复方氨氯西林胶囊在健康志愿者中的药动学

Pharmacokinetics of ampicloxacillin capsule in Chinese healthy volunteers

目的研究在中国健康志愿者中口服复方氨氯西林胶囊的药动学。方法12名健康志愿者,按拉丁方设计随机分组,分别口服复方氨氯西林胶囊0.5,1.0和2.0 g,采用液相色谱串联质谱法检测给药后的血药浓度,DAS1.0软件计算药动学参数。结果健康受试者单剂量口服复方氨氯西林胶囊0.5,1.0,2.0 g,氨苄西林和氯唑西林药-时曲线符合一房室模型,权重采用I/C/C。氨苄西林主要药动学参数分别为t_(1/2)(0.99±s 0.15)、(1.03±0.15)、(1.2±0.3)h;AUC_(0～t)(18±4)、(31±10)、(44±11)mg·h·L^(-1)。氯唑西林主要药动学参数分别为t_(1/2)(1.1±0.3)、(1.12±0.27)、(1.08±0.14)h;AUC_(0～t)(2.3±0.6)、(5.1±1.1)、(10.2±2.0)mg·h·L^(-1)。氨苄西林和氯唑西林各剂量组药动学参数除c_(max)、AUC_(0～t)、AUC_(0～∞)外,t_(max)、t_(1/2)、Ke、MRT差异均无统计学意义,c_(max)、AUC_(0～t)、AUC_(0～∞)均与给药剂量呈线性相关(P<0.01)。结论12名健康受试者分别口服复方氨氯西林胶囊后,在0.5 g～2 g剂量范围内呈线性人体药动学特征。

AIM To study the pharmacokinetics of ampicloxacillin capsule in healthy Chinese volunteers. METHODS Twelve healthy volunteers were selected to administrate 0.5, 1.0, 2.0 g ampicloxacillin capsule respectively. The pharmacokineties parameters were calculate by DAS 1.0 software after the concentration of serum sample were determined by LC-MS-MS. RESULTS The comcentration-time curve of ampicillin and cloxacillin fit one-compartment model. Parameters of ampicillin were t1/2（0.99±s0.15）、（1.03±0.15）、（1.2±0.3）h;AUC0-1（18±4）、（31±10）、（44±11）mg·h·L^-1, respectively. Parameters of cloxacillin were t1/2（1.1±0.3）、（1.12±0.27）、（1.08±0.14）h;AUC0-1（2.3±0.6）、（5.1±1.1）、（10.2±2.0）mg·h·L^-1, respectively. There were no significance difference between different-dose groups of the two drugs in tmax, t1/2, Ke, and MRT. And there is linear correlation between c AUC0-1, AUC0-∞ with dose. CONCLUSION The concentration-time curve of twelve volunteers after single-dose of ampicloxacillin administration fits onecompartment model.