Injecting carfilzomib and preparation method thereof

A carfilzomib and prescription technology, which is applied in the field of carfilzomib for injection and its preparation, to achieve the effects of reducing production costs, solving oxidation, and solving insoluble problems

Inactive Publication Date: 2018-03-16
QILU PHARMA HAINAN +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] In order to solve the above problems, the inventors provide an effective method, which uses a water-soluble solubilizer to increase the solubility of carfilzomib in water, and adds excipients and antioxidants to freeze-dry, effectively solving the problem of carfilzomib. The problem of adding sulfobutyl β-cyclodextrin in the production process of rice avoids the occurrence of allergic reactions, and at the same time avoids the vasospasm and phlebitis caused by the clinical use of carfilzomib injection, which strengthens the clinical application safety, and when reconstituted, the freeze-dried powder injection can quickly dissolve

Method used

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  • Injecting carfilzomib and preparation method thereof
  • Injecting carfilzomib and preparation method thereof
  • Injecting carfilzomib and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

500ml

[0034] Preparation Process:

[0035] 1) Take 0.6g of solubilizer and 0.6g of antioxidant, add to 100ml of water for injection, bubbling nitrogen in the water for 15min, and stir;

[0036] 2) Take 6g of Carfilzomib, add it to the solution obtained in step 1) under the protection of nitrogen, and stir until the solution is clear;

[0037] 3) Take 30g of lactose, add 250ml of water for injection, stir to dissolve;

[0038] 4) Under nitrogen protection, add the solution obtained in step 2) to the solution obtained in step 3), and stir until the solution is clear;

[0039] 5) Add water for injection to 95% of the prescription and adjust the pH to 3.8;

[0040] 6) Add water for injection to 500ml, stir evenly to obtain the intermediate liquid, and retest the pH value of 3.8;

[0041] 7) The intermediate medicinal solution is press-filtered, sub-packaged, freeze-dried, stoppered, capped, packaged, and obtained carfilzomib freeze-dried powder injection. The freeze-drying process is as fol...

Embodiment 2

500ml

[0044] Preparation Process:

[0045] 1) Take 3g of solubilizer and 1.5g of antioxidant, add to 100ml of water for injection, bubbling nitrogen in the water for 15min, and stir;

[0046] 2) Take 6g of Carfilzomib, add it to the solution obtained in step 1) under the protection of nitrogen, and stir until the solution is clear;

[0047] 3) Take 40g of lactose, add 250ml of water for injection, stir to dissolve;

[0048] 4) Under nitrogen protection, add the solution obtained in step 2) to the solution obtained in step 3), and stir until the solution is clear;

[0049] 5) Add water for injection to 95% of the prescription and adjust the pH to 3.4;

[0050] 6) Add water for injection to 500ml, stir evenly to obtain the intermediate liquid, and retest the pH value of 3.5;

[0051] 7) The intermediate medicinal solution is press-filtered, sub-packaged, freeze-dried, stoppered, capped, packaged, and obtained carfilzomib freeze-dried powder injection. The freeze-drying process is as follo...

Embodiment 3

500ml

[0054] Preparation Process:

[0055] 1) Take 2g of solubilizer and 3g of antioxidants, add to 100ml of water for injection, bubbling nitrogen in the water for 15 minutes, and stir;

[0056] 2) Take 6g of Carfilzomib, add it to the solution obtained in step 1) under the protection of nitrogen, and stir until the solution is clear;

[0057] 3) Take 48g of lactose, add 250ml of water for injection, stir to dissolve;

[0058] 4) Under nitrogen protection, add the solution obtained in step 2) to the solution obtained in step 3), and stir until the solution is clear;

[0059] 5) Add water for injection to 95% of the prescription and adjust the pH to 3.7;

[0060] 6) Add water for injection to 500ml, stir evenly to obtain the intermediate liquid, and retest the pH value of 3.8;

[0061] 7) The intermediate medicinal solution is press-filtered, sub-packaged, freeze-dried, stoppered, capped, packaged, and obtained carfilzomib freeze-dried powder injection. The freeze-drying process is as f...

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PUM

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Abstract

The invention discloses an injecting carfilzomib freeze-dried powder injection and a preparation method thereof. The freeze-dried powder injection is prepared from active components of carfilzomib, lactose, an antioxidant, a surfactant and a pharmaceutically acceptable auxiliary material, wherein the surfactant is preferably polyethylene glycol-12-hydroxystearate. Compared with the prior art, theinjecting carfilzomib freeze-dried powder injection provided by the invention is used for overcoming the defect that a main medicine is difficult to dissolve; further, a cyclodextrin inclusion technique is not used, so that a potential safety hazard brought by cyclodextrin is avoided; meanwhile, through adding the antioxidant, raw materials are prevented from being oxidized. The overall productionprocess is simple and the requirements of production and clinical medication can be effectively met.

Description

Technical field: [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a carfilzomib for injection and a preparation method thereof. Background technique: [0002] Carfilzomib is an intravenously administered tetrapeptide epoxy ketone backbone proteasome inhibitor, used for recurrent multiple patients who have received at least 2 previous treatments including bortezomib (Valco) and immunomodulatory therapy Patients with sexual myeloma were approved by the U.S. Food and Drug Administration (FDA) on July 20, 2012. [0003] Although carfilzomib has a good anti-tumor effect, its water solubility is poor, its stability in water is not good, and it is easy to produce impurities. Therefore, the freeze-dried preparation is an ideal dosage form. Moreover, carfilzomib N-oxide is prone to be produced under the conditions of contact with oxygen, so it is necessary to isolate the oxygen during the preparation process. The Kyprolis prescription cu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K38/08A61K47/14A61K47/26A61K47/02A61P35/00
CPCA61K9/0019A61K9/19A61K38/08A61K47/02A61K47/14A61K47/26
Inventor 单衍强庞文李斌王德耿刘敏
Owner QILU PHARMA HAINAN
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