Alginate Oral Film for Ketamine Delivery

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current ketamine formulations lack a non-invasive, needle-free administration method with consistent bioavailability and low variability in plasma concentrations, making them unsuitable for effective anesthesia, pain management, and treatment of amnesia, depression, and bipolar disorder.

Innovation Solution

Development of an oral cavity film comprising an alginate salt of a monovalent cation and ketamine or its pharmaceutically acceptable salt, which adheres to the mucosa, dissolves slowly, and releases the active ingredient, providing consistent plasma levels with reduced variability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If intravenous injection is used to administer ketamine, then rapid and reliable plasma levels are achieved, but needle-stick injuries and overdose risk increase

Engineering Contradiction:
Improveplasma level consistencyVSAvoidneedle-stick injuries
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent replaces the mechanical intravenous injection system with a dissolvable oral film system. The film is placed in the oral cavity and dissolves automatically, eliminating needles and mechanical injection while achieving reliable plasma levels through controlled dissolution and absorption.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

Solution Approach 2:

The patent introduces an intermediary substance (the dissolvable film matrix containing ketamine) that serves as a carrier between the administration site and the bloodstream. The film acts as a temporary reservoir that releases ketamine gradually, mediating the delivery process without requiring direct needle access.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Ease of operation

If oral formulation is used to administer ketamine, then needle-free administration is achieved, but bioavailability is low (40-45%) due to first pass metabolism

Engineering Contradiction:
Improveneedle-free administrationVSAvoidbioavailability
Core Design Contradiction:
Ease of operationVSQuantity of substance

Solution Approach 1:

The patent changes the physical and chemical parameters of ketamine delivery by formulating it in a dissolvable film with specific excipients and pH conditions. This modifies the absorption kinetics and reduces first-pass metabolism effects, improving bioavailability while maintaining the needle-free advantage.

Inventive Principle:
Principle #35Parameter changes

3Ease of operation

If intranasal spray is used to administer ketamine, then non-invasive delivery is achieved, but dose consistency is poor with bioavailability varying from 8 to 50%

Engineering Contradiction:
Improvenon-invasive deliveryVSAvoiddose consistency
Core Design Contradiction:
Ease of operationVSManufacturing precision

Solution Approach 1:

The patent controls the dissolution rate and release parameters of ketamine from the oral film through careful selection of excipients, film thickness, and pH conditions. This ensures consistent dosing across administrations while maintaining non-invasive delivery, eliminating the variability seen in intranasal sprays.

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 alginate film formulation offers a needle-free, bioadhesive delivery system that ensures consistent and effective ketamine levels in the bloodstream, improving treatment efficacy for anesthesia, pain management, and mental health conditions while avoiding the limitations of existing oral and intranasal formulations.

Implementation Method 1

a film suitable for administration to an oral cavity comprising: (i) an alginate salt of a monovalent cation

Methodology Applied
Scientific EffectAdhesion: Adhesive

Implementation Method 2

dissolves slowly, and releases the active ingredient

Methodology Applied
Scientific EffectDissolution:

Data Source

PatentEP4021405B1Pharmaceutical formulation
Publication Date: 2024.11.06 KLARIA PHARMA HLDG AB
  • EP4021405B1 patent drawingFigure 1
  • EP4021405B1 patent drawingFigure 2
  • EP4021405B1 patent drawingFigure 3

AI summary

The present invention relates to films comprising an alginate salt of a monovalent cation or a mixture of alginate salts containing at least one alginate salt of a monovalent cation, and a compound of Formula (I), such as ketamine, or a pharmaceutically acceptable salt thereof. The present invention further relates to methods for manufacturing such films, and the use of such films in anesthesia, pain management, and the treatment of disease, in particular amnesia, depression and bipolar disorder.