Abuse-Proof Solid Pharmaceutical Composition via Viscosity Control

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Solution Overview

Problem

Existing abuse-proof pharmaceutical compositions fail to prevent parenteral administration of active ingredients with potential for abuse, as they either form injectable solutions or agglomerates when dissolved in water, posing challenges for individuals with swallowing difficulties and not effectively deterring misuse.

Innovation Solution

A solid pharmaceutical composition combining silica and guar flour, with an active ingredient and a water-soluble diluent, that dissolves in a glass of water but forms a non-injectable gel or viscous solution when added to a hypodermic syringe, preventing parenteral administration and misuse.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If gelling or thickening agents are added to the pharmaceutical composition, then parenteral administration is prevented, but the composition becomes impossible to administer orally to individuals with swallowing difficulties

Engineering Contradiction:
Improveabuse preventionVSAvoidoral administration accessibility
Core Design Contradiction:
Object-affected harmful factorsVSEase of operation

Solution Approach 1:

The invention changes the concentration parameter of the gelling agent based on the volume of water used. When dissolved in a glass of water (large volume), the gelling agent concentration is low enough to allow easy dissolution and oral administration. When dissolved in a syringe volume (small volume), the concentration becomes high enough to form a non-injectable gel, thus preventing abuse while maintaining accessibility for legitimate use.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates a dynamic system where the physical state of the composition (soluble vs. gel-forming) changes based on the volume of water added. This dynamic behavior allows the same composition to be easily administered orally when prepared correctly, while automatically becoming non-injectable when attempt is made to prepare it for parenteral administration.

Inventive Principle:
Principle #15Dynamics

2Ease of operation

If the composition is made soluble in water for oral administration, then it can be easily taken orally, but it can also be easily extracted and administered parenterally for abuse

Engineering Contradiction:
Improveoral solubilityVSAvoidparenteral administration risk
Core Design Contradiction:
Ease of operationVSObject-affected harmful factors

Solution Approach 1:

The invention applies preliminary anti-action by incorporating a gelling agent that preemptively prevents parenteral administration. The gelling agent is present in the composition before use, and when the composition is dissolved in a small volume of water (syringe volume), the gelling agent activates to form a gel structure that physically blocks parenteral injection, thus counteracting the abuse risk before it can occur.

Inventive Principle:
Principle #9Preliminary anti-action

Solution Approach 2:

The invention utilizes parameter changes where the same soluble composition exhibits different physical properties based on the water volume parameter. In large volumes (oral administration), the composition remains soluble and easily administrable. In small volumes (parenteral preparation), the composition forms a gel with high viscosity, making injection impossible. This parameter-dependent behavior simultaneously achieves oral solubility and parenteral prevention.

Inventive Principle:
Principle #35Parameter changes

3Object-affected harmful factors

If a gelling agent is used to prevent abuse by injection, then parenteral administration is deterred, but the composition may form agglomerates when dissolved in water

Engineering Contradiction:
Improveinjection preventionVSAvoidsolution homogeneity
Core Design Contradiction:
Object-affected harmful factorsVSStability of the object's composition

Solution Approach 1:

The invention carefully selects and adjusts the concentration parameter of the gelling agent to achieve optimal performance. The gelling agent is present at a concentration that is sufficient to form a non-injectable gel when dissolved in small volumes, but low enough to prevent agglomerate formation when dissolved in larger volumes of water for oral administration. This precise parameter control resolves the contradiction between abuse prevention and solution stability.

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 prevents parenteral administration by forming a high osmolarity viscous solution when dissolved in a small volume of water, thereby deterring abuse while allowing oral administration in a larger volume, and maintaining aesthetic acceptability.

Implementation Method 1

guar flour in an amount of from 100 mg to 300 mg

Methodology Applied
Scientific EffectGel formation: Gel

Implementation Method 2

forming a not injectable gel and/or viscous solution

Methodology Applied
Scientific EffectThickening: Non-Newtonian Fluids

Implementation Method 3

silica in an amount of from 10 mg to 1000 mg

Methodology Applied
Scientific EffectDispersion: Dispersion (of waves)

Implementation Method 4

forming a high osmolarity viscous solution

Methodology Applied
Scientific EffectOsmolarity: Osmotic Pressure

Data Source

PatentUS11338039B2Abuse-proof solid pharmaceutical composition
Publication Date: 2022.05.24 E PHARM TRENTO SPA

AI summary

The present invention relates to an abuse-proof solid pharmaceutical composition comprising an active ingredient with potential for abuse, silica in an amount of from 10 mg to 1000 mg, guar flour in an amount of from 100 mg to 300 mg, and a water soluble diluent in an amount of from 500 mg to 5000 mg.