PMID: 8985636Jan 1, 1997Paper

Ocular penetration and pharmacokinetics of topical fluconazole

Cornea
R W YeeM G Rinaldi

Abstract

The high bioavailability and low toxicity of fluconazole, a stable, water-soluble, low-molecular-weight bis-triazole antifungal, makes it a good candidate for consideration as a topical ocular agent. The penetration of fluconazole (0.2%) into the corneas and aqueous humors of New Zealand white rabbits was assayed by gas liquid chromatography (GLC). Peak corneal levels occurred essentially immediately at 5 min in the corneas [debrided, 8.2 +/- 1.2 micrograms/g; nondebrided, 1.6 +/- 0.6 microgram/g; (mean +/- SEM)] and at 15 min after application in the aqueous [debrided, 9.4 +/- 2.3 micrograms/ml; nondebrided, 1.6 +/- 0.6 microgram/ml; (mean +/- SEM)]. Estimating from semilogarithmic plots of the data, the halflife (t1/2) in the debrided eyes was 15 min; in the nondebrided eyes, t1/2 was 30 min. A loading dose of a 20-microliter drop per min for 5 min yielded levels of 59.9 +/- 11.3 micrograms/g (mean +/- SEM) in the debrided corneas and 32.4 +/- 1.9 micrograms/ ml (mean +/- SEM) in the corresponding aqueous humor. A regimen consisting of this loading dose followed by one 20 microliters drop/h for 6 h showed 45.9 +/- 3.5 micrograms/g (mean +/- SEM) in the debrided corneas and 8.8 +/- 1.7 micrograms/ml (mean +/- SEM) in the corre...Continue Reading

Citations

Sep 16, 2008·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·Indu Pal KaurHarinder Singh
Jun 15, 2012·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·Indu Pal KaurShilpa Kakkar
Feb 16, 2013·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·Yan XuShengtao Sun
Mar 29, 2005·Antimicrobial Agents and Chemotherapy·David GoldblumStefan Zimmerli
Oct 15, 2003·Clinical Microbiology Reviews·Philip A Thomas
Jun 17, 2014·International Journal of Antimicrobial Agents·Chin Fen NeohDavid C M Kong
Dec 28, 2011·European Journal of Pharmacology·Jingjing LiuHao Cui
Mar 3, 2009·Journal of Cataract and Refractive Surgery·Matthew C CaldwellAlan D Proia
Aug 18, 2009·Acta Ophthalmologica·Fawzia S HabibDina Fathalla
Jul 20, 2005·American Journal of Ophthalmology·Safiye Yilmaz, Ahmet Maden
Nov 8, 2003·Clinical Techniques in Small Animal Practice·Stacy E Andrew
Mar 28, 2006·American Journal of Ophthalmology·Sachin DevAnita Raghavan
Feb 13, 2001·Experimental Eye Research·O E AbbasoğluE Gürsel
Oct 1, 2010·Saudi Pharmaceutical Journal : SPJ : the Official Publication of the Saudi Pharmaceutical Society·Ola H El-NesrOmaima N El-Gazayerly

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