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碳青霉烯类抗生素的药理学研究。I. PS-5在动物组织中的代谢

Pharmacological studies on carbapenem antibiotics. I. Metabolism of PS-5 in animal tissues.

作者信息

Shibamoto N, Sakamoto M, Iguchi H, Tone H, Fukagawa Y, Ishikura T

出版信息

J Antibiot (Tokyo). 1982 Jun;35(6):721-8. doi: 10.7164/antibiotics.35.721.

Abstract

After injection into mice and dogs, PS-5 showed a very rapid decrease in its blood concentration, compared with cefazolin. Using in vitro experiments with tissue homogenates and acetone powder preparations, the kidney was found to be the primary site of PS-5-inactivation, although the extent of the inactivation varied depending on the species of animals. The comparative stability data of PS-5, NS-5 (deacetylated PS-5), thienamycin and N-formimidoylthienamycin in kidney homogenates of mouse, rabbit, dog and man are presented. Bilateral nephrectomy and the injection of ethylenediaminetetraacetate seemed to prolong the survival time of PS-5 in rats and mice respectively.

摘要

将PS-5注射到小鼠和狗体内后,与头孢唑林相比,其血药浓度迅速下降。通过对组织匀浆和丙酮粉制剂进行体外实验发现,肾脏是PS-5失活的主要部位,不过失活程度因动物种类而异。文中给出了PS-5、NS-5(脱乙酰基PS-5)、噻烯霉素和N-甲酰亚胺基噻烯霉素在小鼠、兔子、狗和人的肾脏匀浆中的相对稳定性数据。双侧肾切除和注射乙二胺四乙酸似乎分别延长了PS-5在大鼠和小鼠体内的存活时间。

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