A novel formulation of an ophthalmic beta-adrenoceptor antagonist.
To minimize ocular discomfort while maintaining efficacy, a delivery system for a topical cardioselective beta-adrenoceptor antagonist, betaxolol was developed. Betaxolol was formulated at 0.25% concentration in a cationic exchange resin, as a suspension. A polyacrylic acid polymer was added to increase viscosity and to increase residence time in the cul-de-sac. No significant settling was observed throughout a four-week observation period. Thus, resuspension of the formulation by frequent shaking was not required for uniformity. In rabbits, the ocular bioavailability of 0.25% betaxolol suspension was equivalent to that of 0.5% betaxolol solution.
Weinreb
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RN
Department of Ophthalmology, School of Medicine, University of California, San Diego 92093.
Jani
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R
D000818:Animals; D015784:Betaxolol / Q000008:administration & dosage*; D009883:Ophthalmic Solutions; D011817:Rabbits; D013535:Suspensions
D009883:Ophthalmic Solutions; D013535:Suspensions; D015784:Betaxolol