A kind of curcumin micellar eye drops and preparation method thereof

Abstract

The invention discloses a curcumin micellar eye drop, comprising curcumin as the main agent, a preservative, and an isotonic regulator, and is characterized in that it also includes polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol copolymer as Drug auxiliary material, dequalinium chloride is a mitochondrial targeting modifier and stabilizer, and the mass ratio of the curcumin main agent and polyethylene caprolactam-polyvinyl acetate-polyethylene glycol block copolymer drug auxiliary material is at 1:12- Between 1:20, the mass ratio of dequalinium chloride and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol copolymer drug excipients is between 1:20-1:40. The curcumin micelle eye drop prepared by the invention has an administration concentration of up to 5 mg / ml, and the micelle particle size is small, the distribution range is uniform, and the drug stability is good. It not only reduces the irritation of administration, but also improves the absorption of the drug by the cornea, reduces the concentration of the drug, prolongs the action time of the drug, reduces the number of administrations, improves the patient's compliance, and has good economical efficiency.

Description

technical field [0001] The invention relates to a curcumin eye drop, in particular to a curcumin micelle eye drop and a preparation method thereof. Background technique [0002] The prevalence of diabetes in my country has increased rapidly in recent years, and diabetes has become a major public health problem in China. The patient's long-term hyperglycemia state leads to lesions in various tissues and organs throughout the body, causing serious diabetes-related complications, including diabetic keratopathy. In addition, diabetic patients are prone to delayed corneal epithelial healing or even non-healing during corneal trauma or corneal surgery. Blindness is difficult to treat, the prognosis is poor, and the patient's economic and mental burden is serious. At present, the clinical treatment methods for diabetic keratopathy are limited. Therefore, it is of great clinical significance to study new therapeutic targets and effective prevention and treatment measures for diabe...

AI Technical Summary

Problems solved by technology

But it also has some disadvantages: (1) As a polysaccharide polymer material, chitosan itself cannot form micelles, so a large amount of surfactants and co-surfactants need to be added to help form chitosan glue However, adding a large amount of surfactants and co-surfactants will inevitably cause ocular surface irritation and safety hazards in topical ocular application; (2) Because chitosan itself cannot form micelles, adding a large amount of surfactants and co-surfactants Auxiliary formation of micelles after the surfactant leads to low drug loading of the micelles, which directly leads to a low concentration of the main drug curcumin in eye drops. Therefore, the concentration of the main drug curcumin in this invention is only 0.005%-0.02%. Treatment of diabetic keratopathy largely ineffective

[0005] Shandong Provincial Institute of Ophthalmology prepared curcumin nano-micelle eye drops by adopting its applied and authorized invention patent "A Cyclosporine A Micellar Eye Drops and Its Preparation Method" (ZL201210529616.9). In the therapeutic effect evaluation study, ocular surface administration of curcumin nanomicelles can partially correct the redox imbalance in the cornea, but the therapeutic effect is limited because the micelles cannot effectively target into the mitochondria

In addition, in the follow-up development process of the Shandong Provincial Institute of Ophthalmology, it was found that the micelles constructed solely based on polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol copolymer and its aqueous solution were stored, and cyclosporine A would gradually Freed from micelles, the effective stability of its aqueous solution at room temperature is only 3 months

Images