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Solid medicinal composition of clopidogrel hydrogen sulfate

A kind of technology of clopidogrel hydrogen sulfate and composition, applied in the stable oral pharmaceutical composition field containing I crystal form clopidogrel hydrogen sulfate, achieves the effects of good reproducibility, stable quality, and overcoming instability

Active Publication Date: 2010-06-09
NANJING CHIA TAI TIANQING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This suggests that mannitol may interact with I crystalline form clopidogrel bisulfate to promote the conversion of I crystalline form clopidogrel bisulfate, so the FDA prescription is not suitable for I crystalline form clopidogrel bisulfate. The safety and effectiveness of use, the inventor needs to develop suitable formula

Method used

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  • Solid medicinal composition of clopidogrel hydrogen sulfate
  • Solid medicinal composition of clopidogrel hydrogen sulfate
  • Solid medicinal composition of clopidogrel hydrogen sulfate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Raw material name 1000 tablets dosage (g)

[0041] Form I Clopidogrel Bisulfate 97.9 (equivalent to Clopidogrel 75g)

[0042] PEG6000 3

[0043] Micronized silica gel 10

[0044] Microcrystalline Cellulose 135

[0045] Low-substituted hydroxypropyl cellulose 12.5

[0046] Gastric-soluble film coating premix appropriate amount

[0047] 1) Pass I crystalline form clopidogrel bisulfate through a 40-mesh sieve for later use.

[0048] 2) Pass the microcrystalline cellulose, low-substituted hydroxypropyl cellulose and micropowder silica gel through a 60-mesh sieve respectively, and dry at 105°C for 2 hours for later use.

[0049] 3) The polyethylene glycol 6000 is jet-pulverized into fine powder for later use.

[0050] 4) After mixing the prescription amount of crystalline form clopidogrel hydrogen sulfate, microcrystalline cellulose and low-substituted hydroxypropyl cellulose evenly, pass through a dry granulator, and granulate with a 20-mesh sieve.

[0051] 5) Pass t...

Embodiment 2

[0056] Raw material name 1000 tablets dosage (g)

[0057] Form I Clopidogrel Bisulfate 32.6 (equivalent to Clopidogrel 25g)

[0058] Polyethylene glycol 6000 150

[0059] Micronized silica gel 30

[0060] Pregelatinized starch 85

[0061] Low-substituted hydroxypropyl cellulose 22

[0062] Gastric-soluble film coating premix appropriate amount

[0063] 1) Pass I crystalline form clopidogrel bisulfate through an 80-mesh sieve for later use.

[0064] 2) Pass pregelatinized starch, low-substituted hydroxypropyl cellulose and micropowder silica gel through 80-mesh sieve respectively, and dry at 105°C for 2 hours for later use.

[0065] 3) Pass polyethylene glycol 6000 through a 60-mesh sieve for later use.

[0066] 4) Mix the prescription quantity I crystal form clopidogrel hydrogen sulfate, polyethylene glycol 6000, pregelatinized starch, low-substituted hydroxypropyl cellulose and 80% prescription quantity of micropowder silica gel evenly, pass through a dry granulator, an...

Embodiment 3

[0072] Raw material name 1000 tablets dosage (g)

[0073] Form I Clopidogrel Bisulfate 97.9 (equivalent to Clopidogrel 75g)

[0074] Polyethylene glycol 6000 2

[0075] Micronized silica gel 10

[0076] Microcrystalline Cellulose 150

[0077] Low-substituted hydroxypropyl cellulose 4

[0078]Gastric-soluble film coating premix appropriate amount

[0079] 1) Pass clopidogrel bisulfate through a 40-mesh sieve for later use.

[0080] 2) Pass the microcrystalline cellulose, low-substituted hydroxypropyl cellulose and micropowder silica gel through a 60-mesh sieve respectively, and dry at 105°C for 2 hours for later use.

[0081] 3) The polyethylene glycol 6000 is jet-pulverized for later use.

[0082] 4) Mix the prescription amount of clopidogrel hydrogen sulfate, microcrystalline cellulose, and low-substituted hydroxypropyl cellulose evenly, pass through a dry granulator, and granulate with a 20-mesh sieve.

[0083] 5) Pass the dry granules through a 18-mesh sieve for gran...

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Abstract

The invention relates to an oral medicinal composition containing I crystal-form clopidogrel hydrogen sulfate, polyethylene glycol and micro-powder silica gel, proper disintegrating agent and filling agent. The auxiliary materials of the composition are low in price and can be obtained easily; the preparation process is simple; the requirement for equipment and environment is not high; and the prepared tablet is stable in quality and good in reproducibility, and is applied to industrialized production. The prepared tablet has good stability in long-term storage and can be maintained stable after being placed for 6 months at the temperature of 40 DEG C, without appearance change and obvious degradation or crystal-form inversion phenomenon; the dissolution rate of the tablet is not reduced after the tablet is placed for a long time; and the dissolution rate of the tablet in 10 minutes can still reach more than 95 percent after the tablet is placed for 6 months at the temperature of 40 DEG C.

Description

technical field [0001] The invention relates to a stable oral pharmaceutical composition, in particular to a stable oral pharmaceutical composition containing I crystal form clopidogrel bisulfate. Background technique [0002] The chemical name of clopidogrel hydrogen sulfate is: S(+)-2-(2-chlorophenyl)-2-(4,5,6,7-tetrahydrothiophene[3,2-c]pyridine-5 ) methyl acetate bisulfate, the structure is as follows formula I. [0003] Formula I [0004] Clopidogrel bisulfate is clinically used as an antithrombotic drug by selectively inhibiting the binding of adenosine diphosphate (ADP) to platelet receptors and the subsequent ADP-mediated glycoprotein GPIIIb / IIIa complex Activated to inhibit platelet aggregation. In addition, clopidogrel bisulfate inhibits platelet aggregation induced by other agonists by blocking platelet activation caused by released ADP. Clopidogrel bisulfate is indicated for patients with recent stroke, myocardial infarction, and established peripheral arte...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4365A61K47/34A61P7/02A61K47/10
Inventor 董平谢华周浩张喜全
Owner NANJING CHIA TAI TIANQING PHARMA
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