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Polyethylene glycol modified human interleukin-2, preparation method and application thereof

A technology of polyethylene glycol and human interleukin, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve problems such as loss of biological activity of drugs

Inactive Publication Date: 2009-11-25
BEIJING SL PHARMA
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  • Summary
  • Abstract
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  • Claims
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Problems solved by technology

Existing studies have proved that the action time of modified protein drugs in vivo is proportional to the number and relative molecular weight of coupled PEG, and the biological activity in vitro is inversely proportional to the number and relative molecular weight of coupled PEG. Modifying protein drugs will cause the drug to lose most of its biological activity

Method used

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  • Polyethylene glycol modified human interleukin-2, preparation method and application thereof
  • Polyethylene glycol modified human interleukin-2, preparation method and application thereof

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Embodiment 1

[0022] 100mg pure growth hormone, dissolved in 20ml 20mMPH6.0PB, added 400mg Y-PEG-NHS ester, reacted at 25°C for 6h, added 2M glycine to terminate the reaction. The reaction mixture was separated by S-300, detected at 250nm, and the samples were collected in sections to separate the multi-modified substance from the single-modified substance and unmodified growth hormone.

[0023] 7.5% reduced SDS-PAGE detection, the purity is greater than 95%. According to the Chinese Pharmacopoeia in 2005, the activity was reduced by 60%.

[0024] Antibody serum was collected from the immunized animals, and the antibody titer of the immune serum was determined. The results showed that the antibody titer of the modified interleukin-2 decreased, indicating that the immunogenicity of the modified interleukin-2 was reduced.

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Abstract

The invention provides polyethylene glycol modified human interleukin-2 so as to improve the physical and chemical property and the biological activity of interleukin-2 self, in particular Y-type polyethylene glycol NHS ester modified interleukin-2. Compared with the prior art, the Y-type polyethylene glycol NHS ester modified interleukin-2 is similar to polyethylene glycol NHS used in PEGasys in structure and performance, but has better chemical stability. The invention preferably selects the Y-type polyethylene glycol with gross molecular weight of 40kDa to improve the molecular weight, thereby reducing glomerular filtration rate, and improving medicament half life; and adopted branched polyethylene glycol can increase steric hindrance of protein medicinal molecules, thereby significantly reducing the immunogenicity of protein molecules.

Description

technical field [0001] The invention relates to a polyethylene glycol modification of protein medicine, in particular to a modification of interleukin-2 by using branched polyethylene glycol. Background technique [0002] Polyethylene glycol is a neutral, non-toxic high molecular polymer with unique physical and chemical properties and good biocompatibility. It is also one of the very few synthetic polymers approved by the FDA that can be used as internal injection medicine. Polyethylene glycol or PEG is highly hydrophilic, has a large hydrodynamic volume in aqueous solution, and is not immunogenic. When coupled to drug molecules or drug surfaces, it can endow the modified drug molecules with excellent properties, change their biodistribution behavior and solubility in aqueous solution, create a space barrier around the modified drug, and reduce the enzyme activity of the drug. solution, avoiding rapid elimination in the metabolism of the kidneys, and allowing the drug to b...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K38/20A61P1/16A61P31/20A61K47/60
Inventor 徐明波王俊玲张鹏杨仲璠连治国吴彦卓
Owner BEIJING SL PHARMA
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