Collegium Pharmaceuticals is developing an abuse-deterrent, sustained-release oral oxycodone formulation (COL-003). The DETERx delivery technology consists of a multiparticulate matrix formulation in a capsule that is designed to be less susceptible to common methods of tampering, such as crushing or chewing prior to ingestion. Company studies showed that the plasma profile for the new-formulation pill was bioequivalent whether it was chewed or taken whole as intended. "It’s an abuse-resistant formulation in that they can’t extract more than is intended for its delivery," Dr. Webster said.
Remoxy (Pain Therapeutics and King Pharmaceuticals) is a long-acting oral oxycodone for the treatment of moderate to severe chronic pain. "This is what I consider an opioid-resistant formulation, meaning it’s got a barrier that is hard to crush, hard to manipulate; and it’s hard to extract" the oxycodone, Dr. Webster said. "It can’t be chewed, snorted, or injected very easily."
A new transmucosal buprenorphine patch is also in the trial phase. According to PharmacoFore, the delivery system’s developer, the novel Bio-Activated Molecular Delivery (Bio-MD) technology deters prescription drug abuse at a molecular level.
"This technology does not involve the reformulation of existing opioid drugs in physical matrices that are easily circumvented by simple extraction methods. Our opioid Bio-MD systems are ‘activated’ to release clinically effective opioid drugs only when exposed to the correct physiologic conditions (i.e., ingested)," the company noted on its Web site.
Essentially, an opioid molecule – any opioid – is attached to the delivery compound. "It’s kind of like a clock. The intrinsic trypsin in our GI tract will activate that clock, which will ... allow that drug to be released," Dr. Webster said. The clock determines how much time it will take for the active compound to be released.
"It’s very early on," he cautioned. The delivery system is in phase I trials. Still, "it looks very interesting that they have the technology now to address multipill abuse. There are ways to design the same technologies so that the triggering system will only allow a certain number of pills or milligrams of medication to be absorbed." Thus, regardless of how many pills an individual takes, no more than the prescribed dose is bioavailable.
Dr. Webster reported that he has significant financial relationships with a number of pharmaceutical companies, including King Pharmaceuticals and Collegium Pharmaceutical.