CN108066295A - Oxiracetam oral disnitegration tablet and preparation method thereof - Google Patents
Oxiracetam oral disnitegration tablet and preparation method thereof Download PDFInfo
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- CN108066295A CN108066295A CN201611004164.7A CN201611004164A CN108066295A CN 108066295 A CN108066295 A CN 108066295A CN 201611004164 A CN201611004164 A CN 201611004164A CN 108066295 A CN108066295 A CN 108066295A
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- oxiracetam
- disintegrant
- solid dispersions
- oral disnitegration
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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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
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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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
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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
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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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
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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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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Abstract
The present invention provides a kind of Oxiracetam oral disnitegration tablet, by containing Oxiracetam solid dispersions 0.8~14%, filler 55~70%, disintegrant 8~25%, lubricant 1~5%, corrigent 0.1~1% is made；Can under the conditions of anhydrous (or the only a small amount of water presence) fater disintegration in oral cavity, enter alimentary canal with swallowing act, internal behavior is consistent with conventional tablet, is very suitable for the patient of dysphagia.Oxiracetam oral disnitegration tablet of the present invention, formula is reasonable, effectively solves drug hygroscopicity and causes material in pelletization easily agglomerating by force, material is sticked in granulation pot wall, cause the non-uniform technical problem of particle, particle fine uniform after wet granulation, angle of repose is between 25~35, it is preferable into graininess and compressibility, it is in good taste, no grittiness, 15min interior energies dissolution more than 80%, it improves patient and takes compliance, there is higher practical value.
Description
Technical field
The present invention relates to Oxiracetams, and in particular to a kind of Oxiracetam oral disnitegration tablet and preparation method thereof.
Background technology
Oxiracetam (Oxiracetam), chemical name are -2 oxo-1-pyrrolidine ethanamide of 4- hydroxyls.Research shows
It can promote the synthesis of Phosphorylcholine and phosphatidyl ethanolamine, promote brain metabolism, through blood-brain barrier to specific nervous centralis road
There is stimulation on road, the neurological functional recovery of patient is acted on it is apparent, to light moderate vascular dementia, senile dementia and each
The curative effect of disease such as kind cerebrovascular disease, cerebral injury, intracranial infection are preferable.Its structure is as follows：
It is studied on oxiracetam preparation, focuses primarily upon oral formulations and injection (comprising freeze drying powder injection) two sides
Face.Injection, directly quickly enters human body, the protection of no human body normal physiological barrier, if therefore dosage is improper or injection is too fast,
Or drug quality endangers it is possible that being brought to patient there are problem or even causes the consequence that can not be retrieved；In addition injection pain
When bitterly, cannot generate scleroma and intravenous injection by patient's self-administer, injection site to cause vascular inflammation being all clinical practice
There are the problem of.Oral formulations (such as conventional tablet, capsule, sustained-release and controlled release piece, dispersible tablet), take, carry, transport and store
It deposits all more convenient.However Oxiracetam is primarily directed to the more low patient of intelligence, and, this kind of patient in the majority with the elderly
Usually for drug dysphagia, oxiracetam capsule agent is taken, conventional tablet is inconvenient.
Oral disnitegration tablet, can under the conditions of anhydrous in oral cavity fater disintegration, enter alimentary canal, internal row with swallowing act
To be consistent with conventional tablet.Compared with ordinary preparation, have it is convenient to take, absorb that fast, bioavilability is high, alimentary canal mucous membrane is pierced
Swash the advantages that property is small, receive significant attention.Chinese patent CN101766595A discloses a kind of levo-oxiracetam Orally disintegrating
Piece is made using auxiliary materials such as levo-oxiracetam raw material, sodium carboxymethyl starch, croscarmellose sodiums by adhesive of water.
It is found when repeating the patent, since levo-oxiracetam water solubility is fabulous, hygroscopicity is strong, and material holds in wet-granulation process
It is easily agglomerating, while most of material is sticked in granulation pot wall, is caused particle uneven, is increased the difficulty of granulation, it is difficult to obtain
Uniformly mixed and relatively narrow particle diameter distribution particle, and compressibility is poor, is unfavorable for preparation production.
The content of the invention
The defects of in order to overcome the prior art, according in a first aspect, it is an object of the invention to provide a kind of Oxiracetams
Oral disnitegration tablet.
Unless otherwise specified, number of the present invention is parts by weight, and the percentage is mass percent.
The object of the present invention is achieved like this：
A kind of Oxiracetam oral disnitegration tablet contains active ingredient and pharmaceutically acceptable required excipient；The work
Property ingredient be Oxiracetam solid dispersions, the excipient include filler, disintegrant, lubricant or/and corrigent.
An embodiment according to the present invention, above-mentioned Oxiracetam oral disnitegration tablet contain Oxiracetam solid dispersions
0.8~14%, filler 55~70%, disintegrant 8~25%, lubricant 1~5%, corrigent 0.1~1%.
An embodiment according to the present invention, above-mentioned Oxiracetam solid dispersions are by Oxiracetam, carrier and solvent
It is made；The carrier for succinic acid, beta-cyclodextrin, Macrogol 6000, polyvinylpyrrolidone, lactose, PLURONICS F87,
The mixing of one or more of hydroxypropyl cellulose；The solvent is absolute ethyl alcohol, 95% ethyl alcohol, acetone, dichloromethane, acetic acid
The mixing of one or more of ethyl ester.
An embodiment according to the present invention, above-mentioned Oxiracetam solid dispersions are made by solvent method.
In order to improve the dissolution efficiency of Oxiracetam oral disnitegration tablet, an embodiment according to the present invention, above-mentioned Austria
La Xitan solid dispersions are made by 1 part of Oxiracetam, 1~12 part of carrier and 15~80 parts of solvents by solvent method.
An embodiment according to the present invention, above-mentioned Oxiracetam solid dispersions are by 1 part of Oxiracetam, 1~8 part of amber
Amber acid and 15~50 parts of absolute ethyl alcohols are made by solvent method.
Or
An embodiment according to the present invention, above-mentioned Oxiracetam solid dispersions by 1 part of Oxiracetam, 3~12 parts
PLURONICS F87 and 30~80 parts of acetone are made by solvent method.
An embodiment according to the present invention, above-mentioned filler for cornstarch, amylum pregelatinisatum, microcrystalline cellulose,
The mixing of one or more of medicinal calcium carbonate, mannitol.
An embodiment according to the present invention, above-mentioned disintegrant is dried starch, sodium carboxymethyl starch, low substituted hydroxy-propyl
The mixing of one or more of cellulose, crosslinked polyvinylpyrrolidone, croscarmellose sodium.
An embodiment according to the present invention, above-mentioned lubricant are magnesium stearate, superfine silica gel powder, talcum powder, hydrogenation plant
The mixing of one or more of object oil.
An embodiment according to the present invention, above-mentioned corrigent for Sucralose, xylitol, acesulfame potassium, Aspartame,
The mixing of one or more of essence.
In order to control the disintegration time limited of Oxiracetam oral disnitegration tablet, an embodiment according to the present invention is above-mentioned to fill out
Agent is filled for one or more compositions in amylum pregelatinisatum, microcrystalline cellulose, mannitol；Disintegrant low substituted hydroxy-propyl fiber
The mixture of one or both plain, in crosslinked polyvinylpyrrolidone.
An embodiment according to the present invention, above-mentioned filler is amylum pregelatinisatum and mannitol mixture, wherein can
Pressure property starch：Weight ratio=1~3 of mannitol:1；Above-mentioned disintegrant is low-substituted hydroxypropyl cellulose and crosslinked polyethylene pyrrole
The mixture of pyrrolidone, wherein low-substituted hydroxypropyl cellulose：The weight ratio of crosslinked polyvinylpyrrolidone is 2~5:1.
Or
An embodiment according to the present invention, above-mentioned filler are amylum pregelatinisatum, microcrystalline cellulose and mannitol
Mixture, wherein amylum pregelatinisatum：Microcrystalline cellulose：Weight ratio=1~2 of mannitol:2~3：1；Above-mentioned disintegrant takes to be low
For hydroxypropyl cellulose and the mixture of crosslinked polyvinylpyrrolidone, wherein low-substituted hydroxypropyl cellulose：Crosslinked polyethylene
The weight ratio of pyrrolidones is 1~3:1.
Or
An embodiment according to the present invention, above-mentioned filler is microcrystalline cellulose and mannitol mixture, wherein micro-
Crystalline cellulose：Weight ratio=2~5 of mannitol:1；Above-mentioned disintegrant is low-substituted hydroxypropyl cellulose and crosslinked polyethylene pyrrole
The mixture of pyrrolidone, wherein low-substituted hydroxypropyl cellulose：The weight ratio of crosslinked polyvinylpyrrolidone is 2~3:1.
To further enhance the production compliance of the present invention, an embodiment according to the present invention, above-mentioned Oxiracetam
Oral disnitegration tablet contains active ingredient and pharmaceutically acceptable required excipient；The active ingredient is Oxiracetam solid
Dispersion, the excipient include filler, disintegrant, lubricant or/and corrigent；The Oxiracetam solid dispersions by
1 part of Oxiracetam, 1~8 part of succinic acid and 20~50 parts of absolute ethyl alcohols are made by solvent method；The filler is amylum pregelatinisatum
And mannitol mixture, wherein amylum pregelatinisatum：Weight ratio=1~3 of mannitol:1；The disintegrant is low substituted hydroxy-propyl
The mixture of cellulose and crosslinked polyvinylpyrrolidone, wherein low-substituted hydroxypropyl cellulose：Crosslinked polyvinylpyrrolidone
Weight ratio be 2~5:1；The lubricant is superfine silica gel powder；The corrigent is Sucralose or Aspartame.
To further enhance the production compliance of the present invention, an embodiment according to the present invention, above-mentioned Oxiracetam
Oral disnitegration tablet contains active ingredient and pharmaceutically acceptable required excipient；The active ingredient is Oxiracetam solid
Dispersion, the excipient include filler, disintegrant, lubricant or/and corrigent；The Oxiracetam solid dispersions by
1 part of Oxiracetam, 1~8 part of succinic acid and 20~40 parts of absolute ethyl alcohols are made by solvent method；The filler forms sediment for compressibility
Powder, microcrystalline cellulose and mannitol mixture, wherein amylum pregelatinisatum：Microcrystalline cellulose：Weight ratio=1~2 of mannitol:2
~3：1；The disintegrant is low-substituted hydroxypropyl cellulose and the mixture of crosslinked polyvinylpyrrolidone, wherein low substitution hydroxyl
Propyl cellulose：The weight ratio of crosslinked polyvinylpyrrolidone is 1~3:1；The lubricant is superfine silica gel powder；The corrigent
For Aspartame.
For the production compliance of the enhancing present invention, an embodiment according to the present invention, above-mentioned Oxiracetam oral cavity collapses
Piece is solved, contains active ingredient and pharmaceutically acceptable required excipient；The active ingredient is Oxiracetam solid dispersions,
The excipient includes filler, disintegrant, lubricant or/and corrigent；The Oxiracetam solid dispersions are by 1 part of Aura
Western smooth, 3~12 parts of PLURONICS F87s and 40~60 parts of acetone are made by solvent method；The filler is microcrystalline cellulose and sweet
Reveal alcohol mixture, wherein microcrystalline cellulose：Weight ratio=2~5 of mannitol:1；The disintegrant is low substituted hydroxy-propyl fiber
The mixture of element and crosslinked polyvinylpyrrolidone, wherein low-substituted hydroxypropyl cellulose：The weight of crosslinked polyvinylpyrrolidone
Amount is than being 2~3:1；The lubricant is superfine silica gel powder；The corrigent is Sucralose.
According to second aspect, it is an object of the invention to provide the preparation methods of above-mentioned Oxiracetam oral disnitegration tablet.It should
Method is added in filler, disintegrant, lubricant or/and corrigent tabletting and is made with Oxiracetam solid dispersions.
An embodiment according to the present invention, the preparation method of Oxiracetam oral disnitegration tablet, using following steps：
(1) solid dispersions are prepared
Oxiracetam in solvent, stirs 5~25min with carrier uniform dissolution, and recycling design dry, pulverize, and crosses 100
Mesh sieve is to get solid dispersions.
(2) preparation of oral disnitegration tablet
By obtained Oxiracetam solid dispersions addition filler, 30~60% disintegrant (the disintegrant total amount of sieving
30~60%), be wetting agent with absolute ethyl alcohol, wet granulation crosses 100 mesh sieves, 30~45 DEG C of dryings, and whole grain adds in residue and collapses
Agent and corrigent and lubricant are solved, it is tabletted.
An embodiment according to the present invention, the preparation method of above-mentioned Oxiracetam oral disnitegration tablet, using following step
Suddenly：
(1), solid dispersions are prepared
1 part of Oxiracetam and 1~8 part of succinic acid uniform dissolution stir 5~25min in 20~50 parts of absolute ethyl alcohols, use
Rotary Evaporators recycling design, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves and disperses to get solid
Body.
(2), the preparation of oral disnitegration tablet
Oral disnitegration tablet contains Oxiracetam solid dispersions 0.8~14%, filler 55~70%, and disintegrant 8~
25%, lubricant 1~5%, corrigent 0.1~1%；Specifically preparation process is：The Oxiracetam solid that sieving obtains is disperseed
Body adds in filler, 40~50% disintegrant (the 40~50% of disintegrant total amount), is wetting agent with absolute ethyl alcohol, wet method system
Grain crosses 100 mesh sieves, 30~45 DEG C of dryings, and whole grain adds in remaining disintegrant and corrigent and lubricant, tabletted.
Advantageous effect：
It, can be under the conditions of anhydrous (or only a small amount of water presence) the present invention provides a kind of Oxiracetam oral disnitegration tablet
The fater disintegration in oral cavity enters alimentary canal with swallowing act, and internal behavior is consistent with conventional tablet, is very suitable for dysphagia
Patient.The present invention uses Oxiracetam solid dispersions to be prepared as active ingredient and pharmaceutically acceptable required excipient
Oxiracetam oral disnitegration tablet effectively solves Oxiracetam bulk pharmaceutical chemicals hygroscopicity and causes material in pelletization easy by force
Agglomerating, material is sticked in granulation pot wall, causes the non-uniform technical problem of particle, Oxiracetam oral disnitegration tablet has been effectively ensured
Produce compliance.
Oxiracetam oral disnitegration tablet prepared by the present invention, formula is reasonable, effectively solves drug hygroscopicity and makes by force
Material is easily agglomerating into pelletization, and material is sticked in granulation pot wall, causes the non-uniform technical problem of particle, wet granulation
Particle fine uniform afterwards, angle of repose is preferable into graininess and compressibility between 25~35, the hardness of the disintegrated tablet of preparation 30~
40N, the basic disintegration of 35s disintegrations is complete in oral cavity, in good taste, no grittiness, and 15min interior energies dissolution more than 80% need not
Special producing condition has production cost low, carries, stores, transports and take convenient feature, improve patient and take compliance
Property, there is higher practical value.
Embodiment
The present invention is specifically described below by embodiment, it is necessary to which indicated herein is that following embodiment is only used
It is further described in the present invention, it is impossible to be interpreted as limiting the scope of the invention, person skilled in art can
Some nonessential modifications and adaptations are made to the present invention according to the invention described above content.The raw materials used in the present invention and reagent are equal
For commercial product.
First, oral disnitegration tablet prepares embodiment
Embodiment 1
(1), solid dispersions are prepared
1 part of Oxiracetam and 1~8 part of succinic acid uniform dissolution stir 5~25min in 20~50 parts of absolute ethyl alcohols, use
Rotary Evaporators recycling design, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves and disperses to get solid
Body.
(2), the preparation of oral disnitegration tablet
Oral disnitegration tablet contains 0.8~14% Oxiracetam solid dispersions, 55~70% fillers (amylum pregelatinisatum and
Mannitol mixture, wherein amylum pregelatinisatum：Weight ratio=1~3 of mannitol:1), 8~25% disintegrant (low-substituted hydroxypropyl
The mixture of base cellulose and crosslinked polyvinylpyrrolidone, wherein low-substituted hydroxypropyl cellulose：Crosslinked polyethylene pyrrolidines
The weight ratio of ketone is 2~5:1), 1~5% lubricant (superfine silica gel powder), 0.1~1% corrigent (Sucralose or A Siba
Sweet tea)；
Specifically preparation process is：
By obtained Oxiracetam solid dispersions addition filler, 40~50% disintegrant (the disintegrant total amount of sieving
40~50%), be wetting agent with absolute ethyl alcohol, wet granulation crosses 100 mesh sieves, 30~45 DEG C of dryings, and whole grain adds in residue and collapses
Agent and corrigent and lubricant are solved, it is tabletted.
Embodiment 2
(1), solid dispersions are prepared
1 part of Oxiracetam and 1~8 part of succinic acid uniform dissolution stir 5~25min in 20~40 parts of absolute ethyl alcohols, use
Rotary Evaporators recycling design, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves and disperses to get solid
Body.
(2), the preparation of oral disnitegration tablet
Oral disnitegration tablet contains 0.8~14% Oxiracetam solid dispersions, 55~70% fillers (amylum pregelatinisatum,
Microcrystalline cellulose and mannitol mixture, wherein amylum pregelatinisatum：Microcrystalline cellulose：Weight ratio=1~2 of mannitol:2~3：
1), 8~25% disintegrants (low-substituted hydroxypropyl cellulose and the mixture of crosslinked polyvinylpyrrolidone, wherein low substitution hydroxyl
Propyl cellulose：The weight ratio of crosslinked polyvinylpyrrolidone is 1~3:1), 1~5% lubricant (superfine silica gel powder), 0.1~
1% corrigent (Aspartame)；
Specifically preparation process is：
By obtained Oxiracetam solid dispersions addition filler, 40~50% disintegrant (the disintegrant total amount of sieving
40~50%), be wetting agent with absolute ethyl alcohol, wet granulation crosses 100 mesh sieves, 30~45 DEG C of dryings, and whole grain adds in residue and collapses
Agent and corrigent and lubricant are solved, it is tabletted.
Embodiment 3
(1), solid dispersions are prepared
1 part of Oxiracetam and 3~12 parts of PLURONICS F87 uniform dissolutions stir 5~25min in 40~60 parts of acetone,
With Rotary Evaporators recycling design, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves to get solid point
Granular media.
(2), the preparation of oral disnitegration tablet
Oral disnitegration tablet contains 0.8~14% Oxiracetam solid dispersions, 55~70% fillers (microcrystalline cellulose and
Mannitol mixture, wherein microcrystalline cellulose：Weight ratio=2~5 of mannitol:1), 8~25% disintegrant (low-substituted hydroxypropyl
The mixture of base cellulose and crosslinked polyvinylpyrrolidone, wherein low-substituted hydroxypropyl cellulose：Crosslinked polyethylene pyrrolidines
The weight ratio of ketone is 2~3:1), 1~5% lubricant (superfine silica gel powder), 0.1~1% corrigent (Sucralose)；It is specific to prepare
Process is：
By obtained Oxiracetam solid dispersions addition filler, 40~50% disintegrant (the disintegrant total amount of sieving
40~50%), be wetting agent with absolute ethyl alcohol, wet granulation crosses 100 mesh sieves, 30~45 DEG C of dryings, and whole grain adds in residue and collapses
Agent and corrigent and lubricant are solved, it is tabletted.
Embodiment 4
(1) preparation of solid dispersions:
By 10g Oxiracetams and 50g succinic acids uniform dissolution in 350mL absolute ethyl alcohols, 20~22min is stirred, with rotation
Turn evaporimeter recycling design, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves and consolidates to get Oxiracetam
Body dispersion.
(2) preparation of oral disnitegration tablet:
The obtained Oxiracetam solid dispersions (8g) of step (1) sieving are added in into filler (amylum pregelatinisatum 45g and sweet
Reveal the mixture of alcohol 18g), 40~50% disintegrant (low-substituted hydroxypropyl cellulose 18g and crosslinked polyvinylpyrrolidone 7g
Mixture), be wetting agent with absolute ethyl alcohol, wet granulation crosses 100 mesh sieves, 30~45 DEG C of dryings, and whole grain adds in remaining disintegration
Agent, corrigent (Aspartame 1g), lubricant (superfine silica gel powder 3g), it is tabletted.
Embodiment 5
(1) preparation of solid dispersions:
By 5g Oxiracetams and 40g succinic acids uniform dissolution in 250mL absolute ethyl alcohols, 20~22min is stirred, with rotation
Evaporimeter recycling design, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves to get Oxiracetam solid
Dispersion.
(2) preparation of oral disnitegration tablet:
The obtained Oxiracetam solid dispersions (5g) of step (1) sieving are added in into filler (amylum pregelatinisatum 35g and sweet
Reveal the mixture of alcohol 30g), 40~50% disintegrant (low-substituted hydroxypropyl cellulose 22g and crosslinked polyvinylpyrrolidone 5g
Mixture), be wetting agent with absolute ethyl alcohol, wet granulation crosses 100 mesh sieves, 30~45 DEG C of dryings, and whole grain adds in remaining disintegration
Agent, corrigent (Sucralose 0.5g), lubricant (superfine silica gel powder 2.5g), it is tabletted.
Embodiment 6
(1) preparation of solid dispersions:
By 3g Oxiracetams and 5g succinic acids uniform dissolution in 80mL absolute ethyl alcohols, 20~22min is stirred, is steamed with rotation
Instrument recycling design is sent out, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves to get Oxiracetam solid point
Granular media.
(2) preparation of oral disnitegration tablet:
The obtained Oxiracetam solid dispersions (3g) of step (1) sieving are added in into filler (amylum pregelatinisatum 50g and sweet
Reveal the mixture of alcohol 20g), 40~50% disintegrant (low-substituted hydroxypropyl cellulose 20g and crosslinked polyvinylpyrrolidone 5g
Mixture), be wetting agent with absolute ethyl alcohol, wet granulation crosses 100 mesh sieves, 30~45 DEG C of dryings, and whole grain adds in remaining disintegration
Agent, corrigent (Aspartame 0.5g), lubricant (superfine silica gel powder 1.5g), it is tabletted.
Embodiment 7
(1), solid dispersions are prepared
4g Oxiracetams in 180mL absolute ethyl alcohols, stir 5~25min, use rotary evaporation with 6g succinic acids uniform dissolution
Instrument recycling design, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves to get solid dispersions.
(2), the preparation of oral disnitegration tablet
Oral disnitegration tablet contains 4g Oxiracetam solid dispersions, 65g fillers (amylum pregelatinisatum, microcrystalline cellulose and
Mannitol mixture, wherein amylum pregelatinisatum：Microcrystalline cellulose：Weight ratio=1 of mannitol:2：1), 25g disintegrants are (low to take
For hydroxypropyl cellulose and the mixture of crosslinked polyvinylpyrrolidone, wherein low-substituted hydroxypropyl cellulose：Crosslinked polyethylene
The weight ratio of pyrrolidones is 1:1), 5g lubricants (superfine silica gel powder), 1g corrigents (Aspartame)；
Specifically preparation process is：
The Oxiracetam solid dispersions that sieving is obtained add in filler, the 50% of disintegrant total amount, use absolute ethyl alcohol
For wetting agent, wet granulation crosses 100 mesh sieves, 30~45 DEG C of dryings, and whole grain adds in remaining disintegrant and corrigent and lubrication
Agent, it is tabletted.
Embodiment 8
(1), solid dispersions are prepared
6 parts of Oxiracetams and 7 parts of succinic acid uniform dissolutions stir 5~25min in 35 parts of absolute ethyl alcohols, are steamed with rotation
Instrument recycling design is sent out, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves to get solid dispersions.
(2), the preparation of oral disnitegration tablet
Oral disnitegration tablet contains 6g Oxiracetam solid dispersions, 68g fillers (amylum pregelatinisatum, microcrystalline cellulose and
Mannitol mixture, wherein amylum pregelatinisatum：Microcrystalline cellulose：Weight ratio=2 of mannitol:3：1), 22g disintegrants are (low to take
For hydroxypropyl cellulose and the mixture of crosslinked polyvinylpyrrolidone, wherein low-substituted hydroxypropyl cellulose：Crosslinked polyethylene
The weight ratio of pyrrolidones is 3:1), 3g lubricants (superfine silica gel powder), 1g corrigents (Aspartame)；
Specifically preparation process is：
The Oxiracetam solid dispersions that sieving is obtained add in filler, the 40~50% of disintegrant total amount, and use is anhydrous
Ethyl alcohol is wetting agent, and wet granulation crosses 100 mesh sieves, 30~45 DEG C of dryings, and whole grain adds in remaining disintegrant and corrigent and profit
Lubrication prescription, it is tabletted.
Embodiment 9
(1), solid dispersions are prepared
1 part of Oxiracetam and 8 parts of succinic acid uniform dissolutions stir 5~25min in 40 parts of absolute ethyl alcohols, are steamed with rotation
Instrument recycling design is sent out, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves to get solid dispersions.
(2), the preparation of oral disnitegration tablet
Oral disnitegration tablet contains 14g Oxiracetam solid dispersions, 56g fillers (amylum pregelatinisatum, microcrystalline cellulose and
Mannitol mixture, wherein amylum pregelatinisatum：Microcrystalline cellulose：Weight ratio=1 of mannitol:3：1), 25g disintegrants are (low to take
For hydroxypropyl cellulose and the mixture of crosslinked polyvinylpyrrolidone, wherein low-substituted hydroxypropyl cellulose：Crosslinked polyethylene
The weight ratio of pyrrolidones is 2:1), 4.5g lubricants (superfine silica gel powder), 0.5g corrigents (Aspartame)；
Specifically preparation process is：
The Oxiracetam solid dispersions that sieving is obtained add in filler, the 40% of disintegrant total amount), use absolute ethyl alcohol
For wetting agent, wet granulation crosses 100 mesh sieves, 30~45 DEG C of dryings, and whole grain adds in remaining disintegrant and corrigent and lubrication
Agent, it is tabletted.
Embodiment 10
(2), solid dispersions are prepared
1 part of Oxiracetam and 8 parts of PLURONICS F87 uniform dissolutions stir 5~25min in 50 parts of acetone, are steamed with rotation
Instrument recycling design is sent out, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves to get solid dispersions.
(2), the preparation of oral disnitegration tablet
Oral disnitegration tablet contains 3g Oxiracetam solid dispersions, 70g fillers (microcrystalline cellulose and mannitol mixing
Object, wherein microcrystalline cellulose：Weight ratio=5 of mannitol:1), 23g disintegrants (low-substituted hydroxypropyl cellulose and the poly- second of crosslinking
The mixture of alkene pyrrolidone, wherein low-substituted hydroxypropyl cellulose：The weight ratio of crosslinked polyvinylpyrrolidone is 3:1),
3.2g lubricants (superfine silica gel powder), 0.8g corrigents (Sucralose)；
Specifically preparation process is：
By obtained Oxiracetam solid dispersions addition filler, 40~50% disintegrant (the disintegrant total amount of sieving
40~50%), be wetting agent with absolute ethyl alcohol, wet granulation crosses 100 mesh sieves, 30~45 DEG C of dryings, and whole grain adds in residue and collapses
Agent and corrigent and lubricant are solved, it is tabletted.
Embodiment 11
(3), solid dispersions are prepared
8g Oxiracetams in 350mL acetone, stir 5~25min with 24g PLURONICS F87s uniform dissolution, are steamed with rotation
Instrument recycling design is sent out, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves to get solid dispersions.
(2), the preparation of oral disnitegration tablet
Oral disnitegration tablet contains 8g Oxiracetam solid dispersions, 68g fillers (microcrystalline cellulose and mannitol mixing
Object, wherein microcrystalline cellulose：Weight ratio=2 of mannitol:1), 18g disintegrants (low-substituted hydroxypropyl cellulose and the poly- second of crosslinking
The mixture of alkene pyrrolidone, wherein low-substituted hydroxypropyl cellulose：The weight ratio of crosslinked polyvinylpyrrolidone is 2:1), 5g
Lubricant (superfine silica gel powder), 1g corrigents (Sucralose)；
Specifically preparation process is：
By obtained Oxiracetam solid dispersions addition filler, 40~50% disintegrant (the disintegrant total amount of sieving
40~50%), be wetting agent with absolute ethyl alcohol, wet granulation crosses 100 mesh sieves, 30~45 DEG C of dryings, and whole grain adds in residue and collapses
Agent and corrigent and lubricant are solved, it is tabletted.
Embodiment 12
(4), solid dispersions are prepared
5g Oxiracetams in 250mL acetone, stir 5~25min with 10g PLURONICS F87s uniform dissolution, are steamed with rotation
Instrument recycling design is sent out, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves to get solid dispersions.
(2), the preparation of oral disnitegration tablet
Oral disnitegration tablet contains 5g Oxiracetam solid dispersions, 65g fillers (microcrystalline cellulose and mannitol mixing
Object, wherein microcrystalline cellulose：Weight ratio=3 of mannitol:1), 24g disintegrants (low-substituted hydroxypropyl cellulose and the poly- second of crosslinking
The mixture of alkene pyrrolidone, wherein low-substituted hydroxypropyl cellulose：The weight ratio of crosslinked polyvinylpyrrolidone is 2:1), 5g
Lubricant (superfine silica gel powder), 1g corrigents (Sucralose)；
Specifically preparation process is：
By obtained Oxiracetam solid dispersions addition filler, 40~50% disintegrant (the disintegrant total amount of sieving
40~50%), be wetting agent with absolute ethyl alcohol, wet granulation crosses 100 mesh sieves, 30~45 DEG C of dryings, and whole grain adds in residue and collapses
Agent and corrigent and lubricant are solved, it is tabletted.
Embodiment 13
(1) preparation of solid dispersions:
By 3g Oxiracetams and 5g PLURONICS F87s uniform dissolution in 80mL dichloromethane, 20~22min is stirred, is used
Rotary Evaporators recycling design, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves to get Oxiracetam
Solid dispersions.
(2) preparation of oral disnitegration tablet:
By the obtained Oxiracetam solid dispersions (3g) of step (1) sieving add in filler (amylum pregelatinisatum), 40~
50% disintegrant (crosslinked polyvinylpyrrolidone) is wetting agent with absolute ethyl alcohol, and wet granulation crosses 100 mesh sieves, 30~45
DEG C drying, whole grain add in remaining disintegrant, corrigent (xylitol 0.5g), lubricant (superfine silica gel powder 1.5g), tabletted.
Embodiment 14
(1) preparation of solid dispersions:
By 3g Oxiracetams and 5g lactose uniform dissolution in 80mL ethyl acetate, 20~22min is stirred, uses rotary evaporation
Instrument recycling design, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves and disperses to get Oxiracetam solid
Body.
(2) preparation of oral disnitegration tablet:
The Oxiracetam solid dispersions (3g) that step (1) sieving obtains are added in into filler (microcrystalline cellulose 50g and jade
The mixture of rice starch 20g), 40~50% disintegrant (low-substituted hydroxypropyl cellulose), be wetting agent with absolute ethyl alcohol, it is wet
Legal system grain crosses 100 mesh sieves, 30~45 DEG C of dryings, and whole grain adds in remaining disintegrant, corrigent (Sucralose 0.5g), lubricant
(superfine silica gel powder 1.5g), it is tabletted.
Embodiment 15
(1) preparation of solid dispersions:
By 3g Oxiracetams and 5g hydroxypropyl celluloses uniform dissolution in 80mL absolute ethyl alcohols, 20~22min is stirred, is used
Rotary Evaporators recycling design, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves to get Oxiracetam
Solid dispersions.
(2) preparation of oral disnitegration tablet:
By the obtained Oxiracetam solid dispersions (3g) of step (1) sieving add in filler (microcrystalline cellulose), 40~
50% disintegrant (mixture of dried starch 20g and crosslinked polyvinylpyrrolidone 5g) is wetting agent with absolute ethyl alcohol, wet method
It pelletized 100 mesh sieves, 30~45 DEG C of dryings, whole grain adds in remaining disintegrant, corrigent (Aspartame 0.5g), lubricant (hydrogen
Change vegetable oil 1.5g), it is tabletted.
Embodiment 16
(1) preparation of solid dispersions:
By 12g Oxiracetams and 12g beta-cyclodextrins uniform dissolution in 95% ethyl alcohol 300mL, 20~22min is stirred, is used
Rotary Evaporators recycling design, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves to get Oxiracetam
Solid dispersions.
(2) preparation of oral disnitegration tablet:
The Oxiracetam solid dispersions (12g) that step (1) sieving obtains are added in into filler microcrystalline cellulose 60g, 40
~50% disintegrant (disintegrant is sodium carboxymethyl starch 22g), is wetting agent with absolute ethyl alcohol, and wet granulation crosses 100 mesh sieves,
30~45 DEG C of dryings, whole grain add in remaining disintegrant, corrigent (acesulfame potassium 1g), lubricant (talcum powder 5g), tabletted.
Embodiment 17
(1) preparation of solid dispersions:
By 4g Oxiracetams and 8g polyvinylpyrrolidones uniform dissolution in 100mL acetone, 20~22min is stirred, is used
Rotary Evaporators recycling design, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves to get Oxiracetam
Solid dispersions.
(2) preparation of oral disnitegration tablet:
The obtained Oxiracetam solid dispersions (4g) of step (1) sieving are added in into filler (cornstarch 50g and medicinal
The mixture of calcium carbonate 20g), 40~50% disintegrant (croscarmellose sodium), be wetting agent with absolute ethyl alcohol, it is wet
Legal system grain crosses 100 mesh sieves, 30~45 DEG C of dryings, and it is (stearic to add in remaining disintegrant, corrigent (essence 0.2g), lubricant for whole grain
Sour magnesium 1.8g), it is tabletted.
Embodiment 18
(1) preparation of solid dispersions:
By 4g Oxiracetams and 6g succinic acids uniform dissolution in 100mL absolute ethyl alcohols, 20~22min is stirred, with rotation
Evaporimeter recycling design, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves to get Oxiracetam solid
Dispersion.
(2) preparation of oral disnitegration tablet:
The obtained Oxiracetam solid dispersions (4g) of step (1) sieving are added in into filler (amylum pregelatinisatum 48g and sweet
Reveal the mixture of alcohol 20g), 40~50% disintegrant (low-substituted hydroxypropyl cellulose 19g and crosslinked polyvinylpyrrolidone 6g
Mixture), be wetting agent with absolute ethyl alcohol, wet granulation crosses 100 mesh sieves, 30~45 DEG C of dryings, and whole grain adds in remaining disintegration
Agent, corrigent (Aspartame 0.5g), lubricant (superfine silica gel powder 2.5g), it is tabletted.
Embodiment 19
(1), solid dispersions are prepared
5g Oxiracetams in 250mL acetone, stir 5~25min with 25g PLURONICS F87s uniform dissolution, are steamed with rotation
Instrument recycling design is sent out, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves to get solid dispersions.
(2), the preparation of oral disnitegration tablet
Oral disnitegration tablet contains 5g Oxiracetam solid dispersions, 69g fillers (microcrystalline cellulose and mannitol mixing
Object, wherein microcrystalline cellulose：Weight ratio=3 of mannitol:1), 21g disintegrants (low-substituted hydroxypropyl cellulose and the poly- second of crosslinking
The mixture of alkene pyrrolidone, wherein low-substituted hydroxypropyl cellulose：The weight ratio of crosslinked polyvinylpyrrolidone is 2:1), 4g
Lubricant (superfine silica gel powder), 1g corrigents (Sucralose)；
Specifically preparation process is：
By obtained Oxiracetam solid dispersions addition filler, 40~50% disintegrant (the disintegrant total amount of sieving
40~50%), be wetting agent with absolute ethyl alcohol, wet granulation crosses 100 mesh sieves, 30~45 DEG C of dryings, and whole grain adds in residue and collapses
Agent and corrigent and lubricant are solved, it is tabletted.
Comparative example 1
By Oxiracetam 4g, amylum pregelatinisatum 48g, mannitol 20g, low-substituted hydroxypropyl cellulose 19g and the poly- second of crosslinking
Alkene pyrrolidone 6g physical mixeds are uniform, are wetting agent with absolute ethyl alcohol, and wet granulation crosses 100 mesh sieves, and 30~45 DEG C of dryings are whole
Grain adds in Aspartame 0.5g, superfine silica gel powder 2.5g, tabletted.
Comparative example 2
By Oxiracetam 3g, microcrystalline cellulose 38g, pregelatinized starch 32g, sodium carboxymethyl starch 15g and cross-linked carboxymethyl
Sodium cellulosate 10g physical mixeds are uniform, are wetting agent with absolute ethyl alcohol, and wet granulation crosses 100 mesh sieves, and 30~45 DEG C of dryings are whole
Grain adds in magnesium stearate 2g, tabletted.
2nd, quality evaluating method
Experiment 1：Into graininess and compressibility inspection
Material to be measured is made freely to be fallen from the fixed funnel of sustained height, accumulation body is formed on the disk that radius is r,
Until material is overflowed from disk border, the height h of accumulation body is measured, replication 3 times is averaged, labeled as hIt is average, i.e. hIt is average
=(h1+h2+h3)/3 calculate arctan (hIt is average/ r), if arctan (hIt is average/ r) 35 ° of ＜, and 25 ° of ＞, that is, think that particle is equal
It is even, beneficial to industrialized production.It is suppressed with the tablet press machine of same model, by hardness control in the range of 25-40N.Emphasis
It checks hardness, and has seen whether the abnormal conditions such as fragmentation, softening or viscous puckery punching.
Experiment 2：Disintegration time limited checks
2ml water (37 DEG C) is taken to be placed in 5ml test tubes, adds in sample prepared by above-described embodiment, starts timing, until all collapsing
Independent fine particle is shattered into, stops timing, records disintegration time, test tube needs to stand in disintegrating procedue, takes 6 progress every time
Detection, takes its average value.
Experiment 3：Mouthfeel inspection
Healthy volunteer 6 is chosen, sample prepared by above-described embodiment is placed on lingual surface and starts timing, until in the oral cavity
Whole disintegration start-stops stop timing, record disintegration time, and experience slice, thin piece from being placed in mouth to the sensation in oral cavity after complete disintegration,
Such as sweet tea/hardship, grittiness etc. is whether there is.
Experiment 4：Dissolved corrosion inspection
In view of the unpub Oxiracetam elution test method in Chinese food Drug Administration official website, it is contemplated that Aura
Western smooth physics, chemistry and biological property, thus it is speculated that absorbed in enteron aisle, while detection bulk pharmaceutical chemicals saturation solubility compared with
Low, in about pH5.6-5.8, saturation solubility is maximum, has pH dependences, and bulk pharmaceutical chemicals are weak acidic drug, therefore determines pH6.8
+ 1% tween of acetate buffer (surface) is screening medium, and condition is as follows：
Testing liquid：+ 1% tween of pH6.8 acetate buffers
Paddle rotating speed：50rpm
Experimental liquid volume：900ml.
The evaluation result of above-described embodiment such as following table.
Oxiracetam oral disnitegration tablet prepared by above-described embodiment (4-19), in 25 DEG C ± 2 DEG C of temperature, relative humidity
Long-term stable experiment is carried out under the conditions of 60% ± 10%, respectively in five March, June, September, December, 18 months time point difference
Detection, sample property, content, related substance meet regulation；Stability study sample is good in taste, shows sample at 18 months
Effect phase internal stability is good.
Oxiracetam oral disnitegration tablet prepared by the present invention, formula is reasonable, effectively solves drug hygroscopicity and makes by force
Material is easily agglomerating into pelletization, and material is sticked in granulation pot wall, causes the non-uniform technical problem of particle, wet granulation
Particle fine uniform afterwards, angle of repose is preferable into graininess and compressibility between 25~35, the hardness of the disintegrated tablet of preparation 30~
40N, the basic disintegration of 35s disintegrations is complete in oral cavity, in good taste, no grittiness, and 15min interior energies dissolution more than 80% need not
Special producing condition has production cost low, carries, stores, transports and take convenient feature, improve patient and take compliance
Property, there is higher practical value.
Claims (9)
1. a kind of Oxiracetam oral disnitegration tablet contains active ingredient and pharmaceutically acceptable required excipient；The activity
Ingredient is Oxiracetam solid dispersions, and the excipient includes filler, disintegrant, lubricant or/and corrigent；Described Austria
La Xitan oral disnitegration tablets contain Oxiracetam solid dispersions 0.8~14%, filler 55~70%, disintegrant 8~25%, profit
Lubrication prescription 1~5%, corrigent 0.1~1%.
2. oral disnitegration tablet as described in claim 1, it is characterised in that：The Oxiracetam solid dispersions are by 1 part of Aura
Western smooth, 1~12 part of carrier and 15~80 parts of solvents are made by solvent method；The carrier is succinic acid, beta-cyclodextrin, polyethylene glycol
6000th, one or more of polyvinylpyrrolidone, lactose, PLURONICS F87, hydroxypropyl cellulose mixing；The solvent
For the mixing of one or more of absolute ethyl alcohol, 95% ethyl alcohol, acetone, dichloromethane, ethyl acetate.
3. oral disnitegration tablet as claimed in claim 2, it is characterised in that：The Oxiracetam solid dispersions are by 1 part of Aura
Western smooth, 3~12 parts of PLURONICS F87s and 30~80 parts of acetone are made by solvent method.
4. such as claim 1-3 any one of them oral disnitegration tablets, it is characterised in that：The filler for cornstarch, can
The mixing of one or more of pressure property starch, microcrystalline cellulose, medicinal calcium carbonate, mannitol；The disintegrant is dried starch, carboxylic
One kind in methyl starch sodium, low-substituted hydroxypropyl cellulose, crosslinked polyvinylpyrrolidone, croscarmellose sodium or
Several mixing；The lubricant is the mixing of one or more of magnesium stearate, superfine silica gel powder, talcum powder, hydrogenated vegetable oil；Institute
Corrigent is stated as the mixing of one or more of Sucralose, xylitol, acesulfame potassium, Aspartame, essence.
5. oral disnitegration tablet as claimed in claim 4, it is characterised in that：The filler is amylum pregelatinisatum, microcrystalline cellulose
The mixture of element and mannitol, wherein amylum pregelatinisatum：Microcrystalline cellulose：Weight ratio=1~2 of mannitol:2~3：1；It is above-mentioned
Disintegrant is low-substituted hydroxypropyl cellulose and the mixture of crosslinked polyvinylpyrrolidone, wherein low substituted hydroxy-propyl fiber
Element：The weight ratio of crosslinked polyvinylpyrrolidone is 1~3:1.
6. oral disnitegration tablet as claimed in claim 4, it is characterised in that：The filler mixes for microcrystalline cellulose and mannitol
Close object, wherein microcrystalline cellulose：Weight ratio=2~5 of mannitol:1；Above-mentioned disintegrant is low-substituted hydroxypropyl cellulose and friendship
Join the mixture of polyvinylpyrrolidone, wherein low-substituted hydroxypropyl cellulose：The weight ratio of crosslinked polyvinylpyrrolidone is 2
~3:1.
7. oral disnitegration tablet as claimed in claim 6, it is characterised in that：The Oxiracetam oral disnitegration tablet, containing active
Ingredient and pharmaceutically acceptable required excipient；The active ingredient be Oxiracetam solid dispersions, the excipient bag
Include filler, disintegrant, lubricant or/and corrigent；The Oxiracetam solid dispersions by 1 part of Oxiracetam, 3~12 parts
PLURONICS F87 and 40~60 parts of acetone are made by solvent method；The filler be microcrystalline cellulose and mannitol mixture,
Middle microcrystalline cellulose：Weight ratio=2~5 of mannitol:1；The disintegrant is low-substituted hydroxypropyl cellulose and crosslinked polyethylene
The mixture of pyrrolidones, wherein low-substituted hydroxypropyl cellulose：The weight ratio of crosslinked polyvinylpyrrolidone is 2~3:1；Institute
Lubricant is stated as superfine silica gel powder；The corrigent is Sucralose.
8. the preparation method of Oxiracetam oral disnitegration tablet as described in claim any one of 1-7, using following steps：
Prepare solid dispersions
（1）Oxiracetam in solvent, stirs 5~25min with carrier uniform dissolution, and recycling design dry, pulverize, and crosses 100 mesh
Sieve is to get solid dispersions；
（2）The preparation of oral disnitegration tablet
By obtained Oxiracetam solid dispersions addition filler, 30~60% disintegrant that sieve（The 30 of disintegrant total amount~
60%）, be wetting agent with absolute ethyl alcohol, wet granulation crosses 100 mesh sieves, 30~45 DEG C of dryings, whole grain, add in remaining disintegrant with
And corrigent and lubricant, it is tabletted.
9. the preparation method of Oxiracetam oral disnitegration tablet as claimed in claim 8, using following steps：
（1）, prepare solid dispersions
1 part of Oxiracetam and 1~8 part of succinic acid uniform dissolution stir 5~25min, with rotation in 20~50 parts of absolute ethyl alcohols
Evaporimeter recycling design, until being dripped there is no liquid, naturally dry crushes, and crosses 100 mesh sieves to get solid dispersions；
（2）The preparation of oral disnitegration tablet
Oral disnitegration tablet contains Oxiracetam solid dispersions 0.8~14%, filler 55~70%, disintegrant 8~25%, lubrication
Agent 1~5%, corrigent 0.1~1%；Specifically preparation process is：
By obtained Oxiracetam solid dispersions addition filler, 40~50% disintegrant that sieve（The 40 of disintegrant total amount~
50%）, be wetting agent with absolute ethyl alcohol, wet granulation crosses 100 mesh sieves, 30~45 DEG C of dryings, whole grain, add in remaining disintegrant with
And corrigent and lubricant, it is tabletted.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611004164.7A CN108066295A (en) | 2016-11-11 | 2016-11-11 | Oxiracetam oral disnitegration tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611004164.7A CN108066295A (en) | 2016-11-11 | 2016-11-11 | Oxiracetam oral disnitegration tablet and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
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Family
ID=62162241
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1582927A (en) * | 2003-08-20 | 2005-02-23 | 范敏华 | Oral disintegrants of nimodipine and their preparation |
| CN101766596A (en) * | 2009-01-04 | 2010-07-07 | 北京润德康医药技术有限公司 | Solid preparation with dextro-oxiracetam as active component |
| CN101766595A (en) * | 2008-12-31 | 2010-07-07 | 北京利乐生制药科技有限公司 | Solid preparation with levo-oxiracetam as active component |
-
2016
- 2016-11-11 CN CN201611004164.7A patent/CN108066295A/en not_active Withdrawn
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1582927A (en) * | 2003-08-20 | 2005-02-23 | 范敏华 | Oral disintegrants of nimodipine and their preparation |
| CN101766595A (en) * | 2008-12-31 | 2010-07-07 | 北京利乐生制药科技有限公司 | Solid preparation with levo-oxiracetam as active component |
| CN101766596A (en) * | 2009-01-04 | 2010-07-07 | 北京润德康医药技术有限公司 | Solid preparation with dextro-oxiracetam as active component |
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