头孢噻肟及其代谢产物的药代动力学研究

PHARMACOKINETICS OF CEFOTAXIME AND ITS METABOLITES

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。

The parameters of pharmacokinetics of Cefotaxime were reported. lg of Cefotaxime was given by im route, iv bolus injection and iv drip to 8 health volunteers, the mean peak serum concentrations were 26.2± 6.8mg/L, 130.7 ±19.4mg/L and 74.5±14.2mg/L, the mean elimination half life(T1/2β)were 1.35 + 0.33, 0.98 + 0.21 and 0.90 ± 0.05h respectively. The mean peak urine concentrations were 2461±1947mg/L (im), 3079±1767mg/L(iv) and 2504±1265mg/L (iv gtt), the cumulative excretion rates within 24h being more than 50% of the given doses. The absolute bioavailability after im injection was 100%. Besidws, the HPLC method for the determination of Cefotaxime and its metabolites, desac-etylcefotaxime, in serum was established and their concentration-time profiles were investigated.