Bortezomib freeze-dried powder injection and preparation method thereof

A technology of bortezomib and freeze-dried powder injection, which is applied in the field of medicine, can solve the problems of increased impurities and poor clarity of bortezomib preparations, and achieve the effects of good resolubility and stability, small total impurities, and avoiding enlargement

Active Publication Date: 2012-11-21
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to solve the poor clarity of the bortezomib preparation after reconstitution, and also to solve the problem that the impurities of the bortezomib preparation increas

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0023] Embodiment 1, bortezomib freeze-dried powder injection

[0024] Weigh 3.5g of bortezomib, 105g of mannitol, and 0.7g of sodium bisulfite, mix and grind for 8 minutes, add 2700mL of water for injection, stir until completely dissolved, add 2.7g of activated carbon for needles, stir for 15 minutes, decarbonize and filter. Add water for injection to the filtrate to 3500mL, stir evenly, and adjust the pH to 6.0 with 1mol / L sodium hydroxide solution. The medicinal solution was sterilized and filtered through a 0.22 μm microporous membrane, filled into 7 mL vials, each bottle filled with a volume of 3.5 mL, half-filled with a rubber stopper, and placed in a lyophilizer for lyophilization.

[0025] First lower the temperature to -8°C and keep it warm for 90 minutes, then quickly drop the temperature to -40°C and keep it warm for 180 minutes, start vacuuming after the cold trap cools down to -40°C, slowly increase the temperature of the shelf to -10°C, and keep it warm for 18 h...

Example Embodiment

[0026] Embodiment 2, bortezomib freeze-dried powder injection

[0027] Weigh 3.5g of bortezomib, 157.5g of dextran, and 3.2g of sodium metabisulfite, mix and grind for 5 minutes, add 2700mL of water for injection, stir until completely dissolved, add 2.7g of activated carbon for needles, stir for 15 minutes, decarbonize and filter. Add water for injection to the filtrate to 3500mL, stir evenly, and adjust the pH to 6.5 with 1mol / L sodium hydroxide solution. The medicinal solution was sterilized and filtered through a 0.22 μm microporous membrane, filled into 7 mL vials, each bottle filled with a volume of 3.5 mL, half-filled with a rubber stopper, and placed in a lyophilizer for lyophilization.

[0028] First lower the temperature to -8°C and keep it warm for 90 minutes, then quickly drop the temperature to -40°C and keep it warm for 120 minutes, start vacuuming after the cold trap cools down to -40°C, slowly increase the temperature of the shelf to -10°C, and keep it warm for...

Example Embodiment

[0029] Embodiment 3, bortezomib freeze-dried powder injection

[0030]Weigh 3.5g bortezomib, 280g excipient (the excipient is a mixture of mannitol and dextran), 2.6g sodium bisulfite, mix and grind for 8 minutes, add 2700mL water for injection, stir until completely dissolved, add 2.7g Activated carbon was used for the needle, stirred for 15 minutes, and decarbonized and filtered. Add water for injection to the filtrate to 3500 mL, stir evenly, and adjust the pH to 6.0 with 0.5 mol / L sodium carbonate solution. The medicinal solution was sterilized and filtered through a 0.22 μm microporous membrane, filled into 7 mL vials, each bottle filled with a volume of 3.5 mL, half-filled with a rubber stopper, and placed in a lyophilizer for lyophilization.

[0031] First lower the temperature to -8°C and keep it warm for 90 minutes, then quickly drop the temperature to -40°C and keep it warm for 200 minutes, start vacuuming after the cold trap cools down to -40°C, slowly increase the...

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Abstract

The invention belongs to the technical field of pharmaceuticals, and specifically relates to a bortezomib freeze-dried powder injection and a preparation method thereof. Directed at poor clarity of a redissolved bortezomib preparation, and fast increase of impurities in the bortezomib preparation with standing time, the present invention provides a bortezomib freeze-dried powder injection which includes bortezomib, an excipient, an antioxidant, and a pH adjusting agent. The resulting preparation is good in redissolution with a dissolution time of 29-36 seconds, while the total impurity content of the preparation is not higher than 1.27% after placing for 9 hours at room temperature. The preparation is good in stability, and helps to increase the safety of drug use.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a bortezomib freeze-dried powder injection and a preparation method thereof. Background technique [0002] Bortezomib (PS-341), trade name Velcade, is a new type of anti-tumor drug developed by Millennium Pharmaceutical Company of the United States. The drug leads to the death of tumor cells by blocking the degradation of various proteins that regulate apoptosis and signal transduction in cells. A large number of studies have found that bortezomib has strong anti-tumor activity against a variety of tumors, especially multiple myeloma, mantle cell lymphoma, other B-cell lymphomas, and Hodgkin's lymphoma in hematological tumors. [0003] Yi Wenyuan and others pointed out in "Research Progress of Proteasome Inhibitors Reversing Multidrug Resistance of Tumors" ("Foreign Medicine and Pharmacy Volume", April 2007, Volume 34, Issue 2) that boronic acid peptides include bor...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/69A61K38/05A61K47/10A61K47/26A61K47/02A61P35/00
Inventor 赵志全赵震震冯中
Owner SHANDONG NEWTIME PHARMA
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