Development and Preliminary Experience with an Ease of Extractability Rating System for Prescription Opioids

Abstract

One important factor in the abuse potential of an opioid product is the ease with which active drug can be extracted. There are currently no standards for testing or reporting extractability. This article describes the development of an Extractability Rating System for use by the pharmaceutical industry and regulators. Despite several limitations, this effort serves as a call for standardized testing and reporting so that products can be accurately rated, and should help establish goals for drug developers who wish to develop "abuse-resistant" opioid products.

Tampering with Prescription Opioids: Nature and Extent of the Problem, Health Consequences, and Solutions

“…To this end, abusers have developed both simple and sophisticated tampering methods specific to each drug product to achieve a better high. Examples of tampering methods include (i) separating the opioid compound from excipients and undesirable active ingredients; (ii) overcoming ER formulations (beads, layers, matrices); (iii) removing the opioid compound from high-dose formulations (patches, pills); and (iv) altering dosage forms for alternate routes of administration (2,3).…”

Issues in Long-term Opioid Therapy: Unmet Needs, Risks, and Solutions

“…In addition, extractability studies are needed to determine how easily this formulation can be modified for misuse or abuse. 48 Another added-ingredient approach is the use of the vitamin niacin, which is designed to induce unpleasant, but temporary, symptoms if too many tablets are consumed. 44 The efficacy of agonist-antagonist and agonist-additional active ingredient formulations in reducing misuse and abuse of opioids in the real world is still untested.…”

Designing a tool allowing for a standardized assessment of resistance to drug diversion

“…Some authors attempted to standardize the evaluation of extractability of active principles from pharmaceutics presentations [59]. These authors referred to opioids, but these studies were based on an interesting method.…”