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Carrier for improving bioavailability of proteins and water solubility of insoluble drugs and preparation method

A technology for insoluble drugs and high availability, which is applied in the fields of peptide/protein components, biochemical equipment and methods, drug combinations, etc., can solve the problems of low protein bioavailability, poor water solubility of hydrophobic drugs, etc., and improve protein bioavailability , Reduce economic burden, reduce the effect of injection frequency

Inactive Publication Date: 2017-07-14
吉林省纳博奥生物科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] The present invention provides a carrier for improving protein bioavailability and water solubility of insoluble drugs, so as to solve the existing problems of low protein bioavailability and poor water solubility of hydrophobic drugs

Method used

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  • Carrier for improving bioavailability of proteins and water solubility of insoluble drugs and preparation method
  • Carrier for improving bioavailability of proteins and water solubility of insoluble drugs and preparation method
  • Carrier for improving bioavailability of proteins and water solubility of insoluble drugs and preparation method

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Embodiment Construction

[0025] Obtained by the following steps:

[0026] (1) synthesis of polyethylene glycol-polybenzyl glutamate block copolymer PEG-b-PBLG;

[0027] (2) Synthesis of PEG-b-PELG ammonolysis product PEG-b-PELG;

[0028] (3) Synthesis of linear polyethylene glycol-brush polybenzyloxycarbonyl lysine block copolymer PEG-b-(PELG-g-PZLL);

[0029] (4) Synthesis of linear polyethylene glycol-brush polybenzyloxycarbonyllysine and polylysine block copolymer PEG-b-(PELG-g-(PZLL-r-PLL));

[0030] Described step (1) comprises the following steps:

[0031]1.1 Preparation of glutamic acid anhydride and lysine anhydride: the preparation of glutamic acid anhydride: add 150-200mL ethyl acetate to a three-necked flask equipped with 6g BLG and 0.09g activated carbon, 40-50℃ oil bath, wait for acetic acid Add 1.32-1.40g of dried triphosgene after reflux of ethyl ester, add 0.16-0.21g of dried triphosgene after 1 hour, the white BLG solid in the reaction system disappears after 2 hours, and the react...

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Abstract

The invention relates to a carrier for improving bioavailability of proteins and water solubility of insoluble drugs and a preparation method and belongs to a carrier for constructing combined loading of a protein drug and a lyophobic drug and a preparation method. The preparation method comprises synthesis of a polyethylene glycol-poly benzyl l-glutamate block copolymer, synthesis of an ammonia product, synthesis of a linear polyethylene glycol-brushed polycarbobenzoxy lysine block copolymer and synthesis of a linear polyethylene glycol-brushed polycarbobenzoxy lysine and polylysine block copolymer. The carrier provided by the invention has the advantages that the problem of bioavailability of the protein drug and the water solubility of insoluble drugs is solved, so that various injections can be prepared; the carrier has the characteristics of improving the bioavailability of the protein drug, increasing the water solubility of the lyophobic drug, reducing the injection frequency, reducing the economical burden of a clinical patient and enhancing the drug effect.

Description

technical field [0001] The invention relates to a carrier and a preparation method for constructing a joint-loaded protein drug and a hydrophobic drug, in particular to a construction and a method for constructing a controlled-release system and a method for jointly loading a protein drug and a hydrophobic drug for anti-tumor. Background technique [0002] In recent years, polymer molecular brushes have shown broad application prospects in the field of biomedicine, such as drug carriers, gene carriers, protein carriers, and biosensing systems. Lumbrokinase is a kind of enzyme complex with antithrombotic, antioxidative, antitumor and immunomodulatory effects, which has been widely studied and used in clinical antitumor therapy. However, lumbrokinase has a short half-life in vivo, low bioavailability, and severe side effects, which greatly limit its clinical application. PEGylation can effectively increase the half-life of lumbrokinase, but the PEGylation reaction increases t...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K9/107C08G81/00C08G65/333A61P35/00A61K38/48A61K31/337
CPCA61K47/34A61K9/1075A61K31/337A61K38/484C08G65/33317C08G81/00C12Y304/21007A61K2300/00
Inventor 仝飞
Owner 吉林省纳博奥生物科技有限公司
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