IPF Inhalation Formulation for Higher Lung Bioavailability

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Solution Overview

Problem

Current treatments for idiopathic pulmonary fibrosis (IPF) are limited in efficacy and associated with tolerability issues, and there are no inhalation formulations specifically designed for clinical use.

Innovation Solution

Development of inhalation formulations, including aerosol inhalation liquid, dry powder inhaler, and soft mist inhaler, containing active drugs like apremilast, ibudilast, and crisaborole, with specific pharmaceutical excipients and preparation methods to enhance bioavailability and reduce respiratory irritation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If oral administration is used for IPF treatment, then the treatment can be administered conveniently, but the bioavailability is limited and tolerability issues arise

Engineering Contradiction:

Improveconvenience of administrationVSAvoidbioavailability and tolerability

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent introduces inhalation as an intermediary administration route between oral and parenteral methods. The inhalation formulation serves as a mediator that delivers the active drug directly to the lungs, bypassing the first-pass metabolism issue of oral administration while avoiding the invasiveness of parenteral methods. This intermediary approach resolves the contradiction by providing both convenience and improved bioavailability/tolerability.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent utilizes pneumatic principles through aerosol generation and inhalation delivery. The formulation is delivered via aerosolized particles that are inhaled through the respiratory system, leveraging the natural pneumatic mechanism of breathing to transport the drug to the target tissue. This pneumatic delivery method achieves improved bioavailability while maintaining ease of operation.

Inventive Principle:

Principle #29Pneumatics and hydraulics

2Ease of manufacture

If no inhalation formulation is used, then the production process remains simple, but the clinical effectiveness and bioavailability are limited

Engineering Contradiction:

Improvesimplicity of production processVSAvoidclinical effectiveness and bioavailability

Core Design Contradiction:

Ease of manufactureVSReliability

Solution Approach 1:

The patent applies parameter changes by transforming the physical state of the drug from solid/oral to aerosolized particulate form. The formulation parameters (particle size, aerosol generation method, excipient composition) are optimized to achieve both improved clinical effectiveness and manageable production complexity. The parameter change enables inhalation delivery while maintaining manufacturing feasibility.

Inventive Principle:

Principle #35Parameter changes

3Reliability

If conventional oral drugs are used, then the treatment approach is established, but the efficacy in preventing disease progression is limited

Engineering Contradiction:

Improveestablished treatment approachVSAvoidefficacy in preventing disease progression

Core Design Contradiction:

ReliabilityVSProductivity

Solution Approach 1:

The patent transitions from one-dimensional oral administration to multi-dimensional inhalation delivery. By changing the administration dimension from gastrointestinal tract to respiratory system, the drug reaches the target tissue more directly and effectively. This dimensional change in delivery route enables improved efficacy in preventing disease progression while maintaining an established treatment framework.

Inventive Principle:

Principle #17Another dimension (Dimensionality change)

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 inhalation formulations demonstrate improved bioavailability and clinical effectiveness in treating IPF, reducing pulmonary fibrosis and oxidative stress, with inhalation methods showing superior results compared to oral administration.

Implementation Method 1

the aerosol inhalation liquid formulation consists of an active drug and a pharmaceutical excipient A

Methodology Applied

Scientific EffectNebulization:

Implementation Method 2

the nonionic surfactant includes, but is not limited to, Tween, Span, polyol, and poloxamer

Methodology Applied

Scientific EffectSurfactant action: Surfactant

Implementation Method 3

the complexing agent is EDTA or a salt thereof

Methodology Applied

Scientific EffectComplexation:

Data Source

PatentUS20260083702A1Inhalation formulation for treating IPF disease and preparation method therefor

Publication Date: 2026.03.26 SUZHOU INHAL PHARMA CO LTD

AI summary

An inhalation formulation for treating an IPF disease. The inhalation formulation is an aerosol inhalation liquid formulation, an inhalation aerosol, a dry powder inhaler or a soft mist inhaler. The inhalation formulation contains an active drug, and the active drug is any one of apremilast, ibudilast, roflumilast, crisaborole, and difamilast. A preparation process for the inhalation formulation is introduced into a conventional formulation. An active component in a conventional oral formulation is prone to being destroyed in the digestive tract, and has low bioavailability, a liver first pass effect, and a slow onset of action. An inhalation formulation capable of significantly alleviating IPF is prepared. Tests prove that the prepared inhalation formulation can effectively increase the bioavailability, and improve the clinical use effect.