CN108853062A - A kind of preparation method of the vertical boron sieve release membranes of skin sense gram - Google Patents
A kind of preparation method of the vertical boron sieve release membranes of skin sense gram Download PDFInfo
- Publication number
- CN108853062A CN108853062A CN201810724670.6A CN201810724670A CN108853062A CN 108853062 A CN108853062 A CN 108853062A CN 201810724670 A CN201810724670 A CN 201810724670A CN 108853062 A CN108853062 A CN 108853062A
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- CN
- China
- Prior art keywords
- preparation
- boron sieve
- vertical boron
- skin sense
- release membranes
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/69—Boron compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
- A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
Abstract
The invention discloses a kind of preparation methods of the vertical boron sieve release membranes of skin sense gram, are prepared from the following raw materials：Active constituent, plasticizer, filler, sorbefacient, suspending agent, binder.The frequency that present invention solution drug uses is excessively high and provides the longer skin residence time and reduces administration number of times, film is prepared using a variety of film forming supplementary product compatibilities, it complements each other, it is indispensable, plasticizer and filler enhance film forming, sorbefacient enhances Medicated Permeation ability, and suspending agent guarantees the dispersibility of raw material in a liquid state, and binder enhances the laminating degree of film and skin.
Description
Technical field
The present invention relates to a kind of preparation methods of the vertical boron sieve release membranes of skin sense gram, belong to field of biomedical materials.
Background technique
Gram vertical boron sieve (Crisaborole) is a kind of phosphodiesterase 4 (PDE4) inhibitor, and this inhibition causes intracellular
Cyclic adenosine monophosphate (cAMP) level increases, for treating fungal infection, in particular for treating onychomycosis and/or dermatophyte
Infection.The drug obtains U.S. Food and Drug Administration (FDA) approval listing in December, 2016, public by Anacor pharmacy
Department researches and develops and is responsible in U.S.'s list marketing, and the chemical name of trade name Crisaborole is 5- (4- cyano-benzene oxygen) -1,
3- dihydro -1- hydroxyl -2,1- benzoxaborole heterocyclic pentylene, English name are 4- ((1-hydroxy-1,3-
Dihydrobenzo [c] [1,2] oxaborol-5-yl) oxy) benzonitri le, shown in chemical structural formula such as formula (I)：
The characteristics of medicament slow release is to reach reduction poisonous side effect of medicine by effective control to drug medical dosage, subtract
Few human body drug resistance, improves the stability of drug and the purpose of effective rate of utilization.Since the high molecular material of selection is different, drug
The control releasing mechanism of molecule is not also identical, therefore the research of Polymer Drug Delayed Release Materials has a very important significance.Mesh
Before, gram vertical boron sieve preparation is largely plaster, without reference to sustained release aspect, needs to pinpoint administration, and be easier to be wiped, cannot
Retain for a long time.
Summary of the invention
In view of above-mentioned deficiency, the preparation method of the vertical boron sieve release membranes of skin sense gram provided by the invention solves what drug used
Frequency is excessively high and provides the longer skin residence time and reduces administration number of times.
In order to solve the above-mentioned technical problem, technical scheme is as follows：
A kind of preparation method of the vertical boron sieve release membranes of skin sense gram, carries out as follows：
A, prepared by membrane matrix：Using spandex and silk as host material, carries out that matrix is made, be spaced in matrix
Hydrofuge item is set, hydrofuge item is that antibacterial yarn and acrylic fibers are worked out, and interval width 2-3mm, hydrofuge width is 2-3mm,
That is film forming matrix；
B, first layer is sustained film preparation：By active constituent, plasticizer, filler, sorbefacient, suspending agent, binder
Sufficiently, the material of molten condition is uniformly applied on the above-mentioned membrane matrix prepared by melting for mixing；
C, second layer extended release film preparation：By active constituent, plasticizer, filler, sorbefacient, suspending agent, binder
Mixing sufficiently, adds suitable quantity of water to dissolve, stirs evenly, it is uniformly applied in above-mentioned release membranes, and drying machine drying is not to bright
Aobvious moisture；
D, it cuts to obtain the final product.
Preferably, each raw material proportioning is as follows：Active constituent 15-25%, plasticizer 20-30%, filler 20-30% inhale
Receive promotor 5-10%, suspending agent 5-10%, binder 6-15%.
Preferably, active constituent includes gram vertical boron sieve and/or gram vertical boron sieve analog derivative.
Preferably, plasticizer is selected from one of glycerol, propenyl, polyethylene glycol and/or glyceryl triacetate or several
Kind.
Preferably, filler is selected from one of microcrystalline cellulose, D-sorbite, converted starch and/or dextrin or several
Kind.
Preferably, sorbefacient is selected from one or more of propylene glycol, polysorbate and/or menthol.
Preferably, suspending agent is selected from one or more of carrageenan, guar gum and/or sodium carboxymethylcellulose.
Preferably, binder in polyvinylpyrrolidone, polycarbophil, chitosan and/or polyvinyl alcohol one
Kind is several.
Preferably, in step C, dryer temperature is 60-80 DEG C.
In the present invention, film is prepared using a variety of film forming supplementary product compatibilities, complemented each other, it is indispensable, it plasticizer and fills out
Agent enhancing film forming is filled, sorbefacient enhances Medicated Permeation ability, and suspending agent guarantees the dispersibility of raw material in a liquid state,
The laminating degree of binder enhancing film and skin.
Membrane matrix provided by the invention carries out that matrix is made, in matrix using spandex and silk as host material
Hydrofuge item is arranged in upper interval, and hydrofuge item is that antibacterial yarn and acrylic fibers are worked out, wherein spandex has good elasticity, silk
Have good skin sense, be prepared into matrix, does not have foreign body sensation after enabling to film to paste on the skin, and film can be with people
Body movement is stretched or is compressed, and is had good hygroscopic hydrofuge item with what yarns and acrylic fibers were worked out, is had both ventilative
With dehumidifying effect, achieve the purpose that jointly with gram vertical boron sieve to dermatophyte treating both manifestation and root cause of disease, and passes through ventilative and dehumidifying, Neng Goujin
One step achievees the effect that close to skin sense.For being spaced and the selection of width, apart from too short, it is inadequate to will lead to matrix strength, holds
Easily distortion falls off in use, and apart from too long, the effect sufficiently to dehumidify is not achieved.
Bilayer film provided by the invention, first layer release membranes are prepared using the raw material of molten condition, second layer extended release film
Using aqueous solution of raw material brushing, when in use, second layer extended release film is labelled on skin, is slowly absorbed into disease to water composition
In stove, the fused raw material of first layer will continue to discharge drug, and due to diluting without solvent, concentration is higher, can be constant
Carry out treat, reach extraordinary slow release treatment effect.
Specific embodiment
Above scheme is described further below in conjunction with specific embodiment；It should be understood that these embodiments are for illustrating
The basic principles, principal features and advantages of the present invention, and the present invention is not by the scope limitation of following embodiment；It is used in embodiment
Implementation condition further adjustment can be done according to specific requirement, the implementation condition being not specified is usually the item in routine experiment
Part.
Embodiment 1
A, prepared by membrane matrix：Using spandex and silk as host material, carries out that matrix is made, be spaced in matrix
Hydrofuge item is set, hydrofuge item is that antibacterial yarn and acrylic fibers are worked out, and interval width 2-3mm, hydrofuge width is 2-3mm,
That is film forming matrix；
B, first layer is sustained film preparation：By gram vertical boron sieve 20%, glycerol 25%, microcrystalline cellulose 25%, propylene glycol 7%,
Carragheen 8%, polyvinylpyrrolidone 15% mixes sufficiently, and the material of molten condition is uniformly applied to above-mentioned preparation by melting
On good membrane matrix；
C, second layer extended release film preparation：By gram vertical boron sieve 20%, propenyl 25%, D-sorbite 25%, polysorbate
7%, guar gum 8%, polycarbophil 15% mixes sufficiently, adds suitable quantity of water to dissolve, stirs evenly, it is uniformly applied to above-mentioned slow
It releases on film, drying machine drying to unobvious moisture；
D, it cuts to obtain the final product.
Embodiment 2
A, prepared by membrane matrix：Using spandex and silk as host material, carries out that matrix is made, be spaced in matrix
Hydrofuge item is set, hydrofuge item is that antibacterial yarn and acrylic fibers are worked out, and interval width 2-3mm, hydrofuge width is 2-3mm,
That is film forming matrix；
B, first layer is sustained film preparation：By gram vertical boron sieve 25%, polyethylene glycol 23%, converted starch 22%, menthol
8%, sodium carboxymethylcellulose 7%, chitosan 15% mixes sufficiently, and the material of molten condition is uniformly applied to above-mentioned by melting
On the membrane matrix prepared；
C, second layer extended release film preparation：By gram vertical boron sieve 25%, glyceryl triacetate 23%, dextrin 22%, menthol
8%, sodium carboxymethylcellulose 7%, polyvinyl alcohol 15% mixes sufficiently, adds suitable quantity of water to dissolve, stirs evenly, it is uniformly smeared
In above-mentioned release membranes, drying machine drying to unobvious moisture；
D, it cuts to obtain the final product.
Comparative example 1
A, prepared by membrane matrix：Using common cloth material as matrix, interval setting hydrofuge item, hydrofuge item are on cotton
Antibacterial yarn and acrylic fibers are worked out, interval width 2mm, and hydrofuge width is 2mm, i.e. film forming matrix；
B, first layer is sustained film preparation：By gram vertical boron sieve 20%, glycerol 25%, microcrystalline cellulose 25%, propylene glycol 7%,
Carragheen 8%, polyvinylpyrrolidone 15% mixes sufficiently, and the material of molten condition is uniformly applied to above-mentioned preparation by melting
On good membrane matrix；
C, second layer extended release film preparation：By gram vertical boron sieve 20%, propenyl 25%, D-sorbite 25%, polysorbate
7%, guar gum 8%, polycarbophil 15% mixes sufficiently, adds suitable quantity of water to dissolve, stirs evenly, it is uniformly applied to above-mentioned slow
It releases on film, drying machine drying to unobvious moisture；
D, it cuts to obtain the final product.
Comparative example 2
A, prepared by membrane matrix：Using spandex and silk as host material, carries out that matrix is made, be spaced in matrix
Hydrofuge item is set, hydrofuge item is that antibacterial yarn and acrylic fibers are worked out, and interval width 5mm, hydrofuge width is 3mm,
Membrane matrix；
B, first layer is sustained film preparation：By gram vertical boron sieve 25%, polyethylene glycol 23%, converted starch 22%, menthol
8%, sodium carboxymethylcellulose 7%, chitosan 15% mixes sufficiently, and the material of molten condition is uniformly applied to above-mentioned by melting
On the membrane matrix prepared；
C, second layer extended release film preparation：By gram vertical boron sieve 25%, glyceryl triacetate 23%, dextrin 22%, menthol
8%, sodium carboxymethylcellulose 7%, polyvinyl alcohol 15% mixes sufficiently, adds suitable quantity of water to dissolve, stirs evenly, it is uniformly smeared
In above-mentioned release membranes, drying machine drying to unobvious moisture；
D, it cuts to obtain the final product.
100 volunteers are selected, are divided into 4 groups, every group of 25 people, every group is tried out the above embodiments 1, embodiment respectively
2, the product of comparative example 1 and comparative example 2 carries out sensory evaluation, and for evaluation score from 1-10,10 points are full marks.According to statistical result
It has been shown that, the product Comfort Evaluation of embodiment 1 are 9 points, and the product comfort level of embodiment 2 is 8 points, comparative example 1 and comparative example 2
Product Comfort Evaluation is 5 points, and extraordinary effect can be reached by showing product of the invention.
Claims (9)
1. a kind of preparation method of the vertical boron sieve release membranes of skin sense gram, which is characterized in that carry out as follows：
A, prepared by membrane matrix：It using spandex and silk as host material, carries out that matrix is made, setting is spaced in matrix
Hydrofuge item, hydrofuge item are that antibacterial yarn and acrylic fibers are worked out, and interval width 2-3mm, hydrofuge width is 2-3mm,
Membrane matrix；
B, first layer is sustained film preparation：Active constituent, plasticizer, filler, sorbefacient, suspending agent, binder are mixed
Sufficiently, it melts, the material of molten condition is uniformly applied on the above-mentioned membrane matrix prepared；
C, second layer extended release film preparation：Active constituent, plasticizer, filler, sorbefacient, suspending agent, binder are mixed
Sufficiently, add suitable quantity of water to dissolve, stir evenly, it is uniformly applied in above-mentioned release membranes, drying machine drying to unobvious water
Point；
D, it cuts to obtain the final product.
2. a kind of preparation method of the vertical boron sieve release membranes of skin sense gram according to claim 1, which is characterized in that each raw material is matched
Than as follows：Active constituent 15-25%, plasticizer 20-30%, filler 20-30%, sorbefacient 5-10%, suspending agent 5-
10%, binder 6-15%.
3. a kind of preparation method of the vertical boron sieve release membranes of skin sense gram according to claim 1, which is characterized in that its activity at
Divide includes gram vertical boron sieve and/or gram vertical boron sieve analog derivative.
4. a kind of preparation method of the vertical boron sieve release membranes of skin sense gram according to claim 1, which is characterized in that its plasticizer
Selected from one or more of glycerol, propenyl, polyethylene glycol and/or glyceryl triacetate.
5. a kind of preparation method of the vertical boron sieve release membranes of skin sense gram according to claim 1, which is characterized in that its filler
Selected from one or more of microcrystalline cellulose, D-sorbite, converted starch and/or dextrin.
6. a kind of preparation method of the vertical boron sieve release membranes of skin sense gram according to claim 1, which is characterized in that it, which is absorbed, promotees
One or more of propylene glycol, polysorbate and/or menthol are selected from into agent.
7. a kind of preparation method of the vertical boron sieve release membranes of skin sense gram according to claim 1, which is characterized in that its suspending agent
Selected from one or more of carrageenan, guar gum and/or sodium carboxymethylcellulose.
8. a kind of preparation method of the vertical boron sieve release membranes of skin sense gram according to claim 1, which is characterized in that its binder
Selected from one or more of polyvinylpyrrolidone, polycarbophil, chitosan and/or polyvinyl alcohol.
9. a kind of preparation method of the vertical boron sieve release membranes of skin sense gram as described in claim 1, which is characterized in that in step C, dry
Dry machine temperature is 60-80 DEG C.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201810724670.6A CN108853062A (en) | 2018-07-04 | 2018-07-04 | A kind of preparation method of the vertical boron sieve release membranes of skin sense gram |
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| CN201810724670.6A CN108853062A (en) | 2018-07-04 | 2018-07-04 | A kind of preparation method of the vertical boron sieve release membranes of skin sense gram |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101568327A (en) * | 2006-12-29 | 2009-10-28 | 巴斯夫欧洲公司 | Rapidly dispersable, particulate film coating agent based on polyvinyl alcohol-polyether graft copolymers |
| CN102504350A (en) * | 2011-10-11 | 2012-06-20 | 福建农林大学 | Degradable food packaging paper and preparation method thereof |
| US20170152273A1 (en) * | 2015-11-30 | 2017-06-01 | Anacor Pharmaceuticals Inc. | Topical Pharmaceutical Formulations For Treating Inflammatory-Related Conditions |
-
2018
- 2018-07-04 CN CN201810724670.6A patent/CN108853062A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101568327A (en) * | 2006-12-29 | 2009-10-28 | 巴斯夫欧洲公司 | Rapidly dispersable, particulate film coating agent based on polyvinyl alcohol-polyether graft copolymers |
| CN102504350A (en) * | 2011-10-11 | 2012-06-20 | 福建农林大学 | Degradable food packaging paper and preparation method thereof |
| US20170152273A1 (en) * | 2015-11-30 | 2017-06-01 | Anacor Pharmaceuticals Inc. | Topical Pharmaceutical Formulations For Treating Inflammatory-Related Conditions |
Non-Patent Citations (2)
| Title |
|---|
| 周祥兴: "《包装用塑料制品的生产配方和生产工艺》", 31 December 2010 * |
| 高涛 等: "《药剂学》", 30 May 2017 * |
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Application publication date: 20181123 |
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