Grepafloxacin concentration in ocular tissues after intravenous infusion in rabbits with intraocular inflammation.
OBJECTIVE
To determine the penetration of grepafloxacin into ocular tissues during experimental ocular inflammation.


METHODS
10 albino and 10 pigmented rabbits underwent a continuous intravenous infusion of the drug 24 h after injecting Salmonella typhimurium toxin intravitreously, creating ocular inflammation. The animals were killed and grepafloxacin levels were determined in plasma and ocular tissues using high performance liquid chromatography.


RESULTS
Grepafloxacin levels achieved a steady-state plasma concentration of 1.5 microg/ml. The drug diffused more towards vascularized tissues (chorioretina and iris) in both albino and pigmented rabbits with a tissue/serum ratio higher than 1. Grepafloxacin showed more affinity to pigmented tissue, rising levels of 40,000-50,000 ng/g in the chorioretina and iris in pigmented animals. After inflammation, grepafloxacin intraocular penetration increased in albino animals with levels exceeding the minimum inhibitory concentration for the most common ocular pathogens.


CONCLUSIONS
Grepafloxacin intraocular penetration is higher in pigmented tissues. Ocular inflammation increases the drug penetration into the vitreous.
Pérez-Oliván
S
S
Department of Ophthalmology, University Hospital Miguel Servet, Zaragoza, Spain. sperezo@able.es
Pinilla
I
I
Bregante
M A
MA
Solans
C
C
Ruiz Moreno
O
O
Garcia
M A
MA
Honrubia
F M
FM
D000818:Animals; D000890:Anti-Infective Agents / Q000493:pharmacokinetics*; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D009877:Endophthalmitis / Q000378:metabolism* / Q000382:microbiology; D015818:Eye Infections, Bacterial / Q000378:metabolism* / Q000382:microbiology; D005260:Female; D024841:Fluoroquinolones / Q000493:pharmacokinetics*; D007262:Infusions, Intravenous; D010879:Piperazines / Q000493:pharmacokinetics*; D011817:Rabbits; D012481:Salmonella Infections, Animal / Q000378:metabolism* / Q000382:microbiology; D012486:Salmonella typhimurium / Q000502:physiology; D014018:Tissue Distribution
D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D010879:Piperazines; C075375:grepafloxacin