Multimicrocapsular Oral Medication with Dual pH and Time Release Coating

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Solution Overview

Problem

Current microparticulate oral pharmaceutical forms with delayed and controlled release struggle to effectively release active principles with low solubility, leading to slower release times that compromise bioavailability and therapeutic efficacy, particularly due to the variability in gastric residence time and pH conditions.

Innovation Solution

The development of a multimicrocapsular oral medicinal product with a coating that includes a swelling agent and a composite material comprising a hydrophilic polymer and a hydrophobic compound, allowing for a double mechanism of 'time-dependent' and 'pH-dependent' release, which accelerates the release of active principles and maintains a high plasma concentration profile.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If a coating film is used to achieve delayed and controlled release of active principles, then the release can be triggered by pH change, but the release time becomes variable due to variability in gastric residence time

Engineering Contradiction:

Improverelease time consistencyVSAvoidgastric residence time variability

Core Design Contradiction:

ReliabilityVSLoss of time

Solution Approach 1:

The patent changes the parameter of the coating film from pH-dependent release to time-dependent release by using a polymer that erodes or dissolves after a specific duration in gastric conditions, thereby making the release profile independent of variable gastric residence times and ensuring consistent drug release timing

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent replaces the chemical mechanism (pH-triggered release) with a temporal mechanism (time-dependent release) by selecting coating materials whose degradation kinetics are governed by time rather than pH changes, thus substituting a mechanism sensitive to physiological variability with one that provides predictable, time-controlled release

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

2Duration of action of moving object

If the coating film is made thicker to prolong release duration, then the lag time increases, but the release rate becomes too slow compromising bioavailability

Engineering Contradiction:

Improverelease durationVSAvoidrelease rate

Core Design Contradiction:

Duration of action of moving objectVSSpeed

Solution Approach 1:

The patent changes the material parameters of the coating film by selecting polymers with specific erosion rates and solubility characteristics that allow optimization of both thickness and release rate, enabling the coating to provide adequate lag time while maintaining sufficient release speed for bioavailability

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent uses composite coating formulations combining multiple polymers or additives that work synergistically to control both the duration and rate of drug release, allowing independent adjustment of lag time and release rate parameters through material composition rather than simply increasing coating thickness

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

This approach ensures consistent and rapid release of active principles, optimizing bioavailability and therapeutic efficacy by adjusting the release kinetics to maintain effective plasma concentrations for a longer duration, reducing interindividual variability, and allowing for higher active principle concentrations and easier industrial production.

Implementation Method 1

The non-enteric coating is based on a hydrophilic polymer and a hydrophobic compound and comprises a swelling agent

Methodology Applied

Scientific EffectSwelling: Hydrogel

Implementation Method 2

The non-enteric coating is based on a hydrophilic polymer and a hydrophobic compound

Methodology Applied

Scientific EffectHydrophilic polymer dissolution: Solvation

Implementation Method 3

time-dependent release triggered after a certain amount of time spent in the stomach

Methodology Applied

Scientific EffectTime-dependent dissolution:

Implementation Method 4

pH-dependent release triggered by a change in pH when the particles enter the small intestine

Methodology Applied

Scientific EffectpH-dependent dissolution:

Data Source

PatentUSRE47084E1Oral medicinal product with modified release of at least one active principle in multimicrocapsular form

Publication Date: 2018.10.16 FLAMEL IRELAND

AI summary

The field of the invention is that of oral pharmaceutical medicinal products or compositions, more particularly of the type of those comprising one or more active principles.The aim of the invention is to provide an improved oral medicinal product that can be administered in one or more daily doses, with modified release of active principle (in particular an active principle), for improving the prophylactic and therapeutic efficacy of such a medicinal product.This aim is achieved by means of the multimicrocapsular oral pharmaceutical form according to the invention in which the release of the AP is controlled by means of a double mechanism of triggering the release: “time triggering” and “pH triggering”. This medicinal product comprises microcapsules with modified release of active principle, each containing a core comprising the active principle and one or more swelling agents, and at least one coating making possible the modified release of the active principle.