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本文报道头孢噻肟的药代动力学研究结果。8名健康志愿者分别肌注、静注和静滴头孢噻肟后,平均高峰血药浓度为26.2±6.8mg/L、130.7±19.4mg/L和74.5±14.2mg/L;平均消除半衰期(T1/2β)分别为1.35±0.33h、0.98± 0.21h和0.90±0.05h。平均高峰尿药分别2461±1947mg/L(im)、3079±1767mg/L(iv)和2505±1266mg/L(iv gtt);50％以上的给药量于24h内自尿中排出。肌注后的绝对生物利用度为100％。本文同时还建立了头孢噻肟及其代谢产物去乙酰头孢噻肟血浓度的高效液相色谱测定法,并对二者体内过程进行了研究。
This article reports the results of the pharmacokinetics of cefotaxime. Eight healthy volunteers were intramuscular, intravenous and intravenous cefotaxime, the average peak plasma concentrations of 26.2 ± 6.8mg / L, 130.7 ± 19.4mg / L and 74.5 ± 14.2mg / L; the average elimination half-life ( T1 / 2β) were 1.35 ± 0.33h, 0.98 ± 0.21h and 0.90 ± 0.05h, respectively. The average peak urinary drug levels were 2461 ± 1947mg / L (im), 3079 ± 1767mg / L (iv) and 2505 ± 1266mg / L (iv gtt), respectively; more than 50% The absolute bioavailability after intramuscular injection was 100%. In the meantime, high performance liquid chromatography (HPLC) of cefotaxime and its metabolite cefotaxime was also established, and the in vivo process of the two drugs was studied.