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Solid preparation of clopidogrel and preparation method thereof

A technology of pidogrel solid and clopidogrel, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, which can solve problems such as stickiness and impact on product quality, and avoid Effect of sticking phenomenon, increasing fluidity of raw materials, and simple preparation process

Active Publication Date: 2011-06-29
QILU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, strictly controlling the content of the L-isomer of clopidogrel and the content of clopidogrel acid is an important index to control the quality of production, in order to improve the stability of the drug and the safety of clinical medication; in addition, large-scale production of clopidogrel tablets Due to the characteristics of the clopidogrel raw material itself, the tableting process is prone to sticking and punching, which affects the product quality, and the above-mentioned various methods cannot solve this problem well.

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

[0048] Name of raw material Amount / g

[0049] Clopidogrel Sulfate 75

[0050] Simethicone 5

[0051] Mannitol 115

[0052] Microcrystalline Cellulose 24

[0053] Hypromellose 14

[0054] Stearic acid 1.5

[0055] Glyceryl behenate 3

[0056] 1. Tablet or capsule after dry granulation:

[0057] A, the clopidogrel sulfate is pulverized through an 80 mesh sieve and mixed evenly with simethicone;

[0058] B. Add mannitol, microcrystalline cellulose and hydroxypropyl cellulose to the mixed powder obtained in step A, mix evenly, dry press into a tablet, grind the obtained tablet and granulate with a 20-mesh sieve;

[0059] C, add stearic acid, glyceryl behenate, mix well;

[0060] D. Tablet pressing, control hardness ≥ 5.0kg / mm 2 , tableting speed 8-10 tablets / hour;

[0061] E. Coat the plain tablet obtained in step D with Opadry 85G68918 coating powder, control the coating temperature at 40°C-50°C, and spray the coating solution according to the weight gain of 3%.

[006...

Embodiment 2

[0071] Name of raw material Amount / g

[0072] Clopidogrel Sulfate 75

[0073] Lactose 80

[0074] Microcrystalline Cellulose 64

[0075] Hypromellose 14

[0076] Stearic acid 1.5

[0077] Hydrogenated castor oil 3

[0078] 1. Tablet or capsule after dry granulation:

[0079] A. Mix clopidogrel sulfate, lactose, microcrystalline cellulose, and hydroxypropyl cellulose uniformly, dry press into tablets, and granulate with a 20-mesh sieve after the resulting tablets are pulverized;

[0080] B, add stearic acid, hydrogenated castor oil, mix well;

[0081] C. Tablet pressing, control hardness ≥ 5.0kg / mm 2 , the tableting speed is 80,000-100,000 tablets / hour;

[0082] D. Coat the plain tablet obtained in step C with Opadry 85G68918 coating powder, control the coating temperature at 40°C-50°C, and spray the coating solution according to the weight gain of 3%.

[0083] If preparing capsules, the granules obtained in step B can be directly poured into capsules.

[0084] 2. Aft...

Embodiment 3

[0091] Name of raw material Amount / g

[0092] Clopidogrel Sulfate 75

[0093] Simethicone 4

[0094] Lactose 70

[0095] Pregelatinized starch 26

[0096] Microcrystalline Cellulose 38

[0097] Crospovidone 20

[0098] Stearic acid 1.5

[0099] Hydrogenated castor oil 3

[0100] 1. Tablet or capsule after dry granulation:

[0101] A. After crushing clopidogrel sulfate through an 80-mesh sieve and mixing it evenly with simethicone, first mix it with 50% pregelatinized starch;

[0102] B. Add lactose, the remaining 50% pregelatinized starch, microcrystalline cellulose and crospovidone to the mixed powder obtained in step A, mix evenly, dry press into tablets, grind the obtained tablets and granulate with a 20-mesh sieve;

[0103] C, add stearic acid, hydrogenated castor oil, mix well;

[0104] D. Tablet pressing, control hardness ≥ 5.0kg / mm 2 , the tableting speed is 80,000-100,000 tablets / hour;

[0105] E. Coat the plain tablet obtained in step D with Opadry 85G68918...

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Abstract

The invention belongs to the field of medicinal preparations, and relates to a solid preparation and a preparation method thereof, in particular to a solid preparation of clopidogrel or pharmaceutically acceptable salt of the clopidogrel as well as a preparation method thereof. The solid preparation is mainly prepared by mixing the clopidogrel or the pharmaceutically acceptable salt thereof with dimeticone and then processing the obtained mixture according to a conventional solid preparation processing method. By adopting the dimeticone, the invention has the advantages of preventing a dextroisomer of the clopidogrel from converting into a levoisomer, preventing the clopidogrel from being degraded into clopidogrel acid, being applicable to the formula and process for large-scale production of the preparation, solving the problem of drug degradation, improving drug stability, solving sticking and picking phenomena during the tabletting process, and improving product quality.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a solid preparation of clopidogrel or a pharmaceutically acceptable salt thereof and a preparation method thereof, mainly comprising tablets and capsules. Background technique [0002] The chemical name of Clopidogrel is (+)-(S)-α-(0-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] [0005] [0006] Clopidogrel is a platelet aggregation inhibitor that selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet receptor and the subsequent ADP-mediated activation of the glycoprotein GP11b / 111a complex, so it can Inhibits...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/4365A61K47/34A61P7/02A61P9/06A61P9/10A61K47/38
Inventor 王晶翼于艳玲杨清敏徐文亮张明会王鹏
Owner QILU PHARMA
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