Ciclosporin A eye drops and preparation method thereof

A technology of eye drops and cyclosporine, which is applied in the field of biomedical materials, pharmacy, and polymer chemistry, to achieve the effects of reducing irritation, increasing tolerance, and improving apparent solubility

Active Publication Date: 2016-10-12
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

However, almost all delivery systems are not fully satisfactory, therefore, the application of cyclosporine A

Method used

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  • Ciclosporin A eye drops and preparation method thereof
  • Ciclosporin A eye drops and preparation method thereof
  • Ciclosporin A eye drops and preparation method thereof

Examples

Experimental program
Comparison scheme
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Example Embodiment

[0025] Example 1--Synthesis of graft copolymer

[0026] Polymer graft copolymer, its molecular formula is: CS-g-CD.

[0027] The synthetic route is:

[0028]

[0029] Synthesis steps:

[0030] S1. Synthesis of CD-COOH: First, put 9.73 g of α-CD and 7.2 g of sodium hydroxide into a flask, dissolve with 30 mL of distilled water; add 1.165 g of sodium chloroacetate, react at 50 °C for 5 h; then use hydrochloric acid to dissolve the system The pH was adjusted to 7, excess methanol was added for precipitation, the precipitate was filtered, and dried in a vacuum dryer at 40°C overnight to obtain a white powdery CD-COOH, yield: > 96%;

[0031] S2. Synthesis of CS-g-CD: 10 mmol CD-COOH and 11 mmol NHS were dissolved in 50 mL of distilled water and placed in a flask equipped with a magnetic stirring bar, the flask was placed in a 4°C water bath, 11 mmol EDC was added, React at 4 °C for 2 h; slowly add the calculated amount of chitosan aqueous solution (CS contains -NH 2 12-33 mm...

Example Embodiment

[0035] Example 2--The preparation of 0.06 wt% cyclosporine A eye drops

[0036] First, weigh 2 grams of the graft copolymer CS-g-CD with a CD grafting rate of 50% in Example 1, add 500 mL of water for injection to it, and stir to dissolve it to a transparent solution; 50 mL of ethanol solution (4 mg / mL) was added to the above solution (1:10, v / v), stirred at low temperature (4 °C) until the system became completely clear, and the insolubles were removed by filtration (CS-g-CD used The amount of cyclosporine A is small, and the cyclosporine A is not completely complexed with it. Here, the filtration action mainly removes the cyclosporine A that has not been complexed); again, at a low temperature (4 ° C), decompression to remove anhydrous ethanol, ultrafiltration tube (molecular weight cut-off 3.5k) and washed 3 times; finally, add water for injection to make up to 250 mL and sterilize to obtain eye drops. The concentration of the eye drops measured by high performance liquid c...

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Abstract

The invention belongs to the technical field of high polymer chemistry, biomedical materials and pharmacy, and particularly discloses ciclosporin A eye drops and a preparation method thereof. Every 1,000 mL of the eye drops are prepared from the following substances: ciclosporin A 30-630 mg, a polymer-grafted copolymer 1-10 g, and the balance of injection water, wherein the polymer-grafted copolymer is chitosan-g-cyclodextrin. The preparation method comprises the following steps: firstly, weighing the chitosan-g-cyclodextrin as the polymer-grafted copolymer, adding and dissolving equivalent injection water in the chitosan-g-cyclodextrin, and stirring and dissolving until a solution is transparent; secondly, adding an ethanol solution of the ciclosporin A in the solution, stirring at the temperature of 0-4 DEG C until a system becomes completely clear; thirdly, removing ethanol under reduced pressure at the temperature of 0-4 DEG C and washing; and finally, adding the injection water and determining the volume, and sterilizing to obtain the final product. The eye drops have the advantages that irritation of the medicine is reduced, the residence time of the medicine on an ocular surface is prolonged, the corneal permeability of the medicine is improved, and the treatment effect of the medicine is also improved.

Description

technical field [0001] The invention belongs to the technical fields of polymer chemistry, biomedical materials and pharmacy, and specifically relates to cyclosporin A eye drops 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 forms have been unable to break ...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K38/13A61K47/48A61P37/06A61P27/02
CPCA61K9/0048A61K9/08A61K38/13
Inventor 栗占荣李景果张俊杰周天洋何继军夏慧芸王丽娅
Owner 河南省眼科研究所
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