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Preparation method of clopidogrel bisulfate solid preparation

A technology of clopidogrel bisulfate solid and clopidogrel bisulfate, which is applied in the field of biomedicine, can solve the problems of increased impurities in drugs, rapid increase of impurities, and decreased stability of drugs, so as to reduce the amount of impurities produced, heat The effect of shortening the time and reducing the impact

Active Publication Date: 2019-10-18
GUANGZHOU BAIYUSN TIANXIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In the above dry granulation process, 20-80 mesh particles are screened in the dry granulation step, and the remaining materials are returned to the granulator to continue granulation. Repeated granulation not only prolongs the production time and increases the production cost, but also the compressibility of the fine powder changes after the second dry method, and the dissolution rate of the obtained granules is different from that of the first dry method, which affects the RSD during dissolution , resulting in tablet dissolution instability
The simple melt granulation process will cause problems such as increased impurities of the drug when heated, poor granulation effect, poor fluidity during tablet compression, and large differences in loading capacity, and slow dissolution of the drug in the preparation, decreased stability of the drug after long-term sample retention, and increased impurities. high speed

Method used

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  • Preparation method of clopidogrel bisulfate solid preparation
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  • Preparation method of clopidogrel bisulfate solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1、4

[0036] See Table 1 and Table 2 for formula (calculated per tablet);

[0037] The preparation method that adopts is as follows:

[0038] Step (1) Weigh clopidogrel bisulfate, anhydrous lactose, PEG-6000, microcrystalline cellulose, and low-substituted hydroxypropyl cellulose according to the formulas in Examples 1 and 4, and mix them uniformly to obtain the first mixture; Put the first mixture into the melt granulation equipment, raise the temperature to 58°C, and keep it warm for 5 minutes to obtain the second mixture; cool the second mixture to 38°C, pass through a 16-mesh sieve for granulation, and obtain granule A;

[0039] Step (2) Mix the granules A with the hydrogenated castor oil (added first) in the formulas of Examples 1 and 4 to obtain the third mixture, and use the dry press granulator to press the third mixture into granules, and set the pressure of the pressing wheel 30bar, use a 1.5mm sieve to sieve to obtain granule B;

[0040] Step (3) Granule B was uniformly...

Embodiment 2、5

[0042] See Table 1 and Table 2 for formula (calculated per tablet);

[0043] The preparation method that adopts is as follows:

[0044] Step (1) Weigh clopidogrel bisulfate, anhydrous lactose, PEG-6000, microcrystalline cellulose, and low-substituted hydroxypropyl cellulose according to the formulas in Examples 2 and 5, and mix them uniformly to obtain the first mixture; Put the first mixture into the melt granulation equipment, raise the temperature to 70°C, and keep it warm for 15 minutes to obtain the second mixture; cool the second mixture to 25°C, pass through a 24-mesh sieve for granulation, and obtain the granule A;

[0045] Step (2) Mix the granule A with the hydrogenated castor oil (added first) in the formulas of Examples 2 and 5 to obtain the third mixture, and press the third mixture into granules with a dry press granulator, and set the pressure of the roller to 70bar. Sizing with a 1.0mm sieve to obtain granule B;

[0046] Step (3) Granule B was uniformly mixed...

Embodiment 3、6

[0048] See Table 1 and Table 2 for formula (calculated per tablet);

[0049] The preparation method that adopts is as follows:

[0050] Step (1) Weigh clopidogrel bisulfate, anhydrous lactose, PEG-6000, microcrystalline cellulose, and low-substituted hydroxypropyl cellulose according to the formulas in Examples 3 and 6, and mix them uniformly to obtain the first mixture; Put the first mixture into the melt granulation equipment, raise the temperature to 60°C, and keep it warm for 10 minutes to obtain the second mixture; cool the second mixture to 30°C, pass through a 20-mesh sieve for granulation, and obtain the granule A;

[0051] Step (2) Mix the granule A with the hydrogenated castor oil (added first) in the formulations of Examples 3 and 6 to obtain the third mixture, and press the third mixture into granules with a dry press granulator, and set the pressure of the roller to 50 bar. Sizing with a 1.2mm sieve to obtain granule B;

[0052] Step (3) Granule B was uniformly ...

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Abstract

The invention relates to a preparation method of a clopidogrel bisulfate solid preparation. The method discloses a two-step granulation process of melt-granulating and then dry-pressing granulating for clopidogrel bisulfate, and the obtained granules have good compressibility and fluidity, and are not easy to stick to a die, so that the problems of tablet sticking, easy revealing or splitting which are common in the preparation of oral tablets of clopidogrel bisulfate is solved. The preparation method can ensure the rapid dissolution of the drug in the preparation, and the long-term retentionof the sample does not increase the impurities. The preparation process of the present invention is highly practical and can be used for large-scale preparation of clopidogrel sulfate bulk drugs withdifferent physical properties.

Description

technical field [0001] The invention belongs to the field of biomedicine, in particular to a preparation method of clopidogrel bisulfate solid preparation. Background technique [0002] According to survey results, ischemic heart disease and cerebrovascular disease have become the main causes of death in 8 major regions of the world, including developed and developing countries. In my country, cardiovascular and cerebrovascular diseases have also become one of the common frequently-occurring diseases of the elderly, especially cerebrovascular diseases, with a prevalence rate as high as 491.8 / 100,000, which is significantly higher than that in Western countries. Therefore, research on the prevention and treatment of such diseases is very important. [0003] The basic drugs for antithrombotic treatment of cerebral infarction are low molecular weight heparin and enteric-coated aspirin, but it takes several days for low-dose aspirin to exert sufficient antiplatelet effect. Clo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/30A61K31/4365A61P9/10
CPCA61K9/2095A61K9/282A61K31/4365A61P9/10
Inventor 谭胜连梁伟俊关展姬黄小光杨轶群傅红燕
Owner GUANGZHOU BAIYUSN TIANXIN PHARMA
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