title: Ocular pharmacokinetics of moxifloxacin after topical treatment of animals and humans.
abstract: The ocular penetration and pharmacokinetics of moxifloxacin in comparison to other fluoroquinolones (ofloxacin, ciprofloxacin, gatifloxacin, norfloxacin, levofloxacin, and lomefloxacin) have been determined by in vitro and ex vivo techniques, as well as in animal and human studies. This article reviews the original pharmacokinetics work performed by Alcon and other studies reported in the ocular fluoroquinolone literature. The results consistently demonstrate higher maximum concentrations for moxifloxacin relative to the other fluoroquinolones in ocular tissues with levels well above its minimum inhibitory concentrations for relevant ocular pathogens. This superior performance is due to the unique structure of moxifloxacin that combines high lipophilicity for enhanced corneal penetration with high aqueous solubility at physiological pH. The latter property creates a high concentration gradient at the tear film/corneal epithelial interface providing a driving force for better ocular penetration for moxifloxacin. In addition, the higher concentration of moxifloxacin in VIGAMOX (i.e., 0.5% vs. 0.3%) allows more antibiotic to be available to ocular tissues. It is clear from the array of studies summarized in this report that moxifloxacin penetrates ocular tissues better (two- to three-fold) than gatifloxacin, ciprofloxacin, ofloxacin, or levofloxacin. This consistent, enhanced penetration of topical moxifloxacin offers powerful advantages for ophthalmic therapy.
authors.affiliation: Alcon Research, Ltd., Fort Worth, Texas 76134-2099, USA.
authors.forename: Stella M
authors.initials: SM
authors.lastname: Robertson
authors.forename: Michael A
authors.initials: MA
authors.lastname: Curtis
authors.forename: Barry A
authors.initials: BA
authors.lastname: Schlech
authors.forename: Andrew
authors.initials: A
authors.lastname: Rusinko
authors.forename: Geoffrey R
authors.initials: GR
authors.lastname: Owen
authors.forename: Olga
authors.initials: O
authors.lastname: Dembinska
authors.forename: John
authors.initials: J
authors.lastname: Liao
authors.forename: David C
authors.initials: DC
authors.lastname: Dahlin
mesh_terms: D000287:Administration, Topical; D000818:Animals; D001082:Aqueous Humor / Q000378:metabolism; D001372:Aza Compounds / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001682:Biological Availability; D002460:Cell Line; D002463:Cell Membrane Permeability; D003320:Corneal Ulcer / Q000188:drug therapy / Q000378:metabolism* / Q000382:microbiology; D015818:Eye Infections, Bacterial / Q000188:drug therapy / Q000378:metabolism* / Q000382:microbiology; D024841:Fluoroquinolones; D006801:Humans; D000077266:Moxifloxacin; D009883:Ophthalmic Solutions / Q000008:administration & dosage / Q000493:pharmacokinetics; D011804:Quinolines / Q000008:administration & dosage / Q000493:pharmacokinetics*; D013666:Tears / Q000378:metabolism; D014822:Vitreous Body / Q000378:metabolism
chemical_list: D001372:Aza Compounds; D024841:Fluoroquinolones; D009883:Ophthalmic Solutions; D011804:Quinolines; D000077266:Moxifloxacin