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Freeze drying agent containing bortezomib and preparation method thereof

A technology of bortezomib and freeze-dried preparation is applied in the field of freeze-dried preparation containing bortezomib and its preparation, and can solve the problems of bortezomib moisture sensitivity, residual freeze-dried product, easy oxidation of bortezomib, etc. The process is simple and easy to implement, the prescription is simple, and the effect of shortening the dispensing time

Inactive Publication Date: 2016-12-07
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 following problems still exist in the samples prepared according to the above prescription and process: ①The organic solvent tert-butanol is used in the production process, and there are residues in the freeze-dried finished product, which increases the risk of medication and has poor safety; ②Bortezomib is easy to oxidize , Oxidation reactions are prone to occur during the preparation process, and as the preparation time prolongs, the related substances increase rapidly; ③Bortezomib is relatively sensitive to moisture, and the high moisture in the freeze-dried finished product affects other indicators of the product

Method used

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  • Freeze drying agent containing bortezomib and preparation method thereof
  • Freeze drying agent containing bortezomib and preparation method thereof
  • Freeze drying agent containing bortezomib and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0036]

[0037] Preparation:

[0038] At room temperature, 0.2g Dissolve HS15 in 200ml of water for injection, add 1.0g of bortezomib, stir well, add 8.0g of mannitol, add 600ml of water for injection and stir until completely dissolved, adjust the pH to 4.0-7.0, add water for injection to 1000ml to obtain an intermediate drug liquid; the intermediate drug solution was filtered through a 0.2 μm pressure filter membrane under nitrogen pressure, and 1 ml was dispensed into an injection bottle, freeze-dried, plugged, capped, and packaged to obtain a freeze-dried powder injection. The freeze-drying process is as follows: pre-freezing stage: 2.5 hours at -45°C, 3 hours at -25°C, 5 hours at -45°C; primary sublimation: 11 hours at -35°C, 22 hours at -25°C, 22 hours at -20°C ℃ for 5.5 hours, -10 ℃ for 4 hours, 0 ℃ for 4 hours; secondary drying: 30 ℃ for 5 hours.

Embodiment 2

[0040]

[0041] Preparation:

[0042] At room temperature, 0.3g Dissolve HS15 in 200ml of water for injection, add 1.0g of bortezomib, stir evenly, add 6.0g of mannitol, add 600ml of water for injection and stir until completely dissolved, adjust the pH to 4.0-7.0, add water for injection to 1000ml to obtain an intermediate drug liquid; the intermediate drug solution was filtered through a 0.2 μm pressure filter membrane under nitrogen pressure, and 1 ml was dispensed into an injection bottle, freeze-dried, plugged, capped, and packaged to obtain a freeze-dried powder injection. The freeze-drying process is as follows: pre-freezing stage: 3 hours at -45°C, 3 hours at -25°C, 6 hours at -45°C; primary sublimation: 12 hours at -35°C, 22 hours at -25°C, 22 hours at -20°C ℃ for 5.5 hours, -10 ℃ for 4 hours, 0 ℃ for 4 hours; secondary drying: 30 ℃ for 4 hours.

Embodiment 3

[0044]

[0045] Preparation:

[0046] At room temperature, 0.4g Dissolve HS 15 in 200ml of water for injection, add 1.5g of bortezomib, stir well, add 11.0g of mannitol, add water for injection and stir until completely dissolved, and adjust the pH to 4.0-7.0. Add water for injection to 1000ml to obtain the intermediate drug solution; the intermediate drug solution is filtered through a 0.2 μm press filter membrane under nitrogen pressure, and then packed in 1ml into injection bottles, freeze-dried, plugged, capped, and packaged to obtain frozen Dry powder injection. The freeze-drying process adopts the freeze-drying process in Example 1.

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Abstract

The invention relates to a freeze drying agent containing bortezomib and a preparation method thereof. The freeze drying agent provided by the invention contains the bortezomib, mannitol and a surface active agent. Through the adding of the surface active agent, the solubility of the bortezomib is improved, and the drug solution preparing time is shortened. The preparation method provided by the invention is simple and practicable in process, and suitable for industrial production, and the obtained product has no solvent residue. In addition, the freeze drying agent prepared by adopting the preparation method provided by the invention is more excellent in the stability.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a bortezomib-containing freeze-dried preparation and a preparation method thereof. Background technique [0002] Bortezomib, chemical name [(1R)-3-methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(pyrazinecarboxy)amino]propyl] Amino] butyl] boronic acid, trade name Velcade (Velcade), developed by the U.S. Millennium Pharmaceuticals company. 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. treatment of bone marrow cancer. [0003] Patent CN103070835A aims at the problem of poor water solubility of bortezomib, uses a mixed solution of mannitol and tert-butanol to increase the dissolution rate of bortezomib, and at the same time uses the order of adding materials to further increase the dissolution rate of bortezomib. [0004] Patent CN103212055B relates to a pharmaceutica...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K47/26A61K47/34A61K38/05A61K31/69A61P35/00
CPCA61K9/19A61K9/0019A61K31/69A61K38/05A61K47/26A61K47/34
Inventor 袁恒立汪艳艳董礼孙运栋孙长安
Owner JIANGSU HANSOH PHARMA CO LTD
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