May 2003
Volume 44, Issue 13
Free
ARVO Annual Meeting Abstract  |   May 2003
Penetration and Distribution of Moxifloxacin and Ofloxacin into Ocular Tissues and Plasma Following Topical Ocular Administration to Pigmented Rabbits
Author Affiliations & Notes
  • S.M. Robertson
    Pharmacokinetics and Drug Metabolism, Alcon Research, Ltd., Fort Worth, TX, United States
  • M. Sanders
    Pharmacokinetics and Drug Metabolism, Alcon Research, Ltd., Fort Worth, TX, United States
  • D. Jasheway
    Pharmacokinetics and Drug Metabolism, Alcon Research, Ltd., Fort Worth, TX, United States
  • D. Trawick
    Pharmacokinetics and Drug Metabolism, Alcon Research, Ltd., Fort Worth, TX, United States
  • J. Veltman
    Pharmacokinetics and Drug Metabolism, Alcon Research, Ltd., Fort Worth, TX, United States
  • S. Hamner
    Pharmacokinetics and Drug Metabolism, Alcon Research, Ltd., Fort Worth, TX, United States
  • B.A. Schlech
    Pharmacokinetics and Drug Metabolism, Alcon Research, Ltd., Fort Worth, TX, United States
  • R. Hilaski
    MPI Research, Inc., Mattawan, MI, United States
  • D.C. Dahlin
    MPI Research, Inc., Mattawan, MI, United States
  • Footnotes
    Commercial Relationships  S.M. Robertson, Alcon E; M. Sanders, Alcon E; D. Jasheway, Alcon E; D. Trawick, Alcon E; J. Veltman, Alcon E; S. Hamner, Alcon E; B.A. Schlech, Alcon E; R. Hilaski, Alcon F; D.C. Dahlin, Alcon E.
Investigative Ophthalmology & Visual Science May 2003, Vol.44, 1454. doi:
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      S.M. Robertson, M. Sanders, D. Jasheway, D. Trawick, J. Veltman, S. Hamner, B.A. Schlech, R. Hilaski, D.C. Dahlin; Penetration and Distribution of Moxifloxacin and Ofloxacin into Ocular Tissues and Plasma Following Topical Ocular Administration to Pigmented Rabbits . Invest. Ophthalmol. Vis. Sci. 2003;44(13):1454.

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      © ARVO (1962-2015); The Authors (2016-present)

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Abstract

Abstract: : Purpose: To measure the ocular penetration and distribution of moxifloxacin and ofloxacin into cornea, aqueous humor, iris-ciliary body, tear film and plasma following a single topical ocular administration of 0.3% solutions to rabbits. Methods: The eyes of male Dutch belted rabbits were dosed with a single drop (30 µL) of either 0.3% moxifloxacin solution or ofloxacin 0.3% (OCUFLOX®). Aqueous humor, cornea, iris-ciliary body, tear film and plasma were collected up to 48 hours for analyses of drug concentrations by reverse phase HPLC. Results: Moxifloxacin was well absorbed into the eye and achieved relatively high concentrations in ocular tissues 30 minutes after the single dose (µg/g: cornea: 12.5; aqueous humor: 1.8; iris-ciliary body: 6.3; tear film 10.3). Maximal concentrations of moxifloxacin were typically 2-fold higher than those found for ofloxacin and remained 2-fold higher over the course of the study. Even 48 hours after the single-drop instillation, moxifloxacin mean concentration in the cornea was 0.25 µg/g, which is about 4-fold above its MIC of 0.06 µg/mL for methicillin-susceptible Staphylococcus aureus. Conversely, ofloxacin cornea concentrations fell below the MIC for this organism of 0.5 µg/mL by 8 hours after dosing. The mean tear film concentration of moxifloxacin was 366 µg/mL at the initial 10-minute sampling time and remained at or above 1 µg/mL over 6 hours post-dose. Prolonged retention of moxifloxacin and ofloxacin was observed in the pigmented iris-ciliary body due to melanin binding which is characteristic of fluoroquinolones. Maximum plasma concentrations were about 0.01 µg/mL for both compounds and declined rapidly. Conclusions: These pharmacokinetic findings predict that significant antimicrobial levels of moxifloxacin can be achieved in ocular tissues after ocular instillation of a single drop or more of moxifloxacin solution at or above 0.3%. Moxifloxacin exhibited better penetration than ofloxacin into ocular tissues with no significant systemic exposure.

Keywords: antibiotics/antifungals/antiparasitics • animal model • anterior chamber 
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