法罗培南钠片剂在健康志愿者中药动学研究  

Evaluation of single dose pharmacokinetics of faropenem in healthy subjects

作　　者：周颖[1] 赵侠[1] 刘玉旺[1] 赵东方[1] 谢娟[1] 孙培红[1] 张慧琳[1] 崔一民[1] 

机构地区：[1]北京大学第一医院药剂科,100034

出　　处：《中国感染与化疗杂志》2007年第3期173-176,共4页Chinese Journal of Infection and Chemotherapy

摘　　要：目的研究健康志愿者单剂量口服法罗培南钠片剂的药动学特点。方法10名受试者在2个周期内分别空腹单剂量口服法罗培南钠片剂300mg、600mg，以高效液相色谱-紫外线（HPLC—UV）法测定其血液、尿液法罗培南浓度，并用Win-Nonlin专业版计算药动学参数。结果单次口服300mg、600mg法罗培南后的主要药动学参数AUC（0-x）分别为（7．612±3．296）和（15.539±7．395）mg·h／L，AUC（0-∞）分别为（7.737±3．328）和（15．716±7．368）mg·h／l，Cmax分别为（3．815±1．053）和（6.885±2．256）mg／L，Tmax分别为1．00和1．00h，t（1／2）分别为1．006和1．055h，CL／F分别为（46．980±22．247）和（46．996±22．475）L／h，V／F分别为（70．151±38.281）和（73．535±40.439）L。尿药浓度测定结果表明，法罗培南12h尿累积排出率分别为（5．96±3.15）和（4．35±1．48）％。结论法罗培南在300～600mg范围内Cmax和AUC随剂量呈比例增加，单剂量给药在健康人体耐受性良好。Objective This study was designed to evaluate the single dose pharmacokinetics of faropenem in healthy Chinese subjects. Methods Ten healthy volunteers received a single dose of faropenem 300 or 600 mg in an open randomized crossover study. The concentrations of faropenem in plasma and urine were measured by HPLC-UV method. The serum concentrationtime data were individually analyzed by WinNonlin. Results The results showed that AUC（0-dast） were （7. 612 ± 3. 296） and （15. 539 ± 7. 395） mg · h/L following oral administration of 300 and 600 mg faropenem. AUC（0-∞） was （7. 737 ± 3. 328） and （15. 716±7.368） mg. h/L. Cmax was （3. 815 ± 1. 053） and （6. 885±2.256） mg/L. Tmax was 1.00andl. 00h. The T1/2 was 1. 006 和 1. 055 h. CL/F was （46. 980± 22. 247） and （46. 996 ± 22. 475） L/h. V/F was （70. 151 ± 38. 281） and （73. 535 ± 40. 439） L. Urinary recovery was （5.96 ± 3.15）% and （4. 35 ± 1.48） % of two doses, respectively. Conclusions Faropenem was well tolerated following single dose in healthy volunteers. Cmax and AUC increase approximately proportional to dose of faropenem from 300 mg to 600 mg.

关 键 词：法罗培南 高效液相色谱-紫外线法 药动学 

分 类 号：R96[医药卫生—药理学]