CN108524648A - One kind gram vertical boron sieve compound health release membranes and preparation method thereof - Google Patents
One kind gram vertical boron sieve compound health release membranes and preparation method thereof Download PDFInfo
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- CN108524648A CN108524648A CN201810667792.6A CN201810667792A CN108524648A CN 108524648 A CN108524648 A CN 108524648A CN 201810667792 A CN201810667792 A CN 201810667792A CN 108524648 A CN108524648 A CN 108524648A
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- extract
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- boron sieve
- vertical boron
- compound health
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- 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)
- A61K36/75—Rutaceae (Rue family)
- A61K36/756—Phellodendron, e.g. corktree
-
- 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
- A61K36/13—Coniferophyta (gymnosperms)
- A61K36/15—Pinaceae (Pine family), e.g. pine or cedar
-
- 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
- A61K9/0012—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
- A61K9/7007—Drug-containing films, membranes or sheets
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/30—Extraction of the material
- A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
- A61K2236/331—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using water, e.g. cold water, infusion, tea, steam distillation, decoction
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/30—Extraction of the material
- A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
- A61K2236/333—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using mixed solvents, e.g. 70% EtOH
Abstract
The invention discloses a kind of gram vertical boron sieve compound health release membranes and preparation method thereof, are formed by following raw material proportioning：Gram vertical 9 18mg of boron sieve, 0.2 1.2mg of Cortex Pseudolaricis extract, 0.2 1.2mg of phellodendron extract, 1 2.5mg of converted starch, 0.6 1.0mg of carbopol, 4 10mg of glycerine.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 compound health 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) 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 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 compound health 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.The present invention is by following technical side
Case is realized：
A kind of gram vertical boron sieve compound health release membranes, are formed by following raw material proportioning：Gram vertical boron sieve 9-18mg, Golden Larch Bark carry
Take object 0.2-1.2mg, phellodendron extract 0.2-1.2mg, converted starch 1-2.5mg, carbopol 0.6-1.0mg, glycerine 4-10mg.
It is preferred that being formed by following raw material proportioning：Gram vertical boron sieve 12-16mg, Cortex Pseudolaricis extract 0.4-1.0mg, Cortex Phellodendri extraction
Object 0.4-1.0mg, converted starch 1.5-2.0mg, carbopol 0.7-0.9mg, glycerine 5-8mg.
More preferably formed by following raw material proportioning：Gram vertical boron sieve 14mg, Cortex Pseudolaricis extract 0.7mg, phellodendron extract
0.7mg, converted starch 1.7mg, carbopol 0.8mg, glycerine 7mg.
The present invention also provides the preparation methods of a kind of gram of vertical boron sieve compound health release membranes, are 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, Cortex Pseudolaricis extract and a phellodendron 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 compound health release membranes.
Wherein, the preparation method of the Cortex Pseudolaricis extract is, by Golden Larch Bark：Water=1:10, in a reservoir by Golden Larch Bark
It is mixed with water, after being heated to 90 DEG C of extraction 2-3h, is collected by filtration filtrate I and residue I, then by residue I：Water=1:8 extract
Filtrate II, merging filtrate I and filtrate II is collected by filtration in 2-3h, is concentrated in vacuo to obtain medicinal extract, then be freeze-dried Golden Larch Bark carries
Take object.
Wherein, the preparation method of the phellodendron extract is, by Cortex Phellodendri：Ethyl alcohol=1:10, in a reservoir by Cortex Phellodendri and second
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
2-3h is extracted, filtrate II, merging filtrate I and filtrate II is collected by filtration, is concentrated in vacuo to obtain medicinal extract, then be freeze-dried
Phellodendron extract.
Preferably, in E steps, oven temperature is 60-80 DEG C.
In the present invention, Golden Larch Bark and Cortex Phellodendri have effects that antimicrobial antiphlogistic, treatment onychomycosis, wherein Cortex Phellodendri also has clear
The effect of hot eliminating dampness, 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
The medicament slow release situation of Fig. 1 embodiments 3, comparative example 1 and comparative example 2.
Specific implementation mode
With reference to embodiment, the invention will be further described.Following embodiment is only used for clearly illustrating this hair
Bright technical solution, and not intended to limit the protection scope of the present invention.
Embodiment 1
A, following raw material is weighed：Gram vertical boron sieve 9mg, Cortex Pseudolaricis extract 0.2mg, phellodendron extract 0.2mg, converted starch
Converted starch is dissolved in deionized water and forms suspension by 1mg, carbopol 0.6mg, glycerine 4mg, spare；
B, carbopol and glycerine are added in above-mentioned suspension, are uniformly mixed；
C, gram vertical boron sieve, Cortex Pseudolaricis extract and a phellodendron 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 18mg, Cortex Pseudolaricis extract 1.2mg, phellodendron extract 1.2mg, denaturation are formed sediment
Converted starch is dissolved in deionized water and forms suspension by powder 2.5mg, carbopol 1.0mg, glycerine 10mg, spare；
B, carbopol and glycerine are added in above-mentioned suspension, are uniformly mixed；
C, gram vertical boron sieve, Cortex Pseudolaricis extract and a phellodendron 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 70 C is cooling,
Cutting takes off film up to gram vertical boron sieve compound health release membranes.
Embodiment 3
A, gram vertical boron sieve 14mg, Cortex Pseudolaricis extract 0.7mg, phellodendron extract 0.7mg, converted starch 1.7mg, carbopol
0.8mg, glycerine 7mg, 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, Cortex Pseudolaricis extract and a phellodendron 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, 80 DEG C of temperature is cooling,
Cutting takes off film up to gram vertical boron sieve compound health release membranes.
Comparative example 1
A, gram vertical boron sieve 14mg, Cortex Pseudolaricis extract 0.7mg, phellodendron extract 0.7mg, converted starch 1.7mg, glycerine
Converted starch is dissolved in deionized water and forms suspension by 7.8mg, spare；
B, carbopol and glycerine are added in above-mentioned suspension, are uniformly mixed；
C, gram vertical boron sieve, Cortex Pseudolaricis extract and a phellodendron 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, 80 DEG C of temperature is cooling,
Cutting takes off film up to gram vertical boron sieve compound health release membranes.
Comparative example 2
A, gram vertical boron sieve 14mg, Cortex Pseudolaricis extract 0.7mg, phellodendron extract 0.7mg, converted starch 1.7mg, carbopol
0.4mg, glycerine 7mg, 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, Cortex Pseudolaricis extract and a phellodendron 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, 80 DEG C of temperature is cooling,
Cutting takes off film up to gram vertical boron sieve compound health release membranes.
The above is only a preferred embodiment of the present invention, it is noted that for the ordinary skill people of the art
For member, without departing from the technical principles of the invention, several improvement and deformations can also be made, these improvement and deformations
Also it should be regarded as protection scope of the present invention.
Claims (7)
1. a kind of gram vertical boron sieve compound health release membranes, which is characterized in that formed by following raw material proportioning：Gram vertical boron sieve 9-
18mg, Cortex Pseudolaricis extract 0.2-1.2mg, phellodendron extract 0.2-1.2mg, converted starch 1-2.5mg, carbopol 0.6-
1.0mg, glycerine 4-10mg.
2. one kind gram vertical boron sieve compound health release membranes according to claim 1, which is characterized in that by following raw material proportioning
It forms：Gram vertical boron sieve 12-16mg, Cortex Pseudolaricis extract 0.4-1.0mg, phellodendron extract 0.4-1.0mg, converted starch 1.5-
2.0mg, carbopol 0.7-0.9mg, glycerine 5-8mg.
3. one kind gram vertical boron sieve compound health release membranes according to claim 1, which is characterized in that by following raw material proportioning
It forms：Gram vertical boron sieve 14mg, Cortex Pseudolaricis extract 0.7mg, phellodendron extract 0.7mg, converted starch 1.7mg, carbopol
0.8mg, glycerine 7mg.
4. the preparation method of a kind of gram of vertical boron sieve compound health 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, Cortex Pseudolaricis extract and a phellodendron 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 compound health release membranes.
5. the preparation method of a kind of gram of vertical boron sieve compound health release membranes according to claim 4, which is characterized in that native chaste tree
The preparation method of bark extract is, by Golden Larch Bark：Water=1:10, Golden Larch Bark is mixed with water in a reservoir, 90 DEG C is heated to and carries
After taking 2-3h, it is collected by filtration filtrate I and residue I, then by residue I：Water=1:8 extract 2-3h, and filtrate II is collected by filtration, and close
And filtrate I and filtrate II, it is concentrated in vacuo to obtain medicinal extract, then carry out being freeze-dried to obtain Cortex Pseudolaricis extract.
6. the preparation method of a kind of gram of vertical boron sieve compound health release membranes according to claim 4, which is characterized in that Cortex Phellodendri
The preparation method of extract is, by Cortex Phellodendri：Ethyl alcohol=1:10, Cortex Phellodendri is mixed with ethyl alcohol in a reservoir, is heated to 60 DEG C of progress
After 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, are collected by filtration
Filtrate II, merging filtrate I and filtrate II are concentrated in vacuo to obtain medicinal extract, then carry out being freeze-dried to obtain phellodendron extract.
7. the preparation method of a kind of gram of vertical boron sieve compound health 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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| Application Number | Priority Date | Filing Date | Title |
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| CN201810667792.6A CN108524648A (en) | 2018-06-26 | 2018-06-26 | One kind gram vertical boron sieve compound health release membranes and preparation method thereof |
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| CN201810667792.6A CN108524648A (en) | 2018-06-26 | 2018-06-26 | One kind gram vertical boron sieve compound health release membranes and preparation method thereof |
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| CN108524648A true CN108524648A (en) | 2018-09-14 |
Family
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| CN201810667792.6A Pending CN108524648A (en) | 2018-06-26 | 2018-06-26 | One kind gram vertical boron sieve compound health release membranes and preparation method thereof |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20170152273A1 (en) * | 2015-11-30 | 2017-06-01 | Anacor Pharmaceuticals Inc. | Topical Pharmaceutical Formulations For Treating Inflammatory-Related Conditions |
-
2018
- 2018-06-26 CN CN201810667792.6A patent/CN108524648A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20170152273A1 (en) * | 2015-11-30 | 2017-06-01 | Anacor Pharmaceuticals Inc. | Topical Pharmaceutical Formulations For Treating Inflammatory-Related Conditions |
Non-Patent Citations (4)
| Title |
|---|
| JEREMY UDKOFF ET AL.: "Current and emerging topical therapies for atopic dermatitis", 《CLINICS IN DERMATOLOGY》 * |
| 熊力夫: "《野葛研究与栽培利用》", 31 May 2007, 湖南科学技术出版社 * |
| 苗明三等: "《中药大辞典》", 30 June 2017, 山西科学技术出版社 * |
| 陈明岭等: "《皮肤病常用中药药理及临床》", 31 October 2017, 中国科学技术出版社 * |
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Application publication date: 20180914 |