静脉滴注头孢哌酮/他唑巴坦复方制剂的健康人体药动学

 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ρ_max为(194.94±40.04)mg·L^-1,t_1/2β为(2.23±0.41)h,AUC_0-∞为(364.41±71.77)mg·h·L^-1,AUC_0-8为(326.73±62.84)mg·h·L^-1,CLs为(5.76±1.2)L·h^-1;他唑巴坦的ρ_max为(26.58±4.07)mg·L^-1,t_1/2β为(0.87±0.12)h,AUC_0-∞为(18.89±4.23)mg·h·L^-1,AUC_0-3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。

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

OBJECTIVE To study the pharmacokinetics of cefoperazone/tazobactam following intravenous administration in healthy volunteers. METHODS 16 Healthy volunteers were administered a single dose of cefoperazone/tazobactam (2 000 mg/500 mg,iv). The plasma concentrations of cefoperazone and tazobactam were determined by identical reversed phase high performance liquid chromatography(RP-HPLC) method. Pharmacokinetic parameters were obtained using DAS1.0 program. RESULTS The pharmacokinetic parameters of cefoperazone were as follows:ρ_max (194.94±40.04) mg·L^-1,AUC_0–8 (326.73±62.84) mg·h·L^-1,AUC_0-∞ (364.41±71.77) mg·h·L^-1,t_1/2β (2.23±0.41) h,CLs (5.76±1.2) L·h^-1;The pharmacokinetic parameters of tazobactam were as follows:ρ_max (26.58±4.07) mg·L^-1,AUC_0–3 (16.91±4.43) mg·h·L^-1 ,AUC_0-∞ (18.89±4.23) mg·h·L^-1,t_1/2β (0.87±0.12) h,CLs (27.80±6.60) L·h^-1. CONCLUSION The pharmacokinetic properties of cefoperazone/tazobactam (2 000 mg/500 mg,iv) in healthy volunteers are 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.