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A kind of preparation method of clopidogrel bisulfate solid preparation

A technology of clopidogrel hydrogen sulfate solid and clopidogrel hydrogen sulfate, which is applied in the field of biomedicine, can solve the problems such as the increase of impurities in the drug, the rapid increase of impurities, the unstable tablet dissolution, and the like, and can reduce the sticking time and the heating time. The effect of shortening and shortening the granulation time

Active Publication Date: 2021-07-02
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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  • A kind of preparation method of clopidogrel bisulfate solid preparation
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  • A kind of 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 the formula (in terms of each 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 hot-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 the pressure of the rollers is set to 30bar, use a 1.5mm sieve to sieve to obtain granule B;

[0040] Step (3) Granule B is u...

Embodiment 2、5

[0042] See Table 1 and Table 2 for the formula (in terms of each 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 hot-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 Granule A;

[0045] Step (2) Mix the granule A with the hydrogenated castor oil (add first) of the formula amount of Example 2 and 5 to obtain the third mixture, and the third mixture is pressed into granules using a dry pressing granulator, and the pressure of the pressure wheel is set at 70bar. Sizing with a 1.0mm sieve to obtain granule B;

[0046] Step (3) ...

Embodiment 3、6

[0048] See Table 1 and Table 2 for the formula (in terms of each 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 hot-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 Granule A;

[0051] Step (2) Mix the granule A with the hydrogenated castor oil (add first) of the formula amount of Example 3 and 6 to obtain the third mixture, and the third mixture is pressed into granules using a dry pressing granulator, and the pressure of the pressure wheel is set at 50 bar. Sizing with a 1.2mm sieve to obtain granule B;

[0052] Step (3)...

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Abstract

The invention relates to a preparation method of clopidogrel bisulfate solid preparation. The invention discloses a two-step granulation process of clopidogrel bisulfate which is firstly melted and granulated, and then dry-pressed. The common problems of tablet sticking, easy uncapping or splitting during preparation of preparations. The invention can ensure rapid dissolution of the medicine in the preparation, and the impurities in the long-term reserved sample of the preparation will not increase greatly. Moreover, the preparation process of the present invention has strong practicability and can be used for large-scale production of clopidogrel bisulfate raw material medicines with different 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 Patents(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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