单次静滴头孢呋辛在肾功能不全患者的药代动力学  

Pharmacokinetics of cefuroxime in patients with renal failure after a single dose intravenous

作　　者：陈玮[1] 李德天[1] 刘霞[2] 刘冠[2] 吕媛[3] 单爱莲[3] 

机构地区：[1]中国医科大学附属盛京医院国家药品临床研究基地,沈阳110004 [2]沈阳华泰药物研究有限公司,沈阳110015 [3]北京大学临床药理研究所,北京100191

出　　处：《中国临床药理学杂志》2010年第5期339-343,共5页The Chinese Journal of Clinical Pharmacology

摘　　要：目的研究肾功能不全患者单次静滴头孢呋辛(抗生素)的药代动力学。方法 20名肾功能不全受试者按照CKD分期分成2组:CKD1-3期组与CKD4-5期组,分别静脉滴注头孢呋辛1000mg后,采用高效液相色谱法,测定不同时刻血浆中头孢呋辛的血药浓度,用DAS2.0版软件计算主要药代动力学参数。同时,测定不同时间段的尿药浓度,计算尿药累积排泄率。结果 2组受试者静脉滴头孢呋辛1000mg后,血浆中头孢呋辛的Cmax分别为(65.06±31.20),(79.33±10.75)μg·mL-1;t1/2分别为(2.42±0.87),(8.58±4.14)h;AUC(0-t)分别为(154.70±81.10),(446.43±95.37)μg.h.mL-1;AUC(0-∞)分别为(162.10±92.64),(798.65±362.83)μg.h.mL-1;CLz分别为(7.68±3.19),(1.45±0.52)mL.min-1;Vz分别为(24.53±9.71),(15.42±3.91)L。12h尿药累积排泄率分别为(39.08±7.86)%,(16.67±5.57)%。结论肾功能不全受试者静脉滴注头孢呋辛后,CKD4-5期患者较CKD1-3期,t1/2明显延长,AUC(0-t)及AUC(0-∞)明显增加;而CLz、Vz及12h尿药累积排泄率均明显降低。Objective To investigate the pharmacokinetics of cefuroxime after a single dose intravenous in different stages renal failure. Methods Twenty subjects were divided into two groups according to CKD stages （CKD 1 -3 group; CKD 4 -5 group）. The plasma cefuroxime concentrations after intravenous administration 1000 mg were determined by HPLC method . Drawing blood concentration - time curve and according to the plasma concentration - time data we calculated the main pharmacokinetic parameters by DAS 2. 0 software. At the same time, urine samples were collected at different intervals and measured urine drug concentration to calculate the cumulative urine excretion rate.Results The main pharmacokinetic parameters of two groups were as follows：Cmax were （65.06 ± 31.2） and （79.33 ± 10. 75 ） μg · mL^-1 ; t1/2 were （2.42 ±0. 87） and （8.58 ±4. 14） h; AUC（0-t） were （ 154.70 ±81.10） and （446.43 ±95.37） μg · h · mL^-1; AUC（0-∞） were （162. 10±92.64） and （798.65 ±362.83） μg · h · mL^-1; CLz were （7.68 ±3.19） and （1.45 ±0.52） mL · min^-1; Vz were （24.53± 9.71 ） and （ 15.42 ±3.91 ） L, respectively. Cumulative 12 h urine excretion accounted for （39.08±7.86）% and （16.67 ± 5.57）%.Conclusion In patients with CKD 4 -5 compare d with CKD 1 -3 the t1/2 was obviously prolonged , AUC（0-t） and AUC（0-∞） was significantly increased, but CLz and VZ was significantly decreased , cumulative 12 h urine excretion was significantly decreased.

关 键 词：头孢呋辛 药代动力学 高效液相色谱法 

分 类 号：R969.1[医药卫生—药理学] R978.1[医药卫生—药学]