CN107811881A - A kind of α ursin nano-compositions of whitening antioxidation and preparation method and application - Google Patents
A kind of α ursin nano-compositions of whitening antioxidation and preparation method and application Download PDFInfo
- Publication number
- CN107811881A CN107811881A CN201711058551.3A CN201711058551A CN107811881A CN 107811881 A CN107811881 A CN 107811881A CN 201711058551 A CN201711058551 A CN 201711058551A CN 107811881 A CN107811881 A CN 107811881A
- Authority
- CN
- China
- Prior art keywords
- arbutin
- alpha
- nano
- composition
- skin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- 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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/60—Sugars; Derivatives thereof
- A61K8/602—Glycosides, e.g. rutin
-
- 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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
-
- 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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
- A61K8/345—Alcohols containing more than one hydroxy group
-
- 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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/36—Carboxylic acids; Salts or anhydrides thereof
- A61K8/361—Carboxylic acids having more than seven carbon atoms in an unbroken chain; Salts or anhydrides thereof
-
- 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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/37—Esters of carboxylic acids
-
- 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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/37—Esters of carboxylic acids
- A61K8/375—Esters of carboxylic acids the alcohol moiety containing more than one hydroxy group
-
- 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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4993—Derivatives containing from 2 to 10 oxyalkylene groups
-
- 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
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/84—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
- A61K8/86—Polyethers
-
- 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
- A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
- A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
-
- 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
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/08—Anti-ageing preparations
-
- 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
- A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
- A61K2800/21—Emulsions characterized by droplet sizes below 1 micron
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Birds (AREA)
- Emergency Medicine (AREA)
- Dermatology (AREA)
- Chemical & Material Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Gerontology & Geriatric Medicine (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention provides α ursin nano-compositions that a kind of stability is good, drugloading rate is big, skin anelasticity has a wide range of application well and its preparation method and application, wherein α ursin nano-composition, include the component of following weight percentage:α ursin 0.1%~20.0%, emulsifying agent 5.0%~50.0%, assistant for emulsifying agent 5.0%~30.0%, liquid fatty 3.0%~15.0%, polyalcohol 5.0%~25.0%, the water of surplus.Present invention also offers the preparation method and purposes of α ursin nano-compositions.α ursin nano-composition drugloading rate provided by the invention is big, and stability is good, and skin anelasticity can be widely used in cosmetics well.The preparation method of α ursin nano-compositions is simple, and technique is easily controllable, suitable industrialization, large-scale production, and organic solvent is not used in whole process, small to skin irritatin, safe.
Description
Technical field
The present invention relates to a kind of alpha-arbutin nano-composition in the application of cosmetic technical field, more particularly to a kind of U.S.
In vain, oxidation resistant alpha-arbutin nano-composition and its preparation method and application.
Background technology
Alpha-arbutin is white, needle-shaped crystals or powder, is typically entered by different microbe transformation method and Enzyme optrode
Prepared by row, the principle of wherein enzymatic synthesis is that a molecule glucose and a molecule quinhydrones combine to form single alpha-arbutin.According to grinding
Study carefully and show that alpha-arbutin whitening effect is higher by 14 times than β-ursin, skin can be rapidly permeated into, increase not influenceing Skin Cell
While growing concentration, effectively suppress the activity of tyrosinase in skin, block the formation of melanin, pass through itself and tyrosine
The combination of enzyme, accelerate the decomposition and excretion of melanin, so as to reduce Skin pigmentation, dispelling stain and freckle.Alpha-arbutin
It is most safely and effectively one of whitening raw material of current Foreign Epidemic, and the skin-whitening of 21st century most competitiveness is dispelled
Spot activating agent, it is external to push alpha-arbutin to Cosmetic Market as a kind of safe and efficient skin lightening activating agent.
Alpha-arbutin is water-soluble good, has wide clinical medicinal and health care of food application prospect.But alpha-arbutin
Itself there is also it is certain the defects of, on the one hand, alpha-arbutin is to light and heat-sensitive, and easily degraded produces under Qiang Guang, intense heat conditions
Quinhydrones, and quinhydrones is toxic to human body;On the other hand, the alpha-arbutin product bioavilability listed at present is low, Qiang Guang, high temperature
Under the conditions of easily degraded discoloration.In addition, the skin anelasticity of alpha-arbutin product is poor at present, active ingredient is difficult in skin surface
Keep time enough.
The content of the invention
In consideration of it, present invention aims at providing, a kind of stability is good, drugloading rate is big, skin anelasticity has a wide range of application well
Alpha-arbutin nano-composition and its preparation method and application.
In order to realize foregoing invention purpose, the present invention provides following technical scheme:
The invention provides a kind of alpha-arbutin nano-composition, include the component of following weight percentage:α-black bearberry
Glycosides 0.1%~20.0%, emulsifying agent 5.0%~50.0%, assistant for emulsifying agent 5.0%~30.0%, liquid fatty 3.0%~
15.0%, polyalcohol 5.0%~25.0%, the water of surplus.
Preferably, the emulsifying agent is Tween 80, polysorbate60, polysorbate40, polysorbas20, Emulsifier EL-60-20, polyoxy
Ethylene castor oil-30, Emulsifier EL-60-35, Emulsifier EL-60-40, Cremophor RH40, PEG-30 hydrogenations
Castor oil, PEG-20 rilanit specials, PEG-10 rilanit specials, PEG-5 rilanit specials, polyethylene glycol 400 monoglyceride,
Polyethylene glycol 400 double glyceride, Macrogol 600 monoglyceride, Macrogol 600 double glyceride, cocoyl glucoside (cocounut oil
The more glycosides of base glucose), ceteareth -20, ceteareth -25, butylol polyether -26 and one kind in lecithin or
Several mixtures.
Preferably, the assistant for emulsifying agent be TC, polyethylene glycol, 1,3-BDO, 1,2-PD,
One or more of mixtures in DPG, 1,2- hexylene glycols, 1,2- pentanediols, oleic acid, octyl dodecanol.
Preferably, the liquid fatty be isopropyl myristate, it is isopropyl palmitate, Miglyol 812N, pungent
Sour capric acid LABRAFIL M 1944CS, polyethylene glycol glyceryl laurate ester, polyethylene glycol tristerin, glyceryl linoleate,
Sefsol 218, two pungent capric acid propylene glycol esters, diethyl sebacate, pungent capric acid cocoa butter, isononyl isononanoate, triacetic acid
One or more of mixtures in glyceride, dimethicone, vitamin E and squalene.
Preferably, the polyalcohol is polyethylene glycol, propane diols, DPG, glycerine, 1,2- hexylene glycols, 1,3- fourths two
One or more of mixtures in alcohol and 1,2- pentanediols.
Preferably, in alpha-arbutin nano-composition of the present invention, the particle diameter of the alpha-arbutin nano-composition
For 15~300nm.
The invention provides a kind of preparation method of alpha-arbutin nano-composition described in above-mentioned technical proposal, including it is as follows
Step:
(1) emulsifying agent, assistant for emulsifying agent, liquid fatty are dissolved, obtains oil phase;
(2) alpha-arbutin, water, polyalcohol are mixed into dissolving, obtains aqueous phase;
(3) aqueous phase for obtaining the step (2) and oil phase obtained by the step (1), mix, obtain α-bear while stirring
Fruit glycosides nano-composition;
(4) got product after the alpha-arbutin nanoemulsions that the step (3) obtains being stood into cooling;
The order of the step (1) and step (2) can exchange.
Preferably, in the preparation method of alpha-arbutin nano-composition of the invention, stirring and dissolving in the step (1)
Temperature is 40~80 DEG C, and the time is 10~30min;The temperature of step (2) the reclaimed water stirring and dissolving is 40~80 DEG C, and the time is
10~30min;The rotating speed that profit mixes in the step (3) is 10~60rpm, and the time is 15~40min;In step (4)
Time of repose is 1~3min.Gained finished product grain size is 15-150nm.
The invention provides preparation described in alpha-arbutin nano-composition described in above-mentioned technical proposal or above-mentioned technical proposal
The alpha-arbutin nano-composition that method obtains cosmetics whitening, it is anti-oxidant in application.
It is another aspect of the invention to provide the alpha-arbutin nano-composition that above-mentioned preparation method obtains.
Another aspect of the present invention is in the answering in effect cosmetic is prepared in the above-mentioned alpha-arbutin nano-composition of offer
With.
Compared with prior art, the present invention has advantages below to the present invention:
1) thermodynamics can be formed after emulsifying agent used in the present invention, assistant for emulsifying agent, liquid fatty, polyalcohol, water mixing
Stable homogeneous dispersion system, in gel, has good stability, good biocompatibility.
2) alpha-arbutin nano-composition drugloading rate provided by the invention is big, and the concentration of active component alpha-arbutin is reachable
15.0%, alpha-arbutin nano-composition sustained release alpha-arbutin, can maintain for a long time as transdermal bank
Valid density, preferably play skin-care effect.Test result indicates that alpha-arbutin nano-composition provided by the invention places 30
After it, conspicuousness change does not occur for character and particle diameter, and stability is good;12h accumulations skin hold-up amount can reach the 5 of bulk drug
More than times, there is excellent skin permeability.Alpha-arbutin nano-composition stability provided by the invention is good, drugloading rate is big,
Skin anelasticity can be widely used in cosmetics well.
3) preparation method of alpha-arbutin nano-composition provided by the invention is simple, and technique is easily controllable, suitable industry
Change, large-scale production, and organic solvent is not used in whole process, it is small to skin irritatin, it is safe.
Brief description of the drawings
Fig. 1 is the alpha-arbutin nano-composition vitro skin accumulation H103 resin figure that embodiment 3-6 is obtained;
Fig. 2 is the alpha-arbutin nano-composition vitro skin accumulation retention curve figure that embodiment 3-6 is obtained;
Fig. 3 is that the alpha-arbutin nano-composition that embodiment 3 obtains removes DPPH power curve figures in vitro.
Embodiment
Provide a kind of alpha-arbutin nano-composition in an embodiment of the present invention, including following weight percentage
Component:Alpha-arbutin 0.1%~20.0%, emulsifying agent 5.0%~50.0%, assistant for emulsifying agent 5.0%~30.0%, liquid fatty
3.0%~15.0%, polyalcohol 5.0%~25.0%, the water of surplus..
The alpha-arbutin nano-composition provided in embodiments of the present invention include weight/mass percentage composition be 0.1%~
20.0% alpha-arbutin, preferably 0.5%~18%, more preferably 1.0%~15.0%.Alpha-arbutin one in the present invention
As prepared by different microbe transformation method and Enzyme optrode, the principle of wherein enzymatic synthesis be a molecule glucose and
One molecule quinhydrones combines to form single alpha-arbutin.Show that alpha-arbutin whitening effect is higher by 14 than β-ursin according to the study
Times, skin can be rapidly permeated into, while skin cell proliferation concentration is not influenceed, effectively suppresses tyrosinase in skin
Activity, the formation of melanin is blocked, by the combination of itself and tyrosinase, accelerate the decomposition and excretion of melanin, so as to subtract
Few Skin pigmentation, dispelling stain and freckle.Alpha-arbutin be current Foreign Epidemic most safely and effectively whitening raw material it
One, and the skin-whitening and speckle eliminating activating agent of 21st century most competitiveness, it is external to pacify alpha-arbutin as one kind
Complete efficient skin lightening activating agent pushes Cosmetic Market to.
The alpha-arbutin nano-composition provided in embodiments of the present invention include weight/mass percentage composition be 5.0%~
50.0% emulsifying agent, preferably 5.0%~48%, more preferably 8.0%~45.0%.In the present invention, the emulsifying agent
Preferably Tween 80, polysorbate60, polysorbate40, polysorbas20, Emulsifier EL-60-20, Emulsifier EL-60-30, polyoxy second
Alkene castor oil-35, Emulsifier EL-60-40, Cremophor RH40, PEG-30 rilanit specials, PEG-20 hydrogenation castors
Sesame oil, PEG-10 rilanit specials, PEG-5 rilanit specials, polyethylene glycol 400 monoglyceride, polyethylene glycol 400 diglycerol
Ester, Macrogol 600 monoglyceride, Macrogol 600 double glyceride, cocoyl glucoside, ceteareth -20, whale
One or more of mixtures in wax stereth -25, butylol polyether -26 and lecithin.Described mixture is preferably 1
The mixture of~4 kinds of emulsifying agents, more preferably Tween 80, polysorbate60, polysorbate40, Emulsifier EL-60-20, polyoxyethylene castor
Sesame oil-30, Emulsifier EL-60-35, Emulsifier EL-60-40, Cremophor RH40, PEG-30 hydrogenated castors
Oil, PEG-20 rilanit specials, polyethylene glycol 400 monoglyceride, polyethylene glycol 400 double glyceride, ceteareth-
20th, ceteareth -25, butylol polyether -26, lecithin mixture.In the present invention, to various emulsifying agents in mixture
Mass ratio do not limit.
The alpha-arbutin nano-composition provided in embodiments of the present invention include weight/mass percentage composition be 5.0%~
30.0% assistant for emulsifying agent, preferably 5.0%~25.0%, more preferably 5.0%~20.0%.In the present invention, it is described to help
Emulsifying agent be preferably TC, polyethylene glycol, 1,3 butylene glycol, 1,2- propane diols, DPG, 1,2- oneself two
Alcohol, 1,2- pentanediols, one or more of mixtures of oleic acid;Described mixture is preferably the mixing of 1~4 kind of assistant for emulsifying agent
Thing, more preferably TC, 1,3-BDO, 1,2-PD, 1,2- hexylene glycols, 1,2- pentanediols, oleic acid
The mixture of 1,3 butylene glycol, 1,2- hexylene glycols.In the present invention, the mass ratio of various assistant for emulsifying agents in mixture is not limited
System.
The alpha-arbutin nano-composition provided in embodiments of the present invention include weight/mass percentage composition be 1.0%~
15.0% liquid fatty;Preferably 3.0%~12.0%%, more preferably 3.0%~10.0%.In the present invention, it is described
Liquid fatty is isopropyl myristate, isopropyl palmitate, Miglyol 812N, caprylic capric polyethylene glycol glycerol
It is ester, polyethylene glycol glyceryl laurate ester, polyethylene glycol tristerin, glyceryl linoleate, Sefsol 218, two pungent
Capric acid propylene glycol ester, diethyl sebacate, pungent capric acid cocoa butter, isononyl isononanoate, glyceryl triacetate, dimethicone,
One or more of mixtures in vitamin E, squalene;Described mixture is preferably the mixing of 1~4 kind of liquid fatty
Thing, more preferably isopropyl myristate, isopropyl palmitate, Miglyol 812N, caprylic capric polyethylene glycol glycerol
It is ester, polyethylene glycol glyceryl laurate ester, polyethylene glycol tristerin, glyceryl linoleate, Sefsol 218, two pungent
Capric acid propylene glycol ester, diethyl sebacate, glyceryl triacetate, dimethicone, vitamin E, squalene.In the present invention,
The mass ratio of various liquid fatties in mixture is not limited.
The alpha-arbutin nano-composition provided in embodiments of the present invention include weight/mass percentage composition be 5.0%~
25.0% polyalcohol, preferably 5.0%~23.0%, more preferably 5%~20%.In the present invention, the polyalcohol is excellent
Elect as polyethylene glycol, propane diols, DPG, glycerine, 1,3 butylene glycol, 1,2- hexylene glycols, one kind in 1,2- pentanediols or
Several mixtures;Described mixture is preferably the mixture of 1~4 kind of polyalcohol, more preferably polyethylene glycol,
Propane diols, glycerine, 1,3 butylene glycol, 1,2- hexylene glycols, 1,2- pentanediols.In the present invention, to various stabilizers in mixture
Mass ratio do not limit, the polyalcohol can strengthen the dissolubility of alpha-arbutin nano-composition, further improve α-bear
Fruit glycosides nano-composition stability.
The alpha-arbutin nano-composition provided in embodiments of the present invention includes the water of surplus, and described water is preferably pure
Change water.
The particle diameter of the alpha-arbutin nano-composition provided in embodiments of the present invention is preferably 15~300nm, more preferably
For 15~100nm.
The preparation method of the alpha-arbutin nano-composition described in such scheme is provided in embodiments of the present invention, including
Following steps:
(1) emulsifying agent, assistant for emulsifying agent, liquid fatty are dissolved, obtains oil phase;
(2) alpha-arbutin, water, polyalcohol are mixed into dissolving, obtains aqueous phase;
(3) aqueous phase for obtaining the step (2) and oil phase obtained by the step (1), mix, obtain α-bear while stirring
Fruit glycosides nano-composition;
(4) got product after the alpha-arbutin nanoemulsions that the step (3) obtains being stood into cooling;
The order of the step (1) and step (2) can exchange.
It is furthermore preferred that the temperature of stirring and dissolving is 40~66 DEG C in the step (1), the time is 15~25min;
It is furthermore preferred that the temperature of step (2) the reclaimed water stirring and dissolving is 40~66 DEG C, the time is 10~25min;
It is furthermore preferred that the rotating speed that profit mixes in the step (3) is 15~45rpm, the time is 20~35min;
Time of repose is 1~2min in preferred step (4).Gained finished product grain size is 15-100nm.
In embodiments of the present invention, emulsifying agent, assistant for emulsifying agent, liquid fatty are dissolved, obtains oil phase.Implement in the present invention
In example, the temperature of the dissolving is preferably 40~80 DEG C, more preferably 40~66 DEG C;The time of the dissolving is preferably 10~
30min, more preferably 15~25min.In embodiments of the present invention, preferably carried out using the mode of jacketed pan heating water bath molten
Solution.It is the emulsifying agent, assistant for emulsifying agent, liquid fatty, consistent described in the dosage of polyalcohol and species and above-mentioned technical proposal, herein
Repeat no more.
Aqueous phase is obtained after alpha-arbutin, water, polyalcohol are mixed into dissolving in embodiments of the present invention.Of the invention real
Apply in example, the temperature that the alpha-arbutin, water mix dissolving is preferably 40~80 DEG C, more preferably 40~66 DEG C;It is described
The time of stirring and dissolving is preferably 10~30min, more preferably 10~25min.In embodiments of the present invention, the α-black bearberry
It is glycosides, water, consistent described in the dosage of polyalcohol and species and above-mentioned technical proposal, it will not be repeated here.
Oil mixing with water stirs to obtain alpha-arbutin nanoemulsions in embodiments of the present invention, is got product after filtering.In this hair
In bright embodiment, the mixing speed during the profit mixes is preferably 10~60rpm, more preferably 15~45rpm.
In the embodiment of the present invention, the time during the profit mixes is preferably 15~40min, more preferably 20~35min.
In the embodiment of the present invention, particle diameter is preferably 15~300nm after the profit mixes filtering, more preferably 15~200nm.
In embodiments of the present invention, the oil phase, the preparation process of aqueous phase dissolved do not have the limitation of time sequencing.
In embodiments of the present invention, aqueous phase adds oil phase mixing or oil phase adds aqueous phase mixing, does not have sequential limit
System.
In embodiments of the present invention, there is provided a kind of alpha-arbutin nano-composition cosmetics whitening, it is anti-oxidant in
Using.
In embodiments of the present invention, there is provided alpha-arbutin nano-composition be added in cosmetics can allow to it is rapid
Skin is penetrated into, while skin cell proliferation concentration is not influenceed, effectively suppresses the activity of tyrosinase in skin, blocks black
The formation of pigment, by the combination of itself and tyrosinase, accelerate the decomposition and excretion of melanin, sunk so as to reduce skin pigment
Product, dispelling stain and freckle, damage caused by exogenous poisonous substance has significant protective effect, and can improve cosmetics
Skin anelasticity, can be widely used in cosmetics, especially in whitening class cosmetics.
In embodiments of the present invention, there is provided alpha-arbutin nano-composition also have and participate in the activity such as anti-oxidant, anti-inflammatory
Effect.
Alpha-arbutin nano-composition provided by the invention is described in detail with reference to embodiment, but can not
They are interpreted as limiting the scope of the present invention.
Embodiment 1
3.0% Tween 80,2.0% Emulsifier EL-60-20,10.0%1,3- butanediols, 1.0% myristic acid is different
Propyl ester, dissolved under 40 DEG C of water bath conditions, obtain oil phase, it is standby;
By 0.1% alpha-arbutin, 10% propane diols, 63.9% water, stirred under 40 DEG C of water bath conditions with 15rpm rotating speed
10min, aqueous phase is obtained, it is standby;
Aqueous phase is added in oil phase, is stirred under 40 DEG C of water bath conditions and 10min is stirred with 15rpm rotating speed, stand 1min,
Produce alpha-arbutin nano-composition finished product.
The particle diameter of alpha-arbutin nano-composition is detected, can obtain the alpha-arbutin nano-composition particle diameter is
33.8nm。
Embodiment 2
By 4.0% polysorbate40,2.0% Emulsifier EL-60-30,3% polyethylene glycol 400 monoglyceride, 5.0% dipropyl
Glycol, 7.0%1,2- hexylene glycols, 1.0% isopropyl palmitate, 2.0% Labraso, in 45 DEG C of water-baths
Under the conditions of dissolve, obtain oil phase, it is standby;
By 1.0% alpha-arbutin, 10% propane diols, 65% water, stirred under 45 DEG C of water bath conditions with 30rpm rotating speed
15min, aqueous phase is obtained, it is standby;
Oil phase is added in aqueous phase, is stirred under 45 DEG C of water bath conditions and 10min is stirred with 30rpm rotating speed, stand 2min,
Produce alpha-arbutin nano-composition finished product.
The particle diameter of alpha-arbutin nano-composition is detected, can obtain the alpha-arbutin nano-composition particle diameter is
28.5nm。
Embodiment 3
By 8.0% Emulsifier EL-60-35,3.0%PEG-30 rilanit specials, 1.0% ceteareth-
25th, 2.0% butylol polyether -26,5.0%1,2- pentanediols, 3.0% oleic acid, 10.0% TC, 1.0% gather
Ethylene glycol glyceryl laurate ester, 3.0% glyceryl linoleate, 1.0% Sefsol 218,1.0% diethyl sebacate,
Dissolved under 50 DEG C of water bath conditions, obtain oil phase, it is standby;
By 5.0% alpha-arbutin, 15.0% polyethylene glycol, 10.0%1,3- butanediols, 32% water, in 50 DEG C of water bath conditions
Under 20min stirred with 45rpm rotating speed, obtain aqueous phase, it is standby;
Aqueous phase is added in oil phase, is stirred under 50 DEG C of water bath conditions and 20min is stirred with 45rpm rotating speed, stand 1min,
Produce alpha-arbutin nano-composition finished product.
The particle diameter of alpha-arbutin nano-composition is detected, can obtain the alpha-arbutin nano-composition particle diameter is
62.3nm。
Embodiment 4
By 2.0% polysorbas20,5.0% Emulsifier EL-60-40,2.0% polyethylene glycol 400 double glyceride, 3.0% whale
Wax stereth -20,8.0%1,3- butanediols, 6.0%1,2- hexylene glycols, 2.0% polyethylene glycol tristerin,
1.0% glyceryl triacetate, 1.0% dimethicone, dissolve under 45 DEG C of water bath conditions, obtain oil phase, standby;
By 5.0% alpha-arbutin, 10.0% propane diols, 5.0%1,2- hexylene glycols, 50% water, under 45 DEG C of water bath conditions
15min is stirred with 35rpm rotating speed, obtains aqueous phase, it is standby;
Aqueous phase is added in oil phase, is stirred under 45 DEG C of water bath conditions and 15min is stirred with 35rpm rotating speed, stand 1min,
Produce alpha-arbutin nano-composition finished product.
The particle diameter of alpha-arbutin nano-composition is detected, can obtain the alpha-arbutin nano-composition particle diameter is
46.7nm。
Embodiment 5
By 10.0%PEG-40 rilanit specials, 2.0% butylol polyether -26,15.0% TC,
1.0% Miglyol 812N, dissolved under 45 DEG C of water bath conditions, obtain oil phase, it is standby;
By 5.0% alpha-arbutin, 20.0% octyl dodecanol, 47.0% water, turned under 45 DEG C of water bath conditions with 20rpm
Speed stirring 15min, obtains aqueous phase, standby;
Aqueous phase is added in oil phase, is stirred under 45 DEG C of water bath conditions and 15min is stirred with 20rpm rotating speed, stand 2min,
Produce alpha-arbutin nano-composition finished product.
The particle diameter of alpha-arbutin nano-composition is detected, can obtain the alpha-arbutin nano-composition particle diameter is
24.5nm。
Embodiment 6
By 7.0% Emulsifier EL-60-40,4.0%PEG-20 rilanit specials, 3.0% butylol polyether-26,8.0%
Propane diols, 4.0% TC, 3.0% 2 pungent capric acid propylene glycol ester, 1.0% vitamin E, 1.0% squalene,
Dissolved under 45 DEG C of water bath conditions, obtain oil phase, it is standby;
By 5.0% alpha-arbutin, 5.0% glycerine, 10.0%1,3- butanediols, 49% water, under 45 DEG C of water bath conditions with
20rpm rotating speed stirring 20min, obtains aqueous phase, standby;
Oil phase is added in aqueous phase, is stirred under 45 DEG C of water bath conditions and 20min is stirred with 20rpm rotating speed, stand 1min,
Produce alpha-arbutin nano-composition finished product.
The particle diameter of alpha-arbutin nano-composition is detected, can obtain the alpha-arbutin nano-composition particle diameter is
42.7nm。
Embodiment 7
By 14.0% Emulsifier EL-60-35,10.0% polyethylene glycol 400 monoglyceride, 12.0% DPG,
5.0% oleic acid, 2.0% isopropyl myristate, 1.0% vitamin E, dissolve under 50 DEG C of water bath conditions, obtain oil phase, standby
With;
By 10.0% alpha-arbutin, 10.0% polyethylene glycol, 5.0%1,2- pentanediols, 30.0% water, in 50 DEG C of water-bath bars
20min is stirred with 20rpm rotating speed under part, obtains aqueous phase, it is standby;
Aqueous phase is added in oil phase, is stirred under 50 DEG C of water bath conditions and 20min is stirred with 20rpm rotating speed, stand 2min,
Produce alpha-arbutin nano-composition finished product.
The particle diameter of alpha-arbutin nano-composition is detected, can obtain the alpha-arbutin nano-composition particle diameter is
15.0nm。
Embodiment 8
By 5.0% polysorbate60,2.0%PEG-40 rilanit specials, 3.0%1,3- butanediols, 9.0% diethylene glycol list second
Base ether, 2.0% Miglyol 812N, 1.0% squalene, dissolve under 45 DEG C of water bath conditions, obtain oil phase, standby;
By 4.0% alpha-arbutin, 10.0%1,3- butanediols, 10.0%1,2- hexylene glycols, 54.0% water, in 45 DEG C of water-baths
Under the conditions of 20min stirred with 20rpm rotating speed, obtain aqueous phase, it is standby;
Aqueous phase is added in oil phase, is stirred under 45 DEG C of water bath conditions and 20min is stirred with 20rpm rotating speed, stand 1min,
Produce alpha-arbutin nano-composition finished product.
The particle diameter of alpha-arbutin nano-composition is detected, can obtain the alpha-arbutin nano-composition particle diameter is
32.6nm。
Embodiment 9
By 12.0% Emulsifier EL-60-35,10.0% propane diols, 5.0%1,2- hexylene glycols, 5.0% oleic acid,
2.0% isopropyl palmitate, 1.0% Sefsol 218,1.0% dimethicone, dissolve under 45 DEG C of water bath conditions, obtain
It is standby to oil phase;
By in 5.0% alpha-arbutin, 10.0% glycerine, 5.0%1,2- pentanediols, 44.0% water, in 45 DEG C of water-bath bars
20min is stirred with 20rpm rotating speed under part, obtains aqueous phase, it is standby;
Aqueous phase is added in oil phase, is stirred under 45 DEG C of water bath conditions and 20min is stirred with 20rpm rotating speed, stand 1min,
Produce alpha-arbutin nano-composition finished product.
The particle diameter of alpha-arbutin nano-composition is detected, can obtain the alpha-arbutin nano-composition particle diameter is
46.3nm。
Embodiment 10
By 12.0% polysorbas20,4.0% Emulsifier EL-60-20,3.0% ceteareth-20,7.0%1,
2- pentanediols, 3.0% oleic acid, 1.0% Labraso, 1.0% polyethylene glycol tristerin, 1%
Glyceryl triacetate, dissolved under 45 DEG C of water bath conditions, obtain oil phase, it is standby;
By 10.0% alpha-arbutin, 10.0% propane diols, 5.0%1,2- hexylene glycols, 43.0% water, in 45 DEG C of water bath conditions
Under 20min stirred with 20rpm rotating speed, it is standby with obtaining aqueous phase;
Aqueous phase is added in oil phase, is stirred under 45 DEG C of water bath conditions and 20min is stirred with 20rpm rotating speed, stand 1min,
Produce alpha-arbutin nano-composition finished product.
The particle diameter of alpha-arbutin nano-composition is detected, can obtain the alpha-arbutin nano-composition particle diameter is
36.4nm。
Embodiment 11
By 12.0% polysorbate60,6.0%PEG-40 rilanit specials, 5.0% oleic acid, 10.0% diethylene glycol mono-ethyl
Ether, 1.0% polyethylene glycol glyceryl laurate ester, 1.0% glyceryl linoleate, 2.0% diethyl sebacate, in 55 DEG C of water-bath bars
Dissolved under part, obtain oil phase, it is standby;
By 5.0% alpha-arbutin, 5.0% polyethylene glycol, 10.0%1,3- butanediols, 43.0% water, in 45 DEG C of water-bath bars
Stirred under part and 20min is stirred with 20rpm rotating speed, obtain aqueous phase, it is standby;
Aqueous phase is added in oil phase, is stirred under 45 DEG C of water bath conditions and 20min is stirred with 20rpm rotating speed, stand 1min,
Produce alpha-arbutin nano-composition finished product.
The particle diameter of alpha-arbutin nano-composition is detected, can obtain the alpha-arbutin nano-composition particle diameter is
72.6nm。
Embodiment 12
By 15.0% Tween 80,13.0% Emulsifier EL-60-35,13.0%PEG-20 rilanit specials, 5.0% 2
Propane diols, 7.0%1,2- hexylene glycols, 2.0% 2 pungent capric acid propylene glycol ester, dissolve under 45 DEG C of water bath conditions, obtain oil phase, standby
With;
By 20.0% alpha-arbutin, 5.0%1,3- butanediols, 10.0%1,2- pentanediols, 10% water, in 45 DEG C of water-bath bars
Stirred under part and 20min is stirred with 20rpm rotating speed, obtain aqueous phase, it is standby;
Aqueous phase is added in oil phase, is stirred under 45 DEG C of water bath conditions and 20min is stirred with 20rpm rotating speed, stand 1min,
Produce alpha-arbutin nano-composition finished product.
The particle diameter of alpha-arbutin nano-composition is detected, can obtain the alpha-arbutin nano-composition particle diameter is
45.3nm。
Embodiment 13
By 15.0% Emulsifier EL-60-40,12.0%PEG-30 rilanit specials, 5.0% propane diols, 5.0%1,
2- pentanediols, 3.0% isopropyl palmitate, 1.0% vitamin E, dissolve under 65 DEG C of water bath conditions, obtain oil phase, standby;
By 10.0% alpha-arbutin, 5.0% polyethylene glycol, 10.0% glycerine, 34.0% water, stirred under 65 DEG C of water bath conditions
Mix and 20min is stirred with 20rpm rotating speed, obtain aqueous phase, it is standby;
Aqueous phase is added in oil phase, is stirred under 65 DEG C of water bath conditions and 20min is stirred with 20rpm rotating speed, stand 1min,
Produce alpha-arbutin nano-composition finished product.
The particle diameter of alpha-arbutin nano-composition is detected, can obtain the alpha-arbutin nano-composition particle diameter is
26.5nm。
Embodiment 14
By 30.0% polysorbate40,2.0% polyethylene glycol 400 double glyceride, 4.0%1,3- butanediols, 1.0% oleic acid,
6.0% TC, 1.0% isopropyl myristate, 1.0% squalene, dissolve under 45 DEG C of water bath conditions, obtain
It is standby to oil phase;
14.0% alpha-arbutin, 15.0%1,2- hexylene glycols, 26% water are added in above-mentioned filtrate, in 45 DEG C of water-bath bars
Stirred under part and 20min is stirred with 20rpm rotating speed, obtain aqueous phase, it is standby;
Aqueous phase is added in oil phase, is stirred under 45 DEG C of water bath conditions and 20min is stirred with 20rpm rotating speed, stand 1min,
Produce alpha-arbutin nano-composition finished product.
The particle diameter of alpha-arbutin nano-composition is detected, can obtain the alpha-arbutin nano-composition particle diameter is
18.9nm。
Embodiment 15
By 11.0% Emulsifier EL-60-20,2.0% ceteareth-25,2.0% lecithin, 5.0% the third
Glycol, 3.0%1,3- butanediols, 1.0% isopropyl myristate, 2.0% Miglyol 812N, in 45 DEG C of water bath conditions
Lower dissolving, obtains oil phase, standby;
6.0% alpha-arbutin, 8.0% propane diols, 8.0%1,2- pentanediols, 52.0% water are added in above-mentioned filtrate,
Stirred under 45 DEG C of water bath conditions and 20min is stirred with 20rpm rotating speed, obtain aqueous phase, it is standby;
Aqueous phase is added in oil phase, is stirred under 45 DEG C of water bath conditions and 20min is stirred with 20rpm rotating speed, stand 1min,
Produce alpha-arbutin nano-composition finished product.
The particle diameter of alpha-arbutin nano-composition is detected, can obtain the alpha-arbutin nano-composition particle diameter is
38.6nm。
Embodiment 16
15.0% Tween 80,6.0%PEG-40 rilanit specials, 5.0% lecithin, 6.0% propane diols, 4.0%1,2-
Hexylene glycol, 2.0% polyethylene glycol glyceryl laurate ester, 1.0% glyceryl linoleate, 3% isopropyl myristate, in 45 DEG C of water
Dissolved under the conditions of bath, obtain oil phase, it is standby;
By 12.0% alpha-arbutin, 5.0%1,3- butanediols, 10.0%1,2- pentanediols, 31% water, in 45 DEG C of water-bath bars
Stirred under part and 20min is stirred with 20rpm rotating speed, obtain aqueous phase, it is standby;
Aqueous phase is added in oil phase, is stirred under 45 DEG C of water bath conditions and 20min is stirred with 20rpm rotating speed, stand 1min,
Produce alpha-arbutin nano-composition finished product.
The particle diameter of alpha-arbutin nano-composition is detected, can obtain the alpha-arbutin nano-composition particle diameter is
17.8nm。
Embodiment 17
By 15.0% polysorbate60,8.0% polyethylene glycol 400 double glyceride, 5.0% cocoyl glucoside, 5.0% lecithin
Fat, 6.0%1,3- butanediols, 1.0% oleic acid, 3.0% TC, 2.0% isopropyl myristate, 1.0%
Squalene, 2.0% glycerine, dissolve under 45 DEG C of water bath conditions, obtain oil phase, standby;
15.0% alpha-arbutin, 8.0% propane diols, 8.0%1,2- pentanediols, 21% water are added in above-mentioned filtrate,
Stirred under 45 DEG C of water bath conditions and 20min is stirred with 20rpm rotating speed, obtain aqueous phase, it is standby;
Aqueous phase is added in oil phase, is stirred under 45 DEG C of water bath conditions and 20min is stirred with 20rpm rotating speed, stand 1min,
Produce alpha-arbutin nano-composition finished product.
The particle diameter of alpha-arbutin nano-composition is detected, can obtain the alpha-arbutin nano-composition particle diameter is
87.4nm。
Embodiment 18
15.0% Tween 80,5.0% ceteareth -20,5.0% lecithin, 5.0%PEG-20 hydrogenated castors
Oil, 2.0% TC, 5.0%1,3- butanediols, 2.0% isopropyl myristate, 1.0% palmitic acid isopropyl
Ester, 2.0% Miglyol 812N, dissolve under 50 DEG C of water bath conditions, obtain oil phase, standby;
8.0% alpha-arbutin, 10.0% propane diols, 5.0% glycerine, 35% water are added in above-mentioned filtrate, in 45 DEG C
Stirred under water bath condition and 20min is stirred with 20rpm rotating speed, obtain aqueous phase, it is standby;
Aqueous phase is added in oil phase, is stirred under 45 DEG C of water bath conditions and 20min is stirred with 20rpm rotating speed, stand 1min,
Produce alpha-arbutin nano-composition finished product.
The particle diameter of alpha-arbutin nano-composition is detected, can obtain the alpha-arbutin nano-composition particle diameter is
19.7nm。
Embodiment 19
The alpha-arbutin nano-composition that embodiment 1~18 is obtained is placed 30 days under closed container, room temperature condition, inspection
The character and particle diameter of sample are looked into, experimental result is as shown in table 1.
The alpha-arbutin nano-composition stability test result of 1 embodiment of table 1~18
Stability test result shows:Alpha-arbutin nano-composition soilless sticking provided by the invention, lamination, and grain
Footpath meets application request between 17~90nm, and sample does not occur reunion lamination, sample grain after placing 30 days yet
Conspicuousness change does not occur for footpath, still meets practical application request, still relatively stable especially in the case of drug concentration height, not
It was found that alpha-arbutin crystallizes precipitation phenomenon, no drug leakage, therefore, alpha-arbutin nano-composition provided by the invention have good
Good stability.
Embodiment 20
Ordinary white cream, ordinary white emulsion and water white transparency aqua matrix are prepared according to cosmetic formula, will
The alpha-arbutin nano-composition that embodiment 6 obtains adds 4.0% and 8.0% and arrives matrix respectively, and is divided into normal temperature sample, heat-resisting
Sample, cold-resistant sample and illumination sample.Normal temperature sample avoid light place, heat-resisting sample is placed in the constant temperature oven of (48 ± 1) DEG C, resistance to
Cold sample is placed in 4 DEG C of refrigerators, and illumination sample is placed at illumination place, about 2 months, is carried out after room temperature to be restored with normal temperature sample
Compare.Observe its character appearance color, whether there is water-oil separating show as.Experimental result is as shown in table 2.
The alpha-arbutin nano-composition of 2 embodiment of table 13 and matrix compounding result of the test
Compounding result of the test shows:After alpha-arbutin nano-composition provided by the invention and matrix compounding, in normal temperature, low
Do not occur discoloration lamination after nearly 2 months days are placed under temperature, high temperature, illumination condition yet, meet practical application request, especially exist
It is still relatively stable in the case of external environment difference, do not find that alpha-arbutin crystallizes precipitation phenomenon, no drug leakage, therefore, this
The alpha-arbutin nano-composition that invention provides has good stability.
Comparative example 1
Alpha-arbutin creme is prepared according to conventional creme preparation method:By 5.0% alpha-arbutin, 3.0% stearic acid,
4.5% glycerin monostearate, 5.0% cetostearyl alcohol, 6.0% dimethyl silicone polymer melt in 75 DEG C of water-baths, obtain
Oil phase;10.0% glycerine, 5.0% propane diols, 0.3% triethanolamine and 65.2% purified water are dissolved in 75 DEG C of water-baths, obtained
To aqueous phase;Oil phase and aqueous phase are stirred, and emulsified, is cooled down, produces the alpha-arbutin creme that content is 5.0%.
Comparative example 2
The alpha-arbutin concentration that the blank creme prepared by the formula in comparative example 1 and method is prepared with embodiment 13 is
10.0% alpha-arbutin nano-composition is according to mass ratio 1:1 is compounded, and obtains the frost of the alpha-arbutin containing about 5.0%
Agent, compareed as creme.
Embodiment 21
It is that barrier layer of 160~220g male SD rats skin of abdomen as penetrating absorption carries out penetrating absorption using body weight.Will
The skin of intact unbroken is fixed between reception tank and supply pool (skin inner layer towards reception tank);Diffusion cell parameter is:Have
Imitate diffusion area 3.14cm2, receive pool volume about 7.0ml, magnetic stirring speed 600rpm;Dissolution medium is full of in reception tank
Physiological saline, bubble is excluded, open stirring, and constant temperature distinguishes even spread sample about to (37.0 ± 0.5) DEG C to skin surface
1g, reception liquid 0.35ml is drawn in 1h, 2h, 4h, 6h, 8h, 10h, 12h, and supplement dissolution medium 0.35ml, reception liquid uses
0.22 μm of organic membrane filtration, the concentration of alpha-arbutin in filtered reception liquid is determined using high performance liquid chromatography, calculated not
With the transdermal amount of time drug accumulation.
Alpha-arbutin unit area is calculated as follows accumulates transdermal amount:
Wherein:QsTo accumulate transdermal amount;S is effective diffusion area;V is physiological saline volume in reception tank;Ci is the 1st time
To reception liquid drug concentration during previous sample;N is n-th sample volume;Reception liquid drug concentration when Cn is the sub-sampling.
Sample prepared by embodiment 3~6 and comparative example 1, comparative example 2 is subjected to penetrating absorption according to the method described above, tested
As a result Fig. 1, Fig. 2 are seen.
As seen from Figure 1, the skin cumulative transit dose of the sample of comparative example 1 is all apparently higher than the skin of the sample of embodiment 3~6
Skin Percutaneous permeability.The 12h Percutaneous permeabilities of comparative example 1 are 1255 μ g/cm2, the 12h Percutaneous permeabilities difference of embodiment 3~6
For 750 μ g/cm2、612μg/cm2、238μg/cm2、322μg/cm2。
As seen from Figure 2, the skin cumulative hold-up of the sample of embodiment 3~6 is all apparently higher than the skin of the sample of comparative example 1
Skin accumulates hold-up.The 12h Percutaneous permeabilities of embodiment 3~6 are respectively 95.5 μ g/cm2、75.2μg/cm2、147.2μg/cm2、
187.5μg/cm2, the 12h Percutaneous permeabilities of comparative example 2 are respectively 286.2 μ g/cm2, the 12h Percutaneous permeabilities of comparative example 1 are only
55μg/cm2。
Alpha-arbutin bulk drug Percutaneous permeability combines much larger than alpha-arbutin nanometer it can be seen from Fig. 1, Fig. 2 contrast
Thing, but the skin hold-up of alpha-arbutin nano-composition is but more than alpha-arbutin bulk drug, can reach the 5.2 of bulk drug
Times.After illustrating that alpha-arbutin is contained by nano-carrier, alpha-arbutin transdermal amount can be significantly reduced, prevents that active component is saturating
Cross skin and enter blood circulation;Its hold-up in skin is increased substantially, it is highly concentrated in whitening target part by active component
Degree accumulation, it can effectively play it and suppress the function of melanocyte tyrosinase activity in skin, so as to effectively strengthen its skin
Whitening effect.
Embodiment 22
Use range of the alpha-arbutin in cosmetics is 3-7%, therefore alpha-arbutin prepared by Example 13~16 is received
Rice composition sample, respectively with the blank creme in comparative example 1 according to mass ratio 1:1 is compounded, and carries out skin irritation examination
Test:
Healthy rabbits 18 are taken, body weight (2.0 ± 0.2) kg, are randomly divided into 6 groups, every group of animal 3,24h will before experiment
Rabbit skin of back both sides unhairing, 24h checks whether skin of unhairing is injured after unhairing, and compromised skin is unfit to do skin irritation examination
Test.The creme for the alpha-arbutin nano-composition preparation that smearing is obtained using embodiment 13~16 3 times daily, it is continuous to smear 7 days,
Smear blank creme (not giving any medicine) simultaneously to be compareed, viewing test result, result of the test is listed in Table 3 below.
Result of the test in table 3 can be seen that the alpha-arbutin nano-composition prepared using embodiment 13~16
The creme and blank creme of preparation are applied to after a rabbit skin without congested, red and swollen phenomenon, illustrate α-black bearberry provided by the invention
Glycosides nano-composition does not have excitant to skin.
The nano-composition of 3 embodiment of table 13~16 and blank group skin irritation observation result
"+" rabbit dermohemia, redness;" ++ " represents that congested, red and swollen phenomenon still exists, but has increase trend;"-" represents
Without congested, red and swollen phenomenon.
Embodiment 23
Use range of the alpha-arbutin in cosmetics is 3-7%.The blank prepared by the formula in comparative example 1 and method
The alpha-arbutin nano-composition that creme is 10.0% with alpha-arbutin concentration prepared by embodiment 13 is according to mass ratio 1:1 is carried out
Compounding, obtains the creme of the alpha-arbutin containing about 5.0%, as test sample, carries out whitening effect experiment:
Using adult inner forearm 2cm × 2cm regions of 10 skin healths as recipient site, side is test block, often
The creme for the alpha-arbutin nano-composition preparation that its smearing is obtained using embodiment 13~16 1 time, it is continuous to smear 28 days;Side
For check plot, blank creme is smeared.Every 7 days melanin content in skin was checked with dermal melanin tester.Result of the test
It is listed in Table 4 below.
Result of the test in table 4 can be seen that the alpha-arbutin nano-composition prepared using embodiment 13 and prepare
Creme and blank creme be applied to after adult's inner forearm that melanin content significantly reduces in skin, present invention offer is provided
Alpha-arbutin nano-composition whitening function it is excellent.
The nano-composition of 4 embodiment of table 13~16 and blank group whitening effect experimental observation result
The measurement range of instrument is 0~999, and measured value is higher, illustrates that the content of melanin in skin is higher.
Embodiment 24
The alpha-arbutin nano-composition that Example 3 obtains, it is divided to two with 25ml150mM phosphate buffers (pH=7.5)
Secondary homogenate, merge homogenate centrifugation 5min (4 DEG C) twice.Supernatant carries out antioxidation activity as sample, removes free radical
Ability determines.Same method prepares and is free of alpha-arbutin but the blank control product including nano-composition other components.
It is accurate to weigh 20mgDPPH with absolute ethyl alcohol constant volume in 250ml volumetric flasks, obtain 2 × 10-4mol/L DPPH
Solution.517nm absworption peak is rolled into a ball using the feature aubergine of DPPH solution, hybrid reaction is loaded, uses spectrophotometry
Meter measure plus the decline with reference to A517 absorption values after antioxidant (vitamin E) and sample, represent its elimination energy to free radical
Power size.Carry out calculating the inhibiting rate of polyphenoils according to the following formula.
In formula:[DPPH]T=0The initial concentration of DPPH.free radical in -0 moment system
[DPPH]tThe concentration of DPPH.free radical in-t system
The purple of solution gradually becomes shallower as in 5min after vitamin E and sample addition free radical system, under light absorption value is rapid
Drop is stable after 70min;Solution colour is without significant change after blank group addition system.As a result Fig. 3 is seen.
It can be drawn by experimental result, nano-composition provided by the invention has certain oxidation resistance.
As seen from the above embodiment, alpha-arbutin nano-composition stability provided by the invention is good, drugloading rate is big, skin
Permeability is good, can be good at playing the effect such as whitening, anti-oxidant, and preparation method of the present invention is simple, easily controllable, suitable work
Industry, large-scale production.
Described above is only the preferred embodiment of the present invention, it is noted that for the ordinary skill people of the art
For member, under the premise without departing from the principles of the invention, some improvements and modifications can also be made, these improvements and modifications also should
It is considered as protection scope of the present invention.
Claims (10)
1. a kind of alpha-arbutin nano-composition, it is characterised in that the alpha-arbutin nano-composition includes following weight hundred
Divide the component of ratio:Alpha-arbutin 0.1%~20.0%, emulsifying agent 5.0%~50.0%, assistant for emulsifying agent 5.0%~30.0%, liquid
Body fat matter 3.0%~15.0%, polyalcohol 5.0%~25.0%, surplus are water.
2. alpha-arbutin nano-composition according to claim 1, it is characterised in that the surfactant is tween
80th, polysorbate60, polysorbate40, polysorbas20, the ether of Emulsifier EL-60-20, the ether of Emulsifier EL-60-30, polyoxyethylene caster
Oily-35 ethers, the ether of Emulsifier EL-60-40, Cremophor RH40, PEG-30 rilanit specials, PEG-20 hydrogenated castors
Oil, PEG-10 rilanit specials, PEG-5 rilanit specials, polyethylene glycol 400 monoglyceride, polyethylene glycol 400 double glyceride,
Macrogol 600 monoglyceride, Macrogol 600 double glyceride, cocoyl glucoside (the more glycosides of cocoyl glucose), cetearyl alcohol
One or more of mixtures in alcohol polyethers -20, ceteareth -25, butylol polyether -26 and lecithin.
3. alpha-arbutin nano-composition according to claim 1, it is characterised in that the cosurfactant is diethyl
Glycol list ethylether, polyethylene glycol, 1,3 butylene glycol, 1,2- propane diols, DPG, 1,2- hexylene glycols, 1,2- pentanediols, oil
One or more of mixtures in acid, octyl dodecanol.
4. alpha-arbutin nano-composition according to claim 1, it is characterised in that the liquid fatty is myristic acid
Isopropyl ester, isopropyl palmitate, Miglyol 812N, Labraso, polyethylene glycol laurate are sweet
Grease, polyethylene glycol tristerin, glyceryl linoleate, Sefsol 218, two pungent capric acid propylene glycol esters, decanedioic acid
In diethylester, pungent capric acid cocoa butter, isononyl isononanoate, glyceryl triacetate, dimethicone, vitamin E and squalene
One or more of mixtures.
5. alpha-arbutin nano-composition according to claim 1, it is characterised in that described polyalcohol is poly- second two
One or more of mixing in alcohol, propane diols, DPG, glycerine, 1,2- hexylene glycols, 1,3 butylene glycol and 1,2- pentanediols
Thing.
6. the alpha-arbutin nano-composition according to Claims 1 to 5 any one, it is characterised in that the α-black bearberry
The particle diameter of glycosides nano-composition is 15~300nm.
7. the preparation method of the alpha-arbutin nano-composition described in claim 6, comprises the following steps:
(1) emulsifying agent, assistant for emulsifying agent, liquid fatty are dissolved, obtains oil phase;
(2) alpha-arbutin, water, polyalcohol are mixed into dissolving, obtains aqueous phase;
(3) aqueous phase for obtaining the step (2) and oil phase obtained by the step (1), mix, obtain alpha-arbutin while stirring
Nano-composition;
(4) got product after the alpha-arbutin nanoemulsions that the step (3) obtains being stood into cooling;
Wherein, the order of the step (1) and step (2) can exchange.
8. the preparation method of the alpha-arbutin nano-composition described in claim 7, it is characterised in that stirred in the step (1)
The temperature for mixing dissolving is 40~80 DEG C, and the time is 10~30min;The temperature of step (2) the reclaimed water stirring and dissolving is 40~80
DEG C, the time is 10~30min;
The rotating speed that profit mixes in the step (3) is 10~60rpm, and the time is 15~40min;
It is preferred that step (4) in time of repose be 1~3min.Gained finished product grain size is 15-300nm.
A kind of 9. alpha-arbutin nano-composition that preparation method as described in claim 7 or 8 obtains.
10. a kind of alpha-arbutin nano-composition as described in claim 1~6 any one is in effect cosmetic is prepared
Using.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN201711058551.3A CN107811881A (en) | 2017-11-01 | 2017-11-01 | A kind of α ursin nano-compositions of whitening antioxidation and preparation method and application |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN201711058551.3A CN107811881A (en) | 2017-11-01 | 2017-11-01 | A kind of α ursin nano-compositions of whitening antioxidation and preparation method and application |
Publications (1)
Publication Number | Publication Date |
---|---|
CN107811881A true CN107811881A (en) | 2018-03-20 |
Family
ID=61604532
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201711058551.3A Pending CN107811881A (en) | 2017-11-01 | 2017-11-01 | A kind of α ursin nano-compositions of whitening antioxidation and preparation method and application |
Country Status (1)
Country | Link |
---|---|
CN (1) | CN107811881A (en) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN108721133A (en) * | 2018-06-28 | 2018-11-02 | 武汉百思凯瑞生物科技有限公司 | A kind of alpha-arbutin conveys nano-composition and its preparation method and application altogether |
CN108785122A (en) * | 2018-06-28 | 2018-11-13 | 武汉百思凯瑞生物科技有限公司 | A kind of anti-acne conveys nano-composition and its preparation method and application altogether |
CN110200883A (en) * | 2019-06-19 | 2019-09-06 | 武汉百思凯瑞生物科技有限公司 | A kind of antiallergic conveys nano-composition and its preparation method and application altogether |
Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101199472A (en) * | 2007-12-24 | 2008-06-18 | 浙江长生鸟珍珠生物科技有限公司 | Pearl vitamin E whitening moisturizing face masque and process for preparing same |
CN105287235A (en) * | 2015-11-25 | 2016-02-03 | 广州立白企业集团有限公司 | Nano-scale biological fiber whitening mask and use method thereof |
CN105434185A (en) * | 2015-02-13 | 2016-03-30 | 马南行 | Cosmetic composition capable of whitening and brightening skin and preparation method thereof |
CN105726387A (en) * | 2016-02-17 | 2016-07-06 | 佛山市芊茹化妆品有限公司 | Skin whitening microemulsion |
CN106580755A (en) * | 2017-03-02 | 2017-04-26 | 武汉百思凯瑞纳米科技有限公司 | Nanometer composition containing skin-moistening and whitening components, and preparation method and application thereof |
CN106822101A (en) * | 2017-02-20 | 2017-06-13 | 刘卫 | A kind of epiphysin nano-composition and its preparation method and application |
-
2017
- 2017-11-01 CN CN201711058551.3A patent/CN107811881A/en active Pending
Patent Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101199472A (en) * | 2007-12-24 | 2008-06-18 | 浙江长生鸟珍珠生物科技有限公司 | Pearl vitamin E whitening moisturizing face masque and process for preparing same |
CN105434185A (en) * | 2015-02-13 | 2016-03-30 | 马南行 | Cosmetic composition capable of whitening and brightening skin and preparation method thereof |
CN105287235A (en) * | 2015-11-25 | 2016-02-03 | 广州立白企业集团有限公司 | Nano-scale biological fiber whitening mask and use method thereof |
CN105726387A (en) * | 2016-02-17 | 2016-07-06 | 佛山市芊茹化妆品有限公司 | Skin whitening microemulsion |
CN106822101A (en) * | 2017-02-20 | 2017-06-13 | 刘卫 | A kind of epiphysin nano-composition and its preparation method and application |
CN106580755A (en) * | 2017-03-02 | 2017-04-26 | 武汉百思凯瑞纳米科技有限公司 | Nanometer composition containing skin-moistening and whitening components, and preparation method and application thereof |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN108721133A (en) * | 2018-06-28 | 2018-11-02 | 武汉百思凯瑞生物科技有限公司 | A kind of alpha-arbutin conveys nano-composition and its preparation method and application altogether |
CN108785122A (en) * | 2018-06-28 | 2018-11-13 | 武汉百思凯瑞生物科技有限公司 | A kind of anti-acne conveys nano-composition and its preparation method and application altogether |
CN108721133B (en) * | 2018-06-28 | 2021-04-13 | 武汉百思凯瑞生物科技有限公司 | Alpha-arbutin co-delivery nano composition and preparation method and application thereof |
CN110200883A (en) * | 2019-06-19 | 2019-09-06 | 武汉百思凯瑞生物科技有限公司 | A kind of antiallergic conveys nano-composition and its preparation method and application altogether |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
CN106822101B (en) | A kind of epiphysin nano-composition and its preparation method and application | |
CN108743430A (en) | A kind of total conveying nano-composition of Symwhite-337 and its preparation method and application | |
CN108721133A (en) | A kind of alpha-arbutin conveys nano-composition and its preparation method and application altogether | |
CN108451837A (en) | A kind of whitening liquid-crystal composition and its preparation method and application | |
CN106691888B (en) | Glabridin nano composition with high skin retention and preparation method and application thereof | |
CN108785122A (en) | A kind of anti-acne conveys nano-composition and its preparation method and application altogether | |
CN101664372B (en) | Antioxidant network efficacy nanoemulsion externally used for skin and preparation method thereof | |
TW200902082A (en) | Useful vesicle for skin external preparation and skin external preparation containing the vesicle | |
CN113226277B (en) | Whitening agent, hyaluronic acid production promoter, collagen production promoter, intracellular active oxygen scavenger, irritation relieving agent, wrinkle improving agent, complex, cosmetic and skin external preparation | |
Malik et al. | Nanostructured gel for topical delivery of azelaic acid: Designing, characterization, and in-vitro evaluation | |
CN106580755A (en) | Nanometer composition containing skin-moistening and whitening components, and preparation method and application thereof | |
CN107242982A (en) | A kind of fair-skinned bright Virgin's milk liquid and preparation method thereof | |
TW200815021A (en) | Nanoliposome using esterified lecithin and method for preparing the same, and composition for preventing or treating skin diseases comprising the same | |
CN110636833A (en) | Topical therapy using taxane nanoparticles for the treatment of skin malignancies | |
CN107496186A (en) | A kind of Kaempferol nano-composition and its preparation method and application | |
CN107811881A (en) | A kind of α ursin nano-compositions of whitening antioxidation and preparation method and application | |
JP5614921B2 (en) | Liquid crystal lamellar cosmetic composition and cosmetic containing the same | |
CN107550775A (en) | Natural plants anti-acne jelly and preparation method thereof | |
CN109481321A (en) | A kind of Trenaxmine flexible lipidosome of whitening spot-removing and its preparation method and application | |
WO2018090149A1 (en) | Putrescine slow-release topical formulations | |
CN115804737B (en) | Moisturizing cream with lamellar liquid crystal structure, preparation method and application | |
CN104523458A (en) | Whitening essence containing bearberry extract lipid nanoemulsion | |
CN106389168B (en) | With the oil-in-water nanometer creams and preparation method that whitening effect is positively charged | |
CN102665672B (en) | Polymersome and process for producing same | |
Farooqui et al. | Permeation enhancer nanovesicles mediated topical delivery of curcumin for the treatment of hyperpigmentation |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
PB01 | Publication | ||
PB01 | Publication | ||
SE01 | Entry into force of request for substantive examination | ||
SE01 | Entry into force of request for substantive examination | ||
RJ01 | Rejection of invention patent application after publication |
Application publication date: 20180320 |
|
RJ01 | Rejection of invention patent application after publication |