 5.0 ( 6 ) -2- 3.0 ( 7 ) 400 3.0 ( 8 ) 2.0 ( 9 ) 5.0 ( 10 ) 0.3 ( 11 ) 0.1 ( 12 ) 0.1 ( 13 ) 0.1 ( 14 ) 0.4 ( 15 ) 0.02 ( 16 ) ( ) 0.01 ( 17 ) 72.87 ( 18 ) 0.1 ( )
(15), (16) and (6) are dissolved in (17) and (9), and dissolving (5), (7), (8), (10)-(12), (14) remain on 70 ℃ (waters) again.On the other hand, (1)-(4) and (13), (18) are mixed, heating for dissolving remains on 70 ℃ (oil phases).Oil phase is added water, carry out pre-emulsifying, carry out uniformly emulsify, fully stir after the emulsifying, be cooled to 30 ℃ simultaneously, obtain emulsion by homogeneous mixer.
Embodiment 10 emulsion blending constituents (% weight) (1) polyoxyethylene (20 moles) polyoxypropylene (2 moles) whale 1.0 ceryl alcohols (2) " シ リ コ one Application KF96 " are 2.0 (manufacturing of KCC of SHIN-ETSU HANTOTAI) (3) atoleine (medium viscosity), 3.0 (4) Tinuvin 360s 1.0 (5) 1 (20cs); 3-butanediol 5.0 (6) glycerine 2.0 (7) ethanol 4.0 (8) carboxyl vinyl polymers 0.3 (9) hydroxypropyl cellulose 0.1 (10) potassium hydroxide 0.05 (11) 1; 2-pentanediol 1.0 (12) butyl p-hydroxybenzoate 0.1 (13) kojic acid, 3.0 (14) Rosa centifolia extracts (1,3-BDO extract) 0.001 (15) ion exchange water 77.449 (preparation method)
In (15), dissolving (14), (5)-(10) remain on 70 ℃ (waters) again with (13) heating for dissolving.On the other hand, (1)-(4) and (11), (12) are mixed, heating for dissolving remains on 70 ℃ (oil phases).Oil phase is added water, carry out pre-emulsifying, carry out uniformly emulsify, fully stir after the emulsifying, be cooled to 30 ℃ simultaneously, obtain emulsion by homogeneous mixer.
Embodiment 11 emulsion blending constituents (% weight) (1) stearic acid 1.5 (2) cetanol 0.5 (3) beeswax, 2.0 (4) polyoxyethylene (20 moles) monooleates 1.0 (5) glyceryl monostearates 1.0 (6) ethanol 3.0 (7) ursin 10.0 (8) sodium hydrogensulfites 0.03 (9) 1; 3-butanediol 5.0 (10) PEG400s, 2.0 (11) Rosa centifolia extracts (1,3-BDO extract) 0.0005 (12) ion exchange water 73.2195 (13) spices 0.15 (14) methyl p-hydroxybenzoate 0.3 (15) butyl p-hydroxybenzoate 0.2 (16) thiolaurine 0.1 (preparation method)
(7), (9) and (10), (16) are added in (12), and heating for dissolving remains on 70 ℃ (waters).In addition, (11) are added dissolving (pure phase) in (6).On the other hand, (1)-(5), (8), (13), (14), (15) are mixed, heating for dissolving remains on 70 ℃ (oil phases).Oil phase is added water, carry out pre-emulsifying, carry out uniformly emulsify, while stirring to wherein adding pure phase by homogeneous mixer.Stir afterwards, be cooled to 30 ℃ simultaneously, obtain emulsion.
Embodiment 12 emulsion blending constituents, (% weight), (1) microwax 1.0, (2) beeswax 1.0, (3) vaseline 2.0, (4) atoleine 10.0, (5) saualane 5.0, (6) jojoba oil 5.0, (7) Arlacel-83 4.0, (8) polyoxyethylene, (20 moles) anhydro sorbitol one oily 1.0 acid esters, (9) ursin 5.0, (10) sodium hydrogensulfite 0.03, (11) tranexamic acid 5.0, (12) 1; 3-butanediol 5.0 (13) sorbierites, 2.0 (14) Rosa centifolia extracts (1,3-BDO extract) 0.00001 (15) Tinosorb S 1.5 (16) ion exchange waters 52.01999 (17) spices 0.2 (18) ethyl-para-hydroxybenzoate 0.1 (19) butyl p-hydroxybenzoate 0.1 (20) dibutyl hydroxy toluene 0.05 (preparation method)
(9), (11)-(14) are added in (16), and heating remains on 70 ℃ (waters).On the other hand, (1)-(8), (10), (15), (17)-(20) are mixed, heating for dissolving remains on 70 ℃ (oil phases).Stir oil phase, in this oil phase, slowly add water simultaneously, carry out uniformly emulsify by homogeneous mixer.Fully stir after the emulsifying, be cooled to 30 ℃ simultaneously, obtain emulsion.
Dimethyl silicone polymer 1.0 (4) octamethylcy-clotetrasiloxanes 25.0 (5) decamethylcyclopentaandoxane 15.0 (6) trimethylsiloxy silicic acid 5.0 (7) volatile oil extracted from eucalyptus' leaves or twigs 3.0 (8) spices 0.05 (9) dipropylene glycol, 2.0 (10) Rosa centifolia extracts (propane diols extract) 0.002 (11) ursin 7.0 (12) sodium hydrogensulfites 0.03 (13) methyl p-hydroxybenzoate 0.1 (14) edetic acid trisodium 0.1 (15) ion exchange water 30.718 (16) potassium chloride 0.5 (preparation method) of embodiment 13 emulsion blending constituents (% weight) (1) isopropyl alcohol 10.0 (2) two isostearic acids two glyceride 0.5 (3) POE modification
With (1)-(8) dissolvings (oil phase), (9)-(16) dissolvings (water) add oil phase with water, and emulsifying obtains emulsion.
Embodiment 14 emulsions
Blending constituent (% weight) A. oil phase
Polydimethylsiloxane 0.5
Decamethylcyclopentaandoxane 1.0
Jojoba oil 0.5B. water
Arbutin 1.0
Rosa centifolia L extract (water extract) 0.005
Alkyl-modified CVP Carbopol ETD2050 0.05
CVP Carbopol ETD2050 0.3
Radix Acaciae senegalis 0.05
Ethanol 8.0
Edetic acid trisodium 0.1
Methyl parahydroxybenzoate 0.1
Phenyl phenol 0.2
Ion exchange water 88.045C. neutralization
KOH 0.15 (preparation method)
With (A) after the dissolving add to mutually after the dissolving (B) mutually in, after the emulsifying, neutralize mutually with (C), obtain emulsion.
Embodiment 15 gels
Blending constituent (% weight) (1) 95% ethanol 10.0 (2) dipropylene glycol 10.0 (3) glycerine, 5.0 (4) polyoxyethylene (15 moles) oleyl alcohol ethers 2.0 (5) ursin 0.5 (6) sodium hydrogensulfite 0.03 (7) ascorbic acid distearyl alcohol ester 0.5 (8) carboxyl vinyl polymer (カ one ボ Port 1
Le 941) (9) caustic potash 0.15 (10) L-arginine 0.1 (11) Rosa centifolia L extract 0.001
(50%1,3-butanediol extract) (12) spice 0.1 (13) phenyl phenol 0.4 (14) ion exchange water 70.219 (preparation method)
With (11), (5), (3) and (8) uniform dissolution (water) in (14).On the other hand, (2), (4) and (6), (7), (12), (13) are dissolved in (1), add it to aqueous phase.Then with (9), (10) neutralization, tackify obtains gel.
Embodiment 16 peel off pack blending constituents (% weight) (pure phase) 95% ethanol, 10.0 polyoxyethylene (15 moles) oleyl alcohol ether 2.0 Uvinul T 150s 1.0 methyl p-hydroxybenzoates 0.3 phenoxetol 0.3 spices 0.2 (water) Rosa centifolia extract 1.0 (50% 1,3-BDO extract) ursin 1.0 sodium hydrogensulfites 0.03 polyvinyl alcohol 12.0 glycerine 3.0 polyethylene glycol 1500s 1.0 ion exchange waters 68.17 (preparation method)
At 80 ℃ of preparation waters, be cooled to 50 ℃.Then add the pure phase of preparation at room temperature, then its homogeneous is mixed, place cooling.
Embodiment 17 mixes powder (powder enters り) profile film blending constituent (% weight) (pure phase) 95% ethanol 5.0 methyl p-hydroxybenzoates 0.11; 2-pentanediol 2.0 spices 0.3 ascorbic acid two oleyl alcohol ester 1.0 (water) Rosa centifolia extract 3.0 (50% 1,3-BDO extract) ursin 1.0 dipropylene glycols 3.0 polyethylene glycol 1500s 0.5 zinc white 15.0 kaolin 8.0 ion exchange waters 61.1 (preparation method)
At room temperature evenly prepare water.To wherein adding the pure phase of preparation at room temperature, mix homogeneously obtains mixing powder profile film.
Embodiment 18 absorptive ointments
Blending constituent (% weight) (1) vaseline 40.0 (2) stearyl alcohol 18.0 (3) haze tallows, 20.0 (4) polyoxyethylene (10 moles) monooleates 0.25 (5) glyceryl monostearate 0.25 (6) intacellin 0.5 (7) Rosa centifolia extract (ethanol extract) 0.5 (8) ion exchange water 20.5 (preparation method)
(6), (7) are added in (8), remain on 70 ℃ (waters).On the other hand, with (1)-(5) at 70 ℃ of mixed dissolutions (oil phase).Oil phase is added aqueous phase, and by the homogeneous mixer uniformly emulsify, cooling obtains absorptive ointment then.
Embodiment 19 toner blending constituents (% weight) (water) ion exchange water 83.6098 glycerine 5.01,3-butanediol 2.0 ascorbic acid-2-glucoside 1.0 Rosa centifolia extracts (water extract) 0.01 light blue 0.0002 editate 0.1 caustic potash 0.2 natrium citricum, 0.15 citric acid 0.03 (pure phase) ethanol (95%) 7.0 polyoxyethylene (60 moles) hardened castor oil ether 0.3 vitamin E acetate 0.1 spices 0.05 methyl p-hydroxybenzoate 0.15 phenoxetol 0.3 (preparation method)
Water and alcohol mutually after each uniform dissolution, are added to aqueous phase with alcohol, uniform mixing.
Embodiment 20 toner blending constituents (% weight) (water) ion exchange water 79.6647 glycerine 5.0 PEG400s 2.0 xylitols 0.5 ascorbic acid-2-glucoside 1.0 Rosa centifolia extracts (water extract) 0.005 fast green 0.0003 metaphosphoric acid 0.1 xanthans 0.1 mosanom 0.1 hyaluronic acid 0.1 trimethylglycine 3.0 caustic potash 0.4 sodium lactate 0.1 lactic acid 0.03 (pure phase) ethanol (95%) 7.0POE oleyl alcohol ether 0.3 vitamin E acetate 0.1 spices 0.05 methyl p-hydroxybenzoate 0.15 phenoxetol 0.3 (preparation method)
Water and alcohol mutually after each uniform dissolution, are added to aqueous phase with alcohol, uniform mixing.
The Dermatologic preparation for beautifying of confirming the foregoing description 3-20 all has good effect in the whitening effect test.Utilizability on the industry
As mentioned above, the invention provides and have tyrosinase activity simultaneously and suppress effect and cyclic adenosine monophosphate (cANP) and produce and suppress effect, have good melanocyte and generate the high completeness Dermatologic preparation for beautifying that suppresses effect, whitening effect.

Claims (4)

1. Dermatologic preparation for beautifying is characterized in that containing the Rosa centifolia L (R.centifolia L. or R.gallica L.var.centifolia (L.) Reg.) that belongs to Rosaceae (Rosaceae) Rosa (Rosa) or its solvent extractable matter as effective ingredient.
2. Melanogenesis inhibitor is characterized in that containing the Rosa centifolia L that belongs to the Rosaceae Rosa or its solvent extractable matter as effective ingredient.
3. tyrosinase activity inhibitor is characterized in that containing the Rosa centifolia L that belongs to the Rosaceae Rosa or its solvent extractable matter as effective ingredient.
4. cyclic adenosine monophosphate (cAMP) produces inhibitor, it is characterized in that containing the Rosa centifolia L that belongs to the Rosaceae Rosa or its solvent extractable matter as effective ingredient.
CNB018131077A 2000-07-19 2001-07-17 External preparations for beautifying skin Expired - Fee Related CN1229094C (en)

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CN1229094C (en) 2005-11-30
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