巴洛沙星片人体药动学研究

目的:研究巴洛沙星片在健康人体内的药动学。方法:采用随机双交叉试验设计,12名健康志愿者口服巴洛沙星片100mg或200mg,用高效液相色谱法测定血、尿药物浓度,用DAS软件进行数据处理。结果:志愿者单剂量口服巴洛沙星片100、200mg的Cmax分别为(0.970±0.245)、(1.849±0.466)μg.mL-1,tmax分别为(1.25±1.10)、(1.24±0.81)h,t1/2分别为(7.14±1.01)(7.11±0.72)h,AUC0～36分别为(7.309±1.368)、(15.214±1.727)μg.h.mL-1,AUC0～∞分别为(7.531±1.386)、(15.695±1.762)μg.h.mL-1,36h尿平均累积排出率分别为(64.47±11.56)%、(63.24±11.93)%。结论:健康志愿者口服巴洛沙星具血药峰浓度高、半衰期长的良好药动学特点。本方法灵敏、准确、可靠、特异性强,可满足药动学研究需要。

Pharmacokinetics of Balofloxacin Tablets in Chinese Healthy Volunteers

OBJECTIVE：To study the pharmacokinetics of balofloxacin tablets in Chinese healthy volunteers.METHODS： A single dose of 100 or 200 mg balofloxacin tablets were given to 12 healthy volunteers in a randomized crossover design. Concentrations of balofloxacin in plasma and urine were determined by HPLC with data processed by DAS （drug and statistics） software.RESULTS： After administration of balofloxacin 100 mg and 200 rag, the Cmax were （0.970±0.245） μg · mL^-1 and （1.849±0.466） μg · mL^-1;the tmax were （1.25±1.10） h and （1.24±0. 81） h;the t1/2 were （7.14±1.01） h and （7.11±0.72） h; the AUC0-36 were （7.309 ± 1.368） μg· h· mL^-1 and （15.214 ± 1. 727） μg ·h·mL^-1; AUC0-∞ were （7. 531 ±1. 386） μg ·h· mL^-1 and （15.695 ± 1. 762） μg · h · mL^-1; the accumulative eliminating rates within 36 h in urine were （64.47 ± 11.56）% and （63.24± 11.93） %, respectively.CONCLUSION： The pharmacokinetics of balofloxacin in healthy volunteer after oral administration was characterized by high peak concentration and long half life.The method is sensitive, accurate, reliable and specific, and can satisfy the requirements for pharmaceutical study.