CN106074416A - A kind of preparation method of Azilsartan potassium salt dispersible tablet - Google Patents
A kind of preparation method of Azilsartan potassium salt dispersible tablet Download PDFInfo
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- CN106074416A CN106074416A CN201610759516.3A CN201610759516A CN106074416A CN 106074416 A CN106074416 A CN 106074416A CN 201610759516 A CN201610759516 A CN 201610759516A CN 106074416 A CN106074416 A CN 106074416A
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- Prior art keywords
- weight portion
- potassium salt
- weight
- azilsartan
- microcrystalline cellulose
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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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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4245—Oxadiazoles
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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
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
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- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
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- General Health & Medical Sciences (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Abstract
The invention discloses the preparation method of a kind of Azilsartan potassium salt dispersible tablet, it comprises the following steps: weighs, prepare binding agent, make wet grain, mixed, tabletting dry, total.Be uniformly dispersed, dissolution is good, tablet is smooth, uniform, cleanliness factor is good dispersible tablet；The inventive method is simple to operate, low to the requirement of equipment, preparation is convenient, be applicable to industrialization large-scale production.
Description
Technical field
The invention belongs to field of medicine preparations, be specifically related to the preparation method of a kind of Azilsartan potassium salt dispersible tablet.
Background technology
Azilsartan potassium salt (azilsartan medoxomil) is Japan's military field research and development.Before the one of Azilsartan
Medicine, is hydrolyzed to Azilsartan during gastrointestinal absorption.On February 22nd, 2011 lists in FDA approval, trade name: Edarbi,
Specification is 40mg, 80mg.In April, 2012, Azilsartan listed in Japan, trade name: Azilva, specification: 20mg, 40mg.A Qi
Husky smooth ester is a kind of selectivity AT1 subtype angiotensin II receptor antagonist.Azilsartan selective exclusion angiotensin
II be combined with AT1 receptor more than 10000 times of AT2 receptor (Azilsartan the affinity of AT1 receptor is exceeded), thus block
The vasoconstriction that angiotensinⅡ causes, Aldosterone Secretion etc. rises blood pressure effect.Its effect does not relies on angiotensinⅡ
Route of synthesis, therefore avoid the ACEI impact on Kallidin I level.With angiotensin-convertion enzyme inhibitor (ACEI) class blood pressure lowering
Medicine is compared, and medication is respectively provided with steady blood pressure lowering, will not cause the advantage of dry cough alone or in combination, the most persistently hypotensive activity.
Diabetics can also be produced potential by part peroxide activator enzyme body proliferator activated receptor-γ (PPAR-γ)
Protective effect, relevant clinical result of the test show its clinical effectiveness be better than present clinical widely used olmesartan medoxomil and
Valsartan.On March 5th, 2012, Edarbi is by global famous medicine and medical research/consultant firm-Decision
Resources company confirms as the golden standard that depressor is evaluated, and to the year two thousand twenty, does not has medicine may substitute this of Edarbi
One golden standard status.Although currently some emerging depressor has certain potentiality, but himself is in effectiveness, safety
It Edarbi may cannot be replaced with the defect on toleration and/or medication.[intellectual property situation] compound patent
(CN1946717) expire on February 22nd, 2025.
Summary of the invention
It is an object of the invention to overcome the shortcoming of prior art, it is provided that the preparation of a kind of Azilsartan potassium salt dispersible tablet
Method, the method is simple to operate, equipment requirements is the highest, the Azilsartan potassium salt dispersible tablet of preparation is uniformly dispersed, stable in properties,
Disintegrate is rapid, bioavailability is high.
The purpose of the present invention is achieved through the following technical solutions: the preparation side of a kind of Azilsartan potassium salt dispersible tablet
Method, it is characterised in that it comprises the following steps:
S1. weigh: weigh each raw material by following formula proportion, standby；Described formula is: Azilsartan potassium salt 20～120 weight
Amount part, starch 30～50 weight portion, microcrystalline Cellulose 50～100 weight portion, carboxymethylstach sodium 35～60 weight portion, lactose 10～
30 weight portions, L-hydroxypropylcellulose 1.5～8 weight portion, PVP K30 1.5～8.5 weight portion, silica 1 5～30 weight
Part, magnesium stearate 1～10 weight portion, ethanol 30～80 weight portion；
S2. binding agent is prepared: ethanol is configured to the solution that concentration is 30%, and is joined by PVP K30 in ethanol solution,
Prepare binding agent；
S3. wet grain is made: by Azilsartan potassium salt, starch, lactose, L-hydroxypropylcellulose, account for microcrystalline Cellulose gross weight 70%
Microcrystalline Cellulose, account for the carboxymethylstach sodium of carboxymethylstach sodium gross weight 60% and put into successively in granulator and be pre-mixed 1～5min,
Binding agent is added in the powder being pre-mixed again, stir 3～7min, add water and make the wet granular that mesh number is 16；
S4. being dried: loaded by wet grain in Fluidbedgranulatingdrier, controlling baking temperature is 70～80 DEG C, is dried to granule aqueous
Amount is 3～5%；
The most always mix: dried granule is added in mixer, add silicon dioxide, magnesium stearate, remaining carboxymethylstach sodium
And microcrystalline Cellulose, airtight mixing 15～25min, set the rotating speed of mixer as 5～10rad/min, i.e. prepare Azilsartan
Ester potassium salt dispersible tablet.
Preferably, described formula is: Azilsartan potassium salt 80 weight portion, starch 50 weight portion, microcrystalline cellulose
Element 70 weight portions, carboxymethylstach sodium 60 weight portion, lactose 15 weight portion, L-hydroxypropylcellulose 3.5 weight portion, PVP K30
4.5 weight portions, silicon dioxide 20 weight portion, magnesium stearate 4.2 weight portion, ethanol 45 weight portion.
The invention have the advantages that
The present invention is by the lot of experiments to dispersible tablet prescription, and the technique obtained solves Azilsartan potassium salt at tabletting
During occur sticking, sliver, take off the phenomenons such as lid, be uniformly dispersed, dissolution is good, tablet is smooth, uniform, clean
Spend good dispersible tablet；The inventive method is simple to operate, low to the requirement of equipment, preparation is convenient, it is extensive to be applicable to industrialization
Produce.
Detailed description of the invention
Below in conjunction with embodiment, the present invention will be further described, and protection scope of the present invention is not limited to following institute
State:
Embodiment 1: the preparation method of a kind of Azilsartan potassium salt dispersible tablet, it comprises the following steps:
S1. weigh: weigh each raw material by following formula proportion, standby；Described formula is: Azilsartan potassium salt 80 weight portion,
Starch 50 weight portion, microcrystalline Cellulose 70 weight portion, carboxymethylstach sodium 60 weight portion, lactose 15 weight portion, L-hydroxypropylcellulose
3.5 weight portions, PVP K30 4.5 weight portion, silicon dioxide 20 weight portion, magnesium stearate 4.2 weight portion, ethanol 45 weight
Part.
S2. binding agent is prepared: ethanol is configured to the solution that concentration is 30%, and PVP K30 is joined ethanol solution
In, prepare binding agent；
S3. wet grain is made: by Azilsartan potassium salt, starch, lactose, L-hydroxypropylcellulose, account for microcrystalline Cellulose gross weight 70%
Microcrystalline Cellulose, account for the carboxymethylstach sodium of carboxymethylstach sodium gross weight 60% and put into successively in granulator and be pre-mixed 1min, then will
Binding agent adds in the powder being pre-mixed, and stirs 3min, adds water and make the wet granular that mesh number is 16；
S4. being dried: loaded in Fluidbedgranulatingdrier by wet grain, controlling baking temperature is 70 DEG C, is dried to granule water content and is
3%；
The most always mix: dried granule is added in mixer, add silicon dioxide, magnesium stearate, remaining carboxymethylstach sodium
And microcrystalline Cellulose, airtight mixing 15min, set the rotating speed of mixer as 5rad/min, i.e. prepare Azilsartan potassium salt and divide
Discrete piece.
Embodiment 2: the preparation method of a kind of Azilsartan potassium salt dispersible tablet, it comprises the following steps:
S1. weigh: weigh each raw material by following formula proportion, standby；Described formula is: Azilsartan potassium salt 40 weight portion,
Starch 40 weight portion, microcrystalline Cellulose 50 weight portion, carboxymethylstach sodium 40 weight portion, lactose 10 weight portion, L-hydroxypropylcellulose 8
Weight portion, PVP K30 8 weight portion, silica 18 weight portion, magnesium stearate 8 weight portion, ethanol 30 weight portion；
S2. binding agent is prepared: ethanol is configured to the solution that concentration is 30%, and is joined by PVP K30 in ethanol solution,
Prepare binding agent；
S3. wet grain is made: by Azilsartan potassium salt, starch, lactose, L-hydroxypropylcellulose, account for microcrystalline Cellulose gross weight 70%
Microcrystalline Cellulose, account for the carboxymethylstach sodium of carboxymethylstach sodium gross weight 60% and put into successively in granulator and be pre-mixed 5min, then will
Binding agent adds in the powder being pre-mixed, and stirs 7min, adds water and make the wet granular that mesh number is 16；
S4. being dried: loaded in Fluidbedgranulatingdrier by wet grain, controlling baking temperature is 80 DEG C, is dried to granule water content and is
5%；
The most always mix: dried granule is added in mixer, add silicon dioxide, magnesium stearate, remaining carboxymethylstach sodium
And microcrystalline Cellulose, airtight mixing 25min, set the rotating speed of mixer as 10rad/min, i.e. prepare Azilsartan potassium salt and divide
Discrete piece.
Embodiment 3: the preparation method of a kind of Azilsartan potassium salt dispersible tablet, it comprises the following steps:
S1. weigh: weigh each raw material by following formula proportion, standby；Described formula is: Azilsartan potassium salt 20 weight portion,
Starch 15 weight portion, microcrystalline Cellulose 35 weight portion, carboxymethylstach sodium 30 weight portion, lactose 10 weight portion, L-hydroxypropylcellulose 3
Weight portion, PVP K30 3 weight portion, silicon dioxide 8 weight portion, magnesium stearate 4 weight portion, ethanol 28 weight portion；
S2. binding agent is prepared: ethanol is configured to the solution that concentration is 30%, and is joined by PVP K30 in ethanol solution,
Prepare binding agent；
S3. wet grain is made: by Azilsartan potassium salt, starch, lactose, L-hydroxypropylcellulose, account for microcrystalline Cellulose gross weight 70%
Microcrystalline Cellulose, account for the carboxymethylstach sodium of carboxymethylstach sodium gross weight 60% and put into successively in granulator and be pre-mixed 2min, then will
Binding agent adds in the powder being pre-mixed, and stirs 4min, adds water and make the wet granular that mesh number is 16；
S4. being dried: loaded in Fluidbedgranulatingdrier by wet grain, controlling baking temperature is 73 DEG C, is dried to granule water content and is
4%；
The most always mix: dried granule is added in mixer, add silicon dioxide, magnesium stearate, remaining carboxymethylstach sodium
And microcrystalline Cellulose, airtight mixing 18min, set the rotating speed of mixer as 7rad/min, i.e. prepare Azilsartan potassium salt and divide
Discrete piece.
Embodiment 4: the preparation method of a kind of Azilsartan potassium salt dispersible tablet, it comprises the following steps:
S1. weigh: weigh each raw material by following formula proportion, standby；Described formula is: Azilsartan potassium salt 10 weight portion,
Starch 25 weight portion, microcrystalline Cellulose 30 weight portion, carboxymethylstach sodium 30 weight portion, lactose 10 weight portion, L-hydroxypropylcellulose 3
Weight portion, PVP K30 2 weight portion, silica 10 weight portion, magnesium stearate 4 weight portion, ethanol 25 weight portion；
S2. binding agent is prepared: ethanol is configured to the solution that concentration is 30%, and is joined by PVP K30 in ethanol solution,
Prepare binding agent；
S3. wet grain is made: by Azilsartan potassium salt, starch, lactose, L-hydroxypropylcellulose, account for microcrystalline Cellulose gross weight 70%
Microcrystalline Cellulose, account for the carboxymethylstach sodium of carboxymethylstach sodium gross weight 60% and put into successively in granulator and be pre-mixed 4min, then will
Binding agent adds in the powder being pre-mixed, and stirs 6min, adds water and make the wet granular that mesh number is 16；
S4. being dried: loaded in Fluidbedgranulatingdrier by wet grain, controlling baking temperature is 78 DEG C, is dried to granule water content and is
4.8%；
The most always mix: dried granule is added in mixer, add silicon dioxide, magnesium stearate, remaining carboxymethylstach sodium
And microcrystalline Cellulose, airtight mixing 22min, set the rotating speed of mixer as 8rad/min, i.e. prepare Azilsartan potassium salt and divide
Discrete piece.
Claims (2)
1. the preparation method of an Azilsartan potassium salt dispersible tablet, it is characterised in that it comprises the following steps:
S1. weigh: weigh each raw material by following formula proportion, standby；Described formula is: Azilsartan potassium salt 20～120 weight
Amount part, starch 30～50 weight portion, microcrystalline Cellulose 50～100 weight portion, carboxymethylstach sodium 35～60 weight portion, lactose 10～
30 weight portions, L-hydroxypropylcellulose 1.5～8 weight portion, PVP K30 1.5～8.5 weight portion, silica 1 5～30 weight
Part, magnesium stearate 1～10 weight portion, ethanol 30～80 weight portion；
S2. binding agent is prepared: ethanol is configured to the solution that concentration is 30%, and is joined by PVP K30 in ethanol solution,
Prepare binding agent；
S3. wet grain is made: by Azilsartan potassium salt, starch, lactose, L-hydroxypropylcellulose, account for microcrystalline Cellulose gross weight 70%
Microcrystalline Cellulose, account for the carboxymethylstach sodium of carboxymethylstach sodium gross weight 60% and put into successively in granulator and be pre-mixed 1～5min,
Binding agent is added in the powder being pre-mixed again, stir 3～7min, add water and make the wet granular that mesh number is 16；
S4. being dried: loaded by wet grain in Fluidbedgranulatingdrier, controlling baking temperature is 70～80 DEG C, is dried to granule aqueous
Amount is 3～5%；
The most always mix: dried granule is added in mixer, add silicon dioxide, magnesium stearate, remaining carboxymethylstach sodium
And microcrystalline Cellulose, airtight mixing 15～25min, set the rotating speed of mixer as 5～10rad/min, i.e. prepare Azilsartan
Ester potassium salt dispersible tablet.
The preparation method of a kind of Azilsartan potassium salt dispersible tablet the most as claimed in claim 1, it is characterised in that described formula
For: Azilsartan potassium salt 80 weight portion, starch 50 weight portion, microcrystalline Cellulose 70 weight portion, carboxymethylstach sodium 60 weight portion,
Lactose 15 weight portion, L-hydroxypropylcellulose 3.5 weight portion, PVP K30 4.5 weight portion, silicon dioxide 20 weight portion, tristearin
Acid magnesium 4.2 weight portion, ethanol 45 weight portion.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610759516.3A CN106074416A (en) | 2016-08-30 | 2016-08-30 | A kind of preparation method of Azilsartan potassium salt dispersible tablet |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610759516.3A CN106074416A (en) | 2016-08-30 | 2016-08-30 | A kind of preparation method of Azilsartan potassium salt dispersible tablet |
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| Publication Number | Publication Date |
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| CN106074416A true CN106074416A (en) | 2016-11-09 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201610759516.3A Pending CN106074416A (en) | 2016-08-30 | 2016-08-30 | A kind of preparation method of Azilsartan potassium salt dispersible tablet |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019130277A1 (en) * | 2017-12-30 | 2019-07-04 | Lupin Limited | Pharmaceutical formulations of azilsartan medoxomil |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060281795A1 (en) * | 2004-02-25 | 2006-12-14 | Takanobu Kuroita | Benzinidazole Derivative and Use As AII Receptor Antagonist |
| CN105079815A (en) * | 2014-04-30 | 2015-11-25 | 广东东阳光药业有限公司 | Azilsartan medoxomil potassium combination and preparation method thereof |
| CN105193753A (en) * | 2015-10-30 | 2015-12-30 | 成都通德药业有限公司 | Preparation method of azithromycin dispersible tablets |
-
2016
- 2016-08-30 CN CN201610759516.3A patent/CN106074416A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060281795A1 (en) * | 2004-02-25 | 2006-12-14 | Takanobu Kuroita | Benzinidazole Derivative and Use As AII Receptor Antagonist |
| CN105079815A (en) * | 2014-04-30 | 2015-11-25 | 广东东阳光药业有限公司 | Azilsartan medoxomil potassium combination and preparation method thereof |
| CN105193753A (en) * | 2015-10-30 | 2015-12-30 | 成都通德药业有限公司 | Preparation method of azithromycin dispersible tablets |
Non-Patent Citations (1)
| Title |
|---|
| 张亚安，等: "抗高血压新药选择性AT1亚型血管紧张素II受体拮抗剂——阿齐沙坦酯", 《药学与临床研究》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019130277A1 (en) * | 2017-12-30 | 2019-07-04 | Lupin Limited | Pharmaceutical formulations of azilsartan medoxomil |
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Application publication date: 20161109 |