中国健康受试者单剂量静脉注射比阿培南的药代动力学

Pharmacokinetics of biapenem injection after a single dose administration in Chinese healthy subjects

目的研究中国健康受试者单剂量静脉注射比阿培南(碳青霉烯类抗生素)的药代动力学及安全性。方法 10名健康受试者分别静脉注射比阿培南300,600mg1h,于1周后交叉注射另一剂量,用高效液相色谱-紫外法测定血浆和尿液中比阿培南的浓度,用WinNonLin计算其主要药代动力学参数。结果 10名受试者分别单剂量使用比阿培南300和600mg后,比阿培南主要药代动力学参数:Cmax分别为(11.33±2.71)和(26.80±5.11)μg·mL-1;AUC0-tn分别为(18.01±4.66)和(42.78±8.81)μg·mL-1.h。结论中国健康受试者单剂量使用比阿培南后,在300～600mg内的体内过程呈线性药代动力学特征。

Objective To study the pharmacokinetics and safety in healthy volunteers following intravenous administration of biapenem. Methods Ten healthy volunteers were randomized to administer a single dose of biapenem at 300 and 600 rag, respectively. They were given the other dose after a week. The concentration of biapenem in human plasma and urine were determined by HPLC -UV. The main pharmacokinetic parameters were calculated with WinNonLin. Results The main pharmacokinetic parameters of biapenem after single doses of 300 and 600 mg were as follows： Cmax were （ 11. 33 ± 2. 71） and （26.80 ±5.11） ug .mL-1 ; AUC0-tn were（ 18.01 ±4.66） and（42.78 ± 8.81 ） ug .mL-1 h, respectively. Conclusion range of 300 -600 mg fit linear The process of biapenem in the dosage dynamic feature.