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Clopidogrel hydrogen sulfate tablet medicine composition and preparation method thereof

A technology of clopidogrel bisulfate tablets and clopidogrel bisulfate, which is applied in the direction of drug combinations, pharmaceutical formulas, medical preparations containing active ingredients, etc., can solve problems affecting the dissolution of the main drug, and achieve improved material fluidity, Good safety and anti-deliquescence effect

Active Publication Date: 2015-04-22
CHENGDU EASTON BIOPHARMACEUTICALS CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, polyglyceryl stearate is a hydrophobic excipient, and it is likely to affect the dissolution of the main drug after being granulated with the main drug.
[0008] The purpose of the present invention is to provide a clopidogrel bisulfate tablet pharmaceutical composition and its preparation method, which can ensure that the clopidogrel bisulfate tablet remains stable during storage and does not convert into levoisomer or degrade into chlorine Pigrel acid; at the same time, it also solves the problem of sticking and punching during the preparation process and improves production efficiency

Method used

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  • Clopidogrel hydrogen sulfate tablet medicine composition and preparation method thereof
  • Clopidogrel hydrogen sulfate tablet medicine composition and preparation method thereof
  • Clopidogrel hydrogen sulfate tablet medicine composition and preparation method thereof

Examples

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Effect test

Embodiment 1

[0043] Embodiment 1: Prescription of clopidogrel bisulfate tablets (in 1000 tablets):

[0044] Element Dosage Clopidogrel bisulfate 32.625g Microcrystalline Cellulose Core 60g Povidone 1.6g lactose 100g Cross-linked polyvinylpyrrolidone 3.5g hydrogenated castor oil 1.0g

[0045] Preparation Process:

[0046] Add 1.6g of povidone into 300ml of ethanol, stir to dissolve the material completely, then slowly add 32.625g of clopidogrel hydrogen sulfate, continue stirring to dissolve, and obtain a clopidogrel hydrogen sulfate solution; take 60g of microcrystalline cellulose ball core Place it in the spray pot on the top of the fluidized bed, set the inlet air temperature to 60°C, and adjust the inlet air flow rate to 40-50m 3 / h to start preheating, when the temperature of the material reaches 48°C, start the liquid supply pump, spray the clopidogrel bisulfate solution into the fluidized bed for granulation, control the speed of the...

Embodiment 2

[0047] Embodiment 2: Prescription of clopidogrel bisulfate tablets (in 1000 tablets):

[0048] Element Dosage Clopidogrel bisulfate 32.625g Microcrystalline Cellulose Core 60g Povidone 1.6g Mannitol 100g Low-substituted hydroxypropyl cellulose 3.5g stearic acid 1.0g

[0049] Preparation Process:

[0050] Add 1.6g of povidone into 300ml of ethanol, stir to dissolve the material completely, then slowly add 32.625g of clopidogrel hydrogen sulfate, continue stirring to dissolve, and obtain a clopidogrel hydrogen sulfate solution; take 60g of microcrystalline cellulose ball core Put it in the spray pot on the top of the fluidized bed, set the inlet air temperature to 60°C, and adjust the inlet air flow rate to 20-30m 3 / h to start preheating, when the temperature of the material reaches 48°C, start the liquid supply pump, spray the clopidogrel bisulfate solution into the fluidized bed for granulation, control the speed of the liq...

Embodiment 3

[0051] Embodiment 3: Prescription of clopidogrel bisulfate tablets (in 1000 tablets):

[0052] Element Dosage Clopidogrel bisulfate 97.875g Microcrystalline Cellulose Core 180g Povidone 4.8g starch 200g Sodium carboxymethyl starch 7.0g polyethylene glycol 2.0g

[0053] Preparation Process:

[0054] Add 1.6g of povidone into 300ml of ethanol, stir to dissolve the material completely, then slowly add 97.875g of clopidogrel hydrogen sulfate, continue stirring to dissolve, and obtain a solution of clopidogrel hydrogen sulfate; take 180g of microcrystalline cellulose ball core Place it in the spray pot on the top of the fluidized bed, set the inlet air temperature to 60°C, and adjust the inlet air flow rate to 30-40m 3 / h to start preheating, when the temperature of the material reaches 48°C, start the liquid supply pump, spray the clopidogrel bisulfate solution into the fluidized bed for granulation, control the speed of the liq...

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Abstract

The invention provides a clopidogrel hydrogen sulfate tablet medicine composition and a preparation method thereof. Magnesium aluminum silicate is adopted in a prescription, so that the material flowability can be improved, deliquescence of medicines can also be effectively prevented, a risk that clopidogrel is degraded to form clopidogrel acid due to moisture absorption can be reduced, and more stable quality can be achieved. The preparation method comprises the following steps: firstly preparing pill cores, and then directly spraying a clopidogrel hydrogen sulfate solution on the pill cores by virtue of fluidized bed coating for performing granulation. By adopting the clopidogrel hydrogen sulfate tablet medicine composition provided by the invention, the mixing uniformity of the medicines can be significantly improved; and moreover, the sticking problem of clopidogrel can be effectively solved, the appearance characteristics of products can be improved, the product yield can be improved, and the requirements for industrial large-scale production can be better met.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a pharmaceutical composition of clopidogrel bisulfate tablets and a preparation method thereof. Background technique [0002] Clopidogrel hydrogen sulfate, the chemical name is 2-(2-chlorophenyl)-2-(6,7-dihydrothieno[3,2-c]pyridin-5-yl)acetate methyl ester hydrogensulfate, The chemical structural formula is: [0003] [0004] Clopidogrel is an inducible platelet aggregation inhibitor that acts by inhibiting the binding of adenosine monophosphate to its receptors. By inhibiting platelet aggregation, it reduces the chance of arterial blockage, achieves the effect of preventing stroke and heart attack, and can effectively treat and prevent atherosclerosis. [0005] It has been reported in the literature that clopidogrel bisulfate oral tablets are easily degraded to clopidogrel acid during storage, especially in wet conditions; and the interaction between clopidogrel a...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4365A61K47/02A61P9/10A61P7/02
Inventor 王颖
Owner CHENGDU EASTON BIOPHARMACEUTICALS CO LTD
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