Silicone Elastomer API Recovery via Silane Crosslinking

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Solution Overview

Problem

Current curable liquid silicone rubber compositions face challenges in releasing active pharmaceutical ingredients, such as levonorgestrel, due to irreversible drug binding within the matrix, which limits the effectiveness of drug delivery devices.

Innovation Solution

A curable liquid silicone rubber composition incorporating an organopolysiloxane with silicon-bonded alkenyl groups, a hydrosilylation catalyst, surface-treated silica filler, a fatty acid ester, and a triazole compound, which allows for increased recovery of active pharmaceutical ingredients with terminal alkene, alkyne, or carbonyl functionalities, preventing complexing and binding into the elastomeric network.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If curable liquid silicone rubber composition is used for drug delivery, then the material provides good physiological inertness and biocompatibility, but the active pharmaceutical ingredient binds irreversibly into the elastomeric network reducing drug recovery

Engineering Contradiction:
Improvephysiological inertnessVSAvoidactive pharmaceutical ingredient recovery
Core Design Contradiction:
ReliabilityVSLoss of substance

Solution Approach 1:

The patent introduces a silane crosslinking agent as an intermediary substance that mediates between the silicone rubber matrix and the active pharmaceutical ingredient. This crosslinking agent forms a separate crosslinked network that prevents direct binding between the API and the silicone elastomer, thereby maintaining drug recovery while preserving the biocompatibility of the silicone material.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite material system consisting of silicone rubber, silane crosslinking agent, and active pharmaceutical ingredient. This composite structure allows the silicone rubber to provide physiological inertness while the silane crosslinking network prevents irreversible API binding, thus resolving the contradiction between reliability and substance loss.

Inventive Principle:
Principle #40Composite materials

2Strength

If silica and resin are added to strengthen silicone elastomer, then the mechanical strength increases, but the hydrophobic nature of the material enhances which limits drug release efficiency

Engineering Contradiction:
Improvemechanical strengthVSAvoiddrug release efficiency
Core Design Contradiction:
StrengthVSProductivity

Solution Approach 1:

The patent modifies the chemical parameters of the silicone elastomer by incorporating silane crosslinking agents that alter the network structure. This changes the interaction between the material and pharmaceutical agents, improving drug release efficiency while maintaining the mechanical strength provided by silica and resin reinforcement.

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 effectively enhances the release of active pharmaceutical ingredients by limiting their complexing and binding, resulting in a silicone elastomer with improved drug delivery properties.

Implementation Method 1

hydrosilylation curable silicone compositions that can be used for the release of active substances

Methodology Applied
Scientific EffectHydrosilylation: Chemical Bonding

Implementation Method 2

Drug release occurs by diffusion through the polymer matrix

Methodology Applied
Scientific EffectDiffusion: Diffusion

Implementation Method 3

incorporating a silane crosslinking agent in a curable liquid silicone rubber composition prevents complexing and binding into the elastomeric network

Methodology Applied
Scientific EffectCrosslinking: Chemical Bonding

Data Source

PatentEP3962489B1Drug delivery silicone compositon to improve active ingredient elution
Publication Date: 2023.03.22 ELKEM SILICONES USA CORP
  • EP3962489B1 patent drawing

AI summary

The invention relates to a new curable liquid silicone rubber composition which after curing provides a silicone elastomer useful as a drug delivery device comprising an active pharmaceutical ingredient (API) having terminal alkene, alkyne or carbonyl functionalities exhibiting an increased recovery of the active pharmaceutical ingredient.