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采用特定高效液相色谱分析技术对志愿者进行拉氧头孢(羟羧氧酰胺菌素)动力学研究。

Latamoxef (moxalactam) kinetics in volunteers studied by a specific HPLC assay technique.

作者信息

Shepherd A M, Hardin T C, Ludden T M, Miner D J, Coleman D L

出版信息

J Antimicrob Chemother. 1983 Oct;12(4):377-86. doi: 10.1093/jac/12.4.377.

Abstract

Pharmacokinetic parameters were calculated from plasma and urine latamoxef ('Moxalactam') levels determined by HPLC assay after single and multiple intramuscular (im) and single intravenous (iv) doses of 500 mg given to eight healthy volunteers. After im administration, systemic bio-availability was 92% after both the first and sixth doses. Peak plasma concentration was 18 mg/l (first dose) and 22 mg/l (sixth dose), reached at 1.2 h and 1.3 h respectively. The terminal phase half-lives were 2.5 h and 2.7 h respectively. After iv administration, the initial phase plasma half-life was 0.23 h and the terminal phase half-life, 2.4 h. Plasma clearance was 87.0 ml/min. The steady state distribution volume was 210 ml/kg. After iv administration, 72% of the dose was found in the urine in the first 24 h. Urinary clearance was 66 ml/min (iv dose) and 63 ml/min (sixth im dose). Most systemic infections will permit eight hourly dosing with 500 mg im or iv. Many urinary infections will be best treated with im administration, rather than iv administration.

摘要

对8名健康志愿者单次和多次肌内注射(im)及单次静脉注射(iv)500mg拉氧头孢(“羟羧氧酰胺菌素”)后,通过高效液相色谱法(HPLC)测定血浆和尿液中的拉氧头孢水平,计算药代动力学参数。肌内注射给药后,首剂和第6剂后的全身生物利用度均为92%。血浆峰浓度分别为18mg/l(首剂)和22mg/l(第6剂),分别在1.2小时和1.3小时达到。终末相半衰期分别为2.5小时和2.7小时。静脉注射给药后,初始相血浆半衰期为0.23小时,终末相半衰期为2.4小时。血浆清除率为87.0ml/min。稳态分布容积为210ml/kg。静脉注射给药后,在最初24小时内72%的剂量可在尿液中检测到。尿清除率为66ml/min(静脉注射剂量)和63ml/min(第6剂肌内注射剂量)。大多数全身感染允许每8小时给予500mg肌内注射或静脉注射。许多泌尿系统感染最好采用肌内注射给药,而非静脉注射给药。

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