CN107982328A - A kind of Roflumilast solid dispersion preparation - Google Patents
A kind of Roflumilast solid dispersion preparation Download PDFInfo
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- CN107982328A CN107982328A CN201711450287.8A CN201711450287A CN107982328A CN 107982328 A CN107982328 A CN 107982328A CN 201711450287 A CN201711450287 A CN 201711450287A CN 107982328 A CN107982328 A CN 107982328A
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- raw material
- roflumilast
- solid dispersion
- dispersion preparation
- zinc
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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)
- A61K36/73—Rosaceae (Rose family), e.g. strawberry, chokeberry, blackberry, pear or firethorn
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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
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
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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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
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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
- A61K31/28—Compounds containing heavy metals
- A61K31/315—Zinc compounds
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
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- 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
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
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- Oil, Petroleum & Natural Gas (AREA)
- Alternative & Traditional Medicine (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention provides a kind of Roflumilast solid dispersion preparation, is made of following raw material：Zinc gluconate, mometasone furoate, loguat leaf, magnesium stearate, borneol, formoterol fumarate, roflumilast, compared with prior art, the present invention have following beneficial effect：Synthesized by part Western medicine and parts of traditional Chinese medicine, play the effect and cheap of synergy, can promote the use of on a large scale.
Description
Technical field
The present invention is a kind of Roflumilast solid dispersion preparation, belongs to pharmaceutical arts.
Background technology
Asthma is a kind of common disease, frequently-occurring disease, is a kind of important diseases for influencing people's physical and mental health, if treatment is too late
When, it is lack of standardization, asthma may be fatal.The mode of western medical treatment asthma delays symptom by bronchodilators or oxygen uptake more at present
Solution, is not treated for the pathogenic factor of asthma.This palliative mode easily makes one platform and produces dependence
Property and recurrent exerbation suddenly, with patient lifetime, seriously affect patient's normal life.
Roflumilast is a kind of oral selective phosphodiesterase-4 (PDE4) inhibitor of Nycomed companies exploitation,
The medicine of a new chronic obstructive pulmonary disease (COPD) for treating asthma and chronic obstructive pulmonary disease.Roflumilast
Mainly it is expressed in the inflammatory cell related with asthma, including eosinophils, neutrophil leucocyte and mast cell.The medicine can be special
Ground acts on certain enzyme for participating in smooth muscle contraction, can prevent cAMP from degrading, so as to block proinflammatory signal transmission, have
Anti-inflammatory activity, clinically treats asthma and Chronic Obstructive Pulmonary Disease obtains the effect of preferable.Roflumilast can also be obvious
Delay the deterioration of Respiratory symptoms, while be greatly enhanced the quality of life of patient.
The content of the invention
In view of the deficienciess of the prior art, it is an object of the present invention to provide a kind of Roflumilast solid dispersion preparation, with
Solve the problems, such as proposed in the above background technology.
To achieve these goals, the present invention is to realize by the following technical solutions：A kind of roflumilast solid point
Granular media preparation, is made of following raw material：Zinc gluconate, mometasone furoate, loguat leaf, magnesium stearate, borneol, Formoterol
Fumarate, roflumilast.
Further, the leaf of feverfew Blumea balsamifera is taken, through steam distillation, cooling, obtains crystallization Chinese mugwort powder, then the powder that will end
It is refined, obtain the borneol in raw material.
Further, magnesium sulfate is dissolved in the water, dissolving ratio 1:10,55 DEG C are warming up to, and be added slowly to
In the sodium stearate solution of preparation, metathesis reaction is carried out under agitation, and the magnesium stearate for reacting generation is separated out with solid, reaction
After the completion of, standing separates clear liquid, then through washing, centrifugal dehydration, the drying at 80~85 DEG C, up to the stearic acid in raw material
Magnesium.
Further, the leaf of rosaceous plant loquat is taken, is shone in natural light to when doing very likely, is bundled into wisp, then shine
It is dry, dry place's storage is placed on after drying, is put into pulverizer and crushes, 100 mesh sieves of mistake after crushing, sieve to obtain loquat in raw material
Leaf.
Further, the zinc gluconate in raw material is fermented using glucose as raw material with Aspergillus, after separating, purifying
With in zinc oxide or zinc hydroxide and obtaining the zinc gluconate in raw material, or by glucose through air oxidation, then with hydroxide
Sodium solution is converted into sodium gluconate, the gluconic acid solution of high-purity is converted into through storng-acid cation exchange resin, finally
It is made with zinc oxide or zinc hydroxide reaction.
Beneficial effects of the present invention：A kind of Roflumilast solid dispersion preparation of the present invention, by part Western medicine and part
Traditional Chinese medicine synthesizes, and plays the effect and cheap of synergy, can promote the use of on a large scale.
Embodiment
To make the technical means, the creative features, the aims and the efficiencies achieved by the present invention easy to understand, with reference to
Embodiment, the present invention is further explained.
The present invention provides a kind of technical solution：A kind of Roflumilast solid dispersion preparation, is made of following raw material：Grape
Saccharic acid zinc, mometasone furoate, loguat leaf, magnesium stearate, borneol, formoterol fumarate, roflumilast.
The leaf of feverfew Blumea balsamifera is taken, through steam distillation, cooling, obtains crystallization Chinese mugwort powder, then Chinese mugwort powder is refined, is obtained
Borneol in raw material.
Magnesium sulfate is dissolved in the water, dissolving ratio 1:10,55 DEG C are warming up to, and be added slowly to the tristearin prepared
In acid sodium solution, metathesis reaction is carried out under agitation, and the magnesium stearate for reacting generation is separated out with solid, quiet after the completion of reaction
Put and separate clear liquid, then through washing, centrifugal dehydration, the drying at 80~85 DEG C, up to the magnesium stearate in raw material.
The leaf of rosaceous plant loquat is taken, is shone in natural light to when doing very likely, is bundled into wisp, then is dried, after drying
Dry place's storage is placed on, is put into pulverizer and crushes, 100 mesh sieves of mistake after crushing, sieve to obtain loguat leaf in raw material.
Zinc gluconate in raw material is fermented using glucose as raw material with Aspergillus, after separating, purifying with zinc oxide or
In zinc hydroxide and the zinc gluconate in raw material is obtained, or by glucose through air oxidation, then is converted with sodium hydroxide solution
For sodium gluconate, the gluconic acid solution of high-purity is converted into through storng-acid cation exchange resin, finally with zinc oxide or
Zinc hydroxide reaction is made.
As one embodiment of the present of invention：A kind of Roflumilast solid dispersion preparation of the present invention, by part Western medicine
Synthesized with parts of traditional Chinese medicine, play the effect and cheap of synergy, can promote the use of on a large scale.
The basic principles, main features and the advantages of the invention have been shown and described above, for this area skill
For art personnel, it is clear that the invention is not restricted to the details of above-mentioned one exemplary embodiment, and without departing substantially from the present invention spirit or
In the case of essential characteristic, the present invention can be realized in other specific forms.Therefore, in all respects, should all incite somebody to action
Embodiment regards exemplary as, and is non-limiting, the scope of the present invention by appended claims rather than on state
Bright restriction, it is intended that including all changes fallen in the implication and scope of the equivalency of claim in the present invention
It is interior.
Moreover, it will be appreciated that although the present specification is described in terms of embodiments, not each embodiment is only wrapped
Containing an independent technical solution, this narrating mode of specification is only that those skilled in the art should for clarity
Using specification as an entirety, the technical solutions in the various embodiments may also be suitably combined, forms those skilled in the art
It is appreciated that other embodiment.
Claims (5)
- A kind of 1. Roflumilast solid dispersion preparation, it is characterised in that：It is made of following raw material：Zinc gluconate, Mometasone Furoate, loguat leaf, magnesium stearate, borneol, formoterol fumarate, roflumilast.
- A kind of 2. Roflumilast solid dispersion preparation according to claim 1, it is characterised in that：Take feverfew Ai Na Fragrant leaf, through steam distillation, cooling, obtains crystallization Chinese mugwort powder, then Chinese mugwort powder is refined, and obtains the borneol in raw material.
- A kind of 3. Roflumilast solid dispersion preparation according to claim 1, it is characterised in that：Magnesium sulfate is dissolved in In water, dissolving ratio 1:10, be warming up to 55 DEG C, and be added slowly in the sodium stearate solution prepared, under agitation into Row metathesis reaction, the magnesium stearate for reacting generation is separated out with solid, after the completion of reaction, standing separate clear liquid, then through washing, Centrifugal dehydration, the drying at 80~85 DEG C, up to the magnesium stearate in raw material.
- A kind of 4. Roflumilast solid dispersion preparation according to claim 1, it is characterised in that：Take rosaceous plant Pi The leaf of rake, shines to when doing very likely in natural light, is bundled into wisp, then dries, and is placed at dry and stores after drying, is put into powder Crushed in broken machine, 100 mesh sieves are crossed after crushing, sieve to obtain loguat leaf in raw material.
- A kind of 5. Roflumilast solid dispersion preparation according to claim 1, it is characterised in that：Glucose in raw material Sour zinc is fermented using glucose as raw material with Aspergillus, after separating, purifying with zinc oxide or zinc hydroxide and obtain raw material in Zinc gluconate, or by glucose through air oxidation, then with sodium hydroxide solution sodium gluconate is converted into, through highly acid sun Ion exchange resin is converted into the gluconic acid solution of high-purity, is finally made with zinc oxide or zinc hydroxide reaction.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711450287.8A CN107982328A (en) | 2017-12-28 | 2017-12-28 | A kind of Roflumilast solid dispersion preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711450287.8A CN107982328A (en) | 2017-12-28 | 2017-12-28 | A kind of Roflumilast solid dispersion preparation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107982328A true CN107982328A (en) | 2018-05-04 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201711450287.8A Pending CN107982328A (en) | 2017-12-28 | 2017-12-28 | A kind of Roflumilast solid dispersion preparation |
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| Country | Link |
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| CN (1) | CN107982328A (en) |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103565806A (en) * | 2012-07-31 | 2014-02-12 | 江苏柯菲平医药有限公司 | Roflumilast oral preparation and preparation method thereof |
| CN104107173A (en) * | 2014-06-27 | 2014-10-22 | 山东泰田新药开发有限公司 | Roflumilast tablet and preparation method thereof |
| CN106176618A (en) * | 2016-09-18 | 2016-12-07 | 佛山市弘泰药物研发有限公司 | A kind of Roflumilast solid dispersion preparation and preparation method thereof |
-
2017
- 2017-12-28 CN CN201711450287.8A patent/CN107982328A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103565806A (en) * | 2012-07-31 | 2014-02-12 | 江苏柯菲平医药有限公司 | Roflumilast oral preparation and preparation method thereof |
| CN104107173A (en) * | 2014-06-27 | 2014-10-22 | 山东泰田新药开发有限公司 | Roflumilast tablet and preparation method thereof |
| CN106176618A (en) * | 2016-09-18 | 2016-12-07 | 佛山市弘泰药物研发有限公司 | A kind of Roflumilast solid dispersion preparation and preparation method thereof |
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| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20180504 |
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