注射用比阿培南健康人体连续给药药动学研究  

Pharmacokinetics of multiple-dose biapenam injection in Chinese healthy subjects

作　　者：朱燕[1] 吕媛[1] 魏敏吉[1] 张朴[1] 康子胜[1] 刘燕[1] 梁军[1] 张曼[1] 肖永红[1] 

机构地区：[1]北京大学第一医院临床药理研究所,北京100034

出　　处：《中国抗生素杂志》2016年第2期149-152,共4页Chinese Journal of Antibiotics

摘　　要：目的通过对比阿培南注射剂在中国健康人群中进行的连续给药药动学研究,进一步了解该药连续给药的药动学特点和可能产生的不良反应,为临床给药方案提供参考。方法采用开放试验设计,空腹给药的试验方法,在12名健康中国受试者(其中包括6名男性和6名女性)中连续7d静脉给予剂量为300mg的比阿培南注射液,每12h一次,并使用HPLC法测定给药后不同时间点的血、尿药物浓度。给药前、给药后分别进行各项指标的观察和检查。结果受试者连续7d静脉点滴300mg比阿培南注射液后第1天和第7天的主要药动学参数分别如下,C_(max)分别为(15.37±1.91)和(15.36±1.34)mg/L;T_(max)分别为(1.00±0.00)和(1.00±0.00)h;AUC_(0-t)分别为(26.55±2.90)和(24.68±1.51)mg·h/L;T_(1/2β)分别为(1.09±0.25)和(1.00±0.25)h;CL分别为(11.10±1.35)和(11.86±0.73)L/h;V_c分别为(7.20±2.64)L,24h尿排出率为57.6%。结论连续7d静脉给予比阿培南300mg药动学结果说明,药物在体内无蓄积,受试者耐受性良好。Objective To evaluate the pharmacokinetic of multiple dose of biapenem injection in Chinese healthy volunteers, to learn more about the drug pharmacokinetic characteristics and possible adverse reactions, To provide reference for the clinical dosage regimen. Methods 12 healthy volunteers （including six men and six women） were enrolled and an open, multiple-dose intravenously 300rag biapenem injection Q12h for 7days. The blood and urine samples were collected at day 1 and day 7 respectively. The concentrations of biapenem in serum and urine were determinated by HPLC method. Results The main pharmacokinetics parameters and day 1 and day 7 were as follows： Cax were （15.37±1.91）, （15.36±1.34）mg/L; Tax were （1.00±0.00）, （1.00 ±0.00）h; AUC（0.t） were （26.55±2.90）, （24.68±1.51） mg.h/L; T1/2β were （1.09±0.25）, （1.00±0.25）h; CL were （11.10±1.35）, （11.86±0.73）L/h and V were （7.72±3.82）, （8.30±3.21）L, respectively. Urinary recoveries were 57.6%. Conclusion The results showed that the main pharmacokinetics parameters of biapenem injection at day 1 and day 7 were similar. There was no accumulation in human body. All the subjects are well-tolerant.

关 键 词：比阿培南 药动学 连续给药 高效液相色谱法 

分 类 号：R978.1[医药卫生—药品]