CN102240255A - Whitening composition containing tyrosinase inhibitor - Google Patents

Whitening composition containing tyrosinase inhibitor Download PDF

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CN102240255A
CN102240255A CN 201110131717 CN201110131717A CN102240255A CN 102240255 A CN102240255 A CN 102240255A CN 201110131717 CN201110131717 CN 201110131717 CN 201110131717 A CN201110131717 A CN 201110131717A CN 102240255 A CN102240255 A CN 102240255A
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tyrosinase inhibitor
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whitening
lightening compositions
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李明贞
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Abstract

The invention discloses a whitening composition containing a tyrosinase inhibitor which comprises 0.1%-2.5% of tyrosinase inhibitors CitrusC, 0.1%-2.5% of vitamin C glucosides (Ascorbic Acid 2-Glucoside) and 0.1%-2.5% of Tranexamic Acid (Tranexamic Acid) by weight. The above components interact in cooperation to enhance skin whitening.

Description

The lightening compositions that contains tyrosinase inhibitor
Technical field
The present invention relates to a kind of cosmetics, more detailed it, be to refer in particular to a kind of lightening compositions that contains tyrosinase inhibitor, but it is the effect of restraint of tyrosinase, form melanin to prevent its spontaneous polymerization in skin.
Background technology
No matter is not hot summer, be the spring, summer, autumn and winter throughout the year, and whiten is the favorite popular topic of full Asia women always.Show that according to the A.C.Nielsen research report women white degree of liking to be beautiful in Taiwan is in the second in the world, is only second to Korea S.
See also shown in Figure 1ly, melanin is in the synthetic catalytic action that depends on multiple ferment of black corpusculum, and wherein one of most important ferment is tryrosinase (tyrosinase).Tryrosinase at first becomes L-3 with tyrosine (tyrosine) hydroxylation, 4-dihydroxyphenylalanine (degree crust; L-dopa).DOPA is degree of being transformed into crust quinone (dopaquinone) soon.Degree clings to intermediate product that occupies the watershed in the process that quinone is melanin formation.Aminothiopropionic acid (cysteine) or glutathion (glutathione) are being arranged when sulfydryl is provided, dopaquinone is transformed into cysteinyldopa, reoxidizes and polymerization changes into the class melanin (pheomelanin) of solubility yellowish-brown.As providing of sulfydryl is not provided, then dopaquinone is cyclized into the dopachrome intermediate product of orange spontaneously.The carboxyl of Dopachrome is lost spontaneously and is produced 5,6-dihydroxyindole (DHI), and oxidation and polymerization change into insoluble high-molecular weight dark brown DHI-melanin rapidly again.If there is dopachrome keto-enol interconvertible enzyme (tautomerase) to exist, dopachrome just can not lose carboxyl, and can be transformed into DHI-2-carboxylic acid (DHICA), reoxidize with polymerization and change into than light brown, solvable slightly, medium sized DHICA-melanin.DHI-melanin and DHICA-melanin are the members of eumelanin (eumelanins), and melanin comprises eumelanin and this two classes pigment of class melanin exactly.
The composition of whitening is at present weeded out the old and bring forth the new, and Japanese cosmetics use the composition of whitening, the American-European cosmetics of draft extraction then to use living skill extraction more, and external maintenance composition is also followed in Taiwan more.The more common composition of whitening in the present skin care products has comprised left-handed vitamin C, vitamin C derivant, kojic acid, Arbutin, vitamin A, fruit acid and some plant extracts.The whitening medicaments composition that belongs to pharmaceutical grade then comprises hydroquinone, azelaic acid, reaches A acid etc., all is to use through physician's prescription.Because of mentioned component mostly is tyrosine ferment competitive inhibitor, before its mechanism of action mainly ties up to the effect of tyrosine ferment, try to be the first and tyrosine (tyrosine) effect, and then tryrosinase (tyrosinase) can't be acted on tyrosine (tyrosine), reach the order ground that suppresses the melanin generation.
But this type of tyrosine ferment competitive inhibitor could act under low ph environment except needs, and for asking the whitening effect that can reach better, its desired content ratio needs more than the finite concentration, the tryrosinase (tyrosinase) of just trying to be the first acts on tyrosine (tyrosine), reaches the effect that suppresses the melanin generation.But also cause the skin irritation sense big more, easily human skin is caused irritated uncomfortable because of concentration is high more.And this type of tyrosine ferment competitive inhibitor composition mostly is the photosensitivity material greatly, to the light instability, browning phenomenon is easily arranged (as Arbutin, kojic acid Kojic acid), xanthochromia phenomenon (ascorbic acid Ascorbic acid and derivant thereof) produces, cause whitening product to be everlasting and used a period of time variable color such as flavescence blackening, cause product stability not good, can cause transportation to store last difficulty again.
Moreover, known whitening product includes divides into the day and night product of two kinds of different components, and product mainly is based on sun composition in the daytime, in order to reduce human skin in the chance that tanned by the sun by ultraviolet in the daytime, to reduce the generation of melanin, night, product was then whitened based on reparation.Yet the trouble when this kind occupation mode is produced and sold except causing, product may cause outside the poor effect if user is misapplied day and night, also might cause the generation of minus effect.
Summary of the invention
In view of addressing the above problem, the present invention proposes a kind of scheme that contains the lightening compositions of tyrosinase inhibitor, and this scheme has composition and obtains convenience, low price, optimal reaction is arranged under neutral pH 7~pH9, is difficult for human skin is caused irritated uncomfortable and tool light stability, is convenient to the advantage of transportation storage.
A kind of lightening compositions that contains tyrosinase inhibitor of the present invention, it consists predominantly of:
The tyrosinase inhibitor of 0.1-2.5% percentage by weight (CitrusC);
The vitamin C glucosides of 0.1-2.5% percentage by weight (Ascorbic Acid 2-Glucoside); And
The bright acid of the biography of 0.1-2.5% percentage by weight (Tranexamic Acid).
In preferred embodiment of the present invention, this tyrosinase inhibitor (CitrusC) is via the method extraction that comprises the following step and get: (1) gets Fericarpium Citri Limoniae, with itself and mixed with propylene glycol; (2) Cell wall of Fericarpium Citri Limoniae cell in the above-mentioned mixed liquor is broken; (3) remove Fericarpium Citri Limoniae and must this extract.
In preferred embodiment of the present invention, the described Fericarpium Citri Limoniae of step (1) is fresh Fericarpium Citri Limoniae, and cuts into pieces.
In preferred embodiment of the present invention, the concentration of described propylene glycol is higher than 50%; More preferably, the concentration of described propylene glycol is higher than 70%; Best, the concentration of described propylene glycol is higher than 80%.
In preferred embodiment of the present invention, the ratio of described Fericarpium Citri Limoniae and propylene glycol is 0.1g/ml-1g/ml.
In preferred embodiment of the present invention, the ratio of described Fericarpium Citri Limoniae and propylene glycol is 0.2g/ml-0.8g/ml.
In preferred embodiment of the present invention, described method of cell disruption comprises ultrasound wave, tissue mashing machine (Waring blender), homogenizer (Homogenizer), French cell press (French cell press) or high speed homogenization mulser (Polytron).
In preferred embodiment of the present invention, described step (2) also comprises sterilization steps afterwards.
In preferred embodiment of the present invention, described sterilization comprises adopts microwave sterilizating, filtration sterilization, ultraviolet disinfection or gamma radiation etc.
The present invention reaches one of effect, tyrosinase inhibitor in the said composition (CitrusC), vitamin C glucosides (Ascorbic Acid 2-Glucoside) can interact to promote skin-whitening effectively synergistically with the bright acid of biography (Tranexamic Acid), can when using, first week have the whitening effect of the best to present, even under the use through long-term (more than continuous two weeks), it still has the melanic effect of suitable reduction.
The present invention reaches two of effect, and the present invention uses tyrosinase inhibitor (CitrusC) as the composition of whitening, and it time has optimal reaction in neutral pH=7~9.
The present invention reaches three of effect, and the tyrosinase inhibitor that the present invention uses (CitrusC) is noncompetitive inhibitor, need not high concentration and can effectively suppress melanin formation.
The present invention reaches four of effect, and the tyrosine ferment inhibitor tool light stability of the present invention's use is not because of light makes the product variable color, so container package that need not special screening optical activity.
Description of drawings
Fig. 1 is the generation type sketch map of known melanin.
Fig. 2 is the present invention's experiment flow sketch map.
Fig. 3 is positive effect (Positive effect%) schematic diagram data () of each group sample.
Fig. 4 is positive effect (Positive effect%) schematic diagram data (two) of each group sample.
Fig. 5 is the intensity of whitening (Whitening intensity%) schematic diagram data of each group sample.
The specific embodiment
For ease of explanation the present invention represented central idea in foregoing invention content one hurdle, express with specific embodiment now.Various different assemblies system is in the ratio that is suitable for exemplifying explanation among the embodiment, but not drawn in the ratio of actual component, close chat earlier bright.
The applicant had before got permission Taiwan I313177 patent system a kind of method that extracts the mixture that contains tyrosine ferment inhibitor in Fericarpium Citri Limoniae was provided: get fresh Fericarpium Citri Limoniae, with its chopping, add propylene glycol again and mix with it.Its mixed proportion is: the broken Fericarpium Citri Limoniae of every 100g adds the propylene glycol of 100-1000ml.This mixed liquor is fully mixed, utilize ultrasonic treatment 1~59 second, sterilize with microwave irradiation again, then mixed liquor is carried out centrifugalize, get the mixture of whitening that contains tyrosine ferment inhibitor that upper strata liquid is the present invention to break cell wall.If get the Fericarpium Citri Limoniae that 100g smashes, extract according to said method, can get the mixture of whitening of propylene glycol volumetric usage 70-90%.
This is one from Fericarpium Citri Limoniae extraction, is referred to as CitrusC through the mixture of whitening that contains tyrosine ferment inhibitor of partial purification gained, and it contains a kind of protein, wins peptide, flavonoid element and flavone compositions such as (flavonoid).Though this protein is tyrosine ferment inhibitor, other composition or the addition effect is arranged, or antiageing effect is arranged, do not need excessive purification thereby relative cost low.
Tyrosine ferment inhibitor (CitrusC) raw material that is extracted according to applicant Taiwan I313177 patent has following characteristic:
1. noncompetitive inhibitor need not high concentration and can effectively suppress melanin formation.
2. at 25-37 ℃ the tyrosine ferment is had high restraint, it can bring into play maximum activity about 25 ℃, even still can reach nearly about 80% inhibition effect to the tyrosine ferment under 37 ℃ (body temperature).
3. optimal reaction time is arranged in neutral pH=7~9, gentle relatively to human skin, be difficult for producing and stimulate anaphylaxis.
4. have a light stability, not because of light makes the product variable color, so container package that need not special screening optical activity is convenient to transportation relatively and is stored.
5. 1,4-benzoquinone (O-QUINONE) has reducing power, can in the generation of melanin cross in, with oppositely reduction of product benzoquinone (O-QUINONE) between among the melanin,, increase whitening effect with the generation of blocking-up melanin.
6. made by the citrus peel, raw material is obtained easily.
This inhibitor is to extract from the citrus peel, through the part biochemical reaction, Main Ingredients and Appearance has flavone (flavonoid) and a kind of victory peptide, this wins peptide is tyrosine ferment inhibitor, other composition of whitening is had the effect of addition, and flavone (flavonoid) has the effect of aging resistance and anti-inflammatory.Its production process does not need excessive purification, and relative cost also can reduce.
So invention will be developed a series of whitening products with Taiwan I313177 patent tyrosine ferment inhibitor raw material as the whitening product effective ingredient, and with its whitening effect of human trial digital proof.
[materials and methods]
One, material
(1) whiten 300 altogether of effectiveness laboratory samples, it is grouped as follows:
1.A group: cream (Creambase)+pass bright acid (Tranexamic Acid) (50 groups)
2.B group: cream (Creambase)+tyrosinase inhibitor (CitrusC) (50 groups)
3.C group: cream (Creambase)+vitamin C glucosides (AA2G) (60 groups)
4.D group: cream (Creambase)+pass bright acid (Tranexamic Acid)+vitamin C glucosides (AA2G)+tyrosinase inhibitor (CitrusC) (80 groups)
5.E group: soft emollient cream of Nivea (30 groups), the about 1 yuan/ml of market price.
6.F group: the fair-skinned cream of Shiseido hundred excellent victories (30 groups), the about 55 yuan/ml of market price.
(2) component prescription:
A, B, C, D group sample composition formula table is as shown in table 1; E and F group are then distinctly listed its composition with table 2 and table 3.
(3) for avoiding experimenter and tester that psychological expectations are arranged, then these 300 groups of samples are all enrolled 1~No. 300 with random number.
Table 1.A, B, C, D group sample composition prescription
Figure BDA0000062335560000051
Figure BDA0000062335560000061
The soft emollient cream composition of table 2.E group Nivea
Figure BDA0000062335560000062
Figure BDA0000062335560000071
The fair-skinned cream composition of table 3.F group Shiseido hundred excellent victories
Figure BDA0000062335560000072
Figure BDA0000062335560000081
Figure BDA0000062335560000091
Two, experimental design
(1) test method of the Sederma of this laboratory reference Merck subsidiary is modified again.Experimental design is represented with Fig. 2.
(2) instrument
Computer: ASUS UL30A system: Joy Silky instrument: Qiao Shi skin matter analyzer
(3) experimental subject
Screen the men and women of the Jiankang skin in 300 experimenter 18-30 years.This experiment mainly with the state-run teachers and students of National Pingtung University of Science ﹠ Technology as tested object.
(4) experimental technique
With the original skin conditions of two hands the back of the hand (Day0) about the instrument detecting experimenter, experimenter's left hand and right hand distinguishes experimental group and matched group (left hand the back of the hand is smeared the big small sample of about grain of rice, right hand the back of the hand is not smeared) uses twice sooner or later, in l after week (the 7th day) measure the experimenter and use the numerical value (D7) of sample after 7 days, measure experimenters in 2 week backs (the 14th days) and use the numerical value (D14) of sample after 14 days.
(5) data representation
Numerical value is with l~100 expressions, and the more little expression melanin of numerical value is few more, otherwise the big more melanin of numerical value is many more.
(6) the degree quantization formula of whitening
1. use 7 day the whiten degree (T0-7) of sample after first week:
T0-7=[(D0-D7)-(D’0-D’7)]/[(D0+D’0)/2]×100%
2. use 7 day the whiten degree (T7-14) of sample after second week:
T7-14=[(D7-D14)-(D’7-D’14)]/[(D7+D’7)/2]×100%
3. use 14 days degree of whitening (T0-14) in 2 weeks of sample continuously:
T0-14=[(D0-D14)-(D’0-D’14)]/[(D0+D’0)/2]×100%
D0: experimental group (left hand the back of the hand) its skin initial condition in the time of the 0th day.
D7: experimental group (left hand the back of the hand) its skin condition in the time of the 7th day.
D14: experimental group (left hand the back of the hand) its skin condition in the time of the 14th day.
D ' 0: matched group (right hand the back of the hand) its skin initial condition in the time of the 0th day.
D ' 7: matched group (right hand the back of the hand) its skin condition in the time of the 7th day.
D ' 14: matched group (right hand the back of the hand) its skin condition in the time of the 14th day.
4. the numerical value that obtains with above-mentioned three kinds of formulas represents that on the occasion of the person its sample has whitening effect to the experimenter, add up to this group sample be on the occasion of number organize effective numerical value divided by this and then can obtain positive effect Positive effect (%).
Three, result and discussion
The main whitening effect of inquiring into the cream sample of different formulations to human body of this test.
Wherein specimen mainly is divided into six groups: the A group is added the cream that 0.1-2.5% passes bright acid (Tranexamic Acid) antiallergic composition for substrate prescription cream, B group and C group are distinctly added 0.1-2.5% tyrosinase inhibitor (CitrusC) whitening composition for substrate prescription cream or are done the composition of the 0.1-2.5% vitamin C glucosides (AA2G) of antioxidant, and the D group then is that substrate prescription cream interpolation 0.1-2.5% passes bright acid (Tranexamic Acid), 0.1-2.5% tyrosinase inhibitor (CitrusC) and 3 kinds of compositions of 0.1-2.5% vitamin C glucosides (AA2G).And E group and F group are to be regarded as the positive control group by commercially available soft emollient cream of open-shelf Nivea and the fair-skinned cream of special counter Shiseido hundred excellent victories in this test, and can understand specimen and commercially available prod, its whitening effect degree and diversity by this experiment.And the component list of E group and F group, then shown in table 2 and table 3: E assembly Fang Zhongwei contains the active ingredient of whitening, only add benzyl salicylate (Benzyl salicylate) as UV absorbent, and contain the whitening composition of vitamin C glucosides (Ascorbyl Glucoside) in the F group, the plant extraction composition that also contains other function, (Tamarix chinensis extract) is Ji extracts such as Ren Ginseng, Rhizoma Zingiberis Recens, Radix Scutellariae, Paeonia suffruticosa, Fructus Rosae Normalis as the Ramulus et Folium Tamaricis extract.
Experimental subjects is mainly student of TaiWan, China National Pingtung University of Science ﹠ Technology and teaching and administrative staff 300 people, about 1: 2 of this experiment M-F, and the range of age 18~30 years old is main screening conditions to have healthy skin.
Table 4 is the effectiveness experimental data of whitening of different formulations cream.By the 3rd figure as can be known A group contain 0.1-2.5% and pass bright acid (Tranexamic Acid) prescription cream sample in 41 experimenters, use the generation that has 46% people that whitening effect is arranged after 7 days, use second week the back than the people of the first week minimizing 2%, and the effect of using 4 one-tenth the people's tool of only having an appointment in 14 days to whiten continuously.Use 2 all A assembly quadrat sampling product as can be known continuously, its tester who produces whitening effect there is no the trend that continues to increase.
41 experimenters of B assembly quadrat sampling product have 44% people that the generation of whitening effect is arranged after using a week, and use the 7th day to 14 days identical with first week, and used for 2 weeks had 4 one-tenth 6 people that the melanic situation of reduction is arranged continuously.Its result shows that the experimenter uses the cream that adds 0.1-2.5% tyrosinase inhibitor (CitrusC), has the people near 44% using a Zhou Houneng that melanin is reduced, and using continuously had 4 one-tenth 7 people that whitening effect is arranged in two weeks, than A group many 5%.In other words, tyrosinase inhibitor (CitrusC) really tool promote the effect whiten.
And C group sample is a substrate prescription cream interpolation 0.1-2.5% vitamin C glucosides (AA2G), uses first all backs to Duo 3%, there was no significant difference than the A group.Using for second week reduced by 5% than first week, and use continuously two week residue 40% testee the generation of whitening effect is arranged.The result shows that its whitening effect of cream that adds vitamin C glucosides (AA2G) had outside the good slightly performance in use in first week, increased in time and can't continue to increase its function.Inference is added separately under the cream life-time service of vitamin C glucosides (AA2G) composition, and mainly as antioxidant usefulness, its whitening effect persistence is subjected to certain restriction to vitamin C glucosides (AA2G) at this prescription.
D group cream sample respectively adds 0.1-2.5% in wherein for passing bright acid (Tranexamic Acid), tyrosinase inhibitor (CitrusC) and vitamin C glucosides (AA2G).Using the D group to have 53% people that the generation of whitening effect is arranged after 7 days, it is soprano in six groups of samples.In other words, the prescription that add to pass bright acid (Tranexamic Acid), tyrosinase inhibitor (CitrusC) and vitamin C glucosides (AA2G) really tool whiten to add and take advantage of effect.So in second 7 day cycle, or because of other external environment factor, more frequent as student's outdoor activities, still have nearly 4 one-tenth testee to possess the effect that continues to whiten.If specimen is used under the situation in two weeks continuously, still have 44% testee to manifest the situation that melanin reduces.
Relatively A, B, C, D organize sample, respectively adding the 0.1-2.5% prescription with the bright acid (Tranexamic Acid) of D group biography, tyrosinase inhibitor (CitrusC) and vitamin C glucosides (AA2G) after the use of first week has the whitening effect of the best to present, and next is that the independent C that adds vitamin C glucosides (AA2G) organizes.And in second 7 day cycle, then better performance being arranged with A group and B group, other C, D all hang down 5~8% than A, B group for three groups.And use continuously under the situation in two weeks with the B group 46% for the highest, secondly for D organize 44%, and that C organizes is minimum.Synthetic data shows that D assembly side adds the effect of taking advantage of mutually because of the bright acid (Tranexamic Acid) of interpolation biography simultaneously, tyrosinase inhibitor (CitrusC) and vitamin C glucosides (AA2G) 0.1-2.5% have its whitening effect, there is the effect of the best to present in the time of can using in first week, passes through under the use in continuous two weeks it and reduce melanic ability and still possess certain effect.
And the E of commercially available prod group soft emollient cream of Nivea and the fair-skinned cream of F group Shiseido hundred excellent victories, its result who presents is not but as expection in this experiment.The E group has 44% experimenter to produce whitening effect after first week of use, and the experimenter of the second week increase nearly 8% reduces melanic situation.But, then keep 44% testee tool whitening effect if continue to use for two weeks.And F group is in first week and there was 41~52% whitening effect to produce in second week, but reduces by 7~13% in the effect of using for two weeks continuously than other five set product.According to containing benzyl salicylate (Benzyl salicylate) in its composition supposition E group sample, normal UV absorbent in the skin care products as sun-proof function, directly isolated ultraviolet contacts human body skin from the source in the approach that melanin forms, blocking-up melanin forms, and because of human skin cell's metabolism in 21~28 days once, also decomposing melanin in the time of cellular metabolism, so it reduces melanic probability and 2 weeks still can keep 44% effect using continuously under the situation.And F group sample uses under the situation in two weeks this experiment test person continuously, whitening effect only has 1/3 testee tool whitening effect, its reason or reduce because of factors such as individual variation, life habit and outdoor activities may cause whitening effect, but with regard to its composition table as can be known its formula components unexpectedly up to kind more than 50 (table 3).Whether cause the absorption capture-effect too much because of containing the composition kind, cause reducing the melanin effect and have a greatly reduced quality, its definite occurrence cause and reaction machine change, and wait further discussion.
Can find obviously that from the 4th figure A, C, D group sample are after using for second week, it reduces the melanin probability and all is downward trend, infer former in response to relevant with the skin adaptability, use product after first week, its whitening effect represents ratio and all reaches more than 45%, but second week descended, show that skin is to the cream composition, or because of under the situation about increasing between in use, Skin Cell adapts to its white-skinned face function gradually, causes to reduce melanic relative effect and can't continue to increase.
The effectiveness experiment of whitening of table 4. different formulations cream
Figure BDA0000062335560000121
* T0-7For use sample record after first week 7 days, T7-14Record in second back 7 days of the week of use sample, T0-14For using the sample time in two 14 days weeks continuously
The whiten trend of degree (index) of relevant different group, difference can be known from table five and the 5th figure and point out that using each set product after one week, degree and expected result that it is whitened quite meet.The effect of A group is the poorest, and the effect that the B group has promotion to whiten because of interpolation tyrosinase inhibitor (CitrusC), C group are added vitamin C glucosides (AA2G) and still had certain whitening effect to promote, but the effect of too late tyrosinase inhibitor (CitrusC).As for D group data show, it is better than the effect of both independent interpolations to add biography bright acid (Tranexamic Acid), tyrosinase inhibitor (CitrusC) and vitamin C glucosides (AA2G) simultaneously.And two kinds of commercially available positive control set products, its whitening effect manifests preferable white-skinned face function in the middle of this experiment test person, particularly the fair-skinned cream of Shiseido hundred excellent victories of F group.Yet overall data shows that each set product all presents downward trend at the whitening effect in second week, but adds the B group exception of tyrosinase inhibitor (CitrusC), and its whitening effect still continued to represent in second week, even effect is better.And two kinds of commercially available positive matched groups, unexpectedly at the white-skinned face function in second week, far away from other group, even than A group weak effect, its reason still remains to be differentiated in this experiment test person.But if inspect 14 days white-skinned face function of continuous use, then produce different variations and deciphering again, wherein represent best effect with commercially available positive control F group, the persistence quite stable of its whitening effect as if, and another commercially available E group also represents good effect.Comprehensively above-mentioned, in this research with the product of D group on chronergy of whitening and degree of stability, best results comparatively speaking.
The degree of whitening of table 5. different formulations cream its different service times
Figure BDA0000062335560000132
Figure BDA0000062335560000141
T0-7Record in first back 7 days of the week of sample for using, T7-14Record in second back 7 days of the week of use sample, T0-14For using the sample time in two 14 days weeks continuously
Four, conclusion
(1) D assembly side adds the effect of taking advantage of mutually because of the bright acid of the biography of adding 0.1-2.5% simultaneously (Tranexamic Acid), tyrosinase inhibitor (CitrusC) and vitamin C glucosides (AA2G) have its whitening effect, there is the effect of the best to present in the time of can using in first week, through under the use in continuous two weeks its to reduce melanic effect still not poor, and not second to the commercially available prod.The formula for a product of suggestion commercialization is an optimum selection with the D group.
The present invention utilizes directly restraint of tyrosinase (tyrosinase) effect of tyrosinase inhibitor (Citrus C), prevents the synthetic reaction of melanin, to reach the effect of whitening.And be only conduct reaction catalyst in chemical reaction of tyrosinase inhibitor (Citrus C) with known whitening product difference, itself does not consume with tryrosinase (tyrosinase) effect, therefore do not need high dose, high concentration, can reach the effect of whitening.
Wherein, this vitamin C glucosides (Ascorbic Acid 2-Glucoside) is the derivant of a vitamin C; though it has been proved reduction effect for one melanin that has generated in laboratory; but because of its molecular weight is difficult to greatly be absorbed by human skin; in the human experimentation process; the whitening effect that adds vitamin C glucosides (Ascorbic Acid2-Glucoside) merely in the constituent of whitening is not good; but because of it is obtained relatively easily; the present invention system utilizes its protection tyrosinase inhibitor (Citrus C) and so on flavone, makes its maintenance not oxidized in order to preservation.
Moreover, because the present invention's tyrosinase inhibitor (Citrus C) is mainly the extract of pure natural, the protein that is comprised in it may produce anaphylaxis for part people's skin, therefore the present invention is use height commercialization at present, obtains the bright acid of easy biography (Tranexamic Acid) in order to avoid the usefulness of allergy and anti-inflammatory, one content that passes bright acid (Tranexamic Acid) need reach ability Pear Power effect more than 3%, the present invention only adds 0.1-2.5% as the non-purpose for whitening of usefulness of avoiding allergy and anti-inflammatory, closes earlier and states clearly.
(2) contain benzyl salicylate (Benzyl salicylate) in the E group sample, in the approach that melanin forms, the directly isolated ultraviolet contact human body skin from the source, blocking-up melanin forms, and the time because of cellular metabolism, also decomposing melanin, so it reduces melanic probability and still can keep effect more than 44%, equally matched with this experiment test sample effect.
(3) F group sample is using under the situation in two weeks continuously, its testee of only surplus 1/3 represents whitening effect, the quite diversification though trace it to its cause, as individual variation, life habit and outdoor activities etc., but its formula components is up to kind more than 50, or, cause certain time point absorption capture-effect and cause whitening effect to reduce also not without possibility because of formula components is many and complicated.
(4) in this research with the product of D group on chronergy of whitening and degree of stability, best results comparatively speaking.
Though the present invention does explanation with a most preferred embodiment, be skillful in this skill person and can make various multi-form changes not breaking away under the present invention spirit and the category.Above illustrated embodiment is only in order to explanation the present invention, and is non-in order to limit the present invention's scope.Such as do not disobey various modifications or the variation that spirit of the present invention is engaged in, all belong to the present patent application claim.

Claims (10)

1. lightening compositions that contains tyrosinase inhibitor comprises:
The tyrosinase inhibitor of 0.1-2.5% percentage by weight;
The vitamin C glucosides of 0.1-2.5% percentage by weight; And
The bright acid of the biography of 0.1-2.5% percentage by weight.
2. a kind of lightening compositions that contains tyrosinase inhibitor as claimed in claim 1 is characterized in that: this tyrosinase inhibitor system is via the method extraction that comprises the following step and get: (1) gets Fericarpium Citri Limoniae, with itself and mixed with propylene glycol; (2) Cell wall of Fericarpium Citri Limoniae cell in the above-mentioned mixed liquor is broken; (3) remove Fericarpium Citri Limoniae and must this extract.
3. a kind of lightening compositions that contains tyrosinase inhibitor as claimed in claim 2 is characterized in that: the described Fericarpium Citri Limoniae of step (1) is fresh Fericarpium Citri Limoniae, and cuts into pieces.
4. a kind of lightening compositions that contains tyrosinase inhibitor as claimed in claim 2, it is characterized in that: the concentration of described propylene glycol is higher than 50%.
5. a kind of lightening compositions that contains tyrosinase inhibitor as claimed in claim 2, it is characterized in that: the concentration of described propylene glycol is higher than 80%.
6. a kind of lightening compositions that contains tyrosinase inhibitor as claimed in claim 2 is characterized in that: the ratio of described Fericarpium Citri Limoniae and propylene glycol is 0.1g/ml-1g/ml.
7. a kind of lightening compositions that contains tyrosinase inhibitor as claimed in claim 2 is characterized in that: the ratio of described Fericarpium Citri Limoniae and propylene glycol is 0.2g/ml-0.8g/ml.
8. a kind of lightening compositions that contains tyrosinase inhibitor as claimed in claim 2 is characterized in that: described method of cell disruption is ultrasound wave, tissue mashing machine, homogenizer, French cell press or high speed homogenization mulser.
9. a kind of lightening compositions that contains tyrosinase inhibitor as claimed in claim 2 is characterized in that: described step (2) also comprises sterilization steps afterwards.
10. a kind of lightening compositions that contains tyrosinase inhibitor as claimed in claim 9 is characterized in that: microwave sterilizating is adopted in described sterilization.
CN 201110131717 2011-05-19 2011-05-19 Whitening composition containing tyrosinase inhibitor Pending CN102240255A (en)

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CN102488921A (en) * 2011-12-22 2012-06-13 韩大庆 Auxiliary agent for enhancing biocompatibility of magnesium phosphate cement and magnesium phosphate cement
CN104886241A (en) * 2015-05-08 2015-09-09 江南大学 A browning inhibitor for fresh-cut fruits and vegetables and a preparation method thereof

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Publication number Priority date Publication date Assignee Title
CN102488921A (en) * 2011-12-22 2012-06-13 韩大庆 Auxiliary agent for enhancing biocompatibility of magnesium phosphate cement and magnesium phosphate cement
CN102488921B (en) * 2011-12-22 2013-10-16 韩大庆 Use of substance chelating with potassium or magnesium ion in auxiliary agent for enhancing biocompatibility of magnesium phosphate cement and the magnesium phosphate cement
CN104886241A (en) * 2015-05-08 2015-09-09 江南大学 A browning inhibitor for fresh-cut fruits and vegetables and a preparation method thereof
CN104886241B (en) * 2015-05-08 2018-06-08 江南大学 A kind of fresh-cut fruit and vegetable browning inhibitor and preparation method thereof

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Application publication date: 20111116