Corneal Penetration Behavior of β-Blocking Agents III: In Vitro–In Vivo Correlations

Aqueous humor levels were determined over time after the topical administration to rabbit eyes of 1% isotonic buffered (pH7.3) solutions of three β-blocking agents, acebutolol hydrochloride, timolol maleate, and bufuralol hydrochloride (arranged in order of increasing lipophilicity). Corneal permeab...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 1983-11, Vol.72 (11), p.1279-1281
Main Authors: Lach, John L., Huang, Hong-Shian, Schoenwald, Ronald D.
Format: Article
Language:English
Subjects:
Acebutolol-corneal permeability in rabbits
Acebutolol—corneal permeability in rabbits, pharmacokinetics, in vitro-in vivo correlations
Adrenergic beta-Antagonists - metabolism
Animals
Aqueous Humor - metabolism
Biological and medical sciences
bufuralol
Bufuralol-corneal permeability in rabbits
Bufuralol—corneal permeability in rabbits, pharmacokinetics, in vitro-in vivo correlations
Chromatography, High Pressure Liquid
Cornea - metabolism
excised rabbit corneas
Eye
In Vitro Techniques
in vitro-in vivo correlations
Kinetics
Medical sciences
Permeability
Permeability-acebutolol
Permeability—acebutolol, timolol, bufuralol, excised rabbit corneas, pharmacokinetics, in vitro-in vivo correlations
pharmacokinetics
Pharmacology. Drug treatments
Rabbits
timolol
Timolol-corneal permeability in rabbits
Timolol—corneal permeability in rabbits, pharmacokinetics, in vitro-in vivo correlations
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Summary:Aqueous humor levels were determined over time after the topical administration to rabbit eyes of 1% isotonic buffered (pH7.3) solutions of three β-blocking agents, acebutolol hydrochloride, timolol maleate, and bufuralol hydrochloride (arranged in order of increasing lipophilicity). Corneal permeability coefficients, determined from a previous in vitro study, were inversely related to the observed time to peak for the three drugs, as expected. Two of the drugs, bufuralol and timolol, did not give the expected rank order for Cmax and AUC, which could result from differences in distribution and/or elimination processes. Aqueous boundary layers were postulated for in vivo comeal permeability which suggested that bufuralol and timolol may have nearly identical effective permeability coefficients in vivo.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600721110