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A kind of ternary block copolymer and its preparation method and eye drops made from it

A ternary block and copolymer technology, applied in the fields of polymer chemistry and biomedical engineering, can solve the problems of limiting drug permeability and achieve the effect of prolonging residence time and high corneal permeability

Active Publication Date: 2017-08-04
河南省眼科研究所
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the special physiological structure and biochemical characteristics of the cornea limit the permeability of drugs

Method used

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  • A kind of ternary block copolymer and its preparation method and eye drops made from it
  • A kind of ternary block copolymer and its preparation method and eye drops made from it
  • A kind of ternary block copolymer and its preparation method and eye drops made from it

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Embodiment 1

[0033] The synthesis of embodiment 1 ternary block copolymer

[0034] Ternary block copolymer, the molecular formula is: PEG-PCL-PEI, and the structural formula is:

[0035] .

[0036] Synthetic steps:

[0037] S1. Synthesis of PEG-PCL-OH: First, put 10.0g PEG-OH (MW: 2000) and 20.6g ε-caprolactone into a flask, and dry under reduced pressure at 70°C for 2h; Add ε-caprolactone 0.1mol% Sn(Oct) in the flask 2 , then seal the flask and immerse it in an oil bath, conduct ring-opening polymerization at 115°C for 24 hours; separate the reaction solution, dissolve the solid in THF, add diethyl ether to precipitate twice for purification, collect the precipitate, and dry it in vacuum at 40°C to obtain PEG- PCL-OH, yield: >96%;

[0038] S2. Synthesis of PEG-PCL-COOH: 1mmol PEG-PCL-OH and 10mmol maleic anhydride were dissolved in 100ml of pre-dried chloroform, placed in a two-necked flask equipped with a magnetic stirring bar and a reflux condenser, and the mixture was Under an ...

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Abstract

The invention belongs to the technical fields of polymer chemistry and biochemical engineering and concretely relates to a tri-block copolymer, a preparation method thereof and an eye drop prepared from the tri-block copolymer. The tri-block copolymer has the molecular formula as follows: PEG-PCL-PEI. The preparation method comprises the steps of firstly, synthesizing PEG-PCL-OH; then, synthesizing PEG-PCL-COOH; and finally, synthesizing PEG-PCL-PEI. The tri-block copolymer disclosed by the invention can be self-assembled to form a micelle system, and furthermore, the eye drop is prepared, so that the cornea barrier is overcome to deliver a drug, the cornea permeability is relatively high, and the standing time of the drug on eyes is prolonged.

Description

technical field [0001] The invention belongs to the technical field of macromolecule chemistry and biomedical engineering, and in particular relates to a ternary block copolymer, a preparation method thereof and an eye drop prepared by using the same. Background technique [0002] Due to its ease of use, low invasiveness and simple formulation, topical eye drops are the preferred method of ophthalmic drug delivery, especially in the treatment of diseases related to the cornea, ocular surface and anterior segment. However, the special physiological structure and biochemical characteristics of the cornea limit the permeability of drugs. In addition, eye-specific defense mechanisms after topical administration, such as lacrimation, tear dilution, and tear replacement can reduce the residence time of the drug solution in the anterior corneal region to 5–6 minutes, and only 1–3% of the drug solution can penetrate into the cornea and into the tissues of the eye. [0003] The mai...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34C08G81/00C08G63/08C08G63/91C08G65/48C08G73/04A61K9/10A61P27/02
Inventor 李景果张俊杰王丽娅周天洋夏慧芸何继军李恒栗占荣贺司宇
Owner 河南省眼科研究所
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