WO2022068173A1 - Inclusion de rétinol, son procédé de préparation et son utilisation - Google Patents

Inclusion de rétinol, son procédé de préparation et son utilisation Download PDF

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Publication number
WO2022068173A1
WO2022068173A1 PCT/CN2021/086675 CN2021086675W WO2022068173A1 WO 2022068173 A1 WO2022068173 A1 WO 2022068173A1 CN 2021086675 W CN2021086675 W CN 2021086675W WO 2022068173 A1 WO2022068173 A1 WO 2022068173A1
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WIPO (PCT)
Prior art keywords
retinol
thickener
polydimethylsiloxane
present disclosure
mixed oil
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PCT/CN2021/086675
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English (en)
Chinese (zh)
Inventor
钱进
向琼彪
李华真
李传茂
邓慧
张伟杰
曾伟丹
张楚标
Original Assignee
广州市科能化妆品科研有限公司
广东丹姿集团有限公司
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Priority to JP2022546684A priority Critical patent/JP2023513098A/ja
Publication of WO2022068173A1 publication Critical patent/WO2022068173A1/fr

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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
    • A61K8/67—Vitamins
    • A61K8/671—Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal
    • 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
    • A61K8/81—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
    • A61K8/8188—Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bonds, and at least one being terminated by a bond to sulfur or by a hertocyclic ring containing sulfur; Compositions of derivatives of such polymers
    • 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
    • A61K8/89—Polysiloxanes
    • A61K8/891—Polysiloxanes saturated, e.g. dimethicone, phenyl trimethicone, C24-C28 methicone or stearyl dimethicone
    • 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
    • A61K8/89—Polysiloxanes
    • A61K8/895—Polysiloxanes containing silicon bound to unsaturated aliphatic groups, e.g. vinyl dimethicone
    • 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

Definitions

  • the present disclosure relates to a retinol encapsulation, a preparation method and application thereof, and in particular to a retinol encapsulation, a preparation method and application thereof, and belongs to the field of cosmetics.
  • Retinoic acid (also known as: retinoic acid, retinoic acid) is a metabolic intermediate product of vitamin A in the body, and plays an important regulatory role in the process of human growth, development and cell differentiation. Retinoic acid can not only promote the synthesis of collagen, but also promote the formation of elastin fibers, which has a good anti-wrinkle effect. However, tretinoin is irritating to the skin, and symptoms such as redness and itching may occur after application. Compared with tretinoin, tretinoin (also known as: retinol) and tretinoin ester (also known as: retinol ester) are less irritating, and are usually used in cosmetics instead of tretinoin.
  • retinol or retinol ester When retinol or retinol ester penetrates into the skin, it will be gradually metabolized into retinoic acid under the oxidation of enzymes, and retinoic acid will play a role in promoting the renewal of epidermal cells. Through this metabolic process, retinoic acid is slowly released on the skin, which can not only avoid strong skin irritation, but also activate cell renewal.
  • the stability of retinol is poor, and it is easily decomposed when exposed to light and heat, especially under the action of ultraviolet rays, and it is more easily decomposed by catalytic decomposition; in addition, retinol is fat-soluble and has poor solubility in water. Therefore, the application of retinol in cosmetics has the disadvantages of instability and low utilization. How to make retinol stably exist in cosmetics and slowly release it on the skin is an important problem to be solved urgently in the current industry.
  • Citation 1 discloses a production method based on a pulsed electric field for an emulsion gel embedded with fat-soluble vitamins, which is to dissolve starch octenyl succinate in water, heat in a water bath, stir until it is completely gelatinized and dissolved, and cool to room temperature ; Add edible oil dissolved in fat-soluble vitamins to obtain a mixed solution; use a high-speed shearing machine and a high-pressure homogenizer to shear and homogenize the obtained mixed solution to obtain a coarse emulsion; add starch into the coarse emulsion, stir Evenly, an emulsion is obtained; the methylcellulose solution is added to the emulsion, and the mixture is uniformly mixed, and then treated with a pulsed electric field, heated in a water bath, degassed, and cooled to obtain an emulsion gel.
  • the fat-soluble vitamins are any one or more of retinol, beta-carotene, lycopene, lutein, tocopherol, sterols, and vitamin K.
  • the fat-soluble vitamin-embedding emulsion needs to be heated in a water bath at 80°C to 95°C, and retinol is not resistant to light and heat, and is easily damaged in the process.
  • Reference 2 discloses a method for preparing hydroxypropyl cyclodextrin inclusion retinol, comprising the following steps: (1) taking 1 part of retinol, adding 10-30 parts of purified water, and heating to 40-80° C. , stir for 0.5 to 2 hours to dissolve; (2) add 3 to 10 parts of hydroxypropyl cyclodextrin to the dissolved retinol solution, and stir at 40 to 80 ° C for 1 to 4 hours to fully encapsulate combined to obtain hydroxypropyl cyclodextrin inclusion retinol.
  • the retinol is encapsulated by hydroxypropyl cyclodextrin to form a slow-release and high-efficiency product.
  • it also needs to be heated at a temperature of 40-80° C. during the preparation process, which is easy to cause damage to the retinol. .
  • the present disclosure first provides a retinol encapsulation.
  • the retinol encapsulation of the present disclosure can form a stable encapsulation of the retinol compound, realize the sustained release of the retinol compound, and will not cause damage to the retinol compound.
  • the present disclosure also provides a method for preparing a retinol encapsulation, which does not require heating of the retinol compound during the preparation process, and will not cause damage to the retinol compound.
  • the present disclosure also provides the application of the retinol encapsulation in skin care products.
  • the retinol compound has a high utilization rate in skin care products, and can effectively remove wrinkles and resist aging.
  • the present disclosure provides a retinol encapsulation comprising the following components:
  • the thickener includes a first thickener, a second thickener and a third thickener;
  • the mass ratio of the retinol mixed oil and the first thickener is (2-4): 1;
  • the first thickener, second thickener and third thickener can be the same or different.
  • the mass ratio of the mixture of the retinol mixed oil and the first thickener, the second thickener and the third thickener is (1-1.4) : (0.05-0.08): (0.02-0.05).
  • a retinol-based wrap according to the present disclosure wherein the retinol-based mixed oil, the first thickener, the second thickener, and the third thickener form a blend that is combined with
  • the mass ratio of the polydimethylsiloxane is (1-2):1.
  • the retinol-based wrap according to the present disclosure, wherein the retinol-based mixed oil includes a retinol-based compound and a dimethicone; preferably, the retinol-based compound and the The mass ratio of the polydimethylsiloxane in the flavonoid mixed oil is (1-2): (1-2).
  • the retinol compound includes retinol and/or retinol ester.
  • the thickening agent comprises vinyl dimethicone/polymethicone silsesquioxane crosspolymer, polydimethylsiloxane One or a combination of two or more of oxane/vinyl polydimethylsiloxane cross-linked polymer and hydroxyethyl acrylate/sodium acryloyl dimethyl taurate copolymer.
  • the present disclosure also provides a method for preparing a retinol encapsulation, which includes the step of mixing each component of the retinol encapsulation.
  • the blend was dispersed in dimethicone to obtain a retinol-based wrap.
  • the present disclosure also provides an application of the retinol encapsulation according to the present disclosure in skin care products; preferably, the skin care products include lotions, creams, lotions, gels or essences.
  • the added amount of the retinol encapsulation is 1-5%.
  • the retinol encapsulation of the present disclosure can form a stable encapsulation for the retinol compound, realize the sustained release of the retinol compound, and will not cause damage to the retinol compound.
  • the preparation method of the retinol encapsulation of the present disclosure is simple and feasible, the raw materials are easy to obtain, the retinol compound does not need to be heated in the preparation process, the damage to the retinol compound will not be caused, and the retinol compound can be satisfied. demand for mass production.
  • the retinol encapsulation provided by the present disclosure can be applied in skin care products, improves the utilization rate of retinol compounds in skin care products, can effectively dilute fine lines, improve skin elasticity, and play an anti-aging role Effect.
  • references to “some specific/preferred embodiments”, “other specific/preferred embodiments”, “embodiments”, etc. refer to the specific elements described in relation to the embodiment (eg, features, structures, properties, and/or characteristics) are included in at least one embodiment described herein, and may or may not be present in other embodiments. Additionally, it should be understood that the described elements may be combined in any suitable manner in the various embodiments.
  • numerical range represented by "numerical value A to numerical value B” means a range including numerical values A and B at the endpoints.
  • the "water” includes deionized water, distilled water, ion-exchanged water, double-distilled water, high-purity water, purified water and any other feasible water that can be used in the cosmetic field.
  • the temperature when “normal temperature” and “room temperature” are used, the temperature may be 10-40°C.
  • a first aspect of the present disclosure provides a retinol encapsulation comprising the following components:
  • the thickener includes a first thickener, a second thickener and a third thickener;
  • the mass ratio of the retinol mixed oil and the first thickener is (2-4): 1;
  • the first thickener, second thickener and third thickener can be the same or different.
  • the thickener and the retinol mixed oil are used as the inner phase, and the polydimethylsiloxane encapsulates the thickener and the retinol mixed oil as the external phase, forming an opposite visual effect.
  • the layers of retinol compounds such as retinol and retinol ester are wrapped, so that the retinol compounds can exist stably in the package, with a sustained release effect, and will not cause retinol compounds. destroy.
  • the thickener in the retinol encapsulation can form stable adsorption to the retinol mixed oil and reduce the desorption of the retinol mixed oil. After the retinol wrap is applied to the skin surface, the wrap spreads layer by layer, so that the retinol compound is slowly released to the skin surface to exert anti-wrinkle and anti-aging effects.
  • Polydimethylsiloxane also known as dimethicone, has lubricating properties and anti-ultraviolet rays in cosmetics. It has good air permeability and obvious dust-proof function. Polydimethylsiloxane has very good permeability to the skin, which can increase the smooth and refreshing feeling of skin care products applied to the skin, and also has a good effect on increasing the softness of the skin.
  • the polydimethylsiloxane of the present disclosure can effectively stabilize the retinol compounds as an outer phase encapsulating the retinol-based mixed oil, the first thickener, the second thickener and the third thickener; After the alcohol coating is applied to skin care products, the outer layer of polydimethylsiloxane will wrap a layer of water phase, and finally form an easy-to-spread "oil-in-water" stable system.
  • the retinol-based mixed oil, the first thickener, the second thickener and the third thickener form a blend
  • the mass ratio of the blend to the polydimethylsiloxane is (1 -2): 1.
  • the mass ratio of the blend to the polydimethylsiloxane may be 1.1:1, 1.2:1, 1.3:1, 1.4:1, 1.5:1, 1.6:1, 1.7:1, 1.8:1 , 1.9:1, etc.
  • the mass ratio of the blend to the polydimethylsiloxane is (1-2): 1, the blend is fully dispersed in the polydimethylsiloxane, forming an effective effect on internal retinol compounds.
  • Package high system stability.
  • the polydimethylsiloxane is added in an amount of 35-55% based on the total mass of the retinol wrap, for example: 40%, 45% , 50%, etc.
  • the amount of polydimethylsiloxane added is 35-55%, the encapsulation can be better achieved.
  • the viscosity of the polydimethylsiloxane is 5-10 ⁇ .
  • the retinol-based oil blend of the present disclosure is formed by mixing a retinol-based compound and dimethicone.
  • Retinols are fat-soluble and can be dispersed in polydimethylsiloxane, helping to encapsulate the first layer of retinols.
  • using the same polydimethylsiloxane as the outermost layer as the oil component to mix the retinol mixture can also improve the compatibility and stability of the system.
  • the viscosity of the polydimethylsiloxane in the retinol-based mixed oil may also be 5-10 ⁇ .
  • the mass ratio of the retinol-based compound and the polydimethylsiloxane is (1-2):(1-2).
  • the mass ratio of the retinol compound and the polydimethylsiloxane is 1:1, 1:2, 2:1, etc.
  • the mass ratio of the retinol compound to the polydimethylsiloxane is (1-2):(1-2)
  • the retinol compound can be sufficiently dispersed in the polydimethylsiloxane.
  • the retinol compounds include retinol and/or retinol esters.
  • the retinol wrap is a retinol wrap formed by wrapping retinol.
  • the retinol is less irritating to the skin, and can be gradually metabolized into retinoic acid on the skin surface, thereby promoting activation and promoting Renew skin cells and improve skin elasticity to reduce fine lines, effectively remove wrinkles and anti-aging.
  • the retinol encapsulation can also be a retinol ester encapsulation formed by encapsulating retinol ester, or a mixture of encapsulating retinol and retinol ester. Compared with retinol, retinol esters have better stability, and can also be metabolized to retinoic acid to exert anti-wrinkle and anti-aging effects.
  • the retinyl esters of the present disclosure may be retinyl palmitate and/or retinyl propionate.
  • the added amount of the retinol mixed oil is 35-55%, for example: 40%, 45%, 50% etc.
  • the added amount of the retinol mixed oil is 35-55%, the effect of the retinol compound can be better exerted.
  • the thickening agent of the present disclosure includes a first thickening agent, a second thickening agent and a third thickening agent, and the first thickening agent, the second thickening agent and the third thickening agent can all use some commonly used thickening agents in the art Thickener, the three can be the same or different.
  • the first thickener, the second thickener and the third thickener By adding the first thickener, the second thickener and the third thickener, the effective adsorption of the retinol mixed oil can be formed, the viscosity of the inner phase can be increased, and the retinol compound in the retinol package can be reduced. desorption.
  • the mass ratio of the retinol-based mixed oil to the first thickener is (2-4):1.
  • the mass ratio of the retinol-based mixed oil to the first thickener may be 2.2:1, 2.5:1, 2.8:1, 3:1, 3.2:1, 3.5:1, 3.8:1 Wait.
  • the mass ratio of the retinol mixed oil and the first thickener is (2-4): 1, the first thickener can effectively adsorb the retinol mixed oil and reduce the amount of retinol in the retinol mixed oil. Retinols are desorbed.
  • the mass ratio of the mixture of the retinol mixed oil and the first thickener, the second thickener and the third thickener is (1-1.4): (0.05-0.08): (0.02- 0.05).
  • the mass ratio of the mixture of retinol mixed oil and the first thickener, the second thickener and the third thickener can be (1-1.4):(0.06-0.08):(0.02- 0.05), or (1-1.4):(0.05-0.07):(0.02-0.05), or 1:(0.06-0.08):(0.02-0.05), 1.4:(0.05-0.07):(0.02- 0.05) etc.
  • the mass ratio of the mixture of retinol mixed oil and the first thickener, the second thickener and the third thickener is (1-1.4):(0.05-0.08):(0.02-0.05)
  • It can fully encapsulate the retinol mixed oil, and is compatible with the polydimethylsiloxane of the outer phase, which is beneficial to obtain the encapsulation with stable system and high adsorption fastness of retinol compounds.
  • the thickeners include vinyl dimethicone/methicone silsesquioxane crosspolymer, dimethicone/vinyl dimethicone One or more combinations of siloxane cross-linked polymer and hydroxyethyl acrylate/sodium acryloyl dimethyl taurate copolymer.
  • the above-mentioned thickener component has good compatibility with other system components while adsorbing the retinol mixed oil.
  • the first thickener is vinyl dimethicone/methicone silsesquioxane crosspolymer
  • vinyl dimethicone/ Methylsiloxane Silsesquioxane Crosspolymer is a silicone powder that absorbs silicone oil, thickens and improves skin feel.
  • the second thickener is a dimethicone/vinyl dimethicone crosspolymer
  • the dimethicone/vinyl dimethicone crosspolymer is A type of silicophilic thickener that can form effective adsorption to retinol-based mixed oils.
  • the third thickener is hydroxyethyl acrylate/sodium acryloyl dimethyl taurate copolymer.
  • Hydroxyethyl acrylate/sodium acryloyl dimethyl taurate copolymer has an emulsifying effect and can improve retinol encapsulation. system stability.
  • the first thickener is added in an amount of 8-16% based on the total mass of the retinol-based package, for example: 10%, 12%, 14% %, etc.; the addition amount of the second thickener is 1-5%, for example: 2%, 3%, 4%, etc.; the addition amount of the third thickener is 0.1-2%, for example: 0.5 %, 1%, 1.5%, etc.
  • the contents of the first thickening agent, the second thickening agent and the third thickening agent are within the above ranges, the performance of the obtained retinol-based encapsulation is more excellent.
  • a thickening agent, a retinol mixed oil and polydimethylsiloxane are mixed to form a polydimethylsiloxane encapsulating the thickening agent, and the thickening agent is then encapsulated.
  • the layer-by-layer packaging of the retinol mixed oil makes the retinol compounds stably exist in the retinol package and can be slowly released on the skin surface.
  • a second aspect of the present disclosure provides a method for preparing a retinol encapsulation according to the first aspect, comprising the step of mixing each component of the retinol encapsulation.
  • the preparation method of the retinol encapsulation comprises the step of mixing each component of the retinol encapsulation at room temperature.
  • the preparation method of retinol encapsulation comprises the following steps:
  • the blend was dispersed in dimethicone to obtain a retinol-based wrap.
  • Mixing the retinol-based mixed oil with the first thickener refers to mixing the retinol-based mixed oil with the first thickener of the powder, and stirring until the first thickener of the powder changes the amount of the oil into the first thickener.
  • the retinol-based mixed oil is sucked dry to obtain a mixture of the retinol-based mixed oil and the first thickener.
  • the retinol-based mixed oil may be a retinol-based mixed oil obtained by mixing a retinol-based compound and dimethicone.
  • the blend it is a blend formed by encapsulating the retinol-based mixed oil with the powders of the first thickening agent, the second thickening agent and the third thickening agent.
  • dispersing the blend in polydimethylsiloxane means dispersing the blend in polydimethylsiloxane with a viscosity of 5-10 ⁇ , so that the outer side of the blend is finally coated with a
  • the polydimethylsiloxane of the oil phase was layered to obtain a retinol-based encapsulation in which the powder was encapsulated in the oil-phase and then the retinol-based mixed oil was encapsulated.
  • the above-mentioned mixing step and dispersion step are all carried out at room temperature, and the mixture of the retinol mixed oil and the first thickener, the second thickener and the third thickener are uniformly dispersed at the end. in polydimethylsiloxane.
  • the preparation method of the retinol compound of the present disclosure does not require heat treatment in the process of encapsulating the retinol compound, and can be carried out at room temperature without causing damage to the activity of the retinol compound, and the preparation method It is simple and easy to implement, the raw materials are easy to obtain, and it is suitable for large-scale industrial preparation.
  • a third aspect of the present disclosure provides an application of the retinol wrap described in the first aspect in a skin care product; preferably, the skin care product includes a lotion, cream, lotion, gel or essence.
  • retinol encapsulation of the present disclosure After the retinol encapsulation of the present disclosure is added to a skin care product, a layer of water phase encapsulation will be formed on the outer side of the polydimethylsiloxane, and finally a stable "oil-in-water” system is obtained, making the skin care product It has anti-aging and wrinkle-removing effects, and the active ingredient retinol compound has stable performance and long acting time.
  • the added amount of the retinol encapsulation is 1-5%, preferably 1.4-4%.
  • the retinol wrap can be added in an amount of 1.5%, 1.7%, 1.9%, 2.0%, 2.2%, 2.4%, 2.6%, 3%, 3.5%, 4.5%, and the like.
  • the added amount of the retinol wrapping is 1-5%, the effect of wrinkle removal and anti-aging can be produced, and the stimulation to human skin can be avoided, so that the product is mild and safe.
  • the present disclosure provides an anti-wrinkle cream comprising the retinol wrap according to the first aspect of the present disclosure.
  • the retinol wraps spread out layer by layer, releasing the innermost retinol compounds to promote the renewal of epidermal cells and reduce the appearance of fine lines.
  • the retinol encapsulation added in the anti-wrinkle cream has the effect of high stability and slow release, which can maximize the anti-wrinkle and anti-aging effects of the retinol compound.
  • the amount of the retinol wrap is 1-5%, preferably 1.4-2.8%.
  • the retinol wrap can be added in an amount of 1.5%, 1.7%, 1.9%, 2.0%, 2.2%, 2.4%, 2.6%, 2.8%, and the like.
  • retinol-based wraps include one or both of retinol wraps and retinol ester wraps. Both retinol wraps and retinol ester wraps have high stability, sustained release, and anti-aging and wrinkle-removing effects.
  • the anti-wrinkle cream of the present disclosure simultaneously adds a retinol wrap and a retinol ester wrap, wherein, based on the total mass of the anti-wrinkle cream, the added amount of the retinol wrap It is 0.5-1.5%, preferably 0.7-1.4%, and the added amount of the retinol ester wrap is 0.5-1.5%, preferably 0.7-1.4%.
  • the retinol ester wrap is a retinyl palmitate wrap and/or a retinyl propionate wrap.
  • the anti-wrinkle cream further includes one or a combination of two or more of moisturizing agents, emulsifiers, oils, thickeners, solvents, skin conditioning agents and preservatives.
  • the formula composition of the wrinkle-removing face cream of the present disclosure is mild, and the efficacy of the retinol wrapping of the present disclosure can be fully exerted.
  • adding a moisturizing agent can have the effect of moisturizing and replenishing water.
  • the added amount of the moisturizing agent of the present disclosure can be 1-10%, preferably 2-6%.
  • the humectant of the present disclosure is propylene glycol.
  • the system stability of the anti-wrinkle cream can be increased by adding an emulsifier, specifically, based on the total mass of the anti-wrinkle cream, the added amount of the emulsifier is 0.5-2%, preferably 0.6-1.2%.
  • the emulsifier includes PEG-20 methyl glucose sesquistearate, methyl glucose sesquistearate, sorbitan isostearate, polyglycerol-3 methyl glucose distearate One or a combination of two or more of acid esters, laureth-7 and isostearyl ether-20.
  • PEG-20 methyl sesquiglucostearate and methyl sesquiglucostearate are added to the wrinkle-removing cream at the same time; wherein, the total mass of the wrinkle-removing cream is In total, the addition amount of PEG-20 methyl sesquiglucostearate is 0.3-1.2%, and the addition amount of methyl sesquiglucostearate is 0.2-0.8%.
  • the wrinkle-removing face cream of the present disclosure further includes oil, and by adding oil to the wrinkle-removing face cream, the evaporation of moisture on the skin surface can be reduced, and the skin can be prevented from dry and cracked.
  • oil by adding oils and fats, a hydrophobic film can be formed on the skin surface, preventing the intrusion of external harmful substances.
  • the amount of oil added is 1-20%, preferably 3-15%.
  • oils and fats include one or a combination of two or more of behenyl alcohol, isononyl isononanoate, dimethiconol and polydimethylsiloxane.
  • behenyl alcohol, isononyl isononanoate, dimethiconol and dimethicone are simultaneously added to the anti-wrinkle cream.
  • the addition of behenyl alcohol is 0.5-2%, preferably 0.5-1.5%
  • the addition of isononyl isononanoate is 1-5%, preferably 1.5-2.5% %
  • the addition amount of dimethiconol is 0.5-5%, preferably 1-3%
  • the addition amount of polydimethylsiloxane is 0.5-5%, preferably 1-3%.
  • the added amount of the thickener in the anti-wrinkle cream of the present disclosure is 0.05-6%, preferably 0.7-2.5%.
  • the thickener of the present disclosure includes polydimethylsiloxane/vinyl dimethicone crosspolymer, ammonium acryloyldimethyltaurate/VP copolymer, xanthan gum, One or a combination of two or more of acrylic acid (ester)/C 10-30 alkanol acrylate cross-linked polymer and hydroxyethyl acrylate/sodium acryloyl dimethyl taurate copolymer.
  • polydimethylsiloxane/vinyl polydimethylsiloxane cross-linked polymer, ammonium acryloyldimethyltaurate/VP copolymer are added to the anti-wrinkle cream at the same time
  • acrylic (ester)/C 10-30 alkanol acrylate cross-linked polymer wherein, based on the total mass of the anti-wrinkle cream, polydimethylsiloxane/vinyl polydimethylsiloxane cross-linked
  • the addition amount of the polymer is 0.05-2%, preferably 0.5-1.5%; the addition amount of the ammonium acryloyldimethyltaurate/VP copolymer is 0.01-2%, preferably 0.1-0.5%; acrylic acid (ester) )/C 10-30 alkanol acrylate cross-linked polymer is added in an amount of 0.01-2%, preferably 0.1-0.5%.
  • the generation of wrinkles can be reduced by adding skin conditioning agents to anti-wrinkle creams.
  • the active ingredients in skin conditioners can penetrate deep into the skin and be absorbed by the skin, thereby improving the condition of the skin.
  • the addition amount of the skin conditioning agent is 1.05-6%, preferably 1.4-4%.
  • the skin conditioning agent includes one or both of D-panthenol and niacinamide.
  • D-panthenol after D-panthenol is absorbed by the skin, it can increase the content of hyaluronic acid in the skin, give the skin luster and moisturizing effect, and can stimulate cell division and regeneration and tissue repair.
  • the added amount of D-panthenol in the anti-wrinkle cream is 0.05-2%, preferably 0.8-1.2%.
  • Niacinamide can maintain the level of ceramides and free fatty acids in the skin, maintain the moisture content of the skin, and enhance the microcirculation of the dermis.
  • the added amount of niacinamide in the anti-wrinkle cream is 1-4%, preferably 1.5-2.5%.
  • a certain amount of preservative can also be added to the anti-wrinkle cream, specifically, based on the total mass of the anti-wrinkle cream, the added amount of the anti-corrosion cream is 0.5-2%, preferably 0.6-1%.
  • the preservatives include one or a combination of two or more of methylparaben, ethylparaben, phenoxyethanol and ethylhexylglycerol.
  • each component of the anti-wrinkle cream can be fully dissolved, and the anti-wrinkle effect can be synergistically exerted.
  • the added amount of the solvent is such that the mass of the solvent and the rest of the components reach 100%.
  • water can be selected as the solvent.
  • the wrinkle-removing cream provided by the present disclosure has mild components and can synergistically synergize; the retinol encapsulation can exist stably, and the wrinkle-removing cream slowly releases the retinol compounds on the surface of the skin after smearing on the hair, so as to play an anti-wrinkle effect. Wrinkle and anti-aging effect.
  • the present disclosure also provides the preparation method of the anti-wrinkle cream according to the third aspect, including the step of mixing the components of the anti-wrinkle cream.
  • the preparation method of anti-wrinkle cream includes the following steps:
  • phase B Mix the emulsifier, grease and remaining thickener as phase B, heat phase B to 80-90°C, and keep stirring to mix phase B evenly;
  • phase B additive phase B into phase A at a temperature of 80-90 °C, and mix them evenly;
  • phase C Use the remaining preservatives and retinol wraps as phase C, when the temperature of the system drops below 40°C, add phase C, homogenize and then discharge.
  • an emulsion comprising the retinol wrap according to the first aspect of the present disclosure.
  • the retinol encapsulation added in the emulsion of the present disclosure has the effects of high stability and sustained release, and can maximize the wrinkle-removing and anti-aging effects of the retinol compound.
  • the added amount of the retinol encapsulation is 1-5%, preferably 2-4%.
  • the retinol wrap may be added in an amount of 1.5%, 1.7%, 1.9%, 2.0%, 2.2%, 2.4%, 2.6%, 2.8%, 3%, 3.5%, 4.5%, and the like.
  • the emulsion further includes one or a combination of two or more of humectants, emulsifiers, thickeners, solvents and preservatives.
  • the formulation composition of the emulsion of the present disclosure is mild, and the efficacy of the retinol encapsulation of the present disclosure can be fully exerted.
  • adding a moisturizing agent can have the effect of moisturizing and replenishing water.
  • the added amount of the moisturizing agent of the present disclosure may be 1-10%, preferably 2-6%.
  • the humectant of the present disclosure is propylene glycol.
  • the system stability of the emulsion can be increased by adding an emulsifier, specifically, based on the total mass of the emulsion, the added amount of the emulsifier is 0.1-2%, preferably 0.3-1.2%.
  • the emulsifier includes PEG-20 methyl glucose sesquistearate, methyl glucose sesquistearate, sorbitan isostearate, polyglycerol-3 methyl glucose distearate One or a combination of two or more of acid esters, laureth-7 and isostearyl ether-20.
  • PEG-20 methyl sesquiglucostearate and methyl sesquiglucostearate are simultaneously added to the emulsion; wherein, based on the total mass of the emulsion, PEG- The addition amount of 20 methyl sesquiglucostearate is 0.05-1.2%, and the addition amount of methyl sesquiglucostearate is 0.05-0.8%.
  • the added amount of the thickener in the emulsion of the present disclosure is 0.05-2%, preferably 0.1-0.8%.
  • the thickener of the present disclosure includes polydimethylsiloxane/vinyl dimethicone crosspolymer, ammonium acryloyldimethyltaurate/VP copolymer, xanthan gum, One or more combinations of acrylic acid (ester)/C 10-30 alkanol acrylate cross-linked polymer, hydroxyethyl acrylate/sodium acryloyl dimethyl taurate copolymer, preferably xanthogen glue.
  • a certain amount of preservative may also be added to the emulsion, specifically, based on the total mass of the emulsion, the added amount of the preservative is 0.5-2%, preferably 0.6-1%.
  • the preservatives include one or a combination of two or more of methylparaben, ethylparaben, phenoxyethanol and ethylhexylglycerol.
  • the present disclosure also provides the preparation method of the emulsion according to the third aspect, including the step of mixing each component of the emulsion.
  • the preparation method of the emulsion comprises the following steps:
  • phase A Mix the moisturizing agent, thickening agent, emulsifier, some preservatives and solvent as phase A, heat phase A to 80-90°C, keep stirring and homogenizing to make phase A evenly mixed;
  • phase B Mix the remaining preservatives and retinol encapsulations as phase B, when the temperature of the system drops below 40°C, add phase B, homogenize and then discharge.
  • Example 1-3 According to the component contents provided in Table 1, three groups of retinol encapsulations in Example 1-3 were prepared, and the preparation method of each group of retinol encapsulations specifically included the following steps:
  • retinol or retinyl palmitate and polydimethylsiloxane with a viscosity of 6 ⁇ are mixed in a mass ratio of 1:1 to obtain a retinol mixed oil.
  • retinol palmitate in embodiment 1 add retinol in embodiment 2, add the mixture of retinol and retinol palmitate in embodiment 3, wherein retinol and retinol palmitate
  • the mass ratio of the acid ester is 1:1.
  • step (2) Mix the retinol-based mixed oil obtained in step (1) with the vinyl polydimethylsiloxane/polymethylsiloxane silsesquioxane cross-linked polymer to form a powder to absorb the oil Dry.
  • step (3) mix the mixture obtained in step (3) with polydimethylsiloxane/vinyl polydimethylsiloxane cross-linked polymer, hydroxyethyl acrylate/sodium acryloyldimethyltaurate copolymer Mixing at room temperature, and then dispersing in polydimethylsiloxane with a viscosity of 6 ⁇ , the retinol encapsulation can be prepared.
  • retinyl palmitate was added in comparative example 1
  • retinyl palmitate was added in comparative example 2
  • retinol mixed oil retinyl palmitate and polydimethylsiloxane were added.
  • the mass ratio is 1:1.
  • Example 1 The retinol encapsulation and retinyl palmitate prepared in Example 1 and Comparative Examples 1-2 were selected as the components of Phase B, and the emulsion was prepared according to the following steps:
  • the retinol wraps prepared in Examples 1-2 were selected as the C-phase components, and the wrinkle-removing creams in Application Examples 1-3 were respectively prepared, wherein the retinol wraps prepared in Examples 1-2 were respectively Corresponding to the wrinkle-removing cream of application examples 1-3, that is, the retinol ester wrap of Example 2 and the retinol wrap of Example 1 were respectively used in the wrinkle-removal cream of Example 1-2, and the application was implemented.
  • the combination of the retinol wrap of Example 1 and the retinol ester wrap of Example 2 was used in the wrinkle-removing facial cream of Example 3;
  • the preparation method includes the following steps:
  • phase B additive phase B into phase A at 85°C, and mix them evenly;
  • the samples a-d in the evaluation of the wrapping effect were selected as the samples to be tested.
  • the samples to be tested were divided into four groups, each group of two 50g transparent PET bottles, in each group, one of them was placed under natural light for 7 days, and the other was refrigerated in the dark. Seven days later, at the same time and under the same conditions, the two batches of samples to be tested were respectively analyzed by high performance liquid chromatography to quantitatively analyze the retinyl palmitate in the samples, and the residual active ingredients were calculated.
  • Table 6 The results are shown in Table 6:
  • the wrinkle-removing cream prepared by Application Example 1-3 has a better effect than the wrinkle-removing cream prepared by Application Example 1-3.
  • the actives are all retinol encapsulated, which retains the activity better than the unencapsulated actives.
  • the effect of the wrinkle-removing cream prepared in application example 1 and application example 3 is equivalent, and the effect of application of comparative example 1 is better than that of application of comparative example 3, which may be due to the fact that retinyl palmitate In the case of retinol, complete breakdown is slower.
  • the retinol encapsulation provided by the present disclosure and the preparation method and application thereof can be applied in industry.

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Abstract

La présente invention concerne le domaine des cosmétiques et concerne une inclusion de rétinol, son procédé de préparation et son utilisation. L'invention concerne une inclusion de rétinol, qui comporte les constituants suivants : une huile de rétinol mélangée ; un agent épaississant ; du polydiméthylsiloxane. L'agent épaississant comprend un premier agent épaississant, un deuxième agent épaississant et un troisième agent épaississant. Le rapport en masse de l'huile de rétinol mélangée au premier agent épaississant est (2-4):1, et le premier agent épaississant, le deuxième agent épaississant et le troisième agent épaississant peuvent être identiques ou différents les uns des autres. L'inclusion de rétinol peut former une inclusion stable pour un composé de rétinol, de sorte qu'une libération prolongée du composé de rétinol est obtenue sans endommager le composé de rétinol. En outre, l'inclusion de rétinol est appliquée dans le produit de soin de la peau, de sorte que le taux d'utilisation du composé de rétinol dans le produit de soin de la peau peut être amélioré, et le produit de soin de la peau parvient à donner l'effet d'élimination efficace des rides et de ralentissement du vieillissement.
PCT/CN2021/086675 2020-09-30 2021-04-12 Inclusion de rétinol, son procédé de préparation et son utilisation WO2022068173A1 (fr)

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