Amorphous Ivacaftor Solid Composition Without pH-Dependent Polymers

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Solution Overview

Problem

Existing formulations of amorphous ivacaftor often require pH-dependent polymers and complex processes like solid dispersions or slugging, which can lead to stability issues, high costs, and poor flow properties.

Innovation Solution

A solid composition of amorphous ivacaftor is developed without pH-dependent polymers, using roller compaction as a preparation method, which simplifies the process and enhances stability and dissolution profiles.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If amorphous ivacaftor is formulated as a solid dispersion within a polymer matrix to improve stability, then stability is improved, but device complexity and manufacturing cost increase

Engineering Contradiction:

ImprovestabilityVSAvoidcomplexity

Core Design Contradiction:

Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent removes pH-dependent polymers from the formulation, extracting the problematic component that caused stability issues while simplifying the overall composition to just amorphous ivacaftor with conventional excipients

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The patent changes the formulation parameters by eliminating the need for pH-dependent polymers and using conventional excipients instead, thereby simplifying the composition while maintaining stability

Inventive Principle:

Principle #35Parameter changes

2Stability of the object's composition

If solid dispersion techniques are used to improve stability, then stability is improved, but manufacturing cost and time increase

Engineering Contradiction:

ImprovestabilityVSAvoidmanufacturing time

Core Design Contradiction:

Stability of the object's compositionVSLoss of time

Solution Approach 1:

The patent eliminates complex solid dispersion techniques and pH-dependent polymers, extracting the unnecessary complexity while retaining the essential stabilizing function through conventional excipients

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The patent uses conventional, inexpensive excipients instead of expensive pH-dependent polymers, reducing manufacturing cost while achieving the desired stability through simpler, more economical materials

Inventive Principle:

Principle #27Cheap short-living objects (Disposable)

3Stability of the object's composition

If pH-dependent polymers are used to maintain amorphous form stability, then stability is improved, but dissolution performance deteriorates

Engineering Contradiction:

ImprovestabilityVSAvoiddissolution performance

Core Design Contradiction:

Stability of the object's compositionVSReliability

Solution Approach 1:

The patent removes pH-dependent polymers from the formulation, eliminating their negative impact on dissolution performance while maintaining stability through conventional excipients that do not interfere with drug release

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The patent changes the formulation composition by replacing pH-dependent polymers with conventional excipients, thereby improving dissolution performance while maintaining the amorphous form stability through alternative mechanisms

Inventive Principle:

Principle #35Parameter changes

4Quantity of substance

If amorphous ivacaftor is used to improve solubility, then solubility is improved, but stability deteriorates due to conversion to crystalline form

Engineering Contradiction:

ImprovesolubilityVSAvoidstability

Core Design Contradiction:

Quantity of substanceVSStability of the object's composition

Solution Approach 1:

The patent uses conventional excipients as intermediaries to stabilize the amorphous form of ivacaftor, preventing conversion to crystalline form while maintaining the solubility advantages of the amorphous state

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite formulation where amorphous ivacaftor is combined with conventional excipients in a simplified matrix, achieving both the solubility benefits of the amorphous form and the stability needed to prevent crystallization

Inventive Principle:

Principle #40Composite materials

Data Source

PatentEP4570241A1Compositions of ivacaftor

Publication Date: 2025.06.18 GENEPHARM A E

Figure 1

AI summary

The present invention relates to a solid composition of amorphous ivacaftor wherein the composition is free from pH dependent polymers and a process for the preparation of such solid compositions.