Abstract:
:The objective of this study was to compare the efficiency of various formulations in maximizing the ratio of ocular to systemic absorption of topically applied timolol in the pigmented rabbit. Formulations of various pHs, tonicities, and concentrations of benzalkonium chloride, EDTA, poly(vinyl alcohol), poly(vinylpyrrolidone), hydroxypropylcellulose, and Na hyaluronate were tested. Ocular absorption was determined by monitoring the timolol concentration in various anterior segment tissues 30 min after instillation of timolol solution, while systemic absorption was determined by monitoring the time course of timolol concentration over 120 min. Timolol was assayed by reversed-phase HPLC. Lowering the solution tonicity to 80 mosmol kg-1 and incorporating polymers into the formulation were the only approaches that promised to improve the safety of topically applied timolol, since they afforded the desired increase in ocular absorption and reduction in systemic absorption. Lowering the solution pH to 6.4 and increasing the tonicity of the solution to 600 mosmol kg-1 reduced systemic absorption but caused either no change or a decrease in ocular absorption. Raising the solution pH to 8.4 and incorporating 0.025% benzalkonium chloride and 0.5% EDTA into the formulation led to an undesirable increase in systemic absorption although ocular absorption was also increased. In the final analysis, the net effect of formulation changes on the ratio of ocular to systemic absorption depended on the interplay of changes in solution drainage; permeability of the cornea, conjunctiva, and nasal mucosa; and fraction of drug in the preferentially absorbed form.
journal_name
Exp Eye Resjournal_title
Experimental eye researchauthors
Podder SK,Moy KC,Lee VHdoi
10.1016/0014-4835(92)90030-vkeywords:
subject
Has Abstractpub_date
1992-05-01 00:00:00pages
747-57issue
5eissn
0014-4835issn
1096-0007journal_volume
54pub_type
杂志文章abstract::Potentiation of retinal degeneration by intense light exposure, and its amelioration by an antioxidant, were studied in a rat model of Smith-Lemli-Opitz syndrome (SLOS), in comparison with normal (control) Sprague-Dawley rats. The SLOS model is created by treating rats with AY9944, a selective inhibitor of cholesterol...
journal_title:Experimental eye research
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journal_title:Experimental eye research
pub_type: 杂志文章
doi:10.1006/exer.1993.1131
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journal_title:Experimental eye research
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journal_title:Experimental eye research
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journal_title:Experimental eye research
pub_type: 杂志文章
doi:10.1006/exer.1993.1015
更新日期:1993-01-01 00:00:00
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journal_title:Experimental eye research
pub_type: 杂志文章
doi:10.1016/0014-4835(92)90047-v
更新日期:1992-03-01 00:00:00
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journal_title:Experimental eye research
pub_type: 杂志文章
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journal_title:Experimental eye research
pub_type: 杂志文章
doi:10.1016/j.exer.2018.09.013
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journal_title:Experimental eye research
pub_type: 杂志文章,评审
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更新日期:2015-04-01 00:00:00
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journal_title:Experimental eye research
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doi:10.1016/j.exer.2015.05.001
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pub_type: 杂志文章
doi:10.1016/j.exer.2019.02.007
更新日期:2019-04-01 00:00:00
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journal_title:Experimental eye research
pub_type: 杂志文章
doi:10.1006/exer.1999.0753
更新日期:2000-01-01 00:00:00
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pub_type: 杂志文章
doi:10.1006/exer.2001.1146
更新日期:2002-06-01 00:00:00
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journal_title:Experimental eye research
pub_type: 杂志文章
doi:10.1016/j.exer.2016.01.004
更新日期:2016-04-01 00:00:00
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journal_title:Experimental eye research
pub_type: 杂志文章
doi:10.1016/0014-4835(86)90017-5
更新日期:1986-01-01 00:00:00
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journal_title:Experimental eye research
pub_type: 杂志文章
doi:10.1016/j.exer.2008.03.013
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doi:10.1016/j.exer.2012.07.007
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journal_title:Experimental eye research
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journal_title:Experimental eye research
pub_type: 杂志文章
doi:10.1016/j.exer.2010.01.004
更新日期:2010-05-01 00:00:00
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journal_title:Experimental eye research
pub_type: 杂志文章,评审
doi:10.1016/j.exer.2005.03.006
更新日期:2005-08-01 00:00:00
abstract::The purpose of this study was to investigate the impact of different diffusion times of mitomycin-C (MMC) on the intrascleral concentration vs depth profile of MMC in an experimental model. Scleral quadrants of eight human donor eyes were exposed to sponges soaked with MMC for an application time of 1 min. After irrig...
journal_title:Experimental eye research
pub_type: 杂志文章
doi:10.1006/exer.2000.0901
更新日期:2000-11-01 00:00:00
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journal_title:Experimental eye research
pub_type: 杂志文章
doi:10.1016/j.exer.2005.02.005
更新日期:2005-09-01 00:00:00
abstract::The identification of genes that modify pathological ocular phenotypes in mouse models may improve our understanding of disease mechanisms and lead to new treatment strategies. Here, we identify modifier loci affecting photoreceptor cell loss in homozygous Mfrp(rd6) mice, which exhibit a slowly progressive photorecept...
journal_title:Experimental eye research
pub_type: 杂志文章
doi:10.1016/j.exer.2013.10.020
更新日期:2014-01-01 00:00:00
abstract::Hyaluronan (HA) distribution in the posterior eye wall from the vitreous through the sclera, with special consideration to localization in the retina and interphotoreceptor matrix (IPM), was evaluated in human, bovine, guinea pig, dog, rat and mouse tissues using a specific probe for HA (bHABC, biotinylated hyaluronan...
journal_title:Experimental eye research
pub_type: 杂志文章
doi:10.1006/exer.1997.0422
更新日期:1998-02-01 00:00:00
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journal_title:Experimental eye research
pub_type: 杂志文章
doi:10.1016/j.exer.2019.107904
更新日期:2020-02-01 00:00:00
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journal_title:Experimental eye research
pub_type: 杂志文章
doi:10.1016/j.exer.2007.07.006
更新日期:2007-10-01 00:00:00
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journal_title:Experimental eye research
pub_type: 杂志文章
doi:10.1016/0014-4835(83)90075-1
更新日期:1983-08-01 00:00:00