Population model analysis of chiral inversion and degradation of bupropion enantiomers, and application to enantiomer specific fraction unbound determination in rat plasma and brain

• Published in: Journal of pharmaceutical and biomedical analysis Vol. 195; p. 113872
• Main Authors: Bhattacharya, Chandrali, Masters, Andrea R., Bach, Christine, Stratford, Robert E.
• Format: Journal Article
• Language: English
• Published: England Elsevier B.V 20.02.2021
• Subjects: Animals; Bioanalysis; Brain; Bupropion; Chiral inversion; In vitro model; Kinetics; Pharmaceutical Preparations; Pharmacokinetic modeling; Protein binding; Rats; Stereoisomerism; Bupropion; Bioanalysis; In vitro model; Kinetics; Chiral inversion; Pharmacokinetic modeling; Protein binding

•Chiral inversion was faster than enantiomer degradation in plasma and brain.•Chiral inversion was faster in plasma (three to five-fold) than brain or buffer.•A model was developed to quantify parallel inversion and degradation kinetics.•Model approach provided reliable enantiomer binding estimates...