单剂量巴洛沙星片在健康人体的药代动力学

Pharmacokinetics of balofloxacin tablets after a single dose in healthy volunteers

目的研究巴洛沙星片(喹诺酮类抗生素)在健康志愿者体内的药代动力学。方法采用随机开放的三周期交叉试验设计,健康志愿者12例随机分成3组,分别单剂量交叉口服巴洛沙星100、200、400mg,以反相高效液相色谱法测定给药后不同时间点巴洛沙星的血浆浓度,血药浓度经DAS软件处理。结果巴洛沙星的主要药代动力学参数:Cmax分别为(0.93±0.30)、(1.97±0.60)、(3.54±0.83)mg.L-1,t1/2分别为(8.78±2.65)、(8.11±1.42)、(7.68±1.31)h,AUC0～t分别为(9.9±1.4)、(20.38±3.20)、(40.02±5.54)mg.h.L-1,AUC0～∞分别为(10.41±1.44)、(21.19±3.16)、(44.07±7.29)mg.h.L-1。结论单剂量口服巴洛沙星片,其消除半衰期t1/2与给药剂量无关;而Cmax、AUC0～t、AUC0～∞与剂量呈明显相关性,且随给药剂量的增大而增加。表明巴洛沙星在体内为线性动力学特征。

Objective To study the pharrnacokinetics of balofloxacin in healthy volunteers after oral administration. Methods Three different doses（ 100,200,400 mg） of balofloxacin was taken separately to 12 healthy volunteers in tri - cycle crossover for an open randomized three groups. The plasma concentration of balofloxacin after administration over time was determination by RP - HPLC. The tatistical analysis was taken out by application of DAS 2.0. Results The main pharmacokinetic parameter of the three groups （100,200,300 mg） were as follows： Cmax were （0.93 ± 0.30）, （ 1.97 ± 0.60）, （ 3.54 ± 0.83 ） mg · L ^- 1 ; t1/2 were （8.78 ±2.65） ,（8.11 ±1.42）, （7.68 ±1.31） h;AUC0-t were （9.9 ±1.4） ,（20.38 ±3.20）, （40.02 ±5.54） mg · h · L^-1;AUC0-∞ were （10.41 ±1.44）, （21.19±3.16）,（44.07 ±7.29）mg · h· L^-1. Conclusion During the metabolic process in a single dose after oral different doses administration in vivo, elimination half life has nothing with dosage. There is significatly dependability between Cmax, AUC0-t, AUC0-∞ and dosage ; Cmax , AUC0-t, AUC0-∞ are increased with the augmentation of administration, which indicates that dynamics of balofloxacin in vivo are linear.