Current approaches in tamper-resistant and abuse-deterrent formulations

Abstract

Context: The escalating abuse of prescription drugs has recently spawned the development of novel drug formulations resistant to various methods of tampering and misuse.

Objective: The intent of this paper is to provide an overview and classification system of formulation approaches, developed to produce what most refer to as abuse-deterrent or tamper-resistant dosage forms.

Methods: A comprehensive literature search was conducted within Embase™ and Medline using key words "abuse deterrentâ and "tamper resistantâ to identify relevant technologies. Only issued patents were examined using the phrase "abuse deterrent compositionâ searched through PatFT from the United States Patent and Trademark Office. Current information from press releases and product innovator websites was obtained for additional data.

Results: Identified formulation approaches were organized into two categories, physical approaches and chemical approaches. Physical approaches were subcategorized into solids, gels or non-intentionals, while chemical approaches were further broken down into agonists/antagonists, aversives, or metabolics. Among issued patents specifying an abuse-deterrent method, nine diverse approaches were found. Most formulations under development combined approaches, and utilized proprietary technologies from pharmaceutical manufacturers.

Conclusions: Prodrug and agonist/antagonist formulations are popular in marketed products, while solid and gel approaches are more recent additions. However, the inclusion of aversive agents or enzyme inhibitors in a product is proving to be more difficult to develop. Overall, detailed formulation and manufacturing methods still remain rather elusive to protect public health. Moreover, these innovative formulations are mostly untried in the general population and their abuse deterring effects has yet to be proven.