Polymeric Matrix for Modified Release Solid Oral Preparations

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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 and allowing for higher dosages and flexible administration forms, including tablets, capsules, and soluble sachets, while maintaining controlled release characteristics.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If traditional tablets and pellets with inert support cores are used, then the active substance can be delivered with modified release, but the volume increases and swallowing becomes difficult

Engineering Contradiction:
Improvemodified releaseVSAvoidvolume
Core Design Contradiction:
ReliabilityVSVolume of moving object

Solution Approach 1:

The invention extracts and removes the inert support core from the traditional tablet structure, retaining only the essential functional components. The active substance is directly coated with polymeric membranes, eliminating the unnecessary inert material that increases volume without contributing to the therapeutic effect.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The invention uses thin polymeric membrane coatings directly on the active substance particles. These flexible film layers provide the modified release function without requiring a bulky inert core, thereby reducing the overall volume while maintaining the controlled release特性.

Inventive Principle:
Principle #30Flexible shells and thin films

2Reliability

If traditional tablets with inert support cores are used, then the active substance can be delivered with modified release, but swallowing becomes difficult especially for high dosages

Engineering Contradiction:
Improvemodified releaseVSAvoidswallowing
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

By removing the inert support core, the invention significantly reduces the physical size and bulk of the dosage form. This extraction of unnecessary material makes the tablet much easier to swallow, particularly for high dosages where traditional formulations would require large volumes.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The invention changes the physical parameters of the dosage form by eliminating the inert core structure. This parameter change from a core-based structure to a coated particle structure results in a compact, easily swallowable form while preserving the modified release function through the polymeric membrane.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If traditional tablets with 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:
Improvemodified releaseVSAvoiddosage structure
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The polymeric membrane-coated active substance particles serve multiple functions simultaneously: they provide the active substance delivery, enable modified release through the membrane, and allow for high dosages in a single unitary form. This multi-functionality eliminates the need to divide dosages into multiple units or combine separate formulations.

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

Solution Approach 2:

The invention merges the functions of the inert support core and the active substance delivery system into a single integrated structure. The active substance particles themselves become the structural basis, coated with functional membranes, combining what were previously separate components into one unified dosage form that can deliver high dosages without division.

Inventive Principle:
Principle #5Merging (Combining)

4Ease of manufacture

If inert support cores are added to the active substance, then the active substance can be formulated into tablets, but the volume of the final administration form must be increased

Engineering Contradiction:
Improvetablet formulationVSAvoidvolume
Core Design Contradiction:
Ease of manufactureVSVolume of moving object

Solution Approach 1:

The invention extracts the inert support core from the formulation, using only the active substance particles as the structural basis. This eliminates the volume contribution from inert materials while maintaining the ability to formulate into tablets through direct coating of the active substance with polymeric membranes.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

By using thin polymeric membrane films directly on the active substance particles instead of bulky inert cores, the invention achieves tablet formulation capability with minimal volume increase. The flexible film structure provides sufficient mechanical integrity for tablet formation without the volume penalty of traditional inert supports.

Inventive Principle:
Principle #30Flexible shells and thin films

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

Enables higher dosages, improved swallowing ease, and flexible administration options without altering modified release properties, including fractionable tablets and extemporaneous suspensions, with enhanced taste masking and uniform gastrointestinal distribution.

Implementation Method 1

particles of active substance, directly and individually covered by one or more layers of polymeric membranes having such characteristics as to keep the active substance fully isolated from the outer environment and to adjust the release according to predeterminated modes

Methodology Applied
Scientific EffectPolymeric membrane controlled release: Semipermeable Membrane

Data Source

PatentUS9333170B2Polyvalent polymeric matrix for modified release solid oral preparations and method of preparation thereof
Publication Date: 2016.05.10 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.