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Active-targeting-type polymer derivative, composition containing polymer derivative, and uses of polymer derivative and composition

A technology of composition and molecular weight, applied in the directions of non-active ingredient medical preparations, microcapsules, capsule delivery, etc., can solve the problems of anti-tumor effect and reduction of side effects, undocumented side effect reduction effect, and untracked in vivo behavior of the composition.

Inactive Publication Date: 2019-04-16
NIPPON KAYAKU CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, detailed side effect reduction effects are not described, the in vivo behavior of the composition is not tracked, and the particle size is as large as about 100 nm in many examples, so it is considered that sufficient antitumor effects and side effects cannot be achieved depending on the type of cancer and the type of animal. reduce

Method used

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  • Active-targeting-type polymer derivative, composition containing polymer derivative, and uses of polymer derivative and composition
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  • Active-targeting-type polymer derivative, composition containing polymer derivative, and uses of polymer derivative and composition

Examples

Experimental program
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Effect test

Embodiment

[0316] Hereinafter, the present invention will be further described through examples. However, the present invention is not limited by these Examples.

[0317] The measurement of the volume-based particle diameter of the block copolymer (A) involved in Examples 1-1, 1-2, and 2 was carried out using a particle diameter and zeta potential measuring device Zetasizer Nano ZS manufactured by Malvern Corporation (measurement temperature: 25°C, Analysis mode: general (normal resolution), material RI: 1.59) was performed.

[0318] The volume-based particle size measurement sample was obtained by adding ultrapure water so that the concentration of the physiologically active substance-bound block copolymer was 1 mg / mL, and dissolving it by ultrasonic waves under ice cooling, and then using a 0.45 μm membrane filter. Filter to obtain a solution.

[0319] In addition, the measurement of the average particle diameter of the composition containing the block copolymer of Examples 3-10 and ...

Synthetic example 1

[0322] Synthesis of polyethylene glycol-polyglutamic acid block copolymer (polyethylene glycol molecular weight 10 kilodaltons, polyglutamic acid polymerization number 21.0)

[0323] After dissolving polyethylene glycol (SUNBRIGHT M141573, manufactured by NOF Corporation, average molecular weight 10 kDalton, 9.0 g) having a methoxy group at one end and a 3-aminopropyl group at one end in DMSO (180 mL), L-glutamic acid-γ-benzyl ester-N-carboxylic acid anhydride (5.7 g) was added, and stirred at 30° C. for 21.0 hours. The reaction solution was added dropwise to a mixed solution of diisopropyl ether (2880 mL) and ethanol (720 mL) over 0.5 hour, and stirred at room temperature for 1 hour. Thereafter, the supernatant was removed, a mixed solution of diisopropyl ether (1440 mL) and ethanol (360 mL) was added, and after stirring for 1 hour, the precipitate was collected by filtration and dried under reduced pressure to obtain a polymer (12.4 g).

[0324] The obtained polymer (12.0 g...

Synthetic example 2

[0328]Synthesis of Polyethylene Glycol-Polyglutamic Acid Block Copolymer (Polyethylene Glycol Molecular Weight 2,000 Daltons, Polyglutamic Acid Polymerization Number 7.9)

[0329] After dissolving polyethylene glycol (SUNBRIGHT M89506, manufactured by NOF Corporation, average molecular weight 2 kilodaltons, 14 g) with a methoxy group at one end and a 3-aminopropyl group at one end in DMSO (280 mL), add L-glutamic acid-γ-benzyl ester-N-carboxylic acid anhydride (16.8 g), stirred at 30°C for 22.5 hours. The reaction solution was added dropwise to a mixed solution of diisopropyl ether (5040 mL) and ethanol (560 mL) over 2.0 hours, and stirred at room temperature for 4.0 hours. Thereafter, the supernatant was removed, a mixed solution of diisopropyl ether (1800 mL) and ethanol (200 mL) was added and stirred, and the precipitate was collected by filtration and dried under reduced pressure to obtain a polymer (31.9 g).

[0330] The obtained polymer (30.0 g) was dissolved in DMF (33...

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Abstract

The present invention addresses the problem of providing a polymer-micelle-type DDS preparation which makes it possible to improve the transfer, permeability and retention of a pharmacologically active substance to and in an affected target tissue, such as a tumor tissue and an inflammation affected tissue, to improve the activity of the pharmacologically active substance, thereby exerting the pharmacologically active effect of the pharmacologically active substance efficiently. A block copolymer (A) comprising a hydrophilic polymer segment containing a polyethylene glycol chain and a hydrophobic polymer segment containing a polyamic acid chain having a hydrophobic substituent in a side chain thereof, wherein the hydrophilic polymer segment and the hydrophobic polymer segment are linked toeach other, a target binding site is bound to the hydrophilic polymer segment, and the molecular weight of a main chain polymer composed of the polyethylene glycol chain and the polyamic acid chain is 2 to 10 kilodaltons inclusive.

Description

technical field [0001] The present invention relates to an active targeting polymer derivative, a composition containing the polymer derivative, and a drug using the substance. The active targeting polymer derivative is a polymer derivative having a target binding site, and Has migration, permeability, and retention to disease target tissues, and / or has excretivity in the kidney and the like. Background technique [0002] Regarding pharmaceuticals, drug delivery systems (DDS) have been developed that control the pharmacokinetics of a physiologically active substance as an active ingredient and deliver it to a specific action site in a living body at a desired drug concentration-action time. Non-Patent Document 1 discloses a DDS preparation, which uses a block copolymer formed by linking polyethylene glycol segments and hydrophobic polymer segments containing polyamino acid chains as a drug delivery carrier. The block copolymer forms a polymer micelle with a polyethylene gly...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G69/40A61K9/51A61K47/34C08L77/00
CPCA61K47/34A61K9/51C08G69/40C08G69/10A61K47/555A61K47/595A61K9/1075C08L77/00
Inventor 栗原大福田刚川野裕辉山本启一朗
Owner NIPPON KAYAKU CO LTD
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