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Pharmaceutical composition containing PEGylated asparaginase and preparation method thereof

An asparaginase and pegylation technology, which is used in drug combinations, medical preparations containing active ingredients, drug delivery, etc., can solve the problems of short validity period, unexpected temperature fluctuations, and high transportation costs, and achieves extended validity period, Not easy to fall off, strong binding effect

Active Publication Date: 2016-07-27
ZONHON BIOPHARMA INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The pharmaceutical dosage forms of PEGylated asparaginase listed at home and abroad are all liquid injections. Liquid injections are sometimes accidentally frozen, and rethawing after freezing will cause PEGylated asparaginase to degrade and reduce activity.
In addition, these liquid preparations need to be stored at 2-8°C, and the validity period is 18 months. They have the following disadvantages: one, the storage conditions of the liquid are high, and special cold storage is required.
2. The transportation cost is high, and liquid injections need the same temperature conditions during transportation, so cold chain transportation is required
3. The quality risk is high. Unexpected fluctuations in temperature during storage and transportation have the risk of causing changes in product quality.
4. The validity period is short, which is not conducive to production and sales
At present, there is no relevant research report on the freeze-dried powder injection of pegylated asparaginase
And the inventor also tried to prepare the freeze-dried powder preparation of pegylated asparaginase with the existing asparaginase freeze-dried powder formulation, but found that the situation of obvious degradation and activity reduction

Method used

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  • Pharmaceutical composition containing PEGylated asparaginase and preparation method thereof
  • Pharmaceutical composition containing PEGylated asparaginase and preparation method thereof
  • Pharmaceutical composition containing PEGylated asparaginase and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] Example 1 Pegylated asparaginase prescription for injection (both in mass percent) and its preparation process

preparation example 1

[0072]

[0073]

[0074] Preparation Process:

[0075] Solution preparation: Prepare a 50mM phosphate buffer solution containing 5% sorbitol, check the pH value at 6.0-8.0 and cool down to below 25°C, dilute pegylated asparaginase with the buffer solution prepared above, and detect the intermediate . The medicinal liquid is sterilized and filtered through a 0.2um microporous filter, filled with a plug and capped, and the water needle is obtained. If it is to be made into freeze-dried powder injection, after filling, half-tighten the stopper, put it into a freeze-drying box, and carry out the freeze-drying process.

[0076] Freeze drying process:

[0077] Pre-freezing stage: Pre-freezing adopts full-speed cooling of the plate layer, and the product temperature drops to -60°C, and keeps for 3 hours to completely freeze the sample.

[0078] Sublimation stage: turn on the vacuum pump, pre-evacuate to 0.40mbar, start sublimation, heat the separator at a rate of 15°C per ho...

preparation example 2

[0081]

[0082] Preparation Process:

[0083] Solution preparation: prepare a phosphate buffer solution containing 3% sorbitol 100mM, check the pH value at 6.0-8.0 and cool down to below 25°C, dilute pegylated asparaginase with the buffer solution prepared above, and detect the intermediate . The medicinal liquid is sterilized and filtered through a 0.2um microporous filter, filled with a plug and capped, and the water needle is obtained. If it is to be made into freeze-dried powder injection, after filling, half-tighten the stopper, put it into a freeze-drying box, and carry out the freeze-drying process.

[0084] Freeze drying process:

[0085]Pre-freezing stage: Pre-freezing adopts full-speed cooling of the plate layer, and the product temperature drops to -60°C, and keeps for 3 hours to completely freeze the sample.

[0086] Sublimation stage: turn on the vacuum pump, pre-evacuate to 0.40mbar, start sublimation, heat the separator at a rate of 20°C per hour, control ...

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Abstract

The invention relates to a pharmaceutical composition containing PEGylated asparaginase. The composition comprises PEGylated asparaginase, sorbitol, a protective agent, a buffering agent and a surfactant; the protective agent is selected from mannitol, sucrose or lactose; and the buffering agent is selected from phosphate or Tris-HCl. The pharmaceutical composition containing PEGylated L-asparaginase is advantageous in that: after refrigeration, samples are not easy to degrade.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a pharmaceutical composition of pegylated asparaginase for injection and a preparation method thereof. Background technique [0002] Asparaginase (ASP), also known as L-asparaginase or L-asparaginase, is an enzyme that catalyzes the hydrolysis of asparagine into aspartic acid. Asparaginase is effective in the treatment of acute lymphoblastic leukemia (ALL) in children or adults. In recent years, drugs containing asparaginase have been used in combination with chemotherapy to treat NK / T cell lymphoma, and achieved good therapeutic effect. NK / T cell lymphoma is a special type of non-Hodgkin's lymphoma in China. It is more common in Asia and Latin America, and the incidence rate in my country is relatively high. NK / T-cell lymphoma can be divided into nasal NK / T-cell lymphoma and non-nasal NK / T-cell lymphoma according to tumorigenesis division. In addition, asp...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K9/08A61K38/50A61K47/48A61K47/10A61P35/02A61P35/00
Inventor 马永王俊邓建华徐春林陈一飞王耀方
Owner ZONHON BIOPHARMA INST
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