Li J T, Hou F, Lu H, Li T Y, Li H
Institute of Clinical Pharmacology, Beijing Medical University, China.
Drugs Exp Clin Res. 1997;23(5-6):145-50.
Pharmacokinetics of ME1207 were evaluated in 5 groups of healthy adult male volunteers given single preprandial administration of 100, 200 and 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 pharmacokinetic 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, respectively, indicating that the drug is not accumulated in the body. Within 24 hours after administration of 100, 200 and 300 mg, 19.93 +/- 5.20, 20.24 +/- 3.72 and 21.29 +/- 5.47%, respectively, of the dose were excreted into urine in an unchanged form.
在5组健康成年男性志愿者中评估了ME1207的药代动力学，这些志愿者分别接受了以下给药方式：空腹单次服用100、200和300毫克；餐后服用200毫克；以及连续7天每12小时服用200毫克。在空腹单次口服100、200和300毫克后，通过高效液相色谱法（HPLC）和生物测定法测定血药浓度。通过这两种方法测定的血清浓度和主要药代动力学参数（Cmax、Tmax、AUC和T1/2 Ke）具有可比性。餐后给药后通过生物测定法测定的Cmax和AUC大于空腹给药后测定的值。在每12小时重复服用200毫克、连续7天的给药过程中，每次给药后1.5小时和12小时测定的血药浓度分别始终约为2.5毫克/升和0毫克/升，这表明该药物在体内无蓄积。在服用100、200和300毫克后的24小时内，分别有19.93±5.20%、20.24±3.72%和21.29±5.47%的剂量以原形排泄到尿液中。
