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Clopidogrel hydrogen sulfate tablets and preparation method thereof

A technology of clopidogrel bisulfate and tablets, which is applied in the fields of pharmaceutical formulations, blood diseases, extracellular fluid diseases, etc., and can solve the problems of restricting the large-scale production of clopidogrel bisulfate medicine, instability of humidity and heat, easy hydrolysis and degreasing, etc. , to achieve the effect of ensuring effectiveness and safety, smooth surface and strong stability

Inactive Publication Date: 2019-05-21
HENAN TIANSHENG TAIFENG PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the main problems in the production process of clopidogrel bisulfate tablets: (1) poor stability: clopidogrel bisulfate has a carboxylate structure, which is unstable to humidity and heat, and is easy to hydrolyze and degrease to form clopidogrel acid; (2) easy sticking: clopidogrel bisulfate raw material is hygroscopic and is easily adsorbed on the metal surface. When it is rubbed and backlogged, it will quickly bond, causing sticking and resulting in poor product quality
These severely limit the large-scale production of clopidogrel bisulfate

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Prescription (preparation of 1000 tablets)

[0021] 1. Project

2. Parts by mass

3. Clopidogrel bisulfate II crystal form (calculated as C16H16ClNO2S)

4.98

5. Pregelatinized starch

6.30

7. Mannitol

8.50

9. Microcrystalline Cellulose

10.25

11. Low-substituted hydroxypropyl cellulose

12.30

13. PEG6000

14. 5

15. Hydrogenated castor oil

16. 5

17. Coating material

18. 1000

[0022] Concrete steps during preparation are as follows:

[0023] 1) Dry microcrystalline cellulose, pregelatinized starch, and mannitol at 80°C until the moisture content is <10% respectively; pass polyethylene glycol 6000 through a 100-mesh sieve with a vibrating sieve, and set aside;

[0024] 2) Preparation of coating solution Add appropriate amount of coating material to 80% ethanol solution 1.2 times its weight, stir well to dissolve it, and set aside;

[0025] 3) For granule production, adjust the fan ...

Embodiment 2

[0030] Prescription (preparation of 1000 tablets)

[0031] 19. Items

20. Parts by mass

21. Clopidogrel bisulfate II crystal form (calculated as C16H16ClNO2S)

22. 98

23. Pregelatinized starch

24. 25

25. Mannitol

26. 55

27. Microcrystalline cellulose

28. 30

29. Low-substituted hydroxypropyl cellulose

30. 20

31. PEG6000

32. 10

33. Hydrogenated castor oil

34. 5

35. Coating material

36. 1000

[0032] Concrete steps during preparation are as follows:

[0033] 1) Dry microcrystalline cellulose, pregelatinized starch, and mannitol at 80°C until the moisture content is <10% respectively; pass polyethylene glycol 6000 through a 100-mesh sieve with a vibrating sieve, and set aside;

[0034] 2) Preparation of coating solution Add appropriate amount of coating material to 80% ethanol solution 1.2 times its weight, stir well to dissolve it, and set aside;

[0035] 3) For granule production, ad...

Embodiment 3

[0040] Prescription (preparation of 1000 tablets)

[0041] 37. Items

38. Parts by mass

39. Clopidogrel bisulfate II crystal form (calculated as C16H16ClNO2S)

40. 98

41. Pregelatinized starch

42. 30

43. Mannitol

44. 45

45. Microcrystalline cellulose

46. 30

47. Low-substituted hydroxypropyl cellulose

48. 25

49. PEG6000

50. 10

51. Hydrogenated castor oil

52. 5

53. Coating material

54. 1000

[0042] Concrete steps during preparation are as follows:

[0043] 1) Dry microcrystalline cellulose, pregelatinized starch, and mannitol at 80°C until the moisture content is <10% respectively; pass polyethylene glycol 6000 through a 100-mesh sieve with a vibrating sieve, and set aside;

[0044] 2) Preparation of coating solution Add appropriate amount of coating material to 80% ethanol solution 1.2 times its weight, stir well to dissolve it, and set aside;

[0045] 3) For granule production, adju...

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PUM

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Abstract

The invention relates to clopidogrel hydrogen sulfate tablets and a preparation method thereof. The tablets comprise the following components by weight percentage: clopidogrel hydrogen sulfate form II, a filler, a disintegrant, an antioxidant, a proper amount of a binder, and a proper amount of a lubricant. The tablets improve the stability of the obtained preparation, and the obtained preparationhas the characteristics of good uniformity, smooth surface of the tablets, small difference in tablet weight, and the like. The dissolution performance is in line with the clinical drug requirements,so that the effectiveness and safety of clinical drugs can be ensured. The preparation process also ensures that no sticking problem is generated during a tableting process.

Description

technical field [0001] The invention belongs to the field of clopidogrel bisulfate preparations, and in particular relates to a clopidogrel bisulfate II crystal form tablet and a preparation method thereof. Background technique [0002] Cardiovascular thrombosis is a disease that seriously threatens human health. Platelet aggregation is an important link in the normal coagulation mechanism, and the adhesion, aggregation, and release reactions of platelets often easily lead to thrombus formation. Therefore, drugs that inhibit platelet aggregation play an important role in the treatment of thrombosis. Clopidogrel is a platelet aggregation inhibitor and active ingredient of antithrombotic drugs in the blood. It selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet receptor and the subsequent ADP-mediated GPⅡb / Ⅲa complex. Activates, inhibits platelet aggregation. In addition, it inhibits platelet aggregation induced by other kinetic agents by blockin...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K31/4365A61K47/38A61K47/36A61K47/26A61K47/10A61P7/02A61P9/10
Inventor 沙薇杨静吕艳歌
Owner HENAN TIANSHENG TAIFENG PHARM TECH CO LTD
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