Nalmefene Nasal Spray Composition for Rapid Emergency Absorption

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Solution Overview

Problem

Existing nalmefene hydrochloride administration methods, such as injections and oral preparations, have slow onset of action and require professional medical personnel, making them unsuitable for rapid and convenient administration in emergencies or for critically ill patients.

Innovation Solution

A stable nasal preparation of nalmefene hydrochloride comprising nalmefene hydrochloride and dodecylphosphocholine, formulated as a nasal spray, which allows for rapid absorption and high bioavailability, enabling untrained individuals to administer an effective dose.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If intravenous or intramuscular injection is used for nalmefene hydrochloride administration, then rapid onset of action is achieved, but professional medical personnel are required and administration is complex

Engineering Contradiction:

Improveonset of actionVSAvoidadministration convenience

Core Design Contradiction:

SpeedVSEase of operation

Solution Approach 1:

The patent uses dodecylphosphocholine as a solubilizing agent and absorption enhancer to enable nalmefene hydrochloride to be administered via nasal spray. This intermediary substance allows the drug to achieve rapid absorption through the nasal mucosa without requiring injection, thus maintaining rapid onset of action while dramatically improving ease of administration for untrained individuals

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent replaces the mechanical injection system (needles, syringes, injection techniques) with a nasal spray delivery system. This substitution eliminates the need for professional medical personnel while maintaining rapid drug delivery through the highly permeable nasal mucosa, achieving both rapid onset and ease of operation

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

2Ease of operation

If oral preparation is used for nalmefene hydrochloride administration, then ease of administration is improved, but onset of action becomes slow

Engineering Contradiction:

Improveadministration convenienceVSAvoidonset of action

Core Design Contradiction:

Ease of operationVSSpeed

Solution Approach 1:

Dodecylphosphocholine acts as an absorption enhancer that facilitates rapid drug uptake through the nasal mucosa. This intermediary enables the oral-like convenience of nasal spray administration while achieving injection-like rapid onset of action, overcoming the slow absorption limitation of traditional oral preparations

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the administration route from oral (slow absorption through gastrointestinal tract) to intranasal (rapid absorption through highly permeable nasal mucosa). This parameter change in the delivery route, combined with the use of dodecylphosphocholine, transforms the onset of action from slow to rapid while maintaining ease of administration

Inventive Principle:

Principle #35Parameter changes

3Productivity

If dodecylphosphocholine is added to the nasal preparation, then absorption and bioavailability are improved, but formulation complexity increases

Engineering Contradiction:

Improveabsorption efficiencyVSAvoidformulation complexity

Core Design Contradiction:

ProductivityVSDevice complexity

Solution Approach 1:

The patent optimizes the concentration of dodecylphosphocholine in the nasal formulation to achieve maximum absorption enhancement while minimizing formulation complexity. By carefully controlling this parameter, the patent achieves high bioavailability without requiring complex multi-component systems or sophisticated delivery devices

Inventive Principle:

Principle #35Parameter changes

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 nasal preparation provides a rapid onset of action and high bioavailability, facilitating easy and timely administration of nalmefene hydrochloride, especially in emergency situations.

Implementation Method 1

nasal administration has the advantages of rapid absorption, high bioavailability

Methodology Applied

Scientific EffectAbsorption: Absorption (physical)

Data Source

PatentUS20260048072A1Pharmaceutical preparation for intranasal administration and preparation method therefor

Publication Date: 2026.02.19 CHENGDU EASTON BIOPHARMACEUTICALS CO LTD

AI summary

The present invention relates to the field of pharmaceutical preparations, and in particular to a composition of a nalmefene hydrochloride nasal preparation and a preparation method therefor. The nalmefene hydrochloride nasal preparation comprises: nalmefene hydrochloride or a hydrate thereof and dodecylphosphorylcholine. A product of the nalmefene hydrochloride nasal preparation is absorbed by the nasal cavity rapidly, so that the problems of inconvenient administration and slow onset of existing preparations are solved, and the technical effect of providing safe, effective, and convenient clinical use is realized.