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Solid preparation of clopidogrel and preparation method thereof

A clopidogrel, solid preparation technology, applied in the field of medicine, can solve the problem of no anti-platelet aggregation and the like

Active Publication Date: 2009-03-25
CHONGQING LUMMY PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] In fact, none of the aforementioned patents can completely solve the problem of clopidogrel degradation. The active D-isomer in clopidogrel sulfate tablets will be converted into the L-isomer of clopidogrel and clopidogrel acid. None of them have the effect of anti-platelet aggregation, and the results of animal experiments show that the toxicity is significantly higher than that of clopidogrel dextro-isomer

Method used

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  • Solid preparation of clopidogrel and preparation method thereof
  • Solid preparation of clopidogrel and preparation method thereof
  • Solid preparation of clopidogrel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] The preparation method of embodiment 1:

[0040] 1) Crush clopidogrel sulfate and β-cyclodextrin and sieve through a 120-mesh sieve, then mix it with pregelatinized starch, micropowder silica gel and anhydrous lactose, and press it into tablets. After crushing the obtained tablet, pass through a 30-mesh sieve to granulate;

[0041] 2) Mix the granules obtained in operation 1) with polyvinylpyrrolidone copolymer VA64, cross-linked polyvinylpyrrolidone and leucine evenly, and then directly compress to obtain tablets or fill capsule shells or directly seal them into aluminum-plastic composite film bags;

[0042] 3) The obtained plain tablet is coated with a film coating with Opadry II coating powder, the coating temperature is 50° C., and the weight gain after coating is 2.3%.

Embodiment 2

[0043] The preparation method of embodiment 2:

[0044] 1) Mix clopidogrel sulfate and β-cyclodextrin through a 100-mesh sieve, polyvinylpyrrolidone copolymer VA64, micropowder silica gel, cross-linked polyvinylpyrrolidone, sodium chloride and leucine, and then press directly Get tablets or fill capsule shells or directly seal them in aluminum-plastic composite film bags;

[0045] 2) The obtained plain tablet is coated with a film coating with Opadry II coating powder, and the weight gain is controlled to 2.5% after coating.

Embodiment 3

[0046] The preparation method of embodiment 3:

[0047] 1) After crushing clopidogrel sulfate and β-cyclodextrin through a 100-mesh sieve, mix it evenly with polyvinylpyrrolidone copolymer VA64, micropowder silica gel, cross-linked polyvinylpyrrolidone, and sodium chloride, and then directly compress to obtain tablets or Filling capsule shells or directly sealing them into aluminum-plastic composite film bags;

[0048] 2) The obtained plain tablet is coated with a film coating with Opadry II coating powder, and the weight gain is controlled to 2.5% after coating.

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Abstract

The invention relates to the clopidogrel solid preparation and the preparation method thereof, which belong to the medicine field. The invention solves the technical problem of preventing the dextro isomer of clopidogrel from transforming into laevo isomer, and preventing clopidogrel from degrading into clopidogrel acid. Concretely, clopidogrel or derivatives thereof and Beta-cyclodextrin are mixed and sieved, so as to prepare the clopidogrel solid preparation through the conventional solid preparation method. Beta-cyclodextrin used as principle medicine wrapping agent can effectively prevent the degrading problem of clopidogrel sulphate, and improve the stability of dextro isomer of clopidogrel sulphate. The result of stability experiment indicates that the clopidogrel laevo isomer and clopidogrel acid are not obviously increased when the clopidogrel solid preparation is stored for long time or used in an accelerated test process so that the clopidogrel solid preparation has good stability and safe clinical application.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a solid preparation of clopidogrel and a preparation method thereof. Background technique [0002] The chemical name of Clopidogrel is (+)—(S)—α—(o—chlorophenyl)—6,7—dihydrothieno[3,2—c]pyridine—5(4H)-acetic acid Methyl ester (Formula I), the ester group of which is readily hydrolyzed to yield a biologically inactive acid (Formula II). Furthermore, the dextro isomer can be transformed into the almost inactive levoisomer (Chemical Formula III) under moist heat conditions. Its structure is as follows: [0003] [0004] Clopidogrel selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet receptor and the subsequent ADP-mediated activation of the glycoprotein GPIIb / IIIa complex, thereby inhibiting platelet aggregation. Clopidogrel itself It is an inactive prodrug, which is metabolized by hepatic cytochrome P450 in vivo into active metabolites to exert ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4365A61K47/40A61P7/02A61P9/10
Inventor 胡显刚安林方霜江坤许辉川
Owner CHONGQING LUMMY PHARMA
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