Concentrations of besifloxacin, gatifloxacin, and moxifloxacin in human conjunctiva after topical ocular administration

Gail Torkildsen1, Joel W Proksch2, Aron Shapiro3, Stephanie K Lynch3, Timothy L Comstock21Andover Eye Associates, Andover, Massachusetts, USA; 2Bausch and Lomb, Inc., Rochester, New York, USA; 3Ora, Inc., Andover, Massachusetts, USAPurpose: To evaluate the pharmacokinetic properties of besifloxacin,...

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Autores principales:	Gail Torkildsen, Joel W Proksch, Aron Shapiro, et al
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2010
Materias:	Ophthalmology RE1-994
Acceso en línea:	https://doaj.org/article/9c1350542d814eaea9272b7a6ddd5d78
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spelling	oai:doaj.org-article:9c1350542d814eaea9272b7a6ddd5d782021-12-02T06:48:26ZConcentrations of besifloxacin, gatifloxacin, and moxifloxacin in human conjunctiva after topical ocular administration1177-54671177-5483https://doaj.org/article/9c1350542d814eaea9272b7a6ddd5d782010-04-01T00:00:00Zhttp://www.dovepress.com/concentrations-of-besifloxacin-gatifloxacin-and-moxifloxacin-in-human--a4226https://doaj.org/toc/1177-5467https://doaj.org/toc/1177-5483Gail Torkildsen1, Joel W Proksch2, Aron Shapiro3, Stephanie K Lynch3, Timothy L Comstock21Andover Eye Associates, Andover, Massachusetts, USA; 2Bausch and Lomb, Inc., Rochester, New York, USA; 3Ora, Inc., Andover, Massachusetts, USAPurpose: To evaluate the pharmacokinetic properties of besifloxacin, gatifloxacin, and moxifloxacin in the conjunctival tissue of healthy volunteers after topical application.Methods: One-hundred eight (108) subjects were randomly assigned to receive one drop of besifloxacin (0.6% suspension), gatifloxacin (0.3% solution), or moxifloxacin (0.5% solution) ophthalmic formulations in one eye prior to conjunctival biopsy. Conjunctival samples were taken from subjects at either 15 minutes, 30 minutes, 2 hours, 6 hours, 12 hours, or 24 hours after dosing.Results: All three fluoroquinolones reached a peak mean concentration 15 minutes after dosing. The mean concentrations of besifloxacin, gatifloxacin, and moxifloxacin at 15 minutes were 2.30 &plusmn; 1.42 &mu;g/g, 4.03 &plusmn; 3.84 &mu;g/g, and 10.7 &plusmn; 5.89 &mu;g/g, respectively. Concentrations decreased with each subsequent time point. At 24 hours after dosing, concentrations of besifloxacin were measurable in 4 of 6 subjects, compared with 3 of 6 subjects for gatifloxacin and 2 of 6 subjects for moxifloxacin. Besifloxacin had the greatest mean residence time (4.7 hours) in the conjunctival tissue. With regard to methicillin-resistant strains of Staphylococcus aureus and Staphylococcus epidermidis, besifloxacin had the greatest area-under-the-curve (AUC) to MIC90 ratio. Nine percent (9%) of study subjects (N = 7) experienced a transient reduction in visual acuity.Conclusion: All three fluoroquinolones were well tolerated and reached levels in the conjunctiva above the MIC90s of methicillin-sensitive S. aureus and S. epidermidis for at least 2 hours.Keywords: besifloxacin, fluoroquinolone, conjunctivitis, pharmacokinetics, minimum inhibitory concentration Gail TorkildsenJoel W ProkschAron Shapiroet alDove Medical PressarticleOphthalmologyRE1-994ENClinical Ophthalmology, Vol 2010, Iss default, Pp 331-341 (2010)
institution	DOAJ
collection	DOAJ
language	EN
topic	Ophthalmology RE1-994
spellingShingle	Ophthalmology RE1-994 Gail Torkildsen Joel W Proksch Aron Shapiro et al Concentrations of besifloxacin, gatifloxacin, and moxifloxacin in human conjunctiva after topical ocular administration
description	Gail Torkildsen1, Joel W Proksch2, Aron Shapiro3, Stephanie K Lynch3, Timothy L Comstock21Andover Eye Associates, Andover, Massachusetts, USA; 2Bausch and Lomb, Inc., Rochester, New York, USA; 3Ora, Inc., Andover, Massachusetts, USAPurpose: To evaluate the pharmacokinetic properties of besifloxacin, gatifloxacin, and moxifloxacin in the conjunctival tissue of healthy volunteers after topical application.Methods: One-hundred eight (108) subjects were randomly assigned to receive one drop of besifloxacin (0.6% suspension), gatifloxacin (0.3% solution), or moxifloxacin (0.5% solution) ophthalmic formulations in one eye prior to conjunctival biopsy. Conjunctival samples were taken from subjects at either 15 minutes, 30 minutes, 2 hours, 6 hours, 12 hours, or 24 hours after dosing.Results: All three fluoroquinolones reached a peak mean concentration 15 minutes after dosing. The mean concentrations of besifloxacin, gatifloxacin, and moxifloxacin at 15 minutes were 2.30 &plusmn; 1.42 &mu;g/g, 4.03 &plusmn; 3.84 &mu;g/g, and 10.7 &plusmn; 5.89 &mu;g/g, respectively. Concentrations decreased with each subsequent time point. At 24 hours after dosing, concentrations of besifloxacin were measurable in 4 of 6 subjects, compared with 3 of 6 subjects for gatifloxacin and 2 of 6 subjects for moxifloxacin. Besifloxacin had the greatest mean residence time (4.7 hours) in the conjunctival tissue. With regard to methicillin-resistant strains of Staphylococcus aureus and Staphylococcus epidermidis, besifloxacin had the greatest area-under-the-curve (AUC) to MIC90 ratio. Nine percent (9%) of study subjects (N = 7) experienced a transient reduction in visual acuity.Conclusion: All three fluoroquinolones were well tolerated and reached levels in the conjunctiva above the MIC90s of methicillin-sensitive S. aureus and S. epidermidis for at least 2 hours.Keywords: besifloxacin, fluoroquinolone, conjunctivitis, pharmacokinetics, minimum inhibitory concentration
format	article
author	Gail Torkildsen Joel W Proksch Aron Shapiro et al
author_facet	Gail Torkildsen Joel W Proksch Aron Shapiro et al
author_sort	Gail Torkildsen
title	Concentrations of besifloxacin, gatifloxacin, and moxifloxacin in human conjunctiva after topical ocular administration
title_short	Concentrations of besifloxacin, gatifloxacin, and moxifloxacin in human conjunctiva after topical ocular administration
title_full	Concentrations of besifloxacin, gatifloxacin, and moxifloxacin in human conjunctiva after topical ocular administration
title_fullStr	Concentrations of besifloxacin, gatifloxacin, and moxifloxacin in human conjunctiva after topical ocular administration
title_full_unstemmed	Concentrations of besifloxacin, gatifloxacin, and moxifloxacin in human conjunctiva after topical ocular administration
title_sort	concentrations of besifloxacin, gatifloxacin, and moxifloxacin in human conjunctiva after topical ocular administration
publisher	Dove Medical Press
publishDate	2010
url	https://doaj.org/article/9c1350542d814eaea9272b7a6ddd5d78
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Concentrations of besifloxacin, gatifloxacin, and moxifloxacin in human conjunctiva after topical ocular administration

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