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Azilsartan tablets and preparation method thereof

A technology for azilsartan tablets and tablet compression, which is applied in the field of preparation of azilsartan granulation, can solve the problems of low dissolution, low penetration, tediousness, etc., and solve the problems of insufficient tablet hardness, slow disintegration and dissolution, Easy compression molding effect

Inactive Publication Date: 2016-08-17
JIANGSU ZHONGBANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation of solid dispersion has many procedures and is cumbersome; although powder direct compression has few procedures and simple process, it has high requirements for auxiliary materials and equipment
In addition, azilsartan is a BCS type 4 compound, which has low solubility and low permeability characteristics, and the prepared tablets generally disintegrate or dissolve out to meet the requirements

Method used

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  • Azilsartan tablets and preparation method thereof
  • Azilsartan tablets and preparation method thereof
  • Azilsartan tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] 10mg tablet specifications:

[0037]

[0038] The preparation method is as follows:

[0039] 1) Micronize the raw material of Azilsartan to a particle size D90≤15μm;

[0040] 2) Lactose monohydrate, microcrystalline cellulose, polyethylene glycol 6000, low-substituted hydroxypropyl cellulose pass through 80 mesh sieve;

[0041] 3) Preparation of adhesive: prepare a 5% solution according to the ratio of hypromellose (5cps): 50% ethanol solution = 5: 100 (W: V);

[0042] 4) Weigh the processed azilsartan, lactose monohydrate, microcrystalline cellulose, and polyethylene glycol 6000 according to the prescription amount, and weigh and mix the low-substituted hydroxypropyl cellulose according to 50% of the prescription amount;

[0043] 5) Put the mixed raw and auxiliary materials into a fluidized bed, and granulate by top spraying. The parameters are as follows:

[0044] Fan frequency (Hz): 25-30

[0045] Inner atomization (bar): 1.8-2.0

[0046] Outer atomization (bar): 2.3-2.6

[0047] I...

Embodiment 2

[0052] 20mg tablet specifications:

[0053]

[0054] The preparation method is as follows:

[0055] 1) Micronize the raw material of Azilsartan to a particle size D90≤15μm;

[0056] 2) Lactose monohydrate, microcrystalline cellulose, polyethylene glycol 6000, low-substituted hydroxypropyl cellulose pass through 80 mesh sieve;

[0057] 3) Preparation of the binder: prepare a 6% solution at the ratio of hypromellose (5cps): 50% ethanol solution = 6: 100 (W: V);

[0058] 4) Weigh the processed azilsartan, lactose monohydrate, microcrystalline cellulose, and polyethylene glycol 6000 according to the prescription amount, and weigh and mix the low-substituted hydroxypropyl cellulose according to 50% of the prescription amount;

[0059] 5) Put the mixed raw and auxiliary materials into a fluidized bed, and granulate by top spraying. The parameters are as follows:

[0060] Fan frequency (Hz): 25-30

[0061] Inner atomization (bar): 1.8-2.0

[0062] Outer atomization (bar): 2.3-2.6

[0063] Inlet air...

Embodiment 3

[0068] 30mg tablet specifications:

[0069]

[0070] The preparation method is as follows:

[0071] 1) Micronize the raw material of Azilsartan to a particle size D90≤15μm;

[0072] 2) Lactose monohydrate, microcrystalline cellulose, polyethylene glycol 6000, low-substituted hydroxypropyl cellulose pass through 80 mesh sieve;

[0073] 3) Preparation of the adhesive: prepare an 8% solution at the ratio of hypromellose (5cps): 50% ethanol solution = 8: 100 (W: V);

[0074] 4) Weigh the processed azilsartan, lactose monohydrate, microcrystalline cellulose, and polyethylene glycol 6000 according to the prescription amount, and weigh and mix the low-substituted hydroxypropyl cellulose according to 50% of the prescription amount;

[0075] 5) Put the mixed raw and auxiliary materials into a fluidized bed, and granulate by top spraying. The parameters are as follows:

[0076] Fan frequency (Hz): 25-30

[0077] Inner atomization (bar): 1.8-2.0

[0078] Outer atomization (bar): 2.3-2.6

[0079] Inlet ...

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Abstract

The invention discloses azilsartan tablets and a preparation method thereof, and belongs to the field of pharmacy. For the azilsartan tablets, each azilsartan tablet is prepared from, by mass, 7.80%-16.30% of azilsartan, 59.78%-70.18% of lactose monohydrate, 15.00%-18.00% of microcrystalline cellulose, 1.15%-1.40% of hydroxypropyl methylcellulose (5cps), 2.20%-2.80% of low-substituted hydroxypropyl cellulose, 2.20%-2.80% of polyethylene glycol 6000 and 0.55%-0.85% of magnesium stearate. By means of a fluidized bed top-spraying granulation method, three processes of mixing, granulation and drying in a traditional technology are completed in one step, the production efficiency is improved, and the prepared granules are uniform in granule size and good in fluidity and compression formability; meanwhile, due to the fact that a disintegrating agent is added internally and externally, the problem that the azilsartan tablets disintegrate and dissolve slowly is solved.

Description

Technical field [0001] The invention relates to the field of pharmacy, discloses an oral preparation containing Azilsartan, and also discloses a preparation method of Azilsartan granulation. Background technique [0002] Azilsartan is an angiotensin II receptor antagonist drug for the treatment of hypertension. It is mostly used for the treatment of hypertension. It is currently the only angiotensin II receptor antagonist (sartan) drug that is in terminal clinical trials. . [0003] Chinese name: Azilsartan; English name: Azilsartan; structural formula is as follows: [0004] [0005] Angiotensin II receptor antagonists (sartans) have maintained a relatively high growth trend since they entered the Chinese market. Since the two varieties of "Kesuya" (Losartan) and "Daiwen" (Valsartan) were launched in my country in 1998, other varieties have also entered my country. At present, sartan drugs cannot become the first choice of the public due to their high quality and high price. Howe...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4245A61K47/38A61P9/12
CPCA61K9/2054A61K9/2095A61K31/4245
Inventor 夏彬许林菊高倩王飞赵华阳陈国萍
Owner JIANGSU ZHONGBANG PHARMA
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