cyclosporine ophthalmic emulsion

Abstract

The invention provides ophthalmic ciclosporin emulsion. The ophthalmic emulsion is characterized by comprising the following components by weight percent: 0.02-0.1% of ciclosporin, 2.5-4% of polyoxyethylated castor oil, 1-3% of middle-chain fatty glyceride, 2-5% of glycerin, 0.2-0.5% of sodium alginate and the balance of water.

Description

technical field [0001] The invention relates to an emulsion with polypeptide as an active ingredient, in particular to a cyclosporine emulsion. Background technique [0002] Cyclosporin (CAS: 59865-13-3, Ciclosporin), also known as cyclosporin A, is produced by certain Hyphomycetes fungi such as Cylindrocarpon lucidum and Tolypocladium inflatum A lipophilic cyclic polypeptide compound isolated from the culture medium of , widely used as an immunosuppressant, the molecular formula is as follows: [0003] [0004] When cyclosporine is prepared as an ophthalmic preparation, it can be used to treat ocular autoimmune diseases such as dry eye, but because cyclosporine is absorbed in the lacrimal gland when needed in the treatment of dry eye, and cyclosporine itself is difficult to absorb in water. Therefore, it is difficult to effectively release cyclosporine in the lacrimal gland when using commonly used eye drops. Chinese patent application CN95194078 discloses a kind of emu...

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Problems solved by technology

[0004] When cyclosporine is prepared as an ophthalmic preparation, it can be used to treat ocular autoimmune diseases such as dry eye, but because cyclosporine is absorbed in the lacrimal gland when needed in the treatment of dry eye, and cyclosporine itself is difficult to absorb in water. Therefore, it is difficult to effectively release cyclosporine in the lacrimal gland when using commonly used eye drops. Chinese patent application CN95194078 discloses a kind of emulsion with cyclosporine as the active ingredient. Dissolving cyclosporine in castor oil Among them, an oil-in-water emulsion made of Tween 80, Kabaum 1342, glycerin, etc. as the main auxiliary materials, Chinese patent application CN2013800165845 discloses an emulsion with cyclosporine as the active ingredient, through polyoxyethyl castor oil Or polyoxyethylated hydrogenated castor oil can obtain a kind of nanoemulsion that does not need to add oil or other emulsifiers again as solubilizer, although above-mentioned preparation can improve the coefficient of cyclosporine in lacrimal gland and can improve its effect of increasing tear secretion , but experiments show that it lacks the persistence of curative effect, as pointed out in the accompanying drawings of CN95194078, the concentration of cyclosporine in the ciliary body and lacrimal gland decreases rapidly over time

Cyclosporin eye drops are used to treat dry eye as an autoimmune disease. The key to its treatment is to make the drug continue to act on the lacrimal gland to play an anti-inflammatory effect. At the same time, it can also restore the tear secretion. The therapeutic effects of existing eye drops are not very satisfactory, so providing a cyclosporin emulsion with a higher concentration that can remain in the target tissue for a longer period of time has become an urgent problem to be solved in the prior art

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