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Characterization and validation of a pharmacokinetic model for controlled-release oxycodone
J W Mandema1, R F Kaiko, B Oshlack
1Stanford University School of Medicine, Department of Anesthesia, California, USA.
British Journal of Clinical Pharmacology
|December 1, 1996
Summary
Controlled-release oxycodone tablets offer effective pain management with twice-daily dosing. This study validates a pharmacokinetic model for CR oxycodone, showing it maintains therapeutic levels longer than immediate-release formulations.
Area of Science:
- Pharmacology
- Pharmacokinetics
- Drug Development
Background:
- Oxycodone is a potent opioid analgesic for moderate to severe pain.
- Immediate-release (IR) formulations require frequent dosing.
- Controlled-release (CR) oxycodone tablets were developed for improved dosing convenience.
Purpose of the Study:
- To develop and validate a pharmacokinetic model for CR oxycodone tablets.
- To compare the pharmacokinetic profiles of CR oxycodone tablets with IR oxycodone solution.
Main Methods:
- A single-dose, randomized, crossover study in 24 healthy male volunteers.
- Pharmacokinetic modeling using NONMEM version IV.
- Model validation using repeated-dose data from 21 additional volunteers.
Main Results:
- A one-compartment model best described oxycodone disposition.
- CR oxycodone absorption followed a bi-exponential model with rapid and slow phases.
- CR oxycodone tablets demonstrated 102.7% bioavailability compared to IR solution.
- The developed model accurately predicted plasma concentrations during repeated dosing.
Conclusions:
- CR oxycodone tablets provide rapid achievement and sustained maintenance of therapeutic plasma concentrations.
- The pharmacokinetic profile of CR oxycodone supports a 12-hourly dosing regimen.
- CR oxycodone offers a viable alternative for effective pain management with improved dosing frequency.