[Pharmacokinetics of norfloxacin and lomefloxacin in aqueous humour analysed by microdialysis].
The pharmacokinetics of norfloxacin (NFLX) and lomefloxacin (LFLX) in rabbit aqueous humour after instillation of 0.3% solution (20 microliters) and oral administration (20 mg/kg) were investigated by microdialysis. We also measured plasma concentration of fluoroquinolones after oral administration. After instillation, the maximum concentration (Cmax) of NFLX and LFLX in the aqueous humour was 0.80 and 1.20 micrograms/ml, and elimination half time (t1/2) was 130 and 96 min, respectively. After oral administration, the Cmax in plasma of NFLX and LFLX was 2.06 and 1.89 micrograms/ml, and the Cmax in aqueous humour was 0.16 and 0.62 microgram/ml, respectively. t1/2 of NFLX in aqueous humour and plasma was 225 and 295 min, and t1/2 of LFLX was 188 and 175 min, respectively. The ratio of aqueous humour/serum concentration of NFLX and LFLX was 7.8 and 35.3% 4 hrs after oral administration. These results suggest that, after instillation, LFLX penetrated better into the aqueous humour, and was eliminated faster, than NFLX, and that after oral administration, NFLX could not panetrate well into the aqueous humor from the blood.
Sato
H
H
Department of Ophthalmology, Showa University School of Medicine, Tokyo, Japan.
Fukuda
S
S
Inatomi
M
M
Koide
R
R
Uchida
N
N
Kanda
Y
Y
Kiuchi
Y
Y
Oguchi
K
K
D000818:Animals; D000890:Anti-Infective Agents / Q000493:pharmacokinetics*; D001082:Aqueous Humor / Q000378:metabolism*; D024841:Fluoroquinolones; D017551:Microdialysis; D009643:Norfloxacin / Q000493:pharmacokinetics*; D015363:Quinolones / Q000493:pharmacokinetics*; D011817:Rabbits
D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D015363:Quinolones; C053091:lomefloxacin; D009643:Norfloxacin