Levofloxacin hydrochloride sustained-release eye drops

Abstract

The invention discloses levofloxacin hydrochloride sustained-release eye drops which are ophthalmic preparations prepared by using levofloxacin hydrochloride as a pharmacodynamic raw material, matching with sodium hyaluronate to play a role of a thickener, and then matching with a metal ion complexing agent pharmaceutically acceptable to local parts of eyes, an osmotic pressure regulator and a pH regulator, wherein per 100 parts by weight of a finished product preparation contains 0.30-1.00 part by weight of levofloxacin hydrochloride and 0.1-1.00 part by weight of sodium hyaluronate. The medicine liquid provided by the invention has high viscosity, prolongs the time of medicine staying in the eyes, improves the absorption of the medicine, and improves the bioavailability of the eye drops; no preservative is added to the eye drops provided by the invention, so as to improve the biological safety of the eye drops.

Description

technical field [0001] The invention relates to medical preparations, especially antibacterial infection medicines for external use in ophthalmology. Background technique [0002] A variety of bacteria can invade the surface of the human eye, causing eye bacterial infections, the most common being bacterial conjunctivitis and bacterial keratitis. If such patients do not receive timely and effective treatment or improper treatment, it can lead to serious damage to the conjunctiva, perforation of corneal ulcer, loss of vision or even blindness. Clinical studies have found that quinolones are more effective drugs for the treatment of these two eye diseases. Levofloxacin hydrochloride is a third-generation quinolone antibiotic. It can penetrate the cell membrane and enter the bacterial body, destroying the activity of bacterial DNA gyrase, making it impossible to perform DNA transcription and replication, and leading to apoptosis of the bacterial cell body. In addition, levofl...

AI Technical Summary

Problems solved by technology

[0003] However, currently clinically used levofloxacin hydrochloride eye drops without thickeners cannot stay in the eyes for a long time, and multiple eye drops are required to maintain the effective therapeutic concentration; traditional levofloxacin eye drops / levofloxacin hydrochloride eye drops / levofloxacin lactate Eye drops such as eye drops use benzalkonium chloride (BAC) as a preservative. Preservatives can inhibit bacterial contamination during the storage and use of eye drops. However, for patients who need to use eye drops for a long time, the preservatives can damage the lipid layer of the corneal epithelium, alter the permeability of the cells, causing more active compounds to pass through

Preservatives can also cause allergic reactions such as conjunctival hyperemia, tearing, photophobia, burning or tingling. Preservatives not only damage the cells that secrete mucus on the ocular surface, but also cause the function of the lacrimal gland to deteriorate, and even damage the eyes leading to blindness.

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