PARP Inhibitor Solid Dispersion Using PVP for Stable Dissolution

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Solution Overview

Problem

Existing pharmaceutical compositions with PARP inhibitors, such as those using copovidone as a carrier material, suffer from stability issues and poor dissolution characteristics, limiting their effectiveness in cancer treatment.

Innovation Solution

A solid dispersion comprising a PARP inhibitor represented by formula I and polyvinylpyrrolidone as a carrier material, with specific weight ratios and excipients, is developed to enhance stability and dissolution.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If copovidone is used as a carrier material for solid dispersion of PARP inhibitors, then the formulation can be prepared, but the stability deteriorates

Engineering Contradiction:

Improveformulation preparationVSAvoidstability

Core Design Contradiction:

Ease of manufactureVSStability of the object's composition

Solution Approach 1:

The patent changes the carrier material parameter from copovidone to polyvinylpyrrolidone, which fundamentally alters the chemical and physical properties of the solid dispersion system. This parameter change resolves the stability issue while maintaining manufacturability, as PVP provides better chemical stability and compatibility with PARP inhibitors during storage.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite material system consisting of PARP inhibitors dispersed in polyvinylpyrrolidone matrix. This composite approach combines the therapeutic benefits of the inhibitor with the stabilizing properties of PVP, achieving both ease of manufacture and improved stability simultaneously.

Inventive Principle:

Principle #40Composite materials

2Ease of manufacture

If conventional carrier materials are used for solid dispersion, then the formulation can be manufactured, but the dissolution characteristics deteriorate

Engineering Contradiction:

Improveformulation manufacturingVSAvoiddissolution characteristics

Core Design Contradiction:

Ease of manufactureVSProductivity

Solution Approach 1:

The patent changes the carrier material parameter to polyvinylpyrrolidone, which has superior solubility and dissolution properties compared to conventional carriers like copovidone. This parameter change enables faster and more complete dissolution of the PARP inhibitor while maintaining ease of manufacturing through standard solid dispersion techniques.

Inventive Principle:

Principle #35Parameter changes

3Duration of action of stationary object

If the solid dispersion is stored for long term, then the formulation remains available for use, but the stability deteriorates

Engineering Contradiction:

Improvestorage durationVSAvoidstability

Core Design Contradiction:

Duration of action of stationary objectVSStability of the object's composition

Solution Approach 1:

The patent uses polyvinylpyrrolidone as a protective carrier material that preemptively shields the PARP inhibitor from degradation during storage. PVP's molecular structure provides a stable matrix that prevents crystallization, oxidation, and hydrolysis of the inhibitor, thereby maintaining stability throughout the storage period.

Inventive Principle:

Principle #11Beforehand cushioning (Prior cushioning)

Solution Approach 2:

The polyvinylpyrrolidone carrier creates an inert microenvironment around the PARP inhibitor molecules, isolating them from reactive oxygen, moisture, and other degrading agents in the storage environment. This protective effect maintains drug stability over extended storage durations.

Inventive Principle:

Principle #39Inert atmosphere (Inert environment)

Data Source

PatentEP3881846B1Pharmaceutical composition comprising PARP inhibitors

Publication Date: 2026.01.28 JIANGSU HENGRUI MEDICINE CO LTD

Figure 1

AI summary

A solid dispersion for PARP inhibitors, comprising a compound represented by formula I and a carrier material, wherein the carrier material comprises polyvinylpyrrolidone. A pharmaceutical composition, comprising a solid dispersion, a filler, a disintegrating agent and a lubricant. A preparation method for the solid dispersion. Use of the solid dispersion or the pharmaceutical composition in the preparation of drugs for treating cancers.