Solid Dispersion Dissolution via Basic Material Neutralization

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Solution Overview

Problem

Existing solid dispersions using acidic polymers often experience delayed dissolution in the upper small intestine, leading to insufficient bioavailability of poorly water-soluble drugs, and may cause decomposition of the acidic polymer.

Innovation Solution

A composition for solid dispersion comprising an acidic polymer, a basic material dispersed in an organic solvent, and a poorly water-soluble drug, which enhances dissolution properties under both soluble pH conditions and relatively low pH conditions in the upper small intestine, while inhibiting decomposition of the acidic polymer.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If acidic polymer is used in solid dispersion to improve solubility of poorly water-soluble drug, then apparent solubility is enhanced, but dissolution is delayed in upper small intestine and bioavailability is insufficient

Engineering Contradiction:

Improveapparent solubilityVSAvoiddissolution property

Core Design Contradiction:

Quantity of substanceVSReliability

Solution Approach 1:

The invention changes the pH parameter by introducing a basic material that neutralizes the acidic polymer in the upper small intestine, transforming the dissolution behavior from delayed to enhanced across a wide pH range (pH 1.2-6.8), thereby resolving the contradiction between apparent solubility and dissolution reliability

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention creates a composite solid dispersion system combining acidic polymer, basic material, and poorly water-soluble drug, where the basic material (e.g., metal hydroxide or carbonate) interacts with the acidic polymer to provide both solubility enhancement and reliable dissolution across different gastrointestinal pH conditions

Inventive Principle:

Principle #40Composite materials

2Reliability

If basic material is added to neutralize acidic polymer for improved dissolution, then dissolution property is enhanced, but acidic polymer decomposes

Engineering Contradiction:

Improvedissolution propertyVSAvoidacidic polymer stability

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The basic material is dispersed in organic solvent before incorporation into the solid dispersion, performing preliminary neutralization action that prevents decomposition of the acidic polymer during storage and administration, while still enabling enhanced dissolution in the gastrointestinal tract

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The organic solvent acts as an intermediary medium that allows the basic material to be dispersed and neutralize the acidic polymer without causing direct decomposition, enabling the basic material to function as a protective agent rather than a decomposing factor

Inventive Principle:

Principle #24Intermediary (Mediator)

3Reliability

If water is added to dissolve basic material for neutralization, then neutralization is achieved, but spray drying becomes impossible due to poor solubility requirements

Engineering Contradiction:

ImproveneutralizationVSAvoidspray drying feasibility

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The organic solvent serves as an intermediary that enables dispersion of the basic material without requiring water, thus maintaining spray drying feasibility while still achieving neutralization of the acidic polymer in the gastrointestinal environment

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the solvent parameter from water-based to organic solvent-based, allowing the basic material to be dispersed and neutralize the acidic polymer without compromising the spray drying process, thereby resolving the contradiction between neutralization and manufacturing ease

Inventive Principle:

Principle #35Parameter changes

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 solid dispersion exhibits excellent dissolution properties across a wide pH range, including the upper small intestine, thereby improving bioavailability and preventing decomposition of the acidic polymer.

Implementation Method 1

a basic material; wherein the basic material is dispersed in the organic solvent

Methodology Applied

Scientific EffectNeutralization: Redox Reactions

Implementation Method 2

the basic material is dispersed in the organic solvent

Methodology Applied

Scientific EffectDispersion: Dispersion (of waves)

Data Source

PatentUS20250025422A1Composition for solid dispersion, solid dispersion, and method of manufacturing the solid dispersion

Publication Date: 2025.01.23 SHIN ETSU CHEMICAL CO LTD

AI summary

Provided is a composition for solid dispersion capable of imparting an excellent dissolution property not only under the pH conditions within the soluble pH range inherent in the acidic polymer but also under relatively low pH conditions in the upper small intestine while inhibiting decomposition of the acidic polymer. The composition for solid dispersion contains an acidic polymer; a basic material; a poorly water-soluble drug; and an organic solvent, wherein the basic material is dispersed in the organic solvent.