Clopidogrel hydrogen sulfate tablet as well as preparation method and use

A technology of clopidogrel bisulfate tablets and clopidogrel bisulfate, which is applied in the field of clopidogrel bisulfate tablets and its preparation, can solve the problems of easy sticking, poor stability and poor fluidity of finished preparations, and reduce The effect of fine powder amount, prolonged drying time, and improvement of fluidity problems

Inactive Publication Date: 2018-04-24
湖南天济草堂制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The purpose of the present invention is to solve the shortcomings of poor fluidity, easy sticking, and poor stability of finished preparations in the prior art, and propose a clopidogrel bisulfate tablet and its preparation method and use

Method used

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  • Clopidogrel hydrogen sulfate tablet as well as preparation method and use
  • Clopidogrel hydrogen sulfate tablet as well as preparation method and use
  • Clopidogrel hydrogen sulfate tablet as well as preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036]

[0037]

[0038] The preparation method comprises the following steps:

[0039] S1. Polyethylene glycol 6000 is mixed with ethanol with a purity of 70% to obtain a 10% polyethylene glycol solution;

[0040] S2. Put clopidogrel bisulfate, microcrystalline cellulose, mannitol, low-substituted hydroxypropyl cellulose, and polyethylene glycol 6000 in a wet granulator, mix for 5 minutes until fully mixed, and then add 10% polyethylene glycol Ethylene glycol solution, make soft material for 1 minute, and granulate through a swing granulator (20 mesh stainless steel sieve);

[0041] S3. Dry the wet granules in a boiling dryer, set the air inlet temperature to 60°C, dry until the material temperature reaches 40°C, stop heating, discharge, and granulate with a 18-mesh sieve;

[0042] S4, mixing the sized clopidogrel hydrogen sulfate particles with hydrogenated castor oil with a particle size of 75 microns, and compressing the mixed product into tablets;

[0043] S5. Coa...

Embodiment 2

[0045]

[0046]

[0047] The preparation method comprises the following steps:

[0048] S1. Polyethylene glycol 4000 is mixed with ethanol with a purity of 60% to obtain a 10% polyethylene glycol solution;

[0049] S2. Put clopidogrel bisulfate, microcrystalline cellulose, mannitol, low-substituted hydroxypropyl cellulose, and polyethylene glycol 4000 in a wet granulator, mix for 5 minutes until fully mixed, and add 10% polyethylene glycol Glycol solution, making soft material for 1 minute, granulating through a swinging granulator (20 mesh stainless steel sieve);

[0050] S3. Dry the wet granules in a boiling dryer, set the air inlet temperature to 60°C, dry until the material temperature reaches 40°C, stop heating, discharge, and granulate with a 18-mesh sieve;

[0051] S4, mixing the sized clopidogrel hydrogen sulfate particles with hydrogenated castor oil with a particle size of 100 microns, and compressing the mixed product into tablets;

[0052] S5. Coating to ob...

Embodiment 3

[0054]

[0055] The preparation method comprises the following steps:

[0056]S1. Polyethylene glycol 5000 is mixed with ethanol with a purity of 80% to obtain a 10% polyethylene glycol solution;

[0057] S2. Put clopidogrel bisulfate, microcrystalline cellulose, mannitol, low-substituted hydroxypropyl cellulose, and polyethylene glycol 5000 in a wet granulator, mix for 5 minutes until fully mixed, and add 10% polyethylene glycol Glycol solution, making soft material for 1 minute, granulating through a swinging granulator (20 mesh stainless steel sieve);

[0058] S3. Dry the wet granules in a boiling dryer, set the air inlet temperature to 60°C, dry until the material temperature reaches 40°C, stop heating, discharge, and granulate with a 18-mesh sieve;

[0059] S4, mixing the sized clopidogrel hydrogen sulfate particles with hydrogenated castor oil with a particle size of 90 microns, and compressing the mixed product into tablets;

[0060] S5. Coating to obtain clopidogr...

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Abstract

The invention discloses a clopidogrel hydrogen sulfate tablet as well as a preparation method and use thereof. The clopidogrel hydrogen sulfate tablet is prepared from the following raw materials in parts by weight: 90 to 100 parts of clopidogrel hydrogen sulfate, 100 to 200 parts of filling agent, 5 to 30 parts of disintegrating agent, 5 to 30 parts of polyethylene glycol, and 5 to 30 parts of anti-sticking agent. The preparation method comprises the following steps: S1: preparing a polyethylene glycol solution; S2: uniformly mixing the clopidogrel hydrogen sulfate, the filling agent and thedisintegrating agent, adding the polyethylene glycol solution, preparing a soft material, then granulating, drying, and shaping; S3: adding the anti-sticking agent, mixing, tabletting, coating, thus obtaining the clopidogrel hydrogen sulfate tablet. The use of the clopidogrel hydrogen sulfate tablet can prevent and treat cerebral-cardio diseases and other artery circulatory disturbance diseases caused by the high clustering degree of blood platelets. The clopidogrel hydrogen sulfate tablet and the preparation method thereof have the advantages that the sticking in the tabletting process and the slow disintegration of the tablet can be effectively reduced, the tabletting process is ensured to be smooth, a main drug is ensured to dissolve out rapidly, and the bioavailability of the drug canbe improved.

Description

technical field [0001] The invention relates to the technical field of drug research and development, in particular to a clopidogrel bisulfate tablet and a preparation method and application thereof. Background technique [0002] Clopidogrel hydrogen sulfate (CAS: 135046-48-9), the sulfate salt of clopidogrel, English name ClopidogrelHydrogen Sulfate, chemical name: (s)-α-(2-chlorophenyl)-6,7- Methyl dihydrothieno[3,2-c]pyridine-5(4H)acetate hydrogensulfate. Clopidogrel bisulfate is an antiplatelet agent. The product was developed by the French pharmaceutical company Sanofi-Aventis and was first launched in the UK and the US in 1998. Clopidogrel bisulfate entered China in 2001. Clopidogrel bisulfate is mainly used clinically to treat acute Myocardial infarction, stroke, and peripheral arterial disease can reduce the time to atherosclerosis. [0003] CN102485218A discloses a dry granulation preparation method of clopidogrel bisulfate tablets. The disadvantages of the dry g...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4365A61K47/10A61K9/28A61P9/10A61P7/02
CPCA61K9/1617A61K9/2031A61K9/2806A61K31/4365
Inventor 李林梅宋太发向忠友翁小涛谢峰索成林王金华彭芳薇
Owner 湖南天济草堂制药股份有限公司
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