CefPiramide sodium powder for injection

Abstract

The invention provides a freeze-dried injection powder of Cefpiramide Sodium. The whole process of the preparation method of the injection powder is carried out in water solution and the obtained Cefpiramide Sodium has high purity. The water content of the product prepared by the freeze-drying technology of the invention can be controlled below 1 percent. The freeze-dried injection powder of Cefpiramide Sodium has high dissolution rate and good stability.

Description

technical field

[0001] The invention relates to a preparation method of cefpiramide sodium freeze-dried powder injection, belonging to the field of pharmaceutical preparations. Background technique

[0002] Cefpiramide Sodium (Cefpiramide Sodium) is a semi-synthetic third-generation cephalosporin antibiotic, which has the characteristics of broad antibacterial spectrum, strong antibacterial activity and stability to lactamase. It is effective against many Gram-positive cocci, including Staphylococcus and Enterococcus, and is also effective against Gram-negative bacilli and anaerobic bacteria. Among them, it has good antibacterial activity against Pseudomonas aeruginosa. Cefpiramide sodium is used for pneumonia caused by sensitive Gram-negative and positive bacteria such as Escherichia coli, Proteus, Klebsiella pneumoniae, Pseudomonas aeruginosa, influenza bacillus, pneumococcus, Staphylococcus aureus, acute bronchitis, Acute exacerbation of chronic bronchitis, bronchiectasi...

Examples

Embodiment 1

[0044] Weigh 730g of sodium benzoate, 100g of sodium dihydrogen phosphate, and 480g of disodium hydrogen phosphate in a reaction kettle, stir and dissolve with 35L of water for injection at room temperature, add 10.0kg of cefpiramic acid, and control the temperature at 20°C, stirring until it does not dissolve; Add 16L of 4% sodium hydroxide solution dropwise at a speed of 155mL / min, stir to dissolve, stop the dropwise addition and keep stirring for 13 minutes every 20 minutes, adjust the pH value to 6.5; add 200g of activated carbon, decolorize for 30 minutes; filter with suction , put the filtrate into a lyophilizer at a rate of 6°C / min to cool down and freeze to -50°C, vacuumize, heat up to -10°C within 5 hours, maintain -10°C for 12 hours, and continue to heat up to within 2.5 hours 20°C, maintain 20°C for 9 hours, then raise the temperature to 37°C within 2 hours, and maintain 37°C for 5 hours to obtain cefpiramide sodium freeze-dried powder injection. Moisture is 0.73%. ...

Embodiment 2

[0046] Weigh 750g of sodium benzoate, 95g of sodium dihydrogen phosphate, and 490g of disodium hydrogen phosphate in a reaction kettle, stir and dissolve with 35L of water for injection at room temperature, add 10.0kg of cefpiramic acid, and control the temperature at 15°C, stirring until it does not dissolve; Add 15L of 4% sodium hydroxide solution dropwise at a rate of 150mL / min, stir to dissolve, stop the dropwise addition and keep stirring for 15 minutes every 25 minutes, adjust the pH value to 7.3; add 200g of activated carbon, decolorize for 30 minutes; filter with suction , put the filtrate into the freeze dryer at a rate of 6.5°C / min to cool down and freeze to -52°C, vacuumize, heat up to -11°C within 5.5 hours, maintain -11°C for 11.5 hours, and continue to heat up to within 3 hours 18°C, maintain 18°C ​​for 8 hours, then raise the temperature to 40°C within 2.5 hours, and maintain 40°C for 5.5 hours to obtain cefpiramide sodium freeze-dried powder. Moisture is 0.69% ...

Embodiment 3

[0048] Weigh 720g of sodium benzoate, 105g of sodium dihydrogen phosphate, and 470g of disodium hydrogen phosphate in a reaction kettle, stir and dissolve with 35L of water for injection at room temperature, add 10.0kg of cefpiramic acid, and control the temperature at 20°C, stirring until it does not dissolve; Add 15.7L of 4% sodium hydroxide solution dropwise at a rate of 160mL / min, stir to dissolve, stop the dropwise addition and keep stirring for 10 minutes every 22 minutes, adjust the pH value to 7.0; add 200g of activated carbon, decolorize for 30 minutes; Filtrate, put the filtrate into a lyophilizer at a rate of 6.5°C / min to cool down and freeze to -55°C, vacuumize, heat up to -10°C within 6 hours, maintain -10°C for 12 hours, and continue to heat up within 2.8 hours to 19°C, the time for maintaining 19°C was 8.5 hours, and then the temperature was raised to 39°C within 2 hours, and the time for maintaining 39°C was 5 hours to obtain cefpiramide sodium freeze-dried powd...

technical field

[0001] The invention relates to a preparation method of cefpiramide sodium freeze-dried powder injection, belonging to the field of pharmaceutical preparations. Background technique

[0002] Cefpiramide Sodium (Cefpiramide Sodium) is a semi-synthetic third-generation cephalosporin antibiotic, which has the characteristics of broad antibacterial spectrum, strong antibacterial activity and stability to lactamase. It is effective against many Gram-positive cocci, including Staphylococcus and Enterococcus, and is also effective against Gram-negative bacilli and anaerobic bacteria. Among them, it has good antibacterial activity against Pseudomonas aeruginosa. Cefpiramide sodium is used for pneumonia caused by sensitive Gram-negative and positive bacteria such as Escherichia coli, Proteus, Klebsiella pneumoniae, Pseudomonas aeruginosa, influenza bacillus, pneumococcus, Staphylococcus aureus, acute bronchitis, Acute exacerbation of chronic bronchitis, bronchiectasi...

Examples

Embodiment 1

[0044] Weigh 730g of sodium benzoate, 100g of sodium dihydrogen phosphate, and 480g of disodium hydrogen phosphate in a reaction kettle, stir and dissolve with 35L of water for injection at room temperature, add 10.0kg of cefpiramic acid, and control the temperature at 20°C, stirring until it does not dissolve; Add 16L of 4% sodium hydroxide solution dropwise at a speed of 155mL / min, stir to dissolve, stop the dropwise addition and keep stirring for 13 minutes every 20 minutes, adjust the pH value to 6.5; add 200g of activated carbon, decolorize for 30 minutes; filter with suction , put the filtrate into a lyophilizer at a rate of 6°C / min to cool down and freeze to -50°C, vacuumize, heat up to -10°C within 5 hours, maintain -10°C for 12 hours, and continue to heat up to within 2.5 hours 20°C, maintain 20°C for 9 hours, then raise the temperature to 37°C within 2 hours, and maintain 37°C for 5 hours to obtain cefpiramide sodium freeze-dried powder injection. Moisture is 0.73%. ...

Embodiment 2

[0046] Weigh 750g of sodium benzoate, 95g of sodium dihydrogen phosphate, and 490g of disodium hydrogen phosphate in a reaction kettle, stir and dissolve with 35L of water for injection at room temperature, add 10.0kg of cefpiramic acid, and control the temperature at 15°C, stirring until it does not dissolve; Add 15L of 4% sodium hydroxide solution dropwise at a rate of 150mL / min, stir to dissolve, stop the dropwise addition and keep stirring for 15 minutes every 25 minutes, adjust the pH value to 7.3; add 200g of activated carbon, decolorize for 30 minutes; filter with suction , put the filtrate into the freeze dryer at a rate of 6.5°C / min to cool down and freeze to -52°C, vacuumize, heat up to -11°C within 5.5 hours, maintain -11°C for 11.5 hours, and continue to heat up to within 3 hours 18°C, maintain 18°C ​​for 8 hours, then raise the temperature to 40°C within 2.5 hours, and maintain 40°C for 5.5 hours to obtain cefpiramide sodium freeze-dried powder. Moisture is 0.69% ...

Embodiment 3

[0048] Weigh 720g of sodium benzoate, 105g of sodium dihydrogen phosphate, and 470g of disodium hydrogen phosphate in a reaction kettle, stir and dissolve with 35L of water for injection at room temperature, add 10.0kg of cefpiramic acid, and control the temperature at 20°C, stirring until it does not dissolve; Add 15.7L of 4% sodium hydroxide solution dropwise at a rate of 160mL / min, stir to dissolve, stop the dropwise addition and keep stirring for 10 minutes every 22 minutes, adjust the pH value to 7.0; add 200g of activated carbon, decolorize for 30 minutes; Filtrate, put the filtrate into a lyophilizer at a rate of 6.5°C / min to cool down and freeze to -55°C, vacuumize, heat up to -10°C within 6 hours, maintain -10°C for 12 hours, and continue to heat up within 2.8 hours to 19°C, the time for maintaining 19°C was 8.5 hours, and then the temperature was raised to 39°C within 2 hours, and the time for maintaining 39°C was 5 hours to obtain cefpiramide sodium freeze-dried powd...

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