国产舒他西林片在健康人体内的药动学及相对生物利用度

Relative bioavailability and pharmacokinetics of domestics sultamicillin tablets in volunteers

目的:在8名健康志愿者体内研究了国产舒他西林片和对照片的药动学和生物利用度。方法:受试者交叉口服单剂量(750 mg)国产片和进口片后，采用高效液相色谱法检测血药浓度。结果:国产片和对照片中两种成分的主要药动学参数分别为：舒巴克坦Cmax为(5.6±0.8) μg·ml^（-1）和(6.1±1.3) μg·ml^（-1）；Tmax为(0.98±0.25) h和(0.91±0.19) h；AUC为(12.8±1.8) mg·h·L^（-1）和(13.1±2.4) mg·h·L^（-1）；其国产片相对生物利用度F为(98.3±10.6)%。氨苄西林Cmax为(7.9±1.2) μg·ml^（-1）和(8.1±1.1) μg·ml^（-1），Tmax为(0.97±0.28) h和(0.84±0.33) h；AUC为(17.5±1.8) mg·h·L^（-1）和(17.1±1.0) mg·h·L^（-1），其国产片相对生物利用度F为(102.2±8.5)%。结论:两种剂型的两种组分的各药动学参数之间差异均无显著性(P＞0.05))，经双向单测t检验，两制剂具生物等效性。

OBJECTIVE：The pharmacokinetics and bioavailability of sultamicillin tablets were compared with those of imported product Unasyn tablet. METHODS：Plasma levels of ampicillin and sulbactam were detected by HPLC UV method. RESULTS：The parameters of the two formulations for sulbactam: C maxof domestic and imported tablets were (5.6±0.8) μg·ml-1 and (6.1±1.3) μg·ml-1； T max(0.98±0.25) h and (0.91±0.19) h； AUC (12.8±1.8) mg·h·L-1and (13.1±2.4) mg·h·L-1 respectively.The relative bioavailability of domestic capsule was (98.26±10.61)%.The parameters of domestic and Unasyn tablets for ampicillin were C max (7.9±1.2) μg·ml^(-1) and (8.1±1.1) μg·ml^(-1)， T max (0.97±0.28) h and (0.84±0.33) h； AUC (17.5±1.8) mg·h·L^(-1) and (17.1±1.0) mg·h·L-1.The relative bioavailability of domestic tablets was (102.20±8.47)%CONCLUSIONS：There was no significant difference between pharmacokinetic parameters for domestic and imported tablets.It was demonstrated that the two preparations were bioequivalent by one two sided tests.