PHASE-I CLINICAL-TRIAL OF CEFDITOREN PIVOXIL (ME-1207) - PHARMACOKINETICS IN HEALTHY-VOLUNTEERS

Pharmacokinetics of ME1207 were evaluated in 5 groups of healthy adult male volunteers given single preprandial administration of 100, 200 a nd 300 mg; postprandial administration of 200 mg; and, administration of 200 mg every 12 h for 7 consecutive days. Blood drug concentrations were determined by HPLC and bioassay after oral single administration of 100, 200 and 300 mg before meals. Serum concentrations and major p harmacokinetic parameters (Cmax, Tmax, AUC and T1/2 Ke) determined by these two methods were comparable. Cmax and AUC determined by bioassay after postprandial administration were greater than those determined after preprandial administration. Blood concentrations determined 1.5 and 12 h after each administration, during repeated administration of 200 mg every 12 hours for 7 days, were always about 2.5 and 0 mg/l, re spectively indicating that the drug is not accumulated in the body Wit hin 24 hours after administration of 700, 200 and 300 mg, 19.93+/-5.20 , 20.24+/-3.72 and 21.29+/-5.47%, respectively, of the dose were excre ted into urine in an unchanged form.