Controlled Release Composition Using Matrix and Microparticles

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Microparticle-based controlled release compositions face issues such as aggregation, high solvent requirements, and difficulty in measuring drug release rates within tissues, making them impractical for sustained medication delivery, especially in solid tumors.

Innovation Solution

A controlled release composition comprising a matrix linked with microparticles, where the microparticles have a higher initial melting temperature than the matrix, allowing for controlled drug release and reducing solvent usage, with the microparticles being uniformly or randomly distributed within the matrix to enhance stability and release profile.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of stationary object

If microparticle-based controlled release composition is used, then sustained release of medicament is achieved, but microparticles form aggregates affecting composition properties

Engineering Contradiction:
Improvesustained release durationVSAvoidmicroparticle aggregation
Core Design Contradiction:
Duration of action of stationary objectVSStability of the object's composition

Solution Approach 1:

The patent introduces a matrix material as an intermediary substance that embeds and stabilizes microparticles, preventing their aggregation. The matrix acts as a spacer and protective medium, maintaining uniform distribution of microparticles while enabling sustained drug release over time.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Duration of action of stationary object

If microparticle-based controlled release composition is used, then sustained release of medicament is achieved, but large amount of solvent is required (80-90% solvent ratio)

Engineering Contradiction:
Improvesustained release durationVSAvoidsolvent volume
Core Design Contradiction:
Duration of action of stationary objectVSQuantity of substance

Solution Approach 1:

The patent changes the physical state and composition parameters by using a matrix material with specific melting temperature characteristics. The matrix material is selected to have a melting temperature higher than the microparticle material, allowing the system to be processed in a molten state and then solidified, thereby eliminating the need for large amounts of solvent while maintaining sustained release properties.

Inventive Principle:
Principle #35Parameter changes

3Duration of action of stationary object

If microparticle-based controlled release composition is implanted, then sustained release of medicament is achieved, but microparticles move easily within tissue making drug release rate measurement impractical

Engineering Contradiction:
Improvesustained release durationVSAvoiddrug release rate measurement
Core Design Contradiction:
Duration of action of stationary objectVSMeasurement precision

Solution Approach 1:

The patent uses the matrix material as a counterbalancing structure that anchors and immobilizes the microparticles within the tissue implantation site. The matrix provides mechanical stability and prevents microparticle migration, creating a stable environment where drug release rate can be accurately measured and controlled.

Inventive Principle:
Principle #8Anti-weight (Counterweight)

4Duration of action of stationary object

If microparticle-based controlled release composition is used, then sustained release of medicament is achieved, but it is impractical for injection into solid tumors

Engineering Contradiction:
Improvesustained release durationVSAvoidinjection feasibility
Core Design Contradiction:
Duration of action of stationary objectVSEase of operation

Solution Approach 1:

The patent transforms the physical state of the composition by utilizing a matrix material that can be melted above its melting temperature. This allows the composition to be injected in a molten, fluid state into solid tumors, and then solidifies in situ to provide sustained release, thereby combining the ease of injection with the benefit of sustained release without requiring large amounts of solvent.

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 composition provides a stable and controlled release of active agents, reducing the frequency of dosing and improving patient compliance, while minimizing solvent use and facilitating precise drug delivery within tissues.

Implementation Method 1

the first material comprises an initial melting temperature TH; the second material comprises a complete melting temperature TL; ΔT=TH−TL; and ΔT>0

Methodology Applied
Scientific EffectMelting: Melting

Data Source

PatentUS10335370B2Controlled release composition
Publication Date: 2019.07.02 XU JIANJIAN
  • US10335370B2 patent drawing
  • US10335370B2 patent drawing
  • US10335370B2 patent drawing

AI summary

The present disclosure provides a controlled release composition comprising a plurality of microparticles and a matrix, wherein: the plurality of microparticles comprises a first material; the matrix comprises a second material; and the melting temperature of the first material is higher than the melting temperature of the second material. Also provided are methods of making and using the same.