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Clopidogrel bisulfate composition tablet and preparation method thereof

A clopidogrel bisulfate and a composition technology are applied in the field of clopidogrel bisulfate composition tablet and preparation thereof, and can solve the problems of affecting drug stability, lack of medical approval, high viscosity and the like, and achieve reduction or prevention. Digestive system diseases, good quality, and the effect of improving hardness

Active Publication Date: 2014-08-20
SHANDONG LUOXIN PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are two main problems in the production of clopidogrel bisulfate tablets: (1) clopidogrel bisulfate has a carboxylate structure, which is unstable to damp heat and is easy to hydrolyze and degrease to form clopidogrel acid. Appropriate active ingredients to maintain its stability
The Chinese patent application number 201110226019.4 discloses a tablet of clopidogrel hydrogen sulfate and a preparation method thereof, and its 3 examples all disclose the tablet of clopidogrel hydrogen sulfate using magnesium stearate as a component. Undoubtedly affect the stability of the drug
Although some foreign patents try to replace magnesium stearate with other substances, either the effect is not good or the substituted substance has no medical approval in China, so it cannot be produced, and it cannot solve the problems in the domestic production of clopidogrel bisulfate tablets.
(2) Due to the high viscosity of the raw material of clopidogrel bisulfate, serious sticking problems are prone to occur in the production process of its tablets, resulting in poor quality of finished products, which also requires appropriate active ingredients to avoid sticking phenomenon
The above reasons restrict the product quality of the existing clopidogrel bisulfate tablets, and cannot guarantee the safe use and long-term storage of clopidogrel bisulfate tablets in clinical practice.

Method used

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  • Clopidogrel bisulfate composition tablet and preparation method thereof
  • Clopidogrel bisulfate composition tablet and preparation method thereof
  • Clopidogrel bisulfate composition tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: Preparation of the clopidogrel hydrogen sulfate composition tablet of the present invention

[0030]

[0031] Pass each active ingredient through a 100-mesh sieve separately; weigh out clopidogrel bisulfate, microcrystalline cellulose, lactose, sodium alginate and carboxymethyl starch and mix thoroughly, and use ethyl alcohol to make soft materials, wet with 18-mesh sieve Granulation method. The granules are dried at about 50℃ by blowing air, and the dried granules are made into 18 meshes. Add crospovidone, magnesium trisilicate and polyethylene glycol 6000 to determine the content of clopidogrel hydrogen sulfate. The content determines the tablet weight. Then Φ10mm shallow concave punching die to press tablets, finally take the gastric-soluble film coating premix, add 85% ethanol to make a coating liquid, and use air stream to spray continuously until the film weight is 2%-4% of the plain tablet, and then dry, Packing, full inspection, and storage.

Embodiment 2

[0032] Example 2: Preparation of the clopidogrel hydrogen sulfate composition tablet of the present invention

[0033]

[0034] Pass each active ingredient through a 100-mesh sieve separately; weigh out clopidogrel bisulfate, microcrystalline cellulose, lactose, sodium alginate and carboxymethyl starch and mix thoroughly, and use ethyl alcohol to make soft materials, wet with 18-mesh sieve Granulation method. The granules are dried at about 50℃ by blowing air, and the dried granules are made into 18 meshes. Add crospovidone, magnesium trisilicate and polyethylene glycol 6000 to determine the content of clopidogrel hydrogen sulfate. The content determines the tablet weight. Then Φ10mm shallow concave punching die to press tablets, finally take the gastric-soluble film coating premix, add 85% ethanol to make a coating liquid, and use air stream to spray continuously until the film weight is 2%-4% of the plain tablet, and then dry, Packing, full inspection, and storage.

Embodiment 3

[0035] Example 3: Preparation of the clopidogrel hydrogen sulfate composition tablet of the present invention

[0036]

[0037]

[0038] Pass each active ingredient through a 100-mesh sieve separately; weigh out clopidogrel bisulfate, microcrystalline cellulose, lactose, sodium alginate and carboxymethyl starch and mix thoroughly, use propylene glycol to make soft materials, and 18-mesh sieve for wet granulation , The granules are air-dried at about 50℃, the dried granules are 18 meshes, and the total mixture of crospovidone, magnesium trisilicate and polyethylene glycol 6000 is added to determine the content of clopidogrel hydrogen sulfate. Film weight. Then Φ10mm shallow concave punching die to press tablets, finally take the gastric-soluble film coating premix, add 85% ethanol to make a coating liquid, and use air stream to spray continuously until the film weight is 2%-4% of the plain tablet, and then dry, Packing, full inspection, and storage.

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PUM

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Abstract

The invention relates to the field of pharmaceutical preparations and in particular relates to a clopidogrel bisulfate composition tablet and a preparation method thereof. The active pharmaceutical ingredients of the clopidogrel bisulfate composition tablet include clopidogrel bisulfate, microcrystalline cellulose, lactose, sodium alginate, carboxymethyl starch, one of alcohol ethyl ester and propylene glycol, cross-linked povidone, polyethylene glycol 6000, magnesium trisilicate, a gastric-solubility film coated premixing agent and 85% alcohol. Preferably, the clopidogrel bisulfate, the microcrystalline cellulose, the lactose, the sodium alginate, the carboxymethyl starch, one of the alcohol ethyl ester and the propylene glycol, the cross-linked povidone, the polyethylene glycol 6000, the magnesium trisilicate, the gastric-solubility film coated premixing agent and the 85% alcohol are uses as the active pharmaceutical ingredients of the clopidogrel bisulfate composition tablet; and the active pharmaceutical ingredients are acted with each other in a cooperative manner, so that the stable performance of the clopidogrel bisulfate is improved and the sticking degree of the clopidogrel bisulfate is lowered, and therefore, the clopidogrel bisulfate composition tablet is beneficial to the quality, the safe use and the long-term storage of the clinical medicaments.

Description

Technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a clopidogrel hydrogen sulfate composition tablet and a preparation method thereof. Background technique [0002] Clopidogrel hydrogen sulfate, its chemical name is methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno(3,2-carbon)pyrimidine-5(4H) )-Bisulfate of acetate. , The structural formula is as follows: [0003] [0004] Clopidogrel bisulfate is a platelet aggregation inhibitor that selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet receptors and the subsequent activation of ADP-mediated glycoprotein GPIIb / IIIa complex. Therefore, platelet aggregation can be inhibited. Clopidogrel bisulfate must undergo biotransformation to inhibit platelet aggregation. In addition to ADP, clopidogrel bisulfate can also block the enhancement of platelet activity caused by the release of ADP by other agonists, thereby inhibiting platelet aggregation caused by...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/28A61K31/4365A61K47/38A61P7/02
Inventor 刘延珍陈磊牛洪芬韩云龙
Owner SHANDONG LUOXIN PHARMA GRP CO LTD