头孢呋辛酯干混悬剂人体相对生物利用度研究  

Bioavailability of cefuroxime axetil suspension in healthy volunteers

作　　者：赵甘霖[1] 张强[1] 孙华东[1] 张大卫[1] 吕万良[1] 

机构地区：[1]北京大学药学院药剂学系,北京100083

出　　处：《中国药学杂志》2001年第9期609-611,共3页Chinese Pharmaceutical Journal

摘　　要：目的　考察头孢呋辛酯干混悬剂的人体相对生物利用度及生物等效性 ,从而评价其临床疗效。方法　本研究以市售的进口头孢呋辛酯片剂 (西力欣 )为对照 ,选用 2 0名健康志愿受试者 ,进行了随机的 2周期交叉实验。以HPLC测定血药浓度并计算药动学参数及生物利用度 ,进而对主要动力学参数进行统计学分析。结果　 2 0名受试者交叉po单剂量头孢呋辛酯干混悬剂和西力欣片 (2 5 0mg)后两者的主要药动学参数较接近 ,头孢呋辛酯干混悬剂的相对生物利用度 (F)达 92 .88%。主要参数的方差分析和双单侧t检验结果表明 ,头孢呋辛酯干混悬剂和西力欣片的AUC0～inf之间无显著性差异 (P >0 .0 5 ) ,91%置信区间在 81.6 %～ 97.2 %之间 ;两种制剂的cmax之间也无显著性差异 (P >0 .0 5 ) ,90 %置信区间为 93.6 %～ 12 1%。结论　头孢呋辛酯干混悬剂与西力欣片具生物等效性。OBJECTIVE To determine the bioavailability and b io equivalence of cefuroxime axetil suspension formulation in healthy adult male vo lunteers.METHODS In a randomized two-period crossover study ,20 healthy male volunteers received single 250 mg-dose of suspension and table t formulations of cefuroxime axetil,respectively,where the tablets were used as the reference.The serum concentrations of cefuroxime were determined by a specif ic high-performance liquid chromatographic (HPLC) method.The pharmacokinetic pa rameters of the two preparations and the relative bioavailability of suspensions after oral administration were calculated with statistical analysis. RESULTS Following oral administration of the two preparations,the mean AUC 0～inf values of the suspension and tablet formulations were (12.14 ±2.44) μg·h·mL -1 and (13.65±2.92) μg·h·mL -1,respectively;c max were (4.68± 1.34) μg·mL -1 and (4.44±1.36) μg·mL -1 ,respectively;t max were (1.30±0.40) h and (1.75±0.62) h,respective ly;MRT were (2.49±0.34) h and (3.01±0.81) h,respectively;t 1/2 were ( 1.07±0.22) h and (1.28±0.53) h,respectively.The relative bioavailability (F ) of cefuroxime axecil suspensions was 92.88%.Analysis of variance revealed th at there were no significant differences between the two preparations of cefurox ime axetil for the mean AUC 0～inf and c max (P>0.05).Two one-sided 't' test showed that 90% confidence intervals of the mean AU C 0～inf and c max of the suspensions compared with the tablets were over the range of 81.6%～97.2% and 93.6%～121%,respectively. CONCLUSION The suspensions and the tablets were bioequivalent.

关 键 词：头孢呋亲酯 相对生物利用度 生物等效性 高效液相色谱法 干混悬剂 

分 类 号：R978.11[医药卫生—药品] R969.1[医药卫生—药学]