论文部分内容阅读
目的:建立人血浆中哌拉西林钠/他唑巴坦钠浓度的HPLC检测法,研究哌拉西林钠他唑巴坦钠在人体中的药动学。方法:采用低、高2个剂量給药方案,单制剂双周期序贯试验设计,测定了12名健康受试者滴注注射用哌拉西林钠/他唑巴坦钠后不同时间内的血药浓度。结果:12名健康受试者静脉滴注45min注射用哌拉西林钠/他唑巴钠(规格:1.25g/支)1支后,哌拉西林钠(注射1.0g)的tmax和Cmax分别为(0.73±0.07)h和(74.8±19.9)mg·mL-1,AUC0-6为(103.4±29.2)mg·mL-1.h,AUC0-∞为(106.5±28.4)mg·mL-1.h,估算的t1/2(消除半衰期)为(1.2±0.6)h,清除率(CL)为(10.0±2.7)L.h-1;他唑巴坦钠(注射0.25g)的tmax和Cmax分别为(0.73±0.07)h和(14.5±2.9)mg·mL-1,AUC0-6为(20.7±3.9)mg·mL-1.h,AUC0-∞为(22.0±4.3)mg·mL-1.h,估算的t1/2为(1.7±0.8)h,CL为(11.8±2.2)L.h-1。12名健康受试者静脉滴注45min注射用哌拉西林钠/他唑巴钠(1.25g/支)2支后,哌拉西林钠(注射2.0g)的tmax和Cmax分别为(0.73±0.07)h和(152.9±24.2)mg·mL-1,AUC0-6为(220.8±47.1)mg·mL-1.h,AUC0-∞为(227.3±48.1)mg·mL-1.h,估算的t1/2为(1.2±0.6)h,清除率(CL)为(9.2±2.2)L.h-1;他唑巴坦钠(注射0.5g)的tmax和Cmax分别为(0.75±0.00)h和(31.2±5.2)mg·mL-1,AUC0-6为(47.5±8.2)mg·mL-1.h,AUC0-∞为(48.5±8.0)mg·mL-1.h,估算的t1/2(消除半衰期)为(0.98±0.17)h,CL为(10.6±1.8)L.h-1。结论:45min结束静脉滴注注射用哌拉西林钠/他唑巴坦钠的体内药动学与文献报道及国外的说明书相近。
OBJECTIVE: To establish a HPLC method for the determination of piperacillin / tazobactam sodium in human plasma and to study the pharmacokinetics of piperacillin-tazobactam sodium in human. Methods: The low and high dose dosing regimens were designed. The single-agent two-cycle sequential test design was used to determine the blood levels of different time after instillation of piperacillin / tazobactam sodium in 12 healthy volunteers Drug concentration. Results: The tmax and Cmax of piperacillin sodium (1.0g injection) in 12 healthy volunteers after intravenous infusion of piperacillin sodium / tazobactam (size: 1.25g / (0.73 ± 0.07) h and (74.8 ± 19.9) mg · mL-1, AUC0-6 was (103.4 ± 29.2) mg · mL-1.h and AUC0-∞ was (106.5 ± 28.4) mg · mL-1. h, the estimated t1 / 2 (elimination half-life) was 1.2 ± 0.6 h and the clearance rate was 10.0 ± 2.7 Lh-1. The tmax and Cmax of tazobactam sodium (0.25g injection) were (0.73 ± 0.07) h and (14.5 ± 2.9) mg · mL-1 respectively. The AUC0-6 was (20.7 ± 3.9) mg · mL-1.h and the AUC0-∞ was (22.0 ± 4.3) mg · mL-1. h, the estimated t1 / 2 was (1.7 ± 0.8) h, and the CL was (11.8 ± 2.2) Lh-1.12 healthy subjects received intravenous infusion of piperacillin / tazobactam (1.25 g / Branch), the tmax and Cmax of piperacillin sodium (2.0g injection) were (0.73 ± 0.07) h and (152.9 ± 24.2) mg · mL-1, respectively and the AUC0-6 was (220.8 ± 47.1) mg · ML-1.h and AUC0-∞ of (227.3 ± 48.1) mg · mL-1.h. The estimated t1 / 2 was 1.2 ± 0.6 h and the clearance rate was 9.2 ± 2.2 Lh- 1, tmax and Cmax were (0.75 ± 0.00) h and (31.2 ± 5.2) mg · mL-1, respectively, and AUC0-6 was (47.5 ± 8.2) mg · mL-1 for tazobactam sodium .h, AUC0-∞ was (48.5 ± 8.0) mg · mL-1. h, the estimated t1 / 2 (elimination half-life) was (0.98 ± 0.17) h, and CL was (10.6 ± 1.8) L · h-1. Conclusion: The in vivo pharmacokinetics of piperacillin / tazobactam sodium for intravenous injection after 45 min is similar to that reported in the literature and abroad.