CN109908097A - Linkou County Mo Fanse collapses sustained release tablets - Google Patents
Linkou County Mo Fanse collapses sustained release tablets Download PDFInfo
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- CN109908097A CN109908097A CN201711326292.8A CN201711326292A CN109908097A CN 109908097 A CN109908097 A CN 109908097A CN 201711326292 A CN201711326292 A CN 201711326292A CN 109908097 A CN109908097 A CN 109908097A
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Abstract
The invention belongs to field of pharmaceutical preparations, and in particular to one kind Linkou County Mo Fanse collapses sustained release tablets.It is invented mainly comprising carrying medicine using blank capsule core coating, and the method being coated through slow release layer prepares carried medicine sustained-release pellet, then oral disintegrating tablet is made through direct powder compression.Its main feature is that being disintegrated after oral fastly, it is suitble to old age children and dysphagia crowd administration, patient's compliance is high, and slow release in vivo, and maintains stable blood concentration, with significant clinical value.
Description
Technical field
The present invention provides a kind of Linkou County Mo Fanse disintegrating tablet with slow releasing function, and one kind is disintegrated rapidly in oral cavity, gulps down
Pharynx is taken, and just has the Mo Fanse forest tract agent of slow releasing function.
Background technique
Whole world parkinsonian about 7 million to one 10,000,000 at present, China just have 2,600,000, rank first in the world, often
Year will also increase by 100,000 neopathy patients.50% or more parkinsonian once had mental symptom (PDP).These spirit
Symptom is mainly shown as illusion and vain hope, and the treatment and tourniquet to parkinsonian carry out bigger challenge.Dopamine is pa
The main target of the gloomy disease treatment of gold, since most of antipsychotics can block dopamine in brain to lead to disturbances in patients with Parkinson disease
Dyskinesia deteriorate, be not suitable for such patient at present.
Mo Fanselin (Pimavanserin), chemical name, 1-(4- luorobenzyl) -3-(4- isobutoxy benzyl) -1-(1-
Methyl piperidine -4- base) urea, Yuan Yanwei Acadia drug company.The reversed and antagonism of Mo Fanselin to 5-HT2A receptor
It is selectively 40 times of 5-HT2C receptor and dopamine receptor with high targeting and specificity.Good effect, specificity is good, keeps away
Exempt from the deterioration of muscular movement, few side effects.Breakthrough treatment status title, April 29 in 2016 are authorized by FDA on 2 9th, 2014
By FDA approval for treat Parkinson illusion and vain hope, current first be also it is only be permitted for treatment Parkinson essence
The drug of refreshing disease.
Oral disintegrating tablet is new formulation developed in recent years, is compared with conventional tablet, which sets without being delivered with water
In that can be disintegrated rapidly on the tip of the tongue, enter stomach by swallowing act and work, is especially suitable for the dysphagias crowd such as old man and children and gives
Medicine.
Parkinson's mental disease is mainly in the elderly, and swallow is weak, and the course of disease is long, needs Long-term taking medicine, is easy to appear leakage
Situation is taken and forgets to take, the present invention provides one kind Linkou County Mo Fanse and collapses sustained release tablets, and said preparation can be not only disintegrated rapidly in oral cavity,
And stable steady release in vivo, it is effectively improved patient's compliance.
Summary of the invention
The present invention provides a kind of Linkou County Mo Fanse disintegrating tablet with slow releasing function, and in particular to Mo Fanselin be live
Property ingredient carried pack clothing and sustained release coating using microcrystalline cellulose as blank capsule core and prepare sustained release pellet, along in oral disintegrating tablet
Acceptable auxiliary material preparation.
Hollow pellet of the present invention uses extrusion spheronization technology, particle size range 0.5mm-0.7mm, and capsule core includes
One or more of microcrystalline cellulose, sugarcane sugar and starch, preferably microcrystalline cellulose and sucrose.
Drug-loaded layer coating solution of the present invention is made of active constituent Mo Fanselin and a kind of coating material, activity at
Dividing with the weight ratio of coating material is 1:1-1:10, preferably 1:3-1:6.
Drug-loaded layer coating of the present invention, is that active constituent is dissolved in coating solution to be coated, used in coating solution
Solvent is water or 50% ethanol solution.
Drug-loaded layer coating material of the present invention by one of ethyl cellulose, hydroxypropyl methylcellulose and povidone or
Several compositions.
Drug-loaded layer coating of the present invention, coating equipment in sugar production line use multifunctional fluidized bed, every 100g blank capsule core drug-loaded layer
Coating weight gain is 30-60g.
Slow release layer coating of the present invention, coating solution used are Aquacoat or Utech NE30D water
Dispersion.
Slow release layer of the present invention is coated, and plasticizer is contained in coating solution used, and the plasticizer is lemon triethylenetetraminehexaacetic acid
One or more of ester, citric acid tri butyl ester and acetyl triethyl citrate.
Slow release layer coating of the present invention, coating equipment in sugar production line is using multifunctional fluidized bed, every 100g load medicine coating of pellets increasing
Weight is 8-30g.
It is lactose, mannitol, microcrystalline cellulose, pregelatinized starch, crosslinking that oral disintegrating tablet of the present invention, which is subjected to auxiliary material,
One or more of sodium carboxymethylcellulose, magnesium stearate.
Detailed description of the invention
Attached drawing 1 is prepared the release profiles that Linkou County Mo Fanse collapses sustained release tablets by embodiment 1.
Attached drawing 2 is prepared the dissolution curve of the Linkou County Mo Fanse disintegrating tablet by comparative example.
Specific embodiment
Technical solution of the present invention is further illustrated combined with specific embodiments below, but does not limit the present invention.
Disintegration time limit test: according to 2015 editions four 0921 disintegration time limit tests of general rule of Chinese Pharmacopoeia, by stainless steel
Pipe is fixed on bracket, is immersed in 1000ml glasss, and the water about 900ml that temperature is 37 DEG C ± 1 DEG C is filled in cup, adjusts height of water level
Sieve is in underwater 15mm ± 1mm when making stainless steel tube lowest order.Start instrument.Take this product 1, set in above-mentioned stainless steel tube into
Row checks, is all disintegrated in Ying 60 seconds and by sieve, if any float or attach in a small amount of lightweight stainless steel inside pipe wall or
Sieve, but without hard-core person, can make to meet the disintegration of regulation opinion mean oral solid formulation under prescribed conditions all disintegration leach or
Sieve should all be passed through in addition to insoluble coating material or broken capsule shells at particle.
Release profiles measuring method: the drug release determination method announced according to FDA, using 0.1M hydrochloric acid as medium, basket method turns
Speed is 100prm, is operated according to methods, and after 12h, with high effective liquid chromatography for measuring release, draws release profiles.
Embodiment 1
Prescription (batch 1000)
Preparation process
(1) weigh recipe quantity microcrystalline cellulose, add appropriate amount of water softwood, extrusion spheronization machine prepares piller, crossed after dry 20 mesh and
30 meshes obtain blank capsule core (0.5-0.7mm).
(2) coating solution is prepared by prescription, weighs blank capsule core 100g, carry out in multifunctional fluidized bed carrying medicine coating weight gain
30g, dry 5min, carries out slow release layer coating weight gain 20g, obtains carried medicine sustained-release pellet.
(3) prescription loading gage medicine pellet, lactose hydrous are weighed, microcrystalline cellulose is mixed with three-dimensional mixer, mixes powder and place
Side's amount magnesium stearate after mixing, presses theoretical slice weight tabletting.
Embodiment 2
Prescription
Preparation process
(1) recipe quantity microcrystalline cellulose and sucrose are weighed, appropriate amount of water softwood is added, extrusion spheronization machine prepares piller, mistake after drying
20 mesh and 30 meshes obtain blank capsule core (0.5-0.7mm).
(2) coating solution is prepared by prescription, weighs blank capsule core 100g, carry out in multifunctional fluidized bed carrying medicine coating weight gain
30g, dry 5min, carries out slow release layer coating weight gain 20g, obtains carried medicine sustained-release pellet.
(3) prescription loading gage medicine pellet is weighed, mannitol, pregelatinized starch, croscarmellose sodium use three-dimensional hybrid
Machine mixes, and mixes powder and recipe quantity magnesium stearate after mixing, by theoretical slice weight tabletting.
Embodiment 3
Prescription (batch 1000)
Preparation process
(1) recipe quantity cornstarch and sucrose are weighed, appropriate amount of water softwood is added, extrusion spheronization machine prepares piller, crosses 20 after dry
Mesh and 30 meshes obtain blank capsule core (0.5-0.7mm).
(2) coating solution is prepared by prescription, weighs blank capsule core 100g, carry out in multifunctional fluidized bed carrying medicine coating weight gain
30g, dry 5min, carries out slow release layer coating weight gain 20g, obtains carried medicine sustained-release pellet.
(3) prescription loading gage medicine pellet, mannitol are weighed, microcrystalline cellulose is mixed with three-dimensional mixer, mixes powder and recipe quantity
Magnesium stearate after mixing, presses theoretical slice weight tabletting.
Comparative example
Prescription (batch 1000)
Preparation process
Recipe quantity Mo Fanselin, mannitol are weighed, microcrystalline cellulose is mixed with three-dimensional mixer, mixes powder and recipe quantity is stearic
Sour magnesium after mixing, presses theoretical slice weight tabletting.
Experimental example
Embodiment 1 and comparative example tablet are carried out disintegration time limited respectively to check and release profiles measurement, as a result such as table 1 and attached
Shown in Fig. 1-2.
According to the experimental results: mouth of the invention collapses sustained release tablets and common oral disintegrating tablet disintegration time limited without significant difference, release
Slowly and stablize, there is significant clinical value.
Claims (10)
1. the Linkou County Mo Fanse collapses sustained release tablets, it is characterised in that blank capsule core is carried out drug-loaded layer coating first and slow release layer is coated
Sustained release pellet is prepared, along with the acceptable auxiliary material of oral disnitegration tablet is prepared by direct tablet compressing technique.
2. blank capsule core according to claim 1, it is characterised in that by one of microcrystalline cellulose, sugarcane sugar and starch or
It is several to be prepared through extrusion spheronization technology.
3. drug-loaded layer coating according to claim 1, it is characterised in that coating solution used is by active constituent Mo Fanselin
It is formed with a kind of coating material, the weight ratio of active constituent and coating material is 1:1-1:10.
4. drug-loaded layer coating according to claim 1, it is characterised in that active constituent is dissolved in coating solution, coating solution
Solvent for use is water or 50% ethanol solution.
5. drug-loaded layer coating according to claim 3, coating material is by ethyl cellulose, hydroxypropyl methylcellulose and povidone
One or more of composition.
6. drug-loaded layer coating according to claim 3, coating equipment in sugar production line is using multifunctional fluidized bed, every 100g blank capsule core load
Medicine layer coating weight gain is 30-60g.
7. slow release layer coating according to claim 1, it is characterised in that coating solution used is Aquacoat
Or Utech NE30D aqueous dispersion.
8. slow release layer coating according to claim 1, it is characterised in that contain plasticizer, the plasticising in coating solution used
Agent is one or more of triethyl citrate, citric acid tri butyl ester and acetyl triethyl citrate.
9. slow release layer coating according to claim 7, coating equipment in sugar production line is using multifunctional fluidized bed, every 100g load medicine pellet packet
Clothing weight gain is 8-30g.
10. mouth according to claim 1 collapses sustained release tablets, it is characterised in that it is cream that the oral disnitegration tablet, which is subjected to auxiliary material,
One or more of sugar, mannitol, microcrystalline cellulose, pregelatinized starch, croscarmellose sodium, magnesium stearate.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711326292.8A CN109908097A (en) | 2017-12-13 | 2017-12-13 | Linkou County Mo Fanse collapses sustained release tablets |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711326292.8A CN109908097A (en) | 2017-12-13 | 2017-12-13 | Linkou County Mo Fanse collapses sustained release tablets |
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| Publication Number | Publication Date |
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| CN109908097A true CN109908097A (en) | 2019-06-21 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201711326292.8A Pending CN109908097A (en) | 2017-12-13 | 2017-12-13 | Linkou County Mo Fanse collapses sustained release tablets |
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Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070264330A1 (en) * | 2006-05-15 | 2007-11-15 | Bo Ragnar-Tolf | Pharmaceutical formulations of pimavanserin |
| CN101500568A (en) * | 2006-05-15 | 2009-08-05 | 阿卡蒂亚药品公司 | Pharmaceutical formulations of pimavanserin |
| CN103054826A (en) * | 2012-12-27 | 2013-04-24 | 北京阜康仁生物制药科技有限公司 | Orally disintegrating tablet of memantine hydrochloride sustained-release pellets and preparation method thereof |
| CN103230379A (en) * | 2013-04-02 | 2013-08-07 | 万特制药(海南)有限公司 | Orally disintegrating sustained-release preparation containing tamsulosin hydrochloride and preparation method thereof |
| CN105326837A (en) * | 2015-10-09 | 2016-02-17 | 北京万全德众医药生物技术有限公司 | Memantine hydrochloride sustained release-donepezil quick release compound capsule |
| CN106265605A (en) * | 2016-09-30 | 2017-01-04 | 天津市聚星康华医药科技有限公司 | A kind of tartaric acid Mo Fanselin oral instant membrane and preparation method thereof |
| CN106606494A (en) * | 2015-10-22 | 2017-05-03 | 天津市汉康医药生物技术有限公司 | Pimavanserin pharmaceutical composition and preparation method thereof |
-
2017
- 2017-12-13 CN CN201711326292.8A patent/CN109908097A/en active Pending
Patent Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070264330A1 (en) * | 2006-05-15 | 2007-11-15 | Bo Ragnar-Tolf | Pharmaceutical formulations of pimavanserin |
| CN101500568A (en) * | 2006-05-15 | 2009-08-05 | 阿卡蒂亚药品公司 | Pharmaceutical formulations of pimavanserin |
| CN103054826A (en) * | 2012-12-27 | 2013-04-24 | 北京阜康仁生物制药科技有限公司 | Orally disintegrating tablet of memantine hydrochloride sustained-release pellets and preparation method thereof |
| CN103230379A (en) * | 2013-04-02 | 2013-08-07 | 万特制药(海南)有限公司 | Orally disintegrating sustained-release preparation containing tamsulosin hydrochloride and preparation method thereof |
| CN105326837A (en) * | 2015-10-09 | 2016-02-17 | 北京万全德众医药生物技术有限公司 | Memantine hydrochloride sustained release-donepezil quick release compound capsule |
| CN106606494A (en) * | 2015-10-22 | 2017-05-03 | 天津市汉康医药生物技术有限公司 | Pimavanserin pharmaceutical composition and preparation method thereof |
| CN106265605A (en) * | 2016-09-30 | 2017-01-04 | 天津市聚星康华医药科技有限公司 | A kind of tartaric acid Mo Fanselin oral instant membrane and preparation method thereof |
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