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Lisdexamfetamine and amphetamine pharmacokinetics in oral fluid, plasma, and urine after controlled oral administration of lisdexamfetamine
Author(s) -
Comiran Eloisa,
Carlos Graciela,
Barreto Fabiano,
Pechanksy Flavio,
Fröehlich Pedro E.,
Limberger Renata P.
Publication year - 2021
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.2254
Subject(s) - pharmacokinetics , oral administration , prodrug , urine , pharmacology , chemistry , metabolite , active metabolite , stimulant , medicine , biochemistry
Abstract Lisdexamfetamine (LDX) is a long‐acting prodrug stimulant indicated for the treatment of attention‐deficit/hyperactivity disorder (ADHD) and binge‐eating disorder (BED) symptoms. In vivo hydrolysis of the LDX amide bond releases the therapeutically active d ‐amphetamine ( d ‐AMPH). This study aims to describe the pharmacokinetics of LDX and its major metabolite d ‐AMPH in human oral fluid, urine and plasma after a single 70 mg oral dose of LDX dimesylate. Six volunteers participated in the study. Oral fluid and blood samples were collected for up to 72 h and urine for up to 120 h post‐drug administration for the pharmacokinetic evaluation of intact LDX and d ‐AMPH. Samples were analyzed by LC‐MS/MS. Regarding noncompartmental analysis, d ‐AMPH reached the maximum concentration at 3.8 and 4 h post‐administration in plasma and oral fluid, respectively, with a mean peak concentration value almost six‐fold higher in oral fluid. LDX reached maximum concentration at 1.2 and 1.8 h post‐administration in plasma and oral fluid, respectively, with a mean peak concentration value almost three‐fold higher in plasma. Intact LDX and d ‐AMPH were detected in the three matrices. The best fit of compartmental analysis was found in the one‐compartment model for both analytes in plasma and oral fluid. There was a correlation between oral fluid and plasma d ‐AMPH concentrations and between parent to metabolite concentration ratios over time in plasma as well as in oral fluid.

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