Imidazolinone Drug Formulation with Cyclodextrin for Stable Dissolution

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Solution Overview

Problem

Existing DNA-PK inhibitors face challenges in achieving stable drug dissolution rates and stability, which affects their efficacy in anti-tumor therapies.

Innovation Solution

A pharmaceutical preparation of an imidazolinone compound, formulated into various dosage forms, including granules, tablets, and capsules, with specific compositions to enhance stability and dissolution, utilizing diluents, disintegrants, and glidants to ensure uniform distribution and rapid drug release.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If DNA-PK inhibitors are formulated for anti-tumor therapy, then therapeutic efficacy is improved, but drug dissolution rate and stability deteriorate

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoiddrug dissolution rate and stability

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent uses cyclodextrin as an intermediary substance to form inclusion complexes with the imidazolinone compound. The cyclodextrin cavity accommodates the drug molecule, improving its dissolution rate and stability without affecting its DNA-PK inhibitory activity. This mediator approach resolves the contradiction between maintaining therapeutic efficacy and improving formulation stability.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention creates a composite pharmaceutical preparation consisting of the imidazolinone compound combined with cyclodextrin in specific ratios (1:3 to 1:10 w/w). This composite material exhibits both the therapeutic properties of the original compound and the enhanced dissolution characteristics provided by the cyclodextrin host structure.

Inventive Principle:

Principle #40Composite materials

2Reliability

If pure imidazolinone compound is used, then DNA-PK inhibitory activity is maintained, but dissolution rate is insufficient

Engineering Contradiction:

ImproveDNA-PK inhibitory activityVSAvoiddissolution rate

Core Design Contradiction:

ReliabilityVSSpeed

Solution Approach 1:

The patent changes the physical and chemical parameters of the drug delivery system by forming inclusion complexes. The cyclodextrin modification alters the solubility parameters and dissolution kinetics of the imidazolinone compound while preserving its molecular structure and biological activity against DNA-PK.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The cyclodextrin molecule provides a porous cavity structure that can accommodate the imidazolinone compound. This porous host-guest complexation enhances the dissolution rate by providing a pre-formed solubilizing environment for the drug molecule.

Inventive Principle:

Principle #31Porous materials

Data Source

PatentEP4635498A1Pharmaceutical preparation of imidazolinone compound, preparation method therefor, and use thereof

Publication Date: 2025.10.22 KANGBAIDA (SICHUAN) BIOTECHNOLOGY CO LTD

AI summary

The present invention relates to a pharmaceutical preparation of an imidazolinone compound and a preparation method therefor. In particular, the present invention relates to a pharmaceutical preparation of a compound represented by formula I