Liquid Capsule Compositions In Situ Matrix Formation

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Solution Overview

Problem

Current extended release systems for active substances via oral administration, particularly in liquid form, face challenges in maintaining controlled release due to variations in temperature and digestive enzyme activity, leading to inconsistent and often inefficient delivery of medications.

Innovation Solution

Development of liquid compositions that form a biodegradable or non-biodegradable matrix in situ upon contact with digestive secretions, using matricial substances like inverted latexes and lipophilic hydrocolloid solutions, which create a viscous or porous structure for controlled release of active substances, independent of pH and digestive enzyme action, allowing for modifiable release durations from one to twenty-four hours.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If liquid forms are used for oral administration, then ease of administration is improved, but controlled release is worsened due to difficulty in avoiding release during time

Engineering Contradiction:
Improveease of administrationVSAvoidcontrolled release
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent incorporates matricial substances (inverted latexes, lipophilic hydrocolloid solutions) into the liquid composition before administration. These substances are pre-positioned in the capsule to undergo phase transition and form a matrix structure upon contact with digestive secretions, enabling controlled release to be established in advance rather than attempting to control release during storage or handling.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent exploits phase transitions of matricial substances (from liquid or dissolved state to gel or solid matrix state) upon contact with water or digestive secretions. This phase change creates a physical barrier that controls the release of active substances, transforming the liquid composition into a sustained-release system while maintaining ease of liquid administration.

Inventive Principle:
Principle #36Phase transitions

2Reliability

If pH-dependent coatings are used, then controlled release is improved, but reliability is worsened due to pH variations in digestive tract

Engineering Contradiction:
Improvecontrolled releaseVSAvoidpH adaptability
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent uses matricial substances that automatically form a protective matrix structure upon contact with digestive secretions, regardless of pH conditions. The system self-regulates release based on the physical properties of the formed matrix rather than relying on pH-dependent dissolution, making the release profile more reliable across varying pH environments in the digestive tract.

Inventive Principle:
Principle #25Self-service

Solution Approach 2:

The patent changes the controlling parameter from pH-dependent chemical dissolution to physical matrix formation through phase transition. By using matricial substances that form gels or solid structures upon contact with water, the release control mechanism becomes independent of pH variations, improving reliability while reducing adaptability requirements.

Inventive Principle:
Principle #35Parameter changes

3Duration of action of moving object

If lipidic matrices are used, then sustained release is improved, but reliability is worsened due to variations in temperature and digestive enzyme activity

Engineering Contradiction:
Improvesustained release durationVSAvoidrelease consistency
Core Design Contradiction:
Duration of action of moving objectVSReliability

Solution Approach 1:

The patent combines matricial substances (inverted latexes, lipophilic hydrocolloid solutions) with active substances in a liquid composition that forms a composite matrix structure upon contact with digestive secretions. This composite approach creates a sustained-release system that is less susceptible to temperature and enzyme variations compared to pure lipidic matrices, as the formed matrix provides more stable physical barriers to release.

Inventive Principle:
Principle #40Composite materials

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 in situ formation of matrices enables a controlled and sustained release of active substances over an extended period, minimizing the impact of pH and digestive enzymes, thereby improving the reliability and duration of medication delivery.

Implementation Method 1

the in situ formation of matrices enables a controlled and sustained release of active substances over an extended period

Methodology Applied
Scientific EffectPhase transition: Phase Change

Implementation Method 2

which create a viscous or porous structure for controlled release of active substances

Methodology Applied
Scientific EffectViscosity formation: Gel

Implementation Method 3

minimizing the impact of pH and digestive enzymes

Methodology Applied
Scientific EffectResistance to dissolution:

Data Source

PatentUS8734839B2Liquid compositions for soft sustained-release capsules and method for production
Publication Date: 2014.05.27 BETON DE PARIS SA
  • US8734839B2 patent drawing
  • US8734839B2 patent drawing

AI summary

The invention relates to liquid compositions for production of soft sustained-release capsules. According to the invention, the sustained release of the active agent is obtained by in situ formation of a matrix, more or less consolidated and biodegradable, by physical modification of the capsule contents on coming into contact with digestive juices on the opening thereof. The above leads to a release time of more than one hour for the active agent previously dissolved or dispersed by means of solvents, said release being modulated by addition of appropriate adjuncts. The invention further relates to a method for production of said liquid compositions. The above finds application in the pharmaceutical, cosmetic and dietary fields.