CN104997736B - A kind of aniracetam granule - Google Patents
A kind of aniracetam granule Download PDFInfo
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- CN104997736B CN104997736B CN201510405421.7A CN201510405421A CN104997736B CN 104997736 B CN104997736 B CN 104997736B CN 201510405421 A CN201510405421 A CN 201510405421A CN 104997736 B CN104997736 B CN 104997736B
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- aniracetam
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- polyethylene glycol
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Abstract
A kind of aniracetam granule, containing aniracetam, polyethylene glycol, hydroxypropyl cellulose, is prepared by the following method：Aniracetam, polyethylene glycol heating melting, this fused solution is added in the ethanol solution of hydroxy propyl cellulose, stirred, finally this suspension is pharmaceutically pelletized on acceptable filler.Compared with prior art, dissolution of the present invention is rapid.
Description
Technical field
The invention belongs to pharmaceutical technology field, and in particular to a kind of aniracetam granule.
Background technology
Aniracetam (Aniracetam), its chemical name are 1- (4- methoxybenzenes acyl group) -2-Pyrrolidone, molecular formula
For C12H13NO3, molecular weight 219.24.Aniracetam (Aniracetam) was ground in 1978 by Roche companies of Switzerland
Work(is made, has successively applied for patent in states such as West Europe, Spain, South Africa.In 1988, the product was by Japanese Roche companies
Listed jointly in Japan registration with company of Fuji.
Aniracetam is gamma-lactam class cerebral function improving medicine of new generation, and it is the reinforcing agent of brain function metabolism.It can be with
By blood-brain barrier, for selectively acting in central nervous system-hippocampus, hippocampus is the transformation of short time recall info, the master of storage
Position is wanted, aniracetam with activation, protection and recovers nerve cell effect to brain cell metabolism.Learning ability and note can be strengthened
Recall function, and can shields to injury of brain function.Zoopery proves, note of the aniracetam to normal rat discrimination learning
Recalling reproducing processes has good facilitation, can be to hypomnesia caused by anti anoxia.
This product is for the headache after cerebral hemorrhage, cerebral infarction, TIA, encephalitis and cerebral concussion, cerebral contusion, head
The brain disorders such as dizzy, extremity numbness, weak, dyscoimesis have improvement result.Particularly to the memory after cranial vascular disease
The hypomnesia of decline, the hypomnesia of person in middle and old age's property, neurasthenia symptom, mental disease and other mentally disturbeds has notable treatment
Effect.This product oral absorption is good, and side effect is less, is safer cerebral function improving medicine.Can be as the prevention of senile dementia
And medicine for treatment.
Adverse reaction occasionally has dry, drowsiness, is disappeared after drug withdrawal.Sometimes may occur in which excitement, headache, nose heave, dizziness, delirium,
Insomnia, sleepy, anxiety etc..Sometimes belch, vomiting, diarrhoea, poor appetite, stomachache etc..Sometimes fash, itch etc. be may occur in which.Have
When may occur in which anaemia.Sometimes GOT, GPT, ALP rise etc..Sometimes BUN is raised.Sometimes Blushing, tinnitus be may occur in which.
After this product oral absorption, peak time is 20~40min in blood, half life 22min, is mainly distributed on stomach and intestine
Road, kidney, liver, brain and blood.Blood concentration measure by difficulty after 4h.After 24h, 71%~85% in urine by discharging, and 4% from excrement
Discharge.Main metabolites are in urine：N- N anisoyl GABAs and 5- hydroxy-2-pyrrolidinones.
The content of the invention
In view of the shortcomings of the prior art, the present invention is screened by lot of experiments to auxiliary material and process optimization, plan provide a kind of
The aniracetam granule of the rapid dissolution of energy.
Specifically, the present invention is realized by following technology：
Aniracetam granule of the present invention, containing aniracetam, polyethylene glycol, hydroxypropyl cellulose, by as follows
Method is prepared：Aniracetam, polyethylene glycol heating melting, this fused solution is added to the ethanol solution of hydroxy propyl cellulose
In, stir, finally this suspension is pharmaceutically pelletized on acceptable filler, produced.
The weight ratio of described aniracetam granule, aniracetam and polyethylene glycol is 1:6-9；Preferably, weight ratio
For 1:8.
The weight ratio of described aniracetam granule, aniracetam and hydroxypropyl cellulose is 1:15-20；Preferably,
Weight ratio is 1:19.
Described aniracetam granule, described filler are the one or more in lactose, mannitol, sucrose.
Compared with prior art, drug-eluting of the present invention is rapid.
Embodiment
Following examples further describe beneficial effects of the present invention, and embodiment is only used for the purpose of illustration, do not limit this
The scope of invention, while obvious change and modification that those of ordinary skill in the art are made according to the present invention are also contained in
Within the scope of the invention.
Embodiment 1
Preparation technology：
Aniracetam, Macrogol 4000 heat melting at 80 DEG C, and this fused solution is added to the hydroxypropyl of recipe quantity
In the ethanol solution of cellulose, stir, finally this suspension is pelletized on lactose, 50 DEG C of dryings, 16 mesh sieve whole grains, sieve
Point, pack and produce.
Embodiment 2
Preparation technology：
Aniracetam, Macrogol 4000 heat melting at 70 DEG C, and this fused solution is added to the hydroxypropyl of recipe quantity
In the ethanol solution of cellulose, stir, finally this suspension is pelletized on mannitol, 60 DEG C of dryings, 14 mesh sieve whole grains,
Screening, packs and produces.
Embodiment 3
Preparation technology：
Aniracetam, Macrogol 4000 heat melting at 70 DEG C, and this fused solution is added to the hydroxypropyl of recipe quantity
In the ethanol solution of cellulose, stir, finally this suspension is pelletized on sucrose, 60 DEG C of dryings, 14 mesh sieve whole grains, sieve
Point, pack and produce.
Comparative example 1
Preparation technology：
Recipe quantity weighed the aniracetam of 200 mesh sieves, Macrogol 4000 is added to the hydroxypropyl cellulose of recipe quantity
Ethanol solution in, stir, finally this suspension pelletized on sucrose, 60 DEG C of dryings, 14 mesh sieve whole grains, sieve, bag
Fill and produce.
Comparative example 2
Preparation technology：
1. according to said medicine formula, citric acid is added in 95% ethanol solution, stirring and dissolving, is configured to include
The mass volume ratio of liquid, citric acid and 95% ethanol is 0.5:100；
2. aniracetam is crossed into 100-120 mesh sieves, insert in boiling-bed drying, inclusion liquid sprayed into the state of boiling,
Dried at 45-55 DEG C, be prepared into aniracetam acidity inclusion compound；
3. aniracetam acidity inclusion compound, lactose, copolyvidone, PVPP, magnesium stearate are well mixed, add
In tablet press machine loading hopper, tabletting is carried out by the way of pressed powder, is pressed into 0.105g aniracetam tablet.
Verify embodiment
Dissolution determination takes this product, according to dissolution method (《Chinese Pharmacopoeia》The second methods of C of two annex of version in 2010 Ⅹ),
Using hydrochloric acid solution (9 → 1000) 900mL as solvent, rotating speed 75rmin-1, operate in accordance with the law, during through 5,15,30min, take solution
10mL, filtration, takes subsequent filtrate 5mL, is placed in 50mL measuring bottles, add hydrochloric acid solution (9 → 1000) to be diluted to scale, shake up, as
Need testing solution.The another aniracetam reference substance being dried under reduced pressure to constant weight of learning from else's experience is appropriate, accurately weighed, add hydrochloric acid solution (9 →
1000) dissolve and dilute and be made containing about 10 μ g solution in every 1mL, as reference substance solution.Take above two solution, photograph is ultraviolet
AAS (《Chinese Pharmacopoeia》Two A of annex IV of version in 2010), trap is determined respectively at 286nm wavelength, is calculated
The stripping quantity of every, limit are the 80% of labelled amount, should meet regulation.
Each embodiment measurement result of table 1
| Embodiment | 5min dissolution rates (%) | 15min dissolution rates (%) | 30min dissolution rates (%) |
| Embodiment 1 | 99.7 | 99.9 | 99.9 |
| Embodiment 2 | 99.7 | 100.1 | 100.1 |
| Embodiment 3 | 99.9 | 100.1 | 100.1 |
| Comparative example 1 | 67.7 | 84.4 | 99.9 |
| Comparative example 2 | 51.5 | 70.2 | 89.4 |
As seen from the table, dissolution of the embodiment of the present invention is rapid；Comparative example 1, polyethylene glycol is added, but do not melt system
Grain, dissolution are more of the invention slow；Comparative example 2, the tablet dissolution of preparation are slow.
Claims (4)
1. a kind of aniracetam granule, it is characterised in that containing aniracetam, polyethylene glycol, hydroxypropyl cellulose, by as follows
Method is prepared：Aniracetam, polyethylene glycol heating melting, this fused solution is added to the ethanol solution of hydroxy propyl cellulose
In, stir, finally this suspension is pharmaceutically pelletized on acceptable filler, produced；Aniracetam and poly- second two
The weight ratio of alcohol is 1:6-9；The weight of aniracetam and hydroxypropyl cellulose ratio is 1:15-20.
2. aniracetam granule according to claim 1, it is characterised in that the weight of aniracetam and polyethylene glycol ratio
For 1:8.
3. aniracetam granule according to claim 1, it is characterised in that the weight of aniracetam and hydroxypropyl cellulose
Amount is than being 1:19.
4. aniracetam granule according to claim 1, it is characterised in that described filler be lactose, mannitol,
One or more in sucrose.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510405421.7A CN104997736B (en) | 2015-07-11 | 2015-07-11 | A kind of aniracetam granule |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510405421.7A CN104997736B (en) | 2015-07-11 | 2015-07-11 | A kind of aniracetam granule |
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| Publication Number | Publication Date |
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| CN104997736A CN104997736A (en) | 2015-10-28 |
| CN104997736B true CN104997736B (en) | 2018-02-23 |
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| CN201510405421.7A Active CN104997736B (en) | 2015-07-11 | 2015-07-11 | A kind of aniracetam granule |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1634039A (en) * | 2004-11-10 | 2005-07-06 | 鲁南制药股份有限公司 | Aniracetam drop pills |
| EP2604592A1 (en) * | 2011-12-12 | 2013-06-19 | Zaklady Farmaceutyczne Polpharma SA | A process for the purification of aniracetam by crystallisation from aqueous solutions |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3018318B2 (en) * | 1997-08-29 | 2000-03-13 | 富山化学工業株式会社 | Fast disintegrating solid preparation |
| CN103860502B (en) * | 2014-04-15 | 2015-12-30 | 张绪伟 | A kind of tablet containing moxonidine hydrochloride and preparation method thereof |
-
2015
- 2015-07-11 CN CN201510405421.7A patent/CN104997736B/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1634039A (en) * | 2004-11-10 | 2005-07-06 | 鲁南制药股份有限公司 | Aniracetam drop pills |
| EP2604592A1 (en) * | 2011-12-12 | 2013-06-19 | Zaklady Farmaceutyczne Polpharma SA | A process for the purification of aniracetam by crystallisation from aqueous solutions |
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| Publication number | Publication date |
|---|---|
| CN104997736A (en) | 2015-10-28 |
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