Preparation method of crystalline clopidogrel bisulfate tablets

A technology for clopidogrel hydrogen sulfate tablets and clopidogrel hydrogen sulfate tablets, which are applied in the directions of medical preparations without active ingredients, medical preparations containing active ingredients, and pill delivery, etc. , can not be dealt with, and the problem of sticking and punching during tableting

Active Publication Date: 2011-11-16
天津泰普制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In order to ensure that its related substances will not increase, therefore: the conventional wet granulation tabletting method cannot be used; if the raw material and auxiliary materials are used for direct tableting, it is not feasible to stick the raw material and have cracks; if the dry granulation tabletting method is used, the raw material granules The surface treatment is not complete, and it is better than direct tableting during tableting. There i

Method used

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  • Preparation method of crystalline clopidogrel bisulfate tablets
  • Preparation method of crystalline clopidogrel bisulfate tablets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Clopidogrel Bisulfate Form I 98.875g

[0054]Methanol 300ml

[0055] Macrogol 4000 10g

[0056] Hydroxypropyl Cellulose 2g

[0057] Lactose 118g

[0058] Microcrystalline Cellulose 19g

[0059] Pregelatinized starch 8.125g

[0060] Hydrogenated Vegetable Oil 3g

[0061]

[0062] Process: Sieve type I clopidogrel hydrogen sulfate according to the above weight for later use; take polyethylene glycol and hydroxypropyl cellulose, stir and dissolve them in methanol, let cool, add type I clopidogrel hydrogen sulfate; evaporate the solvent, Allow to cool to room temperature; sieve the clopidogrel bisulfate inclusion agent granules and mix with other excipients and press into tablets.

Embodiment 2

[0064] Clopidogrel Bisulfate 97.875g

[0065] Acetone 50ml

[0066] Macrogol 6000 5g

[0067] Lactose 118g

[0068] Microcrystalline Cellulose 19g

[0069] Pregelatinized starch 8.125g

[0070] Hydrogenated Vegetable Oil 3g

[0071]

[0072] Process: sieve clopidogrel hydrogen sulfate according to the above weight for later use; take polyethylene glycol, stir in acetone, heat to dissolve, let cool, add clopidogrel hydrogen sulfate, evaporate the solvent, and sieve to obtain clopidogrel hydrogen sulfate Inclusion agent granules, then mixed with other auxiliary materials and pressed into tablets.

Embodiment 3

[0074] Clopidogrel Bisulfate 97.875g

[0075] Chloroform 250ml

[0076] Macrogol 10000 10g

[0077] Lactose 118g

[0078] Microcrystalline Cellulose 19g

[0079] Pregelatinized starch 8.125g

[0080] Hydrogenated Vegetable Oil 3g

[0081]

[0082] Process: sieve clopidogrel hydrogen sulfate according to the above weight for later use; take polyethylene glycol, stir and heat to dissolve in chloroform, let it cool, add clopidogrel hydrogen sulfate, stir and heat to 45°C to dissolve, evaporate to dryness, and sieve to obtain Clopidogrel bisulfate inclusion agent granules, then mixed with other auxiliary materials and compressed into tablets.

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Abstract

The invention provides a preparation method of crystalline clopidogrel bisulfate tablets, comprising the following steps of: mixing a medicinal solvent and an inclusion agent with stirring, dissolving by heating to the temperature of 35-90 DEG C, staying cool to room temperature; adding the crystalline clopidogrel bisulfate with uniformly stirring; drying the medicinal solvent by distillation, sieving to obtain clopidogrel bisulfate inclusion particles; uniformly mixing the obtained clopidogrel bisulfate inclusion particles and a pharmaceutic adjuvant at the weight part ratio of 1:0.02-10, followed by tabletting, wherein the addition amount of the inclusion agent is 0.05-0.2 times the weight of clopidogrel bisulfate and the addition amount of the medicinal solvent is 0.5-10 times the weight of clopidogrel bisulfate. According to the clopidogrel bisulfate tablets provided by the invention, the crystal form is not changed; related substances are not increased, the fluidity and compressibility of the raw materials are enhanced, and the stability of the tablets is raised; in addition, the preparation method of the tablets is more suitable for large-scale industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a preparation method of crystalline clopidogrel bisulfate tablets. Background technique [0002] Cardiovascular and cerebrovascular thrombosis is a common disease in my country and an important cause of death. Especially in recent years, the incidence of thromboembolic diseases, mainly coronary thrombosis and cerebral thrombosis, is on the rise, seriously endangering human health. [0003] Clopidogrel is a platelet aggregation inhibitor. ATC classification is: B01AC / 04. Clopidogrel also selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet receptor and the activation of the secondary ADP-mediated glycoprotein GPlllb / llla complex, thus inhibiting platelet aggregation. Clopidogrel must Platelet aggregation can be inhibited by biotransformation, but no active metabolite producing this effect has been isolated. In addition to ADP, clopi...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4365A61K47/34A61K47/38A61K47/36A61K47/44A61P9/10A61P9/00A61P7/02
Inventor 周世旺刘衡姜瑛
Owner 天津泰普制药有限公司
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