Pirfenidone Sustained-Release Formulation for Stable 24-Hour Blood Levels

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Solution Overview

Problem

Existing pirfenidone products require multiple daily doses, are meal-dependent, cause unstable blood drug concentrations, and result in high peak-to-valley ratios, leading to poor patient compliance and adverse responses.

Innovation Solution

A prolonged-release oral solid formulation of pirfenidone using a sustained-release formulation with specific ratios of swelling, shaping, and adhesive materials, designed to maintain stable blood drug concentrations for 24 hours with a peak-to-valley ratio of 2-10, allowing once-daily administration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If immediate-release formulation is used, then rapid disintegration and absorption occur, but blood drug concentration fluctuates greatly with large peak-to-valley ratio

Engineering Contradiction:

Improvedisintegration and absorption speedVSAvoidblood drug concentration stability

Core Design Contradiction:

SpeedVSStability of the object's composition

Solution Approach 1:

The patent changes the release rate parameter of pirfenidone from rapid (immediate-release) to controlled (prolonged-release), achieving a peak-to-valley ratio between 2-10 and maintaining stable blood drug concentration for 24 hours through optimized formulation with swelling materials, shaping materials, and adhesive materials

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent uses composite materials including swelling materials (sodium carboxymethylcellulose, hydroxypropyl methylcellulose), shaping materials (ethyl cellulose, polyethylene), and adhesive materials (polyoxyethylene, chitosan) to create a prolonged-release formulation that controls drug release kinetics and stabilizes blood concentration

Inventive Principle:

Principle #40Composite materials

2Reliability

If dosing three times a day is required, then adequate blood drug concentration is maintained, but patient compliance deteriorates

Engineering Contradiction:

Improveblood drug concentration maintenanceVSAvoidpatient compliance

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent extends the duration of useful action from 8 hours (three-times-daily dosing) to 24 hours (once-daily dosing) by formulating prolonged-release tablets that continuously release pirfenidone, eliminating the need for multiple daily administrations and improving patient compliance

Inventive Principle:

Principle #20Continuity of useful action

Solution Approach 2:

The patent creates a dynamic release system that adapts to gastrointestinal conditions, where the formulation adjusts its release profile based on pH, moisture, and mechanical stress in the GI tract to maintain stable drug release over 24 hours with once-daily dosing

Inventive Principle:

Principle #15Dynamics

3Speed

If rapid absorption occurs, then quick therapeutic effect is achieved, but adverse responses increase due to high Cmax

Engineering Contradiction:

Improveabsorption speedVSAvoidadverse responses from high Cmax

Core Design Contradiction:

SpeedVSObject-generated harmful factors

Solution Approach 1:

The patent implements periodic drug release instead of rapid single-dose absorption, distributing the drug release over 24 hours to avoid high peak concentrations (Cmax) while maintaining adequate therapeutic levels, thereby reducing adverse responses associated with high Cmax

Inventive Principle:

Principle #19Periodic action

Solution Approach 2:

The patent uses swelling materials and shaping materials that absorb water and expand before drug release, creating a controlled matrix that cushions and modulates the release rate, preventing rapid absorption and high Cmax that cause adverse responses

Inventive Principle:

Principle #11Beforehand cushioning (Prior cushioning)

4Reliability

If meal-dependent administration is required, then absorption is optimized, but flexibility and compliance are reduced

Engineering Contradiction:

Improveabsorption optimizationVSAvoiddosing flexibility

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent creates a universal formulation that functions effectively regardless of meal timing or food intake, allowing administration with or after meals without compromising absorption or efficacy, thereby providing dosing flexibility and improving patient compliance

Inventive Principle:

Principle #6Universality (Multi-functionality)

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 formulation achieves stable blood drug concentrations for 24 hours with a reduced peak-to-valley ratio, improving patient compliance and minimizing adverse responses.

Implementation Method 1

the sustained-release formulation contains a swelling material

Methodology Applied

Scientific EffectSwelling:

Data Source

PatentUS20250312324A1Prolonged-release oral solid formulation of pirfenidone

Publication Date: 2025.10.09 OVERSEAS PHARMACEUTICALS (GUANGZHOU) LTD

AI summary

A prolonged-release oral solid formulation of pirfenidone includes a sustained-release formulation. The sustained-release formulation contains a swelling material, a shaping material and an adhesive material. The weight percentage of the swelling material in the solid formulation is 10%-25%; the weight percentage of the shaping material in the solid formulation is 10%-25%; and the weight percentage of the adhesive material in the solid formulation is 1%-8%. The solid formulation only needs to be taken once a day, regardless of whether it is taken before or after meals. It takes effect quickly after taking it, and can be stably and effectively released for 24 hours, providing a pirfenidone product with significantly improved compliance and stable blood drug concentration.