The pharmacokinetics, safety, and tolerability of meloxicam eye drops in Chinese healthy volunteers were evaluated to provide a basis for the formulation of a phase II clinical trial dosing regimen for this product. Including pre-tests and formal trials, formal trials include single-dose pharmacokinetics tests and multiple-dose tolerance tests (4 times a day for 3 consecutive days).
Meloxicam eye drops is a new class 2 drug of the country. The main ingredients are meloxicam. The other ingredients are hydroxypropyl-β-cyclodextrin, sodium hydroxide, boric acid, sodium chloride and water for injection. Among them, hydroxypropyl-β-cyclodextrin can increase the solubility of meloxicam and improve the stability of the solution. The indication of meloxicam eye drops is non-infectious ocular inflammation, especially for inflammation and complications after cataract surgery. The possible adverse reaction is transient tingling in the eye after eye drops. Meloxicam is a non-steroidal anti-inflammatory drug (NSAIDS) that selectively inhibits COX-2 cyclooxygenase. It is currently widely used in the treatment of acute and chronic inflammation and pain, and its mechanism of action is to prevent the production of prostaglandins (PGs) that cause inflammation by inhibiting cyclooxygenase (COX). Non-infectious ocular inflammation is usually caused by the synthesis and release of inflammatory mediators such as prostaglandin (PG) after eye tissues are stimulated. Because non-steroidal anti-inflammatory drugs have anti-inflammatory, anti-allergic and analgesic effects, and have no adverse effects of glucocorticoids, their application in ophthalmology has been valued.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
80
Meloxicam Eye Drops
Institution of Drug Clinical Trials
Beijing, Beijing Municipality, China
Concentration of drug prototype-meloxicam in tears of each subject, ng · h / ml
In a single administration test, tear samples were collected 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 hours after administration, and 8 eyes were taken at each time point.LC-MS
Time frame: 2 days
Intraocular pressure examination,mmHg
In the multiple dose tolerance test, IOP was performed 2 hours (± 20min) after the second dose of Day2.
Time frame: 1 day
Corneal fluorescence staining,levels
Corneal fluorescence staining during the multiple dose tolerance test (Day1-Day3) 1 h after the last daily dose (time window ± 10 min).
Time frame: 3 days
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