Epinephrine Nasal Spray Formulation for Rapid Anaphylaxis Treatment
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Solution Overview
Problem
Current treatments for anaphylaxis, such as injectable epinephrine, may not provide rapid or effective relief due to administration challenges and variability in absorption.
Innovation Solution
A pharmaceutical spray formulation containing 0.5% to 25% w/w of epinephrine or its salt in water, with optional additives like antioxidants, antimicrobial preservatives, and isotonicity agents, designed for nasal delivery to achieve rapid systemic absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If injectable epinephrine is used for treating anaphylaxis, then the treatment can deliver epinephrine systemically, but the administration is challenging and absorption varies
Solution Approach 1:
The patent replaces the mechanical injection system with a nasal spray formulation that utilizes the nasal mucosa's natural absorptive properties. The spray delivers epinephrine directly to the highly vascular nasal mucosal tissue, allowing rapid absorption into the bloodstream without requiring injection skills or dealing with variable intramuscular absorption. This substitution of administration route from parenteral to mucosal delivery resolves both the ease of operation and reliability contradictions.
2Speed
If traditional epinephrine formulations are used, then the drug can be delivered, but rapid systemic absorption is not achieved
Solution Approach 1:
The patent changes the physical and chemical parameters of the epinephrine formulation by creating a pH-adjusted spray solution (pH 3.0-5.0) that is optimized for nasal mucosa contact. This parameter change enables the formulation to maintain epinephrine stability while facilitating rapid absorption through the nasal mucosa. The spray delivery system also changes the physical state from injectable solution to aerosol droplets, increasing surface area contact and absorption rate, thereby achieving both rapid speed and adequate quantity of systemic availability.
3Reliability
If epinephrine concentration is increased to achieve therapeutic effect, then the treatment efficacy improves, but the formulation stability decreases
Solution Approach 1:
The patent creates a composite formulation system that combines epinephrine with specific excipients including buffers (phosphate, citrate, or acetate buffer at pH 3.0-5.0), antioxidants (sodium metabisulfite or sodium bisulfite), and preservatives (benzalkonium chloride or chlorobutanol). This composite material approach allows the formulation to maintain high epinephrine concentrations (0.1-10 mg/mL) while ensuring stability through the synergistic protective effects of multiple components. The buffer system maintains optimal pH for both stability and absorption, while antioxidants prevent oxidation of epinephrine even at high concentrations.
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 spray formulation enables rapid absorption of epinephrine, achieving therapeutic plasma concentrations within minutes, thereby providing quick relief from anaphylaxis symptoms.
Implementation Method 1
The spray formulation enables rapid absorption of epinephrine, achieving therapeutic plasma concentrations within minutes
Data Source
AI summary
Provided herein are epinephrine spray formulations. Also provided herein are methods of treating anaphylaxis by administering epinephrine spray formulations to subjects in need of such treatment.