Menthol Monolithic Matrix Gastro-Resistant Coating

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Solution Overview

Problem

Current formulations of menthol for treating irritable bowel syndrome (IBS) lack a colon-specific, controlled release mechanism, leading to unsatisfactory homogenous distribution and activity throughout the colonic tract, with existing gastro-resistant coatings failing to ensure slow and gradual release.

Innovation Solution

A monolithic pharmaceutical composition with a hydrophilic matrix of hydroxypropylmethylcellulose incorporating micronized menthol, coated with a gastro-resistant layer to prevent release in the stomach and ensure controlled release in the colon, using a combination of cellulose derivatives and polymers to maintain the structure for at least 2 hours and release the active ingredient over 8-24 hours.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If a gastro-resistant coating is applied to menthol formulations, then release in the stomach is prevented, but release in the colon is not controlled homogeneously

Engineering Contradiction:

Improvegastro-resistanceVSAvoidhomogenous release distribution

Core Design Contradiction:

ReliabilityVSManufacturing precision

Solution Approach 1:

The formulation is divided into multiple functional layers: an inner core containing menthol dispersed in hydroxypropylmethylcellulose matrix, and an outer gastro-resistant coating layer. This segmentation allows the inner matrix to control colon-specific release while the outer layer provides gastric protection, resolving the contradiction between gastro-resistance and homogeneous colonic release.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The patent uses a composite structure combining hydroxypropylmethylcellulose (a hydrophilic polymer) as the matrix material with gastro-resistant coating materials. This composite approach enables both gastric resistance and controlled colonic release, as the hydrophilic matrix swells in colonic fluids to enable homogeneous diffusion of menthol throughout the colon.

Inventive Principle:

Principle #40Composite materials

2Speed

If immediate release formulations are used, then rapid onset of action is achieved, but prolonged pharmacological effect is not obtained

Engineering Contradiction:

Improveonset of actionVSAvoidpharmacological effect duration

Core Design Contradiction:

SpeedVSDuration of action of moving object

Solution Approach 1:

The gastro-resistant coating is applied in advance to protect the menthol from premature release in the stomach. This preliminary protective action ensures that the menthol reaches the colon intact, where it then releases gradually over an extended period, achieving both rapid onset (once in colon) and prolonged duration of action.

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The patent changes the release parameters by using a hydrophilic matrix that responds to pH and fluid conditions in the colon. The hydroxypropylmethylcellulose matrix undergoes swelling and dissolution at colonic pH and fluid conditions, transforming from a protected state in the stomach to an active release state in the colon, thereby achieving both rapid local onset and prolonged effect.

Inventive Principle:

Principle #35Parameter changes

3Reliability

If menthol is administered frequently, then adequate symptom relief is maintained, but patient compliance and convenience are reduced

Engineering Contradiction:

Improvesymptom relief adequacyVSAvoidadministration frequency

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The controlled-release formulation ensures continuous release of menthol throughout the colonic transit time (8-24 hours), maintaining adequate therapeutic levels continuously rather than requiring repeated dosing. This continuous action in the colon provides sustained symptom relief and reduces administration frequency, improving patient compliance.

Inventive Principle:

Principle #20Continuity of useful 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

The composition achieves a gradual, controlled release of menthol in the colon, ensuring homogenous distribution and prolonged pharmacological effect, effectively treating IBS and other gastrointestinal disorders by maintaining the structure and releasing the active ingredient in the ascending, transverse, and descending tracts of the colon.

Implementation Method 1

a core with a monolithic matrix containing hydroxypropylmethylcellulose wherein the menthol is dispersed

Methodology Applied

Scientific EffectHydrophilic absorption: Absorption (physical)

Implementation Method 2

a gastro-resistant coating of core a) wherein the menthol to hydroxypropylmethylcellulose weight ratio ranges from 1:5 - 4:1

Methodology Applied

Scientific EffectPhysical containment through coating: Physical Containment

Data Source

PatentEP3079673B1Modified-release therapeutic systems for oral administration of menthol in the treatment of intestinal disorders

Publication Date: 2018.09.19 MOGON PHARMA

AI summary

MODIFIED-RELEASE THERAPEUTIC SYSTEMS FOR ORAL ADMINISTRATION OF MENTHOL IN THE TREATMENT OF INTESTINAL DISORDERS