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阿洛西林和美洛西林渗入骨骼和组织液的药代动力学研究(作者译)

[Pharmacokinetic studies on the penetration of azlocillin and mezlocillin into bone and tissue fluid (author's transl)].

作者信息

Wittmann D H, Schassan H H, Seidel H

出版信息

Arzneimittelforschung. 1981;31(7):1157-62.

PMID:6456009
Abstract

During and after hip replacement arthroplasty antimicrobial concentrations in serum, bone and tissue-fluid were determined microbiologically using agar diffusion assay technique after 15-min infusion of 5 g 6-[D-2-(2-oxoimidazolidine-1-carboxamido)-2-phenylacetamido] - penicillanic acid (azlocillin) and 5 g 6-[D-2-(3-methylsulfonyl-2-oxoimidazolin-1-ylcarboxamido)-2-phenylacetamido]-penicillanic acid (mezlocillin) and after i.v. bolus injection of 2 g mezlocillin. Serum pharmacokinetic data on the individual patients are computer derived using a modified open two-compartment model. The geometric mean of bone level determinations at defined intervals with deviation factor are presented. These results are related to the organic bone compartment and are expressed in mg/l. From the tissue fluid-concentration curve, peak concentration CP and its time were calculated. The time for which one-fourth of the peak concentration CP 1/4 was maintained in tissue fluid was determined graphically. This concentration is compared with the cumulative minimum inhibitory concentrations of representative bacteria causing bone and joint infections. These results are focused as criteria of valuation of antimicrobial chemotherapy.

摘要

在髋关节置换关节成形术期间及术后,采用琼脂扩散试验技术,在静脉输注5克6-[D-2-(2-氧代咪唑烷-1-甲酰胺基)-2-苯乙酰氨基]-青霉烷酸(阿洛西林)和5克6-[D-2-(3-甲基磺酰基-2-氧代咪唑啉-1-基甲酰胺基)-2-苯乙酰氨基]-青霉烷酸(美洛西林)15分钟后,以及静脉推注2克美洛西林后,对血清、骨和组织液中的抗菌药物浓度进行微生物学测定。使用改良的开放二室模型通过计算机得出个体患者的血清药代动力学数据。给出了在规定间隔时间测定的骨水平的几何平均值及其偏差因子。这些结果与有机骨腔室相关,并以毫克/升表示。根据组织液浓度曲线,计算出峰值浓度CP及其出现时间。通过图形确定组织液中维持四分之一峰值浓度CP 1/4的时间。将该浓度与引起骨和关节感染的代表性细菌的累积最低抑菌浓度进行比较。这些结果作为抗菌化疗评估标准的重点。

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