Literature DB >> 26108255

Comparing the Effect of Tampering on the Oral Pharmacokinetic Profiles of Two Extended-Release Oxycodone Formulations with Abuse-Deterrent Properties.

Jeff Gudin1, Naama Levy-Cooperman2, Ernest A Kopecky3, Alison B Fleming3.   

Abstract

OBJECTIVE: Oxycodone DETERx® is an extended-release (ER), microsphere-in-capsule abuse-deterrent-formulation designed to retain its extended-release properties following tampering or misuse (e.g., chewing, crushing). This study assessed the safety and pharmacokinetics of orally administered intact and crushed Oxycodone DETERx® capsules compared with intact and crushed reformulated OxyContin® tablets and crushed immediate-release oxycodone tablets (IR oxycodone).
METHODS: This was a randomized, open-label, active-controlled, cross-over study. Healthy subjects received five oxycodone treatments (40 mg) with a standardized high-fat, high-calorie meal: Oxycodone DETERx® (intact or crushed), OxyContin® (intact or crushed), and IR oxycodone (crushed). Blood samples were collected for assessment of oxycodone plasma concentrations.
RESULTS: Thirty-eight subjects completed the study. Both crushed and intact Oxycodone DETERx® resulted in lower peak plasma concentrations when compared with IR oxycodone. Crushed Oxycodone DETERx® was bioequivalent to intact Oxycodone DETERx® and exhibited a numerically lower Cmax . Also, median Tmax was unchanged by crushing. In contrast, mean peak plasma oxycodone concentrations for crushed OxyContin® were significantly higher compared with intact OxyContin® and were bioequivalent to IR oxycodone. Median Tmax for crushed OxyContin® was the same as IR oxycodone and 3.25 hours shorter than intact OxyContin®.
CONCLUSIONS: These data demonstrate that when crushed and taken orally, Oxycodone DETERx® maintains its EXTENDED-release profile, while crushed OxyContin® shows a pharmacokinetic profile similar to an immediate-release product. These results suggest that Oxycodone DETERx® may be less attractive to illicit drug users compared with existing abuse-deterrent-formulations, while providing a safer option for patients who may unknowingly crush their medication such as those who have difficulty swallowing. Wiley Periodicals, Inc.

Entities:  

Keywords:  Abuse; Abuse-Deterrent; Extended-Release; Opioids; OxyContin®; Oxycodone DETERx®; Pharmacokinetics; Tamper

Mesh:

Substances:

Year:  2015        PMID: 26108255     DOI: 10.1111/pme.12834

Source DB:  PubMed          Journal:  Pain Med        ISSN: 1526-2375            Impact factor:   3.750


  15 in total

Review 1.  Drug Formulation Advances in Extended-Release Medications for Pain Control.

Authors:  Mark R Jones; Martin J Carney; Rachel J Kaye; Amit Prabhakar; Alan D Kaye
Journal:  Curr Pain Headache Rep       Date:  2016-06

Review 2.  Options for Treating Pain in Cancer Patients with Dysphagia.

Authors:  Sebastiano Mercadante
Journal:  Drugs       Date:  2017-04       Impact factor: 9.546

Review 3.  Updated Clinical Pharmacokinetics and Pharmacodynamics of Oxycodone.

Authors:  Mari Kinnunen; Panu Piirainen; Hannu Kokki; Pauliina Lammi; Merja Kokki
Journal:  Clin Pharmacokinet       Date:  2019-06       Impact factor: 6.447

Review 4.  Oxycodone DETERx® ER Capsules: A Review in Severe, Chronic Pain.

Authors:  Yvette N Lamb; Karly P Garnock-Jones; Susan J Keam
Journal:  Drugs       Date:  2016-12       Impact factor: 9.546

Review 5.  America's Opioid Epidemic: a Comprehensive Review and Look into the Rising Crisis.

Authors:  Peter S Ostling; Kelly S Davidson; Best O Anyama; Erik M Helander; Melville Q Wyche; Alan D Kaye
Journal:  Curr Pain Headache Rep       Date:  2018-04-04

6.  Pharmacokinetics and Bioequivalence Evaluation of a New Oxycodone Tamper-Resistant Tablet Administered with an Opioid Antagonist in Patients with Chronic Pain.

Authors:  Zhu Luo; Jia Miao; Shiqing Shu; Ying Wang; Xiaohong Zhu; Chao Hu; Yali Shen
Journal:  Clin Drug Investig       Date:  2020-02       Impact factor: 2.859

Review 7.  Oxycodone DETERx®: A Novel Abuse-Deterrent, Extended-Release Analgesic Option for the Treatment of Patients with Chronic Pain.

Authors:  Jeff Gudin
Journal:  Pain Ther       Date:  2016-11-21

Review 8.  Oral drug therapy in elderly with dysphagia: between a rock and a hard place!

Authors:  Serena Logrippo; Giovanna Ricci; Matteo Sestili; Marco Cespi; Letizia Ferrara; Giovanni F Palmieri; Roberta Ganzetti; Giulia Bonacucina; Paolo Blasi
Journal:  Clin Interv Aging       Date:  2017-01-31       Impact factor: 4.458

9.  Response to Crudele et al. Commentary on Gudin et al. "Comparing the Effect of Tampering on the Oral Pharmacokinetic Profiles of Two Extended-Release Oxycodone Formulations with Abuse-Deterrent Properties".

Authors:  Jeff Gudin; Ernest A Kopecky; Alison B Fleming
Journal:  Pain Med       Date:  2017-05-01       Impact factor: 3.750

10.  Nonmedical Use of Xtampza® ER and Other Oxycodone Medications in Adults Evaluated for Substance Abuse Treatment: Real-World Data from the Addiction Severity Index-Multimedia Version (ASI-MV®).

Authors:  Jody L Green; Rebekkah S Robbins; Taryn Dailey-Govoni; Stephen F Butler
Journal:  J Pain Res       Date:  2021-06-15       Impact factor: 3.133

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