CN108938602A - A kind of gram vertical boron sieve release membranes of good absorption effect and preparation method thereof - Google Patents
A kind of gram vertical boron sieve release membranes of good absorption effect and preparation method thereof Download PDFInfo
- Publication number
- CN108938602A CN108938602A CN201810706388.5A CN201810706388A CN108938602A CN 108938602 A CN108938602 A CN 108938602A CN 201810706388 A CN201810706388 A CN 201810706388A CN 108938602 A CN108938602 A CN 108938602A
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- Prior art keywords
- absorption effect
- good absorption
- boron sieve
- vertical boron
- gram vertical
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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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
- A61K9/7007—Drug-containing films, membranes or sheets
-
- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- 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
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
-
- 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
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
-
- 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
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
-
- 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 gram vertical boron sieve release membranes of a kind of good absorption effect and preparation method thereof, 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 gram vertical boron sieve release membranes of a kind of good absorption effect and preparation method thereof, belong to biomedical material
Field.
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) benzonitrile, 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, gram vertical boron sieve release membranes of good absorption effect provided by the invention and preparation method thereof are solved
The frequency that drug uses 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 gram vertical boron sieve release membranes of good absorption effect, are prepared from the following raw materials: active constituent, plasticizer, filler,
Sorbefacient, suspending agent, binder.
Preferably, each raw material proportioning is as follows: active constituent 15-25%, plasticizer 20-30%, filler 20-30%, inhales
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 made of propylene glycol, polysorbate, menthol, tsaoko oil and caryophyllus oil.
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, sorbefacient is by propylene glycol 60%, polysorbate 10%, menthol 10%, 10% and of tsaoko oil
Caryophyllus oil 10% forms.
The present invention also provides a kind of preparation methods of gram vertical boron sieve release membranes of good absorption effect, the specific steps are as follows:
A, first layer is sustained film preparation: by active constituent, plasticizer, filler, sorbefacient, suspending agent, binder
Sufficiently, melting is extruded into film with extruder for mixing；
B, 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；
C, it cuts to obtain the final product.
Preferably, in step B, 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.
Sorbefacient provided by the invention is made of a variety of lipophilic ingredients, and penetrating power is strong, and each small molecule has association
Same effect can adsorb composition cage structure for active constituent package from each other and form Water-In-Oil micel wherein, can
The through lesion of skin is effectively passed through, after then being absorbed oiliness carrier by tissue, active constituent is released, effectively treats
The diseases such as fungal infection.
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.
Detailed description of the invention
Fig. 1 is the drug absorption situation of embodiment 1, embodiment 2, comparative example 1 and comparative example 2.
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, first layer is sustained film preparation: by gram vertical boron sieve 20%, glycerol 25%, microcrystalline cellulose 25%, sorbefacient
7% (wherein propylene glycol 60%, polysorbate 10%, menthol 10%, tsaoko oil 10% and caryophyllus oil 10%), carragheen 8%,
Polyvinylpyrrolidone 15% mixes sufficiently, and melting is extruded into film with extruder；
B, second layer extended release film preparation: by gram vertical boron sieve 20%, propenyl 25%, D-sorbite 25%, sorbefacient
7% (propylene glycol 60%, polysorbate 10%, menthol 10%, tsaoko oil 10% and caryophyllus oil 10%), guar gum 8%, poly- card
Non- 15% mixing of wave sufficiently, adds suitable quantity of water to dissolve, stirs evenly, it is uniformly applied in above-mentioned release membranes, drying machine drying
To unobvious moisture, drying temperature is 60 DEG C；
C, it cuts to obtain the final product.
Embodiment 2
A, first layer is sustained film preparation: by gram vertical boron sieve 25%, polyethylene glycol 23%, converted starch 22%, absorption enhancement
Agent 8% (propylene glycol 60%, polysorbate 10%, menthol 10%, tsaoko oil 10% and caryophyllus oil 10%), carboxymethyl cellulose
Sodium 7%, chitosan 15% mixes sufficiently, and melting is extruded into film with extruder；
B, second layer extended release film preparation: by gram vertical boron sieve 25%, glyceryl triacetate 23%, dextrin 22%, absorption enhancement
Agent 8% (propylene glycol 60%, polysorbate 10%, menthol 10%, tsaoko oil 10% and caryophyllus oil 10%), carboxymethyl cellulose
Sodium 7%, polyvinyl alcohol 15% mixes sufficiently, adds suitable quantity of water to dissolve, stirs evenly, it is uniformly applied in above-mentioned release membranes,
For drying machine drying to unobvious moisture, drying temperature is 60 DEG C；
C, it cuts to obtain the final product.
Comparative example 1
A, first layer is sustained film preparation: by gram vertical boron sieve 20%, glycerol 25%, microcrystalline cellulose 25%, sorbefacient
7% (wherein propylene glycol 65%, polysorbate 5%, menthol 10%, tsaoko oil 10% and caryophyllus oil 10%), carragheen 8%,
Polyvinylpyrrolidone 15% mixes sufficiently, and melting is extruded into film with extruder；
B, second layer extended release film preparation: by gram vertical boron sieve 20%, propenyl 25%, D-sorbite 25%, sorbefacient
7% (propylene glycol 65%, polysorbate 5%, menthol 10%, tsaoko oil 10% and caryophyllus oil 10%), guar gum 8%, poly- card
Non- 15% mixing of wave sufficiently, adds suitable quantity of water to dissolve, stirs evenly, it is uniformly applied in above-mentioned release membranes, drying machine drying
To unobvious moisture, drying temperature is 60 DEG C；
C, it cuts to obtain the final product.
Comparative example 2
A, first layer is sustained film preparation: by gram vertical boron sieve 25%, polyethylene glycol 23%, converted starch 22%, absorption enhancement
Agent 8% (propylene glycol 60%, polysorbate 20 %, tsaoko oil 10% and caryophyllus oil 10%), sodium carboxymethylcellulose 7%, shell are poly-
Sufficiently, melting is extruded into film with extruder to 15% mixing of sugar；
B, second layer extended release film preparation: by gram vertical boron sieve 25%, glyceryl triacetate 23%, dextrin 22%, absorption enhancement
Agent 8% (propylene glycol 60%, polysorbate 20 %, tsaoko oil 10% and caryophyllus oil 10%), sodium carboxymethylcellulose 7%, poly- second
Enol 15% mixes sufficiently, adds suitable quantity of water to dissolve, stirs evenly, it is uniformly applied in above-mentioned release membranes, drying machine drying
To unobvious moisture, drying temperature is 60 DEG C；
C, it cuts to obtain the final product.
The above embodiments merely illustrate the technical concept and features of the present invention, and its object is to allow person skilled in the art
Scholar cans understand the content of the present invention and implement it accordingly, and it is not intended to limit the scope of the present invention, it is all according to the present invention
Equivalent change or modification made by Spirit Essence, should be covered by the protection scope of the present invention.
Claims (10)
1. a kind of gram vertical boron sieve release membranes of good absorption effect, which is characterized in that be prepared from the following raw materials: active constituent, plasticising
Agent, filler, sorbefacient, suspending agent, binder, sorbefacient is by propylene glycol, polysorbate, menthol, tsaoko
Oil and caryophyllus oil composition.
2. a kind of gram vertical boron sieve release membranes of good absorption effect according to claim 1, which is characterized in that each raw material proportioning
It is 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 gram vertical boron sieve release membranes of good absorption effect according to claim 1, which is characterized in that its active constituent
Including gram vertical boron sieve and/or gram vertical boron sieve analog derivative.
4. a kind of gram vertical boron sieve release membranes of good absorption effect according to claim 1, which is characterized in that the choosing of its plasticizer
From one or more of glycerol, propenyl, polyethylene glycol and/or glyceryl triacetate.
5. a kind of gram vertical boron sieve release membranes of good absorption effect according to claim 1, which is characterized in that the choosing of its filler
From one or more of microcrystalline cellulose, D-sorbite, converted starch and/or dextrin.
6. a kind of gram vertical boron sieve release membranes of good absorption effect according to claim 1, which is characterized in that the choosing of its suspending agent
From one or more of carrageenan, guar gum and/or sodium carboxymethylcellulose.
7. a kind of gram vertical boron sieve release membranes of good absorption effect according to claim 1, which is characterized in that the choosing of its binder
From one or more of polyvinylpyrrolidone, polycarbophil, chitosan and/or polyvinyl alcohol.
8. a kind of gram vertical boron sieve release membranes of good absorption effect according to claim 1, which is characterized in that its absorption enhancement
Agent is made of propylene glycol 60%, polysorbate 10%, menthol 10%, tsaoko oil 10% and caryophyllus oil 10%.
9. a kind of preparation method of gram vertical boron sieve release membranes of good absorption effect, feature described in -8 exist according to claim 1
In, the specific steps are as follows:
A, first layer is sustained film preparation: active constituent, plasticizer, filler, sorbefacient, suspending agent, binder are mixed
Sufficiently, it melts, is extruded into film with extruder；
B, 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；
C, it cuts to obtain the final product.
10. a kind of preparation method of gram vertical boron sieve release membranes of good absorption effect as claimed in claim 9, which is characterized in that B
In step, dryer temperature is 60-80 DEG C.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810706388.5A CN108938602A (en) | 2018-07-02 | 2018-07-02 | A kind of gram vertical boron sieve release membranes of good absorption effect and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810706388.5A CN108938602A (en) | 2018-07-02 | 2018-07-02 | A kind of gram vertical boron sieve release membranes of good absorption effect and preparation method thereof |
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| CN108938602A true CN108938602A (en) | 2018-12-07 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201810706388.5A Pending CN108938602A (en) | 2018-07-02 | 2018-07-02 | A kind of gram vertical boron sieve release membranes of good absorption effect and preparation method thereof |
Country Status (1)
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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
- 2018-07-02 CN CN201810706388.5A patent/CN108938602A/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: 20181207 |
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