In Vivo Pharmacokinetics of Bromfenac Ophthalmic Solution 0.075%, Bromfenac Ophthalmic Solution 0.07%, and Nepafenac/Amfenac Ophthalmic Suspension 0.3% in Rabbits

Ophthalmology and Therapy
John D SheppardMark C Jasek

Abstract

Little is known of the ocular distribution characteristics of currently branded non-steroidal anti-inflammatory drugs (NSAIDs) in the United States. This study was designed to predict the ocular bioavailability characteristics in humans using Dutch Belted rabbits as a surrogate. Commercially available, topically-applied NSAIDs containing bromfenac or nepafenac/amfenac were evaluated. 126 healthy adult Dutch Belted rabbits were randomly assigned to three treatment cohorts (BromSite® twice daily [BID] in the right eye, BromSite® once daily [QD] in the right eye, Prolensa® QD in the right eye and Ilevro™ QD in the left eye) and 7 post-dosing time points (0.5, 1, 2, 4, 8, 12, 24 h after final instillation). The study eyes received 40 µL of the assigned drug for a consecutive 9 days. Samples of aqueous humor, iris-ciliary body, choroid, sclera, and retina were harvested from the study eyes at the assigned time point after the last dose on the 9th day. NSAID content in ocular tissues was analyzed using high-performance liquid chromatography (HPLC), and area under the curve (AUC0.5-24h), maximum concentration (Cmax), and time to maximum concentration (Tmax) were determined. Peak NSAID concentrations were reached within 1-3 h in the an...Continue Reading

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Citations

Jul 26, 2019·Expert Opinion on Pharmacotherapy·Scott M WentzThomas Ciulla
Oct 9, 2018·Expert Opinion on Pharmacotherapy·Rebecca Russ Soares, M Reza Razeghinejad
Jan 29, 2019·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·Constantine D GeorgakopoulosOlga E Makri
Jan 15, 2021·Advances in Colloid and Interface Science·Brunella GrassiriAndreas Bernkop-Schnürch

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