Cyclosporin A eye drops and preparation method thereof

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

Active Publication Date: 2018-09-04
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 in ophthalmology remains a challenge in ophthalmology research, and there is still much room for improvement

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1--the synthesis of graft copolymer

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

[0027] The synthetic route is:

[0028]

[0029] Synthetic steps:

[0030] 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%;

[0031] 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--0

[0035] Embodiment 2--Preparation of 0.06 wt% cyclosporin A eye drops

[0036] First, take 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 therein, stir and dissolve to a transparent solution; then, anhydrous cyclosporin A Add 50 mL of ethanol solution (4 mg / mL) to the above solution (1:10, v / v), stir at low temperature (4°C) until the system becomes completely clear, and filter to remove insoluble matter (for CS-g-CD The amount is small, cyclosporine A is not completely complexed with it, and the filtration here mainly removes the cyclosporin A that has not been complexed); again, remove absolute ethanol under reduced pressure at low temperature (4°C), ultrafiltration tube (molecular weight cut-off 3.5k) and washed 3 times; finally, add water for injection to a volume of 250 mL, and sterilize to obtain eye drops. The concentration of the eye drops measured by high performance liquid chromatography is 0.06 wt...

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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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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K38/13A61K47/69A61P37/06A61P27/02
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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