CN105193743B - A kind of Montelukast Sodium granular preparation and preparation method thereof - Google Patents
A kind of Montelukast Sodium granular preparation and preparation method thereof Download PDFInfo
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- CN105193743B CN105193743B CN201510747141.4A CN201510747141A CN105193743B CN 105193743 B CN105193743 B CN 105193743B CN 201510747141 A CN201510747141 A CN 201510747141A CN 105193743 B CN105193743 B CN 105193743B
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Abstract
The present invention relates to a kind of Montelukast Sodium granular preparation and preparation method thereof, belong to pharmaceutical technology field.The Montelukast Sodium granular preparation, specification are the 0.5g/4mg in terms of montelukast, are prepared by Montelukast Sodium, protective agent, filler, disintegrant, lubricant, 80% ethanol, purified water.It is accelerated experiment, long term test investigate, appearance, granularity, dissolution rate, content, in relation to material compared with 0 month without significant difference, in acceptability limit, conform to quality requirements.Therefore, Montelukast Sodium granular preparation of the present invention is matched with specific prescription, specific preparation process achieves good technique effect, is provided a kind of different technical solution for the preparation of Montelukast Sodium granular preparation, can more be met clinical demand.
Description
Technical field
The present invention relates to a kind of granular preparation and preparation method thereof, be specifically related to a kind of Montelukast Sodium granular preparation and
Its preparation method, belongs to pharmaceutical technology field.
Background technology
Montelukast Sodium is the antasthmatic developed by Merck companies of the U.S., is obtained in 2 months 1998 in U.S. FDA approval
City, trade name " Singulair ", successively in 71 states such as Canada, Italy, Spain, Sweden, Switzerland, Germany, France
Family's listing.For treating asthma, seasonal allergy and perennial allergic rhinitis (PAR).In the treatment for PAR symptoms
When, suffer from available for 1 years old to 2 years old children asthma, 2 years old to 5 years old children asthma and/or 2 years old to 5 years old allergic rhinitis
Person.
Montelukast Sodium particle obtained Chinese import registration official written reply (import registration certificate number in 2012：Chinese medicines quasi-word
J20140167, manufacturer：Merck Sharp＆Dohme Corp., trade name：Singulair), specification 0.5g:4mg is (with Meng
Lu Site is counted).
Montelukast Sodium is safe and effective, and adverse reaction is relatively low, and patient tolerability and compliance are preferable.Therefore, develop
Montelukast Sodium granular preparation is the hot spot of numerous producer's research and development at present to expand its clinical practice.
The content of the invention
The technical problems to be solved by the invention are to provide a kind of Montelukast Sodium granular preparation, the Montelukast Sodium particle
Preparation has the advantages that stability is high.In addition, the preparation method the present invention further provides the Montelukast Sodium granular preparation.
Technical problem of the present invention is realized by following technical scheme.
A kind of Montelukast Sodium granular preparation, specification are the 0.5g/4mg in terms of montelukast, the Montelukast Sodium particle system
Agent is prepared from the following parts by weight of the components：Montelukast Sodium 4.15, protective agent 15, filler 454.3, disintegrant 25, profit
Lubrication prescription 1.5,80% ethanol 110, purified water 20.
Preferably, above-mentioned Montelukast Sodium granular preparation, the protective agent are dodecyldimethylamine oxide and oxalic acid
Ammonium is with weight ratio 1:2 mixture；The filler is mannitol；The disintegrant is microcrystalline cellulose；The lubricant is
Magnesium stearate.
A kind of preparation method of above-mentioned Montelukast Sodium granular preparation, includes the following steps：
(1) liquid is matched somebody with somebody：The Montelukast Sodium of recipe quantity is added in 80% ethanol, is dissolved to transparent stand-by；
(2) premix：Protective agent, mannitol, microcrystalline cellulose are added in high-speed mixing granulating machine, premix 3min；
(3) softwood processed：Raw material medicine solution is added in pre- mixed material, unlatching high-speed mixing granulating machine, stirring at low speed,
Cutting 8 minutes；
(4) pelletize：Softwood is pelletized through 24 mesh sieve net of oscillating granulator；
(5) dry：Particle is added into multifunctional fluidized bed granulator coater, 50 DEG C of dry 30min；
(6) whole grain：By dried particle through 16 mesh sieve net whole grain of oscillating granulator；
(7) sieve：Particle after whole grain is added in the shaking screen that upper strata is 24 mesh, lower floor is 180 mesh and is sieved；
(8) mix：Particle after screening is added into mixer, adds recipe quantity magnesium stearate, mixes 5min, discharge to obtain Meng
Montelukast sodium granular preparation.
Montelukast Sodium granular preparation of the present invention, by protective agent in prescription, achieves good stability effect
Fruit.Especially when the use of protective agent being dodecyldimethylamine oxide and ammonium oxalate with weight ratio 1:It is accelerated during 2 mixture
Experiment, long term test investigate, appearance, granularity, dissolution rate, content, in relation to material compared with 0 month without significant difference, in qualification
In the range of, conform to quality requirements.Therefore, Montelukast Sodium granular preparation of the present invention is matched with specific prescription, is specific
Preparation process achieve good technique effect, provide a kind of different technology for the preparation of Montelukast Sodium granular preparation
Scheme, can more meet clinical demand.
Embodiment
The present invention is embodied by following embodiments, and following embodiments can be used for explaining the present invention but not as this hair
The restriction of bright protection domain.
Preparation (specification 0.5g/4mg, 1000 bags) label of embodiment Montelukast Sodium granular preparation of the present invention
Composition：
Remarks：Ethanol and purified water vapor away, preparation final products do not occur in the drying process as solvent.It is single
Position dose product Montelukast Sodium dosage calculates：Montelukast Sodium dosage=specification ÷ (montelukast molecular weight ÷ montelukasts
Sodium molecule amount)=4mg ÷ (586.18 ÷ 608.18)=4.15mg
Preparation method：
(2) liquid is matched somebody with somebody：The Montelukast Sodium of recipe quantity is added in 80% ethanol, is dissolved to transparent stand-by；
(2) premix：Dodecyldimethylamine oxide, ammonium oxalate, mannitol, microcrystalline cellulose are added into mixed at high speed system
In grain machine, 3min is premixed；
(3) softwood processed：Raw material medicine solution is added in pre- mixed material, unlatching high-speed mixing granulating machine, stirring at low speed,
Cutting 8 minutes；
(4) pelletize：Softwood is pelletized through 24 mesh sieve net of oscillating granulator；
(5) dry：Particle is added into multifunctional fluidized bed granulator coater, 50 DEG C of dry 30min；
(6) whole grain：By dried particle through 16 mesh sieve net whole grain of oscillating granulator；
(7) sieve：Particle after whole grain is added in the shaking screen that upper strata is 24 mesh, lower floor is 180 mesh and is sieved；
(8) mix：Particle after screening is added into mixer, adds recipe quantity magnesium stearate, mixes 5min, discharge to obtain Meng
Montelukast sodium granular preparation.
Test example stability test
Accelerated test：By the Montelukast Sodium granular preparation prepared by the embodiment of the present invention be positioned over 40 DEG C ± 2 DEG C of temperature,
Under the conditions of relative humidity 75% ± 5%, character, dissolution rate, the situation of change in relation to material are investigated, result of the test see the table below 1.
1 Montelukast Sodium Particle Acceleration result of the test of table
Long term test：Montelukast Sodium granular preparation prepared by the embodiment of the present invention is positioned over 25 DEG C ± 5 DEG C of temperature
Under the conditions of relative humidity 60% ± 5%, character, dissolution rate, the situation of change in relation to material are investigated, result of the test see the table below 2.
2 Montelukast Sodium particle long-term test results of table
The results show：The accelerated experiment of Montelukast Sodium granular preparation prepared by the embodiment of the present invention, long term test are examined
Examine, appearance, granularity, dissolution rate, content, in relation to material compared with 0 month without significant difference, in acceptability limit, meet quality
It is required that.Therefore, Montelukast Sodium granular preparation of the present invention is matched with specific prescription, specific preparation process achieves
Good technique effect, provides a kind of different technical solution for the preparation of Montelukast Sodium granular preparation, can more meet to face
Bed demand.
The technical concept and advantage of above-described embodiment only to illustrate the invention, the present invention can also have other forms to become
Change, as well known to the skilled person, above-described embodiment is functioned only as to the exemplary role in foregoing invention protection domain, right
For those of ordinary skill in the art, there are many conventional deformations and other implementations in the protection domain that the present invention is limited
Example, these deformations and embodiment are all by within the pending protection domain of the present invention.
Claims (1)
1. a kind of Montelukast Sodium granular preparation, specification is the 0.5g/4mg in terms of montelukast, the Montelukast Sodium granular preparation
It is prepared from the following parts by weight of the components：Montelukast Sodium 4.15, protective agent 15, filler 454.3, disintegrant 25, lubrication
Agent 1.5,80% ethanol 110, purified water 20；It is characterized in that, the protective agent is dodecyldimethylamine oxide and oxalic acid
Ammonium is with weight ratio 1:2 mixture；The filler is mannitol；The disintegrant is microcrystalline cellulose；The lubricant is
Magnesium stearate.
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| CN201510747141.4A CN105193743B (en) | 2015-11-05 | 2015-11-05 | A kind of Montelukast Sodium granular preparation and preparation method thereof |
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| CN201510747141.4A CN105193743B (en) | 2015-11-05 | 2015-11-05 | A kind of Montelukast Sodium granular preparation and preparation method thereof |
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| CN105193743A CN105193743A (en) | 2015-12-30 |
| CN105193743B true CN105193743B (en) | 2018-05-08 |
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Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107595783A (en) * | 2017-06-01 | 2018-01-19 | 合肥远志医药科技开发有限公司 | A kind of Menglusitena particle and preparation method thereof |
| CN111110679A (en) * | 2018-10-31 | 2020-05-08 | 长春海悦药业股份有限公司 | Pharmaceutical composition containing montelukast sodium |
| CN112972397A (en) * | 2021-02-22 | 2021-06-18 | 海南鑫开源医药科技有限公司 | Preparation process of montelukast sodium granules |
| CN117731620A (en) * | 2023-12-20 | 2024-03-22 | 翎耀生物科技(上海)有限公司 | High-stability montelukast sodium granule preparation and preparation method thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102973532A (en) * | 2012-12-28 | 2013-03-20 | 南京瑞尔医药有限公司 | Stable montelukast sodium tablet and preparation method thereof |
| CN103239450A (en) * | 2012-02-07 | 2013-08-14 | 齐鲁制药有限公司 | Rapidly-dissolving and stabile montelukast oral solid preparation and preparation method thereof |
| CN104546851A (en) * | 2013-10-29 | 2015-04-29 | 北京韩美药品有限公司 | Particle composition as well as preparation method and preparation thereof |
| CN104644564A (en) * | 2013-11-25 | 2015-05-27 | 天津汉瑞药业有限公司 | Stable granular preparation containing montelukast and preparation method thereof |
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2015
- 2015-11-05 CN CN201510747141.4A patent/CN105193743B/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103239450A (en) * | 2012-02-07 | 2013-08-14 | 齐鲁制药有限公司 | Rapidly-dissolving and stabile montelukast oral solid preparation and preparation method thereof |
| CN102973532A (en) * | 2012-12-28 | 2013-03-20 | 南京瑞尔医药有限公司 | Stable montelukast sodium tablet and preparation method thereof |
| CN104546851A (en) * | 2013-10-29 | 2015-04-29 | 北京韩美药品有限公司 | Particle composition as well as preparation method and preparation thereof |
| CN104644564A (en) * | 2013-11-25 | 2015-05-27 | 天津汉瑞药业有限公司 | Stable granular preparation containing montelukast and preparation method thereof |
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