Composition containing clopidogrel bisulfate crystal particles

A technology of clopidogrel hydrogen sulfate solid and clopidogrel hydrogen sulfate, which is applied in the field of preparations containing the clopidogrel hydrogen sulfate crystal particles and its preparation, can solve the problems of less static electricity, strong static electricity, and difficult realization, and achieve Avoid Mass Generated Effects

Active Publication Date: 2010-10-06
ZHEJIANG HUAHAI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The median particle size D50 of the clopidogrel hydrogen sulfate bulk drug obtained by direct crystallization is 50-100 μm, which has strong static electricity, and the method of direct crystallization with a solvent is used to prepare clopidogrel hydrogen sulfate with less static electricity and a median particle size D50 greater than 120 μm gray is not easy to achieve

Method used

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  • Composition containing clopidogrel bisulfate crystal particles
  • Composition containing clopidogrel bisulfate crystal particles
  • Composition containing clopidogrel bisulfate crystal particles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0084] Turn on the Alexanderwerk dry granulator, set the feeding speed to 20rpm, the pinch wheel speed to 5rpm, the pinch wheel pressure to 30bar, and the pinch wheel gap to 2.5mm, add clopidogrel bisulfate fine powder to the Alexanderwerk dry granulator In the feeding hopper, the sheet or block is formed by the rolling of the pressing wheel, and then the sheet or block is cut into small pieces or small pieces by the cutting knife, and then the whole grain is sized by the whole grain knife, and the speed of the whole grain knife is 100 rpm, and then sieved through an upper sieve of 2.0 mm and a lower sieve of 0.63 mm to obtain clopidogrel hydrogen sulfate crystal particles with a particle size of 120-1000 μm.

[0085] Table 1 Comparison of granule properties between clopidogrel bisulfate crystal granules and starch lactose

[0086]

[0087]

[0088]The median particle diameter D50 of the clopidogrel hydrogen sulfate crystalline particles obtained by Malvern...

Embodiment 2

[0090] A tablet prepared by direct compression of crystalline granules of clopidogrel bisulfate with a median diameter D50 of 150-500 μm.

[0091] Tablet composition:

[0092]

[0093] The clopidogrel bisulfate crystal particles obtained from Example 1 were sieved with a sieve with a pore size of 1.2 mm, and mixed at a speed of 10 rpm for 10 minutes in an HBD-100 mixing drum, and low-substituted hydroxypropyl cellulose and hydroxypropyl cellulose were added. Methylcellulose, starch lactose, continue to mix for 15 minutes and pass through a 1.2mm sieve, pass hydrogenated cottonseed oil through a 250μm sieve, add, continue to mix for 5 minutes and then discharge.

[0094] A circular punch with a diameter of 8.0 is installed on the FETTE tablet press, and 20 kg of the obtained mixture is compressed at a speed of 100,000 tablets / hour, with a core weight of 200 mg and a batch of 100,000 tablets. High-speed tablet pressing, one-sided non-stick punching. The finished clopidogrel...

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Abstract

The invention discloses clopidogrel bisulfate crystal particles with the median particle diameter of at least 120 microns. The invention also discloses a method for preparing the crystal particles, a pharmaceutical composition containing the crystal particles and a preparation method of the pharmaceutical composition.

Description

technical field [0001] The present invention relates to antiplatelet drug clopidogrel hydrogen sulfate crystal particles and a preparation method thereof, as well as a preparation containing the clopidogrel hydrogen sulfate crystal particles and a preparation method thereof. technical background [0002] Clopidogrel is a well-known platelet inhibitor having the following structure. [0003] [0004] It is reported in US4847265 that inhibition of platelet aggregation by clopidogrel can reduce the chance of arterial embolism, effectively prevent and treat diseases such as atherosclerosis and heart disease. Clopidogrel is a viscous oily substance. In order to be more suitable for preparations, clopidogrel is used in preparations in the form of salts, such as clopidogrel bisulfate, named in China as clopidogrel bisulfate and Clopidogrel besylate, etc. [0005] Clopidogrel bisulfate has the following structural formula: [0006] [0007] At present, clopidogrel bisulfate...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D495/04A61K31/4365A61K9/20A61K9/48A61K9/16A61P7/02A61P9/10A61P9/00B01J2/22
Inventor 李巧霞杜江永邱宗杰张龙辉彭俊清胡功允
Owner ZHEJIANG HUAHAI PHARMA CO LTD
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