Tacrolimus ophthalmic in-situ gel preparation and preparation method thereof

Abstract

The invention provides a tacrolimus ophthalmic in-situ gel preparation and a preparation method thereof, which micronizes medicaments or adopts the solid dispersion technology, the cyclodextrin inclusion technology or the like to obviously improve the solubility and then to prepare into an ophthalmic preparation which is in the liquid state in vitro and is in the gel state when being dropped into eyes. The invention is applicable to the treatment for preventing and curing ophthalmic corneal transplantation rejection, keratoconjunctivitis (KC), ocular allergic disorders and the like. The invention prepares tacrolimus into the ophthalmic in-situ gel for the first time. The ophthalmic gel is in the liquid state in vitro, the dosage can be easily and accurately controlled, the operation is convenient, and the ophthalmic gel can be uniformly spread when being dropped into eyes to form the gel. The ophthalmic gel can stay in eyes for long, can not be easily diluted by tears, can maintain the concentration of the effective medicaments, enhances the treatment effect, and has the advantages of less stimulation and good biocompatibility, thereby being an effective new ophthalmic medicine, being applicable to the clinic treatment and having extensive development prospect.

Description

technical field The invention belongs to the field of medicines, and more specifically relates to a tacrolimus ophthalmic in-body gel preparation and a preparation method thereof. Background technique Corneal disease caused by various reasons is currently the most important blinding corneal disease in China, and the number of patients is more than one million every year. Corneal transplantation is the most important method to treat such diseases, and immune rejection after corneal transplantation is The big problem right now. Glucocorticoids are the main means to prevent and treat postoperative graft rejection, but their long-term application can not only lead to many complications, but also often cannot effectively inhibit the rejection of high-risk keratoplasty. In recent years, cyclosporine A has been more and more widely used in ophthalmology, but the solvent of cyclosporine eye drops is oily, and it is very irritating to the eyes after it is instilled into the eyes. Pa...

AI Technical Summary

Problems solved by technology

The purpose of the present invention is to provide a tacrolimus ophthalmic in-body gel preparation and its preparation method, which solves the problems of relatively large toxic and side effects on the human body caused by the oral preparation and injection of tacrolimus in the prior art , wherein the tacrolimus intermediate can increase the solubility of the drug. The ophthalmic gel is in a liquid state in vitro, the dosage is easy to accurately control, and it is convenient to use. After being dropped into the eye, it can spread evenly and form a gel, which stays in the eye It takes a long time, is not easily diluted by tears, can maintain effective drug concentration, enhance the therapeutic effect, and has little irritation and good biocompatibility. It is an effective new ophthalmic drug that can be applied clinically and has broad development prospects.

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