CN110384620A - Symwhite-337 microneedle patch and preparation method thereof - Google Patents

Symwhite-337 microneedle patch and preparation method thereof Download PDF

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Publication number
CN110384620A
CN110384620A CN201910749950.7A CN201910749950A CN110384620A CN 110384620 A CN110384620 A CN 110384620A CN 201910749950 A CN201910749950 A CN 201910749950A CN 110384620 A CN110384620 A CN 110384620A
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CN
China
Prior art keywords
micropin
symwhite
master mold
needle body
microneedle patch
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
Application number
CN201910749950.7A
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Chinese (zh)
Inventor
赵科研
杨淑艳
郭文平
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Wuxi Yuanxu Biotechnology Co Ltd
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Wuxi Yuanxu Biotechnology Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Wuxi Yuanxu Biotechnology Co Ltd filed Critical Wuxi Yuanxu Biotechnology Co Ltd
Priority to CN201910749950.7A priority Critical patent/CN110384620A/en
Publication of CN110384620A publication Critical patent/CN110384620A/en
Pending legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/0204Specific forms not provided for by any of groups A61K8/0208 - A61K8/14
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/347Phenols
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73Polysaccharides
    • A61K8/735Mucopolysaccharides, e.g. hyaluronic acid; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/02Preparations for care of the skin for chemically bleaching or whitening the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/74Biological properties of particular ingredients
    • A61K2800/78Enzyme modulators, e.g. Enzyme agonists
    • A61K2800/782Enzyme inhibitors; Enzyme antagonists
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/80Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
    • A61K2800/91Injection

Abstract

The invention belongs to field of micro-manufacture, more particularly to Symwhite-337 microneedle patch, including needle body and micropin substrate, needle body is evenly distributed on micropin substrate, the Sodium Hyaluronate that the weight percentage that needle body includes is 0.05-1.0% Symwhite-337 and weight percentage is 10-50%.The present invention also provides the preparation methods of above-mentioned Symwhite-337 microneedle patch, Symwhite-337 microneedle patch provided by the invention uses Symwhite-337, pass through micropin technology, Symwhite-337 can be directly injected into flesh bottom, to increase skin to the absorption efficiency of Symwhite-337, double whitening effect.In addition, preparation method provided by the invention, preparation condition requires to readily satisfy, and production scale is easily realized.

Description

Symwhite-337 microneedle patch and preparation method thereof
Technical field
The invention belongs to field of micro-manufacture more particularly to Symwhite-337 microneedle patch and preparation method thereof.
Background technique
With the development of society and the continuous improvement of living standards of the people, requirement of the consumer to daily nursing product is also more next It is higher, it requires the effect of to product also increasingly to refine.Melanin is a kind of protein for being present in everyone skin base layer, Ultraviolet irradiation can enable melanin generate variation, produce a kind of substance for protecting skin, then melanin is again via cell generation That thanks moves layer by layer, has arrived skin epidermis, forms color spot and the unequal skin problem of the colour of skin that we are seen now.
Symwhite-337 is a kind of safe and effective, nonirritant whitening composition, inhibits the ability of TYR enzyme It is 22 times of kojic acid, the ability of inhibition B16V synthetic melanin is 210 times of kojic acid, and whitening effect is the 7000 of arbutin Times, Symwhite-337 can improve colour of skin unevenness, reduce pigmenting of skin caused by ultraviolet light irradiation skin, and have outstanding Inoxidizability and wrinkling resistance.
Most of existing whitening and freckle-removing product only rests on skin surface to the maintenance of skin, can not go deep into flesh bottom, reach To the effect of whitening spot-removing from inside to outside.
Summary of the invention
In order to solve deficiency in the prior art, the present invention provides Symwhite-337 microneedle patch, it is therefore an objective to be Flesh bottom can not quickly be goed deep by solving whitening and freckle-removing product in the prior art, and Symwhite-337 is caused to absorb and utilization efficiency Low technical problem, and the present invention also provides the preparation methods of above-mentioned Symwhite-337 microneedle patch.
Symwhite-337 microneedle patch provided by the invention, specific technical solution are as follows:
Symwhite-337 microneedle patch, including needle body and micropin substrate, the needle body are evenly distributed on the micropin On substrate, the weight percentage that the needle body includes is 0.05-1.0% Symwhite-337 and weight percentage is 10-50% Sodium Hyaluronate.
The preparation method of Symwhite-337 microneedle patch is used to prepare above-mentioned Symwhite-337 microneedle patch Method, which comprises the steps of:
S1 obtains micropin master mold by injection molding, drying and demoulding as mold using silicon micropin, and the micropin master mold is Dimethyl silicone polymer master mold or polytetrafluoroethylene (PTFE) master mold, and the micropin master mold is equipped with pin hole;
Needle body containing Symwhite-337 is made liquid, tiled onto the micropin master mold in step S1, closed by S2 In space, adjustment air pressure is 0.1-5 atmospheric pressure, and retention time 5-10s recycles three times, makes the needle on the micropin master mold Body makes liquid full of needle body, obtains fluid injection micropin master mold;
Fluid injection micropin master mold in step S2 is put into baking wind drying box and is dried by S3, obtains dry micropin master mold;
Backing production liquid containing Sodium Hyaluronate is tiled to the drying micropin master mold in step S3, and is done by S4 It is dry, obtain molding microneedle patch;
S5 removes the molding microneedle patch in step S4 from the micropin master mold, and it is micro- to obtain Symwhite-337 Needle patch.
In some embodiments, in step S2, the needle body production liquid includes that needle point makes liquid and needle body solution, described It is the aqueous solution containing 5% Symwhite-337 that needle point, which makes liquid, and the needle body solution is PVP-K30 and grape sugar weight hundred Divide and mixed than 1:1, is re-dubbed the aqueous solution of 40% concentration;
In step S4, backing production liquid be the Sodium Hyaluronate of 1,000,000-200 ten thousand molecular weight be made into 10% it is water-soluble Liquid.
In some embodiments, include the following steps: in step S2
S21 tiles needle point production liquid onto the micropin master mold in step S1, in confined space, by air pressure tune Whole to 0.1 atmospheric pressure, retention time 10s, circulation three times, enter needle point production liquid in pin hole;
The micropin master mold containing needle point production liquid in step S21 is put in and dries drying in wind drying box by S22, described dry Dry temperature is 50 DEG C, obtains needle point forming micropin master mold;
The needle body solution is taped against on the needle point forming micropin master mold in step S22, in confined space, by gas by S23 Pressure is adjusted to 5 atmospheric pressure, retention time 10s, and circulation three times, makes the needle body on the micropin master mold be full of needle body solution, Obtain fluid injection micropin master mold.
In some embodiments, in step S2, the needle body production liquid is Symwhite-337, molecular weight 8000 Sodium Hyaluronate, divinylsulfone, water according to weight percent 1:1:0.01:100 ratio mix;
In step S4, the backing production liquid is the Sodium Hyaluronate and phenethyl isophthalic two of 1,000,000-200 ten thousand molecular weight 10:1 is mixed phenol in proportion, is re-dubbed 30% aqueous solution.
In some embodiments, in step S2, the needle body solution is taped against on the micropin master mold in step S1, close It closes in space, air pressure is adjusted to 5 atmospheric pressure, retention time 10s, circulation three times, makes the needle body on the micropin master mold Liquid is made full of the needle body, obtains fluid injection micropin master mold.
In some embodiments, in step S4, the temperature condition of the drying is room temperature.
The invention has the following advantages: Symwhite-337 microneedle patch provided by the invention is using between phenethyl Benzenediol, it is highly-safe, without potential irritation and sensibility, be the highest TYR enzyme inhibitor of activity that has been reported that it One, it can effectively inhibit the activity of B16V synthetic melanin, whitening effect is good;It, can will be between phenethyl by micropin technology Benzenediol is directly injected into flesh bottom, to increase skin to the absorption efficiency of Symwhite-337, doubles whitening effect. Furthermore preparation method provided by the invention, preparation condition requires to readily satisfy, and production scale is easily realized.
Detailed description of the invention
Fig. 1 is the step flow chart of Symwhite-337 microneedle patch preparation method provided by the invention;
Fig. 2 is Symwhite-337 microneedle patch micro-structure diagram provided by the invention.
Specific embodiment
To make the objectives, technical solutions, and advantages of the present invention clearer, below in conjunction with specific embodiment, and reference Attached drawing 1-2, the present invention is described in more detail.
Symwhite-337 microneedle patch provided by the invention, specific technical solution are as follows:
Symwhite-337 microneedle patch, including needle body and micropin substrate, the needle body are evenly distributed on the micropin On substrate, the weight percentage that the needle body includes is 0.05-1.0% Symwhite-337 and weight percentage is The Sodium Hyaluronate of 10-50%.
Symwhite-337 microneedle patch provided by the invention be divided into Instant Symwhite-337 microneedle patch and The Symwhite-337 microneedle patch of slow-release.
Embodiment 1
The Symwhite-337 microneedle patch of Instant the preparation method is as follows:
Include the following steps:
S1 obtains micropin master mold by injection molding, drying and demoulding as mold using silicon micropin, and micropin master mold is poly- two Methylsiloxane master mold, and micropin master mold is equipped with pin hole;
Needle point is made liquid (it is the aqueous solution containing 5% Symwhite-337 that needle point, which makes liquid) tiling and arrives step by S21 On micropin master mold in S1, in confined space, air pressure is adjusted to 0.1 atmospheric pressure, retention time 10s, is recycled three times, Enter needle point production liquid in pin hole;
The micropin master mold containing needle point production liquid in step S21 is put in and dries drying in wind drying box by S22, dry Temperature is 50 DEG C, obtains needle point forming micropin master mold;
S23, by needle body solution, (needle body solution is that PVP-K30 and glucose weight percent 1:1 is mixed, and is re-dubbed 40% The aqueous solution of concentration) it is taped against on the needle point forming micropin master mold in step S22, in confined space, air pressure is adjusted to 5 big Air pressure, retention time 10s, circulation three times, make the needle body on micropin master mold full of needle body solution, obtain fluid injection micropin master mold.
Fluid injection micropin master mold in step S23 is put into baking wind drying box and is dried by S3, obtains dry micropin master mold;
S4, backing is made liquid, and (backing production liquid is that the Sodium Hyaluronate of 1,000,000-200 ten thousand molecular weight is made into 10% water Solution) it tiles to the drying micropin master mold in step S3, and be dried at room temperature, obtain molding microneedle patch;
S5 removes the molding microneedle patch in step S4 from micropin master mold, obtains Symwhite-337 microneedle patch Piece.
Benzene second is contained in the Symwhite-337 microneedle patch of the Instant prepared in the present embodiment, the part of only needle point Base resorcinol, this microneedle patch needle body and needle point material are the PVP-K30 that can be dissolved rapidly in water and glucose is constituted, thorn Enter to touch human body cell interstitial fluid quick release after skin and go out Symwhite-337.
Embodiment 2
The Symwhite-337 microneedle patch of slow-release the preparation method is as follows:
Include the following steps:
S1 obtains micropin master mold by injection molding, drying and demoulding as mold using silicon micropin, and micropin master mold is poly- four Vinyl fluoride master mold, and micropin master mold is equipped with pin hole;
S2, by needle body solution (needle body make liquid be Symwhite-337, the Sodium Hyaluronate that molecular weight is 8000, two Vinyl sulfone, water are mixed according to the ratio of weight percent 1:1:0.01:100) it is taped against on the micropin master mold in step S1, close It closes in space, air pressure is adjusted to 5 atmospheric pressure, retention time 5s, circulation three times, makes the needle body on micropin master mold full of needle System makees liquid, obtains fluid injection micropin master mold.
Fluid injection micropin master mold in step S2 is put into baking wind drying box and is dried by S3, obtains dry micropin master mold;
S4, backing is made liquid, and (backing makes the Sodium Hyaluronate and phenethyl isophthalic that liquid is 1,000,000-200 ten thousand molecular weight Diphenol 10:1 by weight percentage mixing, is re-dubbed 30% aqueous solution) it tiles to the drying micropin master mold in step S3, and It is dried under room temperature, obtains molding microneedle patch;
S5 removes the molding microneedle patch in step S4 from micropin master mold, obtains Symwhite-337 microneedle patch Piece.
The Symwhite-337 microneedle patch of the slow-release prepared in the present embodiment, needle body and lining contain benzene second Base resorcinol, this microneedle patch needle body and needle point material are that the Sodium Hyaluronate after being chemically crosslinked is constituted, and are being pierced into skin Cross-linking hyaluronic acid sodium is only swollen insoluble when touching human body cell interstitial fluid, and it is logical to be wrapped in Symwhite-337 therein Cross the gap slow release of cross-linking hyaluronic acid sodium swelling.
Assessment to the whitening spot-removing function of Symwhite-337 microneedle patch provided by the invention
Experimental subjects: choose 150 female volunteers, be randomly divided into 3 groups, every group of 50 volunteers: one group is contrast groups (the whitening for the Sodium Hyaluronate that containing weight percentage be 1.0% Symwhite-337 and weight percentage is 50% Solution), remaining two groups are embodiment group (using the microneedle patch of Examples 1 and 2 respectively).
Experimental method: before volunteer gos out after face's cleaning, whitening solution is smeared, or using embodiment 1 and implement Symwhite-337 microneedle patch in example 2 is carried out continuously 2 weeks.After experiment, subject is asked to make phenethyl isophthalic two Evaluation of the phenol microneedle patch to skin effects, experimental result are shown in Table 1.
Evaluation criterion: A, have the effect of significantly improving skin lightening degree, color spot obviously subtracts light or subsides up to 90% or more The facial melanin of degeneration, it is effective;B, 50% or more color spot recession, effectively;C, substantially unchanged before and after use, in vain.
Table 1
Using Symwhite-337 microneedle patch provided by the invention (2 groups of example 1 group and embodiment) 100 will In hope person, effective 47, effective 50, invalid 3;Obvious effective rate 47%, effective percentage 50%, inefficiency 3%, total effective rate 97%.In use, micropin is pierced into successfully, and all volunteers do not occur sense of discomfort, and it is existing that skin does not occur allergy As.Compared with existing freckle removing and whitening solution, Symwhite-337 microneedle patch of the invention improves in terms of whitening spot-removing to be had The absorptivity of ingredient is imitated, to have more significant effect, and mildly non-stimulated to skin, and can from analysis of experimental data The Symwhite-337 microneedle patch of slow-release is to despeckle better effect out, this is because it can be long lasting for administration, more Conducive to color spot removal.
Above-mentioned preferable possible embodiments only of the invention, are not limitations of the present invention, the present invention is also not limited to above-mentioned Citing, those skilled in the art, within the essential scope of the present invention, made variations, modifications, additions or substitutions, Also it should belong to protection scope of the present invention.

Claims (7)

1. Symwhite-337 microneedle patch, which is characterized in that including needle body and micropin substrate, the needle body is evenly distributed on On the micropin substrate, the weight percentage that the needle body includes is 0.05-1.0% Symwhite-337 and weight percent Content is 10-50% Sodium Hyaluronate.
2. the preparation method of Symwhite-337 microneedle patch is used to prepare Symwhite-337 described in claim 1 The method of microneedle patch, which comprises the steps of:
S1 obtains micropin master mold by injection molding, drying and demoulding as mold using silicon micropin, and the micropin master mold is poly- two Methylsiloxane master mold or polytetrafluoroethylene (PTFE) master mold, and the micropin master mold is equipped with pin hole;
Needle body containing Symwhite-337 is made liquid, tiled onto the micropin master mold in step S1, in confined space by S2 Interior, adjustment air pressure is 0.1-5 atmospheric pressure, and retention time 5-10s recycles three times, fills the needle body on the micropin master mold Full needle body makes liquid, obtains fluid injection micropin master mold;
Fluid injection micropin master mold in step S2 is put into baking wind drying box and is dried by S3, obtains dry micropin master mold;
Backing production liquid containing Sodium Hyaluronate is tiled to the drying micropin master mold in step S3, and is dried by S4, is obtained Microneedle patch must be formed;
S5 removes the molding microneedle patch in step S4 from the micropin master mold, obtains Symwhite-337 microneedle patch Piece.
3. the preparation method of Symwhite-337 microneedle patch according to claim 2, which is characterized in that step S2 In, the needle body production liquid includes needle point production liquid and needle body solution, and the needle point production liquid is to contain 5% phenethyl isophthalic two The aqueous solution of phenol, the needle body solution are that PVP-K30 and glucose weight percent 1:1 is mixed, and are re-dubbed the water of 40% concentration Solution;
In step S4, the backing production liquid is that the Sodium Hyaluronate of 1,000,000-200 ten thousand molecular weight is made into 10% aqueous solution.
4. the preparation method of Symwhite-337 microneedle patch according to claim 3, which is characterized in that in step S2 Include the following steps:
S21, by needle point production liquid tiling on the micropin master mold in step S1, in confined space, by air pressure adjust to 0.1 atmospheric pressure, retention time 10s, circulation three times, enter needle point production liquid in pin hole;
The micropin master mold containing needle point production liquid in step S21 is put in and dries drying in wind drying box by S22, the drying Temperature is 50 DEG C, obtains needle point forming micropin master mold;
The needle body solution is taped against on the needle point forming micropin master mold in step S22 by S23, in confined space, by air pressure tune Whole to 5 atmospheric pressure, retention time 10s, circulation three times, make the needle body on the micropin master mold full of needle body solution, obtain Fluid injection micropin master mold.
5. the preparation method of Symwhite-337 microneedle patch according to claim 2, which is characterized in that step S2 In, needle body production liquid is Symwhite-337, the Sodium Hyaluronate that molecular weight is 8000, divinylsulfone, water according to The ratio of weight percent 1:1:0.01:100 mixes;
In step S4, the backing production liquid is that the Sodium Hyaluronate of 1,000,000-200 ten thousand molecular weight and Symwhite-337 are pressed Ratio 10:1 mixing, is re-dubbed 30% aqueous solution.
6. the preparation method of Symwhite-337 microneedle patch according to claim 5, which is characterized in that step S2 In, the needle body solution is taped against on the micropin master mold in step S1, in confined space, air pressure is adjusted to 5 atmospheric pressure, Retention time is 10s, and circulation three times, makes the needle body on the micropin master mold make liquid full of the needle body, obtains fluid injection micropin Master mold.
7. the preparation method of Symwhite-337 microneedle patch according to claim 1, which is characterized in that step S4 In, the temperature condition of the drying is room temperature.
CN201910749950.7A 2019-08-14 2019-08-14 Symwhite-337 microneedle patch and preparation method thereof Pending CN110384620A (en)

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111494234A (en) * 2020-05-08 2020-08-07 无锡元旭生物技术有限公司 Compound whitening and freckle-removing patch with function components quantitatively released and preparation method thereof
CN113081895A (en) * 2021-05-06 2021-07-09 无锡元旭生物技术有限公司 Soluble noninvasive microneedle patch for removing chloasma and preparation method thereof

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111494234A (en) * 2020-05-08 2020-08-07 无锡元旭生物技术有限公司 Compound whitening and freckle-removing patch with function components quantitatively released and preparation method thereof
CN113081895A (en) * 2021-05-06 2021-07-09 无锡元旭生物技术有限公司 Soluble noninvasive microneedle patch for removing chloasma and preparation method thereof

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