注射用头孢替坦二钠在中国健康人体内的药动学

 目的 研究中国健康受试者静脉注射头孢替坦二钠后的药动学特征。方法 30名健康受试者随机分为3组，男、女各半，分别静脉滴注头孢替坦二钠0.5、1.0、2.0 g，进行低、中、高单剂量药动学研究。1.0 g剂量组并进行多剂量药动学研究。采用HPLC-UV测定血浆中头孢替坦二钠的浓度。应用DAS2.1.1软件计算药动学参数，并进行统计分析。结果 30名健康受试者分别单次静脉滴注头孢替坦二钠0.5，1.0，2.0 g的主要药动学参数如下：ρ_max为(68.03±15.95)、(110.77±17.67)、(225.34±19.63) mg·L^-1；AUC_0-15为(242.88±56.60)、(415.22±54.24)、(856.18±82.72) mg·h·L^-1；t_1/2为(3.67±0.48)、(3.69±0.40)、(3.53±0.26) h。多次给药的主要药动学参数如下：ρ_max为(123.60±15.74) mg·L^-1 ；AUC_0-15为(444.38±62.78) mg·h·L^-1；AUC_SS为(426.87±59.36) mg·h·L^-1；t_1/2为(3.29±0.36) h；ρ_av为(35.57±4.95) mg·L^-1。结论 注射用头孢替坦二钠单剂量静脉滴注后在0.5～2.0 g内呈线性动力学特征；连续给药后在体内无蓄积；性别对注射用头孢替坦二钠的体内药动学无差异。

Pharmacokinetic Study of Cefotetan Disodium for Injection in Chinese Healthy Volunteers

OBJECTIVE To study the pharmacokinetics of cefotetan disodium for injection in Chinese healthy volunteers.METHODS Thirty healthy volunteers were randomly divided into 3 groups with 5 males and 5 females in each group.The volunteers in each group were administered a single dose of cefotetan disodium of 0.5,1.0,or 2.0 g,respectively.Those who got dose of 1.0 g were administered twice daily for 7 d.The concentrations of cefotetan disodium in plasma were determined by HPLC while the pharmacokinetic parameters were calculated by DAS software.RESULTS The main pharmacokinetic parameters of cefotetan disodium after single-dose intravenous administration were as follows: ρmax(68.03 ± 15.95),(110.77 ± 17.67),(225.34±19.63) mg·L-1;AUC0-15(242.88±56.60),(415.22±54.24),(856.18±82.72) mg·h·L-1;t1/2(3.67±0.48),(3.69±0.40),(3.53±0.26) h,respectively.The main pharmacokinetic parameters of cefotetan disodium after multiple-dose administration were as follows: ρmax(123.60±15.74) mg·L-1;AUC0-15(444.38±62.78) mg·h·L-1;AUCSS(426.87±59.36) mg·h·L-1;t1/2(3.29±0.36)h;ρav(35.57±4.95) mg·L-1,respectively.CONCLUSION Cefotetan disodium for injection displays linear pharmacokinetics in the dose range of 0.5 to 2.0 g after single intravenous dosing.There is no significant accumulation after repeated dosing.There is no significant difference in the pharmacokinetic parameters between female and male subjects.