Validation of a Rapid Equilibrium Dialysis Approach for the Measurement of Plasma Protein Binding

2008 ◽  
Vol 97 (10) ◽  
pp. 4586-4595 ◽  
Author(s):  
Nigel J. Waters ◽  
Rachel Jones ◽  
Gareth Williams ◽  
Bindi Sohal
Keyword(s):  
Protein Binding ◽  
Plasma Protein Binding ◽  
Plasma Protein ◽  
Equilibrium Dialysis ◽  
Rapid Equilibrium

Solid-phase microextraction for assessment of plasma protein binding, a complement to rapid equilibrium dialysis

Bioanalysis ◽  
2021 ◽  
Author(s):  
Sheelan Ahmad ◽  
Daniel Baker ◽  
Darragh Murnane ◽  
Neil Spooner ◽  
Ute Gerhard
Keyword(s):  
Protein Binding ◽  
Plasma Protein Binding ◽  
Plasma Protein ◽  
Solid Phase Microextraction ◽  
Solid Phase ◽  
Equilibrium Dialysis ◽  
Free Concentration ◽  
Rapid Equilibrium

Aim: Determination of plasma protein binding ( PPB) is considered vital for better understanding of pharmacokinetic and pharmacodynamic activities of drugs due to the role of free concentration in pharmacological response. Methodology & results: Solid-phase microextraction (SPME) was investigated for measurement of PPB from biological matrices and compared with a gold standard approach (rapid equilibrium dialysis [RED]). Discussion & conclusion: SPME-derived values of PPB correlated well with literature values, and those determined by RED. Respectively, average protein binding across three concentrations by RED and SPME was 33.1 and 31.7% for metoprolol, 89.0 and 86.6% for propranolol and 99.2 and 99.0% for diclofenac. This study generates some evidence for SPME as an alternative platform for the determination of PPB.

Plasma Protein Binding of Disopyramide by Equilibrium Dialysis and Ultrafiltration

1983 ◽  
Vol 5 (1) ◽  
pp. 81-86 ◽  
Author(s):  
Beverley M. David ◽  
Rose Tjokrosetio ◽  
Kenneth F. Ilett
Keyword(s):  
Protein Binding ◽  
Plasma Protein Binding ◽  
Plasma Protein ◽  
Equilibrium Dialysis

Control and Measurement of Plasma pH in Equilibrium Dialysis: Influence on Drug Plasma Protein Binding

2010 ◽  
Vol 39 (3) ◽  
pp. 551-557 ◽  
Author(s):  
Ruth E. Curran ◽  
Christopher R. J. Claxton ◽  
Laura Hutchison ◽  
Paul J. Harradine ◽  
Iain J. Martin ◽  
...  
Keyword(s):  
Protein Binding ◽  
Plasma Protein Binding ◽  
Plasma Protein ◽  
Equilibrium Dialysis ◽  
Drug Plasma

scholarly journals Pharmacokinetics, Tissue Distribution, Plasma Protein Binding Studies of 10-Dehydroxyl-12-Demethoxy-Conophylline, a Novel Anti-Tumor Candidate, in Rats

Molecules ◽  
2019 ◽  
Vol 24 (2) ◽  
pp. 283
Author(s):  
Chengjun Jiang ◽  
Jie Li ◽  
Xianghai Cai ◽  
Nini Li ◽  
Yan Guo ◽  
...  
Keyword(s):  
Protein Binding ◽  
Tissue Distribution ◽  
Plasma Protein Binding ◽  
Plasma Protein ◽  
Equilibrium Dialysis ◽  
Free Fraction ◽  
Ultra Performance Liquid Chromatography ◽  
Sprague Dawley ◽  
Binding Studies ◽  
High Protein Binding

10-Dehydroxyl-12-demethoxy-conophylline is a natural anticancer candidate. The motivation of this study was to explore the pharmacokinetic profiles, tissue distribution, and plasma protein binding of 10-dehydroxyl-12-demethoxy-conophylline in Sprague Dawley rats. A rapid, sensitive, and specific ultra-performance liquid chromatography (UPLC) system with a fluorescence (FLR) detection method was developed for the determination of 10-dehydroxyl-12-demethoxy-conophylline in different rat biological samples. After intravenous (i.v.) dosing of 10-dehydroxyl-12-demethoxy-conophylline at different levels (4, 8, and 12 mg/kg), the half-life t1/2α of intravenous administration was about 7 min and the t1/2β was about 68 min. The AUC0→∞ increased in a dose-proportional manner from 68.478 μg/L·min for 4 mg/kg to 305.616 mg/L·min for 12 mg/kg. After intragastrical (i.g.) dosing of 20 mg/kg, plasma levels of 10-dehydroxyl-12-demethoxy-conophylline peaked at about 90 min. 10-dehydroxyl-12-demethoxy-conophyllinea absolute oral bioavailability was only 15.79%. The pharmacokinetics process of the drug was fit to a two-room model. Following a single i.v. dose (8 mg/kg), 10-dehydroxyl-12-demethoxy-conophylline was detected in all examined tissues with the highest in kidney, liver, and lung. Equilibrium dialysis was used to evaluate plasma protein binding of 10-dehydroxyl-12-demethoxy-conophylline at three concentrations (1.00, 2.50, and 5.00 µg/mL). Results indicated a very high protein binding degree (over 80%), reducing substantially the free fraction of the compound.

Sign in / Sign up

Export Citation Format

Share Document