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TPGS-b-(PCL-ran-PGA) copolymer and preparation method and application thereof

A technology of copolymer, tpgs-b-, which is applied in the fields of pharmaceutical formulations, medical preparations of non-active ingredients, medical science, etc., can solve the problems of slow degradation rate, poor hydrophilicity, and influence on the application range, and achieve simple preparation, The effect of good biocompatibility

Inactive Publication Date: 2012-10-10
SHENZHEN NANO MED BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, linear PCL has high crystallinity, poor hydrophilicity, and slow degradation rate, which affects its application range.

Method used

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  • TPGS-b-(PCL-ran-PGA) copolymer and preparation method and application thereof
  • TPGS-b-(PCL-ran-PGA) copolymer and preparation method and application thereof
  • TPGS-b-(PCL-ran-PGA) copolymer and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] The preparation method of TPGS-b-(PCL-ran-PGA) copolymer includes the following steps:

[0043] Take 95% ε caprolactone monomer, 2% glycolide monomer and 3% polyethylene glycol 1000 vitamin E succinate as raw materials according to the mass percentage content, put them into the polymerization tube, and add the raw material quality 0.5 % Tetramethyldibutylguanidine Acetate, evacuated, filled with nitrogen, sealed the polymer tube, heated at 145°C, reacted for 16 hours, and then obtained TPGS-b-(PCL-ran-PGA) copolymer with a molecular weight of 46000 (I) and (II) where: n=21 caprolactone fragment (A+B+...)=379 glycolide fragment (a+b+...)=23. figure 2 Shown is the synthesis reaction formula of TPGS-b-(PCL-ran-PGA) copolymer. TPGS acts as an initiator.

[0044] image 3 It is the Fourier transform infrared spectrum of TPGS-b-(PCL-ran-PGA) copolymer and TPGS. The carbonyl peak of TPGS is at 1739cm -1 In the TPGS-b-(PCL-ran-PGA) copolymer, the carbonyl peak of TPGS moves to 17...

Embodiment 2

[0046] The preparation method of TPGS-b-(PCL-ran-PGA) copolymer includes the following steps:

[0047] Take 58% of ε-caprolactone monomer, 2% of glycolide monomer and 40% of polyethylene glycol 1000 vitamin E succinate as raw materials according to the mass percentage content, and put the raw material into the polymerization tube. Of 1% zinc powder, evacuated, filled with nitrogen, sealed the polymer tube, heated at 145°C and reacted for 12 hours to obtain a TPGS-b-(PCL-ran-PGA) copolymer (Ⅰ) and a molecular weight of 4200 (II).

[0048] The crude TPGS-b-(PCL-ran-PGA) copolymer (I) and (II) were dissolved in dichloromethane, methanol was added to precipitate the TPGS-b-(PCL-ran-PGA) copolymer, filtered, and The precipitate was dried under vacuum at 50°C to obtain TPGS-b-(PCL-ran-PGA) copolymers (I) and (II) with a molecular weight of 4200, in which: n=23 caprolactone fragments (A+B+……) = 21 glycolide fragment (a+b+...)=2.

Embodiment 3

[0050] The preparation method of TPGS-b-(PCL-ran-PGA) copolymer includes the following steps:

[0051] Take 95% epsilon caprolactone monomer, 2% glycolide monomer and 3% polyethylene glycol 1000 vitamin E succinate as raw materials according to the mass percentage content and put them into the polymerization tube. 0.2% of ethanol iron, evacuated, filled with nitrogen, heated at 150°C in a closed polymerization equipment, and reacted for 12 hours to obtain a TPGS-b-(PCL-ran-PGA) copolymer (Ⅰ) with a molecular weight of 51000 And (Ⅱ).

[0052] Dissolve the crude TPGS-b-(PCL-ran-PGA) copolymer (I) and (II) in ethyl acetate, add petroleum ether to precipitate the TPGS-b-(PCL-ran-PGA) copolymer, and filter. The precipitate was dried in vacuum at 30°C to obtain TPGS-b-(PCL-ran-PGA) copolymers (I) and (II) with a molecular weight of 51000, in which: n=23 caprolactone fragments (A+B+... )=420 glycolide fragment (a+b+...)=26.

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Abstract

The invention discloses a TPGS-b-(PCL-ran-PGA) copolymer as well as a preparation method and application thereof. The copolymer has the following structure as shown in the specification. The TPGS-b-(PCL-ran-PGA) copolymer has the advantages of good biocompatibility, biodegradability, simple preparation and no pollution and is applied to the fields of pharmaceutical preparations and tissue engineering.

Description

Technical field [0001] The invention belongs to the technical field of biological materials, and particularly relates to a TPGS-b-(PCL-ran-PGA) copolymer and a preparation method and application thereof. Background technique [0002] Pharmaceutical excipients are the main material basis for the development of pharmaceutical preparations. Without the research, development and application of new excipients, it is impossible to vigorously develop new drug release system preparations. Polyε-caprolactone (PCL, Polycaprolactone) is a pharmaceutical excipient approved by the US FDA, which has excellent drug permeability, excellent biodegradability and biocompatibility. However, linear PCL has high crystallinity, poor hydrophilicity, and slow degradation rate, which affects its application range. Therefore, it is necessary to reduce the crystallinity of PCL and improve its hydrophilic properties through structural changes and the introduction of hydrophilic segments to make it a more ef...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G63/664C08G65/48A61K47/34A61L27/18A61L17/00A61L31/06
Inventor 梅林张明明
Owner SHENZHEN NANO MED BIOTECH