Nalmefene Formulation with Absorption-Enhancing Adjuvants
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Solution Overview
Problem
Current antidotes for opioid overdose have a lag time in absorption, which can lead to insufficient counteraction of opioid overdose effects, resulting in morbidity and mortality due to the delay in reaching therapeutic levels.
Innovation Solution
A pharmaceutical composition comprising a therapeutically effective amount of an opioid antagonist, such as nalmefene, combined with absorption-enhancing adjuvants like nitric oxide inducers, niacin, or magnesium chloride, to facilitate rapid systemic absorption post-intramuscular or subcutaneous injection, achieving a quick onset of action within 5 minutes or less.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If an opioid antagonist is administered via intramuscular injection to counteract opioid overdose, then the antidote can be delivered effectively, but there is a lag time before the antidote reaches therapeutic levels sufficient to counteract the opioid effects
Solution Approach 1:
The patent changes the physical-chemical parameters of the opioid antagonist formulation by incorporating absorption-enhancing adjuvants (such as nitric oxide inducers, niacin, phosphodiesterase inhibitors, ACE inhibitors, angiotensin receptor blockers, calcium-channel blockers, nitrates, or magnesium chloride). These adjuvants modify the absorption characteristics of the parenteral formulation, accelerating the rate at which the opioid antagonist enters the bloodstream and reaches therapeutic levels, thereby reducing the lag time while maintaining treatment effectiveness.
2Power
If the same dose of opioid analgesic is administered parenterally, then the dose is more potent, but this increases the risk of abuse and overdose
Solution Approach 1:
The patent applies preliminary action by pre-administering absorption-enhancing adjuvants in the formulation before the opioid antagonist needs to be absorbed. These adjuvants are already present in the parenteral formulation and immediately begin enhancing absorption upon injection, creating a preparatory effect that accelerates drug uptake. This preliminary enhancement of absorption capacity allows for safer dosing strategies and reduces the window of opportunity for abuse while maintaining therapeutic potency.
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 composition provides a rapid onset of action, with a mean time to maximum plasma concentration of nalmefene of 2 hours or less intramuscularly and 1 hour or less subcutaneously, effectively counteracting opioid overdose symptoms and preventing morbidity and mortality.
Implementation Method 1
an adjuvant that promotes, enhances, or quickens the systemic absorption rate of the opioid antagonist post intramuscular or subcutaneous injection
Data Source
AI summary
Disclosed in certain embodiments is a pharmaceutical formulation (e.g., parenteral formulation) comprising a therapeutically effective amount of nalmefene or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable adjuvant (e.g., parenterally acceptable adjuvant) that promotes the rate at which the nalmefene or salt thereof is more rapidly absorbed into the systemic circulation of a subject identified as in need thereof.