头孢唑肟经肠胃外给药后在动物体内的药代动力学。
Pharmacokinetics of ceftizoxime in animals after parenteral dosing.
作者信息
Murakawa T, Sakamoto H, Fukada S, Nakamoto S, Hirose T, Itoh N, Nishida M
出版信息
Antimicrob Agents Chemother. 1980 Feb;17(2):157-64. doi: 10.1128/AAC.17.2.157.
The pharmacokinetic profile of ceftizoxime was studied in mice, rats, dogs, and monkeys given the drug in a single parenteral dose. The serum data after an intravenous injection were analyzed by the two-compartment open model. Cefotiam, cefmetazole, cefotaxime, and cefamandole were used as reference drugs. High concentrations of ceftizoxime were attained in the sera of all test animals and in the tissues of rats after parenteral dosing. The serum concentrations of ceftizoxime were higher than those of the other antibiotics in large animals (dogs and monkeys), but were lower in small animals (mice and rats). About 80% of ceftizoxime was excreted unchanged in the 24-h urine of all species tested. The biliary excretion of ceftizoxime was low: 3.7% in rats and 0.59% in dogs. However, therapeutically significant concentrations of ceftizoxime were found in the bile of dogs. Ceftizoxime was stable in biological fluids such as serum, urine, and tissue homogenates, but cefotaxime was unstable in rat tissue homogenates. Binding of ceftizoxime to serum protein in all species was the lowest of all the antibiotics: 31% for humans, 17% for dogs, and 32% for rats.
对小鼠、大鼠、犬和猴单次非肠道给药后头孢唑肟的药代动力学特征进行了研究。静脉注射后的血清数据采用二室开放模型进行分析。头孢替安、头孢美唑、头孢噻肟和头孢孟多用作参比药物。非肠道给药后，所有试验动物的血清以及大鼠组织中均达到了高浓度的头孢唑肟。在大型动物（犬和猴）中，头孢唑肟的血清浓度高于其他抗生素，但在小型动物（小鼠和大鼠）中则较低。在所有受试物种的24小时尿液中，约80%的头孢唑肟以原形排出。头孢唑肟的胆汁排泄量较低：大鼠为3.7%，犬为0.59%。然而，在犬的胆汁中发现了具有治疗意义的头孢唑肟浓度。头孢唑肟在血清、尿液和组织匀浆等生物体液中稳定，但头孢噻肟在大鼠组织匀浆中不稳定。在所有物种中，头孢唑肟与血清蛋白的结合率在所有抗生素中最低：人类为31%，犬为17%，大鼠为32%。
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