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目的研究静脉滴注法罗培南在人体内的药动学特征。方法12名健康志愿者分成3组(每组男、女各2名),分别单剂量交叉静脉滴注法罗培南200、400和800 mg(用5%葡萄糖注射液稀释至250 mL,于45 min内静脉滴注完毕),采用高效液相色谱-紫外检测法测定血浆及尿液药物浓度。结果受试者血药浓度-时间数据用3p87软件拟合,符合一级消除的二房室模型。静脉滴注法罗培南200、400和800 mg主要药动学参数如下:ρmax(实测值)分别为(24±s 5)、(45±9)和(91±22)mg·L-1;t1/2α分别为(0.38±0.10)、(0.40±0.10)和(0.45±0.10)h;t1/2β分别为(1.31±0.26)、(1.41±0.27)和(1.48±0.28)h;Vc分别为(5.3±1.3)、(5.3±0.8)和(6.1±1.8)L;CL分别为(7.3±1.6)、(7.3±1.5)和(7.6±2.2)L·h-1;K10分别为(1.4±0.3)、(1.37±0.21)和(1.27±0.18)h-1;AUC0～12(以梯形法计算)分别为(30±7)、(59±12)和(116±29)mg.h·L-1。尿累积排泄率分别为(30±12)%、(30±13)%和(29±13)%。ρmax、AUC0～12和AUC0～∞在各剂量组间有非常显著差异(P<0.01),其他药动学参数组间无显著差异(P>0.05);800 mg剂量组的α1、t1/2α和K12在男、女健康受试者间有显著差异(P<0.05),其他药动学参数无性别间差异(P>0.05)。结论健康志愿者静脉滴注法罗培南200～800 mg后的体内过程呈线性特征。
Objective To study the pharmacokinetics of faropenem in human beings. Methods Twelve healthy volunteers were divided into 3 groups (2 in each group). Faropenem 200, 400 and 800 mg (diluted to 250 mL with 5% dextrose injection) Intravenous infusion is completed), using high performance liquid chromatography - UV detection of plasma and urine drug concentration. Results The plasma concentration-time data of the subjects were fitted with 3p87 software and fitted with a two-compartment model of primary elimination. The main pharmacokinetic parameters of faropenem at 200, 400 and 800 mg were as follows: ρmax (measured values) were (24 ± s 5), (45 ± 9) and (91 ± 22) mg · L -1; / 2α were (0.38 ± 0.10) and (0.40 ± 0.10) and (0.45 ± 0.10) h, respectively; t1 / 2β were (1.31 ± 0.26) and (1.41 ± 0.27) and (5.3 ± 1.3), (5.3 ± 0.8) and (6.1 ± 1.8) L, respectively; CL were 7.3 ± 1.6, 7.3 ± 1.5 and 7.6 ± 2.2 L · h- ± 0.3), (1.37 ± 0.21) and (1.27 ± 0.18) h-1, respectively; AUC0-12 (calculated by trapezoidal method) were (30 ± 7), (59 ± 12) and (116 ± 29) mg.h · L-1. Urine accumulated excretion rates were (30 ± 12)%, (30 ± 13)% and (29 ± 13)%, respectively. There was no significant difference in the other pharmacokinetic parameters (P> 0.05) between the groups of ρmax, AUC0 ~ 12 and AUC0 ~ ∞ (P <0.01) There was significant difference between K12 and K12 in male and female healthy subjects (P <0.05). There was no significant difference in other pharmacokinetic parameters (P> 0.05). Conclusion The in vivo process of faropenem in healthy volunteers after intravenous infusion of 200 ~ 800 mg is linear.