TABLE 2

Pharmacokinetic parameters of morinidazole and its major metabolites after an intravenous administration of 50 mg/kg of morinidazole to control (n = 6) and 5/6 Nx (n = 11) rats

Data are expressed as mean ± S.D.

Pharmacokinetic ParametersMorinidazoleSulfate ConjugateGlucuronide Conjugates
M0M7M8-1M8-2
Control rats
 Cmax (μg/ml)48.2 ± 6.10.00928 ± 0.003370.0988 ± 0.01340.356 ± 0.087
 tmax (h)0.08 ± 0.000.46 ± 0.290.75 ± 0.271.00 ± 0.00
 t1/2 (h)1.16 ± 0.091.24 ± 0.340.94 ± 0.111.49 ± 0.28
 AUC0–t (μg·h/ml)87.2 ± 11.70.0164 ± 0.00760.257 ± 0.0371.12 ± 0.36
 AUC0–∞ (μg·h/ml)87.3 ± 11.70.0177 ± 0.00810.257 ± 0.0371.12 ± 0.36
 CL (ml/h/kg)582 ± 77
Vss (ml/kg)805 ± 71
 MRT (h)1.39 ± 0.121.75 ± 0.331.86 ± 0.222.21 ± 0.38
5/6 Nx rats
 Cmax (μg/ml)53.2 ± 3.5a0.0828 ± 0.0293b0.810 ± 0.680a4.25 ± 2.68c
 tmax (h)0.08 ± 0.000.82 ± 0.25a1.64 ± 0.50b1.91 ± 0.30b
 t1/2 (h)1.32 ± 0.08c1.88 ± 0.791.06 ± 0.08a1.28 ± 0.11
 AUC0–t (μg·h/ml)91.2 ± 8.70.211 ± 0.081b2.76 ± 2.36a15.7 ± 10.0c
 AUC0–∞ (μg·h/ml)91.3 ± 8.70.214 ± 0.081b2.76 ± 2.36a15.7 ± 10.0c
 CL (ml/h/kg)552 ± 50
Vss (ml/kg)891 ± 41c
 MRT (h)1.62 ± 0.12c2.13 ± 0.13a2.30 ± 0.19c2.65 ± 0.22c
  • AUC0–∞, area under the concentration-time curve from 0 hour to the infinite time; CL, total body clearance; Cmax, maximum plasma concentration; tmax, time to the Cmax. t1/2, apparent elimination half-life; MRT, mean residence time; VSS, volume of distribution at steady state.

  • a P < 0.05 compared with control.

  • b P < 0.001 compared with control.

  • c P < 0.01 compared with control.