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Bortezomib freeze-dried powder injection and preparation process thereof

A technology of bortezomib and freeze-dried powder injection, which is applied in the field of medicine, can solve the problems of poor thermal stability of bortezomib, unmarked oxygen content limit, uneven drug dispersion, etc., optimize the freeze-drying process and shorten the reconstitution time , Increase the effect of drug stability

Active Publication Date: 2017-01-11
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the samples prepared by the above process still have the following problems: ①The temperature in the pre-freezing stage is relatively single, which may easily lead to uneven dispersion of the drug in the freeze-dried sample; ②Bortezomib is easily oxidized, and nitrogen filling can protect bortezomib from oxidation reactions However, the oxygen content limit is not indicated; ③ Bortezomib has poor thermal stability, if its suspension is heated, it will easily cause an increase in impurity content, thereby affecting product quality

Method used

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  • Bortezomib freeze-dried powder injection and preparation process thereof
  • Bortezomib freeze-dried powder injection and preparation process thereof
  • Bortezomib freeze-dried powder injection and preparation process thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043]

[0044] Preparation:

[0045] Heat 330g of tert-butanol to 50°C, add to 500ml of water for injection, stir well, add 10.0g of mannitol, fill with nitrogen and stir well, control the oxygen content of the solution to ≤1%; add 1.0g of bortezomib, stir with nitrogen Uniform, control the oxygen content of the solution ≤ 1%, adjust the pH to 4.0-7.0; add water for injection to 1000ml, fill with nitrogen and stir evenly, control the oxygen content of the bortezomib solution ≤ 1%; bortezomib solution through nitrogen Press-filter through a 0.2 μm microporous filter membrane, dispense 1 ml into injection vials, freeze-dry, stopper, cap, and pack to obtain a freeze-dried powder. The freeze-drying process is as follows, pre-freezing stage: 0°C for 2 hours, -45°C for 3 hours; primary sublimation: -40°C for 11 hours, -35°C for 11 hours, -25°C for 12 hours , -20°C for 5.5 hours, -15°C for 4 hours, 0°C for 4 hours; secondary drying: 30°C for 5 hours; vacuum ≤0.3MPa during freeze...

Embodiment 2

[0047]

[0048] Preparation:

[0049]Heat 330g of tert-butanol to 55°C, add to 550ml of water for injection, stir well, add 10.0g of mannitol, fill with nitrogen and stir well, control the oxygen content of the solution to ≤1%; add 1.0g of bortezomib, stir with nitrogen Uniform, control the oxygen content of the solution ≤ 1%, adjust the pH to 4.0-7.0; add water for injection to 1000ml, fill with nitrogen and stir evenly, control the oxygen content of the bortezomib solution ≤ 1%; bortezomib solution through nitrogen Press-filter through a 0.2 μm microporous filter membrane, dispense 1 ml into injection vials, freeze-dry, stopper, cap, and pack to obtain a freeze-dried powder. The freeze-drying process is as follows, pre-freezing stage: 4 hours at 0°C, 2 hours at -45°C; primary sublimation: 11 hours at -40°C, 11 hours at -35°C, 12 hours at -25°C , -20°C for 5.5 hours, -10°C for 4 hours, 0°C for 4 hours; secondary drying: 30°C for 5 hours; vacuum ≤0.3MPa during freeze-dryin...

Embodiment 3

[0051]

[0052] Preparation:

[0053] Heat 330g of tert-butanol to 55°C, add to 550ml of water for injection, stir well, add 35.0g of mannitol, fill with nitrogen and stir well, control the oxygen content of the solution to ≤1%; add 3.5g of bortezomib, stir with nitrogen Uniform, control the oxygen content of the solution ≤ 1%, adjust the pH to 4.0-7.0; add water for injection to 1000ml, fill with nitrogen and stir evenly, control the oxygen content of the bortezomib solution ≤ 1%; bortezomib solution through nitrogen Press-filter through a 0.2 μm microporous filter membrane, dispense 1 ml into injection vials, freeze-dry, stopper, cap, and pack to obtain a freeze-dried powder. The freeze-drying process is as follows, pre-freezing stage: 0°C for 3 hours, -45°C for 6 hours; primary sublimation: -40°C for 10 hours, -35°C for 12 hours, -25°C for 14 hours , -20°C for 5 hours, -10°C for 5 hours, 0°C for 4 hours; secondary drying: 30°C for 5 hours; vacuum ≤0.3MPa during freeze-d...

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Abstract

The invention relates to a preparation process of freeze-dried powder injection containing bortezomib. The freeze-dried powder injection contains bortezomib and mannite. By controlling the oxygen content in a solution during preparation and a freeze-drying process, the stability of the bortezomib freeze-dried powder injection is greatly increased, and the re-dissolution time of the freeze-dried powder injection is shortened. The process provided by the invention is simple and easy, and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a preparation process of a freeze-dried powder injection containing an active ingredient of bortezomib. Background technique [0002] Bortezomib, chemical name [(1R)-3-methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(pyrazinecarboxy)amino]propyl] Amino]butyl]boronic acid, whose trade name is Velcade, was developed by Millennium Pharmaceuticals in the United States. Bortezomib is a reversible inhibitor of the chymotrypsin-like activity of 26S proteasome in mammalian cells, and it is cytotoxic to various types of cancer cells. In general, it should be reconstituted with 0.9% sodium chloride injection, administered by intravenous or subcutaneous injection, and it is mainly used for the treatment of multiple myeloma. [0003] Patent CN105056205A relates to a pharmaceutical composition containing bortezomib and a preparation method thereof. The composition contains bortezomib, mannitol and tert-b...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K38/05A61K31/69A61K47/10A61K47/26A61K47/36A61P35/00
CPCA61K9/0019A61K9/19A61K31/69A61K38/05A61K47/10A61K47/26A61K47/36
Inventor 孙运栋汪艳艳董礼黄玉超袁恒立
Owner JIANGSU HANSOH PHARMA CO LTD
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