Comparative pharmacokinetics of cefuroxime lysine after single intravenous, intraperitoneal, and intramuscular administration to rats  

作　　者：Long-shan ZHAO Ran YIN Bin-bin WEI Qing LI Zhen-yuan JIANG Xiao-hui CHEN Kai-shun BI 

机构地区：[1]School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China

出　　处：《Acta Pharmacologica Sinica》2012年第11期1348-1352,共5页中国药理学报（英文版）

摘　　要：Aim： To compare the pharmacokinetic parameters of cefuroxime lysine, a new second-generation of cephalosporin antibiotics, after intravenous （IV）, intraperitoneal （IP）, or intramuscular （IM） administration. Methods： Twelve male and 12 virgin female Sprague-Dawley rats, weighing from 200 to 250 g, were divided into three groups （n=4 for each gender in each group）. The rats were administered a single dose （67.5 mg/kg） of cefuroxime lysine via IV bolus or IP or IM injection. Blood samples were collected and analyzed with a validated UFLC-MS/MS method. The concentration-time data were then calculated by compartmental and non-compartmental pharmacokinetic methods using DAS software. Results： After IV, IP or IM administration, the plasma cefuroxime lysine disposition was best described by a tri-compartmental, bi-com- partmental or mono-compartmental open model, respectively, with first-order elimination. The plasma concentration profiles were similar through the 3 administration routes. The distribution process was rapid after IV administration： the value of tl/2（d） was 0.10±0.11 h, 1.36±0.65 h, and 1.25±1.01 h after IV, IP or IM administration. The AUMC0-∞ is markedly larger, and mean residence time （MRT） is greatly longer after IP administration： the value of AUMC0-∞ was 16.84±4.85, 55.33±20.34, and 36.17±13.24 mg.h2/L; the value of MRT was 0.37±0.07 h, 0.93±0.10 h, and 0.65±0.05 h after IV, IP or IM administration. The Cmax after IM injection was significantly higher than that in IP injection （73.51±12.46 vs 49.09±7.06 mg/L）. There was no significantly sex-related difference in other pharma- cokinetic parameters of cefuroxime lysine between male and female rats, except the value of AUC0-∞ via IM administration that was significantly larger in male rats than that in female rats （66.38±16.5 vs 44.23±6.37 mg.h/L）. Conclusion： Cefuroxime lysine shows quick absorption after IV injection, a long retension after IP injection, and a high Cmax after IM injectAim： To compare the pharmacokinetic parameters of cefuroxime lysine, a new second-generation of cephalosporin antibiotics, after intravenous （IV）, intraperitoneal （IP）, or intramuscular （IM） administration. Methods： Twelve male and 12 virgin female Sprague-Dawley rats, weighing from 200 to 250 g, were divided into three groups （n=4 for each gender in each group）. The rats were administered a single dose （67.5 mg/kg） of cefuroxime lysine via IV bolus or IP or IM injection. Blood samples were collected and analyzed with a validated UFLC-MS/MS method. The concentration-time data were then calculated by compartmental and non-compartmental pharmacokinetic methods using DAS software. Results： After IV, IP or IM administration, the plasma cefuroxime lysine disposition was best described by a tri-compartmental, bi-com- partmental or mono-compartmental open model, respectively, with first-order elimination. The plasma concentration profiles were similar through the 3 administration routes. The distribution process was rapid after IV administration： the value of tl/2（d） was 0.10±0.11 h, 1.36±0.65 h, and 1.25±1.01 h after IV, IP or IM administration. The AUMC0-∞ is markedly larger, and mean residence time （MRT） is greatly longer after IP administration： the value of AUMC0-∞ was 16.84±4.85, 55.33±20.34, and 36.17±13.24 mg.h2/L; the value of MRT was 0.37±0.07 h, 0.93±0.10 h, and 0.65±0.05 h after IV, IP or IM administration. The Cmax after IM injection was significantly higher than that in IP injection （73.51±12.46 vs 49.09±7.06 mg/L）. There was no significantly sex-related difference in other pharma- cokinetic parameters of cefuroxime lysine between male and female rats, except the value of AUC0-∞ via IM administration that was significantly larger in male rats than that in female rats （66.38±16.5 vs 44.23±6.37 mg.h/L）. Conclusion： Cefuroxime lysine shows quick absorption after IV injection, a long retension after IP injection, and a high Cmax after IM inject

关 键 词：cefuroxime lysine intravenous administration intramuscular administration intraperitoneal administration PHARMACOKINETICS 

分 类 号：S859.796[农业科学—临床兽医学] S858.28[农业科学—兽医学]