title: Ocular penetration of topically applied norfloxacin 0.3% in the rabbits and in humans.
abstract: The kinetics of topically applied norfloxacin 0.3 percent were studied in rabbit and man. All measurements were performed by high-pressure liquid chromatography. Norfloxacin concentrations were investigated five to 120 minutes in rabbit ocular tissues after instillation of a single drop. In normal eyes, after 30 minutes, mean +/- SEM levels were 14.3 +/- 3.7 micrograms/g in cornea, 3.3 +/- 0.7 micrograms/g in conjunctiva, 0.2 +/- 0.1 microgram/g in aqueous humor. After removal of the corneal epithelium concentrations were as follows: 84.2 +/- 15.8 micrograms/g, 7.3 +/- 2.3 micrograms/g, 8.6 +/- 1.9 micrograms/g respectively. Penetration in posterior ocular tissues were rather poor. In human eyes, the intracorneal concentrations were assessed in patients being operated on corneal grafts. After instillation of 5 drops, the concentration in cornea was 15.5 +/- 2.1 micrograms/g. These data show that therapeutic levels of norfloxacin can be achieved in anterior ocular tissues, which may be of help in superficial infections of the eye.
authors.affiliation: Ophthalmology Department, University of Burgundy, Dijon, France.
authors.forename: A M
authors.initials: AM
authors.lastname: Bron
authors.forename: A
authors.initials: A
authors.lastname: Péchinot
authors.forename: C
authors.initials: C
authors.lastname: Garcher
authors.forename: G
authors.initials: G
authors.lastname: Guyonnet
authors.forename: A
authors.initials: A
authors.lastname: Kazmierczak
mesh_terms: D000293:Adolescent; D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D000818:Animals; D002851:Chromatography, High Pressure Liquid; D003315:Cornea / Q000378:metabolism; D005123:Eye / Q000378:metabolism*; D005260:Female; D006801:Humans; D015948:Keratoplasty, Penetrating; D008297:Male; D008875:Middle Aged; D009643:Norfloxacin / Q000493:pharmacokinetics*; D009883:Ophthalmic Solutions; D011817:Rabbits; D014018:Tissue Distribution
chemical_list: D009883:Ophthalmic Solutions; D009643:Norfloxacin