CN108785379A - One kind gram vertical refrigerant release membranes of boron sieve and preparation method thereof - Google Patents
One kind gram vertical refrigerant release membranes of boron sieve and preparation method thereof Download PDFInfo
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- CN108785379A CN108785379A CN201810667793.0A CN201810667793A CN108785379A CN 108785379 A CN108785379 A CN 108785379A CN 201810667793 A CN201810667793 A CN 201810667793A CN 108785379 A CN108785379 A CN 108785379A
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- Prior art keywords
- gram
- boron sieve
- borneol
- refrigerant release
- release membranes
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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
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/53—Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
- A61K36/534—Mentha (mint)
-
- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
-
- 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
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
-
- 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
- A61P31/02—Local antiseptics
-
- 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 gram vertical refrigerant release membranes of boron sieve and preparation method thereof, are formed by following raw material proportioning：Gram vertical boron sieve 10-20mg, borneol 0.4-1.0mg, peppermint oil 0.01-0.05mg, polyvinylpyrrolidone 0.1-0.5mg, polycarbophil 0.9-1.5mg, glycerine 3-12mg.The frequency that present invention solution drug uses is excessively high and provides the longer skin residence time and reduces administration number of times, polyvinylpyrrolidone has good film forming, but plasticity is insufficient, and polycarbophil and glycerine, which is added, can promote film forming, make the film smooth pliable being prepared.
Description
Technical field
The present invention relates to a kind of gram vertical refrigerant release membranes of boron sieve and preparation method thereof, belong to field of biomedical materials.
Background technology
Gram vertical boron sieve (Crisaborole) is a kind of phosphodiesterase 4 (PDE4) inhibitor, and this inhibition causes intracellular
Cyclic adenosine monophosphate (cAMP) level increases, and for treating fungal infection, is in particular used to treat onychomycosis and/or dermatophyte
Infection.The drug obtains U.S. Food and Drug Administration (FDA) in December, 2016 and ratifies listing, 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 oxygens) -1,
3- dihydro -1- hydroxyl -2,1- benzoxaborole heterocyclic pentylenes, 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 also differs, therefore the research of Polymer Drug Delayed Release Materials has a very important significance.Mesh
Before, gram vertical boron sieve preparation is largely that plaster needs fixed point to be administered, and be easier to be wiped without reference in terms of sustained release, cannot
Retain for a long time.
Invention content
In view of above-mentioned deficiency, provided by the invention gram of vertical refrigerant release membranes of boron sieve and preparation method thereof solve drug and use
Frequency it is excessively high and longer skin residence time is provided 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 refrigerant release membranes of boron sieve, are formed by following raw material proportioning：Gram vertical boron sieve 10-20mg, borneol 0.4-
1.0mg, peppermint oil 0.01-0.05mg, polyvinylpyrrolidone 0.1-0.5mg, polycarbophil 0.9-1.5mg, glycerine 3-12mg.
It is preferred that being formed by following raw material proportioning：Gram vertical boron sieve 15-18mg, borneol 0.5-0.8mg, peppermint oil 0.02-
0.04mg, polyvinylpyrrolidone 0.2-0.4mg, polycarbophil 1.0-1.4mg, glycerine 5-10mg.
More preferably formed by following raw material proportioning：Gram vertical boron sieve 16mg, borneol 0.6mg, peppermint oil 0.04mg, polyethylene pyrrole
Pyrrolidone 0.4mg, polycarbophil 1.3mg, glycerine 8mg.
The present invention also provides the preparation methods of a kind of gram of vertical refrigerant release membranes of boron sieve, which is characterized in that is as follows：
A, each raw material is weighed according to above-mentioned weight, borneol is ground, it is spare；
B, polyvinylpyrrolidone is added in appropriate amount of deionized water, heating water bath stirs evenly, and obtains jelly；
C, polycarbophil and glycerine are added in above-mentioned jelly, are uniformly mixed；
D, gram vertical boron sieve, borneol and a peppermint oil are added in appropriate amount of deionized water, are stirred evenly；
E, the obtained product of C and D is mixed, obtains uniform dope；
F, the dope that E is obtained is toppled on a glass, is uniformly paved, carry out oven drying, cooling, film is taken off in cutting
Up to gram vertical refrigerant release membranes of boron sieve.
Preferably, in step A, borneol is ground to 200-300 mesh.
Preferably, in step B, water bath heating temperature is 40-60 DEG C.
Preferably, in F-step, oven temperature is 60-80 DEG C.
In the present invention, borneol has effects that clearing away heat to and alleviating pain, antimicrobial antiphlogistic, peppermint oil have the effect of refrigerant anti-inflammatory,
Can the scorching hot sense of substantially reduced fungal infection skin surface itch, and a synergistic effect can be generated with gram vertical boron sieve, reinforce production
The effect of product antibacterial.
In the present invention, polyvinylpyrrolidone has good film forming, but plasticity is insufficient, be added polycarbophil and
Glycerine can promote film forming, make the film smooth pliable being prepared.
In the present invention, polyvinylpyrrolidone is first prepared into jelly, then adds polycarbophil and glycerine, according to this
Sequence is mixed, and the effect of each auxiliary material can be given full play to, and is improved quality of forming film, is eventually adding the aqueous solution of active constituent,
Feed liquid is uniformly dispersed, had good sustained release effect.
Description of the drawings
Fig. 1 is the medicament slow release situation of embodiment three, comparative example one and comparative example two.
Specific implementation mode
Said program 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 one
A, following raw material is weighed：Gram vertical boron sieve 10mg, borneol 0.4mg, peppermint oil 0.01mg, polyvinylpyrrolidone
0.1mg, polycarbophil 0.9mg, glycerine 3mg grind borneol to 200 mesh, spare；
B, polyvinylpyrrolidone is added in appropriate amount of deionized water, heating water bath stirs evenly, and 40 DEG C of temperature obtains glue
Shape object；
C, polycarbophil and glycerine are added in above-mentioned jelly, are uniformly mixed；
D, gram vertical boron sieve, borneol and a peppermint oil are added in appropriate amount of deionized water, are stirred evenly；
E, the obtained product of C and D is mixed, obtains uniform dope；
F, the dope that E is obtained to be toppled on a glass, is uniformly paved, carry out oven drying, temperature 60 C is cooling,
Cutting takes off film up to gram vertical refrigerant release membranes of boron sieve.
Embodiment two
A, following raw material is weighed：Gram vertical boron sieve 16mg, borneol 0.6mg, peppermint oil 0.04mg, polyvinylpyrrolidone
0.4mg, polycarbophil 1.3mg, glycerine 8mg grind borneol to 250 mesh, spare；
B, polyvinylpyrrolidone is added in appropriate amount of deionized water, heating water bath stirs evenly, and temperature 50 C obtains glue
Shape object；
C, polycarbophil and glycerine are added in above-mentioned jelly, are uniformly mixed；
D, gram vertical boron sieve, borneol and a peppermint oil are added in appropriate amount of deionized water, are stirred evenly；
E, the obtained product of C and D is mixed, obtains uniform dope；
F, the dope that E is obtained to be toppled on a glass, is uniformly paved, carry out oven drying, temperature 70 C is cooling,
Cutting takes off film up to gram vertical refrigerant release membranes of boron sieve.
Embodiment three
A, following raw material is weighed：Gram vertical boron sieve 20mg, borneol 1.0mg, peppermint oil 0.05mg, polyvinylpyrrolidone
0.5mg, polycarbophil 1.5mg, glycerine 12mg grind borneol to 300 mesh, spare；
B, polyvinylpyrrolidone is added in appropriate amount of deionized water, heating water bath stirs evenly, and temperature 60 C obtains glue
Shape object；
C, polycarbophil and glycerine are added in above-mentioned jelly, are uniformly mixed；
D, gram vertical boron sieve, borneol and a peppermint oil are added in appropriate amount of deionized water, are stirred evenly；
E, the obtained product of C and D is mixed, obtains uniform dope；
F, the dope that E is obtained to be toppled on a glass, is uniformly paved, carry out oven drying, 80 DEG C of temperature is cooling,
Cutting takes off film up to gram vertical refrigerant release membranes of boron sieve.
Comparative example one
A, following raw material is weighed：Gram vertical boron sieve 20mg, borneol 1.0mg, peppermint oil 0.05mg, polyvinylpyrrolidone
0.5mg, glycerine 13.5mg grind borneol to 300 mesh, spare；
B, polyvinylpyrrolidone is added in appropriate amount of deionized water, heating water bath stirs evenly, and temperature 60 C obtains glue
Shape object；
C, glycerine is added in above-mentioned jelly, is uniformly mixed；
D, gram vertical boron sieve, borneol and a peppermint oil are added in appropriate amount of deionized water, are stirred evenly；
E, the obtained product of C and D is mixed, obtains uniform dope；
F, the dope that E is obtained to be toppled on a glass, is uniformly paved, carry out oven drying, 80 DEG C of temperature is cooling,
Cutting takes off film up to gram vertical refrigerant release membranes of boron sieve.
Comparative example two
A, following raw material is weighed：Gram vertical boron sieve 20mg, borneol 1.0mg, peppermint oil 0.05mg, polyvinylpyrrolidone
0.5mg, polycarbophil 0.5mg, glycerine 12mg grind borneol to 300 mesh, spare；
B, polyvinylpyrrolidone is added in appropriate amount of deionized water, heating water bath stirs evenly, and temperature 60 C obtains glue
Shape object；
C, polycarbophil and glycerine are added in above-mentioned jelly, are uniformly mixed；
D, gram vertical boron sieve, borneol and a peppermint oil are added in appropriate amount of deionized water, are stirred evenly；
E, the obtained product of C and D is mixed, obtains uniform dope；
F, the dope that E is obtained to be toppled on a glass, is uniformly paved, carry out oven drying, 80 DEG C of temperature is cooling,
Cutting takes off film up to gram vertical refrigerant release membranes of boron sieve.
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, 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 (7)
1. a kind of gram vertical refrigerant release membranes of boron sieve, which is characterized in that formed by following raw material proportioning：Gram vertical boron sieve 10-20mg, ice
Piece 0.4-1.0mg, peppermint oil 0.01-0.05mg, polyvinylpyrrolidone 0.1-0.5mg, polycarbophil 0.9-1.5mg, glycerine
3-12mg。
2. one kind gram vertical refrigerant release membranes of boron sieve according to claim 1, which is characterized in that by following raw material proportioning
At：Gram vertical boron sieve 15-18mg, borneol 0.5-0.8mg, peppermint oil 0.02-0.04mg, polyvinylpyrrolidone 0.2-0.4mg gather
Ka Bofei 1.0-1.4mg, glycerine 5-10mg.
3. one kind gram vertical refrigerant release membranes of boron sieve according to claim 2, which is characterized in that by following raw material proportioning
At：Gram vertical boron sieve 16mg, borneol 0.6mg, peppermint oil 0.04mg, polyvinylpyrrolidone 0.4mg, polycarbophil 1.3mg, glycerine
8mg。
4. the preparation method of a kind of gram of vertical refrigerant release membranes of boron sieve according to claim 1-3, which is characterized in that specific step
It is rapid as follows：
A, each raw material is weighed according to above-mentioned weight, borneol is ground, it is spare；
B, polyvinylpyrrolidone is added in appropriate amount of deionized water, heating water bath stirs evenly, and obtains jelly；
C, polycarbophil and glycerine are added in above-mentioned jelly, are uniformly mixed；
D, gram vertical boron sieve, borneol and a peppermint oil are added in appropriate amount of deionized water, are stirred evenly；
E, the obtained product of C and D is mixed, obtains uniform dope；
F, the dope that E is obtained is toppled on a glass, uniformly paved, carry out oven drying, cooling, cutting takes off film to obtain the final product
Gram vertical refrigerant release membranes of boron sieve.
5. the preparation method of a kind of gram of vertical refrigerant release membranes of boron sieve according to claim 4, which is characterized in that in step A,
Borneol is ground to 200-300 mesh.
6. the preparation method of a kind of gram of vertical refrigerant release membranes of boron sieve according to claim 4, which is characterized in that in step B,
Water bath heating temperature is 40-60 DEG C.
7. the preparation method of a kind of gram of vertical refrigerant release membranes of boron sieve according to claim 4, which is characterized in that in F-step,
Oven temperature is 60-80 DEG C.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810667793.0A CN108785379A (en) | 2018-06-26 | 2018-06-26 | One kind gram vertical refrigerant release membranes of boron sieve and preparation method thereof |
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| CN201810667793.0A CN108785379A (en) | 2018-06-26 | 2018-06-26 | One kind gram vertical refrigerant release membranes of boron sieve and preparation method thereof |
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| CN201810667793.0A Pending CN108785379A (en) | 2018-06-26 | 2018-06-26 | One kind gram vertical refrigerant release membranes of boron sieve and preparation method thereof |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104306358A (en) * | 2014-11-06 | 2015-01-28 | 哈尔滨乾佰纳生物药业有限公司 | Itching-relieving scar-removing coating agent |
| CN104983674A (en) * | 2015-06-30 | 2015-10-21 | 武汉烺祺生物科技有限公司 | External use drug for quickly relieving itching, eliminating swelling and rash, and resisting mosquito and insect bites |
| US20170152273A1 (en) * | 2015-11-30 | 2017-06-01 | Anacor Pharmaceuticals Inc. | Topical Pharmaceutical Formulations For Treating Inflammatory-Related Conditions |
-
2018
- 2018-06-26 CN CN201810667793.0A patent/CN108785379A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104306358A (en) * | 2014-11-06 | 2015-01-28 | 哈尔滨乾佰纳生物药业有限公司 | Itching-relieving scar-removing coating agent |
| CN104983674A (en) * | 2015-06-30 | 2015-10-21 | 武汉烺祺生物科技有限公司 | External use drug for quickly relieving itching, eliminating swelling and rash, and resisting mosquito and insect bites |
| US20170152273A1 (en) * | 2015-11-30 | 2017-06-01 | Anacor Pharmaceuticals Inc. | Topical Pharmaceutical Formulations For Treating Inflammatory-Related Conditions |
Non-Patent Citations (1)
| Title |
|---|
| 郭宗儒: "含硼外用药他伐硼罗和克立硼罗的研制 ", 《药学学报》 * |
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| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20181113 |
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