呋苄青霉素药代动力学及组织分布的研究

呋苄青霉素是由我国开发成功的一个酰脲类青霉素。本项研究采用微生物法,以狗和正常人为受试对象,以氧哌嗪青霉素和羧苄青霉素为对照进行药代动力学研究,结果表明,3个药的药—时曲线符合二室开放式模型,呋苄青霉素较其它对照药具较高的即刻血浓度和较低的肾清除率。用微生物法和放射自显影法测定的呋苄青霉素在小鼠体内组织分布汪明,呋苄青霉素广泛分布于体内各组织,尤其在肺、肝、肠中的浓度明显高于羧苄青霉素。

PHARMACOKINETICS AND DRUG DISTRIBUTION OF FURBENICILLIN

A study on pharmacokinetics of furbenicillin, one of ureidopenicillins developed in China, wascarried out in six healthy volunteers compared with piperacillin and carbenicillin. Serum and urinesamples were collected for antibiotic assay by using microbiological assay method. A comparative studyon furbenicillin and carbenicillin were also performed in fourteen dogs. The drug distribution of fur-benicillin in mice was studied by using microbiological and autoradiographic techniques. The resultsshowed that the concentration/time ourves of the three drugs fitted a two compattment open modelafter intravenous infusion 1.0 g. The mean peak serum level of furbenicillin was 87.03 mg/L, whichwas 2.1 and 1.7 times hight than that of carbenicillin and piperacillin respectively. The renal cleara-nce of furbenicillin was much lower than that of carbenillin and also obviously lower than that ofpiperacillin, but the total body clearance of the three drugs are similar, Similar results were also obs-erved in dogs. The concentrations of furbenicillin in most tissues were higher than those of carbenibe-nicillin within 1 hour after administration, especially in lung, liver and intestines. The posibility ofpresence of an extrarenal clearance of furbenicillin was discussed.