注射用头孢替坦二钠在中国健康人体内的药动学  

Pharmacokinetic Study of Cefotetan Disodium for Injection in Chinese Healthy Volunteers

作　　者：刘亚妮[1] 刘金梅[1] 马林[1] 吕永宁[1] 李忠芳[1] 师少军[1] 

机构地区：[1]华中科技大学同济医学院附属协和医院药剂科,武汉430022

出　　处：《中国药学杂志》2012年第2期132-136,共5页Chinese Pharmaceutical Journal

摘　　要：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:ρmax为(68.03±15.95)、(110.77±17.67)、(225.34±19.63)mg.L-1;AUC0-15为(242.88±56.60)、(415.22±54.24)、(856.18±82.72)mg.h.L-1;t1/2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:ρmax为(123.60±15.74)mg.L-1;AUC0-15为(444.38±62.78)mg.h.L-1;AUCSS为(426.87±59.36)mg.h.L-1;t1/2为(3.29±0.36)h;ρav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。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 eefotetan 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 eefotetan disodium in plasma were determined by HPLC while the pharma- eokinetic 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 phar- macokinetics 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 pharmaeokinetic parameters between female and male subjects.

关 键 词：头孢替坦二钠 药动学 高效液相色谱法 

分 类 号：R969.1[医药卫生—药理学]