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PEG site-modified asparaginase injection

A technology of asparaginase injection and asparaginase, which is applied in the field of injection of polyethylene glycol N-terminal fixed-point modification of asparaginase, to achieve the effects of stable blood drug concentration, uniform modified product and good therapeutic effect

Active Publication Date: 2020-12-22
ZONHON BIOPHARMA INST +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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At present, there is no report and research on related products at home and abroad

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  • PEG site-modified asparaginase injection
  • PEG site-modified asparaginase injection
  • PEG site-modified asparaginase injection

Examples

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Embodiment 1

[0055] Example 1: Preparation and analysis of pegylated asparaginase with N-terminal site-directed modification

preparation example 1

[0056] Preparation Example 1, the pegylated asparaginase with N-terminal site-specific modification of the present invention is prepared, purified and identified by the following methods:

[0057] 1. Preparation of pegylated asparaginase with N-terminal site-directed modification

[0058] Dissolve L-asparaginase (from Changzhou Qianhong Biochemical Pharmaceutical Co., Ltd.) with 40mM acetic acid-sodium acetate buffer solution of pH5.0 to prepare a 20mg / mL solution, and PEG uses Y-PALD-40K (purchased from Beijing Jiankai Technology Co., Ltd.), according to the molar ratio of asparaginase:PEG:sodium cyanoborohydride of 1:4:200, reacted at 4°C for 12h, and then added 1M glycine to terminate the reaction. The monomodified product Y-PALD-40K-ASP (Mono) and the dimodified product Y-PALD-40K-ASP (Di) were prepared.

[0059] 2. Purification of pegylated asparaginase with N-terminal site-directed modification

[0060] Chromatography conditions: Q ion exchange column (purchased from G...

preparation example 2

[0074] The activity and purity of the monomodified and dimodified products prepared in Preparation Example 2 were not significantly different from the monomodified and dimodified products obtained in Preparation Example 1. Y-PALD-30K-ASP (Mono) and Y-PALD- The purity of 30K-ASP(Di) was higher than 98%.

[0075] Depend on Figure 2a , 2b It can be seen that the modified product Y-PALD-40K-ASP (Mono) and Y-PALD-40K-ASP (Di), Y-PALD-30K-ASP (Mono) and Y-PALD-30K-ASP (Di) Electrophoretic bands are very uniform. Compared with the similar product on the domestic market—pegaspargase (purchased from Jiangsu Hengrui Medicine Co., Ltd.), the uniformity has been greatly improved.

[0076] Figure 2aThe 3rd and 4th lanes show two uniform bands, and the molecular weight corresponding to the first band in the 3rd and 4th lanes is about 200KDa, because PEG molecules will bind a large amount of water molecules in the solution, making Its apparent molecular weight is about 4 times its theor...

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Abstract

The invention relates to a pegylated asparaginase injection realizing site-directed N-terminal modification and a preparation method of the pegylated asparaginase injection. The main ingredient of theinjection is pegylated asparaginase realizing site-directed N-terminal modification, and the injection also contains buffer salt, a protein stabilizer and water, wherein the protein stabilizer is sorbitol. For the pegylated asparaginase injection realizing site-directed N-terminal modification, the stability of asparaginase can be effectively improved, the adverse reaction during the medication process can be reduced, meanwhile, the medication period can be prolonged, the administration times can be reduced, and the pain caused to patients by injection administration can be reduced.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to an injection for modifying asparaginase at the N-terminus of polyethylene glycol. 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, which is more common in Asia and Latin America, and the incidence rate in my country is relatively high. According to the tumor site, NK / T-cell lymphoma can be divided into nasal NK / T-cell lymphoma and non-nasal NK / T-cell lymphoma. In addition, asparaginase is also used in the trea...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/60A61K38/50A61K9/08A61K47/26A61P35/00
CPCA61K9/0019A61K9/08A61K38/50A61K47/26
Inventor 马永王俊
Owner ZONHON BIOPHARMA INST
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