Abstract��
OBJECTIVE:To compare the difference of the pharmacokinetics of intravenous tinidazole and metronidazole in men and to provide a scientific basis for clinical application. METHODS:Six healthy male volunteers were given 400 mg tinidazole or metronidazole by injection intravenously within 30 minutes in a crossover study.The drug concentrations in plasma were determined by HPLC.The parameters of pharmacokinetics were calculated with 3P87 pharmacokinetic program. RESULTS:The mean peak concentrations of tinidazole and metronidazole were (11.92��0.67) and (12.65��0.71) mg��L-1respectively.The concentrations of tinidazole were significantly higher than those of metronidazole from 4 h onwards after injection.Tinidazole maintained effective concentration in blood about 24 h.Conversely,metronidazole kept that about 4 h.The mean elimination t1/2beta was (14.78��0.57) h of tinidazole and (9.55��0.47) h of metronidazole,AUC were (180.6��8.8) and (117.7��9.5) mg��h��L-1,the volume of distribution were (28.5��4.74) and (23.0��2.49) L,and the clearance were (2.22��0.11) and (3.42��0.28) L��h-1,respectively.There was significant difference in these pharmacokinetic parameters between tinidazole and metronidazole. CONCLUSION:Regarding the pharmacokinetics of tinidazole,it can be used as the once daily therapeutic regimen.
2000, Vol. 35 
