Abstract
Purpose::
To use a new rabbit model that simulates dosing in the human eye to predict the ocular penetration and distribution of prednisolone following topical dosing of two commercial formulations.
Methods::
Anesthetised rabbits were given a single topical dose of either new OMNIPREDTM (OP) or PRED FORTE* (PF) prednisolone acetate ophthalmic suspensions (1%). A 30 minute controlled period that simulated the human eye with manual blinking (4 blinks/min) and supplemental tear flow (2 µL/min) followed. Tear samples were collected every 5 minutes, and after euthanasia, aqueous humor and tissue samples were collected at 60 minutes. Prednisolone acetate and alcohol concentrations were quantified using HPLC.
Results::
The mean concentrations of prednisolone (acetate and alcohol combined) (µg/mL or µg/g ± SE) in the tears at the 15 min time point were 280 ± 120 for OP and 170 ± 115 for PF (p > 0.05). The concentrations in the tissues at 1 hour were: in the aqueous humor 0.56 ± 0.11 for OP and 0.43 ± 0.15 for PF (p > 0.05); in the cornea 5.2 ± 1.4 for OP and 3.8 ± 1.1 for PF (p > 0.05); in the palpebral conjunctiva 4.5 ± 2.3 for OP and 4.0 ± 2.3 for PF (p > 0.05); in the bulbar conjunctiva 6.6 ± 2.4 for OP and 6.0 ± 3.9 for PF (p > 0.05).
Conclusions::
Overall, OMNIPREDTM and PRED FORTE* prednisolone acetate ophthalmic suspensions (1%) realized similar tear, aqueous humor, corneal and conjunctival tissue concentrations.*Trademarks are the property of their respective owners
Keywords: inflammation • corticosteroids • conjunctiva