A kind of eye drop with macromolecule graft copolymer as carrier and preparation method thereof

A technology of graft copolymer and eye drops, which is applied in the fields of polymer chemistry, biomedical materials and pharmacy, can solve the problems of low utilization rate and poor corneal passage, reduce irritation, prolong residence time and increase therapeutic effect Effect

Active Publication Date: 2019-02-01
河南省眼科研究所
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to overcome the problems of low drug utilization rate and poor corneal permeability of existing eye drops, the object of the present invention is to provide an eye drop with a polymer graft copolymer as a carrier and a preparation method thereof

Method used

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  • A kind of eye drop with macromolecule graft copolymer as carrier and preparation method thereof
  • A kind of eye drop with macromolecule graft copolymer as carrier and preparation method thereof
  • A kind of eye drop with macromolecule graft copolymer as carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1--the synthesis of graft copolymer

[0028] High molecular graft copolymer, its molecular formula is: CS-g-CD.

[0029] The synthetic route is:

[0030]

[0031] Synthetic steps:

[0032] S1. Synthesis of CD-COOH: First, put 9.73 g α-CD and 7.2 g sodium hydroxide into a flask and dissolve with 30 mL distilled water; add 1.165 g sodium chloroacetate and react at 50°C for 5 h; then dissolve the system with hydrochloric acid Adjust the pH to 7, add excess methanol for precipitation, filter the precipitate, and dry it overnight at 40°C in a vacuum dryer to obtain a white powder CD-COOH, with a yield of > 96%;

[0033] S2. Synthesis of CS-g-CD: Dissolve 10 mmol CD-COOH and 11 mmol NHS in 50 mL of distilled water, place in a flask equipped with a magnetic stirring bar, place the flask in a water bath at 4°C, add 11 mmol EDC, React at 4°C for 2 h; slowly add the calculated amount of chitosan aqueous solution (CS containing -NH 2 The amount is 12~33 mmol), re...

Embodiment 2

[0037] Embodiment 2 ---the preparation of econazole

[0038] Add 100 grams of econazole nitrate to it, add 50 mL of water for injection, after dissolving, gradually add 1 mol / L sodium hydroxide solution to it, adjust the pH value of the solution to 11.0, centrifuge at high speed, discard the supernatant, and inject the lower precipitate After washing with water three times, white econazole powder was obtained after drying.

Embodiment 3--03

[0039] Embodiment 3--Preparation of 0.3 wt% econazole eye drops

[0040]First, take 70 grams of the graft copolymer CS-g-CD with a CD grafting rate of 79% in Example 1, add 800 mL of water for injection to it, stir and dissolve to a transparent solution; then, mix Econazole 3 in Example 2 Add 0.7 g of hydroxysuccinic acid and 0.7 g of hydroxysuccinic acid to the above solution, stir until completely dissolved; finally, add water for injection to make up to 1000 mL, and sterilize with circulating steam at 100 ° C to obtain Yiconazole Eye Drops. The whole solution was prepared at room temperature.

[0041] Existing literature reports that the solubility of econazole in water is 5 mg / L, which can be increased to 3 g / L in the present invention, and the solubility of econazole in water can be increased by 600 times by adopting the scheme of the present invention.

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Abstract

The invention belongs to the technical fields of high polymer chemistry, biomedical materials and pharmacy and particularly discloses eye drops with a polymer-grafted copolymer as a carrier and a preparation method of the eye drops. Each 1000mL of the eye drops are prepared from the following materials: 2g to 30g of eye drops medicament, 10g to 200g of polymer-grafted copolymer, 0.5g to 20g of hydroxysuccinic acid, and the balance of water for injection, wherein the polymer-grafted copolymer is chitosan-g-cyclodextrin. The preparation method comprises the following steps: firstly, weighing the chitosan-g-cyclodextrin serving as the polymer-grafted copolymer, adding the water with dissolved equivalent amount for injection into the chitosan-g-cyclodextrin, and stirring and dissolving until a transparent solution is obtained; secondly, adding the eye drops medicament and the hydroxysuccinic acid into the solution, and stirring to be completely dissolved; finally, adding the water for injection, metering the volume, and sterilizing to obtain the eye drops. After the eye drops disclosed by the invention is applied to an ocular surface, the eye drops have the following predominant advantages that the irritation of the medicament is reduced, the detention time of the medicament on the ocular surface is prolonged, the corneal permeability of the medicament is improved, and the treatment effect of the medicament is improved.

Description

technical field [0001] The invention belongs to the technical fields of polymer chemistry, biomedical materials and pharmacy, and specifically relates to an eye drop with a polymer graft copolymer as a carrier and a preparation method thereof. Background technique [0002] Eye drops have been the preferred method of ophthalmic drug delivery due to their numerous advantages. However, the special physiological structure of the eye forms the tear film barrier and corneal barrier, which seriously limits the permeability of drugs. Enhancing the corneal penetration of eye drops has always been a very challenging and urgent problem in the research and development of ophthalmic drugs. Improving the solubility of hydrophobic drugs, increasing the residence time of drugs on the ocular surface, increasing the sustained release performance, and improving the drug penetration mechanism have become the key to solving the problems of ocular surface drug delivery. Conventional drug dosage ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K47/36A61K47/12A61K45/00A61K31/4174A61P27/02A61P31/10
CPCA61K9/0048A61K9/08A61K31/4174A61K45/00A61K47/12A61K47/36
Inventor 李景果张俊杰何继军栗占荣王丽娅祝磊
Owner 河南省眼科研究所
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