Evaluation of Tissue Binding in 3 Tissues Across 5 Species, and Prediction of Volume of Distribution from Plasma Protein and Tissue Binding

2021 ◽  
pp. DMD-AR-2020-000337
Author(s):  
Frederick Hsu ◽  
Yi-Chen Chen ◽  
Fabio Broccatelli
Keyword(s):  
Plasma Protein ◽  
Volume Of Distribution ◽  
Tissue Binding

How Well Do Lipophilicity Parameters, MEEKC Microemulsion Capacity Factor, and Plasma Protein Binding Predict CNS Tissue Binding?

2012 ◽  
Vol 101 (5) ◽  
pp. 1932-1940 ◽  
Author(s):  
Maciej J. Zamek-Gliszczynski ◽  
Karen E. Sprague ◽  
Alfonso Espada ◽  
Thomas J. Raub ◽  
Stuart M. Morton ◽  
...  
Keyword(s):  
Protein Binding ◽  
Plasma Protein Binding ◽  
Plasma Protein ◽  
Capacity Factor ◽  
Tissue Binding ◽  
Lipophilicity Parameters

Do We Need to Optimize Plasma Protein and Tissue Binding in Drug Discovery?

2011 ◽  
Vol 11 (4) ◽  
pp. 450-466 ◽  
Author(s):  
Xingrong Liu ◽  
Cuiping Chen ◽  
Cornelis E.C.A. Hop
Keyword(s):  
Drug Discovery ◽  
Plasma Protein ◽  
Tissue Binding

Rational Use of Plasma Protein and Tissue Binding Data in Drug Design

2014 ◽  
Vol 57 (20) ◽  
pp. 8238-8248 ◽  
Author(s):  
Xingrong Liu ◽  
Matthew Wright ◽  
Cornelis E. C. A. Hop
Keyword(s):  
Drug Design ◽  
Plasma Protein ◽  
Tissue Binding ◽  
Rational Use ◽  
Binding Data

scholarly journals Biomimetic properties and estimated in vivo distribution of chloroquine and hydroxy-chloroquine enantiomers

ADMET & DMPK ◽  
2021 ◽  
Author(s):  
Klara Livia Valko ◽  
Tong Zhang
Keyword(s):  
Large Volume ◽  
Volume Of Distribution ◽  
Tissue Binding ◽  
Binding Medium ◽  
Acid Glycoprotein ◽  
Phospholipid Binding ◽  
Racemic Mixtures ◽  
High Level ◽  
Drug Efficiency

Chloroquine and hydroxy-chloroquine already established as anti-malarial and lupus drugs have recently gained renewed attention in the fight against the Covid-19 pandemic. Bio-mimetic HPLC methods have been used to measure the protein and phospholipid binding of the racemic mixtures of the drugs. The tissue binding and volume of distribution of the enantiomers have been estimated. The enantiomers can be separated using Chiralpak AGP HPLC columns. From the α-1-acid-glycoprotein (AGP) binding, the lung tissue binding can be estimated for the enantiomers. The drugs have a large volume of distribution, showed strong and stereoselective glycoprotein binding, medium-strong phospholipid-binding indicating only moderate phospholipidotic potential, hERG inhibition and promiscuous binding. The drug efficiency of the compounds was estimated to be greater than 2 % which indicates a high level of free biophase concentration relative to dose. The biomimetic properties of the compounds support the well-known tolerability of the drugs.

Effect of plasma protein and tissue binding on the biologic half-life of drugs

1978 ◽  
Vol 24 (1) ◽  
pp. 1-4 ◽  
Author(s):  
Milo Gibaldi ◽  
Gerhard Levy ◽  
Patrick J. McNamara
Keyword(s):  
Plasma Protein ◽  
Half Life ◽  
Tissue Binding
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