Journal of Pharmacobio-Dynamics
Online ISSN : 1881-1353
Print ISSN : 0386-846X
ISSN-L : 0386-846X
Ocular Pharmacokinetics of Latamoxef and Cefaclor in Rabbits. Penetration into Aqueous Humor
Teruaki KITAURASatsuki TSUKIAIShigeaki ARAIKatsushi MIYAKEMasahiko KIMURAHiroshi FUKUCHI
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Keywords: compartment model
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1988 Volume 11 Issue 10 Pages 694-699

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Abstract
Penetrations of latamoxef (LMOX) and cefaclor (CCL) into the aqueous humor after intravenous or oral administration were investigated in rabbits. Concentrations of antibiotics in plasma and aqueous humor after administration were determined periodically by microbiological assay. LMOX disappeared from plasma in a monoexponential manner with a half-life of 43 min after intravenous administraiton at a dose of 50 mg/kg. The maximum concentration of LMOX in aqueous humor (6.4 μg/ml) was observed 1 h after administration. When CCL was administered orally at a dose of 50 mg/kg, the maximum concentration of CCL in aqueous humor was 1.00 μg/ml 1.5 h after administration, whereas the maximum plasma concentration of 19.2 μg/ml was observed at 30 min. Pharmacokinetic analysis (simultaneous simulation) of plasma and aqueous humor concentration-time courses was made using the best fitted compartment model examined (modified two-compartment model). Prediction of the concentration of antibiotics in aqueous humor from the plasma concentration profile was also examined using the same compartment model in a separate experiment. The predicted concentration in aqueous humor was proved to coincide reasonably well with the measured concentration.
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© The Pharmaceutical Society of Japan
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