头孢克肟颗粒和胶囊在健康人体的生物等效性

目的：评价健康受试者单剂量口服头孢克肟颗粒和胶囊剂人体药动学与生物等效性.方法：按照三制剂三周期交叉试验设计,24位健康志愿受试者交叉口服头孢克肟试验颗粒、头孢克肟试验胶囊或对照药胶囊各200 mg.采用HPLC/MS/MS法测定血浆中头孢克肟的血药浓度,对三种制剂进行生物等效性评价.结果：受试颗粒、胶囊剂和参比胶囊药动学参数：Cmax分别为（4 003.04±177;2 015.76）、（3 673.04±177;2 056.62）和（3 654.35±177;1 91.03）μg·L^-1; tmax分别为（3.46±177;0.81）、（3.74±177;1.35）、（3.57±177;0.41）h;t1/2分别为（3.96±177;0.88）、（4.47±177;1.26）和（3.95±177;0.91）h; AUC0→24分别为（30 860.92±177;13 372.82）、（28 155.24±177;12 893.08）和（27 401.47±177;12 222.24 ）μg·h·L^-1;AUC0~∞分别为（31 555.52±177;13 564.27）、（29 111.76±177;13 058.72）、（27 960.22±177;12 255.11）μg·h·L^-1.试验颗粒、胶囊AUC0→24、AUC0→∞、Cmax的90%可信区间均落在相应参比药范围内.tmax经非参数检验,在不同制剂间差异无统计学意义.受试颗粒、胶囊剂相对于参比胶囊的生物利用度分别为（115.8±177;31.2）%和（105.5±177;23.0）%.结论：头孢克肟受试颗粒及胶囊与参比胶囊具生物等效性.

Bioequivalence of Cefixime Granules and Capsules in Chinese Healthy Volunteers

Objective： To evaluate the bioequivalence and pharmacokinetics of cefixime granules and capsules in Chinese healthy volunteers. Methods： An open randomized, three periods cross over study was adopted recruiting 24 healthy male volunteers. Each volunteer was randomly administered a single oral dose of 200 mg cefixime （ test or reference samples）. The plasma concentration of cefixime was determined by HPLC-MS/MS. Non-compartment model was used in the analysis of pharmacokihetic parameters. Log- arithm-transformed C and AUC were analyzed by the analysis of variance and 90% confidence intervals. Results： Cmax of the test ce- fixime granules, capsules and the reference capsules was （4 003.04±177;2 015.76）、（3 673.04±177;2 056.62）和（3 654.35±177;1 91.03）μg·L^-1, respectively, and t was （3.46±177;0.81）、（3.74±177;1.35）、（3.57±177;0.41）h and （ 3.57 ± 0.41 ） h, respectively. T1/2 was （ 3.96 ± 0.88）, （4.47 ± 1.26） and （3.95 ±0.91 ） h, respectively. AUCo→24 was （30 860.92 ± 13 372.82）, （28 155.24 ± 12 893.08） and （27 401.47 ± 12 222.24） μg·h·L^-1, respectively. AUCo→∞ was（31 555.52 ± 13 564.27）, （29 111.76 ± 13 058.72） and （27 960.22 ± 12 255.11 ） μg·h·L^-1, respectively. Conclusion： The test cefixime granules and capsules are both bioequivalent with the reference capsules.