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PURPOSE: To determine the intraocular penetration of topical drops of betaxolol HCl 0.25% suspension and betaxolol HCl 0.50% solution into the aqueous humor. METHODS: Fifteen patients were randomly assigned to receive topical betaxolol HCl 0.25% suspension (n = 7) or topical betaxolol HCl 0.50% solution (n = 8) the day before cataract surgery. Aqueous samples were collected 2 hours after the administration of the morning dose during cataract surgery. Drug concentrations were determined by high-performance liquid chromatography with fluorescence detection. RESULTS: The mean aqueous humor concentration of topical betaxolol HCl 0.25% suspension was 275.1 ± 168.8 g/mL (range 570-70 μng/mL) and the mean aqueous humor con-centration of topical betaxolol HCl 0.50% solution was 195.4±102.4 μng/mL (range 334-50 μng/mL) (p = 0.281). CONCLUSIONS: The mean aqueous humor concentration of betaxolol 0.25% suspension was higher than betaxolol 0.50% solution; however, the difference was not statistically significant. With twofold reduced concentration and similar anterior chamber penetration, betaxolol 0.25% suspension could be first choice for Beta 1 selective blocker therapy when considered for patients with glaucoma.
Dr. I. Sagdic Yalvac, Department of Ophthalmology, Ankara Education and Research Hospital, Ankara, Turkey and Yeditepe University Eye Hospital, Istanbul, Turkey
11.16 Vehicles, delivery systems, pharmacokinetics, formulation (Part of: 11 Medical treatment)
11.3.4 Betablocker (Part of: 11 Medical treatment > 11.3 Adrenergic drugs)