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Ocular penetration and pharmacokinetics of topical gatifloxacin 0.3% and moxifloxacin 0.5% ophthalmic solutions after keratoplasty.

Publication ,  Journal Article
Holland, EJ; Lane, SS; Kim, T; Raizman, M; Dunn, S
Published in: Cornea
April 2008

PURPOSE: To compare the corneal and aqueous penetration and pharmacokinetics of gatifloxacin 0.3% and moxifloxacin 0.5% ophthalmic solutions and their effect on corneal reepithelialization after penetrating keratoplasty. METHODS: In this randomized, open-label, parallel-controlled study, corneal and aqueous penetration and the pharmacokinetic parameters of topically applied gatifloxacin 0.3% and moxifloxacin 0.5% (2 preoperative doses of 1 drop given 5 minutes apart) were estimated by using a sparse sampling method. Corneal and aqueous samples were collected 0.25, 0.5, 1, or 2 hours after the final dose. The concentration was determined by a high-performance liquid chromatography method. Stromal Cmax:MBC50 (maximum drug concentration in serum to 50% minimum bactericidal concentration) ratios for selected ocular pathogens were also assessed. Postoperative corneal reepithelialization at days 1, 3, and 7 was evaluated and compared between groups. RESULTS: The calculated pharmacokinetic parameters were higher with moxifloxacin 0.5% than with gatifloxacin 0.3%. The stromal Cmax was 48.5 versus 15.7 microg/g (P = 0.04), and the stromal AUC0-2 (area under the concentration-time curve from 0 to 2 hours) was 30.9 versus 13.6 mug.h/g (P < 0.05). The endothelial Cmax was 76.1 versus 7.3 microg/g (P > 0.05), and the endothelial AUC0-2 was 43.9 versus 9.8 microg.h/g (P < 0.05). The aqueous Cmax was 0.9 versus 0.3 microg/mL (P > 0.05), and the aqueous AUC0-2 was 1.2 versus 0.4 microg.h/mL (P < 0.05). Stromal Cmax:MBC50 ratios were higher in the moxifloxacin 0.5% group for each pathogen tested. The corneal reepithelialization rates were comparable between groups. CONCLUSIONS: Topical preoperative moxifloxacin 0.5% achieved greater corneal and aqueous penetration than did gatifloxacin 0.3%. The clinical significance of this difference is not known. Postoperative use of these agents had similar effects on corneal reepithelialization.

Duke Scholars

Published In

Cornea

DOI

ISSN

0277-3740

Publication Date

April 2008

Volume

27

Issue

3

Start / End Page

314 / 319

Location

United States

Related Subject Headings

  • Wound Healing
  • Tissue Distribution
  • Quinolines
  • Ophthalmology & Optometry
  • Ophthalmic Solutions
  • Moxifloxacin
  • Middle Aged
  • Male
  • Keratoplasty, Penetrating
  • Humans
 

Citation

APA
Chicago
ICMJE
MLA
NLM
Holland, E. J., Lane, S. S., Kim, T., Raizman, M., & Dunn, S. (2008). Ocular penetration and pharmacokinetics of topical gatifloxacin 0.3% and moxifloxacin 0.5% ophthalmic solutions after keratoplasty. Cornea, 27(3), 314–319. https://doi.org/10.1097/ICO.0b013e3181608561
Holland, Edward J., Stephen S. Lane, Terry Kim, Michael Raizman, and Steven Dunn. “Ocular penetration and pharmacokinetics of topical gatifloxacin 0.3% and moxifloxacin 0.5% ophthalmic solutions after keratoplasty.Cornea 27, no. 3 (April 2008): 314–19. https://doi.org/10.1097/ICO.0b013e3181608561.
Holland, Edward J., et al. “Ocular penetration and pharmacokinetics of topical gatifloxacin 0.3% and moxifloxacin 0.5% ophthalmic solutions after keratoplasty.Cornea, vol. 27, no. 3, Apr. 2008, pp. 314–19. Pubmed, doi:10.1097/ICO.0b013e3181608561.

Published In

Cornea

DOI

ISSN

0277-3740

Publication Date

April 2008

Volume

27

Issue

3

Start / End Page

314 / 319

Location

United States

Related Subject Headings

  • Wound Healing
  • Tissue Distribution
  • Quinolines
  • Ophthalmology & Optometry
  • Ophthalmic Solutions
  • Moxifloxacin
  • Middle Aged
  • Male
  • Keratoplasty, Penetrating
  • Humans