静脉滴注头孢哌酮/他唑巴坦复方制剂的健康人体药动学

Pharmacokinetics of Cefoperazone/Tazobactam in Healthy Volunteers After an Intravenous Administration

目的研究静脉滴注头孢哌酮/他唑巴坦复方制剂在健康人体内的药动学。方法16名健康男性志愿者静脉滴注头孢哌酮2000mg/他唑巴坦500mg复方制剂,采用反相高效液相色谱法同时测定血浆中头孢哌酮和他唑巴坦浓度,并用DAS1.0程序处理药-时数据。结果头孢哌酮的ρmax为(194.94±40.04)mg·L-1,t1/2β为(2.23±0.41)h,AUC0-∞为(364.41±71.77)mg·h·L-1,AUC08为(326.73±62.84)mg·h·L-1,CLs为(5.76±1.2)L·h-1;他唑巴坦的ρmax为(26.58±4.07)mg·L-1,t1/2β为(0.87±0.12)h,AUC0-∞为(18.89±4.23)mg·h·L-1,AUC03为(16.91±4.43)mg·h·L-1,CLs为(27.80±6.6)L·h-1。结论健康志愿者静脉滴注头孢哌酮2000mg/他唑巴坦500mg复方制剂,头孢哌酮和他唑巴坦均符合一级消除二室模型,其主要药动学参数与文献报道接近,为临床合理用药提供了参考资料。

OBJECTIVE To study the phaxmacokinetics of cefoperasone/tasobactam following intravenous administration in healthy volunteers. METHODS 16 Healthy volunteers were administered a single dose of cefoperazone/tasobactam （2 000 mg/500 mg,iv）. The plasma concentrations of cefoperasone and tasobactam were determined by identical reversed phase high performance liquid chromatography（RP-HPLC） method. Phaxmacokinetic parameters were obtained using DAS1.0 program. RESULTS The phaxmacokinetic parameters of cefoperasone were as follows ：ρmax （ 194.94 ± 40. 04） mg·L^-1 , AUC0-8 （ 326. 73 ± 62. 84 ） mg·h·L^-1, AUC0-∞（ 364. 41 ± 71.77） mg·h·L^-1 ,t1/2β（2. 23 ±0. 41 ） h,CLs （5.76 ± 1.2） L·h ^-1 ;The phaxmacokinetic parameters of tasobactam were as follows： ρmax（26.58 ±4. 07） mg·L^-1,AUC0-3（16.91 ±4. 43） mg·h·L^-1,AUC0-∞ （18. 89 ±4.23） mg·h·L^-1 ,t1/2β（0. 87 ±0. 12） h,CLs （27. 80 ±6. 60） L·h^-1. CONCLUSION The phaxmacokinetic properties of cefoperazone/tasobactam （2 000 mg/500 mg, iv ） in healthy volunteers axe studied successfully. The plasma concentrations-time curve is fitted to a two-compartment model with first-order output. The PK parameters are comparable to those reported in literatures and useful for clinical therapy.