Pharmaceutical Granules with Insoluble Cores for Abuse Deterrence

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Solution Overview

Problem

Current pharmaceutical formulations fail to prevent the misuse of medicinal drugs, particularly through extraction of active ingredients using solvents or crushing, as they do not provide adequate security against inappropriate use.

Innovation Solution

Development of granules with a solid core and multiple layers, including insoluble supports, colorants, metallic pigments, gas-releasing compounds, and embittering agents, which make it difficult to extract the active ingredient by solvent or crushing, and are designed to be easily identifiable upon ingestion or solubilization.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional pharmaceutical formulations are used, then the therapeutic effect is provided, but the formulations can be easily crushed or extracted using solvents for misuse

Engineering Contradiction:
Improveprevention of misuseVSAvoidformulation structure
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The formulation is divided into multiple separate granules, each containing a different active ingredient. This segmentation prevents users from easily extracting and combining ingredients for misuse, as each granule must be consumed separately and completely to achieve the intended therapeutic effect.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

One granule is placed inside another granule, creating a nested structure where the inner granule contains one active ingredient and the outer granule contains another. This nested design ensures that both ingredients are released only when the outer granule dissolves, preventing premature extraction or selective consumption.

Inventive Principle:
Principle #7Nested doll (Nesting)

2Reliability

If the formulation is made more secure against extraction and crushing, then misuse prevention is improved, but the ease of administration and patient acceptance may deteriorate

Engineering Contradiction:
Improvesecurity against inappropriate useVSAvoidease of administration
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

Different granules are coated with distinct colored layers corresponding to different active ingredients. This color-coding system helps patients identify and consume the correct granules while maintaining security, as the colors provide visual confirmation that the granules are being taken as prescribed without compromising the anti-misuse properties.

Inventive Principle:
Principle #32Color changes

Data Source

PatentUS8999392B2Pharmaceutical formulations to prevent the misuse of medicinal drugs
Publication Date: 2015.04.07 DEBREGEAS & ASSOCIES PHARMA

AI summary

Granules having a solid core on which an active ingredient is supported, the core being chosen preferably from among insoluble supports, the granules also having, supported on said the core, the following compounds: one or more coloring agents, one or more metallic pigments, one or more gas-releasing compounds, and optionally one or more embittering agents.