Solid preparation of clopidogrel free alkali and preparation process thereof

A technology of clopidogrel free base and solid preparation, applied in the field of solid preparation of clopidogrel free base and its preparation, to achieve the effect of improving safety, stability and effective therapeutic effect

Inactive Publication Date: 2010-07-07
JBC PHARMLAB +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by this invention is to provide a solid preparation of clopidogrel free base and a preparation method thereof, which solves the problem of clopidogrel hydrolyzate in the production of solid preparations of clopidogrel free base and improves the production rate of clopidogrel. The safety and stability of the solid preparation of the free base make it more effective in its therapeutic effect

Method used

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  • Solid preparation of clopidogrel free alkali and preparation process thereof
  • Solid preparation of clopidogrel free alkali and preparation process thereof
  • Solid preparation of clopidogrel free alkali and preparation process thereof

Examples

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preparation example Construction

[0013] The preparation method of the solid preparation of the above-mentioned clopidogrel free base, the method is prepared by wet granulation, and the specific steps are as follows:

[0014] 1) Mix anhydrous lactose, microcrystalline cellulose, mannitol, and hydroxypropyl cellulose evenly, add clopidogrel free alkali solution for wet granulation, fluidize boiling drying, and sieve the granules through a high-speed crushing and sizing machine with a size of 1.0mm grain.

[0015] 2) Mix the granules obtained in operation 1) with part of the pregelatinized starch, fumed silicon dioxide, and magnesium stearate, and then make a solid preparation through a suitable method.

[0016] In the above operation 1), in order to meet the uniformity of clopidogrel free base, fully stirring and cutting in a high-speed wet granulator is adopted. In order to meet the uniformity of particle size, use a high-speed crushing and sizing machine with a 1.0mm sieve for sizing.

[0017] In the above-...

Embodiment 1

[0019] Tablet prescription with unit tablet weight 0.500g, clopidogrel labeled content 75mg / tablet and wet granulation preparation process

[0020] prescription

quantity

content%

Clopidogrel free base

75g

15％

anhydrous lactose

120g

24％

microcrystalline cellulose

200g

40％

[0021] prescription

quantity

content%

Mannitol

20g

4％

Hydroxypropyl Cellulose

20g

4％

partially pregelatinized starch

50g

10％

fumed silica

10g

2％

Magnesium stearate

5g

1％

Total

500g

100％

[0022] 1) Mix 120g of anhydrous lactose, 200g of microcrystalline cellulose, 20g of mannitol, and 20g of hydroxypropyl cellulose, and add clopidogrel free base (75g) solution for wet granulation, fluidized boiling drying, and granulation by high-speed crushing Granulator 1.0mm sieve for granulation.

[0023] 2) Mix 343g of th...

Embodiment 2

[0025] Tablet prescription with unit tablet weight 0.420g, clopidogrel labeled content 75mg / tablet and wet granulation preparation process

[0026] prescription

quantity

content%

Clopidogrel free base

75g

17.9％

anhydrous lactose

123g

29.3％

microcrystalline cellulose

140g

33.3％

Mannitol

15g

3.6％

Hydroxypropyl Cellulose

15g

3.6％

partially pregelatinized starch

40g

9.5％

fumed silica

8g

1.9％

Magnesium stearate

4g

0.9％

Total

420g

100％

[0027] 1) Mix 123g of anhydrous lactose, 140g of microcrystalline cellulose, 15g of mannitol, and 15g of hydroxypropyl cellulose, add clopidogrel free base (75g) solution for wet granulation, fluidize boiling drying, and granulate through high-speed pulverization Granulator 1.0mm sieve for granulation.

[0028] 2) Mix 374g of the granules obtained in operation 1) with 40g of ...

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Abstract

The invention relates to a solid preparation of clopidogrel free alkali and a preparation process thereof. The solid preparation uses the clopidogrel free alkali as the principal agent, and is mixed with anhydrous lactose, microcrystalline cellulose, mannitol, hydroxy propyl cellulose, part of pregelatinized starch, fumed silica and magnesium stearate which are used as auxiliary materials. The method uses the wet granulation to prepare. The solid preparation of the invention solves the problem of clopidogrel hydrolysates during the production of the solid preparation of the clopidogrel free alkal, and the safety and the stability of the solid preparation of the clopidogrel free alkali are improved, and the solid preparation of the clopidogrel free alkali can be more effective to have the therapeutic effect.

Description

technical field [0001] The invention relates to a solid preparation of clopidogrel free base and a preparation method thereof. Background technique [0002] Clopidogrel is an inducible platelet aggregation inhibitor, which can selectively inhibit the binding of ADP to platelet receptors, and then inhibit the activation of ADP and glycoprotein GP II b / IIIa complex, thereby inhibiting the aggregation of platelets. This product can also inhibit platelet aggregation caused by non-ADP without affecting the activity of phosphodiesterase. This product affects the lifespan of platelets by irreversibly changing platelet ADP receptors. Clopidogrel reduces the chance of arterial blockage by inhibiting platelet aggregation, achieves the effect of preventing stroke and heart attack, and can effectively treat and prevent atherosclerosis. [0003] Clopidogrel is an inactive prodrug that is metabolized into active metabolites by hepatic cytochrome P450. Its structure is as follows: [0...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/48A61K31/4365A61K47/38A61P7/02
Inventor 王建国
Owner JBC PHARMLAB
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