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Clopidogrel hydrogen sulfate solid preparation and preparation method thereof

A technology of clopidogrel bisulfate solid and clopidogrel bisulfate, which is applied in the fields of pill delivery, pharmaceutical formula, medical preparations of non-active ingredients, etc., and can solve problems such as too much, difficult to prepare granules, and affecting the dissolution of preparations

Inactive Publication Date: 2016-06-01
SHENZHEN SALUBRIS PHARMA +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The literature then stated the influence of the amount of molten binder on the granulation effect, and believed that the amount of binder used was too small to prepare granules, while the use of too much binder would easily cause the granules to be hard and easy to form agglomerates. Affect the dissolution of the preparation
However, the batch material used in the melt granulation process is still too much, and the process still has room for improvement

Method used

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  • Clopidogrel hydrogen sulfate solid preparation and preparation method thereof
  • Clopidogrel hydrogen sulfate solid preparation and preparation method thereof
  • Clopidogrel hydrogen sulfate solid preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] prescription:

[0068]

[0069]

[0070] Preparation steps:

[0071] 1) Mix the prescribed amount of clopidogrel bisulfate (D90=67 μm) with the internally added excipients for 20-30 minutes to obtain the internally mixed powder;

[0072] 2) Add the internal mixed powder obtained in step 1) into a fluidized bed granulator, and granulate at 50-60°C for 10-30 minutes to obtain internal phase granules (angle of repose 37°). The obtained granules are uniform and almost free of fine powder;

[0073] 3) Mix the introverted granules obtained in step 2) with the prescribed amount of external excipients for 10 to 20 minutes to obtain the total mixed granules;

[0074] 4) Compressing the blended granules obtained in step 3) into tablets to prepare a solid preparation of clopidogrel hydrogen sulfate (75 mg specification).

[0075] No sticking phenomenon occurred in the tableting process, and the obtained clopidogrel bisulfate solid preparation had a smooth surface.

Embodiment 2

[0077] prescription:

[0078]

[0079] Preparation steps:

[0080] 1) Mix the prescribed amount of clopidogrel bisulfate (D90=60 μm) with the internally added excipients for 20-30 minutes to obtain the internally mixed powder;

[0081] 2) Add the internal mixed powder obtained in step 1) into a fluidized bed granulator, and granulate at 50-60°C for 10-30 minutes to obtain internal phase granules (angle of repose 38°). The obtained granules are uniform and almost free of fine powder;

[0082] 3) Mix the introverted granules obtained in step 2) with the prescribed amount of external excipients for 10 to 20 minutes to obtain the total mixed granules;

[0083] 4) Compressing the blended granules obtained in step 3) into tablets to prepare a solid preparation of clopidogrel hydrogen sulfate (75 mg specification).

[0084] No sticking phenomenon occurred in the tableting process, and the obtained clopidogrel bisulfate solid preparation had a smooth surface.

Embodiment 3

[0086] prescription:

[0087]

[0088] Preparation steps:

[0089] 1) Mix the prescribed amount of clopidogrel hydrogen sulfate (D90=73 μm) with the internally added excipients for 20-30 minutes to obtain the internally mixed powder;

[0090] 2) Add the internal mixed powder obtained in step 1) into a fluidized bed granulator, and granulate at 50-60°C for 10-30 minutes to obtain internal phase granules (angle of repose 38°). The obtained granules are uniform and almost free of fine powder;

[0091] 3) Mix the introverted granules obtained in step 2) with the prescribed amount of external excipients for 10 to 20 minutes to obtain the total mixed granules;

[0092] 4) Compressing the blended granules obtained in step 3) into tablets to prepare a solid preparation of clopidogrel hydrogen sulfate (75 mg specification).

[0093] No sticking phenomenon occurred in the tableting process, and the obtained clopidogrel bisulfate solid preparation had a smooth surface.

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Abstract

The invention provides a clopidogrel hydrogen sulfate solid preparation which is prepared by adopting a melt granulation technology, wherein the bulk drug content in obtained particles is high, the obtained preparation has the characteristics of good uniformity, smooth tablet surface and small tablet weight difference, the digestion performance meets the clinical medication requirement, and the effect is better when special crystal forms are used.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular, the invention relates to a solid preparation of clopidogrel bisulfate and a preparation method thereof. Background technique [0002] Clopidogrel hydrogen sulfate (CAS: 135046-48-9), is the sulfate salt of clopidogrel, English name ClopidogrelHydrogenSulfate, chemical name: (s)-α-(2-chlorophenyl)-6,7-di Methyl hydrothieno[3,2-c]pyridine-5(4H)acetate hydrogensulfate. Clopidogrel bisulfate is an antiplatelet agent. The product was developed by the French pharmaceutical company Sanofi-Aventis and was first launched in the UK and the US in 1998. Clopidogrel bisulfate entered China in 2001 and is clinically used to prevent atherosclerotic thrombosis events . At present, domestic clopidogrel bisulfate preparation products mainly include Plavix of Sanofi-Aventis and Taijia of Shenzhen Xinlitai Pharmaceutical Co., Ltd. [0003] [0004] Clopidogrel bisulfate [0005] Clop...

Claims

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Application Information

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IPC IPC(8): A61K31/4365A61K9/20A61K9/28A61K47/34A61K47/38A61K47/26A61P7/02
CPCA61K9/2018A61K9/2031A61K9/2054A61K9/28A61K31/4365A61K9/2077A61P7/02A61K9/2027A61K9/2095
Inventor 蔡燕霞谭岳尧叶冠豪
Owner SHENZHEN SALUBRIS PHARMA
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