Tamper-Resistant Oral Formulation Using Heat-Labile Gel Matrix

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Solution Overview

Problem

Existing pharmaceutical formulations are susceptible to tampering and abuse, particularly for opioid analgesics, which can lead to unintended routes of administration and increased overdose risk.

Innovation Solution

A solid oral dosage form comprising a heat-labile gelling agent, thermal stabilizer, and optionally a pH-modifying agent, which forms a viscous solution upon tampering, inhibiting extraction and absorption through mechanisms like parenteral or nasal routes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If a solid oral dosage form contains a drug susceptible to abuse (e.g., opioid analgesic), then the dosage form provides pain relief, but the dosage form becomes susceptible to tampering and abuse

Engineering Contradiction:
Improveabuse resistanceVSAvoidtampering susceptibility
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The dosage form incorporates a gelling agent that proactively prevents abuse by forming a viscous gel matrix upon contact with liquids, which physically blocks extraction and administration by unintended routes before tampering can occur

Inventive Principle:
Principle #9Preliminary anti-action

Solution Approach 2:

The formulation changes its physical state parameters by incorporating a gelling agent that alters the texture and viscosity of the dosage form when exposed to liquids, transforming it from a crushable solid to a viscous gel that resists extraction

Inventive Principle:
Principle #35Parameter changes

2Speed

If the dosage form is crushed to liberate drug for illicit use, then immediate availability of active agent is achieved, but the formulation's controlled release property is compromised

Engineering Contradiction:
Improvedrug availability speedVSAvoidcontrolled release integrity
Core Design Contradiction:
SpeedVSStability of the object's composition

Solution Approach 1:

The gelling agent forms a protective gel matrix that prevents crushing and disintegration of the dosage form, thereby maintaining controlled release properties while blocking immediate drug availability through unintended routes

Inventive Principle:
Principle #9Preliminary anti-action

3Reliability

If a gelling agent is included to prevent parenteral and nasal administration, then abuse is deterred, but the dosage form's manufacturability and dosing precision become more difficult

Engineering Contradiction:
Improveabuse deterrenceVSAvoidmanufacturability
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The gelling agent is incorporated in controlled amounts during manufacturing to achieve the desired gel formation properties, allowing standard manufacturing processes to be used while still providing abuse deterrence through viscosity changes

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 formulation significantly reduces abuse potential by maintaining high viscosity and preventing drug recovery, thereby deterring illicit use and overdose.

Implementation Method 1

a heat-labile gelling agent; a thermal stabilizer; and a drug susceptible to abuse

Methodology Applied
Scientific EffectGelling: Gel

Implementation Method 2

forms a viscous solution upon tampering, inhibiting extraction and absorption

Methodology Applied
Scientific EffectViscosity increase:

Implementation Method 3

a heat-labile gelling agent; a thermal stabilizer

Methodology Applied
Scientific EffectThermal stabilization:

Implementation Method 4

optionally a pH-modifying agent

Methodology Applied
Scientific EffectpH modification:

Data Source

PatentUS20250367298A1Tamper Resistant Pharmaceutical Formulations
Publication Date: 2025.12.04 PURDUE PHARMA LP

AI summary

Disclosed in certain embodiments is a solid oral dosage form comprising a heat-labile gelling agent; a thermal stabilizer; and a drug susceptible to abuse.