Polymeric Matrix for Modified Release Without Inert Cores

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Solution Overview

Problem

Traditional oral administration forms of medicaments and food supplements with modified release, such as tablets and pellets, require inert support cores, leading to increased volume and swallowing difficulties, especially for high dosages, and often necessitate dividing the dosage into multiple units.

Innovation Solution

A polyvalent matrix comprising particles of active substances directly coated with polymeric membranes, eliminating the need for inert support cores, allowing for higher dosages and flexible administration forms without altering modified release characteristics, and enabling easy disintegration and taste masking.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Strength

If inert support cores are used to carry active substance, then the structural integrity and handling of dosage forms is improved, but the volume of the final administration form increases leading to swallowing difficulties

Engineering Contradiction:
Improvestructural integrityVSAvoidvolume of dosage form
Core Design Contradiction:
StrengthVSVolume of moving object

Solution Approach 1:

The patent removes the inert support core from the traditional pellet structure, retaining only the active substance particles which are directly coated with polymeric membranes. This extraction of the unnecessary inert component reduces the overall volume and weight of the dosage form while maintaining the essential function of controlled release.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent merges the functions of the inert core and active substance into a single integrated structure where active substance particles themselves serve as the core. The polymeric membrane coating directly encapsulates the active substance, eliminating the need for a separate inert support layer.

Inventive Principle:
Principle #5Merging (Combining)

2Quantity of substance

If inert support cores are used, then the active substance can be delivered, but the total dosage must be divided into several unitary doses

Engineering Contradiction:
Improveactive substance deliveryVSAvoiddosage form complexity
Core Design Contradiction:
Quantity of substanceVSDevice complexity

Solution Approach 1:

The patent creates a universal matrix system based on agglomerates of active substance particles coated with polymeric membranes that can accommodate various dosages and active substances. This multi-functional system eliminates the need for multiple different inert core types and simplifies the dosage form design while maintaining controlled release capabilities.

Inventive Principle:
Principle #6Universality (Multi-functionality)

3Duration of action of moving object

If traditional tablets with inert components are used, then the modified release can be achieved, but the active substance titer is limited

Engineering Contradiction:
Improvemodified releaseVSAvoidactive substance titer
Core Design Contradiction:
Duration of action of moving objectVSQuantity of substance

Solution Approach 1:

The patent changes the fundamental parameters of the matrix structure from inert-core-based to active-substance-based agglomerates. This parameter change allows the active substance titer to be significantly increased since the entire volume of the agglomerate can be occupied by active substance particles rather than being diluted with inert materials.

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 polyvalent matrix achieves higher dosages, flexible administration forms, and improved swallowing ease by eliminating inert cores, ensuring uniform release and taste masking, suitable for geriatric and pediatric use, while maintaining the stability and prolonged-release properties of active substances.

Implementation Method 1

release the active substance in the gastrointestinal tract according to predeterminated modes

Methodology Applied
Scientific EffectDiffusion: Diffusion

Implementation Method 2

keep the active substance fully isolated from the outer environment

Methodology Applied
Scientific EffectPhysical containment: Physical Containment

Data Source

PatentEP2749273B1Solid oral preparation with modified release
Publication Date: 2021.04.07 I P S INT PROD & SERVICES

AI summary

A polymeric matrix for oral administration with modified release and taste masking properties is disclosed, obtained without using inert supports such as sugar spheres, comprising particles of active substance directly and individually covered with a release regulating membrane. Use of such a matrix to prepare various administration forms for oral use as well as the method of its preparation are also disclosed.