Comprehensive Ocular and Systemic Pharmacokinetics of Brinzolamide in Rabbits After Intracameral, Topical, and Intravenous Administration

Brinzolamide is a topical carbonic anhydrase inhibitor which reduces the production of aqueous humor in ciliary body, thereby reducing intra-ocular pressure. It formulated as an ophthalmic suspension. The pharmacokinetics ocular suspensions not well understood. objective this study was to characterize brinzolamide rabbit humor, iris-ciliary plasma, and whole blood. New Zealand White rabbits were dosed via intracameral, intravenous administration. After intracameral administration (4.5 μg) solubilized brinzolamide, concentrations described with two-compartment model, estimated clearance 4.12 μL/min, apparent volume distribution at steady-state 673 μL, terminal half-life 3.4 h. 1% suspension (500 μg), absolute bioavailability based on AUC0-∞ 0.10%. solution (0.75 mg/kg) elimination plasma blood appeared be over two weeks. ratios measured irisciliary body blood, enabled direct comparisons, helped identify significant contribution conjunctival-scleral pathways absorption body. This shows for first-time provides comprehensive pharmacokinetic parameters following