摘要
目的研究注射用硫酸阿司米星(氨基糖苷类抗生素)多剂量给药在健康人体的药代动力学。方法 10名受试者恒速静脉滴注硫酸阿司米星200 mg,30 min,每日2次,间隔12 h,连续7 d。在第1 d和第7 d分别在不同时间取静脉血,收集尿样,给药第4～6 d采取谷浓度。用柱前衍生化-荧光HPLC法测定血药、尿药浓度。结果第1 d与第7 d主要药代动力学参数如下:Cm ax分别为(16.64±3.37),(17.61±2.72)mg.L-1;t1/2β分别为(2.47±0.85),(1.88±0.40)h;AUC0-t分别为(40.92±5.09),(43.61±5.46)mg.h.L-1;AUC0-∞分别为(41.66±5.48),(41.96±3.36)mg.h.L-1;MRT0-t分别为(2.55±0.40),(2.46±0.37)h;MRT0-∞分别为(2.78±0.55),(2.57±0.42)h;Vd分别为(10.92±2.85),(9.76±2.90)L;CL分别为(5.05±0.79),(4.99±0.46)L.h-1;12 h内原型药物经尿排泄累积百分比分别为(86.39±5.79)%和(86.09±8.52)%。第1 d与第7 d主要药代动力学参数比较差异均无统计学意义(P>0.05)。结论阿司米星多剂量连续给药以后第1 d和第7 d主要药代动力学参数结果相似,药物在体内无蓄积。
Objective To evaluate the pharmacokinetics of multiple dose of astromicin injection in Chinese healthy volunteers. Methods Ten male volunteers were administrated intravenously 200 mg of astromiein within 0. 5 h infusion, twice daily for 7 days. The blood and urine samples were collected at day 1 and day 7 respectively. At day 4 - 6, only collected blood sample before infusion. The concentrations of astromiein were determinated by preeolumn derivatization -fluorescence HPLC method. Results The main pharmaeokinetic parameters at day 1 and day 7 were as follows ： The Cmax were （ 16. 64 ± 3.37 ） and （ 17.61 ± 2.72） mg·L^-1; t1/2β were （2.47 ±0.85） and （1.88 ±0.40） h; AUC0-1 were （40.92 ±5.09） and （43.61 ±5.46） mg · h · L^-1; AUC0-1 were （41.66±5.48） and （41.96 ±3.36） mg·h · L^-1; MRT0-1,were （2.55 ± 0.40） and （2.46 ± 0.37） h;MRT0-∞ were （2.78±0.55） and （2.57±0.42） h; Va were （10.92 ±2.85） and （9.76±2.90） L; CLwere （5.05±0.79） and （4.99±0.46） L· h^-1, respectively. Urinary recovery rates were （86.39 ± 5.79 ）% and （86.09 ± 8.52 ） % , respectively. Conclusion The results showed that the main pharmacokinetic parameters of astromicin at day 1 and day 7 were similar. There was no accumulation in human body.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2011年第1期19-23,共5页
The Chinese Journal of Clinical Pharmacology
