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Steady-state bioavailability of controlled-release oxycodone in normal subjects
R F Reder1, B Oshlack, J B Miotto
1Pharmaceutical and Clinical Research, Purdue Frederick Company, Norwalk, Connecticut, USA.
Clinical Therapeutics
|January 1, 1996
Summary
Controlled-release (CR) oxycodone tablets offer comparable bioavailability to immediate-release (IR) oxycodone solutions but with slower absorption. This CR formulation enhances therapeutic flexibility for pain management.
Area of Science:
- Pharmacology
- Clinical Pharmacy
Background:
- Oxycodone is a widely used analgesic.
- Controlled-release (CR) formulations aim to provide sustained drug delivery.
- Immediate-release (IR) formulations offer rapid drug delivery.
Purpose of the Study:
- To compare the steady-state bioavailability and pharmacokinetics of CR oxycodone tablets versus IR oxycodone solution.
- To evaluate the safety and tolerability profiles of both formulations.
Main Methods:
- A randomized, analytically masked, multiple-dose, crossover study was conducted in 24 healthy subjects.
- Subjects received either CR oxycodone tablets (10 mg every 12 hours) or IR oxycodone solution (5 mg every 6 hours) for 4 days.
- Plasma oxycodone concentrations were measured to determine pharmacokinetic parameters.
Main Results:
- Steady-state bioavailability was similar between CR and IR oxycodone (AUC 0-12h: 103.6 vs 99.0 ng.h/mL).
- The time to maximum concentration (Tmax) was significantly longer for CR oxycodone (3.2 hours) compared to IR oxycodone (1.4 hours) (P=0.005).
- Fewer adverse experiences were reported with CR oxycodone compared to IR oxycodone.
Conclusions:
- CR oxycodone tablets demonstrate equivalent bioavailability to IR oxycodone solutions.
- The CR formulation exhibits slower absorption, indicated by a longer Tmax.
- CR oxycodone offers enhanced therapeutic flexibility through independent titration and dosing for pain management.