One kind resists allergic composition
Technical field
The present invention relates to one kind to resist allergic composition.
Background technology
In recent years, with the change of dietary structure, atmosphere pollution, the increase of live and work pressure, autopath is drastically
Increase.Especially in developed countries such as Japan, the U.S., skin sensitivity has become the social concern for influenceing human health.According to
Incomplete statistics, the crowd that the whole world feels sensitiveness skin is more and more, and wherein male accounts for 38%, and women accounts for 61%.Therefore
Cosmetics with antiallergic anti-irritant effect are increasingly subject to the attention of people, have the material of antiallergic anti-irritant activity, especially
Botanical components are favored by scholar and market.With modern experimental means research Chinese traditional herbs, it will help excavate high
Effect, low toxicity, the antiallergy product of low side effect.
Common cutaneous anaphylaxis is referred to as hypersensitivity, also known as allergy in medical science, refers to body by some anti-
During primary stimuli, there is the abnormal specific immune response based on physiological dysfunction or tissue cell insult.It takes
Certainly in two factors:The stimulation of antigen and the reactivity of body.Allergic constitution(irritable the physique)Usually
Allergic reaction and anaphylactia and the people that can not find pathogenic factor occurs by easy, is referred to as " allergic constitution ".Induced
The antigen of quick reaction is referred to as anaphylactogen.The antigenic substance to cause allergic reaction has hundreds of kinds, and they are by sucking, eating, injecting
Or the mode such as contact makes body sensitization.
According to traditional Chinese and western medicine and biology to allergic relevant explanation, with reference to the principle of the traditional Chinese medical science " integrated control ", make up
Product prevent and treat skin sensitivity and are with the common approach stimulated:1. away from anaphylactogen, sensibiligen autostimulation is reduced;2. suppress histamine
Etc. inflammatory mediator release;3. strengthen body barrier function;Above controlling way, the blocking of any one can all obtain certain anti-
Effect is controlled, but to reach good antiallergic effect, it should uses for reference and " overall preventing and treating " idea of the application traditional Chinese medical science, comprehensively and forms net
The preventing and treating of network shape, it can be only achieved excellent antiallergic effect.
The content of the invention
It is an object of the invention to provide a kind of composition with anti-allergic effects.Present invention also offers said composition
Purposes.
The invention provides one kind to resist allergic composition, it be prepared by the raw material of following weight proportion it is outer
Use preparation:
Purslane extract 3-5 parts, herba hedyotis diffusae extract 2-5 parts, shrubby sophora extract 1-3 parts, mint extract 2-3
Part, Radix Sangusorbae extract 1-3 parts, Chinese rhubarb extract 0.5-1 parts.
Further, it is the external preparation being prepared by the raw material of following weight proportion:
5 parts of purslane extract, 4 parts of herba hedyotis diffusae extract, 2 parts of shrubby sophora extract, 2 parts of mint extract, garden burnet
2 parts of extract, 1 part of Chinese rhubarb extract.
Wherein, in the purslane extract, calculated by dry product, general flavone content is no less than 15%w/w;Oldenlandia
In careless extract, calculated by dry product, general flavone content is no less than 1.0%w/w;In shrubby sophora extract, calculated by dry product, it is bitter
The total content of ginseng alkali and oxymatrine is no less than 1.2%w/w;In mint extract, calculated by dry product, general flavone content is not
Less than 2.0%w/w;In Radix Sangusorbae extract, gallic acid content is no less than 4.0%w/w;In Chinese rhubarb extract, calculated by dry product,
The total content of rheum emodin and Chrysophanol is no less than 0.45%w/w.
Further, in the purslane extract, calculated by dry product, general flavone content 18-25%w/w;Long-noded pit viper
In diffusa extract, calculated by dry product, general flavone content 3-7%w/w;In shrubby sophora extract, calculated by dry product, kuh-seng
The total content of alkali and oxymatrine is 2-4%w/w;In mint extract, calculated by dry product, general flavone content 3-5%w/
w;In Radix Sangusorbae extract, gallic acid content 4-5%w/w;In Chinese rhubarb extract, calculated by dry product, rheum emodin and Chrysophanol
Total content be 10-12%w/w.
Wherein, the preparation method of each extract is as follows:Corresponding medicinal material is taken, it is non-on water extract respectively after extracting in water
Polarity or intermediate-polarity macroporous adsorption resin post, after ion, then with 70~80%v/v ethanol elutions, ethanol eluate is collected,
Reclaim ethanol after, dry, i.e., respectively each extract.
In view of in ethanol eluate configuration process, ethanol raw material mass discrepancy, the volatilization loss of ethanol situations such as, may
The deviation of caused concentration of alcohol, the concentration of elution ethanol can receive certain error range in the present invention, such as using
65~85%v/v ethanol is eluted.
The nonpolar or intermediate-polarity macroporous adsorption resin post used in the present invention can select commercially available conventional model, such as
Nonpolar macroporous adsorption resin has HPD-100, HPD-300, D-101, X-5 or H103 etc., and intermediate-polarity macroporous adsorption resin has AB-
8, DA-201, HPD-400 or DM301 etc..Above-mentioned model is only for example, specific make to workable macroreticular resin type
Used time can be not limited to above-mentioned model.Consider for materials'use frequency and cost etc., the specific embodiment of the invention
The middle nonpolar macroporous adsorption resin used is D101, intermediate-polarity macroporous adsorption resin DM301.
Wherein, the composition be using each extract as active component, it is auxiliary plus what is commonly used in pharmaceutically or cosmetically
The preparation for external application to skin that material or complementary composition are prepared.
Wherein, the complementary composition is collagen, vitamin, co-ferment Q10 or/and allantoin.
Wherein, the external preparation is face cream, emulsion, gel, toner or facial mask.
Present invention also offers purposes of the above-mentioned composition in Hyaluronidase inhibitor is prepared.
Present invention also offers above-mentioned composition to prepare antiallergy, antipruritic or/and anti-inflammatory external use skin care or medicine
In purposes.
The present composition, by each Chinese medicinal material extract reasonable compatibility, synergistic function is played, to hyaluronidase
Inhibitory activity it is more good, there is significant antiallergy, anti-inflammatory, antipruritic and other effects, there is provided one kind has antiallergy effect
New skin care item or medicine.
Embodiment
The preparation method of 1 each medicinal substances extract of embodiment
The preparation method of extract is as follows:Weigh each raw material of purslane, oldenlandia diffusa, kuh-seng, peppermint, garden burnet, rheum officinale
Medicine, crush as coarse powder, add water to cook respectively three times, 1.5 hours every time;By the decocting liquid of each bulk drug, D101 macropores are crossed respectively
Resin adsorption, is eluted with water colourless to water lotion, with 70%v/v ethanol elutions to colourless, collects 70% ethanol eluate filtrate, filter
Ethanol is recovered under reduced pressure in liquid, concentrate eluant, concentrate spray drying, produces.
With each extract of high effective liquid chromatography for measuring:In purslane extract, weight percentage containing general flavone is
24.80%;In herba hedyotis diffusae extract, weight percentage containing general flavone is 6.25%;In shrubby sophora extract, the alkali containing ginseng and oxygen
The weight percentage for changing matrine is 3.7%;In mint extract, general flavone content 3.2%;In Radix Sangusorbae extract, do not eat
The sour weight percentage of son is 5.5%;In Chinese rhubarb extract, the total amount containing rheum emodin and Chrysophanol is 10.06%.
The preparation method of 2 each medicinal substances extract of embodiment
The preparation method of extract is as follows:Weigh each raw material of purslane, oldenlandia diffusa, kuh-seng, peppermint, garden burnet, rheum officinale
Medicine, crush as coarse powder, add water to cook respectively three times, 1.5 hours every time;By the decocting liquid of each bulk drug, DM301 macropores are crossed respectively
Resin adsorption, is eluted with water colourless to water lotion, with 80%v/v ethanol elutions to colourless, collects 80% ethanol eluate filtrate, filter
Ethanol is recovered under reduced pressure in liquid, concentrate eluant, concentrate spray drying, produces.
With each extract of high effective liquid chromatography for measuring:In purslane extract, weight percentage containing general flavone is
18.56%;In herba hedyotis diffusae extract, weight percentage containing general flavone is 3.85%;In shrubby sophora extract, the alkali containing ginseng and oxygen
The weight percentage for changing matrine is 2.4%;In mint extract, general flavone content 4.8%;In Radix Sangusorbae extract, do not eat
The sour weight percentage of son is 4.1%;In Chinese rhubarb extract, the total amount 11.36% containing rheum emodin and Chrysophanol.
The preparation of 3 face cream of the present invention of embodiment
A oil phases(Percentage by weight)
Beeswax 3.5%, stearic acid 3.2%, glycerin monostearate 1%, hexadecanol 3.0%, white oil 0.5%, dimeticone
0.5%th, vitamin D 0.6%, vitamin E 0.8%;
B aqueous phases(Percentage by weight)
Purslane extract 5%, herba hedyotis diffusae extract 4%, shrubby sophora extract 2%, mint extract 2%, garden burnet extraction
Thing 2%, Chinese rhubarb extract 1%, polyethylene glycol 400 6.5%, carboxyethyl cellulose 0.31%, allantoin 0.5%, vitamin C 0.5%, go
Ionized water complements to 100%;
Preparation method:After aqueous phase and oil phase are heated into fusing respectively, while aqueous phase stirs, it is slowly added into oil phase and stirs
Mix, continue to stir 1h, stop stirring, stand, be cooled to room temperature, produce antiallergy face cream.Each extract comes from the present embodiment
Embodiment 1.
The preparation of 4 emulsion of the present invention of embodiment
A oil phases(Percentage by weight)
Poloxamer 3%, span601.5%, polysorbate60 2%, dimeticone 18%, tragcanth 0.5%, tristerin
5%th, bone collagen 1%, vitamin E 0.8%;
B aqueous phases(Percentage by weight)
Purslane extract 4%, herba hedyotis diffusae extract 3%, shrubby sophora extract 3%, mint extract 2%, garden burnet extraction
Thing 2%, Chinese rhubarb extract 1%, glycerin extract 7%, carbomer 3.5%, ethyl hydroxy benzoate 2%, polypropylene glycol 0.5%, vitamin
B0.5%, vitamin C 0.5%, deionized water complement to 100%;
Preparation method:It is uniformly mixed after oil phase and aqueous phase are respectively melted, slowly will be mixed while oil phase stirs
Aqueous phase after conjunction, which is added in emulsion tank, to be stirred, and is continuously stirred 20min, is stopped stirring, stands cooling room temperature, produces antiallergy breast
Liquid.Each extract comes from embodiment 1 in the present embodiment.
The preparation of the inventive gel of embodiment 5
Raw material is weighed as following weight percent:Purslane extract 4%, herba hedyotis diffusae extract 4%, shrubby sophora extract
2%th, mint extract 2%, Radix Sangusorbae extract 2%, Chinese rhubarb extract 0.5%, Acritamer 940 1.5%, glycerine 5.5%, triethanolamine
0.1%th, ethyl hydroxy benzoate 0.1%, polyoxyethylene sorbitan monoleate 0.2%, distilled water complement to 100%;
Preparation method:Carbomer and polysorbate are dissolved in 30ml distilled water, triethanolamine solution is added, after stirring evenly
Add purslane extract, herba hedyotis diffusae extract, shrubby sophora extract, mint extract, Radix Sangusorbae extract, rheum officinale extraction
Thing, then ethyl hydroxy benzoate is gradually added into and stirred evenly, produce antiallergy gel.Each extract comes from embodiment 1 in the present embodiment.
The preparation of 6 toner of the present invention of embodiment
Raw material is weighed as following weight percent:Purslane extract 3%, herba hedyotis diffusae extract 5%, shrubby sophora extract
3%th, mint extract 3%, Radix Sangusorbae extract 1%, Chinese rhubarb extract 1%, glycerine 10%, butanediol 1.5%, polysorbate60 3%, tartaric acid 1%,
Citric acid 1%, hyaluronic acid 2%, carboxyethyl cellulose 2.5%, vitamin e1 %, deionized water complement to 100%;
Preparation method:Purslane extract, herba hedyotis diffusae extract, shrubby sophora extract, mint extract, garden burnet extraction
After thing, Chinese rhubarb extract mixing, glycerine, propane diols, tween, tartaric acid, bone collagen, co-ferment Q10, polyethylene glycol are added
400, vitamin E, deionized water complement to that 100ml is well mixed to produce antiallergy toner.Each extract comes in the present embodiment
From embodiment 1.
The preparation of 7 facial mask of the present invention of embodiment
Raw material is weighed as following weight percent:Purslane extract 5%, herba hedyotis diffusae extract 2%, shrubby sophora extract
1%th, mint extract 2%, Radix Sangusorbae extract 3%, Chinese rhubarb extract 0.5%, glycerine 15%, polyethylene glycol-800 16%, trehalose 1%,
Allantoin 0.1%, EDETATE SODIUM 0.1%, co-ferment Q101%, vitamin e1 %, deionized water complement to 100%;
Preparation method:A small amount of deionized water is taken, polyethylene glycol-800, glycerine, trehalose heating stirring is added, is cooled to
Room temperature, allantoin, EDETATE SODIUM, hyaluronic acid, vitamin E are added, add purslane extract, oldenlandia diffusa extraction
Thing, shrubby sophora extract, mint extract, Radix Sangusorbae extract, Chinese rhubarb extract, are sufficiently stirred, and solid matter is divided in colloid
Dissipate uniformly, produce antiallergic mask.Each extract comes from embodiment 1 in the present embodiment.
Beneficial effects of the present invention are illustrated below by way of test example.
The present composition antiallergy of test example 1 is tested
(One)Hyaluronidase body outer suppressioning test
Hyaluronidase (HAase) is hyaluronic acid (HA) Specific lytic enzymes, and HA is in human development and regulation process
In occur and vascularization plays main inhibitory action such as cell adherence, orga- nogenesis, wound healing, tumour, suppress HAase's
Activity can make HA not be decomposed, and maintain normal physiological function.Hyaluronidase is external model experiment.Kakegawa etc. is reported
The various medicines for influenceing histamine release of mast cell can adjust the activity of hyaluronidase, and hyaluronidase activity suppresses and hypertrophy
Correlation (Kakegawa H, the Inhibitory effects of some having had between cells release histamine inhibitory activity
natural product on the activation of hyaluridse and their antiallergic
actions[J].Hen Pharm Bull,1991,40(6):1439~1422).Yoo etc. reports hyaluronidase participation group
Inflammatory process is knitted, is the participant of type i allergic reaction, reaction is participated in the anaphylactoid phase III causes de- of mast cell
Grain(Yoo,Effects of allergy-related drugs on hyaluridase action and histamine
by rat peritoneal mast cell[J].Tachan Sacngri Hakboechi.1988,22:59~72).Therefore
Hyaluronidase body outer suppressioning test can evaluate the antianaphylaxis energy of sample as simple biochemical method.Due to hyalomitome
Sour enzyme external model is simple and easy, so this Bioexperiment method is widely adopted as an index of research anti-allergic effects
With.
Antiallergic activity detects:Elson-Morgan improved methods:
Hyaluronidase is the participant of type i allergic reaction, and research shows that hyaluronidase and inflammation, allergy have strong correlation
Property, the medicine that Kakegawa once reported various histamine release of mast cell can adjust the activity of hyaluronidase.
Preparation of reagents
(1) hyaluronidase:Solvent compound concentration 500u/mL hyaluronidases are done with hac buffer, be now with existing
With, it is impossible to overnight.
(2) potassium hyaluronate:Solvent compound concentration 0.5mg/mL potassium hyaluronates are done with hac buffer
(3)Buffer:Solution A (in the molten 1000mL distilled water of 0.2mol/L. acetic acid, i.e. 11.55mL glacial acetic acid) 4.8mL,
Solution B (0.2mol/L sodium acetate, i.e. 16.4 grams of CH3COONa or 27.2 gram of CH3COONa.3H2O is dissolved in 1000ml distilled water
In) 45.2mL, mixing, 100mL is diluted to, is made into the acetate buffer solution of pH=5.6.
(4) acetic acid acetone soln:50mL1.0mol/L sodium carbonate liquors and 3.5mL acetylacetone,2,4-pentanedione solution are well mixed.(face
With now matching somebody with somebody)
(5) preparation of P-DAB developers:0.8g paradime thylaminobenzaldehydes and 15mLHCl and absolute ethyl alcohol mixing are equal
Even use.
(6)CaCl2Solution:2.5moL/L.
(7) NaOH solution:5moL/L.
(8)Each determinand is configured to the solution for standby of 1.2mg/ml concentration, is grouped as follows:Each taste prepared by embodiment 1
Chinese medical extract, mixed according to the Chinese medical extract proportions of embodiment 3, be identified as 1 group of experiment;Embodiment 2 is prepared each
Taste Chinese medical extract, mixed according to the Chinese medical extract proportions of embodiment 3, be identified as 2 groups of experiment;Prepared by embodiment 1
Each taste Chinese medical extract, mixed respectively by each Chinese medical extract proportions in embodiment 4-7, be individually identified as testing 3-6 groups;
The medicinal extract preparation method of each single medicinal material extract is same as Example 1.
Experimental procedure:
By sample 0.5ml(A, B is managed), distilled water 0.5ml(C, D is managed)Middle addition 0.5ml hyaluronidases(500U/ml)
(A, C is managed)With 0.5ml acetate buffer solutions pH=5.6(B, D is managed)20min is incubated in 37 DEG C;Add CaCl2Solution 0.1ml(A、B、
C, D is managed)20min is incubated in 37 DEG C;It is separately added into 0.5ml potassium hyaluronate liquid(A, C is managed), 0.5ml acetate buffer solutions pH=5.6
(B, D is managed)Room temperature places 10min after being incubated 40min in 37 DEG C;It is separately added into 0.5ml distilled water(A, B, C, D are managed),
0.1ml5mol/L NaOH solutions(A, B, C, D are managed)With 0.5ml acetylacetone,2,4-pentanedione solution(A, B, C, D are managed)Ice after boiling water bath 15min
Water-bath 10min, room temperature 10min is placed, add 1ml P-DAB developers(A, B, C, D are managed)Add anhydrous second after each pipe fully shaking
Alcohol places room temperature 30min, absorbance is surveyed at 530nm to 8ml.
The calculating of antiallergic activity
Hyaluronic acid enzyme inhibition rate(%)=[(C-D)-(A-B)]/(C-D)×100%
In formula:A—(Hyaluronidase+sample+hyaluronidase potassium) sample solution OD values
The OD values of B-(acetate buffer solution+sample+acetate buffer solution) sample blank
The OD values of C-(hyaluronidase+deionized water+hyaluronidase potassium) contrast solution
D-(acetate buffer solution+deionized water+acetate buffer solution) compares the OD values of blank solution
As a result referring to table 1:
Influence of the table 1 to hyaluronidase
Hyaluronidase is the participant of type i allergic reaction, and research shows that hyaluronidase and inflammation, allergy have strong correlation
Property.From experimental result, the inhibiting rate of the present composition is higher than the inhibiting rate of single prescription element, shows that the present invention will be each
After taste medicinal material compound use, synergistic function has been played.As can be seen here, the present composition has significantly to hyaluronidase
Inhibitory action, it can be reached by the suppression to hyaluronidase and suppress anaphylactoid effect.
(Two)Influence to cavy local skin itch
Cavy 40, male and female half and half, 160~190g of body weight, random point four groups.1 group is blank control group;2 groups are the positive
Control group is cloudy with clean that;3 groups are test group 3(The face cream of embodiment 3);4 groups are test group 4(The emulsion group of embodiment 4).Before experiment
3, to instep shaving behind each group cavy right side, it is each that cloudy distilled water, clean that, the face cream of embodiment 3 and the emulsion of embodiment 4 were given respectively
0.5ml/ is only.The same day is tested, at instep shaving behind the coarse sandpaper scratch right side, 1 square centimeter of area is local to apply again 1 time, and last applies
10min after medicine, start in the histamine phosphate liquid 0.05ml/ of surface of a wound drop 0.01% only, hereafter every 3min according to 0.02%, 0.03%,
0.04% concentration incremented by successively, it is 0.05ml/ every time, until cavy occur later licks right metapedes, is returned with finally there is cavy
To lick the histamine phosphate total amount given during right metapedes be itch-threshold to head, and the cause for recording and comparing each group is itched domain.It the results are shown in Table 2.
Table 2 to histamine phosphate cause itch domain reaction influence
Group |
N |
Itch thresholding(μg) |
Blank control group |
10 |
63.13±28.14 |
Clean cloudy group of that |
10 |
185.60±64.02** |
Test group 3 |
10 |
178.07±84.20** |
Test group 4 |
10 |
165.38±53.56** |
Note:Compared with physiological saline group, * P < 0.05, * * P < 0.01
Anaphylactoid to normally behave as pruitus, from experimental result, the present composition has significant stop
Itch effect, it is inhibited to itch caused by allergic reaction.
(Three)Influence to auricle edema caused by mouse dimethylbenzene
Healthy male mice 40,20~22g of body weight is taken, is randomly divided into four groups, every group 10.Blank control group distillation
Water 0.5ml/ only, is applied 1 time for 1 day.Positive controls apply fluocinonide ointment and applied 1 time for 1 day, and above each group applies 0.5g/ only every time;
Test group 3 is that the face cream group of embodiment 3 applies face cream 1 day 1 time, and 0.5g/ is only;Test group 4 is that the emulsion group of embodiment 4 applies emulsion group
1 day 1 time, 0.5g/ is only.Administrated method:Tested material or distilled water are coated in mouse right ear exterior feature, even applied 3 days.1 is small after last coating
When, by the Evans blue physiological saline 0.1ml/10g of mouse tail vein injection 0.5%, then auricle melted paraxylene 0.03ml makes to the right
Do not have and auricle inside and outside.Mouse is taken off into cervical vertebra after 40min to put to death.Left and right auricle diameter 8mm card punch is cut respectively two
Ear lays round auricle with position.Weigh weight in the balance, the difference of left and right auricle weight is swelling, seeks swelling inhibiting rate.Then by ear
Piece shreds, and is put into 7:Soaked 48 hours in 3 acetone physiological saline, 15min is centrifuged with 300rpm, takes supernatant in 600nm wavelength
Colorimetric.OD value is recorded, the results are shown in Table 3.
Influence of the table 3 to auricle edema caused by mouse dimethylbenzene
Group |
n |
Swelling inhibiting rate |
OD value |
Blank control group |
10 |
-- |
0.068±0.021 |
Positive controls |
10 |
60.4 |
0.023±0.013** |
Test group 3 |
10 |
49.6 |
0.031±0.015* |
Test group 4 |
10 |
56.3 |
0.032±0.015* |
Note:Compared with physiological saline group, * P < 0.05, * * P < 0.01
Test result indicates that:Positive group, test group and blank control group relatively have significant difference, illustrate that tested material has suppression
The effect of auricle edema caused by dimethylbenzene processed, show that the present composition has antiinflammatory action, pass through the inhibitory action to inflammation
Reach antianaphylactic effect.
(Four)Influence to capillary permeability caused by rat intracutaneous injection histamine phosphate
Rat 40,180~220g of body weight, male and female half and half, random point four groups.Remove belly wool, area 4 with electric hair cutter
× 5cm, to apply tested material area at unhairing.Blank control group only, is applied 1 time for 1 day with distilled water 0.5ml/.Positive controls apply acetic acid
Fluocinolone acetonide ointment applies 1 time for 1 day, and above each group applies 0.5g/ only every time;The face cream group of embodiment 3 applies face cream 1 day 1 time, 0.5g/
Only(Test group 3);The emulsion group of embodiment 4 applies emulsion group 1 day 1 time, and 0.5g/ is only(Test group 4).It is continuous to apply 7 days, after last coating
30 minutes, by 0.1% Evans blue physiological saline 0.5ml/100g intravenous, animal is put to death after 30min, bloodletting, peels off skin chi
Son measurement stained area, then shreds and is put into 7:3 acetone physiological saline soak 48 hours, centrifuge 15min with 300rpm, take supernatant
Liquid is in 600nm wavelength colorimetrics.Record OD value.It the results are shown in Table 4.
Influence of the table 4 to capillary permeability caused by rat intracutaneous injection histamine
Group |
n |
Stained area |
OD value |
Blank control group |
10 |
68.13±12.37 |
0.239±0.074 |
Positive group |
10 |
30.13±9.58** |
0.113±0.052** |
Test group 3 |
10 |
36.76±11.84* |
0.130±0.039* |
Test group 4 |
10 |
38.59±10.16* |
0.124±0.046* |
Note:Compared with physiological saline group, * P < 0.05, * * P < 0.01
The capillary permeability caused by rat intracutaneous injection histamine phosphate is increased by composition it can be seen from result of the test
Added with inhibitory action, illustrate that the present composition has antiinflammatory action, by reaching antianaphylactic effect to the inhibitory action of inflammation.