Comparative pharmacokinetics of cefuroxime lysine after single intravenous, intraperitoneal, and intramuscular administration to rats
查看参考文献28篇
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文摘
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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-compartmental 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 t_(1/2(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 AUMC_(0-∞) is markedly larger, and mean residence time (MRT) is greatly longer after IP administration: the value of AUMC_(0-∞) was 16.84±4.85, 55.33±20.34, and 36.17±13.24 mg·h~2/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 C_(max) 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 pharmacokinetic parameters of cefuroxime lysine between male and female rats, except the value of AUC_(0-∞) 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 C_(max) after IM injection. After IM administration the AUC_(0-∞) in male rats was significantly larger than that in female rats. |
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来源
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Acta Pharmacologica Sinica
,2012,33(11):1348-1352 【核心库】
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DOI
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10.1038/aps.2012.99
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关键词
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cefuroxime lysine
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intravenous administration
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intramuscular administration
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intraperitoneal administration
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pharmacokinetics
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地址
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School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, 110016
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语种
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英文 |
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ISSN
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1671-4083 |
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学科
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医药、卫生;药学 |
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基金
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supported by the National Key Scientific Project for New Drug Discovery and Development
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文献收藏号
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CSCD:4669573
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