Abstract
Purpose: :
To evaluate the pharmacokinetic profile of topically applied bromfenac sodium ophthalmic solution (BF) 0.1% in subjects undergoing cataract surgery.
Methods: :
Fifty–four subjects undergoing routine cataract surgery with intraocular lens implant (mean age: 72.3 years) were enrolled to quantify the concentration of BF in aqueous humor. One drop of BF 0.1% was administered at a various time from 30 to 345 minutes prior to surgery. Pharmacokinetics was determined following a single dose. A 100 µl sample of aqueous humor was obtained after entering the anterior chamber. The time of sampling was recorded, and the sample was snap–frozen in liquid nitrogen. The concentration of BF in the samples was determined using High Performance Liquid Chromatography.
Results: :
The peak aqueous humor concentration of BF was 78.7 ng/mL at 150–180 minutes after instillation. BF decreased with a half–life of 1.4 hrs. BF concentration remained above IC50 value of cyclooxygenase–2 inhibition during the experiment time points. The duration for retaining the effective concentration was about 12 hrs from computer simulation.
Conclusions: :
Pre–operative instillation of BF demonstrated that the peak aqueous humor concentration occurred 150–180 minutes after instillation with a mean concentration of 78.7 ng/mL. These human data suggest that BF may remain at an effective concentration over 12 hrs in the aqueous humor.
Keywords: cataract • aqueous • pharmacology