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Method for preparing azilsartan solid composition

A solid composition, composition technology, applied in the field of medicine, to achieve the effect of prolonging the shelf life

Inactive Publication Date: 2014-04-09
CHINA RESOURCES SAIKE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In order to reduce the problem of sharp increase of azilsartan impurities in the micronization process, the technical field needs to provide an effective preparation method of azilsartan solid composition

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] In this example, the azilsartan API crushed by jet mill is used to prepare azilsartan tablets, which are made of the following raw materials, of which the weight of the tablet is 130 mg, and 1000 tablets are made: 20 g of azilsartan API (jet milling), lactose 67.2g, PEG6000 2.7g, precrossified starch Starch 1500 15g, hydroxypropyl cellulose (HPC-L) 3g, microcrystalline cellulose PH101 15g, low-substituted hydroxypropyl cellulose 6.4g, and magnesium stearate 0.7 g. The preparation method comprises the following steps:

[0024] 1) Mix azilsartan API (jet milling), PEG6000, HPC-L and about 50ml of water evenly to obtain suspension solution Ⅰ;

[0025] 2) Add lactose, precrossified starch Starch 1500 and microcrystalline cellulose PH101 into the fluidized bed, and fluidize and mix evenly;

[0026] 3) Spray the suspension solution I into the composition in step 3) using a fluidized bed, and dry to prepare the granule I of the azilsartan pharmaceutical composition;

[0027...

Embodiment 2

[0031] In this example, azilsartan tablets were prepared using mechanically sheared and pulverized (low temperature) azilsartan API. Made from the following weights of raw materials, of which the tablet weight is 130mg, made into 1000 tablets: Azilsartan API (mechanically sheared and crushed) 20g, lactose 67.2g, PEG6000 2.7g, precrossified starch Starch 1500 15g, hydroxypropyl Cellulose (HPC-L) 3g, microcrystalline cellulose PH101 15g, low-substituted hydroxypropyl cellulose 6.4g, and magnesium stearate 0.7g. The preparation method comprises the following steps:

[0032] 1) Mix Azilsartan API (mechanically sheared and pulverized), PEG6000, HPC-L with about 50ml of water to obtain suspension solution Ⅰ;

[0033] 2) Add lactose, precrossified starch Starch 1500 and microcrystalline cellulose PH101 into the fluidized bed, and fluidize and mix evenly;

[0034] 3) Spray the suspension solution I into the composition in step 3) using a fluidized bed, and dry to prepare the granule...

Embodiment 3

[0039] The azilsartan tablet is made of the following weight raw materials, wherein the tablet weighs 130mg, and is made into 1000 tablets: azilsartan API 20g, lactose 67.2g, PEG6000 2.7g, precrossed starch Starch 1500 15g, hydroxypropyl Hydroxyl cellulose (HPC-L) 3g, microcrystalline cellulose PH101 15g, low-substituted hydroxypropyl cellulose 6.4g, and magnesium stearate 0.7g. The preparation method of described Azilsartan tablet comprises the following steps:

[0040] 1) Mix Azilsartan API (not micronized), PEG6000, HPC-L and about 50ml of water to obtain suspension solution I;

[0041] 2) Put the suspension solution I into a high-speed stirring bead mill for wet grinding and pulverization to obtain the suspension solution II;

[0042] 3) Add lactose, precrossified starch Starch 1500 and microcrystalline cellulose PH101 into the fluidized bed, and fluidize and mix evenly;

[0043] 4) Spray the suspension solution II into the composition in step 3) using a fluidized bed, a...

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PUM

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Abstract

The invention discloses a method for preparing an azilsartan solid composition. The preparation method comprises the following steps: (1) adding water into azilsartan API (not subjected to micronization) and an adhesive for uniformly mixing to obtain a suspension solution I; (2) performing wet grinding on the suspension solution I to obtain a suspension solution II; (3) adding the suspension solution II into a diluent of a pharmaceutical composition in an injection mode, and drying to prepare granules and powder of an azilsartan pharmaceutical composition; (4) preparing the granules and powder into the medical minimum dose unit of azilsartan. The method has the beneficial effects that the problem that related substances are rapidly increased in the process of preparing azilsartan particles by adopting a conventional grinding method is solved, and the storage period of the azilsartan preparation is favorably prolonged.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a preparation method of azilsartan solid composition. 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 also the only angiotensin II receptor antagonist (sartan) drug in the late clinical stage . The drug was launched by Japan's Takeda Pharmaceutical Company in 2012, and its efficacy in the clinical stage is remarkable. [0003] Azilsartan is a poorly soluble drug with a solubility in water of less than 9 μg / ml. The bioavailability of a drug in the body is greatly affected by the dissolution of the drug. Therefore, in the preparation of its preparation, micronized azilsartan particles are often used, and the particle size is controlled below 15 μm. Conventional particle size reduction methods include mechanical methods and spray dryi...

Claims

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Application Information

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IPC IPC(8): A61K31/4245A61P9/12
Inventor 蒋玲敏白杰杨资伟杨琰
Owner CHINA RESOURCES SAIKE PHARMA
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