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。
Abstract
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.
关键词
头孢替坦二钠 /
药动学 /
高效液相色谱法
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Key words
cefotetan disodium /
pharmacokinetics /
HPLC
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刘亚妮 刘金梅 马林 吕永宁 李忠芳 师少军.
注射用头孢替坦二钠在中国健康人体内的药动学[J]. 中国药学杂志, 2012, 47(2): 132-135
Pharmacokinetic Study of Cefotetan Disodium for Injection in Chinese Healthy Volunteers[J]. Chinese Pharmaceutical Journal, 2012, 47(2): 132-135
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参考文献
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