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- W2024172578 abstract "Abstract. Purpose: This study aimed to develop low‐viscosity aqueous eyedrops containing enalaprilat and its prodrug enalapril maleate in solution, and to evaluate the eyedrops in rabbits. Methods: Aqueous eyedrops with hydroxypropyl‐β‐cyclodextrin containing 0.01–2.9% (w/v) enalaprilat, 1.0% (w/v) enalapril maleate with cyclodextrin or 0.5% (w/v) timolol were prepared. The eyedrops were administered to rabbits and intraocular pressure (IOP) was measured at various time intervals after the administration and the results (mean of 10 experiments ± standard error of the mean) are expressed as the change from baseline (24.7 ± 3.3 mmHg). Results: Enalaprilat possessed sufficient stability to be formulated as an aqueous eyedrop solution with a shelf‐life of several years at room temperature. The maximum decline in IOP after topical administration of one drop of 2.9% enalaprilat solution was 6.2 ± 0.7 mmHg at 4 hours after administration. Duration of activity exceeded 10 hours. A 1% enalaprilat solution lowered IOP by 4.4 ± 0.8 mmHg at 4 hours after administration and had similar duration, and was more potent than 0.5% timolol. The enalapril maleate eyedrops resulted in delayed action, showing maximum potency at 10–22 hours after administration and duration of up to 32 hours. Conclusions: Enalaprilat eyedrops lower IOP in rabbits. The decline in IOP is proportional to the concentration of dissolved enalaprilat in low‐viscosity aqueous eyedrop formulations." @default.
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- W2024172578 date "2010-04-27" @default.
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- W2024172578 title "Enalaprilat and enalapril maleate eyedrops lower intraocular pressure in rabbits" @default.
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- W2024172578 doi "https://doi.org/10.1111/j.1755-3768.2008.01495.x" @default.
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