Cationic Drug Polymer Composition with Long Chain Acid

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Solution Overview

Problem

Existing skin bonding polymer compositions have difficulty absorbing and controlling the release of ionic and water-soluble cationic pharmaceutically active ingredients, such as Imiquimod, due to their highly hydrophobic nature, leading to potential irritation and inefficient delivery.

Innovation Solution

A cationic pharmaceutically active ingredient containing composition is developed, incorporating a hydrophobic polymer/hydrophilic polymer adduct with poly(vinylpyrrolidone-alkylene) polymers and polymers with carboxylic acid or hydroxyl groups, along with a long chain organic acid and high water content, to enhance absorption and controlled release of cationic drugs like Imiquimod.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Strength

If a hydrophobic polymer/hydrophilic polymer adduct is used to provide skin bonding, then skin adhesion is improved, but absorption of ionic and water-soluble cationic active ingredients deteriorates

Engineering Contradiction:

Improveskin adhesionVSAvoidabsorption of cationic active ingredient

Core Design Contradiction:

StrengthVSReliability

Solution Approach 1:

A long chain organic acid is introduced as an intermediary substance between the hydrophobic polymer adduct and the cationic active ingredient. This organic acid acts as a bridge, enabling the hydrophobic polymer matrix to accommodate and release cationic drugs through controlled interactions, thereby resolving the contradiction between skin adhesion and drug absorption

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies the chemical and physical parameters of the polymer adduct by incorporating specific long chain organic acids with particular carbon chain lengths and functional groups. These parameter changes enable the hydrophobic polymer to interact favorably with cationic drugs while maintaining skin bonding properties

Inventive Principle:

Principle #35Parameter changes

2Productivity

If high concentration of cationic active ingredient is used to ensure desired activity, then therapeutic efficacy is improved, but skin irritation increases

Engineering Contradiction:

Improvetherapeutic activityVSAvoidskin irritation

Core Design Contradiction:

ProductivityVSObject-affected harmful factors

Solution Approach 1:

The composition enables continuous and controlled release of the cationic active ingredient over an extended period. This sustained release mechanism allows maintenance of therapeutic efficacy at lower concentrations by providing continuous exposure, thereby reducing peak irritation levels while maintaining overall therapeutic effect

Inventive Principle:

Principle #20Continuity of useful action

Solution Approach 2:

The long chain organic acid pre-establishes controlled release mechanisms within the polymer matrix before application. This preliminary structuring ensures that the cationic active ingredient is released in a controlled manner, preventing sudden high concentrations that would cause irritation while maintaining therapeutic levels over time

Inventive Principle:

Principle #10Preliminary action

3Productivity

If rapid release of cationic active ingredient is achieved to ensure sufficient activity, then therapeutic effect is improved, but side effects increase

Engineering Contradiction:

Improverate of drug releaseVSAvoidside effects

Core Design Contradiction:

ProductivityVSObject-generated harmful factors

Solution Approach 1:

The patent creates a dynamic release system where the rate of cationic active ingredient release can be adjusted based on conditions. The long chain organic acid within the hydrophobic polymer matrix enables modulated release kinetics, allowing the system to adapt release rates to minimize side effects while maintaining therapeutic efficacy

Inventive Principle:

Principle #15Dynamics

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 composition effectively binds and releases cationic active ingredients over a prolonged period, reducing skin irritation and improving the delivery efficacy of drugs like Imiquimod, allowing for a desired level of activity while minimizing side effects.

Implementation Method 1

a long chain organic acid to assist with holding the cationic pharmaceutically active ingredient to the polymer component

Methodology Applied

Scientific EffectElectrostatic attraction: Ion Repulsion/Attraction

Implementation Method 2

allows the active ingredients to be released, over time, to skin tissue

Methodology Applied

Scientific EffectDiffusion: Diffusion

Data Source

PatentUS8735422B2Cationic pharmaceutically active ingredient containing composition, and methods for manufacturing and using

Publication Date: 2014.05.27 SKINVISIBLE PHARMACEUTICALS INC

AI summary

A cationic pharmaceutically active ingredient containing composition is provided. The composition includes a cationic pharmaceutically active ingredient, a hydrophobic polymer/hydrophilic polymer adduct comprising a poly(vinylpyrrolidone/alkylene) polymer and a polymer comprising carboxylic acid groups, hydroxyl groups, or a mixture of carboxylic acid groups and hydroxyl groups, a compatibilizing amount of a long chain organic acid having a carbon chain of at least 8 carbon atoms, and at least about 50 wt. % water.