头孢呋辛酯片人体生物等效性研究

Bioequivalence of Cefuroxime Axetil Tablets in Healthy Volunteer

目的评价头孢呋辛酯片在健康人体的相对生物利用度及生物等效性。方法受试者随机、自身双交叉、单剂量口服受试制剂或参比制剂500 mg,采用高效液相色谱法测定血浆中药物浓度,药代动力学参数采用DAS软件处理获得。结果两种制剂峰浓度(Cmax)分别为(5.58±1.95)μg/mL和(5.54±1.65)μg/mL,达峰时间(Tmax)分别为(2.03±0.97)h和(1.93±0.69)h,半衰期(t1/2)分别为(1.20±0.17)h和(1.19±0.13)h,0～t药时曲线下面积(AUC0-t)分别为(17.94±6.19)μg.h/mL和(17.37±4.73)μg.h/mL,0～∞药时曲线下面积(AUC0-∞)分别为(18.26±6.13)μg.h/mL和(17.64±4.66)μg.h/mL;相对于参比制剂,受试制剂的生物利用度为(106.54±40.59)%。受试制剂和参比制剂的Cmax,AUC0-t,AUC0-∞经对数转换后进行方差分析,两制剂间无显著性差异。结论浙江京新药业股份有限公司研制的头孢呋辛酯片与葛兰素史克制药(苏州)有限公司生产的头孢呋辛酯片具有生物等效性。

Objective To study the bioavailability and bioequivalence of the tested and reference Cefuroxime Axetil Tablets in healthy male volunteers.Methods According to the crossover design,each volunteer was orally given 100 mg Cefuroxime Axetil Tablets.The plasma concentrations were determined by HPLC.The pharmacokinetic parameters were obtained using DAS program.Results Cmax were（5.58± 1.95）μg/mL and（5.54±1.65）μg/mL,Tmax were（2.03±0.97）h and（1.93±0.69）h,t1/2 were（1.20±0.17）h and（1.19±0.13）h, AUC0-t were（17.94±6.19）μg·h/mL and（17.37±4.73）μg·h/mL,AUC0-∞were（18.26±6.13）μg·h/mL and（17.64± 4.66）μg·h/mL,respectively.The relative bioavailability was（106.54±40.59）%.The data of the reference and tested drugs were not different as shown by F test.Conclusion The results show that the two Cefuroxime Axetil Tablets made by two different corporations are bioequivalent.