CN108785263A - The solid composite medicament and preparation method thereof of Pramipexole or its pharmaceutical salts - Google Patents
The solid composite medicament and preparation method thereof of Pramipexole or its pharmaceutical salts Download PDFInfo
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- CN108785263A CN108785263A CN201810376240.XA CN201810376240A CN108785263A CN 108785263 A CN108785263 A CN 108785263A CN 201810376240 A CN201810376240 A CN 201810376240A CN 108785263 A CN108785263 A CN 108785263A
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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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/428—Thiazoles condensed with carbocyclic rings
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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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
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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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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Abstract
The present invention relates to Pramipexole or the solid composite medicaments and preparation method thereof of its pharmaceutical salts.Specifically, solid composite medicament of the present invention contains Pramipexole or its pharmaceutical salts or its solvate as active constituent, also contain sustained-release matrix material, synthos and other excipient.The solid composite medicament has good dissolution rate and stability, still has good release behavior under the conditions of high temperature and humidity.
Description
Technical field
The invention belongs to medicinal chemistry art, be related to a kind of composition of pramipexole or its pharmaceutical salts solid composite medicament and
Preparation method.
Background technology
Parkinson's disease is a kind of common nervous system degeneration disease slowly carried out for betiding the middle-aged and the old.It is clinical
Using static tremor, myotonia and dyskinesia as main feature.With the process of population aging, illness rate increases year by year
It is high.For a long time, the drug replacement therapy based on levodopa is the preferred option for the treatment of of Parkinson disease.But patient is long
Phase often leads to curative effect using levodopa and declines, and will appear the fluctuation to reaction, such as " agent end phenomenon ", " on-off phenomenon ",
And motor complication, such as dyskinesia, myodystony.
Pramipexole, chemical name (S) -2- amino -4,5,6,7,-tetrahydrochysene -6- (propylcarbamic) benzothiazole, structure is as above
It is shown, be a kind of non-ergot class dopamine-receptor stimulant, can effectively exciting dopamine D 2 subgroup receptor, wherein to D3 receptors
Affinity be higher than D2 or D4 receptors, can be used for treating Parkinson's disease, and early application Pramipexole can delay compared with levodopa
Above-mentioned side reaction, and the life quality of patient can be improved.1997, the pramipexole immediate release piece of Bo Lingeyinggehan companiesIt is listed in the U.S., for treating Parkinson's disease, which must daily three times.In order to simplify dosage regimen,
Patient's compliance is improved, the side effect that blood concentration fluctuation is brought is reduced, Boehringer Ingelheim further developed once a day
Sustained-release tablet And it was listed in the U.S. in 2010.
CN101005830B discloses a kind of extended release dosage system of Pramipexole and preparation method thereof, the sustained release preparation packet
Water-swellable polymer containing at least two non-pregelatinized starch, and at least one is for anionic water swelling polymer and extremely
A kind of few neutral water swelling polymer of non-pregelatinized starch.Wherein, anionic water swelling polymer is pH relevant slow
Framework material is released, and the 0.25-25% that content is sustained release preparation total weight, the neutral water swelling polymerization of non-pregelatinized starch
Object is the unrelated sustained-release matrix materials of pH, and content is 10-75%.The sustained release preparation by two different principles obtain with
The relevant or unrelated different release rates of pH value.The oral slow-releasing preparation can treat patient symptom by daily single, to
Improve the convenience and compliance of patient.But using the anionic water swelling polymer of weight described in the patent as pH value
Relevant sustained-release matrix material, the preparation stability of preparation is poor, is postponed in high temperature or super-humid conditions decentralization, release behavior meeting
It varies widely.
CN101005831B is disclosed comprising at least one pregelatinized starch, a kind of anionic polymer and the third is water-soluble
The Pramipexole extended release tablet and preparation method thereof of swollen property polymer.The invention preparation it is anionic water swelling
The content of polymer is similarly the 0.25-25% of total weight, and after the placement of high humidity hot conditions, there is also release behavior generations
The phenomenon that change.This unstability can cause the risk of patient medication process, and increase and wanted to drug packages and storage
It asks, difficulty is caused to commercially producing for preparation.
It is an object of the invention to overcome the deficiencies of the prior art and provide a kind of general with good dissolution rate and stability
Clarke rope solid composite medicament.Further, the present invention optimizes anionic water by the type of preferred sustained-release matrix material
The content of swelling polymer, improves the release performance and stability of sustained release preparation, and has been surprisingly found that and one is added in the formulation
Quantitative synthos can significantly improve stability of preparation under the conditions of high temperature and humidity, to reduce to packing and storing up
The requirement deposited more closes commercially producing for preparation, and ensure that safety of patient during medication.
Invention content
The object of the present invention is to provide a kind of Pramipexole solid composite medicaments, and the composition is in high temperature and humidity item
It is placed under part, still can keep 2 hourly average releasing ratios within the scope of 12-32% in the phosphate buffer of pH6.8,9
For hourly average releasing ratio within the scope of 42-62%, 24 hourly average releasing ratios are not less than 70% good release behavior,
Reduce the pharmaceutical composition risk affected by environment for causing releasing effect to change in use, improves drug safety
Stability reduces pharmaceutical preparation and commercially produces requirement with storage requirement.
The present invention provides a kind of solid composite medicaments, contain active ingredient pramipexole or its pharmaceutical salts or its solvent
Close object, synthos and sustained release framework material.
In some embodiments, the active constituent of the solid composite medicament is Pramipexole or its pharmaceutical salts or salt
Solvate, the pharmaceutical salts be selected from hydrochloride, sulfate, hydrobromate, citrate, hydriodate, phosphate, nitre
Hydrochlorate, benzoate, mesylate, benzene sulfonate, 2- isethionates, tosilate, acetate, propionate, grass
Hydrochlorate, malonate, succinate, glutarate, adipate, tartrate, maleate, fumarate, malic acid
Salt and mandelate, preferably hydrochloride, more preferable dihydrochloride, the most preferably form of dihydrochloride monohydrate.
Further, the content of the active constituent is the 0.05-10%, preferably 0.05- in terms of pharmaceutical composition weight
7%, more preferable 0.05-5%, most preferably 0.05-3%.
" synthos " of the present invention refer to using calcium ion as metal ion, to be selected from phosphate radical (PO4 3-), phosphoric acid
One hydrogen radical (HPO4 2-) and dihydrogen phosphate (H2PO4 -) compound of the anion as acid ion, it is organic to may also include its
Solvate and hydrate.
In some embodiments, synthos of the present invention are selected from calcium phosphate dibasic anhydrous, calcium monohydrogen phosphate two is hydrated
Object and calcium phosphate, preferably calcium phosphate dibasic anhydrous and dicalcium phosphate dihydrate, most preferably dicalcium phosphate dihydrate.
Further, the content of the synthos is the 1.0-30%, preferably 2.0- in terms of pharmaceutical composition weight
20%, more preferable 2.0-10%, most preferably 2.0-5.0%.
In some example schemes, sustained-release matrix material of the present invention polymerize comprising at least two water-swellables
Object, one of which are anionic polymer chosen from the followings：Acrylate copolymer, methacrylate polymer, methacrylic acid
Copolymer, alginate, carrageenan, Arabic gum, xanthans, chitosan, carmethose, carboxymethylcellulose calcium, it is excellent
Select alginate；Another kind is neutral polymer chosen from the followings：Alkylcellulose, hydroxy alkyl cellulose, hydroxyalkyl alkyl are fine
Tie up element, hydroxy alkyl cellulose ester, disaccharides, oligosaccharide and polysaccharide, polyvinyl alcohol, polyvinylpyrrolidone, polyvinylpyrrolidone
With the copolymer of vinylacetate, the combination of polyvinyl alcohol and polyvinylpyrrolidone, polyalkylene oxide, preferably polyoxyethylene or
Polyvinyl alcohol.
In some example schemes, the content of anionic polymer of the present invention is in terms of pharmaceutical composition weight
25-80%, preferably 30-60%, more preferable 30-50%, most preferably 30-40%.
In some example schemes, the content of neutral polymer of the present invention is in terms of pharmaceutical composition weight
10-80%, preferably 20-60%, more preferable 30-60%, most preferably 40-60%.
In some example schemes, sustained-release matrix material of the present invention includes sodium alginate and polyoxyethylene or gathers
Vinyl alcohol it is one or more.
In one embodiment, sustained-release matrix material includes sodium alginate and polyoxyethylene.
In another embodiment, sustained-release matrix material includes sodium alginate and polyvinyl alcohol.
Further, the sodium alginate at 20 DEG C in the solution of 1% weight with about 100 to 1000mPas it is viscous
Degree, preferably 200 to 800mPas viscosity, more preferable 300 to 600mPas, most preferably 400 to 600mPas.
Further, the polyoxyethylated molecular weight ranges are about 900,000 dalton to 7,000,000 dalton,
It is preferred that 1,000,000 dalton to 7,000,000 dalton, more preferable 4,000,000 dalton to 7,000,000 dalton,
Most preferably 5,000,000 dalton are to 7,000,000 dalton.
Further, the molecular weight ranges of the polyvinyl alcohol are about 10,000 dalton to 3,000,000 dalton, excellent
Select 20,000 dalton to 2,000,000 dalton, more preferable 30,000 dalton to 1,000,000 dalton, most preferably
30,000 dalton to 500,000 dalton.
In some embodiments, preparation of the invention is also optionally including other excipient, you can pharmaceutical formulation
With medicament, in order to improve the preparative of said preparation, compactibility, appearance and hide.These preparations medicament includes for example, dilute
Release agent or filler, glidant, adhesive, granulating agent, anti-caking agent, lubricant, fragrance, coloring agent preservative.It may also include
Other conventional excipients known in the art.
It also may include one or more lubricants in solid composite medicament provided by the invention, contribute to tabletting.Lubrication
Agent can be selected from talcum powder, magnesium stearate, zinc stearate, Compritol 888 ATO, NaLS, hydrogenated vegetable oil, colloid two
Silica etc., preferably magnesium stearate.
Further, the content of the lubricant is 0.5%~2% in terms of pharmaceutical composition weight.
" in terms of pharmaceutical composition weight " of the present invention is that the label weight meter not comprising coating agent calculates active constituent
Or the usage amount numberical range of other type pharmaceutic adjuvants.
In embodiments of the invention, the solid composite medicament consists of the following compositions：
In one embodiment, the sustained release preparation consists of the following compositions：
In another embodiment, the sustained release preparation consists of the following compositions：
It is another object of the present invention to provide a kind of method preparing above-mentioned solid composite medicament, the method is
Direct powder compression.
It in some embodiments, can be by active constituent, synthos, slow when being made using direct powder compression
Release framework material and the tabletting after mixing of other excipient.
Description of the drawings
Fig. 1 shows that the tablet of embodiment 1 to 6 originates the release profiles in pH6.8 phosphate buffers.
After the tablet starting and the placement of temperature 60 C condition of Fig. 2 display embodiments 2 in pH6.8 phosphate buffers
Release profiles.
After the tablet starting and the placement of temperature 60 C condition of Fig. 3 display comparative examples 2 in pH6.8 phosphate buffers
Release profiles.
After the tablet starting and the placement of temperature 60 C condition of Fig. 4 display comparative examples 7 in pH6.8 phosphate buffers
Release profiles.
In pH6.8 phosphate after the tablet starting of Fig. 5 display embodiments 2 and 25 DEG C of temperature, the placement of RH92.5% conditions
Release profiles in buffer solution.
In pH6.8 phosphate after the tablet starting of Fig. 6 display comparative examples 2 and 25 DEG C of temperature, the placement of RH92.5% conditions
Release profiles in buffer solution.
In pH6.8 phosphate after the tablet starting of Fig. 7 display comparative examples 4 and 25 DEG C of temperature, the placement of RH92.5% conditions
Release profiles in buffer solution.
In pH6.8 phosphate after the tablet starting of Fig. 8 display comparative examples 5 and 25 DEG C of temperature, the placement of RH92.5% conditions
Release profiles in buffer solution.
In pH6.8 phosphate after the tablet starting of Fig. 9 display comparative examples 6 and 25 DEG C of temperature, the placement of RH92.5% conditions
Release profiles in buffer solution.
In pH6.8 phosphate after the tablet starting of Figure 10 display comparative examples 7 and 25 DEG C of temperature, the placement of RH92.5% conditions
Release profiles in buffer solution.
In pH6.8 phosphate after the tablet starting of Figure 11 display comparative examples 8 and 25 DEG C of temperature, the placement of RH92.5% conditions
Release profiles in buffer solution.
Specific implementation mode
The present invention is explained in greater detail below with reference to embodiment, the embodiment of the present invention is merely to illustrate the skill of the present invention
Art scheme, the spirit and scope of the invention are not limited thereto.
Embodiment 1-3：
Body of Pramipexole dihydrochloride, sodium alginate, polyoxyethylene, calcium monohydrogen phosphate, magnesium stearate are used in the ratio in table 1
Rotation always mixes direct tablet compressing after machine is mixed.
Table 1
Embodiment 4-6:
Body of Pramipexole dihydrochloride, sodium alginate, polyvinyl alcohol, calcium monohydrogen phosphate, magnesium stearate are used in the ratio in table 2
Rotation always mixes direct tablet compressing after machine is mixed.
Table 2
Comparative example 1-3:
By body of Pramipexole dihydrochloride, hydroxypropyl methylcellulose, cornstarch, Carbopol 941, colloidal silicon dioxide, magnesium stearate,
In the ratio in table 3, direct tablet compressing after the machine that always mixed using rotation is mixed.
Table 3
Comparative example 4-6:
Material is weighed by the prescription in table 4, direct tablet compressing after machine is mixed always is mixed using rotation.
Table 4
Comparative example 7~8
It is total mixed using rotation in the ratio in table 5 by body of Pramipexole dihydrochloride, sodium alginate, polyoxyethylene, magnesium stearate
Direct tablet compressing after machine is mixed.
Table 5
Experimental example 1-6：Tablet starting dissolution experiment
According to 2015 editions four general rules, 0,931 first methods of Chinese Pharmacopoeia, using pH6.8 phosphate buffers as dissolution medium,
And dissolution test is carried out at 37 ± 0.5 DEG C.The result shows that：The sustained release preparation of Examples 1 to 6, starting all have good release
Clearance is that 2 hourly average releasing ratios are within the scope of 12-32%, and 9 hourly average releasing ratios are within the scope of 42-62%, 24
Hourly average releasing ratio is not less than 70%.Releasing curve diagram is shown in Fig. 1.
Stability study under the conditions of 60 DEG C
By embodiment 2, comparative example 2 and the exposed tablet of comparative example 7, it is placed in 60 DEG C of baking ovens after placing 1 week, 3 weeks, adopts
With 2015 editions four general rules, 0,931 first methods of Chinese Pharmacopoeia, using pH6.8 phosphate buffers as dissolution medium, determination sample
Release profiles after placement.The result shows that：After comparative example 2 places 1 week, 3 weeks in 60 DEG C of baking ovens, release significantly reduces.Than
After placing 1 week, 3 weeks in 60 DEG C of baking ovens compared with example 7, release slightly reduces.
After embodiment 2 places 1 week, 3 weeks in 60 DEG C of baking ovens, release and start-up phase ratio, no significant changes still have good
Good release behavior, 2 hourly average releasing ratios are within the scope of 12-32%, and 9 hourly average releasing ratios are in 42-62% ranges
Interior, 24 hourly average releasing ratios are not less than 70%, are somebody's turn to do the result shows that solid composite medicament provided by the invention is in high temperature item
Stablize under part, also illustrates that adding synthos in prescription is conducive to solid composite medicament and keeps stable under the high temperature conditions.It releases
Putting curve graph sees Fig. 2 to Fig. 4.
25 DEG C, stability study under the conditions of RH92.5%
By embodiment 2, comparative example 2 and comparative example 4 to the exposed tablet of comparative example 8, it is placed in 25 DEG C, under the conditions of RH92.5%
After placing 1 week, 3 weeks, using 2015 editions four general rules, 0,931 first methods of Chinese Pharmacopoeia, using pH6.8 phosphate buffers as molten
Go out medium, measures the release profiles of sample after placing.The result shows that：Comparative example 2 and comparative example 4 are to comparative example 6, in 60 DEG C of bakings
After being placed 1 week, 3 weeks in case, release significantly increases.Comparative example 7 and comparative example 8, after being placed 1 week, 3 weeks in 60 DEG C of baking ovens,
Release slightly increases.
After embodiment 2 places 1 week, 3 weeks under the conditions of 25 DEG C, RH92.5%, release and start-up phase ratio, without significantly change
Change, still there is good release behavior, within the scope of 12-32%, 9 hourly average releasing ratios exist 2 hourly average releasing ratios
Within the scope of 42-62%, 24 hourly average releasing ratios are not less than 70%.It should be the result shows that solid drugs group provided by the invention
It closes object under conditions of high humidity equally to stablize, also illustrates that adding synthos in prescription similarly serves to favor solid composite medicament in height
It keeps stablizing under the conditions of wet.Releasing curve diagram is shown in Fig. 5 to Figure 11.
Claims (14)
1. a kind of solid composite medicament contains active ingredient pramipexole or its pharmaceutical salts or its solvate, synthos
With sustained release framework material, the content of the preferably described synthos is 1.0-30%, preferably 2.0- in terms of pharmaceutical composition weight
20%, more preferable 2.0-10%, most preferably 2.0-5.0%.
2. solid composite medicament as described in claim 1, it is characterised in that the synthos be selected from calcium phosphate dibasic anhydrous,
Dicalcium phosphate dihydrate and calcium phosphate, preferably calcium phosphate dibasic anhydrous and dicalcium phosphate dihydrate, most preferably calcium monohydrogen phosphate two
Hydrate.
3. solid composite medicament as described in claim 1, it is characterised in that the sustained-release matrix material includes at least two
Water-swellable polymer, one of which are anionic polymer chosen from the followings：Acrylate copolymer, methacrylic polymeric
Object, methacrylic acid copolymer, alginate, carrageenan, Arabic gum, xanthans, chitosan, carmethose, carboxylic
Methylcellulose calcium, preferably alginate；Another kind is neutral polymer chosen from the followings：Alkylcellulose, hydroxy alkyl cellulose,
Hydroxyalkylalkylcellulose, hydroxy alkyl cellulose ester, disaccharides, oligosaccharide and polysaccharide, polyvinylpyrrolidone, gather polyvinyl alcohol
The copolymer of vinylpyrrolidone and vinylacetate, the combination of polyvinyl alcohol and polyvinylpyrrolidone, polyalkylene oxide, preferably
Polyoxyethylene or polyvinyl alcohol, more preferable polyoxyethylene.
4. solid composite medicament as described in claim 1, it is characterised in that the sustained-release matrix material includes at least two
Water-swellable polymer, one of which is anionic polymer, and the content of the anionic polymer is with pharmaceutical composition
The 25-80% of weight meter, preferably 30-60%, more preferable 30-50%, most preferably 30-40%；Another kind is neutral polymer, and
The content of the neutral polymer is 10-80%, preferably 20-60%, the more preferable 30-60% in terms of pharmaceutical composition weight,
Most preferably 40-60%.
5. solid composite medicament as described in claim 1, it is characterised in that the content of active constituent is with pharmaceutical composition
The 0.05-10% of weight meter, preferably 0.05-7%, more preferable 0.05-5%, most preferably 0.05-3%.
6. the solid composite medicament as described in any one of claim 1 to 7, it is characterised in that also contain lubricant, it is described
Lubricant is selected from talcum powder, magnesium stearate, zinc stearate, Compritol 888 ATO, NaLS, hydrogenated vegetable oil, colloid
Silica etc., preferably magnesium stearate.
7. solid composite medicament as claimed in claim 6, it is characterised in that the content of lubricant is with pharmaceutical composition weight
The 0.5-2% of gauge.
8. the solid composite medicament as described in any one of claim 1 to 7, by following weight percents at grouping
At：
9. the solid composite medicament as described in any one of claim 1 to 7, by following weight percents at grouping
At：
10. a kind of such as claim 1-9 any one of them solid composite medicaments, it is characterised in that at 37 ± 0.5 DEG C,
Keep 2 hourly average releasing ratios within the scope of 12-32% in the phosphate buffer of pH6.8.
11. solid composite medicament as claimed in claim 10, it is characterised in that at 37 ± 0.5 DEG C, the phosphate of pH6.8
9 hourly average releasing ratio of dissolution rate is within the scope of 42-62% in buffer solution.
12. such as the solid composite medicament of claim 10 to 11 any one of them, it is characterised in that at 37 ± 0.5 DEG C,
24 hourly average releasing ratios are not less than 70% in the phosphate buffer of pH6.8.
13. a kind of method preparing any one of claim 1-12 solid composite medicaments, the method is that powder is direct
Pressed disc method.
14. claim 1-12 any one of them solid composite medicament is being prepared for treating the use in anti-parkinson drug
On the way.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109700777A (en) * | 2019-02-27 | 2019-05-03 | 中国药科大学 | A kind of pH dependent form drug hydrophobic framework sustained release tablets and preparation method thereof |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101005831A (en) * | 2004-08-13 | 2007-07-25 | 贝林格尔·英格海姆国际有限公司 | Extended release tablet formulation containing pramipexole or a pharmaceutically acceptable salt thereof |
| WO2012002644A2 (en) * | 2010-07-02 | 2012-01-05 | Hyundai Pharm Co., Ltd. | Sustained-release pharmaceutical composition containing pramipexole or pharmaceutically acceptable salt thereof with improved stability |
| CN103040780A (en) * | 2013-01-04 | 2013-04-17 | 杭州朱养心药业有限公司 | Rapidly disintegrating pramipexole tablet drug composition and preparation method thereof |
| CN103520128A (en) * | 2013-10-12 | 2014-01-22 | 石家庄杏林锐步医药科技有限公司 | Pramipexole sustained-release tablet, preparation method and application thereof |
| CN104367562A (en) * | 2013-08-15 | 2015-02-25 | 上海星泰医药科技有限公司 | Pramipexole dihydrochloride slow-release tablets and preparation method thereof |
-
2018
- 2018-04-25 CN CN201810376240.XA patent/CN108785263B/en active Active
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101005831A (en) * | 2004-08-13 | 2007-07-25 | 贝林格尔·英格海姆国际有限公司 | Extended release tablet formulation containing pramipexole or a pharmaceutically acceptable salt thereof |
| CN101884626A (en) * | 2004-08-13 | 2010-11-17 | 贝林格尔.英格海姆国际有限公司 | The prolongation release tablet, the Preparation Method And The Use that comprise pramipexole or its officinal salt |
| WO2012002644A2 (en) * | 2010-07-02 | 2012-01-05 | Hyundai Pharm Co., Ltd. | Sustained-release pharmaceutical composition containing pramipexole or pharmaceutically acceptable salt thereof with improved stability |
| CN103040780A (en) * | 2013-01-04 | 2013-04-17 | 杭州朱养心药业有限公司 | Rapidly disintegrating pramipexole tablet drug composition and preparation method thereof |
| CN104367562A (en) * | 2013-08-15 | 2015-02-25 | 上海星泰医药科技有限公司 | Pramipexole dihydrochloride slow-release tablets and preparation method thereof |
| CN103520128A (en) * | 2013-10-12 | 2014-01-22 | 石家庄杏林锐步医药科技有限公司 | Pramipexole sustained-release tablet, preparation method and application thereof |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109700777A (en) * | 2019-02-27 | 2019-05-03 | 中国药科大学 | A kind of pH dependent form drug hydrophobic framework sustained release tablets and preparation method thereof |
| CN109700777B (en) * | 2019-02-27 | 2021-06-22 | 中国药科大学 | PH-dependent drug hydrophobic skeleton sustained-release tablet and preparation method thereof |
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| CN108785263B (en) | 2021-06-29 |
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