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NR. 3(I)/2004
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Corneal penetration
of topical fluoroquinolones: Aqueous humour concentrations after
application of levofloxacin 0.5% and ofloxacin 0.3% eye drops
Hans-Reinhard Koch1,
Sven C. Kulus1, Markus Roessler1, Auli
Ropo2, Klaus Geldsetzer3
1Hochkreuzklinik Eye Hospital, Bonn, Germany,
2Santen Oy, Clinical Research, Helsinki, Finland,
3Santen GmbH, Germering, Germany |
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| Summary: |
Purpose: To
investigate the penetration of topically applied
levofloxacin 0.5% and ofloxacin 0.3% eye drops into the
aqueous humour of patients undergoing cataract surgery.
Methods: In this randomized, investigator-masked
study, 69 patients received four drops of either
levofloxacin 0.5% or ofloxacin 0.3% eye drops within one
hour (at 60 min, 45 min, 30 min and 15 min) prior to
elective cataract surgery. Aqueous humour samples of at
least 50µl were drawn from the anterior chamber at the
beginning of the cataract operation. Fluoroquinolones
concentrations in anterior chambers were measured using
high performance liquid chromatography (HPLC). In order
to exclude a dilution effect of the anterior chamber
(AC), they were related to the AC volumes (measured by
3D-modelling of central Orbscan slit image photos) and
AC depths (measured by ultrasound).
Results: The mean concentration of levofloxacin
(1139.9 ng/ml, SD 717.1) in the aqueous humour was
significantly higher (p=0.0008) than that of ofloxacin
(621.7 ng/ml , SD 368.7). The aqueous humour
concentrations correlated negatively with the measured
volumes and anterior chambers depths.
Conclusions: The new fluoroquinolone,
levofloxacin, is better soluble in water enabling the
use of higher drug concentrations (0.5%) compared to
other currently available fluoroquinolone eye drops
(0.3%). This study shows that the concentration reached
in the anterior chamber with levofloxacin eyedrops is
about 2-fold higher when compared to that reached with
ofloxacin eye drops. The concentration of the
antibacterial isomer is approximately 3.5 to 4 times
higher when levofloxacin is administered, assuming
negligible stereo-selective uptake. |
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