title: Topically effective ocular hypotensive acetazolamide and ethoxyzolamide formulations in rabbits.
abstract: The effect of topically active 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CyD) eye-drop formulations containing solutions of acetazolamide, ethoxyzolamide or timolol on the intra-ocular pressure (IOP) was investigated in normotensive conscious rabbits. Both acetazolamide and ethoxyzolamide were active but their IOP-lowering effect was less than that of timolol. The IOP-lowering effects of acetazolamide and ethoxyzolamide and that of timolol appeared to be to some extent additive. Combination of acetazolamide and timolol or ethoxyzolamide and timolol in one HP-beta-CyD formulation resulted in a significant increase in the duration of activity compared with HP-beta-CyD formulations containing only acetazolamide, ethoxyzolamide or timolol. Also, it was possible to increase the IOP-lowering effect of acetazolamide by formulating the drug as a suspension in an aqueous HP-beta-CyD vehicle.
authors.affiliation: Department of Pharmacy, Faculty of Medicine, University of Iceland, Reykjavik.
authors.forename: T
authors.initials: T
authors.lastname: Loftsson
authors.forename: H
authors.initials: H
authors.lastname: Frithriksdóttir
authors.forename: E
authors.initials: E
authors.lastname: Stefánsson
authors.forename: S
authors.initials: S
authors.lastname: Thórisdóttir
authors.forename: O
authors.initials: O
authors.lastname: Guthmundsson
authors.forename: T
authors.initials: T
authors.lastname: Sigthórsson
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000086:Acetazolamide / Q000494:pharmacology*; D000287:Administration, Topical; D000818:Animals; D003505:Cyclodextrins; D004338:Drug Combinations; D005016:Ethoxzolamide / Q000494:pharmacology*; D005260:Female; D007429:Intraocular Pressure / Q000187:drug effects*; D008297:Male; D009883:Ophthalmic Solutions; D011817:Rabbits; D013999:Timolol / Q000494:pharmacology; D047392:beta-Cyclodextrins
chemical_list: D003505:Cyclodextrins; D004338:Drug Combinations; D009883:Ophthalmic Solutions; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D013999:Timolol; D000086:Acetazolamide; D005016:Ethoxzolamide