The ocular distribution of 14C-labeled bromfenac ophthalmic solution 0.07% in a rabbit model

George A Baklayan, Mauricio Muñoz Bausch + Lomb, Irvine, CA, USA Purpose: To evaluate the ocular distribution of an advanced formulation of bromfenac ophthalmic solution. Two studies were conducted in rabbits: 1) a 12-hour parallel-group study comparing the ocular distribution of 14C-b...

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Autores principales:	Baklayan GA, Muñoz M
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2014
Materias:	Ophthalmology RE1-994
Acceso en línea:	https://doaj.org/article/2b10da88fae2407d9be9806618ca70ed
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spelling	oai:doaj.org-article:2b10da88fae2407d9be9806618ca70ed2021-12-02T01:46:05ZThe ocular distribution of 14C-labeled bromfenac ophthalmic solution 0.07% in a rabbit model1177-5483https://doaj.org/article/2b10da88fae2407d9be9806618ca70ed2014-09-01T00:00:00Zhttp://www.dovepress.com/the-ocular-distribution-of-14c-labeled-bromfenac-ophthalmic-solution-0-peer-reviewed-article-OPTHhttps://doaj.org/toc/1177-5483 George A Baklayan, Mauricio Muñoz Bausch + Lomb, Irvine, CA, USA Purpose: To evaluate the ocular distribution of an advanced formulation of bromfenac ophthalmic solution. Two studies were conducted in rabbits: 1) a 12-hour parallel-group study comparing the ocular distribution of 14C-bromfenac ophthalmic solution 0.07%, pH 7.8 with that of 14C-bromfenac ophthalmic solution 0.09%, pH 8.3, and 2) a 24-hour study evaluating the ocular distribution of 14C-bromfenac ophthalmic solution 0.07%, pH 7.8.Methods: In the 12-hour study, rabbits were randomized to receive 50 µL of 14C-bromfenac 0.07%, pH 7.8 or 50 µL 14C-bromfenac 0.09%, pH 8.3 in one eye, whereas, in the 24-hour, study both eyes received 50 µL of 14C-bromfenac 0.07%, pH 7.8. Ocular tissues were collected at 1, 2, 4, 8, 12 (both studies) and 24 hours (second study only) following drug instillation, and tissue radioactivity was determined using liquid scintillation chromatography. Results: Measureable levels of bromfenac were observed in all ocular tissues, with the exception of vitreous humor, regardless of formulation. In the 12-hour study, high concentrations of 14C-bromfenac were found in the sclera, followed by the iris/ciliary body, aqueous humor, choroid, retina, and lens. There was no significant difference between the bromfenac 0.07%, pH 7.8 and bromfenac 0.09%, pH 8.3 formulations in any 14C-bromfenac tissue levels at any time point, with the exception of in sclera at 2 hours post-instillation (0.451 µg eq/g versus 0.302 µg eq/g, respectively, P<0.001). There was also no significant difference in the total amount of 14C-bromfenac in the tissues evaluated following instillation of the two formulations. In the 24-hour study evaluating bromfenac 0.07%, pH 7.8 only, high concentrations of 14C-bromfenac were found 1 hour post-instillation in the cornea (2.402 µg eq/g) and conjunctiva (1.049 µg eq/g), two tissues not evaluated in the 12-hour study. The rank order of 14C-bromfenac levels in the other ocular tissues was the same as that observed in the 12-hour study, with measureable amounts of 14C-bromfenac detected through 24 hours in all tissues with the exception of vitreous humor. Conclusion: Bromfenac ophthalmic solution 0.07%, pH 7.8 readily penetrated ocular tissues with levels similar to those of bromfenac ophthalmic solution 0.09%, pH 8.3. Keywords: penetration, topical NSAIDs, pharmacokinetics, eye, pHBaklayan GAMuñoz MDove Medical PressarticleOphthalmologyRE1-994ENClinical Ophthalmology, Vol 2014, Iss default, Pp 1717-1724 (2014)
institution	DOAJ
collection	DOAJ
language	EN
topic	Ophthalmology RE1-994
spellingShingle	Ophthalmology RE1-994 Baklayan GA Muñoz M The ocular distribution of 14C-labeled bromfenac ophthalmic solution 0.07% in a rabbit model
description	George A Baklayan, Mauricio Muñoz Bausch + Lomb, Irvine, CA, USA Purpose: To evaluate the ocular distribution of an advanced formulation of bromfenac ophthalmic solution. Two studies were conducted in rabbits: 1) a 12-hour parallel-group study comparing the ocular distribution of 14C-bromfenac ophthalmic solution 0.07%, pH 7.8 with that of 14C-bromfenac ophthalmic solution 0.09%, pH 8.3, and 2) a 24-hour study evaluating the ocular distribution of 14C-bromfenac ophthalmic solution 0.07%, pH 7.8.Methods: In the 12-hour study, rabbits were randomized to receive 50 µL of 14C-bromfenac 0.07%, pH 7.8 or 50 µL 14C-bromfenac 0.09%, pH 8.3 in one eye, whereas, in the 24-hour, study both eyes received 50 µL of 14C-bromfenac 0.07%, pH 7.8. Ocular tissues were collected at 1, 2, 4, 8, 12 (both studies) and 24 hours (second study only) following drug instillation, and tissue radioactivity was determined using liquid scintillation chromatography. Results: Measureable levels of bromfenac were observed in all ocular tissues, with the exception of vitreous humor, regardless of formulation. In the 12-hour study, high concentrations of 14C-bromfenac were found in the sclera, followed by the iris/ciliary body, aqueous humor, choroid, retina, and lens. There was no significant difference between the bromfenac 0.07%, pH 7.8 and bromfenac 0.09%, pH 8.3 formulations in any 14C-bromfenac tissue levels at any time point, with the exception of in sclera at 2 hours post-instillation (0.451 µg eq/g versus 0.302 µg eq/g, respectively, P<0.001). There was also no significant difference in the total amount of 14C-bromfenac in the tissues evaluated following instillation of the two formulations. In the 24-hour study evaluating bromfenac 0.07%, pH 7.8 only, high concentrations of 14C-bromfenac were found 1 hour post-instillation in the cornea (2.402 µg eq/g) and conjunctiva (1.049 µg eq/g), two tissues not evaluated in the 12-hour study. The rank order of 14C-bromfenac levels in the other ocular tissues was the same as that observed in the 12-hour study, with measureable amounts of 14C-bromfenac detected through 24 hours in all tissues with the exception of vitreous humor. Conclusion: Bromfenac ophthalmic solution 0.07%, pH 7.8 readily penetrated ocular tissues with levels similar to those of bromfenac ophthalmic solution 0.09%, pH 8.3. Keywords: penetration, topical NSAIDs, pharmacokinetics, eye, pH
format	article
author	Baklayan GA Muñoz M
author_facet	Baklayan GA Muñoz M
author_sort	Baklayan GA
title	The ocular distribution of 14C-labeled bromfenac ophthalmic solution 0.07% in a rabbit model
title_short	The ocular distribution of 14C-labeled bromfenac ophthalmic solution 0.07% in a rabbit model
title_full	The ocular distribution of 14C-labeled bromfenac ophthalmic solution 0.07% in a rabbit model
title_fullStr	The ocular distribution of 14C-labeled bromfenac ophthalmic solution 0.07% in a rabbit model
title_full_unstemmed	The ocular distribution of 14C-labeled bromfenac ophthalmic solution 0.07% in a rabbit model
title_sort	ocular distribution of 14c-labeled bromfenac ophthalmic solution 0.07% in a rabbit model
publisher	Dove Medical Press
publishDate	2014
url	https://doaj.org/article/2b10da88fae2407d9be9806618ca70ed
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The ocular distribution of 14C-labeled bromfenac ophthalmic solution 0.07% in a rabbit model

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