CN100548292C - A kind of microemulsion that contains vitamin C and vitamin E - Google Patents

A kind of microemulsion that contains vitamin C and vitamin E Download PDF

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CN100548292C
CN100548292C CNB2006100430537A CN200610043053A CN100548292C CN 100548292 C CN100548292 C CN 100548292C CN B2006100430537 A CNB2006100430537 A CN B2006100430537A CN 200610043053 A CN200610043053 A CN 200610043053A CN 100548292 C CN100548292 C CN 100548292C
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vitamin
microemulsion
oil
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surfactant
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CN1875965A (en
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欧阳五庆
董红宾
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Northwest A&F University
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Abstract

The invention discloses a kind of microemulsion that contains vitamin C and vitamin E, contain vitamin C in the continuous phase of this microemulsion (foreign minister), its content in whole microemulsion is 0.1%~25.0%; Contain vitamin E in the decentralized photo of this microemulsion (inner phase), its content in whole microemulsion is 0.1%~2.0%; The substrate of this microemulsion is made up of surfactant 9.0%~48.0%, oil 1.0%~20.0%, water 40.0%~89.0%.This microemulsion contains vitamin C and vitamin E simultaneously, and can not only work in coordination with and utilize this two kinds of good antioxidants, can also this be the basis, in this microemulsion, add other functional components, be widely used in fields such as cosmetics, medicine.Simultaneously, this microemulsion has better percutaneous permeability and skin spreadability, and safety is good, and the bioavailability height is a kind of invention that has a extensive future.

Description

A kind of microemulsion that contains vitamin C and vitamin E
Technical field
The invention belongs to medicine and cosmetic field, relate to and a kind ofly both can directly be used as cosmetics and medicine, also can add the microemulsion that other active ingredient forms new product on this basis, be specifically related to a kind of microemulsion that contains vitamin C and vitamin E and preparation method thereof.
Background technology
Vitamin C has another name called ascorbic acid, is human nutrition, the necessary micro-organic compound of growth, and metabolism, growth promoter, the health of body is had very important effect, as long-term lacking, will cause the physiological function obstacle and some disease takes place.Its physiological action has: vitamin C can promote the formation of collagen, raise immunity, promote calcium, the absorption of ferrum, promote cholesterol to drain, prevent atherosclerosis, reduce capillary fragility, break-up tissue amine makes vasoconstriction, permeability reduces, and promotes liver cell regeneration, hepatic glycogen is synthetic, strengthen liver detoxification function, antioxidant radical and antioxidation, vitamin C also are the most representative Melanin inhibitors, its mechanism has two: the one, and when tyrosinase catalysis reacts, reducible melanic intermediate DOPA quinone and suppressed melanic generation; Another effect is to make dark oxidized form melanin be reduced into the reduced form melanin of light color.Melanosis, chloasma hepaticum etc. are treated, improved to ascorbic acid energy skin whitening, extensive use in cosmetics and medicine.
The function of vitamin E has: the scavenger of free radical; antioxidant activity; vitamin E is particularly very important to the lymphocytic function of T to normal immunologic function; can increase serum insulin levels and secretion deposit thereof; and islet cells had the certain protection effect; can suppress the hepatic fibrosis that the ferrum overload causes; application in cosmetics is to utilize its antioxidant activity to remove free radical on the one hand; on the other hand; vitamin E is the derivant of unsaturated fatty acid; other greasy functions of the skin absorbs of reinforcement are arranged, can promote the metabolism of skin.As lack vitamin E, can make skin dried-up, coarse.
Vitamin E and vitamin C all are antioxidants, can both play anti-oxidative damage when using separately, effects such as enhancing human body immunity function, but when two kinds of vitamin are used in combination, can strengthen their antioxidant effect.But because the difference of physicochemical property separately, vitamin C is a water solublity, and vitamin E is an oil-soluble, being used in combination of the two still has certain difficulty, the two is difficult to combine when particularly smearing use, and can only make common emulsion reluctantly, but common emulsion has following shortcoming: the formation of (1) common emulsion generally needs the external world that energy is provided, as forming the production cost height through stirring, Ultrasonic Pulverization, milling treatment of colloid etc.; (2) common emulsion is thermodynamic unstable system, will take place coalescent in depositing process and final shared oil/water is biphase; (3) particle diameter of common emulsion is difficult for absorbing generally all greater than 400nm.So it is simpler, more stable to invent a kind of preparation technology, easier diffusion and penetrate into skin, the new medium that can significantly improve the utilization rate of the two has become the current problem that faces.
Summary of the invention
The present invention seeks to shortcoming and defect at above-mentioned prior art, provide a kind of bland to human body, environment is not polluted, more can effectively bring into play a kind of microemulsion of vitamin C and vitamin E effect, this microemulsion has better percutaneous permeability, can strengthen the dissolubility of effective ingredient, but improve the two spreadability on skin.
The technical scheme that realizes the foregoing invention purpose is a kind of microemulsion that contains vitamin C and vitamin E, it is characterized in that, contains vitamin C in the continuous phase of this microemulsion (foreign minister), contains vitamin E in the decentralized photo of this microemulsion (inner phase); Mainly be made up of the raw material of following component: vitamin C 0.1%~25.0%, vitamin E 0.1%~2.0%, surfactant 9.0%~48.0%, oil 1.0%~20.0%, water 40.0%~89.0% are formed.
The present invention is a kind of O/W type microemulsion, mainly as cosmetics and medicinal usage.
In the selection of surfactant, the present invention selects the nonionic surfactant of hypotoxicity and good biocompatibility for use.The toxicity of nonionic surfactant is less relatively, and is more stable in solution, is not subject to the influence of strong electrolyte, inorganic salts, also is not subject to the influence of soda acid, and good with the compatibility of other surfactants, and haemolysis is less.Available surfactant has: polyoxyethylene hydrogenated Oleum Ricini (as RH-40), castor oil polyoxyethylene ether series (as EL-40) and alkylphenol polyoxyethylene series (as TX-8,10 etc.), span-80.When span-80 and above a few class surfactant compound used, its shared ratio (mass ratio) in total surfactant only was 10.0%~30.0%.
The present invention forms this rule of microemulsion when close easily according to the HLB value of the HLB value of the required surfactant of emulsifying oil phase and surfactant, the oils and fats of selecting for use has: one or several of isopropyl myristate (IPM), isopropyl palmitate (IPP), iso-octyl palmitate, Jojoba oil, white mineral oil, caprylic/capric triglyceride (GTCC), mink oil, Adeps Serpentis, almond oil, Fructus Tritici aestivi wet goods composite.These oils and fatss are little to skin irritation, be in a liquid state, do not have bad abnormal smells from the patient under the room temperature, have good emulsibility and wettability, and infiltration is made skin lubrication glossy by skin absorbs easily.
The present invention selects bland cosurfactant, mainly contains glycerol, n-butyl alcohol, 1,3 butylene glycol etc., accounts for 0~25.0% in the surfactant item.Cosurfactant can be adjusted HLB VALUE OF SURFACTANTS (HLB), can further reduce interfacial tension, increases the compliance and the rigidity of film, is inserted in the interfacial film, promotes the formation of the film that radius of curvature is very little, enlarges microemulsion and forms the zone.
The used water of the present invention is distilled water.
Microemulsion that can a kind of transparent and stable of spontaneous formation when the proportioning of some component of the present invention is suitable, and add the appearance that an amount of cosurfactant can be avoided thickness attitudes such as gel or liquid crystal; The emulsibility of some surfactant is fine, when, not needing to add cosurfactant and also sticky attitude can not occur when suitable with the ratio of oil phase, finally forms transparent and uniform and stablizes microemulsion system.
Another object of the present invention is a kind of preparation method that contains vitamin C, vitamin E nano emulsion formulation of arch, may further comprise the steps:
1) it is standby to take by weighing each component vitamin C, vitamin E, surfactant, oil, distilled water;
2) preparation of surfactant phase: with the surfactant use or composite separately of described weight, calculate hydrophile-lipophile balance (HLB) value of this system, stir with the cosurfactant of described weight; The HLB value of common emulsifying agent can be found, because hydrophile-lipophile balance (HLB) value of surfactant has additive properties, the available quality averaging method is obtained the HLB value of surfactant.For example, after two kinds of surfactant A, B mix, the hydrophile-lipophile balance HLB of its mixed surfactant ABValue is
HLB AB=(W AHLB A+W BHLB B)/(W A+W B)
W in the formula A, W B---the quality of blend surfactants A, B;
HLB A, HLB B---the HLB value of surfactant A, B.
3) preparation of oil phase: according to the HLB value of surfactant phase, select one or more oil and vitamin E composite, transfer its ratio, the HLB value of required emulsifying agent is close with surfactant HLB mutually when making it emulsified.Computational methods and 2) with, i.e. certain oily needed HLB value of emulsifying also has additive properties, the available quality averaging method is tried to achieve miscella required HLB value when emulsified.
4) preparation of water: as required, prepare certain density vitamin C aqueous solution.
5) in 9: 1~1: 9 the rule change surfactant phase and the ratio of oil phase, fix its gross mass.The aqueous solution of slow vitaminize C under the room temperature fully stirs, until forming clear, the viscosity O/W type microemulsion similar to aqueous solution.The transparency of observation system directly perceived is to judge whether being microemulsion.The critical water yield when record system becomes clarification by muddiness.
The particle diameter of the microemulsion that the present invention is prepared is placed for a long time or still can be kept transparent, not stratified through 4000rpm * 30min between 10~100nm.Leave standstill under the different temperatures and observed one month, the equilibrium temperature scope of each microemulsion of writing out a prescription is 10~60 ℃.
For effect of the present invention is described, the inventor has made contrast test, has investigated Vit.C, Vit.E, Vit.C+Vit.E (Vit.C and Vit.E's is simply shared) and Vit.C-Vit.E microemulsion of the present invention to H 2O 2The influence of MTT, protein and MDA content in the injured skin fibroblast.
1 materials and methods
1.1 material and reagent mouse skin fibroblast are from moving academy of science of Xibei Univ. of Agricultural ﹠ Forest Science ﹠ Technology Cell Biology Experiment chamber.Trypsin is available from Gibco company, and newborn hyclone is available from Hyclone company, 30%H 2O 2Available from Shanghai Habo Chemical Technology Co., Ltd., MTT, dimethyl sulfoxide (DMSO), Coomassie brilliant blue are available from Sigma company, malonaldehyde (MDA) assay test kit builds up bio-engineering research institute available from Nanjing, and Vit.C contains bio tech ltd (lot number 060408), Vit.E available from the bright industry and trade company limited of Shanghai power (lot number VX05312001) available from Shaanxi section.
1.2 going down to posterity and cultivating after the frozen skin flbroblast recovery of skin flbroblast reaches in the culture bottle, places 37 ℃, 5%CO 2, in 95% saturation of the air humidity incubator, cultivate with the DMEM synthetic medium that contains 10% hyclone.When cell monolayer compiles when reaching 80%, the trypsin with 0.25% adds the EDTA digestion of equivalent, with the Digestive system sucking-off, move into centrifuge tube, add DMEM culture fluid, centrifugal, abandoning supernatant, add new culture medium, after the piping and druming cell evenly is inoculated in culture plate repeatedly.
1.3Vit.C, Vit.E, Vit.C-Vit.E microemulsion and H 2O 2Preparation Vit.C, Vit.E, Vit.C-Vit.E microemulsion and 30%H 2O 2Being diluted to respective concentration with the culture fluid that contains serum tests.
The grouping of test method and dosage is divided into 6 groups and tests 1.4 will be cultured to the skin flbroblast of fusion state.Normal control group, damage matched group (final concentration is 10mmol/L), Vit.C organize (Vit.C+H 2O 2), Vit.E organizes (Vit.E+H 2O 2), Vit.C+Vit.E organizes (Vit.C+Vit.E+H 2O 2), Vit.C-Vit.E microemulsion group (Vit.C-Vit.E microemulsion+H 2O 2).The final concentration of Vit.C, Vit.E is respectively 100 μ mol/L, 50 μ mol/L, and the final concentration of Vit.C and Vit.E is respectively 100 μ mol/L, 50 μ mol/L, H in the Vit.C-Vit.E microemulsion 2O 2Final concentration with the damage matched group.Before damage, Vit.C and Vit.E group add the culture fluid that contains Vit.C and Vit.E respectively and hatch 24h, H 2O 2Induce damage, cultivate 4h again, stop cultivating, detect the content of cell viability, protein and MDA then.
2 observation index and assay method
2.1 cell viability is measured the MTT determination of light absorption method that adopts.
2.2 cell protein is measured the Coomassie brilliant blue method that adopts.Getting cell pyrolysis liquid, is standard series with bovine serum albumin (BSA), and the 595nm place surveys absorbance, calculates protein content.
2.3 the MDA assay adopts thiobarbituricacid (TBA) method in the cell, builds up the MDA test kit of biological product company production by Nanjing and measures.
2.4 statistical procedures gained experimental data all adopts the SPSS10.0 statistical package to carry out correlation analysis.
3 results
Vit.C, Vit.E, Vit.C+Vit.E and Vit.C-Vit.E microemulsion are to H 2O 2The influence of MTT, protein and MDA content sees the following form in the injured skin fibroblast.
Vit.C, Vit.E, Vit.C+Vit.E and Vit.C-Vit.E microemulsion are to H 2O 2The influence of MTT, protein and MDA content in the injured skin fibroblast
Figure C20061004305300081
As seen from the above table, normal control group, Vit.C group and Vit.E group cell viability, protein content all are higher than the damage matched group, and difference has significance (p<0.01); To H 2O 2Oxidative damage due to the fibroblast all there is protective effect; simple shared its effect of Vit.C and Vit.E slightly is better than the Vit.C and the Vit.E effect sum of same concentrations; show that the two has synergism; but the protective effect of Vit.C-Vit.E microemulsion group is better than the Vit.C+Vit.E group; show that the present invention can bring into play the collaborative utilization of Vit.C and Vit.E more fully, can make effective ingredient more easily enter the cell performance thereby its reason is parents' characteristic of microemulsion.
The prepared microemulsion technology of the present invention is simple, good stability, available water infinite dilution to be to adjust concentration.In addition, the prepared microemulsion of the present invention can also be as a kind of substrate, both can the resolubilization fat-soluble medicine, as vitamin A, vitamin D, vitamin K, the volatilization wet goods that from Chinese medicine, extracts; Can add water miscible medicine easily again, as arbutin, glycyrrhizic acid, fruit acid skin care agent etc., can be widely used in fields (as embodiment 12) such as cosmetics and medicine, be a kind of invention that is widely used, has a extensive future.
The specific embodiment
Mode below by embodiment further specifies the present invention, but does not limit the present invention in the described scope of embodiments.
Embodiment 1
Constituent mass/g
EL-40 23.08
IPM 2.05
Vitamin E 0.51
Vitamin C 18.59
Distilled water adds to 100.00
Preparation method: 1) take by weighing each component EL-40 23.08g, IPM 2.05, vitamin E 0.51g, vitamin C 18.59g, distilled water 55.05g, standby; 2) with the EL-40 of described weight in a container, again with IPM: the composite oil and the EL-40 mixing of vitamin E=4: 1; 3) slowly drip 25.0% vitamin C water solution in the container, fully stir, just begun the system water white transparency, along with increasing of water, phenomenons such as bubble increases, viscosity increases, transparency descends, viscosity reduces successively appear in system, system becomes rare suddenly when adding to 9.93g, and the oil-in-water type nano-emulsion forms.
Embodiment 2
Component unit/g
EL-40 21.43
IPM: Jojoba oil=3: 1 2.09
Vitamin E 0.60
Vitamin C 16.62
Distilled water adds to 100.00
Preparation method is with embodiment 1.
Embodiment 3
Component unit/g
RH-40 22.66
IPM 2.01
Vitamin E 0.50
Vitamin C 15.70
Distilled water adds to 100.00
Preparation method is with embodiment 1.
Embodiment 4
Component unit/g
RH-40 18.07
IPM 3.61
Vitamin E 0.92
Vitamin C 10.35
Distilled water adds to 100.00
Preparation method is with embodiment 1.
Embodiment 5
Component unit/g
TX-8 22.32
IPM 1.98
Vitamin E 0.50
Vitamin C 12.80
Distilled water adds to 100.00
Preparation method is with embodiment 1.
Embodiment 6
Component unit/g
TX-8 20.43
IPM 4.09
Vitamin E 1.02
Vitamin C 8.62
Distilled water adds to 100.00
Preparation method is with embodiment 1.
Embodiment 7
Component unit/g
EL-40: glycerol=2: 1 20.43
IPM 1.30
Vitamin E 1.02
Vitamin C 10.52
Distilled water adds to 100.00
Preparation method is with embodiment 1.
Embodiment 8
Component unit/g
EL-40: span-80=13: 7 34.1
White mineral oil 2.80
Vitamin E 1.02
Vitamin C 15.62
Distilled water adds to 100.00
Preparation method is with embodiment 1.
Embodiment 9
Component unit/g
EL-40 13.79
IPM 0.92
Semen Tritici aestivi germ oil 0.18
Almond oil 0.16
Mink oil 0.20
Adeps Serpentis 0.15
Vitamin E 0.12
Vitamin C 8.01
Distilled water adds to 100.00
Preparation method is with embodiment 1.
Embodiment 10
Component unit/g
Tx-8 8.53
1,3 butylene glycol 4.26
IPM 0.95
Semen Tritici aestivi germ oil 0.18
Almond oil 0.16
Vitamin E 0.12
Vitamin C 6.08
Distilled water adds to 100.00
Preparation method is with embodiment 1.
Embodiment 11
Component unit/g
EL-40 13.79
IPM 0.92
Semen Tritici aestivi germ oil 0.18
Almond oil 0.16
Mink oil 0.20
Adeps Serpentis 0.15
Vitamin E 0.12
Amino acid humectant 1.35
Arbutin 2.53
Marine polysaccharide emollient 2.76
Fruit acid skin care agent 3.06
Essence is an amount of
Antiseptic is an amount of
Vitamin C water solution (25.0%) adds to 100.00
Preparation method is with embodiment 1.

Claims (2)

1, a kind of microemulsion that contains vitamin C and vitamin E mainly is made up of the raw material of following component: vitamin C 0.1%~25.0%, vitamin E 0.1%~2.0%, surfactant 9.0%~48.0%, oil 1.0%~20.0%, water 40.0%~89.0%;
Above-mentioned surfactant is meant one or more composite of alkylphenol polyoxyethylene, castor oil polyoxyethylene ether, polyoxyethylene hydrogenated Oleum Ricini, Span-80, or above several surfactant and glycerol, 1,3 butylene glycol cosurfactant is composite;
Said oil is meant one or several composite of isopropyl myristate, Jojoba oil, white mineral oil, iso-octyl palmitate, isopropyl palmitate, tricaprin, mink oil, Adeps Serpentis, almond oil, Semen Tritici aestivi germ oil;
Said water is meant distilled water.
2, the described a kind of application of microemulsion in preparation cosmetics and medicine that contains vitamin C and vitamin E of claim 1.
CNB2006100430537A 2006-06-29 2006-06-29 A kind of microemulsion that contains vitamin C and vitamin E Expired - Fee Related CN100548292C (en)

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Publication number Priority date Publication date Assignee Title
CN101297680B (en) * 2008-04-25 2010-11-03 天津生机集团股份有限公司 Composite vitamin emulsion and preparation thereof
CN101766261B (en) * 2010-01-11 2011-09-28 广东大华农动物保健品股份有限公司 Nano nutrient microemulsion and preparation method thereof
CN102552293B (en) * 2011-12-31 2014-05-21 沈阳药科大学 Compound vitamin submicron emulsion lyophilized powder for injection and preparation method of compound vitamin submicron emulsion lyophilized powder
CN106109413B (en) * 2016-07-29 2019-04-16 河南中医学院 A kind of oil-in-water type nano-emulsion matrix
CN106138083A (en) * 2016-07-29 2016-11-23 河南中医学院 A kind of treat the herbal mixture nanometer emulsifiable paste that skin is chapped from the cold
CN106943395A (en) * 2017-04-18 2017-07-14 扬州大学 The preparation method of anti-oxidant nanoemulsions containing vitamin C and E
CN109939068A (en) * 2019-05-06 2019-06-28 中国海洋大学 One kind having antioxidative nano-lipid emulsion and preparation method thereof

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