Topically effective ocular hypotensive acetazolamide and ethoxyzolamide formulations in rabbits.
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.
Loftsson
T
T
Department of Pharmacy, Faculty of Medicine, University of Iceland, Reykjavik.
Frithriksdóttir
H
H
Stefánsson
E
E
Thórisdóttir
S
S
Guthmundsson
O
O
Sigthórsson
T
T
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
D003505:Cyclodextrins; D004338:Drug Combinations; D009883:Ophthalmic Solutions; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D013999:Timolol; D000086:Acetazolamide; D005016:Ethoxzolamide