DPP1 Inhibitor Tablet Composition for Rapid Dissolution and Bioavailability

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Solution Overview

Problem

Existing treatments for fibrotic bronchiectasis and acute lung injury/acute respiratory distress syndrome lack consistent quality, stability, and bioavailability, and there is a need for a rapid-release pharmaceutical formulation that addresses these issues.

Innovation Solution

A pharmaceutical composition comprising Compound A, a dipeptidyl peptidase small molecule inhibitor, formulated with pharmaceutically acceptable excipients such as fillers, disintegrants, lubricants, and coating materials, ensuring consistent quality, rapid dissolution, and high bioavailability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing treatments are used for fibrotic bronchiectasis and acute lung injury, then treatment is provided, but the quality consistency, stability, and bioavailability are insufficient

Engineering Contradiction:

Improvequality consistency and stabilityVSAvoiddosage precision

Core Design Contradiction:

ReliabilityVSManufacturing precision

Solution Approach 1:

The patent applies parameter changes by optimizing the particle size of Compound A (controlling d(0.9) ≤ 150 μm) and adjusting the formulation composition ratios to achieve rapid dissolution and consistent bioavailability. This resolves the contradiction by modifying physical parameters to improve both reliability and manufacturing precision simultaneously.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent uses composite materials by formulating Compound A with specific excipients including fillers (lactose, microcrystalline cellulose), disintegrants (cross-linked povidone, croscarmellose sodium), and lubricants (magnesium stearate) in optimized ratios. This composite formulation ensures consistent quality, stability, and precise dosage, resolving the technical contradiction between reliability and manufacturing precision.

Inventive Principle:

Principle #40Composite materials

2Speed

If a rapid-release formulation is developed, then absorption speed is improved, but formulation complexity increases

Engineering Contradiction:

Improvedissolution and absorption speedVSAvoidformulation complexity

Core Design Contradiction:

SpeedVSDevice complexity

Solution Approach 1:

The patent employs porous materials by using disintegrants (cross-linked povidone, croscarmellose sodium) that create porous structures in the tablet formulation. These porous structures facilitate rapid water penetration and drug dissolution, achieving fast absorption without requiring complex controlled-release mechanisms, thus resolving the contradiction between speed and complexity.

Inventive Principle:

Principle #31Porous materials

Solution Approach 2:

The patent applies segmentation by controlling the particle size distribution of Compound A (d(0.9) ≤ 150 μm) to ensure rapid dissolution. The fine particle segmentation increases surface area for faster absorption while maintaining a simple formulation structure, resolving the technical contradiction between dissolution speed and formulation complexity.

Inventive Principle:

Principle #1Segmentation

Data Source

PatentEP4684787A1Pharmaceutical composition containing dipeptidyl peptidase small molecule inhibitor

Publication Date: 2026.01.28 HAISCO PHARM PTE LTD

AI summary

A pharmaceutical composition comprising a Dipeptidyl Peptidase 1 (DPP1) small molecule inhibitor, Compound A, and a preparation method thereof, and a use of the pharmaceutical composition in the treatment of diseases or conditions associated with fibrotic bronchiectasis.