CN108785372A - One kind gram vertical boron sieve eliminating dampness diuresis release membranes and preparation method thereof - Google Patents
One kind gram vertical boron sieve eliminating dampness diuresis release membranes and preparation method thereof Download PDFInfo
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- CN108785372A CN108785372A CN201810677385.3A CN201810677385A CN108785372A CN 108785372 A CN108785372 A CN 108785372A CN 201810677385 A CN201810677385 A CN 201810677385A CN 108785372 A CN108785372 A CN 108785372A
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- extract
- gram
- boron sieve
- vertical boron
- eliminating dampness
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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
- 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)
-
- 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)
- A61K36/47—Euphorbiaceae (Spurge family), e.g. Ricinus (castorbean)
-
- 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)
- A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
- A61K36/489—Sophora, e.g. necklacepod or mamani
-
- 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
- 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
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/10—Antioedematous agents; Diuretics
Abstract
The invention discloses a kind of gram vertical boron sieve eliminating dampness diuresis release membranes and preparation method thereof, are formed by following raw material proportioning:Gram vertical boron sieve 9-18mg, shrubby sophora extract 0.2-1.2mg, Herba speranskiae tuberculatae extract 0.2-1.2mg, converted starch 1-2.5mg, carbopol 0.6-1.0mg, glycerine 4-10mg.The frequency that present invention solution drug uses is excessively high and provides the longer skin residence time and reduces administration number of times, resistant starch has good at colloidality, but structure is more loose, and carbopol and glycerine is added being capable of reinforcement structure intensity, so that material is easy film forming, yield rate is improved.
Description
Technical field
The present invention relates to a kind of gram vertical boron sieve eliminating dampness diuresis release membranes and preparation method thereof, belong to biomedical material neck
Domain.
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 boron sieve eliminating dampness diuresis release membranes and preparation method thereof solve drug
The frequency used 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 eliminating dampness diuresis release membranes, are formed by following raw material proportioning:Gram vertical boron sieve 20-35mg, kuh-seng carry
Take object 1-3mg, Herba speranskiae tuberculatae extract 1-3mg, converted starch 4-7mg, carbopol 3-6mg, glycerine 12-20mg.
It is preferred that being formed by following raw material proportioning:Gram vertical boron sieve 25-30mg, shrubby sophora extract 1.5-2.5mg, lopseed extraction
Object 1.5-2.5mg, converted starch 5-6mg, carbopol 4-5mg, glycerine 15-18mg.
More preferably formed by following raw material proportioning:Gram vertical boron sieve 28mg, shrubby sophora extract 2mg, Herba speranskiae tuberculatae extract 2mg,
Converted starch 5.5mg, carbopol 4.5mg, glycerine 16mg.
The present invention also provides the preparation methods of a kind of gram of vertical boron sieve eliminating dampness diuresis release membranes, which is characterized in that specific steps
It is as follows:
A, each raw material is weighed according to above-mentioned weight, converted starch is dissolved in deionized water and forms suspension, it is spare;
B, carbopol and glycerine are added in above-mentioned suspension, are uniformly mixed;
C, gram vertical boron sieve, shrubby sophora extract and a Herba speranskiae tuberculatae extract are added in appropriate amount of deionized water, are stirred evenly;
D, the obtained product of B and C is mixed, obtains uniform dope;
E, the dope that D 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 boron sieve eliminating dampness diuresis release membranes.
Wherein, the preparation method of shrubby sophora extract is, by kuh-seng:Water=1:10, kuh-seng is mixed with water in a reservoir, is added
After heat to 90 DEG C of extraction 2-3h, it is collected by filtration filtrate I and residue I, then by residue I:Water=1:8 extract 2-3h, and filtering is received
Collect filtrate II, merging filtrate I and filtrate II, is concentrated in vacuo to obtain medicinal extract, then carry out being freeze-dried to obtain shrubby sophora extract.
Wherein, the preparation method of Herba speranskiae tuberculatae extract is, by lopseed:Ethyl alcohol=1:10, in a reservoir by lopseed with
Ethyl alcohol mixes, be heated to 60 DEG C carry out cycle extraction 2-3h after, be collected by filtration filtrate I and residue I, then by residue I:Ethyl alcohol=1:
8 extract 2-3h, and filtrate II, merging filtrate I and filtrate II is collected by filtration, is concentrated in vacuo to obtain medicinal extract, then be freeze-dried
Obtain Herba speranskiae tuberculatae extract.
Preferably, in F-step, oven temperature is 60-80 DEG C.
In the present invention, kuh-seng has effects that there is dispelling wind and eliminating dampness, relaxing muscles and tendons to live for heat-clearing and damp-drying drug, desinsection diuresis, lopseed
The effect of blood, further, kuh-seng, can treat eczema wet sore, pruitus, and lopseed can treat the disturbance of lower legs due to pathogenic cold and dampness, both
Chinese medicine can generate synergistic effect with gram vertical boron sieve, reinforce the therapeutic effect of product.
In the present invention, resistant starch has good at colloidality, but structure is more loose, and carbopol and glycerine energy is added
Enough reinforcement structure intensity so that material is easy film forming, improves yield rate.
In the present invention, resistant starch is first prepared into suspension, then adds carbopol and glycerine, carried out according to the sequence
Mixing can give full play to the effect of each auxiliary material, improve quality of forming film, be eventually adding the aqueous solution of active constituent, feed liquid dispersion
Uniformly, had good sustained release effect.
Description of the drawings
Fig. 1 is the medicament slow release situation of embodiment 3, comparative example 1 and comparative example 2.
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 1
A, following raw material is weighed:Gram vertical boron sieve 20mg, shrubby sophora extract 1mg, Herba speranskiae tuberculatae extract 1mg, converted starch
Converted starch is dissolved in deionized water and forms suspension by 4mg, carbopol 3mg, glycerine 12mg, spare;
B, carbopol and glycerine are added in above-mentioned suspension, are uniformly mixed;
C, gram vertical boron sieve, shrubby sophora extract and a Herba speranskiae tuberculatae extract are added in appropriate amount of deionized water, are stirred evenly;
D, the obtained product of B and C is mixed, obtains uniform dope;
E, the dope that D 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 boron sieve compound health release membranes.
Embodiment 2
A, following raw material is weighed:Gram vertical boron sieve 35mg, shrubby sophora extract 3mg, Herba speranskiae tuberculatae extract 3mg, converted starch
Converted starch is dissolved in deionized water and forms suspension by 7mg, carbopol 6mg, glycerine 20mg, spare;
B, carbopol and glycerine are added in above-mentioned suspension, are uniformly mixed;
C, gram vertical boron sieve, shrubby sophora extract and a Herba speranskiae tuberculatae extract are added in appropriate amount of deionized water, are stirred evenly;
D, the obtained product of B and C is mixed, obtains uniform dope;
E, the dope that D 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 boron sieve compound health release membranes.
Embodiment 3
A, following raw material is weighed:Gram vertical boron sieve 28mg, shrubby sophora extract 2mg, Herba speranskiae tuberculatae extract 2mg, converted starch
Converted starch is dissolved in deionized water and forms suspension by 5.5mg, carbopol 4.5mg, glycerine 16mg, spare;
B, carbopol and glycerine are added in above-mentioned suspension, are uniformly mixed;
C, gram vertical boron sieve, shrubby sophora extract and a Herba speranskiae tuberculatae extract are added in appropriate amount of deionized water, are stirred evenly;
D, the obtained product of B and C is mixed, obtains uniform dope;
E, the dope that D 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 boron sieve compound health release membranes.
Comparative example one
A, following raw material is weighed:Gram vertical boron sieve 35mg, shrubby sophora extract 3mg, Herba speranskiae tuberculatae extract 3mg, converted starch
Converted starch is dissolved in deionized water and forms suspension by 7mg, carbopol 2mg, glycerine 20mg, spare;
B, glycerine is added in above-mentioned suspension, is uniformly mixed;
C, gram vertical boron sieve, shrubby sophora extract and a Herba speranskiae tuberculatae extract are added in appropriate amount of deionized water, are stirred evenly;
D, the obtained product of B and C is mixed, obtains uniform dope;
E, the dope that D 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 boron sieve compound health release membranes.
Comparative example two
A, following raw material is weighed:Gram vertical boron sieve 35mg, shrubby sophora extract 3mg, Herba speranskiae tuberculatae extract 3mg, converted starch
7mg, glycerine 26mg, converted starch is dissolved in deionized water and forms suspension, spare;
B, carbopol and glycerine are added in above-mentioned suspension, are uniformly mixed;
C, gram vertical boron sieve, shrubby sophora extract and a Herba speranskiae tuberculatae extract are added in appropriate amount of deionized water, are stirred evenly;
D, the obtained product of B and C is mixed, obtains uniform dope;
E, the dope that D 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 boron sieve compound health release membranes.
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 boron sieve eliminating dampness diuresis release membranes, which is characterized in that formed by following raw material proportioning:Gram vertical boron sieve 20-
35mg, shrubby sophora extract 1-3mg, Herba speranskiae tuberculatae extract 1-3mg, converted starch 4-7mg, carbopol 3-6mg, glycerine 12-20mg.
2. one kind gram vertical boron sieve eliminating dampness diuresis release membranes according to claim 1, which is characterized in that by following raw material proportioning
It forms:Gram vertical boron sieve 25-30mg, shrubby sophora extract 1.5-2.5mg, Herba speranskiae tuberculatae extract 1.5-2.5mg, converted starch 5-6mg,
Carbopol 4-5mg, glycerine 15-18mg.
3. one kind gram vertical boron sieve eliminating dampness diuresis release membranes according to claim 1, which is characterized in that by following raw material proportioning
It forms:Gram vertical boron sieve 28mg, shrubby sophora extract 2mg, Herba speranskiae tuberculatae extract 2mg, converted starch 5.5mg, carbopol 4.5mg are sweet
Oily 16mg.
4. the preparation method of a kind of gram of vertical boron sieve eliminating dampness diuresis release membranes according to claim 1-3, which is characterized in that tool
Steps are as follows for body:
A, each raw material is weighed according to above-mentioned weight, converted starch is dissolved in deionized water and forms suspension, it is spare;
B, carbopol and glycerine are added in above-mentioned suspension, are uniformly mixed;
C, gram vertical boron sieve, shrubby sophora extract and a Herba speranskiae tuberculatae extract are added in appropriate amount of deionized water, are stirred evenly;
D, the obtained product of B and C is mixed, obtains uniform dope;
E, the dope that D 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 boron sieve eliminating dampness diuresis release membranes.
5. the preparation method of a kind of gram of vertical boron sieve eliminating dampness diuresis release membranes according to claim 4, which is characterized in that kuh-seng
The preparation method of extract is, by kuh-seng:Water=1:10, kuh-seng is mixed with water in a reservoir, is heated to 90 DEG C of extraction 2-3h
Afterwards, filtrate I and residue I are collected by filtration, then by residue I:Water=1:8 extract 2-3h, and filtrate II, merging filtrate is collected by filtration
I and filtrate II are concentrated in vacuo to obtain medicinal extract, then carry out being freeze-dried to obtain shrubby sophora extract.
6. the preparation method of a kind of gram of vertical boron sieve eliminating dampness diuresis release membranes according to claim 4, which is characterized in that deep
The preparation method of careless extract is, by lopseed:Ethyl alcohol=1:10, lopseed is mixed with ethyl alcohol in a reservoir, is heated to 60
After DEG C carrying out cycle extraction 2-3h, it is collected by filtration filtrate I and residue I, then by residue I:Ethyl alcohol=1:8 extract 2-3h, mistake
Filtrate II, merging filtrate I and filtrate II are collected in filter, are concentrated in vacuo to obtain medicinal extract, then carry out being freeze-dried to obtain Herba speranskiae tuberculatae extract.
7. the preparation method of a kind of gram of vertical boron sieve eliminating dampness diuresis release membranes as claimed in claim 4, which is characterized in that E steps
In, oven temperature is 60-80 DEG C.
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Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
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US20170152273A1 (en) * | 2015-11-30 | 2017-06-01 | Anacor Pharmaceuticals Inc. | Topical Pharmaceutical Formulations For Treating Inflammatory-Related Conditions |
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2018
- 2018-06-27 CN CN201810677385.3A patent/CN108785372A/en active Pending
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
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US20170152273A1 (en) * | 2015-11-30 | 2017-06-01 | Anacor Pharmaceuticals Inc. | Topical Pharmaceutical Formulations For Treating Inflammatory-Related Conditions |
Non-Patent Citations (1)
Title |
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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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Application publication date: 20181113 |