1. Organization for State Drug Clinical Trial�� Yijishan Hospital�� Wannan Medical College�� Wuhu 241001�� China��2. Center of Drug Metabolism and Pharmacokinetics�� China Pharmaceutical University�� Nanjing 210009�� China
Abstract��
ABSTRACT: OBJECTIVE To study the tolerability�� safety and pharmacokinetics of (S-ornidazole after ascending intravenous infusion doses in healthy Chinese volunteers. METHODS 40 Healthy male and female Chinese volunteers were randomized into 1 (male-female=1��1 of 4 treatment groups to receive a single dose of 500�� 1 000�� 1 250 or 1 500 mg (S-ornidazole�� respectively. Multiple doses (500 mg bid of (S-ornidazole were administered for 5 consecutive days after a 2-week washout period of 500 mg single-dose (S-ornidazole. A single dose of 1 000 mg (R��S-ornidazole was administered as the positive control after a 2-week washout period of 1 000 mg single-dose (S-ornidazole. Adverse events were observed and (S-ornidazole concentrations in plasma were determined using HPLC-UV. The major pharmacokinetic parameters were calculated by BPSS2.0. RESULTS The incidence rates of adverse reactions after single-dose intravenous infusion of 500�� 1 000�� 1 250�� and 1 500 mg (S-ornidazole were 0/9�� 0/10�� 0/10�� and 2/10�� respectively�� and 3/10 following multiple doses of 500 mg (S-ornidazole and 5/10 following a single dose of ornidazole. The main pharmacokinetic parameters of single-dose (S-ornidazole 500�� 1 000�� 1 500 mg or multiple-dose 500 mg were as follows: ��max ��8.63��2.57�� ��18.6��4.08�� ��27.5��10.6�� ��23.4��4.67 mg��L-1�� respectively. AUC0-60 ��109.5 �� 24.0�� ��293.06��69.9�� ��422.9��84.0�� ��412.3��99.4 mg��h��L-1�� respectively. CONCLUSION (S-ornidazole was well tolerated in Chinese healthy volunteers after single-dose intravenous infusion of 500 to 1 500 mg and multiple-dose of 500 mg. The pharmacokinetics is linear over the range of 500 to 1 500 mg with accumulation after multiple doses of 500 mg.
.Tolerability�� Safety and Pharmacokinetics of (S-Ornidazole in Ascending Dose Study in Healthy Chinese Volunteers[J] Chinese Pharmaceutical Journal, 2011,V46(6): 454-457
2011, Vol. 46 
