Insights from BCC Research

Technological Advancements in Opioid Drugs

Posted by BCC Research Staff Analysts on Nov 30, 2018 10:00:00 AM

Opioid-Technology-Advancement

BCC Research’s just published report Opioid Drugs: Global Markets to 2023 provides a comprehensive overview of the opioid market as well as the market for abuse prevention technologies. This edited excerpt provides an overview of a few of these emerging technologies.

Prescription opioids are prescribed for the treatment of chronic pain. High usage and consumption of opioids have resulted in opioid misuse and led to an opioid crisis, especially in the U.S. The fatal drug overdose rate has risen significantly in the last decade.

Abuse-deterrent formulations (ADFs) of opioids are intended to control opioid drug abuse incidence. These formulations retain the efficacy of the drug and minimize the risk of abuse. Abusers often seek to accelerate the absorption of opioids into the bloodstream by crushing them to swallow, snort or smoke the drug or dissolving them to inject the drug. Abuse-deterrent technology contains physical and chemical barriers that are intended to reduce the potential for these forms of abuse.

Pharmaceutical companies are developing numerous abuse‑deterrent products and product candidates, using a variety of technologies. These strategies of abuse-deterrent formulations generally fall under the following categories.

The DETERx Platform Technology

DETERx is a novel, proprietary, patented platform technology of Collegium Pharmaceutical Inc. The technology is designed to maintain the extended-release and safety profiles of highly abused drugs in the face of various methods of abuse and tampering including chewing, crushing or dissolving and then taking them orally or by snorting or injecting.

The DETERx formulation consists of wax-based microspheres that are filled into a capsule. The microspheres are spherical micron-sized beads that are prepared by combining the active ingredient with inactive ingredients. Each microsphere, whether inside or outside the capsule, is designed for abuse deterrence and extended release. The active ingredient is solubilized and homogenously dispersed in each microsphere. More information on the technology’s patents can be found in the full report.

Collegium Pharmaceutical developed the drug Xtampza using DETERx technology. Xtampza microspheres have a median particle size of approximately 300 microns and are composed of the active ingredient (oxycodone), a fatty acid, wax and surfactant excipients, which are all generally recognized as safe (GRAS) by the FDA. The microspheres are formulated through a proprietary melt process in which the active ingredient, as a free base, is combined with fatty acid, wax and surfactant excipients to form a molten solution in which the base is solubilized via an ionic interaction with the fatty acid. The resulting homogenous liquid is spray congealed into small droplets using a proprietary spinning disk manufacturing process. The droplets rapidly congeal into solid wax‑based microspheres, which are then filled into capsules. Differing product strengths are achieved by varying the weight of the microspheres loaded into a capsule. When administered orally as directed, the Xtampza formulation is designed to be administered every 12 hours and releases oxycodone over an extended period in the GI tract by diffusion from the microspheres into gastrointestinal fluids.

Aversion Technology

Acura Pharmaceuticals Inc. owns the proprietary rights of the Aversion platform technologies, which can be used to develop abuse-deterrent products. The technology incorporates gelling ingredients and irritants into tablets to prevent drug abuse by snorting and provide barriers to abuse. The technology prevents drug abuse even for intravenous use. If the abuser mixes the active ingredients with solvents such as alcohol or water to prepare an intravenous injection, the mixing of solvent with the active drug component leads to a conversion of the viscous gel mixture. The gel mixture traps the active ingredient in the gel. Aversion Technology and related opioid products, like Oxaydo, are covered by six U.S. patents, which will lose exclusivity between November 2023 and November 2024.

The SentryBond Technology Platform

The technology, developed by Inspirion Delivery Sciences, combines inactive excipients with active pharmaceutical ingredients in a tablet that is specifically designed to prevent the abuse through various methods of manipulation and routes of administration. For instance, when the drug is subjected to physical manipulation or chemical extraction, SentryBond is designed to maintain the intended release profile of extended-release products and to delay the release of immediate-release products. The technology imparts abuse-deterrent characteristics through physical and chemical methods, without the use of antagonist or aversive agents. The technology is covered by patents in the U.S., and multiple global patent applications are pending.

Guardian Technology

Guardian Technology is a proprietary technology of Egalet Corp. The technology is a polymer matrix tablet that utilizes a novel application of injection molding, which results in tablets that are hard and difficult to manipulate for misuse and abuse. The construct of the tablet allows for controlled release of the active pharmaceutical ingredient in the gastrointestinal tract. This approach offers the ability to design drugs with controlled-release profiles as well as physical and chemical properties that have been demonstrated to resist both common and rigorous methods of manipulation. Drugs manufactured with Guardian Technology have shown increased resistance to physical methods of manipulation, such as crushing, cutting, grinding or breaking using a variety of electrical and mechanical tools. The drugs are also resistant to chemical manipulation and turn into a viscous hydrogel on contact with liquid, making intravenous injection difficult.

BeadTek Technology

Pernix Therapeutics Inc. developed BeadTek technology for abuse-deterrent formulations of opioid drugs. Using this technology, the company developed Zohydro ER. The technology encompasses an indistinguishable mix of inactive beads, active immediate-release hydrocodone beads and active extended-release hydrocodone beads. Zohydro ER with BeadTek delivers an extended release of hydrocodone that provides a 12 hour-dose duration. When taken as prescribed, the inactive beads contained in Zohydro ER with BeadTek remain inert. The inactive beads dissolve independently of the active hydrocodone beads. They are designed not to change the 12 hour-release properties of the medication when taken as directed. However, when the drug is crushed or dissolved in liquids or solvents, a viscous gel is formed that traps the active ingredient within the gel.

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Topics: Pharmaceuticals, Life Sciences