Abuse Deterrent Dosage Form with Functional Score and Effervescent System

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Solution Overview

Problem

Current abuse deterrent solid dosage forms that incorporate high molecular weight polymers for immediate release formulations are unsuitable due to their difficulty in being crushed or split, compromising the functionality of scores intended for dosing regimen evaluation.

Innovation Solution

A pharmaceutical solid dosage form comprising at least one active pharmaceutical ingredient, a low molecular weight hydrophilic polymer, a high molecular weight hydrophilic polymer, and an effervescent system, designed to maintain immediate release and abuse deterrent properties while allowing functional scoring for splitting into equal portions with minimal mass loss.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If high molecular weight hydrophilic polymers are included in the dosage form to provide abuse deterrent properties, then the dosage form becomes difficult to crush and pulverize, but the release of the active ingredient is retarded, making it unsuitable for immediate release formulations

Engineering Contradiction:
Improveabuse deterrent propertiesVSAvoidrelease speed of active ingredient
Core Design Contradiction:
Object-affected harmful factorsVSSpeed

Solution Approach 1:

The patent segments the polymer system into two distinct components: low molecular weight hydrophilic polymer (e.g., Povidone K30) and high molecular weight hydrophilic polymer (e.g., Macrogol). The low molecular weight polymer ensures rapid drug release by forming a porous structure, while the high molecular weight polymer provides abuse deterrent properties through gel formation. This segmentation allows both contradictory requirements to be satisfied simultaneously.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent creates a composite material system combining two polymers with different molecular weights and functions. The low molecular weight polymer (Povidone K30, Mw=40,000 g/mol) provides immediate release characteristics, while the high molecular weight polymer (Macrogol, Mw=6,000 g/mol) provides abuse deterrent properties. The synergistic interaction between these two polymers resolves the contradiction between rapid release and abuse deterrence.

Inventive Principle:
Principle #40Composite materials

2Object-affected harmful factors

If abuse deterrent features are incorporated into solid dosage forms by increasing crushing strength, then the dosage form becomes difficult to crush, but the score functionality is compromised, making it difficult to break into smaller portions

Engineering Contradiction:
Improveabuse deterrent propertiesVSAvoidease of breaking at score
Core Design Contradiction:
Object-affected harmful factorsVSEase of operation

Solution Approach 1:

The patent applies local quality by creating different mechanical properties in different regions of the dosage form. The bulk of the tablet has high crushing strength due to the high molecular weight polymer providing gel formation and structural integrity, making it resistant to crushing and pulverization. However, at the score line, the tablet is designed to have reduced strength to facilitate clean breaking. This local differentiation allows the tablet to be both abuse-deterrent and easily splittable at the score.

Inventive Principle:
Principle #3Local quality

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 dosage form achieves rapid API release and resistance to crushing or pulverization, maintaining abuse deterrent features and allowing precise dosing without forming fine powders, thus preventing inhalation or injection abuse.

Implementation Method 1

an effervescent system

Methodology Applied
Scientific EffectEffervescence:

Implementation Method 2

at least one low molecular weight hydrophilic polymer, at least one high molecular weight hydrophilic polymer

Methodology Applied
Scientific EffectGel formation: Gel

Data Source

PatentEP2968182B8Abuse deterrent solid dosage form for immediate release with functional score
Publication Date: 2018.07.25 SPECGX LLC

AI summary

The present disclosure provides an immediate release, abuse deterrent pharmaceutical solid dosage form comprising at least one functional score. In particular, the immediate release, abuse deterrent solid dosage form comprises at least one low molecular weight hydrophilic polymer, at least one high molecular weight hydrophilic polymer, and an effervescent system.