Polyethylene Oxide Matrix for Zero-Order Release and Abuse Deterrence
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Solution Overview
Problem
There is a need for pharmaceutical dosage forms that provide an extended release of active agents with zero-order release kinetics in a simple and cost-effective manner, while also deterring abuse, particularly for opioid analgesics that are prone to manipulation and misuse.
Innovation Solution
A solid oral extended release pharmaceutical dosage form comprising an extended release matrix formulation with at least one active agent, an anionic surfactant, and at least 40% by weight of polyethylene oxide, which provides a substantially zero-order release profile and abuse-deterrent properties by impeding crushing or pulverization.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Manufacturing precision
If complex tablet structures with multiple layers and membranes are used to achieve zero-order release, then the release control precision is improved, but the device complexity increases
Solution Approach 1:
The patent changes the chemical parameters of the matrix formulation by incorporating specific polymers with controlled degradation rates, surfactants to modify release kinetics, and pH-sensitive materials. This allows zero-order release to be achieved through compositional parameters rather than complex structural design, resolving the contradiction between release precision and structural simplicity
Solution Approach 2:
The patent employs composite matrix materials combining multiple functional components (polymer matrices, surfactants, pH modifiers, and active agents) in a single homogeneous or semi-homogeneous structure. This composite approach achieves complex release profiles through material composition rather than structural complexity, eliminating the need for multiple layers and membranes
2Duration of action of moving object
If extended release dosage forms with higher doses are developed to reduce administration frequency, then the duration of action is improved, but the extent of harmful factors increases due to abuse potential
Solution Approach 1:
The patent converts the high dose content, which is a risk factor for abuse, into a benefit by formulating it in a matrix that provides extended release over 24 hours or longer. The controlled release mechanism ensures that even though the total dose is high, the release rate is controlled to prevent euphoric effects, thereby converting the potential harm of high dosage into the benefit of reduced dosing frequency with maintained safety
Solution Approach 2:
The patent modifies the release rate parameter by using polymers with specific degradation kinetics and surfactants that control dissolution rates. This ensures that the high dose is released slowly and steadily, maintaining plasma concentrations within the therapeutic window and preventing the rapid spike associated with abuse, thus resolving the contradiction between duration extension and abuse deterrence
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The dosage form achieves a controlled and prolonged release of the active agent over 4 to 8 hours, reducing the frequency of administration and minimizing abuse through its formulation, ensuring a pharmaceutically effective and safe delivery of the active agent.
Implementation Method 1
The dosage form achieves a controlled and prolonged release of the active agent over 4 to 8 hours
Implementation Method 2
an extended release matrix formulation with at least one active agent, an anionic surfactant, and at least 40% by weight of polyethylene oxide
Implementation Method 3
an extended release matrix formulation with at least one active agent, an anionic surfactant, and at least 40% by weight of polyethylene oxide
Implementation Method 4
which provides a substantially zero-order release profile and abuse-deterrent properties by impeding crushing or pulverization
Data Source
AI summary
The invention relates to a solid oral extended release pharmaceutical dosage form comprising an extended release matrix formulation. The extended release matrix formulation comprises (1) at least one active agent, (2) at least one anionic surfactant, and (3) at least about 40% by weight (based on the weight of the extended release matrix formulation) of at least one polyethylene oxide. In certain embodiments, the molar ratio of the at least one anionic surfactant to the at least one active agent is from about 1:2 to about 10:1.