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J Ocul Pharmacol Ther ; 24(4): 392-8, 2008 Aug.
Article in English | MEDLINE | ID: mdl-18665811

ABSTRACT

PURPOSE: The aim of this study was to determine the distribution and concentrations of bromfenac ophthalmic solution in ocular tissues following topical instillation in New Zealand White (NZW) rabbits. DESIGN: Two animal studies were conducted. METHODS: A single 50-muL (14)C-bromfenac ophthalmic solution (20-25 muCi or 0.09%) was administered into the right eyes of 14-18 randomly assigned NZW rabbits. At various time points, ocular tissues were collected and analyzed for (14)C-bromfenac contents. Ocular tissues were combusted and the amount of radioactivity was determined by liquid scintillation counting (LSC). Aqueous-humor samples were directly transferred to LSC vials. RESULTS: Peak concentrations of (14)C-bromfenac were observed in the aqueous humor and most ocular tissues at or before 2-hours. The highest concentrations were in the cornea, conjunctiva, and sclera. Similar amounts were detected in the aqueous humor, iris-ciliary body, choroid, and, to a slightly lesser degree, in the retina. Measurable amounts of bromfenac were detected in all samples at the 24-hours time point (> or =0.001 mug equivalent/g). CONCLUSIONS: Significant penetration and measurable amounts of (14)C-bromfenac were detected in all ocular tissues over 24 h, including the sclera, choroid, and retina. These results strongly suggest the utility of bromfenac ophthalmic solution 0.09% in treating inflammation of both the anterior and posterior ocular segments.


Subject(s)
Benzophenones/administration & dosage , Benzophenones/pharmacokinetics , Bromobenzenes/administration & dosage , Bromobenzenes/pharmacokinetics , Eye/drug effects , Eye/metabolism , Administration, Topical , Animals , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics , Aqueous Humor/drug effects , Aqueous Humor/metabolism , Carbon Radioisotopes/administration & dosage , Carbon Radioisotopes/pharmacokinetics , Female , Rabbits , Random Allocation , Time Factors , Tissue Distribution/drug effects , Tissue Distribution/physiology , Vitreous Body/drug effects , Vitreous Body/metabolism
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