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I type clopidogrel hydrogen sulfate particles and preparation method thereof as well as I type clopidogrel hydrogen sulfate solid preparation and preparation method thereof

A technology of clopidogrel hydrogen sulfate and granules, applied in the directions of pill delivery, pharmaceutical formulations, medical preparations of inactive ingredients, etc., can solve problems such as instability of type I clopidogrel hydrogen sulfate

Active Publication Date: 2015-04-08
BEIJING COLLAB PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compared with type II clopidogrel bisulfate, type I clopidogrel bisulfate has higher dissolution rate and bioavailability, but type I clopidogrel bisulfate is unstable and is easily converted into type II clopidogrel bisulfate

Method used

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  • I type clopidogrel hydrogen sulfate particles and preparation method thereof as well as I type clopidogrel hydrogen sulfate solid preparation and preparation method thereof
  • I type clopidogrel hydrogen sulfate particles and preparation method thereof as well as I type clopidogrel hydrogen sulfate solid preparation and preparation method thereof
  • I type clopidogrel hydrogen sulfate particles and preparation method thereof as well as I type clopidogrel hydrogen sulfate solid preparation and preparation method thereof

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preparation example Construction

[0038] The invention provides a preparation method of type I clopidogrel bisulfate granules, comprising the following steps:

[0039] a), the crystal form stabilizer is mixed with a solvent to obtain a crystal form stabilizer solution; type I clopidogrel hydrogen sulfate is mixed with auxiliary materials to obtain a mixture;

[0040] The crystal form stabilizer is one or more of polyvinylpyrrolidone, copovidone and polyethylene glycol; the auxiliary material is a filler and / or a disintegrant;

[0041] b), the crystal form stabilizer solution and the mixture are sequentially mixed, granulated and dried to obtain type I clopidogrel hydrogen sulfate granules.

[0042] In the preparation method of type I clopidogrel bisulfate granules provided by the present invention, firstly, the crystal form stabilizer is mixed with a solvent to obtain a crystal form stabilizer solution. Wherein, the crystal form stabilizer is one or more of polyvinylpyrrolidone, copovidone and polyethylene gl...

Embodiment 1

[0090] Prescription: Clopidogrel 75 mg / tablet

[0091]

[0092] Preparation Process:

[0093] 1) Mix 97.875g of clopidogrel hydrogen sulfate type I, 100g of mannitol, 70g of microcrystalline cellulose, and 17g of low-substituted hydroxypropyl cellulose to obtain a mixed material.

[0094] 2) Dissolving 9 g of polyvinylpyrrolidone (k30) in a small amount of ethanol to obtain a polyvinylpyrrolidone solution.

[0095] 3) Add polyvinylpyrrolidone solution to the mixed material to prepare soft material, which is granulated through a 24-mesh sieve in a swing granulator.

[0096] 4) The prepared granules were dried at 60° C. for 2 hours, then passed through a 18-mesh sieve for granulation, and 8 g of hydrogenated castor oil was added to the granulated granules, mixed evenly, and tableted to obtain a clopidogrel content of 75 mg / Tablets of 1000 tablets.

Embodiment 2

[0098] Prescription: Clopidogrel 75 mg / tablet

[0099]

[0100] Preparation Process:

[0101] 1) Mix 97.875g of clopidogrel hydrogen sulfate type I, 60g of mannitol, 120g of microcrystalline cellulose, and 12g of low-substituted hydroxypropyl cellulose to obtain a mixed material.

[0102] 2) Dissolving 6 g of polyvinylpyrrolidone (k90) in a small amount of ethanol to obtain a polyvinylpyrrolidone solution.

[0103] 3) Add polyvinylpyrrolidone solution to the mixed material to prepare soft material, which is granulated through a 24-mesh sieve in a swing granulator.

[0104] 4) The prepared granules were dried at 60° C. for 2 hours, then passed through a 18-mesh sieve for granulation, and 6 g of hydrogenated castor oil was added to the granulated granules, mixed evenly, and pressed into tablets to obtain a clopidogrel content of 75 mg / Tablets of 1000 tablets.

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Abstract

The invention belongs to the field of medicaments and in particular relates to I type clopidogrel hydrogen sulfate particles and a preparation method thereof as well as an I type clopidogrel hydrogen sulfate solid preparation and a preparation method thereof. The preparation method of the I type clopidogrel hydrogen sulfate particles comprises the following steps: a) mixing a crystal form stabilizer and a solvent to obtain a crystal form stabilizer solution; and mixing I type clopidogrel hydrogen sulfate and adjuncts to obtain a mixture; and b) sequentially carrying out mixing, granulation and drying on the crystal form stabilizer solution and the mixture to obtain the I type clopidogrel hydrogen sulfate particles. The I type clopidogrel hydrogen sulfate particles prepared by the preparation method are prepared into the solid preparation; the stability of the solid preparation is tested, and results show that in long-term stability experiments and accelerated stability experiments, the I type clopidogrel hydrogen sulfate in the solid preparation can not be converted to II type clopidogrel hydrogen sulfate.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to a type I clopidogrel hydrogen sulfate granule and a preparation method thereof and a preparation method of a type I clopidogrel hydrogen sulfate solid preparation. Background technique [0002] Cardiovascular and cerebrovascular disease is a common disease that seriously threatens the health of human beings, especially middle-aged and elderly people over 50 years old. The number of people who die from cardiovascular and cerebrovascular diseases in the world is as high as 15 million every year, ranking first among various causes of death. Cardiovascular and cerebrovascular diseases have become the number one killer with the highest cause of death for human beings, and they are also the "silent evil spirits" of human health. [0003] Clopidogrel is a thienopyridine drug that can significantly reduce the incidence of cardiovascular and cerebrovascular disease deaths. Clopidogre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4365A61K47/32A61K47/34A61P9/00A61P7/02
CPCA61K9/1635A61K9/1641A61K9/2027A61K9/2031A61K9/4866A61K31/4365
Inventor 邱敦有邹德超王珂赵大龙
Owner BEIJING COLLAB PHARMA
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