Lyophilization technology for preparing bivalirudin for injection

A technology for bivalirudin and injection, which is applied in the field of freeze-drying technology for preparing bivalirudin for injection, and can solve problems such as long freeze-drying time, high energy consumption, and unqualified foreign matter

Active Publication Date: 2012-12-12
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The performance of the final product obtained by different freeze-drying processes is quite different, mainly manifested in longer freeze-dry

Method used

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  • Lyophilization technology for preparing bivalirudin for injection
  • Lyophilization technology for preparing bivalirudin for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Get 17.5g of bivalirudin, dissolve it in 70ml of water for injection, add 7.5g of mannitol, and make it dissolve. Slowly add 5% (w / v) lye solution dropwise, adjust the pH value to 5.5, and add water for injection to a volume of 300ml. Under 100-level laminar flow, subpackage, 5ml / bottle, semi-stoppered, and freeze-dry using the following different freeze-drying processes, see the table below for details:

[0054]

[0055] According to the freeze-drying process involved in the present invention, the quality of the prepared samples is stable, and the results of the redissolved visible foreign matter all comply with regulations, thereby improving the safety of clinical medication.

Embodiment 2

[0057] Get 11.6g of bivalirudin, be dissolved in 120ml water for injection, add the mannitol of 7.5g, make it dissolve. Slowly add 5% (w / v) lye solution dropwise, adjust the pH value to 5.5, and add water for injection to a volume of 200ml. Under 100-level laminar flow, subpackage, 5ml / bottle, half-stoppered, and freeze-dry using the following freeze-drying process:

[0058] a. Put the bottle containing the liquid medicine into the freeze dryer;

[0059] b. Reduce the shelf temperature of the freeze dryer to below -40°C at a rate of 35°C per hour;

[0060] c. When the temperature of the product drops below -40°C, keep it warm for 3 hours;

[0061] d. Raise the shelf temperature to -30°C and keep it warm for 3 hours;

[0062] e. Then lower the temperature of the shelf to -45°C and keep it warm for 2 to 4 hours;

[0063] f. Start vacuuming, when the vacuum degree is below 2Pa, start to heat up;

[0064] g. Raise the shelf temperature to -10°C and keep it for 10 hours;

[0...

Embodiment 3

[0071] Get 11.6g of bivalirudin, be dissolved in 120ml water for injection, add the mannitol of 7.5g, make it dissolve. Slowly add 5% (w / v) lye solution dropwise, adjust the pH value to 5.5, and add water for injection to a volume of 200ml. Under 100-level laminar flow, subpackage, 5ml / bottle, half-stoppered, and freeze-dry using the following freeze-drying process:

[0072] a. Put the bottle containing the liquid medicine into the freeze dryer;

[0073] b. Reduce the shelf temperature of the freeze dryer to below -40°C at a rate of 30-35°C per hour;

[0074] c. When the temperature of the product drops below -40°C, keep it warm for 2 to 4 hours;

[0075] d. Start vacuuming, when the vacuum degree reaches below 20Pa, start to heat up;

[0076] e. Raise the shelf temperature to -10°C~-20°C and keep it for 10 hours;

[0077] f. Raise the shelf temperature to 0°C and keep it for 4 hours;

[0078] g. Raise the shelf temperature to 25°C~30°C and keep it warm for 6 hours;

[007...

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Abstract

The invention relates to a lyophilization technology for preparing bivalirudin for injection. According to the technology, pre-freezing processes of bivalirudin are researched without changing the existing bivalirudin formula, and an annealing operation is added, so preparation products are obtained; and compared with preparation products obtained through common lyophilization technologies, the preparation products obtained through the lyophilization technology disclosed in the invention have the advantages of good appearance and stable quality.

Description

technical field [0001] The invention relates to a preparation process of chemical medicine and polypeptide medicine, in particular to a freeze-drying process for preparing bivalirudin for injection. Background technique [0002] The incidence of thrombosis caused by atherosclerosis is increasing year by year in my country, and anticoagulant drugs are extremely important in the treatment of this disease. Bivalirudin (bivalirudin) is a thrombin inhibitor recently used clinically. Early clinical studies have shown that bivalirudin anticoagulant therapy is effective and has a lower incidence of bleeding events, compared with traditional heparin anticoagulant therapy. Safer than using . Bivalirudin directly inhibits the action of thrombin by binding to the catalyst site and the anion export site of the circulation and thrombin clot. [0003] Bivalirudin is a polypeptide composed of 20 amino acids with a molecular weight of 2180. The drug has poor physical stability in aqueous ...

Claims

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Application Information

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IPC IPC(8): A61K38/10A61K9/19A61P7/02
Inventor 王小雷
Owner JIANGSU HANSOH PHARMA CO LTD
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