ABSTRACT
Objective To investigate the pharmacokinetics of cephapirin sodium in healthy volunteers.Methods Twelve healthy volunteers were enrolled and ad ministered with single doses of 0.5,1.0,4.0 g or multiple doses of 1.0 g cephapirin sodium injection by intravenous drip infusion.The concentrations of cephapirin in human plasma and urine were determined by HPLC-MS/MS.The main pharmacokinetic parameters were calculated with WinNonLin 6.3 software. Results The main pharmacokinetic parameters of cephapirin after single dose of 0.5,1.0,4. 0 g and 1.0 g multiple dose cephapirin sodium injection were as follows:Cmaxwere (34.86 ±6.93),(74.77 ±24.23),(319.0 ±44.5),(89.26 ±28.04)μg/mL,AUC0-twere (12.86 ±3.46),(28.31 ±7.46),(163.21 ±34.57),(27.30 ±7.22)μg/(mL·h),t1/2were (0.55 ±0.21),(0.72 ±0.22),(0.71 ±0.27), (0.72 ±0.25),accumulative urine excretion rate of 8 h(1 g)was (44.9 ±12.66)%.Conclusion The process of cephapirin in the dosage range of 0.5 ~4.0 g show linear dynamic feature.There is no accumulation after multiple dosing.Cephapirin sodium was much eli minated from urine in parent drug.
ABSTRACT
The practice of adding antibiotics to anterior chamber-irrigating solutions as a prophylaxis for endophthalmitis has been used recently.To evaluate corneal endothelial toxicity of different concentrations of antibiotics in irrigating solutions, rabbit corneas were mounted in the in-vitro dual-cham-bered specular microscope and the endothelium was perfused with glu-tathione-bicarbonate Ringer solution (GBR)containing antibiotics such as ofloxacin, vancomycin or cephapirin.Mate corneas were perfused with GBR alone and used as control.Corneal thickness was measured every 15 minutes throughout the perfusion period and corneal swelling rates were calculated. Swelling rates of corneas perfused with 2 /ml or 5 /ml ofloxacin, 60 microgram/ml or1 0 /ml vancomycin, and 10 /ml or 20 /ml cephapirin was not significantly different from that of control (p>0.05).The corneas perfused with 20 /ml cephapirin deswelled probably due to high osmolarity of it.Perfusion with 10 /ml vancomycin plus 5 /ml ofloxacin did not show corneal swelling compared to control (p>0.05).This study demonstrates that the above concentra-tions of antibiotics in irrigating solutions do not affect endothelial function of the rabbit cornea.