Active-Free Granule Matrix for Prolonged Release Tablets

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

The manufacturing of prolonged release pharmaceutical dosage forms is complex due to the need to consider the physico-chemical and physiological properties of active agents, making existing methods cumbersome and in need of simplification.

Innovation Solution

Producing granules with prolonged release materials without active agents, then blending and compressing them with active agents to form tablets, which facilitates the creation of prolonged release matrix systems, allowing for uniform size selection and optional milling and curing to enhance properties.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional prolonged release formulation methods are used, then prolonged release properties are achieved, but the manufacturing process becomes complex and cumbersome

Engineering Contradiction:

Improveprolonged release propertiesVSAvoidmanufacturing process complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The formulation is divided into two separate components: active-free granules containing prolonged release materials and pure pharmaceutically active agents. These components are manufactured independently and then combined in a simple blending and compression process, eliminating the need for complex formulation development while maintaining prolonged release properties.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The active-free granules are prepared in advance containing the prolonged release materials, so that when the active agents are added and compressed, the prolonged release matrix is already formed. This preliminary preparation simplifies the overall manufacturing process by separating the matrix formation step from the active ingredient incorporation.

Inventive Principle:

Principle #10Preliminary action

2Ease of manufacture

If pre-manufactured active-free granules are used, then manufacturing is facilitated and simplified, but additional steps like screening and uniformity selection are required

Engineering Contradiction:

Improvemanufacturing facilitationVSAvoidadditional processing steps

Core Design Contradiction:

Ease of manufactureVSProductivity

Solution Approach 1:

The granules are pre-manufactured with controlled size and uniformity, so that when they are blended with active agents and compressed, the prolonged release matrix is already optimally formed. This preliminary preparation, while requiring additional steps, actually simplifies the overall process by separating matrix formation from active ingredient incorporation.

Inventive Principle:

Principle #10Preliminary action

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

This method simplifies the production of prolonged release dosage forms, ensuring consistent and prolonged release profiles, including alcohol resistance and mechanical tamper resistance, while maintaining stability and efficacy over time.

Implementation Method 1

a prolonged release matrix is obtained at least upon compression, which conveys prolonged release properties on the prolonged release pharmaceutical composition

Methodology Applied

Scientific EffectMatrix system:

Implementation Method 2

compressing said granules of step c) to obtain an oral prolonged release pharmaceutical composition in the form of a tablet

Methodology Applied

Scientific EffectCompression: Compression

Data Source

PatentUS9993433B2Manufacturing of active-free granules and tablets comprising the same

Publication Date: 2018.06.12 EURO CELTIQUE SA

AI summary

The present invention relates to prolonged release pharmaceutical dosage forms, the manufacture thereof as well as their use for administration to human beings.