阅读说明：本技术 一种他克莫司滴眼液 (Tacrolimus eye drops ) 是由 李达欣 于 2018-08-30 设计创作，主要内容包括：本发明了公开一种他克莫司滴眼液,属于医药化学品领域,包含以下组分及重量比：水100-120、他克莫司60-80、脱氧胆酸钠50-75、聚乙烯醇40-55、金雀异黄素30-50、氯化钠20-25、癸酸三甘酯18-23、羟丙甲纤维素15-19、磷酸二氢钾13-17、乙酸乙酯10-16、大豆磷脂10-13、蛋黄卵磷脂10-12、聚乙二醇8-12、黄原胶6-9、山嵛酸甘油酯5-8、聚维酮4-6、防腐剂1-3,解决传统眼药水对眼睛存在隐性伤害,无法长期使用的问题。(The invention discloses tacrolimus eye drops, which belong to the field of medical chemicals and comprise the following components in parts by weight: 100-120 parts of water, 60-80 parts of tacrolimus, 50-75 parts of sodium deoxycholate, 40-55 parts of polyvinyl alcohol, 30-50 parts of genistein, 20-25 parts of sodium chloride, 18-23 parts of triglyceride decanoate, 15-19 parts of hydroxypropyl methylcellulose, 13-17 parts of monopotassium phosphate, 10-16 parts of ethyl acetate, 10-13 parts of soybean lecithin, 10-12 parts of egg yolk lecithin, 8-12 parts of polyethylene glycol, 6-9 parts of xanthan gum, 5-8 parts of glyceryl behenate, 4-6 parts of povidone and 1-3 parts of preservative, and solves the problems that the traditional eye drop has recessive injury to eyes and cannot be used for a long time.)

1. The tacrolimus eye drops are characterized by comprising the following components in parts by weight: 100-120 parts of water, 60-80 parts of tacrolimus, 50-75 parts of sodium deoxycholate, 40-55 parts of polyvinyl alcohol, 30-50 parts of genistein, 20-25 parts of sodium chloride, 18-23 parts of triglyceride decanoate, 15-19 parts of hydroxypropyl methylcellulose, 13-17 parts of monopotassium phosphate, 10-16 parts of ethyl acetate, 10-13 parts of soybean lecithin, 10-12 parts of egg yolk lecithin, 8-12 parts of polyethylene glycol, 6-9 parts of xanthan gum, 5-8 parts of glyceryl behenate, 4-6 parts of povidone and 1-3 parts of preservative.

2. The tacrolimus eye drops according to claim 1, which is characterized by comprising the following components in percentage by weight: water 115, tacrolimus 76, sodium deoxycholate 63, polyvinyl alcohol 49, genistein 42, sodium chloride 23, tricaprin 19, hydroxypropyl methylcellulose 17, monopotassium phosphate 16, ethyl acetate 13, soybean lecithin 12, egg yolk lecithin 11, polyethylene glycol 9, xanthan gum 8, glyceryl behenate 6, povidone 5 and preservative 2.

3. Tacrolimus eye drops according to claim 1 or 2, wherein the preservative comprises one or more of benzalkonium chloride, sorbitol.

Technical Field

The invention relates to the field of medical chemicals, and in particular relates to tacrolimus eye drops.

Background

Due to the unique structure of eyes (the surface layer of the cornea is lipophilic, the inner layer is hydrophilic, the blood retinal barrier) and physiological functions (tear elution, tear dilution, nasolacrimal duct drainage and the like), the traditional eye drops have the problems of poor corneal permeability, low bioavailability and the like, and the frequent application of the eye drops for improving the drug concentration and retention time can cause poor tolerance of patients and even toxic and side effects on the surface of eyes.

Tacrolimus (FK 506) is a novel macrolide immunosuppressant, belongs to a calmodulin phosphatase inhibitor, has an immunosuppression mechanism similar to that of cyclosporin A, and has the effect of inhibiting T cells 10-100 times that of cyclosporin A. Tacrolimus is widely applied to the rejection resistance of organ transplantation and the treatment of autoimmune system diseases clinically, and is used for treating eye diseases related to immunity after corneal transplantation in the field of ophthalmology.

Disclosure of Invention

The invention aims to solve the problems that the traditional eye drops have recessive damage to eyes and cannot be used for a long time, and provides tacrolimus eye drops.

In order to solve the technical problems, the invention adopts the following technical scheme:

the tacrolimus eye drops comprise the following components in parts by weight: 100-120 parts of water, 60-80 parts of tacrolimus, 50-75 parts of sodium deoxycholate, 40-55 parts of polyvinyl alcohol, 30-50 parts of genistein, 20-25 parts of sodium chloride, 18-23 parts of triglyceride decanoate, 15-19 parts of hydroxypropyl methylcellulose, 13-17 parts of monopotassium phosphate, 10-16 parts of ethyl acetate, 10-13 parts of soybean lecithin, 10-12 parts of egg yolk lecithin, 8-12 parts of polyethylene glycol, 6-9 parts of xanthan gum, 5-8 parts of glyceryl behenate, 4-6 parts of povidone and 1-3 parts of preservative.

Preferably, the composition comprises the following components in percentage by weight: water 115, tacrolimus 76, sodium deoxycholate 63, polyvinyl alcohol 49, genistein 42, sodium chloride 23, tricaprin 19, hydroxypropyl methylcellulose 17, monopotassium phosphate 16, ethyl acetate 13, soybean lecithin 12, egg yolk lecithin 11, polyethylene glycol 9, xanthan gum 8, glyceryl behenate 6, povidone 5 and preservative 2.

Preferably, the preservative comprises one or more of benzalkonium chloride, and sorbitol.

The implementation of the invention has the following beneficial effects:

the invention takes tacrolimus as a main effective component, sodium chloride, triglyceride caprate, hydroxypropyl methylcellulose, monopotassium phosphate, ethyl acetate, soybean phospholipid, yolk lecithin, polyethylene glycol, xanthan gum, glyceryl behenate and povidone as carriers, opens a corneal osmotic channel, and is matched with medicaments such as sodium deoxycholate, polyvinyl alcohol, genistein and the like to assist and directly act on eyeballs, thereby improving bioavailability, providing long-term effective protection for eyes, not causing burden to the eyes and not damaging the eyes.

Detailed Description

In order to make the objects, technical solutions and advantages of the present invention more apparent, the present invention will be further described in detail with reference to specific embodiments.