Budesonide MMX Multi-Matrix Tablet for Colonic Delivery

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Solution Overview

Problem

Systemic corticosteroids are effective for short-term induction of remission in active inflammatory bowel disease (IBD) but pose significant side effects with long-term use, necessitating alternative agents with fewer adverse effects for maintaining remission.

Innovation Solution

Budesonide, a non-systemic corticosteroid combined with MMX technology, is administered in a multi-matrix tablet form to provide controlled release and distribution in the colon, minimizing systemic absorption and maximizing topical anti-inflammatory effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of stationary object

If systemic corticosteroids are used for long-term maintenance treatment, then remission can be maintained, but side effects and risks increase significantly

Engineering Contradiction:
Improvemaintenance treatment durationVSAvoidside effects and risks
Core Design Contradiction:
Duration of action of stationary objectVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by designing a multi-matrix tablet system where budesonide is delivered specifically to the colon through controlled release mechanisms. The composition includes matrices with different dissolution characteristics (fast, medium, slow release) that ensure the drug is released and absorbed primarily in the colonic region, providing localized anti-inflammatory action while minimizing systemic exposure and associated side effects

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent uses the multi-matrix tablet formulation as an intermediary system between the oral administration route and the colonic target site. The complex matrix structure acts as a mediator that controls drug release kinetics and ensures delivery to the intended location, thereby reducing direct systemic corticosteroid exposure while maintaining therapeutic efficacy for maintenance treatment

Inventive Principle:
Principle #24Intermediary (Mediator)

2Quantity of substance

If non-systemic corticosteroid with high first-pass metabolism is used, then systemic absorption is reduced, but controlled release to colon requires specialized delivery system

Engineering Contradiction:
Improvesystemic absorptionVSAvoiddelivery system complexity
Core Design Contradiction:
Quantity of substanceVSDevice complexity

Solution Approach 1:

The patent employs composite materials by formulating budesonide in a multi-matrix tablet system comprising multiple matrices with different polymer compositions and release characteristics. This composite structure includes fast-release, medium-release, and slow-release matrices that work together to achieve controlled colonic delivery, combining the benefits of reduced systemic absorption with targeted drug release through a sophisticated but integrated delivery system

Inventive Principle:
Principle #40Composite materials

3Object-affected harmful factors

If alternative agents with fewer side effects are used, then safety is improved, but efficacy for induction and maintenance of remission must be maintained

Engineering Contradiction:
Improveside effectsVSAvoidefficacy for remission
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent applies parameter changes by optimizing the budesonide dosage (9mg per tablet), the matrix composition ratios, and the release kinetics parameters to achieve both safety and efficacy. The controlled release profile is specifically designed to maintain adequate colonic drug concentrations for remission induction and maintenance while keeping systemic exposure below thresholds that cause significant side effects, thus balancing safety and therapeutic reliability

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 budesonide MMX composition effectively induces and maintains remission in ulcerative colitis with reduced systemic side effects, as evidenced by decreased UCDAI scores and comparable safety profiles to placebo in extended use studies.

Implementation Method 1

Oral dosage forms of budesonide utilizing the MMX multi-matrix system technology are designed to provide the controlled release and distribution of budesonide throughout the length of the colon

Methodology Applied
Scientific EffectControlled release:

Implementation Method 2

Budesonide, a non-systemic corticosteroid (NSCS) with high first-pass metabolism, combined with MMX technology, which is designed to deliver active drug to the colon, may be a viable therapeutic option

Methodology Applied
Scientific EffectFirst-pass metabolism:

Data Source

PatentEP2814495B1Method for treating intestinal diseases presenting at least one inflammatory component
Publication Date: 2021.07.07 COSMO TECHNOLOGIES LTD

AI summary

The present disclosure relates to methods for treating intestinal diseases presenting at least one inflammatory component such as inflammatory bowel disease or diverticular disease and/or maintaining remission of intestinal diseases presenting at least one inflammatory component such as inflammatory bowel disease (IBD) or diverticular disease using budesonide MMX compositions.