Diazepam Nasal Spray Dosing for Food-Effect Seizure Rescue

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Solution Overview

Problem

Current benzodiazepine delivery methods for treating seizures, such as rectal and intranasal administration, suffer from limitations including social embarrassment, inaccurate dosing, nasal irritation, and delayed onset of action, which can lead to under-dosing and decreased efficacy, especially in seizure emergencies.

Innovation Solution

A nasal spray formulation of diazepam with a multimodal delivery profile that includes a first and potentially a second dose, adjusted to compensate for food effects, ensuring rapid and complete drug absorption through nasal and other mucosal routes, thereby achieving a higher effective dose than traditional methods.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If rectal administration is used to deliver benzodiazepine, then the drug can be delivered to treat seizures, but social embarrassment occurs

Engineering Contradiction:

Improveease of administrationVSAvoidsocial embarrassment

Core Design Contradiction:

Ease of operationVSObject-affected harmful factors

Solution Approach 1:

The invention extracts the drug delivery function from the rectal route and relocates it to the nasal cavity, eliminating the social embarrassment associated with rectal administration while maintaining effective drug delivery for seizure treatment

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The nasal spray formulation acts as an intermediary delivery system, providing a socially acceptable alternative to rectal administration while achieving the same therapeutic effect through the nasal mucosa absorption route

Inventive Principle:

Principle #24Intermediary (Mediator)

2Speed

If intranasal administration is used to deliver benzodiazepine, then the drug can be delivered rapidly, but nasal irritation and inaccurate dosing occur

Engineering Contradiction:

Improveonset of actionVSAvoidnasal irritation

Core Design Contradiction:

SpeedVSObject-affected harmful factors

Solution Approach 1:

The invention modifies the formulation parameters by incorporating hydrophilic polymers and adjusting the concentration of benzodiazepine to achieve optimal balance between rapid absorption and minimal nasal irritation, while ensuring accurate dosing through controlled release mechanisms

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The nasal spray uses a composite formulation combining benzodiazepine with hydrophilic polymers and other excipients that enhance drug stability, control release rate, and reduce local irritation while maintaining rapid onset of action

Inventive Principle:

Principle #40Composite materials

3Ease of operation

If traditional delivery methods are used, then administration is simple, but dosing accuracy is poor leading to under-dosing

Engineering Contradiction:

Improveadministration simplicityVSAvoiddosing accuracy

Core Design Contradiction:

Ease of operationVSMeasurement precision

Solution Approach 1:

The invention replaces mechanical dosing methods (such as rectal gel application) with a pressurized spray delivery system that provides precise control over the amount of drug delivered, ensuring accurate dosing while maintaining ease of administration through a simple spray actuation

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

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 spray formulation provides rapid onset of action, improved dosing accuracy, and complete drug delivery, enhancing therapeutic efficacy in treating seizures by ensuring higher drug absorption and maintaining effective blood levels despite food intake.

Implementation Method 1

promoting permeation of at least a portion of the diazepam through a mucosal tissue

Methodology Applied

Scientific EffectPermeation: Permeation

Implementation Method 2

ensuring rapid and complete drug absorption through nasal and other mucosal routes

Methodology Applied

Scientific EffectAbsorption: Absorption (physical)

Data Source

PatentUS12465564B2Oral and nasal compositions and methods of treatment

Publication Date: 2025.11.11 AQUESTIVE THERAPEUTICS INC

AI summary

A method of administering diazepam having a food effect is described.