头孢哌酮组织穿透模型：扩散系数与蛋白结合率

A model of cefoperazone tissue penetration: diffusion coefficient and protein binding.

作者信息

Meulemans A

机构信息

Laboratoire de Biophysique, Faculté de Médecine Xavier-Bichat, Paris, France.

出版信息

Antimicrob Agents Chemother. 1992 Feb;36(2):295-8. doi: 10.1128/AAC.36.2.295.

DOI:10.1128/AAC.36.2.295

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC188360/

Abstract

The apparent diffusion coefficient of a bound drug, cefoperazone, was studied. The protein binding of cefoperazone was studied by voltammetry, a technique which permitted instant measurements. The apparent diffusion coefficients were similar in agar and fibrin and lower in rat brain tissue. The influence of protein on the value of the apparent diffusion coefficient was negligible. The hypothesis that only the free drug diffuses was supported. The percentage of binding determined by voltammetry corresponded to the true concentration of drug which diffuses and is much lower than the percentage of binding determined by the ultrafiltration centrifugation method. This discrepancy could be explained by the rate of dissociation of the protein-drug complex.

摘要

对一种结合型药物头孢哌酮的表观扩散系数进行了研究。采用伏安法研究了头孢哌酮的蛋白结合情况，该技术可进行即时测量。头孢哌酮在琼脂和纤维蛋白中的表观扩散系数相似，而在大鼠脑组织中较低。蛋白质对表观扩散系数值的影响可忽略不计。仅游离药物扩散这一假设得到了支持。通过伏安法测定的结合百分比与扩散的药物真实浓度相对应，且远低于通过超滤离心法测定的结合百分比。这种差异可通过蛋白质 - 药物复合物的解离速率来解释。

相似文献

1

A model of cefoperazone tissue penetration: diffusion coefficient and protein binding.

Antimicrob Agents Chemother. 1992 Feb;36(2):295-8. doi: 10.1128/AAC.36.2.295.

2

Comparative diffusion study of two nitrosoureas: carmustine and fotemustine in normal rat brain, human and rat brain biopsies.

Chemotherapy. 1991;37(2):86-92. doi: 10.1159/000238838.

3

Measurement and clinical and pharmacokinetic implications of diffusion coefficients of antibiotics in tissues.

Antimicrob Agents Chemother. 1989 Aug;33(8):1286-90. doi: 10.1128/AAC.33.8.1286.

4

Diffusion of penicillin in agar and cerebral cortex of the rat.

Brain Res. 1988 Mar 15;444(1):181-3. doi: 10.1016/0006-8993(88)90926-2.

5

Biliary secretion of cefoperazone and its inter-relationship with bile acid transport in the rat.

Biochem Int. 1987 Sep;15(3):653-8.

6

Effect of acute renal failure on the disposition of cefoperazone.

J Pharm Pharmacol. 1999 Mar;51(3):361-6. doi: 10.1211/0022357991772376.

7

Voltammetric studies on the antibiotic drug cefoperazone quantification and pharmacokinetic studies.

J Pharm Biomed Anal. 2006 Oct 11;42(4):523-7. doi: 10.1016/j.jpba.2006.05.002. Epub 2006 Jun 19.

8

In vitro and in situ evidence for the contribution of Labrasol and Gelucire 44/14 on transport of cephalexin and cefoperazone by rat intestine.

Eur J Pharm Biopharm. 2002 Nov;54(3):311-8. doi: 10.1016/s0939-6411(02)00116-9.

9

Effect of protein binding on serum bactericidal activities of ceftazidime and cefoperazone in healthy volunteers.

Antimicrob Agents Chemother. 1988 Mar;32(3):298-302. doi: 10.1128/AAC.32.3.298.

10

Simultaneous determination of unbound cefoperazone in rat blood and brain using microdialysis.

J Pharm Pharmacol. 2000 Aug;52(8):963-8. doi: 10.1211/0022357001774859.

引用本文的文献

1

Diffusion in brain extracellular space.

Physiol Rev. 2008 Oct;88(4):1277-340. doi: 10.1152/physrev.00027.2007.

2

Influence of serum protein binding on the in vitro activity of anti-fungal agents.

Infection. 1995 Sep-Oct;23(5):292-7. doi: 10.1007/BF01716289.

3

Analysis of vancomycin entry into pulmonary lining fluid by bronchoalveolar lavage in critically ill patients.

Antimicrob Agents Chemother. 1993 Feb;37(2):281-6. doi: 10.1128/AAC.37.2.281.

本文引用的文献

1

Diffusion measurements in agar gel.

Biochemistry. 1962 Jul;1:658-63. doi: 10.1021/bi00910a019.

2

Pharmacokinetics of tissue penetration of antibiotics.

Rev Infect Dis. 1981 Jan-Feb;3(1):45-66. doi: 10.1093/clinids/3.1.45.

3

On-line pharmacokinetics of chloramphenicol in rat cortex by in vivo electrochemical detection.

Chemotherapy. 1984;30(6):353-7. doi: 10.1159/000238293.

4

Anomalous effect of serum on the antimicrobial activity of cefoperazone.

Drugs. 1981;22 Suppl 1:52-9. doi: 10.2165/00003495-198100221-00012.

5

Studies on protein binding of antibiotics. I. Effect of cefazolin on protein binding and pharmacokinetics of cefoperazone.

J Antibiot (Tokyo). 1980 Jun;33(6):625-35. doi: 10.7164/antibiotics.33.625.

6

Biliary excretion of ampicillin, azidocillin and benzylpenicillin in the rat.

Acta Pharmacol Toxicol (Copenh). 1973;33(3):219-28. doi: 10.1111/j.1600-0773.1973.tb02009.x.

7

A rapid method for the determination of salicylate binding by the use of ultrafilters.

J Pharm Pharmacol. 1972 Oct;24(10):786-9. doi: 10.1111/j.2042-7158.1972.tb08883.x.

8

General principles of antibiotic tissue penetration.

J Antimicrob Chemother. 1985 Jan;15 Suppl A:59-75. doi: 10.1093/jac/15.suppl_a.59.

9

Cefsulodin penetration into rat brain: extracellular versus total concentration.

Chemotherapy. 1986;32(5):393-8. doi: 10.1159/000238441.

10

Tissue penetration of antibiotics.

Clin Biochem. 1986 Apr;19(2):90-100. doi: 10.1016/s0009-9120(86)80054-6.

文献AI研究员

20分钟写一篇综述，助力文献阅读效率提升50倍。

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

文档翻译

学术文献翻译模型，支持多种主流文档格式。