CN102125524B - Piracetam orally disintegrating tablets - Google Patents

Piracetam orally disintegrating tablets Download PDF

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Publication number
CN102125524B
CN102125524B CN2010100051221A CN201010005122A CN102125524B CN 102125524 B CN102125524 B CN 102125524B CN 2010100051221 A CN2010100051221 A CN 2010100051221A CN 201010005122 A CN201010005122 A CN 201010005122A CN 102125524 B CN102125524 B CN 102125524B
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China
Prior art keywords
piracetam
adjuvant
principal agent
oral cavity
cavity disintegration
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Expired - Fee Related
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CN2010100051221A
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Chinese (zh)
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CN102125524A (en
Inventor
刘均洪
张媛媛
王繁业
吴汝林
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Qingdao University of Science and Technology
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Qingdao University of Science and Technology
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Priority to CN2010100051221A priority Critical patent/CN102125524B/en
Publication of CN102125524A publication Critical patent/CN102125524A/en
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Abstract

The invention discloses piracetam orally disintegrating tablets and a preparation method thereof. The main drug of the piracetam orally disintegrating tablets is piracetam, and the auxiliary materials comprise microcrystalline cellulose, mannitol, lactose, crosslinked polyvinylpyrrolidone, sodium cyclamate, menthol, silica gel micropowder and magnesium stearate. The piracetam orally disintegrating tablets can effectively treat senile dementia, have convenience in taking, good taste, rapid disintegration, quick absorption and high bioavailability, and provide convenience for patients with senile dementia who have inconvenience in taking medicine.

Description

A kind of piracetam oral cavity disintegration tablet
One, technical field
The present invention relates to a kind of oral drug preparation of treating senile dementia, particularly relate to the good piracetam oral cavity disintegration tablet of a kind of disintegrate rapidly, release and mouthfeel.
Two, background technology
Piracetam is the brain metabolism improving medicine, belongs to the annular derivant of r aminobutyric acid, can promote ATP in the brain, can promote the synthetic conduction that is also just strengthening neural excitation of acetylcholine, has the effect of the brain of promotion intracellular metabolite.Can resist by the injury of brain function due to physical factor, the chemical factor, the strong prestige of the antidromicity due to the anoxia had improved action, can hypermnesis, improve learning capacity.Being used to treat senile dementia clinically, is a line medicine of treatment senile dementia.
Aging trend lets alzheimer disease patient quantity increase, and China will get into aging society, and very important problem of simultaneous---the sickness rate of senile dementia is increasing year by year.
Investigation is found: the mean age that northern China is suffered from senile dementia is 75,76 years old, and the ratio of suffering from senile dementia among the over-65s crowd reaches more than 17%.
Senile dementia patient's activity of daily living descends, and they are not familiar with spouse, children, wears the clothes, has a meal, defecation all can not take care of oneself the inconvenience of particularly taking medicine; The auditory hallucination hallucination in addition that has brings endless misery and worried for people own and on every side.Senile dementia patient's mean survival time (MST) is 5.5 years, and senile dementia has become " the fourth-largest killer " of aged health after cardiovascular diseases, cerebrovascular and cancer.
The piracetam formulation that has gone on the market abroad at present has common oral preparation and two kinds of dosage forms of injection.But many senile dementia patients all have the problem of the difficulty of taking medicine, so the ordinary tablet dosage form is used very inconvenience for the patient of the difficulty of taking medicine.Injection needs medical personnel to inject, and the patient is in and uses inconvenience.Oral cavity disintegration tablet can not need water or only need use low amounts of water, need not to chew, and tablet places lingual surface, after the rapid disintegrate of chance saliva, borrows and swallows power, and medicine can absorb onset rapidly.Compare with conventional tablet, oral cavity disintegration tablet has the following advantages: 1. absorption is fast, bioavailability is high.2. taking convenience: oral cavity disintegration tablet needn't be used water delivery service, and saliva can make its disintegrate or dissolving, can swallow by common dose, can be placed in the water again to take after the disintegrate, can also not need to take medicine with water swallow.Be particularly useful for the inconvenient senile dementia patient that takes medicine.3. intestinal is residual few, and the low medicine of side effect arrives the gastrointestinal tract rapid disintegrate of ability before and is dispersed into trickle granule, causes medicine to distribute in the gastrointestinal tract large tracts of land, and absorption point increases, thereby has reduced medicine to the gastrointestinal local excitation.4. avoid the first pass effect of liver: because oral cavity disintegration tablet rapidly disintegrate in mouth except that major part gets into the gastrointestinal tract with swallowing act, also has the considerable part trans-oral to absorb, thereby rapid-action, first pass effect is little.
Oral cavity disintegration tablet develops by its distinct feature rapidly, becomes the emphasis of tablet exploitation.Oral cavity disintegration tablet is applicable to old people and child's oral medication, especially for the patient of dysphagia, has more suitable use advantage, thereby has found a kind of way of solution for the quality of life of improving patient.
Three, summary of the invention
The object of the present invention is to provide a kind of taking convenience, mouthfeel is good, and disintegrate is rapid, absorbs fast piracetam oral cavity disintegration tablet and preparation method thereof.
The object of the invention can be realized through following measure:
The piracetam oral cavity disintegration tablet comprises principal agent and adjuvant, it is characterized in that principal agent and adjuvant are formulated by following percentage by weight: principal agent 15%-33%, adjuvant 67%-85%.
Principal agent of the present invention is a piracetam, molecular formula: C 6H 10N 2O 2, molecular weight: 140.16.
Principal agent of the present invention and adjuvant are formulated by following percentage by weight:
A. piracetam 15-33%
B. microcrystalline Cellulose 10-30%
C. mannitol 20-55%
D. lactose 10-25%
E. anhydrous citric acid 0.5-1.0%
F. crospolyvinylpyrrolidone 3-10%
G. cyclamate 0.75-2%
H. menthol 0.1-1%
I. micropowder silica gel 0.5-2.5%
J. magnesium stearate 0.2-0.9%
Wherein lactose, mannitol are filler; Microcrystalline Cellulose, crospolyvinylpyrrolidone are disintegrating agent, and wherein microcrystalline Cellulose also has lubricated and disintegration concurrently, and anhydrous citric acid, cyclamate and menthol are correctives; Micropowder silica gel is a fluidizer, and magnesium stearate is as lubricant.
2. the method for preparing of piracetam oral cavity disintegration tablet according to claim 1 comprises raw material pulverizing, weighing mixing, sheeting process.It is characterized in that, comprise following concrete processing step:
Step 1: with piracetam and various adjuvant pulverize separately, cross 40 mesh sieves then, preserve subsequent use respectively;
Step 2: take by weighing principal agent and the various adjuvant that step 1 is produced by principal agent and accessory formula, and with its abundant mix homogeneously; Step 3: the mixed uniformly material of step 2 is sent into tablet machine, carry out direct powder compression.
The invention has the advantages that:
(1) the present invention fills a prescription rationally, and each adjuvant is cheap and easy to get, and good with the principal agent compatibility, preparation technology is simple, is applicable to large-scale industrial production;
(2) the piracetam oral cavity disintegration tablet disintegrate that the present invention relates to is rapid, mouthfeel good, and the no grittiness that enters the mouth and cool taste do not have other uncomfortable taste yet;
(3) piracetam oral cavity disintegration tablet taking convenience of the present invention can effectively be treated senile dementia.Convenience is provided for the senile dementia patient of the inconvenience of taking medicine.
Below in conjunction with specific embodiment the present invention is further described.
The specific embodiment
Embodiment 1
The piracetam oral cavity disintegration tablet comprises principal agent and adjuvant, it is characterized in that by following percentage by weight formulated: principal agent 25%, adjuvant 75%.
Piracetam 100g (25%)
Microcrystalline Cellulose 75g (18.75%)
Mannitol 120g (30%)
Lactose 78g (19.5%)
Anhydrous citric acid 2.25g (0.56%)
Crospolyvinylpyrrolidone 11.25g (2.81%)
Cyclamate 4.5g (1.13%)
Menthol 3.75g (0.94%)
Micropowder silica gel 3.75g (0.94%)
Magnesium stearate 1.5g (0.37%)
Make 1000 altogether
Wherein lactose, mannitol are filler, and microcrystalline Cellulose, crospolyvinylpyrrolidone are disintegrating agent, and anhydrous citric acid, cyclamate and menthol are correctives, and magnesium stearate is a lubricant, and micropowder silica gel is a fluidizer.
The method for preparing of piracetam oral cavity disintegration tablet of the present invention comprises raw material pulverizing, weighing mixing, sheeting process.It is characterized in that concrete processing step is following:
Step 1: with piracetam and various adjuvant pulverize separately, cross 40 mesh sieves then, preserve subsequent use respectively;
Step 2: take by weighing principal agent and the various adjuvant that step 1 is produced by principal agent and accessory formula, and with its abundant mix homogeneously;
Step 3: the component that step 2 mixes is sent into conventional tablet machine, carry out direct powder compression, make sheet and heavily be the piracetam oral cavity disintegration tablet of 400mg.
Result of the test:
Tablet hardness: 33 ± 5N
Disintegration: 19~28s
Disintegrate in intraoral disintegration time limit and mouthfeel: the 40S, no grittiness, cool taste does not have uncomfortable taste embodiment 2
The piracetam oral cavity disintegration tablet comprises principal agent and adjuvant, it is characterized in that by following percentage by weight formulated: principal agent 31.25%, adjuvant 68.75%.
Piracetam 125g (31.25%)
Microcrystalline Cellulose 50g (12.5%)
Mannitol 150g (37.5%)
Lactose 45g (11.25%)
Anhydrous citric acid 2.25g (0.56%)
Crospolyvinylpyrrolidone 15g (3.75%)
Cyclamate 3g (0.75%)
Menthol 3g (0.75%)
Micropowder silica gel 4.5g (1.13%)
Magnesium stearate 2.25g (0.56%)
Make 1000 altogether
Pyrrole of the present invention draws the method for preparing of two smooth oral cavity disintegration tablets with embodiment 1, makes sheet and heavily is the piracetam oral cavity disintegration tablet of 400mg.
Result of the test:
Tablet hardness: 32 ± 5N
Disintegration: 14~27s
Disintegrate in intraoral disintegration time limit and mouthfeel: the 40S, no grittiness, cool taste does not have uncomfortable taste
Embodiment 3
The piracetam oral cavity disintegration tablet comprises principal agent and adjuvant, it is characterized in that by following percentage by weight formulated: principal agent 18.75%, adjuvant 81.25%.
Piracetam 75g (18.75%)
Microcrystalline Cellulose 105g (26.25%)
Mannitol 100.25g (25.06%)
Lactose 84.875g (21.22%)
Anhydrous citric acid 3g (0.75%)
Crospolyvinylpyrrolidone 18.75g (4.69%)
Cyclamate 3.75g (0.94%)
Menthol 0.375g (0.094%)
Micropowder silica gel 6g (1.5%)
Magnesium stearate 3g (0.75%)
Make 1000 altogether
The method for preparing of piracetam oral cavity disintegration tablet of the present invention makes sheet and heavily is the piracetam oral cavity disintegration tablet of 400mg with embodiment 1.
Result of the test:
Tablet hardness: 36 ± 5N
Disintegration: 19~33s
Disintegrate in intraoral disintegration time limit and mouthfeel: the 40S, no grittiness, cool taste does not have uncomfortable taste.
The piracetam oral cavity disintegration tablet disintegrate that the present invention relates to is rapid, mouthfeel good, and the no grittiness that enters the mouth and cool taste do not have other uncomfortable taste yet; Can effectively treat senile dementia, convenience is provided for the senile dementia patient of the inconvenience of taking medicine.

Claims (2)

1. piracetam oral cavity disintegration tablet; Comprise principal agent and adjuvant; It is characterized in that principal agent is a piracetam, adjuvant is microcrystalline Cellulose, mannitol, lactose, anhydrous citric acid, crospolyvinylpyrrolidone, cyclamate, menthol, micropowder silica gel, magnesium stearate; Described principal agent and adjuvant are prepared by following quality:
Piracetam 100g, microcrystalline Cellulose 75g, mannitol 120g, lactose 78g, anhydrous citric acid 2.25g, crospolyvinylpyrrolidone, 11.25g, cyclamate 4.5g, menthol 3.75g, micropowder silica gel 3.75g, magnesium stearate 1.5 g make 1000;
The method for preparing of said piracetam oral cavity disintegration tablet comprises raw material pulverizing, weighing mixing, sheeting process, and concrete processing step is following:
Step 1: with piracetam and various adjuvant pulverize separately, cross 40 mesh sieves then, preserve subsequent use respectively;
Step 2: take by weighing principal agent and the various adjuvant that step 1 is produced by principal agent and accessory formula, and with its abundant mix homogeneously;
Step 3: the mixed uniformly material of step 2 is sent into tablet machine, carry out direct powder compression.
2. piracetam oral cavity disintegration tablet; Comprise principal agent and adjuvant; It is characterized in that principal agent is a piracetam, adjuvant is microcrystalline Cellulose, mannitol, lactose, anhydrous citric acid, crospolyvinylpyrrolidone, cyclamate, menthol, micropowder silica gel, magnesium stearate; Described principal agent and adjuvant are prepared by following quality:
Piracetam 125g, microcrystalline Cellulose 50g, mannitol 150g, lactose 45g, anhydrous citric acid 2.25g, crospolyvinylpyrrolidone 15g, cyclamate 3g, menthol 3g, micropowder silica gel 4.5g, magnesium stearate 2.25 g make 1000;
The method for preparing of said piracetam oral cavity disintegration tablet comprises raw material pulverizing, weighing mixing, sheeting process, and concrete processing step is following:
Step 1: with piracetam and various adjuvant pulverize separately, cross 40 mesh sieves then, preserve subsequent use respectively;
Step 2: take by weighing principal agent and the various adjuvant that step 1 is produced by principal agent and accessory formula, and with its abundant mix homogeneously;
Step 3: the mixed uniformly material of step 2 is sent into tablet machine, carry out direct powder compression.
CN2010100051221A 2010-01-16 2010-01-16 Piracetam orally disintegrating tablets Expired - Fee Related CN102125524B (en)

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CN102125524B true CN102125524B (en) 2012-06-27

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Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104546682A (en) * 2014-12-25 2015-04-29 海南卫康制药(潜山)有限公司 Piracetam composition freeze-dried tablets and preparation method thereof
CN106727898B (en) * 2017-02-21 2020-07-31 阮时宝 Pharmaceutical composition for preventing and treating Alzheimer disease and preparation method thereof
CN111297818B (en) * 2020-04-02 2022-02-22 常州制药厂有限公司 High-drug-loading-capacity piracetam tablet composition and preparation method thereof
CN112022816B (en) * 2020-07-31 2022-08-12 河北君临药业有限公司 Piracetam tablet and preparation method thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1663563A (en) * 2005-02-04 2005-09-07 北京阜康仁生物制药科技有限公司 Compound troxerutin and piracetam formulation and application thereof
CN101274013A (en) * 2007-03-27 2008-10-01 高海 Prescription medicine for curing senile dementia and preparation

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1663563A (en) * 2005-02-04 2005-09-07 北京阜康仁生物制药科技有限公司 Compound troxerutin and piracetam formulation and application thereof
CN101274013A (en) * 2007-03-27 2008-10-01 高海 Prescription medicine for curing senile dementia and preparation

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Granted publication date: 20120627

Termination date: 20130116