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Sofosbuvir tablet and preparation method thereof

A buvir tablet and preparation technology, applied in the field of sofosbuvir tablet and its preparation, can solve the problems of high requirement of dry granulation equipment, low labor efficiency, slow dissolution and the like, and improve drug stability and production efficiency High, dissolution-enhancing effect

Active Publication Date: 2016-02-03
SHIJIAZHUANG NO 4 PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] The purpose of the present invention is to solve the problems that the sofosbuvir crystal form 1 raw material in the existing sofosbuvir tablet technology meets water into a hard colloid and dissolves slowly; dry granulation has high requirements for equipment, complicated process and low labor efficiency

Method used

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  • Sofosbuvir tablet and preparation method thereof
  • Sofosbuvir tablet and preparation method thereof
  • Sofosbuvir tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Product prescription (1000 tablets):

[0035]

[0036] Preparation Process:

[0037] (1) Mix the prescription amount of Sofosbuvir and colloidal silica evenly to obtain mixture one;

[0038] (2) Add direct pressure mannitol, optimized microcrystalline cellulose and croscarmellose sodium to mixture one and mix well to obtain mixture two;

[0039] (3) Add magnesium stearate to the second mixture, mix together, press tablets, coat, and pack.

Embodiment 2

[0041] Product prescription (1000 tablets):

[0042]

[0043] Preparation Process:

[0044] (1) Mix the prescription amount of Sofosbuvir and colloidal silica evenly to obtain mixture one;

[0045] (2) Add direct pressure mannitol, optimized microcrystalline cellulose and croscarmellose sodium to mixture one and mix well to obtain mixture two;

[0046] (3) Add magnesium stearate to the second mixture, mix together, press tablets, coat, and pack.

Embodiment 3

[0048] Product prescription (1000 tablets):

[0049]

[0050] Preparation Process:

[0051] (1) Mix the prescription amount of Sofosbuvir and colloidal silica evenly to obtain mixture one;

[0052] (2) Add direct pressure mannitol, optimized microcrystalline cellulose and croscarmellose sodium to mixture one and mix well to obtain mixture two;

[0053] (3) Add magnesium stearate to the second mixture, mix together, press tablets, coat, and pack.

[0054] For the convenience of comparison with the examples, the following comparative examples are specifically cited for comparative study.

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Abstract

The invention provides a sofosbuvir tablet and a preparation method thereof. The sofosbuvir tablet comprises 10-41%, by total weight of the sofosbuvir tablet, of sofosbuvir, 1-3%, by total weight of the sofosbuvir tablet, of first diluting agent, 53-86%, by total weight of the sofosbuvir tablet, of second diluting agent, 3-10%, by total weight of the sofosbuvir tablet, of disintegrating agent and 0.5-3.0%, by total weight of the sofosbuvir tablet, of lubricating agent. The preparation method is a powder directly-mixing and tabletting method and comprises the following steps: (1) uniformly mixing the sofosbuvir and the first diluting agent to obtain a mixture I; (2) adding and uniformly mixing the second diluting agent and the disintegrating agent in the mixture I to obtain a mixture II; and (3) adding the lubricating agent into the mixture II, totally mixing, tabletting, coating and packaging. Compared with the prior art, the sofosbuvir tablet provided by the invention has the advantages of greatly improving the dissolution rate of the sofosbuvir preparation, enabling the production efficiency to be higher and the preparation cost to be lower, and being capable of adapting to large-scale industrial production.

Description

Technical field [0001] The invention relates to the technical field of medicine, in particular to a sofosbuvir tablet and a preparation method thereof. Background technique [0002] Hepatitis C is a viral hepatitis caused by hepatitis C virus (HCV) infection, which can lead to chronic inflammatory necrosis and fibrosis of the liver, and even hepatocellular carcinoma, which is extremely harmful to the health and life of patients. The US Centers for Disease Control estimates that 4.5 million people are infected in the US alone. According to the World Health Organization, there are more than 200 million infected individuals worldwide, and at least three to four million people are infected each year. Once infected, about 20% of people can clear the virus, but the remaining people may carry HCV for the rest of their lives. 10% to 20% of chronically infected individuals eventually develop destructive sclerosis or cancer of the liver. The viral disease is transmitted parenterally thr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/30A61K31/7072A61K47/04A61K47/26A61K47/38A61P1/16A61P31/14
Inventor 殷殿书赵晓雷孙立杰李彪李朋飞陈雪桃张伟
Owner SHIJIAZHUANG NO 4 PHARMA
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