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Solid pharmaceutical composition containing benzimidazole derivative

A composition and drug technology, applied in the field of preparation of antihypertensive drugs, can solve the problems of failure to prove the dissolution advantage and limited improvement effect

Active Publication Date: 2015-06-17
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, the drug dissolution properties of solid dosage forms containing low-melting oily substances have been improved, but the specific implementation methods given are all dissolution experiments under high pH (pH6.8) conditions, and it has not been proved that it is in the human environment. Dissolution advantage
Determination of the dissolution rate of the pharmaceutical composition provided by this patent application under low pH conditions shows that its improvement effect is very limited

Method used

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  • Solid pharmaceutical composition containing benzimidazole derivative
  • Solid pharmaceutical composition containing benzimidazole derivative
  • Solid pharmaceutical composition containing benzimidazole derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Azilsartan (64g) treated by jet milling (d(0.5)=2.61μm, d(0.9)=5.24μm), mixed with mannitol (200g), microcrystalline cellulose (30g), croscarmellose Sodium cellulose cellulose (16g) was mixed evenly, and 5% hydroxypropyl cellulose aqueous solution was used as a binding agent, granulated, dried in a fluidized bed, and granulated with a 1.0mm sieve. Add 3.3 g of magnesium stearate to the sized granules, and mix well. The resulting mixture was tabletted through a 7.0 mm punch to obtain a plain tablet having the following composition.

[0033] Composition of preparation (per 159.6mg)

[0034]

[0035]

Embodiment 2

[0037] Mix azilsartan (64g) and β-cyclodextrin (384g) uniformly, add 768g of water, grind for 6 hours until it becomes semi-solid, and dry under reduced pressure at 40°C to obtain a solid. The obtained solid was washed with appropriate amount of water and methanol, and dried under reduced pressure to obtain clathrate. Take appropriate amount of clathrate (containing 32g of azilsartan), mix well with mannitol (100g), microcrystalline cellulose (15g), croscarmellose sodium (8g), and use 5% hydroxypropyl cellulose The plain aqueous solution is used as a binder, granulated, fluidized bed dried, and granulated with a 1.0mm sieve. Add 3.3 g of magnesium stearate to the sized granules, and mix well. The resulting mixture was tabletted through a 10.0 mm punch to obtain a plain tablet having the following composition.

[0038] Composition of preparation (per 345.5mg)

[0039]

Embodiment 3

[0041] Azilsartan (64g), mixed with mannitol (90g), microcrystalline cellulose (90g), croscarmellose sodium (15g), sodium carbonate (40g), was mixed with 5% hydroxypropyl The cellulose aqueous solution is used as a binder, granulated, fluidized bed dried, and granulated with a 1.0mm sieve. Add 3 g of magnesium stearate to the sized granules, and mix well. The resulting mixture was tabletted through a 7.0 mm punch to obtain a plain tablet having the following composition.

[0042] Composition of preparation (per 156mg)

[0043]

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PUM

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Abstract

A solid pharmaceutical composition containing a benzimidazole derivative and preparation method therefor, said solid pharmaceutical composition being used for regulating degrees of drug dissolution and / or improving stability, and the uses of same in the preparation of drugs for treating circulatory diseases.

Description

technical field [0001] The invention relates to a solid pharmaceutical composition for improving drug dissolution rate and / or stability, a preparation method thereof, and an application in the preparation of antihypertensive drugs. Background technique [0002] Diseases of the circulatory system, also known as cardiovascular diseases, refer to diseases of the heart, blood vessels, and nervous mechanisms that regulate blood circulation. Heart disease and high blood pressure are the most common. Circulatory system diseases are common diseases, especially in internal medicine diseases. Heart disease is often protracted, affecting life and work, and the mortality rate is also high. With the control of infectious diseases, cardiovascular disease has become more prominent in the cause of population death. Diseases of the circulatory system can be divided into two categories: congenital and acquired. Congenital cardiovascular disease is caused by abnormal development of the grea...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/4184A61K47/02A61P9/00A61P9/12
CPCA61K9/2009A61K9/2013A61K9/2018A61K9/2027A61K9/2031A61K9/2054A61K9/2059A61K9/2846A61K47/6951A61P9/00A61P9/12B82Y5/00A61K9/20A61K31/4184A61K47/02
Inventor 徐坚周晓堂宋阳刘晓枫张春红
Owner JIANGSU HENGRUI MEDICINE CO LTD
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