国产与进口头孢呋辛酯片的人体生物等效性研究

Bioequivalence and Relative Bioavailability of domestic and imported Cefuroxime Axetil Tablets in Health Volunteers

目的：评价国产头孢呋辛酯片的生物等效性。方法：24名健康志愿者随机交叉，自身对照口服单剂量国产头孢呋辛酯片及进口头孢呋辛酯片各500 mg后，进行人体相对生物利用度以及生物等效性研究。服药间隔为1周。血药浓度测定采用微生物法。结果：受试头孢呋辛酯片及参比头孢呋辛酯片的实测平均达峰时间Tmax分别为2.23±0.33 h和2.13±0.54 h；平均峰浓度Cmax分别为3.97±0.55和4.16±0.67 mg·L-1；消除半衰期T1/2ke分别为1.14±0.13及1.15±0.15 h。血药浓度-时间曲线下面积AUC0-t分别为10.57±1.91及10.60±1.97 mg·h·L-1；受试药与参比药比较，相对生物利用度F为100.6±13.1%。Tmax 、Cmax 与AUC0-t经生物等效性检验（双向单侧t检验）P<0.05。结论：国产头孢呋辛酯片与进口参比头孢呋辛酯片相比，其人体相对生物利用度为100.6±13.1%，且两制剂具生物等效性。

OBJECTIVE: To study bioequivalence of cefuroxime axetil tablets. METHODS: The bioequivalence and relative bioavailability of a test domestic formulation of cefuroxime axetil in comparison with a reference imported formulation was investigated in a randomized 2-way cross-over study in 24 healthy volunteers following a single oral dose of 500 mg. The washout period is one week. A microbiological assay was used to determine the plasma levels of cefuroxime. RESULTS: The following pharmacokinetic parameters were derived from the individual plasma concentration time courses and the main parameters for test and reference formulations, Tmax were 2.23±0.33 h and 2.13±0.54 h, Cmax were 3.97±0.55 and 4.16±0.67 mg·L-1, T1/2ke were 1.14±0.13 and 1.15±0.15 h, AUC0-t were 10.57±1.91 and 10.60±1.97 mg·h·L-1, respectively. Compared with reference formulation, the relative bioavailability (F) of test formulation was 100.6±13.1%. The above parameters obtained from two formulations were compared by analysis of variance (ANOVA) and no significant difference was found. The bioequivalence of two formulations was found assessed by a two one-sided test(P<0.05). CONCLUSION: Therefore, from the results of this study it can be concluded that the test formulation is bioequivalent with the reference formulation.