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Preparation Method Of The Solid Formulation Of Clopidogrel Bisulfate

a technology of clopidogrel and bisulfate, which is applied in the field of preparation of clopidogrel bisulfate tablets, can solve the problems of poor final product quality and sticking problem

Inactive Publication Date: 2013-01-10
SHANGHAI ANBISON LAB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent describes a new way to make Clopidogrel bisulfate tablets that don't stick to the punch and die during manufacturing. This is done by adding a substance called Colloidal Silicon Dioxide, which isolates the Clopidogrel bisulfate particles from the environment, reducing the risk of sticking. The result is smoother and clearer tablet surfaces, with no defects caused by sticking.

Problems solved by technology

It is known to one skilled in the art that the most difficult problem in preparation technology of Clopidogrel bisulfate tablets is in that the Clopidogrel bisulfate tends to adhere strongly to the punch and / or the die surfaces of a conventional tablet compression machine, causing picking, sticking or other kinds of surface irregularities on tablets, which consequently leads to poor final product quality.
The root cause is attributed to the extremely hygroscopic nature of Clopidogrel bisulfates which makes the material extremely adhesive to the metal surfaces of the punch and / or the die, and further compression between the upper / lower punch and the die causes the Clopidogrel bisulfate to rapidly form a film on the surface of the punch and die therefore cause a sticking problem.

Method used

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  • Preparation Method Of The Solid Formulation Of Clopidogrel Bisulfate

Examples

Experimental program
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example 1

preparing Clopidogrel Bisulfate Tablets

[0064]97.88 g Clopidogrel bisulfate was mixed with 60.0 g Lactose, 40.00 g Microsrystalline Cellulose. Adding the 10% prepared Hydroxypropyl Cellulose solution and granulation. The granules were dried and screening. Blending with 26.00 g Microcrystalline Cellulose, 6.00 g Crospovidone, 17.00 g of Hydrogenated Vegetable Oil and Sodium Lauryl Sulphate and compression. The tablet weight is 250 mg with diameter 9 mm.

example 2

[0065]97.88 g Clopidogrel bisulfate was mixed with 60.00 g Lactose, 40 g of Microcrystalline Cellulose. Adding the 10% prepared Hydroxypropyl Cellulose solution and granulation. The granules were dried and blended with Aerosil (1.5 g, the weight equivalent to 0.6% of tablet weight), Microcrystalline Cellulose 26.00 g, Crospovidone 6.00 g, 17.00 g Hydrogenated Vegetable Oil and Sodium Lauryl Sulphate. Then compression with tablet weight 250 mg and diameter 9 mm.

example 3

[0066]97.88 g Clopidogrel bisulfate was premixed with Aerosil, (0.75 g, equivalent to 0.3% of tablet weight), then mixed with Lactose 60.00 g, Microcrystalline Cellulose 40.00 g. Adding the 10% prepared Hydroxypropyl Cellulose solution to and granulation. The granules were dried and blended with Microcrystalline Cellulose 26.00 g, Crospovidone 6.00 g, 17.00 g Hydrogenated Vegetable Oil and Sodium Lauryl Sulphate. Then compression with tablet weight 250 mg with diameter 9 mm.

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Abstract

A solid formulation of clopidogrel bisulfate and its preparation method are disclosed. The formulation comprises clopidogrel bisulfate as active ingredient, colloidal silicon dioxide as anti-adherent / coating and the carriers selected from diluent, binder, glidant, disintegrant and / or lubricant.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]The present application is a continuation of pending International patent application PCT / CN2010 / 073879 filed on Jun. 12, 2010 which designates the United States and claims priority from Chinese patent application 201010106188.X filed on Feb. 5, 2010. The content of all prior applications is incorporated herein by reference.FIELD OF THE INVENTION[0002]This invention relates to a method of preparation of Clopidogrel bisulfate tablets.BACKGROUND OF THE INVENTION[0003]Chemically Clopidogrel bisulfate is methyl(+)-(S)-α(2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-acetate sulfate (1:1).[0004]One of Clopidogrel bisulfate structural formula is as follows:[0005]Clopidogrel bisulfate is an inhibitor of ADP-induced platelet aggregation acting by direct inhibition of adenosine diphosphate (ADP) binding to its receptor and of the subsequent ADP-mediated activation of the glycoprotein GPIIb / IIIa complex. In addition to ADP, Clopidogrel also...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/14A61K9/20A61P7/02A61K31/4365
CPCA61K31/4365A61K9/20A61K9/2095A61P7/02A61K9/2009
Inventor LEI, JIFENGSHA, PINGJIN, RONGGENSHI, YUWENSHEN, XINHUA
Owner SHANGHAI ANBISON LAB
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