头孢呋辛酯干混悬剂人体相对生物利用度研究

 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20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 20名受试者交叉po单剂量头孢呋辛酯干混悬剂和西力欣片(250 mg)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AUC_0～inf之间无显著性差异(P＞0.05)，91%置信区间在81.6%～97.2%之间；两种制剂的c_max之间也无显著性差异(P＞0.05)，90%置信区间为93.6%～121%。结论 头孢呋辛酯干混悬剂与西力欣片具生物等效性。

Bioavailability of cefuroxime axetii suspension in healthy volunteers

OBJECTIVE To determine the bioavailability and bioequivalence of cefuroxime axetil suspension formulation in healthy adult male volunteers.METHODS In a randomized two-period crossover study,20 healthy male volunteers received single 250 mg-dose of suspension and tablet formulations of cefuroxime axetil,respectively,where the tablets were used as the reference.The serum concentrations of cefuroxime were determined by a specific high-performance liquid chromatographic (HPLC) method.The pharmacokinetic parameters 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,respectively;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 that there were no significant differences between the two preparations of cefuroxime 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 AUC_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.