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Levofloxacin hydrochloride sustained-release eye drops

A technology of levofloxacin hydrochloride and slow-release eye drops, which is applied to medical preparations of non-active ingredients, organic active ingredients, sensory diseases, etc., can solve problems such as damage to the eyes, change of cell permeability, and degeneration of lacrimal gland function. Effects of improving biosafety, wide-ranging antibacterial and sterilizing capabilities, and reducing risk of damage

Inactive Publication Date: 2016-12-21
GUANGDONG WHOLEWIN TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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.

Method used

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  • Levofloxacin hydrochloride sustained-release eye drops
  • Levofloxacin hydrochloride sustained-release eye drops
  • Levofloxacin hydrochloride sustained-release eye drops

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-6

[0015] Embodiment 1-6 prepares the levofloxacin hydrochloride sustained-release eye drops raw material component and dosage without preservative

[0016]

[0017] According to the technical scheme of the present invention, the optional adjuvant species for preparing levofloxacin hydrochloride sustained-release eye drops without preservatives is not limited to the species listed in the above table, and can also have the following multiple options:

[0018] Metal ion complexing agent: metal ion complexing agents commonly used in pharmacy can be used, such as any one of disodium edetate, sodium gluconate, sodium tartrate, sodium citrate, aminotriacetic acid or any of the described varieties Combination; the amount of the metal ion complexing agent is expressed in weight ratio with levofloxacin, levofloxacin hydrochloride: metal ion complexing agent=1:0.01~0.50.

[0019] Use osmotic pressure regulator to adjust the osmolar concentration of finished eye drops to be 280~330mOsmol...

experiment example 1

[0023] Experimental Example 1 Pharmacodynamics Test

[0024] The preparation prepared by the method described in the embodiment of the present invention 2 is used as test sample, adopts 0.3% levofloxacin hydrochloride eye drops (reference preparation I, Beijing Lixiang Pharmaceutical Co., Ltd., trade name: Langyue, specification 24mg: 8ml), 0.3% levofloxacin hydrochloride eye drops (reference preparation II, Shandong Bausch & Lomb Freda Pharmaceutical Co., Ltd., trade name: Helen, specification 5ml: 15mg), normal saline are as reference substance, pass through pharmacodynamics test, illustrate hydrochloric acid of the present invention Levofloxacin eye drops have a sustained-release effect and can improve the therapeutic effect.

[0025] 1. Establishment of injury-type bacterial conjunctivitis model

[0026] 1.1 Preparation of infection bacteria suspension: Dilute Staphylococcus aureus solution cultured for 2 days to 5×10 with 0.9% sodium chloride injection 9 cfu ml -1 (Det...

experiment example 2

[0040] Pharmacokinetic experiment in experimental example 2 in rabbit eye aqueous humor

[0041]The preparation prepared by the method described in the embodiment of the present invention 2 is used as test sample, adopts 0.3% levofloxacin hydrochloride eye drops (reference preparation I, Beijing Lixiang Pharmaceutical Co., Ltd., trade name: Langyue, specification 24mg: 8ml), 0.3% levofloxacin hydrochloride eye drops (reference preparation II, Shandong Bausch & Lomb Freda Pharmaceutical Co., Ltd., trade name: Helen, specification 5ml: 15mg), normal saline as reference substance, through the pharmacokinetics in the aqueous humor of rabbit eyes The scientific experiment shows that the levofloxacin hydrochloride eye drops of the present invention has sustained release effect and can improve the bioavailability of medicine.

[0042] 1. Administration method: Self-control, cross-over experimental design is adopted, and the washout period is 7 days. Twenty-five healthy New Zealand r...

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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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K47/36A61K31/5383A61P31/04A61P27/02
CPCA61K9/0002A61K9/0048A61K9/08A61K31/5383A61K47/36
Inventor 吴绮峰王延东焦宇辰曾夏芸吕鹏张伟龙
Owner GUANGDONG WHOLEWIN TECH
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