Inhalable L-Epinephrine Formulation for Transmucosal Absorption
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Solution Overview
Problem
Current epinephrine autoinjectors are cumbersome, prone to degradation, costly, and pose needle-related fears, with poor oral bioavailability and rapid degradation when administered orally, limiting their effectiveness in emergency situations like anaphylaxis and sepsis.
Innovation Solution
Development of sublingual and intranasal l-epinephrine formulations that utilize transmucosal absorption to maintain elevated plasma epinephrine levels, avoiding gastrointestinal degradation and needle fears, with methods for consecutive dosing to sustain blood pressure and breathing stabilization.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If traditional epinephrine autoinjectors are used, then rapid epinephrine delivery is achieved, but the device is cumbersome, degrades quickly, and causes needle fear
Solution Approach 1:
The patent replaces the mechanical injection system (needle and syringe) with a chemical delivery system using effervescent tablets that dissolve in water to release epinephrine. This substitution eliminates the mechanical penetration mechanism while maintaining rapid drug delivery through oral ingestion of the dissolved formulation.
Solution Approach 2:
The patent changes the physical and chemical parameters of epinephrine delivery by converting it from a sterile injectable solution to a stable solid tablet form containing effervescent agents. This parameter change allows the drug to be stored at room temperature, transported easily, and administered without needles, while still achieving rapid absorption when dissolved in water.
2Ease of operation
If oral epinephrine administration is used, then needle fear is avoided, but gastrointestinal degradation occurs and bioavailability is poor
Solution Approach 1:
The patent introduces water as an intermediary medium that dissolves the effervescent tablet and facilitates epinephrine absorption. The water-based solution allows the drug to bypass gastrointestinal degradation by enabling rapid absorption through the mucous membranes of the mouth and throat, while still using the convenient oral administration route.
Solution Approach 2:
The effervescent reaction creates a periodic action pattern where carbon dioxide bubbles form and release the epinephrine in controlled pulses. This bubbling action enhances mixing and contact between the drug and absorptive surfaces, improving bioavailability while maintaining the simplicity of oral administration.
3Loss of time
If epinephrine is stored in autoinjectors, then immediate use is possible, but the product degrades rapidly and requires frequent replacement
Solution Approach 1:
The patent segments the epinephrine delivery system into separate components: a stable solid effervescent tablet containing the drug and a separate water source. This segmentation allows the epinephrine to be stored in a stable, non-degradable solid form for extended periods, while still enabling rapid dissolution and absorption when needed by simply adding water.
Solution Approach 2:
The effervescent agents are pre-loaded into the tablet in a stable solid form, prepared in advance for rapid dissolution. This preliminary preparation allows the drug to remain stable during storage while being ready for immediate action when water is added, eliminating the need for refrigeration or frequent replacement of pre-filled injectors.
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 sublingual and intranasal l-epinephrine formulations provide a safer, more convenient, and effective means to maintain stable blood pressure and breathing, overcoming the limitations of traditional autoinjectors by ensuring consistent epinephrine absorption and prolonged efficacy.
Implementation Method 1
The inhalable l-epinephrine formulation is adapted for transmucosal absorption
Data Source
AI summary
The present disclosure provides methods of mimicking epinephrine plasma pharmacokinetic parameters/plasma epinephrine levels of an at least one l-epinephrine injection in humans with an at least one intranasal dosage of an inhalable l-epinephrine formulation adapted for transmucosal absorption. Dosages for sublingual or buccal absorption and/or oral inhalation are also provided. These methods may be helpful when l-epinephrine injection is not available or not possible. The present disclosure also provides methods of pretreating breathing difficulty before intranasal treatment of anaphylaxis. The present disclosure allows formulations for intranasal administration of l-epinephrine to be conveniently carried by soldiers and others, such as in a remote location or battlefield, and such as when emergency medical services are not readily available or accessible. The methods may be able to sustain life and restore proper blood perfusion when someone is having cardiopulmonary difficulty until medical help or transport can arrive.