摘要
目的:研究健康受试者单剂量静脉滴注比阿培南后的药动学特征。方法:30名健康受试者单剂量静脉滴注比阿培南300,600,900mg(各剂量组n=10)后,HPLC法测定其血浆中药物浓度,采用药动学软件DAS进行数据处理计算药动学参数。结果:比阿培南静脉滴注给药后药时曲线符合二室开放模型,低、中、高给药剂量主要药动学参数t1/2分别为(1.23±0.24),(1.1±0.3),(1.02±0.27)h,AUC0-t分别为(40.7±13.5),(77.2±22.1),(129.3±47.5)mg.h.L-1,AUC0-∞分别为(44.8±17.6),(80.1±25.1),(136.6±49.7)mg.h.L-1,CLs分别为(7.6±2.2),(8.1±1.8),(7.9±1.9)L.h-1。结论:受试者静脉滴注比阿培南后,人体耐受性良好,主要药动学参数(AUC0-t)与给药剂量呈良好线性关系,提示比阿培南人体药动学过程为线性动力学过程,其他参数t1/2、CLs经t检验差异均无显著性(P>0.05)。
OBJECTIVE To study the pharmacokinetics of biapenem after intravenous in single dose in Chinese healthy volunteers. METHODS A .single dose of 300 mg （n = 10）, 600 mg （n = 10） and 900 mg （n = 10） biapenem were administratered intravenously in 30 volunteers. Concentration of biapenem in plasma was determined by HPLC and the pharmacokinetics pa- rameters were calculated by DAS software. RESULTS The concentration-time data after single dose of 300, 600, 900 mg biapenem conformed to a two - compartment open model. The main pharmacokinetics parameters t1/2 were （1.23 ± 0. 24）, （1.1 ± 0. 3） and （ 1.02 ± 0. 27） h, respectively; AUG）, were （40. 7 ± 13.5 ）, （77. 2 ± 22. 1 ）, （ 129. 3± 47. 5 ）mg · h · L ^-1 , respectively; AUC0-∞ were （44. 8 ±17. 6）, （80. 1 ± 25. 1 ）, （ 136.6 ± 49.7） mg·h· L^-1 , respectively; CLs were （7. 6 ±2. 2）, （8. 1 ± 1.8）, （7. 9±1.9）L·h ^-1 , respectively. CONCLUSION Biapenem intravenous administration in single dose was well tolerated in all volunteers. Pharmacokinetics study results suggested that the pharmacokinetics parameters （AUC0-t ） of the drug in the dosage range of 300-900 mg in human body nearly fit linearly to the dosage, for other pharmacokinetics parameters （t1/2, CLs）, there were no significant differences by t test （P〈0. 05）.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2010年第15期1286-1288,共3页
Chinese Journal of Hospital Pharmacy
