Department of Pharmaceutical Sciences, Nova Southeastern University, College of Pharmacy, Fort Lauderdale, FL, USA.
Drug Dev Ind Pharm. 2013 May;39(5):611-24. doi: 10.3109/03639045.2012.680468. Epub 2012 Apr 26.
The escalating abuse of prescription drugs has recently spawned the development of novel drug formulations resistant to various methods of tampering and misuse.
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.
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.
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.
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.
最近，处方药物的滥用不断升级，促使人们开发出了新型药物制剂，以抵抗各种篡改和误用方法。
本文旨在概述和分类各种制剂方法，以生产出大多数人所说的的防滥用或防篡改剂型。
通过在 Embase™ 和 Medline 中使用关键词“防滥用”和“防篡改”进行全面文献检索，以确定相关技术。仅通过美国专利商标局的 PatFT 搜索了“防滥用组合物”一词，以检查已发布的专利。还从新闻稿和产品创新者网站获取了额外数据。
将确定的制剂方法分为两类，物理方法和化学方法。物理方法进一步细分为固体、凝胶或非故意物质，而化学方法则进一步细分为激动剂/拮抗剂、厌恶剂或代谢物。在指定防滥用方法的已发布专利中，发现了九种不同的方法。大多数正在开发的制剂都结合了多种方法，并利用了制药商的专有技术。
前药和激动剂/拮抗剂制剂在市售产品中很受欢迎，而固体和凝胶方法是最近才加入的。然而，在产品中加入厌恶剂或酶抑制剂证明更难开发。总的来说，详细的制剂和制造方法仍然相当难以保护公众健康。此外，这些创新制剂在普通人群中大多未经尝试，其防滥用效果仍有待证明。
