CN106265559B - Olanzapine oral disnitegration tablet and preparation method thereof - Google Patents
Olanzapine oral disnitegration tablet and preparation method thereof Download PDFInfo
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- CN106265559B CN106265559B CN201610583234.2A CN201610583234A CN106265559B CN 106265559 B CN106265559 B CN 106265559B CN 201610583234 A CN201610583234 A CN 201610583234A CN 106265559 B CN106265559 B CN 106265559B
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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
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
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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
Abstract
The present invention relates to a kind of novel Olanzapine oral disnitegration tablets and preparation method thereof, belong to technical field of medicine.New pharmaceutical composition of the present invention includes (I) olanzapine particles and (II) additive.Wherein (I) olanzapine particles are to be obtained by the aqueous dispersion of Olanzapine, mannitol, crospovidone and polyvinyl acetate through granulation.The invention further relates to olanzapine particles and include the preparation method of olanzapine orally-disintegrating tablet.
Description
Technical field
The present invention relates to field of pharmaceutical preparations, and in particular to a kind of novel Olanzapine oral disnitegration tablet and its preparation side
Method.
Background technique
Olanzapine is a kind of antipsychotic drug, has pharmacological action to a variety of receptor systems.It is developed by Eli Lilly company
'sRatify in acquisition FDA in 2000, CFDA in 2009 ratifies its application of import, uses
In the acute stage of schizophrenia and other mental diseases for having serious positive symptom and/or negative symptoms and maintain the phase treatment,
Also it can be relieved the secondary affective symptom of schizophrenia and related disease.
Olanzapine has many advantages, such as that long-term efficacy is good, Small side effects, has been faced as a kind of antipsychotic agent
The highly recognition of bed doctor.External listing dosage form has conventional tablet, oral disnitegration tablet, intramuscular injection agent etc. at present, domestic main
For conventional tablet.However ordinary tablet is often due to the disadvantages of patient mismatches treatment, and Compliance is poor, and for old man, children
Er Deng dysphagia group needs more to nurse investment；And intramuscular injection price is higher, patient's compliance is equally poor.
Olanzapine orally-disintegrating tablet, which meets saliva, can be disintegrated rapidly and is dispersed into fine particle, and patient is not required to can quickly will be in mouth with water
Be disintegrated in chamber the particle leached it is autonomous or it is involuntary enter digestive system with swallowing act after play a role, efficiently solve
State the problem of ordinary tablet and intramuscular dose etc..
It is commercially used for preparing Olanzapine oral disnitegration tablet mainly at present including that grind Eli Lilly company dry using freezing for original
Dry technologyOlanzapine oral disnitegration tablet is prepared using wet granular molding technique with TEVA company.But above two system
Preparation Method complex process, production cost are higher, get up so far without extensive development at home.
Existing Olanzapine oral disnitegration tablet patent is mostly based on direct tablet compressing technology, universal disintegration time > 20S；It is filled
Agent more options mannitol, lactose or microcrystalline cellulose etc., but microcrystalline cellulose crude granule is larger, there is obvious gravel in the oral cavity
Sense, and be directed to for the high-incidence lactose intolerance patient in Asia, take lactinated Olanzapine oral disnitegration tablet for a long time, it is clear that
It is not an optimal selection.
WO2006115770 discloses Olanzapine oral disnitegration tablet and uses 75~95% mannitol for diluent, and 1~10%
Disintegrating agent and other auxiliary materials, disintegration time < 20S, the Olanzapine Orally disintegrating of friability < 2% are prepared with compression moulding
Piece.Mannitol dissolves fastly in the oral cavity, in good taste, is highly suitable as the diluent of oral disnitegration tablet, but be mass produced
In, mannitol dosage is excessive in prescription often leads to sticking in tableting processes, and hardness formed is poor to cause prepared mouth to collapse
Piece friability is poor, and then leads to badly broken in aluminium packet and transportational process, and final inconvenience patient takes.
CN101904824 discloses Olanzapine oral disnitegration tablet using 35~74% mannitol, and 10%-40% lactose is dilute
Release agent, 2~10% disintegrating agent and other auxiliary materials.The prescription uses different diluents, reduces the dosage of mannitol, but collapses
It is longer to solve the time.
CN104510717 discloses Olanzapine oral disnitegration tablet using 20~78% mannitol, 10%-40% microcrystalline cellulose
Element is diluent.Although improving disintegration time, due to containing microcrystalline cellulose in prescription, residual, mouth are had on lingual surface
Grittiness sense in chamber, human body compliance are poor；And piece mouldability is poor.
Therefore, it is simple to still need to develop a kind of preparation process, is easy to commercially produce, has stronger hardness so as not to can be in life
The Olanzapine oral disnitegration tablet destroyed in production process or transportational process.
Summary of the invention
In order to solve the above-mentioned technical problems, the present invention provides a kind of Olanzapine oral disnitegration tablets and preparation method thereof.It should
Olanzapine oral disnitegration tablet is convenient to take, good patient compliance, and preparation method is simple, easily amplification production, and production cost is low.
The present invention is realized by the following technical scheme:
A kind of novel Olanzapine oral disnitegration tablet, it includes (I) olanzapine particles；(II) additive.
Olanzapine particles of the invention are by the water dispersion of Olanzapine, mannitol, crospovidone and polyvinyl acetate
System is obtained through granulation.
Inventor is made by a large amount of experiment discovery, by mannitol and disintegrating agent crospovidone by physical method
After grain, mannitol sticking phenomenon can be significantly reduced, but prepared particulate plastic is lower.It is found by inventor's many experiments,
After the aqueous dispersion of mannitol and the mixture of crospovidone and the high polyvinyl acetate of film plasticity is pelletized altogether, can both it drop
The sticking phenomenon of low mannitol, and the plasticity of particle can be improved.
Enabling inventor is in surprise, by preparing the aqueous dispersion of mannitol, crospovidone and polyvinyl acetate
Obtained olanzapine particles are remarkably improved its disintegration and leach speed, are highly suitable as the carrier material of disintegrated tablet.
For the particle for guaranteeing Olanzapine and being prepared by the aqueous dispersion of mannitol, crospovidone and polyvinyl acetate
It is uniformly mixed, inventor has found by many experiments using Olanzapine as particle component units, i.e., by Olanzapine, mannitol, friendship
The aqueous dispersion of connection povidone and polyvinyl acetate is prepared into the particle containing Olanzapine jointly, can effectively solve to be uniformly mixed
The problem of property.
Inventor passes through many experiments, final to determine olanzapine particles each component and its ratio.
Preferably, the partial size that the partial size of the crospovidone is 50% is lower than 40 μm, and 90% partial size is lower than 90 μm.
Preferably, the aqueous dispersion of the polyvinyl acetate is by polyvinyl acetate: povidone is by 5~10 parts:
The aqueous solution of the mixture of 0.05~1 part of weight ratio forms, and further preferred 5~10 parts: 0.5~1 parts.
Preferably, the aqueous dispersion of the polyvinyl acetate refer to containing polyvinyl acetate and povidone 15%~
40% aqueous solution.
Preferably, the crospovidone and the weight ratio of aqueous polyvinyl acetate dispersions are 1:0.5~5, preferably 1:
0.5~2.The weight of the aqueous polyvinyl acetate dispersions is calculated with polyvinyl acetate and povidone dry weight.
Olanzapine particles each component percentage of the invention is as follows:
Preferably, olanzapine particles each component percentage is as follows:
Through olanzapine particles prepared by the present invention optionally and in diluent, disintegrating agent, corrigent and lubricant
One or more combination tabletting, obtains olanzapine orally-disintegrating tablet.
The diluent can be selected from mannitol, pregelatinized starch, sorbierite, maltitol, xylitol, trehalose, reduction
Starch sugar etc.；The optional crospovidone of disintegrating agent, low-substituted hydroxypropyl cellulose, sodium carboxymethyl starch, cross-linked carboxymethyl fiber
Plain sodium etc.；Corrigent can be selected from aspartame, Sucralose, essence etc.；Lubricant can be selected from sodium stearyl fumarate, tristearin
Acid, magnesium stearate, silica, polyethylene glycol etc..
Preferably, Olanzapine oral disnitegration tablet, composition are as follows:
It is highly preferred that Olanzapine oral disnitegration tablet, composition are as follows:
Olanzapine oral disnitegration tablet of the present invention, can be used dry method vertical compression or dry granulation process, and technical process is simple, easily
Amplification production, and production cost is low, the period is short, and the Olanzapine oral disnitegration tablet prepared through this law, ifs vitro disintegration speed is fast, mouth
Disintegration rate < 20S in chamber, and tablet compactibility is good, friability is good, and tablet not will receive damage in production process or transportational process
It is bad.In addition, Olanzapine Orally disintegrating tablet stability of the present invention is preferable, and saved 3 months at 40 DEG C, sample largest single impurity and total miscellaneous
Almost without growth.
On the other hand, the invention also includes the preparation methods of olanzapine particles and olanzapine orally-disintegrating tablet.
Preferably, the preparation of the olanzapine particles includes the following steps:
(a) polyvinyl acetate is weighed in proportion and povidone is configured to 15%~40% (w/w) polyvinyl acetate water
Dispersion；
(b) Olanzapine of recipe quantity and crospovidone are added in above-mentioned aqueous dispersion and are stirred evenly；
(c) above-mentioned aqueous dispersion is sprayed into mannitol surface, be drying to obtain.
Preferably, the preparation method of the Olanzapine oral disnitegration tablet, includes the following steps:
(a) olanzapine particles are prepared；
(b) disintegrating agent, diluent are sieved, by weight weighing and being added in olanzapine particles respectively, are mixed；
(c) be added recipe quantity lubricant mixed into above-mentioned particle, rear tabletting to get；
(d) optionally, the lubricant or corrigent of recipe quantity are added into the mixture of step b.
Preferably, the preparation method of the Olanzapine oral disnitegration tablet, includes the following steps:
(a) olanzapine particles are prepared；
(b) disintegrating agent, diluent are sieved, by weight weighing and being added in olanzapine particles respectively, are mixed, dry method system
Grain；
(c) be added recipe quantity lubricant mixed into above-mentioned particle, tabletting to get；
(d) optionally, the lubricant or corrigent of recipe quantity are added into the mixture of step b.
It is highly preferred that the drying of olanzapine particles is carried out in fluidized bed or centrifugal granulator.
Specific embodiment
In order to better illustrate the present invention and its acquired effect, it is done furtherly below in conjunction with specific embodiment
It is bright, but the scope of the present invention is not limited to the concrete scheme of embodiment.
Embodiment 1
Preparation: polyvinyl acetate and PVP K30 are dissolved in 15ml purified water and stir 5min；Olanzapine and friendship is added
Connection povidone is stirred evenly into above-mentioned solution；Mannitol is put into coating of pellets machine, is sprayed onto sweet dew containing drug solns for above-mentioned
Alcohol surface is atomized, dries to obtain olanzapine particles；Middle control olanzapine particles content；Low-substituted hydroxypropyl cellulose LH-11 is crossed 30
~40 meshes, weigh be added olanzapine particles in mix；The magnesium stearate that recipe quantity is added is mixed into above-mentioned particle；According to Austria
Content is controlled during nitrogen is flat, suppresses the Olanzapine oral disnitegration tablet of different size.
It is obtained with following ingredients weight method substantially the same manner as Example 1 especially suitable for acceptable olanzapine Orally disintegrating
Piece:
Embodiment 2
Preparation: polyvinyl acetate and PVP K30 are dissolved in 20ml purified water and stir 5min；Olanzapine and friendship is added
Connection povidone is stirred evenly into above-mentioned solution；Mannitol is put into coating of pellets machine, is sprayed onto sweet dew containing drug solns for above-mentioned
Alcohol surface is atomized, dries to obtain olanzapine particles；Middle control olanzapine particles content；Low-substituted hydroxypropyl cellulose LH-11 is crossed 30
~40 meshes, weigh respectively and are added in olanzapine particles and mix；The magnesium stearate that recipe quantity is added is mixed into above-mentioned particle；
According to content is controlled in Olanzapine, the Olanzapine oral disnitegration tablet of different size is suppressed.
Embodiment 3
Preparation: polyvinyl acetate and 30 POVIDONE K 30 BP/USP 90 are dissolved in 7ml purified water and stir 5min；Olanzapine and friendship is added
Connection povidone is stirred evenly into above-mentioned solution；Mannitol is put into coating of pellets machine, is sprayed onto sweet dew containing drug solns for above-mentioned
Alcohol surface is atomized, dries to obtain olanzapine particles；Middle control olanzapine particles content；Aspartame is crossed into 80~100 meshes, is handed over
Connection sodium carboxymethylcellulose crosses 30~40 meshes, weighs and is added in olanzapine particles respectively and mixes；The tristearin of recipe quantity is added
Furmaric acid sodium is mixed into above-mentioned particle；According to content is controlled in Olanzapine, the Olanzapine oral disnitegration tablet of different size is suppressed.
Embodiment 4
Preparation: polyvinyl acetate and 30 POVIDONE K 30 BP/USP 90 are dissolved in 19ml purified water and stir 5min；Olanzapine and friendship is added
Connection povidone is stirred evenly into above-mentioned solution；Mannitol is put into coating of pellets machine, is sprayed onto sweet dew containing drug solns for above-mentioned
Alcohol surface is atomized, dries to obtain olanzapine particles；Middle control olanzapine particles content；Copolymerzation with cross-linking dimension ketone is crossed into 30~40 meshes,
It weighs and is added in olanzapine particles respectively and mixed；The sodium stearyl fumarate that recipe quantity is added is mixed into above-mentioned particle；Root
According to content is controlled in Olanzapine, the Olanzapine oral disnitegration tablet of different size is suppressed.
Embodiment 5
Preparation: polyvinyl acetate and PVP K30 are dissolved in 10ml purified water and stir 5min；Olanzapine and friendship is added
Connection povidone is stirred evenly into above-mentioned solution；Mannitol is put into coating of pellets machine, is sprayed onto sweet dew containing drug solns for above-mentioned
Alcohol surface is atomized, dries to obtain olanzapine particles；Middle control olanzapine particles content；Essence is crossed into 80~100 meshes, low substitution
Hydroxypropylcellulose LH-11 crosses 30~40 meshes, pre-paying starch crosses 60~100 meshes, weighs respectively and olanzapine particles are added
Middle mixing；Dry granulation；The silica that recipe quantity is added is mixed into above-mentioned particle；According to content is controlled in Olanzapine, suppress
The Olanzapine oral disnitegration tablet of different size.
Embodiment 6
Preparation: polyvinyl acetate and 30 POVIDONE K 30 BP/USP 90 are dissolved in 25ml purified water and stir 10min；Be added Olanzapine and
Crospovidone is stirred evenly into above-mentioned solution；Mannitol is put into coating of pellets machine, by it is above-mentioned containing drug solns be sprayed onto it is sweet
Reveal alcohol surface, is atomized, dries to obtain olanzapine particles；Middle control olanzapine particles content；Sodium carboxymethylcellulose is crossed 30~40
Mesh, sorbierite cross 60~100 meshes, weigh and are added in olanzapine particles respectively and mix；The polyethylene glycol of recipe quantity is added
It is mixed with silica into above-mentioned particle；According to content is controlled in Olanzapine, the Olanzapine oral disnitegration tablet of different size is suppressed.
Embodiment 7
Preparation: polyvinyl acetate and 30 POVIDONE K 30 BP/USP 90 are dissolved in 30ml purified water and stir 10min；Be added Olanzapine and
Crospovidone is stirred evenly into above-mentioned solution；Mannitol is put into coating of pellets machine, by it is above-mentioned containing drug solns be sprayed onto it is sweet
Reveal alcohol surface, is atomized, dries to obtain olanzapine particles；Middle control olanzapine particles content；Aspartame is crossed into 80~100 meshes,
Croscarmellose sodium crosses 30~40 meshes, and sodium stearyl fumarate 2g is weighed respectively and is added in olanzapine particles and mixes
It is even；The sodium stearyl fumarate that remaining recipe quantity is added is mixed into above-mentioned particle；According to content is controlled in Olanzapine, compacting is different
The Olanzapine oral disnitegration tablet of specification.
Embodiment 8
Preparation: polyvinyl acetate and PVP K30 are dissolved in 15ml purified water and stir 5min；Olanzapine and friendship is added
Connection povidone is stirred evenly into above-mentioned solution；Mannitol is put into coating of pellets machine, is sprayed onto sweet dew containing drug solns for above-mentioned
Alcohol surface is atomized, dries to obtain olanzapine particles；Middle control olanzapine particles content；Crospovidone is crossed into 30~40 meshes, sweet
Dew alcohol crosses 60~100 meshes, weighs and is added in olanzapine particles respectively and mixes；The silica of recipe quantity is added to above-mentioned
It is mixed in grain；According to content is controlled in Olanzapine, the Olanzapine oral disnitegration tablet of different size is suppressed.
Comparative example:
According to olanzapine orally-disintegrating tablet prescription and preparation process disclosed in CN101904824 embodiment 1, inventor is carried out pair
Than test, prescription is as follows:
Preparation method: essence, aspartame, main ingredient are crossed into 80 meshes respectively, essence, aspartame and main ingredient mixing are equal
It is even；Crosslinked polyvinylpyrrolidone sieves with 100 mesh sieve, and mannitol and lactose cross 40 meshes respectively, is sequentially added into is mixed with according to quantity
Essence, aspartame main ingredient in mix, add the magnesium stearate of recipe quantity, sieving mixes, direct tablet compressing to get.
The experiment of 1 disintegration of test example
Ifs vitro disintegration is 1.: using the teat glass of diameter 1.5cm, being added and is preheated to 37 DEG C of water (2ml), drug is put into
Wherein, it stands, for calculating tablet the time required to from the contact water surface to completion disintegration, the drug after disintegration should pass through completely No. 2 sieves (can
It is rinsed with a small amount of water)；
Ifs vitro disintegration is 2.: using 2010 editions Chinese Pharmacopoeias, two annex disintegration time limit tests.
1~8 ifs vitro disintegration of acetonideexample≤8S.
2 friability inspection of test example
Friability inspection is carried out to 1~embodiment of embodiment 8 and comparative example.
| Sample | Friability |
| Embodiment 1 | 0.05% |
| Embodiment 2 | 0.04% |
| Embodiment 3 | 0.06% |
| Embodiment 4 | 0.06% |
| Embodiment 5 | 0.11% |
| Embodiment 6 | 0.03% |
| Embodiment 7 | 0.04% |
| Embodiment 8 | 0.12% |
| Comparative example | 0.29% |
3 human body compliance inspection of test example
Tablet is placed in middle front part on healthy volunteer's tongue, tolerable lingual surface suitably moves up and down, when record tablet is disintegrated
Between, whether there is or not grittiness, lingual surfaces noresidue etc. for tablet taste, lingual surface.1,3,7 patient's compliance of acetonideexample is preferable.
4 Dissolution experiments of test example
Dissolving-out method: dissolution method (the 4th 0,931 second method of general rule of Chinese Pharmacopoeia version in 2015) is investigated above-mentioned
Dissolution rate of the sample in 0.1N HcL, acetonideexample and comparative example 5min dissolve out equal > 95%.
| Sample | 5min dissolution |
| Embodiment 1 | 98% |
| Embodiment 2 | 101% |
| Embodiment 3 | 98% |
| Embodiment 4 | 100% |
| Embodiment 5 | 97% |
| Embodiment 6 | 98% |
| Embodiment 7 | 99% |
| Embodiment 8 | 97% |
| Comparative example | 96% |
5 stability test of test example
Above-mentioned sample 1-8 is placed in transparent vial, it is tightly sealed, and saved 3 months at 40 DEG C, it is protected in sample
3 months before depositing and after saving, examine comparison largest single impurity and total miscellaneous.Tablet is extracted with the mixed solvent of mobile phase, is led to
Cross HPLC measurement largest single impurity and total miscellaneous.Results sample has good stability, after placing three months, largest single impurity and it is total it is miscellaneous almost without
Increase.
Claims (19)
1. a kind of Olanzapine oral disnitegration tablet, which is characterized in that include (I) olanzapine particles；(II) additive, it is described (I)
Olanzapine particles are to be obtained by the aqueous dispersion of Olanzapine, mannitol, crospovidone and polyvinyl acetate through granulation.
2. Olanzapine oral disnitegration tablet according to claim 1, which is characterized in that (II) additive is selected from dilution
One of agent, disintegrating agent, corrigent and lubricant are a variety of.
3. Olanzapine oral disnitegration tablet according to claim 1, which is characterized in that the olanzapine particles are with weight percent
Include following components than meter:
4. Olanzapine oral disnitegration tablet according to claim 3, which is characterized in that the olanzapine particles are with weight percent
Include following components than meter:
5. Olanzapine oral disnitegration tablet according to claim 3 or 4, which is characterized in that the partial size of the crospovidone,
50% partial size is lower than 40 μm, and 90% partial size is lower than 90 μm.
6. Olanzapine oral disnitegration tablet according to claim 3 or 4, which is characterized in that the polyvinyl acetate moisture
Granular media system refers to that mass fraction is 15%~40% polyvinyl acetate and povidone aqueous solution.
7. Olanzapine oral disnitegration tablet according to claim 6, which is characterized in that the aqueous polyvinyl acetate dispersions
Middle polyvinyl acetate: the weight ratio of povidone is 5~10 parts: 0.05~1 parts.
8. Olanzapine oral disnitegration tablet according to claim 7, which is characterized in that the aqueous polyvinyl acetate dispersions
Middle polyvinyl acetate: the weight ratio of povidone is 5~10 parts: 0.5~1 parts.
9. according to claim 1, Olanzapine oral disnitegration tablet described in 3 or 4, which is characterized in that the crospovidone and poly-
The weight ratio of vinyl acetate ester aqueous dispersion is 1:0.5~5.
10. Olanzapine oral disnitegration tablet according to claim 9, which is characterized in that the crospovidone and poly- acetic acid
The weight ratio of ethylene ester aqueous dispersion is 1:0.5~2.
11. -2 described in any item Olanzapine oral disnitegration tablets according to claim 1, which is characterized in that by weight percentage,
Its composition is as follows:
12. Olanzapine oral disnitegration tablet according to claim 11, which is characterized in that the diluent be selected from mannitol,
Pregelatinized starch, sorbierite, xylitol, maltitol, trehalose or reduction starch sugar.
13. Olanzapine oral disnitegration tablet according to claim 11, which is characterized in that the disintegrating agent is selected from the poly- dimension of crosslinking
Ketone, low-substituted hydroxypropyl cellulose, sodium carboxymethyl starch or croscarmellose sodium.
14. Olanzapine oral disnitegration tablet according to claim 11, which is characterized in that the corrigent is selected from A Sipa
Smooth, Sucralose or essence.
15. Olanzapine oral disnitegration tablet according to claim 11, which is characterized in that it is rich that the lubricant is selected from stearic acid
Horse acid sodium, stearic acid, magnesium stearate, silica or polyethylene glycol.
16. a kind of method for preparing olanzapine particles, includes the following steps:
A) polyvinyl acetate is weighed in proportion and povidone is configured to the water dispersion of 15%~40% (w/w) polyvinyl acetate
Body；
B) Olanzapine of recipe quantity and crospovidone are added in above-mentioned aqueous dispersion and are stirred evenly；
C) above-mentioned aqueous dispersion is sprayed into mannitol surface, be drying to obtain.
17. a kind of method for preparing Olanzapine oral disnitegration tablet, includes the following steps:
A) olanzapine particles of preparation the method described in claim 16 preparation；
B) disintegrating agent, diluent are sieved, by weight weighing and being added in olanzapine particles respectively, are mixed；
C) be added recipe quantity lubricant mixed into above-mentioned particle after tabletting to get；
D) optionally, the lubricant or corrigent of recipe quantity are added into the mixture of step b.
18. a kind of method for preparing Olanzapine oral disnitegration tablet, includes the following steps:
A) olanzapine particles of preparation the method described in claim 16 preparation；
B) disintegrating agent, diluent are sieved, by weight weighing and being added in olanzapine particles respectively, are mixed, dry granulation；
C) be added recipe quantity lubricant mixed into above-mentioned particle after tabletting to get；
D) optionally, the lubricant or corrigent of recipe quantity are added into the mixture of step b.
19. according to the method for claim 16, which is characterized in that drying is carried out in fluidized bed or centrifugal granulator.
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| WO2011085188A1 (en) * | 2010-01-07 | 2011-07-14 | Eurand, Inc. | Pharmaceutical compositions comprising anti-psychotic drugs |
| CN102178657A (en) * | 2011-04-11 | 2011-09-14 | 浙江华海药业股份有限公司 | Novel Olanzapine orally disintegrating tablet |
| CN104887634A (en) * | 2015-05-07 | 2015-09-09 | 河北龙海药业有限公司 | Olanzapine orally disintegrating tablets and preparation method thereof |
-
2016
- 2016-07-22 CN CN201610583234.2A patent/CN106265559B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011085188A1 (en) * | 2010-01-07 | 2011-07-14 | Eurand, Inc. | Pharmaceutical compositions comprising anti-psychotic drugs |
| CN102178657A (en) * | 2011-04-11 | 2011-09-14 | 浙江华海药业股份有限公司 | Novel Olanzapine orally disintegrating tablet |
| CN104887634A (en) * | 2015-05-07 | 2015-09-09 | 河北龙海药业有限公司 | Olanzapine orally disintegrating tablets and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| The Influence of Drug Physical State on the Dissolution Enhancement of Solid Dispersions Prepared Via Hot-Melt Extrusion: A Case Study Using Olanzapine;Pina,et al;《JOURNAL OF PHARMACEUTICAL SCIENCES》;20141231;第103卷;第1214-1223页 * |
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| CN106265559A (en) | 2017-01-04 |
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