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Steady-state pharmacokinetic comparison of a new, once-daily, extended-release morphine formulation (Morphelan^TM) and OxyContin® twice daily

Ligand Pharmaceuticals Inc., San Diego, California

Rita Geiser, RN

Ligand Pharmaceuticals Inc., San Diego, California

Gordon Loewen, PhD

Ligand Pharmaceuticals Inc., San Diego, California

Context. Morphelan² (morphine sulfate extended release), a new, once-daily, oral morphine sulfate formulation, releases morphine in a dual-release manner, providing an initial rapid delivery while maintaining therapeutic morphine concentrations throughout a 24-hour period with minimal fluctuation.

Objective. The primary objective of this study was to compare steady-state pharmacokinetic (PK) profiles of morphine and oxycodone following administration of 60 mg of Morphelan, once daily and 20 mg of OxyContin¹ (oxycodone hydrochloride controlled release) twice daily, respectively.

Design, Setting, Participants, Intervention. Thirty-five healthy subjects were randomized to receive Morphelan once daily, or OxyContin twice daily for 7 days in this multiple-dose, open-label, parallel design study.

Measures. Blood samples were obtained on day 7 to determine differences, if any, in the PK parameters that characterize the ability of the formulations to control the release of drug. Safety data were collected throughout the study.

Results. Thirty-two subjects completed the study; 31 subjects were eligible for PK evaluation. The time to reach and maintain threshold concentrations of 50% or 75% of maximum was comparable for Morphelan and OxyContin. However, in comparison to OxyContin twice daily, once-daily Morphelan provided a statistically significantly reduced peak-to-trough fluctuation (%FI = 91% vs 77%, respectively, P= 0.05) and a lower number of fluctuations (2 vs 1, respectively) over a 24-hour period.

Conclusions. Once-daily Morphelan provided an initial rapid release of opioid reaching and maintaining threshold concentrations of 50% and 75% of maximum comparable to OxyContin twice daily. However, Morphelan provided more consistent opioid concentrations throughout a 24-hour period, with less frequent dosing.

Key Words: Morphine • oxycodone • sustained release • extended release • pain • pharmacokinetics

Journal of Oncology Pharmacy Practice, Vol. 7, No. 1, 1-8 (2001)
DOI: 10.1191/1078155201jp075oa


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