Freeze-dried composition containing bortezomib and preparation method of freeze-dried composition

A technology of bortezomib and composition, which is applied in the field of bortezomib-containing freeze-dried composition and its preparation, which can solve the problems of oxygen environment sensitivity and difficulty in dissolving the main drug, so as to improve the stability of the preparation and shorten the preparation time , the effect of avoiding contact

Active Publication Date: 2013-05-01
JIANGSU AOSAIKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] The purpose of the present invention is to overcome the difficulty of dissolving th

Method used

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  • Freeze-dried composition containing bortezomib and preparation method of freeze-dried composition
  • Freeze-dried composition containing bortezomib and preparation method of freeze-dried composition
  • Freeze-dried composition containing bortezomib and preparation method of freeze-dried composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] prescription:

[0063] Bortezomib 50mg Mannitol 1000mg tert-butanol 5g Water for Injection Dilute to 100ml

[0064] Preparation process: Heat tert-butanol to 26°C to make it melt into a liquid state, weigh 5g of tert-butanol, add water for injection to 50% of the total volume of the solution, mix well, fill with nitrogen for 0.5 hours; weigh 1000mg Add mannitol to the mixed solution, and stir until the mannitol is completely dissolved at 60°C to obtain an excipient solution; weigh 50 mg of bortezomib and add it to the excipient solution, stir until completely dissolved at 60°C, and add water for injection To the total volume of the preparation, the preparation intermediate solution is obtained, and the preparation process is filled with nitrogen for protection; after the preparation intermediate solution is qualified, it is filtered, filled according to the volume of 1ml, and sent to a freeze dryer for freeze-drying to obtain a freeze-...

Embodiment 2

[0068] prescription:

[0069] Bortezomib 500mg Mannitol 2500mg tert-butanol 50g Water for Injection Dilute to 100ml

[0070] Preparation process: Heat tert-butanol to 50°C to make it melt into a liquid state, weigh 50g of tert-butanol, add water for injection to 95% of the total volume of the solution, mix well, fill with nitrogen for 2 hours; weigh 2500mg Add mannitol to the mixed solution, and stir until the mannitol is completely dissolved at 50°C to obtain an excipient solution; weigh 500 mg of bortezomib and add it to the excipient solution, stir until completely dissolved at 50°C, and add water for injection To the total volume of the preparation, the preparation intermediate solution is obtained, and the preparation process is filled with nitrogen for protection; after the preparation intermediate solution is qualified, it is filtered, filled according to the volume of 1ml, and sent to a freeze dryer for freeze-drying to obtain a freez...

Embodiment 3

[0075] prescription:

[0076] Bortezomib 175mg Mannitol 1750mg tert-butanol 40g Water for Injection Dilute to 100ml

[0077] Preparation process: Heat tert-butanol to 40°C to make it melt into a liquid state, weigh 40g of tert-butanol, add water for injection to 90% of the total volume of the solution, mix well, and fill with nitrogen for 1 hour; weigh 1750mg Add mannitol to the mixed solution, and stir until the mannitol is completely dissolved at 40°C to obtain an excipient solution; weigh 175 mg of bortezomib and add it to the excipient solution, stir until completely dissolved at 40°C, and add water for injection To the total volume of the preparation, the preparation intermediate solution is obtained, and the preparation process is filled with nitrogen for protection; after the preparation intermediate solution is qualified, it is filtered, filled according to the volume of 2ml, and sent to a freeze dryer for freeze-drying to obtain a fr...

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PUM

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Abstract

The invention belongs to the technical field of medicine, in particular to the field of chemical pharmacy, and particularly relates to a freeze-dried composition containing bortezomib and a preparation method of the freeze-dried composition. The freeze-dried composition and the preparation method aim at overcoming main medicine dissolution difficulty and oxygen environment sensitivity in an environment. A mixed solvent comprising mannitol and tert butyl alcohol is used, so that a dissolution rate of bortezomib is increased significantly, and the dissolution rate of bortezomib can be increased further through an addition sequence of materials. A nitrogen filled environment is used, so that liquid preparation time is shortened greatly, the contact of main medicine components with an aerobic environment is avoided effectively, and contents of relevant substances and total impurities in a final finished product are reduced.

Description

[0001] technical field [0002] The invention belongs to the technical field of medicine, in particular to the field of chemical pharmacy, and more specifically relates to a bortezomib-containing freeze-dried composition and a preparation method thereof. [0003] Background technique [0004] Bortezomib is a proteasome inhibitor, the structure of which is shown in Formula I. Bortezomib can specifically inhibit the chymotrypsin-like activity of 26S proteasome in mammalian cells, affect a series of signaling in cells, and eventually lead to the death of cancer cells. [0005] [0006] Bortezomib is a dipeptide boronic acid derivative formed from leucine and phenylalanine, which can exist in the form of a trimer shown in formula II. In the pH range of 2~6.5, the solubility of bortezomib in water is 3.3~3.8mg / ml. [0007] [0008] in: [0009] [0010] Bortezomib (bortezomib) is a dipeptidyl boronic acid compound, which has a highly efficient and specific protease i...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K38/05A61K31/69A61K47/26A61P35/00
Inventor 陈庆财宗在伟贾元超
Owner JIANGSU AOSAIKANG PHARMA CO LTD
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