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Correlation between reversed-phase high-performance liquid chromatography and plasma protein binding.
J Ganansia1, G Bianchetti, J P Thénot
1Laboratoires d'Etudes et de Recherches Synthélabo, Meudon la Foret, France.
Journal of Chromatography
|October 9, 1987
Summary
Hydrophobic interactions influence both chromatography retention times and plasma protein binding. This study shows retention time can predict protein binding for similar compounds.
Area of Science:
- Analytical Chemistry
- Pharmacology
Background:
- Hydrophobic interactions are crucial in reversed-phase liquid chromatography (RPLC) and plasma protein binding.
- Understanding this relationship aids in predicting drug behavior.
Purpose of the Study:
- To investigate the relationship between chromatographic retention time and plasma protein binding.
- To assess the predictive power of retention time for protein binding in compound series.
Main Methods:
- Experimental investigation using two series of compounds (betaxolol analogues and alpidem).
- Utilized Spherisorb CN and Supelcosil LC 18 DB columns for RPLC.
- Measured retention factors (k') and plasma protein binding percentages.
Main Results:
- For betaxolol analogues, increasing O-alkyl chain length increased retention time (k') and plasma protein binding.
- A sigmoidal relationship was observed between free fraction and log k'.
- For alpidem, structural modifications affecting polarity correlated with changes in both k' and protein binding.
Conclusions:
- Chromatographic retention time can serve as a qualitative predictor of plasma protein binding for structurally similar compounds.
- This finding has implications for drug development and pharmacokinetic profiling.