An abuse-deterrent, microsphere-in-capsule formulation of extended-release oxycodone: alternative modes of administration to facilitate pain management in patients with dysphagia

Abstract

Oxycodone DETERx is the first ER oxycodone formulation that can be administered either intact, sprinkled onto soft foods, or via NG/G tubes, thereby providing options for treating pain in patients who have difficulty swallowing.

The Comparative Pharmacokinetics of Physical Manipulation by Crushing of Xtampza ® ER Compared with OxyContin ®

“…The physicochemical properties of Xtampza ER that limit its ability to be manipulated may help reduce the incidence of unintentional misuse by patients or their caregivers who manipulate analgesics to make them easier to swallow or to enable a different route of administration. In addition to these abuse-deterrent properties, Xtampza ER can be administered via multiple modes [11], allowing clinicians to prescribe one analgesic that can provide treatment for patients who require different modes of administration (e.g., intact, sprinkled onto food, poured into a nasogastric/gastric tube).…”

“…An added benefit of Xtampza ER is the microsphere-in-capsule design. Each microsphere functions as an individual ER drug delivery system, allowing for multiple modes of administration (intact, sprinkled onto food and via nasogastric/gastric tubes) without losing the ER characteristics [11]. This unique design may limit the misuse that occurs when patients, patient caregivers and healthcare providers manipulate ER abuse-deterrent formulation analgesics to facilitate swallowing or enable other modes of administration [11].…”

Oxycodone DETERx®: A Novel Abuse-Deterrent, Extended-Release Analgesic Option for the Treatment of Patients with Chronic Pain

“…Several studies (described in detail in this review) have demonstrated that this microsphere technology ensures the maintenance of the ER characteristics if the capsule contents are crushed or chewed and ingested orally or crushed and insufflated (snorted) intranasally; as a result, oxycodone DETERx is the first oral ER-formulated opioid without language in its boxed warning pertaining to crushing or chewing leading to potential exposure to a fatal dose of opioid. The oxycodone DETERx formulation allows for alternative modes of administration, including sprinkling directly into the mouth from a dosing cup or onto soft foods, as well as administering via nasogastric or gastrostomy tubes [21, 22], making oxycodone DETERx an option for patients with chronic pain who also have difficulty swallowing.

Fig. 1Photograph showing the spherical, microparticulate nature of oxycodone DETERx capsule contents.

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“…The mean plasma oxycodone concentrations over time were superimposable for sprinkled and intact oxycodone DETERx (Fig. 2a), and the peak serum concentration and extent of oxycodone absorption were bioequivalent (Table 2) [20, 22].

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“…The safety of oxycodone DETERx was evaluated in multiple phase 1 single-dose studies [22, 23, 25–27] and one randomized, double-blind, phase 3 study [24]; the treatment-emergent adverse events (AEs) reported during the titration and maintenance portions of the phase 3 study are shown in Table 3. Treatment-related AEs were reported in 366 (50%) patients in the open-label titration phase.…”