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Biocompatible block copolymer, use thereof, and production method thereof

A block copolymer, a technology of biocompatibility, applied in the field of biocompatible block copolymer, its use and manufacture, which can solve the problem of insufficient bioavailability of hydrophobic drugs, disappearance of cytokines, and insufficient drug delivery And other issues

Inactive Publication Date: 2008-12-24
TOKYO CRO INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example: (1) The drug is poorly soluble in body fluids; (2) The drug is unstable under enzyme, pH, and other physiological conditions; (3) The drug cannot pass through membrane barriers such as endothelium and mucous membrane; (4) The drug causes undesirable effects. (5) The drug disappears and excreted rapidly in the blood; (6) The drug lacks the ability to target the target site, etc.
[0003] As a result of the above reasons, the following problems can be exemplified: (1) Difficulty in preparing injections; (2) Difficulty in oral administration of protein drugs; (3) Insufficient delivery of drugs to cancer tissues or brain and nerve tissues; (4) Insufficient mucosal absorption of hydrophilic drugs; (5) Insufficient bioavailability of hydrophobic drugs; (6) Premature disappearance of cytokines in the blood; (7) Lack of transferability to target sites Wait
[0012] However, the above-mentioned International Publication No. 2005 / 003214 pamphlet is also silent about biocompatible block copolymers having a hydrophobic segment formed of amino acid and hydroxycarboxylic acid and a hydrophilic segment formed of polyalkylene oxide. Records of substances and the formation of micelles, microparticles, and complexes based on them

Method used

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Examples

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Embodiment

[0090] The present invention will be described in more detail by giving reference examples and examples below, but they do not limit the present invention.

reference example 1

[0092] Synthesis of Aminoacyl Polyethylene Glycol

[0093] 200 g (0.05 mole) of polyethylene glycol (HO-PEG) with an average molecular weight of 4,000 4000 -OH) was dissolved in 400 mL of acetonitrile. To this solution was added 55 g (0.15 mol) of tert-butoxycarbonyl-L-phenylalanine-N-hydroxysuccinimide ester (Boc-Phe-ONSu) and 2.65 g (0.015 mol) of 4-dimethylamino pyridine, stirred at room temperature for two days. After the reaction, the solvent was distilled off under reduced pressure, and the residue was dissolved in 600 mL of dichloromethane, and washed with 10% aqueous citric acid, saturated aqueous sodium bicarbonate, and saturated brine. The solution was dried over anhydrous sodium sulfate, the solution was concentrated, and ether was added to the residue to precipitate crystals. The obtained crude product was dissolved in acetonitrile, filtered with a 450 nm membrane filter, and the filtrate was concentrated under reduced pressure. Ether was added to the residue t...

reference example 2

[0095] Introduction of tert-butoxycarbonyl-L-leucine into aminoacyl polyethylene glycol

[0096] Dissolve 38.9g (0.01 mol) of the above-mentioned polyethylene glycol-L-phenylalanine ester hydrochloride in 300mL of acetonitrile (ACN)-tetrahydrofuran (THF) 1:1 mixed solvent, add 1.15mL (0.0105 mol) of N -Methylmorpholine (NMM), to which was added 4.92 g (0.015 mol) of tert-butoxycarbonyl-L-leucine-N-hydroxysuccinimide ester (Boc-Leu-ONSu) and stirred at room temperature one night. After the reaction, the solution was concentrated under reduced pressure, and the residue was dissolved in dichloromethane. The solution was washed with 10% aqueous sodium bicarbonate solution, saturated aqueous solution of citric acid, and water, and dried over anhydrous sodium sulfate. The solution was concentrated under reduced pressure, and ether was added to the residue to precipitate crystals.

[0097] The resulting Boc-Leu-Phe-O-PEG 4000 -OH was dissolved in THF and ether was added for recrys...

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Abstract

Disclosed is a biocompatible block copolymer having a hydrophobic segment composed of an amino acid and a hydroxycarboxylic acid, and a hydrophilic segment composed of a polyalkylene oxide. In this biocompatible block copolymer, one end of the hydrophobic segment, which is not bound with the hydrophilic segment, is composed of an amino acid unit.

Description

technical field [0001] The present invention relates to a biocompatible block copolymer having a hydrophobic segment formed of amino acid and hydroxycarboxylic acid and a hydrophilic segment formed of polyalkylene oxide, comprising the biocompatible block copolymer and Micelles, microparticles or complexes of medicines and their uses, pharmaceutical compositions containing them and methods for their manufacture. The micelles, microparticles or complexes can realize drug solubilization, dispersion, stabilization, sustained release, delivery to lesion sites and the like. Background technique [0002] Drugs exert their effects by reaching the site of drug action in the body. There are several reasons why a drug cannot reach its site of action. For example: (1) The drug is poorly soluble in body fluids; (2) The drug is unstable under enzyme, pH, and other physiological conditions; (3) The drug cannot pass through membrane barriers such as endothelium and mucous membrane; (4) T...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/00A61K9/08A61K9/10A61K9/127A61K9/50A61K47/34
CPCA61K9/1075A61L27/18A61L27/54A61L2300/252A61L2300/41A61L2300/414A61L2300/604C08G81/00C08L53/00A61P29/00A61P43/00C08L77/04C08L71/02C08L2666/02C08G65/48A61K9/08A61K47/34
Inventor 片贝良一小滨一弘铃木嘉树
Owner TOKYO CRO INC
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