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Stable tedizolid phosphate medicine composition

A technology of tedizolid and composition, applied in the field of tedizolid pharmaceutical composition and its preparation

Inactive Publication Date: 2016-06-08
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The present invention aims to overcome the problems of poor fluidity and low dissolution rate of the existing tedizolid pharmaceutical composition, and changes the dissolution rate of tedizolid And the shortcomings of low bioavailability, improve the curative effect

Method used

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  • Stable tedizolid phosphate medicine composition
  • Stable tedizolid phosphate medicine composition
  • Stable tedizolid phosphate medicine composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Tedizolid 200g

[0036] Croscarmellose Sodium 50g

[0037] Microcrystalline cellulose 70g

[0038] Micropowder silica gel 0.5g

[0039] Appropriate amount of 10% pregelatinized starch solution

[0040] Preparation

[0041] 1) Dry, pulverize and pass through a 100-mesh sieve to tedizolid, croscarmellose sodium and microcrystalline cellulose respectively to obtain tedizolid powder, croscarmellose sodium and microcrystalline cellulose respectively Cellulose powder;

[0042] 2) Take the prescribed amount of tedizolid, croscarmellose sodium and microcrystalline cellulose, mix well, then add 10% pregelatinized starch solution to make a soft material, pass through a 40-mesh sieve to granulate , to obtain tedizolid wet granules;

[0043] 3) Dry the above tedizolid wet granules at 60°C until the water content is less than 5%, to obtain tedizolid dry granules

[0044] 4) Pass the above-mentioned dry tedizolid granules through a 40-mesh sieve for granulation, then add a lub...

Embodiment 2

[0047] Tedizolid 400g

[0048] Croscarmellose Sodium 100g

[0049] Microcrystalline cellulose 140g

[0050] Micropowder silica gel 1g

[0051] Appropriate amount of 10% pregelatinized starch solution

[0052] Preparation

[0053] 1) Drying, pulverizing and passing tedizolid, croscarmellose sodium and microcrystalline cellulose respectively through a 100-mesh sieve to obtain tedizolid powder and microcrystalline cellulose powder respectively;

[0054] 2) Take the prescribed amount of tedizolid, croscarmellose sodium and microcrystalline cellulose, mix well, then add 10% pregelatinized starch solution to make a soft material, pass through a 40-mesh sieve to granulate , to obtain tedizolid wet granules;

[0055] 3) drying the above tedizolid wet granules at 60°C until the water content is less than 5%, to obtain tedizolid dry granules;

[0056] 4) Pass the above-mentioned dry tedizolid granules through a 40-mesh sieve for granulation, then add a lubricant, mix well, and aft...

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Abstract

The invention discloses a stable tedizolid phosphate medicine composition, which is characterized in that a recipe for preparing 1000 tablets comprises the following ingredients including 200 to 400g of tedizolid phosphate, 70 to 140g of microcrystalline cellulose, 0.5 to 1g of superfine silica gel powder, 50 to 100g of croscarmellose sodium and a proper amount of a 10-percent amylum pregelatinisatum solution. The invention also relates to a preparation method of a tedizolid phosphate tablet. The tedizolid phosphate prepared by the recipe and the preparation method provided by the invention has the advantages of high dissolution rate, high bioavailability and good curative effect.

Description

technical field [0001] The invention relates to a stable tedizolid pharmaceutical composition and a preparation method thereof. Background technique [0002] Tedizolidphosphate (SIVEXTRO) was developed by Cubist Pharmaceuticals and was approved by the FDA on June 20, 2014. It is an oxazolidinone antibacterial drug suitable for the treatment of infections caused by designated susceptible bacteria in adults. Causes acute bacterial skin and skin structure infection (ABSSSI). To reduce the occurrence of drug-resistant bacteria and maintain the effectiveness of SIVEXTRO and other antibacterial drugs, SIVEXTRO should only be used to treat or prevent infections that are proven or strongly suspected to be caused by bacteria. [0003] Its structural formula: [0004] [0005] Through the research on the prior art, the low bioavailability of tedizolid in the human body is still a problem that bothers people and needs to be solved urgently. In addition, the appropriate preparatio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4439A61K47/38A61P31/04A61P17/00
Inventor 严洁李轩
Owner TIANJIN HANKANG PHARMA BIOTECH
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