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A kind of bortezomib freeze-dried powder for injection and preparation method thereof

A technology of bortezomib and freeze-dried powder for injection is applied in the field of bortezomib freeze-dried powder for injection and its preparation, and can solve the problems of increased substance, increased medication risk, excessive moisture and the like

Active Publication Date: 2016-11-16
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The samples prepared according to the above process have the following problems: ① organic solvents, such as tert-butanol, etc. are needed in the production process, and there are certain residues in the final product, which increases the risk of medication; ② bortezomib is sensitive to moisture, and injection The solid content of bortezomib is only 38.5mg, which can easily absorb the moisture migrated in the rubber stopper and cause the moisture to exceed the standard, thereby affecting other indicators of the product such as related substances, visible foreign matter, etc.; Oxygen reaction causes related substances to increase

Method used

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  • A kind of bortezomib freeze-dried powder for injection and preparation method thereof
  • A kind of bortezomib freeze-dried powder for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] (1) Add 2.4L of water for injection into the dispensing tank, keep the water temperature at 45°C, and pass nitrogen into it for 30 minutes; add 3.5g of bortezomib, and use a homogenizer to shear at a high speed (9000 rpm) to the liquid clarify;

[0023] (2) Add 35g of mannitol to the above liquid, stir to dissolve, use 0.1mol / L hydrochloric acid solution to adjust the pH value to 5.0, add water for injection to 3.5L, and fill the liquid in In a vial, add a rubber stopper halfway (the rubber stopper is dried at 105°C for 4 hours), and put it into a lyophilizer for lyophilization.

[0024] (3) The freeze-drying curve is: before the product is put in, the shelf is cooled to -40°C in advance, and the shelf temperature is kept at -40°C for 2 hours after the product is put in; the vacuum pump is started, and the vacuum is drawn to 20Pa; the temperature is slowly raised to -5 °C and maintained for 10 hours; slowly raised to 40 °C and maintained for 4 hours.

[0025] (4) Afte...

Embodiment 2

[0027] (1) Add 2.8L water for injection into the dispensing tank, keep the water temperature at 35°C, and pass carbon dioxide gas into it for 40 minutes; liquid clarification;

[0028] (2) Add 35g of mannitol to the above liquid, stir to dissolve, use 0.1mol / L hydrochloric acid solution to adjust the pH value to 3.0, add water for injection to 3.5L, and fill the liquid in In a vial, add a rubber stopper halfway (the rubber stopper is dried at 110°C for 3 hours), and put it into a lyophilizer for lyophilization.

[0029] (3) The freeze-drying curve is: before the product is placed, the shelf is cooled to -40°C in advance, and the shelf temperature is kept at -40°C for 4 hours after the product is placed; the vacuum pump is started, and the vacuum is drawn to 20Pa; the temperature is slowly raised to -5 °C and maintained for 15 hours; slowly raised to 40 °C and maintained for 6 hours.

[0030] (4) After the freeze-drying is completed, fill the freeze-drying box with nitrogen t...

Embodiment 3

[0032] (1) Add 2.6L of water for injection into the dispensing tank, keep the water temperature at 30°C, and pass argon into it for 50 minutes; add 3.5g of bortezomib, and use a homogenizer to shear at a high speed (16000 rpm) to the liquid clarification;

[0033] (2) Add 35g of mannitol to the above liquid, stir to dissolve, use 0.1mol / L hydrochloric acid solution to adjust the pH value to 4.5, add water for injection to 3.5L, and fill the liquid in In a vial, add a rubber stopper halfway (the rubber stopper is dried at 120°C for 2 hours), and put it into a lyophilizer for lyophilization.

[0034] (3) The freeze-drying curve is: before the product is placed, the shelf is cooled to -40°C in advance, and the shelf temperature is kept at -40°C for 3 hours after the product is placed; the vacuum pump is started, and the vacuum is drawn to 20Pa; the temperature is slowly raised to -5 °C and maintained for 15 hours; slowly raised to 40 °C and maintained for 6 hours.

[0035] (4) ...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and relates to bortezomib freeze-dried powder for injection and a preparation method thereof. The freeze-dried powder comprises 1 part of bortezomib and 8-10 parts of mannitol. According to the preparation method, the dissolution speed of a medicine is increased through high-speed rotation and shearing of a homogenizer, the problem that the active ingredient bortezomib is difficult to dissolve is solved, and solvent residues, generated when an organic solvent such as tertiary butanol and the like is used for dispensing, on an ultimate product are avoided. The process is simple and easy to use and suitable for industrial production, and the obtained product has no solvent residues.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a bortezomib freeze-dried powder for 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] The dosage form of bortezomib currently on the market at home and abroad is freeze-dried powder for injection, the specification is 3.5 mg, and the prescription contains 3.5 mg of active ingredients bortezomib and 35 mg of mannitol. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/69A61K38/05A61P35/00
Inventor 张贵民赵震震程战立
Owner SHANDONG NEWTIME PHARMA
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