【摘要】 目的研究单剂口服吉米沙星在中国健康志愿者中的药动学特性,为制订用于中国人的安全有效的给药方案提供依据。方法12名受试者随机、开放、3交叉单剂空腹口服吉米沙星片剂160mg、320mg和480mg。以高效液相色谱(HPLC)-荧光法测定血、尿样中吉米沙星药物浓度。应用Winnonlin分析软件计算药动学参数。结果受试者单剂空腹口服吉米沙星160mg、320mg和480mg后体内过程均符合非房室模型,平均血清Cmax分别为(0.70±0.19)mg/L、(1.40±0.32)mg/L和(1.84±0.35)mg/L;Tmax中位数分别为1(0.5,2)h、1(0.5,2)h和1.25(1,2)h;平均t1/2分别为(7.06±1.22)h、(7.02±0.94)h和(7.28±0.81)h;平均AUC0-24h分别为(3.86±0.56)mg.h/L、(7.61±0.93)mg.h/L和(11.47±1.68)mg.h/L;平均AUC0-∞分别为(4.01±0.57)mg.h/L、(7.71±0.92)mg.h/L和(11.62±1.72)mg.h/L;平均Vd分别为(411.45±77.88)L、(423.47±59.48)L和(439.21±55.55)L;平均CLt分别为(40.71±6.22)L/h、(42.10±5.46)L/h和(42.26±7.14)L/h;给药后48h内平均累积尿排出率分别为(38.95±6.14)%、(37.84±6.62)%和(35.57±5.07)%。结论中国健康受试者单次空腹口服吉米沙星160～480mg结果显示其符合线性药动学的特性,消除半衰期长。给药量的约40%以原形药物经肾排出。更多还原

【Abstract】 Objective To investigate the pharmacokinetics of gemifloxacin in healthy Chinese subjects in order to provide rationale for developing safe and effective clinical dosage regimen in Chinese patients.Methods Twelve subjects were enrolled in an open label,3-period,single oral dose,cross-over pharmacokinetic study. The subjects sequentially took 3 doses of gemifloxacin (160 mg,320 mg and 480 mg) according to the randomization schedule. The concentrations of gemifloxacin in serum and urine were determined by high performance liquid chromatogram (HPLC). The pharmacokinetic parameters were analyzed by Winnonlin software.Results The pharmacokinetic courses following single crossover oral dose of 160 mg,320 mg and 480 mg gemifloxacin were all consistent with the non-compartment model. The means of C max were (0.70±0.19) mg/L,(1.40±0.32) mg/L and (1.84±0.35) mg/L,respectively. The medians of T max were 1 (0.5,2) h,1 (0.5,2) h and 1.25 (1,2) h,respectively. The means of t 1/2 were (7.06±1.22) h,(7.02±0.94) h and (7.28±0.81) h,respectively. The means of AUC 0-24 h were (3.86±0.56) mg·h/L,(7.61±0.93) mg·h/L and (11.47±1.68) mg·h/L,respectively. The means of AUC 0-∞ were (4.01±0.57) mg·h/L,(7.71±0.92) mg·h/L and (11.62±1.72) mg·h/L,respectively. The means of V d were (411.45±77.88) L,(423.47±59.48) L and (439.21±55.55) L,respectively. The means of CL t were (40.71±6.22) L/h,(42.10±5.46) L/h and (42.26±7.14) L/h,respectively. The means of accumulative urinary excretion at 48 hours post dosing were (38.95±6.14)%,(37.84±6.62)% and (35.57±5.07)%,respectively. Conclusions The results indicate that pharmacokinetic courses following single oral dose of 160 mg,320 mg and 480 mg gemifloxacin are linear. The half-life is long. Gemifloxacin is partly excreted from kidney. About 40% of the dosage is recovered in the urine at 48 hours post dosing.更多还原