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Treatment method of azilsartan crude drug

A processing method and technology of raw material medicine, which is applied in the field of treatment of azilsartan raw material medicine, can solve the problems such as the increase of degradation impurities of azilsartan raw material medicine, and achieve the effect of long storage period

Inactive Publication Date: 2014-04-30
BEIJING PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The most commonly used mechanical methods are ball milling and jet milling. The friction generated during the crushing process will increase the temperature of the material, resulting in a sharp increase in the degradation impurities of the azilsartan API; while the spray drying method requires high heat consumption. When the solvent is evaporated at high temperature, the degradation impurities of azilsartan raw material drug will increase sharply

Method used

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  • Treatment method of azilsartan crude drug
  • Treatment method of azilsartan crude drug
  • Treatment method of azilsartan crude drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] The concrete steps of this embodiment are as follows:

[0022] (1) Take the azilsartan raw material, and measure its particle size with a Malvern laser particle size analyzer, D 90 =120.724μm;

[0023] (2) Weigh the prescribed amount of azilsartan API, granulate, compress, and coat the tablets according to the formula and process in Attached Table 1, and test the influencing factors of the coated tablets to determine its related substances. See the attached table for the results 2.

Embodiment 2

[0025] The concrete steps of this embodiment are as follows:

[0026] (1) Take the azilsartan bulk drug in Example 1, and after adopting mechanical pulverization for 30s, measure its particle size with a Malvern laser particle size analyzer, D 90 =12.463μm;

[0027] (2) Weigh the amount of azilsartan raw material that has been mechanically pulverized in step (1), granulate, compress, and coat the coated tablets according to the formula and process in Attached Table 1, and conduct the influencing factor test on the coated tablets. Determination of its related substances, the results are shown in Table 2.

Embodiment 3

[0029] The concrete steps of this embodiment are as follows:

[0030] (1) Take the azilsartan bulk drug in Example 1, and after being pulverized by jet milling, measure its particle size with a Malvern laser particle size analyzer, D 90 =12.500 μm.

[0031] (2) Take the azilsartan crude drug that has been pulverized in step (1) according to the formulation amount, granulate, compress, and coat the coated tablet according to the formula and process in Attached Table 1, and test the influencing factors of the coated tablet to determine its For the relevant substances, see the attached table 2 for the results.

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Abstract

The invention discloses a treatment method of an azilsartan crude drug. The preparation method comprises the following steps: dissolving azilsartan in a solvent, and extracting azilsartan by applying supercritical fluid in a supercritical state so as to provide particles of the azilsartan crude durg, wherein the D90 grain size is less than 15 micrometers, and the content of single impurities is less than 0.05%. The treatment method disclosed by the invention has the beneficial effects that the treatment method solves the problem that related substances are rapidly increased when conventional crushing methods are adopted to prepare azilsartan particles, and the storage period of the azilsartan preparation is prolonged.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a processing method of azilsartan bulk drug. 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 influenced by the dissolution rate of the drug. Therefore, in the preparation of its preparations, micronized azilsartan particles are often used, with a particle size of D 90 Controlled below 15μm. Conventional particle size reduction methods include mechanical methods and spray d...

Claims

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Application Information

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IPC IPC(8): C07D413/10A61K9/20A61P9/12
CPCC07D413/10Y02P20/54
Inventor 杨资伟蒋玲敏白杰杨琰王文峰
Owner BEIJING PHARMA GRP CO LTD
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