Artificial tear with long ocular surface retention and preparation method thereof

A technology of artificial tears and ocular surface, which is applied in the direction of medical formula, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve the problem of high production cost of hybrid molecules

Active Publication Date: 2021-01-12
THE EYE HOSPITAL OF WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above studies have proved that sialic acid on the ocular surface can be used as an anchoring target to prolong the residence time of artificial tears on the ocular surface, but the strategy of achieving polymer lubricant anchoring through bifunctional hybrid molecules has two drawbacks: 1. Polymer lubricants design specific binding peptides; 2. The production cost of hybrid molecules is relatively high

Method used

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  • Artificial tear with long ocular surface retention and preparation method thereof
  • Artificial tear with long ocular surface retention and preparation method thereof
  • Artificial tear with long ocular surface retention and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment

[0034] (1) Weigh 1g NH 2 -PEG2K-COOH, dissolved in 10mL DMF; add 1.0 equivalent of fluorescein isothiocyanate and appropriate amount of triethylamine; react at room temperature for 6h; concentrate under reduced pressure, precipitate with ice ether, repeat washing 3 times; the product is vacuum-dried;

[0035] (2) Take 1g of the product (1) and dissolve it in 10mL DMF; add 1.5 equivalents of 5-amino-2-(hydroxymethyl)phenylboronic acid cyclomonoester, Ethylcarbodiimide (EDC) and 1.0 equivalent of 4-dimethylaminopyridine (DMAP); react overnight at room temperature; concentrate under reduced pressure, precipitate with glacial ether, and repeat washing 3 times; the product is vacuum-dried.

[0036] Carry out NMR verification, corneal epithelial cell / conjunctival epithelial cell binding force evaluation, isolated cornea / conjunctival binding force evaluation and cytocompatibility evaluation on the products of the examples:

[0037] (1) NMR structure verification of FITC-PEG-PBA: The...

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Abstract

The invention discloses an artificial tear with long ocular surface retention and a preparation method thereof. Active ingredients of the artificial tear are modified by phenylboronic acid, so that the modified artificial tear has the capability of combining ocular surface epithelial cells and ex-vitro tissues. A universal and cheap strategy is provided for constructing the artificial tear with long ocular surface retention, thereby being beneficial to large-scale preparation of the artificial tear with long ocular surface retention property.

Description

technical field [0001] The invention relates to the technical field of ophthalmic pharmaceutical preparations, in particular to artificial tears with prolonged ocular surface retention and a preparation method thereof. Background technique [0002] Dry eye is a common ocular surface disease, with an incidence ranging from 5-30% depending on the region and race. Its symptoms mainly include eye fatigue, gritty feeling, dryness, itching, redness, pain, blurred vision, etc., which seriously affect the quality of life and work efficiency. With the increase in the intensity of eye use in modern life and the continuous increase in life expectancy, the disease burden of dry eye will increase year by year. [0003] Artificial tears are a kind of ocular surface lubricant, which can relieve dry eye symptoms and clinical detection indicators at the same time. It is the first-line therapy for dry eye and is suitable for 80% of the diagnosed population. Due to the function of the ocular...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/54A61K31/765A61P27/04
CPCA61K47/54A61K31/765A61P27/04
Inventor 南开辉王静洁龚赞王天佐管彬
Owner THE EYE HOSPITAL OF WENZHOU MEDICAL UNIV
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