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In vitro assessment of the potential for abuse via the intravenous route of oxycodone DETERx® microspheres

Alison B. Fleming, PhD, Todd A. Scungio, BA, Michael P. Grima, BS, Stephen P. Mayock, BS

Abstract


Objective: Abuse of prescription analgesics is a well-recognized problem, with

nearly 2 million people aged 12 years or older initiating nonmedical use of pain

relievers in 2012. The prevalence of opioid abuse via intravenous (IV) injection

has led to the development of dosage forms designed to deter abuse using different

inactive ingredients and formulation strategies. This study evaluated the IV abuse

potential for a novel, microsphere-encapsulated abuse-deterrent formulation of

oxycodone, Xtampza™ ER (referred to as “oxycodone DETERx”).

Methods: The extraction of oxycodone DETERx and two comparators, extendedrelease

oxycodone (oxycodone ER) and immediate-release oxycodone (oxycodone

IR), was evaluated in small volumes (5 and 10 mL) of water after manipulation of

the dosage forms. The syringeability and injectability of these products were evaluated

to determine the feasibility of using these products via IV injection.

Results: The extraction of oxycodone from oxycodone DETERx was nominal,

with <12 percent extracted under any test condition. Oxycodone ER and oxycodone

IR had as much as 83 and 98 percent oxycodone extracted, respectively.

Injectability and syringeability analyses showed that injection of oxycodone

DETERx microspheres in suspension is not feasible. In contrast, oxycodone ER

and oxycodone IR suspensions were more easily drawn into and expelled from a

syringe. Furthermore, injection of molten oxycodone DETERx microspheres was

also shown to be ineffective.

Conclusion: The chemical and physical properties of oxycodone DETERx provide

barriers to manipulating the microspheres for the purpose of IV injection.


Keywords


opioid, abuse deterrent, oxycodone, DETERx, IV injection, Xtampza ER

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References


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DOI: https://doi.org/10.5055/jom.2016.0312

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