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头孢地嗪,一种氨噻唑基头孢菌素。II. 实验动物体内药代动力学行为的比较研究。

Cefodizime, an aminothiazolylcephalosporin. II. Comparative studies on the pharmacokinetic behavior in laboratory animals.

作者信息

Klesel N, Limbert M, Seeger K, Seibert G, Winkler I, Schrinner E

出版信息

J Antibiot (Tokyo). 1984 Aug;37(8):901-9. doi: 10.7164/antibiotics.37.901.

Abstract

The pharmacokinetic properties of cefodizime, a new aminothiazolyliminomethoxycephalosporin, were studied in laboratory animals and compared with the pharmacokinetics of another long-acting cephalosporin, ceftriaxone. Both cephalosporin derivatives showed high affinity (33-99%) for serum proteins. High and prolonged blood respectively serum levels of the antibiotics were achieved following subcutaneous and intravenous injection into mice, rats, rabbits, dogs and monkeys. Cefodizime elimination half-lives ranged from 1.17 hours in mice to 3.53 hours in rabbits compared to ceftriaxone half-lives ranging from 0.73 hour in mice to 7.31 hours in rabbits. The antibiotics were well distributed in the body and penetrated into tissues and body fluids to a high degree. Particularly high and prolonged levels were detected in the lungs, liver and kidneys of the experimental animals. Large amounts, approximately 35-55% of the given dose, were recovered in the urine of rabbits and dogs, while the recovery rate in the bile of rabbits was only 0.57% for cefodizime and 1.08% for ceftriaxone.

摘要

研究了新型氨噻唑基甲氧基头孢菌素头孢地嗪在实验动物中的药代动力学特性,并与另一种长效头孢菌素头孢曲松的药代动力学进行了比较。两种头孢菌素衍生物对血清蛋白均表现出高亲和力(33%-99%)。对小鼠、大鼠、兔子、狗和猴子进行皮下和静脉注射后,分别在血液或血清中实现了抗生素的高浓度和长时间水平。头孢地嗪的消除半衰期在小鼠中为1.17小时,在兔子中为3.53小时,而头孢曲松的半衰期在小鼠中为0.73小时,在兔子中为7.31小时。抗生素在体内分布良好,并高度渗透到组织和体液中。在实验动物的肺、肝和肾中检测到特别高且持久的水平。在兔子和狗的尿液中回收了大量药物,约占给药剂量的35%-55%,而头孢地嗪在兔子胆汁中的回收率仅为0.57%,头孢曲松为1.08%。

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